Roots of rauwolfia serpentine. Rauwolfia serpentine, marsh dryweed, small periwinkle. Application, chemical composition, side effects, contraindications. Sem. kutrovye - Apocynaceae

Rauvolfia (Rauvolfia serpentina Benth.) Is a perennial shrub; grows in South and Southeast Asia. In medicine, Rauwolfia root is used, containing alkaloids (see) and rescinamine, which have a sedative and hypotensive effect, aymalin and serpentine, which have antiarrhythmic properties, and other alkaloids.

Raunatin(Raunatinum;) contains the sum of alkaloids from rauwolfia roots; has hypotensive, sedative and antiarrhythmic effects.

Apply when; appoint inside at 0.002-0.012 and per day for 3-4 weeks. Release form: tablets of 0.002 g. See also Antihypertensives.

Rice. 58. Rauwolfia serpentine (left - root).

Rauwolfia (Rauwolfia snake; Rauwolfia, or Rauvolfia, serpentina Benth) is a perennial evergreen shrub 0.2-0.6 m high with a straight stem and a vertical rhizome, turning into a thinning, wrinkled, brown root up to 40 cm long; belongs to the kutrovy family (Apocynaceae Lindl.). It grows in South and Southeast Asia (India, Ceylon, Java, the Malay Peninsula). The botanical description of rauwolfia belongs to the German physician Rauwolf (L. Rauwolf, 16th century). In medicine, the root of rauwolfia is used, which is dug up in the 3-4th year of the plant's life and dried. About 40 alkaloids were isolated from rauwolfia, subdivided according to their chemical structure and basicity into three groups: tertiary indole (weak) bases - reserpine (see), rescinamine, yohimbine; tertiary indoline bases (medium strength) - aymalinidr .; Quaternary anhydronium bases (strong) - serpentine, etc. Reserpine is found in other types of rauwolfia (R. canescens Linn., R. micrantha Hook ,. R. tetraphylla L.). By pharmacological properties and therapeutic efficacy greatest value among the alkaloids of rauwolfia are reserpine and rescinamine, which have a sedative and hypotensive effect, as well as aymaline and serpentine, which have an antiarrhythmic effect.

Aimaline, unlike reserpine, is devoid of a tranquilizing effect, but has the ability to reduce the excitability of the myocardium and suppress ectopic impulse formation, lengthen the refractory phase and inhibit the conduction function.

Aymalin used for ventricular and atrial extrasystoles, sinus tachycardia, different forms paroxysmal tachycardia, Wolff-Parkinson-White syndrome. The drug is administered intravenously, intramuscularly and orally. For parenteral administration, a single dose of 50 mg (contents of one ampoule), daily - 100-150 mg. Inside appoint 1-2 pills (50-100 mg) 3-4 times a day for 1-3 weeks. Aimalin is contraindicated in severe lesions of the cardiac conduction system, sharp organic changes in the myocardium, severe heart failure and hypotension.

In medicine, a number of total alkaloid preparations of rauwolfia are also used (Gendon, Giuline, Raudixin, Raupina, Rauwiloid, Rauwoldin, Rivadescin, Wolfina, etc.).

Raunatin(domestic production) - analogue of Gendon, contains mainly alkaloids reserpine, serpentine and aymaline and has hypotensive, antiarrhythmic and, to a lesser extent, sedative effect. Raunatin is mainly used for hypertension, especially in stages I and II. The drug is produced in tablets containing 2 mg of the amount of rauwolfia alkaloids; prescribed after meals, 1-2 tablets per day, gradually increasing daily dose up to 5-6 tablets (10-12 mg). After the therapeutic effect is achieved, the dose is gradually reduced to 1-2 tablets. The course of treatment usually lasts 3-4 weeks. The antihypertensive effect of the total preparations of rauwolfia occurs more gradually than from reserpine; their side effect is much weaker.

Flower formula

Rauwolfia serpentine flower formula: * H (5) L (5) T5P (2).

In medicine

The roots of rauwolfia snakes are used as medicinal raw materials. Decoctions and extracts from them are used as a sedative and hypnotic, are used for acute gastrointestinal diseases, headaches, as a means of toning the muscles of the uterus. Indole alkaloids - reserpine and aymaline - are obtained from the roots, which are the basis for a number of drugs that are effective in the treatment of hypertension, some types of mental illness and have antiarrhythmic effects.

The roots of Rauwolfia snakes can be found in sports supplements. Their presence there is explained by the presence in the plant of the widely advertised alkaloid yohimbine, which is attributed to lipolytic action.

Contraindications and side effects

Preparations of rauwolfia snakes should be used after consulting a doctor and with caution. They are not recommended for pregnant women, persons with chronic diseases of the gastrointestinal tract, such as stomach or duodenal ulcers, diverticulosis and ulcerative colitis. Rauwolfia snakes cannot be combined with alcohol, some antitussives and flu medications. Do not take it without a doctor's recommendation and when taking barbiturates or antipsychotic medications. Inappropriate dosage of rauwolfia can cause poor circulation, depression and restless sleep, aggravated by nightmares. Excessive use of herbal preparations can lead to Parkinson's syndrome, and some doctors suggest that it can also lead to cancer.

