Coderre J A, Glass J D, Packer S, Micca P, Greenberg D
Medical Department, Brookhaven National Laboratory, Upton, NY 11973.
Pigment Cell Res. 1990 Dec;3(6):310-8. doi: 10.1111/j.1600-0749.1990.tb00303.x.
The boron-containing melanin precursor analogue p-boronophenylalanine (BPA) has previously been shown to selectively deliver boron to pigmented murine melanomas when administered in a single intragastric dose. If boron neutron capture therapy is to become a clinically useful method of radiation therapy for human malignant melanoma, the boron carrier must be capable of delivering useful amounts of boron to remote tumor sites (metastases) and to poorly pigmented melanomas. We have now determined the ability of BPA to accumulate in several nonpigmented melanoma models including human melanoma xenografts in nude mice. The absolute amount of boron in the nonpigmented melanomas was about 50% of that observed in the pigmented counterparts but was still selectively concentrated in the tumor relative to normal tissues in amounts sufficient for effective neutron capture therapy. Single intragastric doses of BPA resulted in selective localization of boron in the amelanotic Greene melanoma carried in the anterior chamber of the rabbit eye and in a pigmented murine melanoma growing in the lungs. The ratio of the boron concentration in these tumors to the boron concentration in the immediately adjacent normal tissue was in the range of 3:1 to 4:1. These distribution studies support the proposal that boron neutron capture therapy may be useful as a regional therapy for malignant melanoma.
含硼黑色素前体类似物对硼苯丙氨酸（BPA）先前已被证明，单次胃内给药时可将硼选择性地输送至色素沉着的小鼠黑色素瘤。如果硼中子俘获疗法要成为治疗人类恶性黑色素瘤的一种临床有用的放射治疗方法，硼载体必须能够将足量的硼输送至远处肿瘤部位（转移灶）以及色素沉着较差的黑色素瘤。我们现已确定BPA在几种无色素黑色素瘤模型中（包括裸鼠体内的人黑色素瘤异种移植物）的蓄积能力。无色素黑色素瘤中的硼绝对含量约为有色素黑色素瘤的50%，但相对于正常组织，硼仍选择性地在肿瘤中浓缩，其含量足以进行有效的中子俘获治疗。单次胃内给予BPA可使硼选择性地定位于兔眼前房中携带的无黑色素的格林黑色素瘤以及肺部生长的有色素小鼠黑色素瘤中。这些肿瘤中的硼浓度与紧邻的正常组织中的硼浓度之比在3:1至4:1的范围内。这些分布研究支持了硼中子俘获疗法可用作恶性黑色素瘤区域治疗方法的提议。
