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https://www.readbyqxmd.com/read/28544162/benzimidazole-scaffold-as-anticancer-agent-synthetic-approaches-and-structure-activity-relationship
#1
REVIEW
Neelima Shrivastava, Mohd Javed Naim, Md Jahangir Alam, Farah Nawaz, Shujauddin Ahmed, Ozair Alam
Cancer, also known as malignant neoplasm, is a dreadful disease which involves abnormal cell growth having the potential to invade or spread to other parts of the body. Benzimidazole is an organic compound that is heterocyclic and aromatic in nature. It is a bicyclic compound formed by the fusion of the benzene and imidazole ring systems. It is an important pharmacophore and a privileged structure in medicinal chemistry. According to the World Health Organisation (2015 survey), one in six deaths is due to cancer around the globe, accounting for 8...
May 22, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28539711/flavonoids-isolated-from-the-flowers-of-limonium-bicolor-and-their-in-vitro-antitumor-evaluation
#2
Jian Chen, Jiehui Teng, Li Ma, Haiying Tong, Bingru Ren, Linshan Wang, Weilin Li
BACKGROUND: Limonium bicolor, a halophytic species, can grow in saline or saline-alkali soil, is well known as a traditional Chinese medicine. Recently it attracted much attention for its treatment for cancer. OBJECTIVE: The present study was performed to evaluate this species from the phytochemical standpoint and the possible relationship between the antitumor activity and its natural products. MATERIALS AND METHODS: The chemical constituents from the flowers of L...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28537720/chromone-as-a-privileged-scaffold-in-drug-discovery-recent-advances
#3
Joana Reis, Alexandra Gaspar, Nuno Milhazes, Fernanda M Borges
The use of privileged structures in drug discovery has proven to be an effective strategy allowing the generation of innovative hits/leads and successful optimization processes. Chromone is actually recognized as a privileged structure and a valid template for the design of novel compounds with potential pharmacological interest, particularly in the field of neurodegenerative, inflammatory and infectious diseases as well as diabetes and cancer. Within this framework, this review provides the reader with a literature update following the preceding article entitled Chromone: a valid scaffold in Medicinal Chemistry...
May 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28534965/cucurbitacin%C3%A2-b-induces-autophagy-and-apoptosis-by-suppressing-cip2a-pp2a-mtorc1-signaling-axis-in-human-cisplatin-resistant-gastric-cancer-cells
#4
Xuewen Liu, Chao Duan, Juanli Ji, Te Zhang, Xiaoning Yuan, Yunfei Zhang, Wenjing Ma, Jingyuan Yang, Linsen Yang, Zhiguo Jiang, Huiliang Yu, Ying Liu
Cancerous inhibitor of protein phosphatase 2A (CIP2A) is a human oncoprotein that is overexpressed in multiple kinds of tumors including gastric cancer (GC). Mammalian target of rapamycin complex 1 (mTORC1) over-activation is detected in GC and many other cancers. Previous study found that CIP2A/mTORC1 controls cell growth and autophagy through direct association. CIP2A plays an 'oncogenic nexus' in several cancer types to participate in the tumorigenic transformation and chemoresistance. In the present study, we investigated whether Cucurbitacin B (CuB), a natural compound found in Cucurbitaceae, can be used in cisplatin (DDP)-resistant human GC cell line SGC7901/DDP...
May 18, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28534825/a-novel-combination-of-withaferin-a-and-sulforaphane-inhibits-epigenetic-machinery-cellular-viability-and-induces-apoptosis-of-breast-cancer-cells
#5
Kendra J Royston, Neha Udayakumar, Kayla Lewis, Trygve O Tollefsbol
With cancer often classified as a disease that has an important epigenetic component, natural compounds that have the ability to regulate the epigenome become ideal candidates for study. Humans have a complex diet, which illustrates the need to elucidate the mechanisms of interaction between these bioactive compounds in combination. The natural compounds withaferin A (WA), from the Indian winter cherry, and sulforaphane (SFN), from cruciferous vegetables, have numerous anti-cancer effects and some report their ability to regulate epigenetic processes...
