Isookanin
(Synonyms: 异奥卡宁) 目录号 : GC60950
Isookanin可从Clinacanthusnutans分离得到，可用于多种疾病的研究，包括肿瘤，皮疹，蛇和昆虫叮咬，糖尿病，腹泻，以及作为抗HSV和水痘带状疱疹病毒(VZV)的抗病毒剂
Cas No.:1036-49-3
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
Isookanin, isolated from the leaves of Clinacanthus nutans, can be used for the research of various illnesses including cancers, skin rashes, snake and insects bites, diabetes mellitus, diarrhoea, as an anti-viral agent against HSV and varicella-zoster virus (VZV)[1].
[1]. Abdullahi Aliyu, et al. Subacute Oral Administration of Clinacanthus nutans Ethanolic Leaf Extract Induced Liver and Kidney Toxicities in ICR Mice. Molecules. 2020 Jun 5;25(11):2631.
| Cas No. | 1036-49-3 | SDF | |
| 别名 | 异奥卡宁 | ||
| Canonical SMILES | O=C1C[C@@H](C2=CC=C(O)C(O)=C2)OC3=C(O)C(O)=CC=C13 | ||
| 分子式 | C15H12O6 | 分子量 | 288.25 |
| 溶解度 | 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 | 3.4692 mL | 17.3461 mL | 34.6921 mL |
| 5 mM | 0.6938 mL | 3.4692 mL | 6.9384 mL |
| 10 mM | 0.3469 mL | 1.7346 mL | 3.4692 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。
Isookanin Inhibits PGE2-Mediated Angiogenesis by Inducing Cell Arrest through Inhibiting the Phosphorylation of ERK1/2 and CREB in HMEC-1 Cells
Int J Mol Sci 2021 Jun 16;22(12):6466.PMID:34208772DOI:10.3390/ijms22126466.
Inflammation is increasingly recognized as a critical mediator of angiogenesis, and unregulated angiogenic responses often involve human diseases. The importance of regulating angiogenesis in inflammatory diseases has been demonstrated through some successful cases of anti-angiogenesis therapies in related diseases, including arthritis, but it has been reported that some synthetic types of antiangiogenic drugs have potential side effects. In recent years, the importance of finding alternative strategies for regulating angiogenesis has begun to attract the attention of researchers. Therefore, identification of natural ingredients used to prevent or treat angiogenesis-related diseases will play a greater role. Isookanin is a phenolic flavonoid presented in Bidens extract, and it has been reported that Isookanin possesses some biological properties, including antioxidative and anti-inflammatory effects, anti-diabetic properties, and an ability to inhibit α-amylase. However, its antiangiogenic effects and mechanism thereof have not been studied yet. In this study, our results indicate that Isookanin has an effective inhibitory effect on the angiogenic properties of microvascular endothelial cells. Isookanin shows inhibitory effects in multiple stages of PGE2-induced angiogenesis, including the growth, proliferation, migration, and tube formation of microvascular endothelial cells. In addition, Isookanin induces cell cycle arrest in S phase, which is also the reason for subsequent inhibition of cell proliferation. The mechanism of inhibiting angiogenesis by Isookanin is related to the inhibition of PGE2-mediated ERK1/2 and CREB phosphorylation. These findings make Isookanin a potential candidate for the treatment of angiogenesis-related diseases.
Anti-Inflammatory Activity and Mechanism of Isookanin, Isolated by Bioassay-Guided Fractionation from Bidens pilosa L
Molecules 2021 Jan 6;26(2):255.PMID:33419109DOI:10.3390/molecules26020255.
Bidens pilosa L. (Asteraceae) has been used historically in traditional Asian medicine and is known to have a variety of biological effects. However, the specific active compounds responsible for the individual pharmacological effects of Bidens pilosa L. (B. pilosa) extract have not yet been made clear. This study aimed to investigate the anti-inflammatory phytochemicals obtained from B. pilosa. We isolated a flavonoids-type phytochemical, Isookanin, from B. pilosa through bioassay-guided fractionation based on its capacity to inhibit inflammation. Some of Isookanin's biological properties have been reported; however, the anti-inflammatory mechanism of Isookanin has not yet been studied. In the present study, we evaluated the anti-inflammatory activities of Isookanin using lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. We have shown that Isookanin reduces the production of proinflammatory mediators (nitric oxide, prostaglandin E2) by inhibiting the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated macrophages. Isookanin also inhibited the expression of activator protein 1 (AP-1) and downregulated the LPS-induced phosphorylation of p38 mitogen-activated protein kinase (MAPK) and c-jun NH2-terminal kinase (JNK) in the MAPK signaling pathway. Additionally, Isookanin inhibited proinflammatory cytokines (tumor necrosis factor-a (TNF-α), interleukin-6 (IL-6), interleukin-8 (IL-8), and interleukin-1β (IL-1β)) in LPS-induced THP-1 cells. These results demonstrate that Isookanin could be a potential therapeutic candidate for inflammatory disease.
