RESUMEN
This study aimed to analyze the antiarthritic activity of ginkgolic acid against the Complete Freund's Adjuvant (CFA)-induced arthritis in rats. Arthritis was induced through an intradermal injection of CFA (0.1 mL) at the right hind footpad of adult Wistar Albino rats. Ginkgolic acid was administered orally at doses of 25 mg/kg and 50 mg/kg, respectively, once daily via gavage for 25 days upon inducing arthritis. Indomethacin was administered orally at a dose of 3 mg/kg twice in a week which served as positive control group. The animals were sacrificed and subjected to biochemical and histopathological analysis upon completion of treatment. Ginkgolic acid was able to reverse the arthritic effect (p < 0.01) induced by CFA in a dose dependent manner. Swelling of paw, thymus and spleen index, serum biomarker levels, and pro-inflammatory cytokines were significantly reduced (p < 0.01) by the acid whereas the antioxidant enzyme activities were remarkably restored. The histopathological findings were in agreement with the biochemical results. The results indicate that the antioxidant and anti-inflammatory properties of ginkgolic acid can be credited to the antiarthritic effects, and it can be promoted as a potential agent for therapeutic use against osteoarthritis
Asunto(s)
Animales , Masculino , Ratas , Artritis Experimental/inducido químicamente , Adyuvante de Freund/agonistas , Osteoartritis/patología , Inyecciones Intradérmicas , Indometacina , Antioxidantes/clasificaciónRESUMEN
objective To develop a new method for the adsorption and separation of ginkgolic acid (GA). Methods Using salicylic acid (SA) as a dummy template and 4-vinylpyridine as the functional monomer, molecularly imprinted polymer (MIP) with high adsorbability to GA was synthesized by molecular self-assembly technique. The imprinting mechanism of the polymers was studied by 1H-NMR and IR spectra, and the structure of the polymers was characterized by SEM. The structure of the polymer was analyzed by FT-IR and the adsorption and binding properties of the polymer to total GA were analyzed by HPLC and UV detection. Results MIP had better three-dimensional space structure and adsorption properties. Template molecules were binded to functional monomers with noncovalent bonds. The adsorption rate of GA by polymer MIP in the extract of Ginkgo biloba was 95.9%. The Scatchard analysis reveals that there were two different recognition sites in MIP in the extract of G. biloba, and the apparent maximal combination amount (Qmax1) was 30 mg/g in high affinity recognition sites and with (Qmax2) = 80 mg/g in low affinity recognition sites. And the adsorption kinetics can be best described as the pseudo-second-order kinetics model. Conclusion The preparation of MIP with SA as dummy template has strong adsorption properties for GA, which has a good prospect of popularization and application in the separation and purification of GA.
RESUMEN
An analytical method was developed for determination of ginkgolic acids in Yinxing Tongzhi Dropping Pills by ultra high performance liquid chromatography-triple quadrupole mass spectrometry. The samples were purified by mix-mode anion exchange and reversed-phase SPE. A chromatographic column, Waters Cortecs T3 (50 mm×2.1 mm, 2.7 μm), was used with acetonitrile-methanol-1% acetic acid (44:44:12) as the mobile phase. The ginkgolic acids were detected by electrospray ionization mass spectrometry in negative mode with multiple reaction monitoring (MRM) mode. Ginkgolic acid C13:0, C15:1 and C17:1 possessed good linear correlation in the mass concentration range from 0.2 to 200 μg·L-1, 2 to 200 μg·L-1, 4 to 200 μg·L-1, respectively, with the correlation coefficients more than 0.999. The mean recoveries at spiked levels of 50, 250 and 600 μg·kg-1 were in the range of 70.8%-95.1%, and the RSDs were 0.7%-8.6%. The limits of quantification were 1, 10, 20 μg·kg-1, respectively. The method could be applied to the analysis of ginkgolic acids in complex matrix samples.
RESUMEN
Pharmacological activities and adverse side effects of ginkgolic acids (GAs), major components in extracts from the leaves and seed coats of Ginkgo biloba L, have been intensively studied. However, there are few reports on their hepatotoxicity. In the present study, the metabolism and hepatotoxicity of GA (17 : 1), one of the most abundant components of GAs, were investigated. Kinetic analysis indicated that human and rat liver microsomes shared similar metabolic characteristics of GA (17 : 1) in phase I and II metabolisms. The drug-metabolizing enzymes involved in GA (17 : 1) metabolism were human CYP1A2, CYP3A4, UGT1A6, UGT1A9, and UGT2B15, which were confirmed with an inhibition study of human liver microsomes and recombinant enzymes. The MTT assays indicated that the cytotoxicity of GA (17 : 1) in HepG2 cells occurred in a time- and dose-dependent manner. Further investigation showed that GA (17 : 1) had less cytotoxicity in primary rat hepatocytes than in HepG2 cells and that the toxicity was enhanced through CYP1A- and CYP3A-mediated metabolism.
