Biochanin-A, an isoflavon, showed anti-proliferative and anti-inflammatory activities through the inhibition of iNOS expression, p38-MAPK and ATF-2 phosphorylation and blocking NFκB nuclear translocation

Kole, Labanyamoy; Giri, Biplab; Manna, Sunil K.; Pal, Biswajit; Ghosh, Sudipta

doi:10.1016/j.ejphar.2010.11.026

Cited by 141 publications

(113 citation statements)

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“…PKC-α, HO-1 release and inhibition of LPS mediated p38 MAPK phosphorylation with its specificity towards cancer cell growth inhibition, indicates the association between antiproliferative and anti-inflammatory actions of Biochanin-A [73]. Parthenolide is also working as an anti-inflammatory and anti-tumorogenic agent in similar manner to that of Biochanin-A.…”

Section: Inflammatory Moleculesmentioning

confidence: 89%

Anti-inflammatory and Anti-tumor Activities of Parthenolide: An Update

Dey¹,

Sarkar²,

Giri³

2016

J Chem Biol Ther

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Parthenolide (PTL), the secondary metabolite of feverfew plant (Tanaceum parthenium), has been used in various medical purposes globally. Inflammation represents a physiological response to injury and helps to restore tissue homeostasis. Inflammation and cancer both are associated with genotoxicity, invasion, metastasis, and abnormal tissue repair mechanisms. PTL inhibit major cellular inflammatory and proliferation pathways like NFκB, STAT3, and MAPK along with the activity and expression of several inflammatory mediators including COX. NFκB pathway plays a key role in controlling cell cycle progression and apoptosis together with metastasis and cancer of various types. Elevated NFκB, Wnt/β-catenin pathways are crucial factors of tumorogenesis. PTL inhibits NFκB and Wnt/β-catenin pathways, and thereby promotes apoptosis and suppresses cell proliferation. Experimental data showed that PTL protects normal cells from apoptosis; whereas in cancer cells it induces apoptotic cell death. Hence, parthenolide could be useful in controlling inflammatory diseases alone or together with tumorogenesis due to its evident anticancer potency and anti-inflammatory nature.

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Section: Inflammatory Moleculesmentioning

confidence: 89%

Anti-inflammatory and Anti-tumor Activities of Parthenolide: An Update

Dey¹,

Sarkar²,

Giri³

2016

J Chem Biol Ther

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“…In vivo, intraperitoneally injected genistein was shown to protect rats from endotoxin-induced organ failure (4), and genistein was also found to reduce the degree of inflammation and joint destruction in collagen-induced arthritic mice (5). However, little is known regarding the anti-inflammatory property of biochanin A other than that it was reported to inhibit TNFα and IL-6 production in LPS-induced RAW264.7 cells (2,6).…”

Section: Introductionmentioning

confidence: 99%

“…The antioxidant and radical scavenging activities (7,8), the inhibition of COX-2 expression (9), the modulation of MAPK expression (10) and the modulation of NF-κB expression (11,12) were all implicated in the anti-inflammatory action of genistein. However, little was known regarding the mechanism behind the anti-inflammatory action of biochanin A until it was recently reported to block the activation of NF-κB (6).…”

Section: Introductionmentioning

confidence: 99%

“…LPS-stimulated macrophages were used to study the anti-inflammatory activity of isoflavones. RAW 264.7 cells were seeded at a density of 1x10 6 cells/well in 6-well plates. After 24 h, test substances in less than 0.1% dimethyl sulfoxide (DMSO) solution were added to the culture medium, and cells were incubated for another 3 h. LPS was added at a final concentration of 1 µg/ ml, and cells were incubated for another 24 h. The cells were then centrifuged at 1,000 rpm, the supernatant was aliquoted and samples were stored at -20˚C until cytokines were measured.…”

Section: Introductionmentioning

confidence: 99%

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Biochaninï¿½A ameliorates the cytokine secretion profile of lipopolysaccharide-stimulated macrophages by a PPARγ-dependent pathway

