水溶性金属卟啉衍生物的合成及其对癌细胞生长的抑制活性

SYNTHESIS OF WATER-SOLUBLE DERIVATIVES OF PORPHYRIN-METAL COMPLEX AND ITS EFFCTS ON TUMOR CELL GROWTH

用聚乙二醇(plyethlene glycol)修饰原叶啉(protoporphyrin),以及在原卟啉环中导入金属离子合成7种水溶性金属卟啉衍生物。这些卟啉衍生物对癌细胞的生长有显著的抑制作用,特别是对pp—PEG,hemin—PEG以及pp(Mn)—PEG抑制率很高。在浓度为100μM时抑制率几乎达100％。对于PP—PEG和hemin—PEG当浓度为0.8μM时抑制率即达30％。这种抑制活性与其过氧化物歧化酶样活性和过氧化物酶活性无一致关系。

Protoporphyrim was modified with polye thylene glycol and some metals such as Cu,Pd, Zn,Mn, Ag,Co and Ga were introduced into its active center. The protoporphyrin derivateves exhibited the marked inhibition for the cell growth of highly lung metastic cell line of murine melanoma (B16F10). The inhibit on degree was high,in particular,for protopor-thyrin-PEG,hemin-PEG and protoporphyrin [Mn] -PEG, and almost reached up to 100% at a dose of 100μM,No correlation betweem the inhibition of cell growth and the enzymatic activities of superoxide dismutase and peroxidaes of the protoporphyrin derivatives was observed.