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Potential smoothened inhibitor from traditional Chinese medicine against the disease of diabetes, obesity, and cancer.
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Nowadays, obesity becomes a serious global problem, which can induce a series of diseases such as type 2 diabetes mellitus, cancer, cardiovascular disease, metabolic syndrome, and stoke. For the mechanisms of diseases, the hedgehog signaling pathway plays an important role in body patterning during
Metabolic Impact of Flavonoids Consumption in Obesity: From Central to Peripheral
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The prevention and treatment of obesity is primary based on the follow-up of a healthy lifestyle, which includes a healthy diet with an important presence of bioactive compounds such as polyphenols. For many years, the health benefits of polyphenols have been attributed to their anti-oxidant
Treatment with a constitutive androstane receptor ligand ameliorates the signs of preeclampsia in high-fat diet-induced obese pregnant mice.
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Constitutive androstane receptor (CAR) has been reported to decrease insulin resistance, while obesity and insulin resistance may also be involved in the pathogenesis of preeclampsia. We examined whether a CAR ligand, 1,4-bis(2-(3,5-dichloropyridyloxy)) benzene (TCPOBOP), can ameliorate the signs of
Toward a treatment of diabesity: Rational design, synthesis and biological evaluation of benzene-sulfonamide derivatives as a new class of PTP-1B inhibitors.
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Targeting of protein tyrosine phosphatase-1B (PTP1B) has emerged as a promising strategy for therapeutic intervention of diabetes and obesity. Investigation of new inhibitors with good bioavailability and high selectivity is the major challenge of drug discovery program targeting PTP1B. Therefore,
Cyp2b-Knockdown Mice Poorly Metabolize Corn Oil and Are Age-Dependent Obese.
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We previously made a RNAi-based cytochrome P450 2b (Cyp2b)-knockdown (Cyp2b-KD) mouse to determine the in vivo role of the Cyp2b subfamily in xenobiotic detoxification. Further studies reported here indicate a role for Cyp2b in unsaturated fatty-acid (UFA) metabolism and in turn obesity. Mice were
[The importance of liver changes in workers with chronic benzene exposure].
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Essential parameters of hepatic functioning in 84 labourers, whose exposition to benzene is differing in assimilation as well as length of time is discussed.--45 persons from the same county without contact to benzene or hepatotoxic agents served as control-group. Neither long-term exposure to
Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives.
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Among the 14 human isozymes of carbonic anhydrase (CA, EC 4.2.1.1) presently known, the cytosolic hCA II is the most active and plays a host of physiological functions, whereas the mitochondrial hCA V is unique due to its role in several biosynthetic reactions. An inhibition study of these isozymes
A Novel Inhibitor of the Obesity-Related Protein FTO.
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Fe(II) and α-ketoglutarate-dependent fat mass and obesity associated protein (FTO)-dependent demethylation of m⁶A is important for regulation of mRNA splicing and adipogenesis. Developing FTO-specific inhibitors can help probe the biology of FTO and unravel novel therapeutic targets for treatment of
Obesity Promotes Experimental Colitis by Increasing Oxidative Stress and Mitochondrial Dysfunction in the Colon
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Although obesity is associated with inflammatory bowel disease (IBD), the underlying molecular mechanism still remains unclear. In this study, we evaluated the effects of high-fat diet (HFD)-induced obesity on the development of experimental colitis in mice. The C57BL/6 mice were fed with a HFD for
The constitutive androstane receptor is an anti-obesity nuclear receptor that improves insulin sensitivity.
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Obesity and type 2 diabetes are related metabolic disorders of high prevalence. The constitutive androstane receptor (CAR) was initially characterized as a xenobiotic receptor regulating the responses of mammals to xenotoxicants. In this study, we have uncovered an unexpected role of CAR in
Risk of ischemic heart disease among primary aluminum production workers.
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The risk of ischemic heart disease (IHD) has been studied in relation to working conditions encountered in a primary aluminum smelter employing over 6,000 men. During the period 1975-1983, 306 new cases of IHD were identified which were matched with 575 referents. A logistic regression analysis was
Studies on antidiabetic agents. 11. Novel thiazolidinedione derivatives as potent hypoglycemic and hypolipidemic agents.
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In the course of further chemical modification of the novel antidiabetic pioglitazone (AD-4833, U-72,107), a series of 5-[4-(2- or 4-azolylalkoxy)benzyl- or -benzylidene]-2,4-thiazolidinediones was prepared and evaluated for hypoglycemic and hypolipidemic activities in insulin-resistant, genetically
Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies.
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The combination of antagonism at histamine H(3) receptor and the stimulation of insulin secretion have been proposed as an approach to new dual therapeutic agents for the treatment of type 2 diabetes mellitus associated with obesity. We have designed and synthesized a new series of non-imidazole
Health risk in transport workers. Part II. Dietary compounds as modulators of occupational exposure to chemicals.
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Professional drivers are exposed to a number of factors that have a negative influence on their health status. These include vibrations, noise, the lack of fresh air in the car cabin, shift work (frequently at night), monotony resulting from permanent repetition of certain actions, static loads due
Design and Synthesis of Peroxisome Proliferator-activated Receptor (PPAR) Gamma Antagonists Based on the Principle of Operation of Nuclear Receptor I.
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Peroxisome proliferator-activated receptor γ (PPARγ) antagonist is a molecular target to create drug for the treatment of not only type 2 diabetes and obesity, but also cancer. However, few rational drug design strategies and concepts are available. Here, we utilized the nuclear receptor
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