scholarly journals Inhibitory Effects of 4-(4-Methylbenzamino)benzoate on Adipocyte Differentiation

2015 ◽  
Vol 2015 ◽  
pp. 1-4
Author(s):  
Jin Taek Hwang ◽  
Sanghee Kim ◽  
Bo-ra Yoon ◽  
Inwook Choi ◽  
Sang Yoon Choi
Keyword(s):  
Fatty Acid ◽  
Glucose Metabolism ◽  
Fatty Acid Synthase ◽  
Adipocyte Differentiation ◽  
Ppar Gamma ◽  
Gamma Activity ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Concentration Dependent Manner ◽  
Cellular Expression

The potent suppression of adipocyte differentiation by 4-(4-methylbenzamino)benzoate was discovered during the search for new antiobesity compounds. 4-(4-methylbenzamino)benzoate was observed to suppress adipocyte differentiation in 3T3-L1 cells by 96.8% at 50 μM without cytotoxicity. In addition, 4-(4-methylbenzamino)benzoate reduced the cellular expression of fatty acid synthase in a concentration-dependent manner, as well as suppressing PPAR-gamma activity, which controls fatty acid storage and glucose metabolism. Based on these results, 4-(4-methylbenzamino)benzoate shows potential as an antiobesity material.

Methanol Extract of Mongolian Iris bungei Maxim. Stimulates 3T3-L1 Adipocyte Differentiation

2021 ◽  
Vol 21 (7) ◽  
pp. 3943-3949
Author(s):  
Jaegoo Yeon ◽  
Sung-Suk Suh ◽  
Ui-Joung Youn ◽  
Badamtsetseg Bazarragchaa ◽  
Ganbold Enebish ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Fatty Acid Synthase ◽  
Molecular Mechanisms ◽  
Adipocyte Differentiation ◽  
Methanol Extract ◽  
Regulatory Element ◽  
Peroxisome Proliferator ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Peroxisome Proliferator Activated Receptor

Iris bungei Maxim. (IB), which is native to China and Mongolia, is used as a traditional medicine for conditions such as inflammation, cancer, and bacterial infections. However, the effects of Iris bungei Maxim. on adipocyte differentiation have not been studied. In the present study, we first demonstrated the molecular mechanisms underlying the adipogenic activity of the methanol extract of Mongolian I. bungei Maxim. (IB). IB significantly enhanced intracellular lipid accumulation and adipocyte differentiation in 3T3-L1 preadipocytes in a concentration-dependent manner. Moreover, IB markedly stimulated the expression of genes related to adipogenesis such as peroxisome proliferator-activated receptor γ, adiponectin, and aP2. In addition, we also observed that IB induces lipogenic genes such as fatty acid synthase, sterol regulatory element binding protein 1c, stearoyl-CoA desaturase, and acetyl-CoA carboxylase. Interestingly IB regulated adipocyte differentiation in both the early and middle stages. Taken together, these adipogenic and lipogenic effects of IB suggest its efficacy for the prevention and/or treatment of type 2 diabetes.

scholarly journals The Glucose Sensor ChREBP Links De Novo Lipogenesis to PPARγ Activity and Adipocyte Differentiation

Endocrinology ◽  
2015 ◽  
Vol 156 (11) ◽  
pp. 4008-4019 ◽  
Author(s):  
Nicole Witte ◽  
Matthias Muenzner ◽  
Janita Rietscher ◽  
Miriam Knauer ◽  
Steffi Heidenreich ◽  
...  
Keyword(s):  
Adipose Tissue ◽  
Fatty Acid ◽  
Insulin Sensitivity ◽  
Fatty Acid Synthase ◽  
Adipocyte Differentiation ◽  
De Novo ◽  
Dominant Negative ◽  
De Novo Lipogenesis ◽  
Dependent Manner ◽  
Endogenous Fatty Acid

