【摘要】 本文研究了抗癌药物氮三乙酰肼（Nitrilotriacetic hydrizide,NTH）和生命必需元素以及Al³⁺,Ga³⁺,In³⁺的配位能力并用pH电位法测定了它们在生理条件下(37℃,Ⅰ=150mM dm^-3NaCl)的配合物生成常数。电位滴定数据是用ZPLOT,MINIQUAD,ESTA等计算机程序处理的。实验结果表明NTH与它的非生理活性的母体化合物氮三乙酸相比较,对Zn²⁺,Mn²⁺等过渡元素的配位能力表现较大的差异性。这种情况在Revercan,ICRF-198,ICRF-236和5-烯去甲基斑蝥酸等其他抗肿瘤活性化合物中也曾观察到。 NTH与三价金属Fe³⁺,Ga³⁺,Al（3+）和In³⁺等有较大的配位能力,这与它的烯醇式结构有关。由于这些配合物在广泛的pH范围内生成,以及它的高稳定性,因此有可能被用作为肿瘤定位试剂或生物体营养元素铁传输的有效载体。更多还原

【Abstract】 The binding ability of a number of biological essential metals as well as the IIIA group metals-A13+, Ga3+ and In3+ to the antitumour drug Nitrilotriacetic hydrizide (NTH) has been studied. Formation constants of these NTH complexes have been measured potentiometrically at 37℃ and I - 150mM dm-3 NaCl. The potentiometeric data were treated by the computer programs ZPLOT, MINIQUAD and ESTA.It has been shown that there is an abnormity on metal complexing ability between drug ligand NTH and its inactive parent compound Nitrilotriacetic acid, especially for biological trace metals such as Zn2+ and Mn2+. This situation was also observed in the case of other antitumour agents sach as Revercan, ICRF-198, ICRF-236, Oxabicyclo[ 2 , 2 , 1 ] hept-5-ene-2, 3-dicarboxylic acid. If the chelation does play role on the cancer the abnormity might be the one of reasons which are responsible for the difference in cytotoxicity exhibited by the antitumour agents and the inactive structural analogues.NTH also shows the complex formation of high stability with Fe3+, A13+, Ga3+ and In3+ in a wide range of pH. These complexes might be valuable as a tumour-localizing agents and carrier of trace element.更多还原