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白芷中的呋喃香豆素衍生物及其对 RXRα 转录调控的影响。

Furocoumarin derivatives from radix Angelicae dahuricae and their effects on RXRα transcriptional regulation.

机构信息

School of Pharmaceutical Sciences, Xiamen University, Xiamen 361005, China.

出版信息

Molecules. 2011 Jul 26;16(8):6339-48. doi: 10.3390/molecules16086339.

Abstract

A novel furocoumarin derivative named oxyalloimperatorin (1), together with seventeen furocoumarins 2-18 were isolated from the radix of Angelica dahurica. The chemical structure of new metabolite was characterized by analysis of IR, NMR, and HR-ESI-MS spectroscopic data. Among the isolated compounds, 13, 16, and 18 (each at 20 μM) could significantly promote the gene transcriptional function of nuclear receptor RXRα. While 7-9, 13, 14, and the new structure 1 (each at 20 μM) showed significant reduction in RXRα gene transcriptional activities induced by 9-cis-retinoid acid. The findings indicated that these furocoumarin skeleton derivatives might hold beneficial effects on many intractable diseases, such as cancer and metabolic diseases, due to their potential activities on regulating the transcriptional activation function of RXRα.

摘要

从白芷根部分离得到一个新的呋喃香豆素衍生物,命名为 oxyalloimperatorin(1),并分离得到 17 个呋喃香豆素化合物 2-18。通过分析 IR、NMR 和 HR-ESI-MS 光谱数据,确定了新代谢产物的化学结构。在所分离的化合物中,化合物 13、16 和 18(浓度均为 20μM)能显著促进核受体 RXRα 的基因转录功能。而化合物 7-9、13、14 和新结构 1(浓度均为 20μM)能显著抑制 9-顺式视黄酸诱导的 RXRα 基因转录活性。这些发现表明,由于这些呋喃香豆素骨架衍生物可能具有调节 RXRα 转录激活功能的潜力,因此它们可能对癌症和代谢疾病等许多难治性疾病具有有益的影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ccf4/6264713/afb6edf9e4fb/molecules-16-06339-g001.jpg

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