白术内酯 I作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAtractylenolide ICat. No.: HY-N0201CAS No.: 73069-13-3分式: CHO分量: 230.3作靶点: Toll-like Receptor (TLR); JAK; STAT作通路: Immunology/Inflammation; Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL

2、 (434.22 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 4.3422 mL 21.7108 mL 43.4216 mL5 mM 0.8684 mL 4.3422 mL 8.6843 mL10 mM 0.4342 mL 2.1711 mL 4.3422 mL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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，

3、请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.86 mM); Clear solution此案可获得 2.5 m

4、g/mL (10.86 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.86 mM); Clear solution此案可获得 2.5 mg/mL (10.86 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChem

5、E以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.86 mM); Clear solution此案可获得 2.5 mg/mL (10.86 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 At

6、ractylenolide I 从术根中得到的倍半萜烯，具有神经保护、抗过敏、抗炎和抗癌等多种物活性。 Atractylenolide I 为 TLR4 的拮抗剂，同时在 A375 细胞中，能够降低 JAK2 和 STAT3 的磷酸化平。IC & Target JAK2, STAT31, TLR44体外研究 Atractylenolide I (40, 60, 80, 100, 120, 150 M) dose- and time-dependently reduces the cell viability in human A375melanoma cells after treatment

7、 for 24, 48 and 72 hours. Atractylenolide I (50 and 100 M) induces apoptosis of A375cells in a dose-dependent manner at 48 h of treatment. Atractylenolide I (100 M) significantly reduces protein levelsof phosphorylated JAK2 and STAT3 in A375 cells, without effect on total JAK2 and STAT3. Furthermore

8、,Atractylenolide I inhibits the mRNA expression of STAT3-targeted genes, including Bcl-xL, MMP-2 and MMP-91.Atractylenolide I (up to 100 M) shows no toxicity in normal cells. Atractylenolide I (25, 50 M) decreases the Ox-LDLinduced TNF-, IL-6 and NO production in VSMCs. Atractylenolide I (12.5, 25 o

9、r 50 M) significantly reduces the levelof MCP-1 and inhibits Ox-LDL-induced VSMCs proliferation and migration. Atractylenolide I (25, 50 M) inhibitspositive staining of foam cells, and also significantly decreases lipid accumulation. Atractylenolide I (50 M)suppresses p38MAPK and NF-B p65 expression

10、 in VSMCs stimulated by Ox-LDL3. Atractylenolide I (1, 10, 100 M)downregulates paclitaxel-induced expression of VEGF and survivin via MyD88-dependent TLR4 signaling in EOC cells4.体内研究 Atractylenolide I (5, 10 or 20 mg/kg, p.o.) restores the decreased body weight in mice subjected to chronicunpredict

11、able mild stress (CUMS). Atractylenolide I alleviates CUMS-induced depressive-like behavior, attenuates CUMS-induced imbalances in hippocampal neurotransmitter levels and reduces CUMS-induced increases inhippocampal pro-inflammatory cytokine levels and in the NLRP3 inflammasome in the hippocampi of

12、mice2.PROTOCOLCell Assay 3 Briefly, serum starved VSMCs are pre-treated with indicated concentration of Atractylenolide I for 1 h followed bystimulation with Ox-LDL for 24 h. The purple formazan crystals formed after addition of MTT are solubilized in DMSOand absorbance is measured at 540 nm. The vi

13、ability or proliferation rate is calculated as percentage of control(untreated VSMCs)3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration 2 After adaption for one week, 48 male ICR mice are randomly divided into six groups (eight

14、 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 20mg/kg) or fluoxetine (20 mg/kg) is daily admini

15、stered by oral gavage for 3 weeks. After the last administration ofAtractylenolide I or fluoxetine, behavioral tests are performed2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Nat Commun. 2019 Mar 4;10(1):1015.See

16、 more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. 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 mo

17、use 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-depe