Dimeric Artesunate Glycerophosphocholine Conjugate Nano-Assemblies as Slow-Release Antimalarials to Overcome Kelch 13 Mutant Artemisinin Resistance-Reference-Cited by-同舟云学术

Dimeric Artesunate Glycerophosphocholine Conjugate Nano-Assemblies as Slow-Release Antimalarials to Overcome Kelch 13 Mutant Artemisinin Resistance

Published:2022-05-17 Issue:5 Volume:66 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Du Yawei¹²,Giannangelo Carlo³,He Wei²,Shami Gerald J.¹,Zhou Wenya²,Yang Tuo¹,Creek Darren J.³^ORCID,Dogovski Con¹,Li Xinsong²,Tilley Leann¹^ORCID

Affiliation:

1. Department of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Parkville, Victoria, Australia

2. School of Chemistry and Chemical Engineering, Southeast University, Nanjing, China

3. Drug Delivery Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia

Abstract

Current best practice for the treatment of malaria relies on short half-life artemisinins that are failing against emerging Kelch 13 mutant parasite strains. Here, we introduce a liposome-like self-assembly of a dimeric artesunate glycerophosphocholine conjugate (dAPC-S) as an amphiphilic prodrug for the short-lived antimalarial drug, dihydroartemisinin (DHA), with enhanced killing of Kelch 13 mutant artemisinin-resistant parasites.

Funder

National Science and Technology Major Project

Department of Education and Training | Australian Research Council

Department of Health | National Health and Medical Research Council

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/aac.02065-21

Reference64 articles.

1. World Health Organisation. 2021. World malaria report 2021. https://www.who.int/teams/global-malaria-programme/reports/world-malaria-report-2021.