In silico and in vitro inhibitory potential of an organometallic Cu (II) complex on Leishmania major stages

• Autorzy: Mirzaei M. , Nadushan A.S. , Nooshadokht M. , Abiri A. , Anjomshoa M. , Sharifi I. , Amiheidari B.
• Języki publikacji: EN

Abstrakty

EN

Leishmaniosis results in a serious complication, principally in the tropical and subtropical areas. Metalcored complexes, like meglumine antimoniate (MA) have proven antileishmanial activity. Similarly, in this research, we investigated the effects of Cu (II) dimethoxy bipyridine (CuDMOBP) against Leishmania major stages in silico and in vitro. Molecular docking analysis was carried out on the complex and a protozoan metacaspase. The complex’s antipromastigote and its cytotoxicity towards macrophages were assayed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method to calculate relative Inhibitory Concentration 50% (IC50), Cytotoxic Concentration 50% (CC50), and Selectivity Index (SI). Expression of TNF-α and IL-10 in intracellular amastigotes and induction of apoptosis was also investigated using quantitative real-time PCR. The complex interacted effectively with four amino acid residues including lysine (Lys171), histidine (His193), arginine (Arg44 and Arg243) of the targeted metacaspase. This indicates a potential affinity between the target macromolecule and the complex. MTT results showed significant in vitro inhibitory effects against promastigotes. Reduction in cellular expression of IL-10 and TNF-α was also significant, p<0.05 and p<0.005, respectively. CuDMOBP showed powerful in vitro anti-leishmanial activity and could be introduced as a new leishmanicidal candidate.

• Wydawca: -
• Czasopismo: Annals of Parasitology
• Rocznik: 2021
• Tom: 67
• Numer: 1
• Opis fizyczny: p.45-54,fig.,ref.

Twórcy

autor

Mirzaei M.

• Pathobiology Department, Faculty of Veterinary Medicine, Shahid Bahonar University of Kerman, Kerman, Iran

autor

Nadushan A.S.

• Pathobiology Department, Faculty of Veterinary Medicine, Shahid Bahonar University of Kerman, Kerman, Iran

autor

Nooshadokht M.

• Pathobiology Department, Faculty of Veterinary Medicine, Shahid Bahonar University of Kerman, Kerman, Iran
• Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran

autor

Abiri A.

• Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran

autor

Anjomshoa M.

• Pharmaceutics Research Center, Insitute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran

autor

Sharifi I.

• Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran

autor

Amiheidari B.

• Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran
• Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran

Identyfikatory

DOI

10.17420/ap6701.311