Chlorogenic acid displays several important roles in the therapeutic properties of many herbs, such as antioxidant activity, antibacterial, antiviral, scavenging free radicals and exciting central nervous system. Only about one-third of chlorogenic acid was absorbed in its prototype, therefore, its gut metabolites play a more important role in the therapeutic properties of chlorogenic acid. It is necessary to consider not only the bioactivities of chlorogenic acid but also its gut metabolites. This review focuses on the potential activities and mechanisms of chlorogenic acid and its gut metabolites on central nervous system diseases.
Animals ; Central Nervous System Diseases ; drug therapy ; metabolism ; Chlorogenic Acid ; administration & dosage ; metabolism ; Humans ; Intestines ; drug effects ; metabolism

OBJECTIVEThe objective of this paper is to investigate the pharmacokinetics of Chlorogenic acid (CA)and CA-Baicalin compound after intravenous injection (iv) in rabbits.

METHODTen rabbits were randomly divided into two groups. One group were administered CA (6 mg x kg(-1)) by iv, while the other were treated with CA (6 mg x kg(-1))-baicalin (90 mg x kg(-1)) compound by iv. administration. The concentration of CA in plasma was determined by HPLC. The key parameters of pharmacokinetics were calculated and analyzed by kinetic software.

RESULTBoth Concentration-time courses of CA alone and CA-Baicalin compound were consistent with a two-compartment model after administration. The key pharmacokinetic parameters of CA alone were significantly different from that of CA-Baicalin compound (P < 0.05). Compared with the group treated with CA alone, the group treated with CA-Baicalin compound had dramatic increased in AUC(0-infinity), MRT and T1/2alpha.

CONCLUSIONThere are significant difference between the pharmacokinetics of CA and CA-Baicalin compound in rabbits. Baicalin has impact on the pharmacokinetics of CA in rabbits.

Animals ; Calibration ; Chlorogenic Acid ; administration & dosage ; pharmacokinetics ; Flavonoids ; pharmacology ; Injections, Intravenous ; Linear Models ; Male ; Rabbits ; Tissue Distribution ; drug effects

An LC-MS/MS method was developed and validated for the simultaneous quantification of chlorogenic acid (CGA) and taurocholic acid (TCA) in human plasma using hydrochlorothiazide as the internal standard. The chromatographic separation was achieved on a Hedera ODS-2 column with a gradient elution using 10 mmol·L(-1) of ammonium acetate buffer solution containing 0.5% of formic acid - acetonitrile as mobile phase at a flow rate of 300 μL·min(-1). The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring in negative ESI mode. The method was fully validated over the concentration ranges of 0.1-10 ng·mL(-1) for CGA and 2-150 ng·mL(-1) for TCA. It was successfully applied to a pharmacokinetic study of CGA and TCA in healthy Chinese volunteers after oral administration of Shuanghua Baihe tablets (SBTs). In the single-dose study, the maximum plasma concentration (Cmax), time to reach Cmax (Tmax) and elimination half-life (t1/2) of CGA were (0.763 8 ± 0.542 0) ng·mL(-1), (1.0 ± 0.5) h, and (1.3 ± 0.6) h, respectively. In the multiple-dose study, the Cmax, Tmax and t1/2 of CGA were (0.663 7 ± 0.583 3) ng·mL(-1), (1.1 ± 0.5) h, and (1.4 ± 0.7) h, respectively. For TCA, no significant characteristic increasing plasma TCA concentration-time curve was found in the volunteers after oral administration of SBTs, indicating its complicated process in vivo as an endogenous ingredient.
Adult ; Chlorogenic Acid ; administration & dosage ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; pharmacokinetics ; Female ; Humans ; Male ; Molecular Structure ; Tandem Mass Spectrometry ; methods ; Taurocholic Acid ; administration & dosage ; blood ; pharmacokinetics ; Young Adult

OBJECTIVETo observe the allergenicity of chlorogenic acid (CA) in Qingkailing injection.

METHODCA was administrated to Beagle dogs through intravenous injection, and on experimental allergic sensitization of guinea pigs, it was through intraperitoneal and intravenous injection. The behavioral changes of Beagle dogs and guinea pigs were observed, and changes of the content of histamine, IgE, IgG, IgM, ECP and IL-4 in blood were detected. Then the allergenicity of CA was determined by experimental anaphylactoid and allergic methods.

RESULTThere were no typical behavioral changes and increasement of the content of histamine, IgE, IgG, IgM, ECP and IL-4 in blood.

CONCLUSIONCA can not provoke anaphylactoid and allergic reactions.

