Esculin (hydrate)
(Synonyms: Aesculin, Enallachrome) 目录号 : GC47306
A coumarin with antioxidant and anti-inflammatory activities
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
Esculin is a coumarin that has been found in A. hippocastanum and has antioxidant and anti-inflammatory activities.1,2 It reduces the size of gastric ulcers and decreases increases in the levels of malondialdehyde (MDA) and the activity of myeloperoxidase (MPO) and catalase in a mouse model of ethanol-induced ulcers when used at a dose of 25 mg/kg.1 Esculin (20 mg/kg) decreases LPS-induced increases in the levels of TLR4, MyD88, IRAK4, and phosphorylated NF-?B in the lung, as well as levels of IL-1β, IL-6, and TNF-α in the bronchoalveolar lavage fluid (BALF) in a mouse model of acute lung injury.2
1.Rios, E.R., Rocha, N.F., VenÂncio, E.T., et al.Mechanisms involved in the gastroprotective activity of esculin on acute gastric lesions in miceChem. Biol. Interact.188(1)246-254(2010) 2.Tianzhu, Z., and Shumin, W.Esculin inhibits the inflammation of LPS-induced acute lung injury in mice via regulation of TLR/NF-κB pathwaysInflammation38(4)1529-1536(2015)
| Cas No. | N/A | SDF | |
| 别名 | Aesculin, Enallachrome | ||
| Canonical SMILES | O=C1C=CC2=CC(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)=C(O)C=C2O1.O | ||
| 分子式 | C15H16O9.XH2O | 分子量 | 340.3 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 16 mg/ml,Ethanol: 3 mg/ml,PBS (pH 7.2): 5 mg/ml | 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 | 2.9386 mL | 14.6929 mL | 29.3858 mL |
| 5 mM | 0.5877 mL | 2.9386 mL | 5.8772 mL |
| 10 mM | 0.2939 mL | 1.4693 mL | 2.9386 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。
Inhibition of five natural products from Chinese herbs on the growth of Chattonella marina
Environ Sci Pollut Res Int 2016 Sep;23(17):17793-800.PMID:27250087DOI:10.1007/s11356-016-6755-5.
The effects of five natural products from Chinese herbs including evodiamine, curcumin, 4-methoxysalicylaldehyde, Esculin hydrate, and gramine on the growth of Chattonella marina, one of the most noxious red tide algae, were observed. Among them, gramine exhibited the highest inhibitory rate with LC50, 96h of 0.51 mg/l. After exposure to gramine, the activities of superoxide dismutase (SOD) and catalase (CAT), and content of malondialdehyde (MDA) increased in C. marina, suggesting that gramine could induce microalgae oxidative stress. In addition, chlorophyll a and the maximum quantum yield of photosynthesis (Fv/Fm) decreased following exposure to gramine, indicating the inhibition of photosynthesis activity in the microalgae. Combined with the fast inhibition against the algal cells and environmentally friendly character of gramine, we proposed that gramine might be a potential algaecide against marine harmful algae and that the oxidative damage and photosynthesis inhibition might be responsible for the toxicity of gramine on harmful algae.
Sub-Inhibitory Concentrations of Ciprofloxacin Alone and Combinations with Plant-Derived Compounds against P. aeruginosa Biofilms and Their Effects on the Metabolomic Profile of P. aeruginosa Biofilms
Antibiotics (Basel) 2021 Apr 9;10(4):414.PMID:33918895DOI:10.3390/antibiotics10040414.
Introduction: Alternative anti-biofilm agents are needed to combat Pseudomonas aeruginosa infections. The mechanisms behind these new agents also need to be revealed at a molecular level. Materials and methods: The anti-biofilm effects of 10 plant-derived compounds on P. aeruginosa biofilms were investigated using minimum biofilm eradication concentration (MBEC) and virulence assays. The effects of ciprofloxacin and compound combinations on P. aeruginosa in mono and triple biofilms were compared. A metabolomic approach and qRT-PCR were applied to the biofilms treated with ciprofloxacin in combination with baicalein, Esculin hydrate, curcumin, and cinnamaldehyde at sub-minimal biofilm inhibitory concentration (MBIC) concentrations to highlight the specific metabolic shifts between the biofilms and to determine the quorum sensing gene expressions, respectively. Results: The combinations of ciprofloxacin with curcumin, baicalein, esculetin, and cinnamaldehyde showed more reduced MBICs than ciprofloxacin alone. The quorum sensing genes were downregulated in the presence of curcumin and cinnamaldehyde, while upregulated in the presence of baicalein and Esculin hydrate rather than for ciprofloxacin alone. The combinations exhibited different killing effects on P. aeruginosa in mono and triple biofilms without affecting its virulence. The findings of the decreased metabolite levels related to pyrimidine and lipopolysaccharide synthesis and to down-regulated alginate and lasI expressions strongly indicate the role of multifactorial mechanisms for curcumin-mediated P. aeruginosa growth inhibition. Conclusions: The use of curcumin, baicalein, esculetin, and cinnamaldehyde with ciprofloxacin will help fight against P. aeruginosa biofilms. To the best of our knowledge, this is the first study of its kind to define the effect of plant-based compounds as possible anti-biofilm agents with low MBICs for the treatment of P. aeruginosa biofilms through metabolomic pathways.
