一个新颖的人参皂苷元衍生物及其抗肿瘤活性（英文）

李瑞; 陈晨; 邹澄; 赵庆; 郭巍怡; 黄丽; 杜如男; 杨为民

一个新颖的人参皂苷元衍生物及其抗肿瘤活性（英文）

1. 昆明医科大学药学院暨云南省天然药物药理重点实验室
2. 云南中医学院中药学院

基金项目:

基金： The National Natural Science Fundation of China (8116038); Yunnan Provincial Science and Technology Department-Kunming Medical University Applied Basic Research Joint Special Fund Project (K13201288); Yunnan Provincial Natural Drugs Key Laboratory of Open Research Fund funded projects (2017KPO-04); The Graduate Innovation Fund of Kunming Medical University (2017S070);

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出版历程
- 收稿日期: 2017-04-21

A Novel Derivatives of Ginsenoside Sapogenin and Its Activity Against Tumor

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摘要

摘要: 目的研究人参皂苷元衍生物及其抗肿瘤活性.方法通过Smith降解法水解人参皂苷Rg1和Rb1, 采用硅胶柱层析分离和纯化水解得到的产物, 通过NMR的数据分析鉴定产物的结构.结果分离得到20 (S) -原人参三醇、20 (S) -原人参二醇、1, -羟基双氧乙基原人参三醇 (1) , 1, -羟基双氧乙基原人参二醇 (2) .结论 smith降解法能得到人参皂苷元衍生物, 化合物 (2) 为新颖的人参皂苷元衍生物, 其能抑制细胞周期分裂蛋白25B, 具有抗肿瘤的活性.
- 1, -羟基双氧乙基原人参二醇 /
- 三七总皂苷 /
- Smith降解法 /
- CDC25B /
- 人参皂苷元衍生物
Abstract: Objective To study the derivatives of ginsenoside sapogenins and their activities against tumor.Methods The ginsenosides Rg1 and Rb1 were treated with Smith degradation. The products were separated and purified by silica gel column chromatography. The structures of the products were determined by NMR spectra.The activity of anti-tumor cells of compound (1) and compound (2) was detected with CDC25 B activity assay and fluorescence technique.Results 20 (S) -protopanaxadiol (PD) , 20 (S) -protopanaxatriol (PT) , 1'-hydroxy ethanedioxy PT (1) and 1'-hydroxy ethanedioxy PD (2) were isolated and identified. Conclusion During the Smith degradation, we obtained the derivatives of ginsenoside sapogenins. Compound 2 is a novel derivative of ginsenoside sapogenin.Compound 2 is a novel derivative of ginsenoside sapogenin with higher inhibitory activity against cell division cycle 25 homolog B.
- 1'-hydroxy ethanedioxy-protopanaxatriol /
- Panax notoginseng saponins /
- Smith degradation /
- CDC25B /
- Ginsenoside sapogenin derivative

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参考文献(16)

[1]	[1]YANG C R, DING Y F, SU M, et al.Sanqi Resources and Panax Industry[A].2012 Cross-Strait and CSNRNational Symposium on Traditional Chinese Medicine and Natural Medicinal Resources[C], 49-55.
[2]	[2]Yunnan Institute of Drug Research, Yunnan important natural medicine[M].Kunming:Yunnan Science and Technology Press, 2006:9.
[3]	[3]HAN B H, PARK M H, HAN Y N.Degradation of ginseng saponins under mild acidic conditions[J].Planta Medica, 1982, 44 (11) :146-149.
[4]	[4]QIAO C L, DING Y F, YANG C R.Progresses of Panax notoginseng Saponins in Pharmacology[J].Modern Chinese Medicine, 2012, 14 (11) :25-30.
[5]	[5]LIU J, WANG Y, QIU L, et al.Saponins of Panax notoginseng:Chemistry, cellular targets and therapeutic opportunities in cardiovascular diseases[J].Expert Opin Investig Drugs, 2014, 23 (4) :523-539.
[6]	[6]NG T.Pharmacological activity of sanchi ginseng (Panax notoginseng) [J].JPP, 2006, 58 (8) :1007-1019.
[7]	[7]PU H, DONG C M, ZOU C, et al.Synthesis and Antitumor Activity of Panax Notoglucose Saponin Sulfonamide Derivatives[J].Natural Product Research and Development, 2014, 26 (11) :1739-1744.
[8]	[8]POPOVICH D G, KITTS D D.Stucture-function relationship exists for ginsenosides in reducing cell proliferation and inducing apoptosis in the human leukemia (THP-1) cell line[J].Arch Biochem Biophys, 2002, 406 (1) :1-8.
[9]	[9]LI ZHENG H.Medicinal Chemistry[M].Bei Jing:People's Health Publishing House, 1996, 188.
[10]	[10]KONDO N.Studies on the Constituents of Panacis Japonici Rhizoma.IV1) .The Structure of Chikusetsusaponin V[J].Chem Pharm Bull, 1971, 19 (6) , 1103.
[11]	[11]WEI J X, DU Y C.Modern science research and application[M].Kunming:Yunnan Science and Technology Press, 1996:102-103.
[12]	[12]NAGAI M, ANDO T, TANAKA N, et al.Chemical studies on the Oriental plant drugs.XXVIII1) .Saponins and sapogenins of Ginseng.Stereochemistry of the sapogenin of Ginsenosides-Rb1, Rb2, and Rc[J].Chem Pharm Bull, 1972, 20 (6) :1212-1216.
[13]	[13]HUANG Z Y, ZHAO S D, ZOU C, et al.Synthesis of four derivatives of Panax notoginseng trioside total saponins and ginseng triol[J].Journal of Kunming Medical College, 2011, 32 (11) :10-12.
[14]	[14]YUAN J X, SHAO Y F, ZOU C, et al.The reduction of ginsenoside diol diketone lactone[J].Journal of Kunming Medical University, 2013, 34 (1B) :7-9.
[15]	[15]ZHANG Y, SHAO Y F, ZOU C, et al.Reduction of sodium borohydride by six-uptake of methane.and triterpenes[J].Chinese folk medicine, 2011, 20 (17) :32.
[16]	[16]LI H F, GUO H Z, GUO D A.A novel derivative of ginsenoside sapogenin and its activity against HL-60 cells[J].Chinese Traditional and Herbal Drugs, 2010, 1 (41) :6-8.

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