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Glioblastoma multiforme (GBM) is regarded as the most aggressive form of brain tumor delineated by high cellular heterogeneity; it is resistant to conventional therapeutic regimens. In this study, the anti-cancer potential of garcinol, a naturally derived benzophenone, was assessed against GBM. During the analysis, we observed a reduction in the viability of rat glioblastoma C6 cells at a concentration of 30 µM of the extract (p < 0.001). Exposure to garcinol also induced nuclear fragmentation and condensation, as evidenced by DAPI-stained photomicrographs of C6 cells. The dissipation of mitochondrial membrane potential in a dose-dependent fashion was linked to the activation of caspases. Furthermore, it was observed that garcinol mediated the inhibition of NF-κB (p < 0.001) and decreased the expression of genes associated with cell survival (Bcl-XL, Bcl-2, and survivin) and proliferation (cyclin D1). Moreover, garcinol showed interaction with NF-κB through some important amino acid residues, such as Pro275, Trp258, Glu225, and Gly259 during molecular docking analysis. Comparative analysis with positive control (temozolomide) was also performed. We found that garcinol induced apoptotic cell death via inhibiting NF-κB activity in C6 cells, thus implicating it as a plausible therapeutic agent for GBM. [ABSTRACT FROM AUTHOR]

A receptor-based pharmacophore model describing the binding features required for the multi-kinase inhibition of the target kinases (VEGFR-2, FGFR-1, and BRAF) were constructed and validated. It showed a good overall quality in discriminating between the active and the inactive in a compiled test set compounds with F1 score of 0.502 and Mathew's correlation coefficient of 0.513. It described the ligand binding to the hinge region Cys or Ala, the glutamate residue of the Glu-Lys αC helix conserved pair, the DFG motif Asp at the activation loop, and the allosteric back pocket next to the ATP binding site. Moreover, excluded volumes were used to define the steric extent of the binding sites. The application of the developed pharmacophore model in virtual screening of an in-house scaffold dataset resulted in the identification of a benzimidazole-based scaffold as a promising hit within the dataset. Compounds 8a-u were designed through structural optimization of the hit benzimidazole-based scaffold through (un)substituted aryl substitution on 2 and 5 positions of the benzimidazole ring. Molecular docking simulations and ADME properties predictions confirmed the promising characteristics of the designed compounds in terms of binding affinity and pharmacokinetic properties, respectively. The designed compounds 8a-u were synthesized, and they demonstrated moderate to potent VEGFR-2 inhibitory activity at 10 µM. Compound 8u exhibited a potent inhibitory activity against the target kinases (VEGFR-2, FGFR-1, and BRAF) with IC50 values of 0.93, 3.74, 0.25 µM, respectively. The benzimidazole derivatives 8a-u were all selected by the NCI (USA) to conduct their anti-proliferation screening. Compounds 8a and 8d resulted in a potent mean growth inhibition % (GI%) of 97.73% and 92.51%, respectively. Whereas compounds 8h, 8j, 8k, 8o, 8q, 8r, and 8u showed a mean GI% > 100% (lethal effect). The most potent compounds on the NCI panel of 60 different cancer cell lines were progressed further to NCI five-dose testing. The benzimidazole derivatives 8a, 8d, 8h, 8j, 8k, 8o, 8q, 8r and 8u exhibited potent anticancer activity on the tested cell lines reaching sub-micromolar range. Moreover, 8u was found to induce cell cycle arrest of MCF-7 cell line at the G2/M phase and accumulating cells at the sub-G1 phase as a result of cell apoptosis. [ABSTRACT FROM AUTHOR]

This review article delves into the intricate biological activities of uracil, an essential pyrimidine Base pivotal in RNA structures. Examining its involvement in nucleic acid metabolism, various multifunctional roles, spanning from influencing cell proliferation to its antimicrobial and antiviral properties. The study explores signal transduction pathways affected by uracil, unraveling potential therapeutic applications. By unraveling the nuanced biological mechanisms. This review contributes to a deeper understanding of uracil's impact, offering insights crucial for drug development and advancing biomedical research. [ABSTRACT FROM AUTHOR]

The emergence of nanotechnology as a field of study can be traced back to the 1980s, at which point the means to artificially produce, control, and observe matter on a nanometer level was made viable. Recent advancements in technology have enabled us to extend our reach to the nanoscale, which has presented an unparalleled opportunity to directly target biomolecular interactions. As a result of these developments, there is a drive to arise intelligent nanostructures capable of overcoming the obstacles that have impeded the progress of conventional pharmacological methodologies. After four decades, the gradual amalgamation of bio- and nanotechnologies is initiating a revolution in the realm of disease detection, treatment, and monitoring, as well as unsolved medical predicaments. Although a significant portion of research in the field is still confined to laboratories, the initial application of nanotechnology as treatments, vaccines, pharmaceuticals, and diagnostic equipment has now obtained endorsement for commercialization and clinical practice. The current issue presents an overview of the latest progress in nanomedical strategies towards alleviating antibiotic resistance, diagnosing and treating cancer, addressing neurodegenerative disorders, and an array of applications, encompassing dentistry and tuberculosis treatment. The current investigation also scrutinizes the deployment of sophisticated smart nanostructured materials in fields of application such as regenerative medicine, as well as the management of targeted and sustained release of pharmaceuticals and therapeutic interventions. The aforementioned concept exhibits the potential for revolutionary advancements within the field of immunotherapy, as it introduces the utilization of implanted vaccine technology to consistently regulate and augment immune functions. Concurrently with the endeavor to attain the advantages of nanomedical intervention, it is essential to enhance the unceasing emphasis on nanotoxicological research and the regulation of nanomedications' safety. This initiative is crucial in achieving the advancement in medicine that currently lies within our reach. [ABSTRACT FROM AUTHOR]

Most living organisms secrete tiny lipid bilayer particles encapsulating various biomolecular entities, including nucleic acids and proteins. These secreted extracellular vesicles (EVs) are shown to aid in communication between cells and their environment. EVs are mainly involved in the signalling and manipulation of physiological processes. Plant EVs display similar functional activity as seen in mammalian EVs. Medicinal plants have many bioactive constituents with potential applications in cancer treatment. Particularly, Basil (Ocimum basilicum), has wide therapeutic properties including anti‐inflammatory, anti‐cancer, and anti‐infection, among others. In this study, we focused on using EVs purified from Apoplast Washing Fluid (AWF) of Basil plant leaves as a biological therapeutic agent against cancer. Characterization of Basil EVs revealed a size range of 100–250 nm, which were later assessed for their cell uptake and apoptosis inducing abilities in pancreatic cancer cells. Basil plant EVs (BasEVs) showed a significant cytotoxic effect on pancreatic cancer cell line MIA PaCa‐2 at a concentration of 80 and 160 μg/mL in cell viability, as well as clonogenic assays. Similarly, RT‐PCR and western blot analysis has shown up regulation in apoptotic gene and protein expression of Bax, respectively, in BasEV treatment groups compared to untreated controls of MIA PaCa‐2. Overall, our results suggest that EVs from basil plants have potent anti‐cancer effects in pancreatic cancer cells and can serve as a drug delivery system, demanding an investigation into the therapeutic potential of other medicinal plant EVs. [ABSTRACT FROM AUTHOR]

