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Columbin

Cat. No. M19356
Columbin Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 95  USD95 In stock
20mg USD 150  USD150 In stock
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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 358.39
Formula C20H22O6
CAS Number 546-97-4
Form Solid
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jiaping Pei, et al. Chem Res Toxicol. Cytochrome P450 Enzyme-Mediated Bioactivation as an Underlying Mechanism of Columbin-Induced Hepatotoxicity

[2] Anil Yilmaz, et al. J Nat Prod. Semisynthesis and Kappa-Opioid Receptor Activity of Derivatives of Columbin, a Furanolactone Diterpene

[3] Siddig Ibrahim Abdelwahab, et al. Eur J Pharmacol. 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

[4] A J Nok, et al. J Enzyme Inhib Med Chem. Columbin inhibits cholesterol uptake in bloodstream forms of Trypanosoma brucei-A possible trypanocidal mechanism

[5] Hiroyuki Kohno, et al. Cancer Lett. A bitter diterpenoid furanolactone columbin from Calumbae Radix inhibits azoxymethane-induced rat colon carcinogenesis

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