姜黄素调控NF-κB信号通路对糖尿病模型大鼠胰岛细胞形态和功能的影响

目的 探讨姜黄素通过核因子-κB（NF-κB）信号通路对高糖高脂饮食诱导的糖尿病模型大鼠胰岛细胞形态和功能的影响。方法 采用高糖高脂饲料＋ip链脲佐菌素法制备糖尿病大鼠模型,将模型成功 SD大鼠随机分为5组：模型组、二甲双胍（200 mg·kg^-1,阳性药）组和姜黄素低、中、高剂量（50、150、250 mg·kg^-1）组,对照组不造模。ig给药,每天1次,连续6周,对照组同时注射等量无菌磷酸盐缓冲液（PBS）。观察SD大鼠体质量变化;血糖仪检测空腹血糖;ELISA法检测血清C肽水平;生化分析仪检测血清中糖化血红蛋白、三酰甘油（TG）、总胆固醇（TC）、低密度脂蛋白胆固醇（LDL-C）、高密度脂蛋白胆固醇（HDL-C）、丙氨酸氨基转移酶（ALT）、天冬氨酸氨基转移酶（AST）、总胆红素（TBil）、血肌酐（Scr）、血尿素氮（BUN）、尿酸（UA）水平;取胰腺进行 HE 染色,于光镜下观察胰岛形态学改变;免疫组化染色法观察胰岛 NF-κB 的阳性表达;Western blotting法检测NF-κB信号通路相关蛋白表达;提取胰岛细胞,免疫荧光染色观察胰岛素分泌,葡萄糖刺激的胰岛素分泌（GSIS）实验检测胰岛素分泌量。结果 与模型组比较,各给药组体质量在治疗第2周时开始缓慢增长,第3、4周体质量显著升高（P＜0.05）;血糖水平显著降低（P＜0.05）,血清 C 肽水平显著升高（P＜0.05）;糖化血红蛋白、TG、TC、LDL-C、ALT、AST、Scr、BUN、UA水平显著降低（P＜0.05）,HDL-C水平显著升高（P＜0.05）;胰岛大小和形态逐渐恢复正常,胰岛细胞依次变得更清晰完整,导管系统内的囊性扩张也逐渐减少;NF-κB阳性细胞减少;p-P65蛋白表达显著降低（P＜0.05）,p-IκBα蛋白表达显著升高（P＜0.05）;胰岛原代细胞分泌胰岛素显著增加（P＜0.05）。结论 姜黄素可以保护糖尿病大鼠胰岛细胞正常形态,维持胰岛细胞功能,减轻糖尿病大鼠症状,其机制可能与调控NF-κB信号通路有关。     

参葛定渴片对2型糖尿病大鼠糖代谢调节作用的实验研究

目的 考察参葛定渴片对2型糖尿病大鼠糖代谢的调节作用.方法 采用ig高脂高糖脂肪乳加ip小剂量链脲佐菌素(STZ)的方法,建立2型糖尿病大鼠模型.将造模成功的大鼠随机分为模型组、阳性组和参葛定渴片高、中、低剂量组.实验各组均连续给药4周.同时取健康大鼠为对照组,观察各组大鼠行为学指标,检测其血糖、糖耐量、血清胰岛素水平.结果 与对照组比较,模型组体质量下降,血糖值显著升高、糖耐量能力降低以及血清胰岛素水平升高.与模型组比较,阳性组和参葛定渴片高、中剂量组可显著降低糖尿病大鼠的血糖和血清胰岛素水平(P <0.001、0.01),且参葛定渴片高剂量组可改善糖尿病大鼠的糖耐量(P <0.01).结论 参葛定渴片对2型糖尿病大鼠的糖代谢具有调节作用,可改善糖尿病大鼠的胰岛素抵抗状态.     

