二氢杨梅素诱导人肺腺癌细胞系AGZY-83-a凋亡的实验研究

目的研究二氢杨梅素(dihydromyricetin)对人肺腺癌细胞系AGZY-83-a凋亡的影响及其相关机制。方法采用MTT法检测二氢杨梅素对人肺腺癌细胞AGZY-83-a存活率的影响,应用TUNEL法和Caspase-3活性检测观察二氢杨梅素对AGZY-83-a凋亡的作用,并通过共聚焦显微镜观察二氢杨梅素对肺腺癌细胞内钙的影响。结果MTT结果显示,二氢杨梅素50μmol·L-1对AGZY-83-a的增殖有明显抑制作用,并呈剂量和时间依赖关系;TUNEL实验结果显示二氢杨梅素可以引起AGZY-83-a发生凋亡,且具有剂量依赖性;Caspase-3活性检测结果显示二氢杨梅素可增加肺腺癌细胞Caspase-3活性,说明二氢杨梅素可以诱导AGZY-83-a凋亡;二氢杨梅素可升高肺腺癌细胞内钙,平均荧光强度FI可增加20多倍。结论二氢杨梅素可通过增加细胞内钙诱导AGZY-83-a细胞凋亡,从而发挥抗肿瘤作用。     

蛇葡萄素与苯并芘合用对大鼠肺组织内CYP和GST基因表达的影响

<正>蛇葡萄素(ampelopsis),又名二氢杨梅素(dihydromyrice-tin)、双氢杨梅素等,为一多酚羟基黄酮醇化合物[1],存在于葡萄科、杨梅科、藤黄科等植物中,具有抗炎、抗肿瘤、抗氧化     

二氢杨梅素稳定性影响因素及抑菌活性研究进展

二氢杨梅素是藤茶主要活性成分,资源丰富,有广泛的药理活性,具有良好的应用前景.但其稳定性差,容易受多种因素影响而易被氧化,故本文对二氢杨梅素稳定性影响因素进行综述,为提高二氢杨梅素的有效利用提供依据,同时对其抑菌活性进行简述.     

二氢杨梅素神经保护作用研究进展北大核心CSCD

二氢杨梅素(dihydromyricetin,DHM)是广泛存在于葡萄科蛇葡萄属植物中的一种二氢黄酮类化合物,具有抗炎、抗菌、抗肿瘤、抗氧化、调血糖、降血脂、肝保护等多种药理作用。近年的研究表明,DHM具有很好的神经保护作用,对多种神经系统病变包括阿尔茨海默病、抑郁症、帕金森综合征、脑卒中等均能起到一定的药理作用。该文针对近十年国内外对DHM的神经保护作用的相关研究进行综述,旨在为DHM的神经保护作用研究提供思路。     

制剂新技术与新剂型提高二氢杨梅素生物利用度的研究进展

二氢杨梅素是藤茶的主要药效物质,具有多种显著的药理活性,但低生物利用度制约了其临床应用。近年来,各种制剂技术为改善二氢杨梅素溶解度及提高其生物利用度提供了新途径,为其成药性提供了有效的解决办法。该文综述了二氢杨梅素各种制剂技术与剂型提高其生物利用度的研究进展,分析新剂型在改善二氢杨梅素成药性发展中面临的问题,以期为其开发和应用提供参考。     

二氢杨梅素的稳定性研究

目的:研究二氢杨梅素在不同条件下的稳定性。方法:考察二氢杨梅素在不同pH值、温度、光线、金属离子影响下的稳定性,用反相高效液相色谱法测定其含量。结果:在pH值≤4的弱酸性条件下二氢杨梅素能稳定存在,随着pH值的增加,会加速氧化,特别是在pH值≥9的碱性条件下会立即反应而氧化变黄。温度的升高,Fe3 ,Al3 ,Cu2 等金属离子的存在以及光线均可以加速二氢杨梅素的氧化。结论:为使二氢杨梅素能较长时间稳定存在,需保证其生理活性的条件是弱酸性、避免接触Fe3 ,Al3 ,Cu2 等金属离子、避光低温保存。     

