β-石竹烯作用機制 - Medchemexpress - MCE中國

1、Product Data Sheet-CaryophylleneCat. No.: HY-N1415CAS No.: 87-44-5分式: CH分量: 204.35作靶點: Cannabinoid Receptor; Endogenous Metabolite作通路: GPCR/G Protein; Neuronal Signaling; Metabolic Enzyme/Protease儲存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 Ethanol : 176.67 mg/m

2、L (864.55 mM)DMSO : 1 mg/mL (insoluble or slightly soluble)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 4.8936 mL 24.4678 mL 48.9356 mL5 mM 0.9787 mL 4.8936 mL 9.7871 mL10 mM 0.4894 mL 2.4468 mL 4.8936 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

3、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)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?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%

4、EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 13.25 mg/mL (64.84 mM); Clear solution此案可獲得 13.25 mg/mL (64.84 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 132.5 mg/mL 的澄 EtOH 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% EtOH 90% (20% SBE-CD in saline)Page 1 o

5、f 2 www.MedChemESolubility: 13.25 mg/mL (64.84 mM); Suspended solution; Need ultrasonic此案可獲得 13.25 mg/mL (64.84 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 132.5 mg/mL 的澄均勻。EtOH 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% EtOH 90% corn oilSolubility: 13.25 mg/mL (64.84 mM); Clear solution此案可獲得

6、 13.25 mg/mL (64.84 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 132.5 mg/mL 的澄 EtOH 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 -Caryophyllene個 CB2 受體激動劑。IC & Target Human Endogenous Metabolite(批量添加)體外研究 Among the tested cancer cells, -Caryophyllene demonstrates selective anti-proliferativ

7、e effect against three cancercell lines, namely HCT 116 (colon cancer, IC50=19 M), PANC-1 (pancreatic cancer, IC50=27 M), and HT29 (coloncancer, IC50=63 M) cells, whereas -Caryophyllene exhibits either moderate or poor cytotoxic effects against ME-180, PC3, K562 and MCF-7. Results show that -Caryoph

8、yllene possesses higher selectivity towards the colorectalcancer cells (HCT 116), with selectivity index (SI)=27.9, followed by PANC-1 and HT 29 cells with SI=19.6 and 8,respectively. The apoptotic index estimated for -Caryophyllene treatment on HCT 116 cells after 24 h treatment is640.04. -Caryophy

9、llene at 10 M concentration, causes significant nuclei condensation after 6 h of treatment. -caryophyllene exhibits a dose and time-dependent inhibitory effect on the motility of HCT 116 cells2.體內研究 Treatment with -Caryophyllene at different doses does not show any effects on swimming speed during t

10、he test.Oral treatment with -Caryophyllene ameliorates the rise in -amyloid deposition in the transgenic mice in a roughlydose-dependent manner, and the two higher doses exhibit almost equal effects in modifying the -amyloid burden.The number of activated astroglial cells is higher in vehicle-treate

11、d mouse brains than in -Caryophyllene-treatedmouse brains with different doses. -Caryophyllene is effective at reducing the enhancement of the COX-2 proteinlevel found in vehicle-treated APP/PS1 mice1. Animals treated with -Caryophyllene display higher values of objectrecognition index than their ve

12、hicle-treated counterparts t(14)=4.204, P0.05). Treatment with -Caryophyllene does not significantly alter these seizure-inducedneurochemical changes3.PROTOCOLCell Assay 2 Panel of human cancer cells such as, pancreatic (PANC-1), colorectal (HCT-116 and HT-29), invasive squamous cellcarcinoma (ME-18

13、0), leukemia (K562), hormone sensitive and invasive breast cancer cell line (MCF-7), and prostatic(PC3) adenocarcinoma cell lines are used. Cells are incubated in a humidified CO2 incubator at 37C supplied with 5%CO2. Inhibitory effect of -Caryophyllene on proliferation of the cell lines is tested u

14、sing the MTT assay. Theselectivity index (SI) for the cytotoxicity of -Caryophyllene is calculated using the ratio of IC50 of -Caryophyllene ona normal cell line (NIH-3T3) to the IC50 of -Caryophyllene on cancer cell lines2.MCE has not independently confirmed the accuracy of these methods. They are

15、for reference only.Page 2 of 3 www.MedChemEAnimal Male double transgenic APP/PS1 mice and wild-type littermates are used. The mice are group housed (3 to 5Administration 1 animals/cage) with a 12:12-hour light/dark cycle and ad libitum access to food and water. In this experiment, animalsare orally

16、treated by gavage with 16, 48, or 144 mg/kg of -Caryophyllene every morning for 10 weeks starting at theage of 7 months. All vehicle solutions are used for the respective control animal treatments and the Morris watermaze test is performed1.MCE has not independently confirmed the accuracy of these m

17、ethods. They are for reference only.REFERENCES1. Cheng Y, et al. -Caryophyllene ameliorates the Alzheimer-like phenotype in APP/PS1 Mice through CB2 receptor activation and the PPAR pathway.Pharmacology. 2014;94(1-2):1-12.2. Dahham SS, et al. The Anticancer, Antioxidant and Antimicrobial Properties of the Sesquiterpene -Caryophyllenefrom the Essential Oil of Aquilariacrassna. Molecules. 2015 Jun 26;20(7):11808-29.3. de Oliveira CC, et al. Anticonvulsant activity of -caryophyllene against pentylenetetrazol-induce