2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Neuronal Signaling
  3. Apoptosis Reactive Oxygen Species (ROS) α-synuclein Succinate Dehydrogenase Bcl-2 Family Caspase
  4. Tambulin

Tambulin 是一种具有口服活性的黄酮醇类化合物，被发现存在于 Zanthoxylum armatum 中。Tambulin 可抑制细胞增殖，诱导凋亡 (apoptosis) 并抑制活性氧 (ROS) 的产生。Tambulin 上调 cleaved caspase-3、cleaved caspase-9 和 Bax，下调 Bcl-2 水平。Tambulin 可刺激葡萄糖依赖性胰岛素分泌并诱导内皮非依赖性血管舒张。Tambulin 与琥珀酸脱氢酶 (SDH) 结合 (Ki = 11.02 μM)，并表现出显著的铁离子还原能力。Tambulin 可增强氧化应激抵抗力，减少脂褐素沉积、脂质水平和 α-突触核蛋白 (α-synuclein) 水平，改善在年龄同步化的 L1 雌雄同体秀丽隐杆线虫衰老及帕金森病模型中的运动行为和多巴胺水平。Tambulin 可用于帕金森病、肺鳞状细胞癌和糖尿病的研究。

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Tambulin

Tambulin Chemical Structure

CAS No. : 571-72-2

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Tambulin 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tambulin is an orally active flavonol compound found in Zanthoxylum armatum. Tambulin can inhibit cell proliferation, induce apoptosis and inhibit ROS production. Tambulin upregulates cleaved caspase-3, cleaved caspase-9, and Bax, downregulates Bcl-2 levels. Tambulin can stimulate glucose-dependent insulin secretion and induce endothelium-independent vasorelaxation. Tambulin binds to succinate dehydrogenase (SDH) (Ki = 11.02 μM) and shows significant ferric reducing power. Tambulin can enhances oxidative stress resistance, reduces, lipofuscin deposits, lipid levels, α-synuclein levels, improves locomotary behavior, and dopamine levels in in age-synchronized L1 hermaphrodite Caenorhabditis elegans models of ageing and Parkinson's disease. Tambulin can be used for the researches of Parkinson's disease, lung squamous cell carcinoma, and diabetes[1][2][3][4][5].

IC50 & Target[2]

Caspase 3

 

Caspase-9

 

Bcl-2

 

Bax

 

体外研究
(In Vitro)

Tambulin (5-80 μg/mL; 12-48 h) 抑制 H226 和 H520 LSCC 细胞的增殖[2]。
Tambulin (40 μg/mL) 诱导 H226 和 H520 LSCC 细胞凋亡，该效应被 HDAC1 过表达减弱[2]。
Tambulin (40 μg/mL) 降低 H226 和 H520 LSCC 细胞中 HDAC1 和 Bcl-2 的表达，并增加 cleaved-caspase-3、9 和 Bax 的水平，这些效应被 HDAC1 过表达逆转[2]。
Tambulin (100-400 µM; 60 min) 刺激分离的小鼠胰岛和 MIN6 细胞的葡萄糖依赖性胰岛素分泌[3]。
Tambulin (30 min) 诱导猪冠状动脉环的内皮非依赖性血管舒张 (EC50 = 1.81 μM (去除内皮环)，2.18 μM (完整内皮环))[4]。
Tambulin (1 μM; 30 min) 增强由 Isoproterenol (HY-B0468)、Forskolin (HY-15371) 和 Sodium nitroprusside (HY-B0564) 诱导的内皮细胞非依赖性舒张[4]。
Tambulin (1-10 μM; 30 min) 以浓度依赖性方式抑制 KCl、5-HT、CaCl2 和 U46619 (HY-108566) 诱导的收缩[4]。
Tambulin (1 μM; 30 min) 不影响由 Bradykinin (HY-P0206)、A23187、钾通道激活剂 Levcromakalim (HY-14255) 和 1-EBIO (HY-101360) 以及 NO 非依赖性 sGC 激活剂 YC-1 (HY-14927) 和 BAY 41-2272 (HY-12376) 诱导的内皮松弛[4]
Tambulin (10-50 μg/mL; 24 h) 抑制多种癌细胞和角质形成细胞系的增殖[5]。
Tambulin 与琥珀酸脱氢酶 (SDH) 强力相互作用 (Ki = 11.02 μM)[5]。
Tambulin (10-50 μg/mL) 显示显著的铁还原能力[5]。

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

Tambulin 相关抗体:

Cell Proliferation Assay[2]

Cell Line: H226, H520 cells
Concentration: 5-80 μg/ml
Incubation Time: 12, 24, 48 h
Result: Inhibited H226 and H520 cell proliferation in a dose- and time-dependent manner with IC₅₀ values of 53.02 μg/ml (12 h), 40.86 μg/ml (24 h), 36.61 μg/ml (48 h) for H226 and 52.71 μg/ml (12 h), 39.95 μg/ml (24 h), 36.90 μg/ml (48 h) for H520.