Identification of compounds that inhibit the binding of Keap1a/Keap1b Kelch DGR domain with Nrf2 ETGE/DLG motifs in zebrafish
Basic Clin Pharmacol Toxicol 2019 Sep;125(3):259-270.PMID:30861618DOI:10.1111/bcpt.13222.
The Keap1-Nrf2-ARE system serves as a premier defence mechanism to curb oxidative stress, which remains as one of the major causes of ageing and pathogenesis in various diseases. Nrf2 is the principal master regulator of the cellular defence system, and its activation remains the prospective therapeutic approach against chronic diseases. One of the recent strategies is to disrupt Keap1-Nrf2 protein-protein interaction (PPI) that alters the docking of Keap1 with Nrf2 by compounds occupying a position in the Keap1 blocking the interface with Nrf2. In this study, we made an attempt to identify the compounds with anticancer, antioxidant and anti-inflammatory properties to disrupt Keap1a/b-Nrf2 PPI through in silico molecular docking in zebrafish. The phylogenetic analysis of Keap1 proteins revealed the existence of orthologous Keap1-Nrf2-ARE system in lower vertebrates that includes zebrafish. The DGR domains of zebrafish Keap1a and Keap1b were modelled with Modeller 9.19 using Keap1 of Mus musculus (PDB ID:5CGJ) as template. Based on the docking calculations, top hit compounds were identified to disrupt both Keap1a and Keap1b interaction with Nrf2 which include quercetin 3,4'-diglucoside, flavin adenine dinucleotide disodium salt hydrate, salvianolic acid A, tunicamycin and Esculin. The LC50 of Esculin in 3 dpf zebrafish larvae is 5 mmol/L, and the qRT-PCR results showed that Esculin significantly increased the transcription of Nrf2 target genes-Gstpi, Nqo1, Hmox1a and Prdx1 in 3 dpf zebrafish larvae. These potential hits could serve as safer Nrf2 activators due to their non-covalent disruption of Keap1-Nrf2 PPI and be developed into efficacious preventive/therapeutic agents for various diseases.
Characterization of cellulolytic activity in the gut of the terrestrial land slug Arion ater: Biochemical identification of targets for intensive study
Comp Biochem Physiol B Biochem Mol Biol 2014 Nov-Dec;177-178:29-35.PMID:25150536DOI:10.1016/j.cbpb.2014.08.003.
The level of cellulolytic activity in different areas of the gut of the terrestrial slug Arion ater was assayed at different temperatures and pH values. To do this, crude gut proteins were isolated and assayed using modified dinitrosalicylic acid reducing sugar assay. Crude protein samples were also separated and cellulolytic activity identified using in gel CMC zymography and Esculin hydrate activity gel assays. pH and temperature profiling revealed optimum cellulolytic activity between pH5.0 and 6.0 for different gut regions and retention of up to 90% of activity at temperatures up to 50°C. Zymograms and activity gels revealed multiple endoglucanase and β-glucosidase enzymes. To further investigate the source of this cellulolytic activity bacterial isolates from the gut were tested for endoglucanase and β-glucosidase activity using growth plate assays. 12 cellulolytic microbes were identified using 16S rDNA gene sequencing. These include members of the genera Buttiauxella, Enterobacter, Citrobacter, Serratia and Klebsiella. Gut metagenomic DNA was then subjected to PCR, targeting a 400bp region of the 16SrDNA gene which was subsequently separated and individuals identified using DGGE. This identified members of the genera Citrobacter, Serratia, Pectobacterium, Acinetobacter, Mycoplasma, Pantoea and Erwinia. In summary, multiple glycoside hydrolase enzymes active over a broad range of temperature and pH values in a relatively under studied organism were detected, indicating that the gut of A. ater is a viable target for intensive study to identify novel carbohydrate active enzymes that may be used in the biofuel industry.