血卟啉衍生物YHPD主要成分的核磁共振研究

本文报道国产血卟啉衍生物YHPD作为一种良好的光敏药物,已成功地用于肿瘤的光化学治疗。本文报道了对它的主要组分进行NMR结构分析的结果。将YHPD经高压液相色谱分离后,得到4个主要成分:A,B,C和D。其NMR结果表明,组分A为单乙酰基血卟啉,组分B和C为一对乙烯基次卟啉异构体,组分D通过二维同核相关、二维NOE,~(13)C谱、偏共振和快原子轰击质谱分析,证明为由C—C键相接的原卟啉二聚体。这一发现有助于从组分结构上对国产和国外血卟啉衍生物生物学活性的比较,也有助于认识临床使用的经碱处理的血卟啉衍生物(一种复杂混合物)的成分组成及有效成分。     

NMR STUDY ON THE MAJOR COMPONENTS IN HEMATOPORPHYRIN DERIVATIVE YHPD

The hematoporphyrin derivative YHPD, a China-made product, has been clinically used in photodynamic therapy of tumors as a good photosensitizing drug. The NMR study on the structure of its major components is reported here. In terms of high performance liquid chromatography (HPLC) four major components A, B, C and D were isolated. The NMR results showed that the component A is O-acetylhematoporphyrin, B and C are two isomers of vinyldeuteroporphyrin. The spectra of 2-dimensional homonuclear correlation NMR, 2-dimensional NOE (nuclear overhauser enhancement), ~(13)C-NMR and off-resonance as well as FAB (fast atom bombarding) mass spectrum of component D indicate that it is a protoporphyrin dimer linked by carbon-carbon bond. This finding may providea chemical basis for understanding the difference in biological activity between YHPD and other foreign commercial HPD, as well as the composition of clincally used alkali-treated HPD and its effective component.