Hypoglycemic and hypotensive activity of a root extract of Smilax aristolochiifolia, standardized on N-trans-feruloyl-tyramine.

The metabolic syndrome (MS) is a condition consisting of various metabolic abnormalities that are risk factors for developing kidney failure, cardiovascular, vascular and cerebrovascular diseases, among others. The prevalence of this syndrome shows a marked increase. The aim of this study was to investigate the pharmacological effect of Smilax aristolochiifolia root on some components of MS and obtain some of the active principle using chromatographic techniques. The compound isolated was N-trans-feruloyl tyramine NTF (1), and its structure was determined by spectroscopic and spectrometric analyses. The whole extract and the standardized fractions were able to control the weight gain around 30%; the fraction rich in NTF was able to decrease the hypertriglyceridemia by 60%. The insulin resistance decreased by approximately 40%; the same happened with blood pressure, since the values of systolic and diastolic pressure fell on average 31% and 37% respectively, to levels comparable to normal value. The treatment also had an immunomodulatory effect on the low-grade inflammation associated with obesity, since it significantly decreased the relative production of pro-inflammatory cytokines regarding anti-inflammatory cytokines, both kidney and adipose tissue. Therefore it can be concluded that the extract and fractions of Smilax aristolochiifolia root with NTF are useful to counteract some symptoms of MS in animal models.

Toxicology, genotoxicity, and cytotoxicity of three extracts of Solanum chrysotrichum.

ETHNOPHARMACOLOGICAL RELEVANCE: Infusions of Solanum chrysotrichum (Schldl.) or "sosa" are employed in Traditional Mexican Medicine for the local and systemic treatment of skin and mucosal infections. Different studies have verified its antifungal effectiveness and therapeutic safety in superficial mycosis caused by dermatophytes or yeasts, and have identified a group of spirostanic saponins, denominated SC-2-SC-6, as responsible for the antifungal activity. Of these, SC-2 is the most active molecule. Electron microscopy studies showed that SC-2 disintegrates cell wall and internal membranes of the fungi studied. In order to continue the systematic study of Solanum chrysotrichum, the goal of the present study was to evaluate the toxicity, genotoxicity, and cytotoxicity of the three different extracts of Solanum chrysotrichum. MATERIALS AND METHODS: From the dried leaves of Solanum chrysotrichum, we obtained the aqueous, hydroalcoholic, and ethanolic extracts. Saponins (SC-2-SC-6) were quantified by High-performance liquid chromatography (HPLC). For the toxicology study, we formed four groups: three experimental groups, treated with each of the extracts at 1-g/kg doses per os (po) during 4 weeks, and a negative control group treated with the vehicle. For the genotoxicity study, we added another group, which was treated with cyclophosphamide for 1 week. The cytotoxicity study was carried out with international methods and employing the nasopharyngeal cancer (KB) and breast cancer (MDA) cell lines. RESULTS: The three evaluated extracts did not modify either of the behavioral parameters, and on the hepatic-function biochemical tests (alanine aminotransferase [ALT] and aspartate aminotransferase [AST]), did not showed significant increase on comparing to placebo. The genotoxicity parameters did not exhibit differences between the experimental groups and the placebo (control) group. Histologic analysis showed that the three extracts caused amyloidosis and moderate necrosis in liver, and focal tumefaction in kidney, as well as significant, but clinically irrelevant, elevations of creatinine with the aqueous and hydroalcoholic, but not with the ethanolic, extracts. In addition, the aqueous and ethanolic extracts exhibited interesting cytotoxic activity against the KB cell line. CONCLUSIONS: At the doses administered, the ethanolic extract of Solanum chrysotrichum showed a slightly toxic effect on liver and kidney, without biochemical or genotoxic repercussions and with cytotoxic activity against the KB cell line.

Pharmacological and chemical study to identify wound-healing active compounds in Ageratina pichinchensis.

The aerial parts of Ageratina pichinchensis are used in Mexican traditional medicine for the treatment of skin wounds. Recently, it was demonstrated that the aqueous extract of this plant reduced the time required to cicatrize a wound induced in the rat. The same extract showed a capability to induce overgrowth in normal fetal lung cells (MRC-5). The objective of the present study was isolating and identifying the active compounds in A. pichinchensis that are capable of inducing cellular overgrowth, as well as performing a preliminary evaluation of their anti-inflammatory and toxic effects. By means of bioguided chemical separation of an aqueous extract of A. pichinchensis, the most active compound capable of inducing cellular overgrowth was identified as 7-O-(ß-D-glucopyranosyl)-galactin. In vivo inflammation induced with carrageenan in mice was significantly reduced by the aqueous extract of A. pichinchensis, reaching a decrease of up to 60.6 %. Acute (2 g/kg) and subchronic (1 g/kg for 28 days) oral administration of the aqueous extract of this plant did not affect hepatic function (through alanine aminotransferase and aspartate aminotransferase activity evaluation), while no alterations of the histologic samples of liver and kidney were evidenced.

Efecto de Bursera grandiflora sobre el peso corporal y lipemia en ratones obesos / Effect of Bursera grandiflora on body weight and lipemia in obese mice

Obesity and overweight are clearly related to the caloric intake that leads to a chronic systemic inflammation of low degree. Pharmacological therapy is highly recommended for this disease. Within the Burseraceae family there are species used empirically for the treatment of obesity; one of them, Bursera grandiflora, is also reported for exhibiting anti-inflammatory properties. Evaluate the effect produced by B. grandiflora on a mice model of obesity, its toxicity potential, and chemical identification of the major chemical compound. Mice of the C57B1/6 strain were used. All animals were fed for 8 weeks with a hypercaloric diet. Afterwards, during 7 weeks, animals were daily administered with the hidro-alcoholic extract from B. grandiflora or water (control). At the end of the administration period, plasma cholesterol and triglycerides levels were measured. Moreover, toxicity tests were carried out in mice after acute and chronic administering the B. grandiflora extract. Finally, the main compound in the active extract was identified. Animals treated with the B. grandiflora extract showed a greater food consumption and, paradoxically, without increasing the body weight. Moreover, a decrease of the plasma-triglycerides was observed. Toxicological evaluation showed that the extract administration did not produce any death of the experimental animals or modifications on the organs or behavior. The major compound identified in the extract was scopoletin.

El sobrepeso y la obesidad están claramente vinculados con la ingesta calórica que lleva a la instalación crónica de inflamación sistémica de bajo grado. La terapia farmacológica es altamente recomendable para este padecimiento. Dentro de la familia Burseraceae existen especies utilizadas para el tratamiento de la obesidad, de las cuales, Bursera grandiflora es referida también por su efecto anti-inflamatorio. Evaluar el efecto de B. grandiflora en un modelo de obesidad, su potencial toxicológico, e identificación del compuesto mayoritario. Se utilizaron ratones C57Bl/6 alimentados durante 8 semanas con dieta hipercalórica. Posteriormente, durante 7 semanas se administró diariamente un extracto hidroalcohólico de B. grandiflora o agua (control). Al final se cuantificaron colesterol y triglicéridos. Además, se realizaron pruebas de toxicidad en ratones administrando el extracto de B. grandiflora en forma aguda y subcrónica. Finalmente, se identificó el compuesto mayoritario. Los animales tratados con B. grandiflora registraron el mayor consumo de alimento y, paradójicamente, sin mostrar un crecimiento ponderal y con una disminución de los triglicéridos. Las evaluaciones de toxicología revelaron que la administración del extracto no produjo muertes en los animales de experimentación, ni cambios orgánicos o de comportamiento. El compuesto mayoritario identificado en el extracto activo fue escopoletina.

Toxicological and cytotoxic evaluation of standardized extracts of Galphimia glauca.

Galphimia glauca Cav (Malpighiaceae) has been widely used in Mexican traditional medicine as a remedy for the treatment of mental disorders, principally as a sedative and tranquilizer. The sedative activity of extracts obtained from this plant has been demonstrated with different neuropharmacological models. Different triterpenes, known as galphimines, have been identified from the active extract. Galphimine-B (G-B) possesses anxiolytic activity and is able to selectively inhibit discharges of dopaminergic neurons in the ventral tegmental area in rats. Nevertheless, there have been no toxicological investigations carried out with products obtained from this plant. In this work three different extracts (aqueous, ethanolic, and methanolic) of Galphimia glauca, standardized in the content of three galphimines, were evaluated for their behavioral and pharmaco-toxicological effects. After administering the extracts to mice for 28 days (2.5g/kg, p.o.), no deaths were found and the histopathological analysis of different organs did not show alterations; only the behavioral parameters analyzed showed a diminution of spontaneous activity. The administration of these extracts for 56 days (same doses and route) in mice did not cause any changes in the biochemical parameters that evaluate liver function. On the other hand, no cytotoxic effects were found on KB, UISO, and OVCAR-5 transformed cell lines, but all extracts specifically inhibited colon cancer cell line growth with an ED(50) lower than 2microg/ml. The extracts were also evaluated in genotoxicity tests in vitro (250, 100 and 50microg/ml), which demonstrate that none of the three extracts from Galphimia glauca showed a genotoxic effect.

Hypoglycemic effect and chlorogenic acid content in two Cecropia species.

The hypoglycemic effect of methanol leaf extracts from Cecropia obtusifolia and C. peltata was evaluated in healthy mice. A significant decrease (p < 0.05) in plasma glucose levels was recorded 2 and 4 h after a single oral administration of methanol extracts (1 g/kg). This effect was correlated with the chlorogenic acid contents in both species; C. peltata, containing 19.84 +/- 1.64 mg of chlorogenic acid/g of dried leaves produced the highest decrease (D(alpha 2,60) = 20.18, p < 0.05) of plasma glucose levels (52.8%). The extracts of C. obtusifolia from Tabasco and Veracruz, showed similar hypoglycemic effects (33.3% and 35.7%, respectively) and chlorogenic acid contents (Tukey(0.05) = 1.8859) (13.3 +/- 3.2 mg/g and 13.1 +/- 1.6 mg/g, respectively). The hypoglycemic effect produced by different doses (0.1, 0.25, 0.50, 0.75 and 1 g/kg body wt, p.o.) of C. peltata showed a lineal relationship with chlorogenic acid content, reaching an ED(50) = 0.540 g/kg body wt for extract, and an ED(50) = 10.8 mg/kg body wt for chlorogenic acid. These results suggest that C. peltata is a better hypoglycemic agent than C. obtusifolia, and it could be considered for developing a phytomedicinal product to carry out clinical trials.