一种来自非洲植物加蓬胶木的HIV核糖核酸酶H抑制剂1,3,4,5-四没食子酰芹菜糖醇。

An HIV RNase H inhibitory 1,3,4,5-tetragalloylapiitol from the African plant Hylodendron gabunensis.

作者信息

Takada Kentaro, Bermingham Alun, O'Keefe Barry R, Wamiru Antony, Beutler John A, Le Grice Stuart F J, Lloyd John, Gustafson Kirk R, McMahon James B

机构信息

Molecular Targets Development Program, Center for Cancer Research, National Cancer Institute, Building 1052, Room 121, Frederick, Maryland 21702-1201, USA.

出版信息

J Nat Prod. 2007 Oct;70(10):1647-9. doi: 10.1021/np0702279. Epub 2007 Oct 13.

DOI:10.1021/np0702279

PMID:17935297

Abstract

A new compound, 1,3,4,5-tetragalloylapiitol ( 1), was isolated from the aqueous extract of the plant Hylodendron gabunensis and was found to be a potent inhibitor of RNase H enzymatic activity. The structure of 1 was elucidated by NMR analyses to be an apiitol ( 2) sugar moiety substituted with four gallic acid residues. Optical rotation measurements of the free sugar following basic hydrolysis indicated that the 3 S absolute configuration was the same as that of d-apiitol. Compound 1 inhibited HIV-1, HIV-2, and human RNase H with IC 50 values of 0.24, 0.13, and 1.5 microM, respectively, but it did not show inhibition of E. coli RNase H at 10 microM.

摘要

从加蓬树（Hylodendron gabunensis）的水提取物中分离出一种新化合物1,3,4,5-四没食子酰芹菜糖醇（1），发现它是核糖核酸酶H（RNase H）酶活性的有效抑制剂。通过核磁共振（NMR）分析确定1的结构为一个被四个没食子酸残基取代的芹菜糖醇（2）糖部分。碱性水解后游离糖的旋光测量表明，3S绝对构型与d-芹菜糖醇相同。化合物1对HIV-1、HIV-2和人RNase H具有抑制作用，IC50值分别为0.24、0.13和1.5微摩尔，但在10微摩尔时对大肠杆菌RNase H没有抑制作用。