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

  
@article{APS9984,
	author = {Olajide E. Olaleye and Wei Niu and Fei-fei Du and Feng-qing Wang and Fang Xu and Salisa Pintusophon and Jun-lan Lu and Jun-ling Yang and Chuan Li},
	title = {Multiple circulating saponins from intravenous ShenMai inhibit OATP1Bs in vitro: potential joint precipitants of drug interactions},
	journal = {Acta Pharmacologica Sinica},
	volume = {40},
	number = {6},
	year = {2019},
	keywords = {},
	abstract = {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)1B, 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 ShenMai at 10 mL/kg. Inhibition of human OATP1B1/1B3 and rat Oatp1b2 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/day (compound doses from ShenMai; 7 compounds), 1–10 μmol/day (17 compounds), and },
	url = {http://www.chinaphar.com/article/view/9984}
}