P.G. Department of Zoology, Berhampur University, Berhampur, Odisha, 760007, India.
Computational Biology & Bioinformatics Laboratory, P.G. Dept. of Botany, Berhampur University, Berhampur, Odisha, 760007, India.
Parasitol Res. 2023 Mar;122(3):717-727. doi: 10.1007/s00436-023-07784-9. Epub 2023 Feb 2.
The global malaria control and elimination program faces major threats due to the emergence and transmission of the anti-malarial drug-resistant strain of Plasmodium falciparum. Monitoring of artemisinin (ART) resistance marker Kelch-13 in the malaria-endemic region is essential in mitigating the disease's morbidity and mortality. The current study aimed to generate baseline information for further surveillance in the future. The current research was designed and conducted from July 2019 to June 2021 to monitor Pfkelch13 mutation at the molecular level in the eastern region of India. We also conducted an in silico study to understand the drug-protein interactions between ART and the protein crystal of PfKelch13 (KELCH) with PDB id:4ZGC. The kelch-13 gene was amplified by nested polymerase chain reaction (PCR) and sequenced through the Sanger sequencing method. Reference 3D7 clone (PF3D7_1343700) was used to align and probe all the sequences. The sequence analysis showed the absence of validated or associated mutation in the Kelch-13 propeller domain. The absence of natural selection in drug resistance was confirmed by the Tajima test. Further, in silico interaction studies between the drug ART and the Kelch propeller domain of P. falciparum were evaluated by structure predictions, molecular docking, molecular dynamics (MD) simulations, and estimations of binding free energies for the KELCH-ART complex. The results were compared with the apoprotein (KELCH-APO). The study confirmed the favorable binding of ART with the Kelch-13 propeller domain.
全球疟疾控制和消除计划因恶性疟原虫抗疟药物耐药株的出现和传播而面临重大威胁。在疟疾流行地区监测青蒿素(ART)耐药标志物 Kelch-13 对于减轻疾病的发病率和死亡率至关重要。本研究旨在为未来的进一步监测提供基线信息。本研究设计和实施于 2019 年 7 月至 2021 年 6 月,旨在在印度东部地区从分子水平监测 Pfkelch13 突变。我们还进行了一项计算机模拟研究,以了解 ART 与 PfKelch13(KELCH)蛋白晶体之间的药物-蛋白相互作用,PDB id:4ZGC。通过巢式聚合酶链反应(PCR)扩增 kelch-13 基因,并通过 Sanger 测序法进行测序。参考 3D7 克隆(PF3D7_1343700)用于对齐和探测所有序列。序列分析显示 Kelch-13 螺旋桨结构域中不存在已验证或相关的突变。Tajima 检验证实了耐药性中不存在自然选择。进一步,通过结构预测、分子对接、分子动力学(MD)模拟和结合自由能估计,评估了药物 ART 与恶性疟原虫 Kelch 螺旋桨结构域之间的计算机模拟相互作用。结果与无蛋白(KELCH-APO)进行了比较。研究证实了 ART 与 Kelch-13 螺旋桨结构域的良好结合。