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Studies towards elucidating the potential of 5,10,15,20-tetrakis(p-carboxymethyleneoxyphenyl)porphyrin as a theranostic agent for applications in PET and PDT

Abstract

Porphyrins, owing to their inherent tendency to accumulate in tumorous lesions, are considered suitable for developing agents for theranostic applications involving tumor diagnosis and targeted tumor therapy. The aim of the present work is to study the potential of a porphyrin derivative namely, 5,10,15,20-tetrakis(p-carboxymethyleneoxyphenyl)porphyrin (SPTA) as a theranostic agent for applications in positron emission tomography (PET) and photodynamic therapy (PDT). SPTA was synthesized in-house following a three-step reaction process and characterized by using spectroscopic techniques viz. UV-Vis, FT-IR, 1H-NMR, 13C-NMR spectroscopy as well as by mass spectrometry. SPTA was labeled with 68Ga, a generator produced PET radioisotope and the radiolabeled product was characterized by HPLC. The 68Ga-SPTA complex was prepared with a radiochemical purity >95 % under the optimized conditions. Diagnostic potential of 68Ga-SPTA was evaluated by cell uptake studies in two different tumor cell lines (HT1080 and AT549) which revealed affinity of 68Ga-SPTA towards the cancer cells. The biodistribution studies carried out in Swiss mice bearing fibrosarcoma tumors exhibited accumulation of the radiotracer in tumor. The therapeutic potential of SPTA was evaluated by determining its photocytotoxity employing MTT assay in HT1080 and AT549 cell lines using three different light doses, which indicated significant cytotoxicity of SPTA in presence of light. The present study indicates the possible potential of SPTA in radionuclidic imaging as well as in photodynamic therapy (PDT) thus confirming the promising theranostic nature of the porphyrin derivative.

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Publication details

The article was received on 22 Aug 2017, accepted on 06 Feb 2018 and first published on 12 Feb 2018


Article type: Research Article
DOI: 10.1039/C7MD00433H
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Studies towards elucidating the potential of 5,10,15,20-tetrakis(p-carboxymethyleneoxyphenyl)porphyrin as a theranostic agent for applications in PET and PDT

    M. Guleria, C. Kumar, T. Das, J. Amirdhanayagam, R. Sharma, H. D. Sarma and A. Dash, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C7MD00433H

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