Background and Aim: Hematological and blood chemistry parameters are crucial for evaluating and monitoring canine multicentric lymphoma during chemotherapy. Pre-treatment hematological and blood chemistry parameters can be used as prognostic survival outcomes for this disease. Therefore, this study aimed to investigate the effect of hematological and blood chemistry parameters pre-treatment and 4 weeks post-treatment on the survival outcomes of dogs treated with either a combination of cyclophosphamide, vincristine, and prednisolone (COP) or a combination of COP with L-asparaginase (L-COP) protocols. Materials and Methods: We conducted a retrospective study. Medical records and hematological and blood chemistry parameters of 41 dogs with multicentric lymphoma treated with L-COP (n = 26) and the COP protocols (n = 15) were obtained from the hospital information system. Most cases were classified as high-grade lymphoma based on the Kiel cytological classification. The effects of hematological and blood chemistry parameters on survival outcomes were investigated using the Cox proportional hazard regression model. The median survival time (MST) for each hematological and blood chemistry parameter affecting survival outcome was established and compared using the Kaplan-Meier product limit method with the log-rank test. Results: Dogs with high-grade multicentric lymphoma that were treated with the COP protocol and had monocytosis at pre-treatment had a significantly shorter MST than dogs with normal monocyte counts (p = 0.033). In addition, dogs with azotemia, both pre-treatment and 4 weeks post-treatment, had a significantly shorter MST than dogs with normal serum creatinine levels (p = 0.012). Dogs with high-grade multicentric lymphoma treated with the L-COP protocol who had hypoalbuminemia (serum albumin concentration <2.5 mg/dL) at both pre-treatment and 4 weeks post-treatment had a significantly shorter MST than dogs with normal serum albumin levels (p < 0.001). Furthermore, dogs with leukocytosis at 4 weeks post-treatment had a significantly shorter MST than those with a normal total white blood cell count (p = 0.024). Conclusion: Serum albumin level can serve as a simple negative prognostic indicator of survival outcomes in dogs with high-grade multicentric lymphoma treated with the L-COP protocol. Dogs with hypoalbuminemia pre-treatment and 4 weeks post-treatment tended to have a shorter MST than those with normal serum albumin concentrations. [ABSTRACT FROM AUTHOR]

Background: Ferroptosis, a newly form of regulated cell death (RCD), is characterized by iron dyshomeostasis and unrestricted lipid peroxidation. Emerging evidence depicts a pivotal role for ferroptosis in driving some pathological processes, especially in cancer. Triggering ferroptosis can suppress tumor growth and induce an anti-tumor immune response, denoting the therapeutic promises for targeting ferroptosis in the management of cancer. As an autophagic phenomenon, ferritinophagy is critical to induce ferroptosis by degradation of ferritin to release intracellular free iron. Recently, a great deal of effort has gone into designing and developing anti-cancer strategies based on targeting ferritinophagy to induce ferroptosis. Conclusion: This review delineates the regulatory mechanism of ferritinophagy firstly and summarizes the role of ferritinophagy-induced ferroptosis in cancer. Moreover, the strategies targeting ferritinophagy to induce ferroptosis are highlighted to unveil the therapeutic value of ferritinophagy as a target to manage cancer. Finally, the future research directions on how to cope with the challenges in developing ferritinophagy promoters into clinical therapeutics are discussed. [ABSTRACT FROM AUTHOR]

Artemisia herba-alba L. (A. herba-alba), growing in the Mediterranean regions, contains various phytochemical compounds with exceptional pharmacological and chemical properties. The present study aims to characterize chemical and biological activities of A. herba-alba's methanolic extract according to total protein, total phenols, antioxidant, anti-inflammatory, and anti-hemolytic activities. The study also evaluates the extract's anti-proliferative activity of diverse cancer cell lines in vitro. Liquid chromatography-mass spectrometry (LC-MS) was used to conduct phytochemical analysis of A. herba-alba's extract. The total phenolic amount, total proteins, anti-inflammatory, and anti-hemolytic activity was evaluated in vitro alongside antioxidant activity by various spectrophotometric methods. LC-MS analysis of crude extract reveals that kaempferol, quercetin, geranyl acetate, dihydrolinalool, furanone, vetivenic acid, limonene, eugenol, p-cymene, and naringin represent the major composition (81.5%). A. herba-alba's extract showed 72.07 % antioxidant activity through DPPH radical scavenging with IC50 value 0.67 μg/ml. Furthermore, the extract from A. herba-alba had a 68.71% antihemolytic impact and a 97.55% anti-inflammatory effect. These different bioactivities were linked and correlated to the total phenolic content in the extract (1.41 mg/ml). The correlation between phenolic contents and activity of DPPH scavenging, anti-inflammatory, and anti-hemolytic was expressed with Pearson correlation coefficient and found to be a strong correlation of the extract with R² close to 0.90. Furthermore, strong cytotoxic activity was shown by the extract against tested cancer cell lines. The IC50 values for lung cancer HCC95 was 7.0 μg/mL, breast cancer MDA-MB-231 was 6.9 μg/mL, prostate DU-145 was 6.8 μg/mL, and breast cancer 600MPE was 6.7 μg/mL. According to the research, the methanolic extract of A. herba-alba plant contains numerous phytochemicals, primarily phenolic compounds. The extract exhibits antioxidant, anti-inflammatory, and anti-hemolytic activities, as well as strong cytotoxic activity. [ABSTRACT FROM AUTHOR]

Black garlic (BG) is a fermented form of garlic (Allium sativum L.), produced at precisely defined temperatures, humidities, and time periods. Although garlic has been used for thousands of years, black garlic is a relatively new discovery. There are many bioactive compounds in black garlic that give it medicinal properties, including anti-inflammatory and anti-cancer properties. In our review article, we present scientific studies examining the anti-inflammatory and anti-cancer effects of black garlic. According to research, this effect is mainly due to the reduction in the production of pro-inflammatory cytokines, as well as the ability to scavenge free oxygen radicals and induce apoptosis. In addition, the phytochemicals contained in it have antiproliferative and antiangiogenic properties and inhibit the growth of cancer cells. Black garlic is a valuable source of biologically active substances that can support anti-inflammatory and anti-cancer therapy. Compared to Allium sativum, black garlic has fewer side effects and is easier to consume. [ABSTRACT FROM AUTHOR]

Metal/Metal Oxide nanoparticles (M/MO NPs) exhibit potential biomedical applications due to their tunable physicochemical properties. Recently, the biogenic synthesis of M/MO NPs has gained massive attention due to their economical and eco-friendly nature. In the present study, Nyctanthes arbor-tristis (Nat) flower extract-derived Zinc Ferrite NPs (Nat-ZnFe2O4 NPs) were synthesized and physicochemically characterized by FTIR, XRD, FE-SEM, DLS, and other instruments to study their crystallinity, size, shape, net charge, presence of phytocompounds on NP's surface and several other features. The average particle size of Nat-ZnFe2O4 NPs was approx. 25.87 ± 5.67 nm. XRD results showed the crystalline nature of Nat-ZnFe2O4 NPs. The net surface charge on NPs was -13.28 ± 7.18 mV. When tested on mouse fibroblasts and human RBCs, these NPs were biocompatible and hemocompatible. Later, these Nat-ZnFe2O4 NPs exhibited potent anti-neoplastic activity against pancreatic, lung, and cervical cancer cells. In addition, NPs induced apoptosis in tested cancer cells through ROS generation. These in vitro studies confirmed that Nat-ZnFe2O4 NPs could be used for cancer therapy. Moreover, further studies are recommended on ex vivo platforms for future clinical applications. [ABSTRACT FROM AUTHOR]

Geijera Schott is a plant genus of the Rutaceae Juss. (rue and citrus) family, comprising six species which are all native to Oceania. Of the plants belonging to this genus, the most significant species that has a customary use is Geijera parviflora, which was used by Indigenous Australians, primarily as a pain reliever. Herein, a comprehensive review of the literature published on the genus Geijera from 1930 to 2023 was conducted. This is the first review for this plant genus, and it highlights the chemical constituents reported to date, together with the range of pharmacological properties described from the various species and different parts of the plant. These properties include anti-inflammatory, anti-microbial, anti-parasitic, insect repellent, analgesic, neuroactive, and anti-cancer activities. Finally, a reflection on some of the important areas for future focused studies of this plant genus is provided. [ABSTRACT FROM AUTHOR]

