Picfeltarraenin IB
Picfeltarraenin IA and Picfeltarraenin IB are Potential PI3K and EGFR Inhibitors, they also show stronger AChE inhibition than the known AChE inhibitor Tacrine.
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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.
Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
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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J Nat Prod. 1998 Jun 26;61(6):757-61.
Complement-inhibiting cucurbitacin glycosides from Picria fel-terrae.[Pubmed:
9644059]
Four cucurbitacin glycosides were isolated from Picriafel-terrae and identified by MS and NMR spectroscopy as picfeltarraenin IA (1), Picfeltarraenin IB (2), picfeltarraenin IV (4), and a new compound picfeltarraenin VI (3) (picfeltarraegenin I 3-O-beta-D-xylopyranoside).
METHODS AND RESULTS:
All four compounds acted as inhibitors on both the classical and alternative pathways of the complement system, with compound 3 exhibiting the highest inhibitory activity (IC50 29 +/- 2 microM and 21 +/- 1 microM, respectively). Compounds 1-4 showed no antiviral, antibacterial, or antifungal activities.
CONCLUSIONS:
Picfeltarraenin IA and Picfeltarraenin IB were tested in an in vitro human tumor cell line panel, but displayed no cytotoxic activity.
Pharmacogn Mag. 2013 Oct-Dec; 9(Suppl 1): S25–S31.
Bioassay- and liquid chromatography/mass spectrometry-guided acetylcholinesterase inhibitors from Picriafel-terrae[Pubmed:
24143041]
Picria fel-terrae is a traditional Chinese medicine.
METHODS AND RESULTS:
A new approach to the search for acetylcholinesterase (AChE) inhibitors from Picria fel-terrae is presented.
Bioassay- and LC-MS-guided fractionation of the ethyl acetate extract was from traditional Chinese medicine P.fel-terrae. Following primary extraction, the ethyl acetate extracts fraction of P.fel-terrae showed strong AChE inhibitory activities. So the sample was separated using highperformance liquid chromatography (HPLC). The effluent was split towards two identical 96-well fraction collectors, and the presence of the biologically interesting portion and chromatographic fractions could be readily detected by analyzing selected ion chromatograms through an electrophoresis-electrospray ionization mass spectrometry (ESIMS) system for accurate mass measurement. One 96-well plate was used for a bioassay (AChE-inhibitory assay) and detected the bioactivity and position of the relevant peak in the chromatogram. The positive well in the second 96-well plate was used for identification by LC-(+) ESIMS.
CONCLUSIONS:
As abovementioned, the AChE inhibitory constituents from P.fel-terrae by LC-bioassay-ESIMS were rapid identified. Liquid chromatography/ mass spectrometry (LC-MS) screening detected the presence of six active compounds, identified as picfeltarraenin IA (1), Picfeltarraenin IB (2), picfeltarraenin IV (3), picfeltarraenin X (4), picfeltarraenin XI (5), and one unknown compound. The structures were further determined by 13C NMR. The six compounds expressed stronger AChE inhibition than the known AChE inhibitorTacrine. Above all, the value of this LC-bioassay-ESIMS methodology is highlighted by the finding and structure elucidation of the active constituents from many other structural families of natural products.
Der Pharma Chemica, 2016,8 (19):666-67.
In Silico Analysis of Picfeltarraenin IA and IB as Potential PI3K and EGFR Inhibitor[Reference:
WebLink]
Picfeltarraenin IA and Picfeltarraenin IB are the steroid glycosidefrom Picria fel-terrae Lour., Have been traditionally used inmedication. Epidermal growth factor receptor (EGFR) plays a critical role in the initiation and progression of avariety of human cancers, including breast cancer.An important signaling pathway downstream of EGFR is thePI3K/AKt pathway, which regulates cellular processes as diverse as cell growth, survival, proliferation andmigration.In silico docking using PLANTS program and visualized by Yasara program.
METHODS AND RESULTS:
The model of threedimension enzyme structures used in this research were EGFR and Phosphatidylinositol-3-kinase (PI3K),bindingpocket with the Protein Data Bank (PDB) code 1M17 and 3DBS . Two and three dimension of Picfeltarraenin IA, IBand ZSTK474 as the standard were generated using Marvin Sketch program.
CONCLUSIONS:
Both compoundsand ZSTK474inhibited EGFR and PI3K with docking score -101.7930; -104.6410, -91.7920 and -90.6176 -87.7705; -94.7491respectively.
