OBJECTIVEThrough establishing the rat model of CIA to evaluate the effect and mechanism of Rhizoma Drynariae Flavone on bone destruction of CIA rat.

METHODSSubcutaneous injection of bovine type II collagen was used to induce Wistar rats to fall ill, and then established the rat model of CIA. The rats whose inflammation scores reached to two points or above were randomly divided into four groups, and were treated accordingly. The effect of Rhizoma Drynariae Flavone on bone destruction was evaluated.

RESULTSAt 12 weeks after treatment, bone trabecular area percentage and bone trabecular number in Rhizoma Drynariae Flavone group, Rhizoma Drynariae Flavone-1/2 Etanercept group, Etanercept group was obviously higher than that of sterilization water group (P < 0.05); and the trabecular resolving power of these groups was obviously less than that of sterilization water group (P < 0.05).

CONCLUSIONRhizoma Drynariae Flavone can obviously inhibit inflammation of joint bone destruction of CIA rats,the effect may be related with bone trabecular number reduction and trabecular resolving power increasing.

Animals ; Arthritis, Experimental ; drug therapy ; pathology ; Bone and Bones ; pathology ; Female ; Flavones ; therapeutic use ; Polypodiaceae ; chemistry ; Rats ; Rats, Wistar

Ultra-high-performance liquid chromatography-Q exactive orbitrap tandem mass spectrometry(UHPLC-QEOrbitrap-MS/MS) was used to explore the inhibitory effect and mechanism of ginkgo flavone aglycone(GA) combined with doxorubicin(DOX) on H22 cells. The effects of different concentrations of GA and DOX on the viability of H22 cells were investigated, and combination index(CI) was used to evaluate the effects. In the experiments, control(CON) group, DOX group, GA group, and combined GA and DOX(GDOX) group were constructed. Then the metabolomics strategy was employed to explore the metabolic markers that were significantly changed after combination therapy on the basis of single medication treatment, and by analyzing their biological significance, the effect and mechanism of the anti-tumor effect of GA combined with DOX were explained. The results revealed that when 30 μg·mL~(-1) GA and 0.5 μmol·L~(-1) DOX was determined as the co-administration concentration, the CI value was 0.808, indicating that the combination of GA and DOX had a synergistic anti-tumor effect. Metabolomics analysis identified 23 metabolic markers, including L-arginine, L-tyrosine and L-valine, mostly amino acids. Compared with the CON group, 22 and 17 metabolic markers were significantly down-regulated after DOX treatment and GA treatment, respectively. Compared with the DOX and GA groups, the treatment of GA combined with DOX further down-regulated the levels of these metabolic markers in liver cancer, which might contribute to the synergistic effect of the two. Five key metabolic pathways were found in pathway enrichment analysis, including glutathione metabolism, phenylalanine metabolism, arginine and proline metabolism, β-alanine metabolism, and valine, leucine and isoleucine degradation. These findings demonstrated that the combination of GA and DOX remarkably inhibited the viability of H22 cells and exerted a synergistic anti-tumor effect. The mechanism might be related to the influence of the energy supply of tumor cells by interfering with the metabolism of various amino acids.
Arginine/therapeutic use* ; Doxorubicin/therapeutic use* ; Flavones/therapeutic use* ; Ginkgo biloba/chemistry* ; Glutathione ; Humans ; Isoleucine/therapeutic use* ; Leucine/therapeutic use* ; Liver Neoplasms/drug therapy* ; Metabolomics/methods* ; Phenylalanine/therapeutic use* ; Proline ; Tandem Mass Spectrometry/methods* ; Tyrosine/therapeutic use* ; Valine/therapeutic use* ; beta-Alanine/therapeutic use*

The present study was designed to isolate and characterize the analgesic compounds of Artemisa sacrorum Ledeb. The EtOAc crude extracts from the aerial parts of Artemisa sacrorum Ledeb were separated by chromatography and the structures of new compounds were elucidated based on spectral analyses. Analgesic activities of the isolated compounds were assessed in rats with hot plate test and paw pressure assay. Two new flavone C-glycosides, named as Sacroroside A and B (Compounds 1 and 2) were isolated from the EtOAc crude extract of the aerial parts ofArtemisa sacrorum Ledeb. They showed significant analgesic effects. In conclusion, Compounds 1 and 2 are new natural products, which show significant analgesic effects in a dose-dependent manner.
Analgesics ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Animals ; Artemisia ; chemistry ; Disaccharides ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Flavanones ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Flavones ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Hot Temperature ; Male ; Molecular Structure ; Pain ; drug therapy ; Phytotherapy ; Plant Components, Aerial ; Plant Extracts ; chemistry ; pharmacology ; therapeutic use ; Pressure ; Rats, Wistar