Background: L-arginase, is a powerful anticancer that hydrolyzes L-arginine to L-ornithine and urea. This enzyme is widely distributed and expressed in organisms like plants, fungi, however very scarce from bacteria. Our study is based on isolating, purifying, and screening the marine bacteria that can produce arginase. Results: The highest arginase producing bacteria will be identified by using microbiological and molecular biology methods as Bacillus licheniformis OF2. Characterization of arginase is the objective of this study. The activity of enzyme was screened, and estimated beside partial sequencing of arginase gene was analyzed. In silico homology modeling was applied to generate the protein's 3D structure, and COACH and COFACTOR were applied to determine the protein's binding sites and biological annotations based on the I-TASSER structure prediction. The purified enzyme was undergone an in vitro anticancer test. Conclusions: L-arginase demonstrated more strong anti-cancer cells with an IC50 of 21.4 ug/ml in a dose-dependent manner. L-arginase underwent another investigation for its impact on the caspase 7 and BCL2 family of proteins (BCL2, Bax, and Bax/Bcl2). Through cell arrest in the G1/S phase, L-arginase signals the apoptotic cascade, which is supported by a flow cytometry analysis of cell cycle phases. [ABSTRACT FROM AUTHOR]

Mesenchymal stem cells (MSCs) have tumor-homing ability and play critical roles in tumor treatment, but their dual influences on tumor progression limit their therapeutic applications. Exosomes derived from MSCs (MSC-exosomes) exhibit great potential in targeted tumor treatment due to their advantages of high stability, low immunogenicity, good biocompatibility, long circulation time and homing characteristics. Furthermore, the artificial modification of MSC-exosomes could amplify their advantages and their inhibitory effect on tumors and could overcome the limit of tumor-promoting effect. In this review, we summarize the latest therapeutic strategies involving artificially modified MSCexosomes in tumor treatment, including employing these exosomes as nanomaterials to carry noncoding RNAs or their inhibitors and anticancer drugs, and genetic engineering modification of MSC-exosomes. We also discuss the feasibility of utilizing artificially modified MSC-exosomes as an emerging cell-free method for tumor treatment and related challenges. [ABSTRACT FROM AUTHOR]

Disturbances in immunoregulation may lead to both cancer and autoimmune diseases. Many therapeutic drugs for autoimmune diseases also display antitumor efficacy. The Janus kinase/signal transducer and activator of transcription signaling pathways are involved in the secretion of more than 50 distinct cytokines, which have critical roles in inducing autoimmune diseases and tumorigenesis. Thus, Janus kinases have become classical immunotherapeutic targets for immune disease. More than 70 Janus kinase inhibitors have been approved as immunomodulatory drugs for clinical use, of which 12 are used in the treatment of autoimmune diseases. This systematic review aims to elucidate the anti-tumor role of clinically approved Janus kinase inhibitors that were primarily designed for the treatment of autoimmune diseases and their potential for clinical translation as cancer treatments. [ABSTRACT FROM AUTHOR]

Due to complexity of tumor diseases and resistance of targeted drug, targeted drug usually cannot meet the needs of cancer treatment. Therefore, the conjugate constructed by two anticancer agents maybe a better solution for the tumor diseases. As natural anticancer agents, icaritin and norcantharidin are selected for the construction of conjugate. In the condition of EDCI/DMAP, icaritin is reacted with norcantharidin esters to give the desired 7-esters selectively in a moderate yield. MTT method was used to test the cytotoxicity and intensity on Hep G2 and MCF-7 in vitro. Some of the compounds (4a, 4i and 4j) show a better inhibition against Hep G2 and MCF-7 cell lines in vitro, and are deserved to be a potential drug candidate to develop in vivo. [ABSTRACT FROM AUTHOR]

Design and synthesis of a series of novel hybrid molecules that combine Imidazo[4,5‐c] pyridines with piperdines are presented in this paper. Total 17 derivatives were meticulously synthesized and characterized using 1H NMR, 13C NMR, MS and elemental analysis techniques. The in vitroanticancer activities are estimated by verifying their effectiveness against the MCF‐7 human breast adenocarcinoma and A549 lung cancer cell line, with cisplatin and doxorubicin serving as reference drugs. Several of these compounds demonstrated significant potential, displaying IC50 values within the range of 12.26–84.5 μM for A549, and 13.37–69.82 μM for MCF‐7. Notably, compound 11 bis found to be more potent than the standard drug cisplatin with an IC50 of 12.26±0.8 μM against A549 cells, while compound 11 d exhibited highest inhibition with an IC50 of 13.37±0.4 μM against MCF‐7 cells. Although its effectiveness was moderately lower when compared to doxorubicin, it still retained substantial anticancer activity. Molecular docking studies were performed to decouple the binding affinity and ligand interactions of the compounds with the estrogen receptor alpha (ERα) (PDB ID: 3ERT). The pharmacokinetic evaluation revealed favourable drug‐likeness properties for all the molecules, suggesting their potential as therapeutic agents. [ABSTRACT FROM AUTHOR]

Metallic nanoparticles play a significant role in the catalysis of chemical processes, besides, bimetallic nanoparticles with abundant active sites can reduce metallic nanoparticles toxicity in addition to increasing their catalytic performances. In this work, the platinum, gold, and silver nanoparticles are bio-synthesized using a native bacterium (GFCr-4). Also, the Au-Ag and Au@Ag bimetallic nanoparticles with alloy and core-shell structures, respectively, are biologically synthesized. To improve the synthesis, the effects of various factors like pH, temperature, electron donor, and ionic liquids were investigated. The as-synthesized nanoparticles were characterized with different techniques. The microscope images and dynamic light scattering (DLS) analysis confirm the uniform distribution of as-synthesized nanoparticles with average sizes of 25, 30, 47, 77, and 86 nm obtained for Ag, Au, Pt, Au-Ag alloy, and Au@Ag core-shell, respectively. The catalytic performances of as-synthesized nanoparticles were investigated. The Au-Ag alloy nanoparticles exhibit better catalytic performance than the as-synthesized metallic Au nanoparticles, according to the Gewald reaction. According to the photocatalytic study, the yield can be increased by up to 92% by using PtNPs in the presence of a green LED. Additionally, for the first time, PtNPs were utilized as an effective catalyst in a peroxyoxalate chemiluminescence (POCL) system in the presence of nuclear fast red (NFR) as a novel fluorophore. In addition, the results of the MTT (3-[4,5-dimethylthiazol-2-yl]−2,5 diphenyl tetrazolium bromide) assay revealed that the synthesized eco-friendly nanoparticles have a low effect on the lethality of 3T3 normal cells whereas MCF-7 cancer cells were inhibited up to 77.3% after treatment by PtNPs nanoparticles. • Metallic and bimetallic nanoparticles were synthesized by GFCr-4 bacteria strain. • The platinum nanoparticle size became smaller with Tween 80 additive. • Bio-synthesized nanoparticles showed excellent catalytic activity. • Au-Ag alloy nanoparticles showed lower toxicity and higher catalytic performance. • Bio-synthesized nanoparticles have high cytotoxicity upon cancerous cells.. [ABSTRACT FROM AUTHOR]

