U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 81 - 90 of 259 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Viridicatol is a polar metabolite first isolated from Penicillium cyclopium and P. viridicatum by Birkinshaw and collaborators in 1963. Viridicatol is a 2,3-dihydroxyquinoline which, like its analogue viridicatin, exists in equilibrium with its keto-tautomer. Viridicatol acts as an anti-inflammatory agent by suppressing the expression of pro-inflammatory mediators such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, via inhibition of the nuclear factor-kappa B (NF-κB) pathway in LPS stimulated cells. Further, viridicatol is a selective inhibitor of PTP1B, a potential drug target for the treatment of type 2 diabetes and obesity. Viridicatol revealed potent antibacterial activity against Staphylococcus aureus.
Sinensetin is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis. Sinensetin is a selective inhibitor of α-glucosidase with IC50 value of 0.66 mg/ml. Alpha-glucosidase and α-amylase inhibition could the mechanisms through which sinensetin exert its antidiabetic activity, indicating that it could have potential use in the management of non-insulin-dependent diabetes. Sinensetin inhibits inflammatory gene expression and STAT1 activation. It has meaningful anti-inflammatory properties which may be utilized in the development of novel anti-inflammatory treatments.
Syringin is a compound, extracted from Eleutherococcus senticosus. It is a component of herbs, which are used in traditional Chinese medicine. Several studies have demonstrated the multiple pharmacological properties of syringin, including anti-inflammatory, anti-tumor, and immunomodulatory effect. It was tested in several preclinical studies against type 2 diabetes, cardiac hypertrophy, edema, and arthritis. Syringin was shown to inhibit ICAM-1 expression and is considered as a possible treatment for acute gout.
S-Allylcysteine (SAC), the most abundant organosulfur compound in aged garlic extract, has multifunctional activity via different mechanisms and neuroprotective effects that are exerted probably via its antioxidant or free radical scavenger action. Anticancer effects of SAC were reported in prostate cancer, breast cancer, oral cavity cancer, non-small cell lung cancer, neuroblastoma, and hepatocellular carcinoma through the restoration of E-cadherin, the reduction of Slug and matrix metalloproteinase (MMP) protein expression, and stimulating apoptotic pathways. In addition, recently was revealed, that SAC might have imperative implications for the deterrence and early treatment of type 2 diabetes by reducing the influx of glucose in the polyol pathway, thereby elevating the GSH level and reducing the activities of aldose reductase (AR) and sorbitol dehydrogenase (SDH).
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



4’-Methoxychalcone (4-MC) is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. 4’-Methoxychalcone significantly enhances differentiation of preadipocytes, which is accompanied by the induction of adipogenic genes including PPARgamma and adiponectin. 4’-Methoxychalcone considerably upregulated PPARgamma-induced transcriptional activity and reversed the inhibitory effect of TNF-alpha on adipocyte differentiation and adiponectin expression. 4’-Methoxychalcone could be utilized for the prevention and treatment of metabolic syndrome and diabetes.
Benzyl-beta-D-glucoside (benzyl beta-D-glucopyranoside, BG) is a benzoyl glucoside, a natural substance that can be found in Pteris ensiformis. Benzyl beta-D-glucopyranoside, the constituent of the fruit of Prunus mume has been shown to relieve tension in experimental menopausal model rats (M-rats) caused by ether stress.
Flavonol (3-Hydroxyflavone) is a practically insole synthetic compound, which is not found naturally in plants. 3-hydroxyflavone can be found in a number of food items such as brassicas, pomegranate, red raspberry, and fenugreek, which makes 3-hydroxyflavone a potential biomarker for the consumption of these food products. Flavonol serves as a model molecule as it possesses an excited-state intramolecular proton transfer (ESIPT) effect to serve as a fluorescent probe to study membranes for example or intermembrane proteins.
Cafestol is a diterpene molecule found in coffee beans and has anticarcinogenic properties. Cafestol, a bioactive substance in coffee, increases glucose-stimulated insulin secretion in vitro and increases glucose uptake in human skeletal muscle cells. Cafestol possesses antidiabetic properties in KKAy mice. Consequently, cafestol may contribute to the reduced risk of developing T2D in coffee consumers and has a potential role as an antidiabetic drug.
Stevia is the common word to refer to the plant stevia rebaudiana which is the sweetest of the stevia species of plants and historically used as a sweetening agent. Several studies have suggested that in addition to their sweetness, steviosides and their related compounds, including rebaudioside A and isosteviol, may offer additional therapeutic benefits. These benefits include anti-hyperglycaemic, anti-hypertensive, anti-inflammatory, anti-tumor, anti-diarrheal, diuretic, and immunomodulatory actions. Isosteviol inhibits DNA polymerases and human DNA topoisomerase II. It also retards growth of three different types of human cancer cells and inhibits inflammation induced by TPA. Isosteviol had been in phase II clinical trials for the treatment of Type 2 diabetes mellitus.
Vindoline (VDL) is an indole alkaloid, possessing hypoglycemic and vasodilator effects, and it is also the prodrug of many vinca alkaloids. Vindoline as one of the alkaloids is highly present in young leaves and twigs of Catharanthus roseus, and oral administration of vindoline (100 mg/kg) had an acute hypoglycemic effect on rats. Vindoline acted as a Kv2.1 inhibitor able to reduce the voltage-dependent outward potassium currents finally enhancing insulin secretion. It protected β-cells from the cytokines-induced apoptosis following its inhibitory role in Kv2.1. Moreover, vindoline (20mg/kg) treatment significantly improved glucose homeostasis in db/db mice and STZ/HFD-induced type 2 diabetic rats, as reflected by its functions in increasing plasma insulin concentration, protecting the pancreatic β-cells from damage, decreasing fasting blood glucose and glycated hemoglobin (HbA1c), improving OGTT and reducing plasma triglyceride (TG).