Reduced de novo lipogenesis in adipose tissue, often observed in obese individuals, is thought to contribute to insulin resistance. Besides trapping excess glucose and providing for triglycerides and energy storage, endogenously synthesized lipids can function as potent signaling molecules. Indeed, several specific lipids and their molecular targets that mediate insulin sensitivity have been recently identified. Here, we report that carbohydrate-response element-binding protein (ChREBP), a transcriptional inducer of glucose use and de novo lipogenesis, controls the activity of the adipogenic master regulator peroxisome proliferator-activated receptor (PPAR)γ. Expression of constitutive-active ChREBP in precursor cells activated endogenous PPARγ and promoted adipocyte differentiation. Intriguingly, ChREBP-constitutive-active ChREBP expression induced PPARγ activity in a fatty acid synthase-dependent manner and by trans-activating the PPARγ ligand-binding domain. Reducing endogenous ChREBP activity by either small interfering RNA-mediated depletion, exposure to low-glucose concentrations, or expressing a dominant-negative ChREBP impaired differentiation. In adipocytes, ChREBP regulated the expression of PPARγ target genes, in particular those involved in thermogenesis, similar to synthetic PPARγ ligands. In summary, our data suggest that ChREBP controls the generation of endogenous fatty acid species that activate PPARγ. Thus, increasing ChREBP activity in adipose tissue by therapeutic interventions may promote insulin sensitivity through PPARγ.

scholarly journals Inhibitory effects of garcinone E on fatty acid synthase

RSC Advances ◽  
2018 ◽  
Vol 8 (15) ◽  
pp. 8112-8117 ◽  
Author(s):  
Yan Liang ◽  
Di Luo ◽  
Xuan Gao ◽  
Hao Wu
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Synthase ◽  
Time Dependent ◽  
Inhibitory Effects ◽  
Irreversible Inhibition

Garcinone E exhibits both fast-binding reversible and time-dependent irreversible inhibition on the activity of fatty acid synthase.

scholarly journals Effect of ATP on preadipocyte migration and adipocyte differentiation by activating P2Y receptors in 3T3-L1 cells

2005 ◽  
Vol 393 (1) ◽  
pp. 171-180 ◽  
Author(s):  
Mariko Omatsu-Kanbe ◽  
Kazuko Inoue ◽  
Yusuke Fujii ◽  
Takefumi Yamamoto ◽  
Takahiro Isono ◽  
...  
Keyword(s):  
Cell Line ◽  
Adipocyte Differentiation ◽  
P2y Receptors ◽  
Extracellular Atp ◽  
Dependent Manner ◽  
Fat Cell ◽  
Proliferating Cells ◽  
Concentration Dependent Manner ◽  
Membrane Ruffling

The effect of extracellular ATP on adipogenesis was investigated using the mouse 3T3-L1 cell line. Incubation of cells with ATP (1–100 μM) for 5 min induced actin filament reorganization and membrane ruffling mediated through P2Y receptors. Enhancement of preadipocyte migration into fat cell clusters is one of the essential processes of adipose tissue development in vivo and cell migration assays revealed that stimulation of P2Y receptors enhanced chemokinesis (migration) in a concentration dependent manner. In this cell line, growth arrest is required before initiation of differentiation and growth-arrested post-confluent cells can be converted into adipocytes by the presence of the adipogenic hormones dexamethasone, 3-isobutyl-1-methylxanthine and insulin. On the other hand, those hormones alone do not trigger differentiation in proliferating cells. ATP did not induce differentiation when applied alone to either proliferating or postconfluent cells. By contrast, proliferating cells (density <50%) preincubated with ATP for 5 min and subsequently given the adipogenic hormones in the continued presence of ATP, underwent adipocyte differentiation mediated through phospholipase C-coupled P2Y receptors. These adipocytes were found to show very similar characteristics, including morphology and intracellular triacylglycerol accumulation compared with adipocytes differentiated from post-confluent preadipocytes with those adipogenic hormones. When proliferating cells were preincubated with ATP before the addition of the adipogenic hormones, gene expression of aP2 (adipose protein 2) was markedly increased within 6 days, whereas without ATP pretreatment the expression level stayed very low. These results suggest that extracellular ATP renders preadipocytes responsive to adipogenic hormones during the growth phase.

scholarly journals Twenty Traditional Algerian Plants Used in Diabetes Therapy as Strong Inhibitors of α-Amylase Activity

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Ihcen Khacheba ◽  
Amar Djeridane ◽  
Mohamed Yousfi
Keyword(s):  
Amylase Activity ◽  
Aluminium Chloride ◽  
Total Phenolic ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Concentration Dependent Manner ◽  
Diabetes Therapy ◽  
Methanolic Extracts ◽  
Phenolic Extract ◽  
Gallic Acid Equivalent

