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In the present study, a novel series of sulfamethoxazole and 1-(2-fluorophenyl) piperazine derivatives were designed, synthesized and characterized by FTIR, IH NMR,13C NMR, Mass spectrometry, CHN data, and evaluated for their efficiency as BCL2 inhibitors that could lead to potential antiproliferative activity. The ten newly synthesized compounds were screened for their therapeutic activity using MDA-MB-231 breast cancer cell lines. All the test compounds exhibited moderate to high cytotoxic activity in MTT assay. Among them, compounds 3e and 6b exhibited promising antitumor activity, as evidenced by their IC50 values of 16.98 and 17.33 μM respectively. In addition, both compounds 3e and 6b displayed potential antioxidant and apoptosis induction properties. The qRT-PCR analysis showed down regulation of BCL2 expression and up regulation of Casp3 expression in 3e and 6b treated MDA-MB-231 cells. Further, the interaction between critical amino acids of the active domains of BCL2 and 3e and 6b was evaluated by MD simulation, and the results reflected the potent inhibitory activities of 3e and 6b. In summary, the novel compounds 3e and 6b demonstrate their potent anti-cancer properties by inducing apoptosis and selectively targeting BCL2 and caspases-3. [ABSTRACT FROM AUTHOR]

A new group of thiazolidine-2,4-dione derivatives of ciprofloxacin having butyryl linker 3a-l was synthesized via an alkylation of thiazolidine-2,4-diones with butyryl ciprofloxacin with yield range 48–77% andfully characterized by various spectroscopic and analytical tools. Anti-cancer screening outcomes indicated that 3a and 3i possess antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 ± 1.50 and 25.4 ± 1.43 µM, respectively, using doxorubicin and cisplatin as positive controls with an IC50 of 7.03 ± 0.40 and 5.07 ± 0.29 µM, respectively. Additionally, compound 3j showed promising anticancer activity against human renal cancer A498 cell line with IC50 value of 33.9 ± 1.91 µM while doxorubicin and cisplatin showed IC50 values of 3.59 ± 0.20 and 7.92 ± 0.45, respectively. On the other hand, compound 3i did not show considerable anti-bacterial activity against S. aureus, E. coli and P. aeruginosa, and only moderate activity against K. pneumoniae with only a tenth of the activity of ciprofloxacin, confirming the cytotoxicity observed. Mechanistically, compound 3i inhibited both topoisomerase I and II with IC50 of 4.77 ± 0.26 and 15 ± 0.81 µM. Furthermore, it induced cell cycle arrest at S phase in melanoma LOX IMVI cells. Moreover, 3i provoked substantial levels of early, late apoptosis and necrosis in melanoma LOX IMVI cell line comparable to that induced by doxorubicin. Furthermore, compound 3i increased the expression level of active caspase-3 by 49 folds higher in LOX IMVI cell, increased protein expression level of Bax more than the control by 3 folds and inhibited PARP-1by 33% in LOX IMVI. All results were supported by theoretical docking studies on both tested enzymes confirming potential cytotoxicity for the synthesized hybrids. [ABSTRACT FROM AUTHOR]

This study describes the synthesis of N5‐(4‐(1H‐benzo[d]imidazol‐2‐yl)phenyl)‐N2‐phenylpyridine‐2,5‐diamine derivatives from Orthophenylenediamine (1) and 4‐aminobenzoic acid (2) and all the synthesized chemical moieties screened against a panel of cancer cell lines resulted in the identification compound 6 a with good anti‐cancer potential and a GI50 of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM and 1.56 μM against MDAMB‐231, MCF‐7, A‐549, NCI‐H23 and A‐498 respectively. As the second greatest cause of death globally, cancer continues to pose a serious threat to public health. An essential enzyme called aromatase catalyses the last, rate‐limiting step in the production of oestrogens. As a well‐researched endocrine therapeutic strategy, aromatase inhibitors (AIs) efficiently block the production of oestrogen, which is necessary for aromatase activity. [ABSTRACT FROM AUTHOR]

Tricholoma are significant medicinal and edible mushrooms within Basidiomycota. Known for their various medicinal properties such as anti-tumor, immune regulation, and antioxidant effects, they are regarded worldwide as health foods of the 21st century. Tricholoma species produce various types of secondary metabolites, which have been extensively studied by the scientific community. In 2018, Clericuzio et al. summarized the structures, biosynthesis, and biological activities of over one hundred different secondary metabolites isolated from the fruiting bodies of 25 Tricholoma species. Building on this, the present article reviews the research progress on Tricholoma secondary metabolites from 2018 to 2023, identifying a total of 101 compounds, 46 of which were newly discovered. These secondary metabolites include a wide range of chemical categories such as terpenoids, steroids, and alkaloids, demonstrating broad biological activities. This article aims to provide in-depth scientific insights and guidance for researchers in this field by summarizing the chemical and biological properties of these secondary metabolites, promoting further applications and development of Tricholoma fungi in the pharmaceutical and food industries. [ABSTRACT FROM AUTHOR]

Seaweed endophytes are a rich source of microbial diversity and bioactive compounds. This review provides a comprehensive analysis of the microbial diversity associated with seaweeds and their interaction between them. These diverse bacteria and fungi have distinct metabolic pathways, which result in the synthesis of bioactive compounds with potential applications in a variety of health fields. We examine many types of seaweed-associated microorganisms, their bioactive metabolites, and their potential role in cancer treatment using a comprehensive literature review. By incorporating recent findings, we hope to highlight the importance of seaweed endophytes as a prospective source of novel anticancer drugs and promote additional studies in this area. We also investigate the pharmacokinetic and pharmacodynamic profiles of these bioactive compounds because understanding their absorption, distribution, metabolism, excretion (ADMET), and toxicity profiles is critical for developing bioactive compounds with anticancer potential into effective cancer drugs. This knowledge ensures the safety and efficacy of proposed medications prior to clinical trials. This study not only provides promise for novel and more effective treatments for cancer with fewer side effects, but it also emphasizes the necessity of sustainable harvesting procedures and ethical considerations for protecting the delicate marine ecology during bioprospecting activities. [ABSTRACT FROM AUTHOR]

Featured Application: The application of this study is all computational studies considering venom peptides as potential sources of therapeutics. Animal venom has been gaining traction as a potential source of therapeutics for various diseases. Spiders encompass a wide variety of venom-producing species, of which tarantulas of the family Theraphosidae are widely known across the globe. Research towards tarantula venom therapeutics has led to its potential application as antinociceptives. Death receptors are cellular receptors that induce apoptosis—the body's natural suicide mechanism—to destroy malfunctioning cells. These are particularly of interest in cancer research, as this mechanism is tampered with, resulting in cancer cell proliferation. In this study, the viability of venom toxins from the Theraphosidae family of spiders to induce apoptosis by binding to human death receptors is investigated by carrying out anti-cancer screening, molecular docking, ADMET evaluation, then molecular dynamics and thermodynamic analysis twice, first to ascertain the best receptor–peptide systems per receptor, and secondly to more comprehensively describe binding stability and thermodynamics. Results point to favorable receptor–peptide interactions due to similarities in equilibrium behavior with the death ligand–death receptor systems, along with favorable end-state binding energies and ADMET analysis results. Further inquiry is recommended to assess the real-life efficacy and viability of theraphotoxins as apoptosis therapeutics and further improve on their ability to induce apoptosis. [ABSTRACT FROM AUTHOR]

In this work, the capacities of Si60, C60, B30N30, Sc-Si60, Sc-C60, Sc-B30N30 to deliver the Dacarbazine are examined. The Eadoption of Sc-Si60, Sc-C60 and Sc-B30N30 are -4.45, -4.57 and -4.70 eV. The Ecohesive of Si60, C60 and B30N30 nanocages are -6.23, -6.51 and -6.86 eV, respectively and so the Si60, C60 and B30N30 nanocages are stable nanostructures. Results shown than the Sc-B30N30 has acceptable potential to adsorb and deliver the Dacarbazine. Results shown that the Sc-Si60, Sc-C60 and Sc-B30N30 nanocages have higher capacitates and abilities to deliver and transfer of the Dacarbazine as anticancer drug than other nanostructures in previous works. The adsorption of Dacarbazine on Si60, C60, B30N30, Sc-Si60, Sc-C60, Sc-B30N30 nanocages have the τ values ca 48.8, 51.1, 54.2, 54.9, 57.5 and 62.1 s, respectively. Finally, the Sc-B30N30 is proposed to adsorb and deliver the Dacarbazine. [ABSTRACT FROM AUTHOR]

