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.
For research use only. We do not sell to patients.
- CAS No.: 571-72-2
- Formula: C18H16O7
- Molecular Weight:344.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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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Molecular Weight 344.32
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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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