Essential oils have remained a popular herbal remedy for various chronic diseases since ages. But most of these products lack sufficient clinical evidence for therapeutic value. One such valuable variety of medicinal plants is Guava (Psidium guajava). This plant has found to have various applications in the treatment of different ailments such as diarrhea, dysentery, gastroenteritis, high blood pressure, diabetes, tooth decay and pain relief. Alongside producing benefits for improving coordination and mobility. The medicinal properties of this plant are largely derived from its leaf extract, which is used for treating cough, diarrhea, oral ulcers and swollen gums. Additionally, the fruit of the plant is packed with essential nutrients like vitamins A and C, iron, phosphorus and calcium, as well as many other organic and inorganic compounds, including antioxidants, polyphenols, antiviral compounds and anti-inflammatory compounds. The phenolic components in guava are effective in fighting against cancer cells and preventing premature aging of the skin. Relaxation effects are produced by certain components like terpenes, caryophyllene oxide and p-selinene. Guava leaves contain multiple compounds that act as inhibitors of fungal and bacterial growth. This plant is also rich in antioxidants like quercetin, providing it with radio-protective abilities, to relieve muscle spasms. The extract of guava also demonstrates pain-relieving activity and is effective in reducing inflammation and promoting the production of serum in cases of liver damage. However, there is a need for detailed research to separate and characterize the precise antimicrobial elements and to delve into other potential medicinal impacts. As a result, once the crucial oil components are isolated, they can be employed as a curative solution for combatting contagious illnesses and many other advantages of this plant. [ABSTRACT FROM AUTHOR]

Plants have been utilized for the treatment of various diseases since ages because of their plethora of pharmacological actions and almost inferior side effects. Among all medicinal plants seas buckthorn also came into limelight because of its unique appearance and valuable phytoconstituents as well as medicinal properties. The sea buckthorn known as Hippophae rhamnoides L. belonging to family Elaeagnaceae is a berries bearing plant. This review explores the plant profile, phytochemistry, pharmacological activities including: in vivo, in vitro, clinical studies of the plant and market preparation till date of sea buckthorn. The data was collected by comprehensively searching various scientific search engines i.e., PubMed, Google Scholar, web of science etc. According to literature plant contains various phenolic and non-phenolic secondary metabolites and nutrients. Majorly plants contains Carotenoids, Triterpenoids, Phenolic compounds i.e. Kaempferol, quercetin, gallic acid, Catechin, Epicatechin, Gallo catechin etc. Apart from these different parts of the plants also contains Lipids, Proteins, fatty acids, sterols; volatile compounds, Amino acids, Proteins, Sugars, Pectin, Vitamins (C, E, B, K1, D, A, folic acid) Macro and trace elements (potassium, magnesium, calcium, iron, sodium, manganese, zinc, copper, nickel). Sea buckthorn is known for its antioxidant, anti-cancer, antidiabetic, hepatoprotective, wound healing, anti-bacterial, anti-viral etc. pharmacological properties. In conclusion, the elaborate tapestry of sea buckthorn's phytochemistry and its multifaceted pharmacological actions has illuminated a promising path for both nutritional and therapeutic exploration. However, the paper's identification of substantial data gaps will spur more research and development, particularly for the creation of nutraceuticals and herbal medicines based on sea buckthorn. [ABSTRACT FROM AUTHOR]

A new Schiff base with ligands (L¹ and L²) has been prepared from cinnamaldehyde with aniline (L¹) and 4-hydroxy-3-methoxybenzaldehyde with o-nitroaniline in 1:1 molar ratio. The mononuclear metal(II) complexes [(ML¹L²)] [M= Co(II), Ni(II), Cu(II) and Zn(II)] have been synthesized and characterized. ML¹L² synthesized from ligand (L¹), metal salts and ligand (L²) molar ratio is 1:1:1. Elemental analyses, IR, NMR, Electronic spectra, SEM and molar conductivity have been obtained to clarify the structure of synthesized metal(II) complexes. Square planar geometry is proposed for CoL¹L², NiL¹L² and ZnL¹L², and distorted square planar geometry for CuL¹L² complex. Antibacterial activity of metal(II) complexes, ML¹L² have been tested against Gram(+) and Gram(-) bacteria and fungi. The anti-inflammatory and anti-diabetic actions of the L¹, L², CuL¹L²complexes have been studied. The anticancer activity of L¹, L² and CuL¹L² have been studied as opposed to MCF-7 using MTT assay method. [ABSTRACT FROM AUTHOR]

Ferroptosis, an iron-dependent cell death mechanism driven by an accumulation of lipid peroxides on cellular membranes, has emerged as a promising strategy to treat various diseases, including cancer. Ferroptosis inducers not only exhibit cytotoxic effects on multiple cancer cells, including drug-resistant cancer variants, but also hold potential as adjuncts to enhance the efficacy of other anti-cancer therapies, such as immunotherapy. In addition to synthetic inducers, natural compounds, such as artemisinin, can be considered ferroptosis inducers. Artemisinin, extracted from Artemisia annua L., is a poorly water-soluble antimalarial drug. For clinical applications, researchers have synthesized various water-soluble artemisinin derivatives such as dihydroartemisinin, artesunate, and artemether. Artemisinin and artemisinin derivatives (ARTEs) upregulate intracellular free iron levels and promote the accumulation of intracellular lipid peroxides to induce cancer cell ferroptosis, alleviating cancer development and resulting in strong anti-cancer effects in vitro and in vivo. In this review, we introduce the mechanisms of ferroptosis, summarize the research on ARTEs-induced ferroptosis in cancer cells, and discuss the clinical research progress and current challenges of ARTEs in anti-cancer treatment. This review deepens the current understanding of the relationship between ARTEs and ferroptosis and provides a theoretical basis for the clinical anti-cancer application of ARTEs in the future. [ABSTRACT FROM AUTHOR]

The goal of this work was to develop a physiologically-based pharmacokinetic (PBPK) modeling framework for cisplatin. The model was constructed based on 11 published data sets from rodents; and rabbit, dog, and human data were used to evaluate its utility in predicting plasma and tissue distribution of platinum in larger species, including humans. The model included biotransformation of cisplatin into mobile (k 1) and fixed (k 2) metabolites in all tissues, and subsequent conversion of fixed metabolites to mobile metabolites (k 3) due to protein degradation and turnover. The model successfully captured complex pharmacokinetics of platinum in rodents, and all parameters were estimated with sufficient precision. A separate k 2 parameter was estimated for each included tissue, and the relationship between the rates of formation of mobile and fixed metabolites was established through a scaling factor (k 1 = k 2 · S F , SF=0.74). For interspecies predictions, k 1 and k 2 were shared across all species, and k 3 was scaled allometrically based on protein turnover rate (with an exponent of -0.28). Scaled PBPK model provided a good prediction of total platinum profiles in humans and reasonably captured platinum measurements in human tissues (as obtained from autopsy). [Display omitted] [ABSTRACT FROM AUTHOR]

The rapid emergence of multidrug-resistant pathogens worldwide has raised concerns regarding the effectiveness of conventional antibiotics. This can be observed in ESKAPE pathogens, among others, whose multiple resistance mechanisms have led to a reduction in effective treatment options. Innovative strategies aimed at mitigating the incidence of antibiotic-resistant pathogens encompass the potential use of biosurfactants. These surface-active agents comprise a group of unique amphiphilic molecules of microbial origin that are capable of interacting with the lipidic components of microorganisms. Biosurfactant interactions with different surfaces can affect their hydrophobic properties and as a result, their ability to alter microorganisms' adhesion abilities and consequent biofilm formation. Unlike synthetic surfactants, biosurfactants present low toxicity and high biodegradability and remain stable under temperature and pH extremes, making them potentially suitable for targeted use in medical and pharmaceutical applications. This review discusses the development of biosurfactants in biomedical and therapeutic uses as antimicrobial and antibiofilm agents, in addition to considering the potential synergistic effect of biosurfactants in combination with antibiotics. Furthermore, the anti-cancer and anti-viral potential of biosurfactants in relation to COVID-19 is also discussed. [ABSTRACT FROM AUTHOR]

