WO2023098964A1

WO2023098964A1 - Chromium pectinate propionate compound, to be administered orally and absorbed in the large intestine, for the improvement of sports performance and against metabolic syndrome

Info

Publication number: WO2023098964A1
Application number: PCT/EC2021/050004
Authority: WO
Inventors: Martin Francisco JIMENEZ MEZA
Original assignee: Jimenez Meza Martin Francisco
Priority date: 2021-12-01
Filing date: 2021-12-01
Publication date: 2023-06-08

Abstract

The invention relates to a chromium pectinate propionate compound to be administered orally and absorbed in the large intestine, in order to improve athletic performance and combat metabolic syndrome. The chemical compound has formula X-Y-Z, wherein X is propionic acid, Y is a polyvalent cation or mineral micronutrient (chromium, zinc, calcium, phosphorus, magnesium, sulphur, iron, manganese, cobalt, copper, silicon, nickel, molybdenum or selenium) which is bound to X by its carboxyl group, and Z is a dietary fibre (pectin, inulin, fructooligosaccharides, polydextrose, resistant starch or arabinogalactan), wherein the non-esterified carboxyl groups bind to Y and these bind to X.

Description

QUALIFICATION

Chromium pectinate propionate compound, to be administered orally and absorbed in the large intestine, to improve sports performance and against metabolic syndrome.

DESCRIPTION

FIELD OF INVENTION

The present invention is aimed at the creation of a compound (X-Y-Z) that allows the oral administration and absorption in the large intestine of propionate (X), in quantities independent of those produced in colonic microbial fermentation, which comprises, a dietary fiber (Z), at least one mineral micronutrient (Y) and propionate (X), to contribute to improving sports performance, against metabolic syndrome and reducing metabolic acidosis. In particular, the present invention is oriented towards a compound (X-Y-Z) consisting of pectin as dietary fiber (Z), chromium III and/or zinc as mineral micronutrient (Y), and propionate (X).

BACKGROUND OF THE INVENTION

Previous studies have demonstrated the functions and benefits of propionate (X), mineral micronutrients such as chromium III and/or zinc (Y), and dietary fibers such as pectin (Z), for improving sports performance and against metabolic syndrome. .

Propionate (X) is metabolized in the liver to act as a substrate in gluconeogenesis for the synthesis of glucose as an energy source for the body, contributing to the increase in the contractile capacity of the muscle cell, improving muscle strength during intense exercise and long-lasting, and maintaining cell excitability. At the systemic level, propionate (X) regulates lipid and glucose metabolism. Regarding lipid metabolism, propionate (X) has been shown to decrease hepatic cholesterol synthesis by inhibiting the activity of hydroxymethylglutaryl coenzyme A. It regulates glucose metabolism, while reducing postprandial blood glucose and improving blood glucose. insulin response.

On the other hand, propionate (X) being a substrate for gluconeogenesis, the lactate that is produced for this purpose, is used in the body for other known functions and benefits, which are, acting on the conductance of the dependent potassium channel. of ATP protecting the cell from Ca+ ² overload and death, contributing to the rapid onset of a level of oxygen consumption more adequate for power demand, initiating the work rate of oxidative phosphorylation in the mitochondria, and have an effect as a buffer of acid radicals.

The problem of fatigue and acute muscle pain is due to metabolic acidosis, where the ATP produced via aerobic and anaerobic pathways is hydrolyzed and hydrogen cations are released that lower the pH of the environment, causing acidosis. By using propionate (X) for gluconeogenesis, the lactate accumulated for this purpose takes another path, and since the conversion of pyruvate to lactate is reversible, lactate uses the hydrogen cations produced from ATP hydrolysis to transform again. in pyruvate, thus increasing the pH and decreasing metabolic acidosis, in addition, this pyruvate can enter the aerobic phase with the Krebs cycle, where a greater amount of ATP is produced for the organism, resulting in more energy and an improvement in the sports performance. Additionally, lactate also has a contribution to collagen synthesis and angiogenesis. Mineral micronutrients (Y) are essential elements that perform metabolic and physiological functions to maintain the body's health. Particularly chromium III and zinc (Y) have an action on the basic cellular reactions to maintain homeostasis in the metabolism of carbohydrates, lipids and proteins, as well as in the production of energy. By including chromium III and/or zinc (Y) supplements in the diet, benefits are obtained against metabolic syndrome, which encompasses diseases such as diabetes, obesity, dyslipidemia and increased blood pressure; since they provide a contribution in the reduction of body fat, triglycerides and cholesterol, and in the increase of muscle mass.

