Search

Tragopogon coelesyriacus is a pharmacotherapeutic herbaceous plant belonging to the Asteraceae family and consumed as a vegetable. Here, the methanolic and water extracts of T. coelesyriacus were obtained from its aboveground parts (stem, leaves, and flowers), and the phytochemical potentials were investigated by LC‐HRMS (liquid chromatography–high resolution mass spectrometry) analysis for the first time. The antibacterial, antifungal, and anticarcinogenic activities of T. coelesyriacus extracts were investigated using experimental and in silico methods. T. coelesyriacus methanol extract revealed remarkable inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumonia (MICs = 0.83, 1.67, and 1.67 mg/mL, respectively) compared to Escherichia coli and Enterobacter aerogenes (MIC = 53.3 mg/mL). Inhibitory effects of T. coelesyriacus methanolic extracts were also observed in all Candida species tested, with the highest inhibition on Candida krusei (MIC = 0.83 mg/mL), whereas no inhibitory effect was identified from the water extract. Additionally, both T. coelesyriacus methanolic (IC50 = 86 μg/mL) and water (IC50 = 92 μg/mL) extracts revealed significant selective anticarcinogenic effects on AR42J pancreatic cancer cells. HeLa and MDA‐MB‐231 cells were, however, more resilient to methanol and water extract, respectively. In silico analyses further elucidated the noteworthy antibacterial potential of keracyanin chloride on S. aureus MurB enzyme and the remarkable inhibitory potential of naringin on FYN kinase specific for pancreatic cancer (AR42J) development. In conclusion, T. coelesyriacus phytochemicals with antibacterial, antifungal, and anticancer properties were revealed for the first time, and molecular docking studies on potential targets confirmed good agreement with experimental findings. Therefore, the current studies on T. coelesyriacus provide the basis for investigating new pharmaceutical potentials of other Tragopogon members. [ABSTRACT FROM AUTHOR]

Background: Mammary gland carcinoma is a malignant type of cancer that occurs in mammae tissue. Dimethylbenzene (α) anthracene (DMBA) is a carcinogenic agent that causes mammary cancer by damaging cellular DNA. Flavonoids found in the black soybean (Glycine max L. Merr) exhibit anti-carcinogenic effects. Aim: This study evaluated the anticarcinogenic effects of black soybean extract. Methods: The activity of flavonoid compounds in black soybean was determined in silico. Five groups of rats, four in each group, were established, consisting of a negative control, a positive control, and three treatment groups. Treatment included black soybean extract administration (i.e., T1 = 200, T2 = 400, and T3 = 800 mg of black soybean extract/kg body weight for 10 days). The observed parameters included the immunohistochemical analysis of Breast Cancer 1(BRCA1) and TNF-α. Results: Based on an in silico study, compounds from black soybeans are non-toxic. Functional annotation analysis revealed that most of the target proteins have a role in biological processes associated with cancer development. An in vivo analysis using an animal mammae cancer model indicated that black soybean extracts inhibited mammae cancer progression by attenuating TNF-α and BRCA1 expression. Conclusion: The most effective dosage of black soybean extract was 200 mg/kg body weight. An increase in BRCA1 and TNF-α expression may be related to the effects of catechin, daidzein, genistein, and glycitein, which are present in black soybeans. [ABSTRACT FROM AUTHOR]

A facile and cost-effective sol–gel technique has been used to synthesize nickel chromite (NiCr2O4) nanoparticles (NCNPs) at 7 0 0 ∘ C to investigate their photocatalytic together with antibacterial and anticancer activities. The synthesized nanopowder was characterized by Thermogravimetric thermal analysis (TG-DTA), X-ray Diffraction Spectroscopy (XRD), Field Emission Scanning Electron Microscopy (FE-SEM), High-Resolution Transmission Electron Microscopy (HR-TEM), Fourier Transform-Infrared Spectroscopy (FT-IR), X-ray Photon Electroscopy (XPS) and UV–Visible Diffuse Reflectance Spectroscopy (UV-DRS) and Photoluminescence (PL). Beyond 7 0 0 ∘ C, the thermal durability of NCNPs was confirmed by TG-DTA analysis. The synthesized NPs were cubic structured corresponding to their spinel structure, a crystallite size of 38 nm and an optical bandgap of 2.7 eV. The PL spectra revealed emission bands in the visible and UV regions. The surface-phase-pure elemental and electronic arrangement of the NCNPs were verified by X-ray photon spectroscopy. Photocatalytic activity of NCNPs against Methylene Blue dye revealed 89% degradation in 1 h. The in vitro antibacterial and anticancer activities of NCNPs were also examined. Among the tested microbes, Staphylococcus aureus exhibited the highest level of sensitivity (9 mm), while Escherichia coli had the lowest (5 mm) against NCNPs. The MTT test revealed the significant cytotoxicity of NCNPs against carcinogenic HeLa and MCF-7 cells. Thus, the synthesized NCNPs could be rated as potential photocatalytic, bactericidal and anticarcinogenic agents. Spinel type NiCr2O4 nanoparticles (NCNPs) were successfully prepared, through a facile solgel auto-combustion route, to study their antibacterial and anticancer properties. After characterizations, it was found that the synthesized NCNPs were effective against selected microorganisms. S. aureus exhibited the highest level of sensitivity (9 mm), while E. coli had the lowest (5 mm). Moreover, the MTT test revealed the high cytotoxicity of NCNPs against HeLa and MCF-7 cell lines. These results lead us to the fact that NiCr2O4 NCNPs can be considered as candidates for bactericidal and anti-carcinogenic agents. [ABSTRACT FROM AUTHOR]

The role of estrogens in prostate cancer (PCa) is shrouded in mystery, with its actions going from angelic to devilish. The findings by Huggins and Hodges establishing PCa as a hormone-sensitive cancer have provided the basis for using estrogens in therapy. However, despite the clinical efficacy in suppressing tumor growth and the panoply of experimental evidence describing its anticarcinogenic effects, estrogens were abolished from PCa treatment because of the adverse secondary effects. Notwithstanding, research work over the years has continued investigating the effects of estrogens, reporting their pros and cons in prostate carcinogenesis. In contrast with the beneficial therapeutic effects, many reports have implicated estrogens in the disruption of prostate cell fate and tissue homeostasis. On the other hand, epidemiological data demonstrating the lower incidence of PCa in Eastern countries associated with a higher consumption of phytoestrogens support the beneficial role of estrogens in counteracting cancer development. Many studies have investigated the effects of phytoestrogens and the underlying mechanisms of action, which may contribute to developing safe estrogen-based anti-PCa therapies. This review compiles the existing data on the anti- and protumorigenic actions of estrogens and summarizes the anticancer effects of several phytoestrogens, highlighting their promising features in PCa treatment. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Health Sciences / Sağlık Bilimleri Dergisi is the property of Erciyes Universitesi Saglik Bilimleri Dergisi 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.)

Copyright of Gümüshane Üniversitesi Saglik Bilimleri Dergisi is the property of Gumushane University, Faculty of Health Sciences 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.)

