Nepetin
(Synonyms: 泽兰黄酮,6-Methoxyluteolin) 目录号 : GC38568
Nepetin (6-Methoxyluteolin) 是从 Eupatorium ballotaefolium HBK 分离的天然类黄酮，具有有效的抗炎活性。Nepetin 在 ARPE-19 细胞中抑制 IL-6，IL-8 和 MCP-1 分泌，IC50 值分别为 4.43 μM、3.42 μM 和 4.17 μM。
Cas No.:520-11-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nepetin (6-Methoxyluteolin) is a natural flavonoid isolated from Eupatorium ballotaefolium HBK with potent anti-inflammatory activities. Nepetin inhibits IL-6, IL-8 and MCP-1 secretion with IC50 values of 4.43 μM, 3.42 μM and 4.17 μM, respectively in ARPE-19 cells[1][2].
Pretreatment with Nepetin dose-dependently inhibited IL-6, IL-8 and MCP-1 secretion with IC50 values of 4.43, 3.42 and 4.17 μM, respectively[1].Nepetin (2.5-10 μM; 25 hours; ARPE-19 cells) treatment suppresses IL-1β-induced cytokine (IL-6, IL-8 and MCP-1) expression at mRNA level in ARPE-19 cells[1].Nepetin (2.5-10 μM; 1.5 hours; ARPE-19 cells) treatment dose-dependently inhibits phosphorylation of IKKα/β and IκBα, and nuclear translocation of p65. Nepetin decreases the level of phosphorylated ERK1/2, JNK and p38 MAPK in activated ARPE-19 cells[1]. RT-PCR[1] Cell Line: ARPE-19 cells
[1]. Chen X, et al. Nepetin inhibits IL-1β induced inflammation via NF-κB and MAPKs signaling pathways in ARPE-19 cells. Biomed Pharmacother. 2018 May;101:87-93. [2]. MilitÃo GC, et al. Cytotoxic activity of nepetin, a flavonoid from Eupatorium ballotaefolium HBK. Pharmazie. 2004 Dec;59(12):965-6.
| Cas No. | 520-11-6 | SDF | |
| 别名 | 泽兰黄酮,6-Methoxyluteolin | ||
| Canonical SMILES | O=C1C=C(C2=CC=C(O)C(O)=C2)OC3=CC(O)=C(OC)C(O)=C13 | ||
| 分子式 | C16H12O7 | 分子量 | 316.26 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, away from moisture and 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 | 3.162 mL | 15.8098 mL | 31.6196 mL |
| 5 mM | 0.6324 mL | 3.162 mL | 6.3239 mL |
| 10 mM | 0.3162 mL | 1.581 mL | 3.162 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。
Nepetin reduces virulence factors expression by targeting ClpP against MRSA-induced pneumonia infection
Virulence 2022 Dec;13(1):578-588.PMID:35363605DOI:10.1080/21505594.2022.2051313.
The resistance of Staphylococcus aureus (S. aureus) to various antibiotics has increased dramatically due to the misuse of antibiotics, and thus the development of new anti-infective drugs with new targets is urgently needed to combat resistance. Caseinolytic peptidase P is a case in hydrolase that regulates the virulence level of S. aureus. Here, we found that Nepetin, a small-molecule compound from traditional Chinese herbal flavonoids, effectively inhibits ClpP activity. Nepetin suppressed the virulence of S. aureus and effectively combated the lethal pneumonia caused by MRSA. The results of cellular thermal shift assay showed that Nepetin could bind to ClpP and reduce the thermal stability of ClpP, and the KD value of 602 nM between them was determined using localized surface plasmon resonance. The binding mode of Nepetin and ClpP was further investigated by molecular docking, and it was found that Ser-22 and Gln-47 of ClpP residues were found to be involved in the binding of Nepetin to ClpP. In conclusion, we determined that Nepetin is a ClpP inhibitor and an effective lead compound for the development of a virulence factor-based treatment for MRSA infection.
Nepetin Acts as a Multi-Targeting Inhibitor of Protein Tyrosine Phosphatases Relevant to Insulin Resistance
Chem Biodivers 2022 Jan;19(1):e202100600.PMID:34725898DOI:10.1002/cbdv.202100600.
Protein tyrosine phosphatases (PTPs) are essential modulators of signal transduction pathways and has been implicated in many human diseases such as cancer, diabetes, obesity, autoimmune disorders, and neurological diseases, indicating that PTPs are next-generation drug targets. Since PTPN1, PTPN2, and PTPN11 have been reported to be negative regulators of insulin action, the identification of PTP inhibitors may be an effective strategy to develop therapeutic agents for the treatment of type 2 diabetes. In this study, we observed for the first time that Nepetin inhibits the catalytic activity of PTPN1, PTPN2, and PTPN11 in vitro, indicating that Nepetin acts as a multi-targeting inhibitor of PTPN1, PTPN2, and PTPN11. Furthermore, treatment of mature 3T3-L1 adipocytes with 20 μM Nepetin stimulates glucose uptake through AMPK activation. Taken together, our findings provide evidence that Nepetin, a multi-targeting inhibitor of PTPN1, PTPN2, and PTPN11, could be a promising therapeutic candidate for the treatment of type 2 diabetes.
Nepetin, a natural compound from Inulae flos, suppresses degranulation and eicosanoid generation through PLCγ1 and Akt signaling pathways in mast cells
Arch Pharm Res 2020 Feb;43(2):224-232.PMID:32016828DOI:10.1007/s12272-020-01212-7.
Nepetin derived from the flowers of Inula japonica, Inulae flos, has been reported to exert several biological activities, including anti-inflammatory responses. In this study, we evaluated the anti-allergic property of Nepetin with its molecular mechanisms in bone marrow-derived mast cells (BMMC) and mice. In this in vitro study, we investigated the inhibitory effects of Nepetin on degranulation and generation of leukotriene C4 (LTC4) and prostaglandin D2 (PGD2) in IgE/antigen (Ag)-stimulated BMMC. The effect of Nepetin on passive cutaneous anaphylaxis (PCA) reaction was also studied in mice. Nepetin reduced degranulation and LTC4 generation in BMMC. The IgE/Ag-mediated signaling pathway demonstrated that Nepetin suppressed intracellular Ca2+ level and activation of PLCγ1 and cPLA2. However, MAPKs were not affected by Nepetin in BMMC. In addition, Nepetin treatment reduced PGD2 production and suppressed cyclooxygenase-2 protein expression via the inhibition of the Akt and nuclear factor-κB signaling pathways. With respect to the local allergic response in vivo, oral administration of Nepetin suppressed mast cell-dependent PCA reaction in a dose-dependent manner. The results of this study suggest that Nepetin might have an anti-allergic potential related to mast cell-mediated inflammatory diseases.
Nepetin inhibits osteoclastogenesis by inhibiting RANKL-induced activation of NF-κB and MAPK signalling pathway, and autophagy
J Cell Mol Med 2020 Dec;24(24):14366-14380.PMID:33135301DOI:10.1111/jcmm.16055.
Aseptic prosthetic loosening due to wear particle-induced inflammatory osteolysis is the main cause of failure for artificial joint replacement. The inflammatory response and the production of pro-osteoclastic factors lead to elevation of osteoclast formation and excessive activity results in extensive bone destruction around the bone-implant interface. Here we showed that Nepetin, a natural bioactive flavonoid with proven anti-inflammatory and anti-proliferative properties, potently inhibited RANKL-induced osteoclast differentiation, formation and bone resorption in vitro, and protected mice against the deleterious effects of titanium particle-induced calvarial osteolysis in vivo. Mechanistically, Nepetin attenuated RANKL-induced activation of NF-κB and MAPK signalling pathways and TRAF6-dependent ubiquitination of Beclin 1 which is necessary for the induction of autophagy. In brief, our study demonstrates the potential therapeutic application of Nepetin against osteoclast-mediated osteolytic diseases.
Nepetin inhibits IL-1β induced inflammation via NF-κB and MAPKs signaling pathways in ARPE-19 cells
Biomed Pharmacother 2018 May;101:87-93.PMID:29477475DOI:10.1016/j.biopha.2018.02.054.
Backgrounds: Chronic inflammation in retinal pigment epithelial (RPE) cells is related to the pathogenesis of retinal inflammatory blind causing diseases such as age-related macular degeneration (AMD) and diabetic retinopathy (DR). Nepetin, a natural flavonoid compound, has shown potent anti-inflammatory activities but has not been studied on ocular resident cells yet. Here, we assess the ability of Nepetin to alleviate the inflammatory responses of ARPE-19 cells induced by interleukin (IL)-1β. Methods: The secretion and mRNA expression of inflammatory cytokines IL-6, IL-8 and monocyte chemoattractant protein-1 (MCP-1) induced by IL-1β are measured by enzyme-linked immunosorbent assay (ELISA) and real-time polymerase chain reaction (RT-PCR) respectively. To clarify the underlying action mechanism, we examine the effect of Nepetin on activation of nuclear factor of kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways using Western blot. Results: Nepetin can significantly decrease the three inflammatory mediators at both protein and mRNA level in a dose-dependent manner. Western blot results show that Nepetin can decrease the nuclear translocation of p65 through suppressing phosphorylation of inhibitor of nuclear factor kappa B (IκB) and IκB kinase (IKK). Also, Nepetin can decrease the phosphorylation of extracellular signal-regulated kinases (ERK) 1/2, c-Jun N-terminal kinase (JNK) and p38 MAPK. Conclusions: Taken together, Nepetin abolishes IL-1β-induced IL-6, IL-8 and MCP-1 secretion and mRNA expression by repressing the activation of NF-κB and MAPKs. These results indicate that Nepetin shows potential to be used for prevention and treatment of inflammatory retinal diseases or as a lead compound.