Protosappanin A | CAS:102036-28-2 | Manufacturer ChemFaces

Protosappanin A

ChemFaces products have been cited in many studies from excellent and top scientific journals

Order & Inquiry & Tech Support

Tel: (0086)-27-84237683
Tech: service@chemfaces.com
Order: manager@chemfaces.com
Address: 176, CheCheng Eest Rd., WETDZ, Wuhan, Hubei 430056, PRC

How to Order

Orders via your E-mail:

1. Product number / Name / CAS No.
2. Delivery address
3. Ordering/billing address
4. Contact information
Order: manager@chemfaces.com

Delivery time

Delivery & Payment method

1. Usually delivery time: Next day delivery by 9:00 a.m. Order now

2. We accept: Wire transfer & Credit card & Paypal

Citing Use of our Products

More Impact Factor than five Cite...

* Packaging according to customer requirements(5mg, 10mg, 20mg and more). We shipped via FedEx, DHL, UPS, EMS and others courier.

According to end customer requirements, ChemFaces provide solvent format. This solvent format of product intended use: Signaling Inhibitors, Biological activities or Pharmacological activities.

Size /Price /Stock	10 mM * 1 mL in DMSO / $144.7 / In-stock
Other Packaging	*Packaging according to customer requirements(100uL/well, 200uL/well and more), and Container use Storage Tube With Screw Cap

Featured Products

More...

Soyasaponin Ab

Catalog No: CFN90773
CAS No: 118194-13-1
Price: $ / mg

Sarsasapogenin

Catalog No: CFN99779
CAS No: 126-19-2
Price: $40/20mg

Gracillin

Catalog No: CFN98537
CAS No: 19083-00-2
Price: $80/20mg

3'-Demethylnobiletin

Catalog No: CFN93130
CAS No: 112448-39-2
Price: $188/10mg

Hirsutenone

Catalog No: CFN98646
CAS No: 41137-87-5
Price: $ /

Caffeoyl alcohol

Catalog No: CFN70348
CAS No: 3598-26-3
Price: $318/10mg

Ginsenoside F1

Catalog No: CFN99754
CAS No: 53963-43-2
Price: $90/20mg

Furanodienone

Catalog No: CFN92028
CAS No: 24268-41-5
Price: $218/20mg

Tricetin

Catalog No: CFN70392
CAS No: 520-31-0
Price: $118/10mg

Fisetin

Catalog No: CFN98176
CAS No: 528-48-3
Price: $30/20mg

Description:

Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Targets:

TNF-α | IL Receptor | JAK | STAT | ROS | NO | NADPH-oxidase | NF-kB | IkB | TLR | IFN-γ | IKK | HIV-1 IN

In vitro:

J Pharm Pharmacol. 2015 Oct;67(10):1439-47.

Antimicrobial activity and synergy of antibiotics with two biphenyl compounds, protosappanins A and B from Sappan Lignum against methicillin-resistant Staphylococcus aureus strains.[Pubmed: 25920539 ]

This study aims to investigate antimicrobial ingredients from Sappan Lignum and to evaluate their synergy on methicillin-resistant Staphylococcus aureus strains with antibiotics.
METHODS AND RESULTS:
Bioactivity-guided phytochemical procedures were used to screen the active compounds. Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were assayed by broth microdilution. The synergy was evaluated through checkerboard microdilution and loss of viability assays. Protosappanin A (PsA) and Protosappanin B (PsB) were identified from Sappan Lignum extracts. They showed active against both S. aureus and MRSA with MIC or MIC50 at 64 (PsA) and 128 (PsB) mg/L alone. When they were used in combination with antibiotics, they showed best synergy with amikacin and gentamicin with MIC50 (mg/L) of amikacin reduced more significantly from 32 to four (with PsA) and eight (with PsB), and the fractional inhibitory concentration index (FICI) ranged between 0.078 and 0.500 (FICI50 = 0.375). Moreover, the resistance of MRSA towards amikacin and gentamicin could be reversed by the Clinical and Laboratory Standards Institute criteria. The combined bactericidal mode could as well be synergy. PsA and PsB showed very low cytotoxicity in comparison with their promising activity against MRSA.
CONCLUSIONS:
Protosappanin A and Protosappanin B showed both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA, which warrant further investigations for potential combinatory therapy of MRSA infection.

In vivo:

Naunyn Schmiedebergs Arch Pharmacol. 2010 Jan;381(1):83-92

Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway.[Pubmed: 19924402]