Hippomarathrum scabrum L. is an endemic medicinal plant in Turkey; however, there have been few studies investigating the phytochemistry and biological properties of these plants has not been investigated. The aim of this work is to determine the chemical composition of different extracts (extracts obtained by using supercritical carbon dioxide extraction, accelerated solvent extraction, homogenizer‐assisted extraction, microwave‐assisted extraction, and ultrasound‐assisted extraction from Hippomarathrum scabrum L., and evaluate their biological properties. The analysis revealed that 5‐O‐caffeoylquinic acid, rutin, and isorhamnetin 3‐O‐rutinoside were the main bioactive compounds. The extract obtained by accelerated extraction contains the highest concentration of 5‐O‐Caffeoylquinic acid (7616.74 ± 63.09 mg/kg dry extract) followed by the extract obtained by homogenizer‐assisted extraction (6682.53 ± 13.04 mg/kg dry extract). In antioxidant tests, all extracts expressed significant antioxidant activity. Also, cytotoxic and anticancer effects of these plant extracts were detected in the human prostate cancer cell line. Intrinsic apoptotic genes were up‐regulated and anti‐apoptotic genes were down‐regulated in human prostate cancer cells after inhibition concentration dose treatment. The findings are promising, and suggest the use of these plant extracts could be used as natural sources with different biological activities, as well as anticancer agents. [ABSTRACT FROM AUTHOR]

Carotenoids are naturally occurring compounds that are abundant and possess synergistic properties, contributing to their potential health benefits. This review provides an analysis of synergistic relationships among carotenoid compounds. The concept of synergy is of utmost importance due to the ongoing emphasis on consumer safety issues related to botanical natural products. To date, there is a lack of scientific reports specifically investigating the experimental evidence of synergistic effects associated with carotenoids. The carotenoid compounds purported to exhibit synergistic actions have demonstrated significant efficacy in combating oxidation, neurological diseases, peptic ulcers, tumors, and various other ailments. Furthermore, there have been reports of cancer prevention through apoptosis and the presence of antimicrobial, anti-inflammatory, and estrogenic properties. In addition to the observed combined benefits of carotenoids, this review elucidates the various health advantages associated with carotenoids. Among carotenoids, a substantial amount of data has been reported concerning lycopene. This review also examined the clinical status of the concurrent utilization of carotenoids with other bioactive molecules. As mentioned above, the findings offer valuable insights into the potential advantages of carotenoid compounds when combined, thereby presenting a promising avenue for further investigation in future research activities. • This review highlighted the synergistic effects of dietary carotenoids. • A substantial quantity of preclinical report regarding carotenoid synergism are displayed. • The dose quantity and amount are reduced when used in combination. • Focused on clinical status regarding the synergistic effect of dietary carotenoids. [ABSTRACT FROM AUTHOR]

Nanoparticles of Zinc oxide (ZnONPs), has a variety of applications such as antibacterial property, water treatment for pollutant removal, and as catalysts for organic reactions etc. and have been synthesized utilizing a variety of approaches, including green synthesis, chemical precipitation, sol-gel, hydrothermal synthesis, and microwave-assisted synthesis. In the present work, easy and economically viable ZnONPs were synthesized utilizing Strobilanthes hamiltoniana (SH) leaf extracts. Phytochemicals form S. hamiltoniana act as agents for reducing and capping the metal oxide ions. A range of analytical and microscopic techniques have been used to investigate the physical and chemical properties of ZnONPs. At 360 nm, green synthesized SH-ZnONPs showed robust UV-Vis absorption. The nanosize, shape, and crystalline structure of SH-ZnO NPs were characterized using XRD and electron microscopy techniques. Using SH-ZnO NPs, the photocatalytic activity of textile dyes such as Reactive blue 220 (RB-220), Reactive blue 222A (RB-222A), Reactive yellow 145 (RY-145) and Reactive yellow 86 (RY-86) dyes showed degradation efficiency of 97.3%, 78.57%, 88.88%, and 83.33% after 320 min. ZnONPs exhibited remarkable antibacterial effectiveness against bacterial and fungal pathogens using the Minimum inhibitory concentration approach. Their MIC values were calculated, and free radical scavenging experiments showed antioxidant activity. The SH-ZnONPs were validated using HepG2 (IC50) cancerous cells lines and showed promising anti-cancer activity. These results revealed that SH-ZnO NPs had promising benefits that could be utilized as a viable therapeutic candidate. [ABSTRACT FROM AUTHOR]

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Plant-derived bioactive compounds displayed major therapeutic and chemo-preventive roles in the pathogenesis of numerous chronic malignancies such as cancer and enhanced oxidative stress and inflammation. Antioxidants found in food, such as genkwanin, may reduce oxidative stress and the release of cytokines or pathways that promote inflammation. The goal of this work is to summarize the potential for anticancer effects of genkwanin, a methoxyflavone that is present in a variety of plant species. This review examined and analyzed numerous research studies on identifying, isolating, measuring, and analyzing anticancer properties of genkwanin. The mechanisms involved cellular and molecular activities at various levels, including apoptosis induction and cancer cell growth and proliferation inhibition. Preclinical studies have demonstrated genkwanin’s effects and mechanism of action; however, further research is required to investigate its therapeutic potential thoroughly. Additional research is needed to further our understanding of the pharmacodynamic effects of genkwanin. Additional toxicological study is necessary to evaluate the clinical efficacy and safety of genkwanin, which would help scientists to elucidate a potent drug candidate for cancer management. [ABSTRACT FROM AUTHOR]

Breast cancer remains a leading cause of mortality among women, necessitating heightened attention and innovative treatment approaches. Given the heterogeneous nature of breast cancer, exploring novel therapeutic avenues is crucial. Natural products, with their potential to offer less aggressive alternatives to conventional chemotherapy, have garnered interest. In this study, the potential cytotoxic effect of Feijoa sellowiana fruit extract (FE) was investigated on a panel of human breast cancer cells. GC-MS analysis was performed to identify the active constituents present in the FE extract and MTT analysis was conducted to evaluate the cytotoxicity of FE against breast cancer cells. Results showed a strong efficacy of FE against MDA-MB-453 and MDA-MB-231 cell lines. The cytotoxicity was evident after a 24-hour treatment duration for both lines. It was observed that the two cell lines in which the FE extract was most effective belonged to the triple-negative breast cancer category. The viability of MCF-7 cells decreased to 23.2% after 72 hours of exposure to 1000 µg/mL FE, and this decline was also noticeable at lower concentrations. Conversely, the BT-474 cell line displayed the least susceptibility, with a viability of 43.9% even at the highest concentration of 1000 µg/mL FE. These findings underscore FE's targeted efficacy against triple-negative breast cancer cells, indicating its promise as an alternative avenue to tackle this formidable cancer subtype. [ABSTRACT FROM AUTHOR]

Copyright of Revista Colombiana de Investigaciones Agroindustriales is the property of Revista Colombiana de Investigaciones Agroindustriales del Centro Agropecuario Sena Buga and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The study of the efficacy of Acmella oleracea (L.) flowers on breast cancer is still in its early stages. The molecular interaction mechanisms underlying Acmella oleracea's anti-breast cancer activity will be elucidated using in-silico analysis. For this study, seventeen bioactive compounds were used: spilanthol, alpha-and beta-amyrin ester, stigmasterol, beta-sitosterol, alpha-1-sitosterol, 3-acetylaleuritic acid, scopoletin, vanillic acid, trans-ferulic, (72,9E)-2-oxoundeca- 7,9-dienyl 3-methylbut-2-enoate, beta-caryophyllene, beta-pinene, myrcene, caryophyllene oxide, and limone Canonical smiles were obtained from PubChem and inserted into the PASS server to determine biological activity. Several compounds were docked with protein targets, such as ESR1, MAP2K2, and PGR. We used Pyrx 0.8 software for anchoring molecular interaction and Discovery Studio software to visualize the complex binding. In terms of Antineoplastic, apoptosis agonist, caspase-3, caspase-8 stimulant, ovulation inhibitor, steroid synthesis inhibitor, and TP53 expression enhancer, all the compounds tested positive for anticancer activity. According to Swiss ADME and protox analysis, Acmella oleracea flowers have the potential to modulate apoptosis and cell growth. More research is required to confirm the role of Acmella oleracea bioactive compounds in developing target cancers. The study reveals that Acmella oleracea has numerous bioactive chemicals advantageous for cancer therapy by inducing apoptosis through interaction with ESR1, MAPK2, and PGR protein. [ABSTRACT FROM AUTHOR]

