Water-soluble metalloporphyrinates with excellent photo-induced anticancer activity resulting from high tumor accumulation.

Water-soluble metalloporphyrinates with excellent photo-induced anticancer activity resulting from high tumor accumulation.
J Inorg Biochem. 2017 Feb 04;170:1-7
Authors: Hu X, Ogawa K, Kiwada T, Odani A
Abstract
To develop a water-soluble and tumor-targeted photosensitizer for photodynamic therapy (PDT), a porphyrin framework containing the metal ion gallium(III) was combined with platinum(II)-based groups to produce two new pentacationic metalloporphyrinates, Ga-4cisPtTPyP (5,10,15,20-tetrakis{cis-diammine-chloro-platinum(II)}(4-pyridyl)-porphyrinato gallium(III) hydroxide tetranitrate) and Ga-4transPtTPyP (5,10,15,20-tetrakis{trans-diammine-chloro-platinum(II)} (4-pyridyl)-porphyrinato gallium(III) hydroxide tetranitrate). Both complexes exhibited high singlet oxygen quantum yields (Φ∆) and remarkable photocytotoxicity with appreciable phototoxic indexes (PIs). In particular, Ga-4cisPtTPyP showed a low IC50 value (Colon 26: 0.12μM; Sarcoma 180: 0.08μM) under illumination and its PI up to 1000. With outstanding tumor accumulation (tumor/muscle ratio>9), Ga-4cisPtTPyP almost completely inhibited tumor growth over two weeks in an in vivo PDT assay. These results imply that Ga-4cisPtTPyP could be a promising anticancer agent for use in PDT.
PMID: 28189031 [PubMed - as supplied by publisher]

Source: Journal of Inorganic Biochemistry - February 3, 2017 Category: Biochemistry Authors: Hu X, Ogawa K, Kiwada T, Odani A Tags: J Inorg Biochem Source Type: research