从卵叶米仔兰中分离得到的木脂素和二萜及其生物活性。
Lignans and diterpenes isolated from Tirpitzia ovoidea and their biological activities.
机构信息
Department of Natural Medicine, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China.
Department of Natural Medicine, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China.
出版信息
Chin J Nat Med. 2017 Dec;15(12):938-943. doi: 10.1016/S1875-5364(18)30010-4.
A new lignan, tirpitzin A (17) together with 20 known compounds (1-16, and 18-21) were isolated from the ethyl acetate soluble fraction of ethanol extract of the aerial parts of Tirpitzia ovoidea. The structure of new compound was elucidated by means of spectroscopic analysis. Of the known compounds, 7-21 were isolated from Linaceae family for the first time. The pharmacological activity of the crude extracts was tested using a mouse inflammation model induced by dimethyl benzene. The results demonstrated that the ethyl acetate soluble fraction had anti-inflammatory activity. Moreover, the cytotoxic and anti-inflammatory activities of some compounds were studied. The new compound 17 showed moderate cytotoxic effect against BxPC-3 cell line (IC = 19.51μmol·L) and Compound 10 showed significant cytotoxicity against HepG2, HL-60, U87 and BxPC-3 cell lines with IC values in the range 4.2-8.3μmol·L. Additionally, Compounds 2, 10, 11, and 13 exhibited potent inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages at the concentration of 50μmol·L.
从 Tirpitzia ovoidea 地上部分的乙醇提取物的乙酸乙酯可溶部分分离得到一种新的木脂素，即 tirpitzin A（17），以及 20 种已知化合物（1-16 和 18-21）。新化合物的结构通过光谱分析阐明。在已知化合物中，7-21 是首次从亚麻科中分离得到的。使用二甲苯诱导的小鼠炎症模型测试了粗提取物的药理活性。结果表明，乙酸乙酯可溶部分具有抗炎活性。此外，研究了一些化合物的细胞毒性和抗炎活性。新化合物 17 对 BxPC-3 细胞系表现出中等的细胞毒性作用（IC=19.51μmol·L），化合物 10 对 HepG2、HL-60、U87 和 BxPC-3 细胞系表现出显著的细胞毒性作用，IC 值范围为 4.2-8.3μmol·L。此外，化合物 2、10、11 和 13 在 50μmol·L 的浓度下对 LPS 诱导的 RAW 264.7 巨噬细胞中一氧化氮的产生具有很强的抑制作用。
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