OBJECTIVETo observe the effects of the extract of Buddleja officinalis eye drops (EBOED) on basic tears secretory volume, tear film stability, and expressions of androgen receptors (AR) in castrated rats with dry eye, and to investigate the mechanism of EBOED on dry eye caused by decreased anti-androgen levels.

METHODSForty-five male Wistar rats were randomly divided into the blank group, the model group, and the treatment group (treated by EBOED), respectively. Rats in each group were further divided into three sub-groups (fed for one month, two months, and three months, respectively). There were totally nine groups, with five in each. The dry eye model was established with orchiectomy of rats in the model group and the treatment group. EBOED was given to rats in the treatment group for one successive month. Schirmer I test (SIT) and breakup time of tear film (BUT) were determined in all experimental rats. Expressions of AR was analyzed by flow cytometer.

RESULTSThs SIT value, BUT, and AR positive rate in the model group at the 1st, 2nd, 3rd month were lower than those in the blank group of the same time points (P < 0.01). There was statistical difference in SIT value, BUT, and AR positive rate between the model group and the treatment group at the three time points (P < 0.01). Take the three-month subgroup as an example, the SIT value in the treatment group was (12.667 +/- 5.221) mm, obviously higher than that in the model group (2.676 +/- 1.987) mm. The BUT in the treatment group was (11.758 +/- 4.415) s, obviously longer than that of the model group (4.667 +/- 2.108) s. The AR positive rate in the treatment group was 49.33% +/- 3.44%, obviously higher than that of the model group (33.32% +/- 7.12%, all P < 0.01).

CONCLUSIONSThe main components of EBOED was the flavonoids which could significantly inhibit the occurrence of dry eye in rats with decreased androgen levels. Its mechanism might possibly be similar to androgen.

Animals ; Buddleja ; chemistry ; Dry Eye Syndromes ; drug therapy ; metabolism ; Flavones ; pharmacology ; therapeutic use ; Lacrimal Apparatus ; metabolism ; Male ; Orchiectomy ; Plant Extracts ; pharmacology ; therapeutic use ; Rats ; Rats, Wistar ; Receptors, Androgen ; metabolism

OBJECTIVETo compare the actions of the three flavone ingredients in choerospondias axillaris on arrhythmias Induced by aconitine.

METHODLangendorff perfuse was applied in the experiment, the antiarrhythmic action was to study by using aconitine on the the isolated heart; The antiarrhythmic action of the three flavone ingredients in choerospondias axillaris was to study by using i.v. aconitine in rat to induce arrhythmias.

RESULTCompared with the NS group, sample 1 and sample 2 both significantly prolonged the beginning time of VF of isolated heart and increased the dosage of aconitine, sample 3 reduced the beginning time of VF of isolated heart and decreased the dosage of aconitine, sample 1 and sample 2 both greatly prolonged the beginning time of VE, VT, VF, HA; sample 3 greatly reduced the beginning time of VT,VF. The actions of the three samples were in a concentration-dependent way.

CONCLUSIONSample 1 and sample 2 both resisted the occurrence of arrhythmias induced by aconitine, sample 3 markedly promoted the occurrence of arrhythmias induced by aconitine.

