Chemical constituents of Cardiospermum corindum L. and their distribution in Sapindaceae

AbstractPhytochemical investigation on the aerial parts of Cardiospermum corindum L. led to the isolation of two triterpenes [friedelin (1) and friedelinol (2)], two coumarins, [umbelliferone (4) and scopoletin (5)], three methoxylated flavones [umuhengerin (3), luteolin 3’,4’-dimethyl ether (6) and chrysoeriol (7)], one non-cyanogenic glucoside [epidermin (8)] and one cyclitol [(L)-quebrachitol (9)]. To our knowledge, 2, 3, 6 and 8 were isolated for the first time within Sapindaceae. Of these classes of metabolites, the distribution of methoxylated flavonoids in Cardiospermum is reviewed, including the new records, indicating that polymethoxylated flavonoid (3) may be value as chemotaxonomic markers for this genus

Antimicrobial, Antiproliferative and Proapoptotic Activities of Extract, Fractions and Isolated Compounds from the Stem of Erythroxylum caatingae Plowman

In the study, we have examined the antitumor and antimicrobial activities of the methanol extract, the fractions, a fraction of total alkaloids and two alkaloids isolated from the stem of Erythroxylum caatingae Plowman. All test fractions, except the hexane fractions, showed antimicrobial activity on gram-positive bacteria and fungi. The acetate: methanol (95:5), acetate, chloroform and hexane fractions show the highest cytotoxicity activity against the NCI-H292, HEp-2 and K562 cell lines using MTT. The absence of hemolysis in the erythrocytes of mice was observed in these fractions and 6β-Benzoyloxy-3α-(3,4,5- trimethoxybenzoyloxy) tropane (catuabine B). Staining with Annexin V-FITC and JC-1 was used to verify the mechanism of action of the compounds of E. caatingae that showed cytotoxicity less than 30 μg/mL in leukemic cells. After 48 h of incubation, we observed that the acetate: methanol (95:5), acetate, and chloroform fractions, as well as the catuabine B, increased in the number of cells in early apoptosis, from 53.0 to 74.8%. An analysis of the potential of the mitochondrial membrane by incorporation of JC-1 showed that most cells during incubation of the acetate: methanol (95:5) and acetate fractions (63.85 and 59.2%) were stained, suggesting the involvement of an intrinsic pathway of apoptosis

HPLC-DAD analysis, antinociceptive and anti-inflammatory properties of the ethanolic extract of Hyptis umbrosa in mice

Hyptis umbrosa (syn. Mesosphaerum sidifolium) (Lamiaceae Family) has been used to treat several conditions such as gastrointestinal disorders, skin infections, nasal congestion, fever and cramps. The objective of this study was to evaluate the chemical composition, analgesic and anti-inflammatory profiles of ethanol extract from leaves of Hyptis umbrosa (EEB). HPLC-DAD was used to determine the fingerprint chromatogram of the extract. Male Swiss mice were orally pretreated with EEB (100, 200 or 400 mg/kg; 60 min before initiating algesic stimulation) and antinociceptive activity was assessed using the acetic acid-induced writhing model, formalin test and hyperalgesia induced by glutamate or capsaicin. Also, peritonitis was induced by the intrathoracic injection of carrageenan to quantify the total number of leukocytes. The presence of phenolic compounds in the extract was confirmed using HPLC-DAD. The treatment with EEB, at all doses, produced a significant analgesic effect against acetic acid-induced antinociceptive activity. In the formalin test, only the 400-mg/kg-dose of EEB had a significant effect in the first phase. However, all doses tested were able to reverse nociception in the second phase. The effect of all doses of EEB also showed a significant antinociceptive effect in the glutamate and capsaicin tests and inhibited the carrageenan-induced leukocyte migration to the peritoneal cavity. The present study suggests that the EEB possesses peripheral analgesic action and showed potential in reducing the spreading of the inflammatory processes. Also, it seems to be related with vanilloid and glutamate receptors

Antioxidant, Antinociceptive, and Anti-inflammatory Properties of the Ethanolic Extract of Combretum duarteanum in Rodents

This is a copy of an article published in the Journal of Medicinal Food© 2011 - copyright Mary Ann Liebert, Inc.; Journal of Medicinal Food is available online at: http://online.liebertpub.comThe antioxidant, antinociceptive, and anti-inflammatory activities of the ethanolic extract from leaves of Combretum duarteanum (EEC) were assessed in rodents through in vitro tests. The antioxidant activity was investigated by using thiobarbituric acid reactive species (TBARS), hydroxyl radical–scavenging, and scavenging activity of nitric oxide assays. The antinociceptive activity was investigated by using acetic acid–induced writhing, formalin, and hot-plate tests in mice. The anti-inflammatory activity was assessed in rats by using the carrageenan-induced hind-paw edema test and arachidonic acid–induced paw edema test. EEC possesses a strong antioxidant potential according to the TBARS, nitric oxide, and hydroxyl radical–scavenging assays; it also presented scavenger activity in all in vitro tests. After intraperitoneal injection, EEC (100, 200, and 400 mg/kg) significantly reduced the number of writhes (38.1%, 90.6%, and 97.8%, respectively) in a writhing test and the number of paw licks during phase 1 (30.5% and 69.5%, higher doses) and phase 2 (38.1%, 90.6%, and 97.8%, all doses) of a formalin test when compared with the control group. Naloxone (1.5 mg/kg, intraperito- neally) antagonized the antinociceptive action of EEC (400 mg/kg), and this finding suggests participation of the opioid system. Administration of 200 and 400 mg/kg (intraperitoneally) of EEC exhibited an anti-inflammatory activity in the carrageenin test, which was based on interference with prostaglandin synthesis. This finding was confirmed by the arachidonic acid test. Together, these results indicate that properties of EEC might be further explored in the search for newer tools to treat painful inflammatory conditions, including those related to pro-oxidant states

Efeito vasodilatador do extrato metanólico de Erythroxylum caatingae Plowman sobre anéis mesentéricos de ratos espontaneamente hipertensos (SHR)

Introdução: Erythroxylum caatingae Plowman (ETC) tem revelado a presença de diversos alcalóides com atividade biológica. Objetivo: Avaliar a potencial ação anti-hipertensiva do extrato metanólico da espécie ETC sobre anéis de artéria mesentérica superior isolada de ratos espontaneamente hipertensos (SHR). Metodologia: Para isto, foram realizados ensaios farmacológicos in vitro, e o efeito vasodilatador de ETC (0,01-300 µg/mL) foi observado. Resultados: Em anéis mesentéricos isolados, com endotélio funcional intacto e pré-contraídos com fenilefrina (FEN) (1 µM), ETC induziu relaxamento (CE50 = 14.49 (20.5 – 29.2) µg/mL; Emáx = 110,11 ± 2.4 %; n = 7), de maneira dependente da concentração do extrato e este efeito não foi atenuado após remoção do endotélio vascular (CE50 = 27.41 (21.1 – 35.6) µg/mL; Emáx = 116.7 ± 8.0 %; n = 7; p < 0.05). Estes resultados sugerem que a resposta vasodilatadora induzida por ETC independe dos fatores vasoativos liberados pelo endotélio. Por isso, os experimentos subsequentes foram realizados com preparações na ausência da camada endotelial. Em anéis pré-contraídos com serotonina, ETC apresentou aumento na potência farmacológica, quando comparado aos anéis pré-contraídos com a FEN (CE50 = 9.22 (5.8 – 14.6) µg/mL; n = 11; p < 0.001), entretanto, não houve diferença significante em relação ao seu efeito máximo (Emáx = 112.97 ± 3.5 %; n = 11; p < 0.05). Enquanto que, em anéis pré-contraídos com solução despolarizante de KCl (60 mM), a curva concentração-resposta para ETC não foi significativamente diferente à obtida em anéis pré-contraídos com FEN (CE50 = 20.76 (16.2 – 26.6) µg/mL; Emáx = 106.94 ± 3.6 %, n = 8; p < 0.05). Conclusão: Tomados juntos, estes dados sugerem que ETC promove vasodilatação em anéis mesentéricos de animal SHR, independente da presença do endotélio vascular, e estes efeitos são mais potentes em tônus contraído por ativação de receptores serotoninérgicos, quando comparados a outros vasocontracturantes. Introduction: Erythroxylum caatingae Plowman (ETC) has revealed the presence of several alkaloids with biological activity. Objective: Evaluate the potential antihypertensive action of methanol extract from ETC species in superior mesenteric artery rings isolated from spontaneously hypertensive rats (SHR). Methods: Pharmacological tests were performed in vitro and the vasorelaxant effect of ETC (0.01-300 µg/mL) was observed. Results: In isolated mesenteric rings with a functional and intact endothelium, pre-contracted with phenylephrine (PHE) (1 µM), ETC induced relaxation [EC50 = 14.49 (20.5 - 29.2) µg/mL; MR = 110.11 ± 2.4%, n = 7] in a concentration dependent manner. This effect was not attenuated after removal of the vascular endothelium [EC50 = 27.41 (21.1 - 35.6) µg/mL; MR = 116.7 ± 8.0%, n = 7,

