| Catalogue number | C101407 |
| Chemical name | Galanolactone |
| CAS Number | 115753-79-2 |
| Synonyms | (3E)-3-[2-[(1R,2S,4aS,8aS)-5,5,8a-trimethyl-1-spiro[3,4,4a,6,7,8-hexahydro-1H-naphthalene-2,2’-oxirane]yl]ethylidene]-2-oxolanone |
| Molecular Weight | C20H30O3 |
| Formula | 318.5 |
| Purity | 98% |
| Physical Description | Powder |
| Solvent | Chloroform, Dichloromethane,DMSO |
| Storage | Stored at 2-8°C, Protected from air and light, refrigerate or freeze |
| Applications | Active against Candida albicans; shows cytotoxic activity. Effect of galanolactone on 3T3-L1 adipocyte differentiation was measured by Oil Red O staining, and cytotoxicity effect of galanolactone was analyzed by 3-[4,5-dimethylthiazol -2-yl]-2,5-diphenyltetrazolium bromide assay. The expression of various genes involved in adipogenic action of galanolactone was determined by real-time PCR and Western blot. Peroxisome proliferator-activated receptor γ (PPARγ) luciferase transactivation assay was used to evaluate the PPARγ transcriptional activity of galanolactone in HEK 293T cells. Galanolactone inhibited lipid accumulation and expression of adipocyte fatty acid-binding protein (aP2) and resistin in a dose-dependent manner in 3T3-L1 cells. Treatment with 50 and 100 μM of galanolactone significantly decreased the troglitazone-induced PPARγ transcripitional activity in HEK 293T cells, and suppressed expressions of PPARγ and CCAAT-enhancer-binding protein α (C/EBPα) at mRNA and protein levels in 3T3-L1 cells. These findings suggest that galanolactone exerts anti-obesity effect through down regulation of adipogenic transcription factors and adipogenic marker genes. Galanolactone inhibited contractile responses to 5-HT with a pIC50 value 4.93. pIC50 value of galanolactone against the response to 2-methyl-5-HT, a selective 5-HT3 agonist, in the presence of methysergide at 1 x 10(-5) M was 5.10. pIC50 values of ICS 205-930, a selective 5-HT3 antagonist, were 5.30 and 7.49, respectively. The concentration-response curve of 5-HT was shown as a biphasic curve and galanolactone caused a selective shift to the right of the second phase. In the same preparations, the pIC50 value of galanolactone and ICS 205-930 against the response to carbamylcholine (CCh) was 4.45 and 4.46. The inhibitory effect of galanolactone on the 5-HT response in the stomach fundus and aortic strips was less than that in the ileum. In addition, in the thoracic aorta precontracted with 50 mM K+, the relaxing effect of galanolactone was about 1/10 of that of papaverine. These results suggest that the anti-5-HT effect of galanolactone, a diterpenoid isolated from ginger, is related to antagonism of 5-HT3 receptors. |
| References | 1. Tetrahedron Letters, 1989, 30(5), 553-556. 2. Planta Med., 1988, 54, 117. 3. Journal of the Korean Society for Applied Biological Chemistry, 2012, 55(1), 63-68. 4. Chem. Pharm. Bull. (Tokyo)., 1991, 39(2), 397-399. |
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After Receiving
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