原苏木素 A

Protosappanin A

	产品编号	CFN96956
	CAS编号	102036-28-2
	分子式 = 分子量	C₁₅H₁₂O₅ = 272.25
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Phenols
	植物来源	The herbs of Caesalpinia sappan L.
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产品名称	产品编号	CAS编号	包装	QQ客服
原苏木素 A	CFN96956	102036-28-2	1mg	QQ客服：3257982914
原苏木素 A	CFN96956	102036-28-2	5mg	QQ客服：3257982914
原苏木素 A	CFN96956	102036-28-2	10mg	QQ客服：3257982914
原苏木素 A	CFN96956	102036-28-2	20mg	QQ客服：3257982914

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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.

	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

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原苏木素 A

Protosappanin A

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