期刊
PLANTA MEDICA
卷 76, 期 9, 页码 889-892出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0029-1240796
关键词
Polygonum cuspidatum; Polygonum multiflorum; Polygonaceae; chemical components; anti-HIV-1 activity
资金
- National Natural Science Foundation of China [20872179, 30472141]
- Science and Technology Commission of Shanghai Municipality (STCSM) [08DZ1971504]
- Scientific and Technological Projects of China [2009ZX09501-029, 2008ZX10005-005]
- 973 Program [2009CB522306]
- CAS [KSCX1-YW-R-24, KSCX2-YW-R-185]
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 mu g/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 mu g/mL, 19.97 +/- 5.09, 14.4 +/- 1.34 mu g/mL, and 11.29 +/- 6.26 mu g/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 mu g/mL); however, it possesses very good water solubility and showed almost no cytotoxicity (> 2000 mu g/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.
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