Dietary fibers (Z) are made up of a set of compounds such as polysaccharides, oligosaccharides, lignin and similar substances; that resist digestion and absorption in the human small intestine but can be partially or totally fermented in the large intestine by the colonic microbiota. Pectin, inulin, fructooligosaccharides, polydextrose, resistant starch and arabinogalactan are fibers (Z) with a high degree of fermentation, so they work for the purpose of the compound (X-Y-Z) of the present invention.

Propionate (X) is produced in the body by colonic microbial fermentation of dietary fiber (Z). It is generated from the metabolism of pyruvate, previously produced by the oxidation of glucose through the Embden-Meyerhof glycolytic pathway; which then, through one of the pathways, produces oxaloacetate, the key to starting the Wood-Werkman and Krebs cycles, through which propionate (X) is generated. Through another route, acetate and butyrate are also generated from pyruvate.

Depending on the type and concentration of both the fiber (Z) ingested and the intestinal microbiota, three short-chain fatty acids (acetic, propionic (X) and butyric acid) are produced in almost constant molar ratios of 60:25. :20 respectively, where between 10% and 50% of the propionate (X) is metabolized by the colonic mucosa, and only the remainder reaches the liver to act as a substrate in gluconeogenesis.

The problem is that this mechanism cannot control the efficiency, amount, or exclusivity of propionate (X) that is produced without inevitably and undesirably producing high amounts of hydrogen, carbon dioxide, and methane gas, in addition to producing acetate. which causes detrimental effects on sports performance and metabolic syndrome, such as the synthesis of cholesterol and fatty acids.

Another problem is that the direct oral intake of propionic acid, its ions or salts (X), are previously digested and absorbed in the stomach and small intestine, in the form of triglycerides, without efficiently reaching the large intestine.

However, intrarectal administration of propionate (X) has been shown to be sufficient to produce increased exercise performance. In addition, that the microbiota of the large intestine through the metabolic conversion of lactate to propionate (X), is a natural enzymatic process that improves athletic performance.

In view of the above, there is a need and importance for a compound (X-Y-Z) that can be ingested orally and that transports propionate (X) to be absorbed through the large intestine without being previously absorbed or digested in the stomach and small intestine.

The necessary carrier vehicle that forms part of the compound (XYZ), may be one of the dietary fibers (Z), which may particularly be pectin (Z), which is mainly composed of D-galacturonic acid; which has reactive sites, which, in the presence of a polyvalent cation (Y), such as mineral micronutrients (Y), form a bridge with acid residues from other nearby pectin (Z) molecules, forming a gelatinous mass. Pectin (Z) is available as either a low methoxyl pectin or a high methoxyl pectin. Low methoxyl (Z) pectin has a degree of esterification of less than about 50% and is highly reactive with cations (Y), such as any of the polyvalent mineral micronutrients (Y). High methoxyl (Z) pectin has a degree of esterification of more than about 50% and is less reactive with polyvalent cations.

(AND).

The term "degree of esterification" means the degree to which the free carboxylic acid groups contained in the pectin polygalacturonic acid chain (Z) have been esterified (eg, by methylation) or rendered non-acidic ( g., by amidation).

However, there is also a need for the compound (X-Y-Z) of the invention to make it possible to administer, to the large intestine, larger amounts of propionate (X) independent of the proportions of propionate (X), acetate, butyrate, hydrogen, carbon dioxide and methane gas, which are produced by colonic microbial fermentation of dietary fibers (Z).

Accordingly, there is a need for the composite (X-Y-Z) to contain a food fiber as a carrier matrix (Z); at least one mineral micronutrient (Y) which chemically links the fiber (Z) to the propionate (X); and that this polyvalent cation (Y) has, like propionate (X), properties that provide benefits for sports performance and against metabolic syndrome.

DESCRIPTION OF THE INVENTION

In view of the foregoing, the invention is directed to a compound (X-Y-Z) comprising propionic acid and its ionized forms or salts (X), or a combination thereof; at least one mineral micronutrient (Y) or combination thereof; and a dietary fiber (Z).

The mineral micronutrient (Y) refers to at least one selected from the group of chromium, zinc, calcium, iron, phosphorus, magnesium, sulfur, manganese, cobalt, copper, silicon, nickel, molybdenum and selenium, preferably chromium III and zinc , for its properties to improve sports performance and against metabolic syndrome, which are chemically linked to both propionate (X) through its carboxyl group, and to dietary fiber (Z) through its non-esterified carboxyl group.