Docetaxel (DTX) has become widely accepted as a first-line treatment for metastatic breast cancer; however, the frequent development of resistance provides challenges in treating the disease.C60 fullerene introduces a unique molecular form of carbon, exhibiting attractive chemical and physical properties. Our study aimed to develop dicarboxylic acid-derivatized C60 fullerenes as a novel DTX delivery carrier. This study investigated the potential of water-soluble fullerenes to deliver the anti-cancer drug DTX through a hydrophilic linker. The synthesis was carried out using the Prato reaction. The spectroscopic analysis confirmed the successful conjugation of DTX molecules over fullerenes. The particle size of nanoconjugate was reported to be 122.13 ± 1.63 nm with a conjugation efficiency of 76.7 ± 0.14%. The designed conjugate offers pH-dependent release with significantly less plasma pH, ensuring maximum release at the target site. In-vitro cell viability studies demonstrated the enhanced cytotoxic nature of the developed nanoconjugate compared to DTX. These synthesized nanoscaffolds were highly compatible with erythrocytes, indicating the safer intravenous route administration. Pharmacokinetic studies confirmed the higher bioavailability (~ 6 times) and decreased drug clearance from the system vis-à-vis plain drug. The histological studies reveal that nanoconjugate-treated tumour cells exhibit similar morphology to normal cells. Therefore, it was concluded that this developed formulation would be a valuable option for clinical use. [ABSTRACT FROM AUTHOR]

The use of drugs in chemotherapy poses numerous side effects. Hence the use of natural substances that can help in the prevention and cure of the disease is a dire necessity. Cancer is a deadly illness and combination of diseases, the menace of which is rising with every passing year. The research community and scientists from all over the world are working towards finding a cure of the disease. The use of polyphenols which are naturally derived from plants have a great potential to be used as anti-cancer drugs and also the use of fruits and vegetables which are rich in these polyphenols can also help in the prevention of diseases. The study aims to compile the available literature and research studies on the anti-cancer effects of polyphenols and the signaling pathways that are affected by them. To review the anti-cancer effects of polyphenols, Google Scholar, PubMed and ScienceDirect were used to study the literature available. The article that have been used for literature review were filtered using keywords including cancer, polyphenols and signaling pathways. Majorly articles from the last 10 years have been considered for the review but relevant articles from earlier than 10 years have also been considered. Almost 400 articles were studied for the review and 200 articles have been cited. The current review shows the potential of polyphenols as anti-cancer compounds and how the consumption of a diet rich in polyphenols can help in the prevention of cancer. Because of their capacity to affect a variety of oncogenic and oncosuppressive signaling pathways, phytochemicals derived from plants have been effectively introduced as an alternative anticarcinogenic medicines. [ABSTRACT FROM AUTHOR]

Background: Pancreatic and Gastric cancers are very aggressive and deadly types of cancer that require effective treatment strategies to stop their progression. Nano-drug delivery systems, like those using Auraptene-loaded GQD nanoparticles, play a crucial role in addressing this need by delivering targeted and controlled treatments to cancer cells, making treatment more effective, and reducing side effects. The study focused on investigating the effects of Auraptene, an efficient anticancer compound when loaded into Graphene Quantum Dots (GQDs) on types of human cancer cells. Methods: To create auraptene-loaded graphene quantum dot nanoparticles (AGQD-NP) (Unmodified and modified types) a combination of hydrothermal and high-energy homogenization methods was used. The nanoparticles were characterized by conducting DLS (Dynamic light scattering), FTIR (Fourier-transform infrared spectroscopy), FESEM (Field Emission Scanning Electron microscopy), and zeta potential analysis. bioactivity of AGQD-NP was assessed through tests, including antioxidant capacity measured by ABTS and DPPH scavenging abilities well as cytotoxicity tested using MTT assay on both human cancer cell lines and normal human vascular endothelial cells. Results: The modified AGQD-NP (M-AGQD-NP) demonstrated antioxidant properties by neutralizing free radicals. They also displayed selective toxicity, towards human gastric adenocarcinoma cell-line (AGS) and human pancreatic adenocarcinoma (PANC) cancer cells with IC50 values recorded at 78.8 µg/mL and 89.72 µg/mL respectively. The specific targeting of gastric cancer cells was evident from the differing IC50 values compared to the Human breast adenocarcinoma cell line (MCF-7), Human hepatocellular carcinoma cell line (Hella), and normal vascular endothelial cells (Huvec). Additionally, the induced apoptotic death, in the human pancreatic adenocarcinoma (PANC) cancer cells was confirmed through AO/PI staining and Annexin-based flow cytometry revealing increased expression levels of P53, Caspase3, BAX, and Caspase8. Conclusion: In summary, the M-AGQD-NP have shown encouraging effects displaying antioxidant capabilities and a specific focus, on pancreatic and gastric cancer cells. These findings indicate uses for AGQD-NP as an efficient apoptosis inducer in cancer treatment. Additional In-vivo researches are required to validate their effectiveness, in living organisms. [ABSTRACT FROM AUTHOR]

The substantial impact of nanotechnology on material sciences is exemplified through zinc oxide nanomaterials (ZnO NMs), which play a pivotal role in healthcare and environmental applications. This comprehensive review focuses on the eco‐friendly synthesis of ZnO NMs and their cutting‐edge practices in biomedical, including drug delivery, bioimaging, and anticancer therapies. Exploring environmentally responsible production techniques for ZnO NMs aims to mitigate risks associated with conventional methods, such as the use of costly and toxic precursors. In addition, these green methodologies present opportunities for generating diverse and significant morphologies. The study delves into the inhibitory effects of these NMs against microbes, cancer, and inflammation. The utilization of ZnO NMs in disease treatment and diagnosis prompts us to explore recent developments in emerging biomedical applications. Leveraging ZnO variable optical characteristics, biodegradability, inherent biocompatibility, adaptable surface chemistry, and high stability, the review covers a range of remarkable research studies for novel applications that possibly open up the potential for identifying, treating, and preventing serious human diseases. [ABSTRACT FROM AUTHOR]

The cAMP-responsive element binding protein (CREB) binding protein (CBP), a bromodomain-containing protein, engages with multiple transcription factors and enhances the activation of many genes. CBP bromodomain acts as an epigenetic reader and plays an important role in the CBP-chromatin interaction which makes it an important drug target for treating many diseases. Though inhibiting CBP bromodomain was reported to have great potential in cancer therapeutics, approved CBP bromodomain inhibitor is yet to come. We utilized various in silico approaches like molecular docking, ADMET, molecular dynamics (MD) simulations, MM-PBSA calculations, and in silico PASS predictions to identify potential CBP bromodomain inhibitors from marine natural compounds as they have been identified as having distinctive chemical structures and greater anticancer activities. To develop a marine natural compound library for this investigation, Lipinski’s rule of five was used. Sequential investigations utilizing molecular docking, ADMET studies, 100 ns MD simulations, and MM-PBSA calculations revealed that three marine compounds—ascididemin, neoamphimedine, and stelletin A—demonstrated superior binding affinity compared to the standard inhibitor, 69 A. These compounds also exhibited suitable drug-like properties, a favorable safety profile, and formed stable protein-ligand complexes. The in-silico PASS tool predicted that these compounds have significant potential for anticancer activity. Among them, ascididemin demonstrated the highest binding affinity in both molecular docking and MM-PBSA calculations, as well as a better stability profile in MD simulations. Hence, ascididemin can be a potential inhibitor of CBP bromodomain. However, in vitro and in vivo validation is required for further confirmation of these findings. [ABSTRACT FROM AUTHOR]

Simple Summary: Natural polyphenols are well-known dietary supplements that have been used for medical purposes for a long time. Consuming foods and beverages of plant origin, especially those rich in polyphenolic compounds, may have chemopreventive and therapeutic effects on cancer due to the health-promoting properties of these compounds. Polyphenols are characterized by high structural diversity, which contributes to their wide range of therapeutic effects, including anti-oxidant and anti-cancer activities. These compounds can modulate the expression and activity of many proteins, including enzymes, and regulate multiple cell signaling pathways. Among the molecular targets of anti-cancer agents are matrix metalloproteinases, particularly metalloproteinase-2 and metalloproteinase-9, and nuclear factor-kappa B. Matrix metalloproteinases can degrade the protein components of the extracellular matrix and play key roles in physiological processes such as tissue repair and morphogenesis, as well as in carcinogenesis and other pathological processes. The inhibition of their synthesis and activity is closely related to a reduction in the metastasis and invasion of cancer cells. This review discusses the current state of knowledge concerning the anti-invasive and anti-metastatic potential of selected polyphenols, with a focus on in vitro and in vivo evidence. Polyphenols are natural compounds found in many plants and their products. Their high structural diversity bestows upon them a range of anti-inflammatory, anti-oxidant, proapoptotic, anti-angiogenic, and anti-metastatic properties, and a growing body of research indicates that a polyphenol-rich diet can inhibit cancer development in humans. Polyphenolic compounds may modulate the expression, secretion, or activity of compounds that play a significant role in carcinogenesis, including type IV collagenases, such as matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9), by suppressing cellular signaling pathways such as nuclear factor-kappa B. These enzymes are responsible for the degradation of the extracellular matrix, thus promoting the progression of cancer. This review discusses the current state of knowledge concerning the anti-cancer activity of polyphenols, particularly curcumin, resveratrol, epigallocatechin-3-gallate, genistein, and quercetin, with a specific focus on their anti-invasive and anti-metastatic potential, based on the most recent in vitro and in vivo studies. It appears that polyphenols may be valuable options for the chemoprevention and treatment of cancer via the inhibition of MMP-2 and MMP-9 and the suppression of signaling pathways regulating their expression and activity. [ABSTRACT FROM AUTHOR]

Epithelial ovarian carcinoma poses a significant challenge due to its resistance to chemotherapy and propensity for metastasis, thereby reducing the effectiveness of conventional treatments. Hence, the identification of novel compounds capable of augmenting the anti-cancer efficacy of platinum-based chemotherapy is imperative. Oxyresveratrol (OXY), a derivative of resveratrol, has been demonstrated to possess antiproliferative and apoptosis-inducing effects across various cancer cell lines. Notably, OXY appears to exert its effects by inhibiting the PI3K/AKT/mTOR signaling pathway. However, the synergistic potential of OXY in combination with cisplatin against epithelial ovarian cancer has not yet been elucidated. The current study investigated the synergistic effects of OXY and cisplatin on the ovarian cancer cell lines SKOV3 and TOV21G. We found that OXY significantly enhanced cisplatin's ability to reduce cell viability, induce apoptosis, induce cell cycle arrest, and increase the proportion of cells in the sub-G1 phase. Furthermore, OXY treatment alone dose-dependently inhibited the production of anti-apoptotic proteins including Mcl-1, Bcl-xL, and XIAP under EGF activation. Mechanistically, OXY suppressed the PI3K/AKT/mTOR signaling pathway by reducing phosphorylated AKT, while having no discernible effect on the MAPK pathway. These findings highlight OXY's potential to enhance ovarian cancer cell sensitivity to chemotherapy, suggesting its development as a pharmaceutical adjunct for clinical use in combination therapies. [ABSTRACT FROM AUTHOR]

Skin cancer is threatening more and more people's health; its postoperative recurrence and wound infection are still critical challenges. Therefore, specialty wound dressings with multifunctional bioactivity are urgently desired. Emodin is a natural anthraquinone compound that has anti-cancer and anti-bacterial properties. Herein, we fabricated coaxial electrospinning nanofibers loaded with emodin to exploit a multifunctional wound dressing for skin cancer postoperative management, which encapsulated emodin in a polyvinylpyrrolidone core layer, combined with chitosan-polycaprolactone as a shell layer. The nanofibers were characterized via morphology, physicochemical nature, drug load efficiency, pH-dependent drug release profiles, and biocompatibility. Meanwhile, the anti-cancer and anti-bacterial effects were evaluated in vitro. The emodin-loaded nanofibers exhibited smooth surfaces with a relatively uniform diameter distribution and a clear shell-core structure; remarkably, emodin was evenly dispersed in the nanofibers with significantly enhanced dissolution of emodin. Furthermore, they not only display good wettability, high emodin entrapment efficiency, and biphasic release profile but also present superior biocompatibility and anti-cancer properties by increasing the levels of MDA and ROS in A-375 and HSC-1 cells via apoptosis-related pathway, and long-term anti-bacterial effects in a dose-independent manner. The findings indicate that the emodin-loaded nanofiber wound dressing can provide a potential treatment strategy for skin cancer postoperative management. [ABSTRACT FROM AUTHOR]

Ovarian cancer, a leading cause of cancer-related deaths in women, remains a formidable challenge, especially in the context of platinum-resistant disease. This study investigated the potential of the benzimidazole derivative BNZ-111 as a novel treatment strategy for platinum-resistant ovarian cancer. The human EOC cell lines A2780, HeyA8, SKOV3ip1, A2780-CP20, HeyA8-MDR, and SKOV3-TR were treated with BNZ-111, and cell proliferation, apoptosis, and cell cycle were assessed. It demonstrated strong cytotoxicity in both chemo-sensitive and chemo-resistant epithelial ovarian cancer cell lines, inducing apoptosis and G2/M cell cycle arrest. In vivo experiments using orthotopic and patient-derived xenograft models showed significant tumor growth inhibition without apparent toxicity to vital organs. Unlike paclitaxel, BNZ-111 proved effective in paclitaxel-resistant cells, potentially by bypassing interaction with MDR1 and modulating β-3 tubulin expression to suppress microtubule dynamics. BNZ-111, with favorable drug-like properties, holds promise as a therapeutic option for platinum-resistant ovarian cancer, addressing a critical clinical need in gynecologic oncology. [Display omitted] • The benzimidazole derivative BNZ-111 may be a novel treatment for ovarian cancer. • Disrupting tubulin polymerization is a mechanism of action through which BNZ-111 induces anti-cancer activity. • BNZ-111 demonstrates in vivo efficacy and potential for overcoming paclitaxel resistance. [ABSTRACT FROM AUTHOR]

Natural products have proven to be promising anti-cancer agents due to their diverse chemical structures and bioactivity. This review examines their central role in cancer treatment, focusing on their mechanisms of action and therapeutic benefits. Medicinal plants contain bioactive compounds, such as flavonoids, alkaloids, terpenoids and polyphenols, which exhibit various anticancer properties. These compounds induce apoptosis, inhibit cell proliferation and cell cycle progression, interfere with microtubule formation, act on topoisomerase targets, inhibit angiogenesis, modulate key signaling pathways, improve the tumor microenvironment, reverse drug resistance and activate immune cells. Herbal anti-cancer drugs offer therapeutic advantages, particularly selective toxicity against cancer cells, reducing the adverse side effects associated with conventional chemotherapy. Recent studies and clinical trials highlight the benefits of herbal medicines in alleviating side effects, improving tolerance to chemotherapy and the occurrence of synergistic effects with conventional treatments. For example, the herbal medicine SH003 was found to be safe and potentially effective in the treatment of solid cancers, while Fucoidan showed anti-inflammatory properties that are beneficial for patients with advanced cancer. The current research landscape on herbal anticancer agents is extensive. Numerous studies and clinical trials are investigating their efficacy, safety and mechanisms of action in various cancers such as lung, prostate, breast and hepatocellular carcinoma. Promising developments include the polypharmacological approach, combination therapies, immunomodulation and the improvement of quality of life. However, there are still challenges in the development and use of natural products as anti-cancer drugs, such as the need for further research into their mechanisms of action, possible drug interactions and optimal dosage. Standardizing herbal extracts, improving bioavailability and delivery, and overcoming regulatory and acceptance hurdles are critical issues that need to be addressed. Nonetheless, the promising anticancer effects and therapeutic benefits of natural products warrant further investigation and development. Multidisciplinary collaboration is essential to advance herbal cancer therapy and integrate these agents into mainstream cancer treatment. [ABSTRACT FROM AUTHOR]

Objective: Phyto-oxylipins are lipid molecules produced in plants by the oxidative transformation of unsaturated fatty acids via diverse metabolic pathways. Recently, the chemical diversity and functional significance of oxylipins is gaining significant attention. However, the functional significance of these compounds as anti-cancer agents remains largely uncharacterized. The objective of this review is to provide a comprehensive synthesis and analysis of the functional significance of plant oxylipins as anti-cancer agents to facilitate their exploitation in drug discovery and development. Methods: This review was based on a thorough compilation and analysis of research work carried out on biological significance and implications of plant-derived anti-cancer oxylipins. Curation of data was based on several databases and resources such as Scopus, PubMed, DrugBank and PubChem. Within the context of the scope and subject matter as guided by the objective, no exclusion and inclusion criteria were necessarily employed in the screening of articles. Results: The present review explores the origins, anti-cancer properties and functional mechanisms of phyto-oxylipins. The potential functional significance of new and poorly characterized plant oxylipins have also been highlighted. The prospects of plant oxylipins in research, medicine and biotechnology that could optimize their potential are also explored. Insights into the promising avenues that may originate from innovative therapeutic approaches are also discussed. Conclusion: Despite the rich source of oxylipins in plants, much of their potential as therapeutic agents for cancer treatment remains to be fully established. Clinical investigations are also needed to determine safe doses and effective delivery methods. Research into phyto-oxylipins require significant attention due to the promise it may hold in addressing key challenges in biotechnology, health, and environmental sustainability. [ABSTRACT FROM AUTHOR]