Classification

Rauwolfia serpentine (lat.Rauwolfia serpentine Benth) is a perennial evergreen shrub from the shrub family (lat.Apocynaceae). In addition to the serpentine, several trees and shrubs belong to the genus Rauwolfia (lat.Rauwolfia), but the same alkaloids as in serpentine are found only in grayish rauwolfia (lat.Rauwolfia canescens L.) and rauwolfia vomitus (lat.Rauwolfia vomitoria Afz.)

Botanical description

Evergreen rauwolfia serpentine dwarf shrubs can reach 1 meter in height. Their healing rhizome is vertical, curved, with numerous roots of a grayish-rusty color, 20 to 40 centimeters long. At the break, the rhizome is light, non-fibrous. The stem is covered with whitish bark, usually unbranched. The leaves of the plant are short-petiolate, whorled, in one whorl there are from 3 to 5 oblong-elliptical, obovate or lanceolate leaves, thin, glabrous and shiny, from above pointed and light green alternate or, much less often, opposite. Rauwolfia leaves can be from 8 to 18 centimeters in length. The flowers of the plant are five-membered, collected in umbellate inflorescences. They have a white or pink corolla and bright red pedicels with sepals, a pistil, consisting of two carpels, connected by a filamentous column with a cylindrical stigma. The formula of a rauwolfia snake flower: * H (5) L (5) T5P (2). The fruits of the plant are red, consist of two juicy drupes grown together to the middle.

Spreading

In the wild, rauwolfia snakes grows in India, Thailand, Indochina, Indonesia and Sri Lanka. The plant prefers wet edges rainforest... They tried to cultivate Rauwolfia snake in the territory of the Transcaucasus, but the experience did not give positive results.

Procurement of raw materials

Although the rauwolfia snake is often found in the wild, this raw material is not enough to meet the needs of the pharmaceutical industry, so the plant is grown on plantations. Cultivated plants are harvested at 3-4 years of age, in the fruiting phase, digging with the rhizome. Rhizomes with roots are cut off, cleaned of dirt, trying not to damage the brown bark covering them, the richest in alkaloids. Raw materials with damaged bark are considered defective. Rauwolfia is dried by cutting it into pieces. You can dry snake rauwolfia in clear weather in the open air or in a specially equipped, well-ventilated room, where there are dryers with a temperature of 50-60 ° C.

Chemical composition

Rhizomes of rauwolfia serpentine contain at least 50 different indole alkaloids (1-2% of the total mass), the most important of which are reserpine, rescinamine, aymalin and serpentine. They also contain starch, resins and sterol. The rauwolfia stem contains milky juice, flavonoids and carotenoids.

Pharmacological properties

Medicinal properties rauwolfia snakes are associated with the alkaloids contained in it. Reserpine slows down the heart rate, has a hypotensive effect that develops slowly and lasts for several hours, it has sedative properties, causes drowsiness, close to physiological. Reserpine also lowers body temperature and metabolism, deepens breathing, narrows the pupils, inhibits interoceptive reflexes to blood pressure. Aimaline has antiarrhythmic activity.

Official medicine uses reserpine in tablets and solution as an antihypertensive and sedative for vegetative dystonia, functional disorders of the heart. Previously, reserpine was often used in the treatment of mental illnesses (psychoneuroses), but modern doctors believe that the drug has been overestimated and is prescribed less and less. Aimaline as an antiarrhythmic drug is used for atrial and ventricular extrasystoles, paroxysmal tachycardia. A complex drug of rauwolfia, raunatin has a sedative and hypotensive effect, another complex drug, rasedil, is administered for hypertensive crises and psychosis to relieve agitation. A decoction of rauwolfia roots is used as a sleeping pill.

Application in traditional medicine

In oriental medicine, the root of rauwolfia snake is used for insomnia, headache, nervousness, a number of mental disorders, epilepsy, high blood pressure. Also, the plant is considered effective remedy with constipation, liver disease, edema. It is still used to escape the bites of poisonous reptiles, which is why peasants in India try to have several rauwolfia bushes in the garden. A paste made from the roots of rauwolfia is taken from constipation and rubbed with it, to save oneself from rheumatism. Physicians give rauwolfia as an anthelmintic and antipyretic agent, treat her fever and cholera. Traditional healers recommend a decoction of the roots of the plant in a course to cope with alcoholic psychoses.

In homeopathy, Rauwolfia serpentina is known as Rauvolfia serpentina. In low dilutions, it is prescribed as a remedy for hypertension, in high dilutions, they drink rauwolfia for psychosis and some nervous diseases.

Historical reference

Rauwolfia snake has been known since ancient times. It is mentioned in Indian medical treatises dated 600 BC, and is listed among the 50 main herbs used in Chinese medicine. A decoction of rauwolfia was used to treat the bites of poisonous insects and reptiles. There is a legend that Alexander the Great treated his friend and commander Ptolemy, who was wounded by a poisonous arrow, with a drink from the "snake root", as Rauwolfia is called in India.

The Rauwolfia also has another name given to it by the Indians - "the root of the madmen." The inhabitants of this country believed that the plant was able to cope with such ailments as paranoia, increased anxiety and nervousness. These beneficial features Rauwolfia were tested much later by Western physicians. Isolated from the plant reserpine, in the fifties of the last century, they tried to treat schizophrenia. Of course, the drug was much more effective than the lobotomy adopted at that time, but still it was not a panacea. However, research into the properties of alkaloids isolated from rauwolfia helped determine the area of medicine where it is most appropriate and irreplaceable.

