garlic
1、 Pharmacopoeia standard of garlic       This product is the bulb of Allium sativum L., a lily plant. .
      [properties] the product is quasi spherical, with a diameter of 3-6cm. The surface is covered with white, lavender or purplish red membranous scales. The top is slightly pointed, with residual scape in the middle, and most fibrous root scars at the base. Peeling off the skin, you can see a single head or 6-16 petal shaped small bulbs, which are inserted around the base of the residual flower stem. The bulb petal is slightly ovoid, with a membranous outer skin, a slightly pointed apex, an arcuate bulge on one side, stripped of the membrane, white, fleshy. .
      [identification] take 6G of this product, mash it, keep it at 35 ℃ for 1 hour, add 20ml of absolute ethanol, heat and reflux for 1 hour, filter it, and take the filtrate as the test solution. In addition, take allicin reference substance and add absolute ethanol to make a solution containing 0.4mg per 1ml as the reference solution. According to the test of thin-layer chromatography (general rule 0502), suck 5 μ l of each of the above two solutions, respectively dot on the same silica gel G thin-layer plate, use n-hexane as the developing agent, develop, take out, dry, fumigate with iodine vapor until the spots are clear. In the chromatogram of the test sample, spots with the same color appear at the corresponding position of the chromatogram of the control sample.
      [inspection] the total ash content shall not exceed 2.0% (general rule 2302).
      [extract] measured by the hot leaching method under the determination method of water-soluble extract (general rule 2201), it shall not be less than 63.0%.
      [content determination] determine according to HPLC (general rule 0512).
      Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; ; The detection wavelength was 210nm. The number of theoretical plates should not be less than 3000 according to the allicin peak.
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      Preparation of test solution take about 2G of this product, mash it, accurately weigh it, place it in a corked conical flask, keep it warm in a 35 ℃ water bath for 1 hour, accurately add 20ml of absolute ethanol, weigh it, heat it and reflux for 1 hour, take it out, cool it, weigh it again, make up the lost weight with absolute ethanol, shake it well, filter it, and take the filtrate.
      The determination method is to precisely suck 10 μ l of the reference solution and 10 μ l of the test solution, inject them into the liquid chromatograph, and determine.
      The content of allicin (c6h10s3) in this product shall not be less than 0.15%.
      [nature, taste and meridian tropism] pungent, warm. Return to spleen, stomach and lung meridians.
      [functions and indications] detoxify and detumescence, kill insects and stop dysentery. For carbuncle, sore, scabies, tuberculosis, cough, diarrhea, dysentery.
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      [storage] store in a cool and dry place.


2、 Chemical constituents of garlic
The main chemical components of bulbs are as follows: 1. volatile components garlic oil contains a variety of sulfur-containing volatile compounds, including diallyltrisulfide, commonly known asAllicin（allitridin）， Diallylsulfide, methylallyldisulfide, diallyldisulfide, methylallyltrisulfide, diallyltrasulfide, trans - and CIS allionene, 2-vinyl-1,3-disulfide, 3-vinyl-1,2-disulfide- 5-cyclohexene (3-vinyl-5h-1, 2-dithiin), methylallylsrlfide, Dimethyltrisulfide, dimethyldisulfide, propylallyldisulfide, allylpropyltrisulfide, methylallylpentasulfide, 6-methyl-1-thia-2, 4-cyclohexadiene, 3-methyl-1,2-thia-3-cyclopentene, 3-methyl-1,2-thia-2, 4-cyclohexadiene, 3-methyl-1,2-thia-3-cyclopentene, 3-methyl-1,2-thia-3-cyclopentene, 3-methyl-1,2-thia-3-cyclopentene, 6-methyl-1-thia-2, 4-cyclohexadiene, 3-thia-1,2-thia-cyclopentene, 3-thia-1,2-thia-cyclopentene, 3-thia-1,2-thia-cyclop, 2-dithia-3-cyclopentene）， 4-vinyl-1,2,3-trithia-5-cyclohexene, 3-vinyl-1,2,3-dithia-4-cyclohexene, dipropenyldisulfi De, dithio- (propenyl) - propionate, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, and other compounds were synthesized...The main products of the study were as follows:the main products were as follows: 1.The main products were 4-vinyl-1,2,3-trithia-5-cyclohexene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyltetrahydrothiophene, 2-ethyl.
2. allicin, diallylthiosulfonate, 1-propenyllylthiosulfinate, allyl-1-propenylthiosulfonate, methylallylthiosulfinate, allylmethylthiosulfinate, allylmethylthiosulfinate, methyl-1-propenylthiosulfonate and dimethyl thiosulfinate lthiosulfinate), et al.
3. S-ALKYL (ene) - L-cysteine derivatives AlliinAlliin, s-ally-l-cysteinulfoxide, s-methylcysteinesulfoxide, cycloalliin, s-allyl-l-cysteine, s-propyl-l-cysteine, s-propyl-l-cysteine, s-propyl-l-cysteine, s-propyl-l-cysteine, s-butyl-l-cysteine,the, S-allymercapto-l-cystein and s-methylmercapto-l-cystein, etc.
4. γ - l-glutamyl-l-cysteine, γ - l-glutamyl-s-methyl-l-cysteine, γ - l-glutamyl-s-methyl-l-cysteine, γ - l-glutamyl-s-methyl-l-cysteine, γ - l-glutamyl-s-methyl-l-cysteine sulfoxide, γ - l-glutamyl-s-methyl-l-cysteisulfoxide, γ - l-glutamyl-s - (β - carboxy propyl) - L-cysteine aminoacylglycine [γ -l-glutamyl-s (β -carboxy- β -methyl) -l-cysteinylglycine], γ - l-glutamyl-s-allylmercapto-l-cystein, γ - l-glutamyl-s-allyl-l-cystein, γ - l-glutamyl-s-allyl-l-cystein, γ - l-glutamate-s - (trans-1-propenyl) - L-cystein, etc.
5. glucosinolates: scordinin A1, A2, A3, B1, B2, and B3. Scordinin A1 is a condensation of allyl sulfuronic acid and scormin. quercetin (quercetin) andKaempferol(kaempferol) glucoside.
. Fructans are inulin type polysaccharides, containing 94.4% fructose and 4.3% glucose.
7. 62.2% of neutral lipids, 14.0% of glycolipids and 23.4% of phospholipids are composed of linoleic acid (28.5% - 64.0%) andpalmitic acid（palmitic acid）13.8%-26.6%。 .
8. enzymes such as allinase, polyphenoloxidase, hexokinase and l-serine-o-sulfate lyase.
9. other allixin, adenosine, cis -, trans-2,3-dimethyl-5,6-dithiocyclo [2.1.1] hexane-5-oxide and (Z, z) -d, 1-2,3-dimethyl-1,4-butane disulfide-s, s'- dioxide [(Z, z) -d, 1-2,3-dimethyl-1,4-butane disulfide]ad-s, s'-dioxide].

3、 Pharmacological action of garlic.The study of garlic in the treatment of chronic hepatitis B and its mechanism of action in the treatment of chronic hepatitis B and its mechanism of action in the treatment of chronic hepatitis B and its mechanism of action in the treatment of chronic hepatitis B and its
1. protective effects on the liver 1.1 effects of various components of garlic on cytotoxicity induced by carbon tetrachloride and galactosamine in primary cultured rat hepatocytes garlic volatile oil and s-allylthiocysteine (ASSC) have significant inhibitory effects on cytotoxicity induced by carbon tetrachloride. In the cytotoxicity caused by galactosamine ((gain), garlic volatile oil, alliin and ASSC have significant inhibitory effects, among which garlic volatile oil has the most significant effect.
. The control group was treated with Ig distilled water, and Allicin was divided into three dose groups, namely, low dose group 30mg/ (kg · day), medium dose group 40mg/ (kg · day), and high dose group 60mg/ (kg · day). Three days after administration, rats in each group received 2ml/kg of Ig carbon tetrachloride. Venous blood was collected before and two days after igcc14. Serum glutamic pyruvic transaminase (GPT) and malondialdehyde (MDA), a product of lipid peroxidation, were measured. The results showed that allicin significantly inhibited the increase of GPT activity in CCl4 induced liver injury in rats. At the same time, it also inhibited the increase of serum MDA.
1.3 antioxidant effects of various components of garlic hiknoh reported that garlic volatile oil can significantly inhibit the spontaneous oxidation of linoleic acid, and the antioxidant capacity is consistent with vitamin E. Lujingwu et al., using the spin trapping electron spin resonance experimental method, confirmed that garlic and its water-soluble extract contain selenoprotein (GP2), selenium containing polysaccharide gps2 (molecular weight 13000), GPS3 (molecular weight 15000), and have strong scavenging ability for active oxygen radicals such as hydroxyl radical (· oh) and superoxide anion radical (O2). It can be compared with the commonly used free radical scavengers SEO and vitamin C.
. Jain et al also observed the hypoglycemic effect of garlic extract from Po in rats with diabetes induced by alloxan. The maximum effect occurred 2 hours after taking the medicine, and the blood glucose concentration decreased by 17.9-26.2%. Chang et al found that garlic affected the synthesis of glycogen in the liver, reduced the blood glucose level and increased the plasma islet turbulence level after feeding mice with 14C labeled acetate and giving mice IP with 14C labeled sucrose.
3. anti infection effect 3.1 antiviral effect the inhibitory effect of garlic extract on cytomegalovirus the materials used were the 13th-18th passages of self-made human fetal lung fibroblasts; Cytomegalovirus (CMV) adl69 strain; Eagles' medium was supplemented with 2% calf serum, and garlic solution with different dilutions (1:25, 1:50 and 1:100) was added. After the virus stored in liquid nitrogen was resuspended, the supernatant was centrifuged at 40 ° C (300r/minl0min) and inoculated into the pelleted cell tubes according to the titer of 100tcid50/o.1ml. The solution was changed after adsorption at 37 ℃ for 2h. . Results the viral lesions in the control group were ＋＋＋＋＋; When garlic solution was diluted 1:100, it was only ± - +; 1: 25 could completely inhibit the virus growth when diluted. And the concentration of garlic solution had no obvious effect on fetal lung cells. Within the scope of this experimental design, the antiviral effect of garlic liquid increases with the increase of its concentration. In addition, garlic liquid was used in different stages of the experiment to compare its effect. It was found that only garlic solution was used to treat cells or viruses before virus adsorption, and no garlic solution was added to the maintenance solution after adsorption, which had no obvious effect on the growth of CMV in the future; After virus adsorption, garlic solution was added to the maintenance solution to show its inhibitory effect on CMV; The effect of continuous medication is the strongest since virus adsorption.
3.2 antibacterial effect 3.2.1 antifungal effect has different degrees of inhibitory effect on common pathogenic skin fungi. Allicin has obvious inhibitory effect on Candida albicans at the concentration of 1:51200. At the concentration of 1:200800, it has a very obvious inhibitory effect on Cryptococcus neoformans. The inhibitory concentrations of garlic extract in vitro against Cryptococcus neoformans and Candida albicans compared with nystatin, cycloheximide and amphotericin B are shown in table 18: by microdilution method, the 5% minimum inhibitory concentration (MIC), 90% minimum inhibitory concentration (MIC), 50% minimum fungicidal concentration (MFC) and 90% minimum fungicidal concentration (MFC) of 60 deep fungi of garlic extract in vitro were obtained. .
