Columbin
(Synonyms: 古伦宾) 目录号 : GC31749A diterpenoid furanolactone with diverse biological activities
Cas No.:546-97-4
Sample solution is provided at 25 µL, 10mM.
Columbin is a diterpenoid furanolactone isolated from J. columba, A. albida, and T. bakis that has diverse biological activities.1,2,3,4 It inhibits the growth of T. brucei in vitro and induces complete parasite clearance in T. brucei-infected mice when administered at a dose of 25 mg/kg per day for three days.1 Columbin selectively inhibits COX-2 over COX-1 (EC50s = 53.1 and 327 μM, respectively) and reduces carrageenan-induced paw edema in rats in a dose-dependent manner.2 Dietary feeding of columbin (4, 20, and 100 ppm) reduces the number of lesions in a rat model of azoxymethane-induced colon carcinogenesis.3 Columbin (20-40 mg/kg per day) also reduces sleeping time induced by a mixture of urethane and α-choralose but prolongs sleeping time induced by hexobarbital in mice.4
1.Nok, A.J., Sallau, B.A., Onyike, E., et al.Columbin inhibits cholesterol uptake in bloodstream forms of Trypanosoma brucei-A possible trypanocidal mechanismJ. Enzyme Inhib. Med. Chem.20(4)365-368(2005) 2.Abdelwahab, S.I., Koko, W.S., Mohamed Elhassan Taha, M., et al.In vitro and in vivo anti-inflammatory activities of columbin through the inhibition of cycloxygenase-2 and nitric oxide but not the suppression of NF-κB translocationEur. J. Pharmacol.678(1-3)61-70(2012) 3.Kohno, H., Maeda, M., Tanino, M., et al.A bitter diterpenoid furanolactone columbin from Calumbae Radix inhibits azoxymethane-induced rat colon carcinogenesisCancer Lett.183(2)131-139(2002) 4.Wada, K., Kurihara, T., Yagi, M., et al.Columbin isolated from calumbae radix affects the sleeping time of anesthetized miceBiol. Pharm. Bull.18(4)634-636(1995)
Animal experiment: | Rats: Male Wistar rats are treated as following: i.v. injection of columbin in EtOH and PEG-300 (1:1) is administrated through tail vein at dose of 20 mg/kg. Intraperitoneal (i.p.) injection of columbin in EtOH and PEG-300 (1:1) is administrated at dose of 20 mg/kg. An oral gavage of columbin suspended in oral suspension vehicle is given to rats at dose of 50 mg/kg. Blood samples (50-100 μL) are collected by snipping the tail into heparinized tubes at 0, 5, 15, 30, 45, 60, 120, 240, 360, 480 and 1440 min for i.v. administration, or at 0, 15, 30, 60,120, 180, 240, 360, 480, 1440 min for oral dosing or i.p. injection. The blood samples are stored at −20°C until analysis[2]. Mice: Male Balb/c mice (n=60) are randomly divided into six groups. Columbin is intra-peritoneally administered to mice at the dose of 30, 100, 300 and 700 mg/kg. Aspirin, an anti-inflammatory drug, is used as a positive control. To induce acute phase inflammation in paw, rats are injected subcutaneously into the right hind paw with a 1% solution of carrageenan dissolved in saline 30 min after vehicle or columbin treatment. The paw volumes are measured up to 5 h after the injection at intervals of 1 h. Paw volume is measured with a plethysmometer immediately prior to the injection of carrageenan and thereafter at an interval of 1 h for a period of 5 h[1]. |
References: [1]. Ibrahim Abdelwahab S, et al. In vitro and in vivo anti-inflammatory activities of columbin through the inhibition of cycloxygenase-2 and nitric oxide but not the suppression of NF-κB translocation. Eur J Pharmacol. 2012 Mar 5;678(1-3):61-70. |
Cas No. | 546-97-4 | SDF | |
别名 | 古伦宾 | ||
Canonical SMILES | O=C1[C@](C=C2)(O)[C@@](CC3)(C)[C@@]([C@@](C[C@@H](C4=COC=C4)O5)(C)[C@]3([H])C5=O)([H])[C@]2([H])O1 | ||
分子式 | C20H22O6 | 分子量 | 358.39 |
溶解度 | DMSO : ≥ 100 mg/mL (279.03 mM);Water : < 0.1 mg/mL (insoluble) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7903 mL | 13.9513 mL | 27.9026 mL |
5 mM | 0.5581 mL | 2.7903 mL | 5.5805 mL |
10 mM | 0.279 mL | 1.3951 mL | 2.7903 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。
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- Purity: >98.50%
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