Porphyrin-derived carbon dots for an enhanced antiviral activity targeting the CTD of SARS-CoV-2 nucleocapsid

Abstract

Background Since effective antiviral drugs for COVID-19 are still limited in number, the exploration of compounds that have antiviral activity against SARS-CoV-2 is in high demand. Porphyrin is potentially developed as a COVID-19 antiviral drug. However, its low solubility in water restricts its clinical application. Reconstruction of porphyrin into carbon dots is expected to possess better solubility and bioavailability as well as lower biotoxicity. Methods and results In this study, we investigated the antiviral activity of porphyrin and porphyrin-derived carbon dots against SARS-CoV-2. Through the in silico analysis and assessment using a novel drug screening platform, namely dimer-based screening system, we demonstrated the capability of the antivirus candidates in inhibiting the dimerization of the C-terminal domain of SARS-CoV-2 Nucleocapsid. It was shown that porphyrin-derived carbon dots possessed lower cytotoxicity on Vero E6 cells than porphyrin. Furthermore, we also assessed their antiviral activity on the SARS-CoV-2-infected Vero E6 cells. The transformation of porphyrin into carbon dots substantially augmented its performance in disrupting SARS-CoV-2 propagation in vitro. Conclusions Therefore, this study comprehensively demonstrated the potential of porphyrin-derived carbon dots to be developed further as a promisingly safe and effective COVID-19 antiviral drug.

Natural products as a source of Coronavirus entry inhibitors

“…Another study investigated the antiviral activity of porphyrin, a natural bioactive compound, against the SARS-CoV-2 N protein. Using in silico analyses, porphyrin-derived carbon nanoparticles were found to inhibit nucleocapsid dimerization, an essential step in the formation of a functional N protein ( Fibriani et al., 2023 ). Furthermore, these nanoparticles exhibited in vitro antiviral activity, significantly reducing observable cytopathic effect in infected Vero E6 cells ( Fibriani et al., 2023 ).…”