Next Article in Journal
CNF-Functionalization as Versatile Tool for Tuning Activity in Cellulose-Derived Product Hydrogenation
Next Article in Special Issue
Dissipation Dynamics and Dietary Risk Assessment of Kresoxim-Methyl Residue in Rice
Previous Article in Journal
Chiral Derivatives of Xanthones with Antimicrobial Activity
Previous Article in Special Issue
Characterization and Quantification of Polyphenols and Triterpenoids in Thinned Young Fruits of Ten Pear Varieties by UPLC-Q TRAP-MS/MS
Article Menu
Issue 2 (January-2) cover image

Export Article

Open AccessArticle

A Microbial Transformation Model for Simulating Mammal Metabolism of Artemisinin

1,2, 1,2, 1,2, 1,2, 1,2, 1,2, 1,2,* and 1,2,*
1
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
2
Artemisinin Research Center, Beijing 100700, China
*
Authors to whom correspondence should be addressed.
Academic Editors: Carlo Siciliano and Anna Napoli
Molecules 2019, 24(2), 315; https://doi.org/10.3390/molecules24020315
Received: 4 December 2018 / Revised: 3 January 2019 / Accepted: 8 January 2019 / Published: 16 January 2019
  |  
PDF [2350 KB, uploaded 16 January 2019]
  |  

Abstract

Artemisinin (ART) is a highly effective antimalarial agent isolated from the traditional Chinese herb Qinghao. Metabolism of ART and its derivatives in the body is one of the most pressing issues for pharmaceutical scientists. Herein, an efficient in vitro microorganism model for simulation of metabolism of ART in vivo was developed employing Cunninghamella elegans. Metabolites in the microbial transformation system and plasma of mice pre-administrated ART orally were analyzed by ultra-performance liquid chromatography (UPLC)-electrospray ionization (ESI)-quadrupole time-of-flight (Q-TOF)-mass spectrometry (MSE) combined with UNIFI software. Thirty-two metabolites were identified in vitro and 23 were identified in vivo. After comparison, 16 products were found to be common to both models including monohydroxylated ART, dihydroxylated ART, deoxyartemisinin, hydroxylated deoxyartemisinin, hydroxylated dihydroartemisinin (DHA), and hydroxylated deoxy-DHA. These results revealed that C. elegans CICC 40250 functioned as an appropriate model to mimic ART metabolism in vivo. Moreover, an overall description of metabolites of ART from C. elegans CICC 40250 has been provided. Notably, DHA was detected and identified as a metabolite of ART in mouse plasma for the first time. View Full-Text
Keywords: microbial transformation; Cunninghamella elegans; metabolite; identification; artemisinin; UPLC-ESI-Q-TOF-MSE; UNIFI software; in vivo microbial transformation; Cunninghamella elegans; metabolite; identification; artemisinin; UPLC-ESI-Q-TOF-MSE; UNIFI software; in vivo
Figures

Graphical abstract

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

Share & Cite This Article

MDPI and ACS Style

Ma, Y.; Sun, P.; Zhao, Y.; Wang, K.; Chang, X.; Bai, Y.; Zhang, D.; Yang, L. A Microbial Transformation Model for Simulating Mammal Metabolism of Artemisinin. Molecules 2019, 24, 315.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

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