RESUMO
Alzheimer's disease is the most common neurodegenerative disease, characterized by memory loss and cognitive dysfunction. Raspberry fruits contain polyphenols which have antioxidant and anti-inflammatory properties. In this study, we used molecular imprinting technology to efficiently isolate phenolic components from the raspberry ethyl acetate extracts. Six phenolic components (ellagic acid, tiliroside, kaempferol-3-o-rutoside, gallic acid, ferulic acid and vanillic acid) were identified by UPLC-Q-TOF-MS analysis. Molecular docking was used to predict the anti-inflammatory effects and anti-Alzheimer's potential of these isolated compounds, which showed a good binding ability to diseases and related proteins. However, the binding energy and docking fraction of ellagic acid, tiliroside, and kaempferol-3-o-rutoside were better than those of gallic acid, ferulic acid and vanillic acid. Additionally, by studying the effects of these six phenolic components on the LPS-induced secretion of inflammatory mediators in murine microglial (BV2) cells, it was further demonstrated that they were all capable of inhibiting the secretion of NO, IL-6, TNF-α, and IL-1ß to a certain extent. However, ellagic acid, tiliroside, and kaempferol-3-o-rutoside have better inhibitory effects compared to others. The results obtained suggest that the phenolic components extracted from ethyl acetate extracts of raspberry by molecularly imprinted polymers have the potential to inhibit the progression of Alzheimer's disease.
Assuntos
Impressão Molecular , Doenças Neurodegenerativas , Rubus , Camundongos , Animais , Rubus/química , Antioxidantes/química , Quempferóis/farmacologia , Ácido Elágico/farmacologia , Ácido Elágico/análise , Simulação de Acoplamento Molecular , Fator de Necrose Tumoral alfa , Ácido Vanílico/farmacologia , Polímeros Molecularmente Impressos , Interleucina-6 , Lipopolissacarídeos , Extratos Vegetais/química , Anti-Inflamatórios/farmacologia , Ácido Gálico/farmacologia , Rutina , Mediadores da InflamaçãoRESUMO
10-Hydroxycamptothecin is a drug to cure various cancers. However, the 10-hydroxycamptothecin cannot be widely applied in clinics due to fast elimination and resistance of various cancers to the drug. Nevertheless, co-treatment with tetrandine is known to reverse the resistance of multi-drug resistant cancers, and may present an effective strategy to improve the efficacy of 10-hydroxycamptothecin. In order to improve the bioavailability and prolong the treatment time of the 10-hydroxycamptothecin in vivo, we prepared 10-hydroxycamptothecin-tetrandrine liposome complexes with 10-hydroxycamptothecin as the basic anticancer drug, tetrandrine and liposomes as carriers. In this article, an ultra-high performance liquid chromatography tandem mass spectrometry method for the analysis of 10-hydroxycamptothecin and tetrandrine in plasma has been developed, validated, and utilized to compare the pharmacokinetics of both drugs in the original dosage form and administered as liposome complexes. According to the pharmacokinetic parameters of mean residence time, half-life period and clearance rate, the 10-hydroxycamptothecin-tetrandrine liposome complexes prolongs the retention and circulation time of 10-hydroxycamptothecin in vivo, achieving a good sustained release effect. To the best of our current knowledge, the pharmacokinetic properties of 10-hydroxycamptothecin-tetrandrine liposome complexes in rats have not been reported yet. Our study can provide a helpful reference for further related study.
Assuntos
Antineoplásicos/farmacocinética , Benzilisoquinolinas/farmacocinética , Camptotecina/farmacocinética , Animais , Antineoplásicos/sangue , Antineoplásicos/química , Benzilisoquinolinas/sangue , Benzilisoquinolinas/química , Camptotecina/análogos & derivados , Camptotecina/sangue , Cromatografia Líquida de Alta Pressão , Lipossomos/sangue , Lipossomos/química , Lipossomos/farmacocinética , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em TandemRESUMO
Sophora tonkinensis is widely used as traditional Chinese medicine for treating the swelling of the gums and tongue and mouth sores due to flame stomach fire. It is mainly origin from Guangxi, Sichuan provinces of China. Alkaloids are considered as the major bioactive components. A method was established for identifying alkaloids in S. tonkinensis root by UPLC-Q-TOF-MS/MS and was applied in characterizing alkaloids in S. tonkinensis root of two different habitats. Consequently, twenty-four alkaloids including six new compounds were identified in S. tonkinensis root. Additionally, the difference of alkaloids in S. tonkinensis from Guozhou, Sichuan province was investigated. In the present study, we firstly characterize total alkaloids in S. tonkinensis root by UPLC-Q-TOF-MS/MS and firstly established the characteristic fragmentation pathway of alkaloids with hydroxy in S. tonkinensis root.