Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives

Guanylhydrazones have shown promising antitumor activity in preclinical tumor models in several studies. In this study, we aimed at evaluating the cytotoxic effect of a series of synthetic guanylhydrazones. Different human tumor cell lines, including HCT-8 (colon carcinoma), MDA-MB-435 (melanoma) and SF-295 (glioblastoma) were continuous exposed to guanylhydrazone derivatives for 72 hours and growth inhibition of tumor cell lines and macrophages J774 was measured using tetrazolium salt (MTT) assay. Compounds 7, 11, 16 and 17 showed strong cytotoxic activity with IC50 values lower than 10 μmol L–1 against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, the obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents

Anti-inflammatory effects of methanolic extract of green algae Caulerpa mexicana in a murine model of ulcerative colitis

Inflammatory bowel diseases, which include Crohn's disease and ulcerative colitis, are characterized by chronic and relapsed gut inflammation. Caulerpa mexicana is a type of green marine algae that can be found in tropical areas, such as the Brazilian Coastland. These macrophytes exhibit in vitro and in vivo anti-inflammatory properties such as the ability to reduce both cell migration to different sites and edema formation induced by chemical irritants. The aim of this study was to examine the effect of the C. mexicana methanolic extract on the treatment of colitis induced by dextran sodium sulfate. Acute experimental colitis was induced in BALB/c mice by treatment with 3% dextran sodium sulfate orally for 14 days. During this 14-day period, C. mexicana methanolic extract (2 mg/kg/day) was given intravenously on alternate days. Treatment with the methanolic extract significantly attenuated body weight loss and severe clinical symptoms. This was associated with a remarkable amelioration of colonic architecture disruption and a significant reduction in pro-inflammatory cytokine production. These results suggest that the anti-inflammatory action of C. mexicana methanolic extract on colorectal sites may be a useful therapeutic approach for inflammatory bowel diseases

Highly functionalized piperidines: Free radical scavenging, anticancer activity, DNA interaction and correlation with biological activity

Twenty-five piperidines were studied as potential radical scavengers and antitumor agents. Quantitative interaction of compounds with ctDNA using spectroscopic techniques was also evaluated. Our results demonstrate that the evaluated piperidines possesses different abilities to scavenge the radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the anion radical superoxide (·O2−). The piperidine 19 was the most potent radical DPPH scavenger, while the most effective to ·O2− scavenger was piperidine 10. In general, U251, MCF7, NCI/ADR-RES, NCI-H460 and HT29 cells were least sensitive to the tested compounds and all compounds were considerably more toxic to the studied cancer cell lines than to the normal cell line HaCaT. The binding mode of the compounds and ctDNA was preferably via intercalation. In addition, these results were confirmed based on theoretical studies. Finally, a linear and exponential correlation between interaction constant (Kb) and GI50 for several human cancer cell was observed

Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives

Guanylhydrazones have shown promising antitumor activity in preclinical tumor models in several studies. In this study, we aimed at evaluating the cytotoxic effect of a series of synthetic guanylhydrazones. Different human tumor cell lines, by including HCT-8 (colon carcinoma), MDA-MB-435 (melanoma) and SF-295 (glioblastoma) were continuous exposed to guanylhydrazone derivatives for 72 hours and growth inhibition of tumor cell lines and macrophages J774 was measured using tetrazolium salt (MTT) assay. Compounds 7, 11, 16 and 17 showed strong cytotoxic activity with IC50 values lower than 10 μmol L−1 against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents