Hyperforin
Based on 3 publication(s) in Google Scholar
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
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- CAS No.: 11079-53-1
- Formula: C35H52O4
- Molecular Weight:536.78
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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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Publications Citing Use of MedChemExpress (MCE) Hyperforin
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Biological Activity
TRPC6[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>40 μM
Compound: 1
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Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25871261] |
| HL-60 | IC50 |
>40 μM
Compound: 1
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Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25871261] |
| MCF7 | IC50 |
>40 μM
Compound: 1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25871261] |
| SMMC-7721 | IC50 |
>40 μM
Compound: 1
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Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25871261] |
| SW480 | IC50 |
>40 μM
Compound: 1
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Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25871261] |
Hyperforin has a multi-directional mechanism of action. It blocks conductance of ligand-gated (GABA, NMDA, and AMPA receptors) and voltage-gated channels (Ca2+, K+, and Na+)[2].
Hyperforin (0.1, 1, 10 μM; 2 h) reduces the expression and secretion of IL-17A in γδ T cell in vitro cultured murine splenic γδ T cells[3].
Hyperforin (0.1, 1, 10 μM; 2 h) suppresses phosphorylation of MAPK and STAT3 pathways in TNF-α stimulated HaCaT cells[3].
Hyperforin (IC50=3.7 μmol/L) inhibits the microvascular tube formation and proliferation of HDMEC in a dose-dependent manner without toxic effects[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT cells
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Concentration:0.1, 1, 10 μM; with or without 10, 20 ng/mL TNF-α
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Incubation Time:2 hours
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Result:Reduced the expressions of p-p38, p-ERK, p-JNK, and p-STAT3, especially at the dosage of 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:IMQ-induced psoriasis-like mice model[3]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; once daily for 7 days
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Result:Significantly ameliorated skin lesion throughout the treatment period, demonstrated by the reduced severity score of skin inflammation.
Suppressed infiltration of CD3+ T cells and downregulated expression of Il1, Il6, Il23, Il17a, Il22, antimicrobial peptides (AMPs) in the skin lesion.
Chemical Information
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CAS No. 11079-53-1
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Molecular Weight 536.78
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Formula C35H52O4
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SMILES
CC(C)C([C@@]12[C@@](C)([C@H](C[C@](C/C=C(C)/C)(C(C(C/C=C(C)/C)=C2O)=O)C1=O)C/C=C(C)/C)CC/C=C(C)/C)=O
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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.
Publications (3)
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Journal Impact Factor
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Most Recent
Purity & Documentation
References
[1]. Heiser JH, et al. TRPC6 channel-mediated neurite outgrowth in PC12 cells and hippocampal neurons involves activation of RAS/MEK/ERK, PI3K, and CAMKIV signaling. J Neurochem. 2013 Nov;127(3):303-13. [Content Brief]
[2]. Pochwat B, et al. Hyperforin Potentiates Antidepressant-Like Activity of Lanicemine in Mice. Front Mol Neurosci. 2018 Dec 12;11:456. [Content Brief]
[3]. Zhang S, et al. Hyperforin Ameliorates Imiquimod-Induced Psoriasis-Like Murine Skin Inflammation by Modulating IL-17A-Producing γδ T Cells. Front Immunol. 2021 May 5;12:635076. [Content Brief]
[4]. Adam P, et al. Biosynthesis of hyperforin in Hypericum perforatum. J Med Chem. 2002 Oct 10;45(21):4786-93. [Content Brief]
[5]. Li XX, et al. Hyperforin: A natural lead compound with multiple pharmacological activities. Phytochemistry. 2023 Feb;206:113526. [Content Brief]
[6]. Suzhen Chen, et al. "The phytochemical hyperforin triggers thermogenesis in adipose tissue via a Dlat-AMPK signaling axis to curb obesity." Cell Metabolism 33.3 (2021): 565-580. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hyperforin Related Classifications
HY-116330 Related Classifications
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