Palladium nanoparticles (PdNPs) have gained significant importance due to its prodigious properties and applications. To harness the multifaceted applications of PdNPs, we report a facile synthesis of calix[4]pyrrole tetrabenzohydrazide capped-Palladium nanoparticles (CPTBH-PdNPs) through a one-pot synthetic pathway. Comprehensive characterization using UV–Visible spectroscopy, Transmission Electron Microscopy (TEM), Selected Area Electron Diffraction (SAED), Energy-Dispersive X-ray, X-ray Diffraction, Zeta Potential, and Dynamic Light Scattering techniques confirmed the successful formation of CPTBH-PdNPs. These nanoparticles were employed as catalysts in Suzuki–Miyaura coupling reactions under mild conditions, resulting in efficient bond formations. Furthermore, the CPTBH-PdNPs exhibited remarkable anti-cancer effects against the human breast cancer cell line MDA-MB-231, with an IC50 value of 38.86 µg/mL. Additionally, the nanoparticles demonstrated exceptional efficacy against Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) value of 0.8 µg/mL. These findings highlight the multidimensional nature of calix[4]pyrrole capped PdNPs and suggest their potential application as future materials in various fields. [ABSTRACT FROM AUTHOR]

Several studies have shown that metallic nanoparticles have a therapeutic impact on leukemia cells. On the other hand, the majority of these particles are hazardous to healthy and malignant cells. SrFeO3 nanoparticles were synthesized in the current study using sol–gel procedures. Several analytical methods, including scanning electron microscopy (SEM), transmission electron microscopy (TEM), energy dispersive spectroscopy (EDS), X-ray diffraction (XRD), and dynamic light scattering (DLS), were used to characterize the resulting nanoparticles. The considered particle size utilizing XRD was discovered to be in the range of 50 ± 2 nm, which was further confirmed by DLS analysis. The Nalm-6 (ALL) and the K562 (CML) cell lines and PBMCs (Normal cells) were treated with 25, 50, 100, 150, and 200 µg/ml of strontium nanoparticles for 24 and 48 h. Afterward, the cell viability and cell death were evaluated via MTT assays and flow cytometry analysis. The strontium nanoparticles with concentrations above 150 μg/mL could cause a cytotoxic effect on the Nalm-6 and K562 leukemic cells. Strontium nanoparticles exhibited no harmful impact on healthy PBMCs, even though the flow cytometry examination revealed that apoptosis is the primary process of leukemic cell death. Thus, SrFeO3 nanoparticles show potential for application in future anti-leukemic therapies and pave the way to a new study setting. Highlights: Strontium ferrate nanoparticles suppressed the growth of leukemia cell lines. Strontium ferrate nanoparticles were nontoxic to normal PBMC cells. Strontium ferrate nanoparticles increased apoptosis in leukemia cells. [ABSTRACT FROM AUTHOR]

The green synthesis of metal oxide nanoparticles (NPs) has garnered considerable attention from researchers due to its utilization of eco-friendly solvents during synthesis and cost-effective approaches. This study focuses on the synthesis of titanium oxide (TiO2) and dopamine (DA) carboxymethyl cellulose (CMC)-doped TiO2 (DA/CMC/TiO2) NP using Psidium guajava leaf extract, while also investigating the structural, optical, and morphological and biocidal potential of the prepared NPs. Significantly larger zones of inhibition were observed for DA/CMC/TiO2 NPs compared to TiO2 against various pathogens. Moreover, the MTT assay was carried out to evaluate the anticancer activity of the prepared samples against MG-63 cells, and the results revealed that DA/CMC/TiO2 NPs exhibited significantly higher level of anticancer activity compared to TiO2. The experimental results demonstrated that DA/CMC/TiO2 NPs exhibited enhanced anticancer activity in a dose-dependent manner when compared to TiO2 NPs. [ABSTRACT FROM AUTHOR]

An aurone derivative HJ-1, was isolated from Coreopsis tinctoria in our previous work, showed potential anti-hepatocellular carcinoma activity. From it, seventy-five compounds were synthesized via bioisostere and scaffold hopping strategy, and then submitted to the inhibitory activities evaluation against four tumor cells (HELA, HT-29, A549 and HepG2) through MTT assays. These activities have been discussed in SAR. Based on the results, compounds, thirty compounds showed moderate to good antitumour activity. Among them, five compounds (A3: 3.41 ± 1.03 μM, E3: 5.11 ± 0.23 μM, E8: 4.14 ± 1.21 μM, F2: 5.40 ± 1.18 μM, F4: 7.37 ± 0.87 μM) had achieved a comparable efficiency to the positive control DOX (Doxorubicin) against HT-29 cell lines, Compound A3 and F4 were identified as potential leading compounds. [ABSTRACT FROM AUTHOR]

Camels play an important role in the pastoral mode of life by fulfilling basic demands of livelihood. Various pathologies, such as tuberculosis, hemorrhoids, ascites, increased size of the abdomen, gas colic, anemia, and abdominal tumors, were treated with animal urine, including camels, horses, donkeys, sheep, goats, elephants, and buffalo. Thirty different compounds were analyzed in camel urine by gas chromatography and mass spectrometry. For inductively coupled plasma mass spectrometry analysis, 28 important elements were analyzed in the urine of both camel and bovine. It was found that the inorganic elements are almost similar, except sodium, potassium, iron, zinc, and magnesium are higher in levels in camel urine, while chromium is high in bovine urine. Camel urine also contains different nanoparticles, crystals, and nano-rods with varying shapes and sizes, which offer potent selective cytotoxic activity against several lines of cancer cells. It is believed that the camel's urine has a therapeutic effect for a wide range of diseases such as chill, fever, or even tumors; therefore, it has been consumed in the Arabian Peninsula for a long time. Usually, patients take it directly or by mixing a few drops with camel milk. Camel urine is also used for therapeutic purposes, most widely in Asia, Africa, the United States, the United Kingdom, and other European countries. The religious aspect of using camel urine in treatment comes from the fact that there has been convincing evidence that the Prophet Mohammad (PBUH) suggested the use of camel urine to treat his companions who were suffering from abdominal pains at that time. The camel's urine has anti-diabetic, anti-cancer, antibacterial, antiviral, and antifungal properties. It also has hepato-protective and cardiovascular effects. [ABSTRACT FROM AUTHOR]

