Melting Point | 233-235°C |
Boling Point | 408.8±47.0 °C at 760 mmHg |
Solubility | Insoluble in water, soluble in ethanol. |
Appearance | Brown fine powder |
Storage Condition | Room Temprature |
MDL | MFCD00240717 |
Use | Used as a medicine, can huoxue Huayu Tongluo |
Reference Show more | 1. [IF=2.19] Jiang Liu et al."Optimization of ultrasonic–microwave synergistic extraction of flavonoids from sweet potato leaves by response surface methodology."J Food Process Pres. 2019 May;43(5):e13928 |
Plant Source: | ginkgo biloba leaves |
(IARC) carcinogen classification | 2B (Vol. 108) 2016 |
plant extract | ginkgo biloba extract is Ginkgo biloba (Ginkgo biloba L.) the main components of the dry leaf extract are flavonoids and terpene lactones, which have a variety of health functions and are widely used in food and cosmetics. |
Chemical composition | the chemical composition of Ginkgo biloba leaves is very complex, from which there are more than 140 kinds of compounds, flavonoids and terpene lactones are the two main active components of Ginkgo biloba leaves. Ginkgo flavonoids, also known as monoflavonoids, with kaempferol, quercetin and isorhamnetin glycoside; Ginkgo terpene lactones belong to terpenoid compounds, which are composed of multifonditerpene lactones and diterpene lactones, and bilobalide and ginkgolides. In addition, it also contains polyprenols, organic acids, polysaccharides, amino acids, phenols and trace elements. |
source plant | Ginkgo biloba is an ancient and primitive relict species grown on Earth for approximately 0.2 billion years, there is a "living fossil. China is the home of Ginkgo biloba. At present, China has 70% of the world's ginkgo biloba resources. Ginkgo as a Chinese herbal medicine in the folk use, the earliest found in the XIV century, the daily use of grass, mainly used in Cough, asthma and inflammation. Ginkgo biloba is also known as Duck's foot, Gongsun tree and duck's palm tree. It is a deciduous tree, up to 40m in height. Trunk upright, bark Gray. Branches of two lengths, leaves clustered on short branches, alternate on long branches. The blade was fan-shaped, 4 ~ 8cm in length and 5 ~ 10cm in width. The seed of Ginkgo biloba is called Ginkgo biloba. ginkgo distributed at 19 ° 40~43 ° 40 N, 97 ° 00~126 ° 30 E, with average annual temperature of 14 ℃ ~ 18 ℃, warm and cool in winter and spring, it grows well in summer and autumn under warm and humid climate conditions. It is vulnerable to freezing injury in severe cold Winter (below -20 ℃) and poor growth in the tropics without winter in summer. Ginkgo is widely distributed in China, distributed in the central to western, North from Liaoning, south to Guangdong, east to Taiwan, west to Qinghai are planted to Jiangsu, Shandong, Zhejiang, Hubei, the majority, now Japan, the United States also have introduced. Figure 1 shows ginkgo biloba and its seeds (Ginkgo biloba). |
cardiovascular and cerebrovascular disease treatment drugs | ginkgo biloba extract is commonly used in the treatment of cardiovascular and cerebrovascular diseases, the main active ingredients are flavonoids and diterpenoids of Ginkgo biloba. The flavonoid glycosides of Ginkgo biloba mainly include quercetin, kaempferol and isorhamnetin. Ginkgo diterpene internal lipid composition mainly includes ginkgolides A, B, C, J, M and bilobalide. ginkgo biloba extract has antioxidant activity, cardiovascular activity, anti-inflammatory activity and anti-tumor activity, can expand the cardiovascular and cerebrovascular and arterial blood vessels, at the same time, effectively prevent vascular blockage, for high blood lipids, hypertension, diabetes and other symptoms have a good prevention and treatment effect, indirectly reduce the common eye diseases (cataract, glaucoma, vitreous opacity, retinopathy, diabetes complicated eye disease and other common eye disease) incidence rate, can effectively purify the blood, strengthen the blood vessels, prevention and treatment of heart disease, and the brain barrier effective, anti-aging, prevention of cancer. For the last 10 years, American consumers have been taking ginkgo biloba products as a health food to prevent stroke and coronary heart disease. According to the American Journal of Medicine, researchers from the Department of Medicine at Oregon State University in the United States found that in more than 3 years of clinical research, over 65 years old perennial oral ginkgo biloba preparations can effectively prevent memory degradation and Alzheimer's disease. |
