Prosexual Effect of Chrysactinia mexicana A. Gray (Asteraceae), False Damiana, in a Model of Male Sexual Behavior.

Chrysactinia mexicana A. Gray (Asteraceae) and Turnera diffusa Willd (Turneraceae) are employed in traditional medicine as aphrodisiacs; however, there is no scientific evidence supporting the prosexual properties of C. mexicana. The aim of this study was to determine whether an aqueous extract of C. mexicana (Cm) stimulates rat male sexual behavior in the sexual exhaustion paradigm. Sexually exhausted (SExh) male rats were treated with Cm (80, 160, and 320 mg/kg), an aqueous extract of T. diffusa (Td), or yohimbine. The sexual exhaustion state in the control group was characterized by a low percentage of males exhibiting mounts, intromissions, and ejaculations and no males demonstrating mating behavior after ejaculation. Cm (320 mg/kg), Td, or yohimbine significantly increased the proportion of SExh rats that ejaculated and resumed copulation after ejaculation. In males that exhibited reversal of sexual exhaustion, Cm (320 mg/kg) improved sexual performance by reducing the number of intromissions and shrinking ejaculation latency. The effects of treatments on sexual behavior were not related with alterations in general locomotion. In conclusion, the prosexual effects of Cm, as well as those of Td, are established at a central level, which supports the traditional use of C. mexicana for stimulating sexual activity.

Pro-sexual effects of Turnera diffusa Wild (Turneraceae) in male rats involves the nitric oxide pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: Turnera diffusa Wild has been used in folk medicine by its aphrodisiac and tranquilizing properties. Previously we experimentally showed the aphrodisiac effect of a chemically characterized aqueous extract of Turnera diffusa in male rats. However, the mechanism of action underlying such effects has not been studied. STUDY AIMS: As part of our systematic studies of pharmacological properties of Turnera diffusa, we aimed to analyze whether the increased sexual motivation and the augmented sexual performance of sexually sluggish (SL) male rats treated with Turnera diffusa involves the NO pathway. Additionally we analyzed whether such effects were exerted at the level of the brain or the spinal cord. Finally, anxiety levels and ambulatory activity were also evaluated. MATERIAL AND METHODS: Turnera diffusa (10-40 mg/kg) and sildenafil citrate (10 mg/kg) with or without a nonspecific inhibitor of NO synthase, Nω-nitro-L-arginine methyl esther (L-NAME, 12.5 mg/kg) were evaluated in SL rats, in a standard sexual behavior test and in the fictive ejaculation model in spinal cord transected and urethane-anaesthetized SL rats. Anxiety levels or ambulation were assessed in the burying behavior and open-field tests. RESULTS: Turnera diffusa and sildenafil (both at 10 mg/kg) facilitated expression of male sexual behavior by shortening mainly ejaculation latency. Treatments also facilitated the number of discharges in the ejaculatory motor pattern as well as the number of ejaculatory motor patterns and its associated penile erections. L-NAME prevented the pro-sexual effects of treatments on both experimental models. Besides, the extract of Turnera diffusa (10 mg/kg) produced an anxiolytic-like effect in male rats without affecting ambulation. CONCLUSIONS: Findings from the present work support the notion that pro-sexual effect of the aqueous extract of Turnera diffusa in rats involves the participation of NO pathway, mainly at central level. The anxiolytic-like effect of Turnera diffusa is an advantage to its use for improving sexual performance.

