Fatty Acid Amide Hydrolase (FAAH) Inhibitors: Discovery in Lepidium meyenii (Maca) Extracts
نویسندگان
چکیده
The pentane extract of the Peruvian plant Lepidium meyenii (Maca) has been shown to possess neuroprotective activity in vitro and in vivo. The involvement of the endocannabinoid system has been shown to be a possible mechanism of action. Some of the lipophilic constituents of Maca such as the macamides have been reported to possess significant pharmacological properties as shown in cell culture. However, their fatty acid amide hydrolase (FAAH) inhibitory activity was not determined. The aim of this study was to determine the FAAH inhibitory activity of the pentane extract from Maca, macamides and synthetic derivatives in an in vitro model using human recombinant FAAH. The pentane fraction from Maca and some of the macamides demonstrated a dose-dependent FAAH inhibitory activity. LC-MS/MS analysis demonstrated the presence of the macamides in the pentane extract. These results suggest a potential application of macamides from Maca or new synthesized derivatives (alkamides) as FAAH inhibitors to be used as analgesics, antidepressants, or antianxiety agents.
منابع مشابه
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
Fatty acid amide hydrolase (FAAH) degrades neuromodulating fatty acid amides including anandamide (endogenous cannabinoid agonist) and oleamide (sleep-inducing lipid) at their sites of action and is intimately involved in their regulation. Herein we report the discovery of a potent, selective, and efficacious class of reversible FAAH inhibitors that produce analgesia in animal models validating...
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