In the present work, we have studied the inhibitory effects of aqueous and alcoholic extracts of six Algerian medicinal plants known by their therapeutic virtues against diabetes. The total phenolic compounds content, assayed using Folin-Ciocalteu’s reagent, of the samples ranged from 0.183 mg/g to 43.088 mg/g and from 1.197 mg/g to 7.445 mg/g, expressed as gallic acid equivalent (GAE), for the, respectively, whereas the total flavonoids concentrations, detected using 2% of the aluminium chloride, ranged from 0.41 mg/g to 11.613 mg/g and from 0.0097 mg/g to 1.591 mg/g, expressed as rutin equivalents (RE), for the aqueous and methanolic extracts, respectively. The major plants were found to inhibit enzymatic activities of Aspergillus oryzae-amylase in a concentration dependent manner. The values of the inhibition constants (Ki) have been determined according to the Dixon and Lineweaver-Burk methods. The results showed that the Ki values were less than 55 ppm for the all extracts. A strong inhibition was found in the phenolic extract of Salvia officinalis with a Ki of 8 ppm.

Comparative Effects of Bupivacaine and Ropivacaine on Intracellular Calcium Transients and Tension in Ferret Ventricular Muscle

2004 ◽  
Vol 101 (4) ◽  
pp. 888-894 ◽  
Author(s):  
Yasushi Mio ◽  
Norio Fukuda ◽  
Yoichiro Kusakari ◽  
Yoshikiyo Amaki ◽  
Yasumasa Tanifuji ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Bay K 8644 ◽  
Clinical Settings ◽  
Ca Channel ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Concentration Dependent Manner ◽  
Intracellular Ca ◽  
Slope Difference ◽  
The Relationship

Background Recent evidence suggests that ropivacaine exerts markedly less cardiotoxicity compared with bupivacaine; however, the mechanisms are not fully understood at the molecular level. Methods Isolated ferret ventricular papillary muscles were microinjected with the Ca-binding photoprotein aequorin, and intracellular Ca transients and tension were simultaneously measured during twitch in the absence and presence of bupivacaine or ropivacaine. Results Bupivacaine and ropivacaine (10, 30, and 100 microm) reduced peak systolic [Ca]i and tension in a concentration-dependent manner. The effects were significantly greater for bupivacaine, particularly on tension (approximately twofold). The percentage reduction of tension was linearly correlated with that of [Ca]i for both anesthetics, with the slope of the relationship being approximately equal to 1.0 for ropivacaine and approximately equal to 1.3 for bupivacaine (slope difference, P &lt; 0.05), suggesting that the cardiodepressant effect of ropivacaine results predominantly from inhibition of Ca transients, whereas bupivacaine suppresses Ca transients and the reaction beyond Ca transients, i.e., myofibrillar activation, as well. BAY K 8644, a Ca channel opener, abolished the inhibitory effects of ropivacaine on Ca transients and tension, whereas BAY K 8644 only partially inhibited the effects of bupivacaine, particularly the effects on tension. Conclusion The cardiodepressant effect of bupivacaine is approximately twofold greater than that of ropivacaine. Bupivacaine suppresses Ca transients more markedly than does ropivacaine and reduces myofibrillar activation, which may at least in part underlie the greater inhibitory effect of bupivacaine on cardiac contractions. These results suggest that ropivacaine has a more favorable profile as a local anesthetic in the clinical settings.

Coexpression with β1-subunit modifies the kinetics and fatty acid block of hH1α Na+channels

2000 ◽  
Vol 279 (1) ◽  
pp. H35-H46 ◽  
Author(s):  
Yong-Fu Xiao ◽  
Sterling N. Wright ◽  
Ging Kuo Wang ◽  
James P. Morgan ◽  
Alexander Leaf
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Unsaturated Fatty Acids ◽  
Monounsaturated Fatty Acids ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Α Subunit ◽  
Dependent Inactivation ◽  
Voltage Dependent ◽  
Steady State Inactivation

Voltage-gated cardiac Na+ channels are composed of α- and β1-subunits. In this study β1-subunit was cotransfected with the α-subunit of the human cardiac Na+ channel (hH1α) in human embryonic kidney (HEK293t) cells. The effects of this coexpression on the kinetics and fatty acid-induced suppression of Na+currents were assessed. Current density was significantly greater in HEK293t cells coexpressing α- and β1-subunits ( I Na,αβ) than in HEK293t cells expressing α-subunit alone ( I Na,α). Compared with I Na,α, the voltage-dependent inactivation and activation of I Na,αβ were significantly shifted in the depolarizing direction. In addition, coexpression with β1-subunit prolonged the duration of recovery from inactivation. Eicosapentaenoic acid [EPA, C20:5(n–3)] significantly reduced I Na,αβ in a concentration-dependent manner and at 5 μM shifted the midpoint voltage of the steady-state inactivation by −22 ± 1 mV. EPA also significantly accelerated channel transition from the resting state to the inactivated state and prolonged the recovery time from inactivation. Docosahexaenoic acid [C22:6(n–3)], α-linolenic acid [C18:3(n–3)], and conjugated linoleic acid [C18:2(n–6)] at 5 μM significantly inhibited both I Na,αβ and I Na,α.In contrast, saturated and monounsaturated fatty acids had no effects on I Na,αβ. This finding differs from the results for I Na,α, which was significantly inhibited by both saturated and unsaturated fatty acids. Our data demonstrate that functional association of β1-subunit with hH1α modifies the kinetics and fatty acid block of the Na+ channel.

