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Apigenin

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https://www.readbyqxmd.com/read/28223870/bioactivity-and-chemical-characterization-of-acalypha-fruticosa-forssk-growing-in-saudi-arabia
#1
Ghada Ahmed Fawzy, Areej Mohammad Al-Taweel, Shagufta Perveen, Shabana Iqrar Khan, Fatma Abdulaziz Al-Omary
Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely 2-methyl-5,7-dihydroxychromone 5-O-β-d-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28222613/phytochemical-investigations-and-antiproliferative-secondary-metabolites-from-thymus-alternans-growing-in-slovakia
#2
Stefano Dall'Acqua, Gregorio Peron, Sara Ferrari, Valentina Gandin, Massimo Bramucci, Luana Quassinti, Pavol Mártonfi, Filippo Maggi
CONTEXT: Thymus alternans Klokov (Lamiaceae) is a neglected species of the genus Thymus (Sect. Serpyllum) endemic to Carpathian area, where it is used as a flavouring agent and for medicinal purposes. OBJECTIVE: The aim of the work was to identify antiproliferative constituents from the flowering aerial parts of this plant. MATERIALS AND METHODS: Thymus alternans extracts were analyzed by HPLC-MS(n) and subjected to extensive chromatographic separations...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28220704/functional-characterization-of-a-new-tea-camellia-sinensis-flavonoid-glycosyltransferase
#3
Xianqian Zhao, Peiqiang Wang, Mingzhuo Li, Yeru Wang, Xiaolan Jiang, Lilan Cui, Yumei Qian, Juhua Zhuang, Liping Gao, Tao Xia
Tea (Camellia sinensis) is an important commercial crop, in which the high content of flavonoids provides the health benefits. A flavonoid glycosyltransferase (CsUGT73A20), belonged to Cluster IIIa was isolated from tea plant. The recombinant CsUGT73A20 in E. coli exhibited a broad substrate tolerance towards multiple flavonoids. Among them, kaempferol was the optimal substrate compared to quercetin, myricetin, naringenin, apigenin and kaempferide. However, no product was detected when UDP-galactose was used as the sugar donor...
February 21, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28211698/demethylation-of-polymethoxyflavones-by-human-gut-bacterium-blautia-sp-mrg-pmf1
#4
Supawadee Burapan, Mihyang Kim, Jaehong Han
Polymethoxyflavones (PMFs) were biotransformed to various demethylated metabolites in the human intestine by the PMF-metabolizing bacterium, Blautia sp. MRG-PMF1. Because the newly formed metabolites can have different biological activities, the pathways and regioselectivity of PMF bioconversion were investigated. Using an anaerobic in vitro study, 12 PMFs, 5,7-dimethoxyflavone (5,7-DMF), 5-hydroxy-7-methoxyflavone (5-OH-7-MF), 3,5,7-trimethoxyflavone (3,5,7-TMF), 5-hydroxy-3,7-dimethoxyflavone (5-OH-3,7-DMF), 5,7,4'-trimethoxyflavone (5,7,4'-TMF), 5-hydroxy-7,4'-dimethoxyflavone (5-OH-7,4'-DMF), 3,5,7,4'-tetramethoxyflavone (3,5,7,4'-TMF), 5-hydroxy-3,7,4'-trimethoxyflavone (5-OH-3,7,4'-TMF), 5,7,3',4'-tetramethoxyflavone (5,7,3',4'-TMF), 3,5,7,3',4'-pentamethoxyflavone (3,5,7,3',4'-PMF), 5-hydroxy-3,7,3',4'-tetramethoxyflavone (5-OH-3,7,3',4'-TMF), and 5,3'-dihydroxy-3,7,4'-trimethoxyflavone (5,3'-diOH-3,7,4'-TMF), were converted to chrysin, apigenin, galangin, kaempferol, luteolin, and quercetin after complete demethylation...
February 17, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28207990/carbonic-anhydrase-and-urease-inhibitory-potential-of-various-plant-phenolics-using-in-vitro-and-in-silico-methods
#5
Abdur Rauf, Muslim Raza, Muhammad Saleem, Ufuk Ozgen, Esen Sezen Karaoglan, Gulin Renda, Erhan Palaska, Ilkay Erdogan Orhan
Plant phenolics are known to display many pharmacological activities. In the current study, eight phenolic compounds [e.g. luteolin 5-O-β-glucoside (1), methyl rosmarinate (2), apigenin (3), vicenin 2 (4), lithospermic acid (5), soyasaponin II (6), rubiadin 3-O-β-primeveroside (7), 4(3,4dihydroxybenzoyloxymethyl)phenyl-O-β-D-glucopyranoside (8)] isolated from various plant species were tested at 0.2 mM against carbonic anhydrase-II (CA-II) and urease using microtiter assays. Urease inhibition rate for compounds 1-8 ranged between 5...