May 19, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28533126/sonodynamic-therapy-combined-with-novel-anti-cancer-agents-sanguinarine-and-ginger-root-extract-synergistic-increase-in-toxicity-in-the-presence-of-panc-1-cells-in-vitro
#6
Matthew Prescott, James Mitchell, Stella Totti, Judy Lee, Eirini Velliou, Madeleine Bussemaker
The presence of ultrasound-induced cavitation in sonodynamic therapy (SDT) treatments has previously enhanced the activity and delivery of certain sonosensitisers in biological systems. The purpose of this work was to investigate the potential for two novel anti-cancer agents from natural derivatives, sanguinarine and ginger root extract (GRE), as sonosensitisers in an SDT treatment with in vitro PANC-1 cells. Both anti-cancer compounds had a dose-dependent cytotoxicity in the presence of PANC-1 cells. A range of six discreet ultrasound power-frequency configurations were tested and it was found that the cell death caused directly by ultrasound was likely due to the sonomechanical effects of cavitation...
May 13, 2017: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/28531803/isofraxidin-inhibited-proliferation-and-induced-apoptosis-via-blockage-of-akt-pathway-in-human-colorectal-cancer-cells
#7
Peng Shen, Hong-Gang Wang, Miao-Miao Li, Qian-Yun Ma, Chuan-Wen Zhou, Feng Pan, Rui Xie
BACKGROUND: Isofraxidin (IF), a natural coumarin compound, has been reported to possess anti-cancer activity in human liver cancer. However, whether IF is involved in the regulation of colorectal cancer tumorigenesis and development has been not well elucidated. METHODS: The cell proliferation were assessed by Cell Counting Kit-8 (CCK-8) and colony formation test, respectively. The transwell assays were conducted to estimate cell migration and invasion abilities...
May 19, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28531112/effects-of-polyphenols-on-oxidative-stress-mediated-injury-in-cardiomyocytes
#8
REVIEW
Rosanna Mattera, Monica Benvenuto, Maria Gabriella Giganti, Ilaria Tresoldi, Francesca Romana Pluchinotta, Sonia Bergante, Guido Tettamanti, Laura Masuelli, Vittorio Manzari, Andrea Modesti, Roberto Bei
Cardiovascular diseases are the main cause of mortality and morbidity in the world. Hypertension, ischemia/reperfusion, diabetes and anti-cancer drugs contribute to heart failure through oxidative and nitrosative stresses which cause cardiomyocytes nuclear and mitochondrial DNA damage, denaturation of intracellular proteins, lipid peroxidation and inflammation. Oxidative or nitrosative stress-mediated injury lead to cardiomyocytes apoptosis or necrosis. The reactive oxygen (ROS) and nitrogen species (RNS) concentration is dependent on their production and on the expression and activity of anti-oxidant enzymes...
May 20, 2017: Nutrients
https://www.readbyqxmd.com/read/28530610/saponins-in-pulses-and-their-health-promoting-activities-a-review
#9
REVIEW
Balwinder Singh, Jatinder Pal Singh, Narpinder Singh, Amritpal Kaur
Saponins are a class of natural compounds present in pulses having surface active properties. These compounds show variation in type, structure and composition of their aglycone moiety and oligosaccharide chains. Saponins have plasma cholesterol lowering effect in humans and are important in reducing the risk of many chronic diseases. Moreover, they have shown strong cytotoxic effects against cancer cell lines. However, more epidemiological and clinical studies are required for the proper validation of these health promoting activities...
October 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28530545/synthesis-and-biological-evaluation-of-curcumin-nitroxide-based-molecular-hybrids-as-antioxidant-and-anti-proliferative-agents
#10
Balázs Bognár, Muthulakshmi Kuppusamy, Esha Madan, Tamás Kálai, Mária Balog, József Jekő, Periannan Kuppusamy, Kálmán Hideg
BACKGROUND: Natural products and their derivatives are widely used to treat cancer and other diseases associated with ROS- and RNS-induced damages. METHODS: A series of paramagnetic modified curcumin analogues and 3,5-diarylidene-piperidones (DAP) have been designed, synthesized, and characterized on their anti-proliferative and antioxidant activity. RESULTS: Biological characterization of the new compounds supported the earlier results that incorporation of a nitroxide moiety or its precursor into curcumin or diarylidenylpiperidone (DAP) scaffolds resulted in anti-proliferative effect toward cancerous cell-lines in case of aryl hydroxy and/or methoxy substituent containing derivatives suggesting their potential for targeted therapeutic applications...