3.2.2 effect on other bacteria in the test tube, raw garlic has inhibitory effect on pyogenes, tuberculosis, dysentery, typhoid, paratyphoid and Vibrio cholerae (see table 20). Garlic preparation also has inhibitory effect on cyanobacteria, Streptococcus, chloramphenicol and aureomycin resistant bacteria. The antibacterial active ingredient of garlic may be the combination of the oxygen atom in the garlic capsaicin molecule and the sulfur group in the cysteine molecule necessary for bacterial growth and reproduction, which makes the latter become an inactive substance, interferes with bacterial metabolism, and thus inhibits the growth and reproduction of bacteria. Recently, Liu Wei and others observed that allicin 150ug/ml could eliminate the 140md plasmid carried by s and f2b6121 dysentery bacteria, namely the virulence related large plasmid, at 72h. The eliminated 140md plasmid is a virulence related plasmid, which makes the strain lose invasiveness and become a non-toxic strain. This suggests that allicin may have the effect of eliminating plasmid DNA.
In vitro test of antigenic effect of garlic water extract showed that garlic water extract had the effect of killing amoeba protozoa, and purple skin garlic had better effect than white skin garlic. It is also effective for patients with amebic dysentery. Garlic juice, garlic volatile substances or garlic extract also have obvious killing effect on vaginal Trichomonas in vitro.
3.2.3 effects on inflammation and miscellaneous trauma allisatin, a garlic extract, can inhibit formaldehyde induced foot swelling in rats, but has no obvious effect on the exudation of experimental subcutaneous granulation sac. After the paste made of garlic, rhubarb and mirabilite was applied externally to the right lower abdominal skin of rabbits with normal or experimental appendicitis, in addition to the local skin infrared, it also caused reflex enhancement of the movement of the appendix and colon, proliferation and enlargement of reticuloendothelial cells, and reduction of appendiceal inflammation, indicating that it had obvious stimulatory effect on the reticuloendothelial system of the spleen. Garlic phytofungicide can promote granulation formation and epithelial hyperplasia of infectious wounds in rabbits and rats, eliminate suppuration, and gradually turn the wound from gray to rose red. Histochemical methods confirmed that garlic increased the content of RNA and DNA in rabbits with infectious trauma. Garlic has adrenocorticotropic hormone like effect, and its ethanol or ethyl acetate extract injected into rabbits can increase the excretion of 17 ketosterol in urine.
3.2.4 effect on immune function 3.2.4.1 effect on phagocytic function of peritoneal macrophages in mice twenty five mice of 20-25g were selected and given 1ml of IP beef soup medium for each mouse. After 22 hours, the experimental group received 0.4ml of axillary SC garlic injection (each 1ml was equivalent to 1g of the original drug), and the control group was injected with the same amount of normal saline. After 60 minutes, each mouse was given 0.5ml of 2% chicken red blood cell suspension washed with normal saline. The mice were sacrificed by cervical dislocation 40 minutes after the injection of chicken red blood cells. The peritoneal inflammatory exudate smear was taken and stained with Wright Giemsa mixture. The phagocytic capacity of exudate cells (mainly macrophages) was observed under the microscope, that is, the total number of 100 inflammatory exudate macrophages engulfing chicken red blood cells was divided by 100 as the phagocytic index. The phagocytic index of the experimental group was significantly higher than that of the control group (P < 0.001). Microscopic examination showed that the macrophage cell body was significantly expanded, the air in the cytoplasm was increased, and the phagosomes were increased. The engulfed chicken red blood cells were in various digestive states.
? /Ml, the lysozyme activity was 11.78 ± 1.97ug/ml, and the lysozyme activity was positively correlated with the cell concentration. Two male rats were taken each time, and alveolar macrophages were extracted according to the above method. Garlic injection was mixed with alveolar macrophage suspension (concentration 5x10? /Ml) was mixed at the ratio of 1:10, 1:30, 1:100, 1:500, and then the diameter of the lysozyme ring was measured and the corresponding lysozyme activity was obtained. The results of 13 experiments in 26 rats showed that garlic injection at 1:10 and 1:30 could significantly increase the diameter of the lysozyme ring and lysozyme activity of alveolar macrophages, but it was ineffective when the concentration of garlic was too low (such as 1:100 and 1:500).
. After the patient was injected with garlic injection, the lymphoblastoid cell transformation rate and rose petal reaction were significantly increased. It can be seen from the above that garlic may have an activating effect on immune function.
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4.1 in vitro sperm suppression effect healthy mature male SD rats and golden voles weighing 300 ± 20g and 130 ± 10g respectively were used, and the semen was diluted with normal saline to a sperm count of more than 4x107/ml. Semen from 10 other fertile volunteers was diluted with bww (containing 3mg/ml human serum albumin) with a sperm count of more than 4x107/ml. The inhibitory effect of allicin at different concentrations on animal or human spermatozoa at different times was studied by dish mixing method. When the concentration of allicin was 0.75%, the sperm of human, rat and vole were all arrested and inactivated at 20s. At the concentration of 0.15%, the sperm can be inactivated within 3min. At a lower concentration, allicin has different degrees of spermicity inhibition. .
The effects of allicin at different concentrations on spermatogenesis were compared by tube incubation method. When the concentration of allicin was 0.75%, the sperm of human, rat and vole were inhibited within 20 s. When the concentration was 0.0937%, all the above sperm were inactivated within 3-5 minutes. At the 10th minute, the lowest concentration of sperm inhibition was 0.0468% for human spermatozoa and 0.0029% for rats and voles. It was observed that allicin at a concentration of 0.0075% could inactivate human sperm for 80min; Animal sperm is much more sensitive to drugs, and its concentration of sperm inhibition is even lower.
In addition, at the effective concentration of sperm inhibition, it does not stimulate the vagina of animals, nor inhibit the growth and reproduction of Lactobacillus.
4.2 effect on uterus garlic ethanol extract can enhance the contraction amplitude and frequency of isolated guinea pig uterus, and the muscle tension is also slightly increased. 2mg of garlic ethanol extract has the same effect as 0.001 unit of pituitrin, which can be antagonized by procaine. It also has similar effects on human uterus. .
