Protosappanin A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Protosappanin A 通过调节 CD14/TLR4 依赖性炎症信号通路对脑免疫和神经炎症具有抗氧化/硝化活性。

Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent 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.(In Vitro):Protosappanin A (PsA) and Protosappanin B (PsB) were identified from Sappan Lignum extracts. They showed activity 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 the 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.

Protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) significantly inhibits the production of TNF-α and IL-1β in LPS-activated BV2 microglia. And the mRNA expressions of IL-6, IL-1β, and MCP-1 are reduced by PTA in a dose-dependent manner in BV2 microglial cell line.Protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3, as well as STAT3 nuclear translocation against LPS treatment.Protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) shows obvious effect on disturbing the interaction of transmembrane protein CD14 with Toll-like receptor-4, resulting in the inhibition of NF-κB-dependent oxidative and nitrative stress in LPS-induced BV2 microglia. Western Blot Analysis Cell Line:Murine BV2 microglial cell line.Concentration:12.5, 25, 50 μM.Incubation Time:24 hours.Result:Inhibits the releases of NO, TNF-α and IL-1β in LPS-induced BV2 cells.Attenuated IL-6, IL-1β and MCP-1 gene expressions in the LPS-induced BV2 cells. Suppressed JAK2/STAT3 pathway activation in the LPS-induced BV2 cells.

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PTA

Membrane Transporter/Ion Channel

NADPH

NADPH

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102036-28-2

272.25

C15H12O5

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (459.14 mM)

Oc(cc1)cc(OCC(C2)=O)c1-c(cc1O)c2cc1O

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(-20℃)

With Ice Pack

≥ 2 years