Natural plant flavonoid apigenin directly disrupts Hsp90/Cdc37 complex and inhibits pancreatic cancer cell growth and migration

He, Jing; Ning, Changwen; Wang, Yu; Ma, Tianfang; Huang, He; Liu, Jingbo; Jiang, Yiqun

doi:10.1016/j.jff.2015.06.052

Cited by 29 publications

(14 citation statements)

References 40 publications

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“…In flavone group, apigenin and luteolin are the most studied PC. The apigenin showed anti-mutagenic and apoptotic effects in human lymphoma cells line [119] and inhibited pancreatic cancer cell growth and migration [120]. On the other hand, luteolin exhibited pro-apoptotic activities in colorectal cancer cells [121] and demonstrated anticancer effect on human lung carcinoma cell line (NCI-H460) through Sirt1-mediated apoptosis and the inhibition of cell migration [122].…”

Section: Chemical and Biological Issuesmentioning

confidence: 99%

Phenolic Compounds as Nutraceuticals or Functional Food Ingredients

Caleja

Ribeiro²,

Barreiro³

et al. 2017

CPD

102

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Section: Chemical and Biological Issuesmentioning

confidence: 99%

Phenolic Compounds as Nutraceuticals or Functional Food Ingredients

Caleja

Ribeiro²,

Barreiro³

et al. 2017

CPD

102

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“…Golongan terpenoid pada umumnya yang dapat melakukan penghambatan ini seperti Celastrol (Boridy, Le, Petrecca, & Maysinger, 2014;Klaić, Trippier, Mishra, Morimoto, & Silverman, 2011), Withaferin A (Yu et al, 2010), dan Cucurbitasin (Hall et al, 2015). Golongan flavon seperti Apigenin juga dapat bekerja melalui mekanisme ini (He et al, 2015;Iqbal et al, 2016). Degradasi protein klien adalah mekanisme yang belakangan ini diketahui dapat menghambat aktivitas HSP90.…”

Section: Inhibitor Hsp90unclassified

Kajian Heat Shock Protein 90 (HSP90) dalam Pencarian Kandidat Penghambatnya melalui Ekplorasi Bahan Alam Indonesia

Sitepu

2019

JFG

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Exploration on anticancer candidates on inhibition of Heat Shock Protein (HSP) activity are increasing in the past ten years. Some of HSP90 inhibitor candidates were in third phase of clinical trials. However, this issue is not followed by the emergency of HSP90 inhibitor research in Indonesia, not only study on natural source but also on synthetic candidates. This study aims to look the development of tracking HSP90 inhibitor candidates globally so that it can initiate the related research in Indonesia. Study of HSP90 and its inhibitors were taken from scientific articles in the range from 2009 to 2018. HSP90 and its inhibitors have important values in the dynamics of functions and stability of proteins to maintain survival of cells. This also include the oncogene proteins that involve in cell proliferation such as tyrosine kinases, transcription factors, and regulatory proteins that expression and interaction depend on HSP90. Expression of the transcription factor p53, Alk gene, Wnt gene, glucocorticoid receptors have also links with HSP90 protein activity. Some candidates for inhibitor of HSP90 have been entering clinical trials such as geldanamycin analogues, resorcinol derivatives, and purines analog. Candidates from natural sources that are also being developed such as luteolin, licochalcone A, oleochantal, novobiocin, epigallocathecin gallat, silybin, deguelin, and celastrol from terpenoid class, Apigenin from flavon class, Curcumin, and Gambogat Acid. HSP90 inhibitors which are entering the third phase of clinical trial are ganetespib from the resorcinol derivative and retaspimycin from geldanamisin analog group. Exploration of HSP90 inhibitors from Indonesia natural resources still have great potential to be developed because they have high impact values as anticancer candidates.

