| Description: |
Columbianetin is a new phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage, it also has antifungal activity. Columbianetin has anti-inflammatory effects, it promotes histamine release, and inhibits the histamine release by substance P, suggests that it may be helpful in regulating mast cell-mediated allergic inflammatory responses. (2'S)-columbianetin can be effectively used to protect keratinocytes from UVB induced damage. |
| Targets: |
COX | IL Receptor | TNF-α | NF-kB | NOS | ROS | MAPK | AP-1 |
| In vitro: |
| J Photochem Photobiol B. 2012 Apr 2;109:20-7. | | Protective effect of (2'S)-columbianetin from Corydalis heterocarpa on UVB-induced keratinocyte damage.[Pubmed: 22321694 ] | A salt tolerant plant, Corydalis heterocarpa has been used as a folk medicine to treat travail and spasm. Recent studies have also reported antioxidant and antiinflammatory activities of compounds isolated from C. heterocarpa. In this study, the protective effect of (2'S)-Columbianetin isolated from C. heterocarpa on UVB-induced human keratinocyte (HaCaT) damage was investigated.
METHODS AND RESULTS:
First, the appropriate energy level of UVB irradiation was determined using MTT and LDH assays. And then the protective effect of (2'S)-Columbianetin on UVB induced HaCaT damage was evaluated by measuring; the changes in cell viability, LDH release level, ROS generation, cell cycle arrest and MMP expression levels. Finally, the effect of compound on MAPK and AP-1 signaling pathways were studied to understand the underlying signaling mechanisms. Result demonstrated that the presence of (2'S)-Columbianetin suppressed the reactive oxygen species (ROS) generation, cell cycle arrest at sub-G1 phase and down regulation of MMP expression in UVB treated HaCaT cells. Furthermore, stress activated signaling pathways (ASK1-MAPK) and AP-1 signaling pathway were regulated by (2'S)-Columbianetin treatment.
CONCLUSIONS:
These results suggest that (2'S)-Columbianetin could be effectively used to protect human keratinocytes from UVB induced damage. | | Phytochemistry, 1995, 39(6):1347-50. | | Columbianetin, a phytoalexin associated with celery resistance to pathogens during storage.[Reference: WebLink] | Columbianetin, rather than psoralens, was found to be a new phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage.
METHODS AND RESULTS:
In vitro, Columbianetin had at least 80 times greater antifungal activity than furanocoumarins (psoralens and angelicin). In vivo, the concentration of furanocoumarins in celery was 8μg g−1 fr. wt, and this is less than 0.25% of the concentration required for growth inhibition of celery pathogens. However, the concentration of Columbianetin in vivo was 38μg g−1 fr. wt, and this is close to the concentration required for growth inhibition of celery pathogens in vitro. |
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| In vivo: |
| J Ethnopharmacol. 2013 Oct 28;150(1):175-80. | | The pharmacokinetics and oral bioavailability studies of columbianetin in rats after oral and intravenous administration.[Pubmed: 23994338] | The roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan (RAP) has been used as Traditional Chinese medicine to treat rheumatic disease in China since ancient times, but its action mechanisms was not well understood. Columbianetin is one of the main active constituents isolated from RAP, which has been shown to have various biological activities, but the absorption characteristics and oral bioavailability dose proportionality of columbianetin in vivo were not studied.
METHODS AND RESULTS:
Male Sprague Dawley rats (210-230 g) received either an intravenous (i.v. 5, 10 and 20 mg kg(-1)) or oral (5, 10 and 20 mg kg(-1)) dose of columbianetin. The levels of columbianetin in plasma were measured by a simple and sensitive reversed-phase high-performance liquid chromatography (HPLC) method. The simple liquid-liquid extraction with ethyl acetate was used for sample preparation. Osthole was selected as internal standard (IS).
The chromatographic separation was accomplished on a C18 column at a flow rate of 1 mL min(-1), where water-methanol was used as mobile phase. The calibration curve of the method was linear in the concentration range of 0.05-2000 μg mL(-1). The intra and inter-day accuracy for columbianetin in rat plasma samples were within 8% and the variation was less than 8.3%. This method was suitable for the determination and pharmacokinetic study of columbianetin in rat plasma after both intravenous and oral administration. The results indicated that maximum plasma concentrations(Cmax) for the columbianetin (17-42 μg mL(-1)) were achieved at 0.3-0.5h post-oral dosing and the apparent volume of distribution (V/F) ranged from 0.38 to 0.44 L. Absolute bioavailability of columbianetin was assessed to be 81.13 ± 45.85, 81.09 ± 33.63 and 54.30 ± 23.19%, respectively. Terminal elimination half-life (T1/2) of the columbianetin after oral dosing was 60-90 min and were 2.5-3.3 fold longer than those observed for the i.v. dosing.
CONCLUSIONS:
The pharmacokinetic properties of columbianetin in rat after oral administration were characterized as rapid oral absorption, quick clearance and good absolute bioavailability. The bioavailability of columbianetin ranged from 54 to 81% for 5, 10 and 20 mg kg(-1) oral doses. The bioavailability of columbianetin is independent of the doses studied. Columbianetin showed dose proportionality over the dose range 5-20 mg kg(-1). The results clearly demonstrated that columbianetin was one of the material bases of RAP. Furthermore, an HPLC method was demonstrated in this study for the research of traditional Chinese medicine. |
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