艾纳香总黄酮对急性心肌梗死模型大鼠的药效作用及机制研究

目的研究艾纳香总黄酮对急性心肌梗死(AMI)模型大鼠的药效作用及可能机制。方法采用结扎SD大鼠冠状动脉左前降支的方法建立AMI模型。选取造模成功的50只大鼠,按照随机数字表法分为模型组(0.8%羧甲基纤维素溶液)、阳性对照组(复方丹参片,300 mg/kg)和艾纳香总黄酮低、中、高剂量组(3、10、30 mg/kg),每组10只;另取10只作为假手术组(0.8%羧甲基纤维素溶液)。手术1 d后开始灌胃给药,给药体积均为3 mL/kg,每天给药1次,连续4周。记录术前、术后及每周灌胃给药后大鼠心电图S-T段的变化;检测大鼠血流动力学指标[动脉收缩压(SBP)、舒张压(DBP)、平均动脉压(MAP)、左心室收缩压(LVSP)、左心室舒张末压(LVEDP)、左心室内压最大上升速率(+LVdp/dt_(max))和左心室内压最大下降速率(-LVdp/dt_(max))];检测大鼠血清心肌酶[乳酸脱氢酶(LDH)、肌酸激酶同工酶-MB(CK-MB)]和炎症因子[肿瘤坏死因子α(TNF-α)、白细胞介素6(IL-6)、IL-1β]水平;检测大鼠心肌梗死率和心肌组织中磷脂酰肌醇3激酶(PI3K)、蛋白激酶B(Akt)的磷酸化水平。结果与模型组比较,给药后各组大鼠心电图S-T段均显著降低(P<0.05);艾纳香总黄酮中、高剂量组大鼠SBP、DBP、MAP、LVSP、+LVdp/dt_(max)、-LVdp/dt_(max)及p-PI3K^(Tyr607)/PI3K、p-Akt^(Thr308)/Akt、p-Akt^(ser473)/Akt比值均显著升高(P<0.05),LVEDP、血清心肌酶和炎症因子水平、心肌梗死率均显著降低(P<0.05)。结论艾纳香总黄酮能改善AMI模型大鼠的心功能;其作用机制与抑制炎症因子表达,激活PI3K/Akt信号通路有关。

艾纳香二氢黄酮对脂质过氧化损伤大鼠原代培养肝细胞的保护作用

研究 5种艾纳香二氢黄酮类化合物对过氧化损伤的原代培养肝细胞的保护作用。胶原酶灌流法分离大鼠肝细胞。以 CCl4或 Fe SO4+Cys损伤原代培养肝细胞 ,1× 10 - 4 和 1× 10 - 5 mol/ L 的 5种艾纳香二氢黄酮均能明显抑制受损伤细胞的转氨酶逸出、MDA产生及 GSH耗竭。其中以 2 ,5 -二羟基艾纳香二氢黄酮的作用最强 ,在 CCl4所致肝细胞损伤实验中 ,其抑制 MDA产生的 ED5 0 约为 2 .6× 10 - 6 mol/ L ,保护 GSH的 ED5 0 约为 1.0 8× 10 - 5 mol/ L ,抑制 AL T逸出细胞的 ED5 0 约为 9.39× 10 - 6 mol/

超声辅助双水相提取艾纳香总黄酮的工艺优化及抗氧化活性的研究

以艾纳香为原料、艾纳香总黄酮得率为指标,采用超声辅助乙醇-硫酸铵双水相体系对艾纳香总黄酮提取工艺进行单因素及Box-Behnken响应曲面试验优化,并用羟自由基清除力、DPPH自由基清除力以及还原力与一般回流提取所得的总黄酮的抗氧化能力进行比较研究。结果表明,艾纳香总黄酮超声辅助双水相提取的最佳工艺条件为超声时间31 min、(NH_4)_2SO_4用量0.4 g/m L、液料比为32 m L∶1 g,此条件下提取的艾纳香总黄酮得率为(13.31±0.21)%。对DPPH自由基、羟自由基有较强的清除能力以及较高的还原力,且超声辅助双水相提取的艾纳香总黄酮抗氧化能力显著高于一般回流提取。

艾纳香二氢黄酮对大鼠实验性肝损伤的保护作用

艾纳香二氢黄酮对大鼠实验性肝损伤的保护作用许实波赵金华（中山大学药学系药理学教研室，广州５１０２７５）中国图书分类号Ｒ２８４．１；Ｒ９７５．５艾纳香二氢黄酮（ｂｌｕｍｅａｆｌａｖａｎｏｎｅｓ，ＢＦｓ）包括５种化合物，本文分别命名为ＢＦ－Ⅰ、ＢＦ－Ⅱ、...

