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Hyperforin
Hyperforin
ChemFaces products have been cited in many studies from excellent and top scientific journals
Product Name Hyperforin
Price:
CAS No.: 11079-53-1
Catalog No.: CFN91083
Molecular Formula: C35H52O4
Molecular Weight: 536.80 g/mol
Purity: >=98%
Type of Compound: Miscellaneous
Physical Desc.: Powder
Source: The herbs of Hypericum monogynum
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download: COA    MSDS
Similar structural: Comparison
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Related Screening Libraries
Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
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Biological Activity
Description: Hyperforin acts as an angiogenesis inhibitor, it as a possible antidepressant component of hypericum extracts. Hyperforin acts as a dual inhibitor of 5-LO and COX-1 in intact cells as well as on the catalytic activity of the crude enzymes, suggesting therapeutic potential in inflammatory and allergic diseases connected to eicosanoids.
Targets: COX-1 | 5-LO | 5-HT recepter | GABA recepter
In vitro:
Life Sci. 1998;63(6):499-510.
Hyperforin as a possible antidepressant component of hypericum extracts.[Pubmed: 9718074 ]

METHODS AND RESULTS:
We demonstrate that the phloroglucinol derivative Hyperforin is not only the major lipophilic chemical constituent of the medicinal plant Hypericum perforatum (St. John's wort) but also a potent uptake inhibitor of serotonin (5-HT), dopamine (DA), noradrenaline (NA), GABA and L-Glutamate with IC50 values of about 0.05-0.10 microg/ml (5-HT, NA, DA, GABA) and about 0.5 microg/ml (L-glutamate) in synaptosomal preparations. Furthermore, potencies of two different hypericum extracts in two conventional pharmacological paradigms useful for the detection of antidepressants (behavioral despair, learned helplessness), closely correlate with their Hyperforin contents. In addition, most till now known neuropharmacological properties of the clinically used hypericum extracts can also be demonstrated with pure Hyperforin.
CONCLUSIONS:
It appears, therefore, that this non-nitrogenous constituent is a possible major active principle responsible for the observed clinical efficacies of the extract as an antidepressant and that it could also be a starting point for drug discovery projects engaged in the search of psychoactive drugs with novel mode of action.
Hyperforin Description
Source: The herbs of Hypericum monogynum
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Calculate Dilution Ratios(Only for Reference)
1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8629 mL 9.3145 mL 18.6289 mL 37.2578 mL 46.5723 mL
5 mM 0.3726 mL 1.8629 mL 3.7258 mL 7.4516 mL 9.3145 mL
10 mM 0.1863 mL 0.9314 mL 1.8629 mL 3.7258 mL 4.6572 mL
50 mM 0.0373 mL 0.1863 mL 0.3726 mL 0.7452 mL 0.9314 mL
100 mM 0.0186 mL 0.0931 mL 0.1863 mL 0.3726 mL 0.4657 mL
* Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
Protocol
Kinase Assay:
Biochem Pharmacol. 2002 Dec 15;64(12):1767-75.
Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase.[Pubmed: 12445866 ]
The acylphloroglucinol derivative Hyperforin is the major lipophilic constituent in the herb Hypericum perforatum (St. John's wort). The aim of the present study was to investigate if Hyperforin as well as extracts of H. perforatum can suppresses the activities of 5-lipoxygenase (5-LO) and cyclooxygenases (COX), key enzymes in the formation of proinflammatory eicosanoids from arachidonic acid (AA).
METHODS AND RESULTS:
In freshly isolated human polymorphonuclear leukocytes stimulated with Ca(2+) ionophore A23187, Hyperforin inhibited 5-LO product formation with IC(50) values of about 1-2 microM, in the absence or presence of exogenous AA (20 microM), respectively, being almost equipotent to the well-documented 5-LO inhibitor zileuton (IC(50) = 0.5-1 microM). Experiments with purified human 5-LO demonstrate that Hyperforin is a direct 5-LO inhibitor (IC(50) approximately 90 nM), acting in an uncompetitive fashion. In thrombin- or ionophore-stimulated human platelets, Hyperforin suppressed COX-1 product (12(S)-hydroxyheptadecatrienoic acid) formation with an IC(50) of 0.3 and 3 microM, respectively, being about 3- to 18-fold more potent than aspirin. At similar concentrations, Hyperforin suppressed COX-1 activity in platelets in presence of exogenous AA (20 microM) as well as in cell-free systems. Hyperforin could not interfere with COX-2 product formation and did not significantly inhibit 12- or 15-LO in platelets or leukocytes, respectively.
CONCLUSIONS:
We conclude that Hyperforin acts as a dual inhibitor of 5-LO and COX-1 in intact cells as well as on the catalytic activity of the crude enzymes, suggesting therapeutic potential in inflammatory and allergic diseases connected to eicosanoids.
Planta Med. 2005 Nov;71(11):999-1004.
Hyperforin acts as an angiogenesis inhibitor.[Pubmed: 16320199]
Hyperforin is a plant compound from Hypericum perforatum that inhibits tumor cell proliferation in vitro by induction of apoptosis. Here, we report that Hyperforin also acts as an angiogenesis inhibitor in vitro and in vivo.
METHODS AND RESULTS:
In vitro, Hyperforin blocked microvessel formation of human dermal microvascular endothelial cells (HDMEC) on a complex extracellular matrix. Furthermore, Hyperforin reduced proliferation of HDMEC in a dose-dependent manner, without displaying toxic effects or inducing apoptosis of the cells. To evaluate the antiangiogenic activity of Hyperforin in vivo, Wistar rats were subcutaneously injected with MT-450 mammary carcinoma cells and were treated with peritumoral injections of Hyperforin or solvent. Hyperforin significantly inhibited tumor growth, induced apoptosis of tumor cells and reduced tumor vascularization, as shown by in situ staining of CD31-positive microvessels in the tumor stroma.
CONCLUSIONS:
These data suggest that, in addition to the induction of tumor cell apoptosis, Hyperforin can also suppress angiogenesis by a direct, non-toxic effect on endothelial cells.
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