Fernanda Lima Both

Analgesic Properties of Umbellatine from Psychotria umbellata

Interesting analgesic activity has been previously identified in alkaloids isolated from the genus Psychotria (Rubiaceae). We here report the analgesic activity of umbellatine, a new glycoside indole monoterpene alkaloid isolated from Psychotria umbellata. Umbellatine produced a dose-dependent (100-300 mg/kg) analgesic effect, partially reversed by naloxone, in the tail-flick and hot-plate models. These results suggest an analgesic effect at least in part associated with the activation of opioid receptors. In the formalin- and capsaicininduced pain models, umbellatine (100-300 mg/kg) elicited significant and dose-related antinociception. Umbellatine acts synergistically when co-administered with the NMDA antagonist MK-801. These results indicate the involvement of NMDA receptors in the umbellatine mechanism of action. Such a combined mode of action can be of relevance for developing analgesics useful in neurophatic pain.

Diphenyl diselenide exerts anxiolytic-like effect in Wistar rats : Putative roles of GABAA and 5HT receptors

Diphenyl diselenide [(PhSe)2] is an organoselenium compound which presents pharmacological antioxidant, anti-inflammatory, antinociceptive and antidepressant properties. The present study was designed to investigate the anxiolytic effect of (PhSe)2 in rats, employing the elevated plus maze task. The involvement of 5HT and GABA receptors in the anxiolytic-like effect was also evaluated. (PhSe)2 (5, 25 and 50 micromol/kg, i.p.) did not affect locomotor activity as evaluated in the open open-field test, and learning and memory when assessed in the inhibitory foot-shock avoidance task. However, (PhSe)2 at the 50 micromol/kg dose produced signs of an anxiolytic action, namely a decreased number of fecal boli in the open-field arena and an increased time spent in as well as an increased number of entries to the open arms of the elevated plus maze test. To evaluate the role of GABA and 5HT receptors in the anxiolytic-like effect of (PhSe)2, a selective GABAA receptor antagonist bicuculline, (0.75 mg/kg, i.p.), a non-selective 5HT2A/2C receptor antagonist, ritanserin (2 mg/kg, i.p.), a selective 5HT2A receptor antagonist, ketanserin (1 mg/kg, i.p.), and a selective 5HT1A receptor antagonist, WAY100635 (0.1 mg/kg, i.p.) were used. All the antagonists used were able to abolish the anxiolytic effect of (PhSe)2 suggesting that GABAA and 5HT receptors may play a role in the pharmacological property of this selenocompound in the central nervous system.