Herein, we report the preparation of nickel oxide (NiO) nanosheets in a lyotropic liquid crystal (LLC) medium via a chemical reduction method. The LLC phase exhibiting a lamellar phase was formed using a binary mixture of triton X-100 (68 wt%) and water (32 wt%) at 4 °C. The nanomaterials were prepared in this medium by reducing NiCl2.6H2O using a strong reducing agent, NaBH4. The prepared nanomaterials were characterized through UV–Vis, SEM, FT-IR and XPS techniques. The NiO nanomaterials were found to exhibit good catalytic activity towards reduction and degradation reactions. An apparent rate constant (Kapp) value of 1.4 × 10–2 min−1 was obtained for the reduction reaction of 4-nitrophenol to 4-aminophenol using NiO nanomaterials (300 μL of as-prepared 80 mM dispersion). The nanomaterials showed good recyclability with effective activity until 5th cycle. Further, Kapp of 0.5 × 10–2 min−1 was obtained for the degradation reaction of methylene blue. The anti-bacterial studies suggested that the NiO nanomaterials were effective against gram positive (S. aureus) bacteria and anti-cancer studies of the particles against breast cancer cells (MCF-7) showed an IC50 value of 78.93 μg/mL. [ABSTRACT FROM AUTHOR]

The manipulation of the energy or source of food for cancer cells has attracted significant attention in oncology research. Metabolic reprogramming of the immune system allows for a deeper understanding of cancer cell mechanisms, thereby impeding their progression. A more targeted approach is the restriction of cancer cells through dietary restriction (CR), which deprives cancer cells of the preferred energy sources within the tumor microenvironment, thereby enhancing immune cell efficacy. Although there is a plethora of CR strategies that can be employed to impede cancer progression, there is currently no comprehensive review that delineates the specific dietary restrictions that target the diverse metabolic pathways of cancer cells. This mini-review introduces amino acids as anti-cancer agents and discusses the role of dietary interventions in cancer prevention and treatment. It highlights the potential of a ketogenic diet as a therapeutic approach for cancer, elucidating its distinct mechanisms of action in tumor progression. Additionally, the potential of plant-based diets as anti-cancer agents and the role of polyphenols and vitamins in anti-cancer therapy were also discussed, along with some prospective interventions for CR as anti-tumor progression. [ABSTRACT FROM AUTHOR]

There have been many studies reporting that the regular consumption of fruits and vegetables is associated with reduced risks of cancer and age-related chronic diseases. Recent studies have demonstrated that reducing reactive oxygen species and inflammation by phytochemicals derived from natural sources can extend lifespans in a range of model organisms. Phytochemicals derived from fruits and vegetables have been known to display both preventative and suppressive activities against various types of cancer via in vitro and in vivo research by interfering with cellular processes critical for tumor development. The current challenge lies in creating tailored supplements containing specific phytochemicals for individual needs. Achieving this goal requires a deeper understanding of the molecular mechanisms through which phytochemicals affect human health. In this review, we examine recently (from 2010 to 2024) reported plant extracts and phytochemicals with established anti-aging and anti-cancer effects via the activation of FOXO3 transcriptional factor. Additionally, we provide an overview of the cellular and molecular mechanisms by which these molecules exert their anti-aging and anti-cancer effects in specific model systems. Lastly, we discuss the limitations of the current research approach and outline for potential future directions in this field. [ABSTRACT FROM AUTHOR]

Objective: Solanum nigrum L. (SNL) is a natural drugwith diverse bioactive components and multi‐targeted anti‐tumor effects, gaining increasing attention in clinical application. Method and Results: This paper reviews the studies on SNL by searching academic databases (Google Scholar, PubMed, Science Direct,and Web of Science, among others), analyzing its chemical compositions (alkaloids, saponins, polysaccharides, and polyphenols, among others), andbriefly describes the anti‐tumor mechanisms of the main components. Discussion: This paper discusses the shortcomings of the current research on SNL and proposes corresponding solutions, providing theoretical support for further research on its biological functions and clinical efficacy. [ABSTRACT FROM AUTHOR]

Glioblastoma multiforme (GBM) is a highly aggressive and fatal primary brain tumor. The resistance of GBM to conventional treatments is attributed to factors such as the blood–brain barrier, tumor heterogeneity, and treatment-resistant stem cells. Current therapeutic efforts show limited survival benefits, emphasizing the urgent need for novel treatments. In this context, natural anti-cancer extracts and especially animal venoms have garnered attention for their potential therapeutic benefits. Bee venom in general and that of the Middle Eastern bee, Apis mellifera syriaca in particular, has been shown to have cytotoxic effects on various cancer cell types, but not glioblastoma. Therefore, this study aimed to explore the potential of A. mellifera syriaca venom as a selective anti-cancer agent for glioblastoma through in vitro and in vivo studies. Our results revealed a strong cytotoxic effect of A. mellifera syriaca venom on U87 glioblastoma cells, with an IC50 of 14.32 µg/mL using the MTT test and an IC50 of 7.49 µg/mL using the LDH test. Cells treated with the bee venom became permeable to propidium iodide without showing any signs of early apoptosis, suggesting compromised membrane integrity but not early apoptosis. In these cells, poly (ADP-ribose) polymerase (PARP) underwent proteolytic cleavage similar to that seen in necrosis. Subsequent in vivo investigations demonstrated a significant reduction in the number of U87 cells in mice following bee venom injection, accompanied by a significant increase in cells expressing caspase-3, suggesting the occurrence of cellular apoptosis. These findings highlight the potential of A. mellifera syriaca venom as a therapeutically useful tool in the search for new drug candidates against glioblastoma and give insights into the molecular mechanism through which the venom acts on cancer cells. [ABSTRACT FROM AUTHOR]

This study aims to synthesize inclusion complex derived from sorafenib (Sor) and hydroxypropyl-β-cyclodextrin (HPβCD) (denoted as [Sor-HPβCD]). The complex of Sor with HPβCD has been synthesized in a mixed solvent of H2O-DMSO, with a DMSO volume fraction of 80 %. The results of FTIR, DSC, and UV–Vis analysis have demonstrated the success of complex formation: the intensity of some characteristic peaks for the Sor binding decreased after complex formation, indicating that a part of the guest molecule has entered the cavity of the HPβCD molecule. This is further supported by the DSC analysis results, showing the transformation of the complex's crystalline form to an amorphous form. The phase solubility diagram study also indicates that the solubility of Sor significantly increases, approximately 7 times higher than pure Sor, after complex formation. The results of the cell growth inhibition activity test in a water environment show that the complex inhibits the growth of Hep-G2 cells with an IC50 value of 62.4 μg/mL, while pure Sor does not exhibit activity as it is practically insoluble in water. [ABSTRACT FROM AUTHOR]

Five host-defense peptides (figainin 2PL, hylin PL, raniseptin PL, plasticin PL, and peptide YL) were isolated from norepinephrine-stimulated skin secretions of the banana tree dwelling frog Boana platanera (Hylidae; Hylinae) collected in Trinidad. Raniseptin PL (GVFDTVKKIGKAVGKFALGVAKNYLNS.NH 2) and figainin 2PL (FLGTVLKLGKAIAKTVVPMLTNAMQPKQ. NH 2) showed potent and rapid bactericidal activity against a range of clinically relevant Gram-positive and Gram-negative ESKAPE + pathogens and Clostridioides difficile. The peptides also showed potent cytotoxic activity (LC 50 values < 30 μM) against A549, MDA-MB-231 and HT29 human tumor-derived cell lines but appreciably lower hemolytic activity against mouse erythrocytes (LC 50 = 262 ± 14 μM for raniseptin PL and 157 ± 16 μM for figainin 2PL). Hylin PL (FLGLIPALAGAIGNLIK.NH 2) showed relatively weak activity against microorganisms but was more hemolytic. The glycine-leucine-rich peptide with structural similarity to the plasticins (GLLSTVGGLVGGLLNNLGL.NH 2) and the non-cytotoxic peptide YL (YVPGVIESLL.NH 2) lacked antimicrobial and cytotoxic activities. Hylin PL, raniseptinPL and peptide YL stimulated the rate of release of insulin from BRIN-BD11 clonal β-cells at concentrations ≥100 nM. Peptide YL was the most effective (2.3-fold increase compared with basal rate at 1 μM concentration) and may represent a template for the design of a new class of incretin-based anti-diabetic drugs. [Display omitted] • Figainin 2 PL and raniseptin PL show potent antimicrobial activity against ESKAPE pathogens. • Figainin 2 PL and raniseptin PL are weakly hemolytic. • Figainin 2 PL, raniseptin PL and hylin PL are cytotoxic to human tumor-derived cells. • Raniseptin PL, hylin PL, plasticin-PL and peptide YL stimulate insulin release from BRIN-BD11 cells. [ABSTRACT FROM AUTHOR]

