2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage Epigenetics
  3. Phosphodiesterase (PDE) Apoptosis NO Synthase Caspase PPAR Bcl-2 Family PARP
  4. S-Petasin

S-Petasin 是一种磷酸二酯酶 (PDE) 抑制剂，对 PDE3 和 PDE4 的 IC50 值分别为 25.5 μM 和 17.5 μM。S-Petasin 可抑制胆固醇侧链裂解酶、11β-羟化酶、PPAR-γ，以及 iNOS 在 RNA 和蛋白水平的诱导表达。S-Petasin 可诱导 apoptosis、激活 caspases、切割 PARP、调控线粒体膜通透性，并调节 BCL2/BAX、p53、Bcl-XL、MMP-2、MMP-9、p21、CDK4 和 cyclin D1 的表达。S-Petasin 可减少炎症细胞聚集、细胞因子和 IgE 水平，并提升血清 IgG2a 水平。S-Petasin 可舒张分离的致敏豚鼠气管肌，且具有胃肠道解痉活性。S-Petasin 可降低扁桃体炎严重程度和哮喘发作频率。S-Petasin 可用于前列腺癌、肥胖症、黑色素瘤、过敏性哮喘、哮喘和腹膜炎的研究。

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S-Petasin

S-Petasin Chemical Structure

CAS No. : 70238-51-6

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S-Petasin 相关抗体

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis[1][2][3][4][5].

IC50 & Target[4][2][5]

PDE3

25.5 μM (IC50)

PDE4

17.5 μM (IC50)

PDE3

25.3 μM (Ki)

PDE4

18.1 μM (Ki)

PPARγ

 

iNOS

 

体外研究
(In Vitro)

S-Petasin (10 nM-10 μM; 3-4 days) 呈剂量依赖性抑制 LNCaP、DU145 和 PC3 人前列腺癌细胞的增殖[1]。
S-Petasin (0.1-10 μM; 12-18 h) 可激活胱天蛋白酶级联反应并诱导 LNCaP、DU145 和 PC3 人前列腺癌细胞中的 PARP 裂解，这与细胞凋亡的诱导一致[1]。
S-Petasin (0.1-10 μM; 8-12 h) 可诱导人前列腺癌细胞 LNCaP、DU145 和 PC3 发生线粒体膜通透性破坏、细胞色素 c 释放，调控 BCL2 家族蛋白及 p53 的表达，从而触发线粒体介导的细胞凋亡[1]。
S-petasin (0.31-1.55 μM; 8 days) 可剂量依赖性地抑制 3T3-L1 前脂肪细胞分化和葡萄糖摄取，在最高测试浓度下可将脂质积累量降至 30.18%[2]。
S-petasin (0.31-1.55 μM; 8 days) 可剂量依赖性地抑制分化的 3T3-L1 脂肪细胞中甘油三酯的积累，在最高测试浓度下可将 TG 含量降至 61.04 %[2]。
S-petasin (0.31-1.55 μM) 可剂量依赖性地抑制 3T3-L1 细胞中 PPAR-γ 的表达，且分化处理 8 天后的抑制作用强于处理 24 h 后的作用[2]。
S-petasin (0.31-1.55 μM; 8 days) 可剂量依赖性地抑制分化的 3T3-L1 脂肪细胞中 PPAR-γ 靶基因 (HMGCR、FAS、CD36、Glut4、A-FABP、LPL) 的表达[2]。
S-Petasin (2-160 μM; 24 h) 经 MTT 实验检测，在处理 24 h 后可强效抑制 B16F10 细胞 (IC50 = 42.16 μM) 和 A375 细胞 (IC50 = 36.90 μM) 的增殖[3]。
S-Petasin (10-40 μM; 24 h) 经 Annexin V/PI 流式细胞术检测，在处理 24 h 后可呈浓度依赖性诱导 B16F10 细胞和 A375 细胞凋亡[3]。
S-Petasin (10-40 μM; 24 h) 可通过下调促凋亡前体蛋白、上调 caspase 9、caspase 3 和 PARP-1 的活化剪切产物，在处理 24 h 后诱导 B16F10 细胞和 A375 细胞发生凋亡[3]。
S-Petasin (10-40 μM; 24 h) 可通过降低细胞核内 NF-κB、MMP-2、MMP-9、Bcl-2、Bcl-xL、CDK4 及 cyclin D1 的表达，同时上调 Bax 和 p21 的表达，以浓度依赖的方式调控 B16F10 细胞和 A375 细胞中经 24 h 处理后的下游 p53 靶基因表达[3]。
S-Petasin (4-40 μM; up to 24 h) 可通过划痕愈合实验检测到，其在 24 小时内以浓度依赖的方式抑制 B16F10 细胞和 A375 细胞的迁移[3]。
S-Petasin (4-40 μM; 24 h) 经 24 h 处理后，以浓度依赖的方式抑制 B16F10 细胞和 A375 细胞通过 Max Gel ECM 的侵袭能力[3]。
S-Petasin (10-40 μM; 24 h) 可在处理 24 h 后，以浓度依赖的方式在 B16F10 细胞和 A375 细胞中激活 p53 在 mRNA 和蛋白水平的表达[3]。
S-Petasin (1-100 μM; 30 min) 可竞争性抑制豚鼠肺和心脏中的 PDE3 和 PDE4，对应的 IC50 值分别为 25.5 μM 和 17.5 μM；且在浓度高达 100 μM 时，不会抑制 PDE1、PDE2 或 PDE5[4]。
S-Petasin 可强效抑制 RBL-2H3 肥大细胞中抗原诱导的脱颗粒作用，其 IC50 约为 1 nM[5]。
S-Petasin (1-10 μM; 1 h preincubation, 24 h LPS stimulation) 可浓度依赖性地抑制 LPS 诱导的小鼠腹腔巨噬细胞 iNOS 蛋白和 mRNA 表达、NO 和 PGE2 生成[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

