Loureirin B activates GLP‐1R and promotes insulin secretion in Ins‐1 cells

Abstract

Diabetes mellitus (DM), as a kind of metabolic disease, is characterized by the deficiency of insulin function and secretion, which leads to chronic hyperglycaemia, affecting the metabolism of protein, fat and carbohydrate. 1,2 DM patients mainly manifested as polyphagia, polydipsia, polyuria and weight loss. Type 2 diabetes mellitus (T2DM) accounts for 90-95% of diabetic patients. Insulin resistance and β cell failure (decrease of β cell quality, glucose sensitivity and secretion ability) are the main characteristics. 3,4 DM is regarded by the World Health Organization (WHO) as one of the four main non-communicable diseases (NCDs). 5 Current treatment options for DM include the sole application of exogenous insulin or combining it with allopathic drugs. Those hypoglycaemic drugs decrease fasting blood glucose through many pathways, such as biguanides (metformin), sulphonylureas (glibenclamide) and alpha-glucosidase inhibitors (acarbose and miglitol). 6 Many efforts have been made to explore safe and effective anti-T2DM drugs. 7 Glucagon-like peptide-1 (GLP-1) is a glucose-dependent hormone that stimulates islet beta cells to secrete insulin in a glucose-dependent manner. 8 GLP-1 receptor (GLP-1R) belongs to the glucagon receptor B family and distributes in pancreatic cells, gastrointestinal tract, cardiovascular, lung and central nervous system. 9 GLP-1 continues to activate the GLP-1R, which increases insulin secretion, beta-cell proliferation and regeneration. 10,11 GLP-1R is an important target for insulin secretion, the agonists of which are widely used in the treatment of DM. 12 A series of GLP-1R agonists, such as exdin-4, liraglutide and lixisenatide, have been developed. 13,14 In addition to significantly reducing blood glucose, GLP-1R agonists can also reduce weight, blood pressure, improving the function of β cell, which showed the potential to delay the progress of diabetes and reduce cardiovascular complications. 13 GLP-1R agonists can delay intestinal

Utilization of methanol for condensation interrupted chemoselective transfer hydrogenation of CC, CO, and CN bonds under low catalyst loading

“…Loureirin A and loureirin B are flavonoids extracted from Dracaena cochinchinensis and are extensively used as inhibitors of platelet activation by an impairment of PI3K/Akt signalling and PAI-1, respectively. 17 Using our protocol, both of them were synthesized in good yields starting from their unsaturated counterparts ( 42 and 43 ). 1-(2,4-Dihydroxyphenyl)-3-(4-hydroxyphenyl)propan-1-one was also successfully transfer hydrogenated to achieve davidigenin, an antiallergic compound ( 44 ).…”

Computational Insight into Anti-Obesity Effects of Combined Some Phytobiotics to GLP1R (Glucagon-Like Peptide 1 Receptor) Protein inAnas javanica

“…One of the agonists that have been proven to perform an interaction with GLP1R is Loureirin B. Loureirin B is a natural compound derived from Sanguis draconis and has various pharmacological effects, one of which is hypoglycemic. The interaction in Loureirin B is similar to the interaction of the GLP1 protein, which interacts with GLP1R to increase insulin secretion (Ding et al 2021).…”

“…The result of the interaction between loureirin B and GLP1R has a bond energy of -7.4 kcal/mol. It was previously known that loureirin B could increase insulin production by interacting with the GLP1R protein (Ding et al, 2021). When compared to the docking results of various other active compounds, lourerin B is still at fairly weak bond energy when compared to cynaroside (-9.2 kcal/mol), 14-Deoxy-11,12-didehydroandrographolide (-9.1 kcal/mol), rutin (-8.8 kcal/mol), andrographidine E (-8.6 kcal/mol), and cianidanol (-7.8 kcal/mol).…”

Neuroprotection by dipeptidyl-peptidase-4 inhibitors and glucagon-like peptide-1 analogs via the modulation of AKT-signaling pathway in Alzheimer’s disease

“…Geniposide modulates GLP1 receptors signaling[ 66 ]. Loureirin B is a natural product derived from Sanguis draconis , which promotes insulin secretion of Ins-1 cells through GLP1 receptor[ 67 ]. Lamiophlomis rotata is an orally available Tibetan herb, which specifically reduces pain hypersensitivity states through the activation of GLP1 receptors[ 68 ].…”