Bavachin
(Synonyms: 补骨脂二氢黄酮; Corylifolin) 目录号 : GC17588
A phytoestrogen
Cas No.:19879-32-4
Sample solution is provided at 25 µL, 10mM.
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Bavachin is an acyl-coenzyme A: cholesterol acyltransferase inhibitor [1].
Acyl-coenzyme A: cholesterol acyl transferase (ACAT) is an enzyme responsible for the intracellular esterification of free cholesterol with fatty acids and plays dominant roles in intestinal absorption of cholesterol, hepatic production of lipoproteins and accumulation of cholesteryl ester within macrophages and smooth muscle cells. [1].
Bavachin showed a significant inhibition of ACAT enzyme. The IC50 value of bavachin was 86.0 μM in the ACAT assay system using rat liver microsome [1]. Bavachin is a flavonoid first isolated from Psoralea corylifolia that has been used as a traditional medicine in Asia. In CV-1 cells transfected with plasmids ERα or ERβ, bavachin showed ER ligand binding activity with an EC50 of 320 nM and 680 nM, respectively. Bavachin increased the mRNA levels of estrogen-responsive genes such as pS2 and PR, and decreased the protein level of ERα by proteasomal pathway [2]. Bavachin activated gene expression of proliferator-activated receptorγ (PPARγ), adipogenic transcriptional factors, and CCAAT/enhancer binding protein-α (C/EBPα). Bavachin increased adiponectin expression and secretion in adipocytes. Bavachin increased insulin-induced glucose uptake by differentiated adipocytes and myoblasts. In differentiated adipocytes, bavachin enhanced glucose uptake [3].
References:
[1] Choi J H, Rho M C, Lee S W, et al. Bavachin and isobavachalcone, acyl-coenzyme A: cholesterol acyltransferase inhibitors from Psoralea corylifolia[J]. Archives of pharmacal research, 2008, 31(11): 1419-1423.
[2] Park J, Kim D H, Ahn H N, et al. Activation of estrogen receptor by bavachin from Psoralea corylifolia[J]. Biomolecules & therapeutics, 2012, 20(2): 183-188.
[3] Lee H, Li H, Noh M, et al. Bavachin from Psoralea corylifolia improves insulin-dependent glucose uptake through insulin signaling and AMPK activation in 3T3-L1 adipocytes[J]. International journal of molecular sciences, 2016, 17(4): 527.
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Kinase experiment: |
The chemiluminescent assay is used to confirm PCSEE MAO-A and MAO-B inhibitory effects and to test BNN and BVN hMAO-A and hMAO-B inhibition using MAO-Glo kit. Each enzyme's Arbitrary Light Unit (ALU) is measured in the presence of PCSEE, BNN, BVN, and standard DEP as an MAO-BI positive control. Briefly, hMAO-A and hMAO-B isozymes are diluted to 2× with reaction buffer (pH 7.4) and preincubated with 4× PCSEE, BNN, BVN, or DEP working solutions at RT for 30 min in white opaque 96-well plates. For determining activity inhibition, final 8.5 μg/mL concentrations of PCSEE, BNN, BVN, and DEP are used. For IC50 determination, 8× PCSEE and BNN working solutions are serially diluted using reaction buffers (pH 7.4) to make a 4× concentration. Ten points' range of PCSEE (1.0 to 250.0 μg/mL) and BNN (up to 400 μM (135.4 μg/mL)) final concentrations is used. Controls used are with and without ethanol. Ethanol solvent in controls is kept to a maximum final (volume) of ≤2%. Each isozyme is substituted with the reaction buffer for the blank. Based on our preliminary optimizations and Valley's method, the reaction is initiated by adding 4× luciferin derivative substrate (LDS) for a final (concentration) of 40 and 4 μM for hMAO-A and hMAO-B reactions, respectively. The final volume per well of each reaction is 50 μL. The reaction is optimized for the amount of A and B enzyme used to be incubated for less than 3.5 h at RT. To stop the reaction and produce the luminescence signal RLDR is added to all wells, 50 μL to each well, and incubated for a further 30 min. |
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Cell experiment: |
MTT solution (20 µL) is added to each well of the 96-well plates, the cells are cultured for 4 h, the solution is discarded, and the purple crystal is dissolved in the wells with 150 µL DMSO solution, agitated in a 37°C incubator shaker for 10 min, and the optical density (OD) is measured at 490 nm by the microplate reader. |
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References: [1]. Wang JH, et al. Effects of bavachin and its regulation of melanin synthesis in A375 cells. Biomed Rep. 2016 Jul;5(1):87-92. Epub 2016 May 20. |
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| Cas No. | 19879-32-4 | SDF | |
| 别名 | 补骨脂二氢黄酮; Corylifolin | ||
| 化学名 | (2S)-2,3-dihydro-7-hydroxy-2-(4-hydroxyphenyl)-6-(3-methyl-2-butenyl)-4H-1-benzopyran-4-one | ||
| Canonical SMILES | OC1=CC(O[C@H](C2=CC=C(O)C=C2)CC3=O)=C3C=C1C/C=C(C)/C | ||
| 分子式 | C20H20O4 | 分子量 | 324.4 |
| 溶解度 | ≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | 储存条件 | Store at -20°C,protect from light |
| 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 | 3.0826 mL | 15.4131 mL | 30.8261 mL |
| 5 mM | 0.6165 mL | 3.0826 mL | 6.1652 mL |
| 10 mM | 0.3083 mL | 1.5413 mL | 3.0826 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet