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In vitro anti-HIV and -HSV activity and safety of sodium rutin sulfate as a microbicide candidate
Tao J1,2,3; Hu QX4; Yang J2,3,5; Li RR3; Li XY6; Lu CP1; Chen CY5; Wang L6; Shattock R4; Ben KL*2,3; kben@vip.sina.com
2007
发表期刊ANTIVIRAL RESEARCH
ISSN0166-3542
卷号75期号:3页码:227-233
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摘要Sodium rutin sulfate (SRS) is a sulfated rutin modified from the natural flavonol glycoside rutin. Here, we investigated its in vitro anti-HIV and -HSV activities and its cytotoxic profile. Fifty percent inhibitory concentration (IC50) values of SRS against HIV-1 X4 virus IIIB, HIV-1 R5 isolates Ada-M and Ba-L were 2.3 +/- 0.2, 4.5 +/- 2.0 and 8.5 +/- 3.8 mu M with a selectivity index (SI) of 563, 575 and 329, respectively. Its IC50 against primary R5 HIV-1 isolate from Yunnan province in China was 13.1 +/- 5.5 mu M, with a Sl of 197. In contrast, unsulfated rutin had no activity against any of the HIV-1 isolates tested. Further study indicated that SRS blocked viral entry and virus-cell fusion likely through interacting with the HIV- I envelope glycoprotein. SRS also demonstrated some activity against human herpes simplex virus (HSV) with an IC50 of 88.3 +/- 0.1 mu M and a Sl of 30. The 50% cytotoxicity concentration (CC50) of SRS was >3.0 mM, as determined in human genital ME 180, HeLa and primary human foreskin fibroblast cells. Minimum inhibitory concentration of SRS for vaginal lactobacilli was >3.0 mM. These results collectively indicate that SRS represents a novel candidate for anti-HIV-1/HSV microbicide development.
关键词Microbicide Hiv-1 Hsv Sodium Rutin Sulfate Rutin Viral Entry
资助者This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company. ; This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company. ; This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company. ; This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company.
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资助者This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company. ; This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company. ; This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company. ; This research was partly supported by Drug Discovery Pro- gram of the Chinese Academy of Sciences, and Zhejiang CONBA Pharmaceutics Company.
文献类型期刊论文
条目标识符http://ir.kiz.ac.cn/handle/152453/5379
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通讯作者kben@vip.sina.com
作者单位1.Nanjing Agriculture University, 1 Weigang, Nanjing, Jiangsu 210095, China
2.Kunming Institute of Zoology, Chinese Academy of Sciences, 32 Jiaochang Donglu Kunming, Yunnan 650223, China
3.Kunming Chinawave Biotechnology Co. Ltd., 53 Keyi Road, Kunming, Yunnan 650106, China
4.Centre for Infection, Department of Cellular and Molecular Medicine, St. George’s, University of London, London SW17 0RE, UK
5.Kunming University of Science and Technology, 68 Wenchang Road, Kunming, Yunnan 650242, China
6.Department of Microbiology and Immunology, Kunming Medical College, 191 Renmin Western Road, Kunming, Yunnan 650031, China
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Tao J,Hu QX,Yang J,et al. In vitro anti-HIV and -HSV activity and safety of sodium rutin sulfate as a microbicide candidate[J]. ANTIVIRAL RESEARCH,2007,75(3):227-233.
APA Tao J.,Hu QX.,Yang J.,Li RR.,Li XY.,...&kben@vip.sina.com.(2007).In vitro anti-HIV and -HSV activity and safety of sodium rutin sulfate as a microbicide candidate.ANTIVIRAL RESEARCH,75(3),227-233.
MLA Tao J,et al."In vitro anti-HIV and -HSV activity and safety of sodium rutin sulfate as a microbicide candidate".ANTIVIRAL RESEARCH 75.3(2007):227-233.
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