5. effect on cardiovascular system 5.1 antihypertensive effect experimental dogs induced hypertension by ligating three vessels of four main cerebral arteries in two stages. Po garlic preparation, the blood pressure decreased significantly after 7-10 days, close to normal. The study of acute hypotension in cats anesthetized with urethane found that garlic extract, when injected intravenously at a dose of 0.2g/kg, can reduce blood pressure by 50mmhg or more. The mechanism is that garlic contains a choline like substance, which has little effect on vascular smooth muscle.
5.2 anti atherosclerotic effect 5.2.1 lipid lowering effect 5.2.1.1 effect of new and old garlic on cholesterolemia in rabbits the new and old garlic can reduce hypercholesterolemia healthy blue violet rabbits, weighing between 2.0-2.5kg, were selected according to the basic cholesterol level, and were randomly divided into control, cholesterol, new garlic and old garlic groups, with 10 rabbits in each group, and were raised in cages. Except for the control group, the other groups were fed with cholesterol 0.5g/ day (rats), while the new and old garlic groups were fed with new garlic harvested in May, or old garlic stored indoors for 7mo after harvest, at a dose of 2G / day per rabbit. On the 50th day of experimental observation, fasting blood was taken from ear marginal vein every 10 days, and serum total cholesterol was determined by ferric chloride glacial acetic acid direct chromogenic method. The average serum cholesterol concentration of rabbits in each group fed with cholesterol increased, which was more significant in the cholesterol group and the old garlic group. The increase in dl0 was up to 4-5 times, and 12 times after 1Mo. The increase in serum cholesterol concentration in the new garlic group was relatively slow, and the increase was less than 2 times on experimental D10, and only 5 times after 1Mo. There was significant difference between the two groups (P < 0.05). .
Experimental observation on the protective effect of aortic atherosclerosis 50 days later, the animals were sacrificed by exsanguination of the carotid artery, and the aorta was immediately removed. The degree of aortic atherosclerotic lesions in the old garlic group was similar to that in the cholesterol group, with no significant difference, but it was significantly different from that in the new garlic group (P < 0.01). The new garlic has a better protective effect on the main artery atherosclerosis caused by hypercholesterolemia.
5.2.1.2 effect of garlic essential oil on preventing hyperlipidemia in rabbits effect of garlic essential oil on hyperlipidemia in rabbits short haired littermates weighing 1.2-15kg were randomly divided into three groups according to body weight, serum total cholesterol content, litter type and gender before the experiment. ① Eight rats in garlic oil high-fat diet group. ② 7 rats in the high-fat diet group. ③ There were 6 rats in the control group. ① Garlic oil 20mg/kg/ day was dissolved in quantitative soybean oil and fed once a day. . The animals in each group were fed with ordinary feed, but the animals in the high-fat and garlic oil groups were given 0.2g/kg cholesterol according to body weight every day, dissolved in quantitative lard. . At the beginning of the experiment, the average contents of serum total cholesterol and triglyceride (mg/dl) of animals in each group were similar. At 1.5mo and 3Mo of the experiment, the blood lipids of the two groups of animals taking cholesterol increased, but the increase amplitude of the garlic oil group was significantly smaller than that of the high-fat group. In the high-fat group, the serum total cholesterol at the end of 1.5mo and 3Mo was 19 times and 23 times higher than that at the beginning of the experiment, respectively; The corresponding value of serum total cholesterol in garlic oil group was 14 times and 17 times, and there was significant difference between the two groups. The corresponding values of serum triglyceride in garlic oil group were 1.4 times and 1.8 times; The results of serum lipoprotein electrophoresis showed that at 1.5mo, the ratio of b-lipoprotein / a-lipoprotein in the two groups fed with cholesterol was higher than that in the normal group, and it increased the most at 3Mo, but the B / a values measured twice in the garlic oil group were significantly lower than those in the high-fat group. At 4mo of the experiment, cholesterol lard had been stopped for 20 days, and the blood lipids of the two groups of animals decreased, but the blood lipids of the garlic oil group decreased faster than that of the high-fat group, and the differences of three blood lipids between the two groups were still significant. However, there was no significant difference in liver fat content between the high-fat group and the garlic group.
Effects of garlic essential oil on blood coagulation in hyperlipidemic rabbits the blood coagulation time of the animals in the above groups was also measured by tube method at different periods; The euglobulin dissolution time (ECT) was measured by euglobulin dissolution test to calculate the plasma plasmin activity unit U (unit u=10000/ect). Results there was no significant difference in the average whole blood coagulation time between the groups at the beginning of the experiment. After treatment, the clotting time of the high-fat group was shortened, while that of the garlic Shantou group was prolonged (P < 0.05 for 3Mo, 4mo vs. the beginning). The coagulation time of garlic oil group was significantly longer than that of high-fat group at 3Mo and 4mo (P < 0.05, P < 0.01). The plasma plasmin activity of garlic oil group was better than that of high-fat group during the experimental period, and P < 0.05 at 1.5mo and 4mo. In the experiment, the plasma fibrinogen content in the garlic oil group decreased, and it was significantly lower than that in the high-fat group at the end of 4mo of the experiment (P < 0.05).
Effects of garlic essential oil on atherosclerotic lesions in experimental hyperlipidemic rabbits effects on aorta there were obvious atherosclerotic plaques in the intima of the aorta of the animals in the high-fat and garlic essential oil groups. The former plaques were mostly fused into patches and diffusely distributed in the aortic root. . Lipid deposition could be seen in the abdominal aorta of most animals in the high-fat group, while only one animal in the garlic essential oil group had lesions in the abdominal aorta. The results of microscopic examination are consistent with those of human observation. Effects on coronary arteries in the high-fat group and the garlic oil group, the plaques of the large branches of coronary arteries were mostly mound shaped, with lipid deposits under the intima; . There were varying degrees of intimal thickening, lipid deposition and luminal stenosis in the middle and small branches of coronary arteries in the two groups. Endothelial cell hyperplasia of arterial wall was seen in a few cases. There were significant differences between the high-fat group and the garlic oil group in the number of blood and lesion degree of coronary plaque.