Cell Proliferation Assay[5]

Cell Line: MCF-7, WRL-68, COLO-205, MDA-MB-231, HaCaT
Concentration: 10, 20 and 50 μg/mL
Incubation Time: 24 h
Result: Exhibited antiproliferative activity against tested cell lines with IC₅₀ values of 39.43, 37.96, 45.84, 39.77 and 48.7 μg/mL.
体内研究
(In Vivo)

Tambulin (25-100 μM) 延长寿命，增强氧化应激抵抗力，降低 ROS 水平、脂褐素沉积、蛋白羰基含量、脂质水平、α-突触核蛋白水平和细胞凋亡，改善运动行为、咽泵频率和多巴胺水平，并上调年龄同步化的 L1 雌雄同体秀丽隐杆线虫衰老和帕金森病模型中的基因表达[1]。
Tambulin (20-80 mg/kg; p.o.; daily; 28 days) 抑制雄性 Balb/c 裸鼠肺鳞状细胞癌 CDX 肿瘤生长[2]。

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

Animal Model: age-synchronized L1 hermaphrodite Caenorhabditis elegans models of ageing and Parkinson's disease[1]
Dosage: 25, 50, 100 μM
Administration: Incubation until death
Result: Increased mean lifespan of wild-type worms by 16.79% (23.336 ± 0.565 days vs. 19.981 ± 0.589 days control) at 50 μM.
Enhanced oxidative stress resistance (90% survival at 50 μM vs. 60% control).
Reduced intracellular ROS levels (40.9225 ± 1.99 RFU at 50 μM vs. control) and decreased lipofuscin deposits (117.817 ± 10.438 RFU vs. 166.448 ± 12.98 RFU control) and protein carbonyl content (57.377 ± 1.96% vs. control).
Upregulated mRNA expression of sod-1, sod-3, ctl-2, and daf-16 and increased lifespan of daf-16 mutant worms by 3.46% at 50 μM.
Reduced lipid levels in wild-type (90.10 ± 1.54 RFU vs. 106.8 ± 4.63 RFU control) and NL5901 worms (76.0 ± 1.95 RFU vs. 87.92 ± 1.68 RFU control).
Enhanced locomotary behavior (body bends: 7.66 ± 0.167 in N2, 7.875 ± 0.154 in NL5901 vs. 6.71 ± 0.18 and 6.56 ± 0.29 control; head thrashes: 166.5 ± 1.46 in N2, 168.1 ± 2.39 in NL5901 vs. 158.7 ± 2.02 and 153.8 ± 0.263 control).
Increased pharyngeal pumping (65.00 ± 0.75 in N2, 65.36 ± 0.67 in NL5901 vs. 60.45 ± 1.03 and 60.09 ± 0.73 control).
Decreased apoptosis (average score: 2.17 ± 0.025 in N2, 3.07 ± 0.075 in NL5901 vs. 2.87 ± 0.075 and 3.5 ± 0.05 control) and reduced α-synuclein levels (24.0289 ± 0.877 RFU vs. 29.81 ± 1.03 RFU control).
Augmented dopamine levels (9.04 ± 0.065 ng/ml in N2, 11.49 ± 0.04 ng/ml in NL5901 vs. 7.70 and 7.137 ng/ml control) and upregulated mRNA expression of lagr-1, pdr-1, lrk-1, ubc-12, and ymel-1 in NL5901 worms.
Animal Model: Balb/c nude mice (male, 4 to 6 weeks old, 18 to 22 g, CDX model with H226 or H520 cells)[2]
Dosage: 20, 40, 80 mg/kg
Administration: p.o.; daily; 28 days
Result: Inhibited H226 and H520 CDX tumor growth in a dose-dependent manner with 80 mg/kg being the most effective.
Combined with Cisplatin (HY-17394) to inhibit tumor growth more significantly than either agent alone.
Downregulated HDAC1 and Bcl-2 expression, and upregulated cleaved caspase-3 and Bax expression; these effects were reversed by HDAC1 overexpression.
分子量

344.32

Formula

C18H16O7
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

Tambulin 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tambulin571-72-2ApoptosisReactive Oxygen Species (ROS)α-synucleinSuccinate DehydrogenaseBcl-2 FamilyCaspaseα-SynMCF-7WRL-68COLO-205MDA-MB-231HaCaTH226H520Balb/c
Inhibitorinhibitorinhibit

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