Растительные эбурнаменинподобные индольные вещества (E.L.I.S.) для повышения работоспособности спортсменов
РезюмеВ статье дана характеристика эбурнаменинподобных индольных веществ (E.L.I.S.) растительного происхождения, применяемых в спортивной медицине. Показано, что E.L.I.S. улучшает двигательную координацию и мышечную память, оптимизирует процессы нейрональной регуляции функций организма. Эти эффекты создаются за счет синергичного действия содержащихся в растениях соединений ксантановой природы, что приводит к улучшению кровообращения, потребления глюкозы, оптимизации клеточного метаболизма, продукции нейромедиаторов, улучшению когнитивных свойств и таким образом - к улучшению церебральной активности в целом. В статье описаны многочисленные эффекты E.L.I.S., а также биохимические механизмы эффективности их применения в различных видах спорта, таких, как короткий спринт (100 м), марафон, игровые виды спорта.
Ключевые слова:E.L.I.S., эбурнаменинподобные индольные вещества, ксантины, метаболизм клетки, спортсмены
Вопр. питания. - 2013. - № 6. - С. 19-23.
a.1) Theobromine, obtained from cocoa, which acts as a vasodilator at different levels .
a.2) Theophylline is a cardiac stimulant and muscle relaxant . Oxyphillyne and propentophillyne are interesting derivatives which improve intermittent claudication , and adenosine inhibitors  and activators of cognitive functions .
a.3) Lastly, caffeine is a general stimulant of mental alertness, sufficiently well-known, which is extracted from tea and coffee and kola nut, amongst other plants.
These and other effects have been described for a long time, and it is generally recognized that the extracts or brews of some plants such as coffee, tea, cocoa, or even orally administering the plant itself as it is found in nature or ground or with some degree of preparation have a characteristic stimulating and tonic effect which produces a general invigoration of the physical state and a parallel stimulating action of mental activity, which depending on the plant in question, is more or less marked in some of the sensations relating to physical wellbeing and/or mental alertness that are produced.
The duration and intensity of the stimulating effect on the central nervous system (CNS), can be obtained either on a short term or longer term basis depending on the concentration of the extract or on the plant species used and, ultimately, depending on the quantity and combination of active ingredients found in the plant.
In recent years, research carried out on the mechanism of action related to these extracts in different grades of purity and isolation from their E.L.I.S., has resulted in an extensive range of chemical, pharmacological, clinical and medicinal scientific literature, mainly carried out on their most relevant active ingredients: vincamine, vinburnine and vinpocetine, to which we make reference at the end.
They are sufficiently well-known peripheral vasodilators (pat. US 4,400, 514, pat. ES 549.105) which act as cerebral oxygenators, and as memory activators . The improvement of the motor ability, mental activity and other parameters have been studied in depth in clinical studies carried out on thousands of people.
Furthermore, there are E.L.I.S. addition salts which are known to have similar properties or greatly improved ones and which are additionally soluble in aqueous solutions used to prepare drinks, [European Pat. 0154756], that have better bioavailability.
A note has been made of a series of hypothesis based generally on existing knowledge of cellular biochemistry. The facts most frequently found studied in connection with the effects of the E.L.I.S. are the following:
b.1) Effect on the elasticity/deformability of the erythrocyte, (Fig. 1), and vasodilation of micro-capillaries (Fig. 2). There is clinical evidence that supports the improvement of microcirculation due to these effects.
b.2) Cellular anti hypoxia effect of different tissues, due to the improved use of the available oxygen (Fig. 3), and the improvement in liberating it to the cellular tissue, from the hemoglobin in the erythrocytes (Fig. 4), when acting upon enzymes that affect the aforementioned liberation, such as 2,3 diphosphoglycerol (2,3-DPG).
This action is more and more pronounced as the concentration of 2,3-DPG with respect to the hemoglobin is reduced, which occurs in some people and generally decreases with age (Fig. 5 and 6).
b.3) Special effect on cerebral hypoxia in cerebral neurons. It has also been demonstrated to improve cerebral functioning, in conditions of cerebral hypoxia, as is the case of momentaneous blindness, (black out), in military aircraft crews or space capsules submitted to extreme accelerations, (Fig. 7 and 8).
The beneficial action of the E.L.I.S. has been studied in detail in mountain expeditions at altitudes higher than 5000 m such as the American Andes, and observing that it counteracts the effects of altitude sickness, (Fig. 9). Finally, we outline the framework of global actions relating to the E.L.I.S. It is important to mention the increased cellular metabolism, the greater production of neurotransmitters by the neuronal mitochondria, and the increase in the cellular energy available in the different body tissues, with an improvement of the energy available (Fig. 10).
b.4) Anti ischaemic and thrombolytic effect.
Clinical studies support the effect of the E.L.I.S. in the inhibition of thrombin formation, (Fig. 11) and with them the incidences in thrombosis and in ischaemias in general, and cerebral ones in particular, with their negative consequences for the correct functioning of the whole body, given the essential role of the brain in the orders and control of all the organs (Fig. 12).
