贯叶金丝桃素衍生物的设计、合成与抗病毒活性研究。

Design, synthesis and antiviral activity studies of schizonepetin derivatives.

机构信息

Jiangsu Key Laboratory for High Technology of TCM Formulae Research, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.

出版信息

Int J Mol Sci. 2013 Aug 20;14(8):17193-203. doi: 10.3390/ijms140817193.

DOI:10.3390/ijms140817193

PMID:23965980

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3759959/

Abstract

A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE) inhibition assay in vitro. Compounds M2, M4, M5 and M34 showed higher inhibitory activity against HSV-1 virus with the TC50 values being in micromole. Compounds M28, M33, and M35 showed higher inhibitory activity against influenza virus H3N2 with their TC50 values being 96.4, 71.0 and 75.4 μM, respectively. Preliminary biological activity evaluation indicated that the anti-H3N2 and anti-HSV-1 activities improved obviously through the introduction of halogen into the structure of schizonepetin.

摘要

为了获得有效的抗病毒药物，设计并合成了一系列雪头香内酯衍生物。采用细胞病变效应（CPE）抑制法，在体外评价了这些衍生物对 HSV-1 和流感病毒 H3N2 的抗病毒活性及细胞毒性。化合物 M2、M4、M5 和 M34 对 HSV-1 病毒的抑制活性较高，TC50 值在微摩尔水平。化合物 M28、M33 和 M35 对流感病毒 H3N2 的抑制活性较高，TC50 值分别为 96.4、71.0 和 75.4 μM。初步的生物活性评价表明，通过在雪头香内酯结构中引入卤素，抗 H3N2 和抗 HSV-1 活性明显提高。