Inhibition of green tea and the catechins against 1-deoxy-d-xylulose 5-phosphate reductoisomerase, the key enzyme of the MEP terpenoid biosynthetic pathway

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• 作者：Xian Hui ; Hui Liu ; Fang-Lin Tian ; Fei-Fei Li ; Heng Li ; Wen-Yun Gao ; ^{gaowenyun@nwu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Gallocatechin gallate (PubChem CID ; 5276890) ; Epigallocatechin gallate (PubChem CID ; 65064)
• 刊名：Fitoterapia
• 出版年：2016
• 出版时间：September 2016
• 年：2016
• 卷：113
• 期：Complete
• 页码：80-84
• 全文大小：467 K

文摘

1-Deoxy-d-xylulose 5-phosphate reductoisomerase (DXR) is the first committed enzyme in the MEP terpenoid biosynthetic pathway and also a validated antimicrobial target. Green tea which is rich in polyphenolic components such as the catechins, possesses a plenty of pharmacological activities, in particular an antibacterial effect. To uncover the antibacterial mechanism of green tea and to seek new DXR inhibitors from natural sources, the DXR inhibitory activity of green tea and its main antimicrobial catechins were investigated in this study. The results show that the raw extract of green tea and its ethyl acetate fraction are able to suppress DXR activity explicitly. Further determination of the DXR inhibitory capacity of eight catechin compounds demonstrates that the most active compound is gallocatechin gallate that is able to inhibit around 50% activity of DXR at 25 μM. Based on these data, the primary structure-activity relationship of the catechins against DXR is discussed. This study would be very helpful to elucidate the antimicrobial mechanism of green tea and the catechins and also would be very useful to direct the rational utilization of them as food additives.