vegetation : chemical composition of Chinese herbal medicine > Honegsukle flower P.E
Contents
No. 1
  Honeysuckle Extract: honeysuchle flowers extract main components: chlorogenic acid chlorogenic acid
  The main production enterprise (purity 98% chlorogenic acid in Lonicera japonica): Liuyang ATA Natural Product Contact: Hua Liu received mp: 13875855783 jiehua0501@yahoo.com.cn qq: 37144588
  [Appearance]: White fine powder
  [Pharmacology]: the main rich honeysuckle extract of chlorogenic acid, has a broad antibacterial activity, with gallbladder, bleeding, increased white blood cells and antiviral;
  [Application of dosage forms]: injection suppository, lotion, injection, tablets, capsules and so on.
  [Product Save]: Store in a cool dry, dark, avoid high temperature.
  Chlorogenic acid (chlorogenic acid, cga), also known as coffee tannic acid, caffeic acid by (eafeic acid) and quinic acid (quinic acid) reduced the formation of acid, are phenylpropanoid compounds. cga widely in plants, the honeysuckle, Eucommia were higher, with a wide range of pharmacological effects.
  1, the structure of chlorogenic acid
  Chlorogenic acid (chlorogenic acid, hereinafter referred to as ca), molecular formula: c16h18o9, molecular weight: 354.30, by caffeic acid (caffeic acid) and quinic acid (quinic acid, 1 - hydroxy-hexahydro gallic acid) to generate the reduced acid, synonym coffee tannin, the system name 1,3,4,5 - tetrahydroxy cyclohexane carboxylic acid - (3,4 - dihydroxy cinnamate), the chemical name 3-o-caffeoyl quinic acid (3 - o-caffeoylquinic acid), is a plant in the process of aerobic respiration produced by the shikimic acid pathway of a phenylpropanoid compounds.
  Chlorogenic acid structure:
  2, physical and chemical properties of chlorogenic acid
  Honeysuckle extract chlorogenic acid pharmacokinetics
  Absorption: human studies have shown that, cga oral absorption is poor, only a small part of the prototype in the small intestine to absorb most of it into the colon by microbial metabolism of benzoic acid, acrylic acid and cinnamic acid and other substances after being absorbed. Thus, after oral administration of cga in plasma mainly in the form of metabolites. Antibiotics can affect the normal flora of the colon, thereby affecting its intestinal metabolites cga in plasma concentrations. Protein binding: in vitro study found cga with human serum albumin (has) with j, but when combined with different concentrations of different ways: at low concentrations, only one binding site, a member has with a member of cga; high concentration When there are multiple binding sites. The main binding site in the region has the iia. cga plasma protein binding in vivo was still not clear. Metabolism: cga in the body metabolism has not been fully elucidated. olthof other studies have found cga can be metabolized to 3,4-absorbed. Dihydroxybenzoic acid, 3,4 or two hydroxy benzoic acid, 3 a methoxy. 4. Hydroxy benzoic acid and other substances, metabolites of the colon into the plasma, may be further converted to hippuric acid. p450 enzymes may be involved in this process. Excretion: cga and its metabolites in plasma mainly by renal excretion. Oral administration, mainly in the form of metabolites with the urine, of which the highest proportion of hippuric acid, about cga its half of the total metabolites. After intravenous administration, cga two-compartment model in rats showed the distribution, biological half-life tl / 2 of about o. 2o h.