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“…Heat shock protein 90 (Hsp90) is an essential adenosine triphosphate (ATP) dependent molecular chaperone, and is abundantly expressed in eukaryotic cells [67,68]. Hsp90 plays an important role in various cellular processes, among which cell cycle control, cell survival and different signaling pathways can be cited [69].…”

Section: Cell Cycle Related Proteinsmentioning

confidence: 99%

“…Hsp90 plays an important role in various cellular processes, among which cell cycle control, cell survival and different signaling pathways can be cited [69]. Hsp90 overexpression has been related to tumor cells survival, in adverse conditions such as lack of nutrients, hypoxia and acidosis [68]. Hsp90 has also been related to tumor angiogenesis, and recent studies have suggested that Hsp90 inhibitors promote angiogenesis inhibition, by affecting the PI3K/Akt/eNOS (phosphoinositide 3-kinase/protein kinase B/endothelial nitric oxide) signal transduction pathway in endothelial cells, as well as through downregulation of VEGFR-2 expression [70].…”

Section: Cell Cycle Related Proteinsmentioning

confidence: 99%

“…In a study performed by Banerjee and Mandal [139], two colorectal cell lines (HT-29 and HCT-15), were treated with apigenin and the results showed antiproliferative and apoptotic effects, together with the increase of Apigenin Human multiple myeloma cells Inhibition of CK2 kinase activity and reduction of Cdc37 and Hsp90 phosphorylation [102] Human colorectal cancer cells Anti-proliferative and apoptotic effects Increase in p21 levels through a p53 independent pathway and inhibition of cyclins E expression due to large amounts of the active p21and activation of p16 down-regulated cyclin D1 [139] Human pancreatic cells Induction of cell apoptosis and inhibition of IKK-b-mediated NF-kB activation [140] Human pancreatic cancer cells Inhibition of the proliferation and migration through inhibition of HSP90/ Cdc37 interaction p21 levels and inhibition of cyclins E and D1. In pancreatic cells, different targets of apigenin were observed and this flavonoid was shown to interfere with cell proliferation, apoptosis and migration effects through different mechanism, including inhibition of IKK-b, NF-kB activation [140] and by HSP90/Cdc37 inhibition [68]. Finally, Guimarães et al [123] demonstrated, by using an enzymatic assay, that apigenin was able to inhibit VEGFR-2.…”

Section: Antiangiogenic Potential Of Phenolic Compoundsmentioning

confidence: 99%

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Antiangiogenic compounds: well-established drugs versus emerging natural molecules

et al. 2018

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a b s t r a c tAngiogenesis is the natural and physiologic process of growing blood vessels from pre-existing ones. Pathological angiogenesis occurs when the precise balance of all the molecular pathways that regulate angiogenesis is disrupted, and this process is a critical step in many diseases, including cancer. A limited number of antiangiogenic synthetic drugs have been developed. However, due to toxicity and side effects issues, the search for alternative to existing drugs is ongoing. In this sense, natural molecules obtained from plants or macrofungi, have demonstrated extraordinary potential in the treatment of angiogenesisrelated pathologies, specially taking into consideration its absence or very low toxicity, when compared to synthetic drugs. Using natural compounds as potential angiogenesis modulators is thus a promising field of research, supporting the creation of novel therapies able to reduce the use of drugs and associated side effects. In this review, the current status of antiangiogenic drugs and the wide variety of natural extracts and molecules with antiangiogenic capacities, as well as the angiogenesis molecular pathways and therapeutic targets, are presented. Finally, the challenges that need to be overcome in order to increase the use of natural compounds for clinical purposes are discussed.

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Natural plant flavonoid apigenin directly disrupts Hsp90/Cdc37 complex and inhibits pancreatic cancer cell growth and migration

Cited by 29 publications

References 40 publications

Phenolic Compounds as Nutraceuticals or Functional Food Ingredients

Phenolic Compounds as Nutraceuticals or Functional Food Ingredients

Kajian Heat Shock Protein 90 (HSP90) dalam Pencarian Kandidat Penghambatnya melalui Ekplorasi Bahan Alam Indonesia

Antiangiogenic compounds: well-established drugs versus emerging natural molecules

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