A great fan of Rauwolfia preparations was the spiritual leader of the Indian nation - Mahatma Gandhi. Every day he drank tea from powdered "snake root" and believed that it helped him maintain mental health and balance.

Literature

1. "Atlas of medicinal plants of the USSR" edited by Tsitsin NV, Moscow, State publishing house of medical literature, 1962- 472-473 p.

2. “Medicinal raw materials of plant and animal origin. Pharmacognosy "edited by G. Yakovlev, St. Petersburg, SpetsLit 2006 - 644-646 p.

3. "Medicinal plants" Reference manual edited by N.I.Grinkevich., Moscow, Higher School, 1991 - 274 p.

4. Turova AD, Sapozhnikova EN, "Medicinal plants of the SSR and their application", fourth edition, Moscow, Medicine - 107 p.

5. "Botanical and Pharmacognostic Dictionary", edited by K.F. Blinova. and Yakovleva G.P., Moscow, Higher School, 1990 - 229-230 p.

6. Muravyova D.A., Gammerman A.F., "Tropical and subtropical medicinal plants", Moscow, Medicine, 1974 - 140-142 p.

Rauwolfia snake -Rauwolfia serpentina Benth.

Sem. kutrovye - Apocynaceae

Botanical characteristics. An evergreen shrub containing milky juice, 0.2-0.6 (1) m high. It has a small vertical rhizome with numerous adventitious roots and a long tap root with large lateral roots. The stem is ascending, covered with a whitish cork. The leaves are arranged whorled in 3-4, less often opposite or alternate, oblong-elliptical, obovate or obovate or obovate, pointed at the apex, narrowed at the base into a short petiole, thin, glabrous, shiny, 7.5-17.5 cm long. The flowers are white or pink, collected in apical, less often axillary, dense umbellate inflorescences. The calyx and pedicels are bright red. The fruit consists of two juicy red drupes (Fig. 10.31).

Rice. 10.31. Rauwolfia snake -Rauwolfia serpentina Benth.

Spreading. Naturally occurs in India, Thailand, Burma, Sri Lanka and Indonesia. Cultivated in India. Raw materials are currently being imported to Russia.

Habitat. Grows on the edges of tropical rainforests.

Blank. In places of natural growth, the roots are harvested in the fruiting phase in plants with a well-developed root system. On plantations in India, roots are dug up in the third or fourth year of the plant's life.

External signs. Pieces of roots, cylindrical or split longitudinally, covered with brown cork. The outer surface is longitudinally wrinkled. The break is even. Yellow wood is visible on the break. The bark is not wide, but alkaloids are localized in it, therefore the presence of pieces of roots with exfoliated bark is a defect in raw materials. The smell is characteristic, unpleasant. Taste is not determined (!).

Microscopy. The cork has a characteristic layering - layers of larger and smaller cells alternate. The phloem contains single secretory cells with brown resinous contents. In the cells of the parenchyma, starch grains are quite often found, less often - prismatic crystals of calcium oxalate. The bark lacks mechanical elements (unlike the roots of other rauwolfia species).

Chemical composition. The roots contain a total of 1–2% of indole alkaloids. Currently, more than 50 alkaloids have been isolated (reserpine, aymaline, serpentine, rescinamine, yohimbine, etc.).

Storage. The raw materials are stored according to the B.

Medicines.

1. Raunatin, po tablets 0.002 g each (the sum of alkaloids). Antihypertensive, antiarrhythmic, sedative.

2. Reserpine, tablets of 0.0001 and 0.00025 g. Antihypertensive, sedative.

3. Aymalin, tablets of 0.05 g; solution for injection 2.5%. Antiarrhythmic agent.

4. Reserpine is a part of complex preparations ("Brinerdin", "Trirezid K", "Adelfan-Ezidreks", "Kristepin", etc.).

Pharmacotherapeutic group. Antihypertensive, sedative, antiarrhythmic agent.

Pharmacological properties. Rauwolfia alkaloids have various pharmacological properties. They mainly affect the central nervous system, reserpine and, to a lesser extent, rescinamine have a sedative and hypotensive effect, yohimbine - alpha-adrenergic blocking, aymalin - antiarrhythmic action. The main pharmacological property of reserpine is its sympatholytic effect due to the depletion of norepinephrine resources in adrenergic nerve endings. Reserpine has a complex effect on the body. Its antihypertensive effect is largely associated with the effect on the peripheral nervous system, and neuroleptic effect on the central neurochemical processes. Under the influence of reserpine, systolic and diastolic pressure gradually decreases with different forms and stages of hypertension. The best effect is observed on early stages hypertension, in the absence of pronounced organic changes in the cardiovascular system. The antihypertensive effect persists for a relatively long time after discontinuation of reserpine. Along with a decrease in blood pressure, renal function improves: renal blood flow increases, glomerular filtration increases. There is evidence of positive impact reserpine on lipid and protein metabolism in patients with essential hypertension and coronary atherosclerosis. Aimaline has no neuroleptic activity, moderately lowers blood pressure. Characteristic feature aymaline are antiarrhythmic properties.