Since the first years of history, microbial fermentation products such as bread, wine, yogurt and vinegar have always been noteworthy regarding their nutritional and health effects. Similarly, mushrooms have been a valuable food product in point of both nutrition and medicine due to their rich chemical components. Alternatively, filamentous fungi, which can be easier to produce, play an active role in the synthesis of some bioactive compounds, which are also important for health, as well as being rich in protein content. Therefore, this review presents some important bioactive compounds (bioactive peptides, chitin/chitosan, β-glucan, gamma-aminobutyric acid, L-carnitine, ergosterol and fructooligosaccharides) synthesized by fungal strains and their health benefits. In addition, potential probiotic- and prebiotic fungi were researched to determine their effects on gut microbiota. The current uses of fungal based bioactive compounds for cancer treatment were also discussed. The use of fungal strains in the food industry, especially to develop innovative food production, has been seen as promising microorganisms in obtaining healthy and nutritious food. Fungal-based bioactive compounds have various health benefits. Prebiotic fungi play an active role in the regulation of gut microbiota. Anti-tumor effective fungal components will contribute to alternative medicine. Beta-glucan and chitin are the most promising fungal metabolites for cancer treatment. [ABSTRACT FROM AUTHOR]

The paper offers a comprehensive analysis of the nutritional, medicinal, and bioactive properties of silkworm pupae (SWP), highlighting their potential applications in a range of industries. It explores the rich nutritional profile, emphasizing how important it is for humans and animals to consume them due to their high protein content, vital fatty acids, amino acids, vitamins, and minerals. The SWP also looks into the possible uses of SWP in medicine, highlighting the bioactive substances including flavonoids, polyphenols, and peptides that have a variety of pharmacological properties. Regulatory issues, toxicity, and safety are also covered. Overall, the review highlights the many advantages of SWP, pointing out the possibility of using them in nutritious foods, supplements, and medications. This also calls for further study to optimize extraction techniques and investigate new applications, thereby encouraging the incorporation of SWP into contemporary food and healthcare systems. [ABSTRACT FROM AUTHOR]

Lung malignancy is a major worldwide issue that occurs due to the dysregulation of various growth factors. Lung cancer has no apparent signs in the early stages, which makes it harder to catch it in time and leads to a higher fatality rate. So, the goal of this work was to create and analyze a novel chemical molecule called 4-nitro acetophenone thiosemicarbazone (4-NAPTSc) against the lung cancer cell line A549 and human non-tumorigenic lung epithelial cell line BAES-2B. The ligand was synthesized by refluxing the reaction mixture of 4-nitro acetophenone and thiosemicarbazide and was further characterized by UV, FTIR, and 1H and 13C NMR and Differential Scanning Calorimetry (DSC) study. Cytotoxicity assay/MTT (3-(4,5-dimethylthiazol-2-yl))2,5-diphenyltetrazolium bromide) was used to evaluate the cytotoxicity of the compound. Epidermal growth factor receptors (EGFR), polo-like kinase-1 (PLK1), and vascular endothelial growth factor receptors (VEGFR) were chosen as the target proteins for molecular docking to find potential ligand binding sites and inhibit their function. A novel yellow-colored crystalline solid has been synthesized. 4-NAPTSc had an IC50 of 2.93 μg/mL against the A549 lung cancer cells. When the dosage is increased from 5 to 15 μg/mL along with time, the cell viability falls. Docking results showed that the compound binds with the targeted proteins' amino acid residues, and the likeness profile of the compound is also favorable. This study reveals that the compound has the potential for further investigation and can be used in multitargeted cancer therapies. [ABSTRACT FROM AUTHOR]

This comprehensive review delves into the multifaceted aspects of genipin, a bioactive compound derived from medicinal plants, focusing on its anti-cancer potential. The review begins by detailing the sources and phytochemical properties of genipin, underscoring its significance in traditional medicine and its transition into contemporary cancer research. It then explores the intricate relationship between genipin's chemical structure and its observed anti-cancer activity, highlighting the molecular underpinnings contributing to its therapeutic potential. This is complemented by a thorough analysis of preclinical studies, which investigates genipin's efficacy against various cancer cell lines and its mechanisms of action at the cellular level. A crucial component of the review is the examination of genipin's bioavailability and pharmacokinetics, providing insights into how the compound is absorbed, distributed, metabolized, and excreted in the body. Then, this review offers a general and updated overview of the anti-cancer studies of genipin and its derivatives based on its basic molecular mechanisms, induction of apoptosis, inhibition of cell proliferation, and disruption of cancer cell signaling pathways. We include information that complements the genipin study, such as toxicity data, and we differentiate this review by including commercial status, disposition, and regulation. Also, this review of genipin stands out for incorporating information on proposals for a technological approach through its load in nanotechnology to improve its bioavailability. The culmination of this information positions genipin as a promising candidate for developing novel anti-cancer drugs capable of supplementing or enhancing current cancer therapies. [ABSTRACT FROM AUTHOR]

The chemistry of condensed heterocyclic molecules in terms of their diverse biological properties and role in drug development has been the subject of numerous publications. Tetrazole is a naturally occurring chemical that has been used to create several commercially available drugs and as a result, plays an important role in pharmaceutical chemistry. The current study aimed to create and synthesize seven new 2,5-disubstituted-tetrazole-acetamide derivatives 3a-3g via an N-alkylation reaction of 5-(4-bromophenyl)-2H-tetrazole or 5-(4-chlorophenyl)-2H-tetrazole 1a,1b, and N-acetamide derivatives 2a-2f, and 2g in CH3CN using potassium carbonate as a base in good yields. New molecules were assigned based on nuclear magnetic resonance results (¹H, 13C NMR, and two-dimensional-NMR [heteronuclear single quantum coherence spectroscopy [HSQC]), along with mass spectrometry (EI-MS) techniques. The products' biological activities were confirmed using the tetrazolium (MTT) assay against MCF-7 (breast cancer) and PC3 (prostate cancer) cells and their effects on the normal hepatic cell line, WRL68. Results showed that compounds 3e-3g inhibited PC3 cells with average IC50 values of 32.59, 54.99, and 55.53 μM, respectively. Compounds 3a and 3b demonstrated cytotoxicity against the MCF-7 cell line, with average IC50 values of 94.25 and 68.16 μM, respectively. Compounds 3a, 3c, and 3e-3g on the 3ERT and 3ZK6 receptors demonstrated strong binding capabilities and improved protein interactions according to molecular docking experiments. [ABSTRACT FROM AUTHOR]

Scutellaria baicalensis, commonly known as Chinese Skullcap, is a traditional herb with a long history of cultural use in Chinese medicines. This review focuses on a comprehensive summary of the morphological description, bioactive compounds, drug-herb interactions, and pharmacological activities of Scutellaria baicalensis, as well as its therapeutic applications. A wide-ranging search using databases such as PubMed, Scopus, Google Scholar, and advanced search on the Web was conducted for data collection from prior studies. The plant root contains major active constituents including flavonoids and flavo-glycosides such as wogonin, baicalein, baicalin, oroxylin A, scutellarein, and norwogonin. These compounds have demonstrated a variety of pharmacological activities, combating inflammation, oxidative stress, cancer, neuronal disorders, and liver disorders. Chinese Skullcap represents a promising avenue for potential pharmacotherapeutic formulation advancement, emphasizing the need for further scientific exploration and clinical trials. [ABSTRACT FROM AUTHOR]

Walnuts (Juglans regia L.) are an important source of ellagitannins. They have been linked to positive effects on many pathologies, including cardiovascular disorders, neurodegenerative syndromes, and cancer. The limited bioavailability of ellagitannins prevents them from reaching significant circulatory levels, despite their antioxidant, anti-inflammatory, and chemopreventive properties. Urolithins are ellagitannin gut microbiota-derived metabolites. They have better intestinal absorption and may be responsible for the biological activities of ellagitannins. Recent evidence showed that walnut ellagitannins and their metabolites, urolithins, could have positive outcomes for human health. This study aims to synthesize the current literature on the antioxidant activity and mechanistic pathways involved in the therapeutic potential of walnut ellagitannins and their metabolites. In the eligible selected studies (n = 31), glansreginin A, pedunculagin, and casuarictin were the most prevalent ellagitannins in walnuts. A total of 15 urolithins, their glucuronides, and sulfate metabolites have been identified in urine, blood, feces, breast milk, and prostate tissue in analyzed samples. Urolithins A and B were associated with antioxidant, anti-inflammatory, cardioprotective, neuroprotective, anticarcinogenic, and anti-aging activities, both in preclinical and clinical studies. Despite the promising results, further well-designed studies are necessary to fully elucidate the mechanisms and confirm the therapeutic potential of these compounds in human health. [ABSTRACT FROM AUTHOR]