Aconitine ; Anacardiaceae ; chemistry ; Animals ; Anti-Arrhythmia Agents ; isolation & purification ; therapeutic use ; Arrhythmias, Cardiac ; chemically induced ; prevention & control ; Dose-Response Relationship, Drug ; Female ; Flavones ; isolation & purification ; therapeutic use ; In Vitro Techniques ; Male ; Phytotherapy ; Plants, Medicinal ; chemistry ; Random Allocation ; Rats ; Rats, Wistar

Not only the evolution of the processing of Fructus Crataegi, but also the difference of chemical consitituents, pharmacological effects and clinical application before and after the processing are reviewed, based on 26 references of literature. A way to further study the processing of Fructus Crataegi is provided.
Antidiarrheals ; therapeutic use ; Citric Acid ; analysis ; Crataegus ; chemistry ; Diarrhea ; drug therapy ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; therapeutic use ; Flavones ; analysis ; Fruit ; chemistry ; Hot Temperature ; Humans ; Phytotherapy ; Plants, Medicinal ; chemistry ; Technology, Pharmaceutical ; methods ; Trace Elements ; analysis

OBJECTIVETo observe the effects of Ginkgo Biloba Tablet (GBT) in treating mild cognitive impairment (MCI).

METHODSTotally 113 MCI patients including 58 outpatients at the cognitive impairment clinics of Huadong Hospital, 34 outpatients at Chinese Medicine Clinics of Dongfang Hospital, and 21 outpatients at Feng-lin Community Health Service Center, were assigned to the control group (55 cases) and the treatment group (58 cases). Basic treatment was given to them all. Those in the treatment group took GBT additionally, 1 tablet each time, 3 times a day for 12 successive months. The mini-mental state examination (MMSE) integral, clock drawing task (CDT) integral, MMSE efficacy, CDT efficacy, and dementia conversion rate were detected before treatment, half a year after treatment, and one year after treatment.

RESULTSThere was no significant difference in scores of MMSE and CDT integrals between the two groups before treatment (P>0.05). Compared with before treatment, each score in the treatment group remarkably increased in the treatment group at the 6 months and 12 months after treatment (P<0.01). They were higher than those of the control group at the same time points, showing statistical difference (P<0.01, P<0.05). There was no significant difference in the integrals of MMSE and CDT between the 6 months of treatment and the 12 months of treatment (P>0.05). The total effective rate of MMSE and CDT of the treatment group at the 6 months and 12 months after treatment (MMSE 67.24% and 65.52%; CDT 62.07% and 60.34%) all exceeded those of the control group at the same time points (MMSE 36.36% and 30.91%; CDT 34.55% and 30.91%), showing significant difference (P<0.01). There was no difference in the total effective rate of MMSE and CDT of the treatment group between the two time points (P>0.05). The dementia conversion rates at the 6 months and 12 months after treatment (1.72% and 5.17%) were lower in the treatment group than in the control group (9.09% and 14.55%), showing statistical difference (P<0.05).

CONCLUSIONSOne-year GBT could significantly improve the cognitive function of MCI patients. It could also lower the dementia conversion rate.

Aged ; Aged, 80 and over ; Cognition ; Cognitive Dysfunction ; drug therapy ; psychology ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Female ; Flavones ; pharmacology ; therapeutic use ; Ginkgo biloba ; Humans ; Male ; Middle Aged ; Neuropsychological Tests ; Phytotherapy ; Tablets

OBJECTIVETo study the active fraction and constituents from Potentilla chinesis.

METHODTested fractions were obtained by different solvent-partition from 95% ethanol-extracts of P. chinesis, and tested compound was isolated by repeated chromatography. Anti-diabetes experiment was taken by using alloxan-induced diabetic mice.

RESULTThe fraction F and the tested compound revealed obvious difference comparing with the control group (P <0.01).

CONCLUSIONFraction F and potentilla flavone revealed the significant hypoglycemic effect in alloxan-induced diabetic mice.

Animals ; Blood Glucose ; metabolism ; Diabetes Mellitus, Experimental ; blood ; drug therapy ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; therapeutic use ; Female ; Flavones ; Flavonoids ; pharmacology ; Hypoglycemic Agents ; chemistry ; pharmacology ; therapeutic use ; Male ; Mice ; Potentilla ; chemistry

OBJECTIVETo investigate the effect of nebulized total ginkgo flavone glycosides (TFG) on Th1/Th2 imbalance in mice with athma.

METHODForty-eight BALB/C mice were randomly divided into four groups: group A (control group, n=12); group B (asthmatic model group, n=12); group C (TFG nebulized treated group, n=12); group D (dexamethasone intraperitoneal treated group, n=12). The asthmatic model was established by sensitivity and local activation with Ovalbumin(OVA) and aluminum hydroxide Al(OH)3. TFG (50 g x L(-1), per aerosol per six mice, 30 minutes) was nebulized 20 days after modeling, while dexamethasone (1 g x L(-1)) was intraperitoneal once daily for 10 days. Perfusate of bronchoalveolar lavage fluid(BALF) was collected on day 32. The level of IL-4, IFN-gamma in BALF, and the level of total IgE in serum was determined. The airway inflammation pathology change and the expression of GATA-3 protein in lungs was detected by immunohistochemical staining.

