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04.10.2015


Arctigenin, the endurance drug in Arctium lappa

The medicinal plant Arctium lappa contains the lignan arctigenin, a substance that works like an endurance drug. Researchers at the Shanghai Institute of Materia Medica in China discovered this when they did an animal study, from which you could deduce that an effective daily human dose of arctigenin would be a couple of dozen milligrams.

Arctium lappa
Arctium lappa's common name is Burdock. You can buy extracts of this plant in every drugstore and supplements shop, but we'd immediately add that we don't know how much arctigenin these extracts contain. Not long ago we wrote about a Japanese animal study which showed that arctigenin supplementation combined with fasting helped inhibit tumours.

In vitro

The Chinese exposed heart cells [H9C2] and muscle cells [C2C12] to increasing concentrations of arctigenin [structural formula shown below]. The higher the concentration of arctigenin, the more active AMPK the researchers found in the cells.

AMPK is the enzyme that tells cells that they have to be more careful with the energy they have, and that they need to burn more fatty acids and absorb more glucose. AMPK becomes active as a result of extended periods of physical exercise and as a result of fasting.

ATG = arctigenin.


Arctigenin, the endurance drug in Arctium lappa


Arctigenin, the endurance drug in Arctium lappa


Arctigenin, the endurance drug in Arctium lappa



Arctigenin also activated PGC-1-alpha. We'll spare you the complicated molecular story, but PGC-1-alpha is a key molecule in the provision of energy in cells. If you activate PGC-1-alpha, cells are able to make more and better mitochondria.

In vivo
The researchers then gave sedentary mice 8 mg per kg bodyweight arctigenin [ATG] every day for six weeks. They injected the lignan directly into the small intestine, a form of administration that imitates the effect of oral administration. The human equivalent of this dose would be about 60 mg per day. You'd probably need to add a couple of dozen milligrams more though because probably not all arctigenin would make it intact through the stomach.

A control group was given no active substances [Veh].

At the end of the six weeks the Chinese researchers got the mice to run on a treadmill until they reached the point of exhaustion. The figure below shows that the mice that had been given arctigenin were capable of running for 40 percent longer than the mice in the control group, and covered a 60 percent longer distance.


Arctigenin, the endurance drug in Arctium lappa


Arctigenin, the endurance drug in Arctium lappa



The researchers found the above indications of increased mitochondrial biogenesis in the mice that had been given arctigenin.

Click here for a schema that shows how arctigenin probably works.

Conclusion
"We demonstrated that arctigenin could efficiently increase rodent sedentary treadmill endurance via enhancing AMPK phosphorylation", the researchers wrote. "This natural product induced the accommodation of mitochondrial biogenesis and fatty acid oxidation pathway to promote mitochondrial oxidative capacity without actual physical activities."

"Our results have provided additional understanding of pharmacological functions for arctigenin and the traditional Chinese medicine Arctium lappa, and suggested the potential of arctigenin as a lead compound for anti-obesity or anti type 2 diabetes drug discovery."

Source:
PLoS One. 2011;6(8):e24224.

More:
Lignan in Arctium lappa makes fasting deadlier for cancer cells 28.09.2015
Arctium lappa for more testosterone 11.05.2012