Back to Search
Start Over
Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) [corrected]: a new antibiotic for the treatment of acne.
- Source :
-
Drug design, development and therapy [Drug Des Devel Ther] 2016 Mar 22; Vol. 10, pp. 1235-42. Date of Electronic Publication: 2016 Mar 22 (Print Publication: 2016). - Publication Year :
- 2016
-
Abstract
- Background: Acne is a prominent skin condition affecting >80% of teenagers and young adults and ~650 million people globally. Isotretinoin, a vitamin A derivative, is currently the standard of care for treatment. However, it has a well-established teratogenic activity, a reason for the development of novel and low-risk treatment options for acne.<br />Objective: To investigate the effectiveness of Zolav(®), (a p-carboethoxy-tristyrylbenzene derivative) [corrected] a novel antibiotic as a treatment for acne vulgaris.<br />Materials and Methods: Minimum inhibitory concentration of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) against Propionibacterium acnes was determined by following a standard protocol using Mueller-Hinton broth and serial dilutions in a 96-well plate. Cytotoxicity effects on human umbilical vein endothelial cells and lung cells in the presence of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) were investigated by determining the growth inhibition (GI50) concentration, total growth inhibition concentration, and the lethal concentration of 50% (LC50). The tryptophan auxotrophic mutant of Escherichia coli strain, WP2 uvrA (ATCC 49979), was used for the AMES assay with the addition of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) tested for its ability to reverse the mutation and induce bacterial growth. The in vivo effectiveness of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) was tested in a P. acnes mouse intradermal model where the skin at the infection site was removed, homogenized, and subjected to colony-forming unit (CFU) counts.<br />Results: Susceptibility testing of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) against P. acnes showed a minimum inhibitory concentration of 2 µg/mL against three strains with no cytotoxicity and no mutagenicity observed at the highest concentrations tested, 30 µM and 1,500 µg/plate, respectively. The use of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) at a concentration of 50 µg/mL (q8h) elicited a two-log difference in CFU/g between the treatment group and the control.<br />Conclusion: This study demonstrates the potential of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) as a novel treatment for acne vulgaris.
- Subjects :
- Animals
Anti-Bacterial Agents chemistry
Benzene Derivatives chemistry
Cell Death drug effects
Cell Line
Chemistry, Pharmaceutical
Dose-Response Relationship, Drug
Escherichia coli drug effects
Female
Humans
Male
Mice
Mice, Inbred BALB C
Microbial Sensitivity Tests
Propionibacterium acnes drug effects
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Styrenes chemistry
Acne Vulgaris drug therapy
Acne Vulgaris microbiology
Anti-Bacterial Agents pharmacology
Anti-Bacterial Agents therapeutic use
Benzene Derivatives pharmacology
Benzene Derivatives therapeutic use
Styrenes pharmacology
Styrenes therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 1177-8881
- Volume :
- 10
- Database :
- MEDLINE
- Journal :
- Drug design, development and therapy
- Publication Type :
- Academic Journal
- Accession number :
- 27042015
- Full Text :
- https://doi.org/10.2147/DDDT.S106462