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My CartCAS：20554-84-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 20554-84-1 |
| Name | Parthenolide |
| Molecular Formula | C15H20O3 |
| Molecular Weight | 248.32 |
| 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 |
| EC | EINECS 692-532-0 |
| MDL | MFCD00134592 |
| SMILES | C/C1=C\CC[C@@](C)(O2)[C@H]2[C@@H](OC(C3=C)=O)[C@H]3CC1 |
| InChIKey | KTEXNACQROZXEV-PVLRGYAZSA-N |
| InChI | InChI=1S/C15H20O3/c1-9-5-4-8-15(3)13(18-15)12-11(7-6-9)10(2)14(16)17-12/h5,11-13H,2,4,6-8H2,1,3H3/b9-5+/t11-,12-,13+,15+/m0/s1 |
| PubChem CID | 7251185 |
| Target Point | NF-KB |
| Passage | NF-κB |
| Background | Parthenolide is a sesquiterpene lactone. Parthenolide showed anti-inflammatory activity by inhibiting NF-κB activation. Parthenolide also specifically inhibits HDAC1 protein without affecting other Class I/II HDacs. |
| Biological Activity | Parthenolide 是一种 NF-κB 抑制剂，可降低组蛋白脱乙酰酶 1 (HDAC-1) 和 DNA 甲基转移酶 1。[1-3] |
| In Vitro | 小白菊内酯(PTL)对NSCLC细胞Calu-1，H1792，A549，H1299，H157和H460具有剂量依赖性生长抑制作用。在测试的肺癌细胞中，小白菊内酯可以浓度和时间依赖性方式诱导凋亡蛋白如CASP8，CASP9，CASP3和PARP1的切割，表明在小白菊内酯暴露后触发细胞凋亡。除诱导细胞凋亡外，小白菊内酯还在A549细胞中以浓度依赖性方式诱导G0/G1细胞周期停滞，在H1792细胞中诱导G2/M细胞周期停滞[2]。 |
| In Vivo | 只有具有抗炎特征的HDAC抑制剂小白菊内酯在Phb1 KO肝细胞中显示出有效的抗细胞凋亡作用。实际上，TSA和小白菊内酯处理的肝细胞显示FXR水平增加，CYP7A1，HDAC4，TNFα，TRAIL和Bax水平降低，表明胆汁酸作为特异性HDAC抑制作用的毒性作用较小，导致Phb1的衰减。 KO肝细胞凋亡反应。重要的是，在Phb1 KO小鼠中，小白菊内酯对BDL后的肝损伤具有保护作用。实际上，小白蛋白治疗导致BDL后死亡率降低，并伴有较低的细胞凋亡反应，如坏死区域减少，Tunel染色以及ALT降低所示(8431±957 vs.4225±210)与对照Phb1 KO小鼠相比，U/L)和AST(4805±300 vs.2242±438 U/L)活性[3]。 |
| Cell Experiment | 将人肺癌细胞系接种在96孔板中，并在第二天用给定浓度的小白菊内酯(0，5，10，20μM)处理另外48小时，然后进行SRB或MTT测定。对于SRB测定，如前所述估计活细胞数。处理后，首先丢弃培养基。为了固定贴壁细胞，向每个孔中加入100μL冷的三氯乙酸(10％(w/v))并在4℃下孵育至少1小时。然后将板用去离子水洗涤五次并在空气中干燥。然后向每个孔中加入50μLSRB溶液(0.4％w/v在1％乙酸中)并在室温下温育5分钟。将板用1％乙酸洗涤五次以除去未结合的SRB，然后空气干燥。将残留的结合的SRB用100μL的10mM Tris碱缓冲液(pH 10.5)溶解，然后使用微量滴定板读数器在495nm处读数。执行MTT测定。向每个样品中加入20μLMTT(5mg/mL)并在37℃下孵育4小时，然后加入100μL溶解溶液。细胞活力在595nm处确定[2]。 |
| Animal Experiment | 使用小鼠[3] Phb1 KO小鼠。治疗8-12周龄的男性。在胆管结扎(BDL)前24小时和1小时腹膜内注射小白菊内酯，或在两周内每周两次腹膜内注射小白菊内酯。将肝脏标本快速冷冻用于后续分析[3]。 |
| Data Literature Source | [1]. Nakshatri H，et al. NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DMAPT. Cell Death Dis. 2015 Jan 22;6:e1608. [2]. Zhao X，et al. Parthenolide induces apoptosis via TNFRSF10B and PMAIP1 pathways in human lung cancer cells. J Exp Clin Cancer Res. 2014 Jan 6;33:3. [3]. Barbier-Torres L，et al. Histone deacetylase 4 promotes cholestatic liver injury in the absence of prohibitin-1. Hepatology. 2015 Oct;62(4):1237-48 |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg |
Parthenolide 是一种 NF-κB 抑制剂，可降低组蛋白脱乙酰酶 1 (HDAC-1) 和 DNA 甲基转移酶 1。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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