061槐属植物中的黄酮类化合物及其药理活性

综述了近10年来从槐属植物中分离得到的黄酮类化合物及其药理活性,为该属植物的开发利用提供参考。新分得的黄酮类化合物包括二氢黄酮、二氢黄酮醇、异黄酮、二氢异黄酮和多环系黄酮等,药理活性包括抗菌、抗肿瘤、抗炎、抗病毒、抗雄性激素样作用等。     

二氢杨梅素心血管保护作用的研究进展

二氢杨梅素是藤茶中主要的黄酮类化合物,不仅具有抗氧化、抗肿瘤、降血糖、抗菌消炎、解酒保肝的药理活性,还具有调血脂、抗血栓和防治动脉粥样硬化的作用。本文综述了二氢杨梅素的心血管保护作用和机制,为其进一步的开发与临床应用提供参考。     

显齿蛇葡萄总黄酮的生物活性研究进展

显齿蛇葡萄Ampelopsis Crrossedenta（Hand—Mazz．）W．T．Wa，又名藤茶，为葡萄科蛇葡萄属植物，显齿蛇葡萄总黄酮为其主要化学成分，含量高达45．52％。主要有二氢杨梅素（dihydromyricetin）、又名福建茶素（ampelopsin）、杨梅素（myricetin）、杨梅苷（myricitin）等。近年来，国内外学者对显齿蛇葡萄总黄酮的生物活性非常关注，现就其研究进展综述如下。     

二氢杨梅素对衰老模型小鼠的改善作用

目的： 研究二氢杨梅素对衰老模型小鼠的改善作用。方法： 将50只小鼠随机分为正常组、模型组和二氢杨梅素（250,500,1 000 mg·kg^-1）给药组,皮下注射5% D-半乳糖,注射量为25 mL·kg^-1,每天1次,连续42 d复制小鼠衰老模型。造模同时给药,各组小鼠分别给予相应剂量的二氢杨梅素,连续42 d。末次给药后2 h对小鼠学习记忆能力进行测定,然后测定小鼠脑组织丙二醛（MDA）、脂褐素（LF）含量与超氧化物歧化酶（SOD）、谷胱甘肽过氧化物酶（GSH-Px）活性。结果： 与正常组相比,模型组学习记忆能力出现显著下降（P<0.01）,MDA、LF水平显著升高（P<0.01）,SOD和GSH活性显著降低（P<0.01）。与模型组相比,给予二氢杨梅素后,小鼠学习记忆能力显著提高（P<0.01）,MDA、LF水平显著降低（P<0.01）,SOD和GSH活性显著升高（P<0.01）。结论： 二氢杨梅素能够有效提高机体的抗衰老能力,其机制可能是与二氢杨梅素提高机体的抗氧化能力有关。     

小檗碱类抗微生物化合物研究进展

小檗碱类化合物是一类具有多种生物活性且大量应用于临床的季铵类异喹啉生物碱。近年来,小檗碱类药物的研究与开发受到广泛关注,且逐渐成为一个发展迅速、充满活力的领域。通过结构修饰所得的小檗碱类衍生物具有良好的抗细菌、抗真菌及抗病毒活性,可通过多种靶点对微生物发挥抑制作用。本文综述小檗碱类衍生物在抗细菌、抗真菌及抗病毒方面的研究与开发进展状况,为进一步研发小檗碱类抗微生物药物提供参考。     

肠道微生物次级代谢产物及疾病治疗的研究现状

肠道微生物次级代谢产物化学结构新颖、生物活性多样。目前发现的肠道微生物代谢产物主要包括环二肽及多肽类、生物碱类、内酯类、环酰胺类等,肠道微生物在抗菌、抗病毒、抗炎等方面表现出巨大的研究前景。本文对近几年来肠道微生物来源的次级代谢产物的结构特征、生物活性及肠道微生物在疾病治疗方面的研究进展进行总结和综述。     

Perspectives on the development of novel potentially active quinolones against tuberculosis and cancer

Quinolones and its derivatives comprise an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, antitumor, antiviral, anti-ischemic, antiparasitic and anxiolytic. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side-effects. The present review aims to highlight some recent discoveries on the development of novel quinolone-based compounds with potential antitubercular and anticancer activity.     

