Compostos químicos e aspectos botânicos, etnobotânicos e farmacológicos da Byrsonima verbascifolia Rich ex. A. Juss / Chemical compounds and botanical, ethnobotanical and pharmacological aspects of Byrsonima verbascifolia Rich ex. A. Juss

RESUMO Byrsonima verbascifolia Rich ex. A. Juss é uma espécie do cerrado brasileiro com uso etnobotânico vasto. O objetivo desse trabalho foi realizar um levantamento bibliográfico de artigos originais e revisões, indexados até agosto de 2014 nas bases de dados Periódicos CAPES, Scielo, Scopus, Web of Science e Medline, nos idiomas português e inglês, utilizando a palavra-chave Byrsonima verbascifolia. Foram contemplados a composição química e os aspectos botânicos, etnobotânicos e farmacológicos. Os estudos presentes na literatura avaliaram as atividades antioxidante, antifúngica, antiviral, antimicrobiana, moluscicida, antimutagênica, mutagênica, teratogênica, imunomodulatória, tóxica e citotóxica de extratos dessa espécie. Apenas um estudo avaliou a atividade da Byrsonima verbascifoliaRich ex. A. Juss in vivo, sendo comprovado que o extrato hidrometanólico das folhas não induz teratogênese, mutagênese ou efeito estimulante ou depressor da resposta imune. Metodologias in vitro predominaram o que demonstra a necessidade de investigação científica empregando testes in vivo para a melhor avaliação das outras atividades biológicas mencionadas.

ABSTRACT Byrsonima verbascifolia is a species of Brazilian cerrado with extensive ethnobotanical application. The aim of this study was to perform a bibliographic description of original papers and reviews indexed until August 2014 in the databases of the CAPES Digital Library, Scielo, Scopus, Web of Science and Medline, written in Portuguese and English, using the keyword Byrsonima verbascifolia. The chemical and botanical compositions and the ethnobotanical and pharmacological aspects were contemplated. The researches in the reports evaluated the antioxidant, antifungal, antiviral, antimicrobial, molluscicide, antimutagenic, mutagenic, teratogenic, immunomodulatory, toxic and cytotoxic activities of the extracts of this specie. Only one study evaluated the in vivo activity of the Byrsonima verbascifolia Rich ex. A. Juss and proved that the hydromethanolic extract from the leaves does not induce teratogenesis, mutagenesis, stimulant or depressant effect of the immune response. The In vitro methodologies represented the higher number of researches demonstrating the need of scientific investigation using in vivo tests for better assessment of other biological activities mentioned.

Synthesis, biological evaluation and kinetic studies of glyceride prodrugs of diclofenac.

The prodrugs (glyceride derivatives) 3a and 3b of diclofenac were prepared by reacting 1, 2, 3-trihydroxy propane-1,3-dipalmitate/stearate with the acid chloride of diclofenac as potential prodrugs to reduce the gastrointestinal toxicity associated with them. These prodrugs were evaluated for their ulcerogenicity, anti-inflammatory and analgesic activity. It was found that the prodrugs were significantly less irritating to the gastric mucosa as indicated by severity index of 0.86, 0.78 compared to 1.6 of diclofenac. The prodrugs 3a and 3b showed better anti-inflammatory and analgesic activity than the parent drugs. The hydrolysis of prodrugs 3a and 3b were studied at pH 3, 4, 5 and 7.4. The HPLC analysis showed that the prodrugs were resistant to hydrolysis at pH 3, 4 and 5 indicating that they did not hydrolyze in acidic environment, whereas at pH 7.4 the prodrugs readily released the parent drug in significant quantities. The plasma levels of diclofenac were also analyzed by HPLC in rats after single oral dose of the prodrugs. The results indicated that the parent drugs were readily released. The concentration of diclofenac during the study was found higher in animals treated with prodrugs 3a and 3b compared with animals treated with diclofenac. The concentration of diclofenac was found to be 38.59, 33.6 and 30.36 microg/ml in animals treated with prodrugs 3a, 3b and diclofenac respectively. In conclusion, all these studies indicated that the glyceride prodrugs of diclofenac might be considered as potential biolabile prodrugs of diclofenac.