血糖波动对自发性2型糖尿病GK大鼠肾脏病变的影响

目的 研究血糖波动对糖尿病GK大鼠肾脏病变的影响。方法 5只♂ Wistar大鼠作为正常组,10只♂ GK大鼠按体质量、血糖值随机分为糖尿病组、血糖波动组,每组5只。血糖波动组每日错时腹腔注射葡萄糖及皮下注射胰岛素造成日间血糖波动模型,正常组和糖尿病组每日错时腹腔注射等剂量生理盐水,连续6周。每日观察大鼠一般体征;每周称大鼠体质量;第6周末检测全天9个时间点的血糖值;第3,6周末检测糖化血红蛋白值（glycosylated hemoglobin,GHb）;收集第6周末24 h尿液,生化法检测尿肌酐（urine creatinine,U-CREA）、尿白蛋白总量（total urine albumin,U-ALB）,计算24 h尿蛋白排泄率（urinary protein excretion rate,UAER）;6周末,麻醉处死大鼠,心脏取血,生化法检测血清中血尿素氮（blood urea nitrogen,BUN）,手工法检测血清超氧化物歧化酶（superoxide dismutase,SOD）、丙二醛（malonaldehyde,MDA）及谷胱甘肽过氧化酶（glutathione peroxidase,GSH-Px）;取双肾,称重,计算肾肥大指数,将肾脏置中性甲醛,PAS染色,光镜下观察病理变化。结果 与糖尿病组相比,血糖波动组大鼠GHb、U-CREA、UAER、血清BUN及MDA、肾肥大指数均显著升高（P<0.05）,体质量增长速度、血清SOD及GSH-Px均显著降低（P<0.05）,大鼠肾脏组织形态出现的肾小球损伤及结构改变更加明显。结论 血糖波动会加重糖尿病GK大鼠肾脏病变,其机制可能与升高MDA水平,降低SOD、GSH-Px水平有关。     

金芪降糖片联合胰岛素激活PPAR-α/FGF21信号改善2型糖尿病大鼠胰岛素抵抗

目的 考察金芪降糖片联合胰岛素对2型糖尿病大鼠胰岛素抵抗的改善作用及作用机制。方法 采用高脂饲料喂养联合ip 3次小剂量（35 mg/kg）链脲霉素制备2型糖尿病大鼠模型,选择空腹血糖值>11.1 mmol/L的大鼠进行后续实验。模型大鼠随机分为模型组、金芪降糖片（0.5 g/kg）组、胰岛素（6.5 IU/kg）组和联合给药（金芪降糖片0.5 g/kg+胰岛素6.5 IU/kg）组,另选取10只健康大鼠作为对照组。各组均每天给药1次,连续给药4周,检测大鼠餐后2 h血糖并进行胰岛素耐量试验（ITT）,Elisa方法检测大鼠血清成纤维细胞因子21（FGF21）含量,Western Bloting检测大鼠肝脏PPAR-α表达情况。结果 与对照组比较,模型组餐后血糖明显升高（P<0.01）,胰岛素敏感性、肝脏PPAR-α均显著降低（P<0.01）,血清FGF21升高,但无显著性差异;与模型组比较,联合给药能明显降低2型糖尿病大鼠餐后血糖（P<0.01）,显著增加胰岛素敏感性（P<0.05）,显著升高血清FGF21含量（P<0.01）、增加肝脏PPAR-α表达（P<0.01）,且较两药单用效果更优。结论 金芪降糖片联合胰岛素具有改善2型糖尿病大鼠胰岛素抵抗、增加胰岛素敏感性的作用,其机制可能与协同激活PPAR-α/FGF21信号有关。     

