龙血素 B作用机制 - Medchemexpress - MCE中国

1、Product Data SheetLoureirin BCat. No.: HY-N1504CAS No.: 119425-90-0分式: CHO分量: 316.35作靶点: PAI-1; Potassium Channel; ERK; JNK作通路: Metabolic Enzyme/Protease; Membrane Transporter/Ion Channel; MAPK/ERKPathway; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 D

2、MSO : 150 mg/mL (474.16 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.1611 mL 15.8053 mL 31.6106 mL5 mM 0.6322 mL 3.1611 mL 6.3221 mL10 mM 0.3161 mL 1.5805 mL 3.1611 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20

3、C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL

4、 (7.90 mM); Clear solution此案可获得 2.5 mg/mL (7.90 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.90 mM); Clear solutionPage 1 of 2 www.MedChemE此案可

5、获得 2.5 mg/mL (7.90 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.90 mM); Clear solution此案可获得 2.5 mg/mL (7.90 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L

6、油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Loureirin B从剑叶龙树中分离到的黄酮类化合物，为 PAI-1 的抑制剂，IC50 值为 26.10 M；Loureirin B 同时可以抑制 KATP，以及 ERK、JNK 的磷酸化，具有抗糖尿病的功效。IC & Target PAI-1 KATP ERK JNK26.1 M (IC50)体外研究 Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Loureirin B (1, 0.1, and 0.01 M) increases insulin

7、secretion in Ins-1 cells. Loureirin B (0.01 M) almost causes no toxicity on cells. Loureirin B improves the level ofexpressions of MafA and Pdx-1 and ATP level. Loureirin B inhibits the KATP current but increases the Ca2+i level inIns-1 cells1. Loureirin B inhibits the expression of Col1 and FN, as

8、well as the TGF-1-mediated up regulation of p-JNK. Loureirin B also inhibits the up regulation of p-ERK that is induced by TGF-1. Moreover, Loureirin B inhibits thecontraction of TGF-1-stimulated fibroblasts through the down regulation of p-ERK and p-JNK. However, Loureirin Bdoes not suppress the up

9、 regulation of p-p38 that is induced by TGF-12. Loureirin B downregulates both mRNAand protein levels of type I collagen, type III collagen and -smooth muscle actin in a dose dependent manner in HSfibroblasts. Loureirin B also suppresses fibroblast proliferative activity and redistributes cell cycle

10、, but does not affectcell apoptosis3.体内研究 Loureirin B significantly improves the arrangement and deposition of collagen fibres, decreases protein levels of ColI,ColIII and -SMA and suppresses myofibroblast differentiation and scar proliferative activity, in a rabbit ear scarmodel. Loureirin B effect

11、ively inhibits TGF-1-induced upregulation of ColI, ColIII and -SMA levels, myofibroblastdifferentiation and the activation of Smad2 and Smad3, in NS fibroblasts3.PROTOCOLCell Assay 1 Ins-1 cells are seeded onto 96-well plates and cultured for 48 h to approximately 80-90% confluence. Then, the cellsa

12、re starved in a 2% FBS/DMEM for 12 h. Control group is cultured in medium without loureirin B, while the positivecontrol group is received fresh medium with glimepiride. After the treatment of loureirin B and glimepiride for 4 and8 h, the cell viability is measured by Cell Counting Kit-8 (CCK-8).MCE

13、 has not independently confirmed the accuracy of these methods. They are for reference only.Animal For short, 10 adult New Zealand white male rabbits (2.0-2.5 kg b.w./each) are acclimated and housed under theAdministration 3 standard 12-h light: 12-h dark cycle with free access of water and SPF basa

14、l diet. Rabbit is first anaesthetized with 1%pentobarbital (1.5 mg/kg b.w.), and then, a dermal punch biopsy (104 mm) is created down to bare cartilage on theventral surface of each ear to outline a full-thickness wound. Four punch wounds are made on each ear of the eightrabbits. A dissecting micros

15、cope is used to ensure the complete removal of epidermis, dermis and perichondrium ineach wound. Forty-eight hours after surgery, wounded rabbits are randomLy divided into two groups with eachbeing subcutaneously injected with DMSO solution (0.125% in PBS, 0.25 mL/kg b.w.) on the left ear or loureir

16、in BPage 2 of 3 www.MedChemEsolution (25 g/mL in PBS, 0.25 mL/kg b.w.) on the right ear once every other day for total six times. Two rabbits areused for pilot experiment, four rabbits are sacrificed 14 days after injury (n = 4), and the rest four are sacrificed 28days after injury (n=4). Two of the

17、 four scar tissues on the same ear are processed for Western blot, and the othertwo are used for Masson staining.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Sha Y, et al. Loureirin B promotes insulin secretion through inhibition of KATP

18、 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-1-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-/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 I