抗风湿涂膜剂的体内药物动力学研究

考察抗风湿涂膜剂中辣椒素和乌头类总生物碱在生物体内药动学特征,以获得药动学参数为临床应用提供参考依据.方法为给家兔背部按一定面积涂抹抗风湿涂膜剂后,于不同时间采取血样.分别用高效液相色谱仪和紫外可见分光光度计测定血药质量浓度,通过3P97药动学软件对所得的数据自动拟合获得药动学参数,得辣椒素药动学行为符合一室模型,主要药动学参数为Ka=1.160 013h-1t、1/2(Ka)=0.597 534 h、Ke=0.219 206 2 h-1t、1/2(Ke)=3.162 079 h、AUC=22.084 286(μg/mL)h;乌头类总生物碱药动学行为符合一室模型,主要药动学参数为Ka=0.300 004 9 h-1t、1/2(Ka)=2.310 453 h、Ke=0.185 421t、1/2(Ke)=3.738 234 h、AUC=22.389984(μg/mL).h.药代动力学实验表明,本制剂中辣椒素在动物体内吸收分布速率较快,而代谢消除速率较慢;而乌头类总生物碱吸收与代谢均较慢.二者吸收程度均较好.     

头痛灵贴片质量控制研究

建立头痛灵贴片中组分的鉴别和辣椒素的质量浓度测定方法.采用薄层色谱法鉴别方中白芷、辣椒,采用高效液相色谱法测定方中辣椒素的质量浓度.薄层色谱法专属性强;辣椒素的质量浓度可用相应的测定方法准确测出.本方法操作简便,结果准确,灵敏度高,重复性好,可以控制产品的质量.     

辣椒碱抗病原菌活性及其在番茄酱防腐中的应用

从红辣椒中提取的辣椒碱对金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌这3种常见的病原细菌及黑曲霉、啤酒酵母等7种病原真菌进行拮抗试验。结果表明,辣椒碱具有广谱的抗菌范围和较强的拮抗病原菌的活性,且抗菌活性有明显的量效关系,其中辣椒碱对供试细菌的拮抗作用远大于对供试真菌的作用。将辣椒碱添加到番茄酱中进行防腐试验的结果表明,辣椒碱可有效的抑制微生物的生长,从而延长番茄酱的贮藏期。     

微波辅助提取黄灯笼辣椒中辣椒碱和黄色素的工艺研究

采用微波辅助法从海南栽培的黄灯笼辣椒中提取辣椒碱和黄色素,并分别用HPLC和紫外分光光度计对辣椒碱和黄色素含量进行测定,以正交实验考察辣椒碱和黄色素的最佳提取工艺条件.结果表明,最佳提取工艺为：当m（黄灯笼辣椒）∶V（85％乙醇）=0.4∶50（mg/mL）,提取时间为50 min,提取温度为50 ℃,微波提取功率为700 W,辣椒碱得率可达0.78％;当m（黄灯笼辣椒）∶V（99％乙醇）=1：8（mg/mL）,提取温度55 ℃、提取时间30 min、微波功率600W,黄色素的提取效果最佳.     

大黄素对辣椒素诱导的TRPV1通道电流的抑制作用

本研究通过显微注射技术将TRPV1 cRNA(1ng/nL)注射至非洲爪蟾卵母细胞(20nL/个)体内,放置于G-ORi培养液中,并在(19±1)℃的恒温培养箱内表达.同时利用灌流技术将不同浓度梯度的大黄素、辣椒素按照设计顺序依次灌流进入流动腔,同时控制流速保证非洲爪蟾卵母细胞完全浸没于流动腔内.使用双电极电压钳技术记录0.1,1.0,10.0,50.0μmol/L浓度梯度的大黄素对500nmol/L浓度的辣椒素激活TRPV1电流的影响.得到大黄素作用辣椒素激活TRPV1通道的抑制作用表现出浓度依耐性和电压非依赖性,IC50=38μmol/L,Hill系数n=0.5.结果表明了大黄素对TRPV1位点的相互作用是负协同的,在天然药物里面是一类比较弱的拮抗剂,且大黄素在ORi溶液中开始析出沉淀的浓度在50~60μmol/L之间.我们首次发现了大黄素能够抑制TRPV1通道电流,这可能为开发新的镇痛药物提供理论基础.     

