Genotoxicity and Safety Pharmacology Studies of Indole Alkaloids Extract from Leaves of Alstonia scholaris (L.) R. Br.

Indole alkaloids extract(IAAS)was prepared from leaves of Alstonia scholaris(L.)R.Br.,an evergreen tropical plant widely distributed throughout the world.This plant has been used historically by the Dai ethnic people of China to treat respiratory diseases.This study evaluated the genotoxicity and safety pharmacology of IAAS to support clinical use.The bacterial reverse mutation(Ames)test,in vitro mammalian chromosomal aberration test,and in vivo mammalian erythrocyte micronucleus(MN)test were performed to evaluate genotoxicity.Mice were administered IAAS(240,480,or 960 mg/kg bw)once orally to observe adverse central nervous system effects.Furthermore,beagle dogs were administered IAAS(10,30,60 mg/kg bw)once via the duodenum to evaluate its effects on the cardiovascular and respiratory systems.IAAS with or without S9-induced metabolic activation showed no genotoxicity in the Ames test up to 500μg/plate,in the mammalian chromosomal aberration test up to 710μg/mL,or in the MN test up to 800 mg/kg bw.No abnormal neurobehavioral effects were observed in mice following treatment with up to 960 mg/kg bw of IAAS.Moreover,blood pressure,heart rate,electrocardiogram parameters,and depth and rate of breathing in anesthetized beagle dogs did not differ among the IAAS doses or from the vehicle group.These data indicated that IAAS did not induce mutagenicity,clastogenicity,or genotoxicity,and no pharmaco-toxicological effects were observed in the respiratory,cardiovascular,or central nervous systems.Our results increased understanding of safety considerations associated with IAAS,and may indicate that IAAS is a possible drug candidate.

Two new steroidal alkaloids from Veratrum nigrum var.ussuriense

Two new steroidal alkaloids, veraussines A （1） and B （2） were isolated from the roots and rhizomes of Veratrum nigrum var. ussuriense. Their structures were determined as N-（ethoxycarbonyl）- 1 α,2β,3α, 15α-tetrahydroxy-5fl-jervanin- 12-en- 11 -one （1） and N-（methoxycarbonyl）-1α,2β,3α,15α-tetrahydroxy-5/3-jervanin-12-en-1 l-one （2） by spectroscopic analysis.

Inhibitory effects of Veratrum nigrum L. Var. ussurience Nakai alkaloids on the hypertrophy of cardiomyocytes from neonatal rat

Objective To examine the effects of Veratrum nigrum L.Var.ussurience Nakai alkaloids(VnA)on angiotensin Ⅱ(AngⅡ)-induced cardiomyocyte hypertrophy and to explore its possible mechanism.Methods The cadiocytes were induced by AngⅡ to set up myocardial hypertrophy model,the animals were divided into six groups according to the different treatments:control group,model group,positive control group,VnA group(low,middle and high dose).The cell protein content,the cell diameter and the expression of calcineurin(CaN)were measured respectively by BCA method,the micrometer and immunofluorescence analysis.Results VnA(middle and high dose)and Captopril inhibited significantly the increase in the protein content induced by AngⅡ(P<0.01).VnA and Captopril inhibited significantly the increase in the diameters induced by AngⅡ(P<0.01).By immunofluorescence analysis,the expression of calcineurin(CaN)was obviously increased in the AngⅡ-induced model group.VnA decreased the expression of CaN significantly.Conclusions VnA could inhibit the cardiomyocyte hypertrophy induced by AngⅡ significantly in a dose-dependent manner.The possible mechanism may be related to the inhibition of CaN expression.

A review on medicinal importance,pharmacological activity and bioanalytical aspects of beta-carboline alkaloid "Harmine"

Harmine,a beta-carboline alkaloid,is widely distributed in the plants,marine creatures,insects, mammalians as well as in human tissues and body fluids.Harmine was originally isolated from seeds of Peganum harmal in 1847 having a core indole structure and a pyridine ring.Harmine has various types of pharmacological activities such as antimicrobial,antifungal,antitumor,cytotoxic, antiplasmodial,antioxidaant,antimutagenic,antigenotoxic and hallucinogenic properties.It acts on gamma-aminobutyric acid type A and monoamine oxidase A or B receptor,enhances insulin sensitivity and also produces vasorelaxant effect.Harmine prevents bone loss by suppressing osteoclastogenesis.The current review gives an overview on pharmacological activity and analytical techniques of harmine,which may be useful for researcheres to explore the hidden potential of harmine and and will also help in developing new drugs for the treatment of various diseases.

