“藏茵陈”的基原植物和药用亲缘学

详细比较藏药"藏茵陈"基原植物川西獐牙菜及其混淆品(代用品)抱茎獐牙菜、紫红獐牙菜、四数獐牙菜、红直獐牙菜、大籽獐牙菜、狭叶獐牙菜和椭圆叶花锚的外部形态特征及化学成分,澄清了这一类群在分类上的混乱,发现川西獐牙菜与紫红獐牙菜在习性,花部特征,种子形态和化学成分组成等方面相似性最高,印证了核基因ITS序列的结果。同时分析"藏茵陈"混淆的原因是多种来源和形态相似性造成的,讨论了"藏茵陈"鉴定的方法。通过对獐牙菜属系统关系的分析,提出紫红獐牙菜作为川西獐牙菜替代品的理论依据。     

獐芽菜属植物的药用民族植物学研究

獐牙菜属药用植物作为我国传统药物的重要来源之一,有些品种已被纳入卫生部标准藏药和国家中成药标准汇编内科肝胆分册。针对獐牙菜属药用植物的研究现状,本文从药用民族植物学角度对獐芽菜属药用植物资源的种类和分布、民族应用、化学成分、药理作用、临床应用及开发等几个方面进行了分析和总结,探讨獐牙菜属植物资源的开发利用现状并提出一些建议。     

基于不同DNA序列对四数獐牙菜系统位置分析

以扁蕾属植物为外类群,基于trnL-trnF序列、rpl16序列以及 ITS序列,采用最大简约法对四数獐牙菜的系统位置进行了分析.结果显示:尽管在ITS系统发育树、trnL-trnF系统发育树和rpl16系统发育树中所用的种和数量有所不同,所得到的3种系统发育树的拓扑结构也不一致,但四数獐牙菜的系统位置在3种系统发育树中的结果基本一致.在trnL-trnF系统发育树中,四数獐牙菜与花锚属的H.elliptica、H.brevicornis和H.weddelliana形成了一个单系群;而在ITS和rpl16系统发育树中,四数獐牙菜与歧散獐牙菜先聚在一起,再与花锚属的植物聚为一支支持率较高的单系支.研究表明,四数獐牙菜与Anagalidium属的歧散獐牙菜的亲缘关系最近,其次是与花锚属的植物,而与獐牙菜属植物的亲缘关系较远.本实验系统发育的结果支持将四数獐牙菜从獐牙菜属中分出而归入Anagalidium属的观点.     

３种獐牙菜属植物花蜜腺的发育解剖学研究

獐牙菜属的红直獐牙菜、抱茎獐牙菜和四数獐牙菜３种植物花蜜腺都属花被蜜腺,其结构相似,均由分泌表皮和产蜜组织组成,为结构蜜腺,是花冠其部薄壁组织恢复分和能力形成的,分泌表皮无气孔器,原蜜汁由蜜腺周围的维管束提供,经产蜜组织加工后,由分泌表皮外薄的角质层泌出。四数獐牙菜花蜜腺裸露,凸起,而另２化蜜腺凹限为囊状、;红直獐牙菜为脱落蜜腺、而抱茎獐牙菜和四数獐牙菜为宿存蜜腺,其花蜜腺的性状基本印证了３种獐牙菜属植物的系统位置。     

7种獐牙菜属药用植物形态组织学研究

本文报道了水灵芝(Swertia davidii Franch)、双斑獐牙菜(S.bimaculata(S.et Z.)HK.f.Thoms)、江浙獐牙菜(S.hickinii Burk)、贵州獐牙菜(S.koui-tchensis Franch)、大籽獐牙菜(S.macrosperma C.B.Clarke)、翼梗獐牙菜(S.nervosa Wall)、紫红獐牙菜(S.punicea Hemsl.)等7种獐牙菜属药用植物的药材性状、根茎叶的显微构造和解离组织及粉末特征,为合理开发和利用这一药物资源提供了鉴别依据,也为獐牙菜属植物的形态组织学研究提供了有价值的资料。     

