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DOI: 10.1055/s-0029-1240796
© Georg Thieme Verlag KG Stuttgart · New York
Anti-HIV Activities of the Compounds Isolated from Polygonum cuspidatum and Polygonum multiflorum
Publikationsverlauf
received October 22, 2009
revised December 12, 2009
accepted December 16, 2009
Publikationsdatum:
28. Januar 2010 (online)
Abstract
The 70 % EtOH extract of Polygonum cuspidatum showed inhibitory action against HIV-1-induced syncytium formation at non-cytotoxic concentrations in vitro with a 50 % effective concentration (EC50) of 13.94 ± 3.41 µg/mL. Through bioactivity-guided fractionation, 20 phenolic compounds, including eight stilbenoids, were isolated from the roots of Polygonum cuspidatum, and their anti-HIV‐1 activities were evaluated. Results showed that compounds 1, 13, 14, and 16 demonstrated fairly strong antiviral activity against HIV-1-induced cytopathic effects in C8166 lymphocytes at non-cytotoxic concentrations, with EC50 values of 4.37 ± 1.96 µg/mL, 19.97 ± 5.09, 14.4 ± 1.34 µg/mL, and 11.29 ± 6.26 µg/mL and therapeutic index (TI) values of 8.12, > 10.02, > 13.89, and > 17.71, respectively. Other compounds showed either weak or no effects. Compound 6 also showed weak inhibition (153.42 ± 19.25 µg/mL); however, it possesses very good water solubility and showed almost no cytotoxicity (> 2000 µg/mL), therefore achieving a fairly good TI (13.04). The activities of the two compounds (3 and 18) from Polygonum multiflorum were also assayed. The relationship between molecular structures and their bioactivities was also discussed.
Key words
Polygonum cuspidatum - Polygonum multiflorum - Polygonaceae - chemical components - anti‐HIV‐1 activity
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1 These authors contributed equally to this work.
Prof. Dr. Yongtang Zheng
Key Laboratory of Animal Models and Human Diseases Mechanisms and Laboratory of Molecular Immunopharmacology
Kunming Institute of Zoology
Chinese Academy of Sciences
Kunming
Yunnan 650223
People's Republic of China
Telefon: + 86 87 15 19 56 84
Fax: + 86 87 15 19 56 84
eMail: zhengyt@mail.kiz.ac.cn
Associate Prof. Dr. Kai Xiao
Lab of Toxicology & Pharmacology
Faculty of Naval Medicine
The Second Military Medical University
800 Xinangyin Road
Shanghai 200433
People's Rapublic of China
Telefon: + 86 21 81 87 11 29
Fax: + 86 21 81 87 11 28
eMail: kaixiaocn@gmail.com
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