RESULTCompared with model group, the decreased content of IL-4(49.30 +/- 7.95) ng x L(-1) and increased level of IFN-gamma (49.08 x 5.46) ng x L(-1). were found in BALF, and the level of total IgE (9.47 +/- 1.52) microg x L(-1) in serum also decreased in TFG treated group. In model group, smooth muscle hypertrophing, mucous hyperemia, mucous layer thickening, and inflammatory cell in filtration were observed. Phlegmasia was appeared in the bronchi, which was filled with lots of mucus. In contrast, the inflammatory reaction in TFG and Dexamethasone treated group was less obvious. Expression of GATA-3 was markly increased in model group with decreased expression in TFG treated group.

CONCLUSIONNebulized TFG showed a therapeutic effect for asthmatic mice, the mechanism may be explained by blockingnnnn GATA-3 expression and regulating the disorder Th1/Th2 imbalance.

Aluminum Hydroxide ; pharmacology ; Animals ; Asthma ; chemically induced ; drug therapy ; metabolism ; pathology ; Bronchoalveolar Lavage Fluid ; chemistry ; Dexamethasone ; therapeutic use ; Drugs, Chinese Herbal ; chemistry ; therapeutic use ; Female ; Flavones ; Flavonoids ; chemistry ; GATA3 Transcription Factor ; metabolism ; Ginkgo biloba ; chemistry ; Glycosides ; chemistry ; therapeutic use ; Immunoglobulin E ; blood ; Interferon-gamma ; metabolism ; Interleukin-4 ; metabolism ; Lung ; drug effects ; metabolism ; Male ; Mice ; Mice, Inbred BALB C ; Ovalbumin ; pharmacology ; Random Allocation ; Th1 Cells ; drug effects ; metabolism ; Th2 Cells ; drug effects ; metabolism

OBJECTIVETo study the expression of uncoupling protein 2 (UCP2) in liver of rats with nonalcoholic steatohepatitis (NASH) induced by fat-rich diet, and the effect of total flavones of hawthorn leafon (TFHL) on UCP2.

METHODThe NASH model of rat was induced by 12 weeks of fat-rich diet. Subsequently the rats were administrated with TFHL in accordance with 250, 125 mg x kg(-1) x d(-1) and the Essentiale N with 195.4 mg x kg(-1) x d(-1). The change of liver pathological. The levels of serum ALT and AST, the content of TG, CHOL, MDA and T-AOC activity of liver and were evaluated. The UCP2mRNA expression in liver was detected with RT-PCR, and the contents of UCP2 were examined with ELISA.

RESULTThere are severe steatosis, inflammatory cellular infiltration in the liver of the NASH models. The levels of serum ALT, AST and the contents of TG, CHOL, MDA and UCP2 in the model group were higher than those of in the normal groop. The expression of UCP2mRNA was obviously enhanced and the activity of T-AOC decreased. The expression of UCP2 mRNA of rats was positively correlation with the contents of MDA, TNF-alpha. The inflammation activity in rat liver, the contents of MDA and UCP2, the expression of UCP2 mRNA in the administrated groups were obviously lower than those in the model group, while the activity of T-AOC was higher than that of model.

CONCLUSIONTFHL may alleviate liver injury by means of the suppression of Oxidative stress/lipid peroxidation reaction and the overexpression of UCP2 in liver, which could prevent the further development of NASH.

Animals ; Crataegus ; chemistry ; Enzyme-Linked Immunosorbent Assay ; Fatty Liver ; drug therapy ; metabolism ; Flavones ; chemistry ; therapeutic use ; Gene Expression ; drug effects ; Ion Channels ; genetics ; Liver ; drug effects ; metabolism ; Male ; Mitochondrial Proteins ; genetics ; Plant Leaves ; chemistry ; Polymerase Chain Reaction ; Rats ; Rats, Sprague-Dawley ; Uncoupling Protein 2