Bergaptol
Bergaptol acts as a potent inhibitor of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.Bergaptol shows very good radical scavenging activity, it induces dose-dependent cytotoxic effect on MCF-7 cell viability.
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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.
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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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Bangl. J. Pharmacol., 2016, 11(2):489.
Antitumor and apoptotic effects of bergaptol are mediated via mitochondrial death pathway and cell cycle arrest in human breast carcinoma cells.[Reference:
WebLink]
The aim of the present research work was to investigate the anti-cancer and apoptotic effects of Bergaptol in human breast cancer cells (MCF-7).
METHODS AND RESULTS:
The effects on cell cycle arrest and caspase activation were evaluated. MTT assay was used to evaluate the effect of the compound on cell viability. Cellular morphology was demonstrated by fluorescence microscopy. Flow cytometry was used to analyze effect of Bergaptol on cell cycle and apoptosis. The results revealed that Bergaptol induced dose-dependent cytotoxic effect on MCF-7 cell viability showing IC50 value of 52.2 μM. Bergaptol induced both early and late apoptosis in concentration-dependent manner. After treatment with Bergaptol, an increase in the proportion of cells in the S-phase (37.2, 45.3 and 65.1% as compared to 28.6% in untreated cells) and a reduction in the fraction of cells in the G1 phase (44.1, 41.6 and 35.2% as compared to 51.2% in the untreated cells) was observed.
Bioorg Med Chem. 2007 Jun 1;15(11):3684-91.
Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit.[Pubmed:
17400460]
Grapefruit juice has been shown to increase the oral bioavailability of several clinically important drugs by inhibiting first pass metabolism. Several compounds in grapefruit juice have shown different biological activities. Unique among them are furocoumarins with potent inhibitory activity against cytochrome P450 enzymes.
METHODS AND RESULTS:
In the present study, two bioactive compounds were isolated from grapefruit juice and grapefruit peel oil. The purity of the isolated compounds has been analyzed by HPLC. Structures of the compounds were elucidated by extensive NMR and mass spectral studies and identified as Bergaptol and geranylcoumarin. The isolated compounds were tested for their radical scavenging activity using 2,2'-azobis (3-ethylbenz-thiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazil (DPPH) methods at different concentrations. Bergaptol showed very good radical scavenging activity at all the tested concentrations. Furthermore, these compounds were evaluated for their inhibitory activity against CYP3A4 enzyme.
CONCLUSIONS:
Bergaptol and geranylcoumarin were found to be potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC(50) value of 24.92 and 42.93 microM, respectively.
