Synthesis and Receptor Affinity of Polysubstituted Adenosines

Abstract

In a search for potent and selective adenosine agonists it has been found that 2-hexynyladenosine-5′-N-ethyluronamide (HENECA) displays high affinity at rat A_2A receptor combined with a good A_2A vs A₁ selectivity. The finding that HENECA shows good affinity also for A₃ receptors prompted us to investigate the effect of various substituents in different positions of this molecule.     

丙酮酸乙酯的合成及药理作用研究

丙酮酸乙酯是一种重要的医药中间体,在医药、农药、食品、化妆品等领域有广泛的用途。其合成方法和药理作用一直是研究的热点。近年来愈来愈多的文章报道了丙酮酸乙酯的各种合成及工艺方法,一些新的生理活性也不断见诸于文献。本文从丙酮酸乙酯的合成方法及药理作用两方面进行综述,主要介绍了乳酸乙酯氧化法、有机金属试剂法和酯化法三种合成丙酮酸乙酯的方法,并从工艺角度对各种方法的优缺点进行了分析;阐述了其抗氧化、抗炎、抗肿瘤作用的研究进展,并对丙酮酸乙酯的药物应用前景进行了展望,期望能够为丙酮酸乙酯的进一步成药性研究提供思路和启发。     

Studies Toward Synthesis of C2-Substituted Adenosines: An Efficient Synthesis of 2-(Phenylamino)Adenosine [CV-1808]

Abstract

In this paper we report general and highly efficient synthetic routes to certain C2,N6-disubstituted adenosines including an efficient synthesis of 2-(phenylamino)adenosine [CV-1808, a highly A2 receptor selective adenosine agonist] originally developed as an antianginal agent.     

无患子皂苷的提取、类型及药理活性

无患子是重要的资源植物,其含有丰富的皂苷种类和多样化的药理活性。本文概述了无患子皂苷的提取介质、提取条件和提取效果;综述了其皂苷的结构类型,侧链种类、连接部位、连接方式和产生的植体部位,以及抗菌、灭螺、杀虫、消炎、抗肿瘤、保肝、杀精活性,为无患子皂苷的深入研究和开发奠定基础。     

羊肚菌化学成分及药理活性研究进展

羊肚菌是羊肚菌属(Morchella Dill.ex Pers.)真菌的总称,是一类珍稀食药用菌,营养成分丰富,药用价值高。文中对国内外近50年来发表的有关羊肚菌的化学成分及药理作用的研究进行了综述。化学研究结果显示羊肚菌含有多类化学成分,包括酶、多糖、氨基酸、甾醇、有机酸和微量元素等;药理研究发现羊肚菌具有免疫调节、抗肿瘤、抗疲劳、抗衰老、保护心血管系统、胃黏膜、肾脏和肝脏等多方面的药理活性。     

Measurements of Mutagenic and Antimutagenic Activities of Bile Acids by Rec-assay

To study the carcinogenic activity of bile acids, we examined the mutagenic activity of bile acids by Rec-assay using B. subtilis H17 and M45 strains. Cholic, chenodeoxycholic, lithocholic, and glycolithocholic acids exerted much weaker mutagenicity than mitomicin C (MMC), and deoxycholic and glycodeoxycholic acids showed toxicity toward the bacteria. Most of the conjugated bile acids (glycocholic, taurocholic, and taurodexycholic acids) and their amino acid components (glycine and taurine) were neither toxic nor mutagenic. No bile acids enhanced the mutagenicity of N-methyl-N′-nitro-N-nitrosoguanidine (MNNG), but glycine enhanced both toxicity and mutagenicity of MNNG in a dose-dependent manner. On the other hand, taurine decreased the mutagenicity of MNNG, and most of the bile acids decreased the mutagenicity of MMC. Furthermore, taurocholic acids decreased toxicity and/or mutagenicity of other bile acids. These results suggested that the mutagenic and comutagenic activities of bile acids can be disregarded, but they are antimutagenic in some situations.     

Synthesis and Antiviral Evaluation of Adenosine-N1-Oxide and 1-(Benzyloxy) Adenosines

Abstract

The antiviral activity of adenosine-N¹-oxide (1) and a variety of substituted 1-(benzyloxy) adenosines (2) has been re-investigated and significant in vitro activity vs. Vaccinia virus has been shown. In vivo activity in mice has also been demonstrated.     

