Apigenin

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Apigenin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

520-36-5

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
50mg	询价

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	270.24
Cas No.	520-36-5
Formula	C₁₅H₁₀O₅
Solubility	insoluble in EtOH; insoluble in H2O; ≥9.8 mg/mL in DMSO
Chemical Name	5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one
Canonical SMILES	C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

The polyphenol 4’, 5, 7,-trihydroxyflavone Apigenin (API) is a histone deacetylase (HDAC) inhibitor with IC50 values of 49.16±2.52 μM, 46.95±1.69 μM, 34.31±1.55 μM in MM-B1, MM-F1 and H-Meso-1cells respectively [1].

HDACs are well-known as remarkable molecular targets for anticancer drugs and therapy. HDAC inhibitors (HDACi) promote apoptosis induction by decreasing the functions of HDACs and anti-apoptotic proteins.

API inhibits the growth of MM cell lines. MM-B1, MM-F1 and H-Meso-1 cells were treated with increasing doses of API or vehicle control for different hours by Sulforhodamine B (SRB) and Trypan blue exclusion assays. The inhibition rate of all human cells was increased in a dose- and time-dependent way and attained statistical significance at the doses of 12.5, 25 and 50 μM after 48-72 h exposure [1].

After MM #40a cells inoculation in the peritoneum, the C57BL/6 mice model were following on administration with 20 mg/kg API in solution or with the vehicle alone in the same way. After 2 weeks of treatment, API-treated mice exhibited lower abdominal circumference significantly (p=0.0072) and maintained more survival time as compared with the control group (p=0.0009). Relative to API-treated mice, vehicle-treated mice had a tumor growth risk of 23.17 (p=0.0009) [1].

Reference:

[1]. Masuelli L, Benvenuto M, Mattera R, et al. In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma. Frontiers in pharmacology, 2017, 19:8:373.

试验操作

细胞实验 [1]:
细胞系	恶性间皮瘤 (MM) 细胞系
制备方法	在DMSO中的溶解度大于9.8 mg/mL。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。
反应条件	6.25 ~ 100 μM；24、48和72小时
实验结果	在所有MM细胞系中，Apigenin呈剂量和时间依赖性地抑制细胞生长。给药72小时后，Apigenin对MM-B1、MM-F1和H-Meso-1细胞的IC50值分别为49.16 ± 2.52 μM、46.95 ± 1.69 μM 和34.31 ± 1.55 μM。此外，Apigenin显著诱导活性氧 (ROS) 产生以及DNA损伤。
动物实验 [1]:
动物模型	携带MM #40a细胞的C57BL/6小鼠
给药剂量	20 mg/kg；腹腔注射；每周1次
实验结果	经过2周的治疗后，Apigenin显著降低腹围，其平均值为6.9 cm。在携带MM #40a细胞的C57BL/6小鼠中，与溶剂组相比，Apigenin治疗也延长了生存期的中位数（12周对5.5周）。
注意事项	请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。
References: [1]. Masuelli L, Benvenuto M, Mattera R, Di Stefano E, Zago E, Taffera G, Tresoldi I, Giganti MG, Frajese GV, Berardi G, Modesti A, Bei R. In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma. Front Pharmacol. 2017 Jun 19;8:373.