Application. The raw materials are used to obtain the preparations "Reserpine", "Aimalin", which are pure alkaloids, and the total preparation "Raunatin". "Reserpine" is used to lower blood pressure in hypertension and mental disorders. "Raunatin" has a milder hypotensive and sedative effect, it also has antiarrhythmic and antispasmodic properties. "Aymalin" is an effective remedy for the relief of atrial fibrillation attacks. Reserpine is part of a number of combined medicines used for hypertension.

Other types. Rauwolfia vomitoria Afz., Which grows in tropical Africa from the west coast to Mozambique, r. four-leafed (r. grayish) (R. tetraphylla L. = R. canescens L.), widespread in South America, India, Australia, as well as p. kaffra (R. caffra Soud.), growing in Africa. The first two types are promising for introduction into industrial culture in the Transcaucasus. At the St. Petersburg Chemical-Pharmaceutical Academy, a microcloning technology has been proposed for their breeding, and a method for obtaining biomass of a tissue culture, which is a source of aymaline, has been developed and implemented.

Stage I - the formation of sclerotium - the resting stage of the fungus. Sclerotia ("horns") develop in rye flowers as a result of the proliferation and dense interlacing of mycelium hyphae, they are oblong solid formations of black-purple color 1-3 cm long. Sclerotia fall from mature ears of rye or end up on the ground with grain. They tolerate frost well and begin to sprout next year in the spring.

Stage II - the so-called stroma appear on the germinating sclerotia, consisting of a thin stem and a spherical reddish-purple head, seated with numerous small conical protrusions - the outlets of the fruit bodies (perithecia) - ovoid cavities that form in the peripheral part of the head. In the perithecia, numerous clavate bags (asci) develop, each of which develops 8 filamentous ascospores. By the time the rye blooms, the fruiting bodies of the fungus fully ripen, bags are squeezed out of the mucous swelling stroma, which burst, ascospores are thrown out of the perithecia and are carried by air currents through the flowering rye.

Stage III begins with the ingress of ascospores on the feathery stigmas of rye flowers and their germination. From the plexus of hyphae on the ovary of a flower, a mycelium (mycelium) is formed, as it develops, asexual reproduction of the fungus begins. It consists in the formation of hyphae-conidiophores, separating unicellular colorless conidiospores, at the same time a sticky sugary liquid called "honeydew" is released. Drops of "honeydew" run down the affected ear, taking the conidiospores with them. The sweet liquid attracts insects, which, flying to other ears, carry conidiospores, thereby contributing to a new infection of rye. Conidiospores, once on healthy rye flowers, also germinate, forming a mycelium on the ovary. Gradually, the mycelium of the fungus, growing, destroys the ovary, and instead of grain, a white oblong large mushroom body develops - a young sclerotium. By the time rye ripens, sclerotia also ripens; the hyphae become denser, while the outer layer of the sclerotia is pigmented, turning into a dark purple color. With a strong defeat of rye on individual ears, there can be up to 3-4 sclerotia (Fig. 10.30). Further, when harvesting bread, sclerotia spontaneously fall to the ground or, during threshing, fall into marketable or seed grain.

Rice. 10.30. Ergot - Claviceps purpurea (Fries) Tulasne:

1 - ear of rye with sclerotia; 2 - germinated sclerotium with stroma; 3 - the head of the stroma; 4 - perithecium with asci.

Spreading. Ergot in Russia is found in all natural areas apart from deserts and tundra, its range is associated with the area of rye cultivation.

Habitat. Areas with high relative humidity and moderately warm weather during the flowering period of rye are most favorable for the development of ergot. The optimum temperature for the growth and development of ergot is 24 ºС.

Blank. For the uninterrupted satisfaction of the needs of the pharmaceutical industry in this type of raw material, ergot has been introduced into the culture. Ergot production in specialized farms consists of several stages: 1) harvesting ergot horns, 2) obtaining infectious material, 3) rye contamination. Infection is carried out using special machines at the beginning of earing of rye with an infectious material grown on artificial media containing ergot conidiospores. Sclerotia are harvested as they mature using special machines.

The possibility of artificial cultivation of ergot made it possible to obtain sclerotia with an increased content of alkaloids, as well as to carry out breeding work aimed at obtaining strains of the fungus that produce a certain set of alkaloids. Currently, there are four strains of ergot: ergotamine, ergotoxin, ergocriptine and ergometrine. The first two strains have been introduced into production. The industrial saprophytic culture of ergot has been developed abroad.

^ Drying. Sclerotia are dried in dryers at a temperature of 40 ºС. Higher temperatures lead to decomposition of alkaloids.

Standardization. FS 42-1432-80 ("horns" of the ergot ergotamine strain); VFS 42-458-75 ("horns" of ergot ergotoxin strain).

^ External signs. "Horns" are oblong, almost triangular, somewhat curved, tapering towards both ends, usually with three longitudinal grooves. Length 5-30 mm, width 3-5 mm, the outside color is black or brown-violet, sometimes grayish, with a washable bloom. "Horns" are brittle, the fracture is even, whitish, along the periphery with a narrow brownish-violet border. The smell is weak, peculiar. Taste is not determined (!).

