In vitro Biological Activities of Gold(I) and Gold(III) Bis(N-Heterocyclic Carbene) Complexes

Abstract

The aim of this research is to evaluate for the first time the in vitro leishmanicidal activity and inhibition of a-glucosidase and b-glucuronidase of new gold(I) and gold(III) complexes involving N-heterocyclic carbene (NHC) ligands, with the general formula [Au(X) n (NHC)R 2 ][BF 4 ] (X=Cl, OAc, R = various aromatic and aliphatic substituents). The Au(III) complexes were shown to have a significant antileishmanial activity, and were also found to be more potent inhibitors of a-glucosidase and b-glucuronidase enzymes than the standard drugs. Some complexes were also identified as potent anti-inflammatory agents with activity comparable to that of tested standard drugs, allopurinol and ibuprofen. These gold complexes were also evaluated for their in vitro cytotoxic activity against HeLa (cervical cancer), MCF-3 (breast cancer), and 3T3 (mouse fibroblast) cell lines.Recent advancements in transition-metal-based compounds have found wide medical applications. The use of cisplatin to treat ovarian cancer and the discovery of the gold-based drug auranofin to treat rheumatoid arthritis are among the numerous examples that have seen transition metal complexes combat human ailments. Nowadays, large libraries of platinum-, palladium-, ruthenium-and gold-containing molecules are being synthesized for therapeutic purposes. [1][2][3]

In vitro Anti‐atherogenic Properties of N‐Heterocyclic Carbene Aurate(I) Compounds

“…PAF‐R antagonists have exhibited promising results in vitro and in vivo as anti‐angiogenic molecules in several cancer cells and tumors . Gold complexes similar to those tested in this study have already exhibited anti‐inflammatory activity (respiratory burst assay) and cytotoxicity against HeLa (cervical cancer), MCF‐3 (breast cancer), and 3T3 (mouse fibroblast) cell lines . Notably, PAF has been implicated in coordinating angiogenesis, oncogenic transformation, tumor growth, and metastasis in cancer (AA).…”

“…Furthermore, it has been demonstrated that the PAF‐R antagonist PCA4248 has inhibited experimental human melanoma lung metastasis in nude mice . Therefore, as similar gold complexes to those synthesized for this study possess anticancer activity, further research on the antagonistic actions of the herein presented aurates against the PAF‐R is warranted and currently ongoing in our group, as they are potentially powerful anti‐metastatic agents.…”

“…Cisplatin has since then, shown to inhibit PAF‐induced platelet aggregation . Previous research on gold metal complexes has shown that they also possess putative bioactivities that may be useful in medicinal applications, particularly in relation to cancer treatment . To date, only two gold salts have been developed for medicinal purposes, Au I thiolate and auranofin (Au I thiolate triethylphosphine), which have been used in the treatment of rheumatoid arthritis .…”

“…Two other compounds were tested to quantify any background activity for ligand and neutral complexes. Compound A , [IPr⋅HCl], was examined to study the activity, if any, of the imidazolium ligand and compound B , [AuCl(IPr)], to model the neutral Au I system . Compound A contains the IPr core without the gold moiety (only Cl − as counterion; this will serve as a blank and will thus allow us to confirm the need for the gold moiety when compared with its close counterpart complex 1 ) and compound B represents another class of gold complexes that have shown potential in previous biological studies, though having lower activity than the aurate‐class showcased herein.…”

Synthesis of New Chiral (R)‐BINOL Derivatives under Microwave Irradiation and Evaluation of Their Antibacterial and α‐Glucosidase Inhibitory Activity

“…Diabetes is a group metabolic disorder characterized with high blood sugar levels over a long time. Frequent urination, increased thirst, and increased hunger are caused by high blood sugar, which if not addressed to, will result in serious health issues such as diabetic ketoacidosis, hyperosmolar hyperglycemic state, or death, cardiac and vascular diseases, thrombosis, stroke, chronic kidney disease, foot ulcers, and damage to the eyes ,,. Causes of diabetes are either the pancreas fail to produce enough insulin, or the cells of the body fail to respond adequately to the insulin produced.…”