Isoalantolactone
(Synonyms: 异土木香内酯; (+)-Isoalantolactone; Isohelenin) 目录号 : GN10666
A sesquiterpene lactone with diverse biological activities
Cas No.:470-17-7
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
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Cell experiment: |
Cell viability is assessed by MTT assay. Briefly PANC-1, BxPC3, and HPAC cells are treated with DMSO or Isoalantolactone (5, 10, 20, 40, 80 and 100 μM) in the presence or absence of 3 mM NAC for 24 h. Following treatment, the MTT reagent is added (500 µg/mL) and cells are further incubated at 37°C for 4 h. Subsequently 150 μL DMSO is added to dissolve farmazan crystals and absorbance is measured at 570 nm in a microplate reader. The percentage of cell viability is calculated[2]. |
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Animal experiment: |
Mice[2]In vivo studies for acute and chronic toxicity are conducted on 10-12 week old CD1 mice weighing 27-30 g. The mice are maintained in a specific pathogen-free grade animal facility on a 12-h light/dark cycles at 25±2°C. Mice are randomly divided into four groups. Group A (n=4) administered with 50 µL DMSO intraperitonially for 7 days; Group B (n=4) administered with Isoalantolactone (100 mg/kg body weight) in 50 µL DMSO intraperitonially for 7 days; Group C (n=4) administered with 50 µL DMSO for 30 days and Group D (n=4) administered with Isoalantolactone (100 mg/kg body weight) in 50 µL DMSO intraperitonially for 30 days. At the first and last day of the experiments, the body weight of each mouse is measured. At the end of experiments (at dose day 7 for acute toxicity & dose day 30 for chronic toxicity), mice are anesthetized using Pentobarbital sodium (50 mg/kg ip), blood is collected via cardiac puncture, allowed to clot for 10 min and centrifuge at 1000×g for 10 min at room temperature. Serum is separated and stored at -20°C until analysis. The liver and kidneys are excised and processed for hematoxylin and eosin staining followed established procedures. |
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References: [1]. Lawrence NJ, et al. Cytotoxic Michael-type amine adducts of alpha-methylene lactones alantolactone and isoalantolactone. Bioorg Med Chem Lett. 2001 Feb 12;11(3):429-31. |
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Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.
Isoalantolactone exhibits good cytotoxic activity against the K562 human leukaemia cell line (IC50=1.2 μM) [1]. The cytotoxic effect of Isoalantolactone on pancreatic carcinoma is evaluated using PANC-1, BxPC3 and HPAC cell lines. Treatment with Isoalantolactone for 24 h inhibits PANC-1 cell growth in a dose-dependent manner. The inhibition rate is above 90% at 80 µM and the concentration to achieve 50% growth inhibition (IC50) is 40 µM. A similar trend in loss of cell viability is observed in BxPC3 and HPAC cells on Isoalantolactone treatment with IC50 values 43 and 48 µM respectively. Pretreatment with 3 mM N-Acetyl Cysteine (NAC), a specific ROS scavenger, restores the viability of cells indicating that Isoalantolactone exerts cytotoxic effect on cell viability through ROS generation[2].
The acute and chronic toxic effects of Isoalantolactone in CD1 mice are assessed by measuring the changes in body weight, blood biochemistry and histopathology of liver and kidneys in comparison with control groups. Isoalantolactone is well tolerated by mice and no mortality or any sign of pharmacotoxicity are found at a dose of 100 mg/kg during both experimental periods (7 & 30 days). Body weight gains and food consumption are comparable for control and treated mice during both experimental periods and there were no drug-related changes in histopathological and blood biochemistry parameters. The histopathological changes in liver and kidneys are assessed using hematoxylin and eosin staining and correlated with liver and renal function biomarkers. No obvious morphological changes are observed in liver and kidney structures of control and treatment groups. There is a slight increase in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) level of treatment group at dose day 7 but this increase is not significantly different (P<0.05) from control group. A significant increase in total bilirubin (TBIL) concentration is found in treatment group (1.43±0.26 vs 0.76±0.12 in control, P<0.05) at dose day 7. Similarly the changes in renal function biomarkers are not significantly different (P<0.05) in the serum of control and treatment groups at dose day 7. The concentration of creatinine (Cr) slightly increases whereas concentration of blood urea nitrogen (BUN) slightly decreases in treatment group. The serum level of AST, ALT, TBIL and BUN slightly decreases when mice are injected with Isoalantolactone at a dose of 100 mg/kg for 30 days[2].
References:
[1]. Lawrence NJ, et al. Cytotoxic Michael-type amine adducts of alpha-methylene lactones alantolactone and isoalantolactone. Bioorg Med Chem Lett. 2001 Feb 12;11(3):429-31.
[2]. Khan M, et al. Isoalantolactone induces reactive oxygen species mediated apoptosis in pancreatic carcinoma PANC-1 cells. Int J Biol Sci. 2012;8(4):533-47.
| Cas No. | 470-17-7 | SDF | |
| 别名 | 异土木香内酯; (+)-Isoalantolactone; Isohelenin | ||
| 化学名 | (3aR,4aS,8aR,9aR)-8a-methyl-3,5-dimethylidene-3a,4,4a,6,7,8,9,9a-octahydrobenzo[f][1]benzofuran-2-one | ||
| Canonical SMILES | CC12CCCC(=C)C1CC3C(C2)OC(=O)C3=C | ||
| 分子式 | C15H20O2 | 分子量 | 232.31 |
| 溶解度 | DMF: 15 mg/ml,DMSO: 10 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at 2-8°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 | 4.3046 mL | 21.523 mL | 43.0459 mL |
| 5 mM | 0.8609 mL | 4.3046 mL | 8.6092 mL |
| 10 mM | 0.4305 mL | 2.1523 mL | 4.3046 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。