Protective Effect of GRK2 and Effect of Sanguis Draconis Flavones on Focal Cerebral Ischemia-Reperfusion Injury in Rats

[Objectives] To explore the protective effect of Sanguis Draconis flavones (SDF) on rat focal cerebral ischemia-reperfusion injury (CIRI) models established by middle cerebral artery occlusion (MCAO).[Methods] A total of 60 healthy adult male Sprague-Dawley rats were selected. They were evenly and randomly divided into sham group, model group, edaravone group (12 mg/kg) and SDF group (360 mg/kg), and administered intragastrically and intraperitoneally. The middle cerebral artery of each rat was blocked by suture-occluded method to establish a CIRI model. After ischemia for 2 h and reperfusion for 48 h, the pathological injury on the ischemic side was observed by HE staining;the neuron and myelin sheath structure was observed by transmission electron microscopy;the expression of G protein-coupled receptor kinase 2 (GRK2) was preserved by immunohistochemistry;and the transfer of GRK2 was detected by western-blot.[Results] After 48 h of CIRI, the nuclei of the penumbral cortical neurons shrank, the chromatin was unevenly distributed, the nuclear membrane was dissolved and the mitochondria in the cytoplasm were swollen and vacuolated. The myelin layer was disordered. With this change, the distribution of GRK2 subcellular cells in the penumbra of the injured lateral cortex transferred from the cytoplasm to the membrane. SDF can effectively restore neuronal and myelin sheath structural damage and reduce the functional (membrane coupling) expression of GRK2.[Conclusions] GRK2 may be an effective target for SDF to protect the impaired blood-brain barrier (BBB) in CIRI.

Immunoregulatory Effects of Sanguis Draconis Flavones on Mouse Spleen Lymphocytes

[Objectives] This study aimed to study the effects of Sanguis Draconis flavones( SDF) on the immune regulation of mouse spleen lymphocytes. [Methods]A total of 60 BALB/c male mice were evenly and randomly divided into normal control group,model group,positive group,and high,middle and low-dose SDF groups. The mice in the model group were injected intraperitoneally with cyclophosphamide to establish mouse immunosuppressive model. The mice in the other groups were intragastrically administered at the respective doses,and the body weight was weighed once a week during the administration period. After 30 d of administration,the thymus and spleen indexes,the spleen lymphocyte proliferation ability,the NK cell activity,and the IL-2,IL-4 and INF-γ contents in the culture supernatant were measured. [Results]SDF could significantly increase the thymus and spleen indexes and improve the spleen lymphocyte proliferation ability and NK cell activity of the mice,as well as increasing the IL-2 and INF-γ contents and reducing the IL-4 content in spleen lymphocyte suspension culture. [Conclusions] SDF have good immunoregulatory effect.

A 180-Day Subchronic Oral Toxicity Study of Total Flavones of <i>E. leptorrhizum</i>Stearn in Rats

A subchronic oral toxicity was conducted to evaluate the safety of total flavones of E. leptorrhizum Stearn in Sprague-Dawley rats. The test article was administered once daily by gavage in male and female rats at dose levels of 24, 48, and 96 mg/kg body weight/day for 180 days. 90 and 180 days after administration, ten and tweedy animals (each half of male and female) of each group were tested. 28 days after withdrawal, five male and female rats were tested. There were no significant toxicological changes shown in daily clinical signs, body weight, food consumption, hematology parameters, blood biochemistry, organ weights and histopathological examination except leukocyte differential count. It was concluded that the no-observed-effect level (NOEL) for total flavones of E. leptorrhizum Stearn was >96 mg/kg in SD rats.