艾纳香二氢黄酮对脂质过氧化及活性氧自由基的作用

目的研究5种艾纳香二氢黄酮化合物的抑制脂质过氧化及其对超氧阴离子自由基（O）、羟自由基（·OH）的清除作用。方法：不同浓度的艾纳香二氢黄酮化合物与大鼠组织匀浆或自由基发生系统共治后，比色法测定丙二醛、、·OH生成量。结果：10(－5)～10(－4)mol·L(-1)浓度下，5种艾纳香二氢黄酮类化合物，能够抑制大鼠组织匀浆自氧化及FeSO4／半胱氨酸激发的脂质过氧化，10(－6)～10(－5)mol·L(-1)浓度下能够清除黄嘌呤／黄嘌呤氧化酶系统产生的O，以及抗坏血酸／硫酸铜自由基系统产生的·OH。结论：艾纳香二氢黄酮具有较强的抗氧化作用。

艾纳香二氢黄酮对脂质过氧化损伤的恒河猴原代培养肝细胞及肝亚细胞的保护作用

目的；研究艾纳香二氢黄酮对脂质过氧化致损伤的恒河猴原代培养肝细胞及肝亚细胞的保护作用。方法：艾纳香二氢黄酮与原代培养肝细胞共育后，以CCl4或FeSO4－半胱氨酸致细胞损伤，以脂质过氧化产物丙二醛产生量及转氨酶的漏出量作为损伤程度指标，亚细胞结构与艾纳香二氢黄酮共育后，以FeSO4^-半胱氨酸致脂质过氧化，以丙二醛产生量徇过氧化损伤程度。结果：10及100μmol·L^-1的艾纳香二氢黄酮可降低被损伤的肝细胞中的丙二醛产生，降低转氨酶漏出，抑制肝亚细胞结构中丙二醛生成，结论：艾纳香二氢黄酮具有抑旨质过氧化作用及肝1`业细胞结构保护作用。

艾纳香总黄酮微胶囊制备工艺优化及稳定性研究

采用β-环糊精(β-CD)饱和水溶液法制备艾纳香总黄酮微胶囊,以总黄酮包埋率为指标,以壁芯比、搅拌时间和搅拌温度为考察因素,进行单因素及Box-Behnken响应曲面实验优化微胶囊配方。结果表明:艾纳香总黄酮微胶囊最佳的制备工艺为壁芯比15.4、搅拌时间59 min和搅拌温度40℃,得出的总黄酮包埋率为(60.89±0.23)%,经电镜法观察其形态规则,分布均匀。稳定性实验结果表明,制备的微胶囊在高温、强光下包埋率稳定,高湿条件下包埋率下降,为艾纳香总黄酮的进一步开发利用提供参考。

Effects of Calcium Element on Biomass and Effective Constituents Contents in Blumea balsamifera in Slow Growth Period of Winter

The one-year-old seedlings of Blumea balsamifera （L.） DC. were applied with CaCl2.H2O that supplied Ca in slow growth period of winter three times. The heights, ground diameters, leaf lengths, leaf widths and biomasses of B. balsamifera plants were measured. In addition, the relative contents of total flavones in different parts of B. balsamifera were determined by UV spectrophotometry, and the absolute contents of total flavones were calculated. The relative contents of L-borneol in leaves of B. balsamifera were determined by GC, and the absolute contents of L- borneol were calculated. The results showed that calcium element significantly in- creased the biomasses in leaves, stems and roots of B. balsamifera in slow growth period of winter. The leaf biomass of B. balsamifera in the 5 g/L CaCl2-H2O treat- ment group was significantly higher than those in the other three treatment groups. The leaf biomasses of B. balsamifera in the 10 and 15 g/L CaCl2.H2O treatment groups were significantly higher than that in the CK, with 3.03 and 2.65 times, re- spectively. The application of Ca inhibited the accumulation of total flavones relative contents, but significantly increased the total flavones absolute contents in different parts of B. balsamifera. The relative and absolute contents of L-borneol in the 5 g/L CaCl2 .H2O treatment group were 0.22% and 0.22 g, which were increased by 37.50%, 22.22%, 37.50% and 100%, 100%, 450%, respectively compared with those in the 0, 10 and 15 g/L CaCl2.H2O treatment groups. The Ca element could signifi- cantly promote the accumulation of biomasses in leaves, stems and roots, as well as the absolute contents of total flavones and L-borneol in B. balsamifera in slow growth period of winter.

Protective Actions of Blumea Flavanones on Primary Cultured Hepatocytes and Liver Subcellular Organelle against Lipid Peroxidation

To search for the protective actions of blumea flavanones (BFs) on hepatocytes and hepatic subcellular organelle against lipid peroxidation, monkey′s hepatocytes were isolated and cultured with or without blumea flavanones, then damaged by FeSO 4 cysteine or CCl 4. The lipid peroxidation (malondialdehyde production) and alteration in hepatocyte membrane (leakage of GPT) were estimated. Hepatic subcellular organelles were also isolated and incubated with or without blumea flavanones, then injured by FeSO 4 ascorbate. The generation of malondialdehyde(MDA) was measured. It was found that BFs 10 and 100 μmol·L 1 inhibited the MDA generation and GPT (glutamic pyruvic transaminase) leakage out of hepatocytes that were induced by CCl 4 or FeSO 4 cysteine. BFs could prevent lipid peroxidation initiated by FeSO 4 ascorbate in subcellular organelle suspension. Among BFs, BF 2 possessed the strongest activity. Conclusion: Blumea flavanones possess antioxidation activities that protect monkey′s hepatocytes and hepatic subcellular organelle against injuries induced by FeSO4 or CCl 4.