51,046 results match your criteria anticancer activity

Bacteria as a treasure house of secondary metabolites with anticancer potential.

Semin Cancer Biol 2021 May 9. Epub 2021 May 9.

Institution of Excellence, Vijnana Bhavan, University of Mysore, Manasagangotri, Mysore, 570006, India. Electronic address:

Cancer stands in the frontline among leading killers worldwide and the annual mortality rate is expected to reach 16.4 million by 2040. Humans suffer from about 200 different types of cancers and many of them have a small number of approved therapeutic agents. Read More

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Silver(I)-N-heterocyclic carbene complexes challenge cancer; evaluation of their anticancer properties and in silico studies.

Drug Dev Res 2021 May 12. Epub 2021 May 12.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Sivas Cumhuriyet University, Sivas, Turkey.

Because of the continuous need for efficient therapeutic agents against various kinds of cancers and infectious diseases, the pharmaceutical industry has to find new candidates and strategies to develop novel and efficient drugs. They increasingly use computational tools in R&D stages for screening extensive sets of drug candidates before starting pre-clinical and clinical trials. N-Heterocyclic carbenes (NHCs) can be evaluated as good drug candidates because they offer both anti-cancer and anti-inflammatory features with their general low-toxicity profiles. Read More

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Impact of home-based aerobic training combined with food orientation on food consumption, daily physical activity and cardiorespiratory fitness among breast cancer survivors: six-month clinical trial.

Sao Paulo Med J 2021 May 10. Epub 2021 May 10.

PhD. Physical Education Professional, Postdoctoral Researcher and Adjunct Professor, Postgraduate Program on Movement Sciences and Postgraduate Program on Physiotherapy, Universidade Estadual Paulista (UNESP), Presidente Prudente (SP), Brazil.

Background: Anticancer treatment gives rise to adverse effects such as increased pain and changes to body weight and menstrual cycles, with negative effects on activities of daily living.

Objective: To analyze the effect of food orientation combined with supervised (face-to-face, FF) versus home-based (HB) aerobic training on lifestyle (food consumption and daily physical activity (PA) levels), body composition, metabolic profile and cardiorespiratory fitness, among breast cancer survivors.

Design And Setting: Clinical trial study (six months) conducted at a public university in Presidente Prudente, Brazil. Read More

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Isolation, characterization of galactose-specific lectin from Odoiporus longicollis and its antibacterial and anticancer activities.

Int J Biol Macromol 2021 May 8. Epub 2021 May 8.

Department of Zoology, University of Madras, Guindy Campus, Chennai 600 025, India. Electronic address:

Lectins are renowned hemagglutinins and multivalent proteins with a well known quality for sugar-binding specificity that participate significantly in invertebrate defense functions. Studies on biological activity of lectin from coleopteran insect are very scarce. In this study, lectin from the haemolymph in the grub of banana pest, Odoiporus longicollis was subjected to purification, biochemical and functional characterizations. Read More

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Genetic and Histopathological Alterations in Caco-2 and HuH-7 Cells Treated with Secondary Metabolites of Marine fungi.

J Gastrointest Cancer 2021 May 11. Epub 2021 May 11.

Department of Botany and Microbiology, Faculty of Science, Al-Azhar Uniersity, 11847, Nasr City, Cairo, Egypt.

The present work aimed to study the activity of naturally derived fungal secondary metabolites as anticancer agents concerning their cytotoxicity, apoptotic, genetic, and histopathological profile. It was noticed that Aspergillus terreus, Aspergillus flavus, and Aspergillus fumigatus induced variable toxic potential that was cell type, secondary metabolite type, and concentration dependent. Human colonic adenocarcinoma cells (Caco-2) showed less sensitivity than hepatocyte-derived cellular carcinoma cells (HuH-7), and in turn, the half-maximal inhibitory concentration (IC) was variable. Read More

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QSAR analysis of 3-pyrimidin-4-yl-oxazolidin-2-one derivatives isocitrate dehydrogenase inhibitors using Topomer CoMFA and HQSAR methods.

Mol Divers 2021 May 11. Epub 2021 May 11.

College of Chemistry and Chemical Engineering, Shaanxi University of Science and Technology, Xi'an, 710021, China.

