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Cephaeline

MCE China：Cephaeline

Brand：MedChemExpress (MCE)

Cat. No.HY-N4118

CAS：483-17-0

Synonyms：(-)-Cephaeline; NSC 32944 free base

Purity：98.94%

Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy.

In Vitro：Cephaeline (1-1000 nM, 1 h) inhibits ZIKV NS5 RdRp in the polymerase activity assay with an IC50 value of 976 nM in HEK293 cells[2]. Cephaeline (0.1-1000 μM, 72 h) shows the inhibition effect on Ebola VLP entry with an IC50 value of 3.27 μM in HeLa cells and infection of Ebola live virus with an IC50 value of 22.18 nM in Vero E6 cells[2]. Cephaeline (0-32 μM, 72 h) inhibits cellular viability, growth and migration in mucoepidermoid carcinoma (MEC) cell lines[3]. Cephaeline (5-400 nM, 24, 48 and 72h) induces lung cancer cell death in lung cancer cell line H460 and A549[4]. Cephaeline (0.16, 2.08 and 0.02 μM, 24 h and 48 h) progressively increases histone acetylation in MEC cell lines[3]. Cephaeline (0-100 nM, 24 h) induces ferroptosis in lung cancer cells by targeting NRF2[4].

In Vivo：Cephaeline (2 mg/kg, i.p.,daily for 3 days) suppresses ZIKV load and decreases the NS1 protein and ZIKV RNA in serum of ZIKV infected Ifnar1−/− mice[2]. Cephaeline (5 mg/kg, i.p.,daily for 7 days) effectively suppressed EBOV infection in EBOV mouse models[3]. Cephaeline (5, 10 mg/kg, i.p., a single dose for 12 days) plays an anti-lung cancer role by inducing ferroptosis in tumor xenograft mouse model[4].

IC50 & Target：EBOV

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References：

[1]. N.P.Sahu, et al. Determination of emetine and cephaeline in Ipecac roots by high- performance liquid chromatography. Journal of Chromatography A. 1982 Apr; 238( 2):525-529.

[2]. Yang S, et al. Emetine inhibits Zika and Ebola virus infections through two molecular mechanisms: inhibiting viral replication and decreasing viral entry. Cell Discov. 2018 Jun 5;4:31.  [Content Brief]

[3]. Silva LC, et al. Cephaeline is an inductor of histone H3 acetylation and inhibitor of mucoepidermoid carcinoma cancer stem cells. J Oral Pathol Med. 2022 Jul;51(6):553-562.  [Content Brief]

[4]. Chen P, et al. Cephaeline promotes ferroptosis by targeting NRF2 to exert anti-lung cancer efficacy. Pharm Biol. 2024 Dec;62(1):195-206.  [Content Brief]