extraction method | According to incomplete statistics, the current international standard ginkgo biloba extract is EGb761 produced according to the German Schwabe patent process, appearance of Brown yellow powder, a slight fragrance of Ginkgo biloba. Ginkgo biloba extract is a product extracted from the leaves of Ginkgo biloba ginkgo biloba. The commercial extract is usually standardized as 24% flavonol glycosides and 6% ginkgolides. The production process of Ginkgo biloba extract is reported in the literature, mainly including acetone extraction-lead salt precipitation method, ethanol extraction-macroporous resin adsorption separation method, supercritical carbon dioxide extraction method, alcohol extraction-extraction-chromatography separation method, Etc., the domestic application of more for ethanol extraction-resin separation method. at present, the most widely used method at home and abroad is organic solvent extraction. Because other organic solvents are toxic or volatile, ethanol is generally used as the extractant. Zhang Yonghong and other experiments show that the better conditions for extracting flavonoids from Ginkgo biloba leaves are as follows: 70% ethanol, extraction temperature 90 ℃, solid-liquid ratio 1:20, extraction Times 3, reflux 1.5h each time. 1. Ethanol extraction-macroporous resin adsorption separation method remove impurities and mildew leaves, wash, mince, reflux extract with 70% ethanol, separate extract, filter, recover ethanol under reduced pressure, the residue was removed by high-speed centrifugal separation, diluted with appropriate amount of pure water, added to the macroporous adsorption resin column, washed with water until the eluent is clear and light, then eluted with a certain concentration of ethanol, the eluent was collected and concentrated under reduced pressure, it was obtained by vacuum drying. 2. Acetone extraction-lead hydroxide precipitation method ginkgo biloba leaves were extracted with 60% acetone, cooled and filtered, the extract was extracted with carbon tetrachloride, butanone was added and mixed well, and the acetone-butanone phase was separated and precipitated, the ketone phase was further stirred with solid ammonia sulfate, and the solid material was filtered off. The filtrate was evaporated under reduced pressure to a concentration of 20%-60% solids, and diluted with 50% denatured ethanol to a concentration of 10% solids. The lead hydroxide suspension was added and the precipitate was filtered off. The filtrate is concentrated to half of the volume under reduced pressure, and then ammonia sulfate and butanone are added to the concentrated solution under stirring. After stirring, the butanone-ethanol phase is precipitated; The butanone-ethanol phase is separated from the aqueous phase, then, methyl ethyl ketone was added to the aqueous phase, stirred, and the methyl ethyl ketone-ethanol phase was precipitated and combined in the methyl ethyl ketone-ethanol phase. Ammonia sulfate was added under stirring, and the precipitated aqueous phase was separated after mixing. The butanone-ethanol phase was dried with sodium sulfate, evaporated to dryness under reduced pressure, and the denatured viscous residual liquid was dissolved with denatured ethanol, the precipitated precipitates were separated for 12 hours, evaporated under reduced pressure, and dried under vacuum. |
pharmacological activity | as early as the early 60 s of the 20th century, the extract of Ginkgo biloba leaves has been used abroad to treat cerebrovascular diseases and nervous system diseases, its curative effect is remarkable and no side effect. Ginkgo biloba extract has a strong antioxidant effect, can remove excess free radicals in the body, prevent lipid peroxidation in the body, can expand coronary vessels, increase cerebral blood flow, enhance platelet activating factor antagonism, can treat vascular aging, cerebrovascular insufficiency and other neurological disorders. In addition, there is to improve immunity, anti-aging and other effects. 1. Effect on cardiovascular system ginkgo biloba extract can inhibit the activity of angiotensin converting enzyme (ACE) in normal human serum, thus inhibiting the contraction of small arteries, dilating blood vessels and increasing blood flow. Ginkgolides are highly specific PAF receptor blockers. Ginkgo biloba extract or ginkgolides inhibit platelet activating factor (PAF) and cyclooxygenase or lipoxygenase. Ginkgo biloba extract was well tolerated and antagonized platelet aggregation by PAF, but had no effect on ADP-induced aggregation. 2. ginkgo biloba extract can affect the endocrine system and the interaction between immune system and central nervous system by inhibiting the action of PAF, improve memory function. The anti-hypoxia effect may be related to the increase of cerebral blood flow and the improvement of cerebral energy metabolism during hypoxia, in addition to the improvement of memory deficit caused by nano2. Ginkgolide B can be used in the clinical treatment of stroke. 