Neuropharmacological study of Dracocephalum moldavica L. (Lamiaceae) in mice: sedative effect and chemical analysis of an aqueous extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Dracocephalum moldavica is used as a tranquilizer and as remedy for nervous conditions relief in the Mexican traditional medicine. Despite its intensive use no literature reported neuropharmacological studies on Dracocephalum moldavica as yet. AIM OF THE STUDY: The sedative, anxiolytic-like and antidepressant-like effects of the aqueous extract of aerial parts of Dracocephalum moldavica (Lamiaceae) (DM) were evaluated in behavioral models in mice. The general toxic effects of DM were evaluated as well as their chemical analysis was performed. MATERIALS AND METHODS: DM effects were evaluated on pentobarbital-induced sleeping time (SPT), the hole-board (HBT), and the avoidance exploratory behavior (AEBT) tests and on the forced swimming test (FST). General activity and motor coordination were evaluated in the open field (OFT) and Rota-rod tests, respectively. The acute toxicity of DM was determinate by its LD(50) dose. The chemical analyses DM were performed by chromatographic and HPLC-ESI-MS techniques. RESULTS: DM prolonged the pentobarbital-induced sleeping time, induced sedation in the HBT, decreased spontaneous activity and produced motor coordination impairment in mice. However, DM did not show anxiolytic effects in the AEBT or HBT and it was not effective in FST. The DM-treatment produced mortalities with LD(50)=470 mg/kg body weight. The HPLC-ESI-MS analysis of DM revealed that (acacetin, apigenin and luteolin)-7-O-ß-D-(6″-O-malonyl)-glucoside derivates are the main compounds of DM. CONCLUSIONS: DM induced sedative actions and a general inhibition of CNS activity observed by the decrease of animals' general activity, motor coordination and exploration.

Antidepressant-like effects of an alkaloid extract of the aerial parts of Annona cherimolia in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Several species of Annona (Annonaceae) are used in traditional Mexican medicine by their anti-anxiety, anticonvulsant and tranquilizing properties. It has been reported that the alkaloids isolated from some species of the Annona have affinity to serotonergic 5-HT(1A) receptors and modulate dopaminergic transmission, which is involved in depressive disorders. AIM OF THE STUDY: To investigate the antidepressant-like effect of an alkaloid extract from the aerial parts of Annona cherimola (TA) in mice. MATERIALS AND METHODS: The antidepressant-like effect was evaluated in the forced swimming test. To elucidate a possible mechanism of action, experiments of synergism with antidepressant drugs, such as imipramine (IMI), clomipramine (CLIMI), and fluoxetine (FLX), were carried out. The neurotransmitter content (DA: dopamine, 5HT: serotonin and its metabolites, HVA: homovanillic acid and 5HIAA: 5-hydroxyindoleacetic) in the whole brain of mice were also determined by HPLC method. TA chemical composition was determined using high performance liquid chromatography-electrospray mass spectrometry. RESULTS: The results showed that repeated treatment with TA produced antidepressant-like effects in mice. This effect was not related to an increase in locomotor activity. Administration of TA facilitated the antidepressant effect of IMI and CLIMI as well as increased the turnover of DA and 5-HT. The alkaloids: 1,2-dimethoxy-5,6,6a,7-tetrahydro-4H-dibenzoquinoline-3,8,9,10-tetraol, anonaine, liriodenine, and nornuciferine were the main constituents of TA. CONCLUSIONS: Results showed that TA produces an antidepressant-like action from a generalized increase in monominergic turnover, supporting the use in tradicional medicine of Annona cherimolia, and strongly suggest its therapeutic potency as an antidepressant agent.

Depressant effects of Clinopodium mexicanum Benth. Govaerts (Lamiaceae) on the central nervous system.

