本文選題：科羅索酸 + 氨基酸��； 參考：《南京師范大學》2014年碩士論文

【摘要】：糖尿病是近年來困擾人類健康的最主要的疾病之一,因此對糖尿病的治療藥物的研究與開發(fā)也是近二十年來藥學界的熱點之一。天然來源的科羅索酸具有抗腫瘤、降血糖、抗炎、抗病毒和抗心血管疾病等作用,尤能起到類似于胰島素的生理作用,所以他又被稱為"植物胰島素",具有較好的降血糖活性,受到人們廣泛關注,目前在國內外已被開發(fā)成多種保健品。但是科羅索酸由于其水溶性較差導致生物利用度低,因此迫切需要通過對其結構進行衍生化修飾來增加其親水性,從而提高其生物利用度和藥理活性。本課題以科羅索酸為母體,在28位羧基引入了甘氨酸(Gly)、丙氨酸(Ala)、絲氨酸(Ser)、亮氨酸(Leu)、苯丙氨酸(Phe)和脯氨酸(Pro)這幾種天然α-氨基酸,全新合成出了六種科羅索酸衍生物�；衔锏慕Y構均用1HNMR、12CNMR及ESI-MS進行表征。在對其進行的初步藥理學研究中,我們采用葡萄糖氧化酶法測定培養(yǎng)液中葡萄糖含量,以各組空白孔均值為對照,計算該組各孔培養(yǎng)液中葡萄糖含量的變化值(GC)。同時,用MTT法于酶標儀上測定各組培養(yǎng)液的0D值,最終以GC/MTT表示單位細胞的糖消耗量,并以此為指標評價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 偽 -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.
【學位授予單位】：南京師范大學
【學位級別】：碩士
【學位授予年份】：2014
【分類號】：R914;R96

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相關碩士學位論文 前1條

1 楊耀辰;科羅索酸的氨基酸衍生物合成及其降糖作用初步研究[D];南京師范大學;2014年

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本文編號：1989232