Study of Total Alkaloids from Rhizoma Coptis Chinensis on Experimental Gastric Ulcers

Objective： To study the effects of total alkaloids （TA） extracted from Rhizoma Coptis Chinensis on experimental gastric ulcer models. Methods： Four kinds of experimental ulcer models were established respectively by water-immersion stress, intragastric ethanol, acetic acid erosion, and pylorus ligation. The anti-ulcer effects of TA were evaluated, and compared with that of berberine （Bet） and cimetidine （Oim）. Results： TA showed significant inhibitory effects on ulcerative formation induced by water-immersion stress, intragastric ethanol, and pylorus l igation in dose-dependent manner, and showed therapeutic effect on acetic acid erosion-inducing ulcer, in comparison with the control group. The anti-ulcer activity of Bet was less than TA containing equal content of Bet. TA significantly reduced the free acidity, total acidity and total acid output, but didn＇t affect the gastric juice volume, gastric pepsin activity, adherent mucus quantity of stomach wall and free mucus dissolving in gastric juice. The suppressive activities of TA on gastric acid secretion didn＇t occur when it was administered into dodecadactylon at a dose of 360 mg/kg wt. Moreover, when compared with Oim, the inhibitory effect of TA on gastric acid secretion isn＇t proportional to the inhibitory effects on the formation of the 4 kinds of experimental ulcers. Conclusion： TA is a potent candidate in therapeutic drugs for treating gastric ulcer. Its anti-ulcer effective components and mechanism is not only related to Bet and inhibition of gastric acid, but also to other ingredients of TA and mechanism so far unknown.

RETRACTED:Exploring the Mechanism of Wu Ling San plus Flavor for the Treatment of Diabetic Macular Edema Based on Network Pharmacology and Molecular Docking Techniques

Short Retraction Notice The paper does not meet the standards of “Chinese Medicine ". This article has been retracted to straighten the academic record. In making this decision the Editorial Board follows COPE's Retraction Guidelines. The aim is to promote the circulation of scientific research by offering an ideal research publication platform with due consideration of internationally accepted standards on publication ethics. The Editorial Board would like to extend its sincere apologies for any inconvenience this retraction may have caused. Editor guiding this retraction: Prof. Maythem Saeed (EiC of CM) The full retraction notice in PDF is preceding the original paper, which is marked "RETRACTED".

莨菪烷类药物应用于微循环障碍的研究进展

山莨菪、洋金花等含莨菪烷类小分子的中药在我国应用已有2000余年的历史。莨菪烷类药物属M胆碱受体拮抗剂,是一类可改善微循环障碍的临床常用治疗性药物。本文综述了莨菪烷类药物的药理作用、药代动力学、毒理及临床应用于微循环障碍的研究进展,以期为深入解析莨菪烷类药物与微循环障碍性疾病的关系以及莨菪烷类药物的临床应用提供依据。

半夏化学成分、药理作用研究进展及其质量标志物预测分析

半夏始载于《神农本草经》,味多辛苦,性多温燥,有毒,主归脾、胃、肺经,是我国常见的大宗药材,具有燥湿化痰、降逆止呕、消痞散结之功,常配伍于中药方剂作为君药使用。半夏来源广泛,成分丰富,药效显著,在我国临床治疗史上具有广阔前景。该文以质量标志物(Q-Marker)理论为指导,结合国内外文献报道,归纳总结了半夏化学成分和药理作用,从亲缘关系、传统药性、化学成分有效性、成分可测性和不同配伍环境等方面对半夏进行Q-Marker的预测分析,以期为半夏建立更科学、更合理的质量评价体系,为其进一步综合利用提供参考。

酸枣仁的化学成分、药理作用和临床应用研究进展

酸枣仁主要含有皂苷类、黄酮类、生物碱类、脂肪酸类等成分,具有镇静催眠、抗焦虑、抗抑郁、保护神经、保护心脑血管、保肝、抗氧化等多种活性,广泛应用于医药、食品、保健食品等领域。本文通过查阅文献,系统整理归纳了酸枣仁的化学成分、药理作用及临床应用,以期为酸枣仁资源的可持续开发和合理使用提供理论指导。

钩藤的药理作用及临床应用研究进展

钩藤(Uncaria rhynchophylla)是广西区域特色药材品种之一,具有息风定惊、清热平肝的功效,药用历史悠久。钩藤生物碱是钩藤的主要药效成分,对缓解药物成瘾、阿尔茨海默症、高血压等疾病具有显著功效,其方药天麻钩藤饮、复方钩藤降压片等在临床上广泛应用。随着现代医学研究技术的进步,钩藤生物碱及其方药的治病机理正在不断被发现。本文收集近十年钩藤相关研究文献,以钩藤的药效物质为基础,总结钩藤生物碱及其方药的药理研究成果,分析钩藤的临床应用情况,以期为钩藤的新药研发或新应用提供理论借鉴。

