New Hedgehog/GLI signaling inhibitors from Excoecaria agallocha

Rifai, Yusnita; Arai, Midori A.; Sadhu, Samir Kumar; Ahmed, Firoj; Ishibashi, Masami

doi:10.1016/j.bmcl.2010.11.126

Cited by 43 publications

(25 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…39) Potent inhibitors were isolated from Acacia pennata, 40) Adenium obesum 41) and Excoecaria agallocha. 42 We recently found a new type of Hh inhibitor from Excoecaria agallocha. 42) A new flavonoid glycoside 20 inhibits Hh signaling by arresting the translocation of GLI into the nucleus of PANC1.…”

Section: Discovery Of Hh Signaling Inhibitors From Natural Productsmentioning

confidence: 99%

See 1 more Smart Citation

Approaches to Neural Stem Cells and Cancer Cells Based on Natural Products

Arai

2011

CHEMICAL & PHARMACEUTICAL BULLETIN

Self Cite

View full text Add to dashboard Cite

We have developed "protein-and cell-based screen methods" for the isolation of new natural products. By using VDR (vitamin D receptor) immobilized magnetic beads, two new natural products were isolated rapidly. To find inhibitors of Hes1 protein, which is one of the important transcriptional factors in neural stem cells, a Hes1 dimer plate assay was developed, and then first Hes1 dimer inhibitors were found from our natural products library. As a "cell-based screen method," a reporter gene assay for screening Hh (hedgehog) signaling inhibitors was constructed. New Hh signaling inhibitors were isolated from our natural extracts library. We evaluated their Hh inhibitory activity in Hh related protein synthesis and cytotoxicity against cancers, in which Hh signaling is aberrantly activated. In addition to the naturally made compounds library (extracts library), "small molecules based on natural products" were synthesized. The total synthesis of Melleumin A, B, which were isolated by our group, was achieved. From their synthetic derivatives, inhibitors of the Wnt signal, which has been reported to cause colon cancers, were discovered. Moreover, flavanone and chromone were selected as natural product scaffolds. Many flavonoids and chromones with diverse heterocyclic units were constructed using our efficient synthetic method.

show abstract

Section: Discovery Of Hh Signaling Inhibitors From Natural Productsmentioning

confidence: 99%

“…42 We recently found a new type of Hh inhibitor from Excoecaria agallocha. 42) A new flavonoid glycoside 20 inhibits Hh signaling by arresting the translocation of GLI into the nucleus of PANC1. Moreover, it was revealed that this inhibition was not affected by SMO.…”

Section: Discovery Of Hh Signaling Inhibitors From Natural Productsmentioning

confidence: 99%

Approaches to Neural Stem Cells and Cancer Cells Based on Natural Products

Arai

2011

CHEMICAL & PHARMACEUTICAL BULLETIN

Self Cite

View full text Add to dashboard Cite

show abstract

“…It could be used as purgative and emetic and also be used for curing rheumatism, dermatitis and conjunctivitis 7 . The potent anti-HIV, 8 anticancer, 9,8 and antimicrobial 7,10 effects of the various extracts are also reported. The wound healing properties of the latex of E. agallocha were extensively studied using an animal model and in man.…”

mentioning

confidence: 90%

Untitled

2014

IJPSR

View full text Add to dashboard Cite

Purpose: The focus of the present paper was a preliminary phytochemical and TLC analysis of the various extracts (root, stem and leaf) of the mangrove plant Excoecaria agallocha L. Methods: Phytochemical analysis was carried out using the standard phytochemical assays. TLC analysis of the petroleum ether and chloroform fraction of the leaves was carried out using the solvent system Toluene: Ethyl acetate (in 9:1 ratio) and Toluene: Ethyl acetate: Formic acid (in 5:5:0.2 ratio) for PE and chloroform fractions respectively. Result and conclusion: The results of the preliminary phytochemical screening revealed the presence of various chemical compounds like alkaloids, glycosides, flavonoids, carbohydrates, anthraquinone, tannins, phenols, terpenoids, fixed oil and fats. Organoleptic study revealed the specific nature of the plant parts used in the study. The behavior of the powdered plant parts in presence of various chemicals was studied. TLC analysis of the petroleum ether and chloroform fraction of the leaves of Excoecaria agallocha L. revealed bands indicating the presence of various compounds that could act as potential antimicrobial agents.

show abstract

“…Searching for bioactive natural products targeting Hh/ GLI signaling thus may promote an effective anticancer-strategy. We identified several Hh/GLI-mediated transcriptional inhibitors from plants [3][4][5][6] including 3' ,6-dimethoxy-3'' ,4''-(methylenedioxy)-2,5-epoxylignan-4'-ol (DMEO) which was isolated from Piper nigrum [7]. We have previously adapted the concept of nano magnetic beads to the fast isolation of GLI inhibitory compounds, using GLI-GST culture which was immobilized on the beads and plant extracts [8].…”

Section: Introductionmentioning

confidence: 99%

3’,6-Dimethoxy-3’’,4’’-Methylenedioxy-2,5-Epoxylignan-4’-ol Inhibited Glioma-Associated Oncogene

Rifai¹,

Arai²,

Ishibashi³

2014

J Biomol Res Ther

View full text Add to dashboard Cite

Aberrant activation of Hedgehog (Hh) signaling pathway has been linked to the development of cancers. A naturally occurring Hedgehog inhibitor, 3',6-dimethoxy-3'',4''-(methylenedioxy)-2,5-epoxylignan-4'-ol (DMEO), isolated from Piper nigrum, exhibited selective cytotoxicity against human pancreatic (PANC1) with no toxic effect on normal cells. This compound blocked the translocation of GLI transcription factors into the nucleus in PANC1. RNA interferences of the Smoothened (Smo) function in PANC1 treated with the compound downregulated the mRNA expression of Ptch.

show abstract

New Hedgehog/GLI signaling inhibitors from Excoecaria agallocha

Cited by 43 publications

References 32 publications

Approaches to Neural Stem Cells and Cancer Cells Based on Natural Products

Approaches to Neural Stem Cells and Cancer Cells Based on Natural Products

Untitled

3’,6-Dimethoxy-3’’,4’’-Methylenedioxy-2,5-Epoxylignan-4’-ol Inhibited Glioma-Associated Oncogene

Contact Info

Product

Resources

About