标签归档：leachianone

Kushenol A(Synonyms: Leachianone E)

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Kushenol A (Synonyms: Leachianone E)

Kushenol A (Leachianone E) 从苦参根中分离出来的。Kushenol A 是一种非竞争性酪氨酸酶 (tyrosinase) 抑制剂，可阻止 L-tyrosinase 转化为 L-DOPA，IC50 和 Ki 值分别为 1.1 μM 和 0.4 μM。Kushenol A 是一种类黄酮抗氧化剂，对 α-葡萄糖苷酶 (alpha-glucosidase) (IC50: 45 μM; Ki: 6.8 μM) 和 β-淀粉酶 (beta-amylase) 具有抑制作用。Kushenol A 被认为是化妆品针对皮肤美白和衰老的潜在酶抑制剂。

Kushenol A(Synonyms: Leachianone E)

Kushenol A Chemical Structure

CAS No. : 99217-63-7

规格 价格 是否有货
5 mg ￥8500 询问价格 & 货期
10 mg ￥15000 询问价格 & 货期

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Kushenol A 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Phenols Library
  • Traditional Chinese Medicine Monomer Library
  • Flavonoids Library
  • Anti-Lung Cancer Compound Library
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  • Glucose Metabolism Compound Library

生物活性

Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively[1]. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase[2]. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging[1].

IC50 & Target

IC50: 1.1 μM (tyrosinase); 45 μM (alpha-glucosidase)[1][2]
体外研究
(In Vitro)

Kushenol A (25 μM) exhibits a highly potent inhibitory activity on ABTS+ radical scavenging with an IC50 value of 9.7 ± 0.1 μM, and exhibits inhibits scavenging activity as a percentage 93.7% at 25 μM[1].
Kushenol A (0-60 μg/ml; 24 hours) shows considerable cytotoxic effects against NSCLC cells, exhibits IC50 values of 5.3 μg/ml and 20.5 μg/ml for A549 and NCI‐H226 cells, respectively. It shows an IC50 value of 57.2 μg/ml for BEAS-2B cells[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: NSCLC cell lines, A549 and NCI-H226
Normal human lung epithelial: BEAS-2B
Concentration: 0-60 μg/ml
Incubation Time: 24 hours
Result: Exhibited considerable cytotoxic effects against NSCLC cells.

分子量

408.49

Formula

C25H28O5
CAS 号

99217-63-7
中文名称

苦参新醇A
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献

  • [1]. Kim JH, et al. Kushenol A and 8-prenylkaempferol, tyrosinase inhibitors, derived from Sophora flavescens. J Enzyme Inhib Med Chem. 2018 Dec;33(1):1048-1054.

    [2]. Kim JH, et al. Glycosidase inhibitory flavonoids from Sophora flavescens. Biol Pharm Bull. 2006 Feb;29(2):302-5.

    [3]. Chen H, et al. A Novel Flavonoid Kushenol Z from Sophora flavescens Mediates mTOR Pathway by Inhibiting Phosphodiesterase and Akt Activity to Induce Apoptosis in Non-Small-Cell Lung Cancer Cells.Molecules. 2019 Dec 4;24(24). pii: E4425.

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Leachianone A

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Leachianone A 

Leachianone A 从槐花中分离，具有抗疟疾，抗炎和细胞毒性作用。 Leachianone A 诱导细胞凋亡 (apoptosis)。

Leachianone A

Leachianone A Chemical Structure

CAS No. : 97938-31-3

规格 价格 是否有货
1 mg ￥1600 询问价格 & 货期
5 mg ￥3500 询问价格 & 货期
10 mg ￥6000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent[1]. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways[2].

体外研究
(In Vitro)

Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC50 values are 6.9 μg/ml, 3.4 μg/ml and 2.8 μg/ml in cells with 24-, 48- and 72-hours treatment, respectively[1].
Leachianone A (10-30 μg/ml; 48 hours) indicates that at low concentration of LA (10 μg/ml), a substantial amount of cells is primarily in the early phase of apoptosis, at higher concentrations, induces a shift of the cell population to late apoptotic/ necrotic stage[1].
Leachianone A (10-30 μg/ml; 48 hours) decreases the precursor of caspase-3 in a dose-dependent manner, reduces the protein level of the pro-forms of upstream initiator caspases, caspases-8 and -9, decreases two downstream substrates, namely inhibitor of caspase-activated DNase(ICAD) and poly-ADP-ribose polymerase (PARP) in HepG2 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HepG2 cells
Concentration: 0 μg/ml, 2 μg/ml, 4 μg/ml, 6 μg/ml, 8 μg/ml, 10 μg/ml, 12 μg/ml, 14 μg/ml, 16 μg/ml, 18 μg/ml, 20 μg/ml
Incubation Time: 24-72 hours
Result: Inhibited HepG2 cells survival.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 48 hours
Incubation Time: 10, 20, and 30 μg/ml
Result: Induced the proportion of annexin V-stained cells in both the early and late apoptotic stage.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 48 hours
Incubation Time: 10, 20, and 30 μg/ml
Result: Decreased the protein expression of caspase-3, caspases-8 and -9, reduced ICAD and PARP protein expression.

体内研究
(In Vivo)

Leachianone A (intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days) significantly diminishes the tumor volume by 17-54% in LA-treated nude mice, when compared with those solely given the vehicle[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male nude mice with human hepatoma HepG2 cells[1]
Dosage: 20 mg/kg; 30 mg/kg
Administration: Intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days
Result: Suppressed the tumor growth in vivo.

分子量

438.51

Formula

C26H30O6
CAS 号

97938-31-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Jeong GS, et al. Lavandulyl flavanones from Sophora flavescens protect mouse hippocampal cells against glutamate-induced neurotoxicity via the induction of heme oxygenase-1. Biol Pharm Bull. 2008 Oct;31(10):1964-7.

    [2]. Cheung CS, et al. Leachianone A as a potential anti-cancer drug by induction of apoptosis in human hepatoma HepG2 cells. Cancer Lett. 2007 Aug 18;253(2):224-35. Epub 2007 Mar 26.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务