基于网络药理学及分子对接探究荷叶生物碱抗高尿酸血症的作用机制

目的:运用网络药理学及分子对接分析荷叶生物碱类化合物治疗高尿酸血症的作用机制。方法:通过数据库检索获取荷叶生物碱类化合物作用靶点以及高尿酸血症靶点,通过Cytoscape 3.8.0建立荷叶生物碱类化合物的“成分-疾病-靶点”网络,利用微生信平台进行基因本体论(GO)分析和京都基因与基因组百科全书(KEGG)通路分析,并将核心靶点与关键成分进行分子对接验证。结果:通过文献检索获取27种荷叶生物碱类化合物信息,包括荷叶碱、衡州乌药碱、莲心碱等,预测获得对应靶点337个,高尿酸血症相关靶点926个,关键靶点57个。荷叶生物碱类化合物治疗高尿酸血症的作用机制主要涉及GAPDH、STAT3、JUN、CASP3、PTGS2、XDH、MAPK1等靶基因,这些基因主要通过AGE-RAGE信号通路、PD-1通路、TNF信号通路、IL-17信号通路以及p53信号通路等调控蛋白表达发挥作用。分子对接结果显示化合物与分子靶点对接结果良好,荷叶碱、衡州乌药碱、莲心碱均可与关键靶点自发结合,其中莲心碱与蛋白PTGS2、JUN可形成最稳定结构,结合能可达-9.3 kcal/mol。结论:本研究预测荷叶生物碱类化合物通过调控多靶点、多通路发挥改善高尿酸血症的作用,为荷叶生物碱类化合物治疗高尿酸血症的分子研究提供了科学依据。

吴茱萸生物碱类化学成分临床应用及现代药理药效研究进展

生物碱类化学成分是中药吴茱萸最主要的活性成分,临床应用广泛,药用价值高。现代药理药效研究表明,其总生物碱对心血管系统、消化系统和神经系统具有一定的保护作用,而且也具有抗菌、抗炎和抗肿瘤等作用。吴茱萸中生物碱类化合物的相关研究现已经成为吴茱萸研究的热点,尤其是对吴茱萸碱、吴茱萸次碱、去氢吴茱萸碱的研究取得了较大进展。对吴茱萸中物碱类化学成分、临床应用及现代药理药效等方面的内容进行归纳总结,旨在为吴茱萸中生物碱类化合物的研究、开发与利用提供参考。

蒙自藜芦中的甾体生物碱及抗炎活性研究

目的研究云南药用披麻草植物资源蒙自藜芦中的甾体生物碱成分及其抗炎活性。方法采用硅胶柱色谱法、反相柱色谱法、凝胶柱色谱法和高效液相色谱法(HPLC)制备等多种分离手段对蒙自藜芦根和根茎的乙醇提取部分进行分离,根据波谱数据确定所分离得到的甾体生物碱类化合物的结构,对这些化合物进行抗炎活性初步研究。结果从蒙自藜芦中分离出了8个甾体生物碱,并通过波谱学数据和理化性质分别鉴定为3-当归酰基棋盘花胺(1)、3-藜芦酰基计明碱(2)、介芬胺(3)、藜芦嗪(4)、vermitaline(5)、3-当归酰基棋盘花胺-β-N-氧化物(6)、环杷明(7)、藜芦胺(8)。化合物2、4、7为首次从该植物中分离得到。其中,化合物8对脂多糖(LPS)诱导的一氧化氮产生有明显的抑制作用,在50μmol·L^(-1);时一氧化氮生成抑制率为(47.01±0.41)%,且能够降低炎症因子环氧合酶(COX-2)和诱导型-氧化氮合酶(iNOS)的蛋白表达水平,并呈剂量依赖性。结论本研究可为蒙自藜芦的抗炎活性物质基础及开发利用提供科学依据。

紫堇属植物苄基异喹啉类成分研究进展

全球紫堇属Corydalis约400余种,广泛分布于北温带和非洲南部地区。在我国,该属多种物种作为民间用药具有上千年历史。紫堇属植物富含异喹啉生物碱,对该类成分通常以回流、超声加热、湿法超微粉碎法和酶解辅助技术等方法提取,并使用溶剂分离法、硅胶柱色谱法、反向填料柱色谱法、HPLC法、离子交换树脂法、高效逆流色谱法和活性引导技术等方法进行分离纯化法。紫堇属生物碱有效部位或单体成分都具有较强药理活性,现代药理学表明,该属所含生物碱类成分对心脑血管、抗肿瘤、镇痛、消炎、保肝和抗血小板凝集等均具有显著的药理作用。本文对已报道的紫堇属植物生物碱类成分的结构类型、特征、药理作用以及提取分离方法研究进行综述,为植物药用化学成分富集和安全用药提供借鉴。