Neuropeptides in pelvic afferent pathways

Summary Neurochemical and pharmacological experiments have raised the possibility that several neuropeptides including, vasoactive intestinal polypeptide (VIP), peptide histidine isoleucine amide (PHI), substance P, calcitonin gene-related peptide (CGRP), neurokinin A, cholecystokinin (CCK) and opioid peptides may be transmitters in afferent pathways to the pelvic viscera. These substances are widely distributed in: 1) nerve fibers in the pelvic organs, 2) visceral afferent neurons in the lumbosacral dorsal root ganglia and 3) at sites of afferent termination in the spinal cord. Double, staining immunocytochemical techniques have shown that more than one peptide can be localized in individual visceral afferent neurons and that neuronal excitatory (VIP, substance P, CCK) and inhibitory peptides (leucine enkephalin) can coexist in the same afferent cell. Studies with the neurotoxin, capsaicin, indicate that peptidergic afferent pathways are, involved in the initiation of central autonomic reflexes as well as peripheral axon reflexes which modulate smooth muscle activity, facilitate transmission in automatic ganglia and trigger local inflammatory responses.     

辣椒碱的制备与应用概述

在分析研究国内外关于辣椒碱类物质的研究成果的基础上,对辣椒碱的性质、合成方法、应用领域等方面进行了较详尽的综述,以期为相关研究提供参考。     

Distinct features of recombinant rat vanilloid receptor-1 expressed in various expression systems

In this study, we expressed rat vanilloid receptor 1 (VR1) in various heterologous expression systems using different VR1-encoding vectors, and examined how the VR1 agonists capsaicin and resiniferatoxin affected intracellular calcium. Our results clearly show that the magnitude and kinetics of response as well as the extent of tachyphylaxis differ markedly between systems. Using green fluorescent protein-tagged VR1, we show that much of the VR1 is localized to intracellular membranes. Consistent with this localization, VR1 agonists are able to liberate calcium from intracellular stores in the absence of extracellular calcium. As with other parameters of response, the three expression systems differ in the degree to which, in the absence of extracellular calcium, capsaicin and resiniferatoxin can liberate calcium from the intracellular stores. Our findings emphasize the influence of the expression system on characteristics of the response of VR1 to its ligands and the need for caution in extrapolating such results to other settings.Received 16 June 2003; received after revision 26 July 2003; accepted 31 July 2003     

微波辅助提取辣椒中辣椒素的研究

采用正交实验,用微波辅助提取辣椒中辣椒素,用HPLC法进行辣椒中辣椒素的含量测定,流动相:甲醇-水-冰醋酸(75:25:0.25),流速为1.0 mL/min,检测波长为280nm,柱温为32℃.结果表明,在酒精度50%,提取时间为4 min,料液比1:40加的提取条件下可很好地提取辣椒中的辣椒素,辣椒素的提取率为92.15%.     

辣椒碱主要组分的RP-HPLC法测定

采用RP-HPLC法对辣椒碱样品的主要组分进行了定量的测试.色谱条件为:YMCODS柱(250 mm×4.6 i.d.,5μm),柱温40℃,流动相甲醇-质量分数为0.1%的H3PO4水溶液(75+25),流速0.6 mL/min,检测波长280 nm,进样量5μL.分析过程中,辣椒碱的组分与其他杂质达到基线分离,能够定量测出其总含量.在进样量0.6～60 μg内,其线性回归方程为y=10.749 X+2.731,线性相关系数r为0.999,标准品和样品的相对标准偏差(RSD)分别为1.96%(n=10)和2.35%(n=6),加标回收率为99.22%(RSD=1.59%,n=6),最低检出限为0.04μg.