4-O-Methyl-ascochlorin (MAC), a derivative of the prenyl–phenol antibiotic ascochlorin extracted from the fungus Ascochyta viciae, shows anticarcinogenic effects on various cancer cells. 5-Fluorouracil (5-FU) is used to treat colorectal cancer (CRC); however, its efficacy must be enhanced. In this study, we investigated the molecular mechanisms by which MAC acts synergistically with 5-FU to inhibit cell proliferation and induce apoptosis in CRC cells. MAC enhanced the cytotoxic effects of 5-FU by suppressing the Akt/mTOR/p70S6K and Wnt/β-catenin signaling pathways. It also reduced the viability of 5-FU-resistant (5-FU-R) cells. Furthermore, expression of anti-apoptosis-related proteins and cancer stem-like cell (CSC) markers by 5-FU-R cells decreased in response to MAC. Similar to MAC, the knockdown of CTNNB1 induced apoptosis and reduced expression of mRNA encoding CRC markers in 5-FU-R cells. In summary, these results suggest that MAC and other β-catenin modulators may be useful in overcoming the 5-FU resistance of CRC cells. [ABSTRACT FROM AUTHOR]

Silk sericin (SS), a protein biopolymer, is gaining an increasing attention in a variety of biomedical applications. Our objective was to identify the optimal extraction method yielding the highest silk protein content, to assess its chemical elemental composition, to characterize it, and to compare its conformation by X‐ray diffraction and Fourier‐transform infrared versus that of the commercial one. Herein, alkali and high temperature is the perfect approach. This study aimed further to test whether extracted SS could attenuate the adverse hepatotoxic effects induced by diethylnitrosamine (DEN) in mice. Animals were injected intraperitoneally once weekly for four consecutive weeks with physiological saline (0.9% NaCl), DEN (25 mg/kg), SS (1 g/kg) 90 min prior to DEN injection, melatonin (10 mg/kg) followed within 1 h with the administration of SS and 30 min later with DEN. The results confirmed the hepatotoxicity of DEN manifested by an increase in liver enzymes' activity, and pathological changes in the liver tissue. The combined use of SS and/or melatonin with DEN returned most of the parameters to values similar to the controls. Briefly, chemically characterized SS seems a valuable extract for further consideration as anti‐carcinogenic agent. It has the potential to upgrade liver cancer chemotherapeutic agents. [ABSTRACT FROM AUTHOR]

Arthrospira platensis is a cyanobacterium interesting for its high phycocyanin (C-PC; 10-20% w/w) and protein content (60-70% w/w). These components can be used as food/feed ingredients and additionally C-PC can be used for pharmaceutical applications due to its antioxidative, hepatoprotective and anti-carcinogenic properties. Current methods for C-PC extraction from A. platensis involve cell membrane lysis to release pigments in an aqueous extraction medium. Conventional cell lysis techniques, such as freeze-thawing and bead milling require long processing times and high energy inputs and result in release of other cell components, jeopardising the C-PC extract purity. Natural Deep Eutectic Solvents (NADES) represent an emerging metabolite extraction technology which offers bio-safety, high extraction efficiency, improved stability and specificity towards the desired target compound. The present work focused on C-PC extraction by emerging cell lysis (ultrasonication) and metabolite extraction with hydrophilic NaDES. [ABSTRACT FROM AUTHOR]

Forkhead box protein 1 (FOXP1) serves as a tumour promoter or suppressor depending on different cancers, but its effect in oesophageal squamous cell carcinoma has not been fully elucidated. This study investigated the role of FOXP1 in oesophageal squamous cell carcinoma through bioinformatics analysis and experimental verification. We determined through public databases that FOXP1 expresses low in oesophageal squamous cell carcinoma compared with normal tissues, while high expression of FOXP1 indicates a better prognosis. We identified potential target genes regulated by FOXP1, and explored the potential biological processes and signalling pathways involved in FOXP1 in oesophageal squamous cell carcinoma through GO and KEGG enrichment, gene co‐expression analysis, and protein interaction network construction. We also analysed the correlation between FOXP1 and tumour immune infiltration levels. We further validated the inhibitory effect of FOXP1 on the proliferation of oesophageal squamous cell carcinoma cells through CCK‐8, colony formation and subcutaneous tumour formation assays. This study revealed the anticarcinogenic effect of FOXP1 in oesophageal squamous cell carcinoma, which may serve as a novel biological target for the treatment of tumour. [ABSTRACT FROM AUTHOR]

In recent years, the development of antitumor drugs has been dedicated to natural products. Amygdalin is a natural herbal cyanoglycoside that has anticarcinogenic effect on many types of cancers once hydrogen cyanide (HCN) is released. The main objective of the present study is to synthesize and investigate the potential of carboxymethyl chitosan nanoparticles (CMC NPs) as drug delivery agents for amygdalin encapsulation and its delivery to cancer and normal cell lines. In this study, carboxymethyl chitosan nanoparticles encapsulated with amygdalin (CMC-Am NPs) were prepared and characterized through their particle size, surface charge, chemical structure and dielectric properties. Also, the invitro drug release of amygdalin from CMC NPs was studied. Additionally, the cytotoxcity of the amygdalin and CMC-loaded amygdalin NPs were evaluated through MTT assay. The results showed that the prepared CMC-loaded amygdalin NPs exhibited a small particle size of 129 nm, high zeta potential value of − 43 mV and confirmed the amygdalin stability and compatibility with CMC NPs. Furthermore, the CMC NPs demonstrated sustained release of amygdalin during 24 h. Moreover, compared to free amygdalin, amygdalin-loaded CMC NPs have significant anti-cancerous effect on human colon HCT-116 and breast MCF-7 cancer cell lines while being safe on normal cells BJ1. In conclusion, CMC NPs can be employed as an efficient drug delivery vehicle for controlled and sustained amygdalin release with enhanced cytotoxicity on malignant cells without harming normal cells. [ABSTRACT FROM AUTHOR]

Chrysin flavonoid has been presented as having numerous and promising bioactive effects, such as antioxidant, anticonvulsant, antihypertensive, anti-inflammatory, antineoplastic, antihyperlipidemic, and antidepressant. However, one of the main challenges for advances in studies on the bioactivity of chrysin is its low bioavailability in humans. Thus, aiming to overcome this barrier, several studies have demonstrated the bioactive potential of capsules containing chrysin. The objective of this review was to present the main methodologies used for the encapsulation of chrysin, and its main biological effects demonstrated so far. Our intention is to offer ways to advancement of research in the area of flavonoid encapsulation. As for the encapsulation techniques, it was found that they are diverse, and the most recurrent encapsulating agents were PEG, PLGA polymers and their derivatives, in addition to other agents, such as PCL, albumin, lipids and chitosan.The bioactive effects of the capsules are also numerous, and anticarcinogenic effects are the most frequent, in addition to other effects such as antioxidant, antidiabetic, antimicrobial and neuroprotective. In conclusion, we verified a lack of use of green techniques for the encapsulation of chrysin, and the production of lipid-water emulsions and the dissolution of chrysin in ethanol seems to be alternatives in this regard. In addition, bioactive potential of these capsules can be evaluated in other experimental models, and should advance to clinical trials and application in food formulations. [ABSTRACT FROM AUTHOR]

Emerging research supports that triclosan (TCS), an antimicrobial agent found in thousands of consumer products, exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models. While the intestinal toxicities of TCS require the presence of gut microbiota, the molecular mechanisms involved have not been defined. Here we show that intestinal commensal microbes mediate metabolic activation of TCS in the colon and drive its gut toxicology. Using a range of in vitro, ex vivo, and in vivo approaches, we identify specific microbial β-glucuronidase (GUS) enzymes involved and pinpoint molecular motifs required to metabolically activate TCS in the gut. Finally, we show that targeted inhibition of bacterial GUS enzymes abolishes the colitis-promoting effects of TCS, supporting an essential role of specific microbial proteins in TCS toxicity. Together, our results define a mechanism by which intestinal microbes contribute to the metabolic activation and gut toxicity of TCS, and highlight the importance of considering the contributions of the gut microbiota in evaluating the toxic potential of environmental chemicals.

