Mosloflavone
(Synonyms: 5-羟基-6,7-二甲氧基黄酮) 目录号 : GC39097
Mosloflavone 从 Scutellaria baicalensis Georgi 中分离出的类黄酮，具有抗 EV71 活性。Mosloflavone 在病毒感染的初始阶段抑制 VP2 病毒复制和蛋白质表达，并抑制病毒 VP2 衣壳蛋白合成。 Mosloflavone 是有前途的杀菌剂，可抑制铜绿假单胞菌的毒力和生物膜形成。
Cas No.:740-33-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
[1]. 2.Choi HJ, et al. Inhibitory Effects of Norwogonin, Oroxylin A, and Mosloflavone on Enterovirus 71.Biomol Ther (Seoul). 2016 Sep 1;24(5):552-8. [2]. 2.Hnamte S, et al. Mosloflavone attenuates the quorum sensing controlled virulence phenotypes and biofilm formation in Pseudomonas aeruginosa PAO1: In vitro, in vivo and in silico approach.Microb Pathog. 2019 Jun;131:128-134. [3]. 4.Singh B, et al. Anti-inflammatory and immunomodulatory flavones from Actinocarya tibetica Benth.Nat Prod Res. 2013;27(23):2227-30.
| Cas No. | 740-33-0 | SDF | |
| 别名 | 5-羟基-6,7-二甲氧基黄酮 | ||
| Canonical SMILES | O=C1C=C(C2=CC=CC=C2)OC3=CC(OC)=C(OC)C(O)=C13 | ||
| 分子式 | C17H14O5 | 分子量 | 298.29 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 3.3524 mL | 16.7622 mL | 33.5244 mL |
| 5 mM | 0.6705 mL | 3.3524 mL | 6.7049 mL |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3524 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。
Mosloflavone-Resveratrol Hybrid TMS-HDMF-5z Exhibits Potent In Vitro and In Vivo Anti-Inflammatory Effects Through NF-κB, AP-1, and JAK/STAT Inactivation
Front Pharmacol 2022 Apr 21;13:857789.PMID:35529447DOI:10.3389/fphar.2022.857789.
TMS-HDMF-5z is a hybrid of the natural products Mosloflavone and resveratrol. It was discovered to show potent inhibitory effects against lipopolysaccharide (LPS)-induced production of inflammatory mediators in RAW 264.7 macrophages. However, its mechanism of action is unknown. Hence this study aimed to demonstrate and explore in vitro and in vivo anti-inflammatory effects of TMS-HDMF-5z and its mechanism of action employing RAW 264.7 macrophages and carrageenan-induced hind paw edema. This work revealed that TMS-HDMF-5z suppressed the LPS-induced inducible nitric-oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at the protein, mRNA, and promoter binding levels and tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6, and interferon-β (IFN-β) at the mRNA expression in RAW 264.7 macrophages. The results showed that TMS-HDMF-5z reduced the transcription and DNA binding activities of nuclear factor-κB (NF-κB) through inhibiting nuclear translocation of p65 and phosphorylation of κB inhibitor α (IκBα), IκB kinase (IKK), and TGF-β activated kinase 1 (TAK1). Additionally, TMS-HDMF-5z attenuated the LPS-induced transcriptional and DNA binding activities of activator protein-1 (AP-1) by suppressing nuclear translocation of phosphorylated c-Fos, c-Jun, and activating transcription factor 2 (ATF2). TMS-HDMF-5z also reduced the LPS-induced phosphorylation of Janus kinase 1/2 (JAK1/2), signal transducers and activators of transcription 1/3 (STAT1/3), p38 mitogen-activated protein kinase (MAPK), and MAPK-activated protein kinase 2 (MK2). In rats, TMS-HDMF-5z alleviated carrageenan-induced hind paw edema through the suppressing iNOS and COX-2 via NF-κB, AP-1, and STAT1/3 inactivation. Collectively, the TMS-HDMF-5z-mediated inhibition of NF-κB, AP-1, and STAT1/3 offer an opportunity for the development of a potential treatment for inflammatory diseases.
Mosloflavone attenuates the quorum sensing controlled virulence phenotypes and biofilm formation in Pseudomonas aeruginosa PAO1: In vitro, in vivo and in silico approach
Microb Pathog 2019 Jun;131:128-134.PMID:30959097DOI:10.1016/j.micpath.2019.04.005.
