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模拟自然界对四吡咯染料的β位调节方式,结合卟吩内酯近红外吸收和三线态能级可调、且易于修饰的优点,设计并合成了Gd(Ⅲ)卟吩内半缩醛配合物,并通过水溶性铵基修饰,使之具有两亲性质。该类配合物能较好地敏化O_2,单线态氧量子产率约0.75,且可应用于光毒性治疗,即使在红光(600~700 nm)激发下,其对He La细胞的半数致死浓度(IC50)仍低至1.5μmol·L~(-1)。同时,Gd-4的纵向弛豫率(r1)为1.1 mmol·L~(-1)·s~(-1)(0.5 T,37℃),表明配合物具有磁共振成像造影能力。因此,这类化合物具有光、磁双功能诊疗的潜在应用价值。
In order to simulate the β-site regulation of tetrapyrrole dye in nature and to combine the near-infrared absorption of porpolypyrolactone with the adjustable triplet energy level and easy modification, we designed and synthesized Gd (Ⅲ) , And through the water-soluble ammonium modified to make it amphipathic. The complexes can sensitize O 2 well, and the singlet oxygen quantum yield is about 0.75, which can be applied to phototoxicity therapy. Even under the excitation of red light (600-700 nm), the half-lethality of He La cells The concentration (IC50) was still as low as 1.5μmol·L -1. At the same time, the longitudinal relaxation rate (r1) of Gd-4 was 1.1 mmol·L -1 s -1 (0.5 T, 37 ° C), indicating that the complexes have the ability of magnetic resonance imaging. Therefore, these compounds have the potential applications of light and magnetic bifunctional diagnosis and treatment.