A series of mIDH1 inhibitors derived from 3-pyrimidine-4-oxazolidin-2-ketone derivatives were studied by QSAR model to explore the key factors that inhibit mIDH1 activity. The generated model was cross-verified and non-cross-verified by Topomer CoMFA and HQSAR methods; the independent test set was verified by PLS method; the Topomer search technology was used for virtual screening and molecular design; and the Surflex-Dock method and ADMET technology were used for molecular docking, pharmacology and toxicity prediction of the designed drug molecules. The Topomer CoMFA and HQSAR cross-validation coefficients q are 0. Read More

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Triazole-Based Half-Sandwich Ruthenium(II) Compounds: From Antiproliferative Potential to Toxicity Evaluation.

Inorg Chem 2021 May 11. Epub 2021 May 11.

Instituto de Tecnologia Química e Biológica António Xavier, ITQB NOVA, Universidade Nova de Lisboa, Av. da República, 2780-157 Oeiras, Portugal.

A new series of half-sandwich ruthenium(II) compounds [(η-arene)Ru(L)Cl][CFSO] bearing 1,2,3-triazole ligands (arene = -cymene, L = (); arene = -cymene, L = (); arene = benzene, L = (); arene = benzene, (); = 2-[1-(-tolyl)-1-1,2,3-triazol-4-yl]pyridine and = 1,1'-di--tolyl-1,1'-4,4'-bi(1,2,3-triazole) have been synthesized and fully characterized by H and C NMR and IR spectroscopy, mass spectrometry, and elemental analysis. The molecular structures of , , and have been determined by single-crystal X-ray diffraction. The cytotoxic activity of - was evaluated using the MTS assay against human tumor cells, namely ovarian carcinoma (A2780), colorectal carcinoma (HCT116), and colorectal carcinoma resistant to doxorubicin (HCT116dox), and against normal primary fibroblasts. Read More

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Novel antimicrobial anionic cecropins from the spruce budworm feature a poly-L-aspartic acid C-terminus.

Proteins 2021 May 11. Epub 2021 May 11.

Institut de biologie intégrative et des systèmes (IBIS) and Faculté de médecine, Université Laval, Quebec City, Canada.

Cecropins form a family of amphipathic α-helical cationic peptides with broad-spectrum antibacterial properties and potent anticancer activity. The emergence of bacteria and cancer cells showing resistance to cationic antimicrobial peptides (CAMPs) has fostered a search for new, more selective and more effective alternatives to CAMPs. With this goal in mind, we looked for cecropin homologs in the genome and transcriptome of the spruce budworm, Choristoneura fumiferana. Read More

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Phenylethynylbenzyl-modified biguanides inhibit pancreatic cancer tumor growth.

Sci Rep 2021 May 10;11(1):9854. Epub 2021 May 10.

Département de Chimie-Faculté des Arts et des Sciences, Université de Montréal, 2900 Edouard Montpetit, Succursale Centre-Ville, CP 6128, Montreal, QC, H3C3J7, Canada.

We present the design and synthesis of a small library of substituted biguanidium salts and their capacity to inhibit the growth of pancreatic cancer cells. We first present their in vitro and membrane activity, before we address their mechanism of action in living cells and in vivo activity. We show that phenylethynyl biguanidium salts possess higher ability to cross hydrophobic barriers, improve mitochondrial accumulation and anticancer activity. Read More

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Bortezomib induces methylation changes in neuroblastoma cells that appear to play a significant role in resistance development to this compound.

Sci Rep 2021 May 10;11(1):9846. Epub 2021 May 10.

Department of General Pathology, Pomeranian Medical University, Powstańców Wlkp. 72, 70-111, Szczecin, Poland.

The anticancer activity of bortezomib (BTZ) has been increasingly studied in a number of indications and promising results for the use of this treatment have been shown in neuroblastoma. As BTZ treatment is usually administered in cycles, the development of resistance and side effects in patients undergoing therapy with BTZ remains a major challenge for the clinical usage of this compound. Common resistance development also means that certain cells are able to survive BTZ treatment and bypass molecular mechanisms that render BTZ anticancer activity. Read More

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Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma.

Bioorg Med Chem 2021 May 1;40:116182. Epub 2021 May 1.

