Emetine hydrochloride

Names

[ Name ]:
Emetine hydrochloride

[Synonym ]:
(-)-Emetine hydrochloride
Cephaeline methyl ether HCl
6',7',10,11-Tetramethoxyemetan hydrochloride (1:1)
Cephaeline methyl ether hydrochloride
Emetin-hydrochlorid
EMETINE HYDROCHLORIDE
2H-Benzo[a]quinolizine, 3-ethyl-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-2-[[(1R)-1,2,3,4-tetrahydro-6,7-dimethoxy-1-isoquinolinyl]methyl]-, (2S,3R,11bS)-, hydrochloride (1:1)
Emetine monohydrochloride
Emetan, 6',7',10,11-tetramethoxy-, monohydrochloride
emetine chloride

Biological Activity

[Description]:

Emetine hydrochloride, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine hydrochloride inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine hydrochloride potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect[1][2][3][4].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Emetine hydrochloride accumulates SQSTM1 and MAP1LC3B in SNB-19 cells, indicating autophagy is blocked[1]. Emetine hydrochloride dose-dependently decreases NS1 protein level in HEK293 cells infected with the African prototype, ZIKV MR766 (IC50=52.9 nM). Emetine hydrochloride directly inhibits ZIKV NS5 RNA polymerase activity with an IC50 of 121 nM[1]. Cell Autophagy Assay[1] Cell Line: SNB-19 cells Concentration: 25, 50, 100, 200 nM Incubation Time: For 24 hours Result: Showed the accumulation of SQSTM1 and MAP1LC3B, indicating autophagy was blocked.

[In Vivo]

Emetine hydrochloride (1, 2 mg/kg/day; IP; for 3 days) significantly reduces the serum viral load of ZIKV infected Ifnar1−/− mice[1]. Emetine hydrochloride (1 mg/kg/day; retro-orbital injection; for six days) reduces the levels of circulating ZIKV approximately 10-fold in three-month-old female SJL mice with ZIKVBR[1]. Emetine (0.002, 0.02, 0.2, 2 mg/kg/day; i.p.) not only attenuates blood glucose levels in dose-dependent way but also induces a persistent attenuation of blood glucose levels in C57Bl/6 male mice (20-25 g) [2]. Animal Model: Ifnar1−/− mice[1] Dosage: 1, 2 mg/kg Administration: IP; once daily for 3 days Result: Significantly reduced the serum viral load of ZIKV infected Ifnar1−/− mice.

[References]

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

[2]. Hudson LK, et al. Emetine Di-HCl attenuates Type 1 diabetes mellitus in mice. Mol Med. 2016 Jun 10;22

[3]. Matthews H, et al. Drug repositioning as a route to anti-malarial drug discovery: preliminary investigation of the in vitro anti-malarial efficacy of emetine dihydrochloride hydrate. Malar J. 2013 Oct 9;12:359.

[4]. Khandelwal N, et al. Emetine inhibits replication of RNA and DNA viruses without generating drug-resistant virusvariants. Antiviral Res. 2017 Aug;144:196-204.

[5]. Sands, M, et al. (1977). Antibacterial activity of emetine. Transactions of the Royal Society of Tropical Medicine and Hygiene, 71(5), 454-455.