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Anti-HIV activities of HIV-1 reverse transcriptase inhibitor racemic 11-demethyl-calanolide A
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 5
- DOI:
- 10.3321/j.issn:0513-4870.2008.05.004
- Key Word:
- 11-去甲胡桐素A;胡桐素A;逆转录酶抑制剂
Abstract： 本文比较研究消旋11*去甲胡桐素A[(±)-11-demethyl-calauolide A]和其母体消旋胡桐素A[(±)-calanolide A]在体外、细胞培养内和小鼠体内给药后血清的抗HIV+1(human immunodeficiency virus type 1)活性.二者在体外对HIV-1逆转录酶(reverse transcriptase,RT)的半数抑制浓度(IC50)分别为(3.028±2.514)μmol·L-1和(3.965±5.235)μmol·L-1.在HIV-1感染的MT-4细胞培养内抑制HIV-1细胞病变的IC50和选择指数分别为(1.081±0.337)μmol·L-1和26及(1.297±0.076)μmol·L-1和21.腹腔注射小鼠1次(100 mg·L-1)后30 min和60 min的血清对HIV-1 RT的抑制率前者分别为(42.7±1.5)%和(32.2±6.1)%,后者分别为(40.7±6.3)%和(29.2±6.7)%,说明消旋11-去甲胡桐素A为新非核苷类HIV-1逆转录酶抑制剂,比其母体消旋胡桐素A的抗HIV-1活性略高,值得进一步研究.
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