Anti-HIV-1 integrase diterpenoids from Dichrocephala benthamii |
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| Institution: | 1. Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100193, China;2. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China;1. National Center for Pharmaceutical Crops, Arthur Temple College of Forestry and Agriculture, Stephen F. Austin State University, Nacogdoches, TX 75962-6109, USA;2. College of Life Science, Northeast Forestry University, 26 Hexing Road, Harbin, Heilongjiang 150040, China;1. Faculty of Science, Department of Chemistry, University of Dschang, P.O. Box 67, Dschang, Cameroon;2. Service Commun d’Analyses, Institut de Chimie Moléculaire de Reims (ICMR), CNRS UMR 7312, Bat. 18 B.P. 1039, 51687 Reims, Cedex 2, France;3. Groupe Isolement et Structure, Institut de Chimie Moléculaire de Reims (ICMR), CNRS UMR 7312, Bat. 18 B.P. 1039, 51687 Reims, Cedex 2, France;1. Ege University, Faculty of Science, Department of Chemistry, Bornova, 35100 ?zmir, Turkey;2. University of Salerno, Department of Pharmacy, 84084 Fisciano, Salerno, Italy;3. Ege University, Faculty of Science, Department of Botany, Bornova 35100, ?zmir, Turkey;1. Yunnan Academy of Tobacco Agricultural Sciences, Kunming, Yunnan 650031, PR China;2. Key Laboratory of Tobacco Chemistry of Yunnan Province, China Tobacco Yunnan Industrial Co., Ltd., Kunming 650231, PR China;3. Key Laboratory of Chemistry in Ethnic Medicinal Resources, State Ethnic Affairs Commission & Ministry of Education, Yunnan Minzu University, Kunming 650031, PR China;1. Key Laboratory of Tropical Plant Resources and Sustainable Use, Xishuangbanna Tropical Botanical Garden, Chinese Academy of Sciences, Menglun 666303, PR China;2. University of Chinese Academy of Sciences, Beijing 100049, PR China |
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| Abstract: | Five new clerodane diterpenoid dichrocephnoids A–E (1,2, 6–8) together with three known analogues were isolated from the whole herb of Dichrocephala benthamii C.B. Clarke. Their structures were elucidated on the basis of spectroscopic analyses (UV, IR, MS, 1D and 2D NMR). The relative configurations of the new compounds were established by NOESY correlations, and the absolute configuration of 1 was determined on the basis of CD methods. Dichrocephnoid A (1) possesses a very rare pentacyclic ring system with highly oxygenated functionalities. All of the isolated compounds exhibited inhibitory activity against HIV-1 integrase, however, dichrocephnoid C (6) showed the most promising inhibition of the enzyme with IC50 value of 12.35 ± 1.27 μM. |
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| Keywords: | Asteraceae Clerodane diterpenoids HIV-1 integrase |
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