Quorum sensing (QS) is the cell density dependent communication network which coordinates the production of pathogenic determinants in majority of pathogenic bacteria. Pseudomonas aeruginosa causes hospital-acquired infections by virtue of its well-defined QS network. As the QS regulatory network in P. aeruginosa regulates the virulence determinants and antibiotic resistance, attenuating the QS system seems to be influential in developing next-generation anti-infective agents. In the current study, the QS attenuation potential of a flavonoid, Mosloflavone was investigated against P. aeruginosa virulence and biofilm formation. Mosloflavone inhibited the pyocyanin production, LasB elastase and chitinase by 59.52 ± 2.74, 35.90 ± 4.34 and 61.18 ± 5.52% respectively. The QS regulated biofilm formation and development was also reduced when supplemented with sub-MIC of Mosloflavone. The gene expression studies of Mosloflavone using RT-PCR depicted its ability to down-regulate the expression levels of QS regulated virulence genes such as lasI (60.64%), lasR (91.70%), rhlI (57.30%), chiC (90.20%), rhlA (47.87%), rhlR (21.55%), lasB (37.80%), phzM (42.40%), toxA (61.00%), aprA (58.4%), exoS (78.01%), algD (46.60%) and pelA (50.45%). The down-regulation of QS virulence phenotypes by Mosloflavone could be attributed to its binding affinity with the QS regulatory proteins, LasR and RhlR by competitively inhibiting the binding of natural autoinducers as evidenced from simulation studies. Mosloflavone also exhibited promising potential in controlling bacterial infection in Caenorhabditis elegans model system, in vivo. The anti-biofilm and anti-QS potential of Mosloflavone in the current study illustrated the candidature of Mosloflavone as a promising biocide.
Repurposing Mosloflavone/5,6,7-trimethoxyflavone-resveratrol hybrids: Discovery of novel p38-α MAPK inhibitors as potent interceptors of macrophage-dependent production of proinflammatory mediators
Eur J Med Chem 2019 Oct 15;180:253-267.PMID:31310917DOI:10.1016/j.ejmech.2019.07.030.
Herein, we address repurposing hybrids of Mosloflavone or 5,6,7-trimethoxyflavone with amide analogs of resveratrol from anticancer leads to novel potent anti-inflammatory chemical entities. To unveil the potent anti-inflammatory molecules, biological evaluations were initiated in LPS-induced RAW 264.7 macrophages at 1 μM concentration. Promising compounds were further evaluated at various concentrations. Multiple proinflammatory mediators were assessed including NO, PGE2, IL-6, TNF-α and IL-1β. Compound 5z inhibited the induced production of NO, PGE2, IL-6, TNF-α and IL-1β at the low 1 μM concentration by 44.76, 35.71, 53.48, 29.39 and 41.02%, respectively. Compound 5z elicited IC50 values as low as 2.11 and 0.98 μM against NO and PGE2 production respectively. Compounds 5q and 5g showed potent submicromolar IC50 values of 0.31 and 0.59 μM respectively against PGE2 production. Reverse docking of compound 5z suggested p38-α MAPK, which is a key signaling molecule within the pathways controlling the transcription of proinflammatory mediators, as the molecular target. Biochemical testing confirmed these compounds as p38-α MAPK inhibitors explaining its potent inhibition of proinflammatory mediators' production. Collectively, the results presented 5z as a promising compound for further development of anti-inflammatory agents for treatment of macrophages-and/or immune mediated inflammatory diseases.
Inhibitory Effects of Norwogonin, Oroxylin A, and Mosloflavone on Enterovirus 71
Biomol Ther (Seoul) 2016 Sep 1;24(5):552-8.PMID:27257010DOI:10.4062/biomolther.2015.200.
Severe complications associated with EV71 infections are a common cause of neonatal death. Lack of effective therapeutic agents for these infections underlines the importance of research for the development of new antiviral compounds. In the present study, the anti-EV71 activity of norwogonin, oroxylin A, and Mosloflavone from Scutellaria baicalensis Georgi was evaluated using a cytopathic effect (CPE) reduction method, which demonstrated that all three compounds possessed strong anti-EV71 activity and decreased the formation of visible CPEs. Norwogonin, oroxylin A, and Mosloflavone also inhibited virus replication during the initial stage of virus infection, and they inhibited viral VP2 protein expression, thereby inhibiting viral capsid protein synthesis. However, ribavirin has a relatively weaker efficacy compared to the other drugs. Therefore, these findings provide important information that will aid in the utilization of norwogonin, oroxylin A, and Mosloflavone for EV71 treatment.
Simultaneous Quantification of Five Bioactive Flavonoids in High Altitude Plant Actinocarya tibetica by LC-ESI-MS/MS
J AOAC Int 2015 Jul-Aug;98(4):907-12.PMID:26268971DOI:10.5740/jaoacint.14-270.
An LC/MS method has been developed for the simultaneous quantification of five flavonoids, i.e., Mosloflavone, negletein, gardenin B, 5-methoxy-6,7-methylenedioxyflavone, and 5,6,7-trimethoxyflavone, in different ultrasound assisted solvent extracts of Actinocarya tibetica. The chromatographic separation was achieved on a Chromolith Speed ROD RP-18e column with gradient elution using methanol and 0.1% formic acid in water. The calibration curves of all five analytes showed good linearity (R2>0.991). Accuracy and precision were within the required limits. The developed method could serve as an effective method for QC of A. tibetica. The investigated compounds were determined simultaneously for the first time in A. tibetica or any other plant.