Boletus edulis (BE) is a mushroom well known for its taste, nutritional value, and medicinal properties. The objective of this work was to study the biological effects of BE extracts on human colon carcinoma cells (Caco-2), evaluating parameters related to oxidative stress and inflammation. In this study, a hydroethanolic extract of BE was obtained by ohmic heating green technology. The obtained BE extracts are mainly composed of sugars (mainly trehalose), phenolic compounds (taxifolin, rutin, and ellagic acid), and minerals (K, P, Mg, Na, Ca, Zn, Se, etc.). The results showed that BE extracts were able to reduce cancer cell proliferation by the induction of cell cycle arrest at the G0/G1 stage, as well as cell death by autophagy and apoptosis, the alteration of mitochondrial membrane potential, and caspase-3 activation. The extracts modified the redox balance of the cell by increasing the ROS levels associated with a decrease in the thioredoxin reductase activity. Similarly, BE extracts attenuated Caco-2 inflammation by reducing both iNOS and COX-2 mRNA expression and COX-2 protein expression. In addition, BE extracts protected the intestine from the oxidative stress induced by H2O2. Therefore, this study provides information on the potential use of BE bioactive compounds as anticancer therapeutic agents and as functional ingredients to prevent oxidative stress in the intestinal barrier. [ABSTRACT FROM AUTHOR]

Breast cancer is a major global health concern that requires the development of innovative treatment strategies. Epigallocatechin gallate (EGCG), a polyphenolic phytocompound found abundantly in green tea, has exhibited potential anti-cancer properties, including anti-inflammatory, anti-oxidant, anti-angiogenic, and anti-proliferative effects. However, the clinical translation of EGCG is hindered by its poor bioavailability and stability. Lipid-based nanocarriers have materialized as an optimistic platform for encapsulating various therapeutics due to their high drug-loading capacity, stability, biocompatibility, and versatility. The rationale for encapsulating EGCG-loaded lipid nanoparticles is to enhance the therapeutic efficacy, bioavailability, and targeted delivery of EGCG for breast cancer treatment. This targeted delivery minimizes off-target effects and enhances the accumulation of EGCG within tumors or diseased tissues in a controlled or sustained manner, reducing systemic toxicity. In addition, co-delivery of EGCG with synergistic agents can enhance therapeutic efficacy through complementary mechanisms of action, overcome biological barriers, and can be combined with other treatment modalities, i.e., radiation therapy, immunotherapy, chemotherapy, etc., to achieve synergistic effectiveness and overcome resistance mechanisms. The advancement of EGCG-loaded lipid nanoparticles exhibits the potential effectiveness of EGCG-based treatments, can overcome the challenges of administering EGCG, and can transform cancer therapy and other biomedical applications. Understanding the potential role of Epigallocatechin gallate (EGCG) in breast cancer treatment through various signaling pathways and further loaded into the lipid-based delivery system for the improvement of mechanical and biological characteristics of the EGCG.Article Highlights: Epigallocatechin gallate (EGCG), a green tea polyphenol for preventing breast cancer. PI3K/Akt/mTOR pathway dysregulated in breast cancer, targeting via EGCG. EGCG-loaded lipid nanoparticles for improved therapeutic potential in breast cancer. EGCG exhibits anti-angiogenic effects by inhibiting vascular endothelial growth factor. [ABSTRACT FROM AUTHOR]

Abstract A new group of thiazolidine-2,4-dione derivatives of ciprofloxacin having butyryl linker 3a-l was synthesized via an alkylation of thiazolidine-2,4-diones with butyryl ciprofloxacin with yield range 48–77% andfully characterized by various spectroscopic and analytical tools. Anti-cancer screening outcomes indicated that 3a and 3i possess antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 ± 1.50 and 25.4 ± 1.43 µM, respectively, using doxorubicin and cisplatin as positive controls with an IC50 of 7.03 ± 0.40 and 5.07 ± 0.29 µM, respectively. Additionally, compound 3j showed promising anticancer activity against human renal cancer A498 cell line with IC50 value of 33.9 ± 1.91 µM while doxorubicin and cisplatin showed IC50 values of 3.59 ± 0.20 and 7.92 ± 0.45, respectively. On the other hand, compound 3i did not show considerable anti-bacterial activity against S. aureus, E. coli and P. aeruginosa, and only moderate activity against K. pneumoniae with only a tenth of the activity of ciprofloxacin, confirming the cytotoxicity observed. Mechanistically, compound 3i inhibited both topoisomerase I and II with IC50 of 4.77 ± 0.26 and 15 ± 0.81 µM. Furthermore, it induced cell cycle arrest at S phase in melanoma LOX IMVI cells. Moreover, 3i provoked substantial levels of early, late apoptosis and necrosis in melanoma LOX IMVI cell line comparable to that induced by doxorubicin. Furthermore, compound 3i increased the expression level of active caspase-3 by 49 folds higher in LOX IMVI cell, increased protein expression level of Bax more than the control by 3 folds and inhibited PARP-1by 33% in LOX IMVI. All results were supported by theoretical docking studies on both tested enzymes confirming potential cytotoxicity for the synthesized hybrids.

Abstract Background Pancreatic and Gastric cancers are very aggressive and deadly types of cancer that require effective treatment strategies to stop their progression. Nano-drug delivery systems, like those using Auraptene-loaded GQD nanoparticles, play a crucial role in addressing this need by delivering targeted and controlled treatments to cancer cells, making treatment more effective, and reducing side effects. The study focused on investigating the effects of Auraptene, an efficient anticancer compound when loaded into Graphene Quantum Dots (GQDs) on types of human cancer cells. Methods To create auraptene-loaded graphene quantum dot nanoparticles (AGQD-NP) (Unmodified and modified types) a combination of hydrothermal and high-energy homogenization methods was used. The nanoparticles were characterized by conducting DLS (Dynamic light scattering), FTIR (Fourier-transform infrared spectroscopy), FESEM (Field Emission Scanning Electron microscopy), and zeta potential analysis. bioactivity of AGQD-NP was assessed through tests, including antioxidant capacity measured by ABTS and DPPH scavenging abilities well as cytotoxicity tested using MTT assay on both human cancer cell lines and normal human vascular endothelial cells. Results The modified AGQD-NP (M-AGQD-NP) demonstrated antioxidant properties by neutralizing free radicals. They also displayed selective toxicity, towards human gastric adenocarcinoma cell-line (AGS) and human pancreatic adenocarcinoma (PANC) cancer cells with IC50 values recorded at 78.8 µg/mL and 89.72 µg/mL respectively. The specific targeting of gastric cancer cells was evident from the differing IC50 values compared to the Human breast adenocarcinoma cell line (MCF-7), Human hepatocellular carcinoma cell line (Hella), and normal vascular endothelial cells (Huvec). Additionally, the induced apoptotic death, in the human pancreatic adenocarcinoma (PANC) cancer cells was confirmed through AO/PI staining and Annexin-based flow cytometry revealing increased expression levels of P53, Caspase3, BAX, and Caspase8. Conclusion In summary, the M-AGQD-NP have shown encouraging effects displaying antioxidant capabilities and a specific focus, on pancreatic and gastric cancer cells. These findings indicate uses for AGQD-NP as an efficient apoptosis inducer in cancer treatment. Additional In-vivo researches are required to validate their effectiveness, in living organisms.

Background: Metformin is widely prescribed for type 2 diabetes mellitus and is recognized for its therapeutic benefits beyond glycemic control. This review summarizes current data on metformin's diverse roles in various therapeutic contexts, including treating polycystic ovarian syndrome (PCOS), anti-inflammatory effects, and cancer prevention. Method: This comprehensive examination highlights the multifaceted applications of metformin in modern medicine and its potential to enhance the treatment of inflammatory diseases, cancer, and reproductive disorders. Results and Discussion: Metformin's anti-inflammatory properties may benefit autoimmune disorders, neurological diseases, and cardiovascular illnesses. In women with PCOS, metformin aids in restoring menstrual regularity, inducing ovulation, and improving reproductive outcomes by enhancing insulin sensitivity, modulating ovarian function, and reducing hyperandrogenism. Additionally, emerging evidence suggests that metformin may reduce cancer incidence and mortality in diabetic individuals by modulating cellular metabolism, inducing apoptosis, and inhibiting tumor cell proliferation. Conclusion: Our review suggests promising evidence for metformin's role in cancer prevention, reducing inflammation, and managing PCOS. However, further research is required to identify patient subgroups that will benefit most from metformin therapy, elucidate its mechanisms of action, and optimize dosing regimens.

