1、Product Data SheetLoureirin BCat. No.: HY-N1504CAS No.: 119425-90-0分式: CHO分量: 316.35作靶點: PAI-1; Potassium Channel; ERK; JNK作通路: Metabolic Enzyme/Protease; Membrane Transporter/Ion Channel; MAPK/ERKPathway; Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 D

2、MSO : 150 mg/mL (474.16 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20

3、C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL

4、 (7.90 mM); Clear solution此案可獲得 2.5 mg/mL (7.90 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 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、獲得 2.5 mg/mL (7.90 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.90 mM); Clear solution此案可獲得 2.5 mg/mL (7.90 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L

6、油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Loureirin B從劍葉龍樹中分離到的黃酮類化合物，為 PAI-1 的抑制劑，IC50 值為 26.10 M；Loureirin B 同時可以抑制 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)體外研究 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.體內研究 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