Apigenin
产品说明书
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同义名 : | 金银花 ;4',5,7-Trihydroxyflavone;Apigenol;457Trihydroxyflavone;Spigenin;Apigenine;Versulin;Flavone;Chamomile;NSC 83244;LY 080400;C.I. Natural Yellow 1 |
| CAS号 : | 520-36-5 | |
| 货号 : | A167323 | |
| 分子式 : | C15H10O5 | |
| 纯度 : | 98% | |
| 分子量 : | 270.23 | |
| MDL号 : | MFCD00006831 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 85 mg/mL(314.54 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 4 mg/mL clear PO 0.5% CMC-Na 41 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | CYP2C9 ranks among the most important drug-metabolizing enzymes in humans and hydroxylates 10 to 20% of commonly prescribed drugs[3]. Apigenin, a naturally occurring plant flavone, abundantly present in common fruits and vegetables, is a competitive CYP2C9 inhibitor with a Ki value of 2 μM[3]. It inhibited T-24 cell proliferation in a dose-dependent manner. Apigenin-mediated subG1 phase accumulation was also associated with an increase in the phospho-p53, p53, p21, and p27 levels, and with a decrease in the Cyclin A, Cyclin B1, Cyclin E, CDK2, Cdc2, and Cdc25C levels, thereby blocking cell cycle progression. In addition, apigenin increased the Bax, Bad, and Bak levels, but reduced the Bcl-xL, Bcl-2, and Mcl-1levels, and subsequently triggered the mitochondrial apoptotic pathway. Further analysis demonstrated that apigenin increased the reactive oxygen species (ROS) levels and depleted GSH in T-24 cells at 12h[4]. Apigenin inhibited protein kinase C (PKC) by competing with adenosine triphosphate (ATP). It also reduced the level of tetradecanoyl-phorbol-13-acetate (TPA)-stimulated phosphorylation of cellular proteins and inhibited TPA-induced c-jun and c-fos expression and exhibited the reverting effect on the transformed morphology of these cells[5]. In ovalbumin immunized BALB/C mice, production of IL-4 was down-regulated by apigenin[6]. In vivo studies have also shown that apigenin inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. Oral administration of apigenin was shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice, and also suppresses prostate and breast cancer cell growth through estrogen receptor β1[6]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HEK293 cells | Function assay | 24 h | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=24.9 μM | 24955889 | |
| HEK293 FS cells | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.13 μM | 20731357 | ||
| human H295R cells | Function assay | Inhibition of aromatase expressed in human H295R cells, IC50=1 μM | 18778944 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03365648 | Allergic Rhinoconjunctivitis | Not Applicable | Completed | - | Italy ... 展开 >> Fondazione IRCCS Policlinico San Matteo Pavia, (pv), Italy, 27100 Ospedale regionale San Salvatore - ASL 1 Avezzano Sulmona L'Aquila L'Aquila, AQ, Italy, 67100 A.O.U. Consorziale "Policlinico Giovanni XXIII" Bari, BA, Italy, 70126 A.O.U. Consorziale "Policlinico-Giovanni XXIII" Bari, BA, Italy, 70126 A.O.U. Policlinico Vittorio Emanuele Catania, CT, Italy, 95123 Istituto Giannina Gaslini Genova, GE, Italy, 16132 P.O. San Giovanni di Dio - ASP di Crotone Crotone, KR, Italy, 88900 A.O.U. Policlinico "G. Martino" Messina, ME, Italy, 98124 P.O. G. Salvini di Garbagnate Milanese - ASST Rhodense Garbagnate Milanese, MI, Italy, 20042 Ospedale Civile di Legnano - ASST Ovest Milanese Legnano, MI, Italy, 20162 Fondazione IRCCS Cà Granda Ospedale Maggiore Policlinico Milano, MI, Italy, 20122 Ospedale San Carlo Borromeo - ASST Azienda Socio Sanitaria Territoriale Santi Paolo E Carlo Milano, MI, Italy, 20157 Ospedale Città di Sesto San Giovanni - ASST Nord Milano Sesto San Giovanni, MI, Italy, 20099 Ospedale di Polistena "Santa Maria degli Ungheresi" - ASP di Reggio Calabria Polistena, RC, Italy, 89024 A.O.U. Policlinico Umberto I Roma, RM, Italy, 00161 P.O. di Busto Arsizio - ASST Valle Olona Busto Arsizio, VA, Italy, 21051 Az. Osp. Univ. dell'Università degli Studi della Campania "Luigi Vanvitelli" Napoli, Italy, 80138 收起 << |
| NCT01286324 | Primary Insomnia ... 展开 >> Chronic Insomnia 收起 << | Phase 2 | Completed | - | United States, Michigan ... 展开 >> University of Michigan Department of Family Medicine Ann Arbor, Michigan, United States, 48105 收起 << |
| NCT03139227 | Health Status Unknown | Not Applicable | Recruiting | August 31, 2020 | United States, Ohio ... 展开 >> Ohio State University Comprehensive Cancer Center Recruiting Columbus, Ohio, United States, 43210 Contact: Sagar D. Sardesai, MBBS 614-293-0066 Sagar.Sardesai@osumc.edu Principal Investigator: Sagar D. Sardesai, MBBS Sub-Investigator: Andrea I. Doseff, PhD Sub-Investigator: Maryam Lustberg, MD MPH 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.70mL 0.74mL 0.37mL |
18.50mL 3.70mL 1.85mL |
37.01mL 7.40mL 3.70mL |
| 参考文献 |
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