一种新型抗人类免疫缺陷病毒物质——硫酸甘草酸；通过化学修饰赋予甘草酸逆转录酶抑制活性。
A new anti-human immunodeficiency virus substance, glycyrrhizin sulfate; endowment of glycyrrhizin with reverse transcriptase-inhibitory activity by chemical modification.
作者信息
Nakashima H, Matsui T, Yoshida O, Isowa Y, Kido Y, Motoki Y, Ito M, Shigeta S, Mori T, Yamamoto N
机构信息
Department of Virology and Parasitology, Yamaguchi University School of Medicine.
出版信息
Jpn J Cancer Res. 1987 Aug;78(8):767-71.
Glycyrrhizin sulfate (GLS) was synthesized and investigated for antiviral effect on the human immunodeficiency virus (HIV) in vitro in comparison with the parental anti-HIV compound glycyrrhizin (GL). In MT-4 cells after HIV infection, the virus-induced cytopathic effect and the expression of viral antigens were inhibited by 0.25 mg/ml (0.184 mM) of GLS. Moreover, GLS completely inhibited HIV-induced plaque formation in MT-4 cells at a concentration of 1 mg/ml (736 microM), the 50% inhibitory dose being 0.055 mg/ml (40 microM). GLS was found to be an efficient inhibitor of reverse transcriptase. The effect of GLS was 4 times stronger than that of GL in molar terms.
合成了硫酸甘草甜素（GLS），并与母体抗HIV化合物甘草甜素（GL）比较，研究了其在体外对人类免疫缺陷病毒（HIV）的抗病毒作用。在HIV感染后的MT-4细胞中，0.25mg/ml（0.184mM）的GLS可抑制病毒诱导的细胞病变效应和病毒抗原的表达。此外，GLS在浓度为1mg/ml（736μM）时可完全抑制MT-4细胞中HIV诱导的空斑形成，50%抑制剂量为0.055mg/ml（40μM）。发现GLS是一种有效的逆转录酶抑制剂。从摩尔角度来看，GLS的作用比GL强4倍。
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