3. Effect on digestive system ginkgo biloba extract can significantly improve gastric ulcer and intestinal ulcer induced by PAF and endotoxin in rats, and can partially inhibit the injury of ethanol on stomach. It has potential therapeutic effect on liver cirrhosis. Ginkgolide B may play a role in the treatment of acute pancreatitis. 4. Effects on respiratory system The ethanol extract of Ginkgo biloba leaves has a direct relaxant effect on tracheal smooth muscle. Inhalation of atomized ginkgo biloba extract not only inhibited bronchoconstriction, but also inhibited PAF-induced reduction of white blood cells and eosinophils, Ginkgo biloba extract is of great significance in the inhibition and treatment of bronchial hyperreactivity. 5. Anti-aging effect ginkgo biflavone, isoginkgo biflavone, ginkgo biloba and quercetin in ginkgo biloba leaves all have the effect of inhibiting lipid peroxidation, especially quercetin has stronger inhibitory activity. Effects on graft rejection and other immune reactions ginkgo biloba extract can prolong the survival time of transplanted skin, heterotopic heart xenograft and orthotopic liver xenograft. Ginkgo biloba extract can inhibit the natural killer cell activity of human body to KC526 target cells, and can also prevent the natural killer cell activity caused by interferon. 8. Anti-tumor effect The fat-soluble part of the crude extract of green leaves of Ginkgo biloba leaves could inhibit Epstein-Barr virus, and both heptadecenosalicylic acid and Ginkgo biloba (Bilo-betin) had strong inhibitory activity; total flavonoids of Ginkgo biloba can increase the weight of thymus and the level of SOD activity in tumor-bearing mice, and mobilize the anti-tumor ability of the body. Quercetin and myricetin can inhibit the occurrence of carcinogens. ginkgo biloba extract can directly scavenge lipid free radicals, lipid peroxidation free radicals and alkane free radicals, and terminate the chain reaction of free radicals. At the same time, it can also participate in the regulation and improvement of the activity of superoxide dismutase, glutathione peroxidase and other antioxidant enzymes. The antioxidant effect of flavonoids in EGB even exceeds that of vitamins, and has anti-free radical Aggression properties in vitro. |
pharmacokinetics | 1. Pharmacokinetics of flavonoids flavonoids of Ginkgo biloba are mainly absorbed in the form of aglycones, and the form of glycosides or aglycones of ginkgo flavonoids can hardly be detected in plasma and urine, it mainly exists in the form of glucuronic acid conjugates or sulfuric acid conjugates of aglycones. At the same time, it is also reported that the plasma or urine can be detected after hydrolysis, and the different conclusions may be caused by the sensitivity of the analytical instrument and method, but it also reveals that the bioavailability of flavonoids from Ginkgo biloba is low. There are two main metabolic sites of ginkgo flavone glycosides in vivo: one is the liver, which undergoes a series of reactions under the action of CYP450 in the liver, and produces metabolites with higher water solubility; the second is the intestinal tract, which is hydrolyzed into aglycone under the action of intestinal flora. In contrast to the effect of ginkgo terpene lactones on activating CYP3A enzyme, ginkgo flavonoids show inhibitory effect on CYP3A enzyme activity, which is a problem that needs to be strictly paid attention to in the future experimental process and clinical medication. Quercetin and kaempferol can decrease the activities of CYP1A1, CYP1A2 and CYP3A4 in rat and human liver microsomes. 2. Pharmacokinetics of terpene lactones In the Phase I metabolism of ginkgo terpene lactones, the effects of different lactones on CYP450 enzymes are tissue-specific, different compounds have different effects on it. Ginkgolide A can induce the expression of CYP3A23, and ginkgolide A and B have no effect on the transcription of CYP3A4. Bilobalide can induce the expression of CYP3A4 and CYP2B1. The effect of ginkgolides on CYP450 enzyme system may be the basis of their pharmacological activities. Compared with Phase I metabolism, similar to ginkgo flavonoids, in vitro studies show that the metabolism of ginkgo terpene lactones is also dominated by Phase II metabolism, ginkgolide A and bilobalide have A significant induction effect on the phase II metabolizing enzyme (UGT), glutathione-S-transferase and lipoamide dehydrogenase in rats, while ginkgolide B, C had no significant effect on the same dose. |
