25549-98-8 Purity
98 atom % D
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Specification
Gao J, et al. European Journal of Pharmacology, 2024, 983, 177012.
This study investigated the antiviral potential of cephalotaxine, a key metabolite of harringtonine, in blocking SARS-CoV-2 entry by targeting both the viral spike (S) protein and host TMPRSS2 protease. The experimental work focused on characterizing the dual inhibitory mechanism of cephalotaxine and its analog, 5'-de-O-methylharringtonine, through molecular binding and viral entry assays.
The compounds were evaluated using cell membrane chromatography, confirming their direct binding to both SARS-CoV-2 spike protein and TMPRSS2. Binding affinity was supported by molecular docking analyses, which revealed hydrogen bond formation at critical interaction residues involved in spike-ACE2 and TMPRSS2-nafamostat interfaces.
To assess functional activity, a pseudotyped virus assay was performed. Cephalotaxine exhibited dose-dependent inhibition of SARS-CoV-2 pseudovirus entry and membrane fusion, with enhanced efficacy correlating with increased TMPRSS2 expression levels in host cells. The inhibition of viral entry was monitored using luciferase-based reporter assays, confirming suppression of spike-mediated fusion. Toxicity profiles were evaluated via cytotoxicity assays on normal human cell lines, where cephalotaxine demonstrated low cytotoxicity and favorable safety margins.
These findings establish cephalotaxine as a dual-action membrane fusion inhibitor, offering a promising therapeutic avenue against SARS-CoV-2 and its variants.
The molecular formula of Cephalotaxlen is C18H21NO4.
The molecular weight of Cephalotaxlen is 315.4 g/mol.
The IUPAC name of Cephalotaxlen is (2S,3S,6R)-4-methoxy-16,18-dioxa-10-azapentacyclo[11.7.0.02,6.06,10.015,19]icosa-1(20),4,13,15(19)-tetraen-3-ol.
The InChI of Cephalotaxlen is InChI=1S/C18H21NO4/c1-21-15-9-18-4-2-5-19(18)6-3-11-7-13-14(23-10-22-13)8-12(11)16(18)17(15)20/h7-9,16-17,20H,2-6,10H2,1H3/t16-,17-,18+/m1/s1.
The InChIKey of Cephalotaxlen is YMNCVRSYJBNGLD-KURKYZTESA-N.
The CAS number of Cephalotaxlen is 24316-19-6.
The LCSS Datasheet for Cephalotaxlen provides information on its chemical safety in laboratory settings.
The synonym of Cephalotaxlen is Omacetaxine.
Omacetaxine is used as a protein translation inhibitor for the treatment of chronic myeloid leukemia that is resistant to tyrosine kinase receptor antagonists.
Cephalotaxlen is found naturally in Cephalotaxus hainanensis, Cephalotaxus harringtonia, and other organisms.
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