Armillarisin A
(Synonyms: 亮菌甲素, 假蜜环菌甲素, 假蜜环菌素A) 目录号 : GC61796
ArmillarisinA有用于溃疡性结肠炎(UC)研究的潜力。ArmillarisinA可上调IL-4、下调IL-1β的作用。
Cas No.:53696-74-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Armillarisin A has the potential for the ulcerative colitis (UC) study. Armillarisin A increases IL-4 and lower IL-1β[1].
[1]. Ping Wu, et al. The Effects of Armillarisin A on Serum IL-1β and IL-4 and in Treating Ulcerative Colitis. Cell Biochem Biophys. 2015 May;72(1):103-6.
| Cas No. | 53696-74-5 | SDF | |
| 别名 | 亮菌甲素, 假蜜环菌甲素, 假蜜环菌素A | ||
| Canonical SMILES | OCC1=C2C(OC(C(C(C)=O)=C2)=O)=CC(O)=C1 | ||
| 分子式 | C12H10O5 | 分子量 | 234.2 |
| 溶解度 | 储存条件 | 4°C, protect from light, stored under nitrogen | |
| 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 | 4.2699 mL | 21.3493 mL | 42.6985 mL |
| 5 mM | 0.854 mL | 4.2699 mL | 8.5397 mL |
| 10 mM | 0.427 mL | 2.1349 mL | 4.2699 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。
The Effects of Armillarisin A on Serum IL-1β and IL-4 and in Treating Ulcerative Colitis
Cell Biochem Biophys 2015 May;72(1):103-6.PMID:25420534DOI:10.1007/s12013-014-0413-7.
To study the therapeutic effect of Armillarisin A on patients with ulcerative colitis (UC) and on serum IL-1β and IL-4, sixty patients with UC were randomly divided into three groups: Armillarisin A treatment group (Group I), Armillarisin-combined hormone therapy group (Group II), and hormones treatment as the control group (Group III). Patients in Group I received Armillarisin A 10 mg enema in 100 ml saline. Patients in Group II received Armillarisin A 10 mg and dexamethasone 5 mg enema in 100 ml saline. Patients in Group III received only dexamethasone 5 mg enema in 100 ml saline. The therapeutic efficacy and serum levels of IL-4 and IL-1β were observed. After 4 week treatment, the total effective rates were 90.0 % in Group I and 95.0 % in Group II. Both are higher than it in control group, which was 70.0 %. The serum levels of IL-4 in Groups I and II were significantly higher than it in control group. Compared to IL-4 levels before treatment, the levels of IL-4 after treatment were significantly higher in both Groups I and II. The serum levels of IL-11β were significantly decreased in Groups I and II in comparison to it in control group. Compared to the levels of IL-1β before treatment, the levels of IL-1β were significantly decreased. Armillarisin A shows a significant effect in treating UC. It helps increase IL-4 and lower IL-1β and the mechanism may be related to the body's immunity regulation.
Cholecystolithotomy Combined Armillarisin A versus Cholecystectomy in Cirrhotic Portal Hypertension Patients with Symptomatic Cholelithiasis
Chirurgia (Bucur) 2017 Mar-Apr;112(2):143-151.PMID:28463673DOI:10.21614/chirurgia.112.2.143.
Object: To discover whether cirrhotic portal hypertension patients with symptomatic cholelithiasis would benefit from cholecystolithotomy combined with Armillarisin A in the authors hospital. Methods: Sixty-one patients with cirrhotic portal hypertension and symptomatic gallstone disease who underwent either cholecystolithotomy combined with Armillarisin A (group A) or cholecystectomy (group B) for cholelithiasis from Feb 2007 to March 2011 were retrospectively reviewed. These patients were undergoing simultaneous procedure for esophageal varices. The operation-relevant information, change of laboratory examination data, postoperative complications and symptoms were analyzed. Results: There were no significant differences between group A and group B in mean operative time, intraoperative blood loss, time to resume diet postoperatively and length of hospital stay (P 0.05). The hepatic function biochemical profile and Child-Pugh's score at 2 weeks and 1 month after operations were both altered significantly less in group A than in group B (ALT, 0.008, 0.011; AST, 0.006, 0.003; Child-Pugh's score, 0.010, 0.016, respectively). However, at 6 months postoperatively, the changes were not significant (P 0.05). Except for gallstone recurrence and wound infection, occurrences or development of postoperative complications including biliary fistula, liver failure and subphrenic infection showed significant differences between the two groups (P = 0.037, P = 0.041, P = 0.019, respectively). After a mean follow-up of 4.2 years, all patients remain alive. Twenty-seven patients in group A (93%) are free of biliary symptoms. Conclusion: Cholecystolithotomy combined with using Armillarisin A is a useful treatment for symptomatic gallstones in patients with cirrhotic portal hypertension who are at high risk for cholecystectomy. It preserves gallbladder function and reduces the possibility of liver failure; moreover the rate of recurrent gallstones are relatively low.
Quantitation of Armillarisin A in human plasma by liquid chromatography-electrospray tandem mass spectrometry
J Pharm Biomed Anal 2007 Apr 11;43(5):1860-3.PMID:17250987DOI:10.1016/j.jpba.2006.12.023.
A rapid and sensitive LC-MS/MS method for quantifying Armillarisin A in human plasma after a single oral dose (40 mg) has been developed and validated. Sample preparation used liquid-liquid extraction with a mixture of diethyl ether-dichloromethane (60:40, v/v) in an acidic environment. The retention times of Armillarisin A and the internal standard, probenecid, were 1.63 and 1.78 min, respectively. The calibration curve was linear over the range 0.15-50 ng/mL with a limit of quantitation of 0.15 ng/mL. The coefficient of variation as a measure of intra- and inter-day precision was <9.3% and the accuracy was in the range 92.5-108.0%. The Armillarisin A concentration-time profile in human plasma was determined after an oral dose of a 40 mg tablet.
In vitro glucuronidation of Armillarisin A: UDP-glucuronosyltransferase 1A9 acts as a major contributor and significant species differences
Xenobiotica 2014 Nov;44(11):988-95.PMID:24916899DOI:10.3109/00498254.2014.927084.
1. This study is performed to investigate liver microsomal glucuronidation of Armillarisin A (A.A), an effective cholagogue drug, aiming at characterizing the involved UDP-glucuronosyltranferases (UGT) and revealing potential species differences. 2. A.A glucuronidation in human liver microsomes (HLM) generates one metabolite (M2) glucuronidated at the phenol hydroxyl group, obeying Michaelis-Menten kinetic model. Multiple isoforms including UGT1A1, 1A7, 1A9 and 2B15 can catalyze A.A glucuronidation. Kinetic assays and chemical inhibition studies both demonstrate that UGT1A9 is responsible for A.A glucuronidation in HLM. A.A glucuronidation in Cynomolgus monkey microsomes (CyLM) also follows Michaelis-Menten model, but can additionally catalyze the traced glucuronosyl substitution at the alcohol hydroxyl group (M1). The reactions in liver microsomes from Sprague-Dawley rats (RLM), ICR/CD-1 mouse (MLM), Beagle dog (DLM) all display biphasic kinetics and only M2 is detected. HLM, RLM and CyLM exhibit very similar catalytic activities towards A.A glucuronidation, with the intrinsic clearance values of respective 38, 37 and 37 μL/min/mg, which are much higher than MLM and DLM. 3. This in vitro study indicates that UGT1A9 acts as a major contributor to A.A glucuronidation in human liver, and the reaction displays large species differences.
Qualitative Analysis of Visible Foreign Solids in Armillarisin A Injection Formulations Using Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry
Molecules 2023 Feb 7;28(4):1609.PMID:36838598DOI:10.3390/molecules28041609.
During the trial production of Armillarisin A for injection (AA-I), unidentified needle-like yellow-brown crystals were occasionally observed. Here, we report an ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS) method for determining the source of the visible foreign bodies in the formulations of Armillarisin A active pharmaceutical ingredient (AA-API). AA-API, photolyzed samples, the intermediate polymer, and the excipient analyzed determined after the separation on a Waters Symmetry C18 (3.5 μm, 4.6 × 75 mm) column with a mobile phase consisting of a methanol/acetic acid (0.1 mol/L) aqueous solution (50:50). Furthermore, the crystal type of the visible foreign bodies, the intermediate polymer and AA-API were investigated by X-ray powder diffraction (XRD). The results revealed that the characteristics of the visible foreign solids were the same as those of AA-API as regards UPLC peak position (368 nm) and MS spectrum in negative ion detection mode. The visible foreign solids were thus identified as unpolymerized crystals of AA-API and were attributed to AA-API itself. The results showed that the production process could be improved by changing the stirring method and frequency as well as by optimizing the polymerization temperature to ensure the safety, stability, and control of the product quality in the stage of batch production.