治疗HIV感染的先导天然化合物

已知众多天然产物具有抗HIV活性其中部分化合物的作用靶亦已明确,它不同的结构、不同的机制作用于病毒复制周期中的某一个或多个环节。作为HIV感染化学治疗的先导天然化合物,具有十分重要的研究开发价值。     

本科《天然化合物波谱解析》课程教学方法探讨

《天然化合物波谱解析》是一门研究如何根据天然化合物的波谱研究其化学结构的课程,是中药学和药学专业本科生的一门难度较大的专业课程.本文从本课程与本科《仪器分析》《中药化学》《天然药物化学》等相关课程之间的衔接关系,授课内容、授课重点的选择,课堂教学的授课方式,以及与研究生《天然化合物波谱解析》课程的区别与联系等五个方面讨论本课程的教学方法和教学中应该注意的问题.     

天然药物的开发和利用

在世界范围内销售的药物中,约30％来源于天然产物。有关天然药物的发展、开发和利用的实例已有很多报道。分子生物学、细胞生物学、基因工程学的进展,对从分子和基因水平发现有效药物提供了基础。高通量筛选系统的出现显著加快了药物发现的进程。本文对天然药物的发展、开发现状及应用前景进行综述。     

中国西部天然药物信息数据库的开发

对一个涵盖中国西部地区天然药物生态特性到分子结构方面多种信息的天然药物数据库的建立和其查询系统的开发进行了描述。特别介绍了数据库中引入的量子化学计算,以及该数据库所具有的数据更新方便、查询功能强大等特点,并对应用于定量构效关系研究的前景进行了展望。     

天然产物与药物的发现

目前使用的的很多药物都直接或间接来自天然产物，天然产物形成了新药开发的广泛的物质上来在抗癌，抗感染，抗疟，神经系统，心血和系统和免疫系统药物领域中开发出或正在开发的有重大治疗价值的植物药充分证实了这一点。     

寻找生物活性物质的各种途径

Strathclyde大学植物化学研究室把从天然产物中寻找新的先导化合物作为其主要目标。本文综述了该室近年进行的许多研究,每项研究都反映了获得新化合物或具有生物活性提取物的不同途径。     

国际海洋天然产物研究进展及展望--第10次国际海洋天然产物研讨会简介

国际海洋天然产物研讨会(InternationalSymposium on Marine Natural Products,简称MaNaPro)是反映国际海洋天然产物研究最新趋势、动态和进展的重要的国际性会议,每3年举行1次。自1975年在英国举行第1届MaNaPro会议以来,至今已举行了10次。每次会议都吸引众多国际一流的专家学者前往展示与交流各自的最新研究成果,同时探讨学科新的研究发展方向,对国际海洋     

迷迭香酸药理作用的研究进展

本文综述近年迷迭香酸的主要药理作用的研究进展,该药在抗炎，抗花生四烯酸代谢，免疫调节，抗氧化等方面作用显著，提示从天然产物成分中开发有临床价值的药物是一个引人瞩目的方向。     

