TNF-α在肝衰竭疾病中作用的研究进展

正肝衰竭是多种因素引起的严重肝脏损害,导致其合成、解读、排泄和生物转化等功能发生严重障碍或失代偿,出现以凝血功能障碍、黄疸、肝性脑病、腹水等为主要表现的一组临床证候群[1]。越来越多的证据显示免疫介导的肝损伤在肝衰竭的发病中起到了重要作用[2]。近年来,对肿瘤坏死因子α(tumour necrosis factor-α,TNF-α)的研究越发深     

HPLC测定蒙古扁桃种仁中α-维生素E的含量

目的:利用高效液相法,测定出蒙古扁桃中维生素E的含量.方法:采用色谱为Wondasil C18(4.6 mm×250 mm,5μm),流动相为甲醇-水(98∶2),流速1.0 mL· min-1,柱温25℃,检测波长300 nm,检测器温度为室温(25℃).结果:α-维生素E在1～100 μg呈良好的线性关系,方程为Y=5 176.7X-7 645.8(r =0.999 6),平均回收率为99.4％(n=3,RSD 1.740％),蒙古扁桃桃仁中维生素E的含量在7.12 ～ 15.36 μg·g-1,以雅布格戈壁最高,固阳爬榆树最低.结论:该法可用于测定蒙古扁桃桃仁中的维生素E的含量,结果准确可靠,快速灵敏.     

Vaticanol(B,C and G),α-Viniferin和Hopeaphenol体外抑制小鼠骨髓生成的肥大细胞介质释放

目的:α-viniferin, vaticanol(B, C and G) 和 hopeaphenol 是白黎芦醇的低聚体,具有抗肿瘤和抗氧化等活性,而这些化学保护作用是与其抗炎作用有联系.本文研究旨在了解这些化合物对小鼠骨髓分化肥大细胞(BMMC)组织胺、肿瘤坏死因子和白三烯介质释放的影响,并观察对细胞外信号调节激酶(ERK)的激活作用.方法: 分离小鼠骨髓细胞,培养4～5周(RPMI-1640,IL-3 10 ng/ml),抗-DNP IgE 致敏,以DNP-BSA(30 ng/ml)刺激释放反应.在非免疫刺激释放实验中,A23187作为刺激剂.结果:所试化合物均表现出不同程度的抑制BMMC释放反应的作用.这些化合物对IgE刺激的TNF-α和LTs释放表现出显著的抑制作用,而对IgE刺激的组织胺释放反应,只有vaticanol B和vaticanol C 具有抑制作用(100 μmol/L).在A23187介导的非免疫刺激释放反应中,vaticanol(B,C和G)和hopeaphenol对组织胺释放表现出明显的对抗作用,大多数所试化合物有效地抑制了TNF-α和LTs的释放,唯vaticanol C和vaticanol G对LTs的释放无明显影响.α-viniferin和vaticanol C有效地抑制了IgE刺激的ERK酶的激活.结论:α-viniferin,vaticanol(B,C和G)和hopeaphenol能有效地抑制肥大细胞的炎性介质的释放反应,而对BMMC的细胞活力无明显影响     

肿瘤坏死因子-α在强直性脊柱炎活动期患者中的表达

目的：探讨血清肿瘤坏死因子-α在难治性强直性脊柱炎活动期患者发病中的表达意义.方法：采用免疫学方法,检测76例难治性强直性脊柱炎活动期患者和37例强直性脊柱炎缓解期患者血清中肿瘤坏死因子-α,进行统计学分析.结果：难治性强直性脊柱炎活动期患者组中血清肿瘤坏死因子-α水平均显著高于强直性脊柱炎缓解期患者,表明肿瘤坏死因子-α是难治性强直性脊柱炎活动期患者发病过程中的重要炎症指标.结论：肿瘤坏死因子-α是AS发病相关的细胞因子,直接或间接参与难治性强直性脊柱炎活动期炎症的发生,可以作为难治性强直性脊柱炎活动期AS的实验室指标及疾病转归指标,也可以作为监测肿瘤坏死因子-α蛋白拮抗剂用于强直性脊柱炎活动期临床疗效的观察指标.     

