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Multiple circulating saponins from intravenous Shenmai inhibit OATP1Bs in vitro: potential joint precipitants of drug interactions

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中国药理学与毒理学杂志 2019年第10期 760-760页

作者： Olajide E OLALEYE NIU Wei DU Fei-fei WANG Feng-qing XU Fang salisa pintusophon LU Jun-lan YANG Jun-ling LI Chuan State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences

Shenmai, an intravenous injection prepared from steamed Panax ginseng roots（Hongshen） and Ophiopogon japonicus roots（Maidong）, is used as an add-on therapy for coronary artery disease and cancer;saponins are its bioactive constituents. Since many saponins inhibit human organic anion-transporting polypeptides（OATP）1 B, this investigation determined the inhibition potencies of circulating Shenmai saponins on the transporters and the joint potential of these compounds for Shenmai-drug interaction. Circulating saponins and their pharmacokinetics were characterized in rats receiving a 30 min infusion of Shen Mai at 10 m L·kg-1. Inhibition of human OATP1 B1/1 B3 and rat Oatp1 b2 by the individual saponins was investigated in vitro; the compounds joint inhibition was also assessed in vitro and the data was processed using the Chou-Talalay method. Plasma protein binding was assessed by equilibrium dialysis. Altogether,49 saponins in Shenmai were characterized and graded into: 10-100 μmol·d-1（compound doses from Shenmai;7 compounds）, 1-10 μmol · d-1（17 compounds）, and<1 μmol · d-1（25 compounds, including Maidong ophiopogonins）. After dosing, circulating saponins were protopanaxadiol-type ginsenosides Rb1, Rb2, Rc, Rd, Ra1, Rg3,Ra2, and Ra3, protopanaxatriol-type ginsenosides Rg1,Re, Rg2, and Rf, and ginsenoside Ro. The protopanaxadioltype ginsenosides exhibited maximum plasma concentrations of 2.1-46.6 μmol·L-1, plasma unbound fractions of 0.4%-1.0% and terminal half-lives of 15.6-28.5 h（ginsenoside Rg3, 1.9 h）, while the other ginsenosides exhibited 0.1-7.7 μmol·L-1, 20.8%-99.2 %, and 0.2-0.5 h, respectively. The protopanaxadiol-type ginsenosides, ginsenosides without any sugar attachment at C-20（except ginsenoside Rf）, and ginsenoside Ro inhibited OATP1B3 more potently(IC_50, 0.2-3.5 μmol · L-1) than the other ginsenosides(≥22.6 μmol·L-1). Inhibition of OATP1B1 by ginsenosides was less potent than OATP1B3 inhibition. Ginsenosides Rb1, Rb2, Rc, Rd, Ro, Ra1, Re, and Rg2 like

关键词： coronary artery disease and cancer ginsenosides Shenmai

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