Absorption and bioavailability of artepillin C in rats after oral administration
Absorption and bioavailability of artepillin C in rats after oral administration
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DOI：
10.1021/jf051962y
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发表时间：
2005-12-28
影响因子：
6.1
通讯作者：
Yoshioka, E
中科院分区：
文献类型：
--
作者：
Konishi, Y;Hitomi, Y;Yoshioka, E
Artepillin C (AC) 是巴西蜂胶的一种活性成分，通过跨细胞被动扩散完整地渗透到 Caco-2 细胞中。 AC 穿过 Caco-2 细胞的渗透效率与酚酸和吸收不良的多酚的微生物代谢物一样有效，这些多酚被单羧酸转运蛋白 (MCT) 主动吸收（Biochim. Biophys. Acta 2005, 1713, 138144）。在这里，我们研究了口服 AC 在大鼠中的吸收，以与 MCT 底物对香豆酸 (CA) 的比较来评估其体内药代动力学和生物利用度。给予大鼠100μmol/kg体重的AC或CA，随后从门静脉和腹动脉采血。使用 HPLC-ECD 通过库仑检测对 AC、CA 及其代谢物进行定量。门静脉中完整AC和CA的血清浓度在给药后5-10分钟达到峰值，AC的C-max为19.7μmol/L，CA为74.8μmol/L。根据血清浓度计算门静脉中完整AC和CA的曲线下面积(AUC)分别为182.6和3057.3μmol(中心点)min(中心点)L(-1)。 CA的吸收效率比AC高约17倍。此外，CA的生物利用度比AC高约278倍，AC和CA的腹动脉AUC与门静脉AUC之比分别为0.04和0.70。因此，AC 可能比 CA 更容易被肝脏消除。 AC在体内的生物活性化合物值得进一步研究。
Artepillin C (AC), an active ingredient of Brazilian propolis, permeates intact across Caco-2 cells by transcellular passive diffusion. The permeation of AC across Caco-2 cells is as efficient as that of phenolic acids and the microbial metabolites of poorly absorbed polyphenols, which are actively absorbed by the monocarboxylic acid transporter (MCT) (Biochim. Biophys. Acta 2005, 1713, 138144). Here, the absorption of orally administered AC in rats has been studied to evaluate its pharmacokinetics and bioavailability in vivo in comparison with those of p-coumaric acid (CA), a substrate of MCT. Rats were given 100 mu mol/kg of body weight of AC or CA, and blood was subsequently collected from the portal vein and abdominal artery. AC, CA, and their metabolites were quantified by coulometric detection using HPLC-ECD. The serum concentration of intact AC and CA in the portal vein peaked at 5-10 min after administration, with a C-max of 19.7 mu mol/L for AC and 74.8 mu mol/L for CA. The area under the curve (AUC) for intact AC and CA in the portal vein was calculated from the serum concentration as 182.6 and 3057.3 mu mol(center dot)min(center dot)L(-1), respectively. The absorption efficiency of CA was about 17-fold higher than that of AC. Furthermore, the bioavailability of CA was about 278-fold higher than that of AC, and the ratio of AUC in the abdominal artery to AUC in the portal vein was 0.04 and 0.70, for AC and CA, respectively. Thus, AC is likely to be more susceptible to hepatic elimination than is CA. The bioactive compound of AC in vivo should be investigated further.