Mygalin: An Acylpolyamine With Bactericidal Activity
Inappropriate use of antibiotics favors the selection and spread of resistant bacteria. To reduce the spread of these bacteria, finding new molecules with activity is urgent and necessary. Several polyamine analogs have been constructed and used to control microorganisms and tumor cells. Mygalin is...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2020-01-01
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| Series: | Frontiers in Microbiology |
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| Online Access: | https://www.frontiersin.org/article/10.3389/fmicb.2019.02928/full |
| _version_ | 1811214881865596928 |
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| author | Abraham Espinoza-Culupú Abraham Espinoza-Culupú Elizabeth Mendes Hector Aguilar Vitorino Pedro Ismael da Silva Monamaris Marques Borges |
| author_facet | Abraham Espinoza-Culupú Abraham Espinoza-Culupú Elizabeth Mendes Hector Aguilar Vitorino Pedro Ismael da Silva Monamaris Marques Borges |
| author_sort | Abraham Espinoza-Culupú |
| collection | DOAJ |
| description | Inappropriate use of antibiotics favors the selection and spread of resistant bacteria. To reduce the spread of these bacteria, finding new molecules with activity is urgent and necessary. Several polyamine analogs have been constructed and used to control microorganisms and tumor cells. Mygalin is a synthetic acylpolyamine, which are analogs of spermidine, derived from the hemolymph of the spider Acanthoscurria gomesiana. The effective activity of polyamines and their analogs has been associated with their structure. The presence of two acyl groups in the Mygalin structure may give this molecule a specific antibacterial activity. The aim of this study was to identify the mechanisms involved in the interaction of Mygalin with Escherichia coli to clarify its antimicrobial action. The results indicated that Mygalin exhibits intense dose and time-dependent bactericidal activity. Treatment of E. coli with this molecule caused membrane rupture, inhibition of DNA synthesis, DNA damage, and morphological changes. The esterase activity increased along with the intracellular production of reactive oxygen species (ROS) after treatment of the bacteria with Mygalin. In addition, this molecule was able to sequester iron and bind to LPS. We have shown that Mygalin has bactericidal activity with underlying mechanisms involving ROS generation and chelation of iron ions that are necessary for bacterial metabolism, which may contribute to its microbicidal activity. Taken together, our data suggest that Mygalin can be explored as a new alternative drug with antimicrobial potential against Gram-negative bacteria or other infectious agents. |
| first_indexed | 2024-04-12T06:12:55Z |
| format | Article |
| id | doaj.art-8d5dd2da385a42a1a1816cfc5b4d495d |
| institution | Directory Open Access Journal |
| issn | 1664-302X |
| language | English |
| last_indexed | 2024-04-12T06:12:55Z |
| publishDate | 2020-01-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Microbiology |
| spelling | doaj.art-8d5dd2da385a42a1a1816cfc5b4d495d2022-12-22T03:44:39ZengFrontiers Media S.A.Frontiers in Microbiology1664-302X2020-01-011010.3389/fmicb.2019.02928484617Mygalin: An Acylpolyamine With Bactericidal ActivityAbraham Espinoza-Culupú0Abraham Espinoza-Culupú1Elizabeth Mendes2Hector Aguilar Vitorino3Pedro Ismael da Silva4Monamaris Marques Borges5Ph.D. Program in Biotechnology, University of São Paulo, São Paulo, BrazilBacteriology Laboratory, Butantan Institute, São Paulo, BrazilBacteriology Laboratory, Butantan Institute, São Paulo, BrazilInstitute of Marine and Environmental Technology, University of Maryland Center for Environmental Science, Columbus Center, Baltimore, MD, United StatesLaboratory for Applied Toxinology (LETA), Butantan Institute, São Paulo, BrazilBacteriology Laboratory, Butantan Institute, São Paulo, BrazilInappropriate use of antibiotics favors the selection and spread of resistant bacteria. To reduce the spread of these bacteria, finding new molecules with activity is urgent and necessary. Several polyamine analogs have been constructed and used to control microorganisms and tumor cells. Mygalin is a synthetic acylpolyamine, which are analogs of spermidine, derived from the hemolymph of the spider Acanthoscurria gomesiana. The effective activity of polyamines and their analogs has been associated with their structure. The presence of two acyl groups in the Mygalin structure may give this molecule a specific antibacterial activity. The aim of this study was to identify the mechanisms involved in the interaction of Mygalin with Escherichia coli to clarify its antimicrobial action. The results indicated that Mygalin exhibits intense dose and time-dependent bactericidal activity. Treatment of E. coli with this molecule caused membrane rupture, inhibition of DNA synthesis, DNA damage, and morphological changes. The esterase activity increased along with the intracellular production of reactive oxygen species (ROS) after treatment of the bacteria with Mygalin. In addition, this molecule was able to sequester iron and bind to LPS. We have shown that Mygalin has bactericidal activity with underlying mechanisms involving ROS generation and chelation of iron ions that are necessary for bacterial metabolism, which may contribute to its microbicidal activity. Taken together, our data suggest that Mygalin can be explored as a new alternative drug with antimicrobial potential against Gram-negative bacteria or other infectious agents.https://www.frontiersin.org/article/10.3389/fmicb.2019.02928/fullacylpolyamineMygalinoxidative stressE. coliantimicrobialbiomolecule |
| spellingShingle | Abraham Espinoza-Culupú Abraham Espinoza-Culupú Elizabeth Mendes Hector Aguilar Vitorino Pedro Ismael da Silva Monamaris Marques Borges Mygalin: An Acylpolyamine With Bactericidal Activity Frontiers in Microbiology acylpolyamine Mygalin oxidative stress E. coli antimicrobial biomolecule |
| title | Mygalin: An Acylpolyamine With Bactericidal Activity |
| title_full | Mygalin: An Acylpolyamine With Bactericidal Activity |
| title_fullStr | Mygalin: An Acylpolyamine With Bactericidal Activity |
| title_full_unstemmed | Mygalin: An Acylpolyamine With Bactericidal Activity |
| title_short | Mygalin: An Acylpolyamine With Bactericidal Activity |
| title_sort | mygalin an acylpolyamine with bactericidal activity |
| topic | acylpolyamine Mygalin oxidative stress E. coli antimicrobial biomolecule |
| url | https://www.frontiersin.org/article/10.3389/fmicb.2019.02928/full |
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