antiobesity

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.

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

Nomilin is naturally occurring triterpenoids, have immunomodulatory activity.

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.

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

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)

(±)-Evodiamine, a quinazolinocarboline alkaloid, functions as a Top1 inhibitor and exhibits anti-inflammatory, antiobesity, and antitumor properties by effectively inhibiting the proliferation of a broad range of tumor cells through apoptosis induction [1].

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.