| Description: |
Isopulegol presents depressant- and anxiolytic-like effects, it also
has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABAA receptors and to antioxidant properties.Isopulegol presents significant gastroprotective effects in both ethanol- and indomethacin-induced ulcer models, which appear to be mediated, at least in part, by endogenous prostaglandins, K(ATP) channel opening, and antioxidant properties. |
| Targets: |
GABA Receptor | ATPase | Potassium Channel |
| In vitro: |
| Pharm Res. 2014 Aug;31(8):1907-18. | | Saturated long-chain esters of isopulegol as novel permeation enhancers for transdermal drug delivery.[Pubmed: 24449443] | Saturated long-chain esters of Isopulegol were synthesized and their activities as permeation enhancers for transdermal delivery of amlodipine and flurbiprofen were investigated, in contrast to the saturated fatty acids and Isopulegol, as well as their physical mixtures.
METHODS AND RESULTS:
In vitro permeation experiments, confocal laser scanning microscopy (CLSM) and attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy were introduced to investigate the regulation of enhancers in the skin permeability and biophysical properties. With in vitro cytotoxicity test and in vivo erythema model, the skin irritation of enhancers was evaluated. The esters significantly increased the permeation of amlodipine and flurbiprofen, whereas saturated fatty acids and Isopulegol had no such effect and even decreased the drug permeation when they were used alone or in combination. These results were supported by CLSM and ATR-FTIR studies, which revealed that only the esters could decrease the order of the alkyl chains in the skin lipids. Additionally, almost no skin irritation and cytotoxicity were observed for these esters.
CONCLUSIONS:
Saturated long-chain esters of Isopulegol are shown to be suitable permeation enhancers for transdermal drug delivery. Covalent attachment of Isopulegol and saturated fatty acids might represent a promising strategy to design novel and potent permeation enhancers. |
|
| In vivo: |
| Fitoterapia. 2009 Dec;80(8):506-13. | | Effects of isopulegol on pentylenetetrazol-induced convulsions in mice: possible involvement of GABAergic system and antioxidant activity.[Pubmed: 19559770 ] | The present study investigated the effects of Isopulegol, a monoterpene alcohol, in PTZ-induced convulsions and verified possible involved mechanisms.
METHODS AND RESULTS:
Saline, Isopulegol or diazepam were intraperitonealy injected 30 min before PTZ. The latency for development of convulsions and mortality, as well as the mortality protection percentage was recorded. For investigating the involvement of GABAergic system, flumazenil was utilized. The activity of antioxidant enzyme catalase as well as the levels of reduced glutathione and lipid peroxidation were measured in brain hippocampus. Similarly to diazepam, Isopulegol significantly prolonged the latency for convulsions and mortality of mice. All animals were protected against mortality at higher dose of Isopulegol. Flumazenil pretreatment decreased the prolongation of seizure latency induced by both diazepam and Isopulegol, although it was not able to reverse the latency and protection percent for mortality. Isopulegol also significantly prevented PTZ-induced increase in lipid peroxidation, preserved catalase activity in normal levels, and prevented the PTZ-induced loss of GSH in hippocampus of mice.
CONCLUSIONS:
These results suggest that the anticonvulsant and bioprotective effects of Isopulegol against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABA(A) receptors and to antioxidant properties. |
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