Helioxanthin - CAS 18920-47-3
Catalog number: 18920-47-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
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Helioxanthin and its analogues decreased cellular RNA levels of HBV and antigen expression as well as selective inhibition of HBV replication in a cell culture model. Helioxanthin analogue 8-1 exhibited anti-DHBV activity as demonstrated by quantification of viral DNA, RNA, covalently closed circular DNA and protein synthesis. Analogue 8-1 did not affect the stability of cellular macromolecules and did not have a sustained antiviral effect after drug removal. When DHBV replication was induced, virus-harbouring cells were more susceptible to the cytotoxicity of 8-1 than non-induced cells.
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ACH-126447; ACH 126447; ACH126447
1.Synthesis and biological evaluation of helioxanthin analogues.
Janmanchi D1, Lin CH, Hsieh JY, Tseng YP, Chen TA, Jhuang HJ, Yeh SF. Bioorg Med Chem. 2013 Apr 1;21(7):2163-76. doi: 10.1016/j.bmc.2012.11.037. Epub 2012 Dec 5.
Helioxanthin and analogues have been demonstrated to suppress gene expression of human hepatitis B virus. In the continuous attempt to optimize antiviral activity, various structural motifs were grafted on the helioxanthin scaffold. Many such analogues were synthesized and evaluated for their anti-hepatitis B virus activity. Structure-activity relationships of these helioxanthin derivatives are also discussed. Among these new compounds, 15 exhibits the highest activity against HBV (EC50=0.06 μM). This compound can suppress viral surface antigen and DNA expression. Furthermore, viral RNA is also diminished while the core promoter is deactivated upon treatment by 15. A plausible working mechanism is postulated. Our results establish helioxanthin lignans as potent anti-HBV agents with unique mode of action. Since their antiviral mechanism is distinct from current nucleoside/nucleotide drugs, helioxanthin lignans constitute a potentially new class of anti-HBV agents for combination therapy.
2.Helioxanthin analogue 8-1 inhibits duck hepatitis B virus replication in cell culture.
Ying C1, Tan S, Cheng YC. Antivir Chem Chemother. 2010;21(2):97-103. doi: 10.3851/IMP1686.
BACKGROUND: Current approved anti-HBV treatment cannot completely eliminate HBV infection, and emergence of resistant virus is an important treatment issue. Effective anti-HBV agents with different mechanisms of action on novel target sites are needed for the treatment of HBV infection and for combating the resistant virus, alone or in combination with current anti-HBV strategies. Helioxanthin analogue 8-1 displayed potent anti-HBV activity in human HBV in vitro and in animal models, with a unique antiviral mechanism. Its antiviral activity in other HBV system needs further study.
3.The Total Synthesis of Retrojusticidin B, Justicidin E, and Helioxanthin.
Kao TT1,2, Lin CC1, Shia KS2. J Org Chem. 2015 Jul 2;80(13):6708-14. doi: 10.1021/acs.joc.5b00866. Epub 2015 Jun 15.
Making use of a tandem free radical cyclization process mediated by Mn(OAc)3 as a key operation, the total synthesis of retrojusticidin B, justicidin E, and helioxanthin has been concisely achieved in four or five steps in an overall yield of 45, 33 and 44%, respectively, from a common starting material 5.
4.Helioxanthin suppresses the cross talk of COX-2/PGE2 and EGFR/ERK pathway to inhibit Arecoline-induced Oral Cancer Cell (T28) proliferation and blocks tumor growth in xenografted nude mice.
Lin YM1,2, Kuo WW3, Velmurugan BK4, Hsien HH4, Hsieh YL5, Hsu HH6,7, Tu CC8, Bau DT9, Viswanadha VP10, Huang CY4,5,11. Environ Toxicol. 2015 Oct 14. doi: 10.1002/tox.22204. [Epub ahead of print]
Helioxanthin, an active compound from Taiwania cryptomerioides Hayata, has been shown to have various biological activities. However, their anticancer effect in oral squamous cell carcinoma has not been well established yet. Helioxanthin inhibited the proliferation of oral squamous cell carcinoma cells in a dose-dependent manner by inducing G2/M phase arrest. Similarly, helioxanthin inhibited cyclooxygenase-2, (COX-2), phosphorylated EGFR, and extracellular-signal-regulated kinases (ERK) protein level and further reduced the nuclear accumulation of phosphorylated epidermal growth factor receptor (pEGFR) and activator protein-1(AP-1) family protein, c-fos. Moreover, helioxanthin at the dose of 20 and 30 mg kg-1 for 15 days reduced the tumor growth in animal model. This study demonstrated that Helioxanthin exerts its anticancer activity against oral cancer cells by downregulating EGFR/ERK/c-fos signaling pathway to inhibit COX-2 level and by activating cyclin-dependent kinase inhibitor (p27) to further induce G2/M cell cycle arrest.
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CAS 18920-47-3 Helioxanthin

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