Anacardic acid (6-nonadecyl salicylic acid), an inhibitor of histone acetyltransferase, suppresses expression of nuclear factor-κB–regulated gene products involved in cell survival, proliferation, invasion, and inflammation through inhibition of the inhibitory subunit of nuclear factor-κBα kinase, leading to potentiation of apoptosis

Sung, Bokyung; Pandey, Manoj K.; Ahn, Kwang Seok; Yi, Tongxun; Chaturvedi, Madan M.; Liu, Mingyao; Aggarwal, Bharat B.

doi:10.1182/blood-2007-10-117994

Cited by 230 publications

(170 citation statements)

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“…AA, a natural plant extracts, is considered to be a promising anti-tumor drug with acceptable toxicity and high anti-tumor spectrum. AA inhibits the proliferation of tumor cells in pituitary adenoma (7), breast cancer (15), pulmonary adenocarcinoma, and oral squamous cell carcinoma (24). In our study, the antiproliferation effect of AA on Lncap cells was obvious.…”

Section: Discussionsupporting

confidence: 50%

“…In addition, AA can remarkably suppress the activity of IkBa kinase (24). With varying chain length, AA induces AA works as an inhibitor of p300, a general transcriptional coactivator and important acetyltransferase (25).…”

Section: Discussionmentioning

confidence: 99%

“…It has been widely recosnized as a non-specific histone acetyltransferase inhibitor of p300 (6). Meanwhile, it has shown certain antitumor activities (7,8) by inhibiting histone acetyltransferase (9)(10)(11)(12)(13) and transcriptional factor nuclear factor-κB (14) in cell and animal models. In addition, it may efficiently inhibit the proliferation of breast carcinoma cells (15).…”

Section: Introductionmentioning

confidence: 99%

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Anacardic acid (6-pentadecylsalicylic acid) induces apoptosis of prostate cancer cells through inhibition of androgen receptor and activation of p53 signaling

Jing¹,

Tan²,

Binghai³

et al. 2012

Chin. J. Cancer Res.

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Anacardic acid (AA) is a mixture of 2-hydroxy-6-alkylbenzoic acid homologs. It is widely regarded as a non-specific histone acetyltransferase inhibitor of p300. The effects and the mechanisms of AA in LNCaP cells (prostate cancer cells) remain unknown. To investigate the effect of AA on LNCaP cells, we had carried out several experiments and found that AA inhibits LNCaP cell proliferation, induces G1/S cell cycle arrest and apoptosis of LNCaP cell. The mechanisms via which AA acts on LNCaP cells may be due to the following aspects. First, AA can regulate p300 transcription and protein level except for its mechanisms regulating function of p300 through post-translational modification in LNCaP cells. Second, AA can activate p53 through increasing the phosphorylation of p53 on Ser15 in LNCaP cells. AA can selectively activate p21 (target genes of p53). Third, AA can down-regulates androgen receptor (AR) through supressing p300. Our study suggests that AA has multiple anti-tumor activities in LNCaP cells and warrants further investigation. Chin J Cancer Res 2012;24(4):275-283 www.thecjcr.org culture medium when necessary. DMEM, growth factorreduced matrigel and fetalbovine serum (FBS) were bought from BD Corporation (San Jose, CA). The Lipofectamine™ 2000 and the Total RNA Extraction kit were purchased from Invitrogen (Carlsbad, CA). The MTT Cell Proliferation and Cytotoxicity Assay kit and the Annexin V-FITC & PI Apoptosis Detection kit were purchased from KeyGen Biotech (Nanjing, China). SYBR Green PCR Master Mix were purchased from Fermentas (Burlington, Ontario, Canada). The Total Protein Extraction kit was purchased from ProMab (Changsha, China). Primary antibodies for p300, p21, p53, AR, cyclin D1 and siRNA specifically for p300 were bought from Santa Cruz Biotechnology (Santa Cruz, CA). Primary antibody for phospho-p53 (Ser 15) was purchased from Cell Signaling Technology. RPMI 1640 was purchased from GIBCO. Cell lines and cell cultureLNCaP was purchased from Yinrun (Changsha, China). LNCaP is a classical metastatic prostate adenocarcinoma cell line, derived from metastatic lymph nodes. LNCaP was cultured with both RPMI 1640 and 10% FBS, and subcultured weekly (37 ℃, 5% CO 2 ). p300 siRNA transfectionT h e L n c a p c e l l s w e r e s e e d e d i n t o 6 -w e l l p l a t e s (4×10 4 -5×10 4 cells/well) and cultured in 2 mL basic culture medium containing 10% FBS overnight until the cells were 70% confluent. Cells were transiently transfected with a validated scrambled control siRNA, or p300 siRNA by using InterferinTM transfection reagent. The mixture of siRNA and InterferinTM transfection reagent was incubated for 10 min, added to each well of the 6-well plates and incubated at 37 ℃ for 24 h before drug treatment. Detecting the inhibition of cell growth using MTT assaysLncap cells were treated with AA or transfected with p300 siRNA before drug treatment. Cells were incubated at various concentrations (0, 5, 25, and 125 μmol/L) at a series of time points (0, 4, 24 and 28 h). Then, 5 mg/mL of MTT so...

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Section: Discussionsupporting

confidence: 50%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Anacardic acid (6-pentadecylsalicylic acid) induces apoptosis of prostate cancer cells through inhibition of androgen receptor and activation of p53 signaling

Jing¹,

Tan²,

Binghai³

et al. 2012

Chin. J. Cancer Res.

