Asaraldehyde (Asaronaldehyde) is a selective COX-2 inhibitor. Asaraldehyde (Asaronaldehyde) was found to be the most abundant constituent, but was totally absent in its cultured broth and its natural host, C. kanehirae wood. On feeding with the acid-digested sawdust of C. kanehirae wood or vanillin to the broth for culture, asaraldehyde (Asaronaldehyde) was produced in both cultured broths. Asaraldehyde (Asaronaldehyde) showed 3.32% of prostaglandin H endoperoxide synthase-1 (COX-1) inhibitory activity and 52.69% prostaglandin H endoperoxide synthase-2 (COX-2) inhibitory activity, respectively at 100 mg/ml. 2,4,5-trimethoxybenzaldehyde showed selectivity towards COX-2 enzyme inhibition at 100 ug/ml. The COX-2/COX-1 ratio for compound 1 was 17.68 at 100 ug/ml compared to solvent control.
|Cell lines||3T3-L1 cells|
|Preparation method||Seeding 3T3-L1 cells in 96-well plates at a concentration of 104 /well. Twenty-four hours later, treating the cells with 100 μg/mL of Asaraldehyde for 24 hours or for the whole 8-day differentiation period. Also, testing fully differentiated adipocytes with 100 μg/mL of Asaraldehyde for 24 hours-72 hours to test the cytotoxicity. Culturing cells with MTT at a final concentration of 0.5 mg/mL for another 4 hours at the end of treatment. The purple MTT formazan is dissolved by DMSO and the absorbance at 570 nm is taken with a spectrophotometer. The absorbance is proportional to the viability of adipocytes|
|Incubation time||24 hours|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 30 mg/mL|
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