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Synthesis and In Vitro Studies of a Gd(DOTA)-Porphyrin Conjugate for Combined MRI and Photodynamic Treatment.
Inorganic Chemistry ( IF 4.3 ) Pub Date : 2020-09-22 , DOI: 10.1021/acs.inorgchem.0c02189
Sébastien Jenni 1 , Frédéric Bolze 2 , Célia S Bonnet 3 , Agnès Pallier 3 , Angélique Sour 1 , Éva Tóth 3 , Barbara Ventura 4 , Valérie Heitz 1
Affiliation  

With the aim of developing new molecular theranostic agents, a π-extended Zn(II) porphyrin as photosensitizer for photodynamic therapy (PDT) linked to two GdDOTA-type complexes for magnetic resonance imaging (MRI) detection was synthesized. The relaxivity studies revealed a much higher relaxivity value per Gd ion for this medium sized molecule (19.32 mM–1 s–1 at 20 MHz and 298 K) compared to clinical contrast agents—a value which strongly increases in the presence of bovine serum albumin, reaching 25.22 mM–1 s–1. Moreover, the photophysical studies showed the strong ability of the molecule to absorb light in the deep red (670 nm, ε ≈ 60000 M–1 cm–1) and in the near-infrared following two-photon excitation (920 nm, σ2 ≈ 650 GM). The conjugate is also able to generate singlet oxygen, with a quantum yield of 0.58 in DMSO. Promising results were obtained in cellular studies, demonstrating that the conjugate is internalized in HeLa cells at micromolar concentration and leads to 70% of cell death following 30 min irradiation at 660 nm. These results confirm the potential of the designed molecule as an imaging and therapeutic agent.

中文翻译:

Gd(DOTA)-卟啉结合物的合成及体外研究,用于MRI和光动力治疗。

为了开发新的分子治疗剂,合成了一种π-扩展的Zn(II)卟啉作为光敏剂,用于光动力疗法(PDT),与两个用于磁共振成像(MRI)检测的GdDOTA型复合物连接。弛豫性研究表明,与临床造影剂相比,这种中等大小的分子(20 MHz和298 K时为19.32 mM –1 s –1)的每Gd离子具有更高的弛豫值-在牛血清白蛋白存在下该值会大大增加,达到25.22 mM –1 s –1。此外,光物理研究表明,该分子具有很强的吸收深红色光的能力(670 nm,ε≈60000 M –1 cm –1),并在近红外以下双光子激发(920纳米,σ 2 ≈650 GM)。该缀合物还能够产生单线态氧,在DMSO中的量子产率为0.58。在细胞研究中获得了令人鼓舞的结果,表明缀合物以微摩尔浓度在HeLa细胞中内在化,并在660 nm照射30分钟后导致70%的细胞死亡。这些结果证实了所设计的分子作为成像和治疗剂的潜力。
更新日期:2020-10-05
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