College of Life Science, Nanjing Normal University, No. 1 Wenyuan Road, Nanjing 210037, PR China; Jiangsu Chia Tai Fenghai Pharmaceutical Co. Ltd., No. 9 Weidi Road, Nanjing 210046, PR China. Electronic address:

The ubiquitin proteasome pathway (UPP) plays a critical role in the maintenance of cell homeostasis and the development of diseases, such as cancer and neurodegenerative disease. A series of novel tripeptide propylene oxide compounds as proteasome inhibitors were designed, synthesized and biologically investigated in this manuscript. The enzymatic activities of final compounds against 20S human proteasome were investigated and structure-activity relationship (SAR) was summarized. Read More

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Preparation of cerium-curcumin and cerium-quercetin complexes and their LEDs irradiation assisted anticancer effects on MDA-MB-231 and A375 cancer cell lines.

Photodiagnosis Photodyn Ther 2021 May 7:102326. Epub 2021 May 7.

Department of Chemical Engineering, University of Bonab, Bonab, Iran.

Regardless of the numerous studies that have been done on cancer treatment, it is still the most challenging disease to treat especially resistance forms like triple negative breast cancer and melanoma cancer. Curcumin and quercetin as two important polyphenols from plants have different biological roles including anti-cancer effect. But their application is limited due to their poor solubility in aqueous medium. Read More

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Synthesis of messagenin and platanic acid chalcone derivatives and their biological potential.

Nat Prod Res 2021 May 10:1-10. Epub 2021 May 10.

Organic Chemistry, Martin-Luther-University Halle-Wittenberg, Halle (Saale), Germany.

The chalcone derivatives of 20-oxo-lupanes have been synthesised and screened for some types of biological activity. Ozonolysis of lupanes afforded 20-oxo-derivatives with the following condensation using different aromatic aldehydes by Claisen‒Schmidt reaction to the target compounds. The configuration of 19-[3-(pyridin-3-yl)-prop-2-en-1-one]-fragment was established by X-ray analysis. Read More

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Usnic acid suppresses cervical cancer cell proliferation by inhibiting PD-L1 expression and enhancing T-lymphocyte tumor-killing activity.

Phytother Res 2021 May 10. Epub 2021 May 10.

Molecular Medicine Research Center, College of Pharmacy, Yanbian University, Yanji, China.

The programmed cell death 1 (PD-1)/programmed death ligand 1 (PD-L1) pathway is abnormally expressed in cervical cancer cells. Moreover, PD-1/PD-L1 blockade reduces the apoptosis and exhaustion of T cells and inhibits the development of malignant tumors. Usnic acid is a dibenzofuran compound originating from Usnea diffracta Vain and has anti-inflammatory, antifungal, and anticancer activities. Read More

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Effects of Bacillus subtilis iturin A on HepG2 cells in vitro and vivo.

AMB Express 2021 May 10;11(1):67. Epub 2021 May 10.

Key Laboratory for Space Bioscience and Biotechnology, School of Life Sciences, Northwestern Polytechnical University, 127 Youyi West Road, Xi'an, 710072, Shaanxi, China.

Iturin A with cyclic peptide and fatty acid chain isolated from Bacillus subtilis fermentation shows a variety of biological activities. Among them, the anticancer activity attracted much attention. However, the molecular mechanism of its inhibitory effect on hepatocellular carcinoma was still unclear. Read More

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An improved synthesis of indanocine and antiproliferative activity of 2-benzyl-indanocine via microtubule destabilization.

Chem Biol Drug Des 2021 May 9. Epub 2021 May 9.

CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow, 226015, India.

Indanocine, a potent anticancer investigational drug of National Cancer Institute-USA has been much discussed in recent years. Present communication aimed at total synthesis of indanocine and its close analogues. Total synthesis was improved by double yields than previously reported yields. Read More

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Acetovanillone prevents cyclophosphamide-induced acute lung injury by modulating PI3K/Akt/mTOR and Nrf2 signaling in rats.

Phytother Res 2021 May 9. Epub 2021 May 9.

Physiology Division, Zoology Department, Faculty of Science, Beni-Suef University, Beni Suef, Egypt.

Cyclophosphamide (CP) is a medication used as an anticancer drug and to suppress the immune system. However, its clinical applications are restricted because of the toxic and adverse side effects. The present study investigated the protective effect of acetovanillone (AV), a natural NADPH oxidase inhibitor, against acute lung injury (ALI) induced by CP. Read More

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Cryptotanshinone Inhibits ERα-Dependent and -Independent BCRP Oligomer Formation to Reverse Multidrug Resistance in Breast Cancer.