Antimicrobial and hemolytic activities of crabrolin,a 13-residue peptide from the venom of the European hornet,Vespa crabro,and its analogs

The venom of insects like bee, hornet and wasp contain peptides that exhibit potent biological activities. Many of these peptides are composed of 13-26 residues and are thus accessible through chemical synthesis as well as amenable to studies directed toward structure-function correlations. In this report, we describe antibacterial and hemolytic activities of crabrolin: FLPLILRKIVTAL-NH₂, a 13-residue peptide present in the venom of the hornet Vespa crabro and related peptides. The analogs were chosen so that the role of proline and positively charged amino acids in modulating biological activities could be evaluated. Our results indicate that, although helical conformation is necessary for hemolytic activity, it is not a prerequisite for antibacterial activity. Appropriately positioned, charged and hydrophobic residues and overall hydrophobicity appear to determine antibacterial activity. The discovery of a large number of host-defense peptides in a variety of species in recent years offers a large repertoire of molecules that can be “engineered” based on biophysical principles to yield molecules with specific activities.     

新型血管生成抑制剂Borrelidin抗肿瘤作用及其合成的研究进展

Borrelidin是从娄彻氏链霉菌代谢产物中分离得到的十八元大环内酯化合物,具有良好的抗菌、抗疟和抗病毒等活性。近年报道其具有血管生成抑制活性(IC50=0.8nM),是潜在的血管生成抑制剂,使Borrelidin再受瞩目,而血管生成抑制剂是目前抗肿瘤药物研究的热点之一,加之Borrelidin结构新颖独特,在药物科研开发领域再度引起了科技工作者的兴趣。本文就Borrelidin的抗肿瘤活性、作用机制及其合成的相关研究进行综述。     

Synthesis of some novel 2-substituted benzoxazoles as anticancer, antifungal, and antimicrobial agents

Benzoxazole derivatives show various types of biological properties such as antiviral, antineoplastic, anti-HIV-1, antitubercular, anthelmintic, antimicrobial, and antifungal activities. In the last few years 2-substituted benzoxazole derivatives have been studied extensively for their antitumor, antiviral, and antimicrobial activities. In an effort to identify new candidates that may be of value in designing new, potent, selective, and less toxic anticancer, antiviral, and/or antimicrobial agents, we synthesized 2-[(arylhydrazono) cyanomethyl]-5-chloro benzoxazoles (II), 2-[(arylidene)cyanomethyl]-5-halo benzoxazoles (III), and 2-[(cycloalkylidine)cyanomethyl]-5-chlorobenzoxazoles (IV), and tested them for anticancer, antifungal, and antibacterial activities. Some of these (compounds 11, 14) were found to possess anticancer activity and remarkable antifungal as well as antibacterial activities.     

含磺酰胺结构的抗微生物药物研究进展

 磺酰胺类化合物具有广泛的生物活性,临床上使用含有磺酰胺结构片断的药物众多,其研究与开发备受 关注,日益活跃,发展十分迅速。文中综述了含磺酰胺结构类化合物在抗菌、抗真菌、抗病毒、抗寄生虫、抗结核等领 域的研究与开发进展。     

Synthetic derivatives of chrysin and their biological activities

Chrysin is one of flavones constituents of Orocylumineicum vent. It has been a hot spot as a potential chemopreventive agent and as a natural molecule with numerous biological activities such as antioxidant, antitumor, antiviral, anti-hypertension, anti-diabetic, antibacterial, and so on in recent years. Because of its poor solubility, small intestinal absorption, and the rapid metabolism of glycosylation, a large number of efforts had been made by domestic and foreign researchers on designing its analogs and conjugates to obtain compounds with improved efficacy and selectivity for developing more active drugs for clinic. This article reviews the current research of studying on chrysin derivatives including their properties and possible applications. Additionally, this article also presents the basic information concerning chemical reactivity of chrysin, relevant to the synthesis of its derivatives.     

白屈菜碱的药理作用研究进展

白屈菜碱是白屈菜Chelidonium majus的主要活性成分之一,属于苯并菲啶类生物碱,现作为止痛药应用于临床。随着对白屈菜碱药理作用的深入研究发现,其具有抗肿瘤、镇痛、抗菌、解痉等多种药理作用,且其抗肿瘤作用越来越受到关注。对近年来白屈菜碱药理作用的国内外研究进展做以综述,为其进一步研究与应用提供理论依据。