Natural amino acid conjugates of lithocholic acid as α-2,6-sialyltransferase inhibitors with antimigratory and antiangiogenic activity

Please use this identifier to cite or link to this item: http://ir.lib.ncu.edu.tw/handle/987654321/85742

Title:	Natural amino acid conjugates of lithocholic acid as α-2,6-sialyltransferase inhibitors with antimigratory and antiangiogenic activity
Authors:	陳瑋昇;Chen, Wei-Sheng
Contributors:	化學學系
Keywords:	唾液酸;唾液酸轉移?;癌症轉移;石膽酸;sialic acid;sialyltransferase;metastasis;lithocholic acid
Date:	2021-07-29
Issue Date:	2021-12-07 11:20:33 (UTC+8)
Publisher:	國立中央大學
Abstract:	在這項工作中，石膽酸的氨基酸錯合物被設計、合成並評估了它們的細胞毒性、α-2,6-唾液酸轉移?抑制、抗遷移和抗血管生成作用。在該系列中，具有色氨酸部分的 S1047 顯示可抑制 ST6GalI 活性（IC50 26.5 ± 1.2 μM）、抑制腫瘤生長、延遲癌細胞遷移並減少動物模型（生物體外）中的血管生成以及腫瘤生長。正在進行進一步研究以尋求石膽酸的氨基酸錯合物的臨床應用。;In this work, the amino acid conjugates of lithocholic acid were designed, synthesized and evaluated their cytotoxicity, α-2,6-sialyltransferase inhibition, antimigratory and antiangiogenic effects. Among the series, S1047, possessing the tryptophan moiety, were shown to inhibit ST6GalI activity (IC50 26.5 ± 1.2 μM), suppress tumor growth, delay cancer cell migration, and reduce angiogenesis and tumor growth in animal model (ex vivo). Further study to pursue clinical application of amino acid conjugates of lithocholic acid is in progress.
Appears in Collections:	[Graduate Institute of Chemistry] Electronic Thesis & Dissertation

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