依布硒性质、用途与生产工艺
依布硒是一种小分子抗氧化剂,易于参加各种氧化还原反应,能清除机体内过多的过氧化物,阻断产生自由基的链式反应,因此可治疗多种疾病,维持机体的正常生理功能。长期以来,人们普遍认为依布硒在体内主要通过模拟谷胱甘肽过氧化物酶的反应机制发挥作用。然而,近来的研究表明依布硒在体内更趋向于通过硫氧还蛋白还原酶和硫氧还蛋白反应系统来发挥作用。
依布硒的合成方法主要有以下三种:
A.以N-苯基苯甲酰胺为起始原料,通过n-BuLi使其邻位锂化生成C-Li键,然后让Se原子插入C-Li键形成双阴离子化合物,最后通过适当的氧化剂氧化闭环得到依布硒。以Br2或I2为氧化剂时闭环收率低于20%,采用FeCl3时闭环收率提高到42%,使用CuBr2时收率进一步提高到63%。
B.以2,2′-二硒化双苯甲酸为起始原料,经多步反应得到取代2-甲硒基苯甲酰胺,经PCl5闭环、水解得到依布硒。
C.Lesser和Kamigata等以2,2′-二硒化双苯甲酸为起始原料,通过SOCl2使二硒键裂解,形成中间体3,然后与苯胺反应闭环得到依布硒。
Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161)是HIV-1复制的小分子衣壳抑制剂，在TR-FRET分析中的IC50为46.1 nM。
| Target | Value |
HIV-1
(Cell-free assay)
|
46.1 nM
|
Ebselen (SPI-1005; 0.4-100 μM; 20-24 hours) shows strong antiviral effects at a concentration of 10 μM treatment in COVID-19 virus infected Vero cells. Ebsele covalently binds to C145 of the catalytic dyad in COVID-19 virus Mpro.
Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process.
Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. Ebselen inhibits inositol monophosphatase (IMPase).
Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic, renal cancer cell lines.
RT-PCR
|
Cell Line:
|
COVID-19 virus infected Vero cells
|
|
Concentration:
|
0.4, 1.2, 3.7, 11.1, 33.3, 100 μM
|
|
Incubation Time:
|
20-24 hours
|
|
Result:
|
Showed strong antiviral effects at a concentration of 10 μM treatment.
|
Ebselen (5, 10 mg/kg; IP) decreases 5-HT
2
agonist-induced head twitches in a dose-dependent manner.
|
Animal Model:
|
20-25 g 10-12 week old male C57Bl6 mice
|
|
Dosage:
|
5, 10 mg/kg
|
|
Administration:
|
IP
|
|
Result:
|
Decreased 5-HT
2
agonist-induced head twitches in a dose-dependent manner.
|
依布硒
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