CHEMICAL COMPOSITION OF HAWTHORN AND ITS SIGNIFICANCE IN FOLK MEDICINE

ABSTRACT

The chemical formulas of the substances included in the chemical composition of hawthorn, their effects on the body are explained. The role of hawthorn in folk medicine and the mechanism of action in diseases where it is used are explained. The antioxidant properties of hawthorn, its effect on the cardiovascular system, its use in diabetes, its effect on oncological diseases, its positive effect on cognitive functions, gastrointestinal tract, and lipid metabolism have been analyzed in detail.

АННОТАЦИЯ

Приведены химические формулы веществ, входящих в химический состав боярышника, их действие на организм. Объясняется роль боярышника в народной медицине и механизм действия при заболеваниях, где он применяется. Подробно проанализированы антиоксидантные свойства боярышника, его влияние на сердечно-сосудистую систему, применение при сахарном диабете, влияние на онкологические заболевания, положительное влияние на когнитивные функции, желудочно-кишечный тракт, липидный обмен.

Keywords: Hawthorn, antioxidant, pectin, flavonoids, free radicals, proanthocyanidins, triterpenoids, polyphenols

Ключевые слова: боярышник, антиоксидант, пектин, флавоноиды, свободные радикалы, проантоцианидины, тритерпеноиды, полифенолы.

Introduction. Hawthorn is a member of the family of rhododendrons, widely distributed in Europe, North America and East Asia, and 280 species have been identified to date. More than 150 chemicals have been identified in hawthorn, including some that are less well-studied. Hawthorn contains flavonoids, phenols, terpenoids and pectin. Hawthorn has a therapeutic effect: it affects the amount of glucose in the blood and lipid metabolism in the body, increases the tone of the spleen, has an appetite-stimulating effect[21]. Due to the high content of organic acids in the composition of hawthorn, it is also added to the composition of various food products in order to extend the shelf life [22]. Medicines are produced from hawthorn in many countries of the world. Therefore, it is desirable to expand the production of various food products and food additives from hawthorn. In this article, in order to create a new food additive from hawthorn, we tried to provide detailed analytical coverage of the effects of the substances contained in hawthorn on the body.

Antioxidant activity of hawthorn. Numerous experimental experiments have shown that the main cause of aging, oncological diseases, and neurodegenerative diseases is the accumulation of free radicals in the body. Often, after the formation of free radicals, antioxidant therapy does not help. Therefore, it is better to prevent their formation. Because various factors play a major role in their formation [11]. In order to prevent these processes, it is necessary to regularly consume nutritional supplements with antioxidant properties. Hawthorn contains various substances with antioxidant properties. For example, phenols. These substances are more abundant in the skin of hawthorn compared to the soft part, making the antioxidant properties invisible. Antioxidants also vary depending on extraction methods. For example: The antioxidant property of hawthorn was more strongly demonstrated in methanol and ethanol extracts. X loroform and petroleum ether extracts did not show antioxidant activity [4]. Some sources say that it is impossible to eat hawthorn during pregnancy. But quecetin and procyanidin have not been shown to have any tetrogenic effects when studied. However, quercetin has been observed to slightly reduce fetal weight during pregnancy. Flavonoids contained in hawthorn leaf extract have been proven in experimental experiments to increase the amount of estrogens, primordial follicles and decrease the amount of MDA [17].

Quercetin                                                                        Procyanidin

The aging process is accompanied by disturbances in cognitive functions. Neurons in the cerebral cortex and hippocampus are associated with neurodegeneration processes. As a result, the amount of acetylcholine receptors decreases, the activity of acetylcholinesterase and butyrylcholinesterase decreases. This leads to serious disorders of cognitive and memory processes. HJ Bae et al. (2020) induced cognitive impairment in rats using scopolamine and found that by adding the important terpenoid butanoic acid from hawthorn to the rats' diet, this substance increased the expression of neurotrophic factors in the hippocampus of the brain.

Antidiabetic action of hawthorn. Diabetes is known to cause mild cognitive impairment and dementia in the elderly. Animal experiments have shown that reduced insulin secretion causes loss of neurons and memory loss in the cerebral cortex. In diabetes, the increase in the number of free radicals due to hyperglycemia is the main cause of cognitive dysfunction. Experiments with rats with type 1 diabetes showed that natural antioxidant substances had a positive effect on the cognitive functions of rats. Considering that hawthorn is rich in flavonoids and polyphenols with antioxidant properties, we think it is appropriate to create a nutritional supplement that enhances cognitive functions.