May 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28529596/andrographolide-induces-apoptotic-and-non-apoptotic-death-and-enhances-tumor-necrosis-factor-related-apoptosis-inducing-ligand-mediated-apoptosis-in-gastric-cancer-cells
#11
Sung-Chul Lim, Ho Jong Jeon, Keun Hong Kee, Mi Ja Lee, Ran Hong, Song Iy Han
Andrographolide, a natural compound isolated from Andrographis paniculata, has been reported to possess antitumor activity. In the present study, the effect of andrographolide in human gastric cancer (GC) cells was investigated. Andrographolide induced cell death with apoptotic and non-apoptotic features. At a low concentration, andrographolide potentiated apoptosis and reduction of clonogenicity triggered by recombinant human tumor necrosis factor-related apoptosis-inducing ligand (rhTRAIL). Exposure of GC cells to andrographolide altered the expression level of several growth-inhibiting and apoptosis-regulating proteins, including death receptors...
May 2017: Oncology Letters
https://www.readbyqxmd.com/read/28527578/tr2-and-tr4-orphan-nuclear-receptors-an-overview
#12
Shin-Jen Lin, Dong-Rong Yang, Guosheng Yang, Chang-Yi Lin, Hong-Chiang Chang, Gonghui Li, Chawnshang Chang
Testicular nuclear receptors 2 and 4 (TR2, TR4), also known as NR2C1 and NR2C2, belong to the nuclear receptor superfamily and were first cloned in 1989 and 1994, respectively. Although classified as orphan receptors, several natural molecules, their metabolites, and synthetic compounds including polyunsaturated fatty acids (PUFAs), PUFA metabolites 13-hydroxyoctadecadienoic acid, 15-hydroxyeicosatetraenoic acid, and the antidiabetic drug thiazolidinediones can transactivate TR4. Importantly, many of these ligands/activators can also transactivate peroxisome proliferator-activated receptor gamma (PPARγ), also known as NR1C3 nuclear receptor...
2017: Current Topics in Developmental Biology
https://www.readbyqxmd.com/read/28526832/identification-of-a-novel-chalcone-derivative-that-inhibits-notch-signaling-in-t-cell-acute-lymphoblastic-leukemia
#13
Mattia Mori, Luca Tottone, Deborah Quaglio, Nadezda Zhdanovskaya, Cinzia Ingallina, Marisa Fusto, Francesca Ghirga, Giovanna Peruzzi, Maria Elisa Crestoni, Fabrizio Simeoni, Francesca Giulimondi, Claudio Talora, Bruno Botta, Isabella Screpanti, Rocco Palermo
Notch signaling is considered a rational target in the therapy of several cancers, particularly those harbouring Notch gain of function mutations, including T-cell acute lymphoblastic leukemia (T-ALL). Although currently available Notch-blocking agents are showing anti-tumor activity in preclinical studies, they are not effective in all the patients and often cause severe side-effects, limiting their widespread therapeutic use. Here, by functional and biological analysis of the most representative molecules of an in house library of natural products, we have designed and synthetized the chalcone-derivative 8 possessing Notch inhibitory activity at low micro molar concentration in T-ALL cell lines...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526637/identification-and-biological-activity-of-the-volatile-compounds-of-glycyrrhiza-triphylla-fisch-c-a-mey
#14
Abolfazl Shakeri, Javad Akhtari, Vahid Soheili, Seyedeh Faezeh Taghizadeh, Amirhossein Sahebkar, Rezvan Shaddel, Javad Asili
Chemical composition and biological (antimicrobial, antioxidant and cytotoxic) activities of essential oils (EO) obtained from the aerial parts of Glycyrrhiza triphylla Fisch. & C.A.Mey (G. triphylla) were evaluated in the present study. The EO was isolated and analyzed using gas chromatography-mass spectrometry (GC-MS). Fifty-five compounds representing 99.3% of the total oil composition were identified. Major components of the oil were β-caryophyllene (25.4%), limonene (16.7%), β-myrcene (16.0%) and α-humulene (4...
May 16, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28525533/phenol-concentrations-during-childhood-and-subsequent-measures-of-adiposity-among-young-girls
#15
Andrea L Deierlein, Mary S Wolff, Ashley Pajak, Susan M Pinney, Gayle C Windham, Maida P Galvez, Michael Rybak, Antonia M Calafat, Lawrence H Kushi, Frank M Biro, Susan L Teitelbaum
Phenolic compounds represent a class of environmental chemicals with potential endocrine disrupting capabilities. We investigated longitudinal associations of childhood exposures to phenols, from both man-made and natural sources, and subsequent measures of adiposity among girls enrolled in The Breast Cancer and Environment Research Program, 2004-2007. Baseline (ages 6-8 years) urinary concentrations were obtained for creatinine and phenol metabolites: enterolactone, genistein, daidzein, benzophenone-3, bisphenol A, sum of parabens (methyl, ethyl, and propyl parabens), 2,5-dichlorophenol, and triclosan...
