- FLAVONOIDS OF TINOSPORA MALABARICA
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A dibenzoylethane and an allyloxyflavone isolated from Tinospora malabarica have been assigned the structures 1-(2',4'-dimethoxyphenyl)-3-(3'',4''-methylenedioxyphenyl)-2-methylpropan-1,3-dione and 5-allyloxy-6,7,4-trimethoxyflavone on the basis of chemical and spectroscopic evidence. - Key Word Index: Tinospora malabarica; Menispermaceae; 1,1-dibenzoylethane; allyloxyflavone.
- Prakash, Satya,Zaman, Asif
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- Discovery of 4′-O-methylscutellarein as a potent SARS-CoV-2 main protease inhibitor
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The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has resulted in millions of deaths and seriously threatened public health and safety. Despite COVID-19 vaccines being readily popularized worldwide, targeted therapeutic agents for the treatment of this disease remain very limited. Here, we studied the inhibitory activity of the scutellarein and its methylated derivatives against SARS-CoV-2 main protease (Mpro) by the fluorescence resonance energy transfer (FRET) assay. Among all the methylated derivatives we studied, 4′-O-methylscutellarein exhibited the most promising enzyme inhibitory activity in vitro, with the half-maximal inhibitory concentration value (IC50) of 0.40 ± 0.03 μM. Additionally, the mechanism of action of the hits was further characterized through enzyme kinetic studies and molecular docking. Overall, our results implied that 4′-O-methylscutellarein could be a primary lead compound with clinical potential for the development of inhibitors against the SARS-CoV-2 Mpro.
- Li, Maotian,Li, Yingxia,Wang, Yujie,Wu, Qianqian,Xiao, Yibei,Yan, Shiqiang
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- Synthesis and biological evaluation of methylated scutellarein analogs based on metabolic mechanism of scutellarin in vivo
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Scutellarin (1) could be hydrolyzed into scutellarein (2) in vivo and then converted into methylated, sulfated and glucuronidated forms. In order to investigate the biological activities of these methylated metabolites, eight methylated analogs of scutellarein (2) were synthesized via semi-synthetic methods. The antithrombotic activities of these compounds were evaluated through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (FIB). Their antioxidant activities were assessed by measuring their scavenging capacities toward 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and the ability to protect PC12 cells against H2O2-induced cytotoxicity. Furthermore, the physicochemical properties of these compounds including aqueous solubility and lipophilicity were also investigated. The results showed that 6-O-methylscutellarein (5) demonstrated potent antithrombotic activity, stronger antioxidant activity and balanced solubility and permeability compared with scutellarin (1), which warrants further development of 5 as a promising lead for the treatment of ischemic cerebrovascular disease.
- Shi, Zhi-Hao,Li, Nian-Guang,Wang, Zhen-Jiang,Tang, Yu-Ping,Dong, Ze-Xi,Zhang, Wei,Zhang, Peng-Xuan,Gu, Ting,Wu, Wen-Yu,Yang, Jian-Ping,Duan, Jin-Ao
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- Efficient synthesis of scutellarein
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Scutellarein is a component of Scutellaria, recently known as a potent cytotoxic agent on human leukaemia cells. The aim of this study was the synthesis of scutellarein and its methylated derivative. The new features are the innovating method to afford flavones from flavanones and the A-ring regioselective bromination step that lead to the target molecule by a facile and high-yielding pathway.
- Righi, Giuliana,Silvestri, Ilaria Proietti,Barontini, Maurizio,Crisante, Fernanda,Di Manno, Andrea,Pelagalli, Romina,Bovicelli, Paolo
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p. 1278 - 1284
(2012/09/25)
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- PROCESS TO PREPARE FLAVONES
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The present invention relates to the field of flavor ingredients. More particularly it provides, a process for making 5- hydroxy -polyitιethoxy-f lavones (5-OH-PMF) (I) or improving the organoleptic properties of natural polymethoxy-f lavones (PMF) . The invention's process comprises treating flavones (II) in the presence of a HCl solution in a non-acidic and non -aqueous solvent. (I) (II).
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Page/Page column 6-8
(2008/06/13)
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- Regioselective hydroxylation of 2-hydroxychalcones by dimethyldioxirane towards polymethoxylated flavonoids
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The flavone nucleus is part of a large number of natural products and medicinal compounds. In this presentation the novel regioselective hydroxylation of hydroxyarenes with DMD is described. The results showed further that flavonoids with 5-hydroxy group were selectively oxyfunctionalized at the para-position C8 carbon atom by DMD. Finally, according to this methodology, the naturally occurring isosinensetin, tangeretin, sinensetin, nobiletin, natsudaidain, gardenin B, 3,3′,4′,5,6,7,8- heptamethoxyflavone, quercetin and its derivatives were synthesized.
- Chu, Han-Wei,Wu, Huan-Ting,Lee, Yean-Jang
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p. 2647 - 2655
(2007/10/03)
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