Columbin

A diterpenoid furanolactone with diverse biological activities

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库存: 现货

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5mg

￥537.00

430.00

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10mg

￥862.00

690.00

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25mg

￥1712.00

1370.00

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50mg

￥3012.00

2410.00

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货号: ajce47740
CAS: 546-97-4
别名: 古伦宾
分子式: C20H22O6
分子量: 358.39
纯度: >98%
溶解度: DMSO : ≥ 100 mg/mL (279.03 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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)

Protocol

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].

参考文献:

[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.
[2]. Yang G, et al. Development and validation of an UPLC-MS/MS method for the quantification of columbin in biological matrices: Applications to absorption, metabolism, and pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:13-8.