As more and more peptides are being discovered and rigorously researched, a new player amongst them joined the game, known as Adipotide.
This peptide review provides some information on the potential adipotide benefits and side effects, especially regarding obesity and weight loss.
What Is Adipotide?
Adipotide, aka FTPP or Fat Targeted Proapoptotic Peptide, is a man-made peptidomimetic compound that’s been found to contain pro-apoptotic elements that lead to weight loss in rodents and monkeys.
Originally, Adipotide was formed as a treatment for cancer. It was designed to stop cancer cells in the blood from growing, by starving them. The impact of the peptide has presented that the substance actually deprives adipocytes of blood supply, causing them to die and be reabsorbed.
The first tests were performed on monkeys and rodents. According to the results, rodents presented a 30% reduction in body weight. After 4 weeks of daily administration (injections) of adipotide and 4 weeks of no treatment, ten rhesus, obese females had a 39% decrease in fat deposits and 11% reduction in body weight, on average.
Therefore, researchers are considering Adipotide as a peptide that can potentially help reduce body weight. This is due to the death of fat cells, as well as the reduction of adipose tissue beneath the skin. As a result of the reduced adipose tissue, waist circumference and overall BMI are reduced.
Adipotide is a man-made working compound with the ability to destroy adipocytes and cause a reduction in the overall concentration of subcutaneous fat. It is able to do this by carefully inducing the termination of cells that supply adipocytes within the blood vessels.
R. Pasqualini and Dr. W. Arap are responsible for the creation of adipotide, as a way to treat cancer by starving cancer cells within blood and stopping their growth. They found that the impact of Adipotide actually deprived adipocytes in the blood, causing their death and reabsorption in the body.
Reports from research say that the peptide is still in its trial phase, and is being tested on animals using clinical studies.
What Does Adipotide Do?
Research has found that the way this peptide acts has to do with the discriminatory killing of cells in the blood vessels that feed white adipose tissue. Adipotide leads to the vessels’ shrinkage (atrophy) and inevitably the death of cells (apoptosis), thus, cutting off the blood supply to adipocytes.
This, then, leads to insufficient or no oxygen and blood supply (ischemic injury) to the adipocytes. Since the impact is not reversible, the death of fat cells is also inevitable.
How Does Adipotide Work?
The stereo-chemical structure of this peptide, as presented by molecular analysis, has displayed the ability of adipotide to bind to 2 particular receptors that are found solely in the blood vessels that feed white adipose tissue.
ANXA-2 and Prohibitin are the particular receptors just mentioned. Because of these receptors’ tissue specificity, the peptide has no effect on brown adipose tissue, and so it doesn’t impact the thermogenesis of adaptive, brown fat.
The thermogenesis of brown fat is particularly important for babies, because they don’t have much capacity for heat conservation since the ratio of the body’s surface area to its volume prefers higher levels of heat loss. White adipose tissue is only produced when consumed energy surpasses used energy.
Epidemiological studies about 12 years ago presented that nearly 34 percent of the total American adult population is affected by obesity, which is caused by too much adipose tissue mass. Research has also shown that white adipose tissue is the primary contributor to the obesity of the population.
Body weight increases do not necessarily have to do with obesity, because such increases may result from increases in lean body mass and not exactly from fat cell increase. Obesity is also linked to and contributes to a rise in co-morbidity and mortality rates.
BMI Obesity and Adiposity
As of now, obesity is assessed using the skinfold thickness (anthropometry), Body Mass Index (BMI), and densitometry. A BMI score of thirty (30) is set as the obesity threshold.
A rise in adiposity puts impacted individuals at high risk for a variety of health issues, such as hyperlipidemia, cancers, hypertension, Non-Insulin Dependent Diabetes Mellitus (NIDDM), metabolic syndrome, myocardial infarction, and cerebrovascular accidents.
The morbidity rate is determined by how the adipose tissue is distributed; for example, adiposity localized to the buttocks and lower limbs is far less dangerous than adiposity concentrated in the abdominal region, leading to greater morbidity.
For these reasons, the waist-to-hip ratio is clinically used to determine the chances of an individual developing one or more of the mentioned health conditions. The link between the rise in morbidity and abdominal adiposity is assigned to the knowledge that fat cells within the abdomen have more lipolytic activity than the fat cells of the lower limbs.