Antiviral Activity of Vitis vinifera Leaf Extract against SARS-CoV-2 and HSV-1
Viruses 2021 Jun 29;13(7):1263.PMID:34209556DOI:10.3390/v13071263.
Vitis vinifera represents an important and renowned source of compounds with significant biological activity. Wines and winery bioproducts, such as grape pomace, skins, and seeds, are rich in bioactive compounds against a wide range of human pathogens, including bacteria, fungi, and viruses. However, little is known about the biological properties of vine leaves. The aim of this study was the evaluation of phenolic composition and antiviral activity of Vitis vinifera leaf extract against two human viruses: the Herpes simplex virus type 1 (HSV-1) and the pandemic and currently widespread severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). About 40 phenolic compounds were identified in the extract by HPLC-MS/MS analysis: most of them were quercetin derivatives, others included derivatives of luteolin, kaempferol, apigenin, isorhamnetin, myricetin, chrysoeriol, biochanin, Isookanin, and scutellarein. Leaf extract was able to inhibit both HSV-1 and SARS-CoV-2 replication in the early stages of infection by directly blocking the proteins enriched on the viral surface, at a very low concentration of 10 μg/mL. These results are very promising and highlight how natural extracts could be used in the design of antiviral drugs and the development of future vaccines.
Antioxidant properties of polyphenols from snow chrysanthemum ( Coreopsis tinctoria) and the modulation on intestinal microflora in vitro
Pharm Biol 2022 Dec;60(1):1771-1780.PMID:36093612DOI:10.1080/13880209.2022.2117386.
Context: Coreopsis tinctoria Nutt (Asteraceae), named snow chrysanthemum, is known to have a high level of polyphenols. However, the potential prebiotic effect on modulating intestinal microflora is still unclear. Objective: The chemical composition, antioxidant properties of snow chrysanthemum polyphenols (SCPs) and their effects on human intestinal microbiota were investigated. Materials and methods: SCPs were extracted using ultrasonic-assisted extraction, and further determined using UPLC-QE Orbitrap/MS. Five assays were used to investigate the antioxidant activities of SCPs. Subsequently, the effects of SCPs on intestinal microbiota in vitro were determined by high throughput sequencing and bioinformatics analysis. Results: Marein, Isookanin and cymaroside were the major phenolic compounds, which accounted for 42.17%, 19.53% and 12.25%, respectively. Marein exhibited higher scavenging capacities in DPPH (EC50 = 8.84 µg/mL) and super anion radical assay (EC50 = 282.1 µg/mL) compared to cymaroside and Isookanin. The antioxidant capacity of cymaroside was weakest among the three phenolic compounds due to the highest EC50 values, especially for superoxide anion radical assay, EC50 > 800 µg/mL. The result of in vitro fermentation showed that the three phenolic compounds increased the relative abundances of Escherichia/Shigella, Enterococcus, Klebsiella, etc., and Isookanin notably increased the relative abundance of Bifidobacterium and Lactobacillus. Discussion and conclusions: SCPs exhibited antioxidant properties and potential prebiotic effects on modulating the gut microbiota composition. The findings indicated that SCPs consumption could exert prebiotic activity that is beneficial for human health.
Subacute Oral Administration of Clinacanthus nutans Ethanolic Leaf Extract Induced Liver and Kidney Toxicities in ICR Mice
Molecules 2020 Jun 5;25(11):2631.PMID:32517000DOI:10.3390/molecules25112631.
This study investigated the leaves of Clinacanthus nutans for its bioactive compounds and acute and subacute toxicity effects of C. nutans ethanolic leaf extract (CELE) on blood, liver and kidneys of ICR mice. A total of 10 8-week-old female mice were divided into groups A (control) and B (2000 mg/kg) for the acute toxicity study. A single dose of 2000 mg/kg was administered to group B through oral gavage and mice were monitored for 14 days. In the subacute toxicity study, mice were divided into five groups: A (control), B (125 mg/kg), C (250 mg/kg), D (500 mg/kg) and E (1000 mg/kg). The extract was administered daily for 28 days via oral gavage. The mice were sacrificed, and samples were collected for analyses. Myricetin, orientin, isoorientin, vitexin, isovitexin, Isookanin, apigenin and ferulic acid were identified in the extract. Twenty-eight days of continuous oral administration revealed significant increases (p < 0.05) in creatinine, ALT and moderate hepatic and renal necrosis in groups D and E. The study concluded that the lethal dose (LD50) of CELE in mice is greater than 2000 mg/kg and that repeated oral administrations of CELE for 28 days induced hepatic and renal toxicities at 1000 mg/kg in female ICR mice.