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  3. Jatrorrhizine hydroxide

Jatrorrhizine hydroxide 

目录号: HY-N0749A
产品使用指南

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。

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Jatrorrhizine hydroxide Chemical Structure

Jatrorrhizine hydroxide Chemical Structure

CAS No. : 483-43-2

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Description

Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with 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 of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters[3].

IC50 & Target

IC50: 872 nM (AChE)[1]

In Vitro

Jatrorrhizine has antiplasmodial and antiamoebic activity, it against Plasmodium falciparum and E. histolytica with IC50 values 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 IC50 value of 1.05 μM and reduces 5-HT and NE uptake mediated by hOCT2, hOCT3, and hPMAT with IC50 values 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].

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.
Molecular Weight

355.38

Formula

C₂₀H₂₁NO₅

CAS No.

483-43-2

SMILES

COC1=C(OC)C2=C[N+]3=C(C4=CC(OC)=C(O)C=C4CC3)C=C2C=C1.[OH-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

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

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8139 mL 14.0694 mL 28.1389 mL
5 mM 0.5628 mL 2.8139 mL 5.6278 mL
10 mM 0.2814 mL 1.4069 mL 2.8139 mL
*

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储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -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。

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

JatrorrhizineAChE5-HT ReceptorBacterialAcetylcholinesteraseSerotonin Receptor5-hydroxytryptamine ReceptorneuroprotectiveantimicrobialantioxidantantidepressantAlzheimer’s diseaseADantidepressant-likedepressive disorderquaternary isoquinolinealkaloidantiplasmodialantiamoebicCytotoxicE. histolytica falciparumInhibitorinhibitorinhibit

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