7种獐牙菜属植物花粉形态的研究

本文应用光学显微镜和扫描电子显微镜,对龙胆科(Gentianaceae)獐牙菜属(Swertia L.)7种植物(獐牙菜Swertia bimaculata(S.et z.)HK.f.Thoms.、水灵芝S.davidii Franch.、江浙獐牙菜S.hickinii Burkill.、贵州獐牙菜S.kouitchensisFranch.、大籽獐牙菜S.macrosperma C.B.Clarke.、翼梗獐牙菜S.nervosa Wall.、紫红獐牙菜S.punicea Hemsl.)的花粉形态作了比较观察,找出了它们的鉴别特征,阐明了獐牙菜属植物花粉的外壁外层表面纹饰的三种类型为条纹—网状、网状和瘤状雕纹。     

植物（口山）酮类化合物的波谱特征

结合大量文献和实验工作 ,对植物 (主要是獐牙菜属 )口山酮类化合物的波谱特征进行总结和归纳。     

植物酮类化合物的波谱特征

结合大量文献和实验工作,对植物(主要是獐牙菜属)(口山)酮类化合物的波谱特征进行总结和归纳.     

川西獐牙菜乙酸乙酯部位的化学成分及活性研究

本文对川西獐牙菜Swertia mussotii Franch的化学成分及抗肿瘤活性进行研究。通过采用多种柱层析及半制备等方法对川西獐牙菜乙酸乙酯部位进行分离纯化得到10个化合物;利用其理化性质并结合现代波谱分析方法鉴定化合物的结构;分别为1,5,8-trihydroxy-3-methoxyxanthone(1)、1,7-dihydroxy-3,8-dimethoxyxanthone(2)、1-hydroxy-3,5,8-trimethoxyxanthone(3)、1-hydroxy-3,7,8-trimethoxyxanthone(4)、4,6,8-trihydroxy-1,2,3,5-tetramethoxyxanthone(5)、Luteolin(6)、Isoorientin(7)、Isovitexin(8)、Swertiamarin(9)、Gentiopicroside(10),其中化合物5为首次从龙胆科植物中分离得到,化合物6、8为首次从川西獐牙菜中分离得到。选用黑色素瘤B16细胞模型、神经胶质瘤C6细胞模型和肝癌HepG2细胞模型进行细胞毒性实验,结果表明,化合物5对神经胶质瘤C6细胞表现出相对明显的抑制活性,其IC_(50)值达8. 9μM。     

獐牙菜亚族植物的系统发育分析

獐牙菜亚族(subtribe Swertiinae)是龙胆科(Gentianaceae)中分类处理较困难的一个亚族。为探讨该亚族各属之间和属内的系统关系,选取了该亚族86种及变种,采用ML和BI方法对样本的叶绿体基因mat K和rbc L片段进行分析,构建了该亚族的系统发育树,用马尔科夫蒙特卡洛算法(MCMC)的分子序列贝叶斯分析推算了该亚族的关键演化时间点。结果显示:①龙胆亚族和獐牙菜亚族各自为单系,且互为姐妹类群;②獐牙菜属、假龙胆属、肋柱花属和喉毛花属均不是单系群,各属的种在系统发育树上互有交叉,特别是獐牙菜属的多个种分别聚到不同的支上,与其它属是并系关系;③獐牙菜亚族49个种在约4 Ma开始形成;④分子数据支持何廷农分类系统对于獐牙菜亚属和多枝亚属的属间划分,部分支持多枝亚属下多枝组和宽丝组的划分;⑤异型花属、獐牙菜属、假龙胆属、喉毛花和肋柱花属的属间分类以及獐牙菜属肉根亚属密花组的系统位置仍需进一步讨论。     

Septum-lesioned rats in pharmacological investigations: a re-evaluation.

An objective and quantitative method has been developed for measuring the hyper-reactivity of septum-lesioned rats. Twenty drugs belonging to various classes have been investigated as to their influence on this hyper-reactivity. Seventeen compounds inhibited septal hyperreactivity. One drug (methylphenidate) augmented it, while metamphetamine and physostigmine were ineffective. It has been concluded that the use of septal rats in pharmacological investigations does not fulfil expectations. The model cannot differentiate between depressants of various kinds, antidepressants, narcotics or central cholinolytics any more than do the much more simple procedures routinely used in pharmacological laboratories.     