February 16, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28197841/probing-the-influence-of-carboxyalkyl-groups-on-the-molecular-flexibility-and-the-charge-density-of-apigenin-derivatives
#6
Y J Qi, H N Lu, Y M Zhao, N Z Jin
Apigenin is an important flavonoids due to its antidiabetic bioactivity. It was reported experimentally that the 7-substituent derivative of apigenin has higher biological activity than 4'- and 5-substituted derivatives while introducing sole carboxyalkyl group -(CH2)7COOH into the parent structure. Molecular docking studies indicated that the other two derivatives have lower binding affinities than the 7-substituent derivative (-7.52 kcal mol(-1)), which is considered to be a better inhibitor than the parent molecule...
March 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28192760/competitive-binding-experiments-can-reduce-the-false-positive-results-of-affinity-based-ultrafiltration-hplc-a-case-study-for-identification-of-potent-xanthine-oxidase-inhibitors-from-perilla-frutescens-extract
#7
Zhiqiang Wang, Shin Hwa Kwon, Seung Hwan Hwang, Young-Hee Kang, Jae-Yong Lee, Soon Sung Lim
The purpose of this study was to assess the possibility of using competitive binding experiments with ultrafiltration-HPLC analysis to identify potent xanthine oxidase (XO) inhibitors from the Perilla frutescens extract as an attempt to reduce the number of false positive results. To isolate the enzyme-ligand complex from unbound compounds, the P. frutescens extract was either incubated in the absence of XO, in the presence of XO, or with the active site blocked XO before the ultrafiltration was performed. Allopurinaol was used as the XO active site blocker...
February 6, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28191273/oxidative-stress-triggered-by-apigenin-induces-apoptosis-in-a-comprehensive-panel-of-human-cervical-cancer-derived-cell-lines
#8
Raquel P Souza, Patrícia de S Bonfim-Mendonça, Fabrícia Gimenes, Bianca A Ratti, Vanessa Kaplum, Marcos L Bruschi, Celso V Nakamura, Sueli O Silva, Silvya S Maria-Engler, Marcia E L Consolaro
Recently, the cytotoxic effects of apigenin (4',5,7-trihydroxyflavone), particularly its marked inhibition of cancer cell viability both in vitro and in vivo, have attracted the attention of the anticancer drug discovery field. Despite this, there are few studies of apigenin in cervical cancer, and these studies have mostly been conducted using HeLa cells. To evaluate the possibility of apigenin as a new therapeutic candidate for cervical cancer, we evaluated its cytotoxic effects in a comprehensive panel of human cervical cancer-derived cell lines including HeLa (human papillomavirus/HPV 18-positive), SiHa (HPV 16-positive), CaSki (HPV 16 and HPV 18-positive), and C33A (HPV-negative) cells in comparison to a nontumorigenic spontaneously immortalized human epithelial cell line (HaCaT)...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28185989/enhanced-oral-bioavailability-of-docetaxel-in-rats-combined-with-myricetin-in-situ-and-in-vivo-evidences
#9
Tianyun Hao, Yunni Ling, Meijuan Wu, Yajing Shen, Yu Gao, Shujun Liang, Yuan Gao, Shuai Qian
The purpose of this study was to investigate the effect of myricetin on the pharmacokinetics of docetaxel in rats. In comparison to oral docetaxel alone (40mg/kg), the bioavailability of docetaxel could be significantly enhanced by 1.6-2.4-fold via oral co-administration with various flavonoids (apigenin, naringenin, baicalein, quercetin and myricetin) at a dosage of 10mg/kg, and myricetin showed the highest bioavailability improvement. Further pharmacokinetic studies demonstrated that the presence of myricetin (5-20mg/kg) enhanced both Cmax and AUC of docetaxel with the highest Cmax (162ng/mL, 2...
February 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28181104/apigenin-attenuates-streptozotocin-induced-pancreatic-%C3%AE-cell-damage-by-its-protective-effects-on-cellular-antioxidant-defense
#10
Ning Wang, Wen Jing Yi, Lu Tan, Jia Hui Zhang, Jiamin Xu, Yi Chen, Mengting Qin, Shuang Yu, Jing Guan, Rui Zhang
Pancreatic beta cells are very sensitive to oxidative stress, which is one of the major causes of cell damages in diabetes. Growing interest has focused on the development of effective therapeutics to protect pancreatic cells from oxidative stress and searching for potentially protective antioxidants for treating diabetes. Apigenin, a plant-derived flavonoid, was investigated to determine whether it could protect rat insulinoma cell lines (RINm5F pancreatic beta cells) against streptozotocin (STZ)-induced oxidative damages and the mechanisms implicated...
