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Soybean-Based Functional Foods Through Microbial Fermentation: Processing and Biological Activities
Published in Megh R. Goyal, Arijit Nath, Rasul Hafiz Ansar Suleria, Plant-Based Functional Foods and Phytochemicals, 2021
Arijit Nath, Titas Ghosh, Abinit Saha, Klára Pásztorné Huszár, Szilvia Bánvölgyi, Renáta Gerencsérné Berta, Ildikó Galambos, Edit Márki, Gyula Vatai, Andras Koris, Arpita Das
Several soybean-derived peptides have anti-diabetic activity in addition to their anti-obesity activity [48, 59, 75]. Soybean-derived peptides (such as: Leu-Pro-Tyr-Pro, Iso-Ala-Val-Pro-Gly-Glu-Val-ala, and Iso-Ala-Val-Pro-Thr-Gly-Val-Ala) help glucose metabolism by supporting glucose uptake in liver cells by activation of glucose transporters (GLUT 1 and GLUT 4) [5]. The peptide, Iso-Ala-Val-Pro-Thr-Gly-Val-Ala, inhibits activity of dipeptidyl peptidase IV that is responsible for hydrolysis of peptide hormone glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide [52]. Furthermore, soybean-derived peptides can suppress the activity of α-glucosidase that is located at brush border of the enterocytes of jejunum in small intestine. It is a key enzyme for producing monosaccharide and their absorption on the gut-wall.
Therapeutic Potential of Anthocyanin Against Diabetes
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
Tawheed Amin, H. R. Naik, Bazila Naseer, Syed Zameer Hussain
Anthocyanin-rich black bean coat extracts may decrease the generation of reactive oxygen species (ROS) up to 80% due to its antioxidant activity [84]. This reduction in ROS may protect and improve the ability of β-cells of islets of Langerhans, thereby suggesting an indirect role of anthocyanins in mitigation of diabetes. Dipeptidyl peptidase 4, an essential enzyme, is metabolically related to insulin secretion [84]. Anthocyanin-rich extracts obtained from the coats of black beans have been reported to inhibit Dipeptidyl peptidase 4 [84], thereby suggesting the role of anthocyanins in the prevention and management of diabetes.
Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
While studying pyrrole derivatives, the structure-activity relationship abbreviated as SAR should be emphasized. SAR correlates the structure and medicinal activity of a molecule, which is a mandatory requisite in the pharmaceutical industry. SAR can easily identify the important functional groups and sub-units that play a major role to determine the medicinal effect of a drug. Efforts were taken to develop pyrrole-derived drugs to remove/reduce the harmful secondary responses of many current anti-diabetic drugs. Some anti-diabetic drugs work as dipeptidyl peptidase IV (DPP4) inhibitors. Attempts were taken to reduce the aftereffects through incorporation of pyrrole group to the inhibitor molecule (Mohamed et al., 2014). Replacement of a thienopyrimidine with a pyrrolopyrimidine in the dipeptidyl peptidase IV inhibitor increases activity as well as stability. The activity of these pyrrole derivatives was compared to a widely used medication for diabetes, glimepiride. The pyrrole derivatives showed similar therapeutic activity.
TGR5 agonists for diabetes treatment: a patent review and clinical advancements (2012-present)
Published in Expert Opinion on Therapeutic Patents, 2022
Rachana S. Bhimanwar, Amit Mittal
Kanazawa University conducted a Phase 4 clinical trial on Ursodeoxycholic Acid (UDCA) (21) addressing Glucagon-like peptide-1 (GLP-1) levels (Figure 19). Researchers studied the efficacy and safety of UDCA in people with Type 2 diabetes and chronic liver diseases. Participants (around 16) were administered 900 mg of UDCA for 12 weeks followed by 50 mg of sitagliptin as additive therapy for dipeptidyl peptidase-4 (DPP4) inhibitors. Results showed a decrease in body weight from 72.5 ± 8.4 to 70.6 ± 8.6 kg) and the HbA1c level (7.0%±0.3% to 6.4%±0.5%) in the patients treated with UDCA. The HbA1c level decreased further (6.4% ± 0.5% to 6.0% ± 0.4%) in patients treated with sitagliptin as add-on therapy. A combination of UDCA and the dipeptidyl peptidase-4 inhibitor can therefore be considered a novel treatment of Type 2 diabetes [49,50].
Exendin-4 attenuates inflammation-mediated endothelial cell apoptosis in varicose veins through inhibiting the MAPK-JNK signaling pathway
Published in Journal of Receptors and Signal Transduction, 2020
Glucagon-like peptide-1 (GLP-1) is an incretin hormone produced by the intestinal L-cells from a post-translational processing of proglucagon. Exendin-4 is a biologically synthetic peptide have similar effects on GLP-1. Exendin-4 modulates satiety and reduces gastric emptying typically with a net effect of weight loss [23]. GLP-1 has a short half-life owing to its rapid enzymatic degradation by dipeptidyl peptidase-4 [24]. Accordingly, several analogs including Exendin-4 resistant to dipeptidyl peptidase-4 are routinely used for type-2 diabetes treatment. The concomitant weight loss also observed in non-diabetic patients led to consideration of GLP-1 analogs for obesity care. Previous studies have found the anti-inflammatory effect of Exendin-4 on inflammation response. In the current study, we explored the influence of Exendin-4 on inflammation-mediated cell apoptosis [25].
The emerging role of dipeptidyl-peptidase-4 as a therapeutic target in lung disease
Published in Expert Opinion on Therapeutic Targets, 2020
Hai Zou, Ning Zhu, Shengqing Li
Dipeptidyl-peptidase-4/CD26 (DPP-4) is a highly specific cell-surface ectopeptidase, which cleaves dipeptides from the N-terminus, where a proline residue is in a penultimate position [4]. DPP-4 will preferentially cleave proline at this residue, however, it can also act on alanine and glycine, albeit less rapidly [5]. It has many facets apart from its catalytic capabilities. DPP4 is an integral (type II) transmembrane protein [6], whereas circulating DPP-4 has also been documented and can be measured in plasma [4]. Vascular smooth muscle cells (VSMCs), monocytes, lymphocytes, and hepatocytes are purported to be sources of soluble DPP-4 [7]. Its removal from the cell surface can be mediated by a number of proteases including, matrix metalloproteases (MMPs) [7]. Shed circulating DPP-4 has nominally been assigned as a novel adipokine that can act in both a paracrine and endocrine manner [8], and a novel receptor has been characterized. Furthermore, circulating soluble DPP-4 is elevated in the obese and patients with type II diabetes [9].