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来自厚朴根的抗炎新木脂素。

Anti-inflammatory neolignans from the roots of Magnolia officinalis.

作者信息

Shih Hung-Cheng, Kuo Ping-Chung, Wu Shwu-Jen, Hwang Tsong-Long, Hung Hsin-Yi, Shen De-Yang, Shieh Po-Chuen, Liao Yu-Ren, Lee E-Jian, Gu Qiong, Lee Kuo-Hsiung, Wu Tian-Shung

机构信息

School of Pharmacy, National Cheng Kung University Hospital, College of Medicine, National Cheng Kung University, Tainan 701, Taiwan, ROC.

Department of Biotechnology, National Formosa University, Yunlin 632, Taiwan, ROC.

出版信息

Bioorg Med Chem. 2016 Apr 1;24(7):1439-45. doi: 10.1016/j.bmc.2016.01.049. Epub 2016 Jan 27.

Abstract

Nine neolignan derivatives (1-9) were characterized from the roots of Magnolia officinalis, and their structures were elucidated based on spectroscopic and physicochemical analyses. Among them, houpulins E (1) and M (9) possess novel homo- and trinor-neolignan skeletons. In addition, 15 known compounds (10-24) were identified by comparison of their spectroscopic and physical data with those reported in the literature. Some of the purified constituents were examined for anti-inflammatory activity and, among the tested compounds, houpulins G (3), I (5), J (6), and 2,2'-dihydroxy-3-methoxy-5,5'-di-(2-propenylbiphenyl) (19) significantly inhibited superoxide anion generation and elastase release with IC50 values ranging from 3.54 to 5.48 μM and 2.16 to 3.39 μM, respectively. Therefore, these neolignan derivatives have tremendous potential to be explored as anti-inflammatory agents.

摘要

从厚朴根部分离鉴定出9个新木脂素衍生物(1 - 9),并通过光谱和理化分析确定了它们的结构。其中,厚朴脂素E(1)和M(9)具有新颖的高体和去甲三降新木脂素骨架。此外,通过将其光谱和物理数据与文献报道的数据进行比较,鉴定出15个已知化合物(10 - 24)。对部分纯化成分进行了抗炎活性测试,在测试的化合物中,厚朴脂素G(3)、I(5)、J(6)和2,2'-二羟基-3-甲氧基-5,5'-二-(2-丙烯基联苯)(19)显著抑制超氧阴离子的产生和弹性蛋白酶的释放,IC50值分别为3.54至5.48 μM和2.16至3.39 μM。因此,这些新木脂素衍生物作为抗炎剂具有巨大的开发潜力。

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