What Is Adipose Tissue?
Adipose tissue is made up of lipid-storing adipose cells (adipocytes), and the vascular section where preadipocytes and macrophages are found. Adipose cell hypertrophy results from an increase of lipid discharge, and the rise in adipose mass is caused by the subsequent hyperplasia of adipose cells.
This increase is marked by an elevated differentiation of preadipocytes to adipocytes, as well as a large amount of invading macrophages. Such a transformation and maintenance of elevated adipose mass is held up by a constant blood supply to the fat tissue.
What Is Ischemic Injury?
Ischemic injury – the lack of oxygen and blood supply to the adipose tissue – would prevent the transformation and encourage the death of those injured fat cells. That’s why a peptidomimetic like adipotide would lead to a decrease in adipose mass by producing ischemic injury (that is not reversible) to the fat cells in white adipose tissue.
Adipotide Obesity Treatment
A study was conducted by M G Kolonin et al (2004) [ref 1] with the purpose of presenting that a targeted triggering of cell death in the blood vessels’ white adipose tissue could be utilized as a therapy towards obesity. The study used mice as its test subjects.
The experiment used a peptide motif isolate whose sequence allowed it to discriminatorily target white adipose tissue vasculature. In living organisms, phage display was utilized to separate the peptide motif so that it’s alone.
The results of the study showed researchers that the peptide motif is linked with prohibitin, a multifunctional membrane protein. It was then concluded that prohibitin was a label of vascular white adipose tissue.
Also displayed by the results was the finding that the cell death-causing peptide’s targeting of white adipose tissue vasculature led to the removal of the adipose tissue mass. The reabsorption of the white adipose led to a regularization of the metabolic processes altogether. This regulation took place without any significant side effects.
Monkeys and rodents are biologically different, and this leads to major difficulties in the translation of obesity treatments developed in rats into those for humans. Such challenges would be decreased if test subjects were also primates themselves.
Adipotide and Weight Loss
A team of researchers conducted a study (2011) [ref 3] in which a ligand-directed peptidomimetic was assessed for its functions in monkeys with obesity. The ligand-directed peptidomimetic was also named Adipotide.
The study’s results presented that Adipotide did trigger cell death in white adipose tissue vasculature, resulting in an improved insulin function and an accelerated decrease in weight in the primates.
The decrease in white fat mass was confirmed by dual-energy x-ray absorptiometry (DEXA) and Magnetic resonance imaging (MRI). Results also display an enhancement in the primates’ renal function. Therefore, this research concluded that Adipotide peptide may be considered an obesity-treating peptide prototype.
In another study in 2011 [ref 2] in which vascular labels for various organs were assessed, the research involved filtering of the library of peptides in patients with cancer, with the goal of discovering ligand-receptors particularly for specific vascular beds.
A survey of motifs stemming from biopsies yielded a non-random dispersion pattern which implied the possibility to target particular, systemic vascular beds. Deeper analysis through affinity chromatography , similarity search, and protein arrays uncovered four native ligand-receptors.
Two native ligand-receptors were dispersed in multiple tissues. The other receptors displayed a restricted particular dispersion with RAGE/leukocyte proteinase-3 being held to the development of secondary malignant growth in the bone, and prohibitin/annexin A2 being held to white adipose tissue.
This study presents, therefore, that the receptors expressed in the white fat vasculature of are prohibitin and ANXA-2 (annexin A2).
Adipotide Side Effects
Although the first batch of trials have been successfully performed on monkeys and rodents, researchers have observed some adverse side effects.
One of these adipotide side effects includes wounds of the small kidney that could lead to kidney failure if left untreated. The other noted side effect was dehydration.
You can find Adipotide for sale and other high quality peptides for research by visiting Core Peptides.
- Kolonin, M. G., Saha, P. K., Chan, L., Pasqualini, R., & Arap, W. Reversal of obesity by targeted ablation of adipose tissue. Nature medicine, 2004.
- Staquicini, F. I., Cardó-Vila, M., Kolonin, M. G., … & Arap, W. Vascular ligand-receptor mapping by direct combinatorial selection in cancer patients. Proceedings of the National Academy of Sciences, 2011.
- Barnhart, K. F., Christianson, D. R., Hanley, P. W., … & Pasqualini, R. A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys. Science translational medicine, 2011.
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