延胡索乙素的药理作用研究进展

延胡索是一种常见的中药材,具有活血散瘀、理气止痛的功效。在临床治疗上,延胡索作为一种常见的镇痛药,具有镇痛及催眠作用,常用于内科病痛(如消化性溃疡痛)、产前阵痛、产后子宫缩痛、月经痛、头痛及失眠等症。延胡索的化学成分主要包括生物碱类、萜类、氨基酸类、多糖类、有机酸类及挥发油类等。延胡索乙素是延胡索的主要有效化学成分,对中枢神经系统、心血管系统以及消化系统具有显著作用,可用于止痛镇静、抗药物成瘾、抗心律失常、抗肿瘤、改善血流动力学及降血脂等。本文对延胡索乙素的药理进行总结,为进一步研究此药材提供参考。

An overview on the chemistry, pharmacology and anticancer properties of tetrandrine and fangchinoline(alkaloids) from Stephania tetrandra roots

Tetrandrine(TET) and fangchinoline(FAN) are dominant bisbenzylisoquinoline(BBIQ) alkaloids from the roots of Stephania tetrandra of the family Menispermaceae. BBIQ alkaloids comprise two benzylisoquinoline units linked by oxygen bridges. The molecular structures of TET and FAN are exactly the same, except that TET has a methoxy(-OCH3) group, while FAN has a hydroxyl(-OH) group at C7. In this overview,the current knowledge on the chemistry, pharmacology and anticancer properties of TET and FAN have been updated. The focus is on colon and breast cancer cells, because they are most susceptible to TET and FAN, respectively. Against colon cancer cells, TET inhibits cell proliferation and tumor growth by inducing apoptosis and G1 cell cycle arrest, and suppresses adhesion, migration and invasion of cells.Against breast cancer cells, FAN inhibits cell proliferation by inducing apoptosis, G1-phase cell cycle arrest and inhibits cell migration. The processes involve various molecular mechanisms and signaling pathways. Some insights on the ability of TET and FAN to reverse multi-drug resistance in cancer cells and suggestions for future research are provided.

Research Progress on Chemical Constituents and Pharmacological Effects of Zhuang Medicine Cocculus laurifolius DC.

This paper searched and summarized the relevant research literature on the chemical constituents and pharmacological effects of Cocculus laurifolius DC.,and provides a reference for further research on the quality standard of medicinal materials,clinical drug safety and the development and application of new drugs.The main chemical components of C.laurifolius are isoquinoline alkaloids.C.laurifolius has the pharmacological effects such as analgesic,hypotensive,antibacterial,free radical-scavenging activity,anticonvulsant,neuroprotective activity,anxiolytic and hypnotic effects.

Plant Secondary Metabolites： Biosynthesis, Classification, Function and Pharmacological Properties

Secondary metabolites, also known as phytochemicals, natural products or plant constituents are responsible for medicinal properties of plants to which they belong. The role they play in the plant is not, to date, well known or understood, but it may be beyond the protection. Their classification is based on chemical structure, composition, their solubility in various solvents, or the pathway by which they are synthesized. The main classification system includes three major groups： terpenoids, alkaloids and phenolics. For each one, we find subclasses with complexity in structure. In this review, we deal with the description of second metabolites, their biosynthesis, function, and the current pharmacological findings. Natural products are an important source of drug candidates in pharmaceutical industry, more deeply we understand them, the easier it is for scientists to intervene in alleviating different kind of diseases. The recent references have been consulted for presenting updated information, but also showing the new potentialities of plant second metabolites in drug research and development.

Progress on chemical constituents and pharmacological effects of Piper nigrum L.

Piper nigrum L.,belonging to Piper genus of the Piperaceae family,is a medicinal and edible plant.Studies have shown that there are many chemical constituents in this plant,including alkaloids,lignans,steroids and other compounds.In addition,some chemical components of P.nigrum have potential values to treat cancer,inflammation and other diseases.Research progress on the chemical constituents and pharmacological effects of P.nigrum was reviewed in this study to better explore its potential medicinal value.

莱菔子化学成分及药理作用研究概况

莱菔子是十字花科植物萝卜的干燥成熟种子,具有降气化痰、消食除胀之功。莱菔子的化学成分主要有生物碱类、硫苷类、挥发性成分、脂肪酸、黄酮类等,并具有增强胃肠动力、降血压、降血脂、抗癌、化痰、镇咳、平喘等药理活性。其中最主要的活性成分是芥子碱硫氰酸盐,在降血压、降血脂、抗炎、抗氧化过程中发挥着重要的药理作用。通过检索文献,分类总结了近年来国内外莱菔子化学成分及药理作用的研究报道,以期为莱菔子相关药品及保健品的研究与开发提供参考。参考文献80篇。