目的 研究二氢卟吩P₆-6-(N-乙基)酰胺-7,γ-二甲酯锌(I)的合成及抗胃溃疡活性.方法 蚕沙糊状叶绿素经酸、碱降解反应制得紫红素-18(Ⅲ),Ⅲ经乙胺解后重氮甲烷甲基化制得二氢卟吩P₆-6-(N-乙基)酰胺-7,γ-二甲酯(Ⅱ),Ⅱ与醋酸锌络合制得I;以0.2%吲哚美辛(20 mg/kg)ip大鼠制备胃溃疡模型,并测定溃疡指数和溃疡个数.结果 I的结构经UV、IR、¹HNMR、FAB-MS及元素发射光谱确证.ipI 80mg/kg有极显著降低吲哚美辛诱发的大鼠溃疡指数(P＜0.01)和溃疡个数(P＜0.01).结论 I为新化合物,Ⅱ的波谱数据系首次报道.I对吲哚美辛诱发的大鼠胃溃汤具有显著的保护作用,提示I是一种有开发前景的抗溃疡候选化合物,值得深入研究.

Object To study the synthesis and experimental antigastriculcer activity of zinc chlorin P₆-6-N-ethylamide-7,γ-dimethylester(Ⅰ) Methods Purpurin 18 (Ⅲ) was prepared through alkaline oxidation of pheophorbide a (Ⅳ), which was synthesized by acid degradation using silkworm excrement crude chlorophyll extracts, and then I was synthesized by Zn(OAc) 2 complex reaction with chlorin P₆-6-N-ethylamide-7,γ-dimethylester(Ⅱ), which was formed via methylation as well as acetamide ammonification of Ⅲ Gastric ulcer model was made by ip 0 2% indomethacin at 20 mg/kg in rats and then the indexes and numbers of ulcer in gastric mucosa were measured Results I was identified by UV, IR, ¹HNMR and FAB MS spectra Compared with the control group, ipI at 80mg/kg was found to significantly reduce the index (P<0.01) and the number (P<0.01) of gastric ulcer induced by indomethacin in rats Conclusion I is a new compound and the spectral data of Ⅱ were reported for the first time The preliminary pharmacodynamic Resultsshowed that I has a significant protective effect against indomethacin induced gastric mucosa lesion in rats, and it is suggested that I may be developed as a potential antigastriculcer drug and it is worthy to further study.

国家自然科学基金资助项目 (39522003)