136,332 results match your criteria anticancer

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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Stability study of concentrate-solvent mixture & infusion solutions of Jevtana® cabazitaxel for extended multi-dosing.

J Oncol Pharm Pract 2021 May 12:10781552211016079. Epub 2021 May 12.

Department of Pharmacy & Pharmacology, Antoni van Leeuwenhoek Hospital, Netherlands Cancer Institute, Amsterdam, The Netherlands.

Aim/background: In this study, the prolonged physical and chemical stability of the anticancer agent cabazitaxel, commercially available as Jevtana®, was examined. Both concentrate-solvent mixture and infusion solution were examined with the aim to extend the use of multidose left-over cabazitaxel and infusion solutions and with that reduce financial and environmental waste.

Methods: A validated stability-indicating high-pressure liquid chromatography (HPLC) method with ultraviolet (UV) and photodiode array (PDA) detection was used to examine the purity and any degradation of cabazitaxel. Read More

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Generation of Patient-Derived Colorectal Cancer Organoids for RAS Studies.

Methods Mol Biol 2021 ;2262:349-360

Charité Comprehensive Cancer Center, Charité Universitätsmedizin Berlin, Berlin, Germany.

Human cell line models have been widely used for testing of novel anticancer compounds and for predicting clinical response to monotherapies and combinatorial therapies. For many years, standard monolayer culture conditions were used as gold standard, only surpassed by in vivo testing of mouse models. Recently, the incorporation of three-dimensional culture has been shown to further improve predictive compound testing. Read More

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January 2021

Cannabinoid WIN 55,212-2 Inhibits Human Glioma Cell Growth by Triggering ROS-Mediated Signal Pathways.

Biomed Res Int 2021 22;2021:6612592. Epub 2021 Apr 22.

Postdoctoral Workstation, Taian City Central Hospital, Tai'an, Shandong 271000, China.

Glioblastoma is a highly invasive primary malignant tumor of the central nervous system. Cannabinoid analogue WIN 55,212-2 (WIN) exhibited a novel anticancer effect against human tumors. However, the anticancer potential and underlying mechanism of WIN against human glioma remain unclear. Read More

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Near-infrared absorbing Ru(ii) complexes act as immunoprotective photodynamic therapy (PDT) agents against aggressive melanoma.

Chem Sci 2020 Nov 9;11(43):11740-11762. Epub 2020 Sep 9.

Department of Chemistry and Biochemistry, The University of Texas at Arlington Arlington Texas 76019-0065 USA

Mounting evidence over the past 20 years suggests that photodynamic therapy (PDT), an anticancer modality known mostly as a local treatment, has the capacity to invoke a systemic antitumor immune response, leading to protection against tumor recurrence. For aggressive cancers such as melanoma, where chemotherapy and radiotherapy are ineffective, immunomodulating PDT as an adjuvant to surgery is of interest. Towards the development of specialized photosensitizers (PSs) for treating pigmented melanomas, nine new near-infrared (NIR) absorbing PSs based on a Ru(ii) tris-heteroleptic scaffold [Ru(NNN)(NN)(L)]Cl , were explored. Read More

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November 2020

Oridonin inhibits tumor angiogenesis and induces vessel normalization in experimental colon cancer.

J Cancer 2021 2;12(11):3257-3264. Epub 2021 Apr 2.

Department of Oncology, Shanxi Province Academy of Traditional Chinese Medicine, Shanxi Province Hospital of Traditional Chinese Medicine, Taiyuan, Shanxi 030012, China.

Tumor blood vessels exhibit morphological and functional aberrancies. Its maturity and functionality are closely associated with colon cancer progression and therapeutic efficacy. The direct evidence proving whether oridonin (ORI) has vascular normalization promoting effect from which combination therapies will benefit is still lacking. Read More

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Protective Effects of Silymarin Against D-Gal/LPS-Induced Organ Damage and Inflammation in Mice.

Drug Des Devel Ther 2021 4;15:1903-1914. Epub 2021 May 4.

Chongqing Collaborative Innovation Center for Functional Food, Chongqing University of Education, Chongqing, 400067, People's Republic of China.

Aim: Silymarin contains various flavonoids and exhibits antioxidative, anti-inflammatory, and anticancer effects, in addition to other pharmacological properties. This study explored the alleviating effect of silymarin on multiple-organ damage induced by D-galactose/lipopolysaccharide in Kunming mice.

