State Key Laboratory of Natural Medicines, Department of TCM Pharmaceuticals, School of Traditional Chinese Pharmacy , China Pharmaceutical University , Nanjing 210009 , People's Republic of China.
Department of Traditional Medicine, School of Pharmacy , Haiphong University of Medicine and Pharmacy , 72 A Nguyen Binh Khiem , Haiphong City , Vietnam.
J Nat Prod. 2019 Apr 26;82(4):859-869. doi: 10.1021/acs.jnatprod.8b00920. Epub 2019 Mar 8.
Five new phloroglucinol derivatives, eucalyptins C-G (1-5), together with 13 known analogues (6-18) were isolated from the fruits of Eucalyptus globulus. The structures and absolute configurations of 1-5 were established by means of spectroscopic data analysis, computational calculation methods, and single-crystal X-ray diffraction. Compounds 1-18 were investigated for their immunosuppressive effects in vitro, and 1, 2, 6, and 7 displayed moderate inhibitory activities with IC values of 11.8, 10.2, 18.2, and 19.1 μM, respectively. The stimulation index (SI) of 1 was 64.2 and was compared to that of cyclosporine A (SI = 149.57). Further study demonstrated that 1 exhibited an immunosuppressive effect through inducing apoptosis and inhibiting cytokine secretion.
从桉树果实中分离得到了 5 个新的间苯三酚衍生物，即桉树素 C-G（1-5），以及 13 个已知类似物（6-18）。通过光谱数据分析、计算计算方法和单晶 X 射线衍射，确定了 1-5 的结构和绝对构型。对 1-18 化合物进行了体外免疫抑制活性研究，化合物 1、2、6 和 7 表现出中等抑制活性，IC 值分别为 11.8、10.2、18.2 和 19.1 μM。化合物 1 的刺激指数（SI）为 64.2，与环孢素 A（SI=149.57）进行了比较。进一步的研究表明，1 通过诱导细胞凋亡和抑制细胞因子分泌发挥免疫抑制作用。
