Coexisted components of Salvia miltiorrhiza enhance intestinal absorption of cryptotanshinone via inhibition of the intestinal P-gp

Phytomedicine. 2012 Nov 15;19(14):1256-62. doi: 10.1016/j.phymed.2012.08.007. Epub 2012 Oct 5.


Cryptotanshinone, derived from the roots of Salvia miltiorrhiza Bge and Salvia przewalskii Maxim, is the major active component and possesses significant antibacterial, antidermatophytic, antioxidant, anti-inflammatory and anticancer activities. The objective of this study was to investigate the intestinal absorptive characteristics of cryptotanshinone as well as the absorptive behavior influenced by co-administration of the diterpenoid tanshinones and danxingfang using an in vitro everted rat gut sac model. The results showed a good linear correlation between cryptotanshinone of absorption and the incubation time from 10 to 70min. The concentration dependence showed that a non-linear correlation existed between the cryptotanshinone absorption and the concentration at 100 μg/ml. Coexisting diterpenoid tanshinones and danxingfang could significantly enhance the absorption of cryptotanshinone. Coexisting diterpenoid tanshinones and danxingfang, which influenced cryptotanshinone's absorption, manifested as similar to that of the P-glycoprotein inhibitor. The underlying mechanism of the improvement of oral bioavailability was proposed that coexisting diterpenoid tanshinones and danxingfang could decrease the efflux transport of cryptotanshinone by P-glycoprotein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
  • Abietanes / pharmacology
  • Animals
  • Biological Availability
  • Biological Transport
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Intestinal Absorption
  • Intestinal Mucosa / metabolism
  • Intestines / drug effects*
  • Phenanthrenes / pharmacokinetics*
  • Plant Roots
  • Rats
  • Salvia / chemistry
  • Salvia miltiorrhiza / chemistry*


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Abietanes
  • Phenanthrenes
  • tanshinone
  • cryptotanshinone