Ombuin
(Synonyms: 商陆黄素) 目录号 : GC60276
Ombuin 是从花椒中分离出的，具有广谱抗菌作用，MIC 为 125 至 500 μg/mL。
Cas No.:529-40-8
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
Ombuin, isolated from Zanthoxylum armatum, displays broad spectrum antibacterial effect with MIC ranges from 125 to 500 μg/mL[1].
[1]. Nooreen Z, et al. Characterization and evaluation of bioactive polyphenolic constituents from Zanthoxylum armatum DC., a traditionally used plant. Biomed Pharmacother. 2017 May;89:366-375.
| Cas No. | 529-40-8 | SDF | |
| 别名 | 商陆黄素 | ||
| Canonical SMILES | O=C1C2=C(O)C=C(OC)C=C2OC(C3=CC(O)=C(OC)C=C3)=C1O | ||
| 分子式 | C17H14O7 | 分子量 | 330.29 |
| 溶解度 | DMSO : 100 mg/mL (302.76 mM; Need ultrasonic) | 储存条件 | |
| 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 | 3.0276 mL | 15.1382 mL | 30.2764 mL |
| 5 mM | 0.6055 mL | 3.0276 mL | 6.0553 mL |
| 10 mM | 0.3028 mL | 1.5138 mL | 3.0276 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。
Ombuin ameliorates diabetic nephropathy in rats by anti-inflammation and antifibrosis involving Notch 1 and PPAR γ signaling pathways
Drug Dev Res 2022 Sep;83(6):1270-1280.PMID:35672933DOI:10.1002/ddr.21956.
Diabetic nephropathy (DN) is a common complication of diabetes and it is urgent to develop effective therapies for DN. In this study, high-sucrose and high-fat diet combined with streptozotocin was used to induce DN in rats to observe the effects of natural flavonoid Ombuin on renal function, inflammation, and interstitial fibrosis. Immunohistochemistry and western blotting analysis were used to detect protein expression levels. Results showed that Ombuin significantly improved renal function and pathological injury, inhibited accumulation of advanced glycation end-products, suppressed the release of inflammatory cytokines, and improved renal interstitial fibrosis in DN rats. Ombuin also significantly downregulated the expressions of transforming growth factor beta1 (TGF-β1), connective tissue growth factor (CTGF), fibronectin (FN), p65, phosphorylated (p)-p65, Cleaved-Notch 1, and hairy and enhancer of split 1 (Hes 1), and upregulated the expression of peroxisome proliferator-activated receptor γ (PPAR γ). When PPAR γ activity was inhibited by T0070907, the effects of Ombuin on improving DN were significantly reversed, and the expressions of TGF-β1, FN, CTGF, p-p65, and p65 increased, while the expressions of Cleaved-Notch 1 and Hes 1 were not significantly affected. These results suggest that Ombuin may activate PPAR γ to exert anti-inflammatory and antifibrotic effects by inhibiting Notch 1 activity in DN. It is also possible that Ombuin acts on these two independent signal pathways synchronously.
Preparative separation of quercetin, Ombuin and kaempferide from Gynostemma pentaphyllum by high-speed countercurrent chromatography
J Chromatogr Sci 2019 Mar 1;57(3):265-271.PMID:30566585DOI:10.1093/chromsci/bmy110.
An efficient method for the preparative separation of quercetin, Ombuin and kaempferide from Gynostemma pentaphyllum by high-speed countercurrent chromatography (HSCCC) was successfully developed for the first time. The extraction conditions were optimized by an orthogonal array design L9 (34), while quercetin, Ombuin and kaempferide were efficiently released from rutin, ombuoside and kaempferide glucoside by hydrochloric acid hydrolysis, respectively. Quercetin was purified by HSCCC with two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (4:5:4:5, v/v) in a single run. From 164.7 mg of the crude extract, 90.5 mg quercetin at 99.23% purity was obtained. Ombuin and kaempferide were purified by HSCCC with two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (8:2:5:5, v/v) in a single run. From 50 mg of the crude extract, 0.4 mg of Ombuin at 95.46% purity and 1.1 mg of kaempferide at 98.78% purity were obtained, respectively. Their structures were identified by ultraviolet, Fourier transform infrared, electrospray ionization mass spectrometry (ESI-MS), 1H nuclear magnetic resonance (NMR) and 13C NMR spectra. The purified quercetin had the strongest 1,1-diphenyl-2-picrylhydrazyl and hydroxyl free radical scavenging activities.
Molecular dynamics simulation and pharmacokinetics studies of Ombuin and quercetin against human pancreatic α-amylase
J Biomol Struct Dyn 2022 Dec 16;1-8.PMID:36524470DOI:10.1080/07391102.2022.2155699.
