一种α-黑素细胞刺激素的螯合衍生物，作为恶性黑色素瘤的潜在成像剂。
A chelating derivative of alpha-melanocyte stimulating hormone as a potential imaging agent for malignant melanoma.
作者信息
Bard D R, Knight C G, Page-Thomas D P
机构信息
Strangeways Research Laboratory, Worts' Causeway, Cambridge, UK.
出版信息
Br J Cancer. 1990 Dec;62(6):919-22. doi: 10.1038/bjc.1990.409.
A chelating derivative of alpha-melanocyte stimulating hormone (MSH) has been synthesised, in which two molecules of the hormone are cross-linked by diethylenetriamine pentaacetic acid (DTPA). This compound, bisMSH-DTPA, was equipotent with MSH in an in vitro tyrosinase assay with Cloudman S91 melanoma cells. When DBA/2 mice bearing the same tumour were injected with bisMSH-DTPA labelled with the gamma-emitting isotope indium-111 (111In), the radioactivity became rapidly associated with the melanoma tissue. By 24 h post-injection, radioactivity in tumour tissue was significantly higher (P less than 0.001) than in spleen, lung, brain, eye and skin. Uptake of radioactivity by the tumours was inhibited by a 200-fold molar excess of MSH, whereas uptake by liver, kidney, spleen, lung, brain, eye and skin was unaffected. We conclude that bisMSH-DTPA may offer an alternative to antibody targeting in the imaging of malignant melanoma.
已合成一种α-黑素细胞刺激素（MSH）的螯合衍生物，其中两分子该激素通过二乙烯三胺五乙酸（DTPA）交联。这种化合物，即双MSH-DTPA，在使用Cloudman S91黑色素瘤细胞的体外酪氨酸酶测定中与MSH具有同等效力。当给患有相同肿瘤的DBA/2小鼠注射用发射γ射线的同位素铟-111（111In）标记的双MSH-DTPA时，放射性迅速与黑色素瘤组织结合。注射后24小时，肿瘤组织中的放射性显著高于（P小于0.001）脾脏、肺、脑、眼和皮肤中的放射性。肿瘤对放射性的摄取受到200倍摩尔过量MSH的抑制，而肝脏、肾脏、脾脏、肺、脑、眼和皮肤对放射性的摄取未受影响。我们得出结论，双MSH-DTPA可能为恶性黑色素瘤成像中的抗体靶向提供一种替代方法。
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