4-Methylbenzenecarbothioamide, a hydrogen sulfide donor, inhibits tumor necrosis factor-α and CXCL1 production and exhibits activity in models of pain and inflammation.

The gasotransmitter hydrogen sulfide (H2S) is known to regulate many pathophysiological processes. Preclinical assays have demonstrated that H2S donors exhibit anti-inflammatory and antinociceptive activities, characterized by reduction of inflammatory mediators production, leukocytes recruitment, edema and mechanical allodynia. In the present study, the effects induced by 4-methylbenzenecarbothioamide (4-MBC) in models of pain and inflammation in mice, the mechanisms mediating such effects and the H2S-releasing property of this compound were evaluated. 4-MBC spontaneously released H2S in vitro in the absence of organic thiols. Intraperitoneal (i.p.) administration of 4-MBC (100 or 150 mg/kg) reduced the second phase of the nociceptive response induced by formaldehyde and induced a long lasting inhibitory effect on carrageenan mechanical allodynia. 4-MBC antiallodynic effect was not affected by previous administration of naltrexone or glibenclamide. 4-MBC (50, 100 or 150 mg/kg, i.p.) induced a long lasting inhibitory effect on paw edema induced by carrageenan. The highest dose (150 mg/kg, i.p.) of 4-MBC inhibited tumor necrosis factor-α and CXCL1 production and myeloperoxidase activity induced by carrageenan. Mechanical allodynia and paw edema induced by carrageenan were not inhibited by the 4-MBC oxo analogue (p-toluamide). In summary, 4-MBC, an H2S releasing thiobenzamide, exhibits antinociceptive and anti-inflammatory activities. These activities may be due to reduced cytokine and chemokine production and neutrophil recruitment. The H2S releasing property is likely essential for 4-MBC activity. Our results indicate that 4-MBC may represent a useful pharmacological tool to investigate the biological roles of H2S.

Antioxidant and antifungal activities of Smilax campestris Griseb. (Smilacaceae).

Ethanol extract and fractions obtained from aerial parts of Smilax campestris were examined in order to determine their phenolic composition, antioxidant capacity and antifungal activities. High-performance liquid chromatography coupled with DAD analysis indicated that quercetin and rutin were the main phenolic compounds present in butanol fraction and ethanol extract, respectively. The antioxidant activity assessed by the scavenging ability on 1,1-diphenyl-2-picrylhydrazyl radical was significantly more pronounced for the ethanol extract and butanol fraction than that of the commercial antioxidant 2,6-di-tert-butyl-4-methylphenol. The antifungal activity of extract and fractions was investigated by using microdilution method against five Candida and two Cryptococcus yeast strains. Ethanol extract and fractions exhibited antifungal activities against Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, Candida tropicalis and Cryptococcus gattii. This work provides the knowledge of profile and content of flavonoids and their antioxidant and antifungal activities in the extract and fractions of aerial parts of S. campestris.