Next Article in Journal
Structural Characteristics and Non-Linear Optical Behaviour of a 2-Hydroxynicotinate-Containing Zinc-Based Metal-Organic Framework
Previous Article in Journal
Influence of Fruit Maturity at Harvest on the Intensity of Smoke Taint in Wine
Article Menu

Export Article

Open AccessArticle
Molecules 2015, 20(5), 8928-8940; doi:10.3390/molecules20058928

Absorption and Metabolism Characteristics of Triptolide as Determined by a Sensitive and Reliable LC-MS/MS Method

1,†,* , 2,†
and
3,*
1
Department of Radiatin Oncology, Shanghai Pulmonary Hospital, Tongji University, 507 Zhengmin Road, Shanghai 200433, China
2
Department of Gastroenterology, Changhai Hospital, Second Military Medical University, 168 Changhai Road, Shanghai 200433, China
3
Institute of Traditional Chinese Veterinary Medicine, College of Veterinary Medicine, Nanjing Agricultural University, 1# Weigang, Nanjing 210095, Jiangsu, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 23 March 2015 / Revised: 7 May 2015 / Accepted: 12 May 2015 / Published: 18 May 2015
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [856 KB, uploaded 18 May 2015]   |  

Abstract

In this research, a sensitive and reliable LC-MS/MS method was developed and applied to determine the concentration of triptolide in rat plasma, microsomes, and cell incubation media. The absolute oral bioavailability of triptolide is 63.9% at a dose of 1 mg·kg−1. In vitro, the bidirectional transport of triptolide across Caco-2 cells was studied. A markedly higher transport of triptolide across Caco-2 cells was observed in the basolateral-to-apical direction and was abrogated in the presence of the P-gp inhibitor, verapamil. The result indicated that P-gp might be involved in the absorption of triptolide in intestinal. The metabolic stability was also investigated using human liver microsome incubation systems in vitro. In HLMs, incubations with an initial triptolide concentration of 1 μM resulted in an 82.4% loss of substrate over 60 min, and the t1/2 was 38 min, which indicated that triptolide was easily metabolized in human liver microsomes. In conclusion, the absolute oral bioavailability of triptolide in plasma, transport across Caco-2 cell monolayers, and metabolic stability in human liver microsomes were systematically investigated by using a sensitive and reliable LC-MS/MS method. View Full-Text
Keywords: Caco-2 cells; human liver microsome; P-gp; pharmacokinetics; triptolide Caco-2 cells; human liver microsome; P-gp; pharmacokinetics; triptolide
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Gong, X.; Chen, Y.; Wu, Y. Absorption and Metabolism Characteristics of Triptolide as Determined by a Sensitive and Reliable LC-MS/MS Method. Molecules 2015, 20, 8928-8940.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top