《心术》里的学问

"《心术》在医卫界流行是必然的,它说出了很多医生的心里话。一般人则通过它看到非事件化下的医生,他们的喜怒哀乐,煎熬与追求。于医患理解大有益处。最近,各个地方台都在放《心术》,跟着看。不错。之前,曾听几个医生朋友谈起小说很火,返回读。也不错。     

皮炎湿疹如何用药

皮炎、湿疹的主要症状为瘙痒、红疹,而且病情易反复。皮炎、湿疹经常会被一起提到,因为他们是对同一类疾病不同角度的描述。但是,皮炎、湿疹还是有区别的。临床所谓的皮炎是指病因明确或具有某些特征的湿疹。它们是皮肤科的常见病、多发病。皮炎多数可查出致病源,如接触性皮炎,发病前接触过如油漆、金属小饰品等物品。然而湿疹可能暂时查不出致病源,一旦查出病因,则改称为某某皮炎。     

快乐属于谁,微笑赠给谁

又到人间四月天。每年的愚人节,总会想起一个人。想起他的动人笑脸,想起他离去时的决绝。2003年4月1日,香港文华酒店,张国荣。一个集万千宠爱于一身的人,选择在这样特殊的时间和地点,毫无征兆地离开,让当时还笼罩在SARS阴影中的人们猝不及防。那一夜多少人无心睡眠。还记得他生前的最后一则新闻是这样的:     

红帆素——前列腺的守护者

10月28日是全国男性健康日。记者从我市几家大医院了解到。近年来男性如前列腺炎、前列腺增生以及不育症等疾病的发病率呈上升趋势。随着生活节奏的加快,社会竞争的加剧。巨大的心理压力造成男性长期处于紧张状态,加上久坐、骑车、开车,另外许多男性有吸烟、喝酒的嗜好。没有良好的生活习惯。因而引起发病率上升。从前。男性一般要在45岁左右才出现前列腺病变。现在20几岁的年轻人患前列腺炎的也不少。而且癌变比例也在上升。     

大盘点

神州大地其实就是一个健康的大舞台。如果说2009年是风起云涌,2010年则是暗流涌动。记忆犹新的2009年,我们看了一场故事情节完整的话剧。刚刚过去的2010年,我们欣赏的却是一场歌舞小品大拼盘。     

汶川地震过渡期疾病控制工作措施和体会

目的总结汶川地震后过渡期的疾病控制工作措施,保障灾区群众健康。方法根据地震灾区过渡期卫生防疫工作的实践经验,进行回顾性总结分析。结果总结出重点落实的6项防疫措施:①摸底调查,制定灾区防疫工作计划。②大力开展卫生宣教,让村民养成良好的卫生习惯。③搞好环境卫生,认真开展消杀灭等工作。④进行水质检验,确保饮水安全。⑤加强重点疾病的监测防控,防止传染病暴发流行。⑥加强食品卫生管理,防止发生食源性疾病。采取上述措施后,灾区无传染病暴发流行,无发生群体性食物中毒,实现了大灾之后无大疫的目标。结论采取各项预防措施对于预防地震灾后传染病的流行具有重大的意义。     

患病后该休息还是运动

医院里患者最常听到的问候语是:好好休息,祝你早日康复。传统观念中患病总是与休息联系在一起。休息的医学术语叫制动,包括:卧床(各种伤病住院时普遍的措施)、局部固定(骨折或脱位时常用)等。休息的目的是为了保护身体健康。然而休息并不总是有利于康复。这里要谈的就是休息的另一面。先谈谈心血管疾病。许多患者发病时都采用卧床休     

婚姻就像双轮车

刘姨在大部分人眼中是很幸福的。当公务员的儿子是一个不大不小的官。丈夫事业有成。而刘姨做了二十年的全职太太。刘姨的生活也是很多人羡慕的。如果不是她强烈坚持,她现在唯一需要做的家务都会有人代劳。可是。刘姨却一天比一天不快乐。     

钙：帮助孕妈咪顺利生宝贝

钙是点燃细胞活力的火焰，钙是延续生命进程的使者。如果没有钙，根本就不会有生命的产生。在精子与卵子碰撞的刹那，起决定性因素的就是钙。如果钙摄人不足，精子的活力会大大减弱。对于没有“精气神”的精子，卵子连碰都不碰。而卵子如果缺钙，再活力四射的精子也会与其擦肩而过。许多为不孕煞费苦心的男女，恰恰缺了补充足够的钙这一必备功课。对于孕妈咪而言，能够促进分娩的钙同样扮演着主要角色。     