中医药对类风湿关节炎TNF-α,IL-6影响的研究进展

随着分子生物学技术、免疫学技术与中医药的相互借鉴、融合,医家会将更多的实验动物模型及检测方法用于RA的研究中,其中以TNF-α、IL-6为切入点进行了大量的实验研究,成果显著。中医药对RA TNF-α,IL-6影响的研究将会越来越深入。     

琴叶榕根提取物对α-葡萄糖苷酶、α-淀粉酶的抑制作用

目的:研究琴叶榕根2种提取物对α-葡萄糖苷酶和α-淀粉酶活性的抑制作用。方法:采用超声辅助提取法制备琴叶榕根乙醇提取物,回流提取法制备琴叶榕根水提取物。以pNPG (对-硝基苯基-α-D-吡喃葡萄糖苷)和可溶性淀粉为底物分别测定琴叶榕根提取物对α-葡萄糖苷酶(酵母来源和小鼠小肠来源)和α-淀粉酶活性的影响。结果:琴叶榕根乙醇提取物和水提取物均具有较好的α-葡萄糖苷酶和α-淀粉酶抑制活性,其对酵母菌源α-葡萄糖苷酶的半数抑制浓度(IC50值)分别为:(128.13±3.28)、(1923.45±3.24)μg/mL;对小鼠小肠源α-葡萄糖苷酶的半数抑制浓度(IC50值)分别为:(531.04±5.72)、(2232.27±5.76)μg/mL;对α-淀粉酶的半数抑制浓度(IC50值)分别为:(714.25±4.37)、(1141.28±1.23)μg/mL。结论:琴叶榕根乙醇提取物抑制α-葡萄糖苷酶活性和α-淀粉酶均强于水提取物,有作为新型α-葡萄糖苷酶抑制剂开发价值。     

丹酚酸对房颤大鼠TNF-α,LTCCα1c蛋白表达影响随机平行对照研究

[目的]探讨丹酚酸对房颤大鼠心房肌细胞L型钙通道a1c亚单位(CaLα1c)蛋白表达和肿瘤坏死因子(TNF-ā)影响。[方法]使用随机平行对照方法,将40只清洁级SD大鼠随机取出10只作为空白对照组。其余30只使用乙酞胆碱—氯化钙(Ach-Cacl2)混合液尾静脉注射法复制房颤模型。连续给药4周,心电图有典型房颤改变视为造模房成功。将造模成功的24只(由于部分大鼠在造模中死亡)按区组随机方法随机分为模型组、维拉帕米组、丹酚酸组,8只/组,空白对照组也随机减去2只。维拉帕米干预组给予维拉帕米20mg/kg.d灌胃;丹酚酸治疗组给予注射用丹参多酚酸4mg/kg.d灌胃;模型组及空白对照组用等量蒸溜水灌胃。1次/d,连续4周,自由饮水,给予固定饲料。[结果]模型组CaLa1c蛋白表达水平减低,TNF-α增高;丹酚酸治疗组、维拉帕米干预组均明显改善了房颤大鼠心房组织CaLa1c蛋白表达水平减低状态,降低了外周血TNF-α(P<0.05)。[结论]丹酚酸可能通过改善房颤大鼠心房组织CaLa1c蛋白表达水平的减低和TNF-α增高状态,从而达到治疗AF的作用。     

趋化因子MCP-1＼MIP-1α的表达与脑缺血关系的研究概况

脑血管疾病是严重危害人类健康的三大疾病之一,其发病率、致残率、病死率一直居高不下,脑缺血占脑血管疾病的80％[1]。脑缺血属于中医学“中风”范畴,其病因病机为虚、火、风、痰、气、瘀,以益气祛瘀生新为治法,中医药对于脑缺血后卒中疗效显著[2]。     

