摘要
CalanolideA及其结构类似物是从藤黄科胡桐属植物中分离的一种吡喃型香豆素类化合物 ,对HIV 1型病毒的反转录酶 (ReverseTranscriptase ,RT)有很强且特异的抑制性。该类化合物虽然结构相似但各自对HIV 1病毒的活性差异显著 ;具有不同于其他非核苷类药物 (NNRTIs)对HIV 1的作用机制 ;与其他NNRTIs一样 ,该类化合物也可诱导HIV 1病毒的抗药性突变株 ,但与其他HIVRT药物存在较好的协同性 ;有报道认为HIV的抗药性与RT一级结构的氨基酸残基的改变有关 ;为了解决资源问题 ,目前已有该类化合物化学合成成功的报道。本文综述有关该类化合物研究的最新进展。
Calanolid A and its analogue,a kind of pyranocoumarin derived from tropical trees of Calophyllum,has previously been report to be a unique and specific nonnucleoside inhibitor of reverse transcriptase(RT)of human immunodeficiency virus(HIV)type 1 (HIV-1).The anti-HIV-1 activity was different significantly among the compounds though the structure was similar.The compounds also induce the resistant virus strains in the presence of increasing concentration of each compound just as the other NNRTIs but they generally exhibited highest levels of synergy with most of other anti-HIV drug.There have been reported that the drug-resistance of HIV was correlated to the primary amino acid sequence of HIV-RT.The compounds have been chemically synthesized.The research advance about the compounds was reviewed in this paper.
出处
《天然产物研究与开发》
CAS
CSCD
2004年第3期249-253,共5页
Natural Product Research and Development
基金
广州市科技新星计划项目 ( 2 0 0 0 K 0 0 3 0 1)