医生糖尿病管理质量的改善对2型糖尿病群体血糖管理水平的影响

目的 观察门诊医生的糖尿病管理质量改善措施对2型糖尿病群体血糖管理水平的影响。方法 纳入2017年1~3月就诊于安徽医科大学第二附属医院内分泌科门诊的前100例使用基础胰岛素的2型糖尿病患者，收集患者的空腹血糖、糖化血红蛋白、血脂、血压、低血糖发生情况、健康量表得分、具体降糖方案和门诊医生对于基础胰岛素的信心等作为基线数据。对门诊医生进行培训并以"PDCA"模式进行6个月的质量改善循环后，再次纳入2017年10~12月就诊的前100例使用基础胰岛素的2型糖尿病患者，比较干预前后上述观察指标的差异。结果 门诊医生经糖尿病管理质量改善后，患者整体空腹血糖、糖化血红蛋白、血脂和收缩压等均较干预前下降，而空腹血糖和糖化血红蛋白的达标率、健康状况满意度较干预前提高，差异有统计学意义（P<0.05）。患者舒张压、体质指数、低血糖发生比例及医生对基础胰岛素的信心方面，干预前、后差异无统计学意义（P>0.05）。结论 医生的糖尿病管理质量改善能够提升医生的临床技能，并进一步改善2型糖尿病患者群体的血糖综合管理质量。     

新型国产重组甘精胰岛素对1型糖尿病模型大鼠的降糖作用研究

目的 探讨新型国产重组甘精胰岛素注射液对1型糖尿病模型大鼠的降糖作用。方法 选择健康SD大鼠和链脲佐菌素诱导的1型糖尿病大鼠,甘精胰岛素注射液（来得时）为阳性对照药,健康SD大鼠单次sc 2、4 IU/kg剂量的重组甘精胰岛素注射液,大鼠尾静脉采血,分别测定0 h（给药前）及给药后1、2、4、6、8 h空腹血糖;1型糖尿病模型大鼠连续5 d sc 4、8 IU/kg剂量的重组甘精胰岛素注射液,每天分别测定给药前（0 h）和给药后（4 h）空腹血糖,给药第1、5天测定给药后1、2、4、6、8 h空腹血糖。结果 健康大鼠sc重组甘精胰岛素注射液2、4 IU/kg后,血糖值在2 h下降到最低,与对照组比较差异显著（P<0.01）;模型大鼠连续5 d sc 4、8 IU/kg重组甘精胰岛素注射液,血糖于给药后4~6 h下降至最低点,与模型组比较差异显著（P<0.01）;每天给药4 h后血糖均呈平稳下降趋势,与模型组比较差异显著（P<0.01）,8 IU/kg血糖值与对照组接近。结论 国产重组甘精胰岛素注射液对1型糖尿病模型大鼠有较好的降糖效果,与同剂量阳性药降糖效果相当。     

甘精胰岛素联合门冬胰岛素治疗2型糖尿病的临床评价

目的 评价甘精胰岛素联合门冬胰岛素治疗对2型糖尿病患者的血糖控制效果。方法 选取上海市长宁区天山中医医院内分泌科2013年1月-2016年1月治疗的2型糖尿病患者150例,随机分为两组（n=75）。其中对照组75例采用精蛋白生物合成人胰岛素注射液联合三餐门冬胰岛素治疗;试验组75例采用甘精胰岛素联合三餐门冬胰岛素治疗,均用药6个月。比较两组治疗前后空腹血糖、餐后2 h血糖和糖化血红蛋白（HbA1c）水平、两组生存质量和不良反应情况。结果 治疗6个月时,对照组和试验组患者的空腹血糖、餐后2 h血糖和HbA1c水平均较同组治疗前降低（P<0.05）,且试验组的空腹血糖和HbA1c水平均低于对照组的（P<0.05）,试验组生存质量明显优于对照组（P<0.05）;治疗3个月时,试验组的HbA1c水平低于对照组的,差异均有统计学意义（P<0.05）。试验组轻微低血糖、夜间低血糖和心脑血管发生率明显低于对照组（P<0.05）。结论 甘精胰岛素联合门冬胰岛素治疗对2型糖尿病患者的血糖控制效果显著,可长时间将血糖稳定在正常水平,患者不良反应发生率低、生存质量高。     

