Columbin is an orally active diterpenoid furanolactone from Calumbae radix, has anti-inflammatory and anti-trypanosomal effects. Columbin selectively inhibits COX-2 (EC₅₀=53.1 μM) over COX-1 (EC₅₀=327 μM)^[1][2].

Treatment with columbin or l-NAME inhibits LPS/IFN-γ-induced NO production without affecting the viability of RAW264.7. Pre-treatment of stimulated cells with columbin does not inhibit the translocation of NF-κB to the nucleus in LPS-stimulated cells. COX-1 and COX-2 inhibitory activities of columbin are 63.7±6.4% and 18.8±1.5% inhibition at 100μM, respectively. The interaction of columbin with Tyr385 and Arg120 signifies its higher activity in COX-2, as Tyr385 is reported to be involved in the abstraction of hydrogen from C-13 of arachidonate, and Arg120 is critical for high affinity arachidonate binding^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Columbin inhibits oedema formation in mice paw. At doses of 300 mg/kg and 700 mg/kg, columbin inhibits inflammation from 0 to 5 h and the results are comparable to that of aspirin as a standard anti-inflammatory drug. The inhibitory effect of columbin on carrageenan induced paw oedema in mice may be due to the suppression of the release of mediators responsible for inflammation including prostaglandin^[1]. Columbin is poorly bioavailable (2.8% p.o. and 14% i.p.) in rats, but its transport is rapid across the Caco-2 cell monolayers, suggesting that extensive first-pass metabolism in the liver is the likely reason for its poor bioavailability^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

358.39

C₂₀H₂₂O₆

546-97-4

固体

White to off-white

古伦宾；咖伦宾；青牛胆苦素

• Terpenoids
• Diterpenoids

• 植物
• 其他科

Room temperature in continental US; may vary elsewhere.

DMSO 中的溶解度 : ≥ 100 mg/mL (279.03 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* “≥” means soluble, but saturation unknown.

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

• 方案 一

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

  Solubility: ≥ 2.5 mg/mL (6.98 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

  生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

• 方案 二

  请依序添加每种溶剂： 10% DMSO    90% Corn Oil

  Solubility: ≥ 2.5 mg/mL (6.98 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.  [Content Brief]

  [2]. A J Nok, et al. Columbin inhibits cholesterol uptake in bloodstream forms of Trypanosoma brucei-A possible trypanocidal mechanism.J Enzyme Inhib Med Chem. 2005 Aug;20(4):365-8.  [Content Brief]

  [3]. 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  [Content Brief]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.  [Content Brief]

  [2]. A J Nok, et al. Columbin inhibits cholesterol uptake in bloodstream forms of Trypanosoma brucei-A possible trypanocidal mechanism.J Enzyme Inhib Med Chem. 2005 Aug;20(4):365-8.  [Content Brief]

  [3]. 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  [Content Brief]