4(6)-{2-[4-(2,3,4-三甲氧基苄基)哌嗪-1-基]-2-氧代乙氧基}芳甲酰胍类化合物的合成及其Na~+/H~+交换器1抑制活性

NHE1(Na+/H+交换器1)抑制剂对于心肌缺血再灌注损伤具有较好的保护作用.以苯(或吡啶)甲酰胍为母核,利用拼合原理,在苯(或吡啶)甲酰胍母环上引入4-(2,3,4-三甲氧基苄基)哌嗪-1-甲基,设计并合成了8个未见文献报道的目标化合物.其结构经MS,IR,1H NMR和元素分析确证.体外血小板肿胀模型(PSA)试验结果表明,大部分目标化合物显示出较好的NHE1抑制活性.     

Proteomic analysis reveals platelet factor 4 and beta-thromboglobulin as prognostic markers in severe acute respiratory syndrome

Previously, we reported that proteomic fingerprints were present in sera of patients with severe acute respiratory syndrome (SARS), and could separate patients into subgroups with different prognoses. In the present study, we examined the prognostic values of the SARS-associated proteomic features by biostatistical analysis, and deciphered the identities of those with prognostic values. Data of 20 SARS-associated serum proteomic features and ten serological variables from 38 SARS adult patients before treatment were subjected to multivariate logistic regression. Proteomic features of m/z 6634, m/z 7769, m/z 8635, and m/z 8865 were identified as independent prognostic markers. After purification by cation-exchange chromatography and gel electrophoresis, proteomic features of m/z 7769 and m/z 8865 were found to be platelet factor 4 (PF4) and beta-thromboglobulin (beta-TG) by tandem mass spectrometry, respectively. The associations of decreased serum PF4 and increased serum beta-TG levels with poor prognosis were confirmed by Western blot. Previous studies suggest that PF4 and beta-TG are involved in the pathogenesis of acute respiratory distress syndrome (ARDS) in a negative and positive way, respectively. Our results suggest that PF4 and beta-TG may also play similar roles in the development of ARDS in SARS patients.     

典型的三聚氰胺致幼儿肾结石红外光谱分析

从云南省第一人民医院得到经过医学证实的典型三聚氰胺肾结石,将2 mg肾结石与200 mg KBr一同放入玛瑙研钵中研碎,进行压片。用Perkin-Elemer公司生产的spectrum 100光谱仪得到了该结石的红外光谱。吸收峰在4 000～2 000 cm-1之间有3 487,3 325, 3 162, 2 788 cm-1,在1 700～1 000 cm-1之间有1 694,1 555,1 383,1 340,1 189,1 122 cm-1,在1 000～400 cm-1之间有993,782,748,709,624,585,565,476 cm-1。结石的红外光谱经过与文献报道的饲喂含氰尿酸、三聚氰胺宠物饲料后猫的肾结石的红外光谱图及普通人肾结石的红外光谱图对比,相差很大,说明该患儿结石与宠物结石及普通人肾结石的成分相同的可能性不大;分别与三聚氰胺与尿酸的红外光谱图对比,各有50%的相似性; 将三聚氰胺、尿酸按1∶1混合后,红外光谱出现的峰在4 000～2 000 cm-1 之间有3 469,3 419,3 333,3 132,3 026,2 827 cm-1, 在1 700～1 000 cm-1之间有1 696, 1 656, 1 555, 1 489, 1 439, 1 350, 1 311, 1 198, 1 124, 1 028 cm-1, 在1 000～400 cm-1之间有993,878,814,784,745,708,619,577,475 cm-1,将其与结石的红外光谱对比,发现两张图谱有83.3%的相似性,由此得出典型三聚氰胺尿结石的主要成分为三聚氰胺和尿酸。     

紫心甘薯多糖对四氯化碳肝损伤小鼠的保护作用

研究紫心甘薯多糖对四氯化碳(CCl4)诱导小鼠免疫性肝损伤的保护作用及可能作用机制.以不同剂量的紫心甘薯多糖200、400、800 mg.(kg.d)-1分别给予小鼠灌胃,设立对照组,连续10 d作预处理,腹腔注射0.1%的CCl410 ml.kg-1建立CCl4诱导小鼠肝损伤模型.测定血清谷丙转氨酶(ALT)、谷草转氨酶(AST)、乳酸脱氢酶(LDH)酶活力、总胆红素(TBIL)、总蛋白(TP)含量,测定肝组织中超氧化物岐化酶(SOD)、谷胱甘肽(GSH)、丙二醛(MDA)水平,并进一步观察肝组织病理组织学变化.紫心甘薯多糖各剂量组均能明显地抑制血清中ALT、AST、LDH、TBIL的升高和TP的下降,降低肝脏中MDA的含量,提高肝组织中SOD和GSH活性,减轻CCl4对肝脏细胞的病理损伤.紫心甘薯多糖对CCl4致小鼠急性肝损伤具有明显保护作用,其作用机理可能与抗氧化作用有关.     