Efeito vasodilatador do extrato metanólico de Erythroxylum caatingae Plowman sobre anéis mesentéricos de ratos espontaneamente hipertensos (SHR)

Introdução: Erythroxylum caatingae Plowman (ETC) tem revelado a presença de diversos alcalóides com atividade biológica. Objetivo: Avaliar a potencial ação anti-hipertensiva do extrato metanólico da espécie ETC sobre anéis de artéria mesentérica superior isolada de ratos espontaneamente hipertensos (SHR). Metodologia: Para isto, foram realizados ensaios farmacológicos in vitro, e o efeito vasodilatador de ETC (0,01-300 µg/mL) foi observado. Resultados: Em anéis mesentéricos isolados, com endotélio funcional intacto e pré-contraídos com fenilefrina (FEN) (1 µM), ETC induziu relaxamento (CE50 = 14.49 (20.5 – 29.2) µg/mL; Emáx = 110,11 ± 2.4 %; n = 7), de maneira dependente da concentração do extrato e este efeito não foi atenuado após remoção do endotélio vascular (CE50 = 27.41 (21.1 – 35.6) µg/mL; Emáx = 116.7 ± 8.0 %; n = 7; p < 0.05). Estes resultados sugerem que a resposta vasodilatadora induzida por ETC independe dos fatores vasoativos liberados pelo endotélio. Por isso, os experimentos subsequentes foram realizados com preparações na ausência da camada endotelial. Em anéis pré-contraídos com serotonina, ETC apresentou aumento na potência farmacológica, quando comparado aos anéis pré-contraídos com a FEN (CE50 = 9.22 (5.8 – 14.6) µg/mL; n = 11; p < 0.001), entretanto, não houve diferença significante em relação ao seu efeito máximo (Emáx = 112.97 ± 3.5 %; n = 11; p < 0.05). Enquanto que, em anéis pré-contraídos com solução despolarizante de KCl (60 mM), a curva concentração-resposta para ETC não foi significativamente diferente à obtida em anéis pré-contraídos com FEN (CE50 = 20.76 (16.2 – 26.6) µg/mL; Emáx = 106.94 ± 3.6 %, n = 8; p < 0.05). Conclusão: Tomados juntos, estes dados sugerem que ETC promove vasodilatação em anéis mesentéricos de animal SHR, independente da presença do endotélio vascular, e estes efeitos são mais potentes em tônus contraído por ativação de receptores serotoninérgicos, quando comparados a outros vasocontracturantes. Introduction: Erythroxylum caatingae Plowman (ETC) has revealed the presence of several alkaloids with biological activity. Objective: Evaluate the potential antihypertensive action of methanol extract from ETC species in superior mesenteric artery rings isolated from spontaneously hypertensive rats (SHR). Methods: Pharmacological tests were performed in vitro and the vasorelaxant effect of ETC (0.01-300 µg/mL) was observed. Results: In isolated mesenteric rings with a functional and intact endothelium, pre-contracted with phenylephrine (PHE) (1 µM), ETC induced relaxation [EC50 = 14.49 (20.5 - 29.2) µg/mL; MR = 110.11 ± 2.4%, n = 7] in a concentration dependent manner. This effect was not attenuated after removal of the vascular endothelium [EC50 = 27.41 (21.1 - 35.6) µg/mL; MR = 116.7 ± 8.0%, n = 7,