Inhibitory effects of sea buckthorn procyanidins on fatty acid synthase and MDA-MB-231 cells

Tumor Biology ◽  
2014 ◽  
Vol 35 (10) ◽  
pp. 9563-9569 ◽  
Author(s):  
Yi Wang ◽  
Fangyuan Nie ◽  
Jian Ouyang ◽  
Xiaoyan Wang ◽  
Xiaofeng Ma
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Synthase ◽  
Sea Buckthorn ◽  
Inhibitory Effects

scholarly journals Inhibitory effect of Sphagnum palustre extract and its bioactive compounds on aromatase activity

2016 ◽  
Vol 11 (3) ◽  
pp. 661
Author(s):  
Hee Jeong Eom ◽  
Yong Joo Park ◽  
Hee Rae Kang ◽  
Ha Ryong Kim ◽  
In Jae Bang ◽  
...  
Keyword(s):  
Video Clip ◽  
Inhibitory Effect ◽  
The Other ◽  
Aromatase Activity ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Aromatase Inhibition ◽  
Concentration Dependent Manner ◽  
Cardiac Pain ◽  
Sphagnum Palustre

<p><em>Sphagnum palustre</em> (a moss) has been traditionally used in Korea for the cure of several diseases such as cardiac pain and stroke. In this research, the inhibitory effect of <em>S. palustre</em> on aromatase (cytochrome P<sub>450</sub> 19, CYP19) activity was studied. [1β-<sup>3</sup>H] androstenedione was used as a substrate and incubated with <em>S. palustre</em> extract and recombinant human CYP19 in the presence of NADPH. <em>S. palustre</em> extract inhibited aromatase in a concentration-dependent manner (IC<sub>50</sub> value: 36.4 ± 8.1 µg/mL). To elucidate the major compounds responsible for the aromatase inhibitory effects of <em>S. palustre</em> extract, nine compounds were isolated from the extract and tested for their inhibition of aromatase activity. Compounds <strong>1</strong>, <strong>6</strong>, and <strong>7</strong> displayed aromatase inhibition, while the inhibition by the other compounds was negligible.</p><p><strong>Video Clip</strong></p><p><a href="https://youtube.com/v/n6xeo3RXJVY">Aromatase enzyme activity:</a> 4 min 16 sec  </p>

scholarly journals A bioorthogonal chemical reporter for fatty acid synthase-dependent protein acylation

2021 ◽  
Author(s):  
Krithika P. Karthigeyan ◽  
Lizhi Zhang ◽  
David R. Loiselle ◽  
Timothy A.J. Haystead ◽  
Menakshi Bhat ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Synthase ◽  
Matrix Protein ◽  
De Novo ◽  
Transmembrane Protein ◽  
Cellular Protein ◽  
Metabolic Labeling ◽  
Dependent Manner ◽  
Dependent Protein ◽  
Protein Acylation

Cells acquire fatty acids from dietary sources or via de novo palmitate production by fatty acid synthase (FASN). Although most cells express FASN at low levels, it is upregulated in cancers and during replication of many viruses. The precise role of FASN in disease pathogenesis is poorly understood, and whether de novo fatty acid synthesis contributes to host or viral protein acylation has been traditionally difficult to study. We describe a cell permeable, click-chemistry compatible alkynyl-acetate analog (Alk-4) that functions as a reporter of FASN-dependent protein acylation. In a FASN-dependent manner, Alk-4 selectively labeled the cellular protein interferon-induced transmembrane protein 3 (IFITM3) at its palmitoylation sites, and the HIV-1 matrix protein at its myristoylation site. Alk-4 metabolic labeling also enabled biotin-based purification and identification of more than 200 FASN-dependent acylated cellular proteins. Thus, Alk-4 is a useful bioorthogonal tool to selectively probe FASN-mediated protein acylation in normal and diseased states.

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