Sesamol, the phenolic degradation product of sesamolin, although recognised for its anti-inflammatory effects, has low bioavailability. In this manuscript, we attempted to improve its bioavailability by encapsulation in mixed phosphatidylcholine micelles. Sesamol could be solubilised and entrapped in phosphatidylcholine mixed micelles (PCS) with 96.8% efficiency (particle size 3.0±0.06nm). Fluorescence spectra of PCS revealed lower relative fluorescence intensity (RFI 112) compared to 'free' sesamol (FS) (RFI 271). The bioaccessibility, transport across a monolayer of cells and cellular uptake of PCS was 8.58%, 1.5-fold and 1.2-fold better, respectively, compared to FS. The anti-inflammatory effects of FS and PCS were compared using LPS treated RAW 264.7 cell line and lipoxygenase inhibition. PCS effected downregulation of iNOS protein expression (27%), NO production (20%), ROS (32%) and lipoxygenase inhibition (IC50=31.24μM) compared to FS.

译文

:芝麻素酚,芝麻素酚的酚类降解产物,尽管其具有抗炎作用,但其生物利用度较低。在本手稿中,我们试图通过封装在混合的磷脂酰胆碱胶束中来提高其生物利用度。芝麻酚可以以96.8%的效率(粒径3.0±0.06nm)溶解并截留在磷脂酰胆碱混合胶束(PCS)中。与“游离”芝麻酚(FS)(RFI 271)相比,PCS的荧光光谱显示较低的相对荧光强度(RFI 112)。与FS相比,其生物可及性,单层细胞转运和PCS的细胞吸收分别好8.58%,1.5倍和1.2倍。使用LPS处理的RAW 264.7细胞系和脂氧合酶抑制作用比较了FS和PCS的抗炎作用。与FS相比,PCS对iNOS蛋白表达(27%),NO产生(20%),ROS(32%)和脂氧合酶抑制(IC50 =31.24μM)的下调。

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