Antimicrobial, anti-adherence and antibiofilm activity against Staphylococcus aureus of a 4-phenyl coumarin derivative isolated from Brazilian geopropolis

Author(s)

da Cunha, Marcos Guilherme ^{[1, 2]} ; Orlandi Sardi, Janaina de Cassia ^[2] ; Freires, Irlan Almeida ^[3] ; Franchin, Marcelo ^[2] ; Rosalen, Pedro Luiz ^[2]

Affiliation

^[1] Brazilian Ctr Res Energy & Mat CNPEM, Brazilian Biosci Natl Lab LNBio, BR-13083970 Campinas, SP - Brazil

^[2] Univ Estadual Campinas, Piracicaba Dent Sch, Dept Physiol Sci, 901 Limeira Ave, BR-13414903 Piracicaba, SP - Brazil

^[3] Univ Florida, Dept Oral Biol, Coll Dent, 1395 Ctr Dr, Gainesville, FL 32610 - USA

• Document type: Journal article
• Source: Microbial Pathogenesis; v. 139, FEB 2020.
• Web of Science Citations: 0

Abstract

The discovery of new drug candidates, especially from natural products, remains a promising approach to overcome the alarmingly high microbial resistance rates. A major 4-phenyl coumarin named cinnamoyloxy-mammeisin (CNM) isolated from stingless bee geopropolis showed interesting biological properties; however, its antimicrobial activity against Staphylococcus aureus has never been investigated. In order to clarify these properties, CNM isolated from geopropolis was initially tested against methicillin-susceptible and -resistant S. aureus strains. Further, the effects of CNM were assessed on the microbial adherence to human cells, biofilm formation and mature biofilm. Then, the acute toxicity of the compound was determined in Galleria mellonella. CNM showed bacteriostatic activity against methicillin-susceptible and -resistant S. aureus strains, with MIC of 11.3 mu M. In addition, CNM at 5.7 mu M reduced bacterial adherence to human keratinocytes from 1 to 3 h and disrupted biofilm formation by reducing cell viability and architecture, as evidenced by scanning electron microscopy. The acute toxicity assay indicated no significant harmful effects. Based on these findings, CNM can be considered a promising compound with anti-S. aureus properties and predicted low toxicity. Thus, it may be used as a drug candidate or lead compound for structure/activity optimization. (AU)

• FAPESP's process: 11/23635-6 - Isolation and pharmacological evaluation of bioactive molecules from hexane fraction of M. scutellaris geopropolis
• Grantee: Marcos Guilherme da Cunha
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 12/22002-2 - Chemical elucidation of biocompounds and molecular targets of geopropolis on cancer cell lines
• Grantee: Marcos Guilherme da Cunha
• Support Opportunities: Scholarships abroad - Research Internship - Doctorate