Methods: Kunming mice were injected intraperitoneally with D-galactose (30 mg/kg·BW)/LPS (3 μg/kg·BW) and then treated using silymarin with different doses (75 mg/kg·bw and 150 mg/kg·bw) via intragastric administration. Read More

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Acute toxicity analysis of an inhibitor of BCL2, Disarib, in rats.

Sci Rep 2021 May 11;11(1):9982. Epub 2021 May 11.

Institute of Bioinformatics and Applied Biotechnology, Electronics City, Bangalore, 560100, India.

Apoptosis or programmed cell death is a highly regulated process, which eliminates unwanted and damaged cells. Inhibition of apoptosis is a hallmark of cancer cells. BCL2 family proteins are known to play a vital role in the regulation of apoptosis. Read More

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[A Case of Liver Metastasis of Colorectal Cancer in a Hemodialysis Patient, Underwent Liver Resection and Chemotherapy after Colorectal Resection].

Gan To Kagaku Ryoho 2021 Apr;48(4):552-554

Dept. of Surgery, Ako City Hospital.

A 60 years old man has undergone hemodialysis due to chronic renal failure by diabetic nephropathy. A sigmoid colon cancer and multiple liver metastases(S2, S6)were found, and he had laparoscopic sigmoid colon resection first, it was local resection. The stage was pT3N2aH1, stage Ⅳ, and histopathological examination revealed that the tumor was well‒differentiated adenocarcinoma and RAS, BRAF mutation was negative. Read More

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Modulation of Liver P-Glycoprotien Expression May Contribute to Gossypin Protection against Methotrexate-Induced Hepatotoxicity.

Indian J Pharmacol 2021 Jan-Feb;53(1):25-30

Department of Histology, Faculty of Medicine, Minia University, Minya, Egypt.

Objectives: Methotrexate (MTX) is a broadly used anticancer. Its major side effect is hepatotoxicity. Gossypin is a flavonoid has a hepatoprotective effect as well as antitumor property. Read More

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Synergistic effect of the anti-PD-1 antibody with blood stable and reduction sensitive curcumin micelles on colon cancer.

Drug Deliv 2021 Dec;28(1):930-942

Department of Cell Biology, School of Basic Medical Sciences, Southern Medical University, Guangzhou, China.

Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is a potent anticancer drug with versatile biological activities, while the clinical translation of curcumin is severely limited due to its hydrophobicity, rapid elimination, and metabolism in the blood circulation. Herein, we aim to unravel the potential of curcumin as a synergistic agent with immunotherapy in the treatment of cancers. In an effort to minimize premature release and improve the systemic bioavailability, a superior blood stable and reduction sensitive curcumin micellar formulation, of which the release can be triggered by cancer cells, is rationally designed. Read More

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December 2021

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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Glutathione-Depleting Nanomedicines for Synergistic Cancer Therapy.

ACS Nano 2021 May 11. Epub 2021 May 11.

State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, 2 Sipailou Road, Nanjing 210096, P.R. China.

Cancer cells frequently exhibit resistance to various molecular and nanoscale drugs, which inevitably affects the drugs' therapeutic outcomes. Overexpression of glutathione (GSH) has been observed in many cancer cells, and solid evidence has corroborated the resulting tumor resistance to a variety of anticancer therapies, suggesting that this biochemical characteristic of cancer cells can be developed as a potential target for cancer treatments. The single treatment of GSH-depleting agents can potentiate the responses of the cancer cells to different cell death stimuli; therefore, as an adjunctive strategy, GSH depletion is usually combined with mainstream cancer therapies for enhancing the therapeutic outcomes. Read More

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Prediction of Synthetic Lethal Interactions in Human Cancers using Multi-view Graph Auto-Encoder.

IEEE J Biomed Health Inform 2021 May 11;PP. Epub 2021 May 11.

Synthetic lethality (SL) is a very important concept for the development of targeted anticancer drugs. However, experimental methods for SL detection often suffer from various issues like high cost and low consistency across cell lines. Hence, computational methods for predicting novel SLs have recently emerged as complements for wet-lab experiments. Read More

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Structure-Guided Design of the First Noncovalent Small-Molecule Inhibitor of CRM1.

