古伦宾

中文名称:

古伦宾

中文同义词:

古伦宾, 来源于青牛胆;咖伦宾;COLUMBIN 古伦宾;青牛胆苦素、黄藤内酯、防己内酯、非洲防己苦素;非洲防己苦素;古伦宾;古伦宾对照品

英文名称:

Columbin

英文同义词:

(1s,2s,3s,5s,8r,11r,12s)-5-(3-furyl)-12-hydroxy-3,11-dimethyl-6,14-dioxatetracyclo[10.2.2.02,11.03,8]hexadec-15-ene-7,13-dione;Columbin, 98%, from limacia sagittata;(1R,4R,4aR,6aR,9S,10aS,10bS)-9-(3-Furanyl)-1,4,4a,5,6,6a,9,10,10a,10b-decahydro-4-hydroxy-4a,10a-dimethyl-1,4-etheno-3H,7H-benzo[1,2-c:3,4-c]dipyran-3,7-dione;(1R,4R,4aR,6aR,9S,10aS,10bS)-9-(3-Furanyl)decahydro-4-hydroxy-4a,10a-dimethyl-1,4-etheno-3H,7H-benzo[1,2-c:3,4-c]dipyran-3,7-dione;Tinosporin;(1R,2S,3S,5S,8R,11R,12R)-5-(3-Furyl)-12-hydroxy-3,11-dimethyl-6,14-dioxatetracyclo[10.2.2.02,11.03,8]hexadec-15-ene-7,13-dione;(1R,2S,3S,5S,8R,11R,12R)-5-(3-Furyl)-12-hydroxy-3,11-dimethyl-6,14-dioxatetracyclo[10.2.2.02,11.03,8]hexadec-15-ene-7,13-dione;1,4-Etheno-3H,7H-benzo[1,2-c:3,4-c]dipyran-3,7-dione, 9-(3-furanyl)-1,4,4a,5,6,6a,9,10,10a,10b-decahydro-4-hydroxy-4a,10a-dimethyl-, (1R,4R,4aR,6aR,9S,10aS,10bS)-

CAS号:

546-97-4

分子式:

C20H22O6

分子量:

358.39

EINECS号:

相关类别:

对照品，标准品;中药对照品;标准品;对照品;植物提取物;古伦宾;标准品-对照品;Miscellaneous Natural Products;分析试剂标准品;对照品-中药对照品;标准品 -中药标准品;标准品，对照品

Mol文件:

546-97-4.mol

熔点 

190-191℃

比旋光度 

D +52.5° (pyridine)

沸点 

410.82°C (rough estimate)

密度 

1.36

折射率 

1.4450 (estimate)

储存条件 

-20°C

酸度系数(pKa)

12.14±0.70(Predicted)

用途

古伦宾是呋喃内酯二萜，是从亚特里萨（Jateorhiza）和丁诺斯菌属（Tinospora）的根中分离出来的，被用于亚洲和非洲民间医学中，具有止痛和解热的作用。

生物活性

Columbin 是一种口服活性二萜呋喃内酯，具有抗炎和抗锥虫体作用。Columbin 选择性抑制 COX-2 (EC50=53.1 μM)，选择性高于抑制 COX-1 (EC50=327 μM)。

靶点

COX-2 53.1 μM (EC 50 ) COX-1 327 μM (EC 50 )

COX-2 53.1 μM (EC 50 )

COX-1 327 μM (EC 50 )

体外研究

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.

体内研究

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. 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.

化学性质 

白色针状结晶，易溶于甲醇、乙酸乙酯，几乎不溶于水，来源于金国榄。

用途 

古伦宾具有抗菌的作用。

用途 

用于含量测定/鉴定/药理实验等

WGK Germany 

3

海关编码 

29322090