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|Title:||Determination of trans-2,4,3',4',5'-pentamethoxystilbene in rat plasma and its application to a pharmacokinetic study|
|Authors:||Lin, H.-S. |
|Keywords:||Absolute oral bioavailability|
|Citation:||Lin, H.-S., Spatafora, C., Tringali, C., Ho, P.C. (2012-01-05). Determination of trans-2,4,3',4',5'-pentamethoxystilbene in rat plasma and its application to a pharmacokinetic study. Journal of Pharmaceutical and Biomedical Analysis 57 (1) : 94-98. ScholarBank@NUS Repository. https://doi.org/10.1016/j.jpba.2011.08.020|
|Abstract:||trans-2,4,3',4',5'-Pentamethoxystilbene (2,4,3',4',5'-PMS) is a resveratrol derivative that displayed promising pre-clinical anti-cancer activities. In this study, a simple HPLC method was developed and validated to determine 2,4,3',4',5'-PMS in rat plasma. The lower limit of quantification was 9. ng/ml. The intra- and inter-day precision in terms of relative standard deviation was less than 9.7% and the bias rate ranged from -6.4 to +7.8%. The pharmacokinetics of 2,4,3',4',5'-PMS was subsequently studied in Sprague-Dawley rats. Upon intravenous administration (0.75. mg/kg), 2,4,3',4',5'-PMS displayed moderate clearance (58.5 ± 19.5 ml/min/kg) and terminal elimination half-life (147 ± 61 min). Aqueous solubility appeared to be a barrier to oral absorption. When suspension was given (4. mg/kg), the absolute oral bioavailability was almost nil; when 2,4,3',4',5'-PMS was fully solubilized by randomly methylated-β-cyclodextrin, it possessed a low bioavailability (3.63 ± 2.06%). The pharmacokinetic comparison among 2,4,3',4',5'-PMS and other methoxylated stilbenes suggested that the 2-methoxy group was unfavorable to oral bioavailability. Future investigations on 2,4,3',4',5'-PMS should be focused on chemo-prevention of colorectal carcinogenesis. © 2011 Elsevier B.V.|
|Source Title:||Journal of Pharmaceutical and Biomedical Analysis|
|Appears in Collections:||Staff Publications|
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