Herba Epimedii's biotransformation in vitro simulated gastrointestinal digestion and faecal fermentation systems / 中国药理学与毒理学杂志

OBJECTIVE Epimedium is rich in a variety of beneficial active ingredients, and has been widely used in the ethnopharmacological practices, however, its biotransformation in gastrointestinal digestions remain unclear. This study aimed to investigate the dynamic changes of components and biological activity of Epimedium in the in vitro simu? lated digestion and subsequent human faecal fermentation. METHODS The models of in vitro simulated saliva, gastric and intestinal digestion, as well as colonic fermentation were constructed to simulate the digestion process of Epimedium. The dynamic changes of components of Epimedium during the simulated digestions in vitro and subsequent human faecal fermentation were investigated by UPLC-MS, HPLC-DAD combined with principal component analysis (PCA) and multi-ingredient quantitative analysis. RESULTS A variety of metabolites with high contents were produced after 0.5 h of intestinal digestion and colonic fermentation 0.5 h. Application of PCA to HPLC data showed the obvious separation of colonic fermentation 0.5 h stage samples from other colonic fermentation stages samples (24, 48 and 72 h). Addition? ally, non-digestion and saliva digestion stage samples clustered together, and there was obvious separation between intestinal digestion samples and gastric digestion samples. The contents of epimedium C, icariin and baohuside I all increased significantly after intestinal digestion [58.70 ± 7.08, 47.15 ± 5.68 and (12.78 ± 0.55) mg · g-1] compared with gastric digestion [29.00 ± 5.65, 17.40 ± 4.55 and (2.77 ± 0.19) mg·g-1]. There were significant differences between sample after 0.5 h of colonic fermentation [64.22 ± 9.32, 51.26 ± 6.33 and (16.68 ± 3.19) mg·g-1] and other time points (24, 48 and 72 h) in components and the contents of active ingredient, and the content of these components all decreased with the fermentation time. The ability of scavenging ABTS free radicals [IC50=(0.29 ± 0.02) g · L-1] increased significantly compared with gastric digestion [(1.57 ± 0.02) g·L-1], and after 0.5 h of colonic fermentation, the ability also increased significantly. CONCLUSION Gastrointestinal digestion had a significant impact on the contents of active components in Epimedium, and the metabolism of these components mainly occurred in the colon. The intestinal digestion and colonic fermentation significantly improved the anti-ABTS activity of epimedium.

Microencapsulation of immunoglobulin Y: optimization with response surface morphology and controlled release during simulated gastrointestinal digestion / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Immunoglobulin Y (IgY) is an effective orally administered antibody used to protect against various intestinal pathogens, but which cannot tolerate the acidic gastric environment. In this study, IgY was microencapsulated by alginate (ALG) and coated with chitooligosaccharide (COS). A response surface methodology was used to optimize the formulation, and a simulated gastrointestinal (GI) digestion (SGID) system to evaluate the controlled release of microencapsulated IgY. The microcapsule formulation was optimized as an ALG concentration of 1.56% (15.6 g/L), COS level of 0.61% (6.1 g/L), and IgY/ALG ratio of 62.44% (mass ratio). The microcapsules prepared following this formulation had an encapsulation efficiency of 65.19%, a loading capacity of 33.75%, and an average particle size of 588.75 µm. Under this optimum formulation, the coating of COS provided a less porous and more continuous microstructure by filling the cracks on the surface, and thus the GI release rate of encapsulated IgY was significantly reduced. The release of encapsulated IgY during simulated gastric and intestinal digestion well fitted the zero-order and first-order kinetics functions, respectively. The microcapsule also allowed the IgY to retain 84.37% immune-activity after 4 h simulated GI digestion, significantly higher than that for unprotected IgY (5.33%). This approach could provide an efficient way to preserve IgY and improve its performance in the GI tract.

Microencapsulation of immunoglobulin Y: optimization with response surface morphology and controlled release during simulated gastrointestinal digestion / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Immunoglobulin Y (IgY) is an effective orally administered antibody used to protect against various intestinal pathogens, but which cannot tolerate the acidic gastric environment. In this study, IgY was microencapsulated by alginate (ALG) and coated with chitooligosaccharide (COS). A response surface methodology was used to optimize the formulation, and a simulated gastrointestinal (GI) digestion (SGID) system to evaluate the controlled release of microencapsulated IgY. The microcapsule formulation was optimized as an ALG concentration of 1.56% (15.6 g/L), COS level of 0.61% (6.1 g/L), and IgY/ALG ratio of 62.44% (mass ratio). The microcapsules prepared following this formulation had an encapsulation efficiency of 65.19%, a loading capacity of 33.75%, and an average particle size of 588.75 μm. Under this optimum formulation, the coating of COS provided a less porous and more continuous microstructure by filling the cracks on the surface, and thus the GI release rate of encapsulated IgY was significantly reduced. The release of encapsulated IgY during simulated gastric and intestinal digestion well fitted the zero-order and first-order kinetics functions, respectively. The microcapsule also allowed the IgY to retain 84.37% immune-activity after 4 h simulated GI digestion, significantly higher than that for unprotected IgY (5.33%). This approach could provide an efficient way to preserve IgY and improve its performance in the GI tract.

Identification of Peptide Profiling of Deer Antler by Reversed Phase Liquid Chromatography-Tandem Mass Spectrometry and Bioactivities in Simulated Gastrointestinal Digestion / 分析化学

Reversed phase liquid chromatography-tandem mass spectrometry (RPLC-MS/MS) was utilized to investigate peptide profiling and bioactivities of antler aqueous extract(AAE),digested antler aqueous extract (AED) and powder(PD). A total of 23,417 and 389 peptides,as well as 15,146 and 75 collagen peptides were identified from AAE, AED and PD, respectively. Angiotensin converting enzyme (ACE) inhibitory activity,dipeptidyl peptidase IV(DPP-IV) inhibitory activity,prolyl endopeptidase(PEP) inhibitory activity and antioxidant activity were used to evaluate the bioactivities of AAE,AED and PD,and it was found that the sequence of their bioactivities was AAE<AED<PD. All the results above proved that AED released more collagen peptides and PD possessed better biological activities. It suggests that the two edible ways of antler are complemented each other and have their own advantages.