Tambulin
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.
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- CAS No.: 571-72-2
- Formule: C18H16O7
- Masse moléculaire:344.32
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Caspase 3 |
Caspase-9 |
Bcl-2 |
Bax |
Tambulin (5-80 μg/mL; 12-48 h) inhibits proliferation of H226 and H520 LSCC cells[2].
Tambulin (40 μg/mL) induces apoptosis of H226 and H520 LSCC cells, an effect attenuated by HDAC1 overexpression[2].
Tambulin (40 μg/mL) reduces HDAC1 and Bcl-2 expression and increases cleaved-caspase-3, 9 and Bax levels in H226 and H520 LSCC cells, effects reversed by HDAC1 overexpression[2].
Tambulin (100-400 µM; 60 min) stimulates glucose-dependent insulin secretion in solated mice islets and MIN6 cells[3].
Tambulin (30 min) induces endothelium-independent vasorelaxation in porcine coronary artery rings (EC50 = 1.81 μM (endothelium denuded ring), 2.18 μM (endothelium intact ring))[4].
Tambulin (1 μM; 30 min) enhances endothelium-independent relaxations induced by Isoproterenol (HY-B0468), Forskolin (HY-15371), and Sodium nitroprusside (HY-B0564)[4].
Tambulin (1-10 μM; 30 min) inhibits concentration-dependent contractions induced by KCl, 5-HT, CaCl2, and U46619 (HY-108566)[4].
Tambulin (1 μM; 30 min) does not affect endothelium relaxations induced by Bradykinin (HY-P0206), A23187, potassium channel activators Levcromakalim (HY-14255) and 1-EBIO (HY-101360) and NO-independent sGC activators YC-1 (HY-14927) and BAY 41-2272 (HY-12376)[4].
Tambulin (10-50 μg/mL; 24 h) exhibits antiproliferative activity against multiple cancer and keratinocyte cell lines[5].
Tambulin potently interacts with succinate dehydrogenase (SDH) (Ki = 11.02 μM)[5].
Tambulin (10-50 μg/mL) shows significant ferric reducing power[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H226, H520 cells
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Concentration:5-80 μg/ml
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Incubation Time:12, 24, 48 h
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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.
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Cell Line:MCF-7, WRL-68, COLO-205, MDA-MB-231, HaCaT
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Concentration:10, 20 and 50 μg/mL
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Incubation Time:24 h
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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.
Tambulin (20-80 mg/kg; p.o.; daily; 28 days) inhibits lung squamous cell carcinoma CDX tumor growth in male Balb/c nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:age-synchronized L1 hermaphrodite Caenorhabditis elegans models of ageing and Parkinson's disease[1]
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Dosage:25, 50, 100 μM
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Administration:Incubation until death
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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.
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Animal Model:Balb/c nude mice (male, 4 to 6 weeks old, 18 to 22 g, CDX model with H226 or H520 cells)[2]
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Dosage:20, 40, 80 mg/kg
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Administration:p.o.; daily; 28 days
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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.
Chemical Information
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CAS No. 571-72-2
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Masse moléculaire 344.32
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Formule C18H16O7
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SMILES
O=C1C(O)=C(C2=CC=C(OC)C=C2)OC3=C(C(OC)=CC(O)=C13)OC
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Pandey T, et al. Anti-ageing and anti-Parkinsonian effects of natural flavonol, tambulin from Zanthoxyllum aramatum promotes longevity in Caenorhabditis elegans. Exp Gerontol. 2019;120:50-61. [Content Brief]
[2]. Wang W, et al. Tambulin Targets Histone Deacetylase 1 Inhibiting Cell Growth and Inducing Apoptosis in Human Lung Squamous Cell Carcinoma. Front Pharmacol. 2020;11:1188. Published 2020 Aug 12. [Content Brief]
[3]. Hameed A, et al. Tambulin from Zanthoxylum armatum acutely potentiates the glucose-induced insulin secretion via KATP-independent Ca2+-dependent amplifying pathway. Biomed Pharmacother. 2019 Dec;120:109348. [Content Brief]
[4]. Mushtaq MN, et al.Tambulin is a major active compound of a methanolic extract of fruits of Zanthoxylum armatum DC causing endothelium-independent relaxations in porcine coronary artery rings via the cyclic AMP and cyclic GMP relaxing pathways. Phytomedicine. 2019 Feb;53:163-170. [Content Brief]
[5]. Nooreen Z, et al. Characterization and evaluation of bioactive polyphenolic constituents from Zanthoxylum armatum DC., a traditionally used plant. Biomed Pharmacother. 2017;89:366-375. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tambulin Related Classifications
HY-N17816 Related Classifications
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