Irisolidone
(Synonyms: 尼泊尔鸢尾异黄酮) 目录号 : GC63514
Irisolidone 是葛根花中的主要的异黄酮。Irisolidone 具有较强的保肝活性。Irisolidone 对阴离子通道 VRAC 具有高效阻断作用。
Cas No.:2345-17-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade[1][2][3].
Irisolidone shows the high efficacy for Volume-regulated anion channels (VRAC) blockade with an IC50 of 9.8 μM in HEK293 cells[3].Irisolidone can inhibit endothelial cell proliferation[3].
[1]. Kim SY, et al. Irisolidone, an isoflavone metabolite, represses JC virus gene expression via inhibition of Sp1 binding in human glial cells. Biochem Biophys Res Commun. 2006 May 26;344(1):3-8.
[2]. Zhang G, et al. Pharmacokinetics of irisolidone and its main metabolites in rat plasma determined by ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Nov 15;1005:23-9.
[3]. Xue Y, et al. Natural and synthetic flavonoids, novel blockers of the volume-regulated anion channels, inhibit endothelial cell proliferation. Pflugers Arch. 2018 Oct;470(10):1473-1483.
| Cas No. | 2345-17-7 | SDF | |
| 别名 | 尼泊尔鸢尾异黄酮 | ||
| 分子式 | C17H14O6 | 分子量 | 314.29 |
| 溶解度 | 储存条件 | 4°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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1818 mL | 15.9089 mL | 31.8177 mL |
| 5 mM | 0.6364 mL | 3.1818 mL | 6.3635 mL |
| 10 mM | 0.3182 mL | 1.5909 mL | 3.1818 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。
Herbal Phytomedicine 'Irisolidone' in Chronic Diseases: Biological Efficacy and Pharmacological Activity
Recent Adv Antiinfect Drug Discov 2022;17(1):13-22.PMID:35249525DOI:10.2174/1574891X16666220304231934.
Background: Plant-derived products have been used in medicine as a source of bioactive molecules, mainly due to their medicinal importance and therapeutic potential. Nowadays, plant derived products have been used in the medicine for the development of novel drug leads. Polyphenols are an important class of secondary metabolites found to be present in plants and their derived products. Polyphenols play an important role in the nutrition of human beings and also have a significant role in plant resistance against pests and diseases. Scientific studies have proven the biological importance of flavonoids in medicine and other allied health sectors. Anti-oxidant, analgesic, anti-microbial, anti-inflammatory, anti-viral, anti-tumor and anti-allergic activities are the important pharmacological features of flavonoids. Irisolidone is an important isoflavone found to be present in Pueraria lobata flowers. Methods: To know the medicinal importance and therapeutic potential of Irisolidone in the medicine, numerous scientific research data have been collected from Google, Google Scholar, PubMed, Science Direct, and Scopus. Pharmacological activity data of Irisolidone has been collected and analyzed in the present works to know their health beneficial aspects in the medicine. Detailed pharmacological activities of Irisolidone have been investigated through scientific data analysis of scientific research works. Results: Scientific research data analysis of Irisolidone revealed the anti-inflammatory, antiangiogenic, anti-cancer, anti-platelet, anti-oxidant, anti-hyperlipidemic, immunomodulating, hepatoprotective and estrogenic potential. However, the biological effect of Irisolidone on the gastric system, aldose reductase enzymes, malignant gliomas, and JC virus has also been investigated. Scientific data analysis revealed the significance of analytical tools for the separation and identification of Irisolidone. Conclusion: Present work signified the biological importance and therapeutic potential of Irisolidone in medicine.
Irisolidone attenuates ethanol-induced gastric injury in mice by inhibiting the infiltration of neutrophils
Mol Nutr Food Res 2017 Feb;61(2).PMID:27546737DOI:10.1002/mnfr.201600517.
Scope: This study was designed to determine whether Irisolidone and its glycoside kakkalide, which are the major constituents of the flower of Pueraria lobata (Kudzu) can attenuate ethanol-induced gastritic injury in mice. Methods and results: Irisolidone and kakkalide inhibited IL-8 secretion and NF-κB activation in lipopolysaccharide-stimulated KATO III cells. Therefore, we investigated their protective effects against ethanol-induced gastric injury in mice. Pretreatment with kakkalide or Irisolidone decreased the area of hemorrhagic ulcerative lesions caused by ethanol and suppressed stomach myeloperoxidase activity, CXCL4 secretion, and NF-κB activation. The ameliorating effect of Irisolidone was more potent than that of kakkalide. Conclusion: Irisolidone may attenuate ethanol-induced gastritis by inhibiting the infiltration of immune cells, particularly neutrophils, through the regulation of CXCL-4 or IL-8 secretion.
