Syzygium cumini (L.) Skeels (Myrtaceae) has been traditionally used to treat a number of illnesses. Ethnopharmacological studies have particularly addressed antidiabetic and metabolic-related effects of extracts prepared from its different parts, especially seed, and pulp-fruit, however. there is a lack of studies on phytochemical profile and biological properties of its leaf. As there is considerable interest in bioactive compounds to treat metabolic syndrome and its clustered risk factors, we sought to characterize the metabolic effects of hydroethanolic extract of S. cumini leaf (HESc) on lean and monosodium L-glutamate (MSG)-induced obese rats. HPLC-MS/MS characterization of the HESc polyphenolic profile, at 254 nm, identified 15 compounds pertaining to hydrolysable tannin and flavanol subclasses. At 60 days of age, both groups were randomly assigned to receive HESc (500 mg/kg) or vehicle for 30 days. At the end of treatment, obese+HESc exhibited significantly lower body weight gain, body mass index, and white adipose tissue mass, compared to obese rats receiving vehicle. Obese rats treated with HESc showed a twofold increase in lipolytic activity in the periepididymal fat pad, as well as, brought triglyceride levels in serum, liver and skeletal muscle back to levels close those found in lean animals. Furthermore, HESc also improved hyperinsulinemia and insulin resistance in obese+HESc rats, which resulted in partial reversal of glucose intolerance, as compared to obese rats. HESc had no effect in lean rats. Assessment of ex vivo glucose-stimulated insulin secretion showed HESc potentiated pancreatic function in islets isolated from both lean and obese rats treated with HESc. In addition, HESc (10-1000 µg/mL) increased glucose stimulated insulin Syzygium cumini Dual Effect in MSG-Obese Rats secretion from both isolated rat islets and INS-1E β-cells. These data demonstrate that S. cumini leaf improved peripheral insulin sensitivity via stimulating/modulating β-cell insulin release, which was associated with improvements in metabolic outcomes in MSG-induced obese rats.

O uso de plantas medicinais no tratamento de enfermidades tem ocorrido há muitos anos, sendo a única terapia de certas comunidades. O Diabetes Mellitus é uma desordem metabólica caracterizada pela hiperglicemia, associada a outros fatores de risco. Este trabalho teve como finalidade realizar um levantamento de plantas medicinais utilizadas como hipoglicemiantes por usuários do Programa de Fitoterapia da Universidade Federal do Maranhão – UFMA, São Luís, Maranhão, Brasil. Foram entrevistadas 100 pessoas, através de questionários semiestruturados com obtenção de dados socioeconômicos e variáveis farmacobotânicas com listagem livre de plantas, aplicados entre os meses de março e junho de 2016. A maioria dos entrevistados era do sexo feminino (62%), com idade entre 30 e 59 anos (62%) e ensino médio completo (48%). Foram mencionadas 28 espécies vegetais com a finalidade hipoglicêmica, sendo a berinjela (Solanun melongena L.) a mais citada (31%). As folhas foram as partes da planta mais utilizadas (45%) e infusão foi a forma de preparo mais indicada pelos entrevistados (43%). O estudo das plantas realizado poderá auxiliar estudos posteriores no desenvolvimento de novos medicamentos para o tratamento de diabetes.

Amorphous solid dispersions (ASDs) are a viable alternative to enhance the kinetic solubility of poorly water-soluble drugs. However, there is lack of discussion about the impact of drug loading on dissolution rate and drug diffusion across the membrane generated by supersaturation. So, it was obtained amorphous solid dispersions with nevirapine and polyvinylpyrrolidone K-30 by solvent evaporation method using different drug loadings (10%, 15% and 20% w/w). Thermal analysis, Fourier transform infrared spectroscopy and x-ray diffraction characterized the ASDs, indicating that there was a good miscibility between components which stabilized the drug in its amorphous state. The intermolecular interactions impacted on the ASDs in vitro performance, where they were evaluated to dissolution tests under different conditions and permeability studies. All amorphous systems had an increment in aqueous solubility compared to nevirapine alone, although 10% amorphous solid dispersion (SD 10) kept drug supersaturation at very high concentrations longer, preventing the drug recrystallization, having the greater drug flux on membranes and more intermolecular interactions among the components. Therefore, large quantities of the polymer are required for the stability of the amorphous drug, due to the increase in the number of intermolecular interactions.