Deguelin - CAS 522-17-8
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Not Intended for Therapeutic Use. For research use only.
Deguelin is a naturally occurring rotenoid, is known to be an Akt inhibitor and to have an anti-tumor effect on several cancers.
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1.Deguelin Analogue SH-1242 Inhibits Hsp90 Activity and Exerts Potent Anticancer Efficacy with Limited Neurotoxicity.
Lee SC1, Min HY1, Choi H2, Bae SY1, Park KH1, Hyun SY1, Lee HJ1, Moon J1, Park SH1, Kim JY3, An H1, Park SJ4, Seo JH2, Lee S1, Kim YM5, Park HJ4, Lee SK1, Lee J1, Lee J1, Kim KW6, Suh YG1, Lee HY7. Cancer Res. 2016 Feb 1;76(3):686-99. doi: 10.1158/0008-5472.CAN-15-1492. Epub 2015 Dec 8.
The Hsp90 facilitates proper folding of signaling proteins associated with cancer progression, gaining attention as a target for therapeutic intervention. The natural rotenoid deguelin was identified as an Hsp90 inhibitor, but concerns about neurotoxicity have limited prospects for clinical development. In this study, we report progress on deguelin analogues that address this limitation, focusing on the novel analogue SH-1242 as a candidate to broadly target human lung cancer cells, including those that are chemoresistant or harboring KRAS mutations. In a KRAS-driven mouse model of lung cancer, SH-1242 administration reduced tumor multiplicity, volume, and load. Similarly, in human cell line-based or patient-derived tumor xenograft models, SH-1242 induced apoptosis and reduced tumor vasculature in the absence of detectable toxicity. In contrast to deguelin, SH-1242 toxicity was greatly reduced in normal cells and when administered to rats did not produce obvious histopathologic features in the brain.
2.BAD, a Proapoptotic Protein, Escapes ERK/RSK Phosphorylation in Deguelin and siRNA-Treated HeLa Cells.
Hafeez S1, Urooj M1, Saleem S1, Gillani Z1, Shaheen S1, Qazi MH1, Naseer MI2, Iqbal Z3, Ansari SA2, Haque A4, Asif M5, Mir MA6, Ali A4, Pushparaj PN2, Jamal MS4, Rasool M2. PLoS One. 2016 Jan 8;11(1):e0145780. doi: 10.1371/journal.pone.0145780. eCollection 2016.
This study has been undertaken to explore the therapeutic effects of deguelin and specific siRNAs in HeLa cells. The data provided clearly show the silencing of ERK 1/2 with siRNAs and inhibition of ERK1/2 with deguelin treatment in HeLa cells. Additionally, we are providing information that deguelin binds directly to anti-apoptotic Bcl-2, Bcl-xl and Mcl-1 in the hydrophobic grooves, thereby releasing BAD and BAX from dimerization with these proteins. This results in increased apoptotic activity through the intrinsic pathway involved in rupture of mitochondrial membrane and release of cytochrome C. Evidence for inhibition of ERK1/2 by deguelin and escape of BAD phosphorylation at serine 112 through ERK/RSK pathway has been further fortified by obtaining similar results by silencing ERK 1/2 each with specific siRNAs. Increase in BAD after treatment with deguelin or siRNAs has been interpreted to mean that deguelin acts through several alternative pathways and therefore can be used as effective therapeutic agent.
3.Alkyne Carbonyl Metathesis As a Means To Make 4-Acyl Chromenes: Syntheses of (±)-Deguelin and (±)-Munduserone.
Nayak M1, Kim I1. J Org Chem. 2015 Nov 20;80(22):11460-7. doi: 10.1021/acs.joc.5b02160. Epub 2015 Nov 11.
A highly convergent synthetic approach to rotenoid natural products is described. Successful pairing of two building blocks for Sonogashira cross-coupling and intramolecular alkyne carbonyl metathesis allows ready access to 4-acylchromene, a key substructure of these natural products, leading to syntheses of (±)-deguelin and (±)-munduserone in high overall yields.
4.Deguelins, Natural Product Modulators of NF1-Defective Astrocytoma Cell Growth Identified by High-Throughput Screening of Partially Purified Natural Product Extracts.
Henrich CJ1, Cartner LK1, Wilson JA, Fuller RW, Rizzo AE, Reilly KM, McMahon JB, Gustafson KR. J Nat Prod. 2015 Nov 25;78(11):2776-81. doi: 10.1021/acs.jnatprod.5b00753. Epub 2015 Oct 15.
A high-throughput screening assay for modulators of Trp53/NF1 mutant astrocytoma cell growth was adapted for use with natural product extracts and applied to a novel collection of prefractionated/partially purified extracts. Screening 68 427 samples identified active fractions from 95 unique extracts, including the terrestrial plant Millettia ichthyotona. Only three of these extracts showed activity in the crude extract form, thus demonstrating the utility of a partial purification approach for natural product screening. The NF1 screening assay was used to guide purification of active compounds from the M. ichthyotona extract, which yielded the two rotenones deguelin (1) and dehydrodeguelin (2). The deguelins have been reported to affect growth of a number of cancer cell lines. They potently inhibited growth of only one of a panel of NF1/Trp53 mutant murine astrocytoma cell lines, possibly related to epigenetic factors, but had no effect on the growth of normal astrocytes.
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CAS 522-17-8 Deguelin

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