5.2.1.3 effects of allicin on cAMP levels in arteries and livers of hypercholesterolemic quails seventy two healthy male Korean quails weighing 95-10g and about 6wk old were randomly divided into three groups. . The first group was fed with conventional diet, the second group was fed with 1% high cholesterol diet, and the third group was fed with 1% high cholesterol diet plus 50mg / (kg · day) of allicin. In the experimental phase, after 15, 30, and 45 days, one group of each group was fasted for 12h, and the venous blood was decapitated and sacrificed. Total cholesterol in plasma was measured by high iron sulfuric acid chromogenic method, and camp in aorta, right brachiocephalic artery, and liver was measured by protein binding method. During the whole process, there was no significant change in the plasma cholesterol level of common food tissue, and the garlic neomycin group was significantly lower than the cholesterol group after 15, 30, and 45 days (P < 0.01). Except for the normal diet group, the cAMP levels in the artery and liver of the other two groups gradually decreased, especially in the cholesterol group. After 15 days, the cAMP level of cholesterol group was significantly lower than that of general diet group and Allicin group (P < 0.01, P < 0.05). At this time, although allicin group had been reduced, there was no significant difference with general diet group (P < 0.01). The results after 30 days are basically the same as before. The results after 45 days of experiment were basically the same as before. . The cAMP level in the liver of cholesterol group was significantly lower than that of general diet group and Allicin group after 15 days of experiment (P < 0.05). Although the garlic neoelement has decreased a lot after 30 days, there was no significant difference with the general diet group (P > 0.05), and it was not significantly lower than the general diet group until the 45th day (P < 0.01).
In recent years, studies have found that garlic has a protective effect on experimental rabbit hypercholesterolemia, hypercholesterolemia coagulation, and aortic lipid deposition, and its effective components are alkyl disulfides in volatile oil. Ammonia containing acids such as alliin, cycloalliin, and s-methyl-l-cysteine sulfoxide are also effective ingredients. The sulfoxide group in the thiooxy acid molecule is a necessary structure with pharmacological effects. The experiment showed that S-methyl sulfoxide in one liter half of tryptophan could inhibit the increase of cholesterol in animals fed with high cholesterol. .
5.2.2 effects on Hemorheology 5.2.2.1 allicin can significantly inhibit human platelet aggregation induced by ADP and epinephrine and platelet aggregation in experimental rabbit hypercholesterolemia. Allicin can prevent the decrease of camp caused by cholesterol. In addition, Srivastava confirmed that garlic extract can inhibit all chemical drug-induced hemagglutination in a dose-dependent manner. . Mohammad reported that garlic capsaicin could strongly inhibit the aggregation and release of platelets in plasma, but it failed rapidly when the temperature was above 56 ℃ or the pH value exceeded 8.5.
5.2.2.2 effect of garlic preparation on platelet adhesion activity 5.2.2.2.1 effect of allicin on human platelet adhesion activity and platelet membrane glycoprotein fifteen healthy volunteers (aged 19-44 years without taking antiplatelet drugs within two weeks) were divided into control group and low concentration group. The final concentration of allicin in high concentration group and low concentration group were 100mg/l and 50mg/l respectively. The platelet adhesion activity was measured by glass ball method. Allicin significantly inhibited human platelet adhesion activity, and the low concentration group had shown significant inhibitory effect. ? /L of platelet rich plasma (PRP), and the final concentration of allicin was increased by 100mg / L in the treatment group. The results showed that there was no significant difference in the measured amount of platelet (GPLB) between the allicin treatment group and the control group (P > 0.05).
5.2.2.2.2 effect of garlic extract on rabbit platelet adhesion function nineteen Japanese white rabbits were divided into two groups. Garlic group: the daily feed contained cholesterol of 0.5g/kg, and at the same time, it was nasally fed with 2g/kg garlic extract. . Results in cholesterol group, the platelet adhesion rate increased gradually; The platelet adhesion rate of garlic group decreased steadily. The difference was statistically significant between 3Mo and pre medication (P < 0.05), and the difference was statistically significant between 4mo and cholesterol group and pre medication (P < 0.05).
6. antitumor effect 6.1 effect on human nasopharyngeal carcinoma cell lines (CSN3, csn7), mouse sarcoma cell line (S-180), heal cell line, human liver cancer cell line (7402).
6.1.1 effects on four cancer cell lines CSN3, csn7 and S-180 cell lines were added at the same time of passaging, and HeLa and hepatoma (7402) cell lines were added 24 hours after passaging. The experimental bottle was added with 0.3% of three garlic preparations, and the control bottle was added with 0.2ml (or 0.1ml) of normal saline. The cell growth was recorded at 24, 48, and 72 hours after dosing (csns3, csn7, and S-180 were in suspension growth, and the growth was divided into large clumps (+ +), partial wall detachment (+), and total wall detachment (0) levels). S-180 cell line also took the same amount of cell fluid from its experimental bottle and control bottle, concentrated to about 1million cells per 1ml after centrifugation, and then injected into mice to observe the tumor growth in vivo. Four diluted concentrations of three garlic oil agents acted on four cancer cell lines for three days. Compared with the control, the concentration of 1 / 100 could kill 78-100% of csn1 and S-180 cancer cells, completely inhibit some division of their cancer cells, and make most of the cancer cell nuclei undergo significant degenerative changes such as nuclear fragmentation, nuclear pyknosis, vacuolization, etc. in addition, the S-180 cancer cells treated with 1 / 10 concentration were injected into mice. The control group developed a mass within eight days, but the experimental group did not grow a mass. The results showed that S-180 cancer cells treated with Garlic Solution in vitro did lose some biological characteristics of their original cancer cells . According to the above results, it is believed that the anticancer component in garlic oil is probably diallyl thiosulfonate. It has been reported that the complex of garlic wheat and selenium has significant antitumor effect on S180 in mice (p=0.01). If S-180 cells were transplanted into mice 24 hours before treatment, and then a certain dose of allicin and allithiamine were injected into the tumor site, the tumor growth could be significantly inhibited.
