title: Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) [corrected]: a new antibiotic for the treatment of acne.
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.
  
  
  OBJECTIVE
  To investigate the effectiveness of Zolav(®), (a p-carboethoxy-tristyrylbenzene derivative) [corrected] a novel antibiotic as a treatment for acne vulgaris.
  
  
  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.
  
  
  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.
  
  
  CONCLUSIONS
  This study demonstrates the potential of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) as a novel treatment for acne vulgaris.
authors.affiliation: AXD Pty Ltd, Semaphore Park, Flinders University, Bedford Park, SA, Australia.
authors.forename: Alexa
authors.initials: A
authors.lastname: Dinant
authors.affiliation: School of Chemical and Physical Sciences, Flinders University, Bedford Park, SA, Australia; Boulos & Cooper Pharmaceuticals Pty Ltd, Port Adelaide, SA, Australia.
authors.forename: Ramiz A
authors.initials: RA
authors.lastname: Boulos
mesh_terms: D000152:Acne Vulgaris / Q000188:drug therapy* / Q000382:microbiology*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D001555:Benzene Derivatives / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D004926:Escherichia coli / Q000187:drug effects; D005260:Female; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008826:Microbial Sensitivity Tests; D011425:Propionibacterium acnes / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*
chemical_list: D000900:Anti-Bacterial Agents; D001555:Benzene Derivatives; D013343:Styrenes; C000613147:p-carboethoxy-tristyrylbenzene
keywords: MscL; Zolav®; acne; antibiotic resistance; benzoyl peroxide; isotretinoin