Isoquinoline

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Isoquinoline 是吡啶的类似物。Isoquinoline 为结构基础的生物碱，如对甲苯二异喹啉，邻苯二甲酰异喹啉和萘基异喹啉等具有抗癌活性。

Isoquinoline is an analog of pyridine. Isoquinoline-based alkaloids, such as p-tolyl bisisoquinoline, phthaloyl isoquinoline, and naphthyl isoquinoline, exhibit anticancer activity.Berberine, an isoquinoline alkaloid, exerts anti-inflammatory effects in diabetic mice by downregulating the gene expression ratios of pro-/anti-inflammatory and Th1/Th2 cytokines.Additionally, some isoquinoline-based compounds also possess antidepressant, antibacterial, antimalarial, and anti-HIV activities.

Isoquinoline 化合物，7-fluoro-1,3-diphenylisoquinoline-1-amine (FDPI) (0.1 和 1 mg/kg，胃内给药，每日 1 次，连续 35 天) 可在成年 Swiss 小鼠中消除因慢性不可预测温和应激 (CUMS) 诱导的抑郁样行为。Isoquinoline 生物碱，berberine (50-500 mg/kg，胃内给药，每日 1 次，连续 14 周) 通过下调促炎/抗炎细胞因子及 Th1/Th2 细胞因子的基因表达比率，发挥保护作用，抑制自发性 1 型糖尿病 (T1D) 非肥胖型糖尿病 (NOD) 小鼠的脾脏、肝脏和肾脏中的自发性炎症。Animal Model:Chronic unpredictable mild stress (CUMS)-induced depressive-like male adult Swiss mice model (25–35 g) Dosage:0.1 and 1 mg/kg Administration:Intragastric administration (i.g), once daily for 35 days Result:Effectively abolished depressive-like behavior in CUMS-exposed mice, improving self-care and motivation in the splash test and reducing immobility time in the TST and modified FST.Did not affect spontaneous locomotion, ruling out psychostimulant interference.Prevented the CUMS-induced increase in NF-κB and pro-inflammatory cytokines (TNF-α, INF-γ, IL-1, IL-6) in the prefrontal cortex and serum, while restoring IL-10 levels.FDPI prevented the CUMS-induced elevation of corticosterone and ACTH, counteracting the increase in adrenal weight, suggesting regulation of HPA axis hyperactivity.Prevented the CUMS-induced increase in 5-HT uptake in synaptosomes, indicating modulation of serotonergic neurotransmission.Counteracted the CUMS-induced increase in pro-BDNF and decrease in TrkB in the prefrontal cortex, suggesting a role in neuroplasticity restoration.Exerted antidepressant-like effects at lower doses than paroxetine, but its superiority over paroxetine could not be confirmed due to different administration routes (intragastric vs. intraperitoneal).Demonstrated potential as a multi-target antidepressant, with effects mediated by anti-inflammatory actions, HPA axis modulation, serotonin system regulation, and neurotrophic signaling pathways. Further studies on chronic administration and side effects are needed.

Isoquinoline 生物碱对 Plasmodium falciparum (耐药突变株 K1) 活性具有抑制作用。其中，dehydrodiscretine 和 berberine 的 IC50 少于 1 μM, 而sallocrytopine、 columbamine、 dehydroocoteine、 jatrorrhizine、norcorydine、thalifendine 和 ushinsuninehad 的 IC50 在 1-10 μM。Berberine (一种 Isoquinoline 生物碱) (20-80 μM，14 天) 通过抑制凋亡相关蛋白的变化和减少小胶质细胞激活，发挥抗脑缺血的神经保护作用。Western Blot Analysis Cell Line:Hippocampal neurons (rat)Concentration:20-80 μM Incubation Time:14 days Result:Led that the Bax/Bcl-2 ratio was altered, reduced expression of apoptotic marker Caspase-3.

异喹啉

Others

Other Targets

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119-65-3

129.16

C9H7N

>98% (HPLC)

DMSO : 100 mg/mL (774.22 mM; ultraphonic; )

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(-20℃)

With Ice Pack

≥ 2 years