基于UHPLC-QTOF-MS/MS和分子对接筛选紫菀中润肠通便的效应

目的 通过UHPLC-QTOF-MS/MS和分子对接技术阐明紫菀Aster tataricus中润肠通便作用的效应成分。方法 采用UHPLC-QTOF-MS/MS技术分析体内肠道内容物的成分,再利用SYBYL-X 2.0与Discovery Studio 4.0分子对接软件研究肠道内容物成分与M2受体、M3受体、蛋白激酶C(protein kinase C,PKC)蛋白的相互作用,明确各成分与靶标蛋白的结合强度。结果 体内肠道内容物中共鉴定出28个紫菀中的化学成分,有10个成分均可与M2受体、M3受体及PKC蛋白分子对接较好,其中astin J与3种靶标蛋白结合的平均打分值最高,这些成分均以非共价键方式与靶标蛋白结合,产生氢键、范德华力、经典作用力等相互作用。结论 紫菀中的astin J、asterin F、asterin A、异绿原酸A、异绿原酸B、异绿原酸C、绿原酸、槲皮素、山柰酚和木犀草素共10个成分可能是通过调节M受体及其下游信号通路PKC蛋白的表达发挥润肠通便的作用。     

肉苁蓉分离部位通便作用的实验研究

目的：寻找肉苁蓉的通便有效成分。方法：采用不同溶剂提取、分离及重结晶等方法将肉苁蓉分为半乳糖醇等4个组份，进行对小鼠通便时间的影响实验。结果：半乳糖醇具有显著的缩短通便时间作用，其他各组份作用不显著。结论：半乳糖醇为肉苁蓉的主要通便有效成分。     

聚丙烯酸型高吸水树脂缓泻作用研究

目的探讨聚丙烯酸型高吸水树脂的缓泻作用.方法采用小鼠胃肠推进运动实验、小鼠小肠保水实验和对小鼠便秘模型作用实验,并对实验数据进行统计分析.结果聚丙烯酸型高吸水树脂可使小肠推进距离和小肠推进率增加并显著高于对照组(P<0.01);聚丙烯酸型高吸水树脂组小肠重量明显高于空白对照组(P<0.01),表明聚丙烯酸型高吸水树脂可增加肠道水分;聚丙烯酸型高吸水树脂使便秘小鼠排便粒数显著高于便秘模型组(P<0.01).结论聚丙烯酸型高吸水树脂在一定剂量下具有缓泻作用.     

Constipation Is a Frequent Problem Associated with Vascular Complications in Patients with Type 2 Diabetes: A Cross-sectional Study

Objective Diabetes is recognized as an underlying disease of constipation. However, the prevalence of constipation varies according to the diagnostic criteria applied. We investigated the prevalence of constipation based on the new guideline for constipation in Japanese patients with type 2 diabetes and examined the relationship with the clinical background, including diabetic vascular complications. Methods Questionnaire surveys including items concerning the diagnosis and treatment status of constipation were administered to 410 patients with type 2 diabetes. Results Although 29% of the patients considered that they had experienced constipation (self-judged), only 14% had consulted a physician about constipation. The prevalence of chronic constipation based on the guideline was 26%. After including laxative users, constipation was finally found in 36%. Despite the use of laxatives (n=81), 51% of the patients were still diagnosed with chronic constipation. Patients with constipation (chronic constipation or laxative use) were significantly older and had a longer duration of diabetes than those without constipation. The body mass index (BMI) of patients with constipation (24.9±3.8 kg/m²) was significantly lower than that of those without constipation (26.3±4.6 kg/m²). Diabetic neuropathy (49% vs. 32%) and coronary heart disease (CHD) (27% vs. 13%) were significantly more frequent in the patients with constipation than in those without constipation. A multivariate logistic regression analysis revealed that gender, BMI, diabetic neuropathy, insulin use, and CHD were significantly associated with constipation. Conclusion An accurate diagnosis of constipation is desirable in patients with type 2 diabetes because constipation is independently associated with CHD.     

沙生异翅独尾草不同器官中蒽醌含量的消长规律

目的对沙生类短命植物异翅独尾草在苗期、营养生长期、初花期、盛花期、果期的各器官中大黄素、大黄酚、大黄酸、芦荟大黄素含量变化进行研究。方法高效液相色谱法。结果叶中4种蒽醌类物质在苗期、营养生长期、初花期含量较高,盛花期最低,且叶上部位明显高于叶中和叶下部位。根中苗期4种蒽醌类物质含量都较低,营养生长期芦荟大黄素和大黄素含量较高,初花期和盛花期大黄素含量较高,果期芦荟大黄素和大黄酚含量较高。花中芦荟大黄素、大黄素、大黄酚含量要比花葶高,花葶中大黄酸含量比花高。花葶中4种蒽醌类物质在盛花期含量高于初花期和果期时的含量。同时期各器官蒽醌总量相比:叶>根>花>花葶。结论若选取异翅独尾草作为蒽醌类药材利用,建议最佳采集部位是初花期的叶先端部位。     

大黄醇提液对2.2.15细胞分泌HBsAg、HBeAg的抑制作用

目的:研究大黄醇提液的抗乙型肝炎病毒(HBV)作用.方法:分别以大黄醇提液及大黄蒽醌类衍生物作用于体外培养的2.2.15细胞,观察其对2.2.15细胞HBsAg与HBeAg分泌的影响,评价其抗HBV作用.结果:药物作用于2.2.15细胞11d,大黄醇提液对2.2.15细胞的半数毒性浓度为36.69g/L,大黄蒽醌类衍生物(大黄素、大黄素甲醚、大黄酸、芦荟大黄)对2.2.15细胞的半数毒性浓度分别为1.57g/L、57.30g/L、3.06g/L、＞63g/L.大黄醇提液对HBsAg、HBeAg的半数抑制浓度分别为3.29g/L、2.34g/L,治疗指数分别为12.06、16.96;大黄蒽醌类衍生物(大黄素、大黄素甲醚、大黄酸、芦荟大黄)对HBsAg(HBeAg)的半数抑制浓度分别为1.26(1.74)、3.94(61.16)、0.57(3.54)、1.12(＞63),治疗指数分别为1.24(0.90)、14.54(0.94)、5.37(0.86)、＞52.07(1).结论:大黄醇提液在体外细胞培养中对两抗原的分泌有较好的抑制作用,其作用优于大黄蒽醌类衍生物.     

灌胃大承气汤后大鼠血浆中蒽醌成分的分析

目的 阐明大承气汤经灌胃给药后,5种游离蒽醌成分在大鼠体内的药物动力学特性.方法大鼠灌胃大承气汤9 9/kg后,采集血浆,采用HPLC法测定血浆中芦荟大黄素、大黄酸、大黄素、大黄酚及大黄素甲醚的含量,并用3p87软件进行数据分析.结果 大鼠灌胃大承气汤后,血浆中芦荟大黄素、大黄酸、大黄素、大黄酚及大黄素甲醚的T1/2(Ka)依次是0.362,1.034,1.918,1.89,0.656 h;T1/xke)依次是0.311,1.173,2.33,2.188,0.81 h;Cmax依次是48.47,21.69,10.49,5.76,38.76mg/L;Tmax依次是4,4,6,4,2h;AUC0-t依次是85.733,66.726,65.911,41.84,96.401 mg·L-1·h-1.结论通过建立经灌胃大承气汤后大鼠血浆中5种游离蒽醌成分含量的测定方法,阐明其药动学特性,为经典寒下方大承气汤的体内成分研究提供实验依据.     

Enterohepatic Circulation,Urinary Excretion and Laxative Action of Some Bisacodyl Derivatives after Intragastric Administration in the Rat

Abstract: Bisacodyl (BIS), the parent diphenol (DES) and its sulphuric acid di-ester (picosulphate = PICO) were given by stomach tube to fasted rats at a dose of 3.1 μmol/100 g rat. Bile was sampled in the periods 0–6, 6–12 and 12–18 hrs after drug administration, and assayed for total diphenol (= free + conjugated) by HPLC. Mean fractions (% of dose±S.E.M.) excreted in 5 rats per compound and period were: BIS 74.0±4.7, 51.9±7.9 and 30.8±2.5; DES 41.2±4.3, 46.8±4.7 and 25.1±2.5; PICO 9.0±0.9, 26.0±5.4 and 19.6±3.1. Only minor amounts were excreted as free diphenol. Urine samples taken by bladder puncture and assayed as above furthermore showed that the renal excretion of total diphenol was insignificant compared to the amounts excreted in bile. Practically no diphenol was present in urine 0–6 hrs after the administration of PICO. In experiments with BIS and DES at 0.85 μmol/100 g, total diphenol excreted in bile during 0–6 hrs was: BIS 67.1±2.6 (n = 5); DES: 55.4±3.0 (5). - The latency time for laxative effect was studied in groups of 10 unfasted rats per compound. Cumulative time response curves showed that PICO caused diarrhoea more promptly at 0.85 μmol/100 g than either BIS or DES. In most rats, this delayed action of BIS and DES persisted also at 1.7 μmol/100 g. At 3.1 μmol/100 g, however, the majority of the rats reacted as promptly to these two compounds as to PICO. These results are discussed in relation to the biliary excretion experiments, and interpreted in terms of the relative importance at the different dose levels of: 1. The enterohepatic recirculated fraction, and 2. The non-absorbed fraction, which passes directly to the large intestine. For PICO, the latter fraction is the single determinant of the effect, which is triggered when the di-ester is being hydrolyzed to active diphenol in this part of the GI-tract.     

南极海茸多糖果冻的润肠通便功能研究

目的 制备南极海茸多糖果冻,研究其对便秘小鼠的润肠通便作用.方法 以南极海茸多糖为原料,制备1款酸甜可口的果冻.采用1.苯基-3-甲基-5-吡唑啉酮(PMP)柱前衍生.高效液相色谱法(HPLC)测定果冻中南极海茸多糖的含量.探索了南极海茸多糖果冻对便秘小鼠润肠通便作用:将昆明小鼠随机分为空白组、模型组、阳性对照组、果冻...     

均匀设计优化超临界CO2流体萃取大黄蒽醌的研究

目的:通过均匀设计试验确定超临界二氧化碳流体萃取(SFE-CO2)掌叶大黄中蒽醌类成分的最佳提取工艺条件。方法:以药材粒度、萃取压力、萃取温度、萃取时间和夹带剂用量为考察因素,进行SFE-CO2萃取;用高效液相色谱法测定不同条件下芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚的含量。结果:优选出总蒽醌的最佳萃取工艺条件是萃取压力为38 MPa,萃取温度为70℃,萃取时间为60 m in;夹带剂用量为300 m l。结论:最佳提取工艺可有效萃取掌叶大黄中蒽醌类成分;本含量测定方法可靠、简单易行。