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从花椒中提取的具有细胞毒性和抗疟活性的吖啶酮生物碱。

Acridone alkaloids with cytotoxic and antimalarial activities from Zanthoxylum simullans Hance.

作者信息

Wang Chao, Wan Jinfu, Mei Zhinan, Yang Xinzhou

机构信息

College of Pharmacy, South-Central University for Nationalities, China.

Institute of Yunnan Baiyao Group Co. Ltd, China.

出版信息

Pharmacogn Mag. 2014 Jan;10(37):73-6. doi: 10.4103/0973-1296.126669.

DOI:10.4103/0973-1296.126669
PMID:24696549
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3969663/
Abstract

BACKGROUND

Zanthoxylum simullans Hance is a popular natural spice belonging to the Rutaceae family and it is one of the common prescribed herbs in traditional Chinese medicine.

MATERIALS AND METHODS

The chemical constituents were mainly isolated and purified by silica gel column chromatography and semi-preparative High Performance Liquid Chromatography. Their structures were identified by comparing the spectral data with those reported in the literature. Cytotoxic activities for the isolated acridone alkaloids were evaluated against two prostate cancer cell lines PC-3M and Lymph Node Carcinoma of Prostate (LNCaP), and their antimalarial activities were tested against two different strains of the parasite Plasmodium falciparum 3D7, and Dd2.

RESULTS

The root bark MeOH extract of Z. simullans Hance afforded β-sitosterol, 4-methoxy benzoic acid, daucosterol, and five acridone alkaloids, normelicopidine, normelicopine, melicopine, melicopidine, and melicopicine. All five acridone alkaloids were isolated from this plant for the first time and exhibited certain cytotoxic and antimalarial activities in vitro.

CONCLUSION

Normelicopidine was the most active against PC-3M, LNCaP and Dd2 with IC50 values of 12.5, 21.1, and 18.9 ug/mL respectively.

摘要

背景

青花椒是一种常见的天然香料,属于芸香科,是中药中常用的草药之一。

材料与方法

化学成分主要通过硅胶柱色谱和半制备高效液相色谱进行分离和纯化。通过将光谱数据与文献报道的数据进行比较来鉴定其结构。对分离得到的吖啶酮生物碱对两种前列腺癌细胞系PC-3M和前列腺淋巴结癌(LNCaP)进行细胞毒性活性评估,并对两种不同的恶性疟原虫菌株3D7和Dd2进行抗疟活性测试。

结果

青花椒根皮甲醇提取物得到β-谷甾醇、4-甲氧基苯甲酸、胡萝卜苷以及五种吖啶酮生物碱,降吴茱萸啶、降吴茱萸碱、吴茱萸碱、吴茱萸啶碱和吴茱萸次碱。这五种吖啶酮生物碱均首次从该植物中分离得到,并在体外表现出一定的细胞毒性和抗疟活性。

结论

降吴茱萸啶对PC-3M、LNCaP和Dd2的活性最强,IC50值分别为12.5、21.1和18.9μg/mL。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/088e/3969663/c7ab19378302/PM-10-73-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/088e/3969663/c7ab19378302/PM-10-73-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/088e/3969663/c7ab19378302/PM-10-73-g001.jpg

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