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Biomolecules
Volume 12
Issue 5
10.3390/biom12050725
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Article

Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides

by
Davide Cardella
1,
Wenjing Deng
2,
Louis Y. P. Luk
1,* and
Yu-Hsuan Tsai
1,2,*
1
School of Chemistry, Main Building, Cardiff University, Park Place, Cardiff CF10 3AT, UK
2
Shenzhen Bay Laboratory, Gaoke Innovation Center, Institute of Molecular Physiology, Guangming District, Shenzhen 518132, China
*
Authors to whom correspondence should be addressed.
Biomolecules 2022, 12(5), 725; https://doi.org/10.3390/biom12050725
Submission received: 7 April 2022 / Revised: 10 May 2022 / Accepted: 16 May 2022 / Published: 20 May 2022
(This article belongs to the Section Chemical Biology)
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Abstract

Despite continuous advances, anticancer therapy still faces several technical hurdles, such as selectivity on cellular and subcellular targets of therapeutics. Toward addressing these limitations, we have combined the use of proapoptotic peptides, trimethine cyanine dye, and folate to target the mitochondria of tumor cells. A series of proapoptotic peptides and their conjugates with a cyanine dye and/or folate were synthesized in the solid phase, and their toxicity in different human cell lines was assessed. Cyanine-bearing conjugates were found to be up to 100-fold more cytotoxic than the parent peptides and to localize in mitochondria. However, the addition of a folate motif did not enhance the potency or selectivity of the resulting conjugates toward tumor cells that overexpress folate receptor α. Furthermore, while dual-labeled constructs were also found to localize within the target organelle, they were not generally selective towards folate receptor α-positive cell lines in vitro.
Keywords: cancer; cyanine dyes; folate; mitochondria; proapoptotic peptides; solid-phase synthesis cancer; cyanine dyes; folate; mitochondria; proapoptotic peptides; solid-phase synthesis

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MDPI and ACS Style

Cardella, D.; Deng, W.; Luk, L.Y.P.; Tsai, Y.-H. Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides. Biomolecules 2022, 12, 725. https://doi.org/10.3390/biom12050725

AMA Style

Cardella D, Deng W, Luk LYP, Tsai Y-H. Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides. Biomolecules. 2022; 12(5):725. https://doi.org/10.3390/biom12050725

Chicago/Turabian Style

Cardella, Davide, Wenjing Deng, Louis Y. P. Luk, and Yu-Hsuan Tsai. 2022. "Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides" Biomolecules 12, no. 5: 725. https://doi.org/10.3390/biom12050725

APA Style

Cardella, D., Deng, W., Luk, L. Y. P., & Tsai, Y.-H. (2022). Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides. Biomolecules, 12(5), 725. https://doi.org/10.3390/biom12050725

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