the anti-hiv actions of 7- and 10-substituted camptothecins7 -抗艾滋病行动和10-substituted喜树碱.pdf

Molecules 2010, 15, 138-148; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article The Anti-HIV Actions of 7- and 10-Substituted Camptothecins Yu-Ye Li 1,3,4,5, Shi-Wu Chen 2,*, Liu-Meng Yang 1, Rui-Rui Wang 1, Wei Pang 1 and Yong-Tang Zheng 1,* 1 Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China 2 School of Pharmacy, Lanzhou University, Lanzhou 730000, China 3 Graduate School of the Chinese Academy of Sciences, Beijing 100039, China 4 The First Affiliated Hospital of Kunming Medical College, Kunming, Yunnan 650032, China 5 Yunnan Institute of Dermatology Venereology, Kunming, Yunnan 650032, China * Authors to whom correspondence should be addressed; E-Mails: zhengyt@ (Y.-T.Z.); chenshw@ (S.-W.C.); Tel./Fax: +86 871 5195684. Received: 22 November 2009; in revised form: 18 December 2009 / Accepted: 21 December 2009 / Published: 31 December 2009 Abstract: Camptothecin (CPT), a traditional anti-tumor drug, has been shown to possess anti-HIV-1 activity. To increase the antiviral potency, the anti-HIV activities of two CPT derivatives, 10-hydroxy-CPT and 7-hydroxymethyl-CPT, were evaluated in vitro. The therapy index (TI) of CPT, 10-hydroxy-CPT and 7-hydroxymethyl-CPT against HIV-1IIIB in C8166 were 24.2, 4.2 and 198.1, and against clinical isolated strain HIV-1KM018 in PBMC were 10.3, 3.5 and 66.0, respect