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]. |
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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].
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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. |
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| 结构分类 | - Alkaloids
- Isoquinoline Alkaloids
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| 来源 | - Plants
- Ranunculaceae
- Coptis chinensisFranch.
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| 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 | 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。 |
