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1.
Arch Plast Surg ; 40(6): 697-704, 2013 Nov.
Article in English | MEDLINE | ID: mdl-24286041

ABSTRACT

BACKGROUND: We conducted an experimental study to compare the effect of massage using topical agents (Kelo-cote or Contractubex) on scar formation by massaging the healed burn wound on the dorsal area of Sprague-Dawley (SD) rats. METHODS: Four areas of second degree contact burn were made on the dorsal area of each of 15 SD rats, using a soldering iron 15 mm in diameter. After gross epithelialization in the defect, 15 SD rats were randomly divided into four groups: the Kelo-cote group, Contractubex group, Vaseline group, and control group. Rats in three of the groups (all but the Control group) were massaged twice per day for 5 minutes each day, while those in the Control group were left unattended. For histologic analysis, we performed a biopsy and evaluated the thickness of scar tissue. RESULTS: In the Kelo-cote and Contractubex groups, scar tissue thicknesses showed a significant decrease, compared with the Vaseline and control groups. However, no significant differences were observed between the Kelo-cote and Contractubex groups. In the Vaseline group, scar tissue thicknesses showed a significant decrease, compared with the control groups. CONCLUSIONS: The findings of this study suggest that massage using a topical agent is helpful in the prevention of scar formation and that massage only with lubricant (no use of a topical agent) also has a considerable effect, although not as much as the use of a topical agent. Thus, we recommend massage with a topical agent on the post-burn scar as an effective method for decreasing the scar thickness.

2.
Eur J Med Chem ; 63: 621-8, 2013 May.
Article in English | MEDLINE | ID: mdl-23567950

ABSTRACT

A series of novel aliphatic amido-quaternary ammonium salts were synthesized and evaluated for their anticancer effects involving induction of RhoB. Most of these compounds, featuring open-ring forms of aliphatic amido-quaternary ammonium salts, exhibited potent anti-proliferative activities in human cancer cell lines, including PC-3, NUGC-3, MDA-MB-231, ACHN, HCT-15, and NCI-H23. In further evaluation, the representative compound N,N-diethyl-N-(2-(N-methyltetradecanamido)ethyl)prop-2-en-1-aminium bromide (3b) exhibited potent pro-apoptotic activity, through RhoB activation, in HeLa cells.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Quaternary Ammonium Compounds/chemical synthesis , Quaternary Ammonium Compounds/pharmacology , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , HeLa Cells , Humans , Inhibitory Concentration 50 , Models, Chemical , Molecular Structure , Quaternary Ammonium Compounds/chemistry , Structure-Activity Relationship
3.
Eur J Med Chem ; 46(7): 2861-6, 2011 Jul.
Article in English | MEDLINE | ID: mdl-21543141

ABSTRACT

We synthesized novel aliphatic amido-quaternary ammonium salts in an effort to discover anticancer agents that increase Ras homolog gene family, member B, (RhoB) levels. These compounds exert anti-proliferative activities against several human cancer cell types. Seventeen compounds, varying in aliphatic carbon chain length and N-substituents, were synthesized and their biological activities were evaluated. Of these 17 compounds, compound 3i emerged as the most promising anticancer compound by promoting apoptosis through the RhoB mediated pathway. Potent biological activities observed for these novel aliphatic amido-quaternary ammonium salt analogues support their potential as anticancer, chemotherapeutic agents.


Subject(s)
Amides/chemistry , Antineoplastic Agents/chemical synthesis , Gene Expression Regulation, Neoplastic , Quaternary Ammonium Compounds/chemical synthesis , rhoB GTP-Binding Protein/agonists , Antineoplastic Agents/pharmacology , Apoptosis/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Genes, Reporter , Humans , Luciferases/genetics , Luciferases/metabolism , Piperazines/chemistry , Quaternary Ammonium Compounds/pharmacology , Salts/chemistry , Signal Transduction , Structure-Activity Relationship , rhoB GTP-Binding Protein/genetics , rhoB GTP-Binding Protein/metabolism
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