J Med Chem 2021 May 11. Epub 2021 May 11.

Department of Pathology, State Key Laboratory of Biotherapy and Cancer Centre, West China Hospital, Sichuan University and Collaborative Innovation Centre of Biotherapy, Chengdu 610041, China.

Nuclear export factor chromosome region maintenance 1 (CRM1) is an attractive anticancer and antiviral drug target that spurred several research efforts to develop its inhibitor. Noncovalent CRM1 inhibitors are desirable, but none is reported to date. Here, we present the crystal structure of yeast CRM1 in complex with S109, a substructure of CBS9106 (under clinical test). 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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Primary Macrophage-Based Microrobots: An Effective Tumor Therapy by Dual-Targeting Function and Near-Infrared-Triggered Drug Release.

ACS Nano 2021 May 11. Epub 2021 May 11.

School of Mechanical Engineering, Chonnam National University, 77 Yongbong-ro, Buk-gu, Gwangju 61186, Korea.

Macrophages (MΦs) have the capability to sense chemotactic cues and to home tumors, therefore presenting a great approach to engineer these cells to deliver therapeutic agents to treat diseases. However, current cell-based drug delivery systems usually use commercial cell lines that may elicit an immune response when injected into a host animal. Furthermore, premature off-target drug release also remains an enormous challenge. 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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Bioorthogonal catalytic patch.

Nat Nanotechnol 2021 May 10. Epub 2021 May 10.

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, P. R. China.

Bioorthogonal catalysis mediated by transition metals has inspired a new subfield of artificial chemistry complementary to enzymatic reactions, enabling the selective labelling of biomolecules or in situ synthesis of bioactive agents via non-natural processes. However, the effective deployment of bioorthogonal catalysis in vivo remains challenging, mired by the safety concerns of metal toxicity or complicated procedures to administer catalysts. Here, we describe a bioorthogonal catalytic device comprising a microneedle array patch integrated with Pd nanoparticles deposited on TiO nanosheets. Read More

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Randomised Phase 1b/2 trial of tepotinib vs sorafenib in Asian patients with advanced hepatocellular carcinoma with MET overexpression.

Br J Cancer 2021 May 10. Epub 2021 May 10.

Medical Oncology Department, PLA Cancer Center, Nanjing Bayi Hospital, Nanjing, China.

Background: This open-label, Phase 1b/2 study evaluated the highly selective MET inhibitor tepotinib in systemic anticancer treatment (SACT)-naive Asian patients with advanced hepatocellular carcinoma (aHCC) with MET overexpression.

Methods: In Phase 2b, tepotinib was orally administered once daily (300, 500 or 1,000 mg) to Asian adults with aHCC. The primary endpoints were dose-limiting toxicities (DLTs) and adverse events (AEs). Read More

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RRx-001 ameliorates inflammatory diseases by acting as a potent covalent NLRP3 inhibitor.

Cell Mol Immunol 2021 May 10. Epub 2021 May 10.

Hefei National Laboratory for Physical Sciences at Microscale, the CAS Key Laboratory of Innate Immunity and Chronic Disease, School of Basic Medical Sciences, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, China.

The NLRP3 inflammasome plays a crucial role in innate immune-mediated inflammation and contributes to the pathogenesis of multiple autoinflammatory, metabolic and neurodegenerative diseases, but medications targeting the NLRP3 inflammasome are not available for clinical use. RRx-001 is a well-tolerated anticancer agent currently being investigated in phase III clinical trials, but its effects on inflammatory diseases are not known. Here, we show that RRx-001 is a highly selective and potent NLRP3 inhibitor that has strong beneficial effects on NLRP3-driven inflammatory diseases. 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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The Role of Gut Microbiota in Modulatin Tumor Growth and Anticancer Agent Efficacy.

Mol Cells 2021 Apr 23. Epub 2021 Apr 23.

Graduate School of Medical Science and Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 34141, Korea.

An increasing number of studies have revealed an interaction between gut microbiota and tumors. The enrichment of specific bacteria strains in the intestines has been found to modulate tumor growth and influence the mechanisms of tumor treatment. Various bacteria are involved in modulating the effects of chemotherapeutic drugs currently used to treat patients with cancer, and they affect not only gastrointestinal tract tumors but also distant organ tumors. Read More

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