紫菀属植物化学成分及药理作用研究进展

紫菀属(Aster L.)植物为多年生草本、亚灌木或灌木,该属植物中紫菀(Aster tataricus)为常用中药,具有润肺下气、止咳祛痰之功效,主治气逆咳嗽、痰吐不利、肺虚久咳、痰中带血等症,是临床常用的润肺祛痰止咳药。该属所含化学成分较丰富,已对该属中16种植物做过化学成分研究,分离出的化合物124个,其类型有各种萜类及其苷、肽类、黄酮类、蒽醌类、甾醇类、香豆素、有机酸类及挥发油等。对国内外有关该属植物的化学成分、药理作用和临床应用的最新研究进行了综述,为该药用植物资源的进一步研究和开发利用提供依据。     

Separation and isolation methods for analysis of the active principles of Sho-saiko-to (SST) oriental medicine

Sho-saiko-to (SST) was introduced into Japan as an oriental classical medicine from China approximately 1500 years ago, and it is currently the most representative Kampo medicine (traditional Japanese medicine). SST is manufactured in Japan as an ethical drug on a modern industrial scale in which the quality of ingredients is standardized with Good Manufacturing Practices (GMP) regulation. SST is widely used for the treatment of chronic hepatitis. Experimental and clinical studies including multi-center, placebo-controlled, double-blind studies have demonstrated the various pharmacological effects of SST. SST is prepared from the hot water extraction of seven raw materials, therefore many kinds of constituents are included. Three-dimensional (3D) HPLC analysis is useful for obtaining many kinds of constituents, especially low molecular ultraviolet (UV) quenching compounds, contained in SST as well as its fractions. Fingerprint pattern provided by 3D HPLC analysis makes possible to identify the overall-viewing of SST. Databases of UV spectra of the components of medicinal herbs obtained by reversed-phase (RP) HPLC using a photodiode array (PDA) and fingerprint patterns of crude drugs made by 3D HPLC analysis facilitate the identification, analysis and quality of herbal drugs. Studies using both PDA HPLC and an amino acid analysis with a fluorometric detector have found that SST contains fifteen major low molecular compounds (i.e. baicalin, wogonin-7-O-glucuronide, liquiritin, their three aglycons, liquiritin apioside, glycyrrhizin, saikosaponin b1, saikosaponin b2, ginsenoside Rg1, ginsenoside Rb1, (6)-gingerol, (6)-shogaol and arginine). These compounds have various pharmacological actions, and are assumed to be responsible, at least partly, for the pharmacological effects of SST. Although there have only been a few investigations on high molecular compounds with pharmacological actions contained in SST, several kinds of polysaccharides have been isolated from constituent herbs of SST. This review paper summarizes analytical methods of separation, isolation and identification of compounds with biological activities from SST, which is a mixture drug of medicinal herbs. Accordingly, this paper would not focus on methods of separation, isolation and analysis of particular compounds from each constituent herb of SST.     

TRPM8 ion channel ligands for new therapeutic applications and as probes to study menthol pharmacology

Since the discovery of the TRPM8 gene in 2001, the TRPM8 ion channel, better known as the ‘cold receptor’ has been the target of a significant effort from the pharmaceutical industry to produce small-molecule agonists and antagonists of this receptor for various therapeutic applications ranging from cancer and urological disorders to the treatment of cold hypersensitivity and pain. Recently, a number of clinical studies have implicated menthol, the natural ligand of TRPM8, in facilitating and maintaining cigarette smoking behavior, possibly through its counter-irritant effects. However, a pharmacological link between menthol's action via TRPM8 and nicotine addiction has not been yet been investigated. This review gives an overview of reported small-molecule TRPM8 agonists and antagonists and discusses their efficacy in models of various disease states. These compounds may be useful pharmacological tools to investigate the effect of menthol on nicotine addiction.     