Objectives: Colorectal cancer is one of the most common cancers worldwide. However, surgical intervention and chemotherapy provide only limited benefits for the recovery and survival of patients. The anticarcinogenic effect of genistein has attracted attention because epidemiological studies have shown that soybean consumption is associated with a decrease in the incidence of cancer. There are limited studies on the effects of genistein in colorectal carcinoma cells. We aimed to investigate the cytotoxic, genotoxic, and apoptotic effects of genistein in SW480 and SW620 colon adenocarcinoma cells treated with 5-fluorouracil, the basis of chemotherapy, and the tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) ligand, the mediator of apoptosis, both alone and in combination. Materials and Methods: Cytotoxicity and genotoxicity were determined by MTT and comet assays, respectively. The apoptotic effects were evaluated by reverse transcription-polymerase chain reaction assay, with the additional use of Annexin V FITC, mitochondrial membrane potential (MMP), caspase 3, 8, and 9 activity, and reactive oxygen species (ROS) assay kits. Results: According to our findings, genistein, 5-fluorouracil, and TRAIL had synergistic apoptotic effects because of DR5 upregulation, ROS production, and DNA damage, which were mediated by increased caspase-8, and -9 activity and decreased MMP. Conclusion: The applied combinations of these compounds may contribute to the resistance problem that may occur in treating colorectal cancer, with a decrease in DcR1 and XIAP genes. [ABSTRACT FROM AUTHOR]

Brassicaceae is a family of vegetables found all over the world that has been attracting the attention of researchers due to its rich chemical composition and potential health benefits (antioxidant and anti-inflammatory, as well as antimutagenic activity and potential anticarcinogenic effects). In Italy, various Brassicaceae varieties are commercially available, including traditional local cultivars, which have unique features and genetic diversity. As a result, there is a growing need to protect and recognize these landraces to preserve biodiversity. In this study, non-destructive tools such as Attenuated Total Reflectance-Fourier Transform-Infrared Spectroscopy (ATR-FT-IR) and chemometrics were employed to investigate eight distinct Brassicaceae landraces. The collected data were analyzed using a class modeling approach (Soft Independent Modeling of Class Analogy) and a discriminant classification method (Partial Least Squares Discriminant Analysis) to assess similarities and dissimilarities among the samples, all cultivated in an experimental field under the same pedoclimatic conditions. Remarkably, the combination of IR spectra and chemometric tools allowed accurate classification of the samples according only to their genetic background and despite their inclination to hybridization. The study highlights and demonstrates the importance and applicability of this specific non-destructive method for assisting the management and preservation of the genetic resources related to the local varieties of Brassicaceae. [ABSTRACT FROM AUTHOR]

Purpose: Herein, we sought to determine whether of saponin rich Gypsophila eriocalyx methanol extract (GEME) would exhibit any anti-carcinogenic activity on neuroblastoma cancer cell line (SH-SY5Y). Materials and Methods: We therefore determined GEME's saponin composition using LC-MS analysis, its impact on cell viability using MTT analysis, flow cytometry, and to find out its impact on apoptosis using qRT-PCR analysis. Results: In the LC-MS analysis we determined that GEME contained high amounts of saponin (0.05-0.48 µg/g). We determined that GEME had an IC50 dose of 100 µg/mL at 48 hours. GEME had the effect of substantially increasing the percentage of apoptotic cells (5.19% and 65.21%) and disruption of mitochondria (46.18%). We also demonstrated that BCL2 gene expression (2.76 fold) was significantly reduced than that of the control while BAX (2.21 fold), CASP3 (2.43 fold), CASP7 (2.98 fold), CASP8 (2.23 fold), CASP9 (2.78 fold), and CYCS (2.12 fold) genes were expressed significantly higher than those of the control. Conclusion: Considering the findings, it becomes clear that saponin-rich GEME stands out as a significant anticarcinogenic agent. Its remarkable efficacy is demonstrated through its capabilities to notably reduce cell viability, effectively trigger apoptosis, and significantly increase the rate of mitochondrial disruption in cancer cells. [ABSTRACT FROM AUTHOR]

Copyright of Revista Cientifica de la Facultade de Veterinaria is the property of Universidad del Zulia, Facultad de Ciencias Veterinarias 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 development of novel chemotherapeutic drugs begins with the suppression of cancer and angiogenesis. Ringed compounds with one or more heteroatoms are known as heterocyclic compounds. In organic chemistry and the pharmaceutical sector, heterocyclic compounds containing nitrogen atoms are valuable. In pharmaceutical chemistry, molecules containing a 1,2,3-triazole skeleton are particularly favored. They have great stability, making it simple to bind them to biomolecular targets. In this work, two 1,2,3-triazole scaffolds containing new chemical entities were assessed using the MTT assay against two malignant (MCF-7 and HCT116) and one normal (HUVECs) cell lines with the goal of creating a new leading prodrug for cancer treatment. The ligands were well characterized by FTIR and 1HNMR. In silico ADMET studies show acceptable pharmacokinetic properties. With the aid of the ligands' SWISS target protein prediction, the in silico binding to target proteins was examined. The two compounds exhibited a dose-dependent cytotoxic effect, with the H4 compound demonstrating a favorable selectivity index against MCF-7 breast cancer, indicating its potential as a leading compound for anticancer prodrugs. [ABSTRACT FROM AUTHOR]

Introduction: Resveratrol is a polyphenol stilbene found in red wine, red grape skins and other plants such as mulberries and peanuts. Resveratrol exhibits a wide range of beneficial properties such as anticarcinogenic agent, platelet antiaggregation agent, antiallergenic, antioxidant, and anti-inflammatory agent. Material and Methods: A total of 30 patients diagnosed as chronic periodontitis with diabetes were included in this study. and divided into 2 groups, Group-I (SRP+ resveratrol, n=15) & Group-II (SRP alone, n=15). Resveratrol capsules once daily were prescribed for 3 weeks. Plaque index (PI), Gingival index (MSBI), probing pocket depth (PPD), clinical attachment level (CAL) and serum venous blood sample collection for HbA1c levels. All the parameters were recorded at baseline and at 3 months post-operative. Results: All the parameters in both Group I and Group II showed statistically significant (P=0.001) reduction from baseline to 3 months. improvement from baseline to 3 months. When compared between the two groups, a significant difference was observed in Group I in relation with PI and HbA1c levels at 3 months post-operatively. Conclusion: Resveratrol as adjunctive to SRP has shown reduction in periodontal parameters in chronic periodontitis along with improved glycemic control in diabetes patients. [ABSTRACT FROM AUTHOR]

According to the available ethnobotanical data, the Bouvardia ternifolia plant has long been used in Mexican traditional medicine to relieve the symptoms of inflammation. In the present study, the cytotoxic effect of extracts obtained from the flowers, leaves and stems of B. ternifolia using hexane, ethyl acetate (AcOEt) and methanol (MeOH) was evaluated by applying them to the SiHa and MDA-MB-231 cancer cell lines. An MTT reduction assay was carried out along with = biological activity assessments, and the content of total phenols, tannins, anthocyanins, betalains and saponins was quantified. According to the obtained results, nine extracts exhibited a cytotoxic effect against both the SiHa and MDA lines. The highest cytotoxicity was measured for leaves treated with the AcOEt (ID50 of 75 µg/mL was obtained for MDA and 58.75 µg/mL for SiHa) as well as inhibition on ABTS•+ against DPPH• radical, while MeOH treatment of stems and AcOEt of flowers yielded the most significant antioxidant capacity (90.29% and 90.11% ABTS•+ radical trapping). Moreover, the highest phenolic compound content was measured in the stems (134.971 ± 0.294 mg EAG/g), while tannins were more abundant in the leaves (257.646 mg eq cat/g) and saponins were most prevalent in the flowers (20 ± 0 HU/mg). Screening tests indicated the presence of flavonoids, steroids, terpenes and coumarins, as well as ursolic acid, in all the studied extracts. These results demonstrate the biological potential of B. ternifolia. [ABSTRACT FROM AUTHOR]

