基于支持向量机的5种大黄苷元治疗脑缺血的配伍研究

目的筛选大黄中5种能够治疗脑缺血的大黄苷元(芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚)的最佳配伍。方法采用均匀设计法将大鼠分为14组,每组15只。采用线栓法制备大鼠大脑中动脉闭塞(MCAO)模型,以神经功能症状评分、脑梗死面积为指标,探讨不同配伍的大黄苷元对脑缺血大鼠的影响,同时基于支持向量机(SVM)建立大黄苷元药效预测模型。结果经SVM回归分析,得到大黄苷元最优配伍为芦荟大黄素6.653 4 mg/kg、大黄酸26.000 8 mg/kg、大黄素11.004 2 mg/kg、大黄酚3.841 4 mg/kg和大黄素甲醚3.862 0 mg/kg。结论不同配比的大黄苷元能有效改善大鼠脑缺血的各个指标,采用均匀设计结合SVM的模拟预测方法优选出了5种大黄苷元组分的最佳配比。     

高效液相色谱法同时测定黄氏响声丸中5种蒽醌类成分含量

目的:建立黄氏响声丸中5种蒽醌类活性成分的高效液相色谱含量测定方法,有利于制剂的质量控制.方法:采用高效液相色谱法,色谱柱:Shimadzu VP-ODS柱(4.6mm×250mm,5μm),流动相为乙腈-0.1%磷酸梯度洗脱,流速为1.0ml/min,检测波长为254nm,柱温30℃.结果:5种成分为芦荟大黄素0.0...     

多元回归分析大黄不同炮制品中蒽醌与抑菌活性相关性

目的:采用多元回归分析不同大黄炮制品蒽醌含量和大黄抑菌能力之间的相互关系。方法:采用HPLC法建立大黄中蒽醌的指纹图谱,流动相为乙腈-0.1%磷酸溶液梯度洗脱,检测波长为254 nm。通过大黄不同炮制样品对大肠埃希菌、金黄色葡萄球菌、铜绿假单胞菌的抑制效果来评价其抑菌活性,采用主成分、多元线性回归分析大黄不同蒽醌与抑菌效力的关系。结果:建立大黄不同炮制品的HPLC指纹图谱;大黄蒽醌成分中芦荟大黄素和大黄酸在大黄抑菌中起主要作用,抑菌关联度均达到了90%以上。结论:大黄蒽醌成分与其抑菌效能存在显著相关性,其中芦荟大黄素和大黄酸起到主要作用。     

芦荟大黄素对T淋巴细胞增殖和细胞[Ca2+]i变化的影响

目的研究芦荟大黄素对植物血凝素(PHA)引起的大鼠T淋巴细胞增殖和细胞内Ca2 浓度([Ca2 ]i)变化的影响,探讨芦荟大黄素对T淋巴细胞增殖的作用和机制。方法采用MTT法检测细胞增殖,用单细胞钙成像系统记录细胞胞浆[Ca2 ]i。结果芦荟大黄素对PHA引起的细胞增殖有显著抑制作用,且其抑制作用与剂量有关;加入PHA引起细胞[Ca2 ]i迅速升高,并持续维持高[Ca2 ]i水平,芦荟大黄素对PHA引起的[Ca2 ]i升高有显著抑制作用,其作用途径包括阻断胞内Ca2 释放和抑制胞外Ca2 内流。结论芦荟大黄素可抑制T淋巴细胞增殖,其作用机制可能与抑制淋巴细胞内[Ca2 ]i升高相关。     

Improved lymphatic targeting: effect and mechanism of synthetic borneol on lymph node uptake of 7-ethyl-10-hydroxycamptothecin nanoliposomes following subcutaneous administration

Borneol as a penetration enhancer is widely used in guiding other components through the biological barrier into the targeting organs or tissues. This study aimed at studying effect and mechanism of synthetic borneol (S-BO) on improving lymphatic-targeting ability of 7-ethyl-10-hydroxycamptothecin liposomes (SN-38-Lips) via increasing lymph node uptake. At first, SN-38-Lips prepared had appropriate particle distribution, drug loading property and compatible stability with S-BO. Both in vitro cellular uptake and in vivo fluorescence imaging showed that 2 and 5?mg/mL S-BO, especially 2?mg/mL S-BO, enhanced cytoplasmic fluorescence signal of SN-38-Lips in the macrophages based on phagocytosis effect. And high-intensity zone appeared in the paracortex and medulla of popliteal lymph node. SN-38-Lips were subcutaneously (s.c.) injected into the right footpad of KM rats in the dose of 4?mg/kg following s.c. injection of 1, 2 and 5?mg/mL BO suspension. The lymphatic pharmacokinetics were investigated to explore the promotion law of S-BO, and combined with tissue irritation to optimize S-BO concentrations. The results indicated that 2?mg/mL S-BO could reduce injection-site retention, and prolong residence time and increase uptake of lymph nodes, which would not cause inflammatory reaction of injection site. In conclusion, the present study may provide a basic study for improving lymphatic-targeting ability of SN-38-Lips by the S-BO regulation, and to be the helpful guidance for further study in lymphatic targeting of delivery system.     

