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Alexidine dihydrochloride

Alexidine dihydrochloride用途

Alexidine dihydrochloride 是一种抗癌剂,靶向哺乳动物细胞中的线粒体酪氨酸磷酸酶 PTPMT1,并导致线粒体凋亡。Alexidine dihydrochloride 具有对多种真菌病原体的抗真菌和抗生物膜活性。

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Alexidine dihydrochloride名称

[ CAS 号 ]:
1715-30-6

[ 中文名 ]:
阿来西定二盐酸盐

[ 英文名 ]:
Alexidine dihydrochloride

[英文别名 ]:

Alexidine dihydrochloride
Bisguadine
Sterwin 904
UNII:I2A7616PY1
alexidine 2HCl
1,1'-Hexamethylene-bis(5-[2-ethylhexyl]biguanide)
QR-711
Bisguanidine
Compound-904

Alexidine dihydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 感染

信号通路 >> 抗感染 >> 真菌

[ 靶点 ]

PTPMT1[1]

[体外研究]

盐酸阿列克西丁对大多数假丝酵母菌都显示出活性；除假丝酵母菌和克鲁西假丝酵母菌外,在浮游条件下检测的所有菌株的MIC值均小于1.5μg/mL。有趣的是,盐酸阿列克西丁对临床相关的抗氟康唑念珠菌菌株也显示出显著的活性：白色念珠菌(CA2、CA6和CA10)、光滑念珠菌(CG2和CG5)、副西洛菌(CP5)和金黄色念珠菌(CAU-09和CAU-03)[1]。盐酸阿列克西丁对浮游生物生长的抑制显示出对成像真菌的丝状或增殖的完全抑制。盐酸阿列克西丁能够在低浓度(1.5至6μg/mL)下杀死已知对几乎所有抗真菌药物都有耐药性的念珠菌、隐球菌和曲霉属的成熟生物膜。事实上,在10倍低浓度(150 ng/mL)的浮游mic下,盐酸阿列克西丁可以抑制白念珠菌的侧方酵母形成和生物膜扩散[1]。盐酸阿列克西丁导致50%的人脐静脉内皮细胞和肺上皮细胞死亡,其浓度比杀死浮游真菌病原体所需的MIC高5-10倍[1]。

[体内研究]

选择关注白念珠菌生物膜的形成,因为在这种真菌中已经建立了小鼠生物膜模型,并用于测试已建立的和新的抗真菌药物的效果。显微镜下观察药物对小鼠颈静脉导管内生长的24小时生物膜的影响,发现盐酸阿列克西丁处理的导管内生物膜密度显著降低。事实上,真菌CFU测定显示,与对照组未经处理的生物膜相比,盐酸阿列克西丁抑制了67%的真菌生物膜生长和活性[1]。

[参考文献]

[1]. Mamouei Z, et al. Alexidine Dihydrochloride Has Broad-Spectrum Activities against Diverse Fungal Pathogens. mSphere. 2018 Oct 31;3(5). pii: e00539-18.

Alexidine dihydrochloride物理化学性质

[ 密度 ]:
1.1g/cm3

[ 沸点 ]:
658.2ºC at 760mmHg

[ 熔点 ]:
220.6-223.4ºC

[ 分子式 ]:
C₂₆H₅₈Cl₂N₁₀

[ 分子量 ]:
581.712

[ 闪点 ]:
351.8ºC

[ 精确质量 ]:
580.422302

[ PSA ]:
167.58000

[ LogP ]:
8.60460

[ 外观性状 ]:
固体;White to Almost white powder to crystaline

[ 蒸汽压 ]:
3.38E-17mmHg at 25°C

[ 储存条件 ]:
-20°C;存放于惰性气体之中;避免湿气 (吸湿),加热

Alexidine dihydrochloride安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危险品运输编码 ]:
NONH for all modes of transport

Alexidine dihydrochloride文献

Chemical interaction of alexidine and sodium hypochlorite.

J. Endod. 38(1) , 112-6, (2012)

Recent studies have reported the color change and formation of precipitates containing para-chloroaniline (PCA) after a reaction of sodium hypochlorite (NaOCl) and chlorhexidine (CHX). Alexidine (ALX)...

Quantitative high throughput screening using a primary human three-dimensional organotypic culture predicts in vivo efficacy.

Nat. Commun. 6 , 6220, (2015)

The tumour microenvironment contributes to cancer metastasis and drug resistance. However, most high throughput screening (HTS) assays for drug discovery use cancer cells grown in monolayers. Here we ...

Pan-antimicrobial failure of alexidine as a contact lens disinfectant when heated in Bausch & Lomb plastic containers: implications for the worldwide Fusarium keratitis epidemic of 2004 to 2006.

Eye Contact Lens 38(4) , 222-6, (2012)

ReNu with MoistureLoc (ReNuML), containing the antimicrobial agent alexidine 0.00045%, was associated with the Fusarium keratitis epidemic of 2004 to 2006. Although a single-point source contamination...

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