1486-63-1Relevant articles and documents
Clarification of the role of quercetin hydroxyl groups in superoxide generation and cell apoptosis by chemical modification
Sakao, Kozue,Fujii, Makoto,Hou, De-Xing
, p. 2048 - 2053 (2009)
Accumulated data have suggested that the hydroxyl groups of flavonoids are important for their bioactive function. To directly demonstrate the role of hydroxyl groups, we synthesized a derivative of quercetin, 3,7,3',4'-0- tetrabenzylquercetin (4Bn-Q) tha
Quercetin derivative and preparation method thereof (by machine translation)
-
Paragraph 0017; 0033; 0035-0036; 0041; 0043-0044; 0049, (2019/09/17)
The invention discloses a quercetin derivative and a preparation method, and application thereof. The invention belongs to the field, and aims to solve the problems, such as poor water solubility, low bioavailability and the like in the prior art, provides a quercetin derivative, and the obtained quercetin derivative is far better than quercetin, has higher bioavailability, and can be used for treating cardiovascular and cerebrovascular diseases, resisting cancers and preventing cancer. Another object of the present invention is to provide a method, using quercetin, for protecting a hydroxyl, followed by substitution reaction and hydrogenation reaction to prepare a quercetin derivative, and a method for synthesizing the quercetin derivative. To the invention, the natural quercetin derivative, by substitution reaction at 5 - OH hydroxyl level, is beneficial to improving the water solubility and fat solubility, improving the bioavailability, and the method is simple in principle 37% - 57%, and high in product yield, 96% - 98%f =0000000.5. (by machine translation)
Natural and Synthetic Flavonoids as Potent Mycobacterium tuberculosis UGM Inhibitors
Villaume, Sydney A.,Fu, Jian,N'Go, Inès,Liang, Hui,Lou, Huayong,Kremer, Laurent,Pan, Weidong,Vincent, Stéphane P.
, p. 10423 - 10429 (2017/08/07)
This study reports a novel class of inhibitors of uridine 5′-diphosphate (UDP) galactopyranose mutase (UGM) derived from a screening of natural products. This enzyme is an essential biocatalyst involved in the cell wall biosynthesis of Mycobacterium tuberculosis. Flavonoids are potent inhibitors of UGM. The synthesis of novel methylated flavonoids allowed a structure–activity relationship analysis to be performed and which functional groups and structural elements were required for UGM inhibition could be determined. The binding mode of one of the best inhibitors was found to be noncompetitive. Docking simulations indicated that this molecule was likely to bind UGM in its open conformation, in a cavity recently identified as a “druggable” pocket. Importantly, two of the best inhibitors of the M. tuberculosis UGM displayed moderate activity against whole M. tuberculosis cells. This study reports the first natural products that act as inhibitor of UGM. Given the importance of natural products in medicinal chemistry, these results create new opportunities for the discovery of new antitubercular agents.