| In vitro: |
| Bioorganic & Medicinal Chemistry Letters,2002,12(3): 477–482. | | Protective effects of polygodial and related compounds on ethanol-induced gastric mucosal lesions in rats: structural requirements and mode of action[Reference: WebLink] | The methanolic extract from the leaves of Tasmannia lanceolata was found to potently inhibit ethanol-induced gastric lesions in rats.
METHODS AND RESULTS:
Through bioassay-guided separation, three known sesquiterpenes, polygodial, polygodial 12α-acetal, and polygodial 12β-acetal, and a new sesquiterpene, Methyl isodrimeninol, were isolated as the active constituents. Among them, polygodial showed very potent gastroprotective effects (ED50=0.028 mg/kg, po). From the gastroprotective effects of various reduction and oxidation derivatives of polygodial, the dialdehyde or diacetal structure was found to be essential for the strong activity.
CONCLUSIONS:
Since the gastroprotection of polygodial was attenuated by pretreatment with indomethacin, N-ethylmaleimide, NG-nitro-l-arginine methyl ester and ruthenium red, endogenous prostaglandins, sulfhydryl compounds, nitric oxide and vanilloid receptors may be involved in the protective activity. |
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