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Loureirin B

CAS No. : 119425-90-0

MCE 站：Loureirin B

产品活性：Loureirin B 是从剑叶龙血树中分离到的黄酮类化合物，为 PAI-1 的抑制剂，IC₅₀ 值为 26.10?μM；Loureirin B 同时可以抑制 K_ATP，以及 ERK、JNK 的磷酸化，具有抗糖尿病的功效。

研究领域：Metabolic Enzyme/Protease  |  Membrane Transporter/Ion Channel  |  MAPK/ERK Pathway  |  Stem Cell/Wnt

作用靶点：PAI-1  |  Potassium Channel  |  ERK  |  JNK

In Vitro: Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Loureirin B (1, 0.1, and 0.01??M) increases insulin secretion in Ins-1 cells. Loureirin B (0.01??M) almost causes no toxicity on cells. Loureirin B improves the level of expressions of MafA and Pdx-1 and ATP level. Loureirin B inhibits the KATP current but increases the [Ca²⁺]i level in Ins-1 cells. Loureirin B inhibits the expression of Col1 and FN, as well as the TGF-β1-mediated up regulation of p-JNK. Loureirin B also inhibits the up regulation of p-ERK that is induced by TGF-β1. Moreover, Loureirin B inhibits the contraction of TGF-β1-stimulated fibroblasts through the down regulation of p-ERK and p-JNK. However, Loureirin B does not suppress the up regulation of p-p38 that is induced by TGF-β1. Loureirin B downregulates both mRNA and protein levels of type I collagen, type III collagen and α-smooth muscle actin in a dose dependent manner in HS fibroblasts. Loureirin B also suppresses fibroblast proliferative activity and redistributes cell cycle, but does not affect cell apoptosis.

In Vivo: Loureirin B significantly improves the arrangement and deposition of collagen fibres, decreases protein levels of ColI, ColIII and α-SMA and suppresses myofibroblast differentiation and scar proliferative activity, in a rabbit ear scar model. Loureirin B effectively inhibits TGF-β1-induced upregulation of ColI, ColIII and α-SMA levels, myofibroblast differentiation and the activation of Smad2 and Smad3, in NS fibroblasts.

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