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Qing-Tong Han, Kai Xiao, Kang-Lin Xiang, Gui-Sheng Li, Sheng-Jun Dai
Two new flavonoid glucuronate esters, named scuregeliosides A and B (1-2), as well as three known ones, chrysin-7-O-β-D-glucuronate methyl ester (3), 5,7,4'-trihydroxyflavone-8-O-β-D- glucuronate methyl ester (4) and apigenin-7-O-β-D-glucuronate ethyl ester (5) were isolated from the ethanolic extract of the whole plant of Scutellaria regeliana. Their chemical structures were elucidated on the basis of comprehensive spectroscopic analyses. Five compounds were screened for anti-inflammatory activity in vitro...
May 3, 2018: Chemistry & Biodiversity
Jingxiao Zhang, Lilei Zhang, Yangcheng Xu, Shanshan Jiang, Yueyue Shao
Flavonoids, a class of natural compounds with variable phenolic structures, have been found to possess anti-cancer activities by modulating different enzymes and receptors like CDK6. To understand the binding behavior of flavonoids that inhibit the active CDK6, molecular dynamics (MD) simulations were performed on six inhibitors, chrysin (M01), fisetin (M03), galangin (M04), genistein (M05), quercetin (M06) and kaempferol (M07), complexed with CDK6/cyclin D. For all six flavonoids, the 3'-OH and 4'-OH of B-ring were found to be favorable for hydrogen bond formation, but the 3-OH on the C-ring and 5-OH on the A-ring were unfavorable, which were confirmed by the MD simulation results of the test molecule, 3', 4', 7-trihydroxyflavone (M15)...
2018: PloS One
Nelly Rivera-Yañez, Mario Rodriguez-Canales, Oscar Nieto-Yañez, Manuel Jimenez-Estrada, Maximiliano Ibarra-Barajas, M M Canales-Martinez, M A Rodriguez-Monroy
Propolis is a bee-collected natural product that has been proven to have various bioactivities. This study tested the effects of a Mexican propolis on streptozotocin-induced diabetes mellitus in a murine model. The results showed that an ethanolic extract of propolis of Chihuahua (EEPCh) significantly inhibited increases in blood glucose and the loss of body weight in diabetic mice. EEPCh increased plasma insulin levels in STZ-diabetic mice, whereas, in untreated diabetic mice, there was no detection of insulin...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
Sara Rasouli, Nosratollah Zarghami
Objective: To explore the possibility of a novel chemopreventive strategy for improving breast cancer treatment, the anticancer effects of a combination two natural compounds, Chrysin and Metformin, against T47D breast cancer cells were investigated. Materials and Methods: After treatment of T47D cells with Metformin, Chrysin and the two drugs in combination, toxicity to cancer cells was evaluated by MTT assay. Real time PCR was then used to determine the expression levels of hTERT and cyclin D1 genes. Results: The MTT test findings showed that the combination of metformin and chrysin had high synergistic effects in killing cancer cells...
April 25, 2018: Asian Pacific Journal of Cancer Prevention: APJCP
Yang Li, Yanpeng Li, Jun He, Ding Liu, Qizhi Zhang, Kang Li, Xing Zhang, Guotao Tang, Yu Guo, Yunmei Liu
Chrysin show many different physiological activities, including anti-oxidant, anti-inflammatory, anti-bacterial, anti-allergic, anti-diabetic and so on. In recent years, with the expection to develop more active drug for clinic, the many scholars at home and abroad focused on the synthesis and biological activities of its derivatives. This review summarizes a large number of chrysin derivatives and analyzes their biological structure-activity relationships.
