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Jatrorrhizine hydroxide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Jatrorrhizine hydroxide图片
CAS NO:483-43-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Jatrorrhizine hydroxide 是从黄连中分离得到的生物碱,具有神经保护、抗菌、抗疟原虫和抗氧化活性。Jatrorrhizine hydroxide 是有效的,具有口服活性的乙酰胆碱酯酶 (AChE) (IC50=872 nM) 的抑制剂,是对 BuChE 的选择性为 115 倍。Jatrorrhizine hydroxide 通过抑制 uptake-2 transporter 的活性减少血清素 (5-HT) 和去甲肾上腺素 (NE) 的摄取。
生物活性

Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensiswith neuroprotective, antimicrobial, antiplasmodial and antioxidant activities[1]. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE[2]. Jatrorrhizine hydroxide reduces uptake ofserotonin (5-HT)andnorepinephrine (NE)via inhibition of uptake-2 transporters[3].

IC50& Target

IC50: 872 nM (AChE)[1]

体外研究
(In Vitro)

Jatrorrhizine has antiplasmodial and antiamoebic activity, it againstPlasmodium falciparumandE. histolyticawith IC50values of 3.15 and 82.7 μM, respectively[1].
The hOCT2 (organic cation transporter 2), hOCT3, and PMAT (plasma membrane monoamine transporter) are capable of transporting monoamine neurotransmitters in the brain[3].
Jatrorrhizine has the inhibitory potency of jatrorrhizine on 5-HT and NE uptake in hOCT2-, hOCT3-, and PMAT-transfected cells. Jatrorrhizine strongly inhibits PMAT-mediated MPP+uptake with an IC50value of 1.05 μM and reduces 5-HT and NE uptake mediated by hOCT2, hOCT3, and hPMAT with IC50values of 0.1-1 μM (for OCT2 and OCT3) and 1-10 μM (for PMAT)[3].
Clearance of neurotransmitters released into the synaptic cleft is defined by two distinct processes. Uptake-1, the common target of current applied antidepressants, is comprised of the serotonin transporter (SERT), the “SERT”, had a high affinity but low capacity to take up [3H]5-HT. Uptake-2 transporters are an important supplementary regulation system in monoamine clearancethought to be the “NET”, has low affinity but high capacity to take up [3H]5-HT into brain slices.
Jatrorrhizine significantly inhibited 5-HT and NE uptake in synaptosomes at 25 μM and 50 μM[3].

体内研究
(In Vivo)

Jatrorrhizine (intraperitoneal injection; 5, 10, 20 mg/kg) can significantly reduce the duration of immobility when compared with vehicle control group in tail suspension test (TST)[2].

Animal Model:Male ICR albino mice[2]
Dosage:5, 10, 20 mg/kg
Administration:Intraperitoneal injection; 5, 10, 20 mg/kg
Result:Reduced immobility period in tail suspension test.
分子量

355.38

性状

Solid

Formula

C20H21NO5

CAS 号

483-43-2

结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
  • Phenols
  • Monophenols
来源
  • Plants
  • Ranunculaceae
  • Coptis chinensisFranch.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

H2O : 5 mg/mL(14.07 mM;Need ultrasonic)

DMSO : 3.33 mg/mL(9.37 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8139 mL14.0694 mL28.1389 mL
5 mM0.5628 mL2.8139 mL5.6278 mL
10 mM0.2814 mL1.4069 mL2.8139 mL
*

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。