The Genus Cryptocarya: A Review on Phytochemistry and Pharmacological Activities

Cryptocarya (the laurel family) is a large genus of great economic plants found in tropics and subtropics. Plants of this genus are a rich resource of essential oils, and pharmacological compounds. An overview of phytochemistry and pharmacological aspect is not yet available. This review aims to establish insightful information on phytochemistry, and pharmacological values. The literature collection is based on keywords ‘Cryptocarya’, ‘phytochemistry’, and ‘pharmacology’ using a broad panel of scientific sources, such as Google Scholar, Sciencedirect, and Wiley. Since the 1950s, Cryptocarya plants have been the main object in various phytochemical studies, by which about 390 metabolite compounds were isolated. Alkaloids, α-pyrones, and flavonoids could be seen as the main classes of Cryptocarya isolates. Cryptocarya constituents displayed potential pharmacological values such as anti-inflammatory, antimicrobial, antioxidative, antiviral, vasorelaxant activities, especially cytotoxicity.     

芦荟属药用植物的化学成分和药理活性

芦荟是一种应用范围广泛、历史悠久的传统中药,广泛地供作药用及食用。本文从化学成分和药理活性两方面综述了芦荟属（Aloe）药用植物的研究进展,为芦荟属植物的开发利用提供一定的科学依据。     

柴胡属植物化学成分及药理研究新进展

介绍了近十年来国内外柴胡属植物化学成分及主要化学部位药理研究新进展.为进一步研究开发柴胡提供了依据.     

龙眼的化学成分与药理活性研究

龙眼是一种应用价值很高的传统中药,含有很多重要成分,比如多糖、脂类、多元酚、黄酮类等,传统中医认为龙眼有补益心脾、止痛消肿之功,近年来的研究发现它还有抗癌、抗衰老、抗氧化和免疫调节的作用。本文从龙眼肉、龙眼核两个角度,针对鉴别、化学成分、药理活性等方面,将近年来国内外的研究成果综合分析,并提出对龙眼远大开发前景的展望。     

龙眼的化学成分与药理活性研究

龙眼是一种应用价值很高的传统中药,含有很多重要成分,比如多糖、脂类、多元酚、黄酮类等,传统中医认为龙眼有补益心脾、止痛消肿之功,近年来的研究发现它还有抗癌、抗衰老、抗氧化和免疫调节的作用。本文从龙眼肉、龙眼核两个角度,针对鉴别、化学成分、药理活性等方面,将近年来国内外的研究成果综合分析,并提出对龙眼远大开发前景的展望。     

薄荷化学成分及其药理作用研究进展

对国内外有关薄荷的化学成分和药理作用的研究进行了综述,为进一步研究和开发利用薄荷提供了依据。     

我国药用菊花的化学及药理学研究新进展

对我国药用菊花植物的化学成分和药理学研究进展进行了综述.其主要成分为挥发油、黄酮类化合物等.主要药理作用有抗炎、镇痛、抗病毒、抗菌、抗衰老、抗肿瘤、抗病毒等.     

橙皮苷的药理作用研究进展

橙皮苷广泛存在于各种植物中,具有抗炎、抗氧化、抗菌、抗癌、调节免疫力、防辐射、保护心血管系统等多种药理活性。本文综述了近几年有关橙皮苷、及其配位修饰后的橙皮苷的药理活性方面的最新进展,并对其发展趋势做了分析和讨论。     

虫草属真菌化学成分及药理作用研究进展

虫草属真菌是一类十分重要的药用真菌,具有多种活性物质及广泛的药理作用、对该属真菌的化学成分及药理作用的研究进展进行了综述,为虫草属药用真菌的研究和开发提供依据。     

红车轴草的化学成分及药理作用研究进展

对红车轴草所含的化学成分、药理作用研究和保健品开发现状作一综述。     

猪屎豆属植物化学成分及药理活性研究概况

综述近年来猪屎豆属植物化学成分和药理活性研究概况。提出在化学成分、构效关系、药理等方面均需要进一步开展深入研究的建议。     

野生植物苦豆子的化学成分和主要药理作用

豆科槐属植物苦豆子是一种分布量大的野生荒漠植物,不仅具有耐盐碱、干旱等环境保护性质,其体内作为主要次生代谢产物的生物碱和黄酮两大类化合物也显示出多方面的重要药理作用。就其在抗病毒,抗肿瘤和免疫等药理活性的近期研究做一综述。     

半枝莲化学成分及药理活性研究进展(综述)

半枝莲Scutellaria barbata为我国传统中药,具清热解毒、化瘀止痛、排石利尿等多重功效。化学成分研究表明,半枝莲含有大量黄酮类、二萜类、挥发油类及多糖等化学成分;药理研究表明,半枝莲具有抗肿瘤、抗氧化、抗菌及免疫调节等药理活性。本文综述半枝莲的化学成分及其药理活性研究概况,为其进一步开发利用提供参考。