Columbamine
Columbamine exerts anti-proliferative and anti-vasculogenic effects on metastatic human osteosarcoma U2OS cells with low toxicity. It shows strong acetylcholinesterase (AChE) inhibitory activity with IC50 48.1 μM.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Toxicol Lett. 2012 Dec 17;215(3):174-80.
Columbamine suppresses the proliferation and neovascularization of metastatic osteosarcoma U2OS cells with low cytotoxicity.[Pubmed:
23124089]
Columbamine (COL), an active component of the herb Coptis chinensis, inhibited the proliferation and neovascularization of metastatic osteosarcoma U2OS cells.
METHODS AND RESULTS:
Columbamine effectively suppressed U2OS cell proliferation in vitro with an IC(50) of 21.31±0.38μM, with low cytotoxicity. Mechanistic studies revealed that Columbamine induces cell cycle arrest at the G2/M transition, which is associated with attenuating CDK6 gene expression and diminishing STAT3 phosphorylation. Columbamine did not significantly promote U2OS cell apoptosis at any of the dosages tested. Additionally, Columbamine inhibited U2OS cell-mediated neovascularization, which was accompanied by the down-regulation of matrix metalloproteinase (MMP) 2 expression and reduction of cell migration, adhesion, and invasion. Taken together, our data show that Columbamine exerts anti-proliferative and anti-vasculogenic effects on metastatic human osteosarcoma U2OS cells with low toxicity.
CONCLUSIONS:
These results warrant further investigation of Columbamine as a potential anti-osteosarcoma and anti-cancer drug.
Molecules. 2014 Jan 20;19(1):1201-11.
Anticholinesterase inhibitory activity of quaternary alkaloids from Tinospora crispa.[Pubmed:
24448061]
Quaternary alkaloids are the major alkaloids isolated from Tinospora species. A previous study pointed to the necessary presence of quaternary nitrogens for strong acetylcholinesterase (AChE) inhibitory activity in such alkaloids.
METHODS AND RESULTS:
Repeated column chromatography of the vine of Tinospora crispa extract led to the isolation of one new protoberberine alkaloid, 4,13-dihydroxy-2,8,9-trimethoxydibenzo[a,g]quinolizinium (1), along with six known alkaloids-dihydrodiscretamine (2), Columbamine (3), magnoflorine (4), N-formylannonaine (5), N-formylnornuciferine (6), and N-trans-feruloyltyramine (7). The seven compounds were isolated and structurally elucidated by spectroscopic analysis. Two known alkaloids, namely, dihydrodiscretamine and Columbamine are reported for the first time for this plant. The compounds were tested for AChE inhibitory activity using Ellman's method. In the AChE inhibition assay, only Columbamine (3) showed strong activity with IC50 48.1 µM.
CONCLUSIONS:
The structure-activity relationships derived from these results suggest that the quaternary nitrogen in the skeleton has some effect, but that a high degree of methoxylation is more important for acetylcholinesterase inhibition.