Allergens ; adverse effects ; Animals ; Behavior, Animal ; drug effects ; Chlorogenic Acid ; adverse effects ; Dogs ; Drug Hypersensitivity ; blood ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Female ; Guinea Pigs ; Injections ; Male

To explore the new pattern of Chinese medicine solid preparations (CMSP) in vitro dissolution, a method testing the bio-thermal activity in combination with UPLC was used. Microcalorimetry was used to obtain the characteristic metabolic growth power-time curves and a series of biothermodynamic parameters of the inhibition of Staphylococcus aureus by Yinhuang tablet dissolving solutions at the pH 6.8 (phosphate buffer) dissolution medium at different times. From these results, the cumulative dissolution of Yinhuang tablet based on bio-thermal activity was obtained. The dissolution rates of two components of chlorogenic acid and baicalin were determined by UPLC method. Then f2 similar factor method was used to evaluate the relevance of these two methods. The result showed that f2 values all were more than 50, indicating that there is a good correlation between the two methods of measuring the dissolution rate. It is feasible to determine CMSP in vitro dissolution by using bio-thermal activity, and to provide new evaluation methods for controlling the quality of CMSP.
Calorimetry ; methods ; Chlorogenic Acid ; chemistry ; pharmacology ; Chromatography, Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Flavonoids ; chemistry ; pharmacology ; Quality Control ; Solubility ; Staphylococcus aureus ; drug effects ; physiology ; Tablets ; Thermodynamics

To study on the effects of Achyranthes bidentata on Tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in rats in vivo pharmacokinetic behaviors, a method for the simultaneous determination of chlorogenic acid, isoliquiritin, harpagoside and liquiritigenin in rat plasma was established by UPLC-MS/MS. The analysis was performed on a waters Acquity BEH C18 column (2.1 mm x 100 mm, 1.7 microm) with the mixture of acetonitrile and 0.1% formic acid/water as mobile phase, and the gradient elution at a flow rate of 0.3 mL x min(-1). The analytes were detected by tandem mass spectrometry with the electrospray ionization (ESI) source and in the multiple reaction monitoring (MRM) mode. It turned out that the analytes of Tongsaimai pellets groups C(max) and AUC(Q-infinity) values were higher than that with A. bidentata group, and the C(max) values of chlorogenic acid had significantly difference (P < 0.05), the AUC(0-infinity) values of chlorogenic acid and glycyrrhizin had significantly difference (P < 0.05); The T(max) and CL values of two groups had no significantly difference. Results showed that the established method was specific, rapid, accurate and sensitive for the studies of Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic, and A. bidentata have varying degrees of effects on Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic behaviors.
Achyranthes ; chemistry ; Animals ; Chalcone ; administration & dosage ; analogs & derivatives ; blood ; pharmacokinetics ; Chlorogenic Acid ; administration & dosage ; blood ; pharmacokinetics ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Glucosides ; administration & dosage ; blood ; pharmacokinetics ; Glycosides ; administration & dosage ; blood ; pharmacokinetics ; Glycyrrhizic Acid ; administration & dosage ; pharmacokinetics ; Herb-Drug Interactions ; Male ; Pyrans ; administration & dosage ; blood ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry

Influenza virus is a virus causing upper respiratory tract infection disease with high morbidity and mortality. China is considered as an area with high rate of influenza morbidity. Prevention and treatment of influenza currently rely on vaccines and antiviral agents in the world. In addition, traditional Chinese medicines also have been used in clinical for influenza therapy. In vitro anti-influenza virus activities of 10 traditional Chinese medicines were studied by cytopathic effect (CPE). Qingre Jiedu oral liquid (factory H) had strong antiviral activity against influenza virus A/Guangdong Luohu/219/2006 (H1N1); Yinhuang oral liquid had strong antiviral activity against influenza virus A/Hanfang/359/95 and A/Yuefang/243/72 (H3N2). Qingkailing oral liquid (factory G) had strong antiviral activity against influenza virus A/Jifang/15/90 (H3N2). Qingre Jiedu oral liquid (factory H) had strong antiviral activity against influenza virus A/Jifang/15/90, A/Yuefang/243/72 (H3N2) and virus B.
Administration, Oral ; Animals ; Antiviral Agents ; administration & dosage ; pharmacology ; Bridged Bicyclo Compounds, Heterocyclic ; administration & dosage ; pharmacology ; Cell Line ; Chlorogenic Acid ; administration & dosage ; pharmacology ; Cytopathogenic Effect, Viral ; drug effects ; Dogs ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Flavonoids ; administration & dosage ; pharmacology ; Indoles ; administration & dosage ; pharmacology ; Influenza A Virus, H1N1 Subtype ; drug effects ; Influenza A Virus, H3N2 Subtype ; drug effects ; Influenza B virus ; drug effects ; Iridoids ; administration & dosage ; pharmacology