Background: Skin cancer is becoming a public health concern due to increased exposure to environmental pollutants and UV rays, among other factors. In India, skin neoplasms constitute 2–3% of all human cancer cases, whereas in the USA, 2–3 million cases of non-melanoma skin cancer are reported annually. Various drugs are available in the market for treating skin cancer. Imiquimod (IMQ) is one such drug approved by the USFDA for managing basal cell malignancy, external genital warts, and actinic keratosis. The conventional dosage form of IMQ cream has several side effects that can lead to therapy interruption. Therefore, the present work aims to develop an IMQ nanoemulsion with improved solubility, in vitro drug release and stability. Nanoemulsion was formulated using oleic acid/rose oil, with polysorbate 20/propylene glycol selected as the oil phase and Smix, respectively. Optimization carried out using a 32 factorial design with the aid of a quadratic model. Characterization was conducted for parameters, namely viscosity, pH, drug content, globule size, zeta potential and entrapment efficiency. Thermodynamic stability studies were conducted to assess the stability of the formulation. Furthermore, the optimized system was subjected to TEM analysis, in vitro drug release and in vitro cytotoxicity assay (MTT assay). Results: Nanoemulsions were found to be in the size range of 152.80–470.13 nm and exhibited a spherical shape. Zeta potential values ranged from − 28.93 to − 58.48 mV. DSC measurements indicated the complete solubilization of IMQ in the nanoemulsion system. The optimized formulation F1 displayed the following characteristics: a globule size < 200 nm, a zeta potential > − 55 mV, a polydispersity index < 0.2, % drug content of 102.89 ± 1.06, % entrapment efficiency of 97.59 ± 0.24, a pH of 4.77 ± 0.06, and a viscosity of 4.06 ± 0.06 poise. In vitro IMQ release studies of nanoemulsion and commercial cream showed approximately 70% and 34% drug release, respectively, at the end of 8 h. Moreover, the in vitro cytotoxicity assay depicted that F1 exhibited greater cytotoxic potential compared to the commercial formulation against the A431 cell line. Conclusion: The present investigation showed a significant improvement in in vitro drug release of the BCS class IV drug IMQ and enhanced cytotoxic activity against cancerous cells. IMQ-loaded nanoemulsion represents a promising vehicle for delivering treatment to the skin for treating skin cancer. [ABSTRACT FROM AUTHOR]

Brazilian Amazon contains over 30,000 plant species and foods rich in bioactive compounds such as terpenes, phenolic acids, alkaloids, and flavonoids, of potential health benefits (antioxidant, antimicrobial, antiparasitic, anticancer, gastroprotection, prebiotic effects, among others). The existence of residues from non-edible parts of plants (leaves, roots, stems, branches, barks) or fruit wastes (peel, bagasse, seeds) in the agri-food industry and its supply chain is an important challenge in food loss and waste management. In this critical review several Amazon species, focusing on extracts/essential oils from nonedible parts or wastes, were analyzed in terms of phytochemicals, biological activity, and underlying mechanisms. We hope this review emphasizes the importance of Amazon's sustainability initiatives on population health due to the potential shown against cancer, infectious diseases, and prevention of oral diseases. It is urgent to think about the conversion of amazon food wastes and co-products into high-added-value raw materials to develop novel drugs, food packaging systems, or nutraceutical foods. [ABSTRACT FROM AUTHOR]

Colorectal neoplasms are one of the deadliest diseases among all cancers worldwide. Thymoquinone (TQ) is a natural compound of Nigella sativa that has been used in traditional medicine against a variety of acute/chronic diseases such as asthma, bronchitis, rheumatism, headache, back pain, anorexia, amenorrhea, paralysis, inflammation, mental disability, eczema, obesity, infections, depression, dysentery, hypertension, gastrointestinal, cardiovascular, hepatic, and renal disorders. This review aims to present a detailed report on the studies conducted on the anti-cancer properties of TQ against colorectal cancer, both in vitro and in vivo. TQ stands as a promising natural therapeutic agent that can enhance the efficacy of existing cancer treatments while minimizing the associated adverse effects. The combination of TQ with other anti-neoplastic agents promoted the efficacy of existing cancer treatments. Further research is needed to acquire a more comprehensive understanding of its exact molecular targets and pathways and maximize its clinical usefulness. These investigations may potentially aid in the development of novel techniques to combat drug resistance and surmount the obstacles presented by chemotherapy and radiotherapy. [ABSTRACT FROM AUTHOR]

We conducted a study to create new chemical compounds using indole derivatives, specifically incorporating thiosemicarbazone (8 a–e) and 4‐thiozolidinone‐5‐carboxylic acid (9 a–e) structures. We then tested these compounds against various bacteria and cancer cells. In our antibacterial tests, the compounds showed moderate inhibitory effects on bacterial growth. However, when we examined their effects on cancer cells, we observed specific patterns of activity. Notably, compounds 9 c and 9 d were highly toxic to NCI‐H187 cancer cells, while compounds 8 c, 9 b, 9 c, 9 d, and 9 e exhibited moderate inhibitory activity against KB cancer cells. Compound 8 e displayed strong toxicity against MCF‐7 cancer cells. When we assessed the toxicity of these compounds on normal Vero cells, we found that compounds 8 e, 9 b, 9 c, 9 d, and 9 e were less toxic compared to ellipticine, a known anticancer drug. These results suggest that these newly synthesized compounds may have potential applications in cancer treatment, and further research is necessary to explore their therapeutic possibilities. [ABSTRACT FROM AUTHOR]

As potential intravesical exfoliants for the treatment of bladder cancer, four new imdiazolium salts have been prepared. These compounds are modified on the nitrogen positions of the 4,5‐diphenyl‐1H‐imidazole or benzimidazole rings with naphthalen‐2‐ylmethyl groups, and the 2 positions on the azolium cations are occupied by arene rings. The 4,5‐diphenyl‐1H‐imidazole and benzimidazole precursors are produced from 1,2‐phenylenediamine and benzil respectively, and the imidazolium cations are generated from sequential alkylation of the nitrogen positions using 2‐bromomethyl naphthalene. The four imidazolium salts were screened for their chemotherapuetic activity using the NCI‐60 Human Tumour Cell Line Screen, and we observed that the cytotoxicity was more dependent on the identity of the imidazolium group (benzimidazolium versus diphenylimidazolium) rather than on the 2‐aryl position structure. [ABSTRACT FROM AUTHOR]

Novel 1‐(ethyl/methyl)‐7‐(p‐methoxybenzyl amino) and 7‐amino‐6‐fluoroquinolone‐boron difluoride complexes were synthesized, and their biological activity was studied, comparing the influence of the nature of 7‐substituent as well as N‐1 substituent. The quinolone compounds were characterized by IR, UV‐Vis, 1H, 13C{1H} and 19F{1H} NMR, and mass spectrometry. The antiproliferative effect of the new fluoroquinolone‐boron complexes in breast cancer (BC) derived cell lines MCF‐7 and SKBR‐3 was investigated. Compounds 9 b and 9 a showed antiproliferative in MCF‐7 cells, and 9 b, 11 b, 9 a, 7 a, 7b and 8 a showed similar effects in SKBR‐3 cells. Derivatives with p‐methoxybenzyl amino moieties at C‐7 and an ethyl or methyl group at N‐1 in the fluoroquinolone ring (9 a and 9 b) were the more efficient in both breast cancer cell lines. In addition, an 8‐nitro group to the fluoroquinolone (11 b) improved activity against SKBR‐3 cell proliferation. These compounds represent potential drug candidates for breast cancer treatment. [ABSTRACT FROM AUTHOR]

In this study, antimicrobial, anticarcinogenic and antiparasitic effects of pomegranate (Punica granatum L.) peel were investigated. Peels were separated from pomegranate fruit obtained in season from local markets and markets in Istanbul, Beykoz, and phenolic components were determined by extracting them at 33% ethanol, 78°C and 5 hours operating conditions. It was determined that punigagalagin, caffeic acid, epicatechin and Catechin were the highest in phenolic contents. The obtained extract showed antimicrobial effect against selected microorganisms. In addition, the in vitro anticarcinogenic activity of the extract was determined in breast cancer, gastric cancer and lung cancer cell lines. Finally, the antiparasitic activity of pomegranate peel extract was determined in L. major and L. infantum parasites promostigots and amostigotes, which are cutaneous and visceral leishmaniasis agents. It has been concluded that pomegranate peel extract will be used not only in the food industry but also in non-food applications due to its medicinal properties. [ABSTRACT FROM AUTHOR]

