为了提高辣椒碱溶解度和生物利用度将其制备成微乳,经溶解度实验和伪三元相图确定微乳处方组成和表面活性剂与助表面活性剂的最佳质量比(Km);以粒径和载药量为考察指标,采用星点设计-响应面法优化辣椒碱微乳处方;并对最优处方制备的辣...为了提高辣椒碱溶解度和生物利用度将其制备成微乳,经溶解度实验和伪三元相图确定微乳处方组成和表面活性剂与助表面活性剂的最佳质量比(Km);以粒径和载药量为考察指标,采用星点设计-响应面法优化辣椒碱微乳处方;并对最优处方制备的辣椒碱微乳进行质量评价。辣椒碱微乳最优处方为辣椒碱5.12%,油酸乙酯5.82%,曲拉通X-100和无水乙醇(K_(m)=3∶1)28.54%,加纯化水至5.0 g;制得的微乳为O/W型澄清透明的均一液体,其形态为表面光滑的球形;CAP微乳粒径为16.5±0.17 nm,多分散指数为0.387±0.02,Zeta电位为-12.1±0.12 m V,粘度为33±1.73 m Pa·s;冻融稳定性和离心稳定性良好;红外光谱和差示扫描量热分析表明辣椒碱被包裹在微乳中。将辣椒碱制备成辣椒碱微乳,溶解度得以提高,解决了其水溶性低的问题,为辣椒碱的开发与应用提供一定的参考。展开更多
OBJECTIVE Mitochondrial dys⁃function contributes to the pathogenesis of neuro⁃degenerative diseases such as Parkinson dis⁃ease(PD).Therapeutic strategies targeting mito⁃chondrial dysfunction hold considerable promise ...OBJECTIVE Mitochondrial dys⁃function contributes to the pathogenesis of neuro⁃degenerative diseases such as Parkinson dis⁃ease(PD).Therapeutic strategies targeting mito⁃chondrial dysfunction hold considerable promise for the treatment of PD.Urolithin A(UA)is a gut metabolite produced from ellagic acid-containing foods such as pomegranates,berries,and wal⁃nuts.Recent reports have highlighted the protec⁃tive role of UA in several neurological disorders including Alzheimer disease and ischemic stroke.However,the potential role of UA in PD has not been characterized.In this study,the role of UA in 6-OHDA-induced neurotoxicity in cell cultures and mouse model of PD was investi⁃gated.METHODS In vitro,PC12 cells were exposed to 6-OHDA in the presence or absence of UA.For in vivo study,C57BL/6 mice were ste⁃reotactic injected with 6-OHDA to induce experi⁃mental PD model.UA(10 mg·kg-1)was intraperi⁃toneal injected for 7 d before surgery.RESULTS UA protected against 6-OHDA cytotoxicity and apoptosis in PC12 cells.Prior administration of UA to 6-OHDA lesioned mice ameliorated both motor deficits and nigral-straital dopaminergic neurotoxicity.Moreover,UA attenuated 6-OHDA-induced mitochondrial dysfunction in PC12 cells accompanied by enhanced mitochondrial biogen⁃esis.Mechanically,the neuroprotective effects of UA were mediated by SIRT1-PGC-1αsignaling-mediated mitochondrial biogenesis.CONCLU⁃SION These data provide new insights into the novel role of UA in promoting mitochondria bio⁃genesis and suggest that UA may have potential therapeutic applications for PD.展开更多
文摘为了提高辣椒碱溶解度和生物利用度将其制备成微乳,经溶解度实验和伪三元相图确定微乳处方组成和表面活性剂与助表面活性剂的最佳质量比(Km);以粒径和载药量为考察指标,采用星点设计-响应面法优化辣椒碱微乳处方;并对最优处方制备的辣椒碱微乳进行质量评价。辣椒碱微乳最优处方为辣椒碱5.12%,油酸乙酯5.82%,曲拉通X-100和无水乙醇(K_(m)=3∶1)28.54%,加纯化水至5.0 g;制得的微乳为O/W型澄清透明的均一液体,其形态为表面光滑的球形;CAP微乳粒径为16.5±0.17 nm,多分散指数为0.387±0.02,Zeta电位为-12.1±0.12 m V,粘度为33±1.73 m Pa·s;冻融稳定性和离心稳定性良好;红外光谱和差示扫描量热分析表明辣椒碱被包裹在微乳中。将辣椒碱制备成辣椒碱微乳,溶解度得以提高,解决了其水溶性低的问题,为辣椒碱的开发与应用提供一定的参考。
文摘OBJECTIVE Mitochondrial dys⁃function contributes to the pathogenesis of neuro⁃degenerative diseases such as Parkinson dis⁃ease(PD).Therapeutic strategies targeting mito⁃chondrial dysfunction hold considerable promise for the treatment of PD.Urolithin A(UA)is a gut metabolite produced from ellagic acid-containing foods such as pomegranates,berries,and wal⁃nuts.Recent reports have highlighted the protec⁃tive role of UA in several neurological disorders including Alzheimer disease and ischemic stroke.However,the potential role of UA in PD has not been characterized.In this study,the role of UA in 6-OHDA-induced neurotoxicity in cell cultures and mouse model of PD was investi⁃gated.METHODS In vitro,PC12 cells were exposed to 6-OHDA in the presence or absence of UA.For in vivo study,C57BL/6 mice were ste⁃reotactic injected with 6-OHDA to induce experi⁃mental PD model.UA(10 mg·kg-1)was intraperi⁃toneal injected for 7 d before surgery.RESULTS UA protected against 6-OHDA cytotoxicity and apoptosis in PC12 cells.Prior administration of UA to 6-OHDA lesioned mice ameliorated both motor deficits and nigral-straital dopaminergic neurotoxicity.Moreover,UA attenuated 6-OHDA-induced mitochondrial dysfunction in PC12 cells accompanied by enhanced mitochondrial biogen⁃esis.Mechanically,the neuroprotective effects of UA were mediated by SIRT1-PGC-1αsignaling-mediated mitochondrial biogenesis.CONCLU⁃SION These data provide new insights into the novel role of UA in promoting mitochondria bio⁃genesis and suggest that UA may have potential therapeutic applications for PD.
