目的研究臭梧桐Clerodendrum trichotomum根的化学成分及其抗炎活性。方法利用硅胶柱色谱、葡聚糖凝胶柱色谱并结合半制备HPLC进行分离与纯化;通过理化性质和波谱数据鉴定化合物的结构;根据化合物对趋化因子白细胞介素-8(IL-8)生成的抑制作用考察化合物的抗炎活性。结果从臭梧桐干燥根中分离到4个24-乙基胆甾烷类化合物,分别鉴定为24-ethyl-7-oxocholesta-5,22(E),25-trien-3β-ol(1)、decortinone(2)、22-dehydroclerosterol(3)和clerosterol(4)。结论化合物1~3为首次从臭梧桐的根中分离得到,并确定化合物1的24位的绝对构型为S型。体外抗炎活性筛选显示化合物1可剂量依赖性地抑制由IL-1β诱导的结肠癌HT-29细胞中IL-8的生成。
Objective To investigate the anti-inflammatory chemical constituents from the roots of Clerodendrum trichotomum. Methods The compounds were isolated and purified by silica gel, Sephadex LH-20 column chromatographies, as well as prep-HPLC; Their structures were characterized on the basis ofphysicochemical properties and their spectral analysis; An in vitro anti-inflammatory method was applied to determine their activities against interleukin-8 (IL-8) production. ResuRs Four 24-ethylcholestane derivatives have been identified as 24-ethyl-7-oxocholesta-5, 22(E), 25-trien-3β-ol (1), decortinone (2), 22-dehydroclerosterol (3), and clerosterol (4). Conclusion Coumpounds 1--3 are isolated from the roots of C. trichotomum for the first time. The absolute configuration of C-24 of compound 1 is determined to be S. In an in vitro anti-inflammatory assay, compound 1 is found to show a remarkable inhibition on IL-8 production induced by interleukin-1β (IL-113) in HT-29 cells.