CAS |
73069-13-3 |
Chinese Name |
白术内酯Ⅰ |
English Name |
Atractylenolide I |
Synonyms |
白术油 |
Molecular Formula |
C15H18O2 |
Molecular Weight |
230.3 |
Solubility |
Soluble in DMSO |
Purity |
HPLC≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL |
MFCD09037395 |
SMILES |
O=C1C(C)=C(C[C@@]23[H])C(O1)=C[C@@]3(C)CCCC2=C |
InChIKey |
ZTVSGQPHMUYCRS-SWLSCSKDSA-N |
InChI |
InChI=1S/C15H18O2/c1-9-5-4-6-15(3)8-13-11(7-12(9)15)10(2)14(16)17-13/h8,12H,1,4-7H2,2-3H3/t12-,15+/m0/s1 |
PubChem CID |
5321018 |
Target Point |
Toll-like Receptor (TLR) |
Passage |
Immunology & Inflammation |
Background |
Atractylenolide I, a sesquiterpene, is an antagonist of TLR4 with neuroprotective, antiallergic, anti-inflammatory and anticancer activities. |
Biological Activity |
Atractylenolide I 具有神经保护、抗过敏、抗炎和抗癌等多种生物活性。Atractylenolide I 为 TLR4 的拮抗剂,同时在 A375 细胞中,能够降低 JAK2 和 STAT3 的磷酸化水平。[1-4] |
In Vitro |
在处理24,48和72小时后,白术内酯I(40,60,80,100,120,150μM)剂量和时间依赖性地降低人A375黑素瘤细胞的细胞活力。 Atractylenolide I(50和100μM)在处理48小时时以剂量依赖性方式诱导A375细胞的凋亡。 Atractylenolide I(100μM)显着降低A375细胞中磷酸化JAK2和STAT3的蛋白质水平,而不影响总JAK2和STAT3。此外,Atractylenolide I抑制STAT3靶向基因的mRNA表达,包括Bcl-xL,MMP-2和MMP-9 [1]。 Atractylenolide I(高达100μM)在正常细胞中没有毒性。白术内酯I(25,50μM)降低血管平滑肌细胞中Ox-LDL诱导的TNF-α,IL-6和NO产生。 Atractylenolide I(12.5,25或50μM)显着降低MCP-1的水平并抑制Ox-LDL诱导的VSMC增殖和迁移。 Atractylenolide I(25,50μM)抑制泡沫细胞的阳性染色,并且还显着降低脂质积累。 Atractylenolide I(50μM)抑制ox-LDL刺激的VSMCs中p38MAPK和NF-κBp65的表达[3]。 Atractylenolide I(1,10,100μM)通过EOC细胞中的MyD88依赖性TLR4信号传导下调紫杉醇诱导的VEGF和survivin的表达[4]。 |
In Vivo |
白术内酯I(5,10或20mg / kg,po)恢复经历慢性不可预测的轻度应激(CUMS)的小鼠体重减轻。 Atractylenolide I减轻CUMS诱导的抑郁样行为,减轻CUMS诱导的海马神经递质水平失衡,并减少CUMS诱导的海马促炎细胞因子水平增加和小鼠海马NLRP3炎症小体的增加[2]。 |
Cell Experiment |
简而言之,用指定浓度的白术内酯I预处理血清饥饿的VSMC 1小时,然后用Ox-LDL刺激24小时。加入MTT后形成的紫色甲crystals晶体溶解在DMSO中,在540nm处测量吸光度。活力或增殖率计算为对照(未治疗的VSMC)的百分比[3]。 |
Animal Experiment |
小鼠[2]适应一周后,将48只雄性ICR小鼠随机分成6组(每组8只小鼠):对照组(无应激+盐水载体),模型组(CUMS +盐水载体),三种Atractylenolide I治疗组(CUMS + Atractylenolide I)和氟西汀组(CUMS + FLU)。从第4周起,每天通过口服强饲法给予Atractylenolide I(5,10或20mg / kg)或氟西汀(20mg / kg)3周。在最后一次施用Atractylenolide I或氟西汀后,进行行为测试[2]。 |
Data Literature Source |
[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. |
Unit |
Bottle |
Specification |
5mg 10mM*1mL in DMSO 10mg |