天然药物化学学科的发展以及与相关学科的关系

天然药物不论是历史还是现在都为人类的健康发展做出了重要贡献。天然药物化学是运用现代科学理论与技术研究天然药物中化学成分的一门学科,其发展越来越受到科学家的重视。对天然药物化学学科的发展以及与相关学科的关系进行简要总结和分析,期望为青年科技工作者以启示。     

眷恋

在我们科技队伍里有这样一位化学专家: 他的“核磁共振”一书获得了一九七八年全国科学技术大会著作奖;在我国,他又是把“核磁共振”光谱应用到测定天然产物化学结构的先驱者。他与日本科学家同时在世界上率先研究出药物“一叶萩碱”的化学结构,并发表了学术论文,受到世界上同行、专家们的注意;在国内,他最早研究出“鹰爪”等几十种中草药的有效成分。他参与了国内许多天然产物的测定研究工作,为发展我国中草药事业做出了重要贡献。可是发表论文时,他都不肯留下自己的名字。     

天然药物化学研究与新药开发

自从有人类历史以来,天然药物一直是人类防病治病的主要来源。天然产物是自然界的生物历经千百万年的进化过程通过自然选择保留下来的二次代谢产物,具有化学多样性、生物多样性和类药性。临床上应用的许多药物都直接或间接来源于天然产物,如天然产物可作为药物半合成的前体物、药物化学合成的模板以及为药物设计提供了新的思路。但是在20世纪80～90年代,由于受高通量筛选和组合化学的影响,天然药物的研究一度进入低谷。近10年来天然药物化学在新药研发中的作用又重新受到科学家的重视,天然产物已成为发现治疗重大疾病的药物或重要先导化合物的主要源泉之一。现就天然药物化学在新药开发中的作用进行了回顾与总结,并对其前景进行了展望。     

海洋天然产物化学研究的历史回顾

近年来海洋天然产物越来越引起科学家们的注意，在辽阔的海洋中存在着众多超出想象的结构新颖的化合物。在药物研究中，海洋天然产物已成为发现重要先导药物的主要源泉。现将海洋天然产物化学的发展历史进行简要的回顾。     

药学研究专题

<正>在古代,几乎所有的药物均来源于天然的植物、动物、矿物或它们的加工品,这些药物叫做天然药物(natural medicines)。我国于1994年完成了天然药物资源普查,确认天然药物资源12 807种,是世界上天然药物种类最丰富的国家之一。天然药物与祖国传统医学一起构成了中华民族文化的瑰宝,对中华民族的繁衍昌盛做出了重要贡献。随着科学技术的进步,人们对天然药物的认识不断深化,回归自然的愿望和对天然药物的需求与日俱增,加之合成药开发周期长、投资大,因此,各国转而投向天然药物的研究,掀起了开发的     

端粒、端粒酶的发现和意义——2009年诺贝尔生理学或医学奖简介

2009年诺贝尔生理学或医学奖颁发给3名美国科学家,其主要贡献为解决了生物学研究领域中一个重大问题,即细胞分裂过程中,染色体如何完整复制,它们是如何受到保护而免于降解?Elizabeth H.Blackburn和Jack W.Szostak发现染色体末端的端粒DNA序列能保护染色体不被降解;Carol W.Greider和Elizabeth H.Blackburn鉴定出合成端粒DNA的酶——端粒酶。这些发现为推动衰老及肿瘤等领域的研究做出了巨大贡献。     

拯救生命,医学科学的永恒使命——2008年诺贝尔生理学或医学奖简介

2008年10月6日瑞典卡罗林斯卡医学院将2008年诺贝尔生理学或医学奖授予发现HPV与宫颈癌相关性的德国科学家Harald zur Hausen及发现HIV的两名法国科学家Franc,oise Barré-Sinoussi和Luc Montagnier,以表彰其在病毒学领域所做出的杰出贡献。本文从3位获奖科学家的简介、主要贡献、HPV和HIV发现的重大意义等方面进行综述。     

天然药物化学史话：紫杉醇

癌症是威胁人类健康的第二大疾病,征服癌症是科学家们的一大梦想。天然产物一直是发现新药和药物先导化合物的重要途径之一,很多抗癌药物都是直接或间接来源于天然产物。紫杉醇是目前已发现的最优秀的天然抗癌药物,在临床上已经广泛用于乳腺癌、卵巢癌和部分头颈癌和肺癌的治疗。紫杉醇作为一个具有抗癌活性的二萜生物碱类化合物,其新颖复杂的化学结构、广泛而显著的生物活性、全新独特的作用机制、奇缺的自然资源使其受到了植物学家、化学家、药理学家、分子生物学家的极大青睐,使其成为20世纪下半叶举世瞩目的抗癌明星和研究重点,包括寻找新的生物资源、化学全合成、半合成、衍生物制备、生物转化、生物合成、生物工程、构-效关系研究、作用机制研究、药理学和药效学等研究。2011年是发现紫杉醇结构40周年,对紫杉醇发现的曲折历史过程进行回顾和总结,以纪念这一伟大发现并纪念为紫杉醇的研究与第二代紫杉醇的开发作出贡献的科学家。     

红景天属植物研究

红景天属植物的抗疲劳、抗缺氧、抗衰老等多方面的药理作用正受到人们的广泛关注.我国红景天天然药源丰富,人工栽培技术相对成熟,发展前景十分广阔.到目前为止,已经进行了大量的药理作用研究,作用机理较清楚,但其作为保健品上市的较多,尚需进一步开发,作为药物应用于临床.     