ANTAGONISM OF TOTAL FLAVONES OF GYNOSTEMMA PENTAPHYLLUM (THUNB) MAK TO ANIMAL EXPERIMENTAL ARRHYTHMIA

The action of total flavones of Gynostemma pentaphyllum (Thunb) Mak (TFG) 60 mg/kg i.v. could prevent arrhythmias induced by drugs and myocardial ischemia were investigated. In anesthetized rats and guinea pigs. The results showed that in TFG group the duration of ventricular tachycardia (VT) induced by aconitine in rats was shortened (P<0 01) and the incidence of ventricular fibrillation (VF) and the mortality were decreased (P<0 01) respectively. The arrhythmias induced by i.v. BaCl 2 4 mg/kg in rats were immediately recovered to a normal sinus rhythm and VT induced by i.v. CaCl 2 130 mg/kg in rats was decreased by TFG i.v. TFG i.v. elevated the doses of i.v. strophanthin G to induce ectopic beats (EB), VT, VF and cardiac arrest (CA) in guinea pigs by 89%, 58%, 27%, and 28% (P<0 01) respectively. The incidence of VF induced by coronary artery ligation in rats was decreased (P<0 01), duration of EB, duraton of VT and VF decreased to 45%, 42% and 0% of the NS group respectively. The results suggest that TFG in dosage of 60 mg/kg might be useful for the prevention of VT and VF.

Structure of Flavones and Flavonols. Part II: Role of Position on the O-H Bond Dissociation Enthalpy

The enthalpies of bond dissociations of the hydroxyl groups, the energy of the highest occupied molecular orbitals and the corresponding radicals spin densities of all possible ten isomeric mono-hydroxyl flavones are calculated by means of 3-parameter Becke, Lee, Yang and Parr functional. The structural factors affecting these descriptors of radical-scavenging activity are outlined. The results obtained show that the hydroxyl groups in ring A and C are more involved in the process of a radical-capturing than recently believed.

A NEW AND EFFICIENT SYNTHESIS OF 3-IODO DERIVATIVES OF FLAVONES, THIOFLAVONES AND THIOCHROMONES

The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are potentially useful precursors for the synthesis of C-3 linked binuclear compounds.

Separation and Purification Process of Total Flavones from Litchi Pericarp by Macroporous Absorption Resin

[Objective] This study aimed to optimize the conditions for purification of total flavones from litchi pericarp by macroporous absorption resin.[Method] The flavones adsorption rates and desorption rates of macroporous absorption resins(AB-8,HPD-600,D101) were compared,and the technological parameters of D101 during the purification process were investigated.[Result] D101 macroporous absorption resin was appropriate for the purification of total flavonoids from litchi pericarp.The optimal technological conditions were selected:the pH of sample solution was 5.0;concentration of sample solution was 4 mg/ml,with a volume of 2.5BV;80% ethanol was used as elution solution,with a volume of 2.0BV.[Conclusion] The content of total flavones achieved 83% after separation by D101 macoporous absorption resin.

Antioxidations and Their Correlations with Total Flavones and Anthocyanin Contents in Different Black Rice Varieties

The antioxidations and their correlations with total flavones and anthocyanin contents in different black rice varieties were studied. The results indicated that the great differences in total antioxidant capacity （TAC）, scavenging free radical capacity （SFRC）, total flavones and anthocyanin contents existed among 242 black rice varieties. Comparisons of TAC, SFRC, total flavones and anthocyanin contents of different black rice types showed that the differences between black rice and white rice, indica one and japonica one, and nonglutinous one and glutinous one were significant at 0.01 levels, respectively. This showed that the TAC, SFRC, total flavones and anthocyanin contents of japonica type were higher than those of indica one, and nonglutinous type were higher than glutinous one. According to the fast clustering procedure, 242 black rice varieties could be clustered into 10 clusters, 184 indica rice varieties into 10 clusters, and 58 japonica rice varieties into 6 clusters. Most significant （P〈0.01） correlations existed between TAC and total flavones and anthocyanin contents, and between SFRC and total flavones and anthocyanin contents of black rice, respectively. This showed that the antioxidation of black rice was closely correlated with its active compositions of flavones and anthocyanin.