高效液相色谱法测定七个不同产地椒目中α-亚麻酸的含量

目的:测定七个不同产地椒目中α-亚麻酸的含量。方法:用固定相为C18柱(4.6mm×200mm,5μm);流动相为乙腈:1%醋酸溶液(90:10);检测波长为205nm;流速为1.0mL/min;柱温25℃;进样量20μL。结果:α-亚麻酸含量从高至低分别为:陕西韩城、四川、丹凤、山东、宝鸡、富平、临潼。结论:陕西韩城及四川省的椒目药材质量最高。     

聚乙二醇化干扰素α-2α治疗HBeAg阳性慢性乙型肝炎40例临床疗效观察

目的 考察聚乙二醇干扰素α-2α(派罗欣)对HBeAg阳性慢性乙型肝炎患者的疗效.方法 符合要求的慢性乙型肝炎患者40例,所有患者均使用派罗欣180ug皮下注射,1次/周,连续48周,治疗期间不使用其它抗病毒药物.选取肝功能、乙型肝炎病毒标志物、HBV DNA作为检测指标.结果 治疗48周后,ALT/AST复常率72.5%(29/40),HBsAg血清转换率12.5%(5/40),HBeAg血清转换率45%(18/40),HBV DNA转阴率65%(26/40).结论 派罗欣治疗慢性乙型肝炎能获得HBsAg血清转换,且安全性好.     

桑白皮中α-葡萄糖苷酶抑制和抗氧化活性成分研究

目的：研究桑白皮（Morus alba）的化学成分及其α-葡萄糖苷酶抑制和DPPH自由基清除活性方法：采用硅胶、凝胶柱色谱和制备HPLC等方法进行分离纯化，通过高分辨质谱和核磁鉴定化合物结构结果：从桑白皮提取物中分离得到了13个化合物，其中化合物1，3和8表现出显著的α-葡萄糖苷酶抑制活性，IC50值分别为147.1 ± 1.1，314.1 ± 0.8和207.6 ± 0.1 µM，均低于阳性对照阿卡波糖（418.6 ± 0.1 µM）。化合物10和11均表现出良好的DPPH自由基清除活性，EC50值分别为2.9 ± 0.1和5.0 ± 0.1 µM，均低于阳性对照维生素C的EC50值（54.8 ± 0.1 µM)结论：化合物1、3和8的α-葡萄糖苷酶抑制活性为首次测定。     

Acupuncture at Kŏngzuì (孔最LU 6) for 76 cases of hemorrhoids

Objective

To observe the effect of acupuncture at K?ngzuì (孔最LU 6) for hemorrhoids.

Chemical Constituents from Endophytic Fungus Plectosphaerella cucumerina YCTA2Z1 of Cynanchum auriculatum

Objective: To study the chemical constituents from the Et OAc extract of endophytic fungal Plectosphaerella cucumerina YCTA2 Z1.Methods: The chemical constituents were isolated and purified by silica gel column,Sephadex LH-20,and reverse-phase C-18 column chromatography as well as crystallization.Results: Thirteen compounds were isolated from the EtOAc extract of the fungal strain YCTA2 Z1.Their chemical structures were elucidated according to the spectral evidence.They were identified as caudatin(1),baishouwubenzophenone(2),cynandione B(3),asterbatanoside A(4),p-hydroxyphenethyl-O-β-D-glycoside(5),caffeic acid(6),ferulic acid(7),2,5-dihydroxyacetophenone(8),protocatechuic acid(9),vanillic acid(10),stearic acid(11),azelaic acid(12),and succinic acid(13).Conclusions: It is the first chemical study on endophytic fungi from Cynanchum auriculatum and all the compounds are obtained from the species,the genus,as well as the family Plectosphaerellaceae for the first time.     

Metabolite Characterization of Penta-O-galloyl-??￠-D-glucose in Rat Biofluids by HPLC/QT of MS

Objective: To understand the in vivo metabolic fate of 1,2,3,4,6-Penta-O-galloyl-β-d-glucose(PGG)naturally existed in many medicinal herbs and food plants such as Rhus chinensis,Paeonia suffruticosa,Paeonia lactiflora and Mango.Methods: The metabolites of PGG in rat biofluids were characterized using high performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry(HPLC-QTOF-MS).Results: Ten metabolites in urine,five metabolites in feces and two metabolites in plasma,were observed when the rats were administrated with a single intravenous injection of PGG(20 mg/kg).Conclusion: PGG is firstly metabolized to gallic acid,then gallic acid undergoes sulfation,glucuronidation and methylation by rat liver.The determination of metabolites and the proposed metabolic pathway of PGG in vivo will be benefit to gain deeper insights into its pharmacological activities.     

Chemical Constituents from Kalanchoe hybrida and their Cytotoxicity

Objective:Kalanchoe hybrida(Crassulaceae)is naturalized throughout all the island of Taiwan in China.The preliminary bioassay-guided fractionation of the crude extract of K.hybrida exhibited that the chloroform and n-butanol fractions possessed potent cytotoxicity against MCF-7,NCI-H460,and SF-268 tumor cell lines at 50μg/m L concentration.Therefore,K.hybrida was selected as a target and the chemical constituents from the chloroform and n-butanol fractions of the crude extracts of K.hybrida were identified.The potential constituents were examined for their cytotoxicity against the tumor cell lines.Methods:A combination of conventional chromatographic techniques was performed on the crude extract of K.hybrida.The chemical structures of the purified constituents were identified on the basis of spectroscopic and spectrometric analysis.Results:The purification results had led to the characterization of totally 37 compounds.The isolated compounds 1,2,and 4–12 were examined for their cytotoxicity in vitro,and bufadienolides 4–8 and flavonol glycoside 11 displayed significant cytotoxicity towards all the tested tumor cell lines among these tested compounds.Conclusion:The results indicated that these principles should be responsible for the bioactivity of corresponding partial fractions.The potential constituents could be further investigated to explore the new natural lead drugs.     

药代动力学和核磁共振代谢组学方法评价小檗碱和黄连对脓毒症的治疗效果

目的：脓毒症是由感染引起的系统性炎症反应，经常会导致器官功能障碍。尽管其死亡率和发病率很高，但其病理生理学仍然知之甚少。黄连及其主要活性成分小檗碱（生物碱类化合物）已经在临床上用作抗菌和抗炎药物。本研究的目的是为了研究小檗碱和黄连在大鼠体内的吸收与分布，以及对脓毒症的治疗效果。 方法：对黄连及其主要活性成分小檗碱进行药代动力学和代谢组学研究。 结果：盲肠结扎穿孔诱导的脓毒症大鼠的能量代谢和氨基酸代谢明显被扰乱，而黄连和小檗碱治疗之后能让代谢物的扰乱向正常大鼠回归。 结论：小檗碱与黄连在脓毒症的治疗上，具有相当甚至更好的药效。     

生物黏附辅料对葛根总黄酮类化合物在Caco-2细胞模型中转运的影响

目的:葛根总黄酮（PTF）可治疗心脑血管疾病，但膜通透性差，口服生物利用度低。一些辅料如卡波姆、壳聚糖和羟丙基甲基纤维素可以提高口服生物利用度。传统的体外评价技术，包括大鼠肠灌流和细胞模型，不能评价PTF整体的吸收机制。方法:本研究评价辅料的黏附性及对PTF在Caco-2细胞单层模型中转运的影响。采用cDNA微阵列测定PTF和PTF+辅料给药后的Caco-2细胞的基因表达变化，从基因水平揭示辅料对PTF整体吸收的影响机制。结果:体外黏附和Caco-2细胞转运实验表明，与单独PTF相比，加入辅料后对胃黏膜具有更高的黏附性，且在Caco-2细胞模型中的转运效率更高。PTF与辅料的相互作用显著改变了某些基因的表达，可能影响PTF的吸收效率。结论:不同的生物黏附聚合物能提高PTF的肠道吸收，可能与ATP结合盒(ABC)和溶质载体转运体(SLC)的表达基因有关。     

文冠果种仁粕中的一个新香豆素

Objective: To study the coumarin from the seeds oil leavings of Xanthoceras sorbifolia.Methods: The chemical constituents were isolated and purified by combination of silica gel, macroporous resin, Sephadex LH-20, and ODS column chromatography. Their structures were elucidated by spectral and chemical methods. The cytotoxicity of the new compound against 10 selected human cancer cell lines was assayed.Results: Five comarins were isolated and identified as fraxetin-7-O-β-D-[6'-(3"–hydroxyl–3"-methylglutaryl)] glucopyranoside(1), fraxoside(2), fraxetin(3), scopoline(4), and esculetin(5), respectively.Conclusion: Compound 1 is a new compound. Unfortunately, this compound exhibited no cytotoxicity with tested cell lines.     

佛手柑内酯在MDCK-MDR1细胞中所介导的调节长春新碱转运的机制

目的：研究白芷中佛手柑内酯对长春新碱转运的影响及其可能机制。方法用表观通透性系数（Papp）测定长春新碱经MDCK-MDR1细胞膜的转运，以观察佛手柑内酯对长春新碱转运的影响。采用分子对接预测佛手柑内酯与P-糖蛋白（P-gp）的结合力。通过罗丹明123（Rho123）的蓄积和活性分析，确定了佛手柑内酯对P-gp功能和P-gp ATP酶活性的影响。以1,6-二苯基-1,3- 5-己三烯（DPH）为研究对象，研究了佛手柑内酯对膜流动性的影响，并用Western blot和实时定量pcr 方法：分析了佛手柑内酯对P-gp蛋白和mRNA表达的影响。这些实验阐明了佛手柑内酯对长春新碱的转运的影响，并允许探索佛手柑内酯作用的可能机制。 结果：佛手柑内酯能抑制长春新碱在MDCK-MDR1细胞中的转运，而佛手柑内酯和P-gp之间的结合力较弱。佛手柑内酯能降低Rho123在MDCK-MDR1细胞中的蓄积，增加膜流动性，上调P-gp蛋白和mRNA的表达，但对P-gp ATP酶活性无影响。 结论：佛手柑内酯抑制长春新碱转运的可能机制与佛手柑内酯介导的P-gp蛋白上调、mRNA表达、膜流动性和P-gp酶活性有关。     

JAK2/STAT3信号通路介导灯盏花乙素抗人心脏微血管内皮细胞缺氧-复氧损伤

Objective: To investigate the antagonistic cell injury effect and molecular mechanism of scutellarin(SCU)in hypoxia reoxygenation(HR) treated human cardiac microvascular endothelial cells(HCMECs).Methods: The method of 12 h hypoxia following by 12 h reoxygenation was used to culture HCMECs in vitro to built cell injury model. The groups were divided into control group, model(HR) group, and HR + SCU(0.1 μmol/L, 1 μmol/L, and 10 μmol/L) group. The cell viability was determined by MTT, and oxidative stress was detected by malondialdehyde(MDA) levels by biochemical assay kit. Protein expression of JAK2/p-JAK2 and STAT3/p-STAT3 were evaluated by Western blot.Results: The results of MTT and MDA showed that HR decreased the cell viability(P 0.05) and increased MDA level significantly(P 0.05), SCU played a contrary role in these processes. Western blot analysis indicates that, the expression of JAK2 and p-JAK2, STAT3, and p-STAT3 were increased in model group when compared with control group(P 0.05); Compared with model group, their expression were reduced by SCU(P 0.05).Conclusion: SCU took a protective effect on HR-treated HCMECs, and the molecular mechanism may be associated with the inhibition of JAK2/STAT3 signal transduction pathway.