Emetine dihydrochloride hydrate
(Synonyms: 吐根碱盐酸盐水合物) 目录号 : GC32048
An alkaloid with diverse biological activities
Cas No.:7083-71-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
7.5×105 cells per mL are cultured in 96-well plates in complete medium. Emetine and Ara-C are added at indicated concentrations. Cell viability is measured by 7-AAD exclusion and Hoechst33342 positivity staining by flow cytometry; and cell count is obtained by volume in a FACSCantoII cytometer. Statistical analysis and EC50 determination are calculated in GraphPad. FlowJo software is used for flow cytometry analysis. |
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Animal experiment: |
T1D is induced by administration of streptozotocin (50 mg/kg dissolved in sodium citrate buffer, pH 4.5) to 6 to 8 wk old C57Bl/6 mice intraperitoneally (i.p.) once each day for 5 consecutive days. Mice are given water supplemented with 10% sucrose for six days to prevent sudden hypoglycemia during streptozotocin administration. For time course studies, body weight and blood glucose are measured every other day. Blood glucose is measured with a FreeStyle Lite blood glucose meter. For studies with emetine, mice receive daily administration of emetine dihydrochloride (0.002, 0.02, 0.2 and 2 mg/kg) or saline. Blood glucose with either FreeStyle Lite blood glucose meter or Bayer Contour blood glucose meter and body weight are measured once weekly. At the end of each study, mice are euthanized by CO2 asphyxiation. Blood and pancreas are collected for cytokine analysis. |
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References: [1]. 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 |
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Emetine is an alkaloid that has been found in ipecac root and has diverse biological activities.1,2,3,4 It is active against several strains of E. histolytica amoebae (IC50s = 0.73-10.22 μg/ml).1 Emetine inhibits NF-κB signaling induced by TNF-α or IL-1β (IC50s = 2 and 4.2 μM, respectively, in a cell-based β-lactamase reporter assay), increases caspase-3/7 activity in ME180 cells (EC50 = 1.1 μM), and is cytotoxic to HeLa cells.2 It reduces the infectious virus yield and viral RNA copy numbers in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50s = 0.46 and 0.5 μM, respectively).4 Emetine (5 mg/kg) induces emesis in ferrets, an effect that can be prevented by the serotonin (5-HT) receptor subtype 5-HT3 antagonist ondansetron.3
1.Burchard, G.D., and Mirelman, D.Entamoeba histolytica: Virulence potential and sensitivity to metronidazole and emetine of four isolates possessing nonpathogenic zymodemesExp. Parasitol.66(2)231-242(1988) 2.Miller, S.C., Huang, R., Sakamuru, S., et al.Identification of known drugs that act as inhibitors of NF-κB signaling and their mechanism of actionBiochem. Pharmacol.79(9)1272-1280(2016) 3.Hasegawa, M., Sasaki, T., Sadakane, K., et al.Studies for the emetic mechanisms of ipecac syrup (TJN-119) and its active components in ferrets: Involvement of 5-hydroxytryptamine receptorsJpn. J. Pharmacol.89(2)113-119(2002) 4.Choy, K.-T., Wong, A.-Y., Kaewpreedee, P., et al.Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitroAntiviral Res.178104786(2020)
| Cas No. | 7083-71-8 | SDF | |
| 别名 | 吐根碱盐酸盐水合物 | ||
| Canonical SMILES | CC[C@@H]1[C@H](C[C@@]2([H])C3=CC(OC)=C(OC)C=C3CCN2C1)C[C@]4([H])C5=CC(OC)=C(OC)C=C5CCN4.[H]Cl.[H]Cl.O | ||
| 分子式 | C29H40N2O4 . 2 HCl . H2O | 分子量 | 571.58 |
| 溶解度 | 100mg/mL in water; 1mg/mL in chloroform. | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7495 mL | 8.7477 mL | 17.4954 mL |
| 5 mM | 0.3499 mL | 1.7495 mL | 3.4991 mL |
| 10 mM | 0.175 mL | 0.8748 mL | 1.7495 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Investigating antimalarial drug interactions of Emetine dihydrochloride hydrate using CalcuSyn-based interactivity calculations
PLoS One 2017 Mar 3;12(3):e0173303.PMID:28257497DOI:10.1371/journal.pone.0173303.
