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1.
China Pharmacy ; (12): 508-511, 2017.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-507943

RESUMO

OBJECTIVE:To virtually screen potential α-glycosidase inhibitor ingredients from C. mori and F. mori,and to pro-vide reference for finding out new typeα-glycosidase inhibitor ingredient. METHODS:Surflex-Dock module of Sybyl-x 2.0 molecu-lar simulation software was used to perform the docking of small molecule compound,which was from the ingredients of C. mori and F. mori as ligand stated in literatures,with α-glycosidase. Total score of affinity scoring function was equal to 7 as the thresh-old value,to judge potential α-glycosidase inhibitor ingredient in C. mori and F. mori. RESULTS:After 70 small molecule com-pounds docked with α-glycosidase, 10 compounds showed binding activity (Total score≥7.00). Among them, moracin M-3′-O-β-D-glucopyranoside,5,7,2′-trihydroxyflavanone-4′-O-β-D-glucoside,mulberroside A,resveratrol-4,3′-di-O-β-D-gluco-pyranoside and 1,4-dideoxy-1,4-imino-(2-O-β-D-glucopyranosyl)-D-arabinitol had higher binding activity with α-glycosidase(Total score>8.00). CONCLUSIONS:Multi-constituents of C. mori and F. Mori show potential α-glycosidase inhibitory activity. The method is a kind of highly targeted,rapid and efficient approach to discover α-glycosidase inhibitor from traditional Chinese medi-cine.

2.
Cancer Med ; 5(11): 3156-3165, 2016 11.
Artigo em Inglês | MEDLINE | ID: mdl-27704720

RESUMO

aurora B kinase is highly expressed in several cancer cells and promotes tumorigenesis and progression, and therefore, it is an important target for drug to treat tumors. Quercetin was identified to be an antitumor agent. Herein, we report for the first time that quercetin inhibited aurora B activities by directly binding with aurora B in vitro and in vivo. Ex vivo studies showed that quercetin inhibited aurora B activities in JB6 Cl41 cells and A549 lung cancer cells. Moreover, knockdown of aurora B in A549 cells decreased their sensitivities to quercetin. In vivo study demonstrated that injection of quercetin in A549 tumor-bearing mice effectively suppressed cancer growth. The phosphorylation of histone 3 in tumor tissues was also decreased after quercetin treatment. In short, quercetin can suppress growth of lung cancer cells as an aurora B inhibitor both in vitro and in vivo.


Assuntos
Antineoplásicos/farmacologia , Aurora Quinase B/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Quercetina/farmacologia , Animais , Apoptose , Aurora Quinase B/genética , Aurora Quinase B/metabolismo , Linhagem Celular Tumoral , Proliferação de Células , Modelos Animais de Doenças , Resistencia a Medicamentos Antineoplásicos , Técnicas de Silenciamento de Genes , Humanos , Neoplasias Pulmonares , Melanoma Experimental , Camundongos , Ligação Proteica , Ensaios Antitumorais Modelo de Xenoenxerto
3.
Chinese Medical Ethics ; (6): 353-355, 2015.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-465695

RESUMO

This paper discusses the current prevalence of hospital preparations backward quality standard test methods, quality standards for lack of a serious problem , and analyses the reasons from four aspects , proposed to strengthen the construction of a pharmaceutical ethics; examination and approval departments shall strictly agents registration review technical requirements;rectify and improve the quality of all preparation standards;Introduction and training of strengthen pharmacy personnel , and actively improve the quality standard revision work;hospital in-creasing hardware and software construction , support quality standards revision suggestions for the improvement of work, provide reference standard for quality improvement of hospital preparations .

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