Liyan Sun,1 Jinshuai Lan,1,2 Zhe Li,1,2 Ruifeng Zeng,1,2 Yi Shen,1 Tong Zhang,1,2 Yue Ding1– 3 1School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People’s Republic of China; 2State Key Laboratory of Integration and Innovation of Classic Formula and Modern Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People’s Republic of China; 3National Innovation Platform for Medical Industry-Education Integration, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People’s Republic of ChinaCorrespondence: Yue Ding; Tong Zhang, Email dingyue-2001@hotmail.com; zhangtongshutcm@hotmail.comAbstract: Berberine (BBR), recognized as an oncotherapeutic phytochemical, exhibits its anti-cancer properties via multiple molecular pathways. However, its clinical application is hindered by suboptimal tumor accumulation, rapid systemic elimination, and diminished bioactive concentration owing to extensive metabolic degradation. To circumvent these limitations, the strategic employment of nanocarriers and other drugs in combination with BBR is emerging as a focus to potentiate its anti-cancer efficacy. This review introduced the expansive spectrum of BBR’s anti-cancer activities, BBR and other drugs co-loaded nanocarriers for anti-cancer treatments, and evaluated the synergistic augmentation of these amalgamated modalities. The aim is to provide an overview of BBR for cancer treatment based on nano-delivery. Berberine (BBR), recognized as an oncotherapeutic phytochemical, exhibits its anti-cancer properties via multiple molecular pathways. However, its clinical application is hindered by suboptimal tumor accumulation, rapid systemic elimination, and diminished bioactive concentration owing to extensive metabolic degradation. To circumvent these limitations, the strategic employment of nanocarriers and other drugs in combination with BBR is emerging as a focus to potentiate its anti-cancer efficacy. Nano-delivery systems increase drug concentration at the tumor site by improving pharmacological activity and tissue distribution, enhancing drug bioavailability. Organic nanocarriers have advantages for berberine delivery including biocompatibility, encapsulation, and controlled release of the drug. While the advantages of inorganic nanocarriers for berberine delivery mainly lie in their efficient loading ability of the drug and their slow release ability of the drug. This review introduced the expansive spectrum of BBR’s anti-cancer activities, BBR and other drugs co-loaded nanocarriers for anti-cancer treatments, and evaluated the synergistic augmentation of these amalgamated modalities. The aim is to provide an overview of BBR for cancer treatment based on nano-delivery.Keywords: berberine, anti-cancer, nano drug delivery system, combination therapy

Irrespective of medical technology improvements, cancer ranks among the leading causes of mortality worldwide. Although numerous cures and treatments exist, creating alternative cancer therapies with fewer adverse side effects is vital. Since ancient times, plant bioactive compounds have already been used as a remedy to heal cancer. These plant bioactive compounds and their anticancer activity can also deregulate the microRNAs (miRNAs) in the cancerous cells. Therefore, the deregulation of miRNAs in cancer cells by plant bioactive compounds and the usage of the related miRNA could be a promising approach for cancer cure, mainly to prevent cancer and overcome chemotherapeutic side effect problems. Hence, this review highlights the function of plant bioactive compounds as an anticancer agent through the underlying mechanism that alters the miRNA expression in cancer cells, ultimately leading to apoptosis. Moreover, this review provides insight into using plant bioactive compounds -driven miRNAs as an anticancer agent to develop miRNA-based cancer gene therapy. They can be the potential resource for gene therapy and novel strategies targeting cancer therapeutics.

Novel compounds with pharmacological activity were synthesized from Pd (II), Fe (III), Cr (III), Ni (II), and Cu (II) ions with 4‐{2‐(3‐carboxy‐1‐cyclopropyl‐6‐fluoro‐7‐piperazin‐1‐yl‐2,3‐dihydro‐1H‐quinolin‐4‐ylideneamino)‐phenylimino}‐1‐cyclopropyl‐6‐fluoro‐7‐piperazin‐1‐yl‐1,4‐dihydro‐quinoline‐3‐carboxylic acid (CFPD). The newly synthesized compounds have been investigated by 1H‐ and 13C‐NMR spectra, Fourier transform infrared spectra, CHN analyses, ultraviolet‐visible spectra, mass spectra, molar conductivity, and magnetic moment measurements. In addition, the pH profile of the CFPD complexes showed remarkable stability, and their stability constant was identified in solution. To find out essential characteristics for CFPD and its complexes and to investigate the molecular geometry, computational analysis occurred. Through its nitrogen and OH of carboxylate groups, the ligand interacted with the metal ions to form CFPDPd complex with a square planar geometry and CFPDCu, CFPDCr, CFPDNi, and CFPDFe complexes with octahedral geometry. The M:L ratio of 1:1 was demonstrated by the molar ratio and sequence variation techniques' outcomes. The effect of the investigated CFPD imine ligand on bacterial community and its metal chelate was examined within vitro using a range of fungal and viral pathogens The findings showed that the effectiveness of antimicrobial went with the directive: CFPDPd complex when compared to the highly suppressor complex, fluconazol and ofloxacin as model medication. The novel ligand's and its complexes' in vitro cytotoxic potential against the Hep‐G2, MCF‐7, and HCT‐116 cell lines was also studied. The findings once more indicated that, when compared to vinblastine medication, the CFPDPd chelate is the most active agent. In addition, the complexes showed high reactivity in catching free radicals when their antioxidant activity was examined. By the application of viscosity, spectrum analysis, and gel electrophoreses, the interaction among metal chelates and DNA was determined. Studies on viscosity and spectrophotometric titration showed that every substance in test is a strong DNA binder. Increased hydrophobic and electrostatic interactions between aromatic rings could be the cause of this. In conclusion, these complexes have the potential to be effective bioactive agents. [ABSTRACT FROM AUTHOR]

Abstract A very practical method for the synthesis of unsymmetrical carbamide derivatives in good to excellent yield was presented, without the need for any catalyst and at room temperature. Using a facile and robust protocol, fifteen unsymmetrical carbamide derivatives (9–23) bearing different aliphatic amine moieties were designed and synthesized by the reaction of secondary aliphatic amines with isocyanate derivatives in the presence of acetonitrile as an appropriate solvent in good to excellent yields. Trusted instruments like IR, mass spectrometry, NMR spectra, and elemental analyses were employed to validate the purity and chemical structures of the synthesized compounds. All the synthesized compounds were tested as antimicrobial agents against some clinically bacterial pathogens such as Salmonella typhimurium, Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus aureus and Candida albicans. Compounds 15, 16, 17, 19 and 22 showed potent antimicrobial activity with promising MIC values compared to the positive controls. Moreover, compounds 15 and 22 provide a potent lipid peroxidation (LPO) of the bacterial cell wall. On the other hand, we investigated the anti-proliferative activity of compounds 9–23 against selected human cancerous cell lines of breast (MCF-7), colon (HCT-116), and lung (A549) relative to healthy noncancerous control skin fibroblast cells (BJ-1). The mechanism of their cytotoxic activity has been also examined by immunoassaying the levels of key anti- and pro-apoptotic protein markers. The results of MTT assay revealed that compounds 10, 13, 21, 22 and 23 possessed highly cytotoxic effects. Out of these, three synthesized compounds 13, 21 and 22 showed cytotoxicity with IC50 values (13, IC50 = 62.4 ± 0.128 and 22, IC50 = 91.6 ± 0.112 µM, respectively, on MCF-7), (13, IC50 = 43.5 ± 0.15 and 21, IC50 = 38.5 ± 0.17 µM, respectively, on HCT-116). Cell cycle and apoptosis/necrosis assays demonstrated that compounds 13 and 22 induced S and G2/M phase cell cycle arrest in MCF-7 cells, while only compound 13 had this effect on HCT-116 cells. Furthermore, compound 13 exhibited the greatest potency in inducing apoptosis in both cell lines compared to compounds 21 and 22. Docking studies indicated that compounds 10, 13, 21 and 23 could potentially inhibit enzymes and exert promising antimicrobial effects, as evidenced by their lower binding energies and various types of interactions observed at the active sites of key enzymes such as Sterol 14-demethylase of C. albicans, Dihydropteroate synthase of S. aureus, LasR of P. aeruginosa, Glucosamine-6-phosphate synthase of K. pneumenia and Gyrase B of B. subtilis. Moreover, 13, 21, and 22 demonstrated minimal binding energy and favorable affinity towards the active pocket of anticancer receptor proteins, including CDK2, EGFR, Erα, Topoisomerase II and VEGFFR. Physicochemical properties, drug-likeness, and ADME (absorption, distribution, metabolism, excretion, and toxicity) parameters of the selected compounds were also computed.

Objective(s): Breast cancer is an important women’s malignancy with high cancer-related deaths worldwide. Drug resistance lowers the treatment efficacy in this malignancy. This study aimed to explore the underlying mechanisms of histone deacetylase (HDAC) inhibitor trichostatin A (TSA) to overcome resistance to tamoxifen in breast cancer cells.Materials and Methods: Tamoxifen-resistance in MCF-7 breast cancer cells was simulated. MTT assay was used to detect the cytotoxic effects of HDAC inhibitor and PI3K inhibitor on the cancer cells. Trans-well assay was applied to evaluate the invasion and migration of the treated cancer cells. Flow cytometer assay was also applied to evaluate cell cycle phases in the treated cancer cells. Finally, expression of vascular endothelial growth factor (VEGF), E-cadherin, Vimentin, phosphorylated phosphatidylinositol kinase (p-PI3k), phosphorylated protein kinase B (p-AKT), and phosphorylated mammalian target protein of rapamycin (p-mTOR) was evaluated by western blotting.Results: The obtained results indicated that HDAC inhibitor treatments significantly decreased viability, migration, and invasion in the cancer cells. Furthermore, the frequency of the treated cancer cells significantly increased in the S phase as well as significantly decreasing in the G2/M phase of the cell cycle. Moreover, HDAC inhibitor modified levels of VEGF, E-cadherin, Vimentin, p-PI3k, p-AKT, and p-mTOR proteins. However, HDAC inhibitor combined with PI3K inhibitor exerts more profound effects on the cancer cells as compared to HDAC inhibitor monotherapy.Conclusion: HDAC inhibitors inhibited the survival of breast cancer drug-resistant cells, invasion, migration, and angiogenesis by inhibiting the PI3k/Akt/mTOR signaling pathway.