生物碱类成分对阿尔茨海默症潜在治疗的研究进展

近年来,虽关于阿尔茨海默症（Alzheimer’s disease,AD）的研究越来越深入,但其作用机制尚未明确,并且合成药物的临床效果并不显著,所以天然药物有效成分的开发成为一大热点。天然药物生物碱类在自然界中广泛存在,因取材方便且具有较多生物活性,如抗衰老、抗肿瘤、保护神经等,对其研究越来越多。该文就天然植物中的生物碱成分对AD 的潜在治疗进行综述,为AD 的治疗和研究提供理论依据。     

Value of D-Dimers in patients with acute aortic dissection

Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P ＜ 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (＞0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P ＜0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P ＜ 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.     

Research of combined liver-kidney transplantation model in rats

Objective： To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods： SD rats served as both donors and recipients. 4℃ sodium lactate Ringer＇s was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava （IVC） inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results： Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion： This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.     

BLOOD PRESSURE CHANGE WITH AGE IN SALT-SENSITIVE TEENAGERS

Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P＜ 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P＜ 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.     

Development on Adjustable Calibration Marker for Shock Wave Focus

Shock wave lithotripsy （SWL） is a treatment of choice for upper urinary stones. However, this procedure is inappropriate for obese patients because the focus is often unable to reach the target owing to the limited focal distance in shock wave source. Although treating such patients in a blast path may increase the application length of shock wave source, it＇s difficult to find this path on the lithotripter monitor. For this reason, we invented an adjustable calibration marker in order to set an effective focus in the shock wave hath.     

Study on the TCM Pathogenesis of Angiopathic Complications of Type II Diabetes

Excess production of reactive oxygen species(ROS)of mitochondrion mediated by hyperglycemia is the common pathogenesis of angiopathic complications of diabetes.TCM holds that the damp from the dysfunction of spleen.kidney and liver is the causative factor of complications of diabetes.This is similar to the mechanism of Ros resulting in angiopathic complications of diabetes.When the angiopathic complications of type II diabetes mellitus(T2DM)are difierentiated as caused by turbid damp in TCM can be explained as ROS.Since the obstruction of pathogenic damp in channels and collaterals is said to be the main pathogenesis,the treating principle should be dissolving the damp to remove the obstruction.     

Leptin, Ghrelin and TNF-α before and after Hypo-caloric Traditional Chinese Diet and Auricular Acupuncture

INTRODUCTION Obesity is a complex emergent problem, which can be possibly solved not only by the diet but also by the life style and promotion of a constant physical exercise. 1, 2 No doubt careful attentions must be given to the nutritional condition of obese people, the dietary habits, the somatic build (i.e. distribution of fat mass) and the organic functions linked to formation of the fat mass. All the parameters should be constantly monitored before, during and after a diet treatment. 3, 4, 5     

Relationship between Dysglycemia and Carotid Atherosclerosis in Tibetan Population

People with dysglycemia are at high risk for atherosclerotic diseases. This study aims at investigating the atherosclerotic vascular damage in dysglycemia and its metabolic origin in Tibetan population.     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

安心颗粒对急诊经皮冠状动脉介入术后生活质量影响的研究

目的：评价使用安心颗粒对急诊经皮冠状动脉介入术（PPCI）术后生活质量的影响.方法：将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组（术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次）和对照组（仅接受基础药物治疗）.所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表（MIDAS）、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果：入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异（P＞0.05）;出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低（P＜0.05）;组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低（P＜0.05）.两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血（P＞0.05）.两组发生轻度血小板减少症的患者数比较无差异（P＞0.05）.结论：PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.     

CLINICAL SIGNIFICANCE OF SERUM CYTOKINES IL-1β,sIL-2R,IL-6,TNF-α,AND IFN-v IN ACUTE CORONARY SYNDROME

Objectives To explore serum cytokines levels (including IL-1 β, sIL-2R, IL-6, TNF-α, and IFN-v) and their significance in patients with acute coronary syndrome (ACS) and the subsequent follow-ups, with attempt to estimate the role of various serum inflammatory markers in the diagnosis and assessment of ACS.Methods The study population include 40 patients with acute myocardial infarction (AMI), 40 patients with unstable angina pectoris (UAP), and 40 controls. Among the 80 patients, 60 patients attended a follow up 4 months later. Serum inflammatory markers including IL-1 β, sIL-2R, IL-6, TNF-α, and IFN-v were measured by enzyme linked immunosorbent assay.Results Serum IL- 1 β, sIL-2R, IL-6, TNF-α were significantly higher in AMI group or UAP group compared to the control group and became significantly lower 4 months later in the follow-up patients. Serum levels of IFN-v shows no significant difference between AMI group or UAP group and controls, also showing no significant change when measured in follow up patients. There was no correlation between serum creatine kinase-MB isoenzyme levels and serum inflammatory markers either in UAP or AMI group. Furthermore, when divided into two subgroups using Wagner's QRS scoring system in the AMI group, there is no difference of each serum inflammatory marker between ≤ 6 scores group and ＞ 6 scores group.Conclusion Serum levels of certain inflammatory markers may have some diagnostic value for ACS, and can be a useful marker reflecting disease stability.