N,N′-亚烷基双(取代苯酚)氨基乙酸的合成及对放射性核素钍-234的促排效果

本文报道合成的16个N,N′-亚烷基双(取代苯酚)氨基乙酸除化合物3,4外对放射性钍-234的加速排出均有较好的效果。其中有二个化合物促排效果达到70%以上,根据动物实验结果初步探讨了构效关系。     

黄花远志根中两个新■酮化合物的结构鉴定

从黄花远志（ＰｏｌｙｇａｌａａｒｉｌａｔａＢｕｃｈＨａｍ．）根中分离得到两个新的酮化合物，根据理化性质和光谱（ＵＶ，ＩＲ，ＭＳ，１ＨＮＭＲ，ＤＩＦＮＯＥ和１３ＣＮＭＲ）分析，分别鉴定为１，３二羟基２甲氧基酮（Ｉ）和７羟基１甲氧基２，３亚甲二氧基酮（Ｉ）。药理试验表明Ｉ，Ｉ均具有抑制醛糖酶的作用。     

海藻提取物对实验性高脂大鼠模型的药效学研究

目的：观察海藻提取物对实验性高脂血症大鼠模型的降脂和抗氧化作用。方法：取６０只雄性ＳＤ大鼠，分６组，除对照组外，无喂高脂饲料。给药组同时还以灌胃给药，第１７天取血，测定各组血清中的ＴＣ，ＴＧ，ＨＤＬ，ＭＤＡ和ＳＯＤ。结果：实验结果表明，与高脂模型组比较，海藻提取物组的ＴＣ，ＴＧ和ＭＤＡ水平降低，而ＨＤＬ和ＳＯＤ的水平增高，且有显著差异。     

高效薄层荧光光密度法测定生物样品中的小檗碱含量

建立了高效薄层荧光光密度法测定生物样品中小檗碱的含量,并比较了口服小檗碱(100mg/kg)及含等量小檗碱的黄连粉(2 g/kg)后的血药浓度、降血糖效应和组织分布。     

程序升温毛细管气相色谱的精油成分保留指数研究

本文采用线性程序升温毛细管气相色谱法对200多种天然存在和人工合成的挥发油、香精成分,分别在极性柱(DB-WAX)和非极性柱(DB-1)上进行了Kovats保留指数的测定。归纳了部分化合物的保留指数规律;考察了气体平均线速,程序初温及升温速率对保留指数的影响。并结合我们所开发的色谱数据库管理系统进行了香精的定性分析。     

Bioactivity of compounds isolated from the leaves of the Lantana camara Linn plant

Two compounds with different bioactivitieswere isolated from the leaves of the Lantana camara Linn plant. Compound 1wastriterpenoid (Lantadene B)(22β-dimethylacroyloxy-3-oxoolean-12-en-28-oic-acid, C₃₅H₅₂O₅), which was isolatedfrom n-hexane fraction and obtained as white solid (amorphous). Compound 2was glycosideflavonoid (5-hydroxy-6,4′-dimethoxyflavon-7-O-glucopyranose, C₂₃H₂₄O₁₁), which was isolated from ethyl acetate and obtained as pale yellow solid (amorphous). Extraction was performed withmaceration method using methanol solvent. Subsequently, fractionation was carried out using n-hexane and ethyl acetate solvents. Isolation and purification of both fractions were conductedusing chromatography method. The structure of the isolated compounds was determined throughspectralanalyses of ultraviolet (UV), infrared (IR), and nuclear magnetic resonance (¹H NMR and ¹³C NMR), distortionless enhancement by polarization transfer (DEPT), heteronuclear multiple bond connectivity (HMBC), heteronuclear single quantum correlation (HSQC), and H-H COSY (¹H-¹H homonuclear correlatedspectroscopy). The cytotoxic activity of compound 1 was tested against MCF-7 breast cancer cellsin vitro using MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide), showing very strong cytotoxic activity in inhibiting the growth of MCF-7 breast cancer cells, and the IC₅₀ value was 1.1336 µM. The antioxidant activity of compound 2 was tested using DPPH assay (1,1-diphenyl-2-picrylhydrazyl), showing strong activity in inhibiting free radicals, and its IC₅₀ value was 71.03 mg/L.     

Screening by anti-endomysium antibodies for celiac disease in Tunisian children with type 1 diabetes mellitus

AIM: Celiac disease (CD) and type 1 diabetes mellitus (DM1) can frequently coexist, presumably due to a common genetic predisposition. The present study was designed to evaluate the frequency of CD among Tunisian children with DM1.PATIENTS AND METHODS: A total of 205 diabetic children (92 girls, 113 boys, age range 6 months-15 years, median 11 years) were screened for CD by determination of IgA anti-endomysium antibodies (EMA).RESULTS: EMA were positive in 17 out of 205 (8.3%) children with DM1. The median age of DM1 at onset was significantly lower in patients with EMA than those without EMA (P<10(-7)). In 13 of 17 EMA-positive patients, duodenal biopsy could be performed and a destructive type of CD was confirmed in 11 of them: 8 patients showed total villous atrophy, 3 patients showed a partial villous atrophy. The other two patients showed a normal histological picture with normal number of intraepithelial lymphocytes. Parents of the remaining EMA-positive children refused endoscopy. Thus the prevalence of biopsy-proven CD was 5.3% (11/205). It was 7.6% (7/92) in girls and 3.5% (4/113) in boys but the difference was not statistically significant. Seventy three percent of patients with CD were asymptomatic.CONCLUSIONS: The prevalence of clinically unrecognized CD, found by EMA screening, is high in Tunisian children with DM1. We suggest that children with diabetes should be screened for CD.     

中药桔丙酯联合降糖治疗对2型糖尿病患者甲襞微循环及血液流变学的影响

目的观察中药桔丙酯注射液联合降糖治疗对2型糖尿病甲襞微循环及血液流变学的影响,探讨其治疗机制.方法于2005-10/2006-08选择河北北方学院附属校医院、张家口市第一人民医院门诊及住院收治的2型糖尿病患者48例,为治疗组.应用注射用桔丙酯治疗,桔丙酯180 mg,次,1次,d,连用2周;健康志愿者30例为对照组.采用微循环显微镜,于治疗前后常规检查左手第4指甲襞第一排管袢,按田牛加权积分法对16项指标综合定量分析,判断疗效和甲襞微循环的变化.同时观察2型糖尿病患者治疗前后血液流变学各项指标的变化.结果①治疗组治疗前甲襞微循环及血液流变学各项指标均表现为不同程度的异常,治疗后甲襞微循环及血液流变学各项指标明显改善.甲襞微循环由治疗前的中、重度异常恢复到大致正常,治疗后总积分值低于治疗前(分别为1.52±0.69,4.52±0.82,t=3.96,P＜0.05).②血液流变学指标变化表明,血浆黏度、全血黏度、纤维蛋白原及红细胞电泳等各指标经桔丙酯治疗后均明显降低(P＜0 05).结论中药桔丙酯联合降糖治疗能够明显改善2型糖尿病患者血流变异常及微循环障碍.     

人成釉蛋白C端肽的大量表达及纯化

目的:获得高纯度的重组人成釉蛋白C端肽。方法:实验于2001-01/2004-06在解放军第四军医大学口腔内科实验室解放军第四军医大学基础部生物化学与分子生物学实验室完成。①转化pRSET-A/成釉蛋白原核表达质粒入BL21(DE3)细菌进行大量培养,加入诱导剂IPTG至终浓度为0.1mmol/L,32℃继续振荡诱导培养5h,收集细菌,诱导菌体的裂解上清经金属螯合亲和层析,洗脱Ni-NTA结合蛋白,收集洗脱蛋白,聚丙烯酰胺凝胶电泳法鉴定。②离子交换层析缓冲液(pH 7.4,50 mmol/L Tris·Cl)平衡Q SapharoseHP层析柱,将初步纯化的蛋白样品加在Q Sapharose HP凝胶介质上,梯度洗脱结合的蛋白,收集洗脱峰,制样,聚丙烯酰胺凝胶电泳法鉴定洗脱蛋白。结果:①表达重组人成釉蛋白C端肽的金属螯合亲和层析结果:诱导菌体的裂解上清经金属螯合亲和层析,洗脱下Ni-NTA结合蛋白,经聚丙烯酰胺凝胶电泳法电泳证实获得初步纯化的重组人成釉蛋白C端肽,其中仍含一些杂蛋白。②重组人成釉蛋白C端肽的离子交换层析结果:获得多个蛋白洗脱峰,聚丙烯酰胺凝胶电泳法证实获得纯化的重组人成釉蛋白C端肽。结论:获得了纯化的人成釉蛋白重组蛋白。