Andrographolide
(Synonyms: 穿心莲内酯; Andrographis) 目录号 : GN10718
An inhibitor of NF-κB signaling
Cas No.:5508-58-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 11.0 ± 0.28 μg/ml for α-glucosidase; 11.3 ± 0.29 μg/ml for α-amylase
Andrographolide is an irreversible antagonist of NF-κB. The nuclear factor NF-κB pathway has been considered as a prototypical proinflammatory signaling pathway, based on the role of NF-κB in the expression of proinflammatory genes including chemokines, cytokines and adhesion molecules.
In vitro: Andrographolide was found to suppress the expression of inducible nitric oxide synthase in a concentration-dependent manner. In the andrographolide-treated group, a reduction of Akt, c-Jun N-terminal kinase and p65 phosphorylation was observed. Andrographolide also caused a decrease in Bcl-2/NF-κb expression and a dose-dependent increase in the expression of Cleaved-Caspase3/Bax protein [1].
In vivo: Rats were dosed with andrographolide intragastrically for 5 consecutive days in a hepatoprotection study. Results indicated that andrographolide could up-regulate glutamate cysteine ligase catalytic and modifier subunits, heme oxygenase-1, superoxide dismutase-1, glutathione S-transferase protein and mRNA expression in the heart, liver, and kidney [2].
Clinical trial: N/A
References:
[1] Wang ZM,Kang YH,Yang X,Wang JF,Zhang Q,Yang BX,Zhao KL,Xu LP,Yang LP,Ma JX,Huang GH,Cai J,Sun XC. Andrographolide radiosensitizes human esophageal cancer cell line ECA109 to radiation in vitro. Dis Esophagus.2016 Jan;29(1):54-61.
[2] Chen HW,Huang CS,Li CC,Lin AH,Huang YJ,Wang TS,Yao HT,Lii CK. Bioavailability of andrographolide and protection against carbon tetrachloride-induced oxidative damage in rats. Toxicol Appl Pharmacol.2014 Oct 1;280(1):1-9.
Kinase experiment: | 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]. |
Cell experiment: | 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]. |
Animal experiment: | 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. |
References: [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. | |
| Cas No. | 5508-58-7 | SDF | |
| 别名 | 穿心莲内酯; Andrographis | ||
| 化学名 | (3E,4S)-3-[2-[(1R,4aS,5R,6R,8aS)-6-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidene-3,4,4a,6,7,8-hexahydro-1H-naphthalen-1-yl]ethylidene]-4-hydroxyoxolan-2-one | ||
| Canonical SMILES | CC12CCC(C(C1CCC(=C)C2CC=C3C(COC3=O)O)(C)CO)O | ||
| 分子式 | C20H30O5 | 分子量 | 350.44 |
| 溶解度 | ≥ 16mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8536 mL | 14.2678 mL | 28.5356 mL |
| 5 mM | 0.5707 mL | 2.8536 mL | 5.7071 mL |
| 10 mM | 0.2854 mL | 1.4268 mL | 2.8536 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >98.50%
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