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bioactive compounds

Enxiang Zhang, Shutao Yin, Xiaotong Lu, Linhu Ye, Lihong Fan, Hongbo Hu
Glycycoumarin (GCM) is a representative of bioactive coumarin compounds isolated from licorice, an edible and medicinal plant widely used for treating various diseases including liver diseases. The purpose of the present study is to examine the possibility of GCM as a sensitizer to improve the efficacy of BH3 mimetic ABT-737 against liver cancer. Three liver cancer cell lines (HepG2, Huh-7 and SMMC-7721) were used to evaluate the in vitro combinatory effect of ABT-737/GCM. HepG2 xenograft model was employed to assess the in vivo efficacy of ABT-737/GCM combination...
March 15, 2018: Nutrients
Behjat Javadi
Cancer is the second leading cause of death with profound socio-economic consequences worldwide. Growing evidence suggests the crucial role of diet on cancer prevention and treatment. In Traditional Persian Medicine (TPM) there is a major focus on contribution of special diet and foods to cancer management. In the present article, the cytotoxic and antitumor activities of several food items including plants and animal products recommended by TPM as anticancer agents are discussed. Strong evidence supports the anticancer effects of beetroot (Beta vulgris) and its major compound betanin, cinnamon and cinnamaldehyde, barley (H...
March 15, 2018: Nutrition and Cancer
V C Graça, Maria Inês Dias, Lillian Barros, Ricardo C Calhelha, P F Santos, Isabel C F R Ferreira
Geranium molle L., commonly known as Dove's-foot Crane's-bill or Dovesfoot Geranium, is an herbaceous plant belonging to the Geraniaceae family. Contrary to many other Geranium species, the bioactivity and the phytochemical composition of G. molle seem not to have attracted attention until a recent study from our group regarding the bioactivity of several aqueous and organic extracts of the plant. In particular, we assessed the cytotoxic activity of these extracts against several human tumor cell lines (breast, lung, cervical and hepatocellular carcinomas) and a non-tumor porcine liver primary cell line, inspired by an ethnopharmacological report describing the traditional use of this medicinal plant in some regions of Northeast Portugal for the treatment of cancer...
March 15, 2018: Food & Function
Ren-You Gan, Kin-Weng Kong, Hua-Bin Li, Kao Wu, Ying-Ying Ge, Chak-Lun Chan, Xian-Ming Shi, Harold Corke
The red sword bean ( Canavalia gladiata ) is an underutilized edible bean cultivated in China. It was previously found to have the highest content of antioxidant polyphenols among 42 edible beans, mainly gallic acid, and gallotannins in its red bean coat, an apparently unique characteristic among edible beans. In this study, the main phenolic compounds in red sword bean coats were further separated by Sephadex LH-20 column chromatography, and identified by LC-MS/MS. Furthermore, the FRAP and ABTS antioxidant activities and antibacterial activity (diameter of inhibition zone, DIZ) of main gallotannin-rich fractions were tested...
2018: Frontiers in Chemistry
Masumeh Sanaei, Fraidoon Kavoosi, Ali Valiani, Mohamed Amin Ghobadifar
Background: One of the main causes of mortality is hepatocellular carcinoma (HCC) which accounts for the third leading cause of deaths and one in forty deaths worldwide. The flavonoids, natural antioxidant compounds, account for a major group of polyphenolic compounds. One of the major isoflavones in soybean is genistein (GE) which can inhibit proliferation and induce apoptosis. Isoflavones, major type of phenolic materials, derived from dietary plants and medicinal herbs play a significant role in cancer prevention and treatment...
2018: International Journal of Preventive Medicine
Fan-Cheng Meng, Zheng-Feng Wu, Zhi-Qi Yin, Li-Gen Lin, Ruibing Wang, Qing-Wen Zhang
Background: Coptidis rhizoma (CR) is the dried rhizome of Coptis chinensis Franch., C. deltoidea C. Y. Cheng et Hsiao or C. teeta Wall. (Ranunculaceae) and is commonly used in Traditional Chinese Medicine for the treatment of various diseases including bacillary dysentery, typhoid, tuberculosis, epidemic cerebrospinal meningitis, empyrosis, pertussis, and other illnesses. Methods: A literature survey was conducted via SciFinder, ScieneDirect, PubMed, Springer, and Wiley databases...
2018: Chinese Medicine
Andrea de Oliveira Falcão, Paula Speranza, Tatiane Ueta, Isabela Mateus Martins, Gabriela Alves Macedo, Juliana Alves Macedo
Enzymatic interesterification is used to manipulate oil and fat in order to obtain improved restructured lipids with desired technological properties. However, with raw materials containing significant amounts of bioactive compounds, the influence of this enzymatic process on the bioactivity of the final product is still not clear. Thus, the aim of this study is to evaluate the antioxidant potential and modulatory effects of two raw materials from the Amazonian area, buriti oil and murumuru fat, before and after lipase interesterification, on human hepatoma cells (HepG2)...