  2 Pharmacodynamics
  Cardiovascular protective effect of 2.1
  2.2 The role of anti-mutagenic and anti-cancer
  Animal experiments show that, cga on the incidence of gastric cancer and colon cancer preventive and inhibitory [10,11]. cga anti-mutagenic and anti-cancer effects may be related to the following factors: promoting oxidation: jiang other study found that cga in an alkaline environment for promoting oxidants, can cause cancer cells to produce large dna fragments, and causes nuclear condensation. This effect may be related to hydrogen peroxide. Enhanced aryl hydrocarbon hydroxylase activity: aromatic hydrocarbon hydroxylase is more important metabolic enzyme, its activity increased more resistant cells will increase the mutagenic effect of aromatic compounds, in vitro study found cga can enhance the activity of aryl hydrocarbon hydroxylase . Inhibition of 8-hydroxy deoxyguanosine (8-oh-dg) formation :8-oh-dg is a cancer and cellular oxidative stress during the important material, which in mammalian cells can induce point mutations. cga inhibited 4-nitroquinoline-1 one. Oxide (4-nitroquinoline a 1-oxide, 4nqo)-induced 8-oh-dg's higher, but endogenous 8-oh-dg level of no effect. Inhibition of carcinogen adducts of a dna 【13,15] and the formation of oxygen free radicals play an anti-cancer effect is the important mechanism. 2.3 Antibacterial and antiviral cga inhibited Escherichia coli, Shigella sonnei (d group), Staphylococcus aureus, Bacillus subtilis, Micrococcus luteus and the growth of Legionella bacteria, the antibacterial mechanism and non-competitive bacteria in vivo inhibition of aromatic amine acetyltransferase (nat) on [16-19]. Hu Kejie other in vitro antiviral activity of the cga found cga significantly inhibited syncytial virus, coxsackie b group 3, adenovirus type 7 and so on, and coxsackie adenovirus type 3 b5 also has a certain type of inhibition . chiang, etc. also found cga adenovirus type 11 with a strong inhibitory effect. The anti-viral mechanisms remain to be elucidated.
  Lipid-lowering effect of 2.4
  Intravenous cga can significantly reduce plasma cholesterol and triglyceride levels, liver triglyceride levels are significantly reduced. Sd rats in the food and coffee while adding cga acid, also found in the lung and liver and other tissues of the vit e and cholesterol levels are decreased.
  2.5-versus-leukemia effect
  chiang and other in vitro studies have found cga weak anti-leukemia activity j. bandyopadhyay other studies have shown that cga inhibited ber-abl and c-abl tyrosine kinase, and induction of ber-abl positive cells, including chronic myeloid leukemia patients in vivo ber-abl-positive primary lymphocytes apoptosis. Also found that nude mice implanted cga ph chromosome positive chronic myeloid leukemia cell line k562 destructive [earthworm.
  Immunomodulatory effects of 2.6
  In vitro studies have shown cga not only significantly enhance the influenza virus antigen induced t cell proliferation and can induce human peripheral blood lymphocytes and generation 7-ifn and a-ifn [26-2s]. cga also improve the rats i, igg1 and 4 in wide il l. In a recent study also found that activation of calcineurin cga (eal-eineurin) to enhance macrophage function.
  2.7 hypoglycemic effect
  andrade-cetto a and wiedenfeld h of the study confirmed, cga has a hypoglycemic effect in animals, 3 h and in the hypoglycemic effect of glibenclamide was no significant difference [31 j. The mechanism may be related to the inhibition of a glucose 6 phosphate displacement of a related enzyme and glucose uptake.
  2.8 Other
  cga can inhibit staphylococcal exotoxin induced cytokine and chemokine production, inhibition of hypertrophic scar fibroblast origin (hypertrophic scar-derived fibroblasts, mfs) fibroblasts caused by the contraction of j and the stress grid reaction due to ACTH (acm) increased. ejzemberg so that cga also has anti-complement effect and prove that this effect is generated through the classical pathway [36j. In addition, cga can affect the concentration of trace elements in plasma. After intravenous injection cga, the phosphorus content in rat plasma decreased significantly, while copper, magnesium, sodium and potassium content was significantly increased l2. This suggests that the clinical application of 3, should pay attention to control electrolyte imbalance.
  3 Drug Interactions
  As mentioned earlier antibiotics can affect the absorption in the gastrointestinal tract cga. Another report, also with antibiotics given intravenously Shuanghuanglian, cga (the active ingredient in one of Shuanghuanglian) and will reduce the excretion of antibiotics, which may be excreted with the competitive channels. cga can inhibit iron ion and the Food and 6 non-heme iron absorption, and promote the absorption of aluminum ions. In vitro studies have shown that, cga p4502b1 can inhibit the activity of rat liver, affecting its substrate 7. Ethoxy-4. Trifluoromethyl. Coumarin (7 an ethoxy-4-trifluoromethyl coumarin) metabolism. Speculated cga may affect the human body corresponding to the activity of cyp 2b6, thereby affecting the metabolism of its substrate, but their clinical significance needs to be further confirmed.