The greater the loss of elasticity in arteries and veins, the more frequent these problems will be. This loss of elasticity may be due to inadequate nutritional habits or sedentary lifestyles which may become more acute as time passes, becoming general in old age, and eventually leading to the first symptoms of cognitive deterioration and motor disorders etc.
С. E.L.I.S. & Xanthines
The recent application of E.L.I.S. in functional nutrition, formulated with xanthines and other products frequently used in sports nutrition, such as amino acids, antioxidants, vitamins, etc., validates with scientific reasons the historical use thereof in popular nutrition and medicine.
The active ingredients responsible for the stimulating effects have generally been widely identified, therefore it is known that the xanthines are one of the main activators of mental alertness and wellbeing produced by coffee or tea, and theobromine being responsible for the effect of cocoa and chocolate-based goods. There are clinical works that support the synergy of xanthines with extracts containing E.L.I.S.: (US Pat. 629994 B1, Eurasia Pat. N° 000189, PCT Pat. ES 96/00082, and others).
Finally, we shall describe some pharmacological facts and their possible explanations regarding these synergistic phenomena which appear when administering the E.L.I.S. with the xanthic bases: It is known that the E.L.I.S. lower or inhibit the formation of phosphodiesterases (PDE), as the xanthines also do.
The adenylcyclase acts upon the adenosine monophosphate (AMP) and cyclic adenosine monophosphate (c-AMP) is obtained which, by the action of the PDE, liberates the AMP once again (See PAT FR 80 17165, N° of Publication 2469180). Therefore, if the theophylline inhibits the action of the phosphodiesterases (PDE) and therefore inhibits the formation of the c-AMP, and the E.L.I.S. also do so, there is an interesting synergistic effect to consider and use in order to globally activate the cellular activity in the brain and muscles.
This can be measured by the methods described in the literature (Biochem. Biophys. Acta 302, 50/1973, etc.) on animal tissue, for example pulp of brains of rats, and the inhibitory effect of various purified enzyme concentrations (PDE) can be tabulated and measured perfectly as compared with the c-AMP of the substrate, quantitatively determinable.
If some E.L.I.S. are added to the different solutions of varied concentrations of PDE the way it acts can be observed, evidencing a clear inhibition of the enzymatic activity of the PDE upon the referenced substrate.
The E.L.I.S. can be used to increase the intracellular metabolic processes both in muscular cells and in neurons, with the subsequent increase in the consumption of glucose and onset of fat-moving biochemical processes obtaining a greater supply of energy required to accelerate, activate or implement these processes in the brain and muscles, where energetic resources are very limited as the energy source originating from the movable polysaccharides is also limited. The ATP produced in this way, is the energy source usable for the cellular biochemistry in the whole body.
It was demonstrated that the E.L.I.S. also increase the levels of the serotonine, dopamine and noradrenaline neurotransmitters in the brain, (transmitters of indole nucleus), specifically involved in the cerebral biochemistry for the formation of memories associated with learning and they improve cellular use of oxygen, by the aforementioned anti-hypoxic action.
Measurable data can be obtained by experimentation, measuring the increase of the cerebral concentration of 5 hydroxy-triptophane (5HT) liberated, as well as a clear increase of its metabolite, the 5-hydroxy-indolacetic acid (5HIAA). This effect is at its maximum between 2 and 4 hours after having been administered.
The positive clinical results obtained especially in the CNS, thanks to the modern cerebral ‘scanning‘ techniques, (TAC, RMN) when they are applied to people performing certain cerebral functions, after having administered the E.L.I.S. during adequate periods, as compared to untreated subjects, are extrapolatable to athletes.
An interesting field of study is thus opened regarding the application of E.L.I.S. and xanthines, in different formulations developed specifically for athletes who use the consumption of glucose very differently in its two variations - anaerobic and aerobic.
If we focus our attention closely on different sports, such as weightlifting, sprints in 100 m sprint races, with short spurts of effort being required, and marathons and football, with effort being required for longer periods, where the ratio of both channels of glucose consumption is different, it is evident that an adequate formulation and continued use of functional foods and dietary supplements may lead to improving current Olympic records.
1. Cohen J.L. Analytical Profiles of Drug Substances / Ed. K. Florey. - N.Y.: Academic New Press, 1975. - Vol. 4. - P. 466-493.
2. Fredholm B.B., Lindstrоm K. // Acta Pharmacol. Toxicol. - 1986. - Vol. 58, N 3. - P. 187-192.
3. Hindmarch I., Subhan Z. // Ibid. - 1985. - N 5. - P. 379.
4. Lelo A., Birkett D.J., Robson R.A. et al. // Br. J. Clin. Pharmacol. - 1986. - Vol. 22, N 2. - P. 177-182.
5. Nagata K., Ogawa T., Omosu M. et al. // Arzneimittelforschung. - 1985. - Vol. 35, N 7. - P. 1034-1036. 6. Subhan Z., Hindmarch I. // Eur. J. Clin. Pharmacol. - 1985. - Vol. 28, N 5. - Р. 567-571.