Asunto(s)
Animales , Humanos , Ratas , Células Cultivadas , Citocromo P-450 CYP1A2 , Metabolismo , Citocromo P-450 CYP3A , Metabolismo , Ginkgo biloba , Química , Glucuronosiltransferasa , Metabolismo , Hepatocitos , Química , Metabolismo , Cinética , Hígado , Química , Metabolismo , Microsomas Hepáticos , Química , Metabolismo , Extractos Vegetales , Química , Metabolismo , Toxicidad , Ratas Sprague-Dawley , Salicilatos , Química , Metabolismo , ToxicidadRESUMEN
Pharmacological activities and adverse side effects of ginkgolic acids (GAs), major components in extracts from the leaves and seed coats of Ginkgo biloba L, have been intensively studied. However, there are few reports on their hepatotoxicity. In the present study, the metabolism and hepatotoxicity of GA (17 : 1), one of the most abundant components of GAs, were investigated. Kinetic analysis indicated that human and rat liver microsomes shared similar metabolic characteristics of GA (17 : 1) in phase I and II metabolisms. The drug-metabolizing enzymes involved in GA (17 : 1) metabolism were human CYP1A2, CYP3A4, UGT1A6, UGT1A9, and UGT2B15, which were confirmed with an inhibition study of human liver microsomes and recombinant enzymes. The MTT assays indicated that the cytotoxicity of GA (17 : 1) in HepG2 cells occurred in a time- and dose-dependent manner. Further investigation showed that GA (17 : 1) had less cytotoxicity in primary rat hepatocytes than in HepG2 cells and that the toxicity was enhanced through CYP1A- and CYP3A-mediated metabolism.
Asunto(s)
Animales , Humanos , Ratas , Células Cultivadas , Citocromo P-450 CYP1A2 , Metabolismo , Citocromo P-450 CYP3A , Metabolismo , Ginkgo biloba , Química , Glucuronosiltransferasa , Metabolismo , Hepatocitos , Química , Metabolismo , Cinética , Hígado , Química , Metabolismo , Microsomas Hepáticos , Química , Metabolismo , Extractos Vegetales , Química , Metabolismo , Toxicidad , Ratas Sprague-Dawley , Salicilatos , Química , Metabolismo , ToxicidadRESUMEN
OBJECTIVE: To develop an HPLC method for simultaneous determination of ginkgolic acids(C13:0, C15:1, C17:2, C15:0, C17:1) in Ginkgo Folium. METHODS: The HPLC analysis was carried out on Phenomenex Luna C18(4.6 mm × 250 mm, 5 μm) column with acetonitrile-0.1% phosphoric acid (90:10) as mobile phase eluted at the flow rate of 1.0 mL · min-1. The detective wavelength was set at 310 nm, and the column temperature was set at 30℃. RESULTS: The calibration curve was linear within the range of 1.47-29.40 μg · mL-1 for C13:0, 6.05 -121.00 μg · mL-1 for C15:1 and 8.00 - 160.00 μg · mL-1 for C17:1, respectively. The average recoveries for the three marker compounds are 98.6% - 100.1%. CONCLUSION: This method is simple, accurate, and practical for the quality control of Ginkgo Folium. There are some differences in the contents of the five marker compounds from different producing areas and different collection periods.
RESUMEN
Objective:To develope a method for the separation and preparation ginkgolic acid ? 1. Methods: Ginkgolic acids were extracted by alcohol, and adsorbed by silica gel to remove most of the polar impurities. It was preparated with RP HPLC. Results: The extraction ratio of ginkgolic acid ? 1 by this extraction process was above 84%, and the purity of ginkgolic acid ? 1 reached 98%. Conclusion: This procedure is simple and relatively effective.
RESUMEN
Objective To study the acute toxicity of ginkgolic acids from Ginkgo biloba sarcotestas against fish.Methods The ginkgolic acid mixture was obtained from Ginkgo biloba sarcotestas.The acute toxicities of the ginkgolic acid mixture against the fry of Cyprinus carpio var.and fry of Carassius auratus were detected.Results LC50 and LC90 of the ginkgolic acid mixture against the fry of Cyprinus carpio var.were 1.805 mg/L and 2.191 mg/L,respectively.LC50 and LC90 of the ginkgolic acid mixture against the fry of Carassius auratus were 1.930 mg/L and 2.217 mg/L,respectively.Conclusions The toxicity of ginkgolic acids against the fry of Cyprinus carpio var.and fry of Carassius auratus is medium.