Microbial transformation of artemisinin and its derivatives.
10.19540/j.cnki.cjcmm.20230327.301
- Author:
Xin-Na GAO
1
;
Jing-Jie KANG
2
;
Peng SUN
3
;
Yi-Fan ZHAO
3
;
Dong ZHANG
3
;
Lan YANG
3
;
Yue MA
3
;
Hui-Min GAO
4
Author Information
1. Tianjin University of Traditional Chinese Medicine Tianjin 301617, China Artemisinin Research Center, China Academy of Chinese Medical Sciences Beijing 100700, China.
2. Artemisinin Research Center, China Academy of Chinese Medical Sciences Beijing 100700, China Liaoning University of Traditional Chinese Medicine Dalian 116600, China.
3. Artemisinin Research Center, China Academy of Chinese Medical Sciences Beijing 100700, China.
4. Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China.
- Publication Type:Review
- Keywords:
active derivatives;
artemisinin and derivatives;
microbial transformation;
simulation of metabolism;
structural modification
- MeSH:
Animals;
Antimalarials/pharmacology*;
Antiviral Agents;
Artemether;
Artemisinins;
Mammals
- From:
China Journal of Chinese Materia Medica
2023;48(11):2876-2895
- CountryChina
- Language:Chinese
-
Abstract:
Microbial transformation is an efficient enzymatic approach for the structural modification of exogenous compounds to obtain derivatives. Compared with traditional chemical synthesis, the microbial transformation has in fact the undoubtable advantages of strong region-and stereo-selectivity, and a low environmental and economic impact on the production process, which can achieve the reactions challenging to chemical synthesis. Because microbes are equipped with a broad-spectrum of enzymes and therefore can metabolize various substrates, they are not only a significant route for obtaining novel active derivatives, but also an effective tool for mimicking mammal metabolism in vitro. Artemisinin, a sesquiterpene with a peroxy-bridged structure serving as the main active functional group, is a famous antimalarial agent discovered from Artemisia annua L. Some sesquiterpenoids, such as dihydroartemisinin, artemether, and arteether, have been developed on the basis of artemisinin, which have been successfully marketed and become the first-line antimalarial drugs recommended by WHO. As revealed by pharmacological studies, artemisinin and its derivatives have exhibited extensive biological activities, including antimalarial, antitumor, antiviral, anti-inflammatory, and immunomodulatory. As an efficient approach for structural modification, microbial transformation of artemisinin and its derivatives is an increasingly popular strategy that attracts considerable attention recently, and numerous novel derivatives have been discovered. Herein, this paper reviewed the microbial transformation of artemisinin and its artemisinin, including microbial strains, culture conditions, product isolation and yield, and biological activities, and summarized the advances in microbial transformation in obtaining active derivatives of artemisinin and the simulation of in vivo metabolism of drugs.
