Metabocin: Chili Pepper Component as an Anti-Obesity Drug

Obesity is defined as a condition of abnormal or excessive fat accumulation in adipose tissue, to the extent that health is impaired. The amount of excess fat in absolute terms, and its distribution in the body-either around the waist and trunk (abdominal, central or android obesity) or peripherally around the body (gynoid obesity) – have important health implications. The prevalence of obesity has increased globally over the past few decades. Recent age-adjusted estimates of global obesity prevalence report that at least 30% of men and 35% of women are obese in many countries worldwide, including in North America, Western Europe, Asia, and Australia.

Obesity has a negative influence on many risk factors associated with cardiovascular (CV) disease (CVD), such as increased blood pressure (BP), dyslipidemia, insulin resistance, and type 2 diabetes mellitus (T2DM). The development of these comorbidities is proportionate to the BMI and the degree of obesity. Consequently, individuals who are obese are more likely to develop CVD and manifestations of CVD, particularly coronary heart disease (CHD), angina, myocardial infarction (MI), atrial fibrillation, heart failure (HF) and sudden cardiac death (SCD). Evidence also indicates that morbidity and mortality rates increase proportionally with the degree of obesity in men and women.

Exercise and diet are the standard recommendation, but those are difficult for most people to maintain in the long term, and rebound weight gain usually occurs.

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Calcium concentration and TRCP1 Receptor

Epidemiologic data suggest that people with high calcium intake have a lower prevalence of overweight, obesity, and insulin resistance syndrome. Studies in transgenic mice have demonstrated that calcium influences adipocyte metabolism. High dietary calcium intakes also increases excretion of fecal fat and may increase core body temperature. Calcium from dairy products seems to have more of an impact than calcium from dietary supplements.

The TRPV1 receptor is a member of the vanilloid subclass of the transient receptor potential family (TRP)2 of ion channel proteins. They are non-selective cation channels activated by a range of stimuli including capsaicin, protons, noxious heat, etc. Its activation produces a significant flux of Ca2+ into cells. The resulting increase in [Ca2+]; in turn helps to trigger a number of important physiological and pathophysiological responses.

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Capsaicin stimulates the TRPV1 receptor

Capsaicin (8-methyl-N-vanillyl-6-nonenamide) is an active component of chili peppers, which are plants belonging to the genus Capsicum. It produces a sensation of burning in any tissue with which it comes into contact. Capsaicin and several related compounds are called capsaicinoids and are produced as secondary metabolites by chili peppers.

The best known exogenous activator of TRPV1 receptor is the phytochemical capsaicin. Epidemiological data revealed that the consumption of foods containing capsaicin was associated with a lower prevalence of obesity.

The potential mechanisms underlying the anti-obesity effects of capsaicin include: (1) increase lipid oxidation and inhibit adipogenesis; (2) activate BAT activity and induce thermogenesis; (3) suppress appetite and increase satiety regulated by neuronal circuits in the hypothalamus; (4) modulate the function of gastrointestinal tract and gut microbiome.

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Metabocin

A novel drug based on capsaicin, the compound that gives chili peppers their spicy burn, caused long term weight loss and improved metabolic health in mice eating a high fat diet, in new studies from the University of Wyoming, School of Pharmacy. Metabocin, was designed to slowly release capsaicin throughout the day so it can exert its anti-obesity effect without producing inflammation or adverse side effects.

The research team developed Metabocin, which can be taken orally, to target receptors called TRPV1 that are found in high numbers in fat cells. Stimulating the TRPV1 receptors causes white fat cells to start burning energy instead of storing it, which, in theory, should cause weight loss. The mice in this experiment remained on the drug for 8 months, maintaining the weight loss with no evidence of safety problems.

Most of the capsaicin in spicy food is not well absorbed into the body so it would not produce these effects. The researchers specifically modified the capsaicin into Metabocin for proper absorption and sustained release. Hence the capsaicin uptake needs to be standardized and Metabocin should undergo further quality research validations before getting accepted as weight loss therapy.

©BforBiotech by Bedadyuti Mohanty, Assistant Managing Editor by Profession and Bio-technologist by heart.

 

 

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