Ayanin
(Synonyms: 阿亚黄素) 目录号 : GC60063
Ayanin是从CrotonschiedeanusSchlecht中分离得到的一种具有生物学活性的黄酮类物质。Ayanin是非选择性的磷酸二酯酶(phosphodiesterase1-4)抑制剂，可用于呼吸道疾病的研究，如过敏性哮喘等。
Cas No.:572-32-7
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
Ayanin is a bioflavonoid isolated from Croton schiedeanus Schlecht. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al[1].
Ayanin inhibits interleukin (IL)-4 production from purified basophils with an IC50 value of 2.2 μM[1].
[1]. Fei-Peng Lee, et al. Ayanin, a Non-Selective Phosphodiesterase 1-4 Inhibitor, Effectively Suppresses Ovalbumin-Induced Airway Hyperresponsiveness Without Affecting xylazine/ketamine-induced Anesthesia. Eur J Pharmacol. 2010 Jun 10;635(1-3):198-203.
| Cas No. | 572-32-7 | SDF | |
| 别名 | 阿亚黄素 | ||
| Canonical SMILES | O=C1C(OC)=C(C2=CC=C(OC)C(O)=C2)OC3=CC(OC)=CC(O)=C13 | ||
| 分子式 | C18H16O7 | 分子量 | 344.32 |
| 溶解度 | 储存条件 | 4°C, protect from 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 | 2.9043 mL | 14.5214 mL | 29.0428 mL |
| 5 mM | 0.5809 mL | 2.9043 mL | 5.8086 mL |
| 10 mM | 0.2904 mL | 1.4521 mL | 2.9043 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。
Ayanin diacetate-induced cell death is amplified by TRAIL in human leukemia cells
Biochem Biophys Res Commun 2012 Nov 9;428(1):116-20.PMID:23063980DOI:10.1016/j.bbrc.2012.10.017.
Here we demonstrate that the semi-synthetic flavonoid Ayanin diacetate induces cell death selectively in leukemia cells without affecting the proliferation of normal lymphocytes. Incubation of human leukemia cells with Ayanin diacetate induced G(2)-M phase cell cycle arrest and apoptosis which was prevented by the non-specific caspase inhibitor z-VAD-fmk and reduced by the overexpression of Bcl-x(L). Ayanin diacetate-induced cell death was found to be associated with: (i) loss of inner mitochondrial membrane potential, (ii) the release of cytochrome c, (iii) the activation of multiple caspases, (iv) cleavage of poly(ADP-ribose) polymerase and (v) the up-regulation of death receptors for TRAIL, DR4 and DR5. Moreover, the combined treatment with Ayanin diacetate and TRAIL amplified cell death, compared to single treatments. These results provide a basis for further exploring the potential applications of this combination for the treatment of cancer.
Ayanin, a non-selective phosphodiesterase 1-4 inhibitor, effectively suppresses ovalbumin-induced airway hyperresponsiveness without affecting xylazine/ketamine-induced anesthesia
Eur J Pharmacol 2010 Jun 10;635(1-3):198-203.PMID:20307524DOI:10.1016/j.ejphar.2010.02.055.
In recent in vitro reports, the IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) was 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils, and its therapeutic ratio was >19. Therefore, we were interested in investigating the effects on ovalbumin induced airway hyperresponsiveness in vivo, and to clarify its potential for treating asthma. Ayanin (30-100micromol/kg, orally (p.o.)) dose-dependently and significantly attenuated the enhanced pause (P(enh)) value induced by methacholine in sensitized and challenged mice. It also significantly suppressed the increases in total inflammatory cells, macrophages, lymphocytes, neutrophils, and eosinophils, and levels of cytokines, including IL-2, IL-4, IL-5, and tumor necrosis factor (TNF)-alpha in bronchoalveolar lavage fluid of these mice. However, at 100micromol/kg, it significantly enhanced the level of interferon (IFN)-gamma. In addition, Ayanin (30-100micromol/kg, p.o.) dose-dependently and significantly suppressed total and OVA-specific immunoglobulin (Ig)E levels in the serum and bronchoalveolar lavage fluid, and enhanced the IgG(2a) level in serum of these mice. In the present results, Ayanin did not affect xylazine/ketamine-induced anesthesia, suggesting that Ayanin has few or no adverse effects, such as nausea, vomiting, and gastric hypersecretion. In conclusion, the above results suggest that Ayanin may have the potential for use in treating allergic asthma.
The Spectrum of Pharmacological Actions of Syringetin and Its Natural Derivatives-A Summary Review
Nutrients 2022 Dec 4;14(23):5157.PMID:36501187DOI:10.3390/nu14235157.
Mono- and poly-O-methylated flavonols and their glycoside derivatives belong to the group of natural plant polyphenols with a wide spectrum of pharmacological activities. These compounds are known for their antioxidant, antimutagenic, hepatoprotective, antidiabetic, and antilipogenic properties. Additionally, they inhibit carcinogenesis and cancer development. Having in mind the multidirectional biological activity of methylated flavonols, we would like to support further study on their health-promoting activities; in this review we summarized the most recent reports on syringetin and some of its structural analogues: laricitrin, Ayanin, and isorhamnetin. Natural sources and biological potential of these substances were described based on the latest research papers.
Inhibitory effect of N(G)-nitro-L-arginine methyl ester on the anti-adrenergic response elicited by Ayanin in the pithed rat
Planta Med 2002 Apr;68(4):322-5.PMID:11988855DOI:10.1055/s-2002-26755.
In this study we evaluated the anti-adrenergic response elicited by Ayanin, a flavonoid compound isolated from Croton schiedeanus Schlecht, in the pithed rat, and the inhibitory effect of NO synthase inhibitor N(G)-nitro-L-arginine methyl ester (L-NAME), and its acute toxicity profile in mice. In pithed rats Ayanin (5 - 50 mg/kg i. v.) caused a dose-dependent decrease in the pressor and chronotropic responses induced by intravenous noradrenaline administration (0.25 microg/kg). This anti-adrenergic response was completely abolished by prior treatment with L-NAME (10 mg/kg i.v ) and the inhibitory effect of L-NAME was reversed after intravenous administration of L-arginine (100 mg/kg, i. v.). No lethal or major toxic effects were observed in mice receiving i. p. administration of Ayanin up to a dose of 500 mg/kg. Our findings confirm that Ayanin exerts protective cardiovascular effects against the increase in blood pressure and heart rate mainly through a mechanism that depends on the NO/cyclic guanosine monophosphate (cGMP) pathway without acute toxic effects. These results suggest that extracts of Croton schiedeanus, the native south American plant from which Ayanin was isolated, might be beneficial in cardiovascular disease.
Flavonoids and related compounds as anti-allergic substances
Allergol Int 2007 Jun;56(2):113-23.PMID:17384531DOI:10.2332/allergolint.R-06-135.
The prevalence of allergic diseases has increased all over the world during the last two decades. Dietary change is considered to be one of the environmental factors that cause this increase and worsen allergic symptoms. If this is the case, an appropriate intake of foods or beverages with anti-allergic activities is expected to prevent the onset of allergic diseases and ameliorate allergic symptoms. Flavonoids, ubiquitously present in vegetables, fruits or teas possess anti-allergic activities. Flavonoids inhibit histamine release, synthesis of IL-4 and IL-13 and CD40 ligand expression by basophils. Analyses of structure-activity relationships of 45 flavones, flavonols and their related compounds showed that luteolin, Ayanin, apigenin and fisetin were the strongest inhibitors of IL-4 production with an IC(50) value of 2-5 microM and determined a fundamental structure for the inhibitory activity. The inhibitory activity of flavonoids on IL-4 and CD40 ligand expression was possibly mediated through their inhibitory action on activation of nuclear factors of activated T cells and AP-1. Administration of flavonoids into atopic dermatitis-prone mice showed a preventative and ameliorative effect. Recent epidemiological studies reported that a low incidence of asthma was significantly observed in a population with a high intake of flavonoids. Thus, this evidence will be helpful for the development of low molecular compounds for allergic diseases and it is expected that a dietary menu including an appropriate intake of flavonoids may provide a form of complementary and alternative medicine and a preventative strategy for allergic diseases. Clinical studies to verify these points are now in progress.