Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities

J Nat Prod. 2017 Dec 22;80(12):3241-3246. doi: 10.1021/acs.jnatprod.7b00659. Epub 2017 Nov 29.

Abstract

Four new oxazole-containing diterpenoids, salvianans A-D (1-4), along with three known diterpenoids (5-7), were isolated from Salvia miltiorrhiza cell cultures. The structures of the new compounds were elucidated using spectroscopic methods and single-crystal X-ray diffraction. The evaluation for their anti-HIV-1 activities revealed that 2 and 3 displayed inhibitory activities with IC50 values of 0.03 and 1.2 μM, respectively. The time of addition (TOA) assay and long terminal repeat (LTR) luciferase reporter assay results indicated that compound 2 was an HIV-1 transcription inhibitor and might be a lead compound of antiviral agents acting on HIV-1 transcription.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Cell Culture Techniques
  • Crystallography, X-Ray / methods
  • Diterpenes / chemistry
  • Diterpenes / pharmacology*
  • HEK293 Cells
  • HIV-1 / drug effects*
  • Humans
  • Oxazoles / chemistry
  • Oxazoles / pharmacology*
  • Salvia / chemistry
  • Salvia miltiorrhiza / chemistry*
  • Transcription, Genetic / drug effects

Substances

  • Anti-HIV Agents
  • Diterpenes
  • Oxazoles