用大肠杆菌CM89菌株对三种化学物抗突变作用的研究

本文以 E.coli CM891为靶细胞,用细菌内抗突变作用模式研究了肉桂醛,鞣酸,二烯丙三硫的抗4NQO 突变性及其作用机制。含质粒 pKM101的 CM891的高抗株(抗50μg/ml 氨苄青霉素)能提高该菌株的自发突变率和4NQO 诱发的突变率以及对鞣酸的杀伤抗性。肉桂醛的抗突变性不依赖质粒 pKM101效应,但与暂时性生长延搁有关。鞣酸及二烯丙三硫的抗突变机制可能包括质粒 pKM101介导的易误修复。上述三种化学物中每二种联合应用均显示抗4NQO 突变性的协同效应及对靶细胞的毒性杀伤作用。     

肉桂及其混伪品的HSGC-MS的实验比较研究

目的 比较肉桂及其混伪品的顶空气相指纹图谱，以此鉴别肉桂药材的真伪。方法 采用顶空气相色谱-质谱（HSGC-MS）计算机隧和技术，分别测定肉桂，桂皮，柴桂的指纹图谱并加以比较。结果 肉桂的顶空气相指纹图谱与混伪品桂皮，柴桂有明显区别，其指纹特征峰位于10.60,15.60min处，主要成分为桂皮醛。结论 此方法能有效地鉴别肉桂及其混伪品，具有快速，准确，操作简单，不需对样品进行提取分离，可直接进行测定的特点。     

肉桂醛咳嗽激发试验方法的建立及评价

目的 探讨肉桂醛咳嗽激发试验的方法.方法 采用吸气触发的定量吸入,对35名健康志愿者及25例咳嗽患者行肉桂醛咳嗽激发试验.受试者初步吸入雾化浓度倍增（50,100,200,400,800 mmol/L）的肉桂醛溶液,记录测试期间咳嗽次数.诱发产生≥2和≥5次咳嗽的浓度（C2,C5）,用比对数值lg C2和lg C5来判断咳嗽反应的敏感性,并测定受试者前、后肺功能.结果 所有受试者中仅1名出现轻微不适,有恶心感.两组受试者咳嗽激发前、后肺通气指标FEV1、FVC、FEV1/FVC,{[（3.35±0.53） L,（3.35±0.52）L],[（2.76±0.82） L,（2.71±0.73）L]},{[（3.72±0.70） L,（3.71±0.71）L],[（3.30±0.78） L,（3.29±0.76）L]},{[（90.6±5.42）％,（90.9±4.92）％],[（83.6±4.45）％,（82.4＋5.04）％]},差异无统计学意义（P值均＞0.05）.咳嗽敏感性lg C2和lg C5值分别为[2.48±0.43,2.72±0.35].结合本实验实际吸入浓度,估计肉桂醛咳嗽敏感性正常参考值C2≥200 mmol/L,C5≥400 mmol/L.咳嗽敏感性lg C2和lg C5与性别差异有统计学意义（P＜0.05）.结论定量吸入肉桂醛咳嗽激发试验,对正常咳嗽敏感性的建立有参考意义.     

Beneficial Antioxidative and Antiperoxidative Effect of Cinnamaldehyde Protect Streptozotocin-Induced Pancreatic β-Cells Damage in Wistar Rats

The present study was aimed to evaluate the antioxidant defense system of cinnamaldehyde in normal, diabetic rats and its possible protection of pancreatic β-cells against its gradual loss under diabetic conditions. In vitro free radical scavenging effect of cinnamaldehyde was determined using DPPH (1,1-diphenyl-2-dipicrylhydrazyl), superoxide radical, and nitric oxide radical. Streptozotocin (STZ) diabetic rats were orally administered with cinnamaldehyde at concentrations of 5, 10 and 20 mg/kg body weight for 45 days. At the end of the experiment, the levels of plasma lipid peroxides and antioxidants such as vitamin C, vitamin E, ceruloplasmin, catalase, superoxide dismutase, reduced glutathione and glutathione peroxidase were determined. A significant increase in the levels of plasma glucose, vitamin E, ceruloplasmin, and lipid peroxides and significant decrease in the levels of plasma insulin and reduced glutathione were observed in the diabetic rats. Also the activities of pancreatic antioxidant enzymes were altered in the STZ-induced diabetic rats. The altered enzyme activities were reverted to near-normal levels after treatment with cinnamaldehyde and glibenclamide. Histopathological studies also revealed a protective effect of cinnamaldehyde on pancreatic β-cells. Cinnamaldehyde enhances the antioxidant defense against reactive oxygen species produced under hyperglycemic conditions and thus protects pancreatic β-cells against their loss and exhibits antidiabetic properties.     