Microscopy. On the transverse section of the sclerotia, a brownish-violet border along the edge and a light uniform small-cell structure of the main part of the sclerotia are visible. The dark border (the pigmented part of the sclerotia) consists of two layers: the outer, in places exfoliating, from several rows of hyphae with brownish walls, and the inner, forming a continuous ring and consisting of several rows of strongly compressed hyphae with thick brownish-purple walls. The rest of the sclerotium consists of narrow intertwined hyphae, which have a round, polygonal or oval shape (pseudoparenchyma) in cross-section. Drops of fatty oil are visible in the preparation. When the section is processed with a solution of chlorine-zinc-iodine, the walls of the hyphae are painted in a light yellow color (chitin).

^ Chemical composition. Sclerotia contain alkaloids - derivatives of indole, which can be divided into two groups: derivatives of lysergic acid and alkaloids of the clavine series (penniclavine). The first group is represented by 7 pairs of stereoisomeric compounds. The levogyrate isomers have high biological activity, while the dextrorotatory isomers are not very active. Alkaloids - derivatives of lysergic acid - are divided into 4 types: peptide alkaloids (group of ergotamine, ergotoxine, etc.), alkaloids of the alkanolamide type (ergometrine and ergometrinine), amide-type alkaloids (ergine and erginine), alkaloids of the acid type (carbinol alpha-Lysergic methylcarbinolamide). The total of alkaloids in the raw material of the ergotamine strain contains about 70% of ergotamine, of the ergotoxin strain - about 70% of ergotoxine, the ergocriptine strain - about 80% of ergocriptine, the ergometrine strain contains only ergometrine and ergometrinine. In addition to alkaloids, sclerotia contain free amines and amino acids, up to 35% fatty oil, lactic acid, sugars, pigments.

Storage. During storage, ergot "horns" are often damaged by barn pests (mites, grain moth caterpillars, grain grinder larvae), so they must be stored in a dry, pre-disinfected room (list B). Shelf life 2 years.

^ Medicines.

Ergotal, tablets of 0.0005 and 0.001 g; solution for injection 0.05% (mixture of phosphates of alkaloids). Uterotonic agent.
Ergotamine tartrate, pills 0.001 g each; injection solution 0.05%; oral solution 0.1%. Uterotonic agent.
Ergometrine maleate, tablets of 0.0002 g; solution for injection 0.02%. Uterotonic agent.
Methyl ergometrine hydrotartrate tablets 0.000125 g each; solution for injection 0.02%. Uterotonic agent.
Ergotamine tartrate is a part of combined drugs ("Kofetamin", "Bellataminal", "Bellaspon"), ergotoxin is part of the complex drug "Belloid".
Parlodel (Bromocriptine), tablets, 0.0025 g; capsules of 0.005 and 0.01 g (semi-synthetic ergocriptine derivative). Dopaminomimetic agent.
Dihydrogenated derivatives of peptide alkaloids are used for the production of drugs alpha-adrenergic blocking action ("Vasobral", "Dihydroergocristine mesylate", "Redergin", etc.).

^ Alpha-adrenergic blocking, uterotonic, antispasmodic, sedative.

Pharmacological properties. Ergot alkaloids have a complex effect on the body. One of the characteristic pharmacological features is their ability to cause contraction of the uterus (especially pronounced in ergotamine and ergometrine), another feature of ergot alkaloids (especially their dihydrogenated forms) - alpha-adrenoceptor blocking activity, allowing their use in cardiovascular diseases. Currently, about 30 preparations based on ergot alkaloids are known in the world practice.

Poisoning with ergot alkaloids (ergotism), which occurs when eating contaminated rye bread, proceeds in a convulsive form or in the form of gangrene of the extremities due to irreversible narrowing of the capillaries.

Application. Earlier, ergot preparations were used only in obstetric and gynecological practice to enhance uterine contractions and stop uterine bleeding. Currently, the range of application of ergot alkaloids has expanded significantly.

From the ergotoxin strain, the drug "Ergotal" is produced, which is the sum of the phosphates of alkaloids; uterine bleeding... Ergotamine tartrate and ergotoxin, together with belladonna alkaloids, are part of a number of complex preparations used as antispasmodic, sedatives for hyperexcitability, insomnia, climacteric neuroses, neurodermatitis, vegetative dystonia. "Kofetamine" containing ergotamine tartrate and caffeine is used for migraine, arterial hypotension.

The water-soluble alkaloid ergometrine has a stronger and faster stimulating effect on the muscles of the uterus than other ergot alkaloids, and is more often used in obstetric and gynecological practice. From the ergometrine strain, the preparations "Ergometrine maleate" and "Methylergometrine hydrotartrate" are obtained. The alkaloid ergocriptine is obtained from the ergocriptine strain, which is used in the production of the semi-synthetic drug "Parlodel", which suppresses the secretion of prolactin. It is used for breast tumors.

Dihydrogenated ergot alkaloids are widely used for the production of drugs alpha-adrenergic blocking action, used to treat cardiovascular diseases.

Clavine alkaloids are not yet used in medical practice.

^ Numerical indicators. Humidity no more than 8%; total ash no more than 5%; broken "horns" no more than 30%, damaged by insects - no more than 1%; organic impurity no more than 3%; mineral impurity no more than 1%. The content of the sum of alkaloids for the "horns" of the ergotamine strain in terms of the ergotamine base is not less than 0.3%; the ergotamine content is not less than 0.2%. The content of the sum of alkaloids for the "horns" of the ergotoxin strain in terms of the ergotoxin base is not less than 0.4%; the ergotoxin content is not less than 0.25%. The alkaloids content is determined colorimetrically.

