抗肿瘤活性化合物去甲基斑蟊-5-烯酸的金属配位能力的研究

Binding Ability of Antitumour Compound 7-Oxabicyclo-[2.2.1]-hept-5-ene-2,3-dicarboxylic Acid to Metal Ions

七百多年前我国古书就有过斑蟊作为药物的记载[1].Baranger曾报道过斑蟊素等具有抗癌活性,特别对于淋巴瘤[2].七十年代开始.

The binding ability of antitumour compound 7-oxabicyelo-[2.2.1]-hept-5-ene-2,3-dicarboxylic acid(OHDA)to essential metal ions has been studied potentiometrically at 37±0.1℃and 150mmol·dm^(-3)NaCl.Comparing to other dicarboxylic acids OHDA complexes show extra stability implying the ligation of epoxy oxygen atom to metal ions.The coordination of epoxy oxygen donor has been proved by X-ray crystal diffraction measurements of M2+-OHDA complexes.Speciation studies illustrate that in the region of pH 6-8 the dominant complex species is Zn^(2+)-OHDA,but it is very interesting to note that at low OHDA concentration(10^(-4)-10^(-7)mol·dm^(-3))the Mn^(2+)-OHDA complex species shares the predominant position with Zn^(2+)-OHDA in the complex system.This fact may be related to the antitumour activity of some ligand drug molecules by disturbing normal distribution and metabolism of essential metal ions.