| Autor: |
Johnson TO; Department of Biochemistry, Faculty of Basic Medical Sciences, University of Jos, Jos, Nigeria.; Biotechnology Research Unit, Jaris Computational Biology Center, Jos, Nigeria., Adegboyega AE; Department of Biochemistry, Faculty of Basic Medical Sciences, University of Jos, Jos, Nigeria.; Biotechnology Research Unit, Jaris Computational Biology Center, Jos, Nigeria., Johnson GI; Biotechnology Research Unit, Jaris Computational Biology Center, Jos, Nigeria.; College of Health Sciences, University of Jos, Jos, Nigeria., Umedum NL; Department of Pure and Industrial Chemistry, Nnamdi Azikiwe University, Awka, Anambra State, Nigeria., Bamidele OD; Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Ilorin, Ilorin, Nigeria., Elekan AO; Department of Biochemistry, Adekunle Ajasin University, Akungba-Akoko, Nigeria., Tarkaa CT; Cell Biology and Genetics Unit, Department of Zoology, University of Ibadan, Ibadan, Nigeria., Mahe A; Department of Biochemistry, Federal University, Dutse, Jigawa State, Nigeria., Abdulrahman A; Department of Pharmacognosy and Drug Development, Ahmadu Bello University, Zaria, Nigeria., Adeyemi OE; Department of Biochemistry, Faculty of Basic Medical Sciences, University of Jos, Jos, Nigeria., Okafor D; Department of Biochemistry, Faculty of Basic Medical Sciences, University of Jos, Jos, Nigeria., Yusuf AJ; Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Usmanu Danfodiyo University, Sokoto, Nigeria., Atewolara-Odule OC; Department of Chemical Sciences, Olabisi Onabanjo University, Ago-Iwoye, Nigeria., Ogunmoye AO; Department of Chemical Sciences, Olabisi Onabanjo University, Ago-Iwoye, Nigeria., Ishaya T; Department of Computer Science, University of Jos, Jos, Nigeria. |
| Abstrakt: |
Malaria control efforts have been hampered due to the emergence of resistant malaria parasite strains and the coinciding events of Covid-19. The quest for more effective and safe treatment alternatives is driving a slew of new studies that must be accelerated if malaria can be overcome. Due to its reported antimalarial activity, we studied the effects of extract and fractions of Phyllanthus nivosus leaf on Plasmodium lactate dehydrogenase (pLDH) activity using an in vitro assay. This was followed by an anti-plasmodial study using Plasmodium berghei -infected mice and an in silico identification of the plant's phytochemicals with possible pLDH-inhibitory activity. The activity of pLDH was significantly reduced in the presence of ethanol extract and various solvent fractions of Phyllanthus nivosus leaf, with the ethyl acetate fraction having the best inhibitory activity, which was comparable to that of the standard drug (chloroquine). The ethyl acetate fraction at 100 and 200 mg/Kg also suppressed the parasitaemia of Plasmodium berghei -infected mice by 76 and 80% respectively. Among the 53 compounds docked against pLDH, (-)-alpha-Cadinol, (+)-alpha-phellandrene, and spathulenol, all terpenes from the ethyl acetate fraction of P. nivosus leaf extract, demonstrated docking scores comparable to that of chloroquine. The three chemicals, like chloroquine, displayed important molecular interactions with the amino acid residues of the enzyme's NADH-binding site. According to the in silico ADMET study, the three terpenes have suitable drug-like abilities, pharmacokinetic features, and safety profiles. Hence, they could be considered for further development as antimalarial drugs.Communicated by Ramaswamy H. Sarma. |
