Salvia miltiorrhiza Roots against Cardiovascular Disease: Consideration of Herb-Drug Interactions.

Feng Chen,Li Li,Dan-Dan Tian

doi:10.1155/2017/9868694

Abstract

Salvia miltiorrhiza root (Danshen) is widely used in Asia for its cardiovascular benefits and contains both hydrophilic phenolic acids and lipophilic tanshinones, which are believed to be responsible for its therapeutic efficacy. This review summarized the effects of these bioactive components from S. miltiorrhiza roots on pharmacokinetics of comedicated drugs with mechanic insights regarding alterations of protein binding, enzyme activity, and transporter activity based on the published data stemming from both in vitro and in vivo human studies. In vitro studies indicated that cytochrome P450 (CYP450), carboxylesterase enzyme, catechol-O-methyltransferase, organic anion transporter 1 (OAT1) and OAT3, and P-glycoprotein were the major targets involved in S. miltiorrhiza-drug interactions. Lipophilic tanshinones had much more potent inhibitory effects towards CYPs activities compared to hydrophilic phenolic acids, evidenced by much lower Ki values of the former. Clinical S. miltiorrhiza-drug interaction studies were mainly conducted using CYP1A2 and CYP3A4 probe substrates. In addition, the effects of coexisting components on the pharmacokinetic behaviors of those noted bioactive compounds were also included herein.

Highlights

Cardiovascular disease, one of the top leading causes of mortality across the world, is responsible for 31% of deaths in 2012 [1]
The contents of chemicals in S. miltiorrhiza roots vary among aqueous extracts, organic solvent extracts, oral pills, and injections derived from the single herb of S. miltiorrhiza roots or herbal combination, like Fufang prescription in China
We mainly focus on pharmacokinetic interaction between S. miltiorrhiza roots and drugs both in human in vitro studies and in clinical trials

Summary

Introduction

Cardiovascular disease, one of the top leading causes of mortality across the world, is responsible for 31% of deaths in 2012 [1]. The combination of cardiovascular drugs and S. miltiorrhiza roots highlights potential interactions caused by pharmacokinetic and pharmacodynamic mechanisms. Underlying mechanisms include but are not limit to protein binding and inhibition and induction of enzyme/transporter activities [12] These interactions at the end may cause attenuated efficacy or unwanted toxicity, which suggests necessary dose adjustment. The contents of chemicals in S. miltiorrhiza roots vary among aqueous extracts, organic solvent extracts, oral pills, and injections derived from the single herb of S. miltiorrhiza roots or herbal combination, like Fufang prescription in China. These compounds can cause coronary vasodilatation, suppress thromboxane formation, inhibit platelet adhesion and aggregation, and scavenge free radicals [13]. Influence on pharmacokinetics of bioactive constituents from S. miltiorrhiza roots by other combined herbs or drugs is explored

Pharmacokinetic Interaction Caused by Salvia miltiorrhiza

Findings

Conclusions