转化生长因子-β1/Smad信号转导途径在大黄酸保护糖尿病大鼠肾脏中的机制探讨

目的 研究大黄酸对高脂饮食诱导的2型糖尿病大鼠肾脏的保护作用。方法 采用高脂饮食联合小剂量链脲佐菌素（STZ）35 mg/kg诱导2型糖尿病大鼠模型,分为模型组,大黄酸低、中、高剂量（50、100、150 mg/kg）组,二甲双胍（300 mg/kg）组,另设正常对照组。分别于0、2、4、8周测定大鼠血糖、尿微量白蛋白;8周末检测大鼠血清肌酐（Cr）、尿素氮（BUN）、总胆固醇（TC）与三酰甘油（TG）水平;HE染色观察肾脏组织病理;蛋白印记法检测大黄酸对糖尿病大鼠肾组织转化生长因子-β₁（TGF-β₁）与Smad3蛋白表达的影响。结果 模型组大鼠血糖及尿微量白蛋白较正常对照组均明显升高,大黄酸各剂量组均能降低糖尿病大鼠血糖及尿微量白蛋白水平,其中,大黄酸高剂量组能显著降低糖尿病大鼠血糖及尿微量白蛋白水平（P<0.05）;与模型组相比,大黄酸各剂量组可降低大鼠血清Cr、BUN、TC与TG值,但是大黄酸高剂量组能显著降低糖尿病大鼠血清Cr、BUN、TC与TG值（P<0.05）;病理学观察显示模型组大鼠肾组织病变较为明显,大黄酸高剂量组肾组织病变明显改善,且糖尿病大鼠肾组织TGF-β₁与Smad3蛋白表达显著下降（P<0.05）。结论 大黄酸对糖尿病肾病有预防作用,其机制可能与改善肾功能、调节血脂及下调肾组织TGF-β₁与Smad3蛋白的表达有关。     

西格列汀联合预混胰岛素治疗脆性糖尿病伴高脂血症疗效和安全性的回顾性研究

目的 探讨西格列汀联合预混胰岛素治疗脆性糖尿病伴高脂血症的疗效和安全性。方法 采用回顾性分析法,收集解放军180医院内分泌科门诊脆性糖尿病伴高脂血症患者158例,其中,单用预混胰岛素治疗的78例为对照组,西格列汀联合预混胰岛素治疗的80例为治疗组,随访时间为36周。比较两组治疗前后糖化血红蛋白（HbAlc）、空腹血糖（FPG）、餐后血糖（PPG）、空腹C肽、餐后2 h C肽,每日血糖谷峰浓度均差（△TP）、血脂水平变化及低血糖发生率。结果 治疗后联合组FPG、PPG、△TP、总胆固醇（TC）、三酰甘油（TG）、低密度脂蛋白（LDL-C）较治疗前均有明显下降（P<0.05,P<0.01）,且均低于对照组（P<0.05,P<0.01）;联合组空腹C肽和餐后2 h C肽较治疗前显著升高（P<0.01）,且均高于对照组（P<0.05）。结论 西格列汀联合预混胰岛素治疗脆性糖尿病伴高脂血症可显著改善患者血糖和血脂水平,且不良反应更少。     

肾移植患者SLCO1B3基因多态性与他克莫司血药浓度相关性研究

目的 探究肾移植患者SLCO1B3基因多态性与术后早期他克莫司血药浓度的相关性。方法 选取昆明市第一人民医院68例肾移植患者为研究对象,运用化学免疫发光法监测他克莫司血药浓度,同时采用聚合酶链反应法检测CYP3A5^*3、SLCO1B3 T334G和G699A基因多态性,并进行基因分型,分析各基因型与他克莫司血药浓度的相关性。结果 CYP3A5^*3不同基因型对术后他克莫司血药浓度和标准化血药浓度有影响,差异具有统计学意义(P＜0.05),SLCO1B3 T334G和G699A基因位点不同基因型对术后他克莫司血药浓度和标准化血药浓度无影响,差异均无统计学意义。结论 与CYP3A5^*3/^*3基因型相比,CYP3A5^*1等位基因携带者达到相同的他克莫司浓度需要增加他克莫司给药剂量。SLCO1B3 T334G和G699A基因多态性对肾移植术后早期他克莫司血药浓度无影响。     

