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An efficient synthetic protocol was devised for the preparation of five cationic ruthenium-arene complexes bearing imidazol(in)ium-2-dithiocarboxylate ligands from the [RuCl2(p-cymene)]2 dimer and 2 equiv of an NHC·CS2 zwitterion. The reactions proceeded cleanly and swiftly in dichloromethane at room temperature to afford the expected [RuCl(p-cymene)(S2C·NHC)]Cl products in quantitative yields. When the [RuCl2(p-cymene)]2 dimer was reacted with only 1 equiv of a dithiolate betaine under the same experimental conditions, a set of five bimetallic compounds with the generic formula [RuCl(p-cymene)(S2C·NHC)][RuCl3(p-cymene)] was obtained in quantitative yields. These novel, dual anionic and cationic ruthenium-arene complexes were fully characterized by various analytical techniques. NMR titrations showed that the chelation of the dithiocarboxylate ligands to afford [RuCl(p-cymene)(S2C·NHC)]+ cations was quantitative and irreversible. Conversely, the formation of the [RuCl3(p-cymene)]- anion was limited by an equilibrium, and this species readily dissociated into Cl- anions and the [RuCl2(p-cymene)]2 dimer. The position of the equilibrium was strongly influenced by the nature of the solvent and was rather insensitive to the temperature. Two monometallic and two bimetallic complexes cocrystallized with water, and their molecular structures were solved by X-ray diffraction analysis. Crystallography revealed the existence of strong interactions between the azolium ring protons of the cationic complexes and neighboring donor groups from the anions or the solvent. The various compounds under investigation were highly soluble in water. They were all strongly cytotoxic against K562 cancer cells. Furthermore, with a selectivity index of 32.1, the [RuCl(p-cymene)(S2C·SIDip)]Cl complex remarkably targeted the erythroleukemic cells vs mouse splenocytes., info:eu-repo/semantics/published

Ethnopharmacological relevance Respiratory diseases and asthma, in particular, are nowadays a global health problem. In Rwanda, some traditional healers claim to treat asthma with plant-based recipes, though there is no scientific proof so far. Aim of the study Our study aimed at evaluating the toxicity and the anti-inflammatory effect of plant recipes used in Rwanda against asthma in order to select potential candidates for further characterization of the active compounds. Materials and methods Water (aqueous) and methanol-dichloromethane (organic) extracts from selected folkloric recipes were submitted for toxicity test on THP-1 derived macrophages using CellTiter-Glo Luminescent Cell Viability Assay. The evaluation of the anti-inflammatory effect of the plant extracts was carried out using the Caspase-Glo 1 Inflammasome assay on THP-1 -derived macrophages. Results Most of both organic and aqueous extract showed more than 95% of cell viability up to 200 µg/ml, except for R03Cn organic extract that inhibited 25% of the cell viability. Plant extracts inhibited caspase-1 activation in THP-1 derived macrophages in a dose-dependent manner. Four extracts (R03Cn and R07Kn aqueous extracts, R10MK and R19Sz organic extracts) strongly downregulated the activation of caspase-1 (more than 70% at 50 µg/ml). In general, organic extracts exhibited better caspase-1 inhibitory effects than their aqueous counterparts. Conclusions The inhibition of inflammasome/caspase-1 is one of key mechanisms of action in asthma. Some traditional recipes are active on this mechanism and are thus strong candidates for the treatment of asthma and other inflammasome-mediated diseases. Further investigations are needed to characterize active molecules.

Following an ethnobotanical survey in Southern Rwanda for hepatoprotective remedies, four food and medicinal plants, Crassocephalum vitellinum, Guizotia scabra, Microglossa pyrifolia and Ocimum lamiifolium, were selected for pharmacological and chemical investigations aiming to validate their reported properties. The chemical compositions of essential oils obtained from leaves were investigated by GC-MS; essential oils and methanolic extracts were evaluated for antioxidant activity by 1,1-diphenyl-2-picryhydrazyl (DPPH) and linoleic acid peroxidation assays. C. vitellinum [limonene (34.8%), (E)-β-ocimene (21.8%), β-pinene (8.5%), α-pinene (6.6%), myrcene (6.3%)], G. scabra [germacrene-d (25.5%), limonene (9.7%), (E)-β-ocimene (6.6%)], M. pyrifolia [germacrene-d (58.3%)] and O. lamiifolium [sabinene (12.2%), alpha phellandrene (11.6%)] volatile oils scavenge DPPH (10%, 39%, 27%, and 11% quercetin equivalents) and inhibit linoleic acid peroxidation (13%, 23%, 20%, and 13% Trolox® equivalents). The four methanolic extracts were quite active on the lipid peroxidation model (93%, 93%, 70%, and 67% Trolox equivalents) with modest activity on DPPH (5%, 10%, 8%, and 11% quercetin equivalents). These properties most probably participate in the four plants hepatoprotective activities reported in ethnopharmacological and/or pharmacological studies.