| The Anti-HIV Actions of 7-and 10-Substituted Camptothecins | |
| Li YY1,3,4,5; Chen SW[*]2; Yang LM1; Wang RR1; Pang W1; Zheng YT[*]1; chenshw@lzu.edu.cn; zhengyt@mail.kiz.ac.cn | |
| 2010 | |
| 发表期刊 | MOLECULES
 |
| ISSN | 1420-3049 |
| 卷号 | 15期号:1页码:149-149 |
| 合作性质 | 其它 |
| 摘要 | 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-1(IIIB) in C8166 were 24.2, 4.2 and 198.1, and against clinical isolated strain HIV-1(KM018) in PBMC were 10.3, 3.5 and 66.0, respectively. While the TI of CPT, 10-hydroxy-CPT and 7-hydroxymethyl-CPT against HIV-2(CBL-20) were 34.5, 10.7 and 317.0, respectively, and the TI of the three compounds against HIV-2(ROD) showed the similar values. However, when the antiviral mechanisms were considered, we found there was no inhibition of 7-hydroxymethyl-CPT on viral cell-to-cell transmission, and was no inhibition on reverse transcriptase, protease or integrase in cell-free systems. 7-Hydroxymethyl-CPT showed no selective killing of chronically infected cells after 3 days of incubation. In conclusion, 7-hydroxymethyl-CPT showed more potent anti-HIV activity, while 10-hydroxy-CPT had less efficient activity, compared with the parent CPT. Though the antiviral mechanisms remain to be further elucidated; the modification of -OH residues at C-7 of CPT could enhance the antiviral activity, while of -OH residues at C-10 of CPT had decreased the antiviral activity, which provides the preliminary modification strategy for anti-viral activities enhancement of this compound. |
| 关键词 | Camptothecin Anti-hiv Agents Hiv |
| 资助者 | This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). ; This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). ; This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). ; This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). |
| 收录类别 | SCI |
| 语种 | 英语 |
| 资助者 | This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). ; This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). ; This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). ; This work was supported in part by grants from Scientific and Technological projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), and the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185). |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/4707 |
| 专题 | 科研部门_分子免疫药理学（郑永唐） 科研部门_动物模型与人类重大疾病机理重点实验室 |
| 通讯作者 | chenshw@lzu.edu.cn; zhengyt@mail.kiz.ac.cn |
| 作者单位 | 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 |
| 推荐引用方式 GB/T 7714 | Li YY,Chen SW[*],Yang LM,et al. The Anti-HIV Actions of 7-and 10-Substituted Camptothecins[J]. MOLECULES,2010,15(1):149-149. |
| APA | Li YY.,Chen SW[*].,Yang LM.,Wang RR.,Pang W.,...&zhengyt@mail.kiz.ac.cn.(2010).The Anti-HIV Actions of 7-and 10-Substituted Camptothecins.MOLECULES,15(1),149-149. |
| MLA | Li YY,et al."The Anti-HIV Actions of 7-and 10-Substituted Camptothecins".MOLECULES 15.1(2010):149-149. |
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