Qiu

Lin

et al. 2011

Mol Med Report

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Abstract. The role of peroxisome proliferator-activated receptors (PPARs) as anti-inflammatory mediators has been established, and the fact that some isoflavones are dual agonists of PPARα/γ indicates the involvement of PPARα and/or PPARγ in the anti-inflammatory action of certain isoflavones. However, the dependency of isoflavones on PPARs in their anti-inflammatory action has not been demonstrated. Here, we report the dependency of an isoflavone biochanin A and the independency of another isoflavone genistein in relation to PPARγ to ameliorate the cytokine secretion profile of lipopolysaccharide (LPS)-stimulated mouse RAW264.7 macrophages. A total amount of 10 µmol/l of biochanin A or genistein significantly suppressed the secretion of tumor necrosis factor α (TNFα) and interleukin-6 (IL-6) in LPS-induced RAW264.7 cells, whereas another two isoflavones, formononectin and daidzein, only significantly suppressed the secretion of IL-6. Their antiinflammatory efficiencies were not in correspondence with their PPARα/γ agonist activities. Inhibition of PPARγ activity by its antagonist GW9662 significantly reversed the antiinflammatory effect of biochanin A but not genistein, which demonstrated the dependency of biochanin A and the independency of genistein on PPARγ in their anti-inflammatory actions. Meanwhile, the PPARγ-dependency of biochanin A was further confirmed by the result that the suppression of LPS-induced NF-κB activation by biochanin A was reversed following GW9662 co-treatment. Moreover, inhibition of PPARα activity by its antagonist MK886 did not significantly reverse the anti-inflammatory effects of biochanin A and genistein, indicating that their anti-inflammatory properties were PPARα-independent.

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“…Pharmacological studies have demonstrated that BCA possesses remarkable biological activities such as antioxidant, anti-inflammatory and antihyperglycemic effects (Kole et al, 2011;Yoon et al, 2011;Harini et al, 2012). In addition, BCA has been widely used as dietary supplement for treating premenstrual syndrome, lowering the cholesterol, improving urine production and preventing osteoporosis (Howes et al, 2000;Atkinson et al, 2004;Chedeaui et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Nanostructured lipid carriers as a delivery system of biochanin A

Wang¹,

Cheng²,

Zhou³

et al. 2013

Drug Delivery

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The aim of this study was to explore the nanostructured lipid carriers as a delivery system of biochanin A so as to supply a method to improve its bioavailability. Biochanin A-loaded nanostructured lipid carriers (BCA-NLCs) were prepared by the method of emulsionevaporation and low temperature solidification. Pharmacokinetics was carried out in rats upon oral administration at a dose of 10 mg/kg. BCA-NLC showed spherical formulation and had mean diameter174.68 AE 0.96 nm, zeta potential À20.9 AE 0.8 mv and entrapment efficiency 97.36 AE 0.14%. DSC and XRD studies indicated that BCA was not in crystal state in NLC. In in vitro release study, the BCA from BCA-NLC exhibited a biphasic release pattern with burst release initially and sustained release afterwards. BCA-NLC showed higher AUC value and circulated in blood for a longer time than BCA suspension. The studies demonstrated that NLC could be a potential delivery system for BCA to improve bioavailability.

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Biochanin-A, an isoflavon, showed anti-proliferative and anti-inflammatory activities through the inhibition of iNOS expression, p38-MAPK and ATF-2 phosphorylation and blocking NFκB nuclear translocation

Cited by 141 publications

References 50 publications

Anti-inflammatory and Anti-tumor Activities of Parthenolide: An Update

Anti-inflammatory and Anti-tumor Activities of Parthenolide: An Update

Biochaninï¿½A ameliorates the cytokine secretion profile of lipopolysaccharide-stimulated macrophages by a PPARγ-dependent pathway

Nanostructured lipid carriers as a delivery system of biochanin A

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