Role of Anatabine as an anti - inflammatory agent

Researchers at the Roskamp Institute are interested in the role of inflammation in aging and in particular in diseases like Alzheimer's Disease. We have shown that specific inflammatory chemicals play a key role in promoting the production of the toxic protein, amyloid, and that this in turn promotes more inflammation. Thus, Alzheimer's Disease is the consequence of a destructive cycle of inflammation where inflammatory chemicals cause the release of each other and cause damage and finally death to neurons in the process.

Inflammation is seen as so central to Alzheimer's Disease, and the aging process in general, that researchers have coined the phrase "inflammaging" to illustrate how entwined aging and inflammation are. Here at the Roskamp Institute researchers are testing drugs and naturally occurring compounds that have anti-inflammatory properties.

 Graph above increase in IL-1ß release after LPS stimulate stimulation in whole human blood. A dose-dependent decrease in the IL-1ß response is shown with increasing levels of anatabine. Lipitor which is thought to have some anti-inflammatory properties is shown by comparison, but has no effect on IL-1ß levels at these doses in this assay. For larger image click.

For instance, the graph above shows the effects of increasing doses of anatabine (RCP006 from Rock Creek Pharmaceuticals), a naturally occurring compound, on the release of an inflammatory molecule called interleukin 1-beta (IL-1ß). The graph shows the release of IL-1ß from human blood cells after stimulation with a molecule (LPS) released by bacteria, which typically causes inflammation during infection. The graph shows the expected increase in IL-1ß release after this stimulation. However, in the presence of anatabine there is a dose dependent decrease in the release of IL-1ß. Such results hold promise for the control of inflammation in many human conditions, and research is ongoing at the Roskamp Institute to bring this molecule into clinical studies to test its ability to regulate inflammation.

Anti-inflammatory effects of RCP006

The Roskamp Institute is interested in finding new treatments for the diseases of aging associated with chronic inflammation. In this respect Roskamp Institute scientists are examining the properties of RCP006 whose active ingredient is anatabine. The data shown here are preliminary experiments demonstrating the anti-inflammatory properties of RCP006.

In this experiment whole human blood was treated with LPS to stimulate inflammatory responses. LPS treatment was also accompanied by treatment with known anti-inflammatory compounds or with RCP006. The inflammatory molecule IL-1ß  was measured after 16 hours. The results show a reduced accumulation of IL-1ß  in RCP006 treated blood whereas the commonly used anti-inflammatory agents all triggered an increase in IL-1ß  production at lower doses prior to declines at higher doses. The data shown were generated by summing the area under the curve for the dose response (measured in IL-1ß levels) from zero to the treatment where full inhibition was achieved for each compound. These data are consistent with the active ingredient of RCP006, anatabine, having anti-inflammatory effects in human blood. For larger image of above image click here.

For larger image of above image click here.

LPS induced NF-KB activation in human white blood cells is decreased by RCP006

The Roskamp Institute is interested in finding new treatments for the diseases of aging associated with chronic inflammation. In this respect Roskamp Institute scientists are examining the properties of RCP006 whose active ingredient is anatabine. In further studies of NF-KB activity and anatabine's ability to decrease it, we see that LPS induced NF-KB activation in human white blood cells is decreased at dose equivalents to aspirin or celebrex (which is toxic at these doses).

In this experiment Peripheral blood mononuclear cells were isolated using ficoll paque method, as per manufacturer’s instructions. The cells were activated with LPS 10μg/ml and treated with 1.25mM Anatabine, Celebrex or Aspirin. Cells were incubated at 37°C and 5% CO2 with the above treatments overnight (18hrs) in RPMI media supplemented with 20mg/ml of PHA, 1% penstrep and 1% glutamax.For larger image click here.

 Illustration of how RCP006 might work as an Anti-inflammatory agent. Video source: http://anatabloc.com

Latest Postings

New from the Blog

Upcoming Events