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10.2147/DDDT.S106462

http://scihub22266oqcxt.onion/10.2147/DDDT.S106462
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C4809335!4809335 !27042015
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suck abstract from ncbi


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pmid27042015
      Drug+Des+Devel+Ther 2016 ; 10 (ä): 1235-42
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  • Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) corrected : a new antibiotic for the treatment of acne #MMPMID27042015
  • Dinant A ; Boulos RA
  • Drug Des Devel Ther 2016[]; 10 (ä): 1235-42 PMID27042015 show ga
  • 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. 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. 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. CONCLUSION: This study demonstrates the potential of Zolav(®) (a p-carboethoxy-tristyrylbenzene derivative) as a novel treatment for acne vulgaris.
  • |Acne Vulgaris/*drug therapy/*microbiology [MESH]
  • |Animals [MESH]
  • |Anti-Bacterial Agents/chemistry/*pharmacology/*therapeutic use [MESH]
  • |Benzene Derivatives/chemistry/*pharmacology/*therapeutic use [MESH]
  • |Cell Death/drug effects [MESH]
  • |Cell Line [MESH]
  • |Chemistry, Pharmaceutical [MESH]
  • |Dose-Response Relationship, Drug [MESH]
  • |Escherichia coli/drug effects [MESH]
  • |Female [MESH]
  • |Humans [MESH]
  • |Male [MESH]
  • |Mice [MESH]
  • |Mice, Inbred BALB C [MESH]
  • |Microbial Sensitivity Tests [MESH]
  • |Propionibacterium acnes/drug effects [MESH]
  • |Rats [MESH]
  • |Rats, Sprague-Dawley [MESH]
  • |Structure-Activity Relationship [MESH]


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