双-对硝基苯磷酸酯钠对麻醉家兔没食子酸丙酯药物代谢动力学的影响(英文)

用高效液相色谱测定家兔给予没食子酸丙酯 (PG) 15和 30mg·kg-1后 1 0 ,2 0 ,3 5 ,7 0 ,10 0 ,2 0 0 ,30 0和 40 0min的血浆浓度 ,分析所得血药浓度 时间曲线符合二室开放性模型 .给家兔ip双 对硝基苯磷酸酯钠 (BNPP) 3 4mg·kg-1,再ivPG 15和 30mg·kg-1,所测BNPP组与对照组PG血浆浓度有显著不同 ,t1/ 2 β,MRT以及AUC较对照组显著延长或增加 ,而k10 及Cl显著缩短 ,组间比较均P <0 0 5 ,P <0 0 1,P <0 0 0 1.ivPG5 0 ,10 0及 2 0 0min后其肝 ,肾和血桨中PG浓度也较对照组增高 ,组间比较均P <0 0 5 ,结果表明BNPP对PG在家兔体内的代谢速率有明显影响 .     

Elimination of Deleterious Effects of Free Radicals in Murine Skin Carcinogenesis byBlack Tea Infusion,Theaflavins & Epigallocatechin Gallate

In recent years, numerous reports have been published on the identification of novel, naturally occurring ‍antioxidants from plants, animals, microbial sources and processed food products. Most natural antioxidants are ‍phenolic compounds, which have a modulatory role on physiological functions and biotransformation reactions ‍involved in the detoxification process, thereby affording protection from cytotoxic, genotoxic and metabolic actions ‍of environmental toxicants. As part of our program on evaluation of food, beverage and traditional medicinal plants ‍for their anticarcinogenic activity, the present report deals with the evaluation of aqueous infusion of Black tea ‍(Camellia sinensis), Black tea extract (80% Theaflavins) & EGCG on mice exposed to the chemical carcinogen ‍DMBA. All the four detoxification enzymes studied viz, GST, GPx, SOD and CAT were found to be activated to ‍different degrees following treatment with black tea and two of its active compounds. The activation of the enzymes ‍was accompanied by significant reduction in lipid peroxidation. The effect on apoptosis and cell proliferation was ‍also studied in mice skin following administration of DMBA. Theaflavins, and EGCG significantly inhibited cell ‍proliferation and induced apoptosis. The observation suggests chemopreventive potential of black tea infusion, ‍black tea extract Theaflavins and the compound EGCG.‍     

Allergic contact cheilitis from a lipstick misdiagnosed as herpes labialis: Subsequent worsening due to Zovirax contact allergy

A 29-year-old Turkish woman with allergic contact cheilitis from a lipstick was misdiagnosed as herpes labialis and subsequently worsened with the application of Zovirax cream. Patch tests were positive to Zovirax cream, propylene glycol, the patient's favourite lipstick and propyl gallate. No reaction was seen with Zovirax ophthalmic ointment and Zovirax tablet. The propylene glycol component of the Zovirax cream and the propyl gallate component of the lipstick were regarded as the responsible contact sensitizers. The differential diagnosis was challenging due to concomitant contact sensitization with these agents.     

羟氯喹及没食子酸酯对HaCaT细胞光照射的影响

目的 探讨羟氯喹和绿茶活性成分表没食子儿茶素没食子酸酯(EGCG)对中波紫外线(UVB)损伤永生化角质形成细胞株(HaCaT细胞)的保护作用及其机制。方法 采用UVB定时及定量照射培养的HaCaT细胞,分别加入羟氯喹和EGCG干预处理,以RT-PCR法检测各受试组p53、p21、c-fos基因表达水平。结果 UVB照射后可明显增加HaCaT细胞中p53,p21,c-fos mRNA表达,羟氯喹和EGCG可不同程度地下调上述基因表达水平。结论 羟氯喹和EGCG的光保护作用在HaCaT细胞可能与其抑制p53,p21,c-fos基因表达有关。     

双 -对硝基苯磷酸酯钠对麻醉家兔没食子酸丙酯药物代谢动力学的影响(英文)

用高效液相色谱测定家兔给予没食子酸丙酯 ( PG) 1 5和 30 mg· kg-1后 1 .0 ,2 .0 ,3.5,7.0 ,1 0 .0 ,2 0 .0 ,30 .0和 40 .0 min的血浆浓度 ,分析所得血药浓度 -时间曲线符合二室开放性模型 .给家兔 ip双 -对硝基苯磷酸酯钠 ( BNPP) 3.4mg·kg-1,再 iv PG1 5和 30 mg·kg-1,所测 BNPP组与对照组 PG血浆浓度有显著不同 ,t1/2β,MRT以及AUC较对照组显著延长或增加 ,而 k10 及 Cl显著缩短 ,组间比较均 P<0 .0 5,P<0 .0 1 ,P<0 .0 0 1 .ivPG5.0 ,1 0 .0及 2 0 .0 min后其肝 ,肾和血桨中 PG浓度也较对照组增高 ,组间比较均 P<0 .0 5,结果表明 BNPP对 PG在家兔体内的代谢速率有明显影响 .     