May 19, 2017: American Journal of Epidemiology
https://www.readbyqxmd.com/read/28523727/synthesis-and-antineoplastic-evaluation-of-mitochondrial-complex-ii-succinate-dehydrogenase-inhibitors-derived-from-atpenin-a5
#16
Hezhen Wang, Bader Huwaimel, Kshitij Verma, James Miller, Todd Germain, Nihar Kinarivala, Dimitri Pappas, Paul Brookes, Paul Charles Trippier
Mitochondrial complex II (CII) is an emerging target for numerous human diseases. Sixteen analogues of the CII inhibitor natural product atpenin A5 were prepared to evaluate the structure-activity relationship of the C-5 pyridine side chain. The side chain ketone moiety was determined to be pharmacophoric, engendering a bioactive conformation. Analogue 16c displayed CII IC50 = 64 nM, retained selectivity for CII over mitochondrial complex I (>156-fold) and possessed a ligand-lipophilicity efficiency of 5...
May 18, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28522265/screening-for-bioactive-natural-products-from-a-67-compound-library-of-glycyrrhiza-inflata
#17
Yan Lin, Yi Kuang, Kai Li, Shuang Wang, Wei Song, Xue Qiao, Gulnar Sabir, Min Ye
Licorice shows a variety of pharmacological activities. This work aims to discover bioactive natural products from one botanical source of licorice, Glycyrrhiza inflata. A total of 67 free phenolics were isolated to form a compound library. Based on the bioactivities of licorice, these compounds were screened using cell- or enzyme-based bioassay methods. A total of 11 compounds exhibited potent cytotoxic activities against three human cancer cell lines (HepG2, SW480 and MCF7), while showed little toxicity on human normal cell lines LO2 and HEK293T...
May 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28518408/s-adenosylmethionine-mediated-apoptosis-is-potentiated-by-autophagy-inhibition-induced-by-chloroquine-in-human-breast-cancer-cells
#18
Donatella Delle Cave, Vincenzo Desiderio, Laura Mosca, Concetta Paola Ilisso, Luigi Mele, Michele Caraglia, Giovanna Cacciapuoti, Marina Porcelli
The naturally-occurring sulfonium compound S-adenosyl-L-methionine (AdoMet) is an ubiquitous sulfur-nucleoside that represents the main methyl donor in numerous methylation reactions. In recent years, it has been shown that AdoMet possesses antiproliferative properties in various cancer cells, but the molecular mechanisms at the basis of the effect induced by AdoMet have been only in part investigated. In the present study, we found that AdoMet strongly inhibited the proliferation of breast cancer cells MCF-7 by inducing both autophagy and apoptosis...
May 18, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28515374/polyphyllin-i-overcomes-emt-associated%C3%A2-resistance%C3%A2-to-erlotinib-in-lung-cancer-cells-via-il-6-stat3-pathway-inhibition
#19
Wei Lou, Yan Chen, Ke-Ying Zhu, Huizi Deng, Tianhao Wu, Jun Wang
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) is the most important limiting factor for treatment efficiency in EGFR-mutant non-small cell lung cancer (NSCLC). Much work has linked the epithelial-mesenchymal transition (EMT) to the emergence of drug resistance, consequently, ongoing research has been focused on exploring the therapeutic options to reverse EMT for delaying or preventing drug resistance. Polyphyllin I (PPI) is a natural compound isolated from Paris polyphylla rhizomes and displayed anti-cancer properties...
May 18, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28514834/antitumor-activity-of-brazilian-red-propolis-fractions-against-hep-2-cancer-cell-line
#20
Caroline Olivieri da Silva Frozza, Denis Amilton Santos, Luciane Corbellini Rufatto, Luciane Minetto, Fernando Joel Scariot, Sergio Echeverrigaray, Claus Tröger Pich, Sidnei Moura, Francine Ferreira Padilha, Sibele Borsuk, Lucielli Savegnago, Tiago Collares, Fabiana Kömmling Seixas, Odir Dellagostin, Mariana Roesch-Ely, João Antonio Pêgas Henriques
Continuous increases in the rates of tumor diseases have highlighted the need for identification of novel and inexpensive antitumor agents from natural sources. In this study, we investigated the effects of enriched fraction from hydroalcoholic Brazilian red propolis extract against Hep-2 cancer cell line. Initially 201 fractions were arranged in 12 groups according to their chromatographic characteristics (A-L). After an in vitro cell viability screening, J and L were further selected as promising enriched fractions for this study...
May 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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