4.7 Article

Potent Anti-HIV Ingenane Diterpenoids from Euphorbia ebracteolata

Journal

JOURNAL OF NATURAL PRODUCTS
Volume 82, Issue 6, Pages 1587-1592

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.9b00088

Keywords

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Funding

  1. Research Fund for the Doctoral Program of Higher Education, China [2012007113011]
  2. National Natural Science Foundation of China [81273486]
  3. National Institute of Allergy and Infectious Diseases, NIH, Bethesda, MD, USA [A1033066]

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Two new (1 and 2) and 14 known (3-16) ingenane diterpenoids were isolated from the roots of Euphorbia ebracteolata by bioassay-guided fractionation together with UPLC-MSn analysis. The absolute configurations of the new diterpenoids were established from electronic circular dichroism (ECD) data and ECD calculations. Except for ingenol (16), the ingenane diterpenoids with long aliphatic chain substituents (1-15) exhibited potent activities against HIV-1, with IC50 values of 0.7 to 9.7 nM and selectivity index values of 96.2 to 20 263. From the results, it was concluded that long aliphatic chain substituents are required for the enhanced anti-HIV activity of ingenane diterpenoids.

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