乳源生物活性肽QEPV体内外的吸收转运（英文）

Transepithelial Transport of Milk-Derived Peptide QEPV in Vitro and in Vivo

发酵乳作为一种长寿食品备受关注。多肽Gln-Glu-Pro-Val(QEPV)是一种来源于发酵乳,具有免疫调节作用的生物活性肽。通过Caco-2细胞单层膜模型及小鼠模型,研究乳源性生物活性肽QEPV在体外和体内的转运吸收情况。结果表明:乳源性生物活性肽QEPV具有非常好的稳定性,且能够穿过由Caco-2细胞形成的转运模型,但当QEPV质量浓度高于3.00 mg/mL时穿膜速率趋于稳定。流式细胞术和超高效液相色谱-四极杆飞行时间质谱结果表明Caco-2细胞不能吸收QEPV,由于QEPV是不具有空间结构的小肽,可以初步推测出QEPV主要通过胞旁转运方式透过Caco-2细胞单层膜模型的结论。同时,QEPV可以经过腹腔注射和灌胃方式被小鼠吸收,但肠道吸收效率较差,腹腔吸收效率较好。

Fermented milk benefits human health in many respects. Gln-Glu-Pro-Val （QEPV） is a peptide produced through enzymatic hydrolysis of the milk-derived peptide Gln-Glu-Pro-Val-Leu. QEPV elicits immunomodulatory effects on lymphocytes as a bioactive peptide. In this research, the transepithelial transport of QEPV was investigated in vitro and in vivo by using the Caco-2 cell monolayer model and mouse models. Results showed that QEPV exhibited good stability and it could integrally cross the Caco-2 cell monolayer in vitro. A limited transepithelial transport rate was observed at the concentration of 3.00 mg/mL in the Caco-2 cell monolayer model. Besides, QEPV was not detected in Caco-2 cells by both flow cytometry （FCM） and ultra performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry （UPLC-Q-TOF-MS）. Therefore, QEPV could be absorbed as a bioactive peptide via the paracellular pathway in vitro. The in vivo experiments demonstrated that QEPV could be absorbed by mice via gastrointestinal and peritoneal routes. QEPV was less efficiently absorbed from the intestine than from the peritoneal cavity.