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Emetine dihydrochloride hydrate

Emetine dihydrochloride hydrate用途

Emetine dihydrochloride hydrate 是一种抗原虫药,早期用于治疗肠道和组织的阿米巴病。

Emetine dihydrochloride hydrate名称

[ CAS 号 ]:
7083-71-8

[ 中文名 ]:
Emetine dihydrochloride hydrate

[ 英文名 ]:
Emetine dihydrochloride hydrate

[英文别名 ]:

Emetine,dihydrochloride,hydrate
Emetine hydrochloride hydrate
Emetine dihydrochloride hydrate

Emetine dihydrochloride hydrate生物活性

[ 描述 ]:

Emetine dihydrochloride hydrate 是一种抗原虫药,早期用于治疗肠道和组织的阿米巴病。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[体外研究]

据报道,依他敏亚二盐酸盐水合物对药物敏感的3D7恶性疟原虫寄生虫菌株具有1nM的IC 50值。使用K1抗性分离物测定两种药物的剂量反应曲线,并且分别对于依米丁胺二盐酸盐水合物和DHA建立的IC50值为47±2.1nM和2.6±0.41nM [1]。用环己酰亚胺或依米卡星二盐酸盐水合物处理淋巴母细胞后,通过直接测序相应的cDNA,突变等位基因的表达水平几乎与野生型等位基因同等地升高[2]。 Emetine被鉴定为具有显着浓度依赖性抑制PEDF诱导的TNF分泌的先导化合物,IC50为146nM。依米丁抑制PEDF介导的TNF释放而不影响细胞活力。 Emetine以高结合亲和力(KD = 14.3 nM)与PEDF受体ATGL结合[3]。依米丁治疗降低细胞活力,诱导细胞凋亡,促使AML细胞分化并下调HIF-1α[4]。

[体内研究]

在具有T1D的低剂量链脲佐菌素模型的小鼠中,依米丁(0.002,0.02,0.2和2mg/kg)不会引起体重的任何显着差异。给予依米丁不仅以剂量依赖性方式降低血糖水平,而且还诱导血糖水平的持续衰减。 emetine的每日给药剂量依赖性地减少d 21的高血糖反应。与该观察结果一致,施用emetine而不是载体对照导致血糖水平的持续衰减。 Emetine可在自发性NOD T1D模型中改善疾病严重程度[3]。 Emetine(1 mg/kg)可降低体内异种移植小鼠模型中的白血病负担和治疗后白血病细胞的克隆能力[4]。

[细胞实验]

将7.5×10 5个细胞/ mL在96孔板中在完全培养基中培养。以指定浓度添加依米丁和Ara-C。通过流式细胞术通过7-AAD排除和Hoechst33342阳性染色测量细胞活力;在FACSCantoII细胞计数器中通过体积获得细胞计数。在GraphPad中计算统计分析和EC50测定。 FlowJo软件用于流式细胞术分析。

[动物实验]

通过每天一次腹膜内（ip）给予链脲佐菌素（50mg / kg溶于柠檬酸钠缓冲液，pH4.5）至6至8周龄的C57B1 / 6小鼠诱导T1D连续5天。给予小鼠补充有10％蔗糖的水6天，以防止在施用链脲佐菌素期间突然发生低血糖。对于时间过程研究，每隔一天测量体重和血糖。用FreeStyle Lite血糖仪测量血糖。对于使用依米丁的研究，小鼠每日接受二盐酸依米丁（0.002,0.02,0.2和2mg / kg）或盐水。每周测量一次FreeStyle Lite血糖仪或Bayer Contour血糖仪和体重的血糖。在每项研究结束时，通过CO 2窒息使小鼠安乐死。收集血液和胰腺用于细胞因子分析。

[参考文献]

[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.

[2]. Wu L, et al. PRRT2 truncated mutations lead to nonsense-mediated mRNA decay in Paroxysmal Kinesigenic Dyskinesia. Parkinsonism Relat Disord. 2014 Dec;20(12):1399-404.

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

[4]. Cornet-Masana JM, et al. Emetine induces chemosensitivity and reduces clonogenicity of acute myeloid leukemia cells. Oncotarget. 2016 Apr 26;7(17):23239-50.

[相关活性小分子]

Emetine dihydrochloride hydrate物理化学性质

[ 分子式 ]:
C₂₉H₄₀N₂O_4.2HCl_.H₂O

[ 分子量 ]:
571.58

[ PSA ]:
61.42000

[ LogP ]:
6.74980

Emetine dihydrochloride hydrate安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H315-H319-H335

[ 警示性声明 ]:
P261-P264-P301 + P310-P305 + P351 + P338

[ 危险品运输编码 ]:
UN 1544PSN2 6.1 / PGI

Emetine dihydrochloride hydrate文献

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