Abstract Crocin is a carotenoid compound in saffron with anti-cancer properties. However, its therapeutic application is limited by its low absorption, bioavailability, and stability, which can be overcome through nanocarrier delivery systems. This study used surface-modified Nano-crystalline cellulose (NCC) to deliver crocin to cancer cells. NCC modified with CTAB were loaded with crocin and then conjugated with folic acid (NCF-CR-NPs). The synthesized nanoparticles (NPs) were characterized using FTIR, XRD, DLS, and FESEM. The crystallinity index of NCC was 66.64%, higher than microcrystalline cellulose (61.4%). The crocin loading and encapsulation efficiency in NCF-CR-NPs were evaluated. Toxicity testing by MTT assay showed that NCF-CR-NPs had higher toxicity against various cancer cell lines, including colon cancer HT-29 cells (IC50 ~ 11.6 μg/ml), compared to free crocin. Fluorescent staining, flow cytometry, and molecular analysis confirmed that NCF-CR-NPs induced apoptosis in HT-29 cells by increasing p53 and caspase 8 expression. The antioxidant capacity of NCF-CR-NPs was also evaluated using ABTS and DPPH radical scavenging assays. NCF-CR-NPs exhibited high free radical scavenging ability, with an IC50 of ~ 46.5 μg/ml for ABTS. In conclusion, this study demonstrates the potential of NCF-CR-NPs to deliver crocin to cancer cells effectively. The NPs exhibited enhanced anti-cancer and antioxidant activities compared to free crocin, making them a promising nanocarrier system for crocin-based cancer therapy.

Dan Lv,1 Yuling Liu,1 Ruying Tang,1 Sai Fu,1 Shasha Kong,1 Qian Liao,1 Hui Li,1,2 Longfei Lin1 1Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, 100700, People’s Republic of China; 2Institute of Traditional Chinese Medicine Health Industry, China Academy of Chinese Medical Sciences, Jiangxi, 330006, People’s Republic of ChinaCorrespondence: Hui Li; Longfei Lin, Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Nanxiaojie 16, 8 Dongzhimennei Ave, Beijing, 100700, People’s Republic of China, Tel +86-10-64032658, Email hli1967@icmm.ac; lflin@icmm.ac.cnAbstract: The potential anti-cancer effect of traditional Chinese medicine (TCM) monomers has been widely studied due to their advantages of well-defined structure, clear therapeutic effects, and easy quality control during the manufacturing process. However, clinical trial information on these monomers is scarce, resulting in a lack of knowledge regarding the research progress, efficacy, and adverse reactions at the clinical stage. Therefore, this study systematically reviewed the clinical trials on the anti-cancer effect of TCM monomers registered in the Clinicaltrials.gov website before 2023.4.30, paying special attention to the trials on tumors, aiming to explore the research results and development prospects in this field. A total of 1982 trials were started using 69 of the 131 TCM monomers. The number of clinical trials performed each year showed an overall upward trend. However, only 26 monomers entered into 519 interventional anti-tumor trials, with vinblastine (194, 37.38%) and camptothecin (146, 28.13%) being the most used. A total of 45 tumors were studied in these 519 trials, with lymphoma (112, 21.58%) being the most frequently studied. Clinical trials are also unevenly distributed across locations and sponsors/collaborators. The location and the sponsor/collaborator with the highest number of performed trials were the United States (651,32.85%) and NIH (77). Therefore, China and its institutions still have large room for progress in promoting TCM monomers in anti-tumor clinical trials. In the next step, priority should be given to the improvement of the research and development ability of domestic enterprises, universities and other institutions, using modern scientific and technological means to solve the problems of poor water solubility and strong toxic and side effects of monomers, so as to promote the clinical research of TCM monomers.Keywords: traditional Chinese medicine monomers, anti-cancer, interventional clinical trials, research progress, adverse reactions

Fucoxanthin is a carotenoid, reddish-brown in color, which is mainly derived from marine organisms such as brown algae and diatoms, and has aroused extensive scientific interest due to its unique chemical structure and abundant biological activities. Studies have shown that fucoxanthin processes significant anti-inflammatory and anti-cancer activities. Its anti-inflammatory mechanisms primarily include inhibiting oxidative stress, regulating inflammatory factors, inducting cell autophagy, and resisting cell apoptosis, etc. The main mechanism of anti-cancer activity includes inducing cell autophagy and apoptosis mechanisms, regulating the cell cycle, inhibiting cell migration, and suppressing cell invasion, among other aspects. In this paper, the research progress of anti-inflammatory and anti-cancer activities and related mechanisms of action of fucoxanthin is briefly summarized, which provides the theoretical basis and reference for further research and development of fucoxanthin.

Colorectal carcinoma (CRC) is one of the most common malignancies, though there are no effective therapeutic regimens at present. This study aimed to investigate the inhibitory effects of mannooligosaccharides extracted from coconut meal (CMOSs) on the proliferation and migration of human colorectal cancer HCT116 cells in vitro. The results showed that CMOSs exhibited significant inhibitory activity against HCT116 cell proliferation in a concentration-dependent manner with less cytotoxic effects on the Vero normal cells. CMOSs displayed the ability to increase the activation of caspase-8, –9, and –3/7, as well as the generation of reactive oxygen species (ROS). Moreover, CMOSs suppressed HCT116 cell migration in vitro. Interestingly, treatment of human microvascular endothelial cells (HMVECs) with CMOSs resulted in the inhibition of cell proliferation, cell migration, and capillary-like tube formation, suggesting its anti-vascular angiogenesis. In summary, the results of this study indicate that CMOSs could be a valuable therapeutic candidate for CRC treatment.

Background: Several nano formulations of silver nanoparticles with bioconjugates, herbal extracts and anti-cancerous drug coating have been vividly studied to target cancer. Despite of such extensive studies, AgNPs (silver nanoparticles) have not reached the stage of clinical use. Out of all possible reasons for this failure, the unexplored effect on Cancer Stem Cell (CSC) population and mechanism of action of AgNPs, are the most plausible ones and are worked upon in this study. Methods: AgNPs were synthesized by chemical reduction method using sodium citrate and characterized by UV, FTIR, XRD and electron microscopy. CSC population was isolated from Cal33 cell line by MACS technique. MTT assay, trypan blue exclusion assay, Annexin V and PI based apoptosis assay and cell cycle assay were performed. Results: The results showed that synthesized AgNPs have cytotoxic activity on all cancer cell lines tested with the IC50 value of a wide range (1.5–49.21 µg/ml for cell lines and 0.0643–0.1211 µg/ml for splenocytes and thymocytes). CSCs Cal33 showed higher resistance to AgNP treatment and arrest in G1/G0 phase upon cell cycle analysis. Conclusion: AgNPs as an anti-cancer agent although have great potential but is limited by its off-target effects on normal cells and less effective on cancer stem cells at lower concentrations.

In recent times, there have been notable advancements in comprehending the potential anti-cancer effects of chrysin (CH), a naturally occurring flavonoid compound found abundantly in various plant sources like honey, propolis, and certain fruits and vegetables. This active compound has garnered significant attention due to its promising therapeutic qualities and minimal toxicity. CH’s ability to combat cancer arises from its multifaceted mechanisms of action, including the initiation of apoptosis and the inhibition of proliferation, angiogenesis, metastasis, and cell cycle progression. CH also displays potent antioxidant and anti-inflammatory properties, effectively counteracting the harmful molecules that contribute to DNA damage and the development of cancer. Furthermore, CH has exhibited the potential to sensitize cancer cells to traditional chemotherapy and radiotherapy, amplifying the effectiveness of these treatments while reducing their negative impact on healthy cells. Hence, in this current review, the composition, chemistry, mechanisms of action, safety concerns of CH, along with the feasibility of its nanoformulations. To conclude, the recent investigations into CH’s anti-cancer effects present a compelling glimpse into the potential of this natural compound as a complementary therapeutic element in the array of anti-cancer approaches, providing a safer and more comprehensive method of combating this devastating ailment.