April 23, 2018: Mini Reviews in Medicinal Chemistry
Katarzyna Celińska-Janowicz, Ilona Zaręba, Urszula Lazarek, Joanna Teul, Michał Tomczyk, Jerzy Pałka, Wojciech Miltyk
Propolis evokes several therapeutic properties, including anticancer activity. These activities are attributed to the action of polyphenols. Previously it has been demonstrated, that one of the most abundant polyphenolic compounds in ethanolic extracts of propolis are chrysin, caffeic acid, p -coumaric acid, and ferulic acid. Although their pro-apoptotic activity on human tongue squamous cell carcinoma cells (CAL-27) was established previously, the detailed mechanism of this process remains unclear. Considering the crucial role of proline metabolism and proline dehydrogenase/proline oxidase (PRODH/POX) in the regulation of cancer cell survival/apoptosis, we studied these processes in polyphenol-treated CAL-27 cells...
2018: Frontiers in Pharmacology
Juan Wang, Handong Wang, Kangjian Sun, Xiaoliang Wang, Hao Pan, Jianhong Zhu, Xiangjun Ji, Xiang Li
Background: Chrysin, an active natural bioflavonoid, has been proven to protect against carcinogenesis. However, the role of chrysin in glioblastoma and the potential molecular mechanisms remain to be elucidated. In our previous study, we found that nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) is highly expressed in a variety of glioblastoma cell lines associated with the mitogen-activated protein kinase (MAPK) pathway. The aim of this study was to evaluate the antitumor effects of chrysin in glioblastoma cells and how chrysin is related to the MAPK/Nrf2 signaling pathway...
2018: Drug Design, Development and Therapy
Shi-Mei Qi, Qiang Li, Qi Jiang, Zhi-Lin Qi, Yao Zhang
OBJECTIVE: To investigate the mechanism of chrysin in regulating lipopolysaccharide (LPS)-induced inflammation in RAW264.7 cells. METHODS: RAW264.7 cells were treated with different concentrations (0, 5, 10, 20, 40, 60, 80, 100, 150, and 200 µg/mL) of chrysin for 24 h, and the cell viability was measured using CCK-8. RAW264.7 cells were pre-treated with 10, 30, or 60 µg/mL chrysin for 2 h before stimulation with LPS for different times. The levels of TNF-α, IL-6 and MCP-1 were detected by ELISA, and Western blotting was used to detect the phosphorylation of JAK- 1, JAK-2, STAT-1 and STAT-3...
March 20, 2018: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
Josiane Alhage, Hoda Elbitar, Samir Taha, Jean-Paul Guegan, Zeina Dassouki, Thomas Vives, Thierry Benvegnu
A phenylethanoid, two steroids, a flavone glucoside and a chalcone have been isolated for the first time from the stems of Calicotome villosa together with a previously isolated flavone glucoside. Their structures were determined by spectroscopic analyses (NMR, HRMS) as basalethanoïd B ( 1 ), β-sitosterol and stigmasterol ( 2 ), chrysine-7- O -β-d-glucopyranoside ( 3 ), chrysine 7-((6''- O -acetyl)- O -β-d-glucopyranoside) ( 4 ) and calythropsin ( 5 ). The crude extracts and the isolated compounds (except 4), were evaluated for their antioxidant, antimicrobial (against two Gram-positive bacterial strains: Staphylococcus aureus , Bacillus cereus , four Gram-negative bacterial strains: Staphylococcus epidermidis , Klebsiella pneumonia , Acinetobacter baumanii , and three yeasts: Candida albicans , Candida tropicalis , and Candida glabrata ), hemolytic, antidiabetic, anti-inflammatory and cytotoxic activity...
April 8, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Xuan-Ming Zhang, Dong-Qing An, Long-Long Guo, Ning-Hui Yang, Hua Zhang
This study investigated the flavonoid constituents of a traditional Chinese medical plant Ziziphora clinopodioides Lam. by using ultra-performance liquid chromatography coupled with quadruple time-of-flight mass spectrometry and screened the active components in regulating autophagy.Normal rat kidney (NRK) cells transfected with green fluorescent protein- microtubule-associated protein 1 light Chain 3(GFP-LC3) were treated with Z. clinopodioides flavonoids and its chemical compositions. After 4 h of treatment, the auto-phagy spot aggregation in NRK cells was photographed and observed by laser scanning confocal microscopy...
