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Synthesis and Antitumor Activity of Natural Compound Aloe Emodin Derivatives |
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| Authors: | Bettaswamigowda Shwetha Krisada Sakchaisri Kangdong Liu Joonsung Hwang Sangku Lee Sook J. Jeong Nak K. Soung Jae H. Jang In‐Ja Ryoo Jong S. Ahn Raymond L. Erikson Bo Y. Kim |
| Affiliation: | 1. World Class Institute (WCI), Incurable Diseases Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Cheongwon, Korea;2. Basic Medical College, Zhengzhou University, ZhengZhou, China;3. Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Cheongwon, Korea;4. Department of Molecular and Cellular Biology, Harvard University, Cambridge, MA, USA |
| Abstract: | 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 1H 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. |
| Keywords: | aloe emodin aloe emodin derivatives antitumor activity NCI‐H460 cells Hep G2 cells structure activity relationship |