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1.
Molecules ; 20(3): 5038-49, 2015 Mar 19.
Article in English | MEDLINE | ID: mdl-25808148

ABSTRACT

A number of studies have proposed an anti-diabetic effect for tarchonanthuslactone based on its structural similarity with caffeic acid, a compound known for its blood glucose-reducing properties. However, the actual effect of tarchonanthuslactone on blood glucose level has never been tested. Here, we report that, in opposition to the common sense, tarchonanthuslactone has a glucose-increasing effect in a mouse model of obesity and type 2 diabetes mellitus. The effect is acute and non-cumulative and is present only in diabetic mice. In lean, glucose-tolerant mice, despite a slight increase in blood glucose levels, the effect was not significant.


Subject(s)
Blood Glucose/drug effects , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Type 2/metabolism , Obesity/metabolism , Pyrones/administration & dosage , Animals , Disease Models, Animal , Injections, Intraperitoneal , Male , Mice , Pyrones/chemistry , Pyrones/pharmacology
2.
Biomed Res Int ; 2013: 271276, 2013.
Article in English | MEDLINE | ID: mdl-24369010

ABSTRACT

The aging process causes a number of changes in the skin, including oxidative stress and dyschromia. The kojic acid (KA) is iron chelator employed in treatment of skin aging, and inhibits tyrosinase, promotes depigmentation. Nanotechnology-based drug delivery systems, such as liquid crystalline systems (LCSs), can modulate drug permeation through the skin and improve the drug activity. This study is aimed at structurally developing and characterizing a kojic acid-loaded LCS, consists of water (W), cetostearyl isononanoate (oil-O) and PPG-5-CETETH-20 (surfactant-S) and evaluating its in vitro skin permeation and retention. Three regions of the diagram were selected for characterization: A (35% O, 50% S, 15% W), B (30% O, 50% S, 20% W) and C (20% O, 50% S, 30% W), to which 2% KA was added. The formulations were subjected to polarized light microscopy, which indicated the presence of a hexagonal mesophase. Texture and bioadhesion assay showed that formulation B is suitable for topical application. According to the results from the in vitro permeation and retention of KA, the formulations developed can modulate the permeation of KA in the skin. The in vitro cytotoxic assays showed that KA-unloaded LCS and KA-loaded LCS didn't present cytotoxicity. PPG-5-CETETH-20-based systems may be a promising platform for KA skin delivery.


Subject(s)
Drug Delivery Systems , Pyrones/administration & dosage , Skin Aging/drug effects , Skin/drug effects , Humans , Liquid Crystals/chemistry , Nanotechnology , Pyrones/chemistry , Surface-Active Agents/administration & dosage , Surface-Active Agents/chemistry , Tetracyclines/chemistry , Water/chemistry
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