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.
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.
Chang
C W
CW
Institute of Biochemistry, College of Medicine, National Taiwan University, Taiwan.
Lin
M T
MT
Lee
S S
SS
Liu
K C
KC
Hsu
F L
FL
Lin
J Y
JY
D004257:DNA Polymerase II / Q000037:antagonists & inhibitors*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase; D006801:Humans; D007700:Kinetics; D017705:Lignans / Q000302:isolation & purification / Q000494:pharmacology*; D012194:RNA-Directed DNA Polymerase / Q000187:drug effects*; D018894:Reverse Transcriptase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013634:Tannins / Q000302:isolation & purification / Q000494:pharmacology*
D004365:Drugs, Chinese Herbal; D017705:Lignans; D018894:Reverse Transcriptase Inhibitors; D013634:Tannins; D054303:HIV Reverse Transcriptase; D012194:RNA-Directed DNA Polymerase; D004257:DNA Polymerase II