Investigation of In vitro PDT Activities and In vivo Biopotential of Zinc Phthalocyanines Using 131I Radioisotope. (5th October 2015)

• Record Type: Journal Article
• Authors: Ince, Mine; Er, Ozge; Ocakoglu, Kasim; Lambrecht, Fatma Yurt; Colak, Suleyman Gokhan; Soylu, Hale Melis; Kayabasi, Cagla; Gunduz, Cumhur
• Is Part Of: Chemical biology & drug design. Volume 87:Number 2(2016)
• Page Start: 224
• Page End: 232
• Publication Date: 2015-10-05
• Subjects: 131I -- biodistribution -- cancer -- photodynamic therapy -- phthalocyanine -- radiolabeling; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12659
• Languages: English
• ISSNs: 1747-0277

Abstract

Abstract : Novel octylthio‐containing asymmetrically substituted Zn(II) phthalocyanine ( Zn(II)Pc1 ) and a symmetric derivative ( Zn(II)Pc2 ) have been prepared to investigate the biological potential and ability to photosensitize singlet oxygen for photodynamic therapy applications. In this study, the singlet oxygen generation potential and in vitro photodynamic activities of these compounds have been tested. Both ZnPcs reveal to be very efficient singlet oxygen generators and promising PSs for PDT applications. In vitro PDT activities of the compounds were evaluated in EMT‐6 murine mammary carcinoma and HeLa human cervix carcinoma cell lines. Moreover, Zn(II)Pc1 displayed the phototoxic effects in the mammary cancer cell line (6.25 μ m concentration at 30 J/cm 2 light dose and 12.5 μ m concentration at 20 J/cm 2 light dose), while Zn(II)Pc2 did not show any phototoxic effects both in two cell lines. Zn(II)Pcs were radiolabeled with 131 I in high yields. Biodistribution studies revealed that the radiolabeled Zn(II)Pc1 showed significant uptake in l. intestine, pancreas, brain, and ovary, while Zn(II)Pc2 has significant uptake in ovary and pancreas in normal rats. Hence, these Pcs derivatives could be promising candidate for tumor nuclear imaging. Abstract : Radiolabeled Zn(II)Pc2 demonstrates a potential for nuclear imaging of ovary and pancreatic tumor. Zn(II)Pc1 and 2 are encouraging for novel approaches in PDT; it merits further explanation. Consequently, Zn(II)Pc2 might be using bifunctional agents for nuclear imaging and PDT.