Khellin
(Synonyms: 凯林, 呋喃并色酮, Amicardine, Methafrone, Visammin) 目录号 : GC20110
Khellin 是从阿米芹中提取得到的一种呋喃并色酮，是EGFR抑制剂，IC50为 0.15 µM。它体外具有抗增殖活性，还具有抗痉挛和冠状动脉舒张作用。
Cas No.:82-02-0
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
Khellin is a vasodilator that also has bronchodilatory action.
| Cas No. | 82-02-0 | SDF | |
| 别名 | 凯林, 呋喃并色酮, Amicardine, Methafrone, Visammin | ||
| 分子式 | C14H12O5 | 分子量 | 260.245 |
| 溶解度 | DMSO: 10 mM | 储存条件 | -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 | 3.8425 mL | 19.2127 mL | 38.4253 mL |
| 5 mM | 0.7685 mL | 3.8425 mL | 7.6851 mL |
| 10 mM | 0.3843 mL | 1.9213 mL | 3.8425 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。
Analytical Methods for Furanochromone Natural Product, Khellin and Its Inspired Drug Candidates, Amiodarone and Sodium Cromoglycate
Crit Rev Anal Chem 2022 Jul 1;1-16.PMID:35776740DOI:10.1080/10408347.2022.2094198.
Khellin is the key furanocoumarin of Ammi visnaga L. (Lam.) that exhibits various biological properties. This unique natural product has inspired the discovery of two first-in-class drugs, amiodarone and sodium cromoglycate. A wide range of analytical methods were generated while translating Khellin scaffold into clinically used drugs; however, they have never been reviewed and critically assessed. The present review aims to review and evaluate the analytical techniques for the natural products, Khellin, visnagin, and their inspired drugs, amiodarone and sodium cromoglycate. High-performance liquid chromatography (HPLC) is the extensively used technique in most analytical methods reported for these compounds; however, other techniques including the fluorimetry, luminescence spectrophotometry, potentiometry, voltammetry, FT-Raman spectroscopy, and ELISA were also employed. The review will be helpful for further basic and translational research on furanochromone and related scaffolds.
Extraction, purification and radioiodination of Khellin as cancer theranostic agent
Appl Radiat Isot 2021 Dec;178:109970.PMID:34619628DOI:10.1016/j.apradiso.2021.109970.
Khellin was successfully extracted from Ammi visnaga fruits with a recovery percent of 96.15%. Next radio-iodination of Khellin was successfully achieved with a high yield. The biodistribution study of [131I]iodo-khellin in tumour bearing mice revealed that Khellin preferentially localization at tumour tissue. Target prediction study for [131I]iodo-khellin revealed that PI3K and VEGFR are potential targets for iodo-khellin with good affinity. The results of this study potentiate [131I]iodo-khellin as a good theranostic agent for tumour imaging and therapy.
Enhancing Biopharmaceutical Attributes of Khellin by Amorphous Binary Solid Dispersions
AAPS PharmSciTech 2021 Oct 27;22(8):260.PMID:34705156DOI:10.1208/s12249-021-02126-3.
Khellin, a furanochromone isolated from fruits and seeds of Ammi visnaga, is traditionally used in many eastern Mediterranean countries. The plant decoction and the crystalline substance Khellin have many pharmacological activities. For instance, it acts as a bronchodilator and also relieves renal colic and urethral stones, etc. However, the low water solubility (~ 120 µg/mL) and low bioavailability limit its therapeutic application. Thus, the present research explores the development of its binary and ternary solid dispersion formulations to improve its solubility and dissolution behavior. A 24-well plate miniaturized protocol was established to identify the optimal hydrophilic polymer to prepare its solid dispersions. PEG-4000 was recognized as the favorable hydrophilic carrier in preparation of solid dispersion, SSB17. The formulation displayed ~ five-fold enhancement in the aqueous solubility of Khellin. The binary solid dispersion SSB17 was manufactured at a gram scale and evaluated using 1H-NMR, 13C-NMR, FT-IR, p-XRD, SEM, DSC, in vitro dissolution, and predicted pharmacokinetics. The quantitative dissolution data of SSB17 demonstrated ~ 2-3-fold improvement in AUC at physiological pH conditions. These conclusions highlight the basis for further preclinical studies on solid dispersions of Khellin with improved biopharmaceutical properties.
Development of Gel-in-Oil Emulsions for Khellin Topical Delivery
Pharmaceutics 2020 Apr 26;12(5):398.PMID:32357441DOI:10.3390/pharmaceutics12050398.
Hypopigmentation is a progressive dermatological condition caused by a reduction in the skin pigment, melanin. Its treatment is considered a challenge due to the lack of a highly efficient single therapy. Currently, the main treatments include photochemotherapy, application of corticosteroids and immunosuppressants, and laser. Khellin-based gel-in-oil emulsions appear as a promising alternative since they ensure a concentration of the drug, a natural furanochromone, at the desired location, skin surface. Khellin promotes repigmentation as it forms a dark colored complex after solar irradiation. The aim of this study was the development and characterization (e.g., rheological behaviour, droplet size, tackiness, adhesion and spreadability) of three topical gel-in-oil emulsions prepared with different emollients, formulated through a cold emulsification process, and suitable for the incorporation of Khellin. In vitro studies were performed to evaluate the drug release and permeation profiles across artificial membranes and excised human skin, respectively, using Franz-type vertical diffusion cells. The W/O emulsions developed showed macroscopic appearance, shear-thinning behavior with a mean droplet size from 3.28 to 4.28 μm, suitable for topical application. In vitro studies revealed permeation values of about 1% of Khellin across the stratum corneum, making these gel-in-oil emulsions promising for preclinical and clinical studies. The cold process, being an easy and low energy production method, represents an innovative strategy to produce khellin-based gel-in-oil emulsions to treat patients with hypopigmentation.
Preparation and Characterization of Ascosome Vesicles Loaded with Khellin
J Pharm Sci 2020 Oct;109(10):3114-3124.PMID:32565350DOI:10.1016/j.xphs.2020.06.017.
Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl octanoate or decanoate, and their potential value as drug delivery systems. Khellin, a natural furanochromone with numerous applications in skin pathologies was loaded as model drug in ascosomes. Ascosomes had narrow size distribution, adequate encapsulation efficiency, long-term stability, and antioxidant properties. Increasing amounts of loaded Khellin resulted in a reduction of the vesicle average size, without affecting the polydispersity, suggesting a stabilizing effect. Ascorbyl alkanoates produced remarkably different bilayer organizations and different capabilities to accommodate Khellin in the hydrophobic pocket of the vesicles. The addition ascorbyl alkanoates reduced the amount of water molecules strongly bound to the polar headgroups. Moreover, the loading of Khellin did not induce any significant hydration change in the unilamellar vesicular systems. The narrow size distribution, adequate encapsulation efficiency and long-term stability of ascosomes loaded with Khellin, make these nanostructures suitable for dermatological use and other routes of administrations, preserving the biological properties of ascorbic acid.