Picfeltarraenin IA | CAS:97230-47-2 | Manufacturer ChemFaces

Picfeltarraenin IA

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Description:

Picfeltarraenin IA has anti-inflammatory activity, it is a strong AChE inhibitior, and an potential PI3K and epidermal growth factor receptor (EGFR ) inhibitor. It acts as an inhibitor on both the classical and alternative pathways of the complement system.

Targets:

IL Receptor | PGE | NF-kB | COX | p65 | EGFR | PI3K | Akt

In vitro:

Oncol Lett. 2016 Feb;11(2):1195-1200.

Picfeltarraenin IA inhibits lipopolysaccharide-induced inflammatory cytokine production by the nuclear factor-κB pathway in human pulmonary epithelial A549 cells.[Pubmed: 26893718 ]

The present study aimed to investigate the effect of Picfeltarraenin IA (IA) on respiratory inflammation by analyzing its effect on interleukin (IL)-8 and prostaglandin E2 (PGE2) production. The expression of cyclooxygenase 2 (COX2) in human pulmonary adenocarcinoma epithelial A549 cells in culture was also examined.
METHODS AND RESULTS:
Human pulmonary epithelial A549 cells and the human monocytic leukemia THP-1 cell line were used in the current study. Cell viability was measured using a methylthiazol tetrazolium assay. The production of IL-8 and PGE2 was investigated using an enzyme-linked immunosorbent assay. The expression of COX2 and nuclear factor-κB (NF-κB)-p65 was examined using western blot analysis. Treatment with lipopolysaccharide (LPS; 10 μg/ml) resulted in the increased production of IL-8 and PGE2, and the increased expression of COX2 in the A549 cells. Furthermore, IA (0.1-10 μmol/l) significantly inhibited PGE2 production and COX2 expression in cells with LPS-induced IL-8, in a concentration-dependent manner. The results suggested that IA downregulates LPS-induced COX2 expression, and inhibits IL-8 and PGE2 production in pulmonary epithelial cells. Additionally, IA was observed to suppress the expression of COX2 in THP-1 cells, and also to regulate the expression of COX2 via the NF-κB pathway in the A549 cells, but not in the THP-1 cells.
CONCLUSIONS:
These results indicate that IA regulates LPS-induced cytokine release in A549 cells via the NF-κB pathway.

Picfeltarraenin IA Description

Source:	The herbs of Picria felterrae Lour.
Solvent:	DMSO, Pyridine, Methanol, Ethanol, 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.

Kinase Assay:

Der PharmaChemica, 2016, 8(19):666-670.

In Silico Analysis of Picfeltarraenin IA and IB as Potential PI3K and EGFR Inhibitor.[Reference: WebLink]

Picfeltarraenin IA and IB are the steroid glycoside from Picria fel-terrae Lour., Have been traditionally used in medication. Epidermal growth factor receptor (EGFR) plays a critical role in the initiation and progression of a variety of human cancers, including breast cancer. An important signaling pathway downstream of EGFR is the PI3K/AKt pathway, which regulates cellular processes as diverse as cell growth, survival, proliferation and migration. In silico docking using PLANTS program and visualized by Yasara program.
METHODS AND RESULTS:
The model of three dimension enzyme structures used in this research were EGFR and Phosphatidylinositol-3-kinase (PI3K), binding pocket with the Protein Data Bank (PDB) code 1M17 and 3DBS . Two and three dimension of Picfeltarraenin IA, IB and ZSTK474 as the standard were generated using Marvin Sketch program.
CONCLUSIONS:
Both compounds and ZSTK474 inhibited EGFR and PI3K with docking score -101.7930; -104.6410, -91.7920 and -90.6176 -87.7705; -94.7491 respectively.

Structure Identification:

Pharmacogn Mag. 2013 Oct;9(Suppl 1):S25-31.

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. RESULTS: 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.

Product Name	Picfeltarraenin IA
Price:	$90 / 20mg
CAS No.:	97230-47-2
Catalog No.:	CFN99942
Molecular Formula:	C₄₁H₆₂O₁₃
Molecular Weight:	762.92 g/mol
Purity:	>=98%
Type of Compound:	Triterpenoids
Physical Desc.:	White powder
Source:	The herbs of Picria felterrae Lour.
Solvent:	DMSO, Pyridine, Methanol, Ethanol, etc.
Download:	COA MSDS SDF Manual
Similar structural:	Comparison (Web) (SDF)
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Anti-inflammatory Compound Library Inhibitors Compound Library Anticomplementary Compound Library Triterpenoids Compound Library PI3K Inhibitor Library PGE Inhibitor Library p65 Inhibitor Library NF-kB Inhibitor Library IL Receptor Inhibitor Library EGFR Inhibitor Library COX Inhibitor Library Akt Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	1.3108 mL	6.5538 mL	13.1075 mL	26.2151 mL	32.7688 mL
5 mM	0.2622 mL	1.3108 mL	2.6215 mL	5.243 mL	6.5538 mL
10 mM	0.1311 mL	0.6554 mL	1.3108 mL	2.6215 mL	3.2769 mL
50 mM	0.0262 mL	0.1311 mL	0.2622 mL	0.5243 mL	0.6554 mL
100 mM	0.0131 mL	0.0655 mL	0.1311 mL	0.2622 mL	0.3277 mL

CFN95650	16,23-Oxidoalisol B	169326-06-1	470.7	C₃₀H₄₆O₄
CFN92402	Alisol F	155521-45-2	488.7	C₃₀H₄₈O₅
CFN95657	25-Methoxyalisol F	2221029-53-2	502.7	C₃₁H₅₀O₅
CFN92407	24-Deacetylalisol O	1067510-31-9	470.7	C₃₀H₄₆O₄
CFN92404	Alisol O	928148-51-0	512.7	C₃₂H₄₈O₅
CFN92547	16-Oxoalisol A	124515-98-6	504.7	C₃₀H₄₈O₆
CFN92545	Alisol C	30489-27-1	486.7	C₃₀H₄₆O₅
CFN90199	Alisol C monoacetate	26575-93-9	528.73	C₃₂H₄₈O₆
CFN92405	Alisol K 23-acetate	228095-18-9	526.7	C₃₂H₄₆O₆
CFN99942	Picfeltarraenin IA	97230-47-2	762.92	C₄₁H₆₂O₁₃