The pharmacological profile of TX 066 (17 alpha-acetoxy-6-methyl-19-nor-4,6-pregna-diene-3,20-dione), a new oral progestative

17 alpha-Acetoxy-6-methyl-19-nor-4,6-pregna-diene-3,20-dione (TX 066) has the pharmacological profile of a pure progestogen with no side effect such as androgenic activity. Its pituitary suppressing effect is relatively weak, as is also its antiestrogenic activity. It possesses a powerful antiandrogenic effect, which, in addition to the classic uses for progestogens, may make TX 066 useful in the treatment of certain diseases such as prostatic hypertrophy or the Stein-Leventhal syndrome.     

卡托普利在治疗非心血管疾病中的应用

本文介绍了卡托普利在治疗肝硬化腹水、肾病综合征、原发性醛固酮增多症、甲状腺功能亢进症、流行性出血热、类风湿性关节炎、特发性水肿和高血脂症、婴幼儿肺炎、毛细支气管炎等非心血管疾病中的应用情况。拓宽了卡托普利的临床应用范围。     

左氧氟沙星的不良反应

左氧氟沙星是临床广泛应用的抗菌药，用药期间可能出现的不良反应涉及消化系统、中枢神经系统、心血管系统、血液及内分泌系统等8大系统，包括恶心、呕吐、头晕、头痛、皮肤过敏反应等症状。本文对左氧氟沙星不良反应进行简要综述，旨在引起临床医生的重视，促进其合理应用。     

盐酸小檗碱的心血管药理活性研究进展

小檗碱是一种异喹啉生物碱,存在于黄连、黄檗等植物中,临床常用其盐酸盐.盐酸小檗碱具有强心、抗心律失常、内皮保护、心肌保护、降压、抗动脉粥样硬化、糖尿病性心血管疾病治疗等心血管药理活性作用,是一种富有潜力的心血管疾病治疗药物.本文通过对PubMed数据库进行检索,对盐酸小檗碱的心血管药活性研究进行了综述.     

医学随访研究工作模型和设计模型

本文依据医学随访研究临床过程建立工作模型,反推出设计模型,描述其使用方法,并附以数值实例。与以往同类模型相比,该模型的优点是便于限定失访和终末终检水平,没有来自信息性终检的偏性和无Morgan误差。这类研究的开展日趋广泛,因此,该模型在临床上将十分常用。     

Buprenorphine

Buprenorphine is a mixed agonist-antagonist with high affinity at both mu and kappa opiate receptors. Its pharmacological profile is determined primarily by partial agonism at mu-receptors and unusually slow kinetics at these receptors. Its intrinsic activity is such that in nearly all clinical situations it is as effective an analgesic as morphine with considerably longer duration and much more favourable acute safety. In long-term dosing studies in rodents and primates buprenorphine did not produce the manifestations of physical dependence when treatment was stopped. In self-administration studies in the same species only limited levels of reinforcing efficacy were demonstrated when compared with the opiates. In human former opiate addicts the limited potential of buprenorphine to produce psychological dependence was confirmed as was the favourable physical dependence profile. Some misuse of buprenorphine has been reported in 3 of the 29 countries in which buprenorphine is marketed despite its wide clinical acceptance, particularly as the sublingual formulation.     

N-(4-羟基苯基)维生素甲酰胺诱导肿瘤细胞凋亡的机制

N-(4-羟基苯基)维生素甲酰胺(4-HPR)是一种维甲酸类化合物，通过诱导肿瘤细胞凋亡抑制肿瘤生长，其诱导凋亡的机制包括升高活性氧、神经酰胺的水平和增加Caspase活性等不依赖受体的机制和依赖维甲酸受体的机制，以及在其中发挥作用的其他因素。     

光敏剂5-氨基乙酰丙酸的临床应用

随着第二代光敏剂5-氨基乙酰丙酸等的开发上市,光动力疗法的临床地位逐步确立, 临床应用已从皮肤疾病及体表和腔内肿瘤的诊治逐步扩展至肝癌等脏器肿瘤的治疗.本文重点综述近年5-氨基乙酰丙酸在肿瘤诊断及多种难治性皮肤病治疗中的临床应用及其评价.     

