The chemical composition of traditional Chinese medicine is extremely complex, and some components are common in general higher plants, such as sugars, oils, lipids, waxes, acids, proteins, amino acids, vitamins, pigments, resins, inorganic salts, etc; . Each traditional Chinese medicine often contains a variety of chemical components, but not all chemical components can produce the effect of disease prevention and treatment. The chemical components contained in traditional Chinese medicine are usually divided into effective components and ineffective components. The so-called effective ingredients refer to substances with medical effects or biological activities, such as ephedrine, berberine, baicalein, menthol, etc. The effective components can be expressed by a certain molecular formula or structural formula, and have a certain melting point, boiling point, optical rotation, solubility and other physical and chemical constants, so they are also called effective monomers. . The so-called ineffective ingredients refer to other chemical ingredients coexisting with effective ingredients, which usually have no (or have not been found to have) biological activity and medical effects, such as sugars, acids, oils, proteins, resins, pigments, inorganic salts, etc. However, the division of effective ingredients and ineffective ingredients is not absolute. Many ingredients that were considered ineffective in the past were found to be effective ingredients with the progress of medical practice and traditional Chinese medicine research.
The chemical components (effective components) contained in traditional Chinese medicine have certain pharmacological effects. A traditional Chinese medicine often contains multiple ingredients. Different effective ingredients often have different pharmacological effects, but some different effective ingredients have similar effects. There are many kinds of effective ingredients in Yiwei traditional Chinese medicine, and they can interact with each other, such as synergy, restriction, antagonism, etc. In the compound prescription, the chemical composition and pharmacological effects of traditional Chinese medicine may also change. Therefore, the chemical components and pharmacological effects of traditional Chinese medicine must not be understood and studied in isolation.
Now the main chemical components and pharmacological effects of plant traditional Chinese medicine are briefly introduced as follows.The chemical components (effective components) contained in traditional Chinese medicine have certain pharmacological effects. A traditional Chinese medicine often contains multiple ingredients. Different effective ingredients often have different pharmacological effects, but some different effective ingredients have similar effects. There are many kinds of effective ingredients in Yiwei traditional Chinese medicine, and they can interact with each other, such as synergy, restriction, antagonism, etc. In the compound prescription, the chemical composition and pharmacological effects of traditional Chinese medicine may also change. Therefore, the chemical components and pharmacological effects of traditional Chinese medicine must not be understood and studied in isolation.
1、
Alkaloids are a class of nitrogen-containing organic compounds that can combine with acids to form salts. . Alkaloids have optical activity, strong or special physiological effects. They widely exist in the biological Kingdom (mainly the plant kingdom) and have a wide variety. At present, thousands of alkaloid structures have been clarified. Alkaloids with similar chemical structures are often related not only in families and genera, but also in pharmacological effects.
1) , hydrocarbon amine derivative alkaloids
1. phenylethylamines
Phenylethylamines mainly include epinephrine, ephedrine and cactus alkaloids.
Adrenergic alkaloids are derived from tyrosine in amino acids of protein degraders, which can be converted into neurotransmitters such as dopamine and norepinephrine by dopa in animal neural tissues, and further converted into epinephrine in adrenal medulla. Although epinephrine has not been found in the plant kingdom, other derivatives or intermediates exist widely. For example, the seeds of Lathyrus, such as evergreen oil and rattan, contain dopa. The extracted products can be used as dopamine precursors to treat tremor paralysis caused by dopamine deficiency. In addition to a small amount of dopa, purslane whole herb also contains dopamine and norepinephrine, so intramuscular or intrauterine injection can constrict blood vessels and uterus for hemostasis of postpartum hemorrhage. . Fructus aurantii Immaturus contains synephrine and N-methyl tyramine, which can constrict blood vessels, increase blood pressure and strengthen heart.
Ephedrine is mainly found in the pith of Ephedra stems and branches, with the highest content in autumn, and it also exists in other plants, such as berry yew, rhodomyrrhiza cordata, Aconitum carmichaeli, spotted Asian poppy, etc. Ephedra mainly contains l-ephedrine, followed by d-pseudoephedrine.
