Pro-ejaculatory effect of the aqueous crude extract of cihuapatli (Montanoa tomentosa) in spinal male rats.

In the present study, the pro-sexual effect of the cihuapatli (Montanoa tomentosa) and its possible pro-ejaculatory properties in spinal male rats were examined. Systemic administration of the aqueous crude extracts of Montanoa tomentosa exerted a pro-ejaculatory effect and produced an increase in the number of discharges in the ejaculatory motor patterns in the spinal rats. The cihuapatli-induced ejaculatory responses included the expression of penile erections and penile movements and the potent expulsion of urethral contents and in some cases the expulsion of seminal plugs. The cihuapatli-induced ejaculatory motor patterns were similar to that obtained after systemic oxytocin. Cihuapatli- and oxytocin-induced ejaculatory motor responses and the penile erections and movements were abolished by the pre-treatment with hexamethonium, a selective oxytocin antagonist. Present data show that the cihuapatli extract acts directly at the spinal system in charge of the expression of the ejaculatory motor patterns and suggest that the aqueous crude extract exerts its aphrodisiacs properties by increasing sexual potency acting as an oxytocic agent.

Biosynthesis of uterotonic diterpenes from Montanoa tomentosa (zoapatle).

Montanoa tomentosa (zoapatle) is a Central American plant used in Mexico in traditional herbal medicine to ease childbirth labor and to cure certain female disorders. Recently, crude extracts of M. tomentosa have been reported to have an aphrodisiacal effect on male rats. The bioactive molecules are the uterotonic diterpenes kaurenoic acid (KA), grandiflorenic acid (GF), and monoginoic acid (MO). Roots of M. tomentosa contain all three diterpenes, whereas in leaves only kaurenoic and GF are present. However, despite the pharmacological importance of these compounds, specific information about their biosynthesis and localization in the plant is not available. In this investigation, we followed the metabolic transformation of a tritium-labeled diterpene-precursor via geranylgeranyl diphosphate into each of the three diterpenes. Inhibitors of gibberellin biosynthesis were used to elucidate the sequence of conversion of the intermediates. Our results suggest the biosynthetic conversion of KA into GF by a putative cytochrome P450-like desaturase. Partial characterization of the enzyme revealed that it requires NADPH and O2 but is inhibited by 50 microM paclobutrazol, suggesting a cytochrome P450 desaturase like enzyme (EC 1.14.14.-). Optimal reaction conditions are 32 degrees C and a pH of 7.6, respectively. Apparent kinetics parameters for KA gave a K(m,app) of 36.31 microM, and a V(max, app) of 13.6 nmol KA mg(1)protein h(-1). Based on the data presented, a putative biosynthetic pathway is proposed for the uterotonic diterpenes of M. tomentosa.