Front Oncol 2021 22;11:624811. Epub 2021 Apr 22.

Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.

Both long-term anti-estrogen therapy and estrogen receptor-negative breast cancer contribute to drug resistance, causing poor prognosis in breast cancer patients. Breast cancer resistance protein (BCRP) plays an important role in multidrug resistance. Here, we show that cryptotanshinone (CPT), an anti-estrogen compound, inhibited the oligomer formation of BCRP on the cell membrane, thus blocking its efflux function. Read More

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Exopolysaccharides from modulates the antioxidant status of 1,2-dimethyl hydrazine-induced colon cancer rat model.

3 Biotech 2021 May 19;11(5):225. Epub 2021 Apr 19.

Department of Biotechnology, Kalasalingam Academy of Research and Education, Krishnankoil, 626126 Tamilnadu India.

The aim of the current study is to ascertain the anticancer activity of exopolysaccharides (EPS) from probiotic in the 1, 2-dimethyl hydrazine (DMH)-induced colon cancer rat model and to determine the antioxidant status. Rats were divided into five groups of six animals each. Group I served as control, group II served as cancer control (DMH alone administered), group III as standard drug control (5-FU along with DMH) and group IV and V received EPS in two doses (200 mg/kg body weight and 400 mg/kg body weight along with DMH). Read More

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Green Synthesized Silver Nanoparticles: Antibacterial and Anticancer Activities, Biocompatibility, and Analyses of Surface-Attached Proteins.

Front Microbiol 2021 22;12:632505. Epub 2021 Apr 22.

Department of Microbiology, Nicolaus Copernicus University, Toruń, Poland.

The increasing number of multi-drug-resistant bacteria and cancer cases, that are a real threat to humankind, forces research world to develop new weapons to deal with it. Biogenic silver nanoparticles (AgNPs) are considered as a solution to this problem. Biosynthesis of AgNPs is regarded as a green, eco-friendly, low-priced process that provides small and biocompatible nanostructures with antimicrobial and anticancer activities and potential application in medicine. Read More

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Determination of the antioxidant, antimicrobial and anticancer properties of the honey phenolic extract of five different regions of Bingöl province.

J Food Sci Technol 2021 Jun 22;58(6):2420-2430. Epub 2020 Sep 22.

Department of Biology, Faculty of Arts and Sciences, Bingol University, 12000 Bingol, Turkey.

Bingol is a famous region for honey in Turkey. The amount of phenolic substance is also considered important for the anticancer, antioxidant and antimicrobial properties of honey. Anticancer activity of honey extract was determined as the most effective dose of 1 mg/mL using the WST1 anti-proliferation kit in the PC-3 cell line. Read More

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Exploration of nutritional, antioxidative, antibacterial and anticancer status of : towards valorization of a traditionally preferred unique myco-food.

J Food Sci Technol 2021 Jun 19;58(6):2133-2147. Epub 2020 Aug 19.

Molecular and Applied Mycology and Plant Pathology Laboratory, Centre of Advanced Study, Department of Botany, University of Calcutta, 35, Ballygunge Circular Road, Kolkata, West Bengal 700019 India.

Healthy food trend is becoming popular these days fueling search for ingredients empowered by pharma-nutritional benefits. In contrast, numerous wild-growing mushrooms are traditionally cherished as health promoting gastronomies in India; although credibility of their effects has so far been limited. Hence the present study aimed to unveil a unique tribal cuisine, , with nutritional, chemical and pharmacological relevance. Read More

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The kinetics and release behaviour of curcumin loaded pH-responsive PLGA/chitosan fibers with antitumor activity against HT-29 cells.

Carbohydr Polym 2021 Aug 15;265:118077. Epub 2021 Apr 15.

School of Chemistry and Chemical Engineering, Hefei University of Technology, 230009, Hefei, Anhui, PR China; Anhui Institute of Agro-Products Intensive Processing Technology, 230009, Hefei, Anhui, PR China. Electronic address:

The bioavailability and clinical effect of curcumin (Cur) are greatly restricted due to its physicochemical instability and high hydrophobicity. To overcome the disadvantages, the nanofibers of poly(lactide-glycolide)/chitosan loaded with Cur (PLGA/CS/Cur) was developed here by electrospinning technique for controlled Cur delivery. The incorporated Cur was well-dispersed and maintained crystalline form in PLGA/CS fiber matrix by hydrogen bonding. Read More

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Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells.