The widespread introduction of artemisinin-based combination therapy has contributed to recent reductions in malaria mortality. Combination therapies have a range of advantages, including synergism, toxicity reduction, and delaying the onset of resistance acquisition. Unfortunately, antimalarial combination therapy is limited by the depleting repertoire of effective drugs with distinct target pathways. To fast-track antimalarial drug discovery, we have previously employed drug-repositioning to identify the anti-amoebic drug, Emetine dihydrochloride hydrate, as a potential candidate for repositioned use against malaria. Despite its 1000-fold increase in in vitro antimalarial potency (ED50 47 nM) compared with its anti-amoebic potency (ED50 26-32 uM), practical use of the compound has been limited by dose-dependent toxicity (emesis and cardiotoxicity). Identification of a synergistic partner drug would present an opportunity for dose-reduction, thus increasing the therapeutic window. The lack of reliable and standardised methodology to enable the in vitro definition of synergistic potential for antimalarials is a major drawback. Here we use isobologram and combination-index data generated by CalcuSyn software analyses (Biosoft v2.1) to define drug interactivity in an objective, automated manner. The method, based on the median effect principle proposed by Chou and Talalay, was initially validated for antimalarial application using the known synergistic combination (atovaquone-proguanil). The combination was used to further understand the relationship between SYBR Green viability and cytocidal versus cytostatic effects of drugs at higher levels of inhibition. We report here the use of the optimised Chou Talalay method to define synergistic antimalarial drug interactivity between Emetine dihydrochloride hydrate and atovaquone. The novel findings present a potential route to harness the nanomolar antimalarial efficacy of this affordable natural product.
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.PMID:24107123DOI:10.1186/1475-2875-12-359.
Background: Drug repurposing or repositioning refers to the usage of existing drugs in diseases other than those it was originally used for. For diseases like malaria, where there is an urgent need for active drug candidates, the strategy offers a route to significantly shorten the traditional drug development pipelines. Preliminary high-throughput screens on patent expired drug libraries have recently been carried out for Plasmodium falciparum. This study reports the systematic and objective further interrogation of selected compounds reported in these studies, to enable their repositioning as novel stand-alone anti-malarials or as combinatorial partners. Methods: SYBR Green flow cytometry and micro-titre plate assays optimized in the laboratory were used to monitor drug susceptibility of in vitro cultures of P. falciparum K1 parasite strains. Previously described fixed-ratio methods were adopted to investigate drug interactions. Results: Emetine dihydrochloride hydrate, an anti-protozoal drug previously used for intestinal and tissue amoebiasis was shown to have potent inhibitory properties (IC₅₀ doses of ~ 47 nM) in the multidrug resistant K1 strain of P. falciparum. The sum 50% fractional inhibitory concentration (∑FIC₅₀, ₉₀) of the interaction of Emetine dihydrochloride hydrate and dihydroartemisinin against the K1 strains of P. falciparum ranged from 0.88-1.48. Conclusion: The results warrant further investigation of Emetine dihydrochloride hydrate as a potential stand-alone anti-malarial option. The interaction between the drug and the current front line dihydroartemisinin ranged from additive to mildly antagonistic in the fixed drug ratios tested.
Screening for natural and derived bio-active compounds in preclinical and clinical studies: One of the frontlines of fighting the coronaviruses pandemic
Phytomedicine 2021 May;85:153311.PMID:33067112DOI:10.1016/j.phymed.2020.153311.
Background: Starting December 2019, mankind faced an unprecedented enemy, the COVID-19 virus. The world convened in international efforts, experiences and technologies in order to fight the emerging pandemic. Isolation, hygiene measure, diagnosis, and treatment are the most efficient ways of prevention and intervention nowadays. The health organizations and global care systems screened the available resources and offered recommendations of approved and proposed medications. However, the search for a specific selective therapy or vaccine against COVID-19 remains a challenge. Methods: A literature search was performed for the screening of natural and derived bio-active compounds which showed potent antiviral activity against coronaviruses using published articles, patents, clinical trials website (https://clinicaltrials.gov/) and web databases (PubMed, SCI Finder, Science Direct, and Google Scholar). Results: Through the screening for natural products with antiviral activities against different types of the human coronavirus, extracts of Lycoris radiata (L'Hér.), Gentiana scabra Bunge, Dioscorea batatas Decne., Cassia tora L., Taxillus chinensis (DC.), Cibotium barometz L. and Echinacea purpurea L. showed a promising effect against SARS-CoV. Out of the listed compound Lycorine, Emetine dihydrochloride hydrate, pristimerin, harmine, conessine, berbamine, 4`-hydroxychalcone, papaverine, mycophenolic acid, mycophenolate mofetil, monensin sodium, cycloheximide, oligomycin and valinomycin show potent activity against human coronaviruses. Additionally, it is worth noting that some compounds have already moved into clinical trials for their activity against COVID-19 including fingolimod, methylprednisolone, chloroquine, tetrandrine and tocilizumab. Conclusion: Natural compounds and their derivatives could be used for developing potent therapeutics with significant activity against SARS-COV-2, providing a promising frontline in the fighting against COVID-19.