Aierken et al., (2017) , Shih et al. (2013) proved that 80% methanolic extract of hawthorn lowers blood glucose levels in a series of experimental experiments. This hawthorn extract has been shown to prevent hyperglycemia by stimulating the release of insulin from the pancreas [6]. Diabetic gastroparesis is one of the common clinical complications of type 1 and type 2 diabetes. The development of gastroparesis in 30-50% of patients with diabetes has been reported in several literatures. Often, such patients complain of stomach motility disorders, weight loss, nausea, vomiting, abdominal pain. The use of drugs reduces the symptoms, but due to the side effects, it causes the appearance of secondary symptoms in the body. That is why it is important to use harmless natural and effective means.

Lignin

Motilin

Ghrelin

One of the main symptoms of diabetes is chronic hyperglycemia. And hyperglycemia leads to oxidative stress, which causes all the secondary diseases. Therefore, it is advisable to carry out antioxidant therapy in diabetes. Zheng et al. (2020) compared indicators of antioxidant capacity such as superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and malonyldialdehyde (MDA) before and after giving hawthorn seed ethylacetate extract to rats . increased, MDA decreased. With this, they proved that the substances contained in hawthorn seeds have antioxidant properties [122 articles].

Sin et al. (2021) found that hawthorn contains quercetin (74.58%), hyperoside (9.58%), and this substance is an inhibitor of intestinal alpha glycosidase. When alpha glycosidase is inhibited, the formation and absorption of glucose in the intestines is sharply reduced. Therefore, Chinese medicine has been using hawthorn extracts for the treatment of hyperglycemia for many years. Flavonoids contained in hawthorn have been proven to prevent cardiomyopathy in diabetes [9]. Vitexin, a hawthorn flavonoid, is suitable for use in type 2 diabetes due to its increased cell sensitivity to insulin [2].

Vitexin

Cardiovascular diseases have become one of the most urgent problems today. Despite the great progress made in the treatment of this disease, it is still one of the main causes of death. Oligomeric proanthocyanidins have cardiotonic properties, increase blood flow in coronary arteries, reduce the number of heart contractions. Procyanidins and flavonoids contained in hawthorn extract increase the amount of tsGMF and thereby dilate blood vessels. A hydroalcoholic extract of hawthorn reduces the production of factor X by the liver. It thins the blood. In addition, hawthorn increases the amount of antithrombin III in the heart. A reduction in the synthesis of factor X and an increase in the amount of antithrombin III in the heart reduces blood viscosity. This effect was observed when 100 mg of hawthorn extract was taken. Hawthorn flavonoids improve endothelial functions, lower arterial pressure and dilate blood vessels. When studying the effect of flavonoids on the body, it was found that they act on cells through Ca²⁺ - ATPases, controlling Ca²⁺ homeostasis [14]. In addition to antioxidant and metal chelator functions, flavonoids also have anticarcinogenic effects [15]. Dried fruits of hawthorn have been used to improve digestion and increase appetite [3]. Hawthorn pectins extracted by enzymatic hydrolysis inhibit the synthesis of fatty acids and have been shown in experiments to improve insulin sensitivity in obese rats [19].

Hawthorn seeds are rich in phenolic acids, flavonoids and lignans. Hawthorn seeds have hypolipidemic, anti-inflammatory, analgesic and antioxidant properties due to their rich chemical composition [13]. Ethylacetate extracts of hawthorn extract showed a hypolipidemic effect and prevented a sharp decrease in body mass. In addition, it increased the speed of emptying the stomach and stimulated the movement of the gastrointestinal tract. It was observed that the synthesis of substances such as ghrelin, motilin and gastrin, which control motility, were separated from the gastrointestinal tract in rats given ethylacetate extract and approached the normal state.

The use of hawthorn for violations of lipid metabolism. It was found that the amount of pectin in hawthorn increases further during ripening. As a result of studies, it was found that hawthorn pectin contains 67% uronic acid. When hawthorn pectin was given to rats, it was observed that the amount of ZPLP decreased, the amount of ZYuLP increased, and the rats' body weight decreased. They observed a decrease in expression of pectin 3 methyl 3 hydroxy glutaryl CoA reductase enzyme genes. When the pectin oligosaccharides contained in hawthorn were isolated and given to rats, the formation of bile fluid in the liver was accelerated and cholesterol accumulation was prevented. Ethanol extracts have been shown to prevent hyperlipidemia. In addition, pectin pentaoligogalacturonides have been observed to have anti-obesity and antioxidant properties. regular consumption of hawthorn pectin has been proven to be a cure for cardiovascular diseases and to increase the amount of insulin in the blood [1; 3]. In Germany, hawthorn extracts and teas made from leaves and flowers contain large amounts of flavonoids and proanthocyanidins and are recommended for patients with mild to moderate chronic heart failure. The chemical structure of pectin isolated from hawthorn, apricot, apple, and carrot and its effect on the body were studied. The results of the experiment showed that pectin isolated from the composition of hawthorn proved to be superior in terms of its chemical structure and positive effect on the body. The flavonoids contained in hawthorn dramatically reduce the amount of cholesterol in the blood. In addition, it inhibits the synthesis of cholesterol, fat and fatty acids in the liver. It has a hypolipidemic effect on the body as a whole and prevents atherosclerosis and myocardial infarction. But in order to reveal the full mechanism and reasons of these processes, it is desirable to conduct many experimental experiments [10].

