BUȘURICU Florica1, ANGHEL Andreea Hortense2*, MARGARITTI Doina1, MITITELU Magdalena3, SCHRÖDER Verginica1
1Faculty of Pharmacy, Ovidius University, Mamaia Blvd. 124, 900527, Constanta, Romania
2Faculty of Biology, Bulevardul 1 Mai 3-5, 900123, Constanta, Romania
3Faculty of Pharmacy, UMF Carol Davila, Bucharest, Romania
*Corresponding author: andreeaanghel1970@@hotmail.com
Caffeine is one of the stimulants of the central nervous system which increases the cognitive ability, memory, intellectual and physical performance, which is why it is accepted to be often added to energy drinks and food supplements with or without other combinations based on plant extracts (guarana, ginseng, ginger) and synthetic nutrients (vitamins and minerals). In this study, we aim to highlight the benefits of caffeine and the indications regarding the consumption of products containing caffeine ± plant extracts, as well as the importance of avoiding the association of these products with central nervous system stimulants, MAOIs antidepressants or blood anticoagulants. The study aims to inform readers about the many possibilities of protecting health through moderate caffeine consumption, but also the negative effects of its high consumption, especially if it is associated with plant extracts that can interact. In our previous personal research, we focused on the study of the two categories of coffee (Robusta and Arabica) in terms of nutritional value and determination of ochratoxin A. In the future we intend to test the energizing action of caffeine in combination with various plant extracts, by the cytotoxicity test using the larvae of Artemia sp. (using BSLA citotoxicity test), used in some personal studies to highlight the toxic effect of food additives.
Specialists warn us that for a good food safety and security, we must follow the instructions on the amount of caffeine allowed by EFSA, read food labels carefully and avoid possible interactions with plant extracts added to energy products.
Keywords: caffeine, vegetable extracts, interactions
What is caffeine and what are its benefits?
Present in various caffeinated beverages, foods, food supplements and medicines, caffeine is known for: energy and central nervous system stimulating effect, intensifying mental activity and intellectual effort, producing at the same time a strong feeling of pleasure. Caffeine stimulates the respiratory centre, accelerating and increasing the amplitude of respiration; at the digestive system’s level, it stimulates gastric secretion, and at the renal level, it exerts a diuretic effect . Consumed in large quantities, it is responsible for the appearance of toxic phenomena manifested by anxiety, agitation and tremors of the extremities, tachycardia, extra systoles, palpitations, angina pain, gastric hyperacidity and diuresis [2, 3]. Caffeine decreases the amount of sleep and mainly the temporal organization of slow sleep and REM . Coffee is one of the world’s most popular drinks, and it is produced in more than 50 countries (fig.1 and 2). Caffeine can be extracted from the leaves, seeds and / or fruits of over 60 plants, among which we list: coffee beans, cocoa beans, tea leaves, kola nuts and guarana fruit. Depending on the source, caffeine has different names .
Fig.1 The world’s leading coffee producers (https://www.bbc.com/news/business-43742686)
Fig.2 Global coffee production (refference)
Natural sources of caffeine and their biological potential
Of these agricultural sources for caffeine, green coffee beans (unroasted) remain among the most traded in the world. Coffee beans, which contain coffee seeds, are produced by several species of a small perennial shrub like the coffee tree type. In order to make coffee, the ripe coffee beans are roasted, ground and subjected to extraction methods, obtaining caffeine (the name of the caffeine in coffee beans).
The main constituents known in green coffee, variable by plants and by cultivation lands are: proteins 8-14%; lipids 12-14%; carbohydrates 6%; mineral elements 4-5%, among which magnesium, potassium and phosphoric acid predominate; trace elements – manganese 1.3-3.2 mg, copper 1-3mg, zinc 0.2-0.7mg; B-complex vitamins (predominantly vitamin PP 16-26mg); organic acids, including 0.3% citric acid and 0.05% oxalic acid; purine alkaloids (caffeine, theobromine, theophylline); polyphenols . Baked and roasted beans for coffee preparation contain water-soluble compounds, of which the most specific and responsible for organoleptic and pharmaceutical properties are: caffeine, caffetannic acid (this name includes chlorogenic and cofalic acids), coffeol, carbohydrates, fats, especially albumin between proteins, tannins. When roasting are formed volatile compounds from fats, known as caffeine, in a proportion of 10-16%, being dark colour, gives the coffee its specific aroma and are formed predominantly from olein, stearin and palmitic. Roasting does not alter the amount of caffeine in the grains, but results less caffeine when the grains are measured by volume, as the grains increase in volume . An advantage of frying is that it reduces the content of ochratoxin A, which can often be in larger quantities than those allowed by FAO and WHO; roasting can reduce the content of ochratoxin A by 69-96% . It is well known the carcinogenic effect of mycotoxins, implicitly ochratoxin, manifested by the induction of tumours in the kidney, liver and urinary tract [9, 10, 11], which requires the consumer to pay attention to the quality of coffee consumed.
The bitter taste of coffee is given in symbiosis by the low content of sugar, caffeine and caffetannic acid (which is also responsible for the acidity of coffee) . Caffeine varies between 0.90% -2.0% and is partially free. Modern extraction methods emphasize the combined form with chlorogenic acid ranging from 5-6% . Nowadays, the two species of coffee, the Robusta coffee of West and Central Africa sub-Saharan Africa and the Arabica coffee, originating in southern -Western Ethiopia, are commercially recognized and cultivated. Growers appreciate Arabica coffee more than Robusta coffee. Robusta coffee tends to be bitter and less aromatic (aromatic oils 10%), whereas, compared to Arabica, it has more chlorogenic acid (10%), with about 40- 50% more caffeine (1.8- 4.0%) and is more resistant to leaf rust (Hemileia vastatrix). Arabica Coffee has a lower caffeine content (0.9-1.4%) and chlorogenic acid (6.5%), but a higher sugar content (8-9%) and essential oils (about 16-18%), a wide range of natural flavours, slightly fruity, caramel, nuts, honey, chocolate; aromas given by the peculiarities of the soil and the type of coffee origin. If from this variety a more acidic traditional Italian espresso is obtained, quality Robusta seeds generate an espresso, with a perfect taste and a better foam . Chlorogenic acids, like all polyphenols, are known to be biological antioxidants, able to counteract the harmful effects of excessive oxidation in the human body [14, 15]. Researches have linked the consumption of these coffee acids with slowing the absorption of glucose in the human intestine, which reduces the risk of developing type 2 diabetes [16, 17, 18]. Regarding the anticancer effect, the studies are not so conclusive , although other studies show a significant increase in antioxidant activity with the degree of roasting, based on the formation of Maillard reaction compounds (antioxidant compounds of melanoidin) which largely compensate for the decrease in polyphenols during frying .
Another source of caffeine, called theine, is Camellia sinensis L.(O.) Kuntze (syn. Thea sinensis L.), from the Theacea family, a plant known to us in Romania under the name of tea, originally from China. The leaves have a varied composition in polyphenols – compounds with organoleptic and pharmacological importance (36%), purine alkaloids (caffeine, theobromine, and theophylline), vitamin C, minerals and amino acids . The values of caffeine content reported in the literature for black tea and green tea are between 1 – 5% from its dry weight, varying depending on the type, mark and method of obtaining. Consumption statistics show that black tea is preferred among consumers – 78%, to the detriment of green tea, which reaches a percentage of 20% . Caffeine is also found in kola nuts, which represent the fruit of the Kola tree (Cola acuminata și Cola nitida) from West Africa. Kola extract is appreciated for its effects as a stimulant of the central nervous system, reduces hunger and thirst, and acts as a bronchodilator . Kola extract extracted by different methods, is used safely for human consumption, approved by Food and Drug Administration of the USA (FDA), constituting the common food flavour initially from Coca-Cola and Pepsi-Cola, and now from many popular energy drinks . Conventional extraction methods have some disadvantages, because they use solvents, they destroy by oxidation the active principles which are thus deprived of a large part of their physiological value, and the caffeine content is low, being in the free form whose value is certainly not higher. Than that of a product obtained by using synthetic caffeine. The advantageous process that qualitatively improves the extract, being completely stabilized with a high content of combined caffeine, associated with alkaloids and phenolic compounds, is the one that inactivates oxidases from the beginning, making it possible to maintain the association of alkaloids and phenolic compounds .
For people who want to consume more coffee or those with osteoporosis, it is recommended to drink decaffeinated coffee. For pharmaceutical and cosmetic purposes, although caffeine can now be obtained also by synthesis, it is preferable to use the natural form obtained by decaffeinating coffee beans. A decaffeination process, much agreed and which does not involve the use of solvents that could intoxicate the final product, consists in the “Swiss water process”. After decaffeination, coffee beans have a residual caffeine content of 0.1%, so that coffee made from decaffeinated coffee beans has a low content of 3-5 mg of caffeine per 100 mL of coffee, compared to caffeinated coffee beans. Researches demonstrate that the other compounds are not affected, even polyphenolic compounds, healthy for the body, which is an advantage for consumers of decaffeinated coffee, and the process ensures high extraction yield .
