Synthesis, characterization, and evaluation of biological activities of new 4′‐substituted ruthenium (II) terpyridine complexes: Prospective anti‐inflammatory properties

Abstract

The synthesis and characterization of Ru (II) terpyridine complexes derived from 4′ functionalized 2,2′:6′,2″‐terpyridine (tpy) ligands are reported. The heteroleptic complexes comprise the synthesized ligands 4′‐(2‐thienyl)‐ 2,2′:6′,2″‐terpyridine) or (4′‐(3,4‐dimethoxyphenyl)‐2,2′:6′,2″‐terpyridine and (dimethyl 5‐(pyrimidin‐5‐yl)isophthalate). The new complexes [Ru(4′‐(2‐thienyl)‐2,2′:6′,2″‐terpyridine)(5‐(pyrimidin‐5‐yl)‐isophthalic acid)Cl2] (9), [Ru(4′‐(3,4‐dimethoxyphenyl)‐2,2′:6′,2″‐terpyridine)(5‐(pyrimidin‐5‐yl)‐isophthalic acid)Cl2] (10), and [Ru(4′‐(2‐thienyl)‐2,2′:6′,2″‐terpyridine)(5‐(pyrimidin‐5‐yl)‐isophthalic acid)(NCS)2] (11) were characterized by 1H‐ and 13C‐NMR spectroscopy, C, H, N, and S elemental analysis, UPLC‐ESI‐MS, TGA, FT‐IR, and UV‐Vis spectroscopy. The biological activities of the synthesized ligands and their Ru (II) complexes as anti‐inflammatory, antimicrobial, and anticancer agents were evaluated. Furthermore, the toxicity of the synthesized compounds was studied and compared with the standard drugs, namely, diclofenac potassium and ibuprofen, using hemolysis assay. The results indicated that the ligands and the complex 9 possess superior anti‐inflammatory activities inhibiting albumin denaturation (89.88–100%) compared with the standard drugs (51.5–88.37%) at a concentration of 500 μg g−1. These activities were related to the presence of the chelating N‐atoms in the ligands and the exchangeable chloro‐ groups in the complex. Moreover, the chloro‐ and thiophene groups in complex 9 produce a higher anticancer activity compared with its isothiocyanate derivative in the complex 11 and the 3,4‐dimethoxyphenyl moiety in complex 10. Considering the toxicity results, the synthesized ligands are nontoxic or far less toxic compared with the standard drugs and the metal complexes. Therefore, these newly synthesized compounds are promising anti‐inflammatory agents in addition to their moderate unique broad antimicrobial activity.

Evaluation of the potential therapeutic anti-inflammatory, anti-proliferative, and apoptotic effects of Viburnum tinus leaves different extracts.

“…The powerful anti-tumor agent should eliminate cancer cells without any negative impacts possible on normal cells by what described as selective index (SI).The higher the SI value, the more selectivity it is. The SI value of more than 10 was thought to be anticancer, whereas a value of less than 2 was assumed to be hazardous [20], In the current data, MeOH has the highest selective index on HepG2, followed by crude extract and CH 2 Cl 2 , with n-Hexane having the lowest, while MeOH has the highest selective index in Caco2, followed by n-Hexane, crude extract, and CH 2 Cl 2 , while n-Hexane has the highest selective index against MCF7, followed by CH 2 Cl 2 , crude extract, and finally MeOH. All of the extracts have a greater SI, indicating that various extracts have distinct anticancer effectiveness on various cell types.…”

“…The anti-inflammatory activity of V.tinus leaves different extracts Crude , CH 2 CL 2 (fraction), n-Hexane(fraction), MeOH (fraction) were evaluated using the following assays Protein denaturation inhibition [ [17]; [18]], Proteinase inhibition [ [19]] , Membrane stabilization [ [20] and [21]] and Inflammatory cytokine inhibition [ [22] , [21] ; [23]] assays with modifications . Diclofenac potassium (Catafast 50mg) obtained from Novartis was used as reference drug.…”

Synthesis and anti-infective potency study of a Ru-based complex bearing benzonitrile against Staphylococcus aureus

“…[11][12][13] Compared with organic molecules, Ru-based complexes are easy to modify in terms of structure and morphology, and have excellent photostability and DNA binding ability. [14][15][16][17] Therefore, they have been widely investigated for use as antibacterial, anti-cancer, and anti-malarial agents, amongst other uses. For example, arene ruthenium(II) complexes containing benzhydrazone derivative ligands exhibit excellent potency against both Grampositive and Gram-negative bacteria.…”