6.1.2 effect on normal human lymphocytes and csn7 cancer cell line treated with self-made garlic water extract injection respectively. After csn7 cancer cells and normal human lymphocytes were stimulated by PHA to divide for 24 hours in vitro, garlic solution caused a series of degenerative changes in the morphology of csn7 cancer cells and their chromosomes, but the morphology of normal human lymphocytes and their chromosomes did not change, and there was a tendency to increase the division rate. At the same time, csn7 cancer cells were observed for three consecutive days. It was found that compared with the corresponding control (24, 48, 72 hours), with the extension of garlic action time to 72 hours, the growth of clumps disappeared, the ratio of total cells decreased, and the mortality increased sharply. .
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6.2 effect on reticulosarcoma (ARS), hepatoma ascites (HEPA), Ehrlich ascites carcinoma (EAC) and 615 leukemia (L615) pure bred chinchilla of 615 leukemia (L615) was selected, and hybrid mice with other tumors were used, weighing 18-22g. The male and female mice with both muscle and muscle were established into mouse models of reticulosarcoma, Ehrlich ascites carcinoma and hepatoma ascites according to the provisions of the in vivo screening protocol for antitumor drugs (Draft) formulated by the national conference in 1973. Garlic oil injection and garlic distilled water were used to treat them. Results garlic oil injection significantly prolonged the life of reticulosarcoma and hepatoma ascites carcinoma mice, with prolongation rates of 51.5% and 42.9%, garlic distilled liquid 1 ml once a day, the effect is not significant enough, the life prolongation rate is 31.7% and 26.9%, the above two preparations have no life prolonging effect on the mouse abdomen and l-615.
6.3 the effect on solid tumors in animals is the same as that in 6.2. White rats weighing 50-100g were used for walker cancer 286 (W-256). Garlic oil preparation and synthetic allicin IP used in the test or local injection of 50-100mg/kg of tumor body had significant tumor inhibition effect, and the inhibition rate was 40-54%. Garlic distilled injection was also effective by IP twice a day, and the inhibition rate was about 40%. The synthetic allicin injection had significant inhibitory effect on ARS solid tumor and liver cancer solid tumor after 7-day treatment, and the inhibitory rates were 56.9% and 50.4%, respectively.
6.4 anti leukemia effect 6.4.1 dose response of normal bone marrow GM-CFU to allicin and homoharringtonine bone marrow samples of normal ribs were taken, and mononuclear cell suspensions were isolated and prepared. . Allicin also has obvious ANTI LEUKEMIA colony growth effect with good specificity.
6.4.2 effects and killing effects of allicin and homoharringtonine on the growth of L-CFU bone marrow from acute nonlymphocytic leukemia was isolated, and the growth of L-CFU was sensitized with allicin at a concentration of 10ug/ml and homoharringtonine at a concentration of 10-7mg/ml. Results allicin significantly inhibited the growth of leukemic cell colonies, clusters and clones (P < 0.01), and homoharringtonine also had a similar effect. The killing effect of allicin was stronger than that of homoharringtonil.
6.5 effects on human gastric cancer cells 6.5.1 effects on human gastric adenocarcinoma cells (SGC) and poorly differentiated mucinous adenocarcinoma cells (MGC)using cancer cell cloning technology, raw garlic homogenate (GJ) and Allicin were respectively applied to two kinds of gastric cancer cells. The results showed that garlic homogenate 1.6mg/ml killed SGC by 1LOG, and killed all cells when 3mg/ml. The killing effect on MGC was slightly worse, 4mg/ml reached 1LOG killing, 8mg/ml reached 21og killing, and the dosage of allicin was 1 / 125-1 / 500 of GJ, the effect was the same to 24ug/ml, killing SGC cells completely or killing MGC cells above 21og. The results of GJ and Allicin in vitro test basically followed the first-order kinetics killing (logarithmic killing).
6.5.2 relevant effects on inducing human lymphocytes (SCE) and inhibiting SGE colony formation 6.5.2.1 the effect of inducing SCE is the venous blood of healthy people. Heparin is used for anticoagulation, and 0.3-0.4ml anticoagulant is added to every 4mlf10 complete culture medium. The final concentrations of substrate hemagglutinin and BrdU were 80ug/ml and 10ug/ml, respectively. The final ALT concentrations were 0.10, 20, 40, and 80umol/l (80umol/l=14.24ug/ml). Incubate at 37 ℃ in the dark for 7z hours. Routine chromosome preparation, upg method for color development, and the SCE frequency was counted under the oil microscope. 50-100 cells were counted in each group. 80umol/L。 There was a significant difference between the mean number of SCE in the group and that in the blank control group (P > 0.05). . . The half inhibitory concentration of allicin on SGC cell colony formation was 1.78ug/ml. There was a correlation between the effect of ALT on colony formation (CFA) of sGC cells and the induction of SCE (r = -0.82), suggesting that these two effects may be the result of the same mechanism of alt.
6.5.2.2 effect on DNA and RNA synthesis of sGC cells SCG cells in logarithmic growth phase were seeded in 20ml small round bottles, with about 106 cells in each bottle. After incubation at 37 ℃ for 12h, 14C TDR and 3H ur were added to make the final concentration of 0.1uci/ml and 1uci/ml respectively. Garlicin was added to the treatment group to make the final concentration 20ug/ml. The blank control group was added with the same amount of normal saline. The number of dead cells in ≥ 1000 cells in the administration group and the blank control group were counted, and the relative survival rate of cells in the administration group was calculated. . Allicin short-term killing SGC cells. It can be seen that 20ug/ml allicin did not significantly increase the mortality of sGC cells within 2 hours, indicating that the inhibitory effect on DNA and RNA synthesis occurred in living cells.
6.6 other anticancer effects 6.6.1 feeding fresh garlic to female c3h/he mice with breast cancer can completely inhibit its development. It is believed that the anticancer active ingredient of fresh garlic may be garlic capsaicin. However, fresh garlic had no effect on leukemia in akr/j mice.
