Abstract
Coralyne is a synthetic analog of berberine related to protoberberine-isoquinoline alkaloids. Isoquinoline derivatives and analogs are renowned as potent radiosensitizers with potential medical application. In the present study, we investigated the effect of coralyne on the cell death, cytoskeletal changes and cell cycle progression of irradiated A549 cells. A clonogenic assay revealed that coralyne pretreatment decreased the viability of A549 cells in a time- and dose-dependent manner. Moreover, exposure to coralyne and ionizing radiation (IR) markedly altered the filamentous actin cytoskeletal architecture and integrin-β binding sites of A549 cells. Treatment with 1–25 µM coralyne in combination with 2 Gy of IR significantly reduced the percentage of cells in G2/M phase compared with 2 Gy IR alone. These results indicate that coralyne is a potent radiosensitizing agent that may find an application in medicine.
Highlights
Published: 28 May 2021Isoquinoline-protoberberine alkaloids are an important class of natural metabolites with interesting biological properties; their semi-synthetic and synthetic monomeric and dimeric derivatives have been synthesized
It was significantly inwere confirmed by confocal microscopy, which revealed that coralyne accumulated in the creased in cells treated with all concentrations of coralyne for 2, 24, 48, and 72 h
To further understand the mechanisms behind the observed G2/M phase abrogation and the G1 phase arrest phenotype due to the combined treatment of cells, we investigated the expression of three genes related to cell cycle progression in cells, namely cyclin B1interacting protein 1 (CCNB1IP1), cyclin-dependent kinase inhibitor 1 (CDKN1A) and cyclin D-binding Myb-like transcription factor 1 (DMTF1)
Summary
Isoquinoline-protoberberine alkaloids are an important class of natural metabolites with interesting biological properties; their semi-synthetic and synthetic monomeric and dimeric derivatives have been synthesized. Many studies reported that these compounds have antimicrobial, anti-inflammatory, antimalarial, antiviral, anticholesterol, and anticancer properties [1,2,3]. Whereas the pharmacological effects of naturally occurring protoberberine alkaloids, berberine, have been the subject of extensive in vitro, in vivo and clinical studies, information about the biological properties of coralyne is scarce. Coralyne (13-methyl [1,3] benzodioxolo [5,6-c]-1,3-dioxolo[4, 5-i]-phenanthridium) has the same tetracyclic structure as berberine and palmatine, but differs in terms of its substituents. Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations
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