December 2017: Food Technology and Biotechnology
Xiang-Mei Tan, Lu-Ying Li, Li-Yan Sun, Bing-Da Sun, Shu-Bin Niu, Meng-Hua Wang, Xiao-Yan Zhang, Wen-Song Sun, Gui-Shan Zhang, Hui Deng, Xiao-Ke Xing, Zhong-Mei Zou, Gang Ding
Endophytic fungi from desert, arid, and grassland areas are an ecologically important but unique group with poor chemical investigation. During our ongoing study to mine bioactive secondary metabolites from unique fungal environments, a new shunt product spiciferone F (1) including two new analogs spiciferones G (2) and H (3) together with four known ones spiciferone A (4), spiciferol A (5), 6, and 7 were isolated from endophytic fungus Phoma betae inhabiting in plant Kalidium foliatum (Pall.) Moq from Ningxia Province of West China...
March 14, 2018: Journal of Antibiotics
Yong-Zhe Zhu, Jing-Wen Liu, Xue Wang, In-Hong Jeong, Young-Joon Ahn, Chuan-Jie Zhang
The human β-site amyloid cleaving enzyme (BACE1) has been considered as an effective drug target for treatment of Alzheimer's disease (AD). In this study, Urechis unicinctus (U. unicinctus) , which is a Far East specialty food known as innkeeper worm, ethanol extract was studied by bioassay-directed fractionation and isolation to examine its potential β-site amyloid cleaving enzyme inhibitory and antimicrobial activity. The following compounds were characterized: hecogenin, cholest-4- en -3-one, cholesta-4,6- dien -3-ol, and hurgadacin...
March 14, 2018: Marine Drugs
Silvia Revoltella, Giorgia Baraldo, Birgit Waltenberger, Stefan Schwaiger, Philipp Kofler, Julia Moesslacher, Astrid Huber-Seidel, Konrad Pagitz, Roland Kohl, Pidder Jansen-Duerr, Hermann Stuppner
NADPH oxidase 4 (Nox4) has recently been implicated as driving force in cellular senescence. Thus, there is growing interest to develop Nox4 inhibitors, which might be valuable agents for cosmeceutical applications. Alpine plants represent a valuable source for the identification of novel bioactive natural products with anti-ageing effects, especially substances that protect plants against UV radiation, which is also known to contribute to the ageing of human skin. Therefore, the aim of this study was to identify novel Nox4 inhibitors from alpine plants...
March 14, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
E M Kithsiri Wijeratne, Maria C F Oliveira, Jair Mafezoli, Ya-Ming Xu, Sandro Minguzzi, Pedro H J Batista, Otília D L Pessoa, Luke Whitesell, A A Leslie Gunatilaka
Withanolides constitute a valuable class of bioactive natural products because some members of the class are known to exhibit cytotoxic activity and also induce a cytoprotective heat-shock response. In order to understand the relationship between their structures and these dual bioactivities of the withanolide scaffold, we obtained 25 analogues of withaferin A (WA) and withanolide D (WD) including 17 new compounds by semisynthesis involving chemical and microbial transformations. Hitherto unknown 16β-hydroxy analogues of WA and WD were prepared by their reaction with triphenylphosphine/iodine, providing unexpected 5β-hydroxy-6α-iodo analogues (iodohydrins) followed by microbial biotransformation with Cunninghamella echinulata and base-catalyzed cyclization of the resulting 16β-hydroxy iodohydrins...
March 14, 2018: Journal of Natural Products
Christine Lembke, Daniel Stettin, Franziska Speck, Nico Ueberschaar, Sam De Decker, Wim Vyverman, Georg Pohnert
Recently the first pheromone of a marine diatom was identified to be the diketopiperazine (S,S)-diproline. This compound facilitates attraction between mating partners in the benthic diatom Seminavis robusta. Interestingly, sexualized S. robusta cells are attracted to both the natural pheromone (S,S)-diproline as well as to its enantiomer (R,R)-diproline. Usually stereospecificity is a prerequisite for successful substrate-receptor interactions, and especially pheromone perception is often highly enantioselective...
March 14, 2018: Journal of Chemical Ecology
Youssef Rouphael, Giampaolo Raimondi, Luigi Lucini, Petronia Carillo, Marios C Kyriacou, Giuseppe Colla, Valerio Cirillo, Antonio Pannico, Christophe El-Nakhel, Stefania De Pascale
Interest in the role of small bioactive molecules (< 500 Da) in plants is on the rise, compelled by plant scientists' attempt to unravel their mode of action implicated in stimulating growth and enhancing tolerance to environmental stressors. The current study aimed at elucidating the morphological, physiological and metabolomic changes occurring in greenhouse tomato (cv. Seny) treated with omeprazole (OMP), a benzimidazole inhibitor of animal proton pumps. The OMP was applied at three rates (0, 10, or 100 μM) as substrate drench for tomato plants grown under nonsaline (control) or saline conditions sustained by nutrient solutions of 1 or 75 mM NaCl, respectively...