. The garlic polypeptide extracted from garlic was fed to the transplanted Morris hepatocellular carcinoma rats at the concentration of 2.5% or 5%, which showed a dose-dependent relationship with the inhibition of Morris hepatocellular carcinoma within 3 weeks.
6.7 anti tumor mechanism 6.7.1 protective effect on gastric mucosa 6.7.1.1 protective effect on gastric mucosal injury induced by hydrochloric acid in rats effect of garlic liquid on gastric mucosal injury induced by 0.6mol/lhcl Wister rats, either male or female, weighing 180-300g, were used. Rats fasted for 36h were divided into three groups with 13 rats in each group, namely the control group (1ml normal saline); Garlic high concentration group (30% garlic liquid, namely 30g raw garlic, mashed, added 100ml distilled water, centrifuged at 1000r/min for lmin, and then took the supernatant; With 1ml); In the low concentration Garlic Solution Group (10% garlic solution 1ml), the animals were treated with 0.6mol/lhci1mlig for 30 minutes, and then decapitated for 1 hour to observe the gastric mucosal injury index. The results showed that in the 30% garlic solution group, the injury index decreased from 69.6 ± 8.8 (x ± SX) in the control group to 4.9 ± 0.6 (P < 0.001N = b), and the injury inhibition rate was 93%; .
Effect of Garlic Solution on gastric acid secretion in rats with pylorus ligation after fasting for 36 hours under ether anesthesia, the control group was gavaged with 1ml normal saline, and the experimental group was gavaged with 1ml 30% garlic solution and immediately subjected to pylorus ligation. The animals were sacrificed 3 hours later, and all gastric juice was collected to measure the volume of gastric juice, total acidity (titrated with 0.1mol/lnaoh) and total acid output. The results showed that the gastric juice secretion, total acidity and total acid excretion of 30% garlic solution group were 3.6 ± 0.2ml, 798 ± 5.7ml and 300 ± 44.0ml respectively (n = 10, (x ± SX), while those of the control group were 3.8 ± 0.2ml, 87.1 ± 4.7ml and 344.0 ± 36.0) ml respectively. There was no significant difference between the two groups, indicating that 30% garlic solution had no significant effect on gastric juice secretion, total acidity and total acid excretion of rats.
Effects of indomethacin on the cytoprotective effect of Garlic Solution ① indomethacin on gastric mucosal damage indomethacin is a prostaglandin synthase inhibition system. Rats fasted for 36 hours were given 1ml of indomethacin at the dose of 5mg/kg by gavage (n = 10), and were sacrificed 3H later. No gastric mucosal damage was found by naked eyes and histological examination. ② Effect of indomethacin on the cytoprotective effect of Garlic Solution rats fasted for 36 hours were randomly divided into three groups, with 12 rats in each group. The first and second groups were treated with normal saline 1mlig; The third group was treated with indomethacin (5mg/kg) 1mlig. One hour later, 1ml of normal saline was used in group 1; 1mlig of 30% garlic solution was used in groups 2 and 3; 0.6mol/lhci1mlig was used in groups 1, 2 and 3 30 minutes later, and the animals were decapitated and sacrificed 1 hour later. The results showed that the gastric mucosal injury index of indomethacin + 30% garlic solution + 0.6mol/lhci group (n = 12) was 64.5 ± 5.1, and that of 0.6mol/lhcl group (n = 12) was 67.0 ± 5.4. There was no significant difference between the two groups (P > 0.05), indicating that indomethacin can reverse the cytoprotective effect of garlic solution.
; Thus preventing the damage of HCl and pepsin to the gastric mucosa.
6.7.1.2 protective effect on gastric mucosa damage induced by nitroso muscle in rats the inhibitory effect of diallyl sulfide (DAS) on MNNG induced nuclear deformation and ornithine decarboxylase activity was tested with Wister rats. The purity of Das reached 97% and was dissolved in DMSO. Das solution (or DMSO) Ig or injection volume was 0.1ml/125g, once Ig or IP. Results compared with dmsoig or IP pretreatment group without DAS, Na and ODC activities induced by MNNG (20mg/kg) were significantly decreased in DAS (200mg/kg) Ig or IP pretreatment group (P < 0.05). However, DAS itself had no inhibitory effect on Na and ODC activities. These results suggest that Das can significantly inhibit the activities of Na and ODC in rat glandular gastric mucosa induced by mn-ng. The inhibitory effect of dasip on Na and ODC activity induced by MNNG (20mg/kg) increased with the increase of injection dose, and the dose was significantly correlated with the inhibitory effect. There was a significant difference between each increasing dose group (50mg/kg, 200mg/kg, 400mg/kg) and the previous dose (P < 0.05). .
Effect of diallyl sulfide on pH in rat glandular stomach the pH values of Das solution and DMSO were 8.99 and 8.45, respectively. After 30 minutes of Das or dmsoig, the pH (x ± SX) in the glandular gastric cavity was 5.96 ± 0.46 and 5.38 ± 0.72, respectively; After 3 hours of Das or dmsoip, the pH of rat glandular gastric cavity was 4.93 ± 0.20 and 5.27 ± 0.17, respectively. There was no significant difference in pH between Das treated group and DMSO treated group (P < 0.05). . However, MNNG does not need metabolic activation, but directly exerts carcinogenic effects on the gastric mucosa. Neither oral administration nor injection of Das stimulated obvious gastric acid secretion, suggesting that Das does not act through MNNG acidolysis, and may directly inactivate mn-ng in the gastric cavity.
Because the injection and oral administration of Das have the same effect on inactivating MNNG in the gastric mucosa, it has been reported that Das can stimulate the GST activity of rat liver, forestomach and small intestine, and the latter can catalyze the binding of glutathione with carcinogens, thus inactivating carcinogens.
