Kuwanon H
(Synonyms: 桑皮酮 H；桑黄酮 H) 目录号 : GC38510
Kuwanon H 是桑白皮中的黄酮类化合物，为非肽类蛙皮素受体 (bombesin receptor) 拮抗剂。Kuwanon H 可特异性抑制细胞内胃泌激素释放肽 CRP 与(GRP-preferring recepotr) 受体的结合，Ki 值为 290 nM。
Cas No.:76472-87-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells[1].
[1]. Mihara S, et al. Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9.
| Cas No. | 76472-87-2 | SDF | |
| 别名 | 桑皮酮 H；桑黄酮 H | ||
| Canonical SMILES | OC1=CC(O)=C(C(C(C/C=C(C)/C)=C(C2=C(C=C(O)C=C2)O)O3)=O)C3=C1[C@@H]4[C@H]([C@H](C5=C(C=C(O)C=C5)O)CC(C)=C4)C(C6=C(C(C/C=C(C)/C)=C(O)C=C6)O)=O | ||
| 分子式 | C45H44O11 | 分子量 | 760.82 |
| 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 | 1.3144 mL | 6.5719 mL | 13.1437 mL |
| 5 mM | 0.2629 mL | 1.3144 mL | 2.6287 mL |
| 10 mM | 0.1314 mL | 0.6572 mL | 1.3144 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。
Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry
Biochem Biophys Res Commun 1995 Aug 15;213(2):594-9.PMID:7646517DOI:10.1006/bbrc.1995.2173.
Kuwanon G and H, isolated from the methanol extract of Morus bombycis, inhibited specific binding of [125I]gastrin-releasing peptide (GRP) to GRP-preferring receptors in murine Swiss 3T3 fibroblasts with Ki values of 470 and 290 nM, respectively. Kuwanon H was one order of magnitude less potent for inhibiting [125I]bombesin binding to neuromedin B (NMB)-preferring receptors in rat esophagus membranes. This compound antagonized bombesin-induced increases in the cytosolic free calcium concentration and GRP-induced DNA synthesis in Swiss 3T3 cells. Thus, Kuwanon H, and possibly kuwanon G also, are specific antagonists for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.
Discovery and characterization of the flavonoids in Cortex Mori Radicis as naturally occurring inhibitors against intestinal nitroreductases
Chem Biol Interact 2022 Dec 1;368:110222.PMID:36244406DOI:10.1016/j.cbi.2022.110222.
Gut bacterial nitroreductases are found to be heavily related with the intestinal toxicity of nitroaromatic compounds in food or medicine, which can be converted into mutagenic and enterotoxic nitroso or N-hydroxyl intermediates. Thus, inhibiting the gut microbe-encoded nitroreductases has become an attractive method to reduce the mutagen metabolites in colon and prevent intestinal diseases. In this study, the inhibitory effects of sixteen constituents in Cortex Mori Radicis on two kinds of gut bacterial nitroreductases (EcNfsA and EcNfsB) were evaluated with nitrofurazone (NFZ) as substrate and NADPH as electron donor. The results clearly demonstrated that four flavonoids including kuwanon G, kuwanon A, sanggenol A and kuwanon C showed dual inhibition on both EcNfsA and EcNfsB mediated NFZ reduction; morusin, morin, and sanggenone C were strong inhibitors towards EcNfsA; Kuwanon H and kuwanon E exhibited effective inhibition on EcNfsB. Further inhibition kinetic analysis and molecular docking simulations displayed that all inhibitors above suppressed both EcNfsA and EcNfsB activities in competitive manners, except non-competitive inhibition of morin on EcNfsA and non-competitive inhibition of kuwanon C on EcNfsB, respectively. Taking together, these findings revealed that most flavonoids in Cortex Mori Radicis presented effective inhibition on gut microbial nitroreductases, suggesting that Cortex Mori Radicis might be a promising candidate for ameliorating nitroreductases mediated intestinal mutagenicity.
Rapid Screening of Nonalkaloid α-Glucosidase Inhibitors from a Mulberry Twig Extract Using Enzyme-Functionalized Magnetic Nanoparticles Coupled with UPLC-MS/MS
J Agric Food Chem 2022 Sep 28;70(38):11958-11966.PMID:36107153DOI:10.1021/acs.jafc.2c03435.