HPLC法测定夏黄颗粒中芦荟大黄素、大黄酸、厚朴酚、和厚朴酚、大黄素、大黄酚和大黄素甲醚

目的建立HPLC法同时测定夏黄颗粒中芦荟大黄素、大黄酸、厚朴酚、和厚朴酚、大黄素、大黄酚和大黄素甲醚。方法采用Diamonsil C18色谱柱(250 mm×4.6 mm,5μm);流动相:甲醇–0.1%磷酸水溶液,梯度洗脱;检测波长254 nm;体积流量1.0 m L/min;柱温30℃;进样体积20μL。结果芦荟大黄素、大黄酸、厚朴酚、和厚朴酚、大黄素、大黄酚、大黄素甲醚分别在23.8~238.4、22.8~228.0、25.8~228.0、78.7~787.2、16.7~167.2、16.6~166.4、17.5~175.2μg线性关系良好;平均加样回收率分别为99.78%、99.36%、99.71%、98.65%、99.37%、99.42%、98.78%,RSD值分别为1.88%、2.05%、2.03%、2.01%、2.56%、2.35%、2.17%。结论本法快速、简便、准确,可用于夏黄颗粒的质量控制。     

A Modified Method for Isolation of Rhein from Senna

A simple and efficient method for the isolation of rhein from Cassia angustifolia (senna) leaves is described in which the hydrolysis of the sennosides and extraction of the hydrolysis products (free anthraquinones) is carried out in one step. Further isolation of rhein is achieved from the anthraquinone mixture. This method reduces the number of steps required for isolation of rhein as compared to conventional methods.     

三黄泻心汤煎煮过程中13种指标成分动态变化与分布规律研究

目的 建立经典名方三黄泻心汤（Sanhuang Xiexin Decoction,SXD）中13种指标成分（表小檗碱、黄连碱、巴马汀、小檗碱、黄芩苷、汉黄芩苷、黄芩素、汉黄芩素、大黄酸、芦荟大黄素、大黄素、大黄酚、大黄素甲醚）的含量同时测定方法,探索SXD煎煮过程中成分动态变化和分布规律,揭示SXD复合分散体系的制剂特征。方法 按照SXD传统煎煮方法制备煎液,建立样品中13种指标成分的含量同时测定方法,检测各指标成分在汤剂、离心上清液、离心沉积物中的含量;进一步地,分别制备浸泡结束、刚沸腾以及煎煮不同时间后的样品进行测定,绘制SXD煎煮过程中13种指标成分动态变化和分布规律图,分析煎煮过程中各成分在汤剂、离心上清液和离心沉积物中的含量变化情况。结果 SXD煎液中,含量最高的指标成分为黄芩苷（15.496 mg/g）,其次为小檗碱（3.048 mg/g）,含量最低的指标成分为大黄素甲醚（0.046 mg/g）;离心沉积物中黄连碱、小檗碱含量分别为离心上清液的4.13、3.44倍,离心上清液中黄芩苷、汉黄芩苷、芦荟大黄素含量分别为离心沉积物的2.04、2.76、1.33倍;煎煮过程中,自浸...     

HPLC同时测定喘舒片中5种蒽醌类成分的含量

目的:建立HPLC法测定喘舒片(升华硫、大黄粉、黄芩提取物等)中5种蒽醌类成分的含量.方法:色谱柱:Lanbo(R) Kromasil C18柱,流动相:甲醇-0.3%磷酸(80∶20),柱温:30℃,流速:1.0 mL/min,检测波长:254 nm.结果:芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚平均回收率分别为97.47%,98.18%,97.75%,98.00%,98.06%,芦荟大黄素在进样量0.093 6～O.468 μg、大黄酸在进样量0.098～0.49μg、大黄素在进样量0.106～0.53μg、大黄酚在进样量0.232～1.16 μg、大黄素甲醚在进样量0.147 6～0.738μg范围内与峰面积呈良好线性关系.结论:该方法简便、灵敏、结果准确可靠,适用于该制剂中蒽醌类成分的质量控制.     

Gamma irradiation of aloe-emodin induced structural modification and apoptosis through a ROS- and caspase-dependent mitochondrial pathway in stomach tumor cells

Purpose: The changes in molecular structure and the physiological properties of a gamma-irradiated aloe-emodin were examined.

Materials and methods: Aloe-emodin was gamma-irradiated at doses ranging from 0 to 150 kGy, and the molecular structure was then analyzed using high-performance liquid chromatography (HPLC). AGS cells were cultured in RPMI medium and treated gamma irradiated aloe-emodin. Cell viability was measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Apoptosis efficiency was investigated by cell cycle arrest, cell morphology, and signaling pathway. The structure of new radiolytic peak was identified by the hydrogen-nuclear magnetic resonance (¹H NMR).

Results: HPLC results showed that gamma irradiation induced new radiolytic peaks that were distinguishable from the aloe-emodin standard, and the area of new peaks was increased as the radiation dose increased. Gamma-irradiated aloe-emodin treatment significantly increased the cytotoxicity in AGS tumor cells. We also found that 150?kGy aloe-emodin increased the expression of Bax, cytosolic cytochrome c, PARP cleavage, and the activation of caspases-8, -9, -3, Bid, and Bcl-2. Treatment of 150?kGy aloe-emodin induced ROS production, DNA fragmentation, alterations of cell morphology, and the migration in AGS cells. Gamma-irradiated aloe-emodin induced an increase of sub-G1 phase and depolarization of mitochondrial membrane potential in AGS cells. We also confirmed that fractionated AEF1 (new radiolytic peak) induce the cell death, migration, an increase of sub-G1 phase and cytochrome c in a ROS-dependent manner.

Conclusions: The radiolysis product (AEF1) of aloe-emodin transformed by gamma-irradiation strongly induced apoptotic cell death in AGS cells, indicating AEF1 is a potential candidate drug for use in anti-cancer drug.