Apigenin (4′,5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
IC50 & Target
Ki: 2 μM (CYP2C9)[1]
体外研究 (In Vitro)
Apigenin (4′,5,7-Trihydroxyflavone) inhibits cytochrome P450 2C9 (CYP2C9) with a Ki of 2 μM in the CYP2C9 RECO system (a purified, reconstituted enzyme system containing recombinant human CYP2C9, P450 reductase, cytochrome b5, and liposomes)[1]. Apigenin inhibits the cell proliferation. The growth inhibition rate (IR) of 20, 40, and 80 μM of Apigenin is 38%, 71%, and 99% respectively on the 7thd. after exposure to Apigenin for 24 or 48 h, the clone formation of SGC-7901 cells is suppressed in a dose- and time-dependent manner. The cloning efficiency in 80 μM is 9.8% and 5% after treatment with Apigenin for 24 and 48 h, while in the control group it is 40.4% and 43.4%[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Apigenin (4′,5,7-Trihydroxyflavone), a natural flavonoid, possesses a broad spectrum of biological properties, including antioxidative, anti-inflammatory, anticancer, and neuroprotective effects. Apigenin (125 mg/kg and 250 mg/kg) alleviates Adriamycin (ADR) (24 mg/kg)-induced myocardial injury. Apigenin inhibits serum aspartate amino transferase (AST) release. Apigenin reduces serum lactate dehydrogenase (LDH) release. Apigenin reduces serum creatine kinase (CK) contents[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
270.24
Formula
C15H10O5
CAS 号
520-36-5
中文名称
芹菜素
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34.
[2]. Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4.
[3]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676.
Cell Assay [2]
The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of human gastric cancer SGC-7901 cells are harvested with 0.2% EDTA and plated at a density of 2.5×103/well in 96-well microtiter plates. After an overnight incubation to allow cell attachment, the medium is replaced by fresh medium containing different concentrations (0, 20, 40, and 80 μM) of Apigenin. Control wells receive DMSO (0.2%). Each concentration of Apigenin is repeated in four wells. After incubation for 24 h, one plate is assayed with a microplate reader at the wavelength of 570 nm. Before the assay, MTT (5 mg/mL in PBS) is added to each well and incubated for 4 h, then MTT solution is removed from the wells by aspiration. After careful removal of the medium, 0.1 mL of DMSO is added to each well, and the plate is shaken for 15 min. The data of 7 d are fed into the computer and the growth curve is drawn. The growth inhibition rate (IR) is calculated[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [3]
Mice[3] Sixty healthy Kunming mice (26±2 g) are randomly assigned into two groups: a control group (n=15) and an ADR group (n=45). The ADR group is divided into three subgroups: ADR only without Apigenin (ADR, n=15), low-dose Apigenin (125 mg/kg/day, n=15), and high-dose Apigenin (250 mg/kg/day, n=15). All Apigenin-treated groups are treated daily via gastric gavage for seventeen days with a 125 or 250 mg/kg/day dose. ADR (3 mg/kg/day) is injected intraperitoneally into animals at an interval of 48 h (in total, eight times at a cumulative dose of 24 mg/kg). The mice in the control group receive injections of 0.9% sterile saline. On the 17th day after the first treatment, the mice are sacrificed, and blood samples are collected. A number of hearts are fixed with 2.5% glutaraldehyde fixative for electron microscopy analysis, and the others are stored at -80°C for western blot analysis.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34.
[2]. Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4.
[3]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676.
Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor with an IC50 value of 3.12 μM.
IC50 & Target
IC50: 3.12 μM (xanthine oxidase)[1]
体外研究 (In Vitro)
Baicalein suppresses mitogen induced T cell proliferation and cytokine secretion in vitro. Pre-treatment with baicalein significantly suppresses Con A or anti-CD3/CD28 mAb induced proliferation as well as cytokine secretion at 25 μM. Baicalein treatment induces DNA binding of NF-κB but inhibits thioredoxin activity in the nuclear compartment[2]. Baicalein suppresses proliferation, migration, and invasion of MDA-MB-231 cells in a time- and dose-dependent manner. Baicalein significantly decreases the expression of SATB1 in MDA-MB-231 cells. Baicalein also downregulates the expression of Wnt1 and β-catenin proteins and transcription level of Wnt/β-catenin-targeted genes[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Baicalein suppresses induction of graft versus host disease but does not inhibit homeostatic proliferation of T-cells in mice. This observation clearly shows potent anti-inflammatory activity of baicalein in vivo[2]. Rats treated with baicalein are protected against an increase in heart to body weight ratio, plasma level of brain natriuretic peptides, intraventricular septum thickness, myocardial collagen volume of left ventricle (all P<0.05, respectively). The antifibrotic effects of baicalein are further illustrated by the suppressed expression of left ventricle pro-collagens I and III accompanied by the decreased expression of 12-lipoxygenase, and by reduced expression and activity of matrix metallopeptidase 9 and extracellular signal-regulated kinases. Baicalein can inhibit cardiac fibrosis in hypertensive rats[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
270.24
Formula
C15H10O5
CAS 号
491-67-8
中文名称
黄芩素
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.
[2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89.
[3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41.
[4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81.
Cell Assay [3]
MTT assay is conducted to evaluate the effect of baicalein on proliferation of breast cancer cells. MDA-MB-231 cells are routinely digested, collected, and then seeded in 96-well plates at a density of 8×103 cells/well. After incubation for 12-24 hours, cells are treated with 0, 20, 40, 60, 80, 100, and 120 μM baicalein according to their experimental grouping and then incubated at 37°C for 24, 48, and 72 hours[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2][4]
Rats: Baicalein is suspended in 1% methylcellulose. Rats are treated with baicalein suspension via oral garvage. SHR and WKY rats are divided into 4 groups (n=8 per group): 12-week treatment with high-dose (200 mg/kg/day) or low-dose (50 mg/kg/day) group; and 4-week treatment with high-dose or low-dose group. The 12-week and 4-week negative control groups of SHR and WKY rats (n=8 per group) receive vehicle while positive control groups (Val group, n=8 per group) receive valsartan (20 mg/kg/day) for comparison[4].
Mice: To study the in vivo anti-inflammatory efficacy of baicalein, graft-versus-host disease (GVHD) model is used. Splenic lymphocytes from C57BL/6 mice are incubated with baicalein in vitro (25 μM, 4h) and adoptively transferred to immune-compromised Balb/c mice[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.
[2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89.
[3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41.
[4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81.
