Combined chemical transformation and biological transformation of artemisinin: A facile approach to diverse artemisinin derivatives.

ABSTRACT: Introduction: Artemisinin (1) is a milestone compound in malaria treatment, and it exhibits a broad scope of bioactivities. Herein, sequential chemo-reduction and biotransformation of artemisinin were undertaken to obtain a series of artemisinin derivatives. Methods: First, 10-deoxyartemisinin (2) and 9-ene-10-deoxyartemisinin (3) were synthesized after simple handling with boron trifluoride/diethyl ether and sodium borohydride. Then, biotransformation of 10-deoxyartemisinin was conducted with Cunninghamella echinulata CGMCC 3.4879 and Cunninghamella elegans CGMCC 3.4832, and the transformed products were separated and identified. The antimalarial activity of these products was tested in vitro against Plasmodium falciparum 3D7.

SUBMITTER: Gao X 

PROVIDER: S-EPMC9902651 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature