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Article

Design, Synthesis and Characterization of [G10a]-Temporin SHa Dendrimers as Dual Inhibitors of Cancer and Pathogenic Microbes

by
Arif Iftikhar Khan
1,2,
Shahzad Nazir
1,2,
Aaqib Ullah
1,2,
Muhammad Nadeem ul Haque
1,2,
Rukesh Maharjan
2,
Shabana U. Simjee
2,3,
Hamza Olleik
4,
Elise Courvoisier-Dezord
4,
Marc Maresca
4,* and
Farzana Shaheen
1,2,*
1
Third World Center for Science and Technology, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
2
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
3
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
4
Aix-Marseille Univ., CNRS, Centrale Marseille, iSm2, 13013 Marseille, France
*
Authors to whom correspondence should be addressed.
Biomolecules 2022, 12(6), 770; https://doi.org/10.3390/biom12060770
Submission received: 26 April 2022 / Revised: 20 May 2022 / Accepted: 29 May 2022 / Published: 31 May 2022
(This article belongs to the Special Issue Active Peptides as Functional Biomolecules: In Vitro and In Vivo Studies)
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Abstract

As the technologies for peptide synthesis and development continue to mature, antimicrobial peptides (AMPs) are being widely studied as significant contributors in medicinal chemistry research. Furthermore, the advancement in the synthesis of dendrimers’ design makes dendrimers wonderful nanostructures with distinguishing properties. This study foregrounds a temporin SHa analog, [G10a]-SHa, and its dendrimers as globular macromolecules possessing anticancer and antibacterial activities. These architectures of temporin SHa, named as [G10a]-SHa, its dendrimeric analogs [G10a]2-SHa and [G10a]3-SHa, and [G10a]2-SHa conjugated with a polymer molecule, i.e., Jeff-[G10a]2-SHa, were synthesized, purified on RP-HPLC and UPLC and fully characterized by mass, NMR spectroscopic techniques, circular dichroism, ultraviolet, infrared, dynamic light scattering, and atomic force microscopic studies. In pH- and temperature-dependent studies, all of the peptide dendrimers were found to be stable in the temperature range up to 40–60 °C and pH values in the range of 6–12. Biological-activity studies showed these peptide dendrimers possessed improved antibacterial activity against different strains of both Gram-positive and Gram-negative strains. Together, these dendrimers also possessed potent selective antiproliferative activity against human cancer cells originating from different organs (breast, lung, prostate, pancreas, and liver). The high hemolytic activity of [G10a]2-SHa and [G10a]3-SHa dendrimers, however, limits their use for topical treatment, such as in the case of skin infection. On the contrary, the antibacterial and anticancer activities of Jeff-[G10a]2-SHa, associated with its low hemolytic action, make it potentially suitable for systemic treatment.
Keywords: temporin SHa; D-alanine; antimicrobial peptide; Rink amide resin; dendrimer; antibacterial; anticancer temporin SHa; D-alanine; antimicrobial peptide; Rink amide resin; dendrimer; antibacterial; anticancer

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MDPI and ACS Style

Khan, A.I.; Nazir, S.; Ullah, A.; Haque, M.N.u.; Maharjan, R.; Simjee, S.U.; Olleik, H.; Courvoisier-Dezord, E.; Maresca, M.; Shaheen, F. Design, Synthesis and Characterization of [G10a]-Temporin SHa Dendrimers as Dual Inhibitors of Cancer and Pathogenic Microbes. Biomolecules 2022, 12, 770. https://doi.org/10.3390/biom12060770

AMA Style

Khan AI, Nazir S, Ullah A, Haque MNu, Maharjan R, Simjee SU, Olleik H, Courvoisier-Dezord E, Maresca M, Shaheen F. Design, Synthesis and Characterization of [G10a]-Temporin SHa Dendrimers as Dual Inhibitors of Cancer and Pathogenic Microbes. Biomolecules. 2022; 12(6):770. https://doi.org/10.3390/biom12060770

Chicago/Turabian Style

Khan, Arif Iftikhar, Shahzad Nazir, Aaqib Ullah, Muhammad Nadeem ul Haque, Rukesh Maharjan, Shabana U. Simjee, Hamza Olleik, Elise Courvoisier-Dezord, Marc Maresca, and Farzana Shaheen. 2022. "Design, Synthesis and Characterization of [G10a]-Temporin SHa Dendrimers as Dual Inhibitors of Cancer and Pathogenic Microbes" Biomolecules 12, no. 6: 770. https://doi.org/10.3390/biom12060770

APA Style

Khan, A. I., Nazir, S., Ullah, A., Haque, M. N. u., Maharjan, R., Simjee, S. U., Olleik, H., Courvoisier-Dezord, E., Maresca, M., & Shaheen, F. (2022). Design, Synthesis and Characterization of [G10a]-Temporin SHa Dendrimers as Dual Inhibitors of Cancer and Pathogenic Microbes. Biomolecules, 12(6), 770. https://doi.org/10.3390/biom12060770

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