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鸦胆子根中的苦木素类化合物及其对人癌细胞系的抗增殖活性。

Quassinoids from the Root of and Their Antiproliferative Activity on Human Cancer Cell Lines.

作者信息

Tung Nguyen Huu, Uto Takuhiro, Hai Nguyen Thanh, Li Gang, Shoyama Yukihiro

机构信息

Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Nagasaki International University, Sasebo, Nagasaki 859-3298, Japan.

Department of Pharmacy, School of Medicine and Pharmacy, Vietnam National University, Hanoi, Vietnam.

出版信息

Pharmacogn Mag. 2017 Jul-Sep;13(51):459-462. doi: 10.4103/pm.pm_353_16. Epub 2017 Jul 19.

Abstract

BACKGROUND

The roots of Jack have traditionally been used as an aphrodisiac tonic besides the other remedies for boils, fever, bleeding gums, and wound ulcer. Recently, the antiproliferative activity of has been reported and remained attractive to natural chemists.

OBJECTIVE

The objective of this study was to study on antiproliferative compounds from the root of .

MATERIALS AND METHODS

Column chromatography was used to separate individual compounds, spectroscopic data including nuclear magnetic resonances and mass spectrometry were analyzed to determine the chemical structure of the isolates and for biological testing, antiproliferative activity of compounds was tested on seven human cancer cell lines (KATO III, HCT-15, Colo205, HepG2, PC-3, Jurkat, HL-60) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method.

RESULTS

Nine quassinoids including a new C longilactone-type quassinoid glycoside were characterized from the roots of the title plant. Among them, the major quassinoid eurycomanone exhibited selectively potential antiproliferative activities on the leukemia cell lines (HL-60 and Jurkat) and had very low toxic effects on normal skin fibroblast cell line (NB1RGB).

CONCLUSION

The current study reveals one new quassinoid glycoside and the potential active component (eurycomanone) from for the leukemia treatment.

SUMMARY

Nine quassinoids (1-9) including one new quassinoid glycoside (9) and eight known ones were isolated from the roots of The structure of the new quassinoid 9 was determined by extensive chemical and spectroscopic analysesThe major quassinoid, eurycomanone (3), exhibited selectively potential antiproliferative activities on both Jurkat and HL-60 leukemia cells and had very low toxic effects on normal skin fibroblast cell line (NB1RGB). COSY: Correlation spectroscopy; HMBC: Heteronuclear multiple-bond correlation; HMQC: Heteronuclear multiple quantum correlation; NMR: Nuclear magnetic resonance; NOESY: Nuclear Overhauser enhancement spectroscopy; TLC: Thin layer chromatography.

摘要

背景

除了用于治疗疖子、发烧、牙龈出血和伤口溃疡等其他疾病外,杰克树的根传统上还被用作壮阳滋补品。最近,已报道了其抗增殖活性,这仍然吸引着天然化学家。

目的

本研究的目的是研究杰克树根中的抗增殖化合物。

材料与方法

采用柱色谱法分离单个化合物,分析包括核磁共振和质谱在内的光谱数据,以确定分离物的化学结构,并进行生物学测试,通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐法在七种人类癌细胞系(KATO III、HCT-15、Colo205、HepG2、PC-3、Jurkat、HL-60)上测试化合物的抗增殖活性。

结果

从标题植物的根中鉴定出九种苦木素类化合物,包括一种新的C长内酯型苦木素类糖苷。其中,主要的苦木素类化合物刺蒺藜皂苷元对白血病细胞系(HL-60和Jurkat)表现出选择性潜在抗增殖活性,对正常皮肤成纤维细胞系(NB1RGB)的毒性作用非常低。

结论

本研究揭示了一种新的苦木素类糖苷和杰克树中用于白血病治疗的潜在活性成分(刺蒺藜皂苷元)。

总结

从杰克树的根中分离出九种苦木素类化合物(1-9),包括一种新的苦木素类糖苷(9)和八种已知化合物。通过广泛的化学和光谱分析确定了新苦木素类化合物9的结构。主要的苦木素类化合物刺蒺藜皂苷元(3)对Jurkat和HL-60白血病细胞均表现出选择性潜在抗增殖活性,对正常皮肤成纤维细胞系(NB1RGB)的毒性作用非常低。COSY:相关光谱法;HMBC:异核多键相关;HMQC:异核多量子相关;NMR:核磁共振;NOESY:核Overhauser增强光谱法;TLC:薄层色谱法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/323d/5551365/defbd94acfde/PM-13-459-g001.jpg

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