科罗索酸的氨基酸衍生物合成及其降糖作用初步研究

发布时间：2018-06-07 02:10

本文选题：科罗索酸 + 氨基酸　；参考：《南京师范大学》2014年硕士论文

【摘要】：糖尿病是近年来困扰人类健康的最主要的疾病之一,因此对糖尿病的治疗药物的研究与开发也是近二十年来药学界的热点之一。天然来源的科罗索酸具有抗肿瘤、降血糖、抗炎、抗病毒和抗心血管疾病等作用,尤能起到类似于胰岛素的生理作用,所以他又被称为"植物胰岛素",具有较好的降血糖活性,受到人们广泛关注,目前在国内外已被开发成多种保健品。但是科罗索酸由于其水溶性较差导致生物利用度低,因此迫切需要通过对其结构进行衍生化修饰来增加其亲水性,从而提高其生物利用度和药理活性。本课题以科罗索酸为母体,在28位羧基引入了甘氨酸(Gly)、丙氨酸(Ala)、丝氨酸(Ser)、亮氨酸(Leu)、苯丙氨酸(Phe)和脯氨酸(Pro)这几种天然α-氨基酸,全新合成出了六种科罗索酸衍生物。化合物的结构均用1HNMR、12CNMR及ESI-MS进行表征。在对其进行的初步药理学研究中,我们采用葡萄糖氧化酶法测定培养液中葡萄糖含量,以各组空白孔均值为对照,计算该组各孔培养液中葡萄糖含量的变化值(GC)。同时,用MTT法于酶标仪上测定各组培养液的0D值,最终以GC/MTT表示单位细胞的糖消耗量,并以此为指标评价各化合物的降血糖活性。
[Abstract]:Diabetes is one of the most important diseases in human health in recent years. Therefore, the research and development of diabetes drugs is one of the hot spots in pharmaceutical field in the last two decades. The natural source of Corozo acid has anti-tumor, anti-blood glucose, anti-inflammatory, anti-virus and anti-cardiovascular diseases and so on, especially plays a physiological role similar to insulin, so he is also known as "plant insulin", which has good hypoglycemic activity. At present, it has been developed into a variety of health products at home and abroad. However, because of the low bioavailability of Corozo acid due to its poor water solubility, it is urgent to improve its bioavailability and pharmacological activity by derivatization modification of its structure to increase its hydrophilicity. In this paper, six kinds of natural 伪 -amino acids, glycine, alanine Alaeum, serine, leucine, phenylalanine and proline, were introduced into 28 carboxyl groups and six derivatives of Corozo acids were synthesized. The structures of the compounds were characterized by 1H N MR12 CNMR and ESI-MS. In the preliminary pharmacological study, glucose content in culture medium was determined by glucose oxidase method, and the change value of glucose content in culture medium was calculated with blank hole mean value of each group as control. At the same time, MTT method was used to measure the 0D value of the culture medium in each group. Finally, the sugar consumption per unit cell was expressed by GC/MTT, and the hypoglycemic activity of each compound was evaluated.
【学位授予单位】：南京师范大学
【学位级别】：硕士
【学位授予年份】：2014
【分类号】：R914;R96

【相似文献】