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Kushenol I Sale

(Synonyms: 苦参醇) 目录号 : GC60220

Kushenol I 是从苦参根部提取的一种天然产物。

Kushenol I Chemical Structure

Cas No.:99119-69-4

规格 价格 库存 购买数量
1mg
¥1,260.00
现货
5mg
¥3,150.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Kushenol I is a natural compound isolated from the roots of Sophora flavescens[1].

[1]. Rong Huang, et al. A new flavonoid from Sophora flavescens Ait., Natural Product Research, 31:19, 2228-2232.

Chemical Properties

Cas No. 99119-69-4 SDF
别名 苦参醇
Canonical SMILES O=C1[C@H](O)[C@@H](C2=CC=C(O)C=C2O)OC3=C(C[C@H](C(C)=C)C/C=C(C)\C)C(O)=CC(OC)=C13
分子式 C26H30O7 分子量 454.51
溶解度 DMSO : 100 mg/mL (220.02 mM; Need ultrasonic) 储存条件 4°C, protect from light
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2002 mL 11.0009 mL 22.0017 mL
5 mM 0.44 mL 2.2002 mL 4.4003 mL
10 mM 0.22 mL 1.1001 mL 2.2002 mL
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Research Update

A Novel Method for Identifying Parkin Binding Agents in Complex Preparations of Herbal Medicines

Oxid Med Cell Longev 2022 Jan 18;2022:3260243.PMID:35087614DOI:10.1155/2022/3260243.

Parkin is a crucial E3 ubiquitin ligase for initiating mitophagy through the PINK1/Parkin pathway. Regulating the expression and activity of parkin can remedy mitophagy and human disease. We developed an efficient method to isolate natural parkin ligands from herbal medicines by combining centrifugal ultrafiltration and liquid chromatography/mass spectrometry. The heterologous expression technology identified functionally active and pure parkin proteins. After evaluating the reliability of the method using DL-selenomethionine and DL-dithiothreitol as positive controls, this method was successfully applied to capture parkin ligands from Polygoni Cuspidati Rhizoma et Radix and Sophorae Flavescentis Radix. LC/MS identified seven novel parkin-targeting compounds, namely, 7,4'-dihydroxy-5-methoxy-8-(γ, γ-dimethylallyl)-flavanone, Kushenol I, kurarinone, sophoraflavanone G, torachrysone-8-O-glucoside, apigenin, and emodin, supported by the molecular docking analysis. Five of the seven novel compounds (Kushenol I, kurarinone, sophoraflavanone G, apigenin, and emodin) can activate parkin in in vitro autoubiquitination assays. Meanwhile, Kushenol I and kurarinone had antisteatosis activity in fat emulsion-damaged human hepatocytes. These results confirmed the effectiveness of the method for identifying parkin ligands from complex preparations, useful to advance drug discovery from medicinal herbs.

A new flavonoid from Sophora flavescens Ait

Nat Prod Res 2017 Oct;31(19):2228-2232.PMID:28278618DOI:10.1080/14786419.2017.1297992.

A new flavonoid, 8-(3-hydroxymethyl-2-butenyl)-5,7,2',4'-tetrahydroxyflavanone (1), along with seven known compounds, (2R)-3α,7,4'-Trihydroxy -5-methoxy-8-prenylflavanone (2), (2R)-3β,7,4'- Trihydroxy-5-methoxy-8-prenylflavanone (3), 3,7-dihydroxycoumarin (4), Shandougenines B (5), Specionin (6), Kushenol N (7) and Kushenol I (8) were isolated from the roots of Sophora flavescens. Among them, Compound 5 was isolated from Leguminous plants, and compounds 4 and 6 were isolated from Sophora flavescens for the first time. Their structures were elucidated by the aid of NMR, HRMS, HMBC and CD spectroscopic methods.

Inhibition of Cytochrome P450 Activities by Sophora flavescens Extract and Its Prenylated Flavonoids in Human Liver Microsomes

Evid Based Complement Alternat Med 2019 Mar 13;2019:2673769.PMID:31001351DOI:10.1155/2019/2673769.

Sophora flavescens possesses several pharmacological properties and has been widely used for the treatment of diarrhea, inflammation, abscess, dysentery, and fever in East Asian countries. S. flavescens is a major source of prenylated flavonoids, such as sophoraflavone and kushenol. In this study, we examined the effects of S. flavescens extract and its prenylated flavonoids on cytochrome P450 (CYP) isoform activity in human liver microsomes. The extract inhibited CYP2C8, CYP2C9, CYP2C19, and CYP3A activities, with IC50 values of 1.42, 13.6, 19.1, and 50 µg/mL, respectively. CYP2B6 was only inhibited in human liver microsomes preincubated with the extract. CYP3A4 was more strongly inhibited by the extract in the presence of NADPH, suggesting that the extract may inhibit CYP2B6 and CYP3A4 via mechanism-based inactivation. Prenylated flavonoids also inhibited CYP isoforms with different selectivity and modes of action. Kushenol I, leachianone A, and sophoraflavone G inhibited CYP2B6, whereas kushenol C, Kushenol I, kushenol M, leachianone A, and sophoraflavone G inhibited CYP3A4 via mechanism-based inhibition. Our results suggest that S. flavescens may contribute to herb-drug interactions when coadministered with drugs metabolized by CYP2B6, CYP2C8, CYP2C9, and CYP3A4.

Biosyntheses characterization of alkaloids and flavonoids in Sophora flavescens by combining metabolome and transcriptome

Sci Rep 2021 Apr 1;11(1):7388.PMID:33795823DOI:10.1038/s41598-021-86970-0.

Sophora flavescens are widely used for their pharmacological effects. As its main pharmacological components, alkaloids and flavonoids are distributed in the root tissues wherein molecular mechanisms remain elusive. In this study, metabolite profiles are analyzed using metabolomes to obtain biomarkers detected in different root tissues. These biomarkers include alkaloids, phenylpropanoids, and flavonoids. The high-performance liquid chromatography analysis results indicate the differences in principal component contents. Oxymatrine, sophoridine, and matrine contents are the highest in the phloem, whereas trifolirhizin, maackiain, and Kushenol I contents are the highest in the xylem. The transcript expression profiles also show tissue specificity in the roots. A total of 52 and 39 transcripts involved in alkaloid and flavonoid syntheses are found, respectively. Among them, the expression levels of LYSA1, LYSA2, AO2, AO6, PMT1, PMT17, PMT34, and PMT35 transcripts are highly and positively correlated with alkaloids contents. The expression levels of 4CL1, 4CL3, 4CL12, CHI5, CHI7, and CHI9 transcripts are markedly and positively correlated with flavonoids contents. Moreover, the quantitative profiles of alkaloids and flavonoids are provided, and the pivotal genes regulating their distribution in S. flavescens are determined. These results contribute to the existing data for the genetic improvement and target breeding of S. flavescens.

HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root)

Mol Divers 2011 May;15(2):361-72.PMID:21207144DOI:10.1007/s11030-010-9297-7.

An EtOAc extract from the roots of Sophora flavescens (Kushen) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes transiently expressing GABA(A) receptors with subunit composition, α (1) β (2) γ (2S). HPLC-based activity profiling of the extract led to the identification of 8-lavandulyl flavonoids, Kushenol I, sophoraflavanone G, (-)-kurarinone, and kuraridine as GABA(A) receptor modulators. In addition, a series of inactive structurally related flavonoids were characterized. Among these, kushenol Y (4) was identified as a new natural product. The 8-lavandulyl flavonoids are first representatives of a novel scaffold for the target.