Atractylenolide I
(Synonyms: 白术内酯 I) 目录号 : GN10627A sesquiterpene with diverse biological activities
Cas No.:73069-13-3
Sample solution is provided at 25 µL, 10mM.
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
Atractylenolide I (40, 60, 80, 100, 120, 150 μM) dose- and time-dependently reduces the cell viability in human A375 melanoma cells after treatment for 24, 48 and 72 hours. Atractylenolide I (50 and 100 μM) induces apoptosis of A375 cells in a dose-dependent manner at 48 h of treatment. Atractylenolide I (100 μM) significantly reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, without effect on total JAK2 and STAT3. Furthermore, Atractylenolide I inhibits the mRNA expression of STAT3-targeted genes, including Bcl-xL, MMP-2 and MMP-9[1]. Atractylenolide I (up to 100 μM) shows no toxicity in normal cells. Atractylenolide I (25, 50 μM) decreases the Ox-LDL induced TNF-α, IL-6 and NO production in VSMCs. Atractylenolide I (12.5, 25 or 50 μM) significantly reduces the level of MCP-1 and inhibits Ox-LDL-induced VSMCs proliferation and migration. Atractylenolide I (25, 50 μM) inhibits positive staining of foam cells, and also significantly decreases lipid accumulation. Atractylenolide I (50 μM) suppresses p38MAPK and NF-κB p65 expression in VSMCs stimulated by Ox-LDL[3]. Atractylenolide I (1, 10, 100 μM) downregulates paclitaxel-induced expression of VEGF and survivin via MyD88-dependent TLR4 signaling in EOC cells[4].
Atractylenolide I (5, 10 or 20 mg/kg, p.o.) restores the decreased body weight in mice subjected to chronic unpredictable mild stress (CUMS). Atractylenolide I alleviates CUMS-induced depressive-like behavior, attenuates CUMS-induced imbalances in hippocampal neurotransmitter levels and reduces CUMS-induced increases in hippocampal pro-inflammatory cytokine levels and in the NLRP3 inflammasome in the hippocampi of mice[2].
References:
[1]. Atractylenolide I, et al. The JAK2/STAT3 pathway is involved in the anti-melanoma effects of atractylenolide I. Exp Dermatol. 2018 Feb;27(2):201-204.
[2]. Gao H, et al. Anti-depressant-like effect of atractylenolide I in a mouse model of depression induced by chronic unpredictable mild stress. Exp Ther Med. 2018 Feb;15(2):1574-1579.
[3]. Li W, et al. Atractylenolide I restores HO-1 expression and inhibits Ox-LDL-induced VSMCs proliferation, migration and inflammatory responses in vitro. Exp Cell Res. 2017 Apr 1;353(1):26-34.
[4]. Huang JM, et al. Atractylenolide-I sensitizes human ovarian cancer cells to paclitaxel by blocking activation of TLR4/MyD88-dependent pathway. Sci Rep. 2014 Jan 23;4:3840.
Cell experiment: |
Briefly, serum starved VSMCs are pre-treated with indicated concentration of Atractylenolide I for 1 h followed by stimulation with Ox-LDL for 24 h. The purple formazan crystals formed after addition of MTT are solubilized in DMSO and absorbance is measured at 540 nm. The viability or proliferation rate is calculated as percentage of control (untreated VSMCs)[3]. |
Animal experiment: |
Mice[2]After adaption for one week, 48 male ICR mice are randomly divided into six groups (eight mice per group): Control group (unstressed + saline vehicle), model group (CUMS + saline vehicle), three Atractylenolide I treatment groups (CUMS + Atractylenolide I) and a fluoxetine group (CUMS + FLU). From the 4th week, Atractylenolide I (5, 10 or 20 mg/kg) or fluoxetine (20 mg/kg) is daily administered by oral gavage for 3 weeks. After the last administration of Atractylenolide I or fluoxetine, behavioral tests are performed[2]. |
References: [1]. Atractylenolide I, et al. The JAK2/STAT3 pathway is involved in the anti-melanoma effects of atractylenolide I. Exp Dermatol. 2018 Feb;27(2):201-204. |
Cas No. | 73069-13-3 | SDF | |
别名 | 白术内酯 I | ||
化学名 | (4aS,8aS)-3,8a-dimethyl-5-methylidene-4a,6,7,8-tetrahydro-4H-benzo[f][1]benzofuran-2-one | ||
Canonical SMILES | CC1=C2CC3C(=C)CCCC3(C=C2OC1=O)C | ||
分子式 | C15H18O2 | 分子量 | 230.13 |
溶解度 | DMF: 2 mg/ml,DMSO: 2 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.09 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at 2-8°C,protect from light |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.3454 mL | 21.7269 mL | 43.4537 mL |
5 mM | 0.8691 mL | 4.3454 mL | 8.6907 mL |
10 mM | 0.4345 mL | 2.1727 mL | 4.3454 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
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 | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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