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Ipomoea pes-caprae (Convolvulaceae), popularly known as “salsa-da-praia”, is used in folk medicine for the treatment of several diseases, including hypertension. The aim of this research was to evaluate hypotensive activity attributed to this species and identify the bioactive compounds responsible for this effect. Hydroalcoholic extract of aerial parts of Ipomoea pes-caprae (PIEA) was fractionated by column chromatography with Amberlite XAD-2, thus achieving a methanolic fraction (PIEA-M). The chemical profile investigation of PIEA-M was conducted by Ultra Performance Liquid Chromatography coupled to Mass Spectrometry (UPLC-MS) and compound isolation through High Performance Countercurrent Chromatography (HPCCC). Hemodynamic evaluations of PIEA, PIEA-M and isolated compounds were carried out on normotensive rats. The locomotor activity of PIEA and PIEA-M were performed by Rota Rod test using Swiss mice. UPLC-MS analysis of PIEA-M led to the identification of 11 compounds corresponding to seven phenolic acids and four flavonoids. By means of HPCCC, quercetin 6”-O-acetyl-3-O- glucoside (1), a mixture of quercetin-3-O-galactoside and quercetin-3-O- glucoside (2) and quercetin 3-O-glucoside (3) were isolated. PIEA, PIEA-M and the obtained compounds (1 and 2) significantly reduced blood pressure. Also, PIEA and PIEA-M caused significant impairment on mice locomotor activity. These results indicate the potential of Ipomoea pes-caprae as a source of hypotensive agents suggesting that phenolic compounds present in the species are responsible for its hypotensive activity. Resumo Ipomoea pes-caprae (Convolvulaceae), conhecida popularmente como “salsa-da-praia”, é usada na medicina popular para o tratamento de várias doenças, incluindo a hipertensão. O objetivo desta pesquisa foi avaliar a atividade hipotensora atribuída a essa espécie e identificar os compostos bioativos responsáveis por esse efeito. O extrato hidroalcoólico das partes aéreas de Ipomoea pes-caprae (PIEA) foi fracionado por cromatografia em coluna com Amberlite XAD-2, obtendo-se uma fração metanólica (PIEA-M). A investigação do perfil químico de PIEA-M foi realizada por Cromatografia :íquida de Ultra-Eficiência acoplada a Espectrometria de Massas (CLUE-EM) e isolamento de compostos por Cromatografia Contracorrente de Alto Desempenho (CCCAD). Avaliações hemodinâmicas dos PIEA, PIEA-M e compostos isolados foram realizadas em ratos normotensos. A atividade locomotora de PIEA e PIEA-M foi realizada pelo teste de Rota Rod usando camundongos suíços. A análise CLUE-EM do PIEA-M levou à identificação de 11 substâncias correspondentes a sete ácidos fenólicos e quatro flavonoides. Por meio de CCCAD, a quercetina 6”-O-acetil-3-O-glicosídeo (1), uma mistura de quercetina-3-O-galactosídeo e quercetina-3-O-glicosídeo (2) e quercetina 3-O-glicosídeo (3) foram isolados. PIEA, PIEA-M e as substâncias obtidas (1 e 2) reduziram significativamente a pressão sanguínea. Além disso, o PIEA e o PIEA-M causaram um prejuízo significativo na atividade locomotora dos camundongos. Estes resultados indicam o potencial de Ipomoea pes-caprae como fonte de agentes hipotensores, sugerindo que os compostos fenólicos presentes na espécie são responsáveis por sua atividade hipotensora.

WOS: 000374883700008, This study was planned to investigate possible antinociceptive activity of 1,5-diaryl-3-[4-(methylsulfonyl) phenyl]-4,5-dihydro-1H-pyrazole derivatives (2a-s), based on the analgesia-inducing potential of 4,5-dihydro-1H-pyrazole moiety carrying compounds. Tail-clip and hot-plate tests, measuring centrally organized responses to a noxious stimulus, were performed in order to examine antinociceptive potential of the test compounds (100 mg/kg, i.p). In addition, peripherally mediated antinociceptive effect was evaluated by acetic acid-induced writhing tests. Motor coordination of the animals was tested in a Rota-rod apparatus. Among the tested compounds 2c, 2e, 2g, 2h, 2j, 2l, 2m, 2o and 2r prolonged the reaction time, measured in the tail-clip and hot-plate tests, with respect to the control values. The same compounds also decreased the quantity of acetic acid-induced writhing behaviours. In the Rota-rod tests, compound 2r was the only derivative decreasing the falling latency of mice. The obtained results indicated that some of the tested 4,5-dihydro-1H-pyrazole derivatives induce notable antinociceptive activity by effecting both of the central and peripheral nociceptive pathways. In addition, this study provided some information about structure-activity relationship for the compounds carrying similar chemical scaffold. Nevertheless, it should be noted that mechanism of action for these agents should be clarified with further detailed investigations.

