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β-取代羟基卟啉的锌(II)和铜(II)配合物作为肿瘤光敏剂

Zinc(II) and copper(II) complexes of beta-substituted hydroxylporphyrins as tumor photosensitizers.

作者信息

Huang Qimao, Pan Zhiquan, Wang Ping, Chen Zhangping, Zhang Xiaolian, Xu Hansheng

机构信息

Hubei Key Lab of Novel Reactor & Green Chemical Technology, Wuhan 430073, PR China.

出版信息

Bioorg Med Chem Lett. 2006 Jun 1;16(11):3030-3. doi: 10.1016/j.bmcl.2005.02.094. Epub 2006 Mar 15.

Abstract

Novel photosensitizers beta-(hydroquinon-2-yl)-5,10,15,20-tetra(4-hydroxylphenyl)porphyrinato zinc(II) (Zn(II)P) and beta-(hydroquinon-2-yl)-5,10,15,20-tetra(4-hydroxylphenyl)porphyrinato copper(II) (Cu(II)P) were synthesized and characterized. Their ability of producing singlet oxygen under irradiation was detected by the measurement of decomposition of 1,3-diphenylisobenzofuran (DPBF). The preliminary biological activity studies show that the Zn(II)P has photo-toxicity on human chronic myelogenous leukemia cell (K562) and could cleave supercoiled DNA (pBR 322 DNA), while the Cu(II)P has inferior biological activity. Results showed Zn(II)P having high anti-tumor activity, which presents a promising photosensitizer for photodynamic therapy.

摘要

合成并表征了新型光敏剂β-(对苯二酚-2-基)-5,10,15,20-四(4-羟基苯基)卟啉锌(II)(Zn(II)P)和β-(对苯二酚-2-基)-5,10,15,20-四(4-羟基苯基)卟啉铜(II)(Cu(II)P)。通过测量1,3-二苯基异苯并呋喃(DPBF)的分解来检测它们在光照下产生单线态氧的能力。初步生物学活性研究表明,Zn(II)P对人慢性髓性白血病细胞(K562)具有光毒性,并且能够切割超螺旋DNA(pBR 322 DNA),而Cu(II)P的生物学活性较差。结果表明Zn(II)P具有较高的抗肿瘤活性,是一种有前景的光动力治疗光敏剂。

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