2018: Frontiers in Plant Science
Mohamed E M Saeed, Nuha Mahmoud, Yoshikazu Sugimoto, Thomas Efferth, Heba Abdel-Aziz
For decades, natural products represented a significant source of diverse and unique bioactive lead compounds in drug discovery field. In Clinical oncology, complete tumors remission is hampered by the development of drug-resistance. Therefore, development of cytotoxic agents that may overcome drug resistance is urgently needed. Here, the natural benzophenanthridine alkaloid sanguinarine has been studied for its cytotoxic activity against multidrug resistance (MDR) cancer cells. We investigated the role of the ATP-binding cassette (ABC) transporters BCRP/ABCG2, P-glycoprotein/ABCB1 and its close relative ABCB5 in drug resistance...
2018: Frontiers in Pharmacology
Melissa Conte, Josselin Lupette, Khawla Seddiki, Coline Meï, Lina J Dolch, Valerie Gros, Caroline Barette, Fabrice Rébeillé, Juliette Jouhet, Eric Marechal
Microalgae are a promising feedstock for the production of triacylglycerol (TAG) for a variety of potential applications, ranging from food and human health to biofuels and green chemistry. However, obtaining high TAG yields is challenging. A phenotypic assay for accumulation of oil droplets was developed to screen a library of 1,200 drugs, annotated with pharmacology information, to select compounds that trigger TAG accumulation in the diatom Phaeodactylum. Using this screen, we identified 34 molecules acting in a dose-dependent manner...
March 13, 2018: Plant Physiology
Shaoyi Cai, Gengzheng Zhu, Xiaohong Cen, Jingjie Bi, Jingru Zhang, Xiaoshan Tang, Kun Chen, Kui Cheng
Toll-like receptor 2 (TLR2) can recognize pathogen-associated molecular patterns to defense against invading organisms and has been represents an attractive therapeutic target. Until today, none TLR2 small molecule antagonist have been developed in clinical trial. Herein, we designed and synthesized 50 N-benzylideneaniline compounds with the help of CADD. And subsequent in vitro studies leading to the optimized compound SMU-A0B13 with most potent inhibitory activity to TLR2 (IC50 =18.21 ± 0.87 μM)...
March 10, 2018: Bioorganic & Medicinal Chemistry
Chao Han, Shanshan Wang, Zhongrui Li, Chen Chen, Jiqin Hou, Dingqiao Xu, Ruizhi Wang, Yaolan Lin, Jianguang Luo, Lingyi Kong
Countercurrent chromatography (CCC) has gradually become a widely used method for preparative separation of bioactive natural molecules. These molecules generally contain distinct scaffolds and characteristics that cannot be readily isolated from plants. While one-dimensional CCC is typically used for the initial purification with insufficiently resolved peaks after locating bioactive components, two-dimensional (2D) or multi-dimensional CCC strategies are employed to improve the resolution of peaks. However, these methods usually present certain disadvantages, such as complicated procedures and increased time consumption, experimental costs, and equipment requirements...
August 3, 2018: Analytica Chimica Acta
Jiahuan Chen, Tao Zhang, Qiubo Zhang, Yang Liu, Lingyu Li, Jinguang Si, Zhong-Mei Zou, Huiming Hua
The pericarp of Zanthoxylum bungeanum Maxim., commonly known as Sichuan pepper, is a widely used spice to remove fishy odor and add palatable taste. A phytochemical investigation of the 95% ethanol extract of Sichuan pepper resulted in the isolation of twenty-one isobutylhydroxyamides, including eight new ones named ZP-amides G-N, among which the chiral resolution of racemic ZP-amide A and ZP-amide B were successfully accomplished. The protective activity on corticosterone-treated PC12 cells of the isolated isobutylhydroxyamides was also evaluated...
March 14, 2018: Journal of Agricultural and Food Chemistry
Shuwei Zhang, Chun Yang, Emmanuel Idehen, Shi Lei, Lishuang Lv, Shengmin Sang
Black tea consumption has been associated with many health benefits including the prevention of cancer and heart disease. However, the chemical composition of black tea has not been fully explored. Most studies have examined different interactions between the four major tea catechins, and few studies have examined the interaction between catechins and other components in tea. In the present study, we tested our hypothesis that the ortho-dihydroxyl structure of chlorogenic acid (CGA) could react with the vic-trihydroxy structure of (-)-epigallocatechin 3-gallate (EGCG) and (-)-epigallocatechin (EGC) to generate theaflavin-type of compounds during black tea fermentation...
March 13, 2018: Journal of Agricultural and Food Chemistry
Jie Tan, Min Zhou, Xinhua Cui, Zhuocai Wei, Wanxing Wei
A series of oxime ethers with C₆-C₄ fragment was designed and virtually bioactively screened by docking with a target, then provided by a Friedel-Crafts reaction, esterification (or amidation), and oximation from p -substituted phenyl derivatives (Methylbenzene, Methoxybenzene, Chlorobenzene). Anti-hepatitis B virus (HBV) activities of all synthesized compounds were evaluated with HepG2.2.15 cells in vitro. Results showed that most of compounds exhibited low cytotoxicity on HepG2.2.15 cells and significant inhibition on the secretion of HBsAg and HBeAg...
March 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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