February 8, 2017: In Vitro Cellular & Developmental Biology. Animal
https://www.readbyqxmd.com/read/28176247/apigenin-alleviates-stz-induced-diabetic-cardiomyopathy
#11
Huang-Jun Liu, Yun-Lin Fan, Hai-Han Liao, Yuan Liu, Si Chen, Zhen-Guo Ma, Ning Zhang, Zheng Yang, Wei Deng, Qi-Zhu Tang
Apigenin is an important component of fruits and vegetables in human daily diets. Several cellular and animal models have been performed to demonstrate its anti-oxidant and anti-inflammatory bioactivities. However, the cardioprotective effects of apigenin in diabetic cardiomyopathy (DCM) remain unclear. In this study, we intended to explore the roles of apigenin in cardiac remodeling of DCM. Male C57BL/6 J mice were treated with streptozotocin (STZ, 50 mg/kg) for 5 consecutive days to induce DCM. The echocardiography and catheter-based measurements of hemodynamic parameters were performed to evaluate the cardiac function...
February 7, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28167419/comparative-pharmacokinetic-profiles-of-selected-irreversible-tyrosine-kinase-inhibitors-neratinib-and-pelitinib-with-apigenin-in-rat-plasma-by-uplc-ms-ms
#12
Hadir M Maher, Nourah Z Alzoman, Shereen M Shehata, Ashwag O Abahussain
Neratinib (NER) and pelitinib (PEL) are irreversible tyrosine kinase inhibitors (TKIs) that have been recently employed in cancer treatment. Apigenin (API), among other flavonoids, is known to have antioxidant, anti-proliferative, and carcinogenic effect. API can potentiate the antitumor effect of chemotherapeutic agents and/or alleviate the side effects of many anticancer agents. Since TKIs are mostly metabolized by CYP3A4 enzymes and that API could alter the enzymatic activity, potential drug interactions could be expected following their co-aministration...
January 31, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28166786/chemical-constituents-and-coagulation-activity-of-agastache-rugosa
#13
Pengran Cao, Pingyao Xie, Xuebiao Wang, Jinmei Wang, Jinfeng Wei, Wen-Yi Kang
BACKGROUND: In the Chinese traditional medicine, plant of Agastache rugosa (Fisch. & C.A. Mey.) Kuntze (A. rugosa) has been used to treat nausea, vomiting and dispel damp. However, currently, few reports about the chemical constituents, especially the non-volatile components of A. rugosa are available. METHODS: Through separation with various column chromatographies to elucidate the chemical constituents of A. rugosa, the biological activities of the major constituents were investigated...
February 6, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28164719/phytochemical-analysis-antiproliferative-and-antioxidant-activities-of-chrozophora-tinctoria-a-natural-dye-plant
#14
Feyza Oke-Altuntas, Selma Ipekcioglu, Ayse Sahin Yaglioglu, Lutfi Behcet, Ibrahim Demirtas
CONTEXT: Chrozophora tinctoria (L.) A. Juss. (Euphorbiaceae) is known as 'dyer's-croton' and used to obtain dye substances. Recently, natural antioxidants and colorants have been of interest because of their safety and therapeutic effects. OBJECTIVE: This study investigates the antiproliferative and antioxidant activities of the various extracts and fractions from C. tinctoria and analyzes their phytochemical contents. MATERIALS AND METHODS: The aerial parts of C...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28159725/topical-treatments-of-saussurea-costus-root-and-thuja-orientalis-l-synergistically-alleviate-atopic-dermatitis-like-skin-lesions-by-inhibiting-protease-activated-receptor-2-and-nf-%C3%AE%C2%BAb-signaling-in-hacat-cells-and-nc-nga-mice
#15
Hye Jeong Yang, Min Jung Kim, Suna Kang, Na Rang Moon, Da Sol Kim, Na Ra Lee, Kang Sung Kim, Sunmin Park
ETHNOPHARMACOLOGICAL RELEVANCE: The root of Saussurea costus (Aucklandia lappa Decne, Aucklandiae Radix, SC) and Thuja orientalis L. (TOL) have been traditionally used as anti-inflammatory agents in Korea. However, they have not been studied for the efficacy of atopic dermatitis (AD) treatment, a chronic inflammatory skin disease. We investigated the efficacy of topical applications with 1,3-butyleneglycol extracts of SC and TOL to alleviate the symptoms of AD. MATERIALS AND METHODS: HaCaT cells and the dorsal skin of Nc/Nga mice had a local exposure of house mite extracts and 2,4-dinitrochlorobenzene (DNCB), respectively...
