Brazilin inhibits activities of protein kinase C and insulin receptor serine kinase in rat liver

Kim, Seong‐Gon; Kim, You-Me; Khil, Lee-Yong; Jeon, Sun-Duck; So, Daeho; Moon, Chang-Hyun; Moon, Chang-Kiu

doi:10.1007/bf02974018

Cited by 31 publications

(16 citation statements)

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“…For example their antimicrobial activities against Salmonella typhosa, Staphylococcus aureus, Brucella suis, and Shigella flexneri have been described (Pratt and Yuzuriha, 1959). Brazilin is also known to inhibit enzymes such as NO synthase (Sasaki et al, 2007), xanthine oxidase (Nguyen et al, 2005), protein kinase C (Kim et al, 1998), and aldose reductase (Moon et al, 1985). Methyl gallate and gallic acid also showed good antimicrobial activity against Bacillus subtilis ATCC 9372 and Staphylococcus aureus MRSA ATCC 33591 (Kubo et al, 2003(Kubo et al, , 2004.…”

Section: Resultsmentioning

confidence: 99%

Antimicrobial compounds isolated from Haematoxylon brasiletto

Rivero-Cruz

2008

Journal of Ethnopharmacology

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Section: Resultsmentioning

confidence: 99%

Antimicrobial compounds isolated from Haematoxylon brasiletto

Rivero-Cruz

2008

Journal of Ethnopharmacology

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“…Brazilin is associated with enhancement of insulin receptor function by a decrease in serin phosphorylation. 17 Other studies have also reported that brazilin can stimulate glucose transport in vitro and decrease gluconeogenesis in hepatocytes isolated from diabetic rats. Brazilin is also reported to inhibit aldose reductase activity.…”

Section: Discussionmentioning

confidence: 96%

“…Based on research, it has been known that tannins inhibit enzymes. 17 Tannins give positive results in certain tests because of their reaction with enzyme proteins. Tannin is known to have specific properties to precipitate protein and non-specific inhibitory activity for some hydrolytic enzymes such as lipase, α-glucosidase, α-amylase and invertase.…”

Section: Discussionmentioning

confidence: 99%

“…Tannin is known to have specific properties to precipitate protein and non-specific inhibitory activity for some hydrolytic enzymes such as lipase, α-glucosidase, α-amylase and invertase. [17][18][19] DPP-IV enzyme is a class of protein, that can react and bind to tannin and form precipitate, so the enzyme activity decreases as a result of enzyme complexation. A study by Adamczyk et al found that tannin are more than just inhibitors, but rather modifiers of enzyme activity.…”

Section: Discussionmentioning

confidence: 99%

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The Antidiabetic Effectivity of Indonesian Plants Extracts via DPP-IV Inhibitory Mechanism

Setyaningsih¹,

Saputri²,

Mun’im³

2019

JYP

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Background: Nature provides a rich source of antidiabetic medicines. More than 1.200 plants have been reported to have anti-diabetic activities and more than half of the drugs on the market come from natural products. Therefore, research for developing new antidiabetic drugs from natural sources is necessary to properly evaluate various mechanism of action, efficacy and safety at toxicological, physiological, pharmacological and molecular levels before these drugs applied in treatment of diabetes. This study aims to examine and determine the highest activity of 10 ethanol extracts from Indonesian plants selected for in vitro inhibitory activity of dipeptidyl peptidase-IV (DPP-IV). Materials and Methods: This research studied DPP-IV inhibitory mechanism from 10 plant extract, namely Caesalpinia sappan, Cinchona officinalis, Elephantopus scaber, Foeniculum vulgare, Morus nigra, Muntingia calabura, Phyllanthus niruri, Psidium guajava, Rheum palmatum and Vernonia amygdalina using the spectrophotometric method and Sitagliptin as a positive control. The effectiveness of inhibition was assessed by percent inhibition. Tannin removal test was performed to exclude false-positive results. Results: The ethanolic extract of Caesalpinia sappan exhibited DPP-IV inhibitory activity greater than 80%, which was not markedly different from that of Sitagliptin at 85%. Brazilin, an active compound from Caesalpinia sappan gave the inhibition at greater than 78%. Tannin removal test for Caesalpinia sappan gave the inhibition at 74.16%. The High Performance Liquid Chromatography (HPLC) analysis result displayed that brazilin content on Caesalpinia sappan extract was 91.94%. Conclusion: Based on these results, Caesalpinia sappan ethanol extract has a potential effect as a better antidiabetic agent than other extracts used in this study.