April 3, 2018: Natural Product Research
Giuseppe Sciortino, Daniele Sanna, Valeria Ugone, Agustí Lledós, Jean-Didier Maréchal, Eugenio Garribba
The interaction of metallodrugs with proteins influences their transport, uptake, and mechanism of action. In this study, we present an integrative approach based on spectroscopic (EPR) and computational (docking) tools to elucidate the noncovalent binding modes of various VIV O compounds with lysozyme, a prototypical model of protein receptor. Five VIV O-flavonoid drug candidates formed by quercetin (que), morin (mor), 7,8-dihydroxyflavone (7,8-dhf), chrysin (chr), and 5-hydroxyflavone (5-hf)-effective against several osteosarcoma cell lines-and two benchmark VIV O species of acetylacetone (acac) and catechol (cat) are evaluated...
April 3, 2018: Inorganic Chemistry
Fatemeh Tavakoli, Rana Jahanban-Esfahlan, Khaled Seidi, Masoumeh Jabbari, Ramezan Behzadi, Younes Pilehvar-Soltanahmadi, Nosratollah Zarghami
Due to the high rate of drug resistance among malignant melanoma cases, it seems necessary to introduce an efficient pharmaceutical approach to melanoma treatment. For this purpose, Curcumin (Cur) and Chrysin (Chr), two natural anti-cancers, were co-encapsulated in PLGA-PEG nanoparticles (NPs), characterized by DLS, FTIR and FE-SEM and investigated for their effects on MMPs, TIMPs and TERT genes expression in C57B16 mice bearing B16F10 melanoma tumours. The results showed that the expression of MMP-9, MMP-2 and TERT genes were significantly decreased in all treated groups compared to the control...
April 1, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Soodabeh Davaran, Hamed Fazeli, Aliyeh Ghamkhari, Fariborz Rahimi, Ommoleila Molavi, Maryam Anzabi, Roya Salehi
A Novel poly [2-hydroxyethyl methacrylate-Lactide-dimethylaminoethyl methacrylate quaternary ammonium alkyl halide] [P(HEMA-LA-MADQUAT)] copolymer was synthesized through combination of ring opening polymerization (ROP) and 'free' radical initiated polymerization methods. This newly developed copolymer was fully characterized by FT-IR,1 HNMR and13 CNMR spectroscopy. Micellization of the copolymer was performed by dialysis membrane method and obtained micelles were characterized by FESEM, dynamic light scattering (DLS), zeta potential (ξ), and critical micelle concentration (CMC) measurements...
March 21, 2018: Journal of Biomaterials Science. Polymer Edition
Mônica S Campos, Naiara C S Ribeiro, Rodrigo F de Lima, Mariana B Santos, Patrícia S L Vilamaior, Luis O Regasini, Manoel F Biancardi, Sebastião R Taboga, Fernanda C A Santos
Chrysin is a bioflavonoid found in fruits, flowers, tea, honey and wine, which has antioxidant, anti-inflammatory, antiallergic and anticarcinogenic properties. This flavone has also been considered as beneficial for reproduction due its testosterone-boosting potential. Thus, the aim of this study was to evaluate the effects of chrysin on the prostate and gonads of male and female adult gerbils. In addition, a comparative analysis of the effects of testosterone on these same organs was conducted. Ninety-day-old male and female gerbils were treated with chrysin (50mgkg-1day-1) or testosterone cypionate (1mgkg-1week-1) for 21 days...
