| CAS |
No.119425-90-0 |
| 中文名称 |
龙血素 B |
| 英文名称 |
Loureirin B |
| 别名 |
龙血素B;LR-B;LoureirinB; |
| 分子式 |
C18H20O5 |
| 分子量 |
316.35 |
| 溶解性 |
Soluble in DMSO(Need ultrasonic) |
| 纯度 |
HPLC≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD07781421 |
| SMILES |
COC1=CC(=C(C(=C1)OC)CCC(=O)C2=CC=C(C=C2)O)OC |
| InChIKey |
ZPFRAPVRYLGYEC-UHFFFAOYSA-N |
| InChI |
InChI=1S/C18H20O5/c1-21-14-10-17(22-2)15(18(11-14)23-3)8-9-16(20)12-4-6-13(19)7-5-12/h4-7，10-11，19H，8-9H2，1-3H3 |
| PubChem CID |
189670 |
| 靶点 |
PAI-1 |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
Loureirin B 是PAI-1 的抑制剂，具有抗糖尿病的活性。 |
| 生物活性 |
Loureirin B， a flavonoid extracted from Dracaena cochinchinensis， is an inhibitor of plasminogen activator inhibitor-1 (PAI-1)， with an IC50 of 26.10?μM; Loureirin B also inhibits KATP， the phosphorylation of ERK and JNK， and has anti-diabetic activity.[1-4] |
| In Vitro |
Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Loureirin B (1， 0.1， and 0.01?μM) increases insulin secretion in Ins-1 cells. Loureirin B (0.01?μM) 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[1]. 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[2]. 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[3]. |
| 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[3]. |
| 细胞实验 |
Ins-1 cells are seeded onto 96-well plates and cultured for 48?h to approximately 80-90% confluence. Then， the cells are starved in a 2% FBS/DMEM for 12?h. Control group is cultured in medium without loureirin B， while the positive control group is received fresh medium with glimepiride. After the treatment of loureirin B and glimepiride for 4 and 8?h， the cell viability is measured by Cell Counting Kit-8 (CCK-8).[1-4] |
| 动物实验 |
For short， 10 adult New Zealand white male rabbits (2.0-2.5 kg b.w./each) are acclimated and housed under the standard 12-h light: 12-h dark cycle with free access of water and SPF basal diet. Rabbit is first anaesthetized with 1% pentobarbital (1.5 mg/kg b.w.)， and then， a dermal punch biopsy (10×4 mm) is created down to bare cartilage on the ventral surface of each ear to outline a full-thickness wound. Four punch wounds are made on each ear of the eight rabbits. A dissecting microscope is used to ensure the complete removal of epidermis， dermis and perichondrium in each wound. Forty-eight hours after surgery， wounded rabbits are randomLy divided into two groups with each being subcutaneously injected with DMSO solution (0.125% in PBS， 0.25 mL/kg b.w.) on the left ear or loureirin B solution (25 μg/mL in PBS， 0.25 mL/kg b.w.) on the right ear once every other day for total six times. Two rabbits are used for pilot experiment， four rabbits are sacrificed 14 days after injury (n = 4)， and the rest four are sacrificed 28 days after injury (n=4). Two of the four scar tissues on the same ear are processed for Western blot， and the other two are used for Masson staining.[1-4] |
| 数据来源文献 |
[1]. Sha Y， et al. Loureirin B promotes insulin secretion through inhibition of KATP channel and influx of intracellular calcium. J Cell Biochem. 2017 Aug 17.
[2]. He T， et al. Loureirin B Inhibits Hypertrophic Scar Formation via Inhibition of the TGF-β1-ERK/JNK Pathway. Cell Physiol Biochem. 2015;37(2):666-76.
[3]. Bai X， et al. Loureirin B inhibits fibroblast proliferation and extracellular matrix deposition in hypertrophic scar via TGF-β/Smad pathway. Exp Dermatol. 2015 May;24(5):355-60.
[4]. Yu Jiang， et al. Bioactivity-Guided Fractionation of the Traditional Chinese Medicine Resina Draconis Reveals Loureirin B as a PAI-1 Inhibitor. Evidence-Based Complementary and Alternative Medicine |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
中文
英语
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