Cellular transport of anti-inflammatory pro-drugs originated from a herbal formulation of Zingiber cassumunar and Nigella sativaReportar como inadecuado




Cellular transport of anti-inflammatory pro-drugs originated from a herbal formulation of Zingiber cassumunar and Nigella sativa - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.

Chinese Medicine

, 4:19

First Online: 25 September 2009Received: 07 December 2008Accepted: 25 September 2009

Abstract

BackgroundThe rhizome of Zingiber cassumunar and the seed of Nigella sativa are two ingredients in Thai traditional medicine to relieve dysmenorrhea and adjust the menstrual cycle. Mixture of these two herbs produces three esters, namely E-4-3,4-dimethoxyphenylbut-3-en-1-yl linoleate 1, E-4-3,4-dimethoxyphenylbut-3-en-1-yl oleate 2 and E-4-3,4-dimethoxyphenylbut-3-en-1-yl palmitate 3. The aim of this study is to examine in vitro absorption of these esters and evaluate their transport across the membrane.

MethodsIn vitro transport of these three esters was observed in Caco-2 cell monolayers. The ester compounds 1, 2 and 3 at a concentration of 10 μM were hydrolyzed by porcine liver esterase.

ResultsAll esters transported across the Caco-2 cell without enzymatic hydrolysis. The apparent permeability coefficients Papp of compound 1 at 53 μM and 106 μM were 13.94 0.60 × 10 and 14.33 0.17 × 10cm-s respectively, while those of compound 2 were 9.45 0.29 × 10 and 10.08 0.32 × 10cm-s, respectively. Papp values of compound 3 were 7.48 0.31 × 10cm-s at 53 μM and 8.60 0.55 × 10cm-s at 106 μM. Papp values of the parent compound compound D, i.e. E-4-3,4-dimethoxyphenylbut-3-en-1-ol were 8.53 0.83 × 10cm-s at 53 μM and 16.38 0.61 × 10cm-s at 106 μM. The ester hydrolysis of compounds 1, 2 and 3 by porcine liver esterase was monitored by HPLC and the hydrolysis reactions were completed within 10 minutes.

ConclusionUsing the Caco-2 cell monolayer model, the present study finds that compounds E-4-3,4-dimethoxyphenylbut-3-en-1-yl linoleate 1, E-4-3,4-dimethoxyphenylbut-3-en-1-yl oleate 2 and E-4-3,4-dimethoxyphenylbut-3-en-1-yl palmitate 3 originated from Prasaplai preparation a Thai herbal formula may be transported through a facilitated mechanism and serve as pro-drugs to increase the compound D level in the blood.

AbbreviationsHSV-1herpes simplex virus-1

DMEMDulbecco-s modified Eagle-s medium

FBSfetal bovine serum

TEERtrans-epithelial electrical resistance

HBSSHank-s balanced salt solution

HEPESn-2-hydroxyethyl piperazine-n-2-ethanosulfonic acid

PBSphosphate buffered saline

Pappapparent permeability coefficient

ODSoctadecylsilane.

Electronic supplementary materialThe online version of this article doi:10.1186-1749-8546-4-19 contains supplementary material, which is available to authorized users.

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Autor: Prasan Tangyuenyongwatana - Jariya Kowapradit - Praneet Opanasopit - Wandee Gritsanapan

Fuente: https://link.springer.com/



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