Mulberry twigs are an important source of α-glucosidase inhibitors. To date, research studies on α-glucosidase in mulberry twigs have mainly focused on alkaloids such as 1-deoxynojirimycin (DNJ). Preliminary studies have shown that there may be more active nonalkaloid α-glucosidase inhibitors in mulberry twigs. In this study, we immobilized α-glucosidase on Fe3O4@SiO2 for the first time and rapidly screened four nonalkaloid α-glucosidase inhibitors (kuwanon G, kuwanon C, Kuwanon H, and morusin) using ligand fishing technology with ultrahigh-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) from the mulberry twig extract of Jialing 20, the excellent artificial triploid variety of mulberry cultivated extensively in Southwest China. The half maximal inhibitory concentrations (IC50) of Kuwanon H and kuwanon G were 2.82 ± 0.68 and 2.83 ± 0.31 μM, respectively, with better inhibition activity than that of DNJ (with an IC50 of 7.04 ± 0.82 μM). Meanwhile, the molecular docking results showed that the action sites of these two isopentenyl flavonoids on α-glucosidase were different from that of DNJ. In brief, this work is beneficial to discovering new α-glucosidase inhibitors from mulberry twigs quickly and accurately and provides a theoretical basis for the mulberry twig extract as a functional food or a natural hypoglycemic drug source, as well as a reference for directional breeding of mulberry, which greatly improves the exploitation and utilization value of mulberry twigs as an agricultural byproduct in the fields of agricultural production, functional food, and natural medicine.
Natural Flavones from Morus alba against Methicillin-Resistant Staphylococcus aureus via Targeting the Proton Motive Force and Membrane Permeability
J Agric Food Chem 2019 Sep 11;67(36):10222-10234.PMID:31385700DOI:10.1021/acs.jafc.9b01795.
The emergence and rapid spread of methicillin-resistant Staphylococcus aureus (MRSA) critically requires alternative therapeutic options. New antibacterial drugs and strategies are urgently needed to combat MRSA-associated infections. Here, we investigated the antibacterial activity of flavones from Morus alba and the potential mode of action against MRSA. Kuwanon G, Kuwanon H, mulberrin, and morusin displayed high efficiency in killing diverse MRSA isolates. On the basis of structure-activity analysis, the cyclohexene-phenyl ketones and isopentenyl groups were critical to increase the membrane permeability and to dissipate the proton motive force. Meanwhile, mechanistic studies further showed that kuwanon G displayed rapid bactericidal activity in vitrowith difficulty in developing drug resistance. Kuwanon G targeted phosphatidylglycerol and cardiolipin in the cytoplasmic membrane through the formation of hydrogen bonds and electrostatic interactions. Additionally, kuwanon G promoted wound healing in a mouse model of MRSA skin infection. In summary, these results indicate that flavones are promising lead compounds to treat MRSA-associated infections through disrupting the proton motive force and membrane permeability.
Antioxidant, Anti-α-Glucosidase, Antityrosinase, and Anti-Inflammatory Activities of Bioactive Components from Morus alba
Antioxidants (Basel) 2022 Nov 11;11(11):2222.PMID:36421408DOI:10.3390/antiox11112222.
The root bark of Morus alba L. (Mori Cortex) is used to treat diuresis and diabetes in Chinese traditional medicine. We evaluated different solvent extracts and bioactive components from the root bark of Morus alba L. for their antioxidant, anti-α-glucosidase, antityrosinase, and anti-inflammatory activities. Acetone extract showed potent antioxidant activity, with SC50 values of 242.33 ± 15.78 and 129.28 ± 10.53 µg/mL in DPPH and ABTS radical scavenging assays, respectively. Acetone and ethyl acetate extracts exhibited the strongest anti-α-glucosidase activity, with IC50 values of 3.87 ± 1.95 and 5.80 ± 2.29 μg/mL, respectively. In the antityrosinase assay, the acetone extract showed excellent activity, with an IC50 value of 7.95 ± 1.54 μg/mL. In the anti-inflammatory test, ethyl acetate and acetone extracts showed significant anti-nitric oxide (NO) activity, with IC50 values of 10.81 ± 1.41 and 12.00 ± 1.32 μg/mL, respectively. The content of the active compounds in the solvent extracts was examined and compared by HPLC analysis. Six active compounds were isolated and evaluated for their antioxidant, anti-α-glucosidase, antityrosinase, and anti-inflammatory properties. Morin (1) and oxyresveratrol (3) exhibited effective antioxidant activities in DPPH and ABTS radical scavenging assays. Additionally, oxyresveratrol (3) and Kuwanon H (6) showed the highest antityrosinase and anti-α-glucosidase activities among all isolates. Morusin (2) demonstrated more significant anti-NO and anti-iNOS activities than the positive control, quercetin. Our study suggests that the active extracts and components from root bark of Morus alba should be further investigated as promising candidates for the treatment or prevention of oxidative stress-related diseases, hyperglycemia, and pigmentation disorders.