Antioxidant capacity, cytotoxicity on two vital cell lines and the anti-cancer activity of methanolic Urtica dioica L. leaf extract (UDE) collected from Duzkoy, Giresun, Turkey were studied by determining safe concentration. The antioxidant capacity of the extract was expressed as vitamin C equivalency by spectrophotometric MTT assay. The cytotoxic concentration 50% was measured by the linearity between UDE concentrations (CC50) and the cell viability of non-cancer kidney cell lines (BHK-21, MDBK). The anti-cancer activity was conducted on human hepatocellular carcinoma cells (HepG2) by determining inhibition concentration (IC50) on cell proliferation. The vitamin C equivalence of UDE increased linearly by increasing the concentration. The cytotoxic and non-toxic concentrations of UDE were determined on BHK-21 and MDBK with 15.71 mg/ml and 5.14 mg/ml of CC50 respectively. The extract inhibited the proliferation of human hepatocellular carcinoma cells with a 2.46 mg/ml of IC50. In conclusion, the present study tried to explain in detail the dose-dependent activity of Urtica dioica L. leaf extract. The dose-response results showed that Urtica dioica L. leaf extract could have low cytotoxicity, but potential anti-cancer activity at safe concentrations. [ABSTRACT FROM AUTHOR]

Purpose: Tissue-specific drug uptake has not been well studied, compared to the deeper understanding of drug resistance mediated by the cellular efflux system such as MDR1 proteins. It has been suggested that many drugs need active or defined transporters to pass the cell membrane. In contrast to efflux components induced after anti-cancer drugs reach the intracellular compartment, drug importers are required for initial drug responses. Furthermore, tissue-specific uptake of anti-cancer drugs may directly impact the side effects of many drugs when they accumulate in healthy tissues. Therefore, linking anti-cancer drugs to their respective drug import transporters would directly help to predict drug responses, whilst minimizing side effects. Methods: To identify drug transporters of the commonly used anti-cancer drug doxorubicin, we performed focused CRISPR activation and knockout genetic screens targeting all potential membrane-associated transporters and proteins. We monitored the direct uptake of doxorubicin by fluorescence-activated cell sorting (FACS) as the screening readout for identifying transporters/proteins directly involved in doxorubicin uptake. Results: Integrating the data from these comprehensive CRISPR screenings, we confirmed previously indicated doxorubicin exporters such as ABCB1 and ABCG2 genes, and identified novel doxorubicin importer gene SLC2A3 (GLUT3). Upregulation of SLC2A3 led to higher doxorubicin uptake and better cell killing, indicating SLC2A3 could be a new marker to predict doxorubicin drug response and minimize side effects for the personalized application of this conventional chemotherapeutic drug. Conclusions: Our study provides a comprehensive way for identifying drug transporters, as exemplified by the commonly used anti-cancer drug doxorubicin. The newly identified importers may have direct clinical implications for the personalized application of doxorubicin in treating distinct tumors. Our results also highlight the necessity of combining both CRISPR knockout and CRISPR activation genetic screens to identify drug transporters. [ABSTRACT FROM AUTHOR]

Objectives: Prostate cancer (PCa) is a significant health problem in men worldwide. Although there are numerous treatment choices for PCa, acquired resistance limits treatment success. Therefore, there is a need for new approaches as powerful resources for use in alternative or supportive therapeutic strategies for anticancer therapeutics. Theranekron® is a commercially available alcoholic extract of Tarantula cubensis. Recent studies have shown the potent anticancer effect of theranekron in human tumors, including PCa. Herein, we comparatively examined the antiproliferative activity of theranekron and its biochemical action on androgenic signaling and cell cycle-related cyclin proteins in androgendependent PCa cells, LNCaP, VCaP, and 22Rv1. Materials and Methods: Human androgen-dependent PCa cells, LNCaP (CRL-1740TM), 22Rv1 (CRL-2505TM), and VCaP (CRL-2876TM) were used to evaluate the effect of theranekron in vitro. The impact of theranekron on cell viability was evaluated using a WST-1-based viability test. Its impact on AR, cyclin A2, cyclin B1, and cyclin E1 was examined by immunoblotting. To test the anti-malignant effect of theranekron on 3D tumor formation of PCa cells, soft agar assay was used. Results: Our results indicated that theranekron treatment significantly reduced the viability of PCa cells. It remarkably decreased the protein levels of AR, cyclin A2, cyclin B1, and cyclin E1 in a dose-dependent manner. In addition, Theranekron administration strongly limited the 3D tumor formation of LNCaP, 22Rv1, and VCaP cells. Conclusion: Our findings strongly suggest that theranekron may offer potent therapeutic efficacy against androgen-dependent PCa cells. Moreover, it may be a potent component for preventing acquired resistance to chemotherapeutics. [ABSTRACT FROM AUTHOR]

Cancer, the biggest cause of death globally, remains a tough illness despite enormous advances in therapy. In the present study, 1,3-benzodioxole-tagged dacarbazine derivates were investigated as microtubule inhibitors in order to control cancer as microtubules are involved in cell proliferation. The tubulin protein was analyzed and its structure was validated by various protein validation tools. The binding potential of 1,3-benzodioxole-based dacarbazine-tagged derivatives with tubulin was checked using molecular docking software HEX 8.0 CUDA and AutoDock Vina. Swiss ADME online Web server and pkCSM are used for studying pharmacokinetic and pharmacological studies of compounds. The docking analysis ADME studies displayed that Compounds 1 and 2 bind effectively with the tubulin protein and showed potential properties to use as a potent anticancer drug. [ABSTRACT FROM AUTHOR]

The relevance of medicinal plants as a primary source of therapeutic agents in the modern world cannot be overemphasized. Anogeissus leiocarpus (A. leiocarpus), of the family Combretaceae, is a renowned medicinal plant used in folkloric medicine for the management of various illnesses, particularly in developing countries. In African traditional medicine, the edible stem bark used as a chewing stick reportedly possesses numerous biological activities. Stem bark extract from A. leiocarpus exhibits anti-parasitic, antihypertensive, and anti-tubercular effects. Additionally, A. leiocarpus bark extract is used in traditional medicine in Sudan to alleviate cough and in Ivory Coast to treat parasitic diseases. The plant reportedly possesses other medicinal properties, including anti-diabetic, antiinflammatory, anti-malarial, and anti-cancer activities due to the presence of important phytochemicals, such as phenols, flavonoids, saponins, and alkaloids. Compounds including, serinic acid, arjungenin, isoquercetin, vitexin, kaempferol and some others have been identified as bioactives from various parts of the plant. [ABSTRACT FROM AUTHOR]

Background: The saliva and salivary glands of ticks possess a wide range of immuno-pharmacologically active molecules that effectively modulate the activity of enzymes, antibodies, and amines that have a role in different biological processes. Derived components from saliva and salivary glands of hard ticks Ixodidae have been characterized as potential natural sources for discovering promising anti-cancer drug candidates. Methods: The anti-cancer activity of salivary gland extracts (SGEs) from Hyalomma anatolicum, Hyalomma dromedarii, Hyalomma marginatum, and Hyalomma schulzei was assessed. MTT assays and flow cytometry were done on the HT-29 colorectal cancer cell line to evaluate the anti-viability and proliferative inhibition. Results: Based on the MTT assay results, the SGEs from Hy. dromedarii had the highest and lowest substantial antiviability effects on the HT-29 cancer cell and human foreskin fibroblast (HFF) normal cell, respectively. The cytometric assessment revealed a significant increase in the apoptosis and necrosis ratio of the HT-29 cancer cells after treatment with Hy. dromedarii SGEs. Conclusion: The results demonstrated that Hy. dromedarii SGEs have significant anti-proliferative, anti-viability, and apoptotic potential. The result of this study suggests that Hy. dromedarii SGEs is an appropriate candidate for further investigations to identify and purify the mechanisms and molecules involved in the anti-cancer activity of the SGEs. [ABSTRACT FROM AUTHOR]