Pharmacological Properties of Melanin and its Function in Health

The biological pigment melanin is present in most of the biological systems. It manifests a host of biological and pharmacological properties. Its role as a molecule with special properties and functions affecting general health, including photoprotective and immunological action, are well recognized. Its antioxidant, anti‐inflammatory, immunomodulatory, radioprotective, hepatic, gastrointestinal and hypoglycaemic benefits have only recently been recognized and studied. It is also associated with certain disorders of the nervous system. In this MiniReview, we consider the steadily increasing literature on the bioavailability and functional activity of melanin. Published literature shows that melanin may play a number of possible pharmacological effects such as protective, stimulatory, diagnostic and curative roles in human health. In this MiniReview, possible health roles and pharmacological effects are considered.     

银屑病发病机制的免疫学研究进展

银屑病是多基因遗传背景下的免疫性疾病,与T细胞、树突状细胞等多种免疫细胞以及血管内皮生长因子等多种细胞因子有关,发病机制复杂,病因尚不明确。银屑病的组织病理学表现为角质形成细胞过度增生、炎症细胞聚集和真皮乳头部血管增生扩张,其皮损中多种细胞因子表达增加。本文就银屑病发病机制的免疫学研究进展作一综述。     

Occurrence of paralytic shellfish poison (PSP) in the starfish Asterina pectinifera collected from the Kure Bay, Hiroshima Prefecture, Japan.

Assays were made for paralytic toxicity of marine invertebrates inhabiting at the coasts of Hiroshima Bay, where the infestation of bivalves such as cultured oysters with paralytic shellfish poison (PSP) has been occurred. The starfish Asterina pectinifera collected at the estuary of Nikoh River, Hiroshima Bay, was found to contain moderate levels of paralytic toxicity. Its highest toxicities as PSP found on July 30, 1999 were 12.5 MU/g for whole body, 11.0 MU/g for integument tissues and 3.9 MU/g for viscera, respectively. The toxicity of integument was changed from 3.6 to 11.0 MU/g in 1 year. Its paralytic toxin principles were identified as PSP toxins, composing mainly from saxitoxin (STX) group toxins such as carbamoyl-N-hydroxy neosaxitoxin (hyneoSTX), and STX, by HPLC and LC-MS, accounting for over 90 mol%. The PSP toxins contained in the starfish A. pectinifera considered to be transferred from bivalves or detritus living in the same area, which were contaminated with PSP. However, the involved pathway may be different from that of Asterias amurensis which was infested directly through food chain from its food bivalves, for its toxin pattern.     

糖肽类抗生素N-甲基无糖万古霉素的分离、纯化和结构鉴定

目的 利用含N-甲基转移酶的粗酶液对无糖万古霉素进行催化,从得到的反应液中分离、纯化N-甲基无糖万古霉素,并进行结构鉴定。方法 利用大孔树脂吸附、中压反相制备色谱等方法进行分离纯化。利用光谱分析,进行结构解析。结果 分离到一个糖肽类化合物N-甲基无糖万古霉素。结论     

alpha-Glycosidase inhibitory activity of hexagalloylglucose from the galls of Quercus infectoria

Hexagalloylglucose (3-O-digalloyl-1,2,4,6-tetra-O-galloyl-beta-D- glucose), which was isolated from the methanol extract of the galls of Quercus infectoria, significantly inhibited alpha-glycosidases such as sucrase, maltase and isomaltase. Its inhibitory activity was comparable to acarbose being used as a hypoglycemic agent, while the inhibitory activity on alpha-amylase was approximately 10 times lower than that of acarbose. The results indicate that, when compared to acarbose, hexagalloylglucose might reduce the side effects by reducing inhibition of alpha-amylase.     

肾素-血管紧张素系统的新成员:ACE2

血管紧张素转换酶2(angiotensin-converting enzyme 2,ACE2)是新发现的血管紧张素转换酶(ACE)的第一个同系物,ACE2与ACE结构虽部分相似,但功能特性却不同.在肾素-血管紧张素系统(rennin-angiotensin system,RAS)中ACE2与ACE共同参与血管紧张素代谢,调节心血管系统活动,研究发现ACE2与高血压、糖尿病以及肾脏、生殖等系统的疾病发生发展密切相关.本文就ACE2的新近研究进展做一综述.     