Extracellular vesicles (EVs) are membrane-bound organelles that are generally released by eukaryotic cells and enclose various cellular metabolic information, such as RNA, meta-proteins, and versatile metabolites. The physiological properties and diverse functions of food-derived EVs have been extensively elucidated, along with a recent explosive upsurge in EV research. Therefore, a concise review of the health effects of food-derived EVs is necessary. This review summarizes the structural stability and uptake pathways of food-derived EVs to target cells and their health benefits, including antioxidant, anti-inflammatory, and anticarcinogenic effects, gut microbiome modulation, and intestinal barrier enhancement. [ABSTRACT FROM AUTHOR]

Monensin is an ionophore antibiotic that inhibits the growth of cancer cells. The aim of this study was to investigate the apoptosis‐mediated anticarcinogenic effects of monensin in SH‐SY5Y neuroblastoma cells. The effects of monensin on cell viability, invasion, migration, and colony formation were determined by XTT, matrigel‐chamber, wound healing, and colony formation tests, respectively. The effects of monensin on apoptosis were determined by real‐time polymerase chain reaction, TUNEL, Western blot, and Annexin V assay. We have shown that monensin suppresses neuroblastoma cell viability, invasion, migration, and colony formation. Moreover, we reported that monensin inhibits cell viability by triggering apoptosis of neuroblastoma cells. Monensin caused apoptosis by increasing caspase‐3, 7, 8, and 9 expressions and decreasing Bax and Bcl‐2 expressions in neuroblastoma cells. In Annexin V results, the rates of apoptotic cells were found to be 9.66 ± 0.01% (p < 0.001), 29.28 ± 0.88% (p < 0.01), and 62.55 ± 2.36% (p < 0.01) in the 8, 16, and 32 μM monensin groups, respectively. In TUNEL results, these values were, respectively; 35 ± 2% (p < 0.001), 34 ± 0.57% (p < 0.001), and 75 ± 2.51% (p < 0.001). Our results suggest that monensin may be a safe and effective therapeutic candidate for treating pediatric neuroblastoma. [ABSTRACT FROM AUTHOR]

Colorectal cancer (CRC) is one of the most common cancers worldwide. Epidemiological studies indicate that consumption of fruits and vegetables containing procyanidins is associated with lower CRC risk. This study investigated the capacity of two dimeric procyanidins composed of epicatechin gallate (ECG) or epigallocatechin gallate (EGCG) isolated from persimmons, to inhibit CRC cell growth and promote apoptosis, characterizing the underlying mechanisms. ECG and EGCG dimers reduced the growth of five human CRC cell lines in a concentration (10-60 μM)- and time (24-72 h)-dependent manner, with a 72 h-IC50 value in Caco-2 cells of 10 and 30 μM, respectively. ECG and EGCG dimers inhibited Caco-2 cell proliferation by arresting the cell cycle in G2/M phase and by inducing apoptosis via the mitochondrial pathway. In addition, ECG and EGCG dimers inhibited cell migration, invasion, and adhesion, decreasing the activity of matrix metalloproteinases (MMP-2/9). Mechanistically, ECG and EGCG dimers inhibited the activation of lipid raft-associated epidermal growth factor (EGF) receptor (EGFR), without affecting its localization at lipid rafts. In particular, ECG and EGCG dimers reduced EGFR phosphorylation at Tyr1068 residue, prevented EGFR dimerization and activation upon stimulation, and induced EGFR internalization both in the absence and presence of EGF. Furthermore, ECG and EGCG dimers increased EGFR phosphorylation at Tyr1045 residue, providing a docking site for ubiquitin ligase c-Cbl and induced EGFR degradation by the proteasome. Downstream of EGFR, ECG and EGCG dimers inhibited the activation of the MEK/ERK1/2 and PI3K/AKT signaling pathways, downregulating proteins involved in the modulation of cell survival. In conclusion, ECG and EGCG dimers reduced CRC cell growth by inhibiting EGFR activation at multiple steps, including the disruption of lipid rafts integrity and promoting EGFR degradation. These results shed light on a potential molecular mechanism on how procyanidins-rich diets may lower CRC risk.

This study was designed to assess the ameliorative effects of eugenol and to propose the possible mechanisms of action of eugenol in diethylnitrosamine (DENA)/acetylaminofluorene (AAF)-caused lung cancer in Wistar rats. To induce lung cancer, DENA at a dose of 150 mg/kg body weight (b.wt) for 2 weeks were intraperitoneally injected once each week and AAF was administered orally at a dose of 20 mg/kg b.wt. four times each week for the next 3 weeks. DENA/AAF-administered rats were orally supplemented with eugenol at a dose of 20 mg/kg b.wt administered once a day until 17 weeks starting from the 1st week of DENA administration. Lung histological lesions, including sheets of tumor cells, micropapillary adenocarcinoma, and apoptotic cells, resulting from the DENA/AAF dosage, were ameliorated by eugenol treatment. However, a significant drop in the levels of LPO in the lungs and a remarkable rise in GSH content and GPx and SOD activities were observed in DENA/AAF-administered rats treated with eugenol compared with those in DENA/AAF-administered controls. Moreover, in DENA/AAF-administered rats, eugenol supplementation significantly reduced TNF-α and IL-1β levels and mRNA expression levels of NF-κB, NF-κB p65, and MCP-1 but significantly elevated the level of Nrf2. Furthermore, the DENA/AAF-administered rats treated with eugenol exhibited a significant downregulation of Bcl-2 expression levels in addition to a significant upregulation in P53 and Bax expression levels. Otherwise, the administration of DENA/AAF elevated the protein expression level of Ki-67, and this elevation was reversed by eugenol treatment. In conclusion, eugenol has effective antioxidant, anti-inflammatory, proapoptotic, and antiproliferative properties against lung cancer. [ABSTRACT FROM AUTHOR]

Despite the well-described anticarcinogenic effects of endocannabinoids, the influence of the endocannabinoid system on tumor angiogenesis is still debated. In the present study, conditioned medium (CM) from A549 and H358 lung cancer cells treated with ascending concentrations of the monoacylglycerol lipase (MAGL) inhibitor JZL184 and 2-arachidonoylglycerol (2-AG), a prominent MAGL substrate, caused a concentration-dependent reduction in human umbilical vein endothelial cell (HUVEC) migration and tube formation compared with CM from vehicle-treated cancer cells. Comparative experiments with MAGL inhibitors JW651 and MJN110 showed the same results. On the other hand, the angiogenic properties of HUVECs were not significantly altered by direct stimulation with JZL184 or 2-AG or by exposure to CM of JZL184- or 2-AG-treated non-cancerous bronchial epithelial cells (BEAS-2B). Inhibition of HUVEC migration and tube formation by CM of JZL184- and 2-AG-treated A549 cells was abolished in the presence of the CB1 antagonist AM-251. Increased release of tissue inhibitor of metalloproteinase-1 (TIMP-1) from JZL184- or 2-AG-stimulated A549 or H358 cells was shown to exert an antiangiogenic effect on HUVECs, as confirmed by siRNA experiments. In addition, JZL184 caused a dose-dependent regression of A549 tumor xenografts in athymic nude mice, which was associated with a decreased number of CD31-positive cells and upregulation of TIMP-1-positive cells in xenograft tissue. In conclusion, our data suggest that elevation of 2-AG by MAGL inhibition leads to increased release of TIMP-1 from lung cancer cells, which mediates an antiangiogenic effect on endothelial cells. [ABSTRACT FROM AUTHOR]

Plants belonging to the Fabaceae family have great importance in animal nutrition and the protection of human health (antidiabetic, anticarcinogenic, antioxidant, anti-inflammatory, and cardiovascular). Onobrychis, known as a potent antioxidant, anticarcinogenic and antimicrobial agent, its high phenolic substance is one of the important genera of this family. In this study, chloroform (OAC), ethanol (OAE), and water (OAW) extract of Onobrychis argyrea subsp. argyrea (O. argyrea) specie was prepared; and the antiproliferative, antimicrobial, and antioxidant activities were investigated. The antiproliferative effects of the extracts were evaluated on different cancer cell lines by XTT colourimetric method. OAE demonstrated the most excellent efficacy against all cell lines, according to the findings. MCF-7 83.71%, A549 92.14%, and HT-29 72.24% were all inhibited. The antimicrobial activity of OAE and OAW extracts against Staphylococcus aureus, Escherichia coli, and Streptococcus pneumoniae was determined using the disc-diffusion technique. Finally, antioxidant power was determined using DPPH and FRAP methods. In the DPPH research, OAE and OAW extracts showed the highest levels of inhibition (IC50: 34.12±0.2 and 21.58±0.12, respectively). OAE (257.95±1.40) and OAW (282.14±0.83) extracts showed high activity with similar results in the FRAP method. Total phenolic content was determined as 226.15±1.89 mg GAE/g for OAE and 146.52±0.71 mg GAE/g for OAW, respectively. These results show that the species is an essential source of antioxidants. These studies are the first data for Onobrychis argyrea subsp. argyrea. All these results show that the plant has various biological activities and rich secondary metabolites. [ABSTRACT FROM AUTHOR]

Purpose: The purpose of the studies described in this mini review article was to identify nontoxic compounds that could prevent or suppress the radiation induced malignant transformation of cells and be useful as human cancer preventive agents. Conclusions: (1) Many different types of potential anticarcinogenic substances were evaluated initially for their abilities to prevent or suppress radiation induced malignant transformation in vitro, and certain anticarcinogenic protease inhibitors (APIs) were observed to be the most powerful anticarcinogenic agents at suppressing this surrogate endpoint biomarker of radiation carcinogenesis. (2) Within the category of APIs, those that inhibited the activity of chymotrypsin were effective at far lower molar concentrations than other APIs. The soybean-derived protease inhibitor known as the Bowman-Birk inhibitor (BBI) is a particularly powerful chymotrypsin inhibitor that is able to prevent radiation induced transformation in vitro (at concentrations down to nanomolar levels) as well as radiation induced carcinogenesis in vivo without toxicity. (3) There were many other unusual characteristics of APIs that led to the selection of one of these APIs, BBI, as the most appropriate compound for us to develop as a human cancer preventive agent. As one example, the APIs have an irreversible effect on carcinogenesis, while the effects are reversible for most anticarcinogenic agents when they are removed from carcinogenesis assay systems. (4) Numerous studies were performed in attempts to determine the potential mechanisms by which the APIs could prevent or suppress radiation induced carcinogenesis in in vitro and in vivo systems, and the results of these studies are described in this review article. The APIs and the proteases which interact with them appear to play important roles in radiation carcinogenesis. (5) Preparations for human trials using BBI began decades ago. The cost of preparing purified BBI was far too high to consider performing human trials with this agent, so BBI Concentrate (BBIC), a soybean extract enriched in BBI, was developed for the specific purpose of performing human trials with BBI. BBIC achieved Investigational New Drug (IND) Status with the Food and Drug Administration in April, 1992, and human BBIC trials began at that time. (6) Several human trials were performed using BBIC and they indicated many potentially beneficial health effects produced by BBIC administration to people in various forms (e.g. tablets). 7) It is hypothesized that BBI takes the place of a-1-antichymotrypsin, an important regulatory compound in the human body, and helps to maintain homeostasis. [ABSTRACT FROM AUTHOR]

Patients who have undergone curative‑intent therapy for head and neck squamous cell carcinoma (HNSCC) exhibit a high rate of development of second primary tumors (SPTs), which are frequently lethal. A chemoprevention strategy that prevents SPTs would have a major impact on patient outcomes. Sulforaphane, a naturally‑occurring compound derived from cruciferous vegetables exhibits chemopreventive activity against HNSCC in a preclinical model. The effects of sulforaphane are considered to be mediated, in large part, through increased protein expression of the transcription factor nuclear factor erythroid 2‑related factor 2 (NRF2). Development of sulforaphane chemoprevention for HNSCC would benefit from the identification of robust biomarkers of sulforaphane activity in HNSCC cells and normal mucosal epithelial cells. The present study revealed that sulforaphane potently induces multiple oxidative stress‑associated genes at the RNA and protein levels, in HNSCC cells and Het‑1A cells, a non‑tumorigenic mucosal epithelial cell line. In the present analysis, HMOX1 and HSPA1A were identified as the most highly upregulated genes following sulforaphane treatment, suggesting their potential value as biomarkers to guide clinical trials. Sulforaphane induction of HMOX1 and HSPA1A was validated in vivo in murine tissues. Furthermore, the impact of sulforaphane treatment of HNSCC cells on the expression levels of natural killer group 2D (NKG2D) and DNAX accessory molecule‑1 (DNAM‑1) ligands, which are activators of natural killer (NK) cells, was examined. NRF2‑dependent upregulation of the NKG2D ligand MICA/B was observed. However, only one of the six HNSCC cell lines studied exhibited enhanced sensitivity to NK cell‑mediated killing following sulforaphane treatment, suggesting that this may not be a general mechanism of sulforaphane chemopreventive activity in HNSCC. In summary, the present study identified robust biomarkers of sulforaphane activity in HNSCC and normal tissues, supporting their application in the development of sulforaphane chemoprevention approaches for HNSCC.

Neohesperidin (NH), a natural flavonoid, exerts multiple actions, such as antioxidant, antiviral, antiallergic, vasoprotective, anticarcinogenic and anti-inflammatory effects, as well as inhibition of tumor progression. In this study, the NH–taro starch complex is prepared, and the effects of NH complexation on the physicochemical properties, structure and in vitro digestibility of taro starch (TS) are investigated. Results showed that NH complexation significantly affected starch gelatinization temperatures and reduced its enthalpy value (ΔH). The addition of NH increased the viscosity and thickening of taro starch, facilitating shearing and thinning. NH binds to TS via hydrogen bonds and promotes the formation of certain crystalline regions in taro starch. SEM images revealed that the surface of NH–TS complexes became looser with the increasing addition of NH. The digestibility results demonstrated that the increase in NH (from 0.1% to 1.1%, weight based on starch) could raise RS (resistant starch) from 21.66% to 27.75% and reduce RDS (rapidly digestible starch) from 33.51% to 26.76% in taro starch. Our work provided a theoretical reference for the NH–taro starch complex's modification of physicochemical properties and in vitro digestibility with potential in food and non-food applications. [ABSTRACT FROM AUTHOR]

Medicinal plants and their bioactive constituents play a vital role in the prevention of oxidative stress mediated diseases such as cancer and diabetes mellitus. The aim of this study is to investigate the reactive oxygen species (ROS) scavenging and anti-proliferative potential of veratric acid in vitro. The study analysed the antioxidant potential of veratric acid using in vitro free radical scavenging assays. The anti-proliferative potential of veratric acid was assessed by utilizing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, mitochondrial membrane potential (MMP) changes, intracellular ROS generation measurement and by determining the morphological alterations using Acridine orange/Ethidium bromide (Ao/EtBr) staining in the subline of Keratin-forming tumour cell line HeLa (KB). Veratric acid showed a good antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), superoxide and hydroxyl radicals and the effect was found to be much comparable to that of the reference drug, ascorbic acid. Veratric acid significantly reduced the cell viability of KB cells and IC50 was 80 µg/ml. Veratric acid reduced the cell viability by generating excess ROS through activation of MMP depolarization and by inducing the apoptotic cell death of KB cells. The in vitro antioxidant and antiproliferative effect of veratric acid could be used further to validate its anti-carcinogenic potential using ideal experimental animal models. [ABSTRACT FROM AUTHOR]