S-Petasin 相关抗体:

Western Blot Analysis[1]

Cell Line: LNCaP, DU145, PC3 (human prostate cancer cell lines)
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 12, 18 h
Result: Reduced levels of procaspase 3, 7, 8, and 9 in LNCaP cells after 12 and 18 h.
Reduced levels of procaspase 3, 8, and 9 in DU145 cells after 12 and 18 h (procaspase 7 levels were unchanged).
Reduced levels of procaspase 3, 7, 8, and 9 in PC3 cells after 12 and 18 h.
Induced dose-dependent cleavage of PARP in all three cell lines after 12 and 18 h.

Western Blot Analysis[1]

Cell Line: LNCaP, DU145, PC3 (human prostate cancer cell lines)
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 8, 12 h
Result: Increased release of cytochrome c from mitochondria in LNCaP cells after 8 and 12 h.
Increased release of cytochrome c from mitochondria, downregulated BCL2, and downregulated p53 in PC3 cells after 8 and 12 h.
Increased release of cytochrome c from mitochondria, upregulated p53, upregulated BAX, downregulated BCL2, and induced BAX translocation in DU145 cells after 8 and 12 h.

Apoptosis Analysis[3]

Cell Line: B16F10 murine melanoma cells, A375 human melanoma cells
Concentration: 10-40 μM
Incubation Time: 24 h
Result: Increased the proportion of Annexin V and PI positive cells in a concentration-dependent manner in both B16F10 and A375 cells.

Western Blot Analysis[3]

Cell Line: B16F10 murine melanoma cells, A375 human melanoma cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 24 h
Result: Decreased expression of pro-caspase 9, pro-caspase 3, and pro-PARP-1, while upregulated expression of cleaved-caspase 9, cleaved-caspase 3, and cleaved-PARP-1 in both B16F10 and A375 cells.\nDecreased nuclear NF-κB expression and suppressed MMP-2 and MMP-9 expression in a dose-dependent manner in both B16F10 and A375 cells.
Downregulated Bcl-2 and Bcl-xL expression, while upregulating Bax expression in a dose-dependent manner in both B16F10 and A375 cells.
Upregulated p21 expression, while suppressing CDK4 and cyclin D1 expression in a dose-dependent manner in both B16F10 and A375 cells.

Cell Migration Assay[3]

Cell Line: B16F10 murine melanoma cells, A375 human melanoma cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 24 h
Result: Reduced the number of migrated B16F10 and A375 cells in a dose-dependent manner, with statistically significant inhibition at all tested concentrations.