^ ROOWOLFIA ROOT SNAKE - RADICES RAUWOLFIAE SERPENTINAE

Rauwolfia snake -Rauwolfia serpentina Benth.

Sem. kutrovye - Apocynaceae

Rice. 10.31. Rauwolfia snake -Rauwolfia serpentina Benth.

Spreading. Naturally occurs in India, Thailand, Burma, Sri Lanka and Indonesia. Cultivated in India. Raw materials are currently being imported to Russia.

Habitat. Grows on the edges of tropical rainforests.

^ External signs. Pieces of roots, cylindrical or split longitudinally, covered with brown cork. The outer surface is longitudinally wrinkled. The break is even. Yellow wood is visible on the break. The bark is not wide, but alkaloids are localized in it, therefore the presence of pieces of roots with exfoliated bark is a defect in raw materials. The smell is characteristic, unpleasant. Taste is not determined (!).

^ Chemical composition. The roots contain a total of 1–2% of indole alkaloids. Currently, more than 50 alkaloids have been isolated (reserpine, aymaline, serpentine, rescinamine, yohimbine, etc.).

Storage. The raw materials are stored according to the B.

Medicines.

1. Raunatin, po tablets 0.002 g each (the sum of alkaloids). Antihypertensive, antiarrhythmic, sedative.

2. Reserpine, tablets of 0.0001 and 0.00025 g. Antihypertensive, sedative.

3. Aymalin, tablets of 0.05 g; solution for injection 2.5%. Antiarrhythmic agent.

4. Reserpine is a part of complex preparations ("Brinerdin", "Trirezid K", "Adelfan-Ezidreks", "Kristepin", etc.).

^ Pharmacotherapeutic group. Antihypertensive, sedative, antiarrhythmic agent.

Pharmacological properties. Rauwolfia alkaloids have various pharmacological properties. They mainly affect the central nervous system, reserpine and, to a lesser extent, rescinamine have a sedative and hypotensive effect, yohimbine - alpha-adrenergic blocking, aymalin - antiarrhythmic action. The main pharmacological property of reserpine is its sympatholytic effect due to the depletion of norepinephrine resources in adrenergic nerve endings. Reserpine has a complex effect on the body. Its antihypertensive effect is largely associated with the effect on the peripheral nervous system, and neuroleptic effect on the central neurochemical processes. Under the influence of reserpine, systolic and diastolic pressure gradually decreases in different forms and stages of hypertension. The best effect is observed in the early stages of hypertension, in the absence of pronounced organic changes in the cardiovascular system. The antihypertensive effect persists for a relatively long time after discontinuation of reserpine. Along with a decrease in blood pressure, renal function improves: renal blood flow increases, glomerular filtration increases. There is evidence of a positive effect of reserpine on lipid and protein metabolism in patients with essential hypertension and coronary atherosclerosis. Aimaline has no neuroleptic activity, moderately lowers blood pressure. Aymaline is characterized by its antiarrhythmic properties.

^ Other types. Rauwolfia vomitoria Afz., Which grows in tropical Africa from the west coast to Mozambique, r. four-leafed (r. grayish) (R. tetraphylla L. = R. canescens L.), widespread in South America, India, Australia, as well as r. kaffra (R. caffra Soud.), growing in Africa. The first two types are promising for introduction into industrial culture in the Transcaucasus. At the St. Petersburg Chemical-Pharmaceutical Academy, a microcloning technology has been proposed for their breeding, and a method for obtaining biomass of a tissue culture, which is a source of aymaline, has been developed and implemented.

^ LEAVES OF PINK CATARANTUS - FOLIA CATHARANTHI ROSEI

Catharanthus pink (periwinkle pink) - Catharanthus roseus (L.) G. Don f. (= Vinca rosea L.)

Sem. kutrovye - Apocynaceae

Other names: pervinkle, lochner pink

Botanical characteristics. Tropical evergreen subshrub 30-60 cm high. The stem is almost cylindrical, more often glabrous, highly branched (up to 65 shoots are formed in adult plants). Leaves are opposite, short-petiolate, whole-edged, elliptical or oblong-elliptical with a wedge-shaped base; the venation is pinnate, the central vein protrudes from the lower side. The leaves are up to 8 cm long, up to 3.5 cm wide, they are leathery, shiny, dark green, sometimes pubescent on the underside. The flowers are regular, five-membered, with a double perianth, arranged in pairs in the leaf axils. The cup is small, five-part. Corolla spine-petal, with a long tube and a wide five-part limb, raspberry pink, pink or white... The fruit is a crescent-shaped, dark brown, two-leafed plant with numerous seeds (Fig. 10.32).

Rice. 10.32. Catharanthus pink -Catharanthus roseus (L.) G. Don f.

Spreading. The homeland of the catharanthus is about. Java.

Habitat. Cultivated as an annual crop. Industrial production of raw materials is established in the zone of semi-humid-subtropical climate (Georgia); in the Kuban-Priazovsky district Krasnodar Territory(Russia), in the zone of moderate continental climate, as well as in the zone of arid climate in the Chimkent region (Kazakhstan).

Blank. Plants are mowed in the phase of mass flowering or the beginning of fruiting at a height of 10-15 cm from the soil surface.