Kakkalide and Irisolidone alleviate 2,4,6-trinitrobenzenesulfonic acid-induced colitis in mice by inhibiting lipopolysaccharide binding to toll-like receptor-4 and proteobacteria population
Int Immunopharmacol 2019 Aug;73:246-253.PMID:31112869DOI:10.1016/j.intimp.2019.05.008.
The flower of Pueraria lobata (family Fabaceae) has been clinically used in traditional Chinese medicine to counteract symptoms associated with drinking alcohol and liver injury and to alleviate inflammatory diseases. Its major constituent kakkalide is metabolized to Irisolidone by gut microbiota. This research study was undertaken to understand the anti-colitis mechanism of kakkalide and Irisolidone in vitro and in vivo. Kakkalide and its metabolite Irisolidone inhibited lipopolysaccharide (LPS)-stimulated NF-κB activation and TNF-α expression in macrophages. They also inhibited LPS-induced phosphorylation of IRAK1 and TAK1 and activation of NF-κB by inhibiting the binding of Alexa Fluor 488-conjugated LPS in vitro. Orally administered Irisolidone or kakkalide alleviated colon shortening and myeloperoxidase activity in mice with 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colitis. Their treatments also protected epithelial cell disruption and infiltration of CD11b+/CD11c+ cells in the colon. Furthermore, they suppressed TNBS-induced expression of M1 macrophage markers TNF-α, CD80, CD86, and Arg2 expression while the expression of M2 macrophage markers Arg1, CD163, CD206, and IL-10 was induced. They also suppressed the fecal Proteobacteria population. Overall, the anti-colitic effects of Irisolidone were superior to those of kakkalide. Kakkalide and its metabolite Irisolidone inhibited inflammation in vitro and in vivo by inhibiting LPS binding to toll-like receptor 4 and gut proteobacteria population.
Irisolidone, an isoflavone metabolite, represses JC virus gene expression via inhibition of Sp1 binding in human glial cells
Biochem Biophys Res Commun 2006 May 26;344(1):3-8.PMID:16630573DOI:10.1016/j.bbrc.2006.03.165.
Progressive multifocal leukoencephalopathy (PML) is a fatal demyelinating disease that results from an oligodendrocyte infection caused by the JC virus. Therefore, inhibiting the expression of JC virus is important for preventing and/or treating PML. This study found that Irisolidone, an isoflavone metabolite, significantly inhibited the JC virus expression in primary cultured human astrocytes and glial cell lines. Studies examining the underlying mechanism revealed that a mutation of the Sp1 binding site downstream of the TATA box (Sp1-II) dramatically diminished the inhibitory activity of Irisolidone. In addition, an Irisolidone treatment repressed Sp1 binding to Sp1-II site, which is important for the basal JC virus promoter activity. The results suggest that the inhibitory effect of Irisolidone against the JC virus may be attributed at least in part to the suppression of Sp1 binding to the JC virus promoter region. Therefore, the inhibition of the JC virus expression by Irisolidone might provide therapeutic potential for PML caused by the JC virus.
Metabolic profile of Irisolidone in rats obtained by ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry
J Chromatogr B Analyt Technol Biomed Life Sci 2013 Dec 15;941:1-9.PMID:24184829DOI:10.1016/j.jchromb.2013.09.033.
Irisolidone, a major isoflavone found in Pueraria lobata flowers, exhibits a wide spectrum of bioactivities, while its metabolic pathway in vivo has not been investigated. In this study, an ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF MS) method was employed to investigate the in vivo metabolism of Irisolidone in rats. Plasma, bile, urine, and feces were collected from rats after a single 100mg/kg oral dose of Irisolidone. Protein precipitation, solid phase extraction (SPE) and ultrasonic extraction were used to prepare samples of plasma, bile/urine, and feces, respectively. A total of 46 metabolites were detected and tentatively identified based on the mass spectral fragmentation patterns, elution order or confirmed using available reference standards. The metabolic pathways of Irisolidone in rats included decarbonylation, reduction, demethylation, demethoxylation, dehydroxylation, hydroxylation, sulfation, and glucuronidation. The relative content of each metabolite was also determined to help understand the major metabolic pathways of Irisolidone in rats.