After decades of research and development concerning cancer treatment, cancer is still at large and very much a threat to the global human population. Cancer remedies have been sought from all possible directions, including chemicals, irradiation, nanomaterials, natural compounds, and the like. In this current review, we surveyed the milestones achieved by green tea catechins and what has been accomplished in cancer therapy. Specifically, we have assessed the synergistic anticarcinogenic effects when green tea catechins (GTCs) are combined with other antioxidant-rich natural compounds. Living in an age of inadequacies, combinatorial approaches are gaining momentum, and GTCs have progressed much, yet there are insufficiencies that can be improvised when combined with natural antioxidant compounds. This review highlights that there are not many reports in this specific area and encourages and recommends research attention in this direction. The antioxidant/prooxidant mechanisms of GTCs have also been highlighted. The current scenario and the future of such combinatorial approaches have been addressed, and the lacunae in this aspect have been discussed. [ABSTRACT FROM AUTHOR]

• Novel benzohydrazide derivative with monoclinic crystal system and C 2/c space group. • Intermolecular N–H···O hydrogen bonds form infinite chains along the b -axis. • Dominant interactions in crystal packing: hydrogen bonding and van der Waals interactions. • Strong anticancer effects: IC 50 of 85 µM for MCF7 and 115 µM for MDA-MB-231 cells. • Computational analyses predict good oral availability and binding to ERRγ receptor. Polycyclic aromatic compounds (PACs) are a class of organic molecules known for their significant biological activity, including anticancer properties. These compounds often interact with biological macromolecules, making them crucial in the development of new therapeutic agents. In this study, we report a new benzohydrazide derivative, (E)-4-(hexyloxy)-N'-(1-(naphthalen-2-yl)ethylidene)benzohydrazide (2), which incorporates a naphthalene ring, a typical PAC, as a core structural element. The structure of the compound was analyzed using FTIR, 1H NMR, 13C NMR and elemental analysis. Moreover, single crystal X-ray crystallography studies demonstrated that the compound adapted monoclinic crystal system with C 2/c space group. In the crystal structure, the intermolecular N–H···O hydrogen bonds link the molecules into infinite chains along the b -axis direction. The dominant interactions formed in the crystal packing were found to be hydrogen bonding and van der Waals interactions according to the Hirshfeld surface (HS) analysis. The evaluation of energy frameworks showed that stabilization of the compound was dominated by dispersion energy contribution. The anticancer activity of the compound was tested by employing several cellular assays. The compound showed strong anticancer effects, with IC 50 values of 85 µM for MCF7 cells and 115 µM for MDA-MB-231 cells, indicating dose-dependent suppression of cell viability, migration, and colony formation. Computational analyses indicated favorable binding of compound 2 to ERRγ and predicted good oral availability of the generated compound. Pathway analysis using KEGG pathways identified significant enrichment in pathways related to cancer. These results highlight the compound's promise as a potential treatment option for breast cancer, prompting further exploration in future studies. [Display omitted] [ABSTRACT FROM AUTHOR]

Papillary thyroid carcinoma (PTC) is the most common malignant tumor of the endocrine system globally. Formononetin (FMNT), an isoflavonoid, exerts anti-tumorigenic effects and chromobox homolog 4 (CBX4) exerts tumor-promoting effect in specific types of tumors. Nevertheless, the predictive values and biological functions of FMNT and CBX4 in the pathological progress of PTC have not been fully understood till now. In the present study, the human PTC cell line TPC-1 was exposed to 0, 10, 30 and 100 µM FMNT for 24 h to elucidate the precise effects of FMNT on the biological behaviors of PTC cells. Moreover, FMNT-treated TPC-1 cells were transfected with oe-CBX4 to evaluate whether CBX4 was implicated in the anticarcinogenic effects of FMNT against PTC. It was demonstrated that FMNT treatment suppressed the proliferation, clone formation, migration, invasion, EMT, angiogenesis and stemness of PTC cells in a dose-dependent manner. Furthermore, it was verified that FMNT targeted CBX4 to downregulate its expression in a dose dependent manner. The suppressive effects of FMNT on the proliferation, clone formation, migration, invasion, EMT, angiogenesis and stemness of PTC cells were partially reversed by CBX4 overexpression. Upregulation of CBX4 abolished the tumor suppression effects of FMNT in the malignant progression of PTC. In conclusion, FMNT might act as a promising anti-tumorigenic agent in PTC, which depends on the downregulation of CBX4. [ABSTRACT FROM AUTHOR]

Recent progress in the treatment of advanced melanoma has led to unprecedented improvements in overall survival and, as these new melanoma treatments have been developed and deployed in the clinic, much has been learned about the natural history of the disease. Now is the time to apply that knowledge toward the design and clinical evaluation of new chemoprevention agents. Melanoma chemoprevention has the potential to reduce dramatically both the morbidity and the high costs associated with treating patients who have metastatic disease. In this work, scientific and clinical melanoma experts from the national Melanoma Prevention Working Group, composed of National Cancer Trials Network investigators, discuss research aimed at discovering and developing (or repurposing) drugs and natural products for the prevention of melanoma and propose an updated pipeline for translating the most promising agents into the clinic. The mechanism of action, preclinical data, epidemiological evidence, and results from available clinical trials are discussed for each class of compounds. Selected keratinocyte carcinoma chemoprevention studies also are considered, and a rationale for their inclusion is presented. These data are summarized in a table that lists the type and level of evidence available for each class of agents. Also included in the discussion is an assessment of additional research necessary and the likelihood that a given compound may be a suitable candidate for a phase 3 clinical trial within the next 5 years.

There is considerable evidence that melatonin may be of use in the prevention and treatment of cancer. This manuscript will review some of the human, animal and cellular studies that provide evidence that melatonin has oncostatic properties. Confirmation that melatonin mitigates pathogenesis of cancer will be described from both direct study of its effects on carcinogenesis, and from indirect findings implicating disruption of the circadian cycle. A distinction is made between the role of melatonin in preventing the initiation of the tumorigenic pathway and the ability of melatonin to retard the progression of cancer. Melatonin appears to slow down the rate of advancement of established tumors and there is evidence that it constitutes a valuable complement to standard pharmacological and radiation treatment modalities. There are instances of the beneficial outcomes in cancer treatment which utilize a range of hormones and vitamins, melatonin being among the constituents of the mix. While these complex blends are empirically promising, they are only briefly mentioned here in view of the confounding influence of a multiplicity of agents studied simultaneously. The last section of this review examines the molecular mechanisms that potentially underlie the oncostatic effects of melatonin. Alterations in gene expression following activation of various transcription factors, are likely to be an important mediating event. These changes in gene activity not only relate to cancer but also to the aging process which underlies the onset of most tumors. In addition, epigenetic events such as modulation of histone acetylation and DNA methylation patterns throughout the lifespan of organisms need to be considered. The antioxidant and immunoregulatory roles of melatonin may also contribute to its cancer modulatory properties. Naturally, these mechanisms overlap and interact extensively. Nevertheless, in the interest of clarity and ease of reading, each is discussed as a separate topic section. The report ends with some general conclusions concerning the clinical value of melatonin which has been rather overlooked and understudied.

In this work, two marine green macro algae are potential (Enteromorpha intestinalis and Ulva lactuca species) as a source of several critical bioactive substances. Bioactive phenolic and flavonoids compounds were explored. Antioxidant properties and anticancer effects, such as cytotoxicity of different extracts of Enteromorpha sp and Ulva lactuca sp, have been investigated. The methanolic extracts have the most robust free radical activity (91.89 %) as well as ethyl acetate (86.70%), followed by water extract (82.47 %) and hexane extract (77.25 %) of Ulva sp compared to ascorbic acid as standard (98.16%). Percentage inhibition on free radical scavenging generation by the methanolic extract was found to be increasing in Enteromorpha sp (83.85 %), followed by water extract (81.14%); ethyl acetate extract (80.56 %) and hexane extract (71.76%). The methanolic extract of Enteromorpha sp and Ulva sp yielded data demonstrating a high total phenolic content of 66.8 and 40.3 as mg GAE /g sample, respectively. The Enteromorpha sp and Ulva sp extracted with methanol were significantly higher in their content of total flavonoids (49.4 and 32.1 as quercetin mg/g sample, respectively) than the other extracts. The obtained data reveal that methanol extract had the highest anticancer activity. There was no inhibition of all cancer cells of the samples extracted with water. The results showed that this type of algae contains unique and innovative chemical active antitumor components and can act as an antioxidant and anti-carcinogenic agent of the liver and colon for future applications in the pharmaceutical industries. [ABSTRACT FROM AUTHOR]

The antibacterial activity of an Ulvan-based silver nanoparticle (AgNP) system was evaluated in the current study. The green synthesis of biogenic silver nanoparticles was conducted using Ulvan, a sulphated polysaccharide extracted from Ulva lactuca. A novel mouthwash containing AgNPs was prepared, and tested for its efficacy and safety. AgNPs were confirmed with spectrophotometric analysis (UV–A visible spectrophotometer), and the characterisation was established with Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and transmission electron microscopy (TEM). The AgNPs were spherical, and their average size was 8–33 nm, as shown via TEM. The antioxidant assay was conducted via DDPH assay, wherein the AgNPs, at a concentration of 50 μL/mL, showed 93.15% inhibition. Furthermore, anticancer activity was tested by evaluating the cell viability utilising the method of an MTT assay on the 3T3-L1 cell lines. AgNPs, at 30 µL/mL, showed maximal cell viability, denoting no cytotoxic effect. The silver-nanoparticle-based mouthrinse, at a concentration of 100 µL/mL, demonstrated antimicrobial activity against Streptococcus mutans, Staphylococcus aureus, Lactobacillus, and Candida albicans. This study shows that mouthwash prepared from the Ulvan-silver nanoparticle system could be a nontoxic and effective oral antimicrobial agent. [ABSTRACT FROM AUTHOR]

Siraitia grosvenorii is the fruit of a cucurbitaceous vine endemic to China. Its extract has been used as a sweetener and exhibits various anti-inflammatory and anticarcinogenic effects mediated via its antioxidant properties. In the present study, we aimed to clarify the preventive or ameliorative effects of S. grosvenorii extract (SGE) on nonalcoholic steatohepatitis-like lesions induced in male Hsd: Sprague Dawley rats fed a choline-deficient, methionine-lowered, L-amino acid-defined diet for 13 weeks. This diet increased hepatotoxicity parameters and upregulated the expression of inflammation- and fibrosis-related genes in the liver, resulting in the progression of hepatic lesions, oxidative stress, hepatocellular apoptosis, and fibrosis. Furthermore, this diet upregulated the expression of phosphorylated nuclear factor-xB (NF-kB) and CD44. SGE administration inhibited these lesions, similar to CD44, a factor that controls hepatic inflammation and fibrosis. These results revealed that SGE impacts the disease stage via antioxidative effects and regulation of CD44 expression. SGE was found to be useful for preventing and treating steatohepatitis. [ABSTRACT FROM AUTHOR]

In this study, a new metal complex, bis(μ-4-chlorobenzoato-κ2O:O′)bis[(4-chlorobenzoato-κ2O:O′-bis(isonicotinamide-κN)copper(II)] (1), was synthesized. The crystal structures of the complex were determined by single-crystal XRD. In addition, the structure was characterized by elemental analysis and FTIR spectroscopy. The intermolecular interactions of the complex were determined by Hirshfeld surface analysis. The optical and fluorescence properties of the complex were recorded with the help of UV–Vis and fluorescence spectrophotometer. In addition, the anticarcinogenic effects of the complex on DLD-1, MCF-7 and PC-3 cell lines and their cytotoxic properties on human lymphocyte cells were investigated by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The complex has a dimeric structure. The intermolecular interactions that contribute the most to the crystal structure are H⋯H, O⋯H/H⋯O and H⋯C/C⋯H interactions. The complex was exhibited broad emission peaks between 350 and 550 nm. It was determined that the complexes did not cause cytotoxic effects on lymphocyte cells. Complex 1 caused a strong cytotoxic effect on DLD-1 colon cancer cells. The complex was determined to cause low cytotoxicity on MCF-7 and PC-3 cells. The interactions of the complex with synthetic DNA dodecamer were investigated by molecular docking. It has been determined that the complex inhibits these proteins through hydrophobic, electrostatic and non-covalent interactions. [ABSTRACT FROM AUTHOR]

Flavonoids are a category of plant-derived compounds which exhibit a large number of health-related effects. One of the most well-known and studied flavonoids is kaempferol, which can be found in a wide variety of herbs and plant families. Apart from their anticarcinogenic and anti-inflammatory effects, kaempferol and its associated compounds also exhibit antibacterial, antifungal, and antiprotozoal activities. The development of drugs and treatment schemes based on these compounds is becoming increasingly important in the face of emerging resistance of numerous pathogens as well as complex molecular interactions between various drug therapies. In addition, many of the kaempferol-containing plants are used in traditional systems all over the world for centuries to treat numerous conditions. Due to its variety of sources and associated compounds, some molecular mechanisms of kaempferol antimicrobial activity are well known while others are still under analysis. This paper thoroughly documents the vegetal and food sources of kaempferol as well as the most recent and significant studies regarding its antimicrobial applications. [ABSTRACT FROM AUTHOR]

Nature derived product drew a lot of interest because of their potential nutritional and therapeutics value. Most natural compounds are now processed and developed as possible antioxidative, antimitotic, antimicrobial, anti-inflammatory, antiangiogenic, and anti-carcinogenic pharmaceutical agents. Indeed, several natural products have been used as lead compounds in the development of most potent physiologically relevant chemicals for therapeutic application. In the current study antioxidant and anticancer potential of tuber extract of Dioscorea bulbifera have been determined as well as its antimicrobial potential against pathogenic bacteria. The IC50 value for the extract was found to be 55µg/ml for MCF-7 and 75µg/ml for MD-AMB-231 human breast cancer adenocarcinoma whereas minimum inhibitory concentration (MIC) value of the methanolic extract against S. aureus was 0.19 mg/ml and minimum bactericidal concentration (MBC) was 1.56 mg/ml. Further to identify compounds responsible for antioxidant, anticancer and antimicrobial activity GCMS analysis of the extract was conducted. Histopathological and haematological assay were carried out on animal model to identify any toxic effect of extract on vital organ system. This study may be used to provide the groundwork for the creation of novel nature-derived drugs whose biological activity can be determined by further purification, characterization, and validation of the active phytochemicals and their mechanism of action. [ABSTRACT FROM AUTHOR]

In this study, the DNA cleavage activities of a series of new silicon phthalocyanines were studied to measure their potential for cancer treatment. For this purpose, 2-(2,4,6-tris((dimethylamino)methyl)phenoxy)ethan-1-ol (2) and 2-(2-(2,4,6-tris((dimethylamino)methyl)phenoxy)ethoxy)ethan-1-ol (3) were synthesized and used for the preparation of axially di-substituted silicon phthalocyanines. The resulting phthalocyanines were quaternized in the presence of iodomethane. Characterization of all the newly synthesized compounds was carried out using several spectroscopic approaches including mass, UV-vis, FT-IR, and NMR spectroscopies. Plasmid DNA (pBR322) cleavage, topoisomerase enzyme activity and binding situation with calf thymus DNA (CT-DNA) of the new silicon phthalocyanines were measured using an agarose gel electrophoresis assay. 1-QSi exhibited remarkable cleavage activities on supercoiled plasmid DNA at all the studied concentrations. Compound 3-QSi displayed significant cleavage activities on supercoiled plasmid DNA only at 200 μg mL−1. Besides, compound 3-QSi exhibited higher human topoisomerase I inhibition activity compared to compound 2-QSi. Moreover, all the compounds were screened for biological activities. The cytotoxicity and apoptosis activities were studied against DLD-1 colorectal cancer cell lines at different concentrations ranging from 6.25 to 100 μg mL−1. The results indicated that the studied compounds can be utilized as anticarcinogenic agents. [ABSTRACT FROM AUTHOR]

