Synthesis and Antitumor Activity of Natural Compound Aloe Emodin Derivatives

被引:28
作者
Thimmegowda, Naraganahalli R. [1 ,2 ]
Park, Chanmi [1 ]
Shwetha, Bettaswamigowda [1 ]
Sakchaisri, Krisada [1 ]
Liu, Kangdong [1 ,3 ]
Hwang, Joonsung [1 ]
Lee, Sangku [1 ]
Jeong, Sook J. [1 ]
Soung, Nak K. [1 ]
Jang, Jae H. [4 ]
Ryoo, In-Ja [4 ]
Ahn, Jong S. [4 ]
Erikson, Raymond L. [5 ]
Kim, Bo Y. [1 ]
机构
[1] KRIBB, Incurable Dis Res Ctr, WCI, Ochang 363883, Cheongwon, South Korea
[2] Govt SKSJT Inst, Dept Chem, Bangalore 560001, Karnataka, India
[3] Zhengzhou Univ, Basic Med Coll, Zhengzhou 450001, Peoples R China
[4] KRIBB, Chem Biol Res Ctr, Ochang 363883, Cheongwon, South Korea
[5] Harvard Univ, Dept Mol & Cellular Biol, Cambridge, MA 02138 USA
关键词
aloe emodin; aloe emodin derivatives; antitumor activity; NCI-H460; cells; Hep G2 cells; structure activity relationship; CANCER; DEATH; CELLS;
D O I
10.1111/cbdd.12448
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In this study, we have synthesized novel water soluble derivatives of natural compound aloe emodin 4(a-j) by coupling with various amino acid esters and substituted aromatic amines, in an attempt to improve the anticancer activity and to explore the structure-activity relationships. The structures of the compounds were determined by H-1 NMR and mass spectroscopy. Cell growth inhibition assays revealed that the aloe emodin derivatives 4d, 4f, and 4i effectively decreased the growth of HepG2 (human liver cancer cells) and NCI-H460 (human lung cancer cells) and some of the derivatives exhibited comparable antitumor activity against HeLa (Human epithelial carcinoma cells) and PC3 (prostate cancer cells) cell lines compared to that of the parent aloe emodin at low micromolar concentrations.
引用
收藏
页码:638 / 644
页数:7
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