“无毒草药”也伤眼

大多数人想当然地认为：“天然的东西就绝对是安全的”。就这一观点，很大一部分人都比较信赖中草药，觉得它是纯天然的，无毒副作用。     

The debate on DDT

The paper reviews the early toxicologic and pharmacologic studies carried out by the author and his associates from 1943 to 1947, which were largely responsible for launching DDT as an agent for the control of typhus, malaria, yellow fever, and related vector-borne diseases. After reviewing recent studies conducted at the University of Miami, which dealt with organochlorine pesticides in human tissues, the tumorigenicity of aldrin, dieldrin and endrin (rat), six-generation mouse and three-generation dog reproduction studies, synergism of DDT and aldrin (dog), and the fate of DDT and aldrin during a period of severe starvation (rat), it is pointed out that it is primarily the overuse and misuse of DDT in pest control that have caused the pollution in our ecology. It is emphasized that the requirements for pest control differ the world over and that it must therefore be left to the national regulatory agencies to legislate the safe use of DDT and related pesticides. It is recommended that future human and animal studies with DDT and its derivatives give consideration to: (a) the balance and metabolism of the various hormones, (b) reproduction (estrus, libido, mammary development, milk production, (c) hepatic microsomal enzyme activities, (d) cancer prevention and cancer production, (e) excessive body weight changes induced by disease, unbalanced diet or starvation, and (f) the effects of DDT and its derivatives when absorbed in combination with other related and even unrelated compounds.Presented at the joint meeting of the Scandinavian and German Pharmacological Societies, Copenhagen, Denmark, July 20–23, 1971.     

肠道菌群与健康、疾病和药物作用的影响

肠道菌群作为人体内一个复杂的微生态系统,在维持人体微生态的稳态中,肠道菌群在维持宿主生理功能具有上非常重要的作用,也对许多代谢性疾病、免疫性疾病以及肿瘤都有着密切的关系,且对于药物治疗合理安全有效具有重要意义。本文从正视存在人体的细菌的有益性和有害性、肠道菌群与健康和寿命、肠道菌群与疾病以及药物作用的影响等4方面分析和讨论。肠道菌群与不同类型药物的关系已经成为近些年的热点研究领域,本文分别讨论免疫治疗、化学药物、抗生素和中药的相关问题,希望为认识药物治疗过程、科学合理用药、认识药物作用机制、新药研究开发等研究有所参考。     

海星皂苷生物活性与制备研究进展

海洋是全球药物研发的重要宝库，提高海洋生物资源深度开发和高值化利用能力，是我国海洋强国战略的重要组成部分，也是促进海洋经济可持续发展及实施“蓝色药库”的关键途径之一。海星属典型的棘皮动物，进化地位和生物学特征独特，是国际公认的药用/保健用海洋生物。海星中含有皂苷、多糖、多肽、氨基酸、胶原蛋白、甾醇及生物碱等多种营养成分和活性物质，其中海星皂苷在抗肿瘤、抗炎、抗衰老及降血脂等方面展现出良好的生物活性，在食品和药物研发领域具有巨大的发展潜力和广阔的应用前景。本文系统检索了近30年海星皂苷的研发现况，并且对近15年来海星皂苷的生物活性、提取分离及相关专利等方面取得的研究进展进行梳理，进而为其在营养保健和药物研发中的应用提供相关理论支持。     

Molecular handling of cadmium in transporting epithelia

Cadmium (Cd) is an industrial and environmental pollutant that affects adversely a number of organs in humans and other mammals, including the kidneys, liver, lungs, pancreas, testis, and placenta. The liver and kidneys, which are the primary organs involved in the elimination of systemic Cd, are especially sensitive to the toxic effects of Cd. Because Cd ions possess a high affinity for sulfhydryl groups and thiolate anions, the cellular and molecular mechanisms involved in the handling and toxicity of Cd in target organs can be defined largely by the molecular interactions that occur between Cd ions and various sulfhydryl-containing molecules that are present in both the intracellular and extracellular compartments. A great deal of scientific data have been collected over the years to better define the toxic effects of Cd in the primary target organs. Notwithstanding all of the new developments made and information gathered, it is surprising that very little is known about the cellular and molecular mechanisms involved in the uptake, retention, and elimination of Cd in target epithelial cells. Therefore, the primary purpose of this review is to summarize and put into perspective some of the more salient current findings, assertions, and hypotheses pertaining to the transport and handling of Cd in the epithelial cells of target organs. Particular attention has been placed on the molecular mechanisms involved in the absorption, retention, and secretion of Cd in small intestinal enterocytes, hepatocytes, and tubular epithelial cells lining both proximal and distal portions of the nephron. The purpose of this review is not only to provide a summary of published findings but also to provide speculations and testable hypotheses based on contemporary findings made in other areas of research, with the hope that they may promote and serve as the impetus for future investigations designed to define more precisely the cellular mechanisms involved in the transport and handling of Cd within the body.     