Background Achyranthes Aspera Linn., known as Chirchira (Hindi), Agadha (Marathi) is an indigenous herb found in India. The herb has been reported to have variety of activities like antifertility, antihyperlipidemic, antidiabetic, immunomodulatory, anticarcinogenic, diuretic and cardiotonic, analgesic, anti-inflammatory, hypnotic, antifungal and antibacterial activity. It has been also reported to have central anti-nociceptive activity in thermal induced pain methods in our earlier studies. We wanted to study its neuropharmacological effects, which may throw light on understanding the underlying mechanism for its central activity. Purpose The present study was designed to evaluate CNS depressant and behavioral effects of A. Aspera extract and to study the phytochemical responsible for these activities with possible mode of action. Methods The effects on behavioral activity was studied using open field test (OFT). The extract was given intraperitoneally at a dose of 400 mg/kg. Diazepam (2mg/kg body weight i.p.) was used as standard. Data was analyzed by ANOVA test followed by Dunnett’s test. All the results were expressed as Mean (±SEM). P

WOS: 000299691000013, PubMed ID: 21462070, This study was designed to investigate possible antidepressant-like effects of the extract prepared from the flowers of Hypericum montbretti Spach. (Guttiferae, Clusiaceae). Phytochemical constituents of the methanolic extract were analysed by HPLC method. The main flavonoid component was detected as rutin, and another highly concentrated phenolic compound was quercitrin. Antidepressant activity of the extract was examined by tail suspension and modified forced swimming tests, whereas the motor coordination of the animals was tested by the Rota-Rod apparatus. Reboxetine at a dose of 20 mg kg(-1) was used as a reference drug. Dose-dependent antidepressant activity was observed in both tests following the administration of extract at 100 and 250 mg kg(-1) doses. To the best of our knowledge, this is the first study reporting the antidepressant activity of H. montbretti extract. Additionally, the results of this work support previous papers reporting the antidepressant activity of rutin.

WOS: 000266030800031, PubMed ID: 18922604, In the present study, some pyrazoline derivatives were synthesized to investigate their potential antinociceptive activities. 1-[(Benzoxazole/benzimidazole-2-yl)thioacetyl]pyrazoline derivatives were obtained by reacting 3,5-diaryl-1-(2-chloroacetyl)pyrazolines with 2-marcaptobenzoxazole/benzimidazole. The chemical structures of the compounds were elucidated by IR, H-1 NMR and FAB(+)-MS spectral data and Elemental Analyses. All of the compounds (100 mg/kg) exhibited significant antinociceptive activities in both hot plate and acetic acid-induced writhing tests. Naloxone (5 mg/kg) pre-treatment reversed the antinociceptive activities suggesting the involvement of opioid system in the analgesic actions. None of the compounds impaired motor coordination of animals when assessed in the Rota-Rod model. These results support the previous papers reporting the opioid sensitive antinociceptive activities of various benzoxazole/benzimidazole-pyrazoline derivative compounds

Background: Achyranthes aspera Linn., an indigenous herb, has been reported to have antifertility, antihyperlipidemic, antidiabetic, immunomodulatory, anticarcinogenic, diuretic, cardiotonic, analgesic anti-inflammatory, hypnotic, antifungal, antibacterial, and central antinociceptive activities. Aims: This study was designed to evaluate depressant effects on central nervous system (CNS) and behavioral effects of ethanol extract of A. aspera (EEAA) and to find the phytochemical responsible for these activities. Materials and Methods: The pharmacological assays used to study CNS depressant effect in albino mice were rota rod and actophotometer performance test. Effects on behavioral activity were studied using open field test. The extract was given intraperitoneally (i.p.) at a dose of 400 mg/kg. Diazepam (2 mg/kg body weight i.p.) was used as standard. Statistical Analysis Used: Data were analyzed by using analysis of variance followed by Dunnett's test. P < 0.05 was considered significant. Results: Phytochemical screening revealed presence of triterpenoids, saponins, alkaloids (betaine, achyranthine), and steroids as major constituents. The result of this study reflected that EEAA (400 mg/kg i.p.) decreased locomotor activity, produced muscle relaxation, and showed anxiolytic activity. Conclusions: EEAA exhibit CNS depressant and significant anxiolytic activity comparable to diazepam.