The dietary fiber (Z) refers to one selected from the group of pectins, inulin, fructooligosaccharides, polydextrose, resistant starch and arabinogalactan, preferably pectin with a low degree of esterification.

PREPARATION OF THE MATERIAL OF THE INVENTION

The description of a preferred way to carry out the present invention is to use pectin

(Z) with a low degree of esterification, or carry out a chemical and/or enzymatic de-esterification.

Example 1. Pectin (Z) is diluted to a concentration between 1% and 2%, in an alkaline solution between pH 9 and 12 of chromium III propionate (XY) with a concentration between 0.5% and 1 %; heat the solution to 80°C and stir for 30 minutes, then adjust the pH to less than 4 to maintain pectin (Z) stability. To obtain it in powder, you can perform an Iophilization of the obtained solution.

Example 2. Pectin (Z) is diluted to a concentration between 1% and 2%, in an alkaline sodium hydroxide solution with a pH between 9 and 12, and is kept at 4°C under stirring for 48 hours; then the solution is adjusted with hydrochloric acid to a minimum pH of 4.5 and propionate is added Chromium III (XY) at a concentration between 0.5% and 1%; heat to 80°C and stir for 30min; then the pH is adjusted below 4 to maintain the stability of the pectin (Z). To obtain it in powder form, the obtained solution can be lyophilized.

Example 3. The pectin (Z) is subjected to an alkaline solution of 9 to 12 pH, of chromium III and/or zinc hydroxide (Y), in which the deesterified pectin (Z) can unite with its carboxyl groups , chrome and/or zinc (X). The concentration of pectin (Z) can be between 1% and 2%, and that of chromium III hydroxide and/or zinc (Y) between 0.5% and 1%. It is kept stirring at 4°C for 48 hours.

Propionic acid (X) is added to this chromium/zinc pectinate (YZ) solution at a concentration between 0.5% and 1% and is adjusted with hydrochloric acid to a minimum pH of 4.5; it is heated to 80°C and stirred for 30 minutes; then the pH is adjusted below 4 to maintain the stability of the pectin (Z). To obtain this powdered solution, it can be subjected to a lyophilization process.

Example 4. The pectin (Z) is subjected to an alkaline solution of 9 to 12 pH, of chromium III chloride and/or zinc chloride (Y), in which the deesterified pectin (Z) can unite with its groups carboxyls, chromium and/or zinc (X). The concentration of pectin (Z) can be between 1% and 2%, and that of chromium III chloride and/or zinc (Y) between 0.5% and 1%. It is kept stirring at 4°C for 48 hours.

Example 5. The pectin (Z) is subjected to an alkaline solution of 9 to 12 pH, of chromium III sulfate and/or zinc sulfate (Y), in which the deesterified pectin (Z) can unite with its groups carboxyls, chromium and/or zinc (X). The concentration of pectin (Z) can be between 1% and 2%, and that of chromium III sulfate and/or zinc (Y) between 0.5% and 1%. It is kept stirring at 4°C for 48 hours.

In view of the preferred embodiments presented above, various methods, concentrations and materials of native or modified food fibers can be prepared, particularly de-esterified pectin (Z); In the same way, different concentrations and sources of mineral micronutrients can be used in ionized form, bases or salts, mainly chromium and/or zinc (Y); in the case of propionate (X) it can be used as acid, salt or ionized; and as a pH adjuster, various acids or bases can be used.

Because many variations, modifications, and changes in detail can be made to the described preferred embodiment of the present invention, it is intended that all aspects of the foregoing description of execution be construed as illustrative and not limiting. Therefore, the scope of the invention should be determined by the appended claims and their legal equivalents.

Claims

5 CLAIMS

1. Chemical compound to administer propionate and mineral micronutrients orally, to the large intestine, regardless of the proportions of propionate produced in the colonic microbial fermentation of food fibers, with the formula:

X AND Z

Where

X is propionic acid, its ionized form or salts, or the combination thereof;

Y is at least one polyvalent cation or mineral micronutrient selected from the group of chromium, zinc, calcium, phosphorus, magnesium, sulfur, iron, manganese, cobalt, copper, silicon, nickel, molybdenum, and selenium, which binds to X by its carboxyl group; and

Z is one of the dietary fibers selected from the group of pectin, inulin, fructooligosaccharides, polydextrose, resistant starch and arabinogalactan, where the non-esterified carboxyl groups are attached to Y, and these to X.