Antiviral Potential of Naphthoquinones Derivatives Encapsulated within Liposomes

Autor: Gustavo B. da Silva, Rosa Bellavita, Izabel Christina Nunes de Palmer Paixão, Stefania Galdiero, Viveca Giongo, S.G. De-Simone, Camilly P. Pires De Melo, Annarita Falanga
Přispěvatelé: Giongo, Viveca, Falanga, Annarita, De Melo, Camilly P Pire, da Silva, Gustavo B, Bellavita, Rosa, De-Simone, Salvatore G, Paixão, Izabel C, Galdiero, Stefania
Rok vydání: 2021
Předmět:
Zdroj: Molecules
Volume 26
Issue 21
Molecules, Vol 26, Iss 6440, p 6440 (2021)
ISSN: 1420-3049
DOI: 10.3390/molecules26216440
Popis: HSV infections, both type 1 and type 2, are among the most widespread viral diseases affecting people of all ages. Their symptoms could be mild, with cold sores up to 10 days of infection, blindness and encephalitis caused by HSV-1 affecting immunocompetent and immunosuppressed individuals. The severe effects derive from co-evolution with the host, resulting in immune evasion mechanisms, including latency and growing resistance to acyclovir and derivatives. An efficient alternative to controlling the spreading of HSV mutations is the exploitation of new drugs, and the possibility of enhancing their delivery through the encapsulation of drugs into nanoparticles, such as liposomes. In this work, liposomes were loaded with a series of 2-aminomethyl- 3-hydroxy-1,4-naphthoquinones derivatives with n-butyl (compound 1), benzyl (compound 2) and nitrobenzene (compound 3) substituents in the primary amine of naphthoquinone. They were previously identified to have significant inhibitory activity against HSV-1. All of the aminomethylnaphthoquinones derivatives encapsulated in the phosphatidylcholine liposomes were able to control the early and late phases of HSV-1 replication, especially those substituted with the benzyl (compound 2) and nitrobenzene (compound 3), which yields selective index values that are almost nine times more efficient than acyclovir. The growing interest of the industry in topical administration against HSV supports our choice of liposome as a drug carrier of aminomethylnaphthoquinones derivatives for formulations of in vivo pre-clinical assays.
Databáze: OpenAIRE
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