摘要
在体外观察绿茶提取物(GTE)及其中3种成份──没食子酰表没食子儿茶素(EG-CG)、没食子酰表儿茶素(ECG)及表没食子儿茶素(EGC)对克隆的人免疫缺陷病毒1型逆转录酶(HIV-1 RT)、鸭乙型肝炎病毒复制复合体逆转录酶(DHBV RCs RT),单纯疱疹病毒1型DNA聚合酶(HSV-1 DNAP)及牛胸腺DNA聚合酶α(CT DNAPα)活性的抑制作用,结果4种化合物的IC_(50)浓度分别为EGCG0.0066μmol/L,ECG0.084μmol/L、GTE0.1μg/ml和EGC7.2μmol/L。动力学研究发现EGCG对HIV-1 RT的外源性模板(rA)·(dT)_(12-18)为混合型抑制,对底物dTTP为非竞争性抑制。牛血清白蛋白可显著降低儿茶素衍生物对HIV-1RT的抑制作用。
Catechin derivatives including (-)-epicatechin gallate (ECG), (- )-epigall-ocatechin gallate (EGCG), ( - )-epigallocatechin (EGC) and green tea extract (GTE) were found to inhibit the activities of cloned human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT), duck hepatitis B virus replication complexes reverse transcriptase (DHBV RCs RT), herpes simplex virus 1 DNA polymerase (HSV-1 DNAP) and cow thymus DNA polymerase a (CT DNAP a). EGCG and ECG were shown to be, very potent inhibitors of HIV-1 RT. According to the IC50 values for HIV-1 RT, these compounds can be ordered as EGCG 0.0066μmol/L>ECG 0.084*mol/L>GTE 0. 1μg/ml>EGC 7.2*mol/L. DHBV RCs RT was the least sensitive to these, compounds. Kinetic study showed that EGCG exerts a mixed inhibition with respect to external template inducer poly (rA).oligo (dT)12-18 and a noncompetitive inhibition with respect to substrate dTTP for HIV-1 RT. Bovine serum albumin significantly reduced the inhibitory effects of catechin analogues and GTE on HIV-1 RT. In tissue culture GTE inhibited the cytopathic effect of coxsackie B3 virus, but did not inhibit the cytopathic effects of HSV-1, HSV-2, influenza A or influenza B viruses.
出处
《中国医学科学院学报》
CAS
CSCD
北大核心
1992年第5期334-338,共5页
Acta Academiae Medicinae Sinicae
关键词
儿茶素
病毒逆转录酶
艾滋病毒
catechin viruses reverse transcriptase enzyme inhibitors