A Study on the Whitening Efficacy of Flavones in Lotus Leaf

Taking lotus flavones as the research object, cytotoxicity was evaluated by MTT test, inhibitory effects onthe activity of tyrosinase was studied, and DPPH scavenging experiments were carried out. Lotus flavoneswere used in a formula of skin cream and facial whitening effects were examined. Results shows that lotusflavones are exhibited no cytotoxicity at a concentration equal or less than 1%, and it can decrease the activityof tyrosinase at a concentration between 0.02%~0.30%. Lotus flavones can scavenge DPPH radical. The skincream containing lotus flavones declines facial melanin content. Lotus flavones have good biological safety andare suitable in cosmetics as whitening agents.

萱草活性成分黄酮干对糖尿病大鼠抗动脉粥样硬化活性的研究

研究萱草活性成份黄酮干对糖尿病大鼠血糖、血脂、血浆脂蛋白脂质过氧化的影响.方法取20只雄性大鼠(Ⅱ型糖尿病模型),随机分为2组:对照组喂普通饲料,实验组喂添加10 g/kg黄酮干的饲料20周,观察血液生化指标的变化.血液生化指标采用试剂盒测定,血浆脂蛋白采用序列超速离心分离法分离.结果喂饲萱草活性成份黄酮干的糖尿病大鼠血糖为(10.3±0.7)mmol/L,动脉粥样硬化指数为0.38±0.12,血浆过氧化脂质水平为(13.7±0.2)mmol/L;丙二醛(MDA)水平为(7.45±1.26)(nmol/mgHb),超氧化歧化酶(SOD)活性为(153.47±37.91)(活力单位/m l);未喂饲黄酮干的对照组糖尿病大鼠上述指标分别为(13.5±1.6)mmol/L、0.54±0.24和(20.1±2.8)mmol/L,(13.01±0.74)(nmol/mgHb),和(210.98±40.11)(活力单位/m l),差异有显著性.结论萱草活性成份黄酮干具有明显的降低血糖、改善动脉粥样硬化指数、抑制脂质过氧化的作用.表4,参5.

In Vitro Anti-viral Activities and Structureactivity Relationship Studies of Flavones and Dihydroflavone Derivatives as Influenza Virus Potential Neuraminidase Inhibitors

From the bioassay tests, 14 neuraminidase inhibitors （NIs） flavones and dihydroflavones derivatives from natural plants displayed different degree of inhibitory activities. Further- more, compounds No. 8 and 14 showed good inhibitory activity against influenza A virus with IC50 = 835.4 and 860.6 μg/mL. Then, to investigate interactions between NIs and neuraminidase （NA）, molecular docking was performed. Docking results indicated that Arg118, Asp151, Arg292 and Arg371 were the key residues in the active pocket of 2ht8. Main influencing factors of interactions between NIs and NA were hydrogen bond and electrostatic, then hydrophobic factor. Moreover, experimental activities of NIs were consistent with total scores of the docking. In order to understand the chemical-biological interactions governing their activities toward NA, QSAR models of 14 NIs were developed. The obtained HQSAR （hologram quantitative structure activity relationship）, PLS （partial least squares） and SRA （stepwise regression analysis） models were robust and had good exterior predictive capabilities. Moreover, squared multiple correlation coefficients （R2） and squared cross-validated correlation coefficients （Q2） of HQSAR and PLS models based on descriptors by Gaussian and Sarchitect were 0.832 and 0.721, 0.925 and 0.688, 0.892 and 0.692, respectively. R2 and SE （standard error） of SRA model based on descriptors by Gaussian were 0.922 and 0.072. Therefore, these models may be further used to design and evaluate the bioactivity of new compounds.

Research Progress of Total Flavones in Marchantia convoluta

According to the literature retrieval,the composition,detection method,preparation method and product development of total flavones in Marchantia convoluta were reviewed and prospected. This paper will provide a theoretical basis for further study and product development of total flavones in M. convoluta.