Drying. In the air in the shade or in dryers at a temperature of 40-50 ºС. After drying, the leaves are threshed to separate and remove the stems.

Standardization. VFS 42-1106-81.

External signs. Broken, rarely whole leaves with small amount other parts of the plant (leafy tops of stems with buds, flowers or unripe fruits, pieces of thin stems, flowers and unripe fruits). Leaves are short-petiolate, elliptical or oblong-elliptical with a wedge-shaped base, whole-edged, slightly longitudinally wrinkled, with pinnate venation and a central vein protruding from the lower side. The stem is round or flattened, up to 0.2 cm thick, with two pairs of weakly protruding ribs. The flowers are regular, five-membered, tubular-funnel-shaped; the corolla tube is 8-10 times longer than the calyx. Fruits are long leaflets with numerous oval pitted seeds. The color of the leaves is dark green, the stems are yellowish-green with a purple tint, the flowers are yellowish or pale lilac, the fruits are brownish-green, the mature seeds are black, the unripe seeds are greenish-brown, brown. The smell is peculiar, unpleasant. Taste is not determined (!).

Microscopy. When examining the leaf from the surface, small polygonal, predominantly erect-walled epidermal cells, oval or almost rounded stomata, often in pairs approaching, surrounded by 3-5 epidermal cells (anomocytic type), and 1-4-cell simple hairs are visible. Single small prismatic crystals of calcium oxalate are sometimes seen along the veins in the parenchyma. On the underside of the leaf, stomata and hairs are more numerous.

^ Chemical composition. About 80 indole alkaloids were isolated from the aerial part of pink catharanthus, of which 26 are dimers. Among the latter, alkaloids with antitumor activity were found; vinblastine, vincristine, and leurosine are of particular interest. The content of these alkaloids in the leaves is very low: vinblastine is about 0.005%, vincristine is 0.001%.

Storage. Raw materials are stored according to list B, in a cool, dark place. Expiration date 1 year.

Medicines.

1. Vinblastine (Rosevin), lyophilized powder for injection, 0.005 g (available as sulfate). Cytostatic agent.

2. Vincristine, lyophilized powder for injection, 0.0005 g each (available as sulfate). Cytostatic agent.

^ Pharmacotherapeutic group. Cytostatic, antineoplastic agent.

Pharmacological properties. Catharanthus pink is of great interest for medicine in connection with the antitumor activity noted both in the herbal preparations of the plant and in the isolated alkaloids isolated from the plant. The most active alkaloids in this respect are vinblastine and vincristine. They have antitumor cytostatic activity, block cell mitosis at the metaphase stage, suppress the multiplication of tumor cells and lymphocytes, and to a lesser extent affect erythropoiesis. By the nature of the action, vinblastine is close to colchicine, although it has a completely different chemical structure from colchicine. There is evidence that vincristine stimulates adrenal function and increases corticosterone production. This plays a role in its antitumor action, increases antitumor immunity.

Application. Vinblastine is prescribed for generalized forms of lymphogranulomatosis, lymph and hematosarcomas and other tumor diseases. Vincristine is similar in chemical structure and mechanism of action to vinblastine. It is used in the complex therapy of acute leukemia, neuroblastoma, melanoma, breast cancer and other malignant tumors. Semi-synthetic derivatives are obtained on the basis of vinblastine, which are also used as antitumor agents.

^ Numerical indicators. The content of vinblastine, determined photocolorimetrically, is not less than 0.02%; humidity not more than 14%; total ash no more than 13%; leaves that have changed their natural color (yellowed, brownish, blackened), no more than 6%; stems no more than 15%; organic impurity no more than 1%; mineral impurity no more than 1%.

^ GRASS BARVINKA SMALL - NERVE VINCAE MINORIS

Small periwinkle - Vinca minor L.

Sem. kutrovye - Arosupaseae

Other names: brilliant green, hornbeam grass, burial ground

Botanical characteristics. Evergreen shrub 20-35 cm high with a thin horizontal rhizome. It has two types of shoots: vertically located generative and vegetative creeping shoots. Leaves are opposite, short-petiolate, oblong-elliptical, leathery. The flowers are axillary, five-membered, with a double perianth, solitary, blue, with long pedicels. The corolla is funnel-shaped, dark blue. The fruit is a two-leafed plant with small seeds (Fig. 10.33). Blooms from April to September. Fruits are rare. Propagated by vegetative shoots.

Rice. 10.33. Small periwinkle - Vinca minor L.

Spreading. Ukraine, Belarus, Moldova, North Caucasus. The main procurement areas are Moldova and the south of Ukraine (Carpathian, Transcarpathian, Khmelnytsky and Vinnitsa regions).

Habitat. In hornbeam, oak-hornbeam, oak forests and among thickets of bushes.

Blank. The grass is harvested in spring and early summer (until July) in the flowering - fruiting phase, cutting off at a height of 3-5 cm from the soil surface. Then it is cleaned of impurities and delivered to the drying site.

^ Security measures. Do not pull out rooted vegetative shoots and uproot plants, as this leads to the destruction of thickets. Harvesting in one place can be carried out no more than 1 time in 3 years.