March 7, 2018: Reproduction, Fertility, and Development
Farida Larit, Khaled M Elokely, Narayan D Chaurasiya, Samira Benyahia, Manal A Nael, Francisco León, Mohammad Sanad Abu-Darwish, Thomas Efferth, Yan-Hong Wang, Djamila Belouahem-Abed, Samir Benayache, Babu L Tekwani, Stephen J Cutler
BACKGROUND: Monoamine oxidases (MAOs) are outer mitochondrial membrane flavoenzymes. They catalyze the oxidative deamination of a variety of neurotransmitters. MAO-A and MAO-B may be considered as targets for inhibitors to treat neurodegenerative diseases and depression and for managing symptoms associated with Parkinson's and Alzheimer's diseases. PURPOSE: The objective was to evaluate the inhibitory effect of Hypericum afrum and Cytisus villosus against MAO-A and B and to isolate the compounds responsible for the MAO-inhibitory activity...
February 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Almas F Memon, Amber R Solangi, Saima Q Memon, Arfana Mallah, Najma Memon
Recently, an increasing interest has been observed in ionic liquids (ILs) due to their potentialities in various chemical processes. ILs have some unique properties making them excellent additives in CE. In this work a simple, rapid, and reliable CZE method has been developed and validated using 1-butyl-3-methyl imidazolium hexafluorophosphate (BMIM-PF6 ) ionic liquid as a buffer additive for the determination/separation of five flavonoids including hesperedin, epicatechin (EC), epigallocatechin gallate (EGCG), and morin using photodiode array (PDA) detector...
February 27, 2018: Electrophoresis
François Chassagne, Mohamed Haddad, Aurélien Amiel, Chiobouaphong Phakeovilay, Chanthanom Manithip, Geneviève Bourdy, Eric Deharo, Guillaume Marti
Liver cancer is a major health burden in Southeast Asia, and most patients turn towards the use of medicinal plants to alleviate their symptoms. The aim of this work was to apply to Southeast Asian plants traditionally used to treat liver disorders, a successive ranking strategy based on a comprehensive review of the literature and metabolomic data in order to relate ethnopharmacological relevance to chemical entities of interest. We analyzed 45 publications resulting in a list of 378 plant species, and our point system based on the frequency of citation in the literature allowed the selection of 10 top ranked species for further collection and extraction...
February 23, 2018: Fitoterapia
Marie Švecová, Pavel Ulbrich, Marcela Dendisová, Pavel Matějka
Spectroscopy of surface-enhanced Raman scattering (SERS) is nowadays widely used in the field of bio-science and medicine. These applications require new enhancing substrates with special properties. They should be non-toxic, environmentally friendly and (bio-) compatible with examined samples. Flavonoids are natural antioxidants with many positive effects on human health. Simultaneously, they can be used as reducing agent in preparation procedure of plasmonic enhancing substrate for SERS spectroscopy. The best amplifiers of Raman vibrational spectroscopic signal are generally silver nanoparticles (AgNPs)...
April 15, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Piotr Kuś, Igor Jerković, Martina Jakovljević, Stela Jokić
The scope of current study was to apply supercritical CO2 for extraction of black poplar buds (Populus nigra L.) and to optimize the extraction parameters (pressure and temperature) using response surface methodology aimed at maximum extraction yield, total phenolic content (TP), ferric reducing antioxidant power (FRAP) and individual amount of selected bioactive phenolics. The pressure and temperature influenced significantly the extract yield (0.38-10.28 g/100 g), TP content (21.62-31.09 μg GAE/mg), FRAP capacity (0...
April 15, 2018: Journal of Pharmaceutical and Biomedical Analysis
Seema Menon, Lincy Lawrence, Vipin P Sivaram, Jose Padikkala
BACKGROUND: Oroxylum indicum Vent., a Dasamula plant used in Ayurveda possesses antioxidant properties. OBJECTIVES: To evaluate the cardioprotective effect of 70% methanolic extract of O. indicum Vent. root bark (OIM) against doxorubicin induced cardiomyopathy in female Sprague Dawley rats. MATERIALS AND METHODS: Cardiotoxicity was induced by intra-peritoneal injection of doxorubicin 30 mg/kg body weight (b.w.) for 4 consecutive days after a ten-day pre-treatment of animals with OIM at 200 mg/kg b...
February 2, 2018: Journal of Ayurveda and Integrative Medicine
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