The pharmacological action of phenylethylamine alkaloids is mainly to directly or indirectly act on the adrenergic receptors of adrenergic nerve terminal effectors to produce various physiological effects of sympathetic nerve excitation, such as skin and mucosal vasoconstriction and pressor effect, which are used for some bleeding, nasal mucosal swelling, allergic shock; Exciting cardiac action, for cardiac arrest; .
2. quaternary ammonium hydrocarbon
Quaternary ammonium hydrocarbons mainly exist in the biological world as choline and its derivatives. Acetylcholine is often formed in animals and plays an important role as a neurotransmitter; In plants, betaine is finally formed. Astragalus membranaceus, Lycium barbarum, Herba Artemisiae Scopariae, Herba Lysimachiae, Herba agrimoniae, Herba Polygonati, shepherd's purse, Poria cocos and other Chinese herbal medicines contain these alkaloids. Betaine can participate in the metabolism of fat supplying methyl groups, while choline can form soluble lecithin with fatty acids and phosphoric acids to participate in fat transport. Therefore, both of them belong to lipotropic drugs to prevent and treat fatty liver and atherosclerosis caused by fat deposition in the vascular wall. In addition, muscarine contained in fly catching mushrooms has a structure similar to acetylcholine, which is more stable than acetylcholine and is not easy to be destroyed. It can produce symptoms such as vomiting, abdominal pain, diarrhea, salivation, miosis, circulatory depression, which are similar to parasympathetic excitation of acetylcholine, and can be antagonized and detoxified with atropine.
3. colchicines
. Colchicines are plant hormones that inhibit the mitosis of plant cells; Clinically, it can significantly inhibit the division of animal cancer cells, and can be used in skin cancer and leukemia, but it also has a greater inhibition of hematopoietic system and gastrointestinal toxicity. In addition, small doses of colchicine can promote the release of corticosteroids, have anti-inflammatory effects, and can be used to relieve acute gout.
4. other hydrocarbon amines
(1) Amidoalkalines
The fruits of Capsicum in Solanaceae, Zanthoxylum in Rutaceae and Senecio in Compositae contain polyene amine alkaloids, which are spicy and locally irritating. Some can increase appetite. Taking large amounts of them orally often can promote the formation of gastric ulcer. Injection has the effect of pressor and Bronchoconstrictor. In addition, a class of diaminoamides, trischizocine and trischizocine, were found to have the effect of inhibiting tumor cell division from Solanaceae trischizocine plants. There are mainly capsaicin, Dihydrocapsaicin, nordihydrocapsaicin, and synthetic capsaicin.
(2) Guanidines
Motherwort alkaloid contained in Leonurus labiata and some plants of Leguminosae, such as swainsonine contained in swainsonine, belong to guanidine alkaloids, which have the effects of uterine contraction, sedation, hypotension and diuresis. The caprine contained in the seeds of leguminous goat beans has a relatively simple guanidinium hydrocarbon, which can reduce blood glucose.
2) , pyridine derivative alkaloids
Pyridine derivatives are widely distributed in the biological world, especially nicotinic acid, which exists in almost all biological cells and can be converted into nicotinamide, which can promote biological oxidation in tissue respiration. When animals lack it, it can cause leprosy, so it is also called vitamin PP, which belongs to B vitamins; Nicotinic acid can dilate peripheral blood vessels and reduce cholesterols in blood, which can be used for cardiovascular diseases. Chinese herbal medicine such as fermented soybean is rich in content.
When there is a heterocyclic substitution at the 3 position of the pyridine ring, the toxicity increases. For example, nicotine, resveratrol, and resveratrol have strong toxicity. They are mainly used to kill insects and treat ringworm. They can make the animal body ganglion, striated muscle, and central nervous system excited first and then paralyzed. Therefore, the star anise containing resveratrol has a rhabdomyorelaxant effect, and is used for traditional Chinese medicine anesthesia and muscle cramp pain. Apigenine has a similar piperidine ring, and it also has strong rhabdomyoparalysis toxicity. The oxidized isopomegranate peel base of the side chain can paralyze tapeworms, and has an anthelmintic effect. Genistein, which is found in the genera of Plantago, Chamaecrista, chickpea and sophora, has a prominent excitatory effect on the homologous organs of the ganglion, such as carotid body and adrenal medulla. The same effect is also found for Campanulaceae, so it is used for excitatory respiration. Matrine contained in Sophora flavescens, Sophora tonkinensis and cassia lanceolata has diuretic, pressor and other effects, and can inhibit the growth of tumor cells. Oxymatrine has the effect of increasing white blood cells.
