W. Harry Feinstone Department of Molecular Microbiology and Immunology, The Johns Hopkins Bloomberg School of Public Health, Baltimore, MD, 21205, USA.
The Johns Hopkins Malaria Research Institute, Baltimore, MD, 21205, USA.
Nat Commun. 2023 Oct 12;14(1):6415. doi: 10.1038/s41467-023-42030-x.
Long-acting injectable medications, such as atovaquone, offer the prospect of a "chemical vaccine" for malaria, combining drug efficacy with vaccine durability. However, selection and transmission of drug-resistant parasites is of concern. Laboratory studies have indicated that atovaquone resistance disadvantages parasites in mosquitoes, but lack of data on clinically relevant Plasmodium falciparum has hampered integration of these variable findings into drug development decisions. Here we generate atovaquone-resistant parasites that differ from wild type parent by only a Y268S mutation in cytochrome b, a modification associated with atovaquone treatment failure in humans. Relative to wild type, Y268S parasites evidence multiple defects, most marked in their development in mosquitoes, whether from Southeast Asia (Anopheles stephensi) or Africa (An. gambiae). Growth of asexual Y268S P. falciparum in human red cells is impaired, but parasite loss in the mosquito is progressive, from reduced gametocyte exflagellation, to smaller number and size of oocysts, and finally to absence of sporozoites. The Y268S mutant fails to transmit from mosquitoes to mice engrafted with human liver cells and erythrocytes. The severe-to-lethal fitness cost of clinically relevant atovaquone resistance to P. falciparum in the mosquito substantially lessens the likelihood of its transmission in the field.
长效注射药物,如阿托伐醌,为疟疾提供了一种“化学疫苗”的前景,将药物疗效与疫苗耐久性结合在一起。然而,耐药寄生虫的选择和传播令人担忧。实验室研究表明,阿托伐醌耐药使寄生虫在蚊子中处于劣势,但缺乏关于临床相关疟原虫的相关数据,这阻碍了将这些可变发现纳入药物开发决策。在这里,我们生成了对阿托伐醌具有抗性的寄生虫,它们与野生型亲本仅在细胞色素 b 的 Y268S 突变上有所不同,这种突变与人类阿托伐醌治疗失败有关。与野生型相比,Y268S 寄生虫表现出多种缺陷,在蚊子中的发育缺陷最为明显,无论是来自东南亚(斯氏按蚊)还是非洲(冈比亚按蚊)。无性 Y268S 疟原虫在人类红细胞中的生长受到损害,但寄生虫在蚊子中的损失是渐进的,从配子体出芽减少,到卵囊数量和大小减少,最后到没有孢子。Y268S 突变体无法从蚊子传播到移植有人肝细胞和红细胞的小鼠。疟原虫对阿托伐醌的临床相关耐药性在蚊子中造成的严重至致命的适应性成本,大大降低了其在野外传播的可能性。