天山棱子芹化学成分的研究(英文)

从天山棱子芹中首次分离得到15个已知化合物,通过NMR、MS及IR等波谱数据,分别鉴定为6,7二羟基香豆素(1),(+)marmesin(2),marmesinin(3),5,7,4′三羟基黄酮(4),莰非醇3OαL吡喃鼠李糖甙(5),藤黄菌素3′OβD吡喃葡萄糖甙(6),(R)6hydroxy3(2hydroxypropan2yl)6methylcyclohex2enone(7),4羟基苯甲酸(8),3甲氧基4羟基苯甲酸(9),3甲氧基4,5亚甲二氧基苯甲酸(10),丁香酸甲酯(11),丁香酸甲酯4OβD吡喃葡萄糖甙(12),姜油酮4′OβD吡喃葡萄糖甙(13),2(4羟基苯基)乙醇(14)和正二十八醇(15)。其中化合物7为一新的天然产物。

Development of mild and efficient method for synthesis of substituted flavones using oxalic acid catalyst

草酸酸被用作催化剂让 2-hydroxychalcones 的 intramolecular cyclisation 在好收益形成黄酮。催化剂的效率被证明，许多底层从对充满电子的芳基醛和 2-hydroxychalcone 电子缺乏。

栾树不同部位总黄酮的提取及含量测定

通过微波辅助提取的L9(34)正交实验方法与索氏回流提取法,分别提取栾树果实、枝叶中总黄酮,确定微波辅助提取法较适宜,并得到其最佳提取工艺参数是:微波处理1min、水浴10min、固(原料)液(提取溶剂)比为1:20。以微波助提最佳工艺提取栾树总黄酮,通过NaNO2-Al(NO3)3-NaOH显色体系的510nm分光光度法测定其含量,得栾树果实、枝、叶中总黄酮含量分别为1.78%、0.27%、0.45%。对2003年9月、10月、11月分别采集的栾树果实进行提取及测定,3个采集时间的栾树果实中总黄酮含量分别为0.71%、1.78%、2.70%,总黄酮含量随果实趋向成熟而显著递增。

The Effects of Total Flavones of Hippophae Rhamnoides L. on Cardiac function and Hemodynamics of Normal Subjects

Healthy volunteers were randomly divided into TFH group(22 subjects) and placebo control group (20 subjects). We used double-blind method. The cardiac performance and hemodynamics of the subjects before and after administration of TFH or placebo were determined by Admittance and STI methods, Oral TFH in a dose of 10 mg could significantly decrease the PEP/LVET, ICT/LVET and ICT of the mormal subjects(P<0.05). Oral TFH could increase SV(P<0.05). CO, CI, SWI, CWI and LI also tended to increase. Oral TFH also markedly reduced TPR (P<0.05) and increasedc (P<0.05). After administration of TFH, HR and HP did not significantly change(P>0.05). After administration of placebo, the parameters observed did not significantly change(P>0.05). The above results show that TFH can strengthen myocardial contractility and pump function of the heart, reduce total peripheral vascular resistance and increase vascular clasticity in normal subjects.

HPLC法同时测定蒙药清肝玛努-4醇提物中6种成分的含量及指纹图谱的建立

目的建立同时测定蒙药清肝玛努-4醇提物中马钱苷酸、龙胆苦苷、芍药苷、牡荆素、甘草苷、甘草酸铵等成分的HPLC含量测定方法及指纹图谱研究。方法采用Agilent Eclipse XDB-C_(18)色谱柱(250 mm×4.6 mm,5μm),流动相为0.1%磷酸水溶液-乙腈,梯度洗脱,流速为1.0 mL/min,检测波长为230 nm(芍药苷、牡荆素、甘草苷)、237 nm(马钱苷酸)、250 nm(甘草酸铵)、270 nm(龙胆苦苷),柱温为30℃,进样量为10μL。结果蒙药清肝玛努-4醇提物中马钱苷酸、龙胆苦苷、芍药苷、牡荆素、甘草苷和甘草酸铵的质量浓度分别在0.0203~0.1210、0.0533~0.3177、0.0213~0.1270、0.0115~0.0690、0.0141~0.0838和0.0351~0.2091 mg/mL范围内与色谱峰面积呈良好的线性关系(r≥0.9998),平均回收率分别为94.75%、99.49%、92.32%、95.82%、101.29%和98.04%,RSD分别为1.11%、0.76%、0.99%、2.75%、1.09%和2.43%(n=6)。建立了蒙药清肝玛努-4醇提物的HPLC指纹图谱,以S1号样品色谱图为参照图谱,通过多点校正和全谱峰匹配,生成对照指纹图谱,共确定10个共有峰,经与对照品比对指认了其中8个成分。结论所建立的测定方法及指纹图谱准确、可靠、重复性好、专属性强,为蒙药清肝玛努-4的质量控制及后续开发提供了依据。