PURPOSE: To evaluate the inhibitory effect of chlorogenic acid on laser-induced choroidal neovascularization (CNV) in a rat model. METHODS: Intraperitoneal injection of chlorogenic acid (10 mg/kg) was inititated one day prior to laser photocoagulation and continued for eight days. Eyes were removed 14 days after laser photocoagulation. Fluorescein angiography was employed at seven and 14 days to assess the CNV lesions, and histological examination was performed. Quantification of CNV size and leakage were performed both in histological sections and fluorescein angiography in order to compare the inhibitory effects of chlorogenic acid on CNV with the results of the control. RESULTS: Histological analysis showed no significant difference in CNV size between the treated and control groups. However, CNV leakage on fluorescein angiography had significantly decreased in the chlorogenic acid-treated group at 14 days after laser photocoagulation compared with that of the control group. In addition, CNV size on fluorescein angiography had significantly decreased in the treated group at seven and 14 days. CONCLUSIONS: These results suggest that chlorogenic acid has anti-angiogenic effects on CNV and may be useful as an inhibitor in the treatment or prevention of neovascular age-related macular degeneration.
Angiogenesis Inhibitors/*administration & dosage ; Animals ; Capillary Permeability/drug effects ; Chlorogenic Acid/*administration & dosage ; Choroid/pathology ; Choroidal Neovascularization/diagnosis/etiology/*physiopathology ; Fluorescein Angiography ; Injections, Intraperitoneal ; Laser Coagulation ; Radiation Injuries ; Rats ; Rats, Inbred BN

OBJECTIVETo study the intestinal absorption kinetics characteristic of the main four active ingredients in Shuanghuanglian oral liquid (SHL) and to investigate the influence of herbal compatibility in SHL on absorption of main effective ingredients.

METHODThe in situ rat circulation model was used to investigate the concentration change differences of the four active components in SHL during perfusion.

RESULTThe absorption quantity of different concentrations of baicalin, chlorogenic acid, phillyrin and forsythoside A ranging from 40-160, 6-24, 3-12, 2.6-10.4 mg x L(-1) respectively was linear with concentration and showed no saturation at high concentration. The absorption rate constant K(a) and the hourly absorption percentages A were essentially unchanged. The pH changing from 5.0-7.43 had little influence on the absorption of phillyrin except baicalin, chlorogenic acid and forsythoside A. The calculated K(a) and A of the four active ingredients had no significant differences from that obtained after perfusing via duodenum, jejunum, ileum and colon; The calculated K(a) and A of baicalin in Scutellariae Radix (SR), chlorogenic acid in Lonicerae Japonicae Flos (LJF) and phillyrin in Forsythiae Fructus (FF) had no significant differences compared with that in SHL, but the calculated K(a) and A of forsythoside A in FF were obviously superior to that in SHL.

CONCLUSIONThe intestinal absorption of the four active ingredients in SHL was mainly passive diffusion and had no difference in different segments of rat intestine; the compatibility of SHL compounds changed the absorption of forsythoside A in FF obviously.

Administration, Oral ; Animals ; Chlorogenic Acid ; analysis ; pharmacokinetics ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; analysis ; pharmacokinetics ; Glucosides ; analysis ; pharmacokinetics ; Glycosides ; analysis ; pharmacokinetics ; Hydrogen-Ion Concentration ; Intestinal Absorption ; drug effects ; Intestines ; drug effects ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo determine the parameters of pharmacokinetics in rabbits, and to provide a scientific basis for clinical application of Yinhuang compound microenema.

METHODHPLC was used to determine the concentrations of chlorogenic acid and baicalin in the plasma samples of rabbits, then analyze these data by the pharmacokinetics program 3P97 to determine the parameters of pharmacokinetics and the compartmental model of both ingredients in Yinhuang compound microenema.

RESULTBaicalin showed two compartment model in rabbits and the main parameters of pharmacokinetics were as follows: t(1/2)alpha of 0.311 h, t(1/2)beta of 1.640 h, AUC of 1.531 x 10(-2) g x h x L(-1), tmax of 0.287 h, Vd of 2.182 L. Chlorogenic acid showed two compartment model in rabbits and the main parameters of pharmacokinetics were as follows: t(1/2)alpha of 0.324 h, t(1/2)beta of 1.206 h, AUC of 2.135 x 10(-2) g x h x L(-1), tmax of 0.317 h,Vd of 2.251 L.

CONCLUSIONThe main components in Yinhuang compound microenema baicalin and chlorogenic acid are absorbed quickly and absolutely after rectal administration, which have good characters of pharmacokinetics.

Animals ; Area Under Curve ; Bupleurum ; chemistry ; Chlorogenic Acid ; blood ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacokinetics ; Enema ; Female ; Flavonoids ; blood ; Lonicera ; chemistry ; Male ; Plants, Medicinal ; chemistry ; Rabbits