antidiabetic

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Rutin hydrate (Sophorin), a kind of glycoside, widely exists in many plants including citrus fruit.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

Costunolide (Costus lactone) has anti-inflammatory and anti-oxidant properties and mediates apoptosis.

D-Tagatose (D-(-)-Tagatose), a rare natural hexoketose and isomer of D-galactose, occurs naturally in Sterculia setigera gum and is found in small quantities in various foods such as sterilized and powdered cow's milk, hot cocoa, and various cheeses, yogurts, and other dairy products. It can be synthesized from D-galactose by isomerization under alkaline conditions in the presence of calcium. D-Tagatose has numerous health benefits, including promotion of weight loss, no glycemic effect, anti-plaque, non-cariogenic, anti-halitosis, prebiotic, and anti-biofilm properties; it is beneficial for organ transplants, enhancement of flavor, improvement of pregnancy and fetal development, treatment of obesity, and reduction in symptoms associated with type 2 diabetes, hyperglycemia, anemia, and hemophilia. (PMID: 17492284).

Glymidine sodium is a sulfonamide hypoglycemic agent which stimulates insulin secretion.

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

Glibornuride, a blocker of ATP-sensitive K+ channels (pKi: 5.75), inhibits high-affinity [3H]-glibenclamide binding with potencies corresponding to its K+ channel activity.

KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete.

Mifobate (SR-202) is a potent and specific antagonist of PPARγ, exhibiting antiobesity, antidiabetic, and antiatherosclerotic effects[1].

Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation.

MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.

Enavogliflozin (DWP-16001) is an orally available small molecule and sodium glucose transporter 2 inhibitor.

Azoramide, a small-molecule modulator, has the antidiabetic activity of unfolded protein response.

AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).

Vomicine is a natural product from Strychnos nux-vomica, the S. nux-vomica extracts show antihyperglycemic activity in experimental animals.

Bruceine E is isolated from B. javanica seeds with hypoglycemia effects. Bruceine E can be used for studies about acting as an insulin secretagogue.

Arjunolic acid has antioxidant, anti-inflammatory, antinociceptive and anticholinesterasic (AChE and BuChE) activities, it may as promising targets for the development of innovative multi-functional medicines for Alzheimer desease treatment.

Flavanomarein demonstrates potent antioxidative property, including free radical scavenging activity, inhibition of lipid peroxidation, as well as lipid-lowering effects in human HepG2 hepatocellular carcinoma cells treated with free fatty acids (FFAs).

Marein shows neuroprotective effect on PC12 cell damage induced by methylglyoxal, which is due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway, it may be a potent compound for preventing/counteracting diabetic e