RESUMO
The global natural product-based industry is growing fast with the introduction of new phytochemicals and herbal extract products from different geographical regions. Swertia paniculata is a well-known plant with medicinal properties; however, the quality control for its major phytochemical constituents from the Himalayan geographical region is nevertheless reported. Therefore, the first objective of this investigation was to characterize and optimize the extraction process while the second objective was to validate a quantitative analytical method for chiratol from S. paniculata herbal extract. The chiratol was characterized with spectral analysis. The optimum extraction condition for the highest yield of metabolite was realized in chloroform as a solvent system under ultrasonication. The ultra-high performance liquid chromatography coupled with photodiode array detection method for analytical quantification was validated for specificity, linearity, limits of detection, limits of quantification, precision, repeatability, recovery, and robustness using Eclipse Plus C18 column (100 mm × 4.6 mm × 3.5 µm id). The gradient elution of water/acetonitrile as mobile phase was used at a flow rate of 0.5 ml/min. The recovery percentage was very satisfactory with values within specification. The robustness parameters showed no substantial influence of evaluated parameters by the Youden test. The developed method was ascertained to be appropriate for the proposed purpose.
Assuntos
Cromatografia Líquida de Alta Pressão , Compostos Fitoquímicos , Swertia , Xantonas , Cromatografia Líquida de Alta Pressão/métodos , Limite de Detecção , Modelos Lineares , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Reprodutibilidade dos Testes , Swertia/química , Xantonas/análise , Xantonas/química , Xantonas/isolamento & purificaçãoRESUMO
The 1,3-dipolar cycloaddition of deoxy-azido sugars 1 with O-benzylquercetin alkynes (5-7) to afford regioselective triazole-linked O-benzylquercetin glycoconjugates (8-10) was investigated in the presence of CuI/DIPEA in dichloromethane. All the developed glycoconjugates (8-10) were evaluated for anti-leishmanial activity against the promastigotes and amastigotes of Leishmania donovani. Graphical Abstract Click Inspired Synthesis of Antileishmanial Triazolyl O-Benzylquercetin Glycoconjugates.
Assuntos
Química Click , Quercetina/química , Tripanossomicidas/síntese química , Tripanossomicidas/farmacologia , Animais , Linhagem Celular/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , Leishmania donovani/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Camundongos , Triazóis/síntese química , Tripanossomicidas/químicaRESUMO
The therapeutic areas of infectious diseases and oncology have benefited from abundant scaffold diversity in natural products, able to interact with many specific targets within the cell and indeed for many years have been source or inspiration for the majority of FDA approved drugs. The present review describes natural products (NPs), semi-synthetic NPs and NP-derived compounds that have undergone clinical evaluation or registration from 2005 to 2010 by disease area i.e. infectious (bacterial, fungal, parasitic and viral), immunological, cardiovascular, neurological, inflammatory and related diseases and oncology.