Protosappanin A as one major and effective ingredient from Caesalpinia sappan L. exhibited antirejection activity obviously in heart-transplanted rat.
METHODS AND RESULTS:
The present study was designed to screen out the potential target genes of Protosappanin A with microarray technology and reveal some molecular mechanism of immunosuppressive effect. Rats performed with ectopic peritoneal heart transplantation were randomized into three groups receiving different treatments for 7 days: Protosappanin A group (25 mg kg(-1)), cyclosporine A group (10 mg kg(-1)), and control group. The differentially expressed genes responding to Protosappanin A were analyzed with microarrays. Among common differentially expressed genes, the ones of interest were selected for further evaluation by real-time quantitative reverse transcriptase polymerase chain reaction (qRT-PCR), Western blot, immunochemistry, immunofluorescence, and ELISA. Among the 146 common differentially expressed genes, NF-kappaB and related genes like IkappaBa, IFN-r, and IP10 were selected for verification. The results of qRT-PCR, Western blot, immunochemistry, and ELISA showed that Protosappanin A significantly reduced the expression of NF-kappaB, IFN-r, and IP10 (p < 0.05) and increased IkappaBa expression (p < 0.05) in graft. Moreover, the immunochemistry staining of NF-kappaB and IkappaBa was mainly observed in infiltrating mononuclear cells. Strikingly, immunofluorescent staining localized NF-kappaB to the TCR-positive T cells in graft. Furthermore, Protosappanin A exhibited inhibitory effect on T cell proliferation in recipients after 7-day treatment. In conclusion, Protosappanin A might act on T cells through inhibiting NF-kappaB activation and downstream gene expressions of IFN-r and IP10, meanwhile reducing T cell proliferation responding to alloantigen, so as to induce immunosuppressive effect.
CONCLUSIONS:
The results encourage a potential therapeutic evaluation of Protosappanin A for clinical organ transplantation or other T cell-mediated immune disorders. Additionally, our study also verified the feasibility of microarray utilization in Chinese herb research to explore molecular mechanism and promote development of scientific theories.

Protosappanin A Description

Source:	The herbs of Caesalpinia sappan L.
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.

Kinase Assay:

Chin J Nat Med. 2017 Sep;15(9):674-679.

Protosappanin A exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia.[Pubmed: 28991528 ]

Microglial activation and resultant neuroinflammatory response are implicated in various brain diseases including Alzheimer's disease and Parkinson's disease. Treatment with anti-neuroinflammatory agents could provide therapeutic benefits for such disorders. Protosappanin A (PTA) is a major bioactive ingredient isolated from Caesalpinia sappan L..
METHODS AND RESULTS:
In this work, the anti-neuroinflammatory effects of PTA on LPS-stimulated BV2 cells were investigated and the underlying mechanisms were explored. Results showed that PTA significantly inhibited the production of TNF-α and IL-1β in LPS-activated BV2 microglia. Moreover, the mRNA expressions of IL-6, IL-1β, and MCP-1 were reduced by PTA in a dose-dependent manner. Furthermore, PTA suppressed JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3, as well as STAT3 nuclear translocation against LPS treatment.
CONCLUSIONS:
These observations suggested a novel role for PTA in regulating LPS-induced neuroinflammatory injuries.

Int Immunopharmacol. 2012 Dec;14(4):558-69.

Protosappanin A inhibits oxidative and nitrative stress via interfering the interaction of transmembrane protein CD14 with Toll-like receptor-4 in lipopolysaccharide-induced BV-2 microglia.[Pubmed: 23000519 ]

Oxidative and nitrative stresses have been established to play a pivotal role in neuroinflammation. During inflammation-mediated neurodegenerative diseases, including Alzheimer's disease and Parkinson's disease, reactive oxygen species (ROS) and nitric oxide (NO) are produced by activated microglia, further inducing increased neuronal injury in the brain. Protosappanin A (PTA) is a bioactive compound isolated from a traditional Chinese medicine, Caesalpinia sappan L. (Lignum Sappan), showing immunosuppressive effects. However, the molecular mechanisms responsible for the anti-oxidative and nitrative activity of PTA have not been elucidated, particularly in central nervous system.
METHODS AND RESULTS:
In this study, we found that PTA significantly inhibited ROS and NO production by suppression of NADPH oxidase and inducible nitric oxide synthase (iNOS) activity on lipopolysaccharide (LPS)-stimulated BV-2 microglia. Moreover, PTA modulated IKK/IκB/NF-κB inflammation signal pathway to inhibit the activity and expressions of NADPH oxidase and iNOS. A further study indicated that PTA didn't inhibit LPS interaction with transmembrane protein CD14, which is a receptor for LPS binding. However, PTA interfered with the interaction of CD14 with Toll-like receptor (TLR4), an early cell event of IKK/IκB/NF-κB inflammation signal activation, resulting in a block on LPS translocation from CD14 to TLR4. Therefore, CD14/TLR4 interaction may be a potential drug target in neuroinflammation-related oxidative and nitrative stress.
CONCLUSIONS:
Taken together, these results suggest that PTA has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway.

Product Name	Protosappanin A
Price:	$318 / 10mg
CAS No.:	102036-28-2
Catalog No.:	CFN96956
Molecular Formula:	C₁₅H₁₂O₅
Molecular Weight:	272.25 g/mol
Purity:	>=98%
Type of Compound:	Phenols
Physical Desc.:	Powder
Source:	The herbs of Caesalpinia sappan L.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS
Similar structural:	Comparison
Guestbook:

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	3.6731 mL	18.3655 mL	36.7309 mL	73.4619 mL	91.8274 mL
5 mM	0.7346 mL	3.6731 mL	7.3462 mL	14.6924 mL	18.3655 mL
10 mM	0.3673 mL	1.8365 mL	3.6731 mL	7.3462 mL	9.1827 mL
50 mM	0.0735 mL	0.3673 mL	0.7346 mL	1.4692 mL	1.8365 mL
100 mM	0.0367 mL	0.1837 mL	0.3673 mL	0.7346 mL	0.9183 mL

CFN60145	Axitinib	319460-85-0	386.47	C₂₂H₁₈N₄OS
CFN90701	Polyphyllin H	81917-50-2	871.0	C₄₄H₇₀O₁₇
CFN96087	Dregeoside A11	89020-11-1	1101.3	C₅₅H₈₈O₂₂
CFN98840	Tectochrysin	520-28-5	268.3	C₁₆H₁₂O₄