山竹子素作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetGarcinolCat. No.: HY-107569CAS No.: 78824-30-3分式: CHO分量: 602.8作靶點(diǎn): AChE; Histone Acetyltransferase; Apoptosis; Endogenous Metabolite作通路: Neuronal Signaling; Epigenetics; Apoptosis; Metabolic Enzyme/Protease儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) Ethano

2、l : 20 mg/mL (33.18 mM; Need ultrasonic and warming)DMSO : 20 mg/mL (33.18 mM; Need ultrasonic and warming)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.6589 mL 8.2946 mL 16.5893 mL5 mM 0.3318 mL 1.6589 mL 3.3179 mL10 mM 0.1659 mL 0.8295 mL 1.6589 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

3、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。BIOLOGICAL ACTIVITY物活性 Garcinol種從印度藤 提取的聚異戊烯 苯甲酮，對酰膽堿酯酶 (AChE) 和丁酰膽堿酯酶 (BChE) 具有抗膽堿酯酶的特性，IC50 分別為 0.66 M 和 7.39 M。Garcinol 還抑制組蛋酰轉(zhuǎn)移酶 (HATs, IC50=7 M) 和 p300/CPB相關(guān)因 (PCAF, IC50=5 M)。Garcinol 具有抗炎和抗癌活性。IC & Target Hu

4、man Endogenous Metabolite(批量添加)體外研究Garcinol (10-50 M; 24-72 hours) can inhibit the proliferation of two HNSCC cell lines tested (CAL27 and UMSCC1) ina time- and dose-dependent manner3.Garcinol (10-50 M; 24-72 hours) induces apoptosis in HNSCC cells3.Garcinol (50 M; 1-6 hours) suppresses phosphorylat

5、ion and degradation of the constitutive IB in a time-dependent manner3.Page 1 of 2 www.MedChemECell Proliferation Assay3Cell Line: CAL27 and UMSCC1 cellsConcentration: 10, 25, 50 MIncubation Time: 24, 48, and 72 hoursResult: Inhibited the proliferation of two HNSCC cell lines in a time- and dose-dep

6、endentmanner.Apoptosis Analysis3Cell Line: CAL27 and UMSCC1 cellsConcentration: 10, 25, 50 MIncubation Time: 24, 48, and 72 hoursResult: Induced apoptosis in HNSCC cells.Western Blot Analysis3Cell Line: CAL27 cellsConcentration: 50 MIncubation Time: 1, 2, 4, 6 hoursResult: Suppressed phosphorylation

7、 and degradation of the constitutive IB in a time-dependent manner.體內(nèi)研究 Garcinol (i.p.; 1 and 2 mg/kg; five times/week for 4 consecutive weeks) induces significant inhibition of tumor growth3.Animal Model: Five-week-old athymic nu/nu male mice bearing subcutaneous CAL27 tumors3Dosage: 1 and 2 mg/kgA

8、dministration: I.p.; five times/week for 4 consecutive weeksResult: Induced significant inhibition of tumor growth.REFERENCES1. Lenta BN, et al. Leishmanicidal and cholinesterase inhibiting activities of phenolic compounds from Allanblackia monticola and Symphonia globulifera.Molecules. 2007 Jul 20;

9、12(8):1548-57.2. Ciochina R, et al. Polycyclic polyprenylated acylphloroglucinols. Chem Rev. 2006 Sep;106(9):3963-86.3. Li F, et al. Garcinol, a polyisoprenylated benzophenone modulates multiple proinflammatory signalingcascades leading to the suppression of growth andsurvival of head and neck carcinoma. Cancer Prev Res (Phila). 2013 Aug;6(8):843-54.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been fully validated for medical applications.