A call for using natural compounds in the development of new antimalarial treatments - an introduction

Natural compounds, mostly from plants, have been the mainstay of traditional medicine for thousands of years. They have also been the source of lead compounds for modern medicine, but the extent of mining of natural compounds for such leads decreased during the second half of the 20th century. The advantage of natural compounds for the development of drugs derives from their innate affinity for biological receptors. Natural compounds have provided the best anti-malarials known to date. Recent surveys have identified many extracts of various organisms (mostly plants) as having antiplasmodial activity. Huge libraries of fractionated natural compounds have been screened with impressive hit rates. Importantly, many cases are known where the crude biological extract is more efficient pharmacologically than the most active purified compound from this extract. This could be due to synergism with other compounds present in the extract, that as such have no pharmacological activity. Indeed, such compounds are best screened by cell-based assay where all potential targets in the cell are probed and possible synergies identified. Traditional medicine uses crude extracts. These have often been shown to provide many concoctions that deal better with the overall disease condition than with the causative agent itself. Traditional medicines are used by ~80 % of Africans as a first response to ailment. Many of the traditional medicines have demonstrable anti-plasmodial activities. It is suggested that rigorous evaluation of traditional medicines involving controlled clinical trials in parallel with agronomical development for more reproducible levels of active compounds could improve the availability of drugs at an acceptable cost and a source of income in malaria endemic countries.     

Sigma receptors. Putative links between nervous, endocrine and immune systems.

The sigma receptor is a neuronal substrate that binds several psychoactive compounds. These include cocaine, some steroids, dextromethorphan, phencyclidine (PCP), and benzomorphans such as pentazocine and N-allyl-normatezocine (SKF-10047). Many newer atypical antipsychotic drugs also bind to the sigma receptor. The sigma receptor, however, is not the PCP receptor. The sigma receptor exists in the central nervous system, endocrine, immune and certain peripheral tissues. Progesterone and certain steroids have been shown to represent endogenous ligands for the sigma receptor. The sigma receptor resides likely in the nonsynaptic region of the plasma membrane. The sigma receptor exists in two forms: high-affinity and low-affinity. The solubilized sigma receptor retains all of the pharmacological characteristics of a membrane-bound receptor. A major physiological role of the sigma receptor may involve the modulation of a tonic potassium channel.     

Genetic and pharmacological aspects of histamine H3 receptor heterogeneity

Histaminergic H3 receptors modulate the release of neurotransmitters within the CNS and periphery. Ligands for these receptors have potential clinical utility in a variety of disease states. However, the pharmacological characteristics of these receptors have been enigmatic for more than a decade because of the diversity of pharmacological effects observed with the limited number of heretofore-available compounds. Recent cloning of the H3 receptor has revealed interspecies differences in the protein sequences in key regions, the existence of splice variants that differ in composition between species, and potential differences in signal transduction processes between either different tissues and/or species. This review attempts to summarize these findings within the context of the molecular biological and pharmacological data accumulated to date. Also, we suggest a nomenclature strategy to reduce potential confusion that has arisen from different naming systems used by various investigators. While some facets of this genetic and pharmacological diversity help to rationalize various aspects of H3 receptor heterogeneity, there remains an insufficient repertoire of selective ligands, assays, or other measures to completely resolve all components of this diversity. The promise of newly available tools to further explore H3 receptor function may provide the insight to bring the promised clinical potential of H3 receptor ligands to realization.     

Chemical constituents and bioactivities of starfish

Starfish have been the research topic in many chemical and pharmacological laboratories due to their complex secondary metabolites and diverse bioactivities. The aim of this review is to provide an up-to-date review on the chemistry and bioactivity of compounds isolated from all kinds of starfish to illustrate the chemodiversity and biological significance of these constituents, along with their geographical distribution where it is discernible.     

Isoflavonoids, genistein, psi-tectorigenin, and orobol, increase cytoplasmic free calcium in isolated rat hepatocytes.

Isoflavonoid compounds, genistein, psi-tectorigenin and orobol have been implicated as inhibitors of tyrosine-specific protein kinase and phosphatidylinositol turnover. These compounds have been frequently used as a pharmacological tool to assess signal transduction pathways in various cell systems. In the course of analyzing signaling pathways in rat hepatocytes, we obtained an unexpected finding that these compounds transiently increase cytoplasmic free calcium. Since the Ca2+ mobilizing effect was observed in 1 microM calcium containing buffer, the source of the Ca2+ may be intracellular stores. Thus, when interpreting data obtained using these compounds, caution is needed.