RP-HPLC法测定杜仲冲剂中3种成分的含量

目的:建立杜仲冲剂中京尼平苷酸(GPA)、绿原酸(CA)、京尼平苷(GP)3种成分含量测定方法。方法:采用反相高效液相色谱法,Diamonsil(钻石)C18色谱柱(5μm,150 mm×4.6 mm),甲醇-水-冰醋酸(14∶86∶1.2)为流动相,检测波长237 nm。结果:该方法线性关系良好。GPA,CA,GP的精密度分别为1.82%,1.38%,1.92%。加样回收率分别为97.5%,97.9%,96.8%。结论:本方法简便快捷、重现性好,可用于同时测定杜仲冲剂中3种有效成分含量。     

栀子苷及京尼平的动物肝毒性机制研究进展

栀子苷及京尼平是我国首批药食两用药材栀子的主要成分,具有广泛的药理活性和临床应用价值,在长期临床应用中尚未见到严重的不良事件报道。但是近年来的动物实验及细胞实验报道栀子苷有剂量依赖的肝毒性,且其体内衍生物京尼平较栀子苷的毒性效应更甚。现从栀子苷及京尼平的结构、体内代谢、动物实验中的肝毒性效应,栀子苷及京尼平通过选择性抑制CYP450酶系、诱导过氧化损伤、诱导肝实质细胞凋亡、影响胆红素代谢及胆汁酸合成与运输从而产生肝损伤等方面进行总结,并提出人和动物之间是否存在毒性反应差异等问题,以期临床关注栀子的安全性评价,促进其进一步的深入研究。     

栀子苷对1型糖尿病小鼠心肌损伤的保护作用和机制研究

目的:探究栀子苷对1型糖尿病小鼠心肌损伤的保护作用及可能的机制.方法:将32只C57BL/6J小鼠随机分为4组:对照组、1型糖尿病模型组(STZ组)、25mg/kg栀子苷给药组(GE25组)、50mg/kg栀子苷给药组(GE50组).测定血糖和体重水平,HE和Masson染色检测心肌纤维化,免疫组化检测LC3B、P62...     

Geniposide alleviates pressure overload in cardiac fibrosis with suppressed TGF-β1 pathway

BackgroundCardiac fibrosis is one of the main contributors to the pathogenesis of heart failure. Geniposide (GE), a major iridoid in gardenia fruit extract, has recently been reported to improve skeletal muscle fibrosis through the modulation of inflammation response. This investigation aimed to illuminate the cardio-protective effect and the potential mechanism of GE in cardiac fibrosis.Material and methodsA transverse aortic contraction (TAC) induction mice model was established and GE (0 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg) was administered by oral gavage daily for 4 weeks. Hemodynamic parameters, Masson’s trichrome stain, and hematoxylin-eosin (HE) staining were estimated and cardiomyocyte fibrosis, interstitial collagen levels, and hypertrophic markers were analyzed using qPCR and western blot. In vitro, H9C2 cells were exposed to the Ang II (1 μM) pretreated with GE (0.1 μM, 1 μM, and 10 μM). Cardiomyocyte apoptosis was detected. Moreover, the transforming growth factor β1 (TGF-β1)/Smad2 pathway was assessed in vivo and in vitro.ResultsGE significantly ameliorated TAC-induced cardiac hypertrophy, ventricular remodeling, myocardial fibrosis, and improved cardiac function in vivo, and it inhibited Ang II-induced cardiomyocyte apoptosis in vitro. We further observed that the inflammatory channel TGF-β1/Smad2 pathway was suppressed by GE both in vivo and in vitro.ConclusionThese results indicate that GE inhibited myocardial fibrosis and improved hypertrophic cardiomyocytes with attenuated the TGF-β1/Smad2 pathway and proposed to be an important therapeutic of cardiac fibrosis reduced by TAC.     

热毒宁吸入粉雾剂的制备与质量标准研究

目的：建立热毒宁吸入粉雾剂的质量标准。方法：通过实验对热毒宁吸入粉雾剂进行制备工艺优化,采用高效液相色谱法(HPLC)测定热毒宁吸入粉雾剂中绿原酸、栀子苷和青蒿素的含量。运用激光粒度仪测定热毒宁吸入粉雾剂的粉末粒径分布,结合药典和相关法规的要求,制定热毒宁吸入粉雾剂的质量标准。结果：15 g金银花和12 g青蒿在3倍体积的水中提取6 h,可以获得最佳的挥发油提取量,在6倍水体积,pH=2.5的条件下,提取240 min可以获得最优的绿原酸和浸膏得率。在乙醇浓度为70%,提取时间180 min, 6倍加液条件下,获得最佳的栀子醇提物得率。在温度80℃、风速600 L/h,进药量3 mL/min的条件下进行喷雾干燥,发现乙醇含量为60%时为最优条件,其粒径分布在1～5μm的体积百分数为67.6%,且得粉率为71.2%。喷雾微粉在25℃条件下储存1个月和3个月,药物分别降解0.25%和2.13%,水分分别增加0.02%和0.05%,且在避光和正常光照条件下无明显变化。热毒宁喷吸入雾剂中绿原酸含量不低于5.0%、青蒿素含量不低于3.2%、栀子苷含量不低于6.8%。热毒宁喷吸入雾剂中总菌落数低于...