Diosimin
(Synonyms: 地奥司明) 目录号 : GN10706
A citrus-derived flavonoid
Cas No.:520-27-4
Sample solution is provided at 25 µL, 10mM.
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Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
Treatment with Diosmin causes a dose dependent increase in the amount of adducts formed (up to a 7-fold increase in adducts at 5 μM Diosmin). At 5 μM, Diosmin increases the cytotoxicity of 7,12-dimethylbenz(a)anthracene (DMBA), shifting the IC50 of DMBA from an estimated 1.2 μM to 400 nM. Diosmin is not cytotoxic in itself at the concentrations tested. Diosmin causes an increase in CYPIAI activity in MCF-7 cells in a time- and dose-dependent fashion. Diosmin causes a dose-dependent increase in CYPIAI mRNA after 24 h of incubation, causes a long-lasting increase in CYPIAI mRNA accumulation that reaches its peak after 48 h of incubation[1].
Diosmin significantly decreases the malondialdehyde (MDA) levels and increases the activities of total-superoxide dismutase (T-SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) in the retina of rats compare with the ischemia group (P<0.05), and suppresses the ischemia/reperfusion (I/R)-induced reduction in the a- and b-wave amplitudes of the electroretinograms (ERGs) (P<0.05). The thickness of the entire retina, inner nuclear layer, inner plexiform layer, and outer retinal layer and the number of cells in the ganglion cell layer are significantly less after I/R injury (P<0.05), and Diosmin remarkably ameliorates these changes on retinal morphology. Diosmin also attenuates the I/R-induced loss of retinal ganglion cells (RGCs) of the rat retina (P<0.05)[2].
References:
[1]. Ciolino HP, et al. Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affectcytochrome P450 1A1 activity. Cancer Res. 1998 Jul 1;58(13):2754-60.
[2]. Tong N, et al. Diosmin protects rat retina from ischemia/reperfusion injury. J Ocul Pharmacol Ther. 2012 Oct;28(5):459-66.
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Cell experiment: |
MCF-7 cells are plated at 25,000 cells/well in 24-well plates. After 24 h, the medium is changed to medium containing 5 μM Diosmin. After an additional 24 h, the medium is again changed with medium containing 5 μM Diosmin. After 3 days, the total cell growth is assessed by sulforhodamine[1]. |
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Animal experiment: |
Healthy male Wistar rats (n=112) weighing 180 to 200 g each are used in this study. The animals are randomly assigned to the following 4 groups, which include combinations of the ischemia/reperfusion (I/R) injury model or sham injury with the i.g. administration of Diosmin or vehicle solution: sham+vehicle (SV) group, sham+Diosmin (SD) group, model+vehicle (MV) group, and model+Diosmin (MD) group. For intragastric administration, 5 mL of 2% Diosmin per kilogram weight of the rat, or the same volume of vehicle solution, is administered intragastrically 30 min before the onset of ischemia, and then daily after I/R injury until the animals are sacrificed. Using an overdose of anesthesia, 8 rats from each group are sacrificed 24 h after I/R injury, and their eyeballs harvested for determination of the malondialdehyde (MDA) level and the activities of total-superoxide dismutase (T-SOD), glutathione peroxidase (GSH-Px), and catalase (CAT). At 7 days post-I/R injury, electroretinograms (ERGs) are recorded in 6 rats per group. Meanwhile, 6 rats in each group are randomly chosen for retrograde labeling of retinal ganglion cells (RGCs) , and the remaining 8 rats from each group are histopathologically examined[2]. |
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References: [1]. Ciolino HP, et al. Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affectcytochrome P450 1A1 activity. Cancer Res. 1998 Jul 1;58(13):2754-60. |
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| Cas No. | 520-27-4 | SDF | |
| 别名 | 地奥司明 | ||
| 化学名 | 5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxychromen-4-one | ||
| Canonical SMILES | CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=CC(=C4C(=C3)OC(=CC4=O)C5=CC(=C(C=C5)OC)O)O)O)O)O)O)O)O | ||
| 分子式 | C28H32O15 | 分子量 | 608.17 |
| 溶解度 | ≥ 21.6mg/mL in DMSO | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6443 mL | 8.2214 mL | 16.4428 mL |
| 5 mM | 0.3289 mL | 1.6443 mL | 3.2886 mL |
| 10 mM | 0.1644 mL | 0.8221 mL | 1.6443 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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