心磷脂对细胞色素C氧化酶质子泵功能的影响

 用胆酸盐透析法将猪心线粒体细胞色素C氧化酶重组在含心磷脂和二肉豆寇磷脂酰胆碱的脂质体上,以还原态细胞色素C作为酶反应底物,记录脂酶体囊泡外介质液pH的变化,pH下降幅度可以反映细胞色素C氧化酶质子泵的功能。 心磷脂含量不同的细胞色素C氧化酶脂酶体质子泵功能不同。心磷脂含量在10％—40％(w/w)范围内,随心磷脂含量增高,该酶质子泵功能增强;当心磷艏含量超过50％时,该酶质子泵功能却随心磷脂含量的增加表现出下降的趋势。阿霉素可以与心磷脂紧密结合,抑制细胞色素C氧化酶的质子泵功能。然而,少量阿霉素却能增强含70％心磷脂的脂酶体的质子泵功能。     

Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase

Trichomonas vaginalis continues to be a major health problem with drug-resistant strains increasing in prevalence. Novel antitrichomonal agents that are mechanistically distinct from current therapies are needed. The NIH Clinical Compound Collection was screened to find inhibitors of the uridine ribohydrolase enzyme required by the parasite to scavenge uracil for its growth. The proton-pump inhibitors omeprazole, pantoprazole, and rabeprazole were identified as inhibitors of this enzyme, with IC₅₀ values ranging from 0.3 to 14.5 μM. This suggests a molecular mechanism for the in vitro antitrichomonal activity of these proton-pump inhibitors, and may provide important insights toward structure-based drug design.     

Antiprotozoal activity of proton-pump inhibitors

Parasitic diseases are still a major health problem in developing countries. In our effort to find new antiparasitic agents, in this Letter we report the in vitro antiprotozoal activity of omeprazole, lansoprazole, rabeprazole and pantoprazole against Trichomonas vaginalis, Giardia intestinalis and Entamoeba histolytica. Molecular modeling studies were an important tool to highlight the potential antiprotozoal activity of these drugs. Experimental evaluations revealed a strong activity for all compounds tested. Rabeprazole and pantoprazole were the most active compounds, having IC₅₀ values in the nanomolar range, which were even better than metronidazole, the drug of choice for these parasites.     

质子泵抑制剂对冠心病患者嗜铬粒蛋白A 影响的临床意义

目的:本研究旨在探讨质子泵抑制剂(PPI)对心内科拟诊断为冠心病患者的嗜铬粒蛋白A(CgA)水平影响的临床意义。方法:113名拟诊冠心病的住院患者,分为PPI组(药物治疗中加入PPI,共62例)和非PPI组(药物治疗中无PPI,共51例),收集其外周血清,用ELISA法检测样本血清中CgA水平,同时应用化学发光法检测样本血清中NT-proBNP水平。比较PPI组和非PPI组CgA、NT-proBNP水平的差异。结果:因为CgA、NT-proBNP均为非正态分布资料,两者均通过对数转换为正态分布资料;PPI组的LN CgA的均数显著高于非PPI组(4.62±0.97和3.91±0.89,P=0.000)。而两组LN NT-proBNP的均数无显著差异(5.41±1.46和5.59±2.00,P=0.580)。结论:在心功能等临床特征具有可比性的情况下,是否使用PPI对CgA水平的影响很大;而对BNP无明显影响。评价CgA在心功能分级或冠心病预后等方面的应用,不能忽略PPI联用对CgA数值的影响。     

质子泵抑制剂对冠心病患者嗜铬粒蛋白A影响的临床意义

目的：本研究旨在探讨质子泵抑制剂（vii）对心内科拟诊断为冠心病患者的嗜铬粒蛋白A（CgA）水平影响的临床意义。方法：113名拟诊冠心病的住院患者,分为PPI组（药物治疗中加入PPI,共62例）和非PPI组（药物治疗中无PPI,共51例）,收集其外周血清,用ELISA法检测样本血清中CgA水平,同时应用化学发光法检测样本血清中NT—proBNP水平。比较PPI组和非PPI组CgA、NT．proBNP水平的差异。结果：因为CgA、NT．proBNP均为非正态分布资料,两者均通过对数转换为正态分布资料;PPI组的LNCgA的均数显著高于非PPI组（4．62±0．97和3．91±0．89,P=0．000）。而两组LNNT-proBNP的均数无显著差异（5．41±1．46和5．59±2．00,P=0．580）。结论：在心功能等临床特征具有可比性的情况下,是否使用PPI对CgA水平的影响很大;而对BNP无明显影响。评价CgA在心功能分级或冠心病预后等方面的应用,不能忽略PPI联用对CgA数值的影响。