RP-HPLC测定不同产地肉桂中桂皮醛和肉桂酸的含量

目的：建立不同产地肉桂中有效成分桂皮醛和肉桂酸的含量测定方法。方法：采用高效液相色谱法，测定了16个产地肉桂中桂皮醛和肉桂酸的含量。色谱柱：迪马公司Diamonsil^TM（钻石）C18柱（250mm×4．6mm，5μm）；检测波长：285nm；温度：20℃；流动相：乙腈-0．3％磷酸水溶液（35：65）；流速：1mL·min^-1。结果：建立了同时测定肉桂中桂皮醛和肉桂酸的高效液相色谱法，产自越南的肉桂中桂皮醛和肉桂酸的含量明显高于其他产地。结论：本法简便、快速、准确，适用于肉桂中桂皮醛和肉桂酸的含量测定。     

反相高效液相色谱法测定消瘤胶囊中桂皮醛及桂皮酸的含量

目的 :测定消瘤胶囊中桂皮醛和桂皮酸的含量。方法 :反相高效液相色谱 (RP- HPLC)法 ,乙腈∶ 0 .1 %磷酸溶液 (32∶ 78)为流动相 ,Luna C1 8柱为固定相 ,流速 1 .0 ml· min-1 ,检测波长 2 85 nm。结果 :桂皮醛在 2 .63～ 2 6.3μg/ ml,桂皮酸在 0 .736～ 7.36μg/ ml,呈现出良好的线性关系 ,相关系数分别为 0 .9996,0 .9999。加样回收率桂皮醛为 98.4% ,桂皮酸为 98.7%。仪器精密度为 1 .3% ,方法精密度为 2 .2 %。结论 :方法快速简便 ,重现性好     

3D QSAR studies on cinnamaldehyde analogues as farnesyl protein transferase inhibitors

Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies on 59 cinnamaldehyde analogues as Farnesyl Protein Transferase (FPTase) inhibitors were investigated using comparative molecular field analysis (CoMFA) with the PLS region-focusing method. Forty-nine training set inhibitors were used for CoMFA with two different grid spacings, 2A and 1A. Ten compounds, which were not used in model generation, were used to validate the CoMFA models. After the PLS analysis, the best predictive CoMFA model showed that the cross-validated value (r2cv) and the non-cross validated conventional value (r2ncv) are 0.557 and 0.950, respectively. From the CoMFA contour maps, the steric and electrostatic properties of cinnamaldehyde analogues can be identified and verified.     

HPLC法测定加味苓桂术甘汤中桂皮醛的含量

目的建立测定加味苓桂术甘汤中桂皮醛含量的HPLC方法。方法采用Diamonsil C18柱(5μm,4.6mm×150mm),流动相为甲醇-0.03mol·L-1醋酸铵(50∶50),在290nm波长处检测,流速0.8mL·min-1,柱温40℃。结果桂皮醛在0.523～2.61μg·mL-1范围内呈良好的线性关系,r=0.9998;平均加样回收率为98.6%,RSD=0.95%(n=6)。测得加味苓桂术甘汤中桂皮醛的含量为8.10μg·mL-1。结论该方法灵敏、准确、重现性好,适用于测定加味苓桂术甘汤中桂皮醛的含量。     

Transient receptor potential A1 (TRPA1) activity in the human urethra--evidence for a functional role for TRPA1 in the outflow region

Background

A role for the transient receptor potential (TRP) A1 ion channel in rat lower urinary tract (LUT) sensation and disease has been proposed, but in the human LUT no information on TRPA1 activity is available.

Objectives

To investigate the distribution of TRPA1 in the human urethra and to study the effect of TRPA1 agonists on isolated urethral strip preparations.

Design, settings, and participants

Urethral specimens were obtained preoperatively from 10 patients and were freshly prepared for Western blot, immunohistochemistry, and functional in vitro investigations.

Measurements

The expression patterns of TRPA1 were studied with Western blot and immunohistochemistry. The effects of allyl isothiocyanate (AI), cinnamaldehyde (CA), and NaHS (donor of H₂S) on tension of urethral strips were investigated in tissue baths.

Results and limitations

TRPA1 immunoreactivity (-IR) was found in nerve fibres in the suburothelial space and was also located to nerve fibres of the muscle layer. Single TRPA1-IR nerves extended into the urothelium. A majority, but not all TRPA1-IR nerves also expressed immunoreactivity for CGRP or TRPV1. In the urothelium, TRPV1 was located to the outer layers whereas TRPA1 was observed in basal urothelial cells. Interspersed between strands of smooth muscle cells of the urethral wall, TRPA1- and vimentin-IR cells containing central nuclei and slender cytoplasmatic extensions were observed.In functional experiments, TRPA1-agonists had no contractile effect in urethral preparations. After precontraction with phenylephrine, AI, CA, and NaHS caused concentration-dependent relaxations of urethral strip preparations.

Conclusions

The localization of TRPA1 to nerves that also express TRPV1 and CGRP, and in urothelial cells and interstitial cells, as well as the findings that TRPA1 agonists can modify tone of urethral preparations, propose a role for TRPA1 in afferent and efferent sensory signaling of the human outflow region.