红景天苷及其类似物合成研究进展

红景天苷为景天科植物红景天的主要活性成分。研究发现,红景天苷具有抗缺氧、抗疲劳、抗微波辐射、兴奋中枢神经和调节内分泌等药理活性,由于其结构简单,毒性小,广泛的药理活性而倍受人们的关注。笔者从化学合成和生物合成两个方面对红景天苷及其类似物的合成进行了综述。     

红景天苷心肌保护作用机制的研究进展

红景天苷是景天科植物大花红景天的主要活性成分,存在于该植物的根及根茎中。大量的研究证明,红景天苷具有多种药理学作用,包括显著的抗氧化、抗炎、抗纤维化,改善心功能等作用。近年来,有许多关于红景天苷的药理研究,但红景天苷在心血管疾病中的应用及其机制研究仍然欠缺。本综述介绍红景天苷心肌保护作用机制的研究进展。     

红景天苷药理作用及机制

红景天系蔷薇目景天科红景天属多年生草本或亚灌木野生植物,红景天苷是红景天最有效的活性成分之一,不仅有抗疲劳、抗衰老、免疫调节、清除自由基、增强记忆改、善睡眠等药理作用,还可以起到保护心脏,抵抗辐射对人体的伤害,保护保护造血系统的药理作用。本文综述了近年来国内外对红景天苷对心、脑、肾、肝、神经、皮肤的作用其和药理方面的研究,以其为红景天苷的进一步开发、利用提供参考。     

红景天浸膏粉除鞣质方法研究

红景天为红景天科植物的茎,具抗缺血、抗缺氧、抗疲劳、提高运动能力等功效[1].主含红景天苷及鞣质.红景天苷为红景天的活性成分,而鞣质的存在影响红景天溶液的澄明度和口味.为了矫正其涩味,提高澄明度,须除去其中的鞣质成分.现采用明胶溶液沉淀鞣质法除去红景天中的鞣质成分.     

红景天苷防治帕金森病的药理作用研究进展

帕金森病已成为威胁老年人身心健康的主要疾病之一。红景天苷是从红景天中提取的主要活性化合物之一，具有多种药理作用。红景天苷可通过抑制细胞凋亡、增强细胞自噬、降低氧化应激反应、降低炎症反应、促进胶质细胞源性神经营养因子的表达、提高多巴胺转运蛋白的表达以达到防治帕金森病的作用。总结了红景天苷防治帕金森病的药理作用及其作用机制，为红景天苷的临床使用提供参考。     

人参皂苷Rb1与红景天苷对抗皮肤光老化作用

目的:分析红景天苷与人参皂苷Rb1对抗皮肤光老化的作用.方法:设定4组,空白对照组1(未经UVB照射)、空白对照组2(经UVB照射)、人参皂苷Rb1组与红景天苷组,以MTT法对细胞增殖活性予以检测,再检测细胞中SOD(超氧化物歧化酶)、MDA(丙二醛)、CAT(氧化氢酶)及GSH(谷胱甘肽)含量.结果:红景天苷与人参皂苷Rb1可提升细胞内CAT、SOD及GSH活性,减少MDA生成量,与0μg·mL-1对比P<0.05.结论:人参皂苷Rb1与红景天苷可有效对抗皮肤光老化.     

红景天苷在大鼠体内药物代谢动力学的研究进展

药理学研究已经确认红景天苷具有抗炎、抗肿瘤、免疫调节,促进骨生长、骨骼肌生长、抗氧化、增体质,抗疲劳,抗肌萎缩,抗骨质疏松,抗痴呆,保护肝脏、神经、肺、呼吸道、心脏、血管、肾脏以及降血糖、调血脂、抗肥胖等药理作用。综述红景天苷在大鼠体内药物代谢动力学的研究文献资料,对其研究进展做了分析,为红景天苷的临床研究及其合理使用提供参考。     

基于分子对接技术筛选二至丸治疗骨质疏松的活性成分及验证

本研究借助分子对接技术和体外验证实验筛选中药复方二至丸治疗骨质疏松的活性成分。首先采用分子对接技术将二至丸中的化合物与4个骨质疏松相关靶点进行对接,初步挑选得到红景天苷、特女贞苷、酪醇、槲皮素和蟛蜞菊内酯等5个活性成分。然后采用含有不同浓度化合物的α-Mem培养基培养小鼠MC3T3-E1成骨细胞,检测细胞增殖率和矿化结节,细胞验证结果表明,红景天苷、特女贞苷和槲皮素对MC3T3-E1细胞增殖较为明显,红景天苷对MC3T3-E1细胞矿化作用较特女贞苷和酪醇效果更好。本文采用的分子对接技术及体外验证研究可以用于二至丸抗骨质疏松活性成分的筛选,同时可为中药药效活性成分的研究提供方法借鉴。     

红景天苷对肾脏保护作用的药理机制研究进展

药理学研究已经证实红景天苷具有抗炎、抗肿瘤、免疫调节、促进骨和骨骼肌生长、抗氧化、增体质以及抗疲劳、抗肌萎缩、抗骨质疏松、抗痴呆和保护肝脏、神经、肺、呼吸道、心脏、血管的作用,以及具有降血糖、调血脂、抗肥胖等药理作用。综述红景天苷保护肾脏作用的研究资料,并认为红景天苷极有可能被开发成防治代谢综合征、心脑血管病及其并发症药物,并对其药理机制研究进展做了分析。     

红景天苷药理作用的研究进展

红景天苷是中药红景天的主要有效成分之一,其药理作用是多种多样的,应用前景十分广阔.本文分别从红景天苷抗肿瘤及增强免疫功能、对心血管系统影响、对中枢神经系统的作用、对肝肾作用、抗缺氧作用,其他作用等方面综述了近年来国内外对其在药理方面的研究,以其为红景天苷的进一步研究开发利用提供更多参考.     

前列腺素类化合物化学全合成研究现状

综述近年来前列腺素类化合物全合成研究的新进展以及对新药研发的推动作用。前列腺素是一类重要的具有多种生物活性且低毒性的内源性天然产物,在医药领域用途广泛,其全合成研究也备受关注,并取得长足发展。     

Practical and efficient approach to the synthesis of guineensine

A total synthesis of guineensine, a secondary metabolite of the Piperaceae family, has been executed in 12 steps with an overall yield of 27%. Key steps in the synthesis featured novel application of a Julia–Kocienski olefination reaction which effectively constructed alkenamide skeleton. This contributes a unique approach to the synthesis of the piperamide alkaloids.     

Practical and efficient approach to the synthesis of guineensine

A total synthesis of guineensine, a secondary metabolite of the Piperaceae family, has been executed in 12 steps with an overall yield of 27%. Key steps in the synthesis featured novel application of a Julia-Kocienski olefination reaction which effectively constructed alkenamide skeleton. This contributes a unique approach to the synthesis of the piperamide alkaloids.     

Total synthesis of cajanine and its antiproliferative activity against human hepatoma cells

Cajanine, a constituent of Cajanaus cajan L., used in traditional Chinese medicine, is a promising drug candidate because of its broad range of bioactivities. However, the total synthesis of cajanine and its derivatives has never been reported. Herein, we report the total synthesis of cajanine in nine steps with an overall yield of 10% together with its analog, longistyline A, in 8% yield. The antiproliferative activity of the two compounds against a human hepatoma cell line is also reported.     

一个氢化橙酮衍生物的全合成

本文以2．4％的总收率首次全合成了一个氢化橙酮衍生物,即4-甲氧基-2,6-二羟基-2-苄基-3（2H）-苯并呋喃酮。以问苯三酚为起始原料,该合成工作涉及的关键反应包括：傅克酰基化、Williamson关环、催化氢化、羟醛缩合、烯醇化以及Rubottom氧化反应等。     

Synthesis of grandisol,the sexual attracting insect pheromone

In this issue, Suh’s group reported a new formal total synthesis of (±)-grandisol featuring a palladium-catalyzed 4-exo-trig cyclization. Grandisol’s interesting cyclobutane structure has been a popular test model for various cyclization methods over the years. This report summarizes Suh’s formal synthesis of grandisol along with a concise review of the four-membered ring cyclization strategies employed in the synthesis of grandisol.     

