PHOTOSENSITIZING PROPERTIES OF MONO-L-ASPARTYL CHLORIN E(6) (NPE6) - A CANDIDATE SENSITIZER FOR THE PHOTODYNAMIC THERAPY OF TUMORS
PHOTOSENSITIZING PROPERTIES OF MONO-L-ASPARTYL CHLORIN E(6) (NPE6) - A CANDIDATE SENSITIZER FOR THE PHOTODYNAMIC THERAPY OF TUMORS
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DOI：
10.1016/1011-1344(93)80006-u
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发表时间：
1993-02-01
影响因子：
5.4
通讯作者：
BOMMER, JC
中科院分区：
文献类型：
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作者：
SPIKES, JD;BOMMER, JC
人们对二氢卟酚作为肿瘤光动力疗法的光敏剂产生了很大的兴趣，因为它们对红色有很强的吸收作用，而光在红色中可以有效地渗透到哺乳动物组织中。单-L-天冬氨酰二氢卟酚e6 (NPe6)在pH 7.4的磷酸盐缓冲液中，在400和654 nm处有吸收峰，摩尔吸收系数分别为180000和40000 M-1 cm-1。在缓冲液中，NPe6 三联体在 440 nm 处有峰值，在氩气下的寿命约为 300 mu。该三线态被基态氧 (k(Q) = 1.9 X 10(9) M-1 s-1) 有效猝灭，并形成单线态氧，如其近红外发光所鉴定。单线态氧产生的量子产率为0.77。 NPe6 可有效光氧化许多底物，包括糠醇、半胱氨酸、组氨酸、色氨酸和人血清白蛋白。 这些反应被叠氮化物有效抑制（叠氮化物不会淬灭 NPe6 三联体），表明它们可能是由单线态氧介导的。 因此，NPe6 具有一系列理想的光特性，可作为临床肿瘤光动力治疗中使用的敏化剂。
There is a large amount of interest in chlorins as photosensitizers for the photodynamic therapy of tumors because of their strong absorption in the red, where light penetration into mammalian tissues is efficient. Mono-L-aspartyl chlorin e6 (NPe6), in phosphate buffer of pH 7.4, had absorption peaks at 400 and 654 nm with molar absorption coefficients of 180000 and 40000 M-1 cm-1 respectively. In buffer, the NPe6 triplet had a peak at 440 nm and a lifetime under argon of approximately 300 mus. The triplet was efficiently quenched by ground state oxygen (k(Q) = 1.9 X 10(9) M-1 s-1) with the formation of singlet oxygen, as identified by its near infrared luminescence. The quantum yield of singlet oxygen production was 0.77. A number of substrates were efficiently photo-oxidized by NPe6, including furfuryl alcohol, cysteine, histidine, tryptophan and human serum albumin. These reactions were efficiently inhibited by azide (which did not quench NPe6 triplets), indicating that they are probably mediated by singlet oxygen. Thus, NPe6 bas a desirable array of photoproperties for a sensitizer to be used in the clinical photodynamic therapy of tumors.