Weakened acute type condition for tetrahedral triangulations and the discrete maximum principle

We prove that a discrete maximum principle holds for continuous piecewise linear finite element approximations for the Poisson equation with the Dirichlet boundary condition also under a condition of the existence of some obtuse internal angles between faces of terahedra of triangulations of a given space domain. This result represents a weakened form of the acute type condition for the three-dimensional case.

     

支气管哮喘发作期血清部分微量元素的研究

对60例支气管哮喘发作患者血清中部分微量元素进行了观察,并同正常人群进行了对照。发现与正常人群有一定的差别。讨论了其原因。     

补肾调肝法治疗对精液异常患者精液微量元素改变的观察

研究了２６例精液异常患者使用补肾调肝法治疗后其精液锌、铜、铅等元素的改变。２６例患者在治疗后精液质量有明显改善,其中精液中锌含量与治疗前相比有明显提高,治疗前后分别为（２．０６＋１．０９）ｍｍｏｌ．Ｌ和（２．４８±１．０５）ｍｍｏｌ·Ｌ（Ｐ＜０.０１）,差异具有显著性意义。精液中的铜含量也有所提高。铅含量比治疗前减少,但并不具显著性。     

Some theorems in the X-M-PN space

ＬｅｔＲｂｅｔｈｅｓｅｔｄｅｎｏｔｉｎｇａｌｌｒｅａｌｎｕｍｂｅｒｓ,Ｒ ｂｅｔｈｅｓｅｔｄｅｎｏｔｉｎｇａｌｌｎｏｎｎｅｇａｔｉｖｅｒｅａｌｎｕｍｂｅｒｓ.ＡｍａｐｐｉｎｇＦ:Ｒ→Ｒ ｉｓｃａｌｌｅｄａｄｉｓｔｒｉｂｕｔｉｏｎｆｕｎｃｔｉｏｎ,ｉｆｉｔｉｓａｎｏｎｄｅｃｒｅａｓｉｎｇｆｕｎｃｔｉｏｎａｎｄｌｅｆｔｃｏｎｔｉｎｕａｔｉｏｎｓａｔｉｓｆｙｉｎｇｔｈｅｆｏｌｌｏｗｉｎｇｃｏｎｄｉｔｉｏｎｓ:ｉｎｆｔ∈ＲＦ(ｔ)=0,ｓｕｐｔ∈ＲＦ(ｔ)=1,Ｄ ｔｈｅｓｅｔｏｆａｌｌｄｉｓｔｒｉｂｕｔｉｏｎｆｕｎｃｔ…     

离子液体的毒性

离子液体因其特有的物化性质受到越来越多的关注,并被认为是环境友好的"绿色产品"。但是有关离子液体的潜在毒性一直被人们所忽视,直到最近才有少量报道。本文综述了离子液体毒性研究的相关情况：详细介绍了离子液体毒性研究的各种方法及优缺点;离子液体对各类生物的急性毒性和慢性毒性;离子液体的各部分组成,尤其是阳离子核种类、取代烷基碳链长度和阴离子种类对离子液体毒性的影响情况,以及SAR理论在离子液体毒性研究中的应用情况。在此基础上提出今后离子液体毒性研究的发展方向。     

Antioxidative,Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury

Sepsis is the major cause of acute kidney injury (AKI) in severely ill patients, but only limited therapeutic options are available. During sepsis, lipopolysaccharide (LPS), an endotoxin derived from bacteria, activates signaling cascades involved in inflammatory responses and tissue injury. Apamin is a component of bee venom and has been shown to exert antioxidative, antiapoptotic, and anti-inflammatory activities. However, the effect of apamin on LPS-induced AKI has not been elucidated. Here, we show that apamin treatment significantly ameliorated renal dysfunction and histological injury, especially tubular injury, in LPS-injected mice. Apamin also suppressed LPS-induced oxidative stress through modulating the expression of nicotinamide adenine dinucleotide phosphate oxidase 4 and heme oxygenase-1. Moreover, tubular cell apoptosis with caspase-3 activation in LPS-injected mice was significantly attenuated by apamin. Apamin also inhibited cytokine production and immune cell accumulation, suppressed toll-like receptor 4 pathway, and downregulated vascular adhesion molecules. Taken together, these results suggest that apamin ameliorates LPS-induced renal injury through inhibiting oxidative stress, apoptosis of tubular epithelial cells, and inflammation. Apamin might be a potential therapeutic option for septic AKI.