Arecoline not only has the deworming effect similar to that of punicarpine paralyzing tapeworm, but also has the effect of exciting m-choline receptor, which can cause diarrhea, salivation, promote digestion, miosis, and hypotension. In addition, colchicine has the effect of improving the excitability of nerve cells, which is used in nerve palsy. Excess can cause central excitation and convulsion. Gentiana alkaloid a, also known as gentianin a, longcholine, has many central inhibitory effects, such as stability, cooling, analgesia, anticonvulsant, etc., in addition to muscle relaxant, hypotensive, anti-inflammatory and anti allergic effects.
3) , pyrrole derivative alkaloids
The alkaloids are divided into pyrrole derivatives and double fused pyrrolidine derivatives. Pyrrole derivatives, such as solanaceous anisodamine, belladonna, pseudophysalis and coca leaf, contain less direct effects of coca liquid alkali (coumarine) and coca leaf alkali (red coumarin), as well as water containing threonine in Leonurus labiata, which has a similar atropine like effect after being hemisynthesized into coca leaf alcohol bitter almond ester.
,Senecio base, Senecio phenanthroline, etc. have weak atropine like blocking effect on m-choline receptor to relax smooth muscle, relieve spasm and asthma, reduce secretion and dilate pupil, etc; Leguminosae, Pistacia, etcMonocrotaline, monocrotaline nitrogen oxide, meimeizhushidou, rufous Shidou, monocrotaline glandularis, and eupatorine, pilocarpine, Ranunculus sinapine, Senecio, Senecio, etc. in the Porphyra family, tianmustard, inverted teapot, and sargassum have weak atropine like effects, have certain toxicity to the liver, and inhibit the mitosis of hepatocytes, so they have different degrees of inhibitory effects on a variety of tumors, and are clinically used for the treatment of skin cancer.
4) , topiramate derivative alkaloids
This kind of alkaloid is an ester compound formed by the combination of troponin (hyoscyamol), scopolamine, 6-hydroxytroponin (anisodamine), torol, aikangning and other amino alcohols derived from troponin with troponin acid, benzoic acid, cinnamic acid or crotonic acid. The ester alkaloids of the first three amino alcohols are mainly found in the leaves, roots, stems, flowers, fruits, and seeds of many Solanaceae plants, also known as belladonna alkaloids, mainly including solanine, solamine, solanine, solanine, solanine, solanine, and so on; The benzoic acid or cinnamate alkaloids of iconin and methyl iconin are mainly found in the leaves of the coca family, also known as Coca alkaloids.
Belladonna alkaloids mainly block the m-choline receptor, making the neurotransmitter acetylcholine and cholinergic drugs unable to exert muscarinic effects, so they can relax smooth muscle, relieve gastrointestinal spasm, relax circular muscle and ciliary muscle, dilate pupil, paralyze crystal regulation, and inhibit gland secretion. In addition, atropine and hyoscyamine with tropine structure also have central excitatory effects such as activating the brain and medulla oblongata. Scopolamine and anisodine, which contain the structure of scone, also have sedative and anti syncope effects.
Coca alkaloids, mainly contained in coca leaves, can excite the center, enhance mental and physical activity, produce euphoria and other effects, and are addictive; Local effect, strong penetration, can paralyze sensory nerve endings, used for mucosal anesthesia.
5)
The alkaloids of common quinoline derivatives can be mainly divided into the following categories
1. cinchona alkaloids
More than 30 kinds of such alkaloids, such as quinine, quinidine, cinchonine, cinchonine, and kopling, exist in the bark of plants such as cinchona and Coprinus in Rubiaceae. Quinine and quinidine are common and important alkaloids in this class. They can kill Plasmodium in the inner phase of erythrocytes and control the onset of symptoms, but they cannot eliminate Plasmodium in the outer phase of erythrocytes, so they cannot prevent the recurrence of benign malaria. Quinine also has antipyretic and analgesic effects, excites the uterus, inhibits cardiac muscle and striated muscle, reduces its excitability, and has local anesthetic effects. Quinidine has a strong inhibitory effect on cardiac muscle and striated muscle. It is mainly used for tachycardia and striated muscle spasm.