6.7.2 effect on gastric cancer 6.7.2.1 effect on the content of nitrite and nitrate in gastric juice raw garlic can reduce the content of nitrite in gastric juice, but has no effect on the content of nitrite in gastric juice. There was no effect on nitrate content in gastric juice.
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6.7.2.3 inhibition of nitrate reduction by nitrate reductase the crude extract of nitrate reductase was extracted from Escherichia coli, and the effect of garlic on inhibition of nitrate reductase in reducing No3 to NO2 was observed. The results showed that garlic and its preparations could inhibit the reduction of NO3 to no2- by nitrate reductase. The highest inhibition rates of garlic juice, garlic oil and Allicin were 97.93%, 57.93% and 50.34%, respectively. It is suggested that one of the mechanisms of garlic inhibiting no3- reduction of no2- is related to the inhibition of nitrate reductase activity.
6.7.2.4 blocking the synthesis of nitrosamines garlic extract can block the synthesis of dimethylnitrosamine (DMN), diethylnitrosamine (DEN) and dibutylnitrosamine (DBN) in vitro, and has an obvious dose effect relationship. The experiment also shows that its blocking effect is independent of the reduced ascorbic acid in garlic. Under the condition of simulated gastric juice, garlic juice had the strongest blocking effect on the synthesis of N-diethylnitrosamine, and the blocking rate was 81.22%. It can also block the promoting effect of bacteria and molds on nitrosamine synthesis. The mechanism of its blocking effect is related to the sulfhydryl compounds contained in garlic. The clinical experiment observation also showed that the content of nitrosamine in stomach was significantly reduced after Po allicin (20mg) for 30 days (P < 0.05). .
6.7.3. anti mutagenic effect allicin mutagens methyl methanesulfonate (MMS) and cyclophosphamide (CY) induced sex linked recessive lethality in Drosophila has a very significant and certain inhibitory effect. .
. Fresh garlic, garlic oil and Allicin had no effect on cyclic adenosine monophosphate (cAMP) and cyclic aconitine monophosphate (CGMP) in the plasma of tumor bearing mice, and there was no difference in the content of cGMP in tumor tissues, but the cAMP level was significantly higher than that of the control group (P < 0.05).
6.7.2.5 effect on tumor immunity eighty four Wister rats, weighing 131 ± 16.29g, were randomly divided into two groups with 42 rats in each group. Each mouse was subcutaneously injected with 1%mana (methylpentyl nitrosamine) solution in the hind limb at a dose of 5mg/kg, once a week. The experimental group was treated with 50% garlic solution Ig at a dose of 10ml/kg six times a week before mana. The control group was gavaged with equal volume of normal saline. Weigh yourself once every 2wk. After a 105 day trial, the rats were anesthetized with 0.43% sodium pentobarbital and dissected after 24h of non administration. The histological changes of esophageal mucosa were divided into grade III, i.e. hyperplastic lesions, precancerous lesions and carcinomas, which were statistically analyzed by chi square test. At the same time, thymus, spleen and body weight of each mouse were weighed at the time of dissection. The immune organ index and peripheral lymphocyte were calculated with the formula of immune organ index = immune organ weight (mg/kg), and t-test was performed. Fifty one esophageal tumors were observed with naked eyes in 50% garlic solution (n = 42), with an average of 1.2 tumors per mouse. The tumor diameter was 0.1-2mm. In the control group (n = 42), 29 tumors occurred in the esophagus, with an average of 1.9 tumors per mouse, and the tumor diameter was 0.2-3mm. Histological examination revealed that garlic had a significant inhibitory effect on esophageal epithelial proliferation, and no carcinogenesis occurred (Table 9). It was significantly different from the control group.
The results showed that 50% garlic solution had no significant effect on thymus index (P > 0.05), but significantly increased spleen fat index.
Effect of garlic on peripheral blood T lymphocytes the peripheral blood T lymphocytes of 50% Garlic Solution Group (n = 10) was 78.6 ± 5.5%, while the control group (n = 10) was only 69.6 ± 7.0%. The difference between the two groups was very significant (P < 0.01).
7. other effects if the paste made of garlic and mirabilite is locally applied to the right lower abdomen of rabbits, the skin becomes red, even blisters, and the appendiceal and colonic motor reflexes are strengthened. The paste made of rhubarb, mirabilite and garlic plus vinegar applied externally to the right lower abdominal skin of normal and experimental appendicitis rabbits has obvious stimulatory effect on the reticuloendothelial system of the appendix and spleen, which is manifested by the proliferation and enlargement of reticular cells and the reduction of inflammation of the appendix. . The phytobactericide in garlic has some stimulatory effects on experimental infectious and sterile wounds in rabbits and rats, and accelerates granulation formation and epithelial proliferation (the drug does not contact the wound but uses its vapor). For infectious trauma, the wound can change from gray to rose red, the suppuration phenomenon is eliminated, the odor disappears, and the epithelium proliferates widely. The contents of RNA and DNA in infectious wounds of rabbits treated with phytobactericide were increased by histochemical method.
Oral administration of garlic preparation satal can improve the symptoms of chronic lead poisoning, and its effect may be due to the large amount of sulfide in it. Allisatin, proposed from garlic, has an inhibitory effect on formaldehyde induced arthritis in rats, but has no effect on the exudation of experimental subcutaneous granulation sac. Intramuscular injection of garlic ethanol extract or monoethyl acetate extract in rabbits can increase the excretion of 17 ketosterol in urine, which is similar to the effect of ACTH. The ethanol extract can also excite the uterus and strengthen the excitatory effect of estradiol on the uterus. An anticoagulant component was proposed from garlic, which has the effect of reducing blood calcium in both test tube and overall test. Rabbits injected with 70mg intravenously can see muscle twitching and can be fatal. Scordinc13 (cosmetic), a glycoside extracted from the water-soluble part of garlic and alliumscorodoprasuml., can be intravenously injected into dogs and rabbits to temporarily reduce blood pressure, excite respiration, inhibit isolated rabbit heart, vasoconstrict isolated rabbit ear, and excite isolated rabbit intestine. .