Aloperine 是一种在苦参类植物中的生物碱,其具有抗癌,抗炎、抗肿瘤和抗病毒特性,可用于研究过敏性接触性皮炎湿疹和其他皮肤炎症。
产品描述
Aloperine exhibits anti-inflammatory, antibacterial, antiviral, and anti-tumor properties.
体外活性
Aloperine局部应用到NC/Nga小鼠,在第13天和第14天,剂量依赖性降低2,4-二硝基氟苯(DNFB)诱导的皮炎(皮炎指数和耳厚度).1% Aloperine局部应用到BALB/c小鼠,抑制DNFB诱导的耳厚度和耳红斑增高,且明显降低耳活检组织匀浆中DNFB诱导的肿瘤坏死因子-α(TNF-α),白细胞介素-1β(IL-1β)和白细胞介素-6(IL-6)的mRNA和蛋白水平上调.Aloperine剂量依赖性降低DNFB诱导的淋巴细胞侵润和嗜酸性粒细胞浸润.Aloperine处理也剂量依赖性降低DNFB诱导的肥大细胞浸润.Aloperine处理NC/Nga小鼠的耳朵活组织检查切片,明显剂量依赖性降低TNF-α,IL-1β 和 IL-6细胞因子水平.Aloperine明显降低DNFB诱导的IL-4,IL-13和IFN-γ水平提高,同时以剂量依赖性方式增加IL-10水平.
体内活性
与对白血病细胞的作用相反,高达1 mM Aloperine在72小时时不显著降低正常PBMNC的存活力。20 μM Aloperine处理48小时,明显剂量依赖性诱导HL-60细胞凋亡和自噬。Aloperine作用于HL-60 细胞,在72小时时可观察到最强的细胞毒性,抑制率为94.1%。
细胞实验
Cells are seeded in 96-well plates in 100-μL culture medium. After incubation of 4 hours for leukaemia cells and of 24 hours for solid cancer cells, experimental media containing either excipient control or Aloperine are added to appropriate wells. Five concentrations of Aloperine for 48-hour treatment are used to determine the in vitro IC50 growth inhibitory values of Aloperine in cancer cells. After incubation, 10 μL of MTT solution (5 mg/mL) is added to each well. The plates are then incubated for 4 hours at 37 °C. Intracellular formazan crystals are dissolved by addition of 100 μL of isopropanol-HCI-SDS solution to each well. After an overnight incubation at 37 °C, the optical density of the samples is determined at 570 nm. DNA fragmentation is analysed after the extraction of DNA from cells exposed to the indicated doses of Aloperine for 48 hours using apoptotic DNA ladder kit. For autophagy detection, cells are collected and incubated with PBS containing 5 μM acridine orange for 15 minutes. The acridine orange is removed and the cells are resuspended in 100 μL of PBS. Fluorescent micrographs are obtained with an inverted fluorescent microscope. Autophagy is quantified based on the mean number of cells displaying intense red staining for three fields (containing at least 50 cells per field) for each experimental condition.(Only for Reference)
Cas No.
56293-29-9
分子式
C15H24N2
分子量
232.36
储存和溶解度
DMSO:10 mM
Ethanol:46 mg/mL (197.96 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years