2. Camptotheca alkaloids
For example, camptothecin, hydroxycamptothecin, methoxycamptothecin and deoxycamptothecin are found in Camptotheca acuminata, a plant of the purple tree family, while camptothecin and 9-methyl camptothecin are found in mahbi wood, a plant of the Oleaceae family. Camptothecins have anticancer effects. In addition, it has the effects of inhibiting herpesvirus, immunosuppression and anti early pregnancy.
3. ketoquinoline alkaloids
Bergamot alkaloid and echinophylline are found in the genus Bergamot of Rutaceae and echinophylline of Compositae, respectively. The former is an anticancer active ingredient discovered in recent years, which has broad-spectrum inhibitory effects on a variety of experimental tumors.
4. furaquinoline alkaloids
Dictamnine, γ - cryptophylline, colocasine, and acridium are found in plants of the genera dictamnine, Colocasia, Evodia, Zanthoxylum, and cryptophyllum in Rutaceae, which have sedative, cooling, and bacteriostatic effects.
5. hydroquinoline alkaloids
Lycopodine and extensin, which are found in Lycopodium of Lycopodiaceae, have the effects of spasmolysis, analgesia, and treatment of rheumatoid arthritis.
6) , isoquinoline derivative alkaloids
Isoquinoline alkaloids are a large group of alkaloids with the largest number and categories, and are also the most widely distributed. More than 500 species are known and can be divided into 20 categories; Most derivatives of tetrahydroisoquinoline are decarboxylated from tyrosine to phenylethylamine, and then cyclized to form.
1. simple Isoquinolines and tetrahydroisoquinolines
It is often found in cactus, Chenopodiaceae, Papaveraceae, Ranunculaceae and other plants. The pharmacological effects are mainly manifested in the central nervous system and peripheral smooth muscle. For example, pilocarpine has antihypertensive effects such as central sedation and vasosmooth muscle spasmolysis, and has an excitatory effect on the uterus.
2. Benzylisoquinolines and benzyl tetrahydroisoquinolines
There are more than 30 kinds of these two alkaloids, which are mainly distributed in the plants of tetrandriaceae, Magnoliaceae, Papaveraceae, Nymphaeaceae and Lauraceae. It mainly has the effects of smooth muscle spasmolysis, local anesthesia, sedation, bronchial dilation excited by β - adrenergic receptor and heart rate acceleration; Quaternary ammonium salts have curare like rhabdomyorelaxation.
3. morphine alkaloids
There are about 10 species, mainly divided into morphine and sinomenine. The former mainly exists in Papaveraceae; The latter is mainly distributed in plants such as tetrandriaceae. Morphine mainly acts on the central nervous system, with central effects such as analgesia, sedation, antitussive, inhibition of respiration and addiction, and central excitatory effects such as emesis, miosis, spinal cord excitation, while it has a spastic effect on gastrointestinal smooth muscle; Sinomenine has strong excitatory effect and mild analgesic and sedative effects, but its anti-inflammatory effect is obvious. Therefore, sinomenine, tetrandrine and tetrandrine, which contain such alkaloids, are mostly used to dispel rheumatism and relieve pain.
4. diparaisoquinolines and diparatetrahydroisoquinolines
More than 70 kinds of alkaloids are known, mainly distributed in Berberidaceae, tetrandridaceae, Papaveraceae, Annonaceae and Rutaceae. For example, both tetrahydropalmatine B and tetrahydropalmatine a can easily penetrate the blood-brain barrier and have obvious central inhibitory effects such as analgesia, stability, cooling and antiemesis; Berberine has antibacterial, anticancer and anti amoeba effects. It can improve the phagocytic capacity of white blood cells, maintain mild sedation, cooling and other central inhibitory effects. In addition, it can expand coronary blood vessels and has a transient hypotensive effect.