  4 Conclusion
  With the gradual deepening of the cga study, we cga 9 has become even more comprehensive understanding of this for us and the rational use of pharmaceutical science has provided an important theoretical basis. Cga from the current pharmacokinetic study suggests the bioavailability of oral cga low, but also on the activity of microorganisms in the colon. Therefore, the efficacy is best to play cga intravascular administration, and the effects produced by oral cga may be a direct result of its metabolites. In pharmacodynamics, the newly discovered cga significant pharmacological activity. Role, can provide new ideas for drug development. Because of drug interactions, combination therapy in clinical practice when we want to draw attention, such as: Alzheimer's patients, when aluminum ions 12cga while taking the drug and may increase due to increased absorption of aluminum damage the central nervous; The patients with iron deficiency anemia, oral iron supplementation combined with the cga will reduce the effect. cga interaction with antibiotics depends on the results of 13 cga mode of administration, oral administration, the antibiotic can reduce the cga and its metabolites in plasma, thus reducing the efficacy of cga; intravenous administration may be due to reduction of two excretion was enhanced by increasing efficacy or adverse reactions. In conclusion, chlorogenic acid has a variety of pharmacological effects and are widely distributed, accelerate research and development of chlorogenic acid has very important significance.
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No. 2
  Honeysuckle Extract: HoneySuchle Flowers Extract Ingredients: chlorogenic acid chlorogenic acid
  [Appearance]: White fine powder
  [Pharmacology]:
  1. Antimicrobial and enhance immune function: results show that honeysuckle on the typhoid bacillus, paratyphoid bacillus, Escherichia coli, Proteus, Pseudomonas aeruginosa, Bordetella pertussis, Vibrio cholerae, staphylococcus, streptococcus, pneumococcus, Meningococcal so inhibit.
  2, inhibition of drug-resistant protein synthesis: honeysuckle extract against Staphylococcus aureus resistant plants had significant respiratory stimulation, and more for drug-resistant strains led to De-surgical inflammation, such as the treatment of tuberculosis complicated by respiratory tract infections, pneumonia, acute dysentery and diarrhea. Also used to reduce the throat carrier rate.
  Dosage: the amount per hundred kg of body weight of 1 g per gram of active ingredient extract is equivalent to 15 times more raw medicinal herbs. To 20 kg per gram of water is still valid.
  [Application of dosage forms]: injection suppository, lotion, injection, tablets, capsules and so on.
  [Product Save]: Store in a cool dry, dark, avoid high temperature.
  Chlorogenic acid (chlorogenic acid, CGA), also known as coffee tannic acid, caffeic acid by (eafeic acid) and quinic acid (quinic acid) reduced the formation of acid, are phenylpropanoid compounds. CGA widely in plants, the honeysuckle, Eucommia were higher, with a wide range of pharmacological effects.
  1, the structure of chlorogenic acid
  Chlorogenic acid (Chlorogenic acid, hereinafter referred to as CA), Molecular formula: C16H18O9, Molecular weight: 354.30, by caffeic acid (Caffeic acid) and quinic acid (Quinic acid, 1 - hydroxy-hexahydro gallic acid) to generate the reduced acid, synonym coffee tannin, the system name 1,3,4,5 - tetrahydroxy cyclohexane carboxylic acid - (3,4 - dihydroxy cinnamate), the chemical name 3-O-caffeoyl quinic acid (3 - O-caffeoylquinic acid), is a plant in the process of aerobic respiration produced by the shikimic acid pathway of a phenylpropanoid compounds.
  Chlorogenic acid structure:
  2, physical and chemical properties of chlorogenic acid
  Honeysuckle extract chlorogenic acid pharmacokinetics
  Absorption: human studies have shown that, CGA oral absorption is poor, only a small part of the prototype in the small intestine to absorb most of it into the colon by microbial metabolism of benzoic acid, acrylic acid and cinnamic acid and other substances after being absorbed. Thus, after oral administration of CGA in plasma mainly in the form of metabolites. Antibiotics can affect the normal flora of the colon, thereby affecting the CGA and its intestinal metabolite concentrations in plasma. Protein binding: CGA found in vitro with human serum albumin (HAS) with J, but when combined with different concentrations of different ways: at low concentrations, only one binding site, a member of HAS with a member of CGA; high concentration When there are multiple binding sites. With the main part of the IIA in the HAS region. CGA plasma protein binding in vivo was still not clear. Metabolism: CGA metabolism in the body has not been fully elucidated. Olthof and other studies have found CGA can be metabolized to 3,4-absorbed. Dihydroxybenzoic acid, 3,4 or two hydroxy benzoic acid, 3 a methoxy. 4. Hydroxy benzoic acid and other substances, metabolites of the colon into the plasma, may be further converted to hippuric acid. P450 enzymes may be involved in this process. Excretion: CGA and its metabolites in plasma mainly by renal excretion. Oral administration, mainly in the form of metabolites with the urine, of which the highest proportion of hippuric acid, and its metabolite CGA about half of the total. After intravenous administration, CGA in rats showed a two-compartment model distribution, biological half-life tl / 2 of about O. 2O h.
