Obesity has emerged as public health problem, resulting in significant burden of non-communicable diseases. A team of scientists at Maharaja Sayajirao University (MSU), Baroda have claimed success with a potent anti-obesity agent in studies done in laboratory animals.
The group, led by Prof. Mange Ram Yadav, has designed new molecules that seem to be effective in controlling food intake in preliminary studiesdone in rats. The researchers screened database of chemical compounds and identified a chemical moiety, phenothiazine, that can be modified to act as an anti-obesity agent. These compounds containing phenothiazineact on Cannabinoid Receptor 1 and inhibit it.
Cannabinoid Receptor 1 (CB1R)is a class of receptors present in the brain and other tissues and organs like eyes, mouth and oral cavity, cardiovascular system, gastrointestinal tract, and immune system. These receptors are involved in various functions like regulating our appetite, pain andemotions. A receptor is a molecule on the surface of a cell that receives chemical signals from the outside and results in initiating a response inside the cell.
Prof. Yadav with his research team
" Cannabinoid Receptor 1 (CB1R)is a class of receptors present in the brain and other tissues and organs like eyes, mouth and oral cavity, cardiovascular system, gastrointestinal tract, and immune system. "
“Activation of CB1R leads to increased food intake, while inhibition of this receptor decreases the feeding,” researchers explained. By exploiting this quality of CB1R, the team designed new molecules that target and inhibit this receptor and thus lead to decreased food intake. They further modified the molecule in such a way that it does not reach the brain and only acts on cells outside the central nervous system. This may help in avoiding side effects like anxiety and depression.
Preliminary studies done in rats showed significant decrease in food intake as compared torats in the control group. This study results have been published recently in journalScientific Reports.
“This group has reported the role of phenothiazine nucleus containing compounds as peripherally acting cannabinoid 1(CB1) receptor antagonists for management of obesity. The investigations have indicated good physiochemical and pharmacokinetic properties suggesting their drug- like behaviour”, noted Dr. Gita Chawla, Associate Professor in Department of Pharmaceutical Chemistry, Jamia Hamdard, who was not connected with the study.
“We are currently in the process of chemical modification and optimization of molecule activity that can then be converted in the form of drug”, Prof. Yadav told India Science Wire.He said he has file apatent application in India for these compounds.
The team included Mayank Kumar Sharma, JatinMachhi, Prashant Murumkar and M R Yadav. (India Science Wire)