Norisoboldine 是一种具有口服活性的天然芳基烃受体 (AhR) 激动剂。Norisoboldine 作为林参中主要的异喹啉类生物碱，可用于类风湿性关节炎和溃疡性结肠炎的研究。
| 生物活性 | Norisoboldine is an orally active naturalaryl hydrocarbon receptor(AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis[1][2]. |
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体外研究
(In Vitro) | Norisoboldine (1~30 μM; 0~24 hours; CD4+T cells) activates AhR under hypoxic microenvironment and significantly downregulates mRNA expression of miR-31[2].
Norisoboldine (30 μM; 0~24 hours; CD4+T cells) inhibits glycolysis in hypoxia[2].
Norisoboldine (1~30 μM; 0~72 hours; Treg cells) promotes Treg differentiation in hypoxia[2].
Norisoboldine (10, 30 μM) facilitates the disassociation of HSP90/AhR complexes, the nuclear translocation of AhR, and the formation of AhR/ARNT complexes. Norisoboldine induces generation of Treg cells in hypoxia is independent of miR-31[2].
Western Blot Analysis[2] | Cell Line: | CD4+T cells | | Concentration: | 1~30 μM | | Incubation Time: | 24 hours | | Result: | Activated AhR in cells under hypoxic microenvironment. |
RT-PCR[2] | Cell Line: | CD4+T cells | | Concentration: | 1~30 μM | | Incubation Time: | 24 hours | | Result: | Significantly downregulated mRNA expression of miR-31. |
Immunofluorescence[2] | Cell Line: | CD4+T cells | | Concentration: | 30 μM | | Incubation Time: | 24 hours | | Result: | Inhibited glycolysis in hypoxia. |
Cell Differentiation Assay[2] | Cell Line: | Treg cells | | Concentration: | 1~30 μM | | Incubation Time: | 72 hours | | Result: | Promoted Treg differentiation in hypoxia. |
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体内研究
(In Vivo) | Norisoboldine (10~40 mg/kg; p.o.; 20 days) significantly reduces the severity of joint swelling and erythema during the course of the experiment[1].
Norisoboldine (40 mg/kg; i.g.; 10 days) induces enhancement of CYP1A1 expression and suppresses expressions of Glut1 and HK2 in colons[2].
| Animal Model: | Male ICR mice (18–22 g) | | Dosage: | 10~40 mg/kg | | Administration: | P.o. | | Result: | Significantly reduced the severity of joint swelling and erythema during the course of the experiment. |
| Animal Model: | Female C57BL/6 mice (18–22 g) | | Dosage: | 40 mg/kg | | Administration: | I.g. | | Result: | Induced enhancement of CYP1A1 expression and suppressed expressions of Glut1 and HK2 in colons. |
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| 中文名称 | 去甲异波尔定；去甲基异波尔定；新木姜子碱；去甲依波而定 |
| 结构分类 | - Alkaloids
- Isoquinoline Alkaloids
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| 来源 | - Plants
- Lauraceae
- Lindera aggregata(Sims) Kosterm.
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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: DMSO : ≥ 62.5 mg/mL(199.46 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.1913 mL | 15.9566 mL | 31.9132 mL | | 5 mM | 0.6383 mL | 3.1913 mL | 6.3826 mL | | 10 mM | 0.3191 mL | 1.5957 mL | 3.1913 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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