Natural products inhibiting Candida albicans secreted aspartic proteases from Tovomita krukovii

Planta Med. 2002 Jan;68(1):49-54. doi: 10.1055/s-2002-20049.

Abstract

Assay-guided fractionation of the ethanol extract of Tovomita krukovii resulted in the identification of four new xanthones (1 - 4) and ten known compounds (5 - 14). The structures of compounds 1 - 14 were determined by spectral data to be 3,5-dihydroxy-4-methoxyxanthone (1), 1,3,5,7-tetrahydroxy-8-isoprenylxanthone (2), 1,3,5-trihydroxy-8-isoprenylxanthone (3), 1,5,7-trihydroxy-8-isoprenylxanthone (4), 1,3,7-trihydroxy-2-isoprenylxanthone (5), 1,5-dihydroxyxanthone (6), 1,6-dihydroxy-5-methoxyxanthone (7), 1,3,5-trihydroxyxanthone (8), 1,3,6-trihydroxy-5-methoxyxanthone (9), 1,6-dihydroxy-3,5-dimethoxyxanthone (10), 1,3,7-trihydroxyxanthone (11), 3-geranyl-2,4,6-trihydroxybenzophenone (12), betulinic acid (13), and 3,4-dihydroxybenzoic acid (14). Compounds 2, 3, 12 and 13 showed inhibitory effects against Candida albicans secreted aspartic proteases (SAP) with IC50 values of 15 microg/ml, 25 microg/ml, 40 microg/ml, and 6.5 microg/ml, respectively, while the other compounds were inactive. In addition, compound 12 showed activity against C. albicans, C. neoformans, S. aureus and methicillin resistant S. aureus (MRS).

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antifungal Agents / chemistry
  • Antifungal Agents / isolation & purification
  • Antifungal Agents / pharmacology*
  • Aspartic Acid Endopeptidases / drug effects
  • Aspartic Acid Endopeptidases / metabolism
  • Candida albicans / drug effects*
  • Clusiaceae*
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Pepsin A / drug effects
  • Pepsin A / metabolism
  • Plant Bark / chemistry
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Plant Stems / chemistry
  • Xanthenes / chemistry
  • Xanthenes / isolation & purification
  • Xanthenes / pharmacology*
  • Xanthones*

Substances

  • 3,5-dihydroxy-4-methoxy-xanthone
  • Antifungal Agents
  • Plant Extracts
  • Xanthenes
  • Xanthones
  • Aspartic Acid Endopeptidases
  • Pepsin A