齐墩果-9(11),12(13)-二烯-30-酸3β-(2-O-β-D-葡糖醛酸吡喃糖基-β-D-葡糖醛酸吡喃糖苷)的合成及抗HIV-1活性
Synthesis and Anti-HIV-1 Activity of Olean-9(11),12(13)-Dien-30-Oic Acid 3β-(2-O-β-D-Glucuronopyranosyl-β-D-Glucuronopyranoside).
作者信息
Baltina L A, Stolyarova O V, Kondratenko R M, Gabbasov T M, Baltina L A, Plyasunova O A, Il'ina T V
机构信息
1Institute of Organic Chemistry, Ufa Scientific Center, Russian Academy of Sciences, Ufa, Bashkortostan Russia.
2Bashkir State Medical University, Ufa, Bashkortostan Russia.
出版信息
Pharm Chem J. 2014;48(7):439-443. doi: 10.1007/s11094-014-1127-2. Epub 2014 Nov 12.
The glycyrrhizic acid (GA) analog olean-9(11),12(13)-dien-30-oic acid 3β-(2--β-D-glucuronopyranosyl-β-D-glucuronopyranoside) () was synthesized via reduction of GA by NaBH in refluxing 2-PrOH:HO with subsequent work up with HCl (5%). The cytotoxicity and antiviral activity of this glycoside against HIV-1 was studied in MT-4 cell culture. It was found that was practically non-toxic for MT-4 cells while inhibiting accumulation of virus-specific protein p24 and RNA-dependent DNA-polymerase activity of HIV-1 reverse transcriptase (RT) (IC 3.1 ±1.0 μg/mL).
通过在回流的2-丙醇：水中用硼氢化钠还原甘草酸（GA），随后用5%盐酸后处理，合成了甘草酸（GA）类似物齐墩果-9(11),12(13)-二烯-30-酸3β-(2--β-D-葡糖醛酸吡喃糖基-β-D-葡糖醛酸吡喃糖苷)（）。在MT-4细胞培养中研究了该糖苷对HIV-1的细胞毒性和抗病毒活性。发现对MT-4细胞几乎无毒，同时抑制病毒特异性蛋白p24的积累和HIV-1逆转录酶（RT）的RNA依赖性DNA聚合酶活性（IC 3.1±1.0μg/mL）。
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