Drying. Airy under awnings, in attics with good ventilation or in dryers at a temperature of 40-50 ° C, spreading in a thin layer (3-5 cm). It is better to lay out the grass on a stretched mesh, gauze. In good weather, the raw material dries up in 5-7 days.

Standardization. VFS 42-1728-87.

External signs. The raw material is represented by aerial shoots with flowers and leaves. Stems glabrous, cylindrical, up to 30 cm long. Leaves are oblong-elliptical, short-petiolate, with a whole edge slightly curved on the underside, shiny, leathery. There is a slight pubescence on the upper side of the leaf along the petiole. Flowers are single. The calyx is 2.5 times shorter than the corolla tube, with 5 lanceolate teeth. The corolla is dark blue, tubular-funnel-shaped with inverse triangular bend lobes. The color of the leaves is dark green above, lighter below. The stems are light green. There is no smell. Taste is not determined (!).

Impurities. Other types of periwinkle are not allowed for harvesting, which have the following distinctive features: herbaceous periwinkle (Vinca herbacea W. et L.) - rounded ovoid leaves, thin, falling for the winter, purple corolla; periwinkle large (Vinca major L.) - leaves are ovoid, heart-shaped at the base, hibernating, azure corolla.

Microscopy. Cells of the upper and lower epidermis with sinuous, partly clearly thickened walls. The stomata of the paracytic type are located only on the underside of the leaf. Along the main vein on the upper side of the leaf, there are single-celled thick-walled pointed hairs and small papillae along the edge of the leaf. The leaves contain numerous straight, unsegmented lactates with greenish-yellow contents. Multicellular glands are visible on the petiole.

^ Chemical composition. The herb of periwinkle minor contains about 20 alkaloids - indole derivatives, their total amount is about 2% (vincamine, isovincamine, reserpine, isoaymaline, akuammycin, vincaminorine, minorin, etc.). The herb also contains triterpene saponins, flavonoids (rutin, robinin), carotenoids (8 mg%), tannins.

Storage. In dry, well-ventilated rooms on racks, according to list B. Shelf life 4 years.

Medicines.

1. Vinkanor, po tablets 0.02 g each (purified amount of alkaloids hydrochlorides). Antispasmodic, vasodilator, hypotensive, sedative.

2. Vinpocetine (Cavinton), tablets of 0.005 g; solution for injection 0.5% (ethyl ester of apovincamine acid - a semi-synthetic derivative of the alkaloid vincamine). An agent that improves cerebral circulation and oxygen supply to the brain.

^ Pharmacotherapeutic group. Vasodilator, antihypertensive, sedative.

Pharmacological properties. Herbal preparations from the herb of periwinkle and the amount of alkaloids have vasodilating, hypotensive and mild sedative properties. They dilate mainly the vessels of the brain, increase cerebral blood flow, improving the supply of oxygen to the brain; increase urine output; improve the functional state of the myocardium; normalize blood clotting indicators, increase the anticoagulant activity of plasma, strengthen the walls of the capillaries. Among the alkaloids of vinca minor, alkaloids with antiarrhythmic activity similar to the action of aymaline were found. Vinca minor alkaloids selectively act on cerebral circulation, relieving arterial spasm and increasing venous tone, and reducing the ischemic zone in cerebral strokes. The alkaloid vincamine moderately lowers blood pressure and has sedative properties. The mechanism of hypotensive action is based on the ability to reduce vascular tone and resistance of peripheral vessels, to expand the vessels of the brain.

Application. Small periwinkle has been used for a long time, it was known to Pliny and Dioscorides. In the Middle Ages, it was considered valuable medicinal plant... Periwinkle preparations are used for hypertension of I and II stages. They are most effective in cerebral forms of hypertension, in ischemic disorders of cerebral circulation, diencephalic syndromes. Vinca preparations are used for headaches of various origins: with organic lesions of cerebral vessels, atherosclerosis, hypertension, ischemia, with vasomotor, autonomic and diencephalic pathology, with increased intracranial pressure, with osteochondrosis.

^ Numerical indicators. The content of the sum of alkaloids, determined titrimetrically in terms of vincamine hydrochloride, is not less than 0.4%; humidity not more than 14%; total ash no more than 10%; blackened leaves no more than 2%; organic impurity no more than 5%; mineral impurity no more than 1%.

^ HERBA PASSIFLORAE - HERBA PASSIFLORAE

Passionflower (passionflower) incarnate - Passiflora incarnata L.

Sem. passionflower (passionflower) - Passifloraceae

Other names: incarnate passionflower, incarnate passionflower, cavalier star

^ Botanical characteristics. Perennial herbaceous tropical liana, reaching 6-9 m in length in the humid subtropics of Georgia. The stem is climbing, glabrous, rounded. Leaves are alternate, long-petiolate, leathery, green above, grayish below, tripartite, up to 20 cm long and wide. The lobes are elliptical with a pointed apex and a finely serrated edge. Antennae develop in the leaf axils. Flowers on long pedicels are located singly in the leaf axils, large (7-9 cm in diameter), regular, five-membered, with a double perianth. Sepals are lanceolate, leathery, bearing spiny outgrowths at the apex. The corolla consists of almost free petals and a "crown" (two rings of threadlike fringes) of bright purple color. The fruit is an edible, juicy berry of yellow-orange color with black seeds (Figure 10.34).

Rice. 10.34. Incarnate Passiflora - Passiflora incarnata L.