2. Academic Validation
  3. Potent Anti-HIV Ingenane Diterpenoids from Euphorbia ebracteolata

Potent Anti-HIV Ingenane Diterpenoids from Euphorbia ebracteolata

  • J Nat Prod. 2019 Jun 28;82(6):1587-1592. doi: 10.1021/acs.jnatprod.9b00088.
Ya-Si Huang 1,  Yan Lu 1,  Chin-Ho Chen 2,  Kuo-Hsiung Lee 3 4,  Dao-Feng Chen 1
Affiliations

Affiliations

  • 1 Department of Pharmacognosy, School of Pharmacy , Fudan University , Shanghai 201203 , People's Republic of China.
  • 2 Duke University Medical Center, Box 2926 , SORF , Durham , North Carolina 27710 , United States.
  • 3 Natural Products Research Laboratories, UNC Eshelman School of Pharmacy , University of North Carolina , Chapel Hill , North Carolina 27599-7568 , United States.
  • 4 Chinese Medicine Research and Development Center , China Medical University and Hospital , Taichung 40402 , Taiwan.
PMID: 31184480 DOI: 10.1021/acs.jnatprod.9b00088
Abstract

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-MS n 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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