富锗木耳菌丝体不同溶剂提取物的体外抗氧化能力

为探索富锗木耳菌丝体不同溶剂提取物的体外抗氧化能力,以富锗木耳菌丝体为材料,通过水、70%乙醇和乙酸乙酯对富锗木耳菌丝体进行了物质提取,比较了不同提取物对超氧阴离子自由基、羟自由基和DPPH自由基的清除能力。采用隶属函数值评价了不同溶剂提取物的综合抗氧化能力,并对物质含量与抗氧化能力进行了相关性分析。结果表明:富锗木耳菌丝体有机锗含量为542.83μg/g。不同溶剂提取物的提取率和物质含量均不同,水和乙醇提取物的提取率较高,水提取物中多糖含量最多,乙酸乙酯提取物中多酚和黄酮含量最多。不同溶剂提取物对自由基均有一定的清除能力,且随着提取物浓度的增加而增加。水提取物对超氧阴离子自由基清除率最强,当提取物浓度为9 mg/mL时,清除率最高为43.32%。70%乙醇提取物对羟自由基和DPPH自由基的清除效果最好,当提取物浓度为9 mg/mL时,清除率分别为70.10%和76.99%。多糖、多酚和黄酮在清除自由基中均发挥不同的作用,70%乙醇提取物的综合抗氧化能力最强。多糖、多酚和黄酮含量均与DPPH自由基清除率有显著(P<0.05)正相关。70%乙醇提取物中多酚含量与羟自由基清除率有显著(P<0.05)正相关。多糖、多酚及黄酮对超氧阴离子自由基的清除率均有显著(P<0.05)影响。富锗木耳菌丝体含有较高含量的有机锗,提取物对自由基具有一定的清除能力,具有较好的抗氧化性能。本研究对开发富锗木耳功能食品具有一定指导意义。

超声辅助提取油莎豆油的工艺优化及品质分析

为提高油莎豆油的得率且保证成品品质,本研究采用超声辅助正己烷法对油莎豆油的提取工艺进行响应面试验优化,确定最优提取条件后对油莎豆油品质进行分析。在油的品质研究中,采用25℃(常温)、47℃(超声辅助提取最佳温度)、60℃(高温)三个温度对比超声作用对油样中总酚含量、总黄酮含量、1, 1-二苯基-2-三硝基苯肼(1,1-diphenyl-2-picrylhydrazyl,DPPH)自由基清除率、脂肪酸组成及含量的影响。结果表明:脱皮油莎豆研磨后在料液比1:15 (g/mL)、超声时间20 min、超声温度47℃、粉碎粒度70目时,油莎豆油的得率为25.01%±0.03%,油样为黄橙色微浊状态,具有豆类特有的香气。油莎豆油对DPPH自由基有一定的清除作用,超声可更好地溶出油莎豆中的营养物质,但对油莎豆中黄酮类物质的破坏效应相对较大,酚酸类物质在高温时含量显著(P<0.05)下降。在25~60℃间超声作用和温度的变化对脂肪酸的种类和含量的影响不大,油酸(C18:1)含量最高,约为73.81%~74.00%。本试验结果可以为油莎豆油脂的开发利用提供一定基础和理论依据。