乙肝是一种性病

您知道吗?乙肝病毒的传播方式和艾滋病病毒传播方式是一样的。也就是说,我们可以把乙肝看做一种性病。它不能通过空气传染。通过食物传染的可能性也微乎其微。乙肝,没有您想象的那样可怕。     

酶抑制剂类抗病毒药物的研究进展

介绍了HIV逆转录酶抑制剂和蛋白酶抑制剂、DNA聚合酶抑制剂、肌苷单磷酸(IMP)脱氢酶抑制剂、S-腺苷高半胱氨酸(SAH)水解酶抑制剂以及胞嘧啶三磷酸核苷酸(CTP)合成酶抑制剂的研究进展,并图解说明了这几种抑制剂的作用机制.     

Synthesis and evaluation of a new series of tri-, di-, and mono-N-alkylcarbamylphloroglucinols as bulky inhibitors of acetylcholinesterase

1,3,5-Tri-N-alkylcarbamylphloroglucinols (1-4) are synthesized as a new series of bulky inhibitors of acetylcholinesterase that may block the catalytic triad, the anionic substrate binding site, and the entrance of the enzyme simultaneously. Among three series of phloroglucinol-derived carbamates, tridentate inhibitors 1,3,5-tri-N-alkylcarbamylphloroglucinols (1-4), bidentate inhibitors 3,5-di-N-n-alkylcarbamyloxyphenols (5-8), and monodentate inhibitors 5-N-n-alkylcarbamyloxyresorcinols (9-12), tridentate inhibitors 1-4 are the most potent inhibitors of mouse acetylcholinesterase. When different n-alkylcarbamyl substituents in tridentate inhibitors 1-4 are compared, n-octylcarbamate 1 is the most potent inhibitor of the enzyme. All inhibitors 1-12 are characterized as the pseudo substrate inhibitors of acetylcholinesterase. Thus, tridentate inhibitors 1-4 are supposed to be hydrolyzed to bidentate inhibitors 5-8 after the enzyme catalysis. Subsequently, bidentate inhibitors 5-8 and monodentate inhibitors 9-12 are supposed to yield monodentate inhibitors 9-12 and phloroglucinol, respectively, after the enzyme catalysis. This means that tridentate inhibitors 1-4 may act as long period inhibitors of the enzyme. Therefore, inhibitors 1-4 may be considered as a new methodology to develop the long-acting drug for Alzheimer's disease. Automated dockings of inhibitor 1 into the X-ray crystal structure of acetylcholinesterase suggest that the most suitable configuration of inhibitor 1 to the enzyme binding is the (1,3,5)- (cis,trans,trans)-tricarbamate rotamer. The cis-carbamyl moiety of this rotamer does not bind into the acetyl group binding site of the enzyme but stretches out itself to the entrance. The other two trans-carbmayl moieties of this rotamer bulkily block the tryptophan 86 residue of the enzyme.     

COX-2 inhibitors with a methylsulfoxide pharmacophore

Novel methylsulfoxide analogues, of known selective cyclooxygenase-2 (COX-2) inhibitors, with a methylsulfone moiety are claimed as COX-2 inhibitors. The inhibitors are useful for the treatment of COX-2-mediated disorders comprising inflammation and inflammation-associated disorders. The clinical applicability for development of the claimed sulfoxide analogues as COX-2 inhibitors is eval-uated against the car-diovascular and gastrointestinal safety.     

Naturally occurring cell adhesion inhibitors

This paper reviews naturally occurring cell adhesion inhibitors derived from a plant, microbial and marine origin. Plant-derived inhibitors are classified according to a type of structure. Microbially and marine-derived inhibitors were described according to age. In addition, effects of inhibitors on cell proliferation and that of standards on cell adhesion are listed as much as possible.     

Inhibition of diamine oxidase by antihistaminic agents and related drugs.

Various drugs were tested as inhibitors of diamine oxidase on the basis of chemical relationships to the enzyme substrates. It was found that serotonine tryptamine and phenformin are good competitive inhibitors while cimetidine and pheniprazine are non-competitive inhibitors. Other antihistaminic drugs like promethazine are less powerful inhibitors.     