Bioorg Med Chem 2021 Apr 30;40:116187. Epub 2021 Apr 30.

Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address:

Carboxylesterase 2 (CES2) is one of the most important Phase I drug metabolizing enzymes in the carboxylesterase family. It plays crucial roles in the bioavailability of oral ester prodrugs and the therapeutic effect of some anticancer drugs such as irinotecan (CPT11) and capecitabine. In addition to the well-known roles of CES2 in xenobiotic metabolism, the enzyme also participates in endogenous metabolism and the production of lipids. Read More

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A study on MAPK/ERK and CDK2-Cyclin-E signal switch "on and off" in cell proliferation by bis urea derivatives of 1, 4-Diisocyanatobenzene.

Bioorg Chem 2021 Apr 23;112:104940. Epub 2021 Apr 23.

Department of Chemistry, Sri Venkateswara Arts College (TTD's), Sri Venkateswara University, Tirupati, Andhra Pradesh, India. Electronic address:

A series of novel substituted bisurea 1,4-Diisocyanatobenzene compounds were designed, synthesized and introduced as potent anticancer compounds and screened for their in vitro anti-proliferative activities in human cancer cell lines. The structures of all titled compounds were characterized using Fourier-transform infrared mass spectra, nuclear magnetic resonance spectroscopy, elemental analysis and evaluated their sustainability using biological experiments. A selected group of ten derivatives were apprised for their anti-proliferative activity. Read More

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Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization.

Bioorg Med Chem Lett 2021 May 6:128095. Epub 2021 May 6.

School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address:

Human esophageal squamous cell carcinoma (ESCC) is one of the most lethal cancers in human digestive system. It is necessary to discover novel antitumor agents for the treatment of esophageal cancers because of its poor prognosis. Indoline has been reported as an efficient anticancer fragment to design novel anticancer agents. Read More

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In vitro and in vivo combinatorial anticancer effects of oxaliplatin- and resveratrol-loaded N,O-carboxymethyl chitosan nanoparticles against colorectal cancer.

Eur J Pharm Sci 2021 May 6:105864. Epub 2021 May 6.

Department of Gastroenterology, Renmin Hospital of Wuhan University, Wuhan, Hubei Province, 430060, China. Electronic address:

Background: Oxaliplatin (OXE) combined with other chemotherapy drugs against colorectal cancer had been reported in the literature before, however, the efficacy of oxaliplatin combined with natural compounds was elusive. In addition, the clinical bioactivity and therapeutic dose of antitumor drugs are severely limited due to poor targeting and side effects. NDDSs offers an excellent strategy to overcome the disadvantages of small molecule anticancer drugs. Read More

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Exploiting the metabolic energy demands of drug efflux pumps provides a strategy to overcome multidrug resistance in cancer.

Biochim Biophys Acta Gen Subj 2021 May 6:129915. Epub 2021 May 6.

Human Disease and Membrane Transport Laboratory, Division of Biomedical Science & Biochemistry, Research School of Biology and Medical School, The Australian National University, Canberra 2601, Australia. Electronic address:

Background: P-glycoprotein (P-gp) is a prevalent resistance mediator and it requires considerable cellular energy to ensure ATP dependent efflux of anticancer drugs. The glycolytic pathway generates the majority of catabolic energy in cancer cells; however, the high rates of P-gp activity places added strain on its inherently limited capacity to generate ATP. This is particularly relevant for compounds such as verapamil that are believed to trap P-gp in a futile transport process that requires continuing ATP consumption. Read More

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The antiandrogenic effect of neferine, liensinine, and isoliensinine by inhibiting 5-α-reductase and androgen receptor expression via PI3K/AKT signaling pathway in prostate cancer.

Pharmazie 2021 May;76(5):225-231

School of Medicine, Yichun University, Yichun, China.

Neferine, liensinine, and isoliensinine are bisbenzylisoquinoline alkaloids extracted from seed-embryos of Gaertn. In this study, we evaluated the anticancer activities and mechanism of action of these natural products in prostate cancer cells by MTT, wound healing, ELISA and Western blotting. Neferine, liensinine, and isoliensinine showed growth inhibition and displayed a significant anti-migration activity in prostate cancer cells. Read More

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