  2 Pharmacodynamics
  Cardiovascular protective effect of 2.1
  2.2 The role of anti-mutagenic and anti-cancer
  Animal experiments show that, CGA on the incidence of gastric cancer and colon cancer preventive and inhibitory [10,11]. CGA anti-mutagenic and anti-cancer effects may be related to the following factors: promoting oxidation: Jiang and other study found that CGA in an alkaline environment for promoting oxidants, can cause cancer cells to produce large DNA fragments, and causes nuclear condensation. This effect may be related to hydrogen peroxide. Enhanced aryl hydrocarbon hydroxylase activity: aromatic hydrocarbon hydroxylase is more important metabolic enzyme, its activity increased more resistant cells will increase the mutagenic effect of aromatic compounds, in vitro study found that CGA can enhance the activity of aryl hydrocarbon hydroxylase . Inhibition of 8-hydroxy deoxyguanosine (8-OH-dG) formation :8-OH-dG is a cancer and cellular oxidative stress during the important material, which in mammalian cells can induce point mutations. A CGA can inhibit 4-nitroquinoline-1. Oxide (4-nitroquinoline a 1-oxide, 4NQO)-induced 8-OH-dG in the higher, but endogenous 8-OH-dG levels had no effect. Inhibition of carcinogen DNA adducts of a 【13,15] and the formation of oxygen free radicals play an anti-cancer effect is the important mechanism. 2.3 Antibacterial and antiviral activity of CGA can inhibit Escherichia coli, Shigella sonnei (D), Staphylococcus aureus, Bacillus subtilis, Micrococcus luteus and the growth of Legionella bacteria, the antibacterial mechanism and non-competitive bacteria in vivo inhibition of aromatic amine acetyltransferase (NAT) on [16-19]. Hu Kejie other in vitro antiviral activity of the CGA found that CGA could significantly inhibit syncytial virus, Coxsackie B group 3, adenovirus type 7 and so on adenovirus type 3 and Coxsackie B5 has some inhibitory effect . Chiang and others also found that adenovirus type 11 CGA has a strong inhibitory effect. The anti-viral mechanisms remain to be elucidated.
  Lipid-lowering effect of 2.4
  Intravenous administration of CGA can decrease plasma cholesterol and triglyceride levels, liver triglyceride levels are also significantly reduced. SD rats in the food while adding CGA and caffeic acid, also found in the lung and liver and other tissues of the Vit E and cholesterol levels are decreased.
  2.5-versus-leukemia effect
  Chiang and other in vitro studies found that CGA has a weak anti-leukemia activity of J. Bandyopadhyay and other studies have shown that CGA inhibits Ber-Abl and c-Abl tyrosine kinase, and induction of Ber-Abl positive cells, including chronic myeloid leukemia patients in vivo Ber-Abl-positive primary lymphocytes apoptosis. Also found that the implanted nude mice CGA Ph chromosome positive chronic myeloid leukemia cell line K562 destructive [earthworm.
  Immunomodulatory effects of 2.6
  In vitro studies have shown that CGA is not only significantly enhance the influenza virus antigen induced T cell proliferation and can induce human peripheral blood lymphocytes and generation 7-IFN and a-IFN [26-2s]. CGA also improve the rats I, IgG1 and IL-Canton 4 in l. In a recent study also found that CGA is able to activate calcineurin (eal-eineurin) to enhance macrophage function.
  2.7 hypoglycemic effect
  Andrade-Cetto A, and Wiedenfeld H of the study confirmed, CGA has a hypoglycemic effect in animals, 3 h and in the hypoglycemic effect of glibenclamide was no significant difference [31 J. The mechanism may be related to the inhibition of a glucose 6 phosphate displacement of a related enzyme and glucose uptake.