Influence of cadmium and copper on tissue element levels of pregnant rats

In the current study, we examined the effects of Cd on Cd, Cu, Zn and Fe levels in placenta and maternal and fetal plasma and tissues, the placental weight, total fetal and maternal body weights, and fetal and maternal tissue weights during pregnancy. A total of 21 adult female rats were treated during gestation with drinking water containing one of the following: 70 mg/L of CdCl₂, a combination of 70 mg/L of CdCl₂ and 70 mg/L of CuSO₄, or no addition (control). Placenta Cu and Fe levels, fetal liver and kidney Cu levels, and fetal liver tissue weights were lower in the group administered Cd than in the control group. Also, Cd levels in the placenta, maternal and fetal liver, and maternal kidney were higher in the group treated with Cd than in controls. In the group administered both Cd and Cu, fetal body and tissue weights did not change, but Cd levels in the placenta, maternal and fetal liver, and maternal kidneys were higher than in controls. Zn and Fe levels in the maternal kidney and fetal liver were also lower in this group. Cd exposure during pregnancy resulted in Cd accumulation in maternal and fetal tissues during pregnancy and a decrease in the total weight of fetuses, and the combination of Cd and Cu caused some changes in the both maternal and fetal levels of Cu, Zn, and Fe, but it did not cause changes in the total fetal body weight or the weights of individual tissues.     

Effects of DN-2327, a new anxiolytic,diazepam and buspirone on exploratory activity of the rat in an elevated plus-maze

In the present study, the effects of a new anxiolytic, DN-2327, were compared to those of diazepam and buspirone in rats in the elevated plus-maze test. Two indices of anxiety were obtained in this test: the number of entries into the open arms expressed as a percentage of the total number of arm entries and the percentage of time spent on the open arms. Both a typical anxiolytic, diazepam, at 2.5, 5 and 10 mg/kg, PO and a new anxiolytic, DN-2327, at 2.5 and 5 mg/kg, PO dose-dependently increased the two indices: the percentage of time spent on the open arms and the percentage of open-arm entries. On the other hand, pentylenetetrazol (PTZ) at 10 and 20 mg/kg, IP decreased the two indices dose dependently as did yohimbine at 1.5 and 3 mg/kg, IP. DN-2327 at 2.5 and 5 mg/kg, PO and diazepam at 5 and 10 mg/kg, PO dose dependently and significantly increased the two indices that were suppressed following administration of PTZ at 10 mg/kg, IP. The effects of both DN-2327, 5 mg/kg, PO, and diazepam, 10 mg/kg, PO, on the two indices were significantly antagonized by the benzodiazepine (BZD) receptor antagonist flumazenil, 20 mg/kg, IP. Buspirone (2.5–20 mg/kg, PO) did not affect either of the two responses but dose dependently decreased the number of rearings, although in the Vogel conflict test, the anti-conflict activity of buspirone was equipotent to that of diazepam and DN-2327 at the minimum effective dose (10 mg/kg, PO) of each drug. In conclusion, the present experiment revealed that the anxiolytic effect of DN-2327 in this test was clear, whereas buspirone showed no apparent effect.     

Subacute toxicity evaluation of a new camptothecin anticancer agent CKD-602 administered by intravenous injection to rats

The subacute toxicity of a new camptothecin anticancer agent, CKD-602, was investigated after 4-week repeated intravenous administration of the chemical in Sprague-Dawley rats. The test chemical was administered intravenously to rats at dose levels of 0, 0.003, 0.013, or 0.067 mg/kg/day for males and 0, 0.004, 0.018, or 0.089 mg/kg/day for females. At the end of the treatment period, 10 rats/sex/group were sacrificed. The remaining 5 rats/sex in the vehicle control and high dose groups continued the study without treatment for 2 weeks (recovery period). During the test period, clinical signs, mortality, body weights, food and water consumption, ophthalmoscopy, urinalysis, hematology, serum biochemistry, gross findings, organ weights, and histopathology were examined. In both sexes of the high dose group, an increase in the incidence of abnormal clinical signs and paleness of the eyes, a reduction in the body weight gain, food consumption and urine protein, and an increase in the water consumption were observed. Hematological investigations revealed a decrease in the red blood cells, hemoglobin and hematocrit and an increase in the mean corpuscular volume, mean corpuscular hemoglobin, platelets, and reticulocytes in a dose-dependent manner. Serum total cholesterol and total protein values were lower in females than those of controls, but not in males. An increase in the heart and liver weights and a decrease in the thymus weight were also found. Histopathological alterations included an increase in the incidence of atrophy of the sternal marrow, atrophy, fibrosis and mast cell hyperplasia of the femoral marrow, atrophy of the white pulp and extramedullary hematopoiesis of the spleen, atrophy of the thymus, auricular hypertrophy of the heart, extramedullary hematopoiesis and centriacinar telangiectasis of the liver, follicular degeneration of the ovary, and inflammation of the tail. The major treatment-related effects were not recovered at the end of 2-week recovery period. There were no adverse effects in the low and middle dose groups of both genders. In the present experimental conditions, the target organs were determined to be bone marrow, blood cells, spleen, liver, thymus, and heart. The no-observed-adverse-effect level was considered to be 0.013 mg/kg/day for males and 0.018 mg/kg/day for females.     

The concept of conditional pharmacology and toxicology

The concept of conditional pharmacology as initially elucidated by Dr Michael Whitehouse and his colleagues from their studies of drug-disease interactions has broad import in a rational drug discovery and development programme. The concept can be extended to toxicology and thus can be viewed as encompassing virtually all means and methods of discovering and enhancing the efficacy, while reducing the toxicity of drugs and biologics. The concept involves employing the physiological or metabolic activity, genetic and/or molecular structure of the host, of the disease process and/or of the parasite to activate and target the drug or biologic, as well as to regulate and delimit its activity. Thus, the concept not only applies to the treatment of inflammatory diseases, but also to the treatment of neoplastic and infectious diseases, to facilitating wound healing, and is in fact an underlying assumption, and expected consequence, of successful gene therapy. The concept applies to clinical studies as well, arguing for more pharmacokinetic and chrono-pharmacological studies in the early phases of clinical testing and the inclusion in later-stage clinical trials of more diverse populations, as regards age, gender and ethnicity, if the indication warrants. Facilitating and monitoring compliance, post-as well as pre-market approval, also are critical components of the fully implemented concept.     

北方旱寒区冬油菜根系抗寒指标分析

为了研究北方旱寒区冬油菜根部生理特性与其抗寒性的相关性,对6个不同抗寒性冬油菜品种整个生育期根部的干物质积累、含水量、可溶性蛋白含量及相关保护性酶活性的变化进行了分析,并将各指标与越冬率进行了相关性分析,用与越冬率相关性显著、极显著的6个指标对冬油菜进行聚类分析。结果表明,降温前,各指标与越冬率的相关性均不显著;降温后,越冬率与可溶性蛋白含量、SOD活性极显著正相关,与POD、APX活性显著正相关,与根直径、根冠比、CAT活性正相关,与根含水量负相关;根据聚类分析结果,可将试验材料分为3类,第1类：07-G01,天油2号,天油4号,此类抗寒性弱,为耐寒性品种;第2类：上党,74-1,此类抗寒性一般,为中抗寒性品种;第3类：陇油6号,此类抗寒性强,为强抗寒性品种。由此推断,在北方旱寒区,冬油菜越冬前根直径大、根冠比高、根含水量低有利于冬油菜安全越冬;降温后,冬油菜可溶性蛋白、SOD、POD 、CAT和 APX酶活性值越高,其抗寒性越强。