Protective Effect of Propyl Gallate Against Oxidized Low-Density Lipoprotein-Induced Injury of Endothelial Cells

Objective:To evaluate the protective effect of propyl gallate(PG),an alkyl ester of gallic acid which is an active ingredient of Radix Paeoniae,against oxidized low-density lipoprotein(ox-LDL)-induced apoptosis and death in endothelial cells(ECs) and to find out its preliminary mechanism.Methods:The cultured endothelial cells were divided into normal,model(ox-LDL),control(fetal bovine serum),PG high dose(20 μg/mL),PG middle dose(10 μg/mL),and PG low dose(5 μg/mL) groups,each derived from three different pools of umbilical cords.The model of injured human umbilical vein endothelial cells(HUVECs)was induced by ox-LDL.The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide(MTT) assay,Hoechst 33258 staining,flow cytometry and measurement of nitrogen monoxidum(NO) release were used to evaluate the protective effect of PG against ox-LDL-induced apoptosis and death in HUVECs.To find out the mechanism of this protective effect,the expression of endothelial nitric oxide synthase(eNOS) mRNA,eNOS protein expression,immunofluorescence of intracellular reactive oxygen species(ROS) and activities of malondialdehyde(MDA),superoxidedismutase(SOD) and glutathione peroxidase(GPx) were observed.Results:PG significantly reduced ox-LDL-induced apoptosis and cell death.The percentage of cells death and apoptosis was significantly higher in the ox-LDL group than that in the control group(P0.05).Compared with the control group,the cells death and apoptosis of PG group was no different(P0.05).As compared with the ox-LDL group,results of the PG high dose group showed that cell viability was significantly increased(P0.05),the level of NO release,expression of eNOS mRNA,densitometric value of eNOS protein expression,as well as the activities of SOD and GPx were all significantly higher(all P0.05).Conclusion:PG could potentially serve as a novel endothelial protective agent against ox-LDL-induced injury of endothelial cell.     

棓丙酯与抗生素联合抗多重耐药鲍曼不动杆菌作用研究

目的 探讨棓丙酯与临床上常用抗生素(头孢他啶、环丙沙星和阿米卡星)对多重耐药鲍曼不动杆菌的联合抑菌作用.方法 根据临床药敏结果选取9株鲍曼不动杆菌多重耐药菌株和鲍曼不动杆菌标准菌株ATCC19606作为实验对象,用棋盘滴定法测定棓丙酯分别与头孢他啶、环丙沙星和阿米卡星的联合抑菌效应.结果 除鲍曼不动杆菌标准菌株外,9株鲍曼不动杆菌多重耐药菌株对三种抗生素皆耐药,棓丙酯对各株细菌均有一定的抑制作用,且对耐药株和标准菌株的最低抑菌浓度(MIC)基本相同;棓丙酯分别与头孢他啶、环丙沙星、阿米卡星联用后抑菌作用表现为相加.结论 棓丙酯对鲍曼不动杆菌生长具有抑制作用,与抗生素联用后抗菌活性增加.     

表没食子儿茶素没食子酸酯对2型糖尿病大鼠生化指标的影响

目的:观察表没食子儿茶素没食子酸酯(epigollatecatechin gallate,EGCG)对2型糖尿病大鼠血液生化指标的影响。方法:采用链脲佐菌素联合高脂饮食复制2型糖尿病大鼠模型,Wistar大鼠造模后随机分为正常对照组、模型对照组、EGCG大、中、小剂量[50、20、10 mg/(kg·d)]组治疗4周后。检测血清中门冬氨酸氨基转移酶(AST)、丙氨酸氨基转移酶(ALT)、总胆固醇(TCHO)、甘油三酯(TG)、尿素氮(UREA)、肌酐(CREA)变化。结果:与对照组比较,三组EGCG治疗组大鼠AST、ALT、UREA和CREA水平明显降低(P<0.05,P<0.01);低浓度EGCG组对TCHO的影响无统计学差异(P>0.05),中、高浓度EGCG组TCHO、TG的影响有统计学意义(P<0.05)。结论:EGCG具有改善血脂紊乱,保护肝肾功能的作用。     

儿茶素单体在治疗炎症性肠病作用中对NF-κB信号通路的影响

目的探索儿茶素单体表没食子儿茶素没食子酸酯(EGCG)在治疗炎症性肠病(IBD)模型大鼠作用中对NF-κB信号通路的影响。方法将36只健康SD大鼠随机分为正常对照组、模型组、EGCG治疗组,每组12只,以三硝基苯磺酸(TNBS)灌肠制作大鼠IBD模型。灌肠用药2周后,分别用ELISA检测肠组织中PGE2、NO含量;免疫组化检测肠粘膜COX-2、iNOS的蛋白表达;Western Blotting检测大鼠肠粘膜NF-κB p65蛋白水平的变化。结果①模型组肠组织内PGE2、NO含量显著增高。EGCG治疗组大鼠肠组织内PGE2、NO含量与模型组相比显著减少(P=0.000);②模型组肠粘膜组织中COX-2表达明显增强,正常结肠组织未见或少见COX-2蛋白表达。而EGCG灌肠后大鼠肠组织中COX-2的表达显著下降。③模型组肠粘膜组织中iNOS表达明显增强,正常结肠组织未见或少见iNOS蛋白表达。而EGCG灌肠后大鼠肠组织中iNOS的表达显著下降。④正常大鼠肠组织NF-κB p65蛋白水平较低,模型组肠组织内NF-κB p65蛋白水平显著增加。EGCG可显著抑制肠组织内NF-κB p65蛋白水平表达。结论 EGCG可通过降低NF-κB p65蛋白的表达,下调COX-2、iNOS的表达,使其产物PGE2、NO生成减少,从而达到减轻炎症的目的。因此NF-κB可作为EGCG治疗大鼠实验性结肠炎的一个有效的分子"靶点"。