山楂酸作用機制 - Medchemexpress - MCE中國

1、Product Data SheetMaslinic acidCat. No.: HY-N0629CAS No.: 4373-41-5分式: CHO分量: 472.7作靶點: NF-B; Bacterial; HIV作通路: NF-B; Anti-infection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 DMSO : 100 mg/mL (211.55 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg

2、 5 mg 10 mgConcentration制備儲備液1 mM 2.1155 mL 10.5775 mL 21.1551 mL5 mM 0.4231 mL 2.1155 mL 4.2310 mL10 mM 0.2116 mL 1.0578 mL 2.1155 mL請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)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?/p>

3、照 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(jié)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(nèi)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 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.29 mM); Suspended solution; Need ultrasonic此案可獲得 2.5 mg/mL (5.29 mM) 的均勻懸濁液，懸濁液可于服和腹腔

4、注射。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。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.29 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.29 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 油中，混合均勻。

5、BIOLOGICAL ACTIVITY物活性 Maslinic acid 可抑制 NF-B p65 的 DNA 結(jié)合活性, 并消除 IB- 磷酸化。IC & Target p65體外研究 Maslinic acid (MA) inhibits LPS-induced NF-B translocation to nucleus and phosphorylation of IB-. Maslinic acidhas also been reported to suppress NF-B regulated osteoclastogenesis in bone marrow monocytes a

6、nd inhibit TNF-induced NF-B activity and its downstream genes expression in pancreatic cancer cells. To confirm if the anti-inflammatory effects of olive pomace extracts (OPEs) inRAW264.7 cells can be attributed to Maslinic acid, dose-dependence experiments determined the effective concentration of

7、Maslinic acid to be 10-20 M. 20 M Maslinicacid significantly suppresses TNF- production and inhibits IL-1, IL-6, and COX-2 mRNA expression in RAW 264.7 cell.Maslinic acid (at 10 and 20 M) significantly suppresses the DNA-binding activity of NF-B p65 in LPS-induced RAW264.7 cells. Pretreatment with M

8、aslinic acid significantly reduces the LPS-induced phosphorylation of IB-1.體內(nèi)研究 Paw swelling is alleviated when mice are administered with 200 mg/kg Maslinic acid (MA), significantly suppressinginflammation, compared to the carrageenan induced control group, 4 h after -carrageenan injection (0.910.5

9、1 mm and 1.790.4 mm, respectively)1.PROTOCOLCell Assay 1 RAW 264.7 cells are seeded in 96-well culture plates at a density of 1105 cells/mL and after incubation for 24 h, aretreated with OPE1 (300 g/mL or 400 g/mL), OPE2 (20 g/mL or 40 g/mL), or Maslinic acid (10 M or 20 M) , aswell as with/without

10、LPS at the same time. Cell viability i determined using the WST-1 reagent. Briefly, WST-1 reagent(10 L) is added to each well and incubated for 1h in a humidified incubator. The absorbance of the samplesmeasured at 450 nm (reference wavelength is 750 nm). Viability is expressed as a percentage of th

11、e absorbancemeasured in LPS-treated cells1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice1Administration 1 Five-week-old male Balb/c mice (19-21 g) are housed in a conventional condition and provided with the free accessto standard rodent c

12、how and water. Edema is induced by intraplantar injection of 100 L 1% carrageenan into thehind left paw. Maslinic acid is tested initially at a dose of 200 mg/kg, orally administered 60 min before and aftercarrageenan injection. Paw thickness is measured using electronic digital calipers, 2, 3, and

13、4 h following carrageenantreatment. Mice are sacrificed by carbon dioxide inhalation 4 h after carrageenan injection1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Fukumitsu S, et al. Anti-inflammatory and anti-arthritic effects of pentacyclic triterpenoids maslinic acid through NF-B inactivation. Mol Nutr Food Res.2016 Feb;60(2):399-409.McePdfHeightPage 2 of 3 www.MedChemECaution: