Synthesis, characterization, crystal structure and in vitro antiproliferative assays of the 2-thiouracilato(triphenylphosphine)gold(I) complex

In Silico, In Vitro, and In Vivo Antitumor and Anti-Inflammatory Evaluation of a Standardized Alkaloid-Enriched Fraction Obtained from Boehmeria caudata Sw. Aerial Parts

“…By evaluating mean tumor volume variation (MTVV, %) during fifteen experimental days, all treatments (BcAEF, doxorubicin and piroxicam) promoted significant reduction in tumor growth in comparison to vehicle-treated animals from the 9th day on (Figure 5A). Considering the last experimental day (15th day), doxorubicin (chemotherapeutic agent control) inhibited tumor progression by 45 40.71% (166.56 ± 9, 85), and 36.41% (178.64 ± 21.91) at 3, 10, and 30 mg kg −1 respectively, in comparison to Erhlich-bearing mice in the vehicle group (280.91 ± 38.27). During the whole experiment, the animals from the experimental groups (3, 10, and 30 mg kg −1 doses of BcAEF and 30 mg kg −1 dose of BcAEF without tumor) and those treated with piroxicam showed a body weight evolution similar to that observed for naïve (Satellite group) and Ehrlich-bearing mice from the vehicle group.…”

“…The antiproliferative activity of BcAEF was tested on all nine human tumor cell lines and in the non-tumor line, being determined by the sulforhodamine B assay as previously described [7,44]. The TGI values (concentration that inhibits 100% cell growth) were determined through non-linear regression, type sigmoidal, analyzed using Origin 8.0 software (OriginLab Corporation, Northampton, MA, USA) [7,45]. BcAEF was tested in final concentrations of 0.0025, 0.025, 0.25 and 2.5 µg mL −1 .…”

Investigation of the anticancer activities and mechanisms of action of metal complexes with bioactive ligands

“…Nevertheless, due the severe toxicities of gold cyanide compounds, Jacques Forestier identified the biological activities of thiolate gold compounds, which were further applied in the treatment of rheumatoid arthritis (RA) [70]. One of the most representative drugs of this type is auranofin (Figure 4), an orally administered thiolate phosphine gold(I) coordination compound [77]. Auranofin presents a two-coordination linear geometry.…”

“…Because of the context of auranofin, gold(I) phosphine compounds have been evaluated as potential anticancer agents [77,[81][82][83][84]. For example, studies have shown that larger and more lipophilic substituents of the phosphine enhance the cytotoxicity of the gold compounds [85], while the thiosugar moiety, present in auranofin, is not mandatory for its pharmacological action [86].…”