異土木香內(nèi)酯作用機制 - Medchemexpress - MCE中國

1、Product Data SheetIsoalantolactoneCat. No.: HY-N0780CAS No.: 470-17-7分式: CHO分量: 232.32作靶點: Apoptosis; Autophagy; Bacterial; Endogenous Metabolite作通路: Apoptosis; Autophagy; Anti-infection; Metabolic Enzyme/Protease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 :

2、50 mg/mL (215.22 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 4.3044 mL 21.5220 mL 43.0441 mL5 mM 0.8609 mL 4.3044 mL 8.6088 mL10 mM 0.4304 mL 2.1522 mL 4.3044 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，-

3、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(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 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.76 mM); Clear solution此案可

4、獲得 2.5 mg/mL (10.76 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 (10.76 mM); Clear solution此案可獲得 2.5 mg/mL (10.76 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www

5、.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.76 mM); Clear solution此案可獲得 2.5 mg/mL (10.76 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。BIOLOGICAL ACTIVI

6、TY物活性 Isoalantolactone種烷化劑，作細胞凋亡 (apoptosis) 誘導劑。IC & Target Human Endogenous Metabolite(批量添加)體外研究 Isoalantolactone exhibits good cytotoxic activity against the K562 human leukaemia cell line (IC50=1.2 M) 1. Thecytotoxic effect of Isoalantolactone on pancreatic carcinoma is evaluated using PANC-1, B

7、xPC3 and HPAC cell lines.Treatment with Isoalantolactone for 24 h inhibits PANC-1 cell growth in a dose-dependent manner. The inhibitionrate is above 90% at 80 M and the concentration to achieve 50% growth inhibition (IC50) is 40 M. A similar trend inloss of cell viability is observed in BxPC3 and H

8、PAC cells on Isoalantolactone treatment with IC50 values 43 and 48 Mrespectively. Pretreatment with 3 mM N-Acetyl Cysteine (NAC), a specific ROS scavenger, restores the viability of cellsindicating that Isoalantolactone exerts cytotoxic effect on cell viability through ROS generation2.體內(nèi)研究 The acute

9、 and chronic toxic effects of Isoalantolactone in CD1 mice are assessed by measuring the changes in bodyweight, blood biochemistry and histopathology of liver and kidneys in comparison with control groups.Isoalantolactone is well tolerated by mice and no mortality or any sign of pharmacotoxicity are

10、 found at a dose of 100mg/kg during both experimental periods (7 & 30 days). Body weight gains and food consumption are comparable forcontrol and treated mice during both experimental periods and there were no drug-related changes inhistopathological and blood biochemistry parameters. The histopatho

11、logical changes in liver and kidneys areassessed using hematoxylin and eosin staining and correlated with liver and renal function biomarkers. No obviousmorphological changes are observed in liver and kidney structures of control and treatment groups. There is a slightincrease in serum alanine amino

12、transferase (ALT) and aspartate aminotransferase (AST) level of treatment group atdose day 7 but this increase is not significantly different (P0.05) from control group. A significant increase in totalbilirubin (TBIL) concentration is found in treatment group (1.430.26 vs 0.760.12 in control, P0.05)

13、 at dose day 7.Similarly the changes in renal function biomarkers are not significantly different (P0.05) in the serum of control andtreatment groups at dose day 7. The concentration of creatinine (Cr) slightly increases whereas concentration ofblood urea nitrogen (BUN) slightly decreases in treatme

14、nt group. The serum level of AST, ALT, TBIL and BUN slightlydecreases when mice are injected with Isoalantolactone at a dose of 100 mg/kg for 30 days2.PROTOCOLCell Assay 2 Cell viability is assessed by MTT assay. Briefly PANC-1, BxPC3, and HPAC cells are treated with DMSO orIsoalantolactone (5, 10,

15、20, 40, 80 and 100 M) in the presence or absence of 3 mM NAC for 24 h. Followingtreatment, the MTT reagent is added (500 g/mL) and cells are further incubated at 37C for 4 h. Subsequently 150 L DMSO is added to dissolve farmazan crystals and absorbance is measured at 570 nm in a microplate reader. T

16、hepercentage of cell viability is calculated2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemEAnimal Mice2Administration 2 In vivo studies for acute and chronic toxicity are conducted on 10-12 week old CD1 mice weighing 27-30 g.

17、Themice are maintained in a specific pathogen-free grade animal facility on a 12-h light/dark cycles at 252C. Mice arerandomly divided into four groups. Group A (n=4) administered with 50 L DMSO intraperitonially for 7 days; GroupB (n=4) administered with Isoalantolactone (100 mg/kg body weight) in

18、50 L DMSO intraperitonially for 7 days;Group C (n=4) administered with 50 L DMSO for 30 days and Group D (n=4) administered with Isoalantolactone(100 mg/kg body weight) in 50 L DMSO intraperitonially for 30 days. At the first and last day of the experiments,the body weight of each mouse is measured.

19、 At the end of experiments (at dose day 7 for acute toxicity & dose day30 for chronic toxicity), mice are anesthetized using Pentobarbital sodium (50 mg/kg ip), blood is collected viacardiac puncture, allowed to clot for 10 min and centrifuge at 1000g for 10 min at room temperature. Serum isseparated and stored at -20C until analysis. The liver and kidneys are excised and processed for hematoxylin andeosin staining followed established procedures.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