From bench to health equity: In vitro insights on bioinspired peptides as multifunctional antidiabetic agents
1
Department of Anatomy, University of Pretoria, Pretoria, South Africa
2
Department of Biochemistry, Ahmadu Bello University, Zaria, Nigeria
Popul. Med. 2026;8(Supplement Supplement 1):
ABSTRACT
BACKGROUND:
Type 2 diabetes mellitus (T2DM), as a multifactorial metabolic disorder involving insulin resistance, oxidative stress, and inflammation, continues to drive a need for new therapeutics including bioinspired multifunctional agents. Herein, a first study evaluated antidiabetic potentials of bioactive peptides from African yam (Dioscorea spp.) including AVIAIMF and GPADPF, as well as taro (Colocasia esculenta), NGDF and NGNW. The second study investigated previously reported α-glucosidase inhibitory peptides such as YPG (synthetic), STYV (including its digested fragment STY) and SQSPA, both derived from Aspergillus awamori and Silkworm pupae respectively.
METHODS:
All peptides were synthesised and tested using in vitro and cell-based models. Dipeptidylpeptidase-IV (DPP-IV) inhibition, oxygen radical absorbance capacity (ORAC), inhibition of methylglyoxal (MGO)-induced advanced glycation end-products (AGEs), inhibition of nitric oxide (NO) in vitro, inhibition of lipid accumulation in 3T3-L1 adipocytes, cytotoxicity studies using 3T3-L1 adipocytes and Caco-2 cells, were evaluated. Principal component analysis was also used to identify multifunctional relationships among bioactivities in the first study. Results and conclusion Yam- and taro-derived peptides significantly (p<0.05) inhibited DPP-IV, with NGDF showing the highest potency. On the other hand, YPG, SQSPA, STY, and STYV also inhibited DPP-IV even more so for YPG and SQSPA. The tuber-derived AVIAIMF, GPADPF, and NGNW inhibited methylglyoxal-induced AGE formation and demonstrated antioxidant and NO scavenging activities (p<0.05) without cytotoxicity in Caco-2 cells. For the α-glucosidase inhibitory peptides, STYV and STY showed significantly (p<0.05) higher scavenging of reactive species. However, YPG significantly prevented lipid accumulation in differentiating 3T3-L1 cells. In addition, the peptides showed favourable multifunctional profiles without cytotoxicity in differentiating or fully differentiated 3T3-L1 cells. These peptides have demonstrated antidiabetic activities by modulating enzymatic, oxidative, and lipid pathways, supporting their use as multifunctional therapeutics for T2DM management. Their development aligns with SDG3 (Good Health and Well-being), offering a sustainable approach to improving metabolic health.
Type 2 diabetes mellitus (T2DM), as a multifactorial metabolic disorder involving insulin resistance, oxidative stress, and inflammation, continues to drive a need for new therapeutics including bioinspired multifunctional agents. Herein, a first study evaluated antidiabetic potentials of bioactive peptides from African yam (Dioscorea spp.) including AVIAIMF and GPADPF, as well as taro (Colocasia esculenta), NGDF and NGNW. The second study investigated previously reported α-glucosidase inhibitory peptides such as YPG (synthetic), STYV (including its digested fragment STY) and SQSPA, both derived from Aspergillus awamori and Silkworm pupae respectively.
METHODS:
All peptides were synthesised and tested using in vitro and cell-based models. Dipeptidylpeptidase-IV (DPP-IV) inhibition, oxygen radical absorbance capacity (ORAC), inhibition of methylglyoxal (MGO)-induced advanced glycation end-products (AGEs), inhibition of nitric oxide (NO) in vitro, inhibition of lipid accumulation in 3T3-L1 adipocytes, cytotoxicity studies using 3T3-L1 adipocytes and Caco-2 cells, were evaluated. Principal component analysis was also used to identify multifunctional relationships among bioactivities in the first study. Results and conclusion Yam- and taro-derived peptides significantly (p<0.05) inhibited DPP-IV, with NGDF showing the highest potency. On the other hand, YPG, SQSPA, STY, and STYV also inhibited DPP-IV even more so for YPG and SQSPA. The tuber-derived AVIAIMF, GPADPF, and NGNW inhibited methylglyoxal-induced AGE formation and demonstrated antioxidant and NO scavenging activities (p<0.05) without cytotoxicity in Caco-2 cells. For the α-glucosidase inhibitory peptides, STYV and STY showed significantly (p<0.05) higher scavenging of reactive species. However, YPG significantly prevented lipid accumulation in differentiating 3T3-L1 cells. In addition, the peptides showed favourable multifunctional profiles without cytotoxicity in differentiating or fully differentiated 3T3-L1 cells. These peptides have demonstrated antidiabetic activities by modulating enzymatic, oxidative, and lipid pathways, supporting their use as multifunctional therapeutics for T2DM management. Their development aligns with SDG3 (Good Health and Well-being), offering a sustainable approach to improving metabolic health.
| eISSN: | 2654-1459 |
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