Research Center, Chengdu Medical College , Xindu Avenue 783, Chengdu 610500, People's Republic of China.
J Nat Prod. 2017 Apr 28;80(4):864-871. doi: 10.1021/acs.jnatprod.6b00697. Epub 2017 Feb 20.
Six new monoterpenoid indole alkaloids, kopsinidines C-E (1-3), 11,12-methylenedioxychanofruticosinic acid (4), 12-methoxychanofruticosinic acid (5), and N(4)-methylkopsininate (7), as well as chanofruticosinic acid (6, as a natural product) and 23 known alkaloids, were obtained from the twigs and leaves of Kopsia officinalis. Their structures were characterized by physical data analysis. All isolated compounds were evaluated for their immunosuppressive activity on human T cell proliferation. Rhazinilam (29) significantly inhibited human T cell proliferation activated by anti-CD3/anti-CD28 antibodies (IC = 1.0 μM) and alloantigen stimulation (IC = 1.1 μM) without obvious cytotoxicity for naïve human T cells and peripheral blood mononuclear cells (0-320 μM). Although it did not affect T cell activation, it induced T cell cycle arrest in the G/M phase and inhibited proinflammatory cytokine production in activated T cells.
从黄桐的嫩枝和叶中分离得到了 6 个新的单萜吲哚生物碱，分别为 kopsinidines C-E（1-3）、11,12-亚甲基二氧基香豆佛吕替酸（4）、12-甲氧基香豆佛吕替酸（5）和 N(4)-甲基考斯辛碱（7），以及香豆佛吕替酸（6，作为一种天然产物）和 23 种已知生物碱。通过物理数据分析对其结构进行了表征。所有分离得到的化合物都进行了人 T 细胞增殖的免疫抑制活性评价。瑞沙啉（29）对由抗-CD3/抗-CD28 抗体（IC = 1.0 μM）和同种抗原刺激（IC = 1.1 μM）激活的人 T 细胞增殖具有显著的抑制作用，对幼稚人 T 细胞和外周血单个核细胞（0-320 μM）没有明显的细胞毒性。尽管它不影响 T 细胞的激活，但它诱导 T 细胞周期停滞在 G/M 期，并抑制激活的 T 细胞中促炎细胞因子的产生。
