Stelleralides A-C, novel potent anti-HIV daphnane-type diterpenoids from Stellera chamaejasme L.

Stelleralides A-C, novel potent anti-HIV daphnane-type diterpenoids from Stellera chamaejasme L.
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DOI:
10.1021/ol200889s
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发表时间:
2011-06-03
期刊:
影响因子:
5.2
通讯作者:
Lee, Kuo-Hsiung
Lee, Kuo-Hsiung
中科院分区:
化学1区
文献类型:
--
作者:
Asada, Yoshihisa;Sukemori, Aya;Watanabe, Takashi;Malla, Kuber J.;Yoshikawa, Takafumi;Li, Wei;Koike, Kazuo;Chen, Chin-Ho;Akiyama, Toshiyuki;Qian, Keduo;Nakagawa-Goto, Kyoko;Morris-Natschke, Susan L.;Lee, Kuo-Hsiung

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从瑞香狼毒(Stellera chamaejasme L.)的根中分离出三种新的1 - 烷基瑞香烷型二萜,狼毒内酯A - C(4 - 6)以及五种已知化合物。通过广泛的光谱分析阐明了4 - 6的结构。几种分离出的化合物显示出较强的抗HIV活性。化合物4显示出极强的抗HIV活性(EC90为0.40 nM)且细胞毒性最低(IC50为4.3 μM),似乎是一种有希望开发成为抗艾滋病临床试验候选药物的化合物。
Three novel 1-alkyldaphnane-type diterpenes, stelleralides A–C (4–6), and five known compounds were isolated from the roots of Stellera chamaejasme L. The structures of 4–6 were elucidated by extensive spectroscopic analyses. Several isolated compounds showed potent anti-HIV activity. Compound 4 showed extremely potent anti-HIV activity (EC90 0.40 nM) with the lowest cytotoxicity (IC50 4.3 μM), and appears to be a promising compound for development into anti-AIDS clinical trial candidates.
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