The aim of the study was to demonstrate canned pork as a functional meat product due to the presence of potentially anti-cancer factors, e.g., (a) bioactive peptides with potential activity against cancer cells; (b) lowering the content of sodium nitrite and with willow herb extract. In silico (for assessing the anticancer potential of peptides) and in vitro (antiproliferation activity on L-929 and CT-26 cell lines) analysis were performed, and the obtained results confirmed the bioactive potential against cancer of the prepared meat product. After 24 h of incubation with peptides obtained from meat product containing lyophilized herb extract at a concentration of 150 mg/kg, the viability of both tested cell lines was slightly decreased to about 80% and after 72 h to about 40%. On the other hand, after 72 h of incubation with the peptides obtained from the variant containing 1000 mg/kg of freeze-dried willow herb extract, the viability of intestinal cancer cells was decreased to about 40%, while, by comparison, the viability of normal cells was decreased to only about 70%. [ABSTRACT FROM AUTHOR]

Plants belonging to the genus Hypericum L. are widely used in traditional folk medicine due to their hypericin and pseudohypericin contents. In this study, we investigated the biological activity, phenolic and elemental content of methanol and acetone extracts of sheepskin grass, Hypericum heterophyllum Vent. a species that that lacks both hypericin and pseudohypericin. The total antioxidant status of the extracts was determined by commercial kits. Antibacterial effect of extracts was investigated on seven bacterial strains. Cytotoxic effects of the extracts on lung cancer cell lines were determined by MTT (3-4,5-dimethyl-thiazolyl-2,5-diphenyltetrazolium bromide) method. Phenolic content was determined by LC-ESI-MS/MS. Elements in the plant were determined by ICP-OES. The total phenolic content and antioxidant status of the species' methanol extract were found to be higher than the acetone extract. Both of the extracts at a concentration of 20% have an antibacterial effect, especially the antibacterial effect of acetone extract. It was determined that acetone extract has an anticarcinogenic impact depending on the dose. Chlorogenic acid, miquelianin and isoquercitrin are the most abundant flavonoids in methanol and acetone extract. The plant contains Ca, K, and Mg elements in high concentrations. The phenolic substances and elements in H. heterophyllum, widely used in our country, have been presented for the first time in the literature. Besides, it can be said that the plant has antioxidant, anticarcinogen, and antimicrobial activities due to the crucial flavonoids and elements it contains. [ABSTRACT FROM AUTHOR]

Postsurgical treatment is of great importance to combat tumor recurrence and metastasis. Anti-CD47 antibodies (aCD47) can block the CD47-signal regulatory protein-alpha (CD47-SIRPα) pathway to restore immunity. Here, an in-situ gel implantation was engineered by crosslinking chitosan (CS) and pullulan (Pul) for postsurgical treatment. A highly selected chemotherapeutic, cyclopamine (Cyc), encapsulated in liposomes (Cyc-Lip) was co-loaded with aCD47 in gels for chemoimmunotherapy. Importantly, a sequential drug release kinetics can be achieved. Nanotherapeutics were confirmed to be released prior to aCD47 in a burst-release manner, which was benefit for immediately killing residual tumor cells followed by releasing tumor antigens. Meanwhile, aCD47 was released in a sustained-release manner to restore macrophage functions and exert anti-tumor immune responses. Afterwards, the efficacy of in-situ chemoimmunotherapy was confirmed on 4T1 mouse breast cancer models, which could not only efficiently augment anti-tumor effect to inhibit tumor recurrence but also establish a long-term immune memory to combat tumor metastasis. [Display omitted] • A gel consisting of chitosan and pullulan was engineered as the drug depot for postsurgical chemoimmunotherapy. • Chemotherapeutics and antibodies in the gel were sequentially and sustainedly released. • The gel based-combination strategy possesses a great potential for postsurgical tumor recurrence and metastasis suppression. [ABSTRACT FROM AUTHOR]

Introduction: The extraction of vegetable oils with organic solvents pollutes the environment and is expensive. Ultrasound-assisted extraction (UAE) has provided important benefits in the production of oils, such as: higher revenues, decreased operation time and solvent consumption, which makes it friendly to the planet. Objective: Provide the conceptual foundations, applications and potentialities of ultrasoundassisted extraction in the performance, physical-chemical characteristics and bioactivity of oils obtained from plant sources. Materials and Methods: 71 original and review publications were studied, using techniques and methodologies related to the extraction and characterization of vegetable oils using EAU, solvents and pressing in different types of seeds corresponding to the period 2013-2022, considering the quality and nature of the publications. Results and Discussion: The reviewed articles showed that, with the UAE in vegetables, vegetable and essential oils, and phenolic compounds were obtained; from both the seeds (chia), the leaves (soursop) and the mesocarp (avocado pulp). The new contributions and methods optimized the extraction of the required compounds, with the need to apply them in the food, cosmetic and pharmaceutical process industry. Conclusions: The review of the articles dealing with the production of vegetable oils using the EAU, established that this technique used organic solvents such as hexane, but its consumption is lower than traditional methods; decreased work times; the yields of the extracts were more efficient and the bioactive properties benefit the organism as antioxidants (canola) or anticarcinogenic (olive). [ABSTRACT FROM AUTHOR]

Current studies show that approximately one-third of all cancer-related deaths are linked to diet and several cancer forms are preventable with balanced nutrition, due to dietary compounds being able to reverse epigenetic abnormalities. An appropriate diet in cancer patients can lead to changes in gene expression and enhance the efficacy of therapy. It has been demonstrated that nutraceuticals can act as powerful antioxidants at the cellular level as well as anticarcinogenic agents. This review is focused on the best studies on worldwide-available plant-derived nutraceuticals: curcumin, resveratrol, sulforaphane, indole-3-carbinol, quercetin, astaxanthin, epigallocatechin-3-gallate, and lycopene. These compounds have an enhanced effect on epigenetic changes such as histone modification via HDAC (histone deacetylase), HAT (histone acetyltransferase) inhibition, DNMT (DNA methyltransferase) inhibition, and non-coding RNA expression. All of these nutraceuticals are reported to positively modulate the epigenome, reducing cancer incidence. Furthermore, the current review addresses the issue of the low bioavailability of nutraceuticals and how to overcome the drawbacks related to their oral administration. Understanding the mechanisms by which nutraceuticals influence gene expression will allow their incorporation into an "epigenetic diet" that could be further capitalized on in the therapy of cancer. [ABSTRACT FROM AUTHOR]

Lignans have long been known for their abundant therapeutic properties due to their polyphenolic structure. Linseed is the richest plant source of lignans and has been studied widely for their properties. The most prevalent lignan, secoisolariciresinol diglucoside (SDG), is consumed with linseed and converted into mammalian lignans, enterodiol (END) and enterolactone (ENL), by the gut microbiota. SDG can easily be assessed using HPLC and its deglycosylated form viz secoisolariciresinol can be asses using GC–MS techniques. Variety of extraction and analysis methods has been reported for plant lignans. SDG is known to have therapeutic properties including anti-oxidant, anti-cancerous, anti-inflammatory, modulation of gene expression, anti-diabetic, estrogenic and anti-estrogenic. Despite a large number of bioactivities, strong evidences for the underlying mechanisms for most of the properties are still unknown. SDG is most studied for its anti-cancerous properties. But the use of lignans as anti-carcinogenic agent is limited and commercially not reported due to challenges of purification at commercial level, rapid metabolism, untargeted delivery and toxic compounds associated with lignans. Exploration of more prominent and active derivatives of SDG and their targeted drug delivery should be an important research toward the use of bioactive lignans of linseed. [ABSTRACT FROM AUTHOR]