1. PI3K/Akt/mTOR Apoptosis Autophagy
  2. mTOR PI3K Akt Apoptosis Autophagy
  3. Houttuynin

Houttuynin (3-Oxododecanal) 是一种口服有效的 mTOR/PI3K/AKT 抑制剂。Houttuynin 可降低 PI3KAKT 的表达及磷酸化水平,同时降低 mTOR 的表达水平,从而抑制 PI3K/AKT 信号通路。Houttuynin 可通过线粒体途径和死亡受体途径诱导细胞凋亡 (apoptosis),将细胞周期阻滞于 G2/M 期并诱导自噬 (autophagy)。Houttuynin 可用于乳腺癌的相关研究。

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Houttuynin

Houttuynin Chemical Structure

CAS No. : 56505-80-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Houttuynin (3-Oxododecanal) is an orally active mTOR/PI3K/AKT inhibitor. Houttuynin reduces expression and phosphorylation levels of PI3K and AKT, and expression levels of mTOR, inhibiting the PI3K/AKT signaling pathway. Houttuynin induces apoptosis via mitochondrial and death receptor pathways, arrests cell cycle in the G2/M phase and induces autophagy. Houttuynin can be used for the research of breast cancer.

体外研究
(In Vitro)

Houttuynin (50-150 μM;24-48 小时) 可呈浓度和时间依赖性抑制人乳腺癌 MCF-7 细胞的活性[1]
Houttuynin (50-150 μM;24 小时) 可呈剂量依赖性诱导 MCF-7 人乳腺癌细胞凋亡[1]
Houttuynin (50-150 μM) 可在体外以剂量依赖方式调控人乳腺癌 MCF-7 细胞中凋亡相关蛋白的表达,上调促凋亡蛋白并下调抗凋亡蛋白 Bcl-2[1]
Houttuynin (50-150 μM) 可在体外以剂量依赖的方式抑制人乳腺癌 MCF-7 细胞中的 PI3K/AKT 信号通路,降低磷酸化 PI3K、AKT、mTOR 及 Bad 蛋白的表达,但不改变总 PI3K、AKT 或 mTOR 的水平[1]

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

Cell Viability Assay[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 50 μM; 100 μM; 150 μM
Incubation Time: 24 h; 48 h
Result: Inhibited MCF-7 cell viability in a concentration- and time-dependent manner, with statistically significant differences observed between each treatment group and the control group.

Apoptosis Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 50 μM; 100 μM; 150 μM
Incubation Time: 24 h
Result: Increased the proportion of early and late apoptotic MCF-7 cells in a dose-dependent manner.
Resulted in a significant increase in apoptotic cells compared to the control group at 150 μM.
Caused a dose-dependent decrease in the number of MCF-7 cells showing green fluorescence (viable cells) and a dose-dependent increase in the number of cells showing red-orange fluorescence (apoptotic cells).
体内研究
(In Vivo)

Houttuynin (100 mg/kg;口服;每日给药,持续 7 周) 可通过抑制过度激活的肾素-血管紧张素-醛固酮系统 (RAAS) 与过氧化作用,减轻大鼠冠状动脉结扎诱导的心室重构[3]

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

Animal Model: Sprague-Dawley (male, 200-220 g, ventricular remodeling induced by left coronary artery ligation)[3]
Dosage: 100 mg/kg
Administration: p.o.; daily; 7 weeks
Result: Increased systolic blood pressure, diastolic blood pressure, left ventricular systolic pressure to 133.05 mmHg, +dP/dtmax to 10,260.45 mmHg/s, and -dP/dtmax to -7202.37 mmHg/s compared to CAL controls.
Reduced left ventricular end-diastolic pressure to 0.22 mmHg compared to CAL controls.
Significantly decreased left ventricular weight index and heart weight index compared to CAL controls.
Reduced cardiomyocyte cross-section area, myocardial interstitial collagen volume fraction, and perivascular collagen volume fraction compared to CAL controls.
Reduced myocardial angiotensin I to 1.43 ng/mL, angiotensin II to 104.79 pg/mL, and endothelin-1 to 60.62 pg/mg·prot concentrations compared to CAL controls.
Reduced serum aldosterone to 1.04 ng/mL concentration compared to CAL controls.
Increased serum nitric oxide concentration to 19.06 μmol/l compared to CAL controls.
Reduced serum hydroxyproline concentration compared to CAL controls.
Increased serum glutathione peroxidase activity and catalase activity to 4.52 U/mL compared to CAL controls.
分子量

198.31

Formula

C12H22O2

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
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Houttuynin
目录号:
HY-134641
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