toxicity reaction | LD50 of Ginkgo biloba extract was (1202.5±141.3)μg/g, equivalent to crude drug (7.8±0.9)g/Kg; Intragastric administration of (17.9±1.0)g/kg, equivalent to crude drug (116.4±6.5)g/kg. The dog was injected with 10 to 40 times the clinical dosage of the drug for 1 week, Nausea, Vomit, Diarrhea, loss of appetite, etc., the tissue section found that the small intestinal mucosa secretion, anesthetized dogs, the intestinal peristalsis of the rabbit was enhanced, and the local blood vessels were hardened by injection. both ginkgo biloba extract and ginkgo biloba extract have hemolytic effect. Ginkgo biloba extract has anesthetic effect on the central nervous system of frog. Intravenous injection of Ginkgo biloba 0.2g/kg, the first transient pressor effect, and then decreased blood pressure, Dyspnea, animal convulsions and death; General dose of flavonols on blood coagulation system had no effect, A higher dose may interfere with blood clotting. The LD50 of the tail vein of the mice was 242mg/kg, and the symptoms of acute poisoning were shortness of breath, not moving, and died of respiratory paralysis. white fruit acid has hemolytic effect. Ginkgo flavonoids with therapeutic amount of 100 to 1000 times, the guinea pig can cause moderate intensity decrease in blood pressure, faster breathing, heart rate slowed down. |
drug interaction | ginkgo biloba extract is commonly used in the treatment of cardiovascular disease drugs, often with anti-platelet, sedation, lipid-lowering drugs and other combined application. Ginkgo biloba and its monomer components such as quercetin, kaempferol and isorhamnetin have inhibitory effects on CYP3A4, CYP2C9, CYP2B6, etc, B and bilobalide and other lactones have the induction effect on CYP1A2, CYP2B1/2, CYP3A2, CYP2C19, UGT1A1, etc., and are P-glycoprotein substrates, and the role of complex, therefore need to arouse widespread attention. in recent years, there have been reports of individual cases of bleeding caused by taking ginkgo biloba preparations or combined with other anticoagulant drugs. Ginkgo biloba extract inhibits PAF leading to bleeding, and ginkgolide B is considered to be the most important component in inhibiting PAF. But there is no corresponding control study. At present, there are great differences in the composition and amount of ginkgo leaf products on the market. The dose and specific amount of ginkgolide B associated with bleeding are unknown. There may also be other ingredients in the product that can cause bleeding. Therefore, the research in this area remains to be further in-depth. Therefore, according to the results of the present study, the cases of hemorrhage caused by ginkgo biloba extract preparation should be notified to the physician, and enough attention should be paid. And try to avoid ginkgo biloba extract preparation and aspirin, warfarin and other anticoagulant drugs. |
application field | 1. Flavonoids in ginkgo biloba leaves have antioxidant activity, can be added as antioxidants in oils and cakes, the total flavonoids with yellow, and wide solubility, both water-soluble and fat-soluble, so the total flavonoids can play a role in colorants. Processing of Ginkgo biloba into ultrafine powder in food. The ginkgo biloba ultrafine grinding, according to 5%~ 10% added in cakes, biscuits, noodles, candy, ice cream, can be processed into a health effect of Ginkgo biloba food. ginkgo biloba extract is a food additive in Canada and approved for over-the-counter in Germany and France. Ginkgo biloba is included in the United States Pharmacopeia (24th edition) and ginkgo biloba extract is used as a dietary supplement in the United States. The international ginkgo products have reached more than 30 kinds, the main dosage forms include: ginkgo leaf, ginkgo Oral Liquid, ginkgolide injection, Ginkgo Leaf Extract and Dipyridamole Injection, ginkgo ketone ester drop pills, compound ginkgo biloba granules, ginkgo biloba extract and so on. From 2009 to 2011, the sales of Ginkgo biloba preparations and DDDs ranked in the top three of the commonly used cardiovascular traditional Chinese medicine. ginkgo biloba leaves contain a small amount of proanthocyanidins and urushiic acids, which are toxic to human body. When ginkgo biloba leaves are used as raw materials for food processing, special treatment should be carried out to reduce the content of proanthocyanidins and urushiic acids. But in the dose range currently used, without any acute and chronic toxicity, no teratogenic effect. The Ministry of Health approved ginkgo biloba extract as a new food additive in 1992. In recent years, the total flavonoids of Ginkgo biloba leaves have been widely used in food industry, and the research and development of Ginkgo biloba leaves have broad prospects. 2, daily chemical industry The combination of Ginkgo biloba extract and skin absorption enhancer can also prevent the irritation caused by the adhesive used in the external ointment and patch, can be emulsion, ointment, creams, sols and plasters, etc. The skin care products containing GBE in the market now mainly include anti-aging cleanser, body wash, lipstick, eye cream, etc. GBE can also be used in the production of hair growth and hair care products. Chen Yan even add ginkgo biloba extract in toothpaste, according to its research, has a certain anti-caries effect. |