Cocoa beans are another source of caffeine. They are the seeds of the tree Theobroma cacao, native from the Amazon region and currently cultivated in several regions of the world, and by grinding them the cocoa powder is obtained. Cocoa powder has a complex chemical composition, which gives it nutritional value. It is rich in minerals (magnesium, copper, iron, calcium, phosphorus, selenium, potassium and zinc), antioxidant compounds especially flavonoids, catechins and epicatechins, caffeine, theobromine. Depending on the degree of fermentation and the type of cocoa beans, the caffeine content will vary between 0.1-0.5%. Among the benefits of cocoa consumption, we list: improving chronic fatigue syndrome, preventing heart disease, lowering blood pressure, lowering cholesterol, regulating blood sugar, protects against neurodegenerative diseases . Cocoa is consumed mainly in the form of chocolate, and the higher the percentage of cocoa in chocolate, the more likely it is to produce health benefits. Although cocoa is generally safe when consumed in moderation, large amounts can also cause side effects, such as: acne, migraines, allergies, skin inflammation . Caffeine can also be obtained from roasted red seeds of Paullinia cupana, a species of liana that grows in the Amazon forests of Brazil, in the form of a dry paste, known as guarana. In the area, its seeds are known as the fruit of youth, due to its healing properties and energizing effect, and guarana (as is called caffeine in guarana fruit) is added to food supplements, as a thermogenic substance and with the same benefits as of caffeine. Compared to coffee beans, guarana has almost twice as much caffeine (3 – 7%), and in combination with caffeine, has short-term beneficial effects. Despite the lack of well-founded studies on its associative properties with other food supplements, drugs and stimulants, is considered an attractive additive for energy drink producers [24,27,.
Caffeine interactions with some vegetable extracts
Energy drinks contain as main active ingredients- caffeine and sugars, to which are added mixtures of other substances, which provide an additional stimulant, over that provided only by caffeine, but are not subject to the same reporting requirements as caffeine and sugars. Frequently, when vegetable extracts are added to coffee (guarana, ginseng, cinnamon, and vanilla), it is taken into account the possible interactions that may occur depending on the concentration of caffeine, the respective extracts in the energy product, the amount of product consumed and for the administration of medicines / food supplements. It will be avoided association with central nervous system stimulants, MAOI antidepressants, sedatives or antiplatelet agents .
The beneficial or toxic effect of a chemical compound obtained from a plant source (as is the case with the caffeine in this paper) or any food additive in the composition of a food, food supplement or drug can be assessed by the BSLA cytotoxicity test [28, 29] or the PLDT planar mobility test . The stimulant effect of caffeine is mediated by a number of mechanisms, including intracellular calcium mobilization, phosphodiesterase inhibition, caffeine binding to benzodiazepine receptors, and adenosine receptor level antagonism .
By combining the administration of energy products with ginseng, insomnia will set in, and blood pressure will rise and trigger a number of heart problems. The addition of guarana will increase the caffeine content and thus its effects ; ginger extract has a stomachic, carminative effect and inhibits the accumulation of cholesterol . Clinical evidence shows that ginger is effective only in symptoms of nausea and vomiting associated with pregnancy, not in nausea and vomiting associated with other aetiologies, so there are European countries that currently recommend avoiding the administration of dietary supplements with ginger for these symptoms that may affect foetal development .
Caffeine intake from caffeine products
Regarding the safety of caffeine intake, the European Food Safety Authority (EFSA) recommends consumption as part of a balanced diet for health, if it does not exceed 400 mg daily (equivalent to up to 5 cups of coffee per day), and single doses should be up to 200 mg. Pregnant women are advised to limit their caffeine intake to 200 mg from all sources. EFSA has also recommended that single doses of 100 mg of caffeine may increase sleep latency and reduce sleep duration for some adults, especially when consumed near bedtime [32, 33]. In order to avoid toxic accidents, caffeine consumption should be done with great responsibility, especially since food ± medicines with such ingredient can be consumed simultaneously. We need to get used to reading the labels of the products consumed, so as to avoid the administration of an amount that exceeds the values recommended by EFDA. The highest concentration of caffeine is found in espresso coffee (130 mg / 100 mL coffee), followed by filter coffee (45mg /100 mL filter coffee), while in green tea we find a concentration of 20 mg caffeine / 100 mL tea; in 50 g chocolate about 30 mg caffeine, in hot chocolate about 5 mg caffeine / 100 mL, and in energy drinks an average of 50 mg caffeine / 100 mL product. The lethal dose for caffeine is 100 mg / kg body weight [7, 8].
The coffee remains in the top of your favourite natural drink, with a tonic effect unmatched by any other natural drink, but should be consumed in moderation. Scientific experts point out that for consumer safety, added caffeine and plant extracts must be included in the list of ingredients on the appropriate product labels. The added plant extracts may interact, and the health of the body may be affected, so that the association with central nervous system stimulants, MAOI antidepressants or blood anticoagulants should be avoided. Often, the lack of basic information from the manufacturer or consumer, calls into question how the combination of ingredients used in the preparation could affect the health of those who consume it. The negative effects of excessive consumption are usually short-lived once the individual returns to his regular pattern of consumption.
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