Thimmegowda Naraganahalli R, Park Chanmi, Shwetha Bettaswamigowda, Sakchaisri Krisada, Liu Kangdong, Hwang Joonsung, Lee Sangku, Jeong Sook J, Soung Nak K, Jang Jae H, Ryoo In-Ja, Ahn Jong S, Erikson Raymond L, Kim Bo Y
World Class Institute (WCI), Incurable Diseases Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Cheongwon, 363-883, Korea; Department of Chemistry, Govt.S K S J T Institute, Bangalore, Karnataka, 560001, India.
Chem Biol Drug Des. 2015 May;85(5):638-44. doi: 10.1111/cbdd.12448. Epub 2014 Nov 5.
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 (1) H 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.
在本研究中，我们通过与各种氨基酸酯和取代芳香胺偶联，合成了天然化合物芦荟大黄素4(a - j)的新型水溶性衍生物，旨在提高其抗癌活性并探索构效关系。通过¹H NMR和质谱确定了化合物的结构。细胞生长抑制试验表明，芦荟大黄素衍生物4d、4f和4i有效降低了HepG2（人肝癌细胞）和NCI - H460（人肺癌细胞）的生长，并且在低微摩尔浓度下，一些衍生物对HeLa（人上皮癌细胞）和PC3（前列腺癌细胞）细胞系表现出与母体芦荟大黄素相当的抗肿瘤活性。