New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors

Over the past decade, therapeutics that target subsets of the 518 human protein kinases have played a vital role in the fight against cancer. Protein kinases are typically targeted at the adenosine triphosphate (ATP) binding cleft by type I and II inhibitors, however, the high sequence and structural homology shared by protein kinases, especially at the ATP binding site, inherently leads to polypharmacology. In order to discover or design truly selective protein kinase inhibitors as both pharmacological reagents and safer therapeutic leads, new efforts are needed to target kinases outside the ATP cleft. Recent advances include the serendipitous discovery of type III inhibitors that bind a site proximal to the ATP pocket as well as the truly allosteric type IV inhibitors that target protein kinases distal to the substrate binding pocket. These new classes of inhibitors are often selective but usually display moderate affinities. In this review we will discuss the different classes of inhibitors with an emphasis on bisubstrate and bivalent inhibitors (type V) that combine different inhibitor classes. These inhibitors have the potential to couple the high affinity and potency of traditional active site targeted small molecule inhibitors with the selectivity of inhibitors that target the protein kinase surface outside ATP cleft.     

Small molecule kinase inhibitors as anti-cancer therapeutics

Protein kinases have emerged as the most important class of targets in oncology drug discovery because of their major roles in regulating cellular growth and survival. At least, 11 kinase inhibitors have received FDA approval to be used as cancer treatments, and there are continuous efforts to bring more candidates from laboratory benches to the clinic. Although many protein kinase inhibitors directly interact with the ATP binding site, other can alter the kinase conformation to prevent productive ATP binding. Herein we discuss the different mechanisms of action of kinase inhibitors and provide classification of the inhibitors according to their binding sites. Some of these are allosteric inhibitors, ATP competitive inhibitors, protein substrate competitive inhibitors, and covalent bond forming inhibitors. This review provides a broad overview of the relation between mechanism of action and the issues of target selectivity and resistance. Special attention was given to the kinase inhibitors currently in clinical trials.     

Inhibitors of absorption as anti-obesity drugs]

There are two types of anti-obesity agents which are classified as inhibitors of absorption: inhibitors of lipid and carbohydrate absorption. Inhibitors of lipid absorption consist of lipase inhibitor (orlistat, Nomma Herb's extract (CT-II) and fat substitute (olestra, sucrose polyester). Orlistat is now available as an anti-obesity drug in the USA and Europe. CT-II may be useful as a functional diet. Application of fat substitute is still limited in snack food. As for inhibitors of carbohydrate absorption, alpha-glucosidase inhibitors are now available as anti-diabetic drugs. To develop these agents for anti-obesity drug, solution of adverse effects on the gastrointestinal tract are necessary.     

Inhibitors of de novo folate enzymes in Plasmodium falciparum

Antifolates, inhibitors of folate synthesis or folate conversion, are used for malaria treatment. They are developed as synergistic combinations of inhibitors of dihydrofolate reductase (DHFR) and of dihydropteroate synthase (DHPS). DHPS inhibitors are sulfur-based drugs, analogs of sulfanilamide. These compounds compete with para-aminobenzoic acid in the active site of DHPS. The discovery of new antifolates is based on the identification of DHFR inhibitors; little work has been done on sulfur-based drugs because of their toxicity. As a result, only a few sulfur-based drugs are available. In this review, the hypothesis that compounds that compete with pteridine derivatives in active sites of de novo folate enzymes can be used as synergizers of DHFR inhibitors is discussed. If correct, this could lead to the identification of a new family of synergizers of DHFR inhibitors.     

Synthetic and phytocompounds based dipeptidyl peptidase-IV (DPP-IV) inhibitors for therapeutics of diabetes

Currently antidiabetic therapeutic strategies are mainly based on synthetic hypoglycemic agent. Antidiabetic drugs are associated with significant adverse effects of hypoglycemia, dysfunction of insulin and weight gain. Nowadays, the novel Dipeptidyl peptidase-IV (DPP-IV) inhibitors unique approach for the management of diabetes has been considered to be safe, as DPP-IV inhibitors reduce blood glucose level by monitoring hyperglycemia including positive effects on body weight as it remains neutral, improves glycated hemoglobin levels and do not induce hypoglycemia. Inhibitors help to protect degradation of Glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP), gut hormones which helps to suppresses postprandial glucagon release, delay gastric emptying and regulate satiety. Therefore, the innovation of DPP-IV inhibitor based drugs regulates activity of incretin hormones such as GLP-1 and GIP. Commercially available DPP-IV inhibitors are chemically synthesized with good therapeutic value. However, the durability and long-term safety of DPP-IV inhibitors remains to be established. On the other hand, phytocompounds-based DPP-IV inhibitors are alternative and safe to use as compared to synthetic. Numerous novel antidiabetic compounds and group of compounds emerging in clinical development are through DPP-IV inhibition. This review summarized recent progress made on DPP-IV inhibitors from both synthetic as well as from natural sources.