RESUMO
Piperine (PIP) is a natural alkaloid isolated from Piper longum L. that presents antioxidant, anticonvulsant, antimicrobial, neuroprotective, larvicidal, antiparasitic, anticancer effect and other pharmacological properties. However, the low aqueous solubility is the main barrier to its development from the laboratory to the clinic as a drug. Several strategies have been used to overcome this obstacle, like the incorporation of PIP into different drug delivery systems turned out to be highly efficient. In addition, several methods for the quantitative and qualitative analysis of PIP in various raw materials, including biological fluids (plasma, urine, metabolites, brain), plants and drug delivery systems, were investigated. Most recently high-performance liquid chromatography was used together with several detectors for this purpose. Therefore, this review presents a summary of characteristics chemical and biological properties of PIP as well as several techniques and analytical methods to optimize the analytical signal, increase sensitivity, selectivity and reduce the effects of interference for this drug.
Assuntos
Alcaloides/análise , Benzodioxóis/análise , Portadores de Fármacos/química , Piperidinas/análise , Alcamidas Poli-Insaturadas/análise , Disponibilidade Biológica , Encéfalo/metabolismo , Cromatografia Líquida de Alta Pressão/métodos , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Humanos , Solubilidade , Espectrometria de Massas em Tandem/métodos , ÁguaRESUMO
The biotransformation of the lignan (-)-cubebin by filamentous fungi Aspergillus terreus and Aspergillus niger is an efficient bioprocess for obtaining (-)-hinokinin and (-)-parabenzlactone. The relevance of getting (-)-hinokinin is due to its promising effect against oral pathogens, especially S. sanguinis (both MIC and MBC 12.5 µg/mL), and other previous reported effects against Chagas disease and as anti-inflammatory. The advantage of using fungal transformation is the use of non-toxic and/or non-pollutant reagents and/or solvents in comparison with semi-synthesis. Microbial transformation of (-)-cubebin is also important to evaluate its human metabolism, since Aspergillus species are capable of mimicking P450 reactions, providing possible products of the metabolism, which is important in the assessment of its efficacy and safety. Furthermore, the present study describes a reliable RP-HPLC method to perform quantification of (-)-hinokinin in fungal extracts. It is simple, fast, selective, linear, precise, accurate and robust according to validation guidelines.