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“…Brazilin is also used as a natural red pigment for histological staining [7]. Several studies have shown that the anti-hyperglycemic [8], anti-hepatotoxic [9], and anti-inflammatory effects of brazilin are caused by the inhibition of inducible nitric oxide synthase (NOS) in macrophage cells [10], and vasorelaxation induced by the activation of NOS in endothelial cells [4]. …”

Section: Introductionmentioning

confidence: 99%

Brazilin isolated from Caesalpinia sappan L. acts as a novel collagen receptor agonist in human platelets

Chang

Huang

et al. 2013

J Biomed Sci

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BackgroundBrazilin, isolated from the heartwood of Caesalpinia sappan L., has been shown to possess multiple pharmacological properties.MethodsIn this study, platelet aggregation, flow cytometry, immunoblotting analysis, and electron spin resonance (ESR) spectrometry were used to investigate the effects of brazilin on platelet activation ex vivo. Moreover, fluorescein sodium-induced platelet thrombi of mesenteric microvessels was also used in in vivo study.ResultsWe demonstrated that relatively low concentrations of brazilin (1 to 10 μM) potentiated platelet aggregation induced by collagen (0.1 μg/ml) in washed human platelets. Higher concentrations of brazilin (20 to 50 μM) directly triggered platelet aggregation. Brazilin-mediated platelet aggregation was slightly inhibited by ATP (an antagonist of ADP). It was not inhibited by yohimbine (an antagonist of epinephrine), by SCH79797 (an antagonist of thrombin protease-activated receptor [PAR] 1), or by tcY-NH2 (an antagonist of PAR 4). Brazilin did not significantly affect FITC-triflavin binding to the integrin αIIbβ3 in platelet suspensions. Pretreatment of the platelets with caffeic acid phenethyl ester (an antagonist of collagen receptors) or JAQ1 and Sam.G4 monoclonal antibodies raised against collagen receptor glycoprotein VI and integrin α2β1, respectively, abolished platelet aggregation stimulated by collagen or brazilin. The immunoblotting analysis showed that brazilin stimulated the phosphorylation of phospholipase C (PLC)γ2 and Lyn, which were significantly attenuated in the presence of JAQ1 and Sam.G4. In addition, brazilin did not significantly trigger hydroxyl radical formation in ESR analysis. An in vivo mouse study showed that brazilin treatment (2 and 4 mg/kg) significantly shortened the occlusion time for platelet plug formation in mesenteric venules.ConclusionTo the best of our knowledge, this study provides the first evidence that brazilin acts a novel collagen receptor agonist. Brazilin is a plant-based natural product, may offer therapeutic potential as intended anti-thrombotic agents for targeting of collagen receptors or to be used a useful tool for the study of detailed mechanisms in collagen receptors-mediated platelet activation.

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Brazilin inhibits activities of protein kinase C and insulin receptor serine kinase in rat liver

Cited by 31 publications

References 30 publications

Antimicrobial compounds isolated from Haematoxylon brasiletto

Antimicrobial compounds isolated from Haematoxylon brasiletto

The Antidiabetic Effectivity of Indonesian Plants Extracts via DPP-IV Inhibitory Mechanism

Brazilin isolated from Caesalpinia sappan L. acts as a novel collagen receptor agonist in human platelets

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