NEU-P11 anti-obesity: synthetic analog is no worse than natural melatonin
A new synthetic analogue of melatonin will help fight obesityOver the past few years, obesity has become a real scourge of modern society.
The number of patients around the world is growing so rapidly that it's time to talk about an epidemic. This situation is largely determined by changes in the diet of people, an increase in the amount of fats and carbohydrates consumed. It is known that obesity is associated with, for example, type II diabetes mellitus, insulin resistance, insomnia, high blood pressure and atherosclerotic changes. Of course, in the course of treatment, it is necessary to deal not so much with concomitant diseases as with the main cause, that is, obesity. That is why the development of effective drugs to combat overweight is a very promising area of research.
The company "Neurim Pharmaceuticals Ltd." has developed a synthetic analogue of melatonin – the drug NEU-P11. According to numerous studies, melatonin is synthesized mainly at night and has a number of important properties: it has a hypnotic effect, affects the deposition of subcutaneous fat, changes in body weight, appetite, etc. That is, melatonin plays a regulatory role in lipid-carbohydrate metabolism, and also affects changes in body weight. That is why the researchers paid close attention to it.
In January 2009 The journal "Pharmacological Research" published the results of research by Chinese scientists from various institutes, in particular the Institute of Cardiovascular Disease, the Institute of Pharmacy and Pharmacology, etc. (Meihua S., Xiaojian D. et al., 2009). The researchers modeled obesity on rats and, accordingly, studied the effect of NEU-P11 on them.
60 male rats were selected for research. 12 of them received a regular diet (a mixture of cereals), 48 rats received a diet consisting of 53% of a mixture of cereals, 10% of fat and 37% of sucrose. Thus, the researchers modeled a diet that leads to obesity and an increased risk of developing diabetes. After 20 weeks, the rats were divided into 4 groups: positive control (received parenteral saline), obese rats receiving saline, NEU-P11 at a dosage of 10 mg/kg body weight and melatonin at a dosage of 4 mg/kg body weight, respectively. The duration of such treatment was 8 weeks. After that, the following parameters were measured: body weight, blood plasma composition (special attention was paid to the amount of triglycerides, cholesterol and insulin), activity of antioxidant enzymes and insulin resistance.
The results of the studies indicate the effectiveness of NEU-P11 in reducing body weight. After 8 weeks of using this drug, the body weight of obese rats decreased so much that it could be compared with that of control group animals. The same effect was found for melatonin, however, when using NEU-P11, body weight decreased faster, from which the researchers concluded that NEU-P11 is a more effective remedy. (Whether this is due to the difference in dosage is not clear from the brief retelling, but probably this fact is explained in the original article – NOTE) It was also noted that NEU-P11, like melatonin, does not affect feed intake. (It should be assumed that the experimental rats continued to sit on a high-calorie diet? – VM.)
During the increase in body weight in rats, the number of hypertrophied adipocytes (cells from which adipose tissue is formed) increased, which synthesized insulin resistance factors (for example, tumor necrosis factor-alpha). These factors reduce the absorption of glucose, which can lead to a decrease in its consumption in the muscles. As it was revealed during the study, the sensitivity to insulin decreased in obese rats, at the same time the amount of glucose, triglycerides, cholesterol increased in blood plasma compared to rats with normal body weight. Like melatonin, NEU-P11 significantly reduced insulin resistance. It also increased the activity of antioxidant enzymes and reduced the amount of the oxidative stress marker MDA.
Thus, the data obtained confirm the effectiveness of NEU-P11 in the fight against obesity. Clinical trials of the drug are next in line.
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