antiobesity

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

CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Cetilistat (ATL-962) is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes.

1-Deoxynojirimycin (Moranoline) is a potent α-glucosidase inhibitor, suppressing postprandial blood glucose, thereby possibly preventing diabetes mellitus.

KY-226 is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B)(IC50: 0.25 μM,)

TGR5 is a potent TGR5(GPCR19) agonist.

1-Deoxynojirimycin hydrochloride (Moranoline) is a potent and selective inhibitor of alpha-glucosidase, most commonly found in mulberry leaves. Duvoglustat is used to suppress the elevation of postprandial hyperglycemia.

Nomilin is naturally occurring triterpenoids, have immunomodulatory activity.

Tigogenin is one of steroidal sapogenins which is widely used for synthesizing steroid drugs. It might have protective effect on bone and be helpful in preventing the development of osteoporosis.

5,7-DIMETHOXYFLAVONE possessed remarkable leishmanicidal potential.

N-Aminopiperidine hydrochloride (Piperidin-1-amine hydrochloride) is a metabolite (M1) of the canabinoid receptor 1 antagonist Rimonabant, an antiobesity agent.

Phloracetophenone (1-(2,4,6-Trihydroxyphenyl)ethanone) has antiobesity and hypolipidemic effects, may be partly mediated by delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

(±)-Evodiamine is an alkaloid isolated from Evodiae fructus and a topoisomerase I inhibitor. It also inhibits adipocyte differentiation and diabetes by downregulating IGF-1/HIF-1α and IL-6/STAT pathways. As an inhibitor of NF-κB activation, it suppresses invasion, promotes apoptosis, and inhibits TNF-induced Akt activation.

LY-79771, a phenethanolamine antiobesity agent, can be effective in preventing fat regain following energy deprivation.

Ro 22-0654, a novel lipid synthesis inhibitor, has antiobesity effects.

Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body weight and food intake and increases core body temperature in mice when administered at a dose of 36 μg/animal.5Intrathecal administration of NMU-23 decreases the mechanical pain threshold in the von Frey test in rats.6 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBr. J. Pharmacol.158(1)87-103(2009) 2.Szekeres, P.G., Muir, A.I., Spinage, L.D., et al.Neuromedin U is a potent agonist at the orphan G protein-coupled receptor FM3J. Biol. Chem.275(27)20247-20250(2000) 3.Hosoya, M., Moriya, T., Kawamata, Y., et al.Identification and functional characterization of a novel subtype of neuromedin U receptorJ. Biol. Chem.275(38)29528-29532(2000) 4.Brighton, P.J., Wise, A., Dass, N.B., et al.Paradoxical behavior of neuromedin U in isolated smooth muscle cells and intact tissueJ. Pharmacol. Exp. Ther.325(1)154-164(2008) 5.Peier, A., Kosinski, J., Cox-York, K., et al.The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2)Endocrinology150(7)3101-3109(2009) 6.Yu, X.H., Cao, C.Q., Mennicken, F., et al.Pro-nociceptive effects of neuromedin U in ratNeuroscience120(2)467-474(2003)

GLS1 Inhibitor-7 (compound 4d) is a GLS1 antagonist with an IC50 value of 46.7 μM, showing potential applications in anticancer, antiaging, and antiobesity therapies [1].

Epitheaflagallin 3-O-gallate is a promising functional food material with potential antiobesity and antiperiodontal disease activities, suppressing tumor growth through [the] suppression of angiogenesis.

Erycibelline has antiobesity activity, it may be a useful therapeutic agent for body weight control by downregulating adipogenesis and lipogenesis.

Tachioside has antiobesity, antioxidant and α-glucosidase inhibitory activities, it decreases lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis, shows antiobesity activities. Tachioside can inhibit nitric oxide production in lipopolysaccharides-stimulated RAW 264.7 cells with IC50 value of 12.14 μM.