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从木贼中提取的石松型生物碱具有细胞毒性和胆碱酯酶抑制活性。

Lycodine type alkaloids from Lycopodiastrum casuarinoides with cytotoxic and cholinesterase inhibitory activities.

机构信息

Department of Dermatology, Second Hospital of Jilin University, Changchun 130041, China.

Department of E.N.T., Second Hospital of Jilin University, Changchun 130041, China.

出版信息

Fitoterapia. 2018 Nov;131:86-90. doi: 10.1016/j.fitote.2018.10.021. Epub 2018 Oct 21.

Abstract

A chemical investigation on the 70% EtOH extract of the aerial parts of Lycopodiastrum casuarinoides led to the isolation of six novel lycodine type alkaloids, lycocasuarines A-F (1-6). The structures of the isolated compounds were established based on 1D and 2D (HH COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated alkaloids were tested in vitro for cytotoxic potentials against seven malignant melanoma cell lines as well as acetylcholinesterase (AChE) and butyrocholinesterase (BuChE) inhibitory activities. As a result, alkaloids 1 and 3 exhibited significant cytotoxic activities against all the tested tumor cell lines with IC values <10 μM and the inhibitory activities for AchE (0.94 ± 0.15 and 0.24 ± 0.03 μM, respectively) and BuchE (1.82 ± 0.12 and 7.31 ± 0.42 μM, respectively).

摘要

对鹿角叶 Lycopodiastrum casuarinoides 的地上部分 70%乙醇提取物进行化学研究,分离得到了六种新型石松堿型生物碱,分别命名为 lycocasuarines A-F(1-6)。根据 1D 和 2D(HH COSY、HMQC 和 HMBC)NMR 光谱以及高分辨率质谱,确定了分离得到的化合物的结构。对分离得到的生物碱进行了体外细胞毒性测试,评估了它们对七种恶性黑素瘤细胞系的抑制作用,以及乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BuChE)抑制活性。结果表明,生物碱 1 和 3 对所有测试的肿瘤细胞系均具有显著的细胞毒性,IC 值均<10 μM,对 AchE(分别为 0.94 ± 0.15 和 0.24 ± 0.03 μM)和 BuchE(分别为 1.82 ± 0.12 和 7.31 ± 0.42 μM)的抑制活性也较强。

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