Cell Invasion Assay[3]

Cell Line: B16F10 murine melanoma cells, A375 human melanoma cells
Concentration: 4 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 24 h
Result: Reduced the number of invaded B16F10 and A375 cells in a dose-dependent manner, with statistically significant inhibition at all tested concentrations.
体内研究
(In Vivo)

S-Petasin (10-30 μmol/kg (3.3-9.9 mg/kg); s.c.; 2 hours before, 6 and 24 hours after secondary OVA provocation) 可在过敏性哮喘小鼠模型中呈剂量依赖性地显著减轻气道高反应性、减少炎症细胞浸润、抑制促炎细胞因子的产生并调节免疫球蛋白水平[4]。
S-Petasin (1 mg/kg; i.p.; 1 h before each ovalbumin nebulization) 可抑制卵清蛋白诱导的 BALB/c 小鼠支气管肺泡灌洗液中嗜酸性粒细胞、巨噬细胞和淋巴细胞的聚集，与未接受治疗的哮喘小鼠相比，其总细胞计数降低了 80%[5]。
S-Petasin (1 mg/kg; i.p.; single dose 1 h prior to LPS injection) 可减少 LPS 诱导的 C57BL/6 小鼠腹腔总细胞、多形核白细胞及单核白细胞的聚集[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (female, 8-12 weeks old, allergic asthma model via OVA sensitization and challenge)[4]
Dosage: 10 μmol/kg; 30 μmol/kg
Administration: s.c.; 2 hours before, 6 and 24 hours after secondary OVA provocation
Result: Attenuated the enhanced pause (P_enh) value induced by 50 mg/mL methacholine in a dose-dependent and significant manner.
Suppressed increases in total inflammatory cells, neutrophils, and eosinophils in BALF in a significant manner.
Suppressed increases in lymphocytes in BALF at 30 μmol/kg dose, while 10 μmol/kg dose had no effect.
Left macrophage counts in BALF unchanged at both doses.
Suppressed increases in BALF levels of IL-2, IL-5, TNF-α, and IFN-γ in a significant manner at both doses.
Suppressed increases in BALF IL-4 levels at 30 μmol/kg dose, while 10 μmol/kg dose had no effect.
Reversed the reduction in serum total IgG2a levels in a significant manner at 30 μmol/kg dose.
Suppressed increases in serum total IgE, serum OVA-specific IgE, and BALF OVA-specific IgE in a dose-dependent and significant manner at both doses.
Suppressed increases in BALF total IgE levels at 30 μmol/kg dose, while 10 μmol/kg dose had no effect.
Animal Model: BALB/c (male, 6-week-old, adapted for 1 week prior to experimentation; asthma induced by intraperitoneal ovalbumin + alum on days 1 and 14, nebulized ovalbumin exposure on days 28-30)[5]
Dosage: 1 mg/kg
Administration: i.p.; 1 h before each ovalbumin nebulization; 3 doses (days 28, 29, 30)
Result: Blunted ovalbumin-induced increase in total BALF cell number by approximately 80%.
Almost completely inhibited accumulation of macrophages and lymphocytes to PBS-treated basal levels.
Inhibited eosinophil accumulation by approximately 36%.
Animal Model: C57BL/6 (peritonitis induced by intraperitoneal 1 mg/kg LPS)[5]
Dosage: 1 mg/kg
Administration: i.p.; single dose 1 h prior to LPS injection
Result: Reduced total peritoneal cell counts by 36% relative to LPS-induced controls.
Inhibited polymorphonuclear leukocyte accumulation by approximately 37%.
Inhibited mononuclear leukocyte accumulation by approximately 42%.
Did not significantly alter macrophage counts.
分子量

334.47

Formula

C19H26O3S
CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

S-Petasin 相关分类

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Keywords:

S-Petasin70238-51-6Phosphodiesterase (PDE)ApoptosisNO SynthaseCaspasePPARBcl-2 FamilyPARPNitric oxide synthasesNOSPeroxisome proliferator-activated receptorspoly ADP ribose polymerasePDE4PPAR-γiNOSB16F10PDE3cholesterol side-chain cleavage enzyme3T3-L1DU14511β-hydroxylaseLNCaPInhibitorinhibitorinhibit

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