Mechanochemical Synthesis, In vivo Anti-malarial and Safety Evaluation of Amodiaquine-zinc Complex - - - Mehanohemijska sinteza i procena in vivo antimalarijske efikasnosti i bezbednosti amodiakin-cink kompleksa
Journal Title: Acta Facultatis Medicae Naissensis - Year 2017, Vol 34, Issue 3
Abstract
So far, some prospective metal-based anti-malarial drugs have been developed. The mechanochemical synthesis and characterization of Zn (II) complex with amodiaquine and its anti-malarial efficacy on Plasmodium berghei-infected mice and safety evaluation were described in this study. Solvent-free mechanochemical synthesis and characterization of Zn (II) complex with amodiaquine as well as its anti-malarial efficacy on NK-65 Plasmodium berghei-infected mice and safety were evaluated. Derivatization of amodiaquine with zinc (II) ion enhanced the activity of the drug through significant (p < 0.05) enhancement of parasitemia suppression in established malaria infection in comparison with the controls, while its capacity to clear malaria parasite was similar to that of chloroquine. A significant reduction in the liver, kidney and small intestinal activities of alkaline phosphatase, lactate dehydrogenase and alanine and aspartate aminotransferases was observed, while their levels increased significantly in the plasma. Levels of PCV, Hb, RBC and lymphocytes were significantly reduced (p < 0.05), and significant elevation (p < 0.05) in WBC and neutrophil concentrations across all the treatment groups when compared with control was observed. The result indicates that coordination of zinc (II) to amodiaquine by mechanical induction improved its anti-malarial activity, while the alterations in the investigated biochemical parameters suggest functional and structural toxicity. Thus, Zn (II) complex with amodiaquine may not be completely safe for prolonged and repeated use as an oral anti-malarial remedy. - - - Do sada su razvijeni neki od antimalarijskih lekova na bazi metala. U ovoj studiji opisana je mehanohemijska sinteza, karakterizacija kompleksa Zn (II) sa amodiakinom, kao i njegova antimalarijska efikasnost na miševima zaraženim Plasmodium bergheimom i procena njegove bezbednosti. U studiji je procenjena mehanohemijska sinteza bez upotrebe rastvarača i karakterizacija kompleksa Zn (II) sa amodiakinom, kao i njegova antimalarijska efikasnost na NK-65 miševima inficiranim pomoću Plasmodium berghei. Derivatizacija amodiakina sa cink (II) jonom povećala je aktivnost leka kroz značajno poboljšanje (p < 0,05) supresije parazitemije kod potvrđene malarije u poređenju sa kontrolnom grupom, dok je njegov kapacitet za čišćenje parazita malarije bio sličan onome kod hlorokvina. Zapaženo je značajno smanjenje aktivnosti alkalne fosfataze, laktat dehidrogenaze, alanina i aspartat aminotransferaza u jetri, bubrezima i tankom crevu, dok su se njihovi nivoi značajno poveća liu plazmi. Nivoi PCV, Hb, RBC i limfocita bili su značajno smanjeni (p < 0,05), a uočeno je i značajno povećanje (p < 0,05) koncentracija leukocita i neutrofila u svim grupama koje su lečene u poređenju sa kontrololnom grupom. Rezultat ukazuje da je koordinacija cinka (II) sa amodiakinom pomoć u mehaničke indukcije poboljšala njegovu antimalarijsku aktivnost, dok su izmene u ispitivanim biohemijskim parametriama ukazivale na funkcionalnu i strukturnu toksičnost. Stoga, kompleks Zn (II) sa amodiakinom ne može biti potpuno bezbedan za produženu i ponovljenu upotrebu kao oralni antimalarijski lek.
Authors and Affiliations
Rotimi Olusanya Arise, Sunday-Nwaso Elizabeth, Samuel Tobi Farohunbi, Mikhail Olugbemiro Nafiu, Adedibu Clement Tella
Keywords
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- EP ID EP347987
- DOI 10.1515/afmnai-2017-0024
- Views 88
- Downloads 0
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