Thermal behavior and biological activity of [Co2(Cl)2 tpmc](BF4)2 complex

Abstract

A large number of interesting Co (II) complexes with macrocyclicligands have been synthesized and the recognition of its complexes as important bioactive compounds in vitro and in vivo has aroused growing interest in these agents as potential drugs for therapeutic use in various diseases. Numerous available information on their bioinorganic properties and mode of action in several biological systems, combined with the new possibilities imposed by the development of medical chemistry, opens space for the development of a new generation of highly active drugs with minimized side effects which could add significantly to the current clinical research and practice. In this paper we attempt to present some properties of the earlier isolated the first Co(II)tpmc complex for which crystal structure confirmed chair conformation of macrocycle. Complex with formula [Co2(Cl)2tpmc](BF4)2 (tpmc = N,N',N'',N'''-tetrakis(2-pyridylmethyl)-1,4,8,11-tetraazacyclotetradecane), was studied on thermal behaviour and biological activity. TG-DTA analysis indicates that complex decomposition in a single step in the range of 365-435 °C. Investigated cytotoxic activity against two human cancer cell lines: HeLa (human cervix adenocarcinoma) and K562 (human myelogenous leukaemia). Complex was also preliminary assayed in vitro toward bacteria, fungi and mould together with the starting material for the synthesis (ligands, simple salts and solvents) as test substances. Investigated complex showed a moderate activity against strains of bacteria and were inactive against the tested fungi and mould. Minimal inhibitory concentration suppressing the visible growth of bacteria was determined. Biological investigations show the complex has significant cytotoxic potential.

Poznavanje biološke uloge kobalta i prepoznavanje njegovih kompleksa kao važnih bioaktivnih jedinjenja razlozi su sve veće zainteresovanosti za potencijalnu terapijsku primenu ovih kompleksa kod različitih bolesti. Brojne dostupne informacije o njihovim osobinama i načinu delovanja u nekoliko bioloških sistema, u kombinaciji sa novim mogućnostima koje nameće razvoj medicinske hemije, otvaraju prostor za razvoj nove generacije visoko aktivnih lekova sa minimalnim nuspojavama. U ovom radu smo ispitali neke osobine ranije izolovanog Co (II) tpmc kompleksa, prvog kod koga je rendgenska strukturna analiza potvrdila da se makrciklični ligand nalazi u konformaciji stolice. Ispitivane su termogravimetrijske I biološke osobine kompleksa [Co2(Cl)2tpmc](BF4)2 (tpmc = N, N', N'', N'''-tetrakis (2-piridilmetil) -1,4,8,11-tetraazaciklotetradekan). TG-DTA analiza ukazuje da je razlaganje kompleksa u jednom koraku u rasponu temperature od 365 -435 ° C. Ispitivana je citotoksična aktivnost na dve ljudske ćelijske linije karcinoma: HeLa (adenokarcinom grlića maternice) i K562 (mijelogena leukemija). Antimikrobno djelovanje kompleksa kvantifikovano je određivanjem minimalne inhibitorne koncentracije (MIC) korišćenjem bakterija Staphylococcus saprophyticus, Staphylococcus xylosus, Bacillus cereus, soja kvasca Candida albicans i plesni Aspergillus niger. Biološka ispitivanja su pokazala da kompleks ima značajan citotoksični potencijal I umerenu aktivnost prema bakterijama soja Staphylococcus.