Modulation of P-glycoprotein ATPase activity by some phytoconstituents.
In the present investigation 16 phytoconstituents, which are active moieties found in several medicinal herbs, have been evaluated for their P-glycoprotein (P-gp) stimulation/inhibition profiles using a P-gp-dependent ATPase assay in rat jejunal membrane (in vitro). Acteoside, agnuside, catechin, chlorogenic acid, picroside -II and santonin showed an inhibitory effect. Negundoside, picroside -I and oleanolic acid caused a stimulatory effect. Andrographolide, apocyanin, berberine, glycyrrhizin, magniferin and piperine produced a biphasic response (stimulation at low concentration and inhibition at high concentration). The results suggested that a possible interaction of these phytoconstituents at the level of P-gp, could be an important parameter in determining their role in several key pharmacodynamic events.
Najar
I A
IA
Division of Pharmacology, Indian Institute of Integrative Medicine, (Formerly Regional Research Laboratory), CSIR, Jammu 180 001, India.
Sachin
B S
BS
Sharma
S C
SC
Satti
N K
NK
Suri
K A
KA
Johri
R K
RK
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000187:drug effects*; D000251:Adenosine Triphosphatases / Q000378:metabolism*; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D005260:Female; D005960:Glucosides / Q000494:pharmacology*; D007413:Intestinal Mucosa / Q000187:drug effects; D008297:Male; D051381:Rats; D017208:Rats, Wistar
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000470:Alkaloids; D005960:Glucosides; D000251:Adenosine Triphosphatases