Pectin

Anticancer activity. It is already known to science that regular consumption of fruits and vegetables can prevent cancer. Hawthorn also contains substances that can prevent the proliferation of cancer cells. Traditional Chinese medicine has been using hawthorn for gastrointestinal disorders. Li et al. (2013) demonstrated that triterpenoids in hawthorn have an anti-cancer effect. Tsiao et al. (2015) noted that triterpenoids extracted from hawthorn inhibited the proliferation of breast cancer and liver cancer. They mentioned that ursolic acid contained in hawthorn inhibits the proliferation of cancer cells and activates apoptosis. It has been shown that ursolic acid causes the destruction of mitochondria due to the activation of apoptosis enzymes. Through a series of experiments, it was found that hawthorn polysaccharides stop the proliferation of colon and stomach cancer cells, stop the cell cycle in S or G2/M phases, and activate apoptosis factors [4; 5].

Triterpenoid

The main oligomeric proanthocyanidins of hawthorn are proanthocyanidin B2, epicatechin, proanthocyanidin C1 and proanthocyanidin B5. When the anticancer effects of hawthorn oligomeric procyanidins were studied in colorectal cancer, it was found that HCT116 inhibited the proliferation of cancer cells by arresting the cell cycle [18]. The preferred chemotherapies are agents that only affect transformed cells without affecting normal cells. Experimental experiments with polysaccharides isolated from various plants revealed that these substances have an antiproliferative effect. Inducing apoptosis factors in cancer cells is known to give the most effective results. In this way, it is possible to reduce the size of cancer cells. It was found that the activity of caspase 3, 7, 8, 9 increased in the experiments conducted with homogenous polysaccharides of hawthorn [16].

Ursolic acid                                                                             Epicatechin

Procyanidin C1                                                     Procyanidin B2

Procyanidin B5

Anti-inflammatory action of hawthorn. Huang et al. (2011) studied the effect of Chinese hawthorn on the inflammatory process by giving it to rats, and the experiments confirmed that hawthorn reduced the formation of inflammatory mediators. This type of hawthorn was later shown to inhibit the formation of butanoic acid and pentacyclic triterpene inflammatory mediators. In experimental experiments, it was mentioned that flavonoids contained in 70% ethanolic extract of hawthorn have anti-inflammatory effect. Polyphenols and flavonoids in hawthorn have also been shown to prevent inflammation and have a healing effect. The flavonoids contained in the 70% extract of hawthorn had an anti-inflammatory effect. In experiments, pectin oligosaccharides contained in hawthorn have been proven to have an anti-inflammatory effect on the liver [8]. The lyophilized hydroalcoholic extract of hawthorn inhibits the synthesis of inflammatory factors and increases the paracellular permeability of Caco-2 cells due to its richness in flavonoids, thereby showing protection against epithelial barrier dysfunction. Pectin oligosaccharides extracted from hawthorn have been observed to increase their shelf life when added to infant formula.

Oleanolic acid                                                                                H  yperoside

Vitexin                                                                                 Rutin

Chlorogenic acid

The main flavonoids identified in hawthorn.

Summary. Hawthorn contains dozens of biologically active substances, which are the basis for its use as a healing food. Currently, cancer is the second leading cause of death in the world after cardiovascular diseases. Since hawthorn contains many biologically active substances, creating a new nutritional supplement based on hawthorn can prevent many diseases, including diabetes and its complications, inflammation of the gastrointestinal tract, diabetic gastroparesis, atherosclerosis and heart attack, as well as oncological diseases. Prevents and treats neurodegenerative changes in aging processes. Scientists from all over the world have studied the chemical composition of hawthorn and created various medicines and foods. But nowadays in our Republic, there are almost a lot of foods prepared from hawthorn. Hawthorn fruit skin contains carbohydrates (76.06-79.16 g), pectin substances (15.95-17.88 mg), polyphenols (2.06-2.43 mg), flavonoids (0.41-0.60 mg), citric acid (3.74-3.98 mg), vitamin C (0.37-0.42 mg) and minerals (Ca, Fe, P; 0.35-0.43 mg). Currently, more than 150 chemical substances have been identified in hawthorn leaves, flowers, and fruits, including flavonoids, pectin (6.4% in the fruit), lignans, monoterpenoids, triterpenoids, and organic acids. In various experimental and clinical studies, it is possible to use them as a treatment for many diseases. Therefore, it is appropriate to create food supplements from hawthorn species that are common in Uzbekistan.

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