Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 866# Yuhangtang Road, Hangzhou, 310058, People's Republic of China.
State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long Taipa, Macau, People's Republic of China.
BMC Complement Med Ther. 2020 Feb 3;20(1):29. doi: 10.1186/s12906-020-2831-y.
Crocetin is a major active component of saffron, which has a wide range of pharmacological effects. However, due to its low solubility, the pharmacological effects of crocetin cannot be better utilized.
In this study, we modified the chemical structure of crocetin by conjugating with ethylamine and 4-Fluorbenzylamine to enhance its solubility and biological activities. The solubility and the influence of synthesized derivatives on the proliferation of tumor cells and the inflammatory effect of macrophage were investigated.
It was shown that, compared with the crocetin, the synthesized derivatives have much higher solubility. Moreover, the inhibitory effect of the derivatives on varieties of tumor cells, including human ovarian carcinoma cell line, human lung cancer cell line, rat melanoma cell line was enhanced after the modification. Besides that, the derivatives were improved for the anti-inflammatory efficacy with the cytotoxicity decreased.
The synthesized derivatives were shown for their good solubility and the great potential in tumor and inflammation treatment.
西红花酸是西红花的主要活性成分，具有广泛的药理作用。然而，由于其溶解度低，西红花酸的药理作用不能得到更好的利用。
本研究通过与乙胺和 4-氟苯甲胺偶联，修饰西红花酸的化学结构，以提高其溶解度和生物活性。研究了合成衍生物的溶解度以及对肿瘤细胞增殖和巨噬细胞炎症效应的影响。
与西红花酸相比，合成衍生物的溶解度大大提高。此外，修饰后的衍生物对多种肿瘤细胞（包括人卵巢癌细胞系、人肺癌细胞系、大鼠黑色素瘤细胞系）的抑制作用增强。此外，衍生物的抗炎效果得到改善，同时细胞毒性降低。
合成衍生物具有良好的溶解度，在肿瘤和炎症治疗方面具有很大的潜力。
