Study on the mechanism of synergistic effect of artemisinin on antimalarial activity

Artemisinin-based combination therapies (ACTs) are now the most effective anti-malarial method. However, Plasmodium falciparum has been currently reported to be resistant to artemisinin. It was found in previous studies that synergistic components included in Artemisia annua L. (SCIAaL, including artemisinic acid, arteannuin B and scopoletin) themselves showed no significant anti-malarial activities, but they could significantly strengthen the anti-malarial activity of artemisinin. Therefore, it is speculated that the synergistic effects of SCIAaL on the anti-malarial activity of artemisinin might base on the following two synergistic mechanisms: 1. SCIAaL might inhibit the auto-induced metabolism of artemisinin, then reverse the decreased concentration of artemisinin in vivo; 2. SCIAaL might also block the bindings of intracellular transporters and artemisinin, inhibit the efflux of artemisinin from plasmodium, then increase the intracellular concentration of artemisinin, and finally decrease the resistance of Plasmodium to artemisinin. In view of the incomparable superiorities of traditional Chinese medicine and natural products in the field of drug resistance to the chemical medicines, the current research results will be helpful to the development of new anti-malarial strategy, provide new targets for the treatment of malaria, and ultimately provide the foundation for the development of new artemisinin-based anti-malarial compositions with low drug resistance.

Drug Resistance
Drug-based Strategies

Jan 2016 — Dec 2019

$84,697

China