ABSTRACT
Historically organometallic compounds have been used to cure certain diseases with limited applications. Although bismuth belongs to the category of heavy metals, many of its derivatives have found applications in modern drug discovery research, mainly because of its low toxicity and higher bioavailability. Being an eco-friendly mild Lewis acid, compounds having bismuth as a central atom are capable of binding several proteins in humans and other species. Bismuth complexes demonstrated antibacterial potential in syphilis, diarrhea, gastritis, and colitis. Apart from antibacterial activities, bismuth compounds exhibited anticancer, antileishmanial, and some extent of antifungal and other medicinal properties. This article discusses major synthetic methods and pharmacological potentials of bismuth complexes exhibiting in vitro activity to significant clinical performance in a systematic and timely manner.Copyright © 2022 Elsevier Ltd
ABSTRACT
BACKGROUND: This study was carried out to synthesize a new complex of Fe(II) with isoleucine dithiocarbamate ligand and to determine its potential as an anticancer and antiviral agent for SARSCOV-2. METHODS: The synthesized complexes were then characterized by UV-vis and FT-IR spectroscopy and their melting points. The value of the conductivity of the complex compound is also determined. Anti-cancer activity was tested in vitro and molecular docking. Its potential as an antiviral against SARSCOV-2 was also carried out by molecular docking. Pharmacokinetics/ADMET properties were also carried out on the complex. RESULT: Spectral results showed the successful synthesis of Fe(II) isoleucine dithiocarbamate complex. The complex produced UV-vis spectra at 268 and 575 nm, and the IR data at 399-599 cm-1 showed the coordination between the Fe(II) atoms with sulphur, nitrogen and oxygen of the isoleucine dithiocarbamate ligand. Fe(II) isoleucine dithiocarbamate had a cytotoxicity effect on the MCF-7 cell line (IC50 =613 µg/mL). The complex significantly caused morphological changes in the breast cancer cell line, finally leading to cell apoptosis. CONCLUSION: Cytotoxic test of Fe(II) isoleucine dithiocarbamate showed moderate anticancer activity on MCF-7 cancer cells and showed antiviral activity against SARSCOV-2 by interfering with spike glycoprotein -ACE2 receptors, and inhibiting major proteases and 3Clpro.
Subject(s)
Antineoplastic Agents , COVID-19 Drug Treatment , Coordination Complexes , Angiotensin-Converting Enzyme 2 , Antineoplastic Agents/chemistry , Antiviral Agents/pharmacology , Coordination Complexes/pharmacology , Ferrous Compounds , Humans , Isoleucine , Ligands , Molecular Docking Simulation , Nitrogen , Oxygen , Spectroscopy, Fourier Transform Infrared , SulfurABSTRACT
Ten transition metal dithiocarbamate (DTC)complexes of the type [M(κ 2-Et2DT)2] (1-5), and [M(κ 2-PyDT)2] (6-10) (where M = Co, Ni, Cu, Pd, and Pt; Et2DT = diethyl dithiocarbamate; PyDT = pyrrolidine dithiocarbamate) were synthesized and characterized by different methods. The dithiocarbamate acted as bidentate chelating ligands to afford a tetrahedral complexes with Co(II) ion and square planner with other transition metal ions. The dithiocarbamate complexes showed good activity against the pathogen bacteria species. The results showed the Pt-dithiocarbamate complexes are more active against all the tested bacteria than the Pd-dithiocarbamate complex. The dithiocarbamate complexes displayed the maximum inhibition zone against E. coli bacteria, whereas the lowest activity of the dithiocarbamate against Salmonella typhimurium bacteria. The cytotoxicity of the Pd(II) and Pt(II) complexes was screened against the MCF-7 breast cancer cell line and the complexes showed moderate activity compared with the cis-platin. The results indicated that the MCF7 cells treated with 500 µg\ml of ligands and Pd(II) and Pt(II) complexes after 24 hr exposure showed intercellular space and dead cells. Finally, molecular docking studies were carried out to examine the binding mode of the synthesized compounds against the proposed target; SARS COV2 RNA-dependent RNA polymerase.