Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1
Type 2 diabetes mellitus remains a critical global health challenge, driving the pursuit of novel therapeutic strategies. This study investigated the anti-diabetic efficacy of the peptide 1CBR, derived from sodium caseinate hydrolysate, administered orally at 25 mg/kg/day to db/db mice over a 4-week...
Saved in:
| Main Authors: | , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-05-01
|
| Series: | Foods |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2304-8158/14/11/1953 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1850160562031296512 |
|---|---|
| author | Pei-Yu Wu Cheng-Hong Hsieh Ali Iqbal Yu-Shun Lin Ming-Wei Cheng Ling-Hsuan Chang Shang-Ming Huang Kuo-Chiang Hsu |
| author_facet | Pei-Yu Wu Cheng-Hong Hsieh Ali Iqbal Yu-Shun Lin Ming-Wei Cheng Ling-Hsuan Chang Shang-Ming Huang Kuo-Chiang Hsu |
| author_sort | Pei-Yu Wu |
| collection | DOAJ |
| description | Type 2 diabetes mellitus remains a critical global health challenge, driving the pursuit of novel therapeutic strategies. This study investigated the anti-diabetic efficacy of the peptide 1CBR, derived from sodium caseinate hydrolysate, administered orally at 25 mg/kg/day to db/db mice over a 4-week period. Glucose tolerance was evaluated via oral glucose tolerance tests (OGTT), while plasma dipeptidyl peptidase-IV (DPP-IV) activity, glucagon-like peptide-1 (GLP-1), and insulin concentrations were quantified using enzyme-linked immunosorbent assays (ELISA). Two bioactive peptides, GPFPLPD and APDSGNFR, were isolated and characterized, exhibiting half-maximal inhibitory concentrations (IC<sub>50</sub>) of 99.12 µM and 73.07 µM for DPP-IV inhibition, respectively, and both significantly stimulated GLP-1 secretion in enteroendocrine cells in vitro. Pharmacokinetic analysis in Sprague–Dawley rats demonstrated oral bioavailability of 11.28% and 19.12% for these peptides, surpassing typical expectations for peptide-based agents. Collectively, these results provide compelling evidence that 1CBR-derived peptides exert glucose-lowering effects through the dual mechanisms of DPP-IV inhibition and GLP-1 stimulation, combined with favorable oral absorption profiles. These findings underscore the potential of 1CBR peptides as promising candidates for development into nutraceuticals or pharmaceutical agents for diabetes management. |
| format | Article |
| id | doaj-art-2203e56c7aa340288d8ec823f46d82d3 |
| institution | OA Journals |
| issn | 2304-8158 |
| language | English |
| publishDate | 2025-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Foods |
| spelling | doaj-art-2203e56c7aa340288d8ec823f46d82d32025-08-20T02:23:07ZengMDPI AGFoods2304-81582025-05-011411195310.3390/foods14111953Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1Pei-Yu Wu0Cheng-Hong Hsieh1Ali Iqbal2Yu-Shun Lin3Ming-Wei Cheng4Ling-Hsuan Chang5Shang-Ming Huang6Kuo-Chiang Hsu7Department of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanDepartment of Nutrition, China Medical University, 100 Sec. 1, Jingmao Road, Taichung 406040, TaiwanType 2 diabetes mellitus remains a critical global health challenge, driving the pursuit of novel therapeutic strategies. This study investigated the anti-diabetic efficacy of the peptide 1CBR, derived from sodium caseinate hydrolysate, administered orally at 25 mg/kg/day to db/db mice over a 4-week period. Glucose tolerance was evaluated via oral glucose tolerance tests (OGTT), while plasma dipeptidyl peptidase-IV (DPP-IV) activity, glucagon-like peptide-1 (GLP-1), and insulin concentrations were quantified using enzyme-linked immunosorbent assays (ELISA). Two bioactive peptides, GPFPLPD and APDSGNFR, were isolated and characterized, exhibiting half-maximal inhibitory concentrations (IC<sub>50</sub>) of 99.12 µM and 73.07 µM for DPP-IV inhibition, respectively, and both significantly stimulated GLP-1 secretion in enteroendocrine cells in vitro. Pharmacokinetic analysis in Sprague–Dawley rats demonstrated oral bioavailability of 11.28% and 19.12% for these peptides, surpassing typical expectations for peptide-based agents. Collectively, these results provide compelling evidence that 1CBR-derived peptides exert glucose-lowering effects through the dual mechanisms of DPP-IV inhibition and GLP-1 stimulation, combined with favorable oral absorption profiles. These findings underscore the potential of 1CBR peptides as promising candidates for development into nutraceuticals or pharmaceutical agents for diabetes management.https://www.mdpi.com/2304-8158/14/11/1953type 2 diabetes mellitussodium caseinate hydrolysatedipeptidyl peptidase-IVglucagon-like peptide-1 |
| spellingShingle | Pei-Yu Wu Cheng-Hong Hsieh Ali Iqbal Yu-Shun Lin Ming-Wei Cheng Ling-Hsuan Chang Shang-Ming Huang Kuo-Chiang Hsu Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1 Foods type 2 diabetes mellitus sodium caseinate hydrolysate dipeptidyl peptidase-IV glucagon-like peptide-1 |
| title | Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1 |
| title_full | Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1 |
| title_fullStr | Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1 |
| title_full_unstemmed | Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1 |
| title_short | Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1 |
| title_sort | bioactive peptides from sodium caseinate hydrolysate with high oral absorption regulate blood glucose in type 2 diabetic mice via inhibition of dpp iv and stimulation of glp 1 |
| topic | type 2 diabetes mellitus sodium caseinate hydrolysate dipeptidyl peptidase-IV glucagon-like peptide-1 |
| url | https://www.mdpi.com/2304-8158/14/11/1953 |
| work_keys_str_mv | AT peiyuwu bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT chenghonghsieh bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT aliiqbal bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT yushunlin bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT mingweicheng bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT linghsuanchang bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT shangminghuang bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 AT kuochianghsu bioactivepeptidesfromsodiumcaseinatehydrolysatewithhighoralabsorptionregulatebloodglucoseintype2diabeticmiceviainhibitionofdppivandstimulationofglp1 |