ETHNOPHARMACOLOGICAL RELEVANCE: The decoction of leaves of Clinopodium mexicanum Benth. Goaverts (Lamiaceae), commonly known as "Toronjil de Monte", is used in the Mexican traditional medicine to induce sleep, as well as sedative and analgesic remedy. AIM OF THE STUDY: To evaluate the putative depressant effects of an aqueous extract of the medicinal plant Clinopodium mexicanum on the central nervous system (CNS). MATERIALS AND METHODS: The effects of the extract (AECM) on mice were tested in several animal paradigms, including sodium pentobarbital-induced sleep, open field tests, and hole-board tests. The effects of AECM on pentylenetetrazole- and picrotoxin-induced convulsions in mice and on the antithermonociceptive response in the hot-plate paradigm were also tested. Additionally, the active extract (AECM) was analyzed with HPLC-ESI-MS techniques. RESULTS: Mice acutely treated with AECM at 100, 200, 500 and 1000mg/kg doses prolonged the sleeping time induced by sodium pentobarbital (42mg/kg). This extract, at 100 and 200mg/kg doses, showed a sedative effect in the hole-board paradigm and decreased spontaneous activity in mice. AECM at 10, 100 and 200mg/kg prolonged the onset of seizures induced by pentylenetetrazole (90mg/kg) and antagonized tonic convulsions induced by picrotoxin (10mg/kg). Additionally, AECM inhibited the response to a thermonociceptive stimulus. The intraperitoneal AECM treatment produced mortality with an LD(50)=2154mg/kg. Chemical analysis showed that the flavanone glycosides neoponcirin, poncirin, and isonaringenin are the main compounds of the active extract. CONCLUSIONS: This study demonstrates that an acutely administered single dose of an aqueous extract of Clinopodium mexicanum can exert depressant effects on the CNS. These findings are in agreement with the traditional use of Clinopodium mexicanum to induce sleep as well as sedative and analgesic remedy. The chemical analysis of AECM revealed the presence of the flavanone glycosides neoponcirin, poncirin, and isonaringin.

Turnera diffusa Wild (Turneraceae) recovers sexual behavior in sexually exhausted males.

ETHNOPHARMACOLOGICAL RELEVANCE: In folk medicine, Turnera diffusa Wild (Turnera diffusa, Turneraceae) is considered as an aphrodisiac, but its ability to restore copulation in sexually inhibited subjects has not been reported. AIM OF THE STUDY: To determine whether Turnera diffusa recovers sexual behavior in sexually exhausted (SExh) male rats and to identify the main components in an aqueous extract. MATERIALS AND METHODS: SExh males were treated with Turnera diffusa, 20-80 mg/kg, yohimbine, 2 mg/kg, or vehicle. RESULTS: Yohimbine and Turnera diffusa (80 mg/kg) significantly increased the percentage of males achieving one ejaculatory series and resuming a second one. In addition, Turnera diffusa significantly reduced the post-ejaculatory interval. These effects were not associated to an increase in locomotor activity or anxiety-like behaviors. The HPLC-ESI-MS analysis showed the presence of caffeine, arbutine, and flavonoids as the main compounds in the active extract. CONCLUSION: The results support the use of Turnera diffusa as an aphrodisiac in traditional medicine and suggest possible therapeutic properties of Turnera diffusa on sexual dysfunction. The flavonoids present in active extract may participate in its pro-sexual effect, which is analogous to those produced by yohimbine, suggesting a shared mechanism of action.

Anxiolytic-like actions of the hexane extract from leaves of Annona cherimolia in two anxiety paradigms: possible involvement of the GABA/benzodiazepine receptor complex.

A hexane extract of leaves of Annona cherimolia produced anxiolytic-like actions when administered to mice and tested in two animal models of anxiety: the mouse avoidance exploratory behavior and the burying behavior tests. In order to discard unspecific drug-actions on general activity, all treatments studied in the anxiety paradigms were also analyzed in the open field test. Results showed that A. cherimolia induced anxiolytic-like actions at the doses of 6.25, 12.5, 25.0 and 50.0 mg/kg. Picrotoxin (0.25 mg/kg), a GABA-gated chloride ion channel blocker, antagonized the anxiolytic-like actions of A. cherimolia, while a sub-effective dose of muscimol (0.5 mg/kg), a selective GABA(A) receptor agonist, facilitated the effects of a sub-optimal dose of A. cherimolia (3.12 mg/kg). Thus, the involvement of the GABA(A) receptor complex in the anxiolytic-like actions of A. cherimolia hexane extract is suggested. In addition the extract was also able to enhance the duration of sodium pentobarbital induced sleeping time. Taken together, results indicate that the hexane extract of A. cherimolia has depressant activity on the Central Nervous System and could interact with the GABA(A) receptor complex. On the other hand, the chromatographic separation of this extract led to the isolation of palmitone, and beta-sitosterol as major constituents. In addition a GC-MS study of some fractions revealed the presence of several compounds such beta-cariophyllene, beta-selinene, alpha-cubebene, and linalool that have been reported to show effects on behavior that could explain some of the extract effects.