January 31, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28159282/phytochemical-composition-of-fractions-isolated-from-ten-salvia-species-by-supercritical-carbon-dioxide-and-pressurized-liquid-extraction-methods
#16
Vaida Šulniūtė, Audrius Pukalskas, Petras Rimantas Venskutonis
Ten Salvia species, S. amplexicaulis, S. austriaca, S. forsskaolii S. glutinosa, S. nemorosa, S. officinalis, S. pratensis, S. sclarea, S. stepposa and S. verticillata were fractionated using supercritical carbon dioxide and pressurized liquid (ethanol and water) extractions. Fifteen phytochemicals were identified using commercial standards (some other compounds were identified tentatively), 11 of them were quantified by ultra high pressure chromatography (UPLC) with quadruple and time-of-flight mass spectrometry (Q/TOF, TQ-S)...
June 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28155259/complementary-cereals-and-legumes-for-health-synergistic-interaction-of-sorghum-flavones-and-cowpea-flavonols-against-lps-induced-inflammation-in-colonic-myofibroblasts
#17
Shima Agah, Hyemee Kim, Susanne Talcott, Joseph M Awika
SCOPE: Cereals and legumes are traditionally consumed together in many cultures, and may provide complementary health benefits beyond what is known about improved indispensable amino acid intake. Here we use an in vitro model of inflammatory pathways to investigate whether the different flavonoids in sorghum and cowpea could synergistically reduce inflammation. METHODS AND RESULTS: Interactive effect of combining apigenin and quercetin, as well as extracts (70% acetone, v/v) from a flavone-dominated white sorghum and flavonol-dominated white cowpea, against LPS-induced NF-κB and downstream cytokines (TNF-α, IL-6, IL-8) gene and protein expression was evaluated using the CCD18co colon myofibroblasts...
February 3, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28154327/characterization-of-phenolic-constituents-from-ephedra-herb-extract
#18
Yoshiaki Amakura
 Ephedra Herb (Japanese name: mao) is defined as the terrestrial stem of Ephedra species. It is one of the most important crude drugs in Kampo prescriptions such as maoto, kakkonto, and shoseiryuto. The traditional biological properties of Ephedra Herb are mainly attributable to ephedrine alkaloids. Recently, our research group has found that Ephedra Herb extract also shows alkaloid-independent pharmacological action; therefore, we focused on polyphenols, other active ingredients of Ephedra Herb extract. Reports on the constituents of the extract other than ephedrine alkaloids are limited, although condensed tannins of procyanidin A-type have been found in some Ephedra species...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28152014/apigenin-selective-ck2-inhibitor-increases-ikaros-expression-and-improves-t-cell-homeostasis-and-function-in-murine-pancreatic-cancer
#19
Nadine Nelson, Karoly Szekeres, Cristina Iclozan, Ivannie Ortiz Rivera, Andrew McGill, Gbemisola Johnson, Onyekachi Nwogu, Tomar Ghansah
Pancreatic cancer (PC) evades immune destruction by favoring the development of regulatory T cells (Tregs) that inhibit effector T cells. The transcription factor Ikaros is critical for lymphocyte development, especially T cells. We have previously shown that downregulation of Ikaros occurs as a result of its protein degradation by the ubiquitin-proteasome system in our Panc02 tumor-bearing (TB) mouse model. Mechanistically, we observed a deregulation in the balance between Casein Kinase II (CK2) and protein phosphatase 1 (PP1), which suggested that increased CK2 activity is responsible for regulating Ikaros' stability in our model...
2017: PloS One
https://www.readbyqxmd.com/read/28145860/synergistic-antibacterial-effect-of-apigenin-with-%C3%AE-lactam-antibiotics-and-modulation-of-bacterial-resistance-by-a-possible-membrane-effect-against-methicillin-resistant-staphylococcus-aureus
#20
K Akilandeswari, K Ruckmani
Methicillin-resistant Staphylococcus aureus (MRSA) infections are easily spread among infected patients, where resistance has dramatically increased resulted in serious health issues. Therefore, there is a need to develop alternative natural or combination drug therapies. Apigenin (AP) is a natural poly phenolic flavonoid has been found to possess many beneficial biological actions. The aim of this study was to investigate the anti-MRSA efficacy and synergistic effect of apigenin (AP) and in combination with ampicillin (AM) and ceftriaxone (CEF)...
December 30, 2016: Cellular and Molecular Biology
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