tannins and chebulinic-acid

To study effects of chebulinic acid on erythroid and megakaryocytic differentiation in K562 cells.. The benzidine staining method was used to evaluate hemoglobin synthesis; the expression of erythroid specific glycophorin A (GPA) protein and megakaryocytic surface marker CD61 was determined by flow cytometry using fluorescence labeled antibodies; erythroid and megakaryocytic mRNA expression was analyzed by RT-PCR.. During erythroid differentiation induced by butyric acid (BA) or hemin, chebulinic acid not only inhibited the hemoglobin synthesis of BA- and hemin-treated K562 cells in concentration-dependent manner with IC50 of 4 micromol/L and 40 micromol/L respectively, but also inhibited another erythroid differentiation marker acetylcholinesterase at the concentration of 50 micromol/L in the cells either treated or untreated with each erythroid differentiation inducers, whereas chebulinic acid 50 micromol/L did not change GPA protein expression in these cells significantly. When K562 cells were treated with TPA 50 microg/L for 72 h to induce megakaryocytic differentiation, the presence of chebulinic acid 50 micromol/L slightly provoked the decrease of GPA protein expression induced by TPA. Chebulinic acid did not change the TPA-induced CD61 expression at the same concentration. Chebulinic acid also reduced the mRNA levels of erythroid relative genes including gamma-globin, PBGD, NF-E2, and GATA-1 genes in K562 cells either treated or untreated with BA, whereas chebulinic acid upregulated the mRNA levels of GATA-2 transcription factor in these cells.. Chebulinic acid had inhibitory effect on erythroid differentiation likely through changing transcriptional activation of differentiation relative genes, which suggests that chebulinic acid or other tannins might influence the efficiency of some anti-tumor drugs-induced differentiation or the hematopoiesis processes.

Topics: Acetylcholinesterase; Cell Differentiation; DNA-Binding Proteins; Erythrocytes; Erythroid-Specific DNA-Binding Factors; GATA1 Transcription Factor; GATA2 Transcription Factor; Gene Expression Regulation; Globins; Glycophorins; Humans; Hydrolyzable Tannins; Integrin beta3; K562 Cells; Megakaryocytes; NF-E2 Transcription Factor; NF-E2 Transcription Factor, p45 Subunit; RNA, Messenger; Tannins; Transcription Factors

We used the agar dilution method to evaluate the antibacterial effect of Terminalia macroptera leaf (Tml) extract against nine reference and clinical Neisseria gonorrhoeae strains, including penicillin- and tetracycline-resistant and -susceptible strains. Tml possesses anti-N. gonorrhoeae activity against all of the strains and the minimum inhibitory concentrations (MIC) were between 100 and 200 microg ml(-1). We then used a liquid-liquid partition method to divide the Tml extract into five fractions and determined the anti-N. gonorrhoeae activity of each of the fractions. All of the fractions showed antibacterial activity. The most active one was identified as the diethyl ether fraction and had MIC values of between 25 and 50 microg ml(-1) against all of the strains.

Topics: Anti-Bacterial Agents; Benzopyrans; Ellagic Acid; Flavonoids; Gallic Acid; Glucosides; Hydrolyzable Tannins; Luteolin; Neisseria gonorrhoeae; Plant Extracts; Plant Leaves; Tannins; Terminalia

To analyze the hydrolyzable tannins-chebulinic acid (I) and chebulagic acid(II) in Fructus Chebulae and its confusion varieties by using high performance capillary electrophoresis (HPCE) method.. Using a capillary (375 microns OD x 50 microns ID; 81.5 cm x 61.5 cm) and a power supply set at 24 kV, with phosphate-borate buffer containing 20 mmol.L-1 Na2HPO4-60 mmol.L-1 boric acid and a UV detector at 280 nm, sample solution was loaded in decompression mode at the positive end of the capillary, the loading time was 5 s.. The linear ranges of I and II were 0.0842-0.842 and 0.842 and 0.0940-0.940 mg.mL-1 respectively, the correlation coefficient were 0.9966 and 0.9957, the average recoveries were 95.6% (RSD = 4.0%, n = 5) and 95.0% (RSD = 4.4%, n = 5), the RSDs (n = 5) of measurement precision test were 2.2% and 1.7%, the RSDs (n = 6) of reproduction test were 5.4% and 4.0% respectively. The contents of I and II were obviously interrelated with the variety and characteristics of Fructus Chebulae, the contents of I and II in the confusion varieties of Fructus Chebulae were very low.. It is suitable to use I and II as the criterion in quality evaluation of Fructus Chebulae, and the HPCE method is effective for quality evaluation of the crude Fructus Chebulae.

Topics: Benzopyrans; Drug Contamination; Electrophoresis, Capillary; Fruit; Glucosides; Hydrolyzable Tannins; Plants, Medicinal; Quality Control; Tannins; Terminalia

Three hydrolyzable tannins chebulinic acid (I), chebulagic acid(II) and 1,3, 6-tri-O-galloyl-beta-D-glucose (III) in Fructus Chebulae from different habitats were determined by RP-HPLC method. The contents of I and II were obviously interrelated with the variety and characteristics of Fructus Chebulae. It's suitable to use I and II as indexes in quality evaluation of the crude drug of Fructus Chebulae.

Topics: Benzopyrans; Fruit; Glucosides; Hydrolyzable Tannins; Plants, Medicinal; Quality Control; Species Specificity; Tannins; Terminalia

1. The effects of chebulinic acid, which has been shown to elicit blood pressure lowering effect in rats, on aortic vascular contraction as well as cardiac contraction were studied in rats. 2. Chebulinic acid had no effect on KCl-induced aortic contraction, but irreversibly inhibited the contractile responses to phenylephrine in an apparently non-competitive manner. Chebulinic acid also inhibited contractile responses of rat aorta to 5-hydroxytryptamine and angiotensin II. 3. Chebulinic acid inhibited the binding of [3H]-prazosin to dog aortic microsomal membranes in a concentration-dependent manner with an IC50 value of 0.34 mmol/L. Results of saturation binding experiments suggest a mixed mode of inhibition by chebulinic acid (i.e. a decrease in both the maximal number of binding sites and the affinity for prazosin). 4. Chebulinic acid concentration-dependently and reversibly inhibited the maximal left ventricular pressure of rat heart in a Langendorff preparation with 50% inhibition occurring at a concentration of 0.3 nmol/L. 5. We conclude that chebulinic acid exerts non-specific inhibitory actions in vascular preparations. Its inhibitory effect on cardiac contraction was reversible and three orders of magnitude more potent than that on vascular contraction. We suggest that the hypotensive effect of chebulinic acid is probably mediated via the decrease in cardiac output resulting from reduced left ventricular contraction.

Topics: Adrenergic alpha-Antagonists; Animals; Antihypertensive Agents; Aorta, Thoracic; Dogs; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Hydrolyzable Tannins; Hypertension; In Vitro Techniques; Male; Microsomes; Muscle Contraction; Muscle, Smooth, Vascular; Myocardial Contraction; Prazosin; Rats; Rats, Wistar; Tannins