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“…Cyclin D1 belongs to important Cyclin, mainly promoting cycle progression from G0 into G1 phase, increasing the cell percentage in mitotic phase. In addition, the activated NF-κB /p65 also regulates antiapoptotic gene expressions including Bcl-2, Bcl-xl (Sung et al, 2008). NF-κB is indispensable for ER recruitment to ERE of antiapoptotic gene promoter (Pradhan et al, 2012).…”

Section: Discussionmentioning

confidence: 99%

“…Estrogen receptor coactivator, p300/CBP ( (cAMP-responsive element binding protein)-binding protein) may be important for estrogen mediating the acetylation of NF-κB. Acetylation of NF-κB/p65 at discrete sites regulates distinct nuclear functions of NF-κB, and acetylation of lysine 310 is required for enhanced transactivation potential of NF-κB/ p65 (Chen et al, 2002), promoting relevant target genes expression (Sung et al, 2008). There may be a critical relationship between the protein expression of CyclinD1, Bcl-2, Bcl-xl and the enhanced acetylation of lysine 310 of NF-κB/p65.…”

Section: Introductionmentioning

confidence: 99%

Garcinol, an Acetyltransferase Inhibitor, Suppresses Proliferation of Breast Cancer Cell Line MCF-7 Promoted by 17β-Estradiol

Xia¹,

Liu²,

Zhang³

et al. 2014

Asian Pacific Journal of Cancer Prevention

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The acetyltransferase inhibitor garcinol, a polyisoprenylated benzophenone, is extracted from the rind of the fruit of Garcinia indica, a plant found extensively in tropical regions. Anti-cancer activity has been suggested but there is no report on its action via inhibiting acetylation against cell proliferation, cell cycle progression, and apoptosis-inhibtion induced by estradiol (E 2 ) in human breast cancer MCF-7 cells. The main purposes of this study were to investigate the effects of the acetyltransferase inhibitor garcinol on cell proliferation, cell cycle progression and apoptosis inhibition in human breast cancer MCF-7 cells treated with estrogen, and to explore the significance of changes in acetylation levels in this process. We used a variety of techniques such as CCK-8 analysis of cell proliferation, FCM analysis of cell cycling and apoptosis, immunofluorescence analysis of NF-κB/ p65 localization, and RT-PCR and Western blotting analysis of ac-H3, ac-H4, ac-p65, cyclin D1, Bcl-2 and Bclxl. We found that on treatment with garcinol in MCF-7 cells, E 2 -induced proliferation was inhibited, cell cycle progression was arrested at G0/G1 phase, and the cell apoptosis rate was increased. Expression of ac-H3, ac-H4 and NF-κB/ac-p65 proteins in E 2 -treated MCF-7 cells was increased, this being inhibited by garcinol but not ac-H4.The nuclear translocation of NF-κB/p65 in E 2 -treated MCF-7 cells was also inhibited, along with cyclin D1, Bcl-2 and Bcl-xl in mRNA and protein expression levels. These results suggest that the effect of E 2 on promoting proliferation and inhibiting apoptosis is linked to hyperacetylation levels of histones and nonhistone NF-κB/ p65 in MCF-7 cells. The acetyltransferase inhibitor garcinol plays an inhibitive role in MCF-7 cell proliferation promoted by E 2 . Mechanisms are probably associated with decreasing ac-p65 protein expression level in the NF-κB pathway, thus down-regulating the expression of cyclin D1, Bcl-2 and Bcl-xl.

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Biological and Biomedical Aspects of Metal Phenolates

Ming

2014

Patai's Chemistry of Functional Groups

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The phenol functionality is involved in diverse biological processes and functions, serving as a proton donor and as a metal‐binding ligand. It is commonly found in many biochemicals (such as siderophores and the amino acids tyrosine and tryptophan), pharmaceuticals (including antibiotics, metal‐chelating agents, and diagnostic agents), and natural products (such as polyphenols, flavonoids, and salicylic acid). In association with other functional groups, the phenol moiety forms various types of metal‐binding sites of diverse structures and functions, for example, for iron binding and transport, in enzymes for oxygenation of substrates, and for biotransformation of aromatic compounds. Many environmentally hazardous aromatic compounds such as bisphenol A, PCB, and DDT can be degraded by tyrosinate(phenolate)‐containing metalloenzymes from microorganisms, which provides a clue for bioremediation of these toxic substances. Moreover, the phenol‐containing wet‐adhesive byssal proteins from some clams and mussels has stimulated further development of adhesive materials for medical and other applications; and the study of binding of transferrin with nanoparticles affords better understanding of protein–mineral interfacial interactions. In addition to these naturally occurring metal‐phenolate centers, there are many metal complexes of phenol and derivatives that exhibit various catalytic activities and serve as structural and/or functional model systems for tyrosinate‐containing metalloproteins.

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Cited by 230 publications

References 57 publications

Anacardic acid (6-pentadecylsalicylic acid) induces apoptosis of prostate cancer cells through inhibition of androgen receptor and activation of p53 signaling

Anacardic acid (6-pentadecylsalicylic acid) induces apoptosis of prostate cancer cells through inhibition of androgen receptor and activation of p53 signaling

Garcinol, an Acetyltransferase Inhibitor, Suppresses Proliferation of Breast Cancer Cell Line MCF-7 Promoted by 17β-Estradiol

Biological and Biomedical Aspects of Metal Phenolates

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