The recent progresses on chemical components and pharmacological activities of the genus Gentiana were summarized. The main chemical constituents of this genus are iridoids, xanthone and flavone. There were more than ninety iridoid compounds, one hundred xanthone compounds, and thirty four flavone compounds isolated up till now. And flavone compounds were obtained mainly from aerial part. The plants of this genus had broad bioactivities such as antifungal activity, anti-inflammatory activity and liver protective effect. These mentioned above would be helpful for further studies on the plants of the genus Gentiana.
Animals ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Flavones ; Flavonoids ; chemistry ; pharmacology ; Gentiana ; chemistry ; Humans ; Xanthones ; chemistry ; pharmacology

OBJECTIVETo investigate the possible mechanisms of nobiletin for anticancer by studying the inhibition effects of nobiletin on tubulin polymerization.

METHODIn vitro nobiletin was added into the tubulin polymerization-depolymerization system and the absorption values were recorded at 350 nm under 37 degrees C.

RESULTAs compared with controls, the absorption values in reaction system decreased significantly in nobiletin treatment groups. When nobiletin final concentrations in reaction system were 5.0, 7.5, 10.0 and 12.5 micromol x L(-1), the maximum absorption values were 0 130, 0.109, 0.086 and 0.071 with 16.7%, 30.1%, 44.9% and 54.5% of inhibition rate, respectively. The results suggested that nobiletin could inhibit tubulin polymerization.

CONCLUSIONThe inhibition effect of nobiletin on tubulin polymerization is the possible mechanism for anticancer.

Animals ; Flavones ; pharmacology ; Protein Binding ; drug effects ; Swine ; Tubulin ; chemistry ; metabolism ; Tubulin Modulators ; pharmacology

Flavone compound is a polyphenolic compound widely existing in plants and has an extensive biological activity. In recent years, it has been found to have a significant anti-cancer effect, as in combating cell proliferation, inducing cell apoptosis, interfering with cellular signal transduction, increasing the activity of the cancer repressor gene and inhibiting the expression of oncogene. This paper reviews the mechanism by which flavone compound, induces the apoptosis of prostate cancer cells.
Animals ; Apoptosis ; drug effects ; Flavones ; pharmacology ; Humans ; Male ; Prostatic Neoplasms ; pathology ; Rats ; Tumor Cells, Cultured

Athletes ; Exercise ; Flavones/pharmacology* ; Humans ; Hydrocortisone/blood* ; Resistance Training ; Stress, Physiological/drug effects*

OBJECTIVETo observe the metabolism-based interaction of diphenytriazol and flavone compounds.

METHODSFlavone compounds kaempferol, isoharmnten and Elsholtzia blanda benth extract were chosen as the substrate of glucuronidation in the phase II metabolism. The metabolism was investigated in different rat liver microsome incubates pretreated with beta-naphthoflavone (BNF), diphenytriazol and tea oil (control). The concentrations of residual substrate were determined by HPLC. Quercetin and kaempferol were coincubated with diphenytriazol in control microsome to evaluate the inhibition for phase I metabolism. The concentration of diphenytriazol was determined by HPLC.

RESULTThe phase II metabolic activity of kaempferol, isoharmnten and Elsholtzia blