| CAS |
No.5508-58-7 |
| 中文名称 |
穿心莲内酯(10mM in DMSO,无菌） |
| 英文名称 |
Andrographolide(10mM in DMSO，Sterile） |
| 分子式 |
C20H30O5 |
| 分子量 |
350.45 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
NF-κB |
| 通路 |
NF-κB |
| 背景说明 |
Andrographolide是一种 NF-κB 抑制剂，通过共价修饰内皮细胞中 p50 的半胱氨酸残基而抑制 NF-κB 活化，而不影响 IκBα 降解或 p50/p65 核易位。 |
| 生物活性 |
Andrographolide is a NF-κB inhibitor， which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.[1-2] |
| In Vitro |
Andrographolide (AP) concentration-dependently suppresses receptor activator of nuclear factor kappa B ligand (RANKL)-mediated osteoclast differentiation and bone resorption in vitro and reduces the expression of osteoclast-specific markers. Andrographolide attenuates inflammation by inhibition of TNFα-induced NF-κB activation through covalent modification of reduced Cys62 of p50， without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide also inhibits the ERK/MAPK signalling pathway without affecting p38 or JNK signalling. Andrographolide inhibits osteoclast differentiation of RAW 264.7 cells in a concentration-dependent manner. Andrographolide suppresses osteoclast formation in a concentration-dependent manner without any obvious cytotoxic effects， in both BMMs and RAW 264.7 cells. Andrographolide treatment substantially reduces the area of bone resorption. Only approximately 30% of the bone resorption observed in the control group is achieved after treatment with 2.5?μM Andrographolide. Osteoclastic bone resorption is almost completely inhibited after treatment with 10?μM Andrographolide[1]. |
| In Vivo |
Treatment with Andrographolide (5 or 30?mg/kg) reduces the extent of bone loss induced by LPS. Moreover， Andrographolide slightly increases the BMD and cortex thickness compared to LPS treatment. Histological examination confirms the protective effects of Andrographolide on LPS-induced bone loss. LPS injection leads to inflammatory bone erosion and increased numbers of TRAP-positive osteoclasts[1]. |
| 细胞实验 |
Effects of Andrographolide on cell proliferation are determined with a CCK-8. BMMs are plated in 96-well plates at a density of 3×103 cells per well in triplicate. Twenty-four hours later， the cells are treated with increasing concentrations of Andrographolide (0， 2.5， 5， 10 or 20?μM) for 2 days. Next， 10?μL CCK-8 is added to each well， and the plates are then incubated at 37°C for an additional 2?h. The optical density (OD) is then measured with an ELX800 absorbance microplate reader at a wavelength of 450?nm (650?nm reference). The cell viability is calculated[1]. |
| 动物实验 |
Mice[1]
C57BL/6 mice (8 weeks old) are divided into four groups of seven mice each. Mice are injected i.p. with Andrographolide (5 or 30?mg/kg body weight) or PBS as a control 1 day before injection of LPS (5?μg/g body weight). Andrographolide or PBS is injected intraperitoneally every other day for 8 days. LPS is injected intraperitoneally on days one and four. All mice are killed 8 days after the initial LPS injection， and the left femurs of all animals are scanned with a high-resolution micro-CT at a resolution of 9?μm. |
| 激酶实验 |
In vitro osteoclastogenesis assays are preformed to examine the effects of Andrographolide on osteoclast differentiation. Bone marrow macrophages (BMM) cells are prepared. Briefly， cells extracted from the femur and tibiae of a 6-week-old C57/BL6 mouse are incubated in complete cell culture media and 30?ng/mL?M-CSF in a T-75?cm2 flask for proliferation. When changing the medium， the cells are washed in order to deplete residual stromal cells. After reaching 90% confluence， cells are washed with PBS three times and trypsinized for 30?min to harvest BMMs. Cells adhering to the bottom of the dish are classified as BMMs; these BMMs are plated in 96-well plates at a density of 8×103 cells per well in triplicate and incubated in a humidified incubator containing 5% CO2 at 37°C for 24?h. The cells are then treated with various concentrations of Andrographolide (0， 2.5， 5， or 10?μM) plus M-CSF (30?ng/mL) and RANKL (50?ng/mL). After 5 days， cells are fixed and stained for tartrate-resistant acid phosphatase (TRAP) activity. TRAP-positive multinucleated cells with more than five nuclei are counted as osteoclasts[1]. |
| 数据来源文献 |
[1]. Zhai ZJ， et al. Andrographolide suppresses RANKL-induced osteoclastogenesis in vitro and prevents inflammatory bone loss in vivo. Br J Pharmacol. 2014 Feb;171(3):663-75.
[2]. Gupta S， et al. Broad-spectrum antiviral properties of andrographolide. Arch Virol. 2017 Mar;162(3):611-623. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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