Diabetes mellitus (DM) is a group of metabolic disorders characterised by chronic hyperglycaemia. DM is currently one of the top ten causes of death in humans. Chronic hyperglycaemia in DM leads to long-term damage and failure of different organs in the body. Type 2 DM (T2D) is the most common DM form, characterised by peripheral insulin resistance, relative insulin deficiency, impaired hepatic glucose production regulation and pancreatic β cell dysfunction. The human pancreatic α-amylase (HPA) inhibitor is currently one of the most effective methods developed to inhibit hyperglycaemia in T2D patients. However, the current standard drug available, acarbose, has been associated with severe side effects following prolonged use in patients. Therefore, an alternative drug capable of effectively inhibiting HPA with minimal side effects is required. Based on our previous study, we further explored the therapeutic potential of quercetin and Ombuin via molecular dynamics (MD) simulation. The Desmond Simulation Package was used to run 100-ns MD simulations to examine the steady nature and conformational stability of the ligand-HPA complexes. Post-simulation molecular mechanics-generalised born surface area (MM-GBSA) analysis of HPA's binding free energy with quercetin and Ombuin was explored. The lead compounds' drug-likeness, absorption, distribution, metabolism and elimination properties were also studied using the SwissADME tool. These results indicate that quercetin and Ombuin have great potential as anti-DM drugs with more favourable properties than acarbose.Communicated by Ramaswamy H. Sarma.
Therapeutic potential of Chromolaena odorata phyto-constituents against human pancreatic α-amylase
J Biomol Struct Dyn 2022 Mar;40(4):1801-1812.PMID:33054572DOI:10.1080/07391102.2020.1833758.
Type II Diabetes Mellitus (DM) is caused by insulin resistance in peripheral tissue and impaired insulin secretion through a dysfunction of the pancreatic β-cell. Acarbose is an anti-DM drug, it is effective but its continuous use may lead to undesirable side effects. Hence, the development of novel drugs from natural source that have both anti-diabetic and anti-oxidant activities, with little or no side effect during long-term use is of great importance. To investigate the anti-DM and anti-oxidant phyto-constituents of Chromoleana odorata, e-pharmacophore model was generated using human pancreatic α-amylase (HPA) standard inhibitor, Acarbose to map important pharmacophoric features of HPA, and used to screen several phyto-constituents of C. odorata to match at least 4 sites of the generated hypothesis. Glide and Induced Fit Docking followed by Prime MM-GBSA calculation, drug-likeness and ADME studies were employed for high fitness (>1.0) compounds retrieved from e-pharmacophore screening process. The drug-likeness properties of the lead compounds, Quercetin and Ombuin were analyzed taking into account the Lipinski's and Veber's rules. Further, machine-learning approach was used to generate QSAR model. The computed model, kpls_desc_19 was used to predict the bioactivity (pIC50) of Quercetin and Ombuin. Phyto-constituents of C. odorata; Quercetin and Ombuin have shown better and promising results when compared to that of the standard, acarbose. Based on the present study, orally delivered Quercetin and Ombuin from C. odorata are relatively better inhibitor of HPA, thus they can be a useful therapeutic candidate in the management/treatment of DM when compared to acarbose.Communicated by Ramaswamy H. Sarma.
In vitro antimycobacterial studies of flavonols from Bauhinia vahlii Wight and Arn
3 Biotech 2021 Mar;11(3):128.PMID:33614388DOI:10.1007/s13205-021-02672-4.
Mycobacterial infections and fast-growing strains are increasing globally with 8 million new cases and 1.8 million fatalities per annum worldwide. The acid-fast bacterium, Mycobacterium tuberculosis (M.t), can spread diseases like tuberculosis (Tb) and weaken the immune system. In Ayurveda, the Bauhinia genus is most valued for the treatment of tuberculosis lymphadenitis. The objective of the present study is to identify anti-tubercular compounds from the under-investigated medicinal plant B. vahlii Wight and Arn. using bioassay guided isolation. The antimycobacterial activity was evaluated against non-virulent strains: Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743). Also, antibacterial and cytotoxicity activities were tested to identify the specificity of the isolated metabolites. Bioassay-guided isolation yielded three known flavonols, namely quercetin (1), Ombuin (2), and kaempferol (3), from the methanolic extract of bark of B. vahlii. The results of antimycobacterial activity tests revealed that 2 showed much better mycobactericidal activity than 1 and 3 under ex vivo condition with minimum inhibitory concentration (MIC) values ranged from 0.05 ± 0.01 to 0.26 ± 0.01 nM, and half-maximal inhibitory concentration (IC50) values ranged from 2.85 ± 0.14 to 7.21 ± 1.09 nM against dormant and active forms, respectively. Also, compound 2 showed higher resistance with MIC values > 100 μg/mL against both Gram-positive and Gram-negative bacteria and the least cytotoxicity up to 100 μg/mL concentration against the tested series of cancer cell lines. The results revealed the Ayurvedic use of extracts of the Bauhinia genus for treating tuberculosis, and the key bioactive compounds were found to be flavonols (1-3). The present work provides the first evidence for the presence of antimycobacterial compounds in B. vahlii. Supplementary information: The online version contains supplementary material available at 10.1007/s13205-021-02672-4.