Synthesis of optically active trans 4-cyclohexyl-L-proline as an intermediate product in the preparation of fosinopril

A nine-step synthesis of trans 4-cyclohexyl-L-proline has been developed on a laboratory scale. The product is an intermediate in the preparation of fosinopril--an effective hypotensive drug. The total yield of the synthesis was 25%. The final product was 99.7% pure. Analytical methods were developed for each step of the synthesis (HPLC, TLC, IR, 1H-NMR, 13C-NMR, GC-MS, [alpha]D).     

New enzymatic strategies for enantiomers of lactams and amino acids

To fulfil the requirements of modern go-ahead research, new direct and indirect enzymatic strategies and new techniques have been devised for the preparation of enantiopure beta- and gamma-lactams and beta- and gamma-amino acids, and some of them have been scaled up. For example, a formal total synthesis of enantiopure Anatoxina, a neurotoxic alkaloid, but a potent and stereospecific agonist at nicotinic acetylcholine receptors has been introduced. An efficient and very simple method has been developed for the synthesis of the antibacterial cispentacin [(1R,2S)-2-amino-1-cyclopentanecarboxylic acid] and 8 new derivatives. A highly efficient enzymatic procedure has been elaborated for the synthesis of the blockbuster drug Abacavir and Carbovir intermediate (1S,4R)-4-aminocyclopent-2-ene-1-carboxylic acid. The first enzymatic method has been devised for the synthesis of (R)-3-amino-4-(2,4,5-trifluorophenyl)butanoic acid, the intermediate for the new antidiabetic drug Sitagliptine. Direct enzymatic strategies have been reported for the synthesis of (2R,3S)-3-phenylisoserine, a key intermediate of the side-chain of the antitumor product Taxol. A new enzymatic method has been developed for the total synthesis of crispine A enantiomers with antitumor activity. As amino acids are among the main products in the above-mentioned enzymatic methods, a new gas-chromatographic method has been acquired for the enantioseparation of acyclic and carbocyclic cis- and trans-beta-amino acids via a rapid double derivatization technique (esterification followed by N-acylation). APPLICABILITY: Through the utilization of enzymes, efficient enantioselective procedures in organic media have been developed and applied for the preparation of enantiopure, biologically active (beta- and gamma-lactams and beta- and gamma-amino acids (Scheme 15). Two of our recently elaborated enzymatic methods for the synthesis of beta- and gamma-amino acids have been patented. Acros Organics and BioBlocks Inc. serve as the sales companies of more than 20 enantiopure products that we have prepared by enzymatic methods.     

Structures and total syntheses of the plecomacrolides

The plecomacrolides are a large family of natural products typically featured with a 16- or 18-membered macrolactone possessing two conjugated diene units and a hemiacetal side chain. The macrocycle skeleton is connected with the side chain through a three-carbon linker, forming a biologically important intramolecular hydrogen bonding network among the lactone/linker/hemiacetal structural motif. Many members of the plecomacrolides act as selective inhibitors of vacuolar H+-ATPases (V-ATPases) and they are considered to have the potential for treatment of postmenopausal osteoporosis. Significant progress has been achieved in recent years in the area of plecomacrolide total synthesis. These include the total synthesis of bafilomycin A1 by Evans, Toshima, Hanessian, and Roush, of bafilomycin V1 by Marshall, of hygrolidin by Hashimoto and Yonemitsu, of concanamycin F by Paterson and Toshima, and of formamicin by Roush. The synthetic strategies and key transformations used in the total synthesis are discussed.     

柳珊瑚酸的研究进展

柳珊瑚酸是近年来研究复较多的一种具独特结构的海洋生物神经毒素。本文介绍有关柳珊瑚酸的分离提取与结构确定，全合成研究，衍生物制备和生理活性研究进展及其应用前景。