Jatrorrhizine hydroxide

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CAS NO:

483-43-2

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 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

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。