EFFECT OF POLICOSANOL SUCCESSIVE DOSE INCREASES ON PLATELET AGGREGATION IN HEALTHY VOLUNTEERS

Policosanol is a cholesterol-lowering drug with hypocholesterolemic effects demonstrated in experimental models, healthy volunteers and type II hypercholesterolemic patients. In addition, antiplatelet effects of policosanol have been shown in experimental models and healthy volunteers. The effect of successively increasing doses of policosanol on platelet aggregation was investigated in a randomized, placebo-controlled, double-blind study conducted in 37 healthy volunteers. The volunteers were on a placebo-baseline period (two tablets per day) for 7 days and thereafter they received randomly, under double-blind conditions, placebo or policosanol (10mgday⁻¹) for 7 days. After this period dosage was doubled to 20mgday⁻¹for the next 7 days and then again doubled to 40mgday⁻¹, while the control group received placebo tablets all the time. Platelet aggregation as well as coagulation time was measured at baseline and after each dosing step. Results showed that antiplatelet effects of policosanol were successfully enhanced throughout the study, thus suggesting a dose-dependent relationship. No significant effect was reached during the first dosing period, but significant reductions of epinephrine and ADP-induced platelet aggregation were observed after the second one. Finally, a significant inhibition of platelet aggregation induced by all the agonists was observed at the last dosing step. Coagulation time remained unchanged during the trial.     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

鼻渊净胶囊的HPLC指纹图谱研究

目的 建立鼻渊净胶囊的高效液相色谱(HPLC)指纹图谱.方法 采用Agilent SB-C18(4.6 mm×250 mm,5μm)色谱柱,乙腈-水为流动相、以1.0 ml/min流速行梯度洗脱,检测波长210 nm,柱温30℃,洗脱时间为80 min.采用中药色谱指纹图谱相似度评价系统(2004A版)对检测出色谱进行...     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF THE CLASS III ANTIARRHYTHMIC SUBSTANCE / -SOTALOLIN VITRO: REVERSIBLE INHIBITION OF CHOLINESTERASE ISOENZYMES FROM BLOOD AND THE HUMAN CENTRAL NERVOUS SYSTEM

Inhibitory effects of the class III antiarrhythmic compound / -sotalol on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and the human caudate nucleus and on serum cholinesterase (ChE; EC 3.1.1.8) were studiedin vitrousing a spectrophotometric kinetic assay with acetylthiocholine (ASCh) as substrate. Sotalol concentrations in the assays varied from 0.32 to 3.2m . All isoenzymes studied were inhibited by / -sotalol in a reversible and concentration-dependent manner. Double reciprocal plots of the reaction velocity against varying ASCh concentrations revealed that / -sotalol reduced substrate affinity (apparent Michaelis constant, KM, increased) of serum ChE, but did not change the enzyme's maximal rate of ASCh hydrolysis (V_max). Thus, / -sotalol inhibition of serum ChE was of the competitive type (rate constant for reversible competitive inhibition: K_i=0.51m ). In contrast, / sotalol reduced the maximal reaction velocity of the AChE isoenzyme from the central nervous system (caudate nucleus), but had no influence on substrate affinity of the enzyme (K_Mwith ASCh unchanged) indicating purely non-competitive inhibition kinetics (rate constant of reversible non-competitive inhibition: K_i′=0.44m ). / -sotalol inhibition of erythrocyte AChE was of mixed competitive/non-competitive type (K_i=0.31m , K_i′=0.49m ). Non-competitive / -sotalol inhibition of caudate nucleus AChE and the non-competitive component of erythrocyte AChE inhibition cannot be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Peak / -sotalol plasma levels as described in the literature for both humans (15μ ) and experimental animals (dogs: 18μ ; rats: 260μ ) as well as maximal myocardial concentrations of the substance (dogs: 46μ ; rats: 478μ ) are in the range of about 2% to 100% of the sotalol inhibition rate constants determined in the present paper for cholinesterase isoenzymesin vitro. Thus, / -sotalol inhibition of ACh hydrolysisin vivomay contribute to both the well known antiarrhythmic potential and proarrhythmic side effects of the compound.     