5. protoopioids
Nearly 20 species of this kind are known and mainly exist in Papaveraceae, Berberidaceae, Rutaceae and other plants. It is mainly divided into cryptopine, α - allocryptopine and protoopioid. The central sedative effect is weakened in turn, which can inhibit the myocardium, block atrioventricular conduction, slow down heart rate, dilate coronary vessels, and reduce blood pressure. In addition, it also has transient effects of exciting uterine smooth muscle and relaxing striated muscle.
6. benzophenanthridines
There are about 30 kinds of alkaloids in this class, mainly distributed in Papaveraceae, Rutaceae and other plants. It mainly has mild central inhibition, local anesthesia and analgesia, inhibits smooth muscle, relieves gastrointestinal and bronchial spasm, and some have bacteriostatic, nematicidal and anticancer effects.
7. there are more than 10 kinds of phthalyl isoquinoline alkaloids, which are mostly found in Papaveraceae, Berberidaceae and other plants. They have antitussive, analgesic, central excitation, uterine excitation, inhibition of gastrointestinal smooth muscle and cardiac muscle and other effects. Berberine, berberine hydrochloride, epiberberine, 13 methyl berberine, demethylene berberine, Dihydroberberine, tetrahydroberberine, berberine, berbamine and so on are alkaloids from Berberidaceae plants.
8. aporphines and pre aporphines
There are many alkaloids in this class, with more than 100 known species and a wide distribution. They often exist in Papaveraceae, Magnoliaceae, Nymphaeaceae, tetrandraceae, Berberidaceae, Ranunculaceae, Aristolochiaceae and Lauraceae plants. They have a variety of physiological activities, and have mild sedative, cough relieving and analgesic effects on the central nervous system, central emetic and expectorant effects; It has spasmolytic effect on smooth muscle. Some alkaloids have neurogenic blocking hypotension and mild curare like rhabdomyorelaxation. .
9. dibenzylisoquinolines and aporphine Benzylisoquinolines
The number of alkaloids in this category is the largest, reaching more than 700 species, which are mainly distributed in plants such as tetrandriaceae, Berberidaceae, Ranunculaceae, Nymphaeaceae, Magnoliaceae and lianyetongaceae. ; Tetrandrine can inhibit smooth muscle, anti-inflammatory, anti shock, analgesic, antipyretic and local anesthesia, and also inhibit amoeba and some bacteria. Some alkaloids can also significantly inhibit tumor, mildly block α - adrenoceptor and reduce blood pressure. The alkaloids in Coptis chinensis, a Ranunculaceae plant, mainly includeBerberine.
10. about 14 kinds of alkaloids of emetine are known, which mainly exist in plants such as Rubiaceae and Illicium. Emetine hydrochloride can inhibit the synthesis of nuclear proteins, inhibit a variety of protozoa, molds, bacteria and viruses, and inhibit tumor growth.
11. there are about 30 kinds of benzocyclopentadienyl isoquinoline alkaloids, which exist in Amaryllidaceae and momordiaceae plants. They are cytotoxic and can inhibit the growth of granulocytic leukocytes and spermatogonia, and have strong inhibitory effects on sarcoma S-37 and leukemia L-1210 in mice; It also has inhibitory effect on Amoeba protozoa; It can inhibit the heart, excite smooth muscle and uterus, and has anti-inflammatory, antipyretic, sedative and emetic effects.
12. there are more than 10 kinds of Erythrina alkaloids, which mainly exist in legumes, tetrandriaceae and other plants. They have a mild curare like effect to block the acetylcholine transmission of striated muscle endplate, and can relax striated muscle and relieve myofiber myotonic spasm.
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Classification and pharmacological effects of chemical constituents of traditional Chinese medicine (Ⅰ) -- alkaloids
Classification and pharmacological effects of chemical constituents of traditional Chinese medicine (Ⅱ) -- glycosides
Classification and pharmacological effects of chemical constituents of traditional Chinese medicine (Ⅲ) -- other categories.The first part of this paper is the introduction of the classification of chemical constituents of traditional Chinese medicine..the second part of this paper.The second part is the introduction of the classification of chemical constituents of traditional Chinese medicine and their pharmacological effects