  2.8 Other
  CGA can also be caused by inhibition of staphylococcal exotoxins cytokine and chemokine production, inhibition of hypertrophic scar fibroblast origin (hypertrophic scar-derived fibroblasts, mFs) fibroblasts caused by the contraction of J and the stress grid reaction due to ACTH (ACm) increased. Ejzemberg so that CGA also has anti-complement effect and prove that this effect is generated through the classical pathway [36J. In addition, CGA can affect the concentration of trace elements in plasma. After intravenous injection of CGA, the phosphorus content in rat plasma decreased significantly, while copper, magnesium, sodium and potassium content was significantly increased l2. This suggests that the clinical application of 3, should pay attention to control electrolyte imbalance.
  3 Drug Interactions
  As mentioned earlier CGA antibiotics can affect the absorption in the gastrointestinal tract. Another report, also with antibiotics given intravenously Shuanghuanglian, CGA (the active ingredient in one of Shuanghuanglian) and will reduce the excretion of antibiotics, which may be excreted with the competitive channels. CGA can also inhibit the iron ion and the Food and 6 non-heme iron absorption, and promote the absorption of aluminum ions. In vitro studies have shown that, CGA can inhibit the activity of rat liver P4502B1, affecting its substrate 7. Ethoxy-4. Trifluoromethyl. Coumarin (7 an ethoxy-4-trifluoromethyl coumarin) metabolism. Speculated that CGA may affect the human body corresponding CYP 2B6 activity, thereby affecting the metabolism of its substrate, but their clinical significance needs to be further confirmed.
  4 Conclusion
  With the gradual deepening of the CGA study, 9 we CGA has become even more comprehensive understanding of this for us and the rational use of pharmaceutical science has provided an important theoretical basis. CGA from the current pharmacokinetic study suggests the oral bioavailability of CGA low, but also on the activity of microorganisms in the colon. Therefore, the best to play the efficacy CGA intravascular administration, and the effects produced by oral administration of CGA may be a direct result of its metabolites. In pharmacodynamics, the new CGA found significant pharmacological activity. Role, can provide new ideas for drug development. Because of drug interactions, combination therapy in clinical practice when we want to draw attention, such as: Alzheimer's patients, when aluminum ions 12CGA while taking the drug and may increase due to increased absorption of aluminum damage the central nervous; The patients with iron deficiency anemia, oral iron supplementation combined with the CGA will reduce the effect. CGA interaction with antibiotics depends on the results of 13 CGA mode of administration, oral administration, the antibiotic can reduce the CGA and its metabolites in plasma, thus reducing the efficacy of CGA; intravenous administration may be due to reduction of two excretion was enhanced by increasing efficacy or adverse reactions. In conclusion, chlorogenic acid has a variety of pharmacological effects and are widely distributed, accelerate research and development of chlorogenic acid has very important significance.
  Name: different chlorogenic acid B, 4 -
  Second, caffeoylquinic acid
  (1S, 3R, 4R, 5R) -3,4-Bis [[(E) -3 - (3,4-dihydroxyphenyl) prop-2-enoyl] oxy] -1,5-dihydroxycyclohexane-1-carboxylic acid
  Isochlorogenic acid B
  Different chlorogenic acid B
  3,4-Dicaffeoylquinic acid
  CAS No. :14534 -61-3
  Molecular Formula: C25H24O12
  Source: Honeysuckle
  Pharmacological effects: with heat, detoxification, cool breeze cooling effect, with broad-spectrum antimicrobial and antioxidant effect.
  References:
  National Pharmacopoeia Committee. Chinese Pharmacopoeia, Ⅰ Ministry [S]. Beijing: Chemical Industry Press ,2000:177-177.
  Zhongfang Xiao, Pengguang Fang, Lin Huibin, et al. Honeysuckle appearance and inner quality of the relationship between index [J]. Herbs, 1997,20 (1) :42-4
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English Expression
  1. n.:  Honegsukle flower P.E
Related Phrases
Milkvetch Root glycanvegetation extracttraditional Chinese medicine extract
jinhuasu
Containing Phrases
medicine made of two or more ingredients Honegsukle flower P.E