Integrin alpha v beta 3 as a therapeutic target for blocking tumor-induced angiogenesis

The integrin receptor alphavbeta3 has been shown to play a critical role in several distinct processes, such as angiogenesis, osteoclast-mediated bone resorption and tumor metastasis. Its expression is upregulated in newly synthesized blood vessels produced in response to a variety of tumors and purified angiogenic factors. Studies show that alphavbeta3 is a critical target downstream from perhaps all angiogcnic factors. Proof-of-principle that alphavbeta3 antagonists such as monoclonal antibodies and small molecules block angiogenesis and tumor growth has been obtained in several animal models. Many endogenous inhibitors of angiogenesis such as angiostatin, endostatin and tumstatin seem to work through the alphavbeta3 receptor further emphasizing the critical role of this receptor in angiogenesis. In addition, the alphavbeta3 receptor has been clearly implicated in several pathological processes such as rheumatoid arthritis, osteoporosis, and metastasis of prostate cancer to bone. Thus alphavbeta3 may prove to be an important target for pharmacological intervention in more than one clinical setting.     

The effects of drugs on sperm

Spermatogenesis is a complex process which takes about 70 days in the human. Its endocrine control may be affected by various hormones, antihormones or psychotrophic drugs. Cytotoxic agents, or industrial chemicals such as dibromochloropropane, directly affect the germinal epithelium. Sperm maturation may be impaired by alpha-chlorohydrin, antiandrogens, or sulphasalazine, and sperm motility in the female genital tract can be inhibited by vaginal spermicides such as nonoxynol-9 and by propranolol. Drug treatment of idiopathic oligozoospermia is disappointing, though gonadotrophins or their releasing hormone are useful in treating gonadotrophin deficiency. As far as contraception is concerned, there is still no suitable 'male pill': combinations of hormonal steroids are not sufficiently effective and gossypol appears to be too toxic.     

银杏叶提取物对缺血-再灌注细胞凋亡的影响

缺血-再灌注（IR）是一种常见的临床病理生理过程，如心肌梗死、脏器移植、断肢再植以及四肢动脉栓塞等的血管再通，其具体的发生机制仍未阐明。研究发现，细胞凋亡可能在缺血-再灌注损伤（IRI）中起着重要作用。近年来，关于银杏叶提取物（GBE）对IR引起细胞凋亡的影响的研究较多，通过查阅大量文献，发现在动物实验中，GBE可降低不同器官因IR导致的细胞凋亡率的升高，包括肝脏细胞、神经细胞、心肌细胞等，其发生可能是通过对氧化应激的影响及对细胞因子的影响而实现的。     

Castleman病患者的病理学所见(附5例报告)

目的探讨Castleman病的临床病理学特点。方法通过5例经手术及病理证实的Castleman病的病例分析,结合文献复习,对本病的病因、临床表现、病理、诊断、鉴别诊断、治疗及预后进行讨论。结果本组男3例、女2例;年龄32～51岁,平均38.6岁。临床上4例为局灶型、1例为多中心型。组织病理学分型:透明血管型2例,浆细胞型3例。结论Castleman病是一种罕见的淋巴组织增生性良性疾病。其诊断依赖于病理组织学形态,并须结合其临床资料。治疗方面,手术切除是首选,应用干扰素类抗病毒药物,有助于控制本病的发展。     

肢体缺血预适应保护远隔组织器官的应用研究进展

肢体缺血预适应是指肢体短暂缺血后使肢体本身骨骼肌或远隔组织能耐受较长时间的缺血损伤。肢体缺血预适应具有很强的临床应用价值,可以通过机体不太重要的器官预适应而保护重要器官如心脏、肺、脑、小肠、胃、肝等,其机制可能与神经与体液因素、局部或全身因素、钾通道、腺苷受体、阿片受体、线粒体等有关。     

Diphoterine for emergent eye/skin chemical splash decontamination: a review

Eye/skin chemical splashes are a significant problem. Diphoterine is an hypertonic, polyvalent, amphoteric compound developed in France as an eye/skin chemical splash water-based decontamination solution. In vitro and in vivo, it actively decontaminates approximately 600 chemicals, including acids, alkalis, oxidizing and reducing agents, irritants, lacrimators, solvents, alkylating agents, and radionuclides. Its chemical bond energy for such agents is greater than that of tissue receptors. Its hypertonicity impedes chemical tissue penetration and may remove some amount of skin/cornea-absorbed toxicants not already bound to tissue receptors. Diphoterine chemical reactions are not exothermic. Diphoterine and its acid/alkali decontamination residues are not irritating to the eyes or skin; it is essentially nontoxic. Diphoterine can prevent eye/skin burns following chemical splashes and results in nearly immediate pain relief.