喙果黑面神化学成分研究

目的研究大戟科植物喙果黑面神(Breynia rostrata Merr.)的化学成分。方法利用硅胶、凝胶等色谱技术分离纯化化学成分,根据化合物的理化性质和光谱数据进行结构鉴定。结果从喙果黑面神的正丁醇萃取部分分离得到4个化合物,分别鉴定为6-O-甲基丙酰基-α-D-吡喃葡糖(6-O-methylpropanoyl-α-D-glucopyranose,1);4″-苯酚基-6-O-甲基丙酰基-β-D-吡喃葡糖苷(4″-phenolic-6-O-methylpropanoyl-β-D-glucopyranoside,2);1-O-没食子酰基-β-D-吡喃葡糖苷(1-O-galloyl-β-D-glucopyranoside,3);熊果苷(arbutin,4)。结论化合物1和2为新化合物,3和4均为首次从该种植物分离得到。     

EFFECTS OF 2-GUANIDINE-4-METHYLQUINAZOLINE ON GASTRIC ACID SECRETION IN RATS

In this study 2-guanidine-4-methylquinazoline (2-GMQ) appeared to decrease basal and stimulated gastric acid secretion, while structurally related compounds as dimethyl- biguanide, cyanoguanidine and 2-cyanoamino-4-methylpyrymidine did not. Thus, there is an antisecretory effect when the biguanide group is associated with a lipophilic structure. The antisecretive effects exerted by 2-GMQ are associated with anti H₂-histamine activity.The anti H₂-histamine nature of the effects of 2-GMQ was confirmed by the capacity of this compound of depressing the chronotropic activity of the isolated guinea pig auricle increased by histamine, as well as relaxant activity in rat uterus contracted by histamine, since both preparations are rich in H₂-histamine receptors.     

栝楼不同药用部位质量控制的研究进展

瓜蒌子、瓜蒌皮、瓜蒌、天花粉来源于栝楼的不同药用部位,4味药材均为常用的大宗药材,现行版《中国药典》对其制定的质量标准过于简单,无法科学合理地控制其质量。本文对瓜蒌子、瓜蒌皮、瓜蒌、天花粉安全性和有效组分的研究进行综述,明确了相关研究存在的问题并针对问题提出建议,为科学全面的药材及饮片标准的制定提供参考依据。     

AMELIORIATION OF CHEMICALLY-INDUCED HEPATOCYTE INJURY BY CYCLOSPORINE A

Cyclosporine A, beside its current applications, possesses potential hepatoprotective effects. This study was directed to investigate the effect of Cyclosporine A pretreatment on hepatic injury due to carbon tetrachloride (CCl₄) and -galactosamine. Rats were injected by two successive doses of Cyclosporine A (5mgkg⁻¹day⁻¹). Six hours after the second dose, 1mlkg⁻¹of CCl₄was administered i.p. Effects associated with Cyclosporine A pretreatment were examined by using isolated hepatocytes and hepatocytes that were immobilized and continuously perfused. -Galactosamine (5m ) was added directly to the perfusion medium. After isolation, hepatocytes were examined histologically by light and electron microscopy, immobilized and perfused for further metabolic functional activity evaluation. Cyclosporine A pretreatmentin vivoproduced hepatoameliorative effects of various degrees which were statistically significant as manifested by: (1) an increased trypan blue exclusion after CCl₄; (2) an improved ureagenesis after CCl₄; (3) a reduction in the lipid droplets accumulation in the cytoplasm produced by CCl₄administration; (4) well preserved cytoplasmic organelles as mitochondria, endoplasmic reticulum ER, nuclear chromatin structures that were altered by CCl₄; and (5) an increased hepatocytes survival in the agarose gel matrix, reduction of LD leakage and improvement of ureagenesis after -galactosamine addition to the perfusion medium. The beneficial effect of Cyclosporine A pretreatment in modifying hepatotoxicity of chemical insults merits further studies.