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Terpenoids and their anti-HIV-1 activities from Excoecaria acerifolia
Institution:1. Key Laboratory of Biology and Genetic Resources of Tropical Crops, Ministry of Agriculture, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, People''s Republic of China;2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, People''s Republic of China;3. Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, People''s Republic of China;4. Hainan Key Laboratory for Research and Development of Natural Products from Li Folk Medicine, Haikou 571101, People''s Republic of China;1. CSL Behring GmbH, Preclinical Research and Development, Marburg, Germany;2. Quotient Bioresearch Metabolic Chemistry, Rushden, UK
Abstract:Five new diterpenoids named excocarinols A–E (1–5) including three pimaranes, one cleistanthane, and one nor-beyerane, together with nine known compounds, were isolated from the EtOAc extract of the Chinese ethnodrug Gua-jing-ban (Excoecaria acerifolia Didr.). Their structures were elucidated by the analysis of spectroscopic data including 1D, 2D NMR and HR-MS. The anti-HIV-1 bioassay on the diterpenoids showed that excocarinol A (1) exhibited moderate anti-HIV-1 activity with EC50 5.58 μM and SI (Selection Index) over 112.71.
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