Differential inhibition of reverse transcriptase and cellular DNA polymerase-alpha activities by lignans isolated from Chinese herbs, Phyllanthus myrtifolius Moon, and tannins from Lonicera japonica Thunb and Castanopsis hystrix

Antiviral Res. 1995 Aug;27(4):367-74. doi: 10.1016/0166-3542(95)00020-m.

Abstract

Two lignans, phyllamycin B and retrojusticidin B isolated from Phyllanthus myrtifolius Moon have been demonstrated to have a strong inhibitory effect on human immunodeficiency virus-1 reverse transcriptase activity (HIV-1 RT), but much less inhibitory effect on human DNA polymerase-alpha (HDNAP-alpha) activity. Fifty percent inhibitory concentrations of phyllamycin B and retrojusticidin B were determined to be 3.5 and 5.5 microM for HIV-1 RT, and 289 and 989 microM for HDNAP-alpha, respectively. The mode of inhibition was found to be non-competitive inhibition with respect to template-primer and triphosphate substrate. Several tannins such as caffeoylquinates (CQs) isolated from Lonicera japonica Thunb, galloylquinates (GQs) and galloylshikimates (GSs) purified from Castanopsis hystrix were shown to have a much less selective inhibitory effect on HIV-1 RT.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • DNA Polymerase II / antagonists & inhibitors*
  • Drugs, Chinese Herbal / chemistry
  • Drugs, Chinese Herbal / pharmacology*
  • HIV Reverse Transcriptase
  • Humans
  • Kinetics
  • Lignans / isolation & purification
  • Lignans / pharmacology*
  • RNA-Directed DNA Polymerase / drug effects*
  • Reverse Transcriptase Inhibitors / isolation & purification
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Structure-Activity Relationship
  • Tannins / isolation & purification
  • Tannins / pharmacology*

Substances

  • Drugs, Chinese Herbal
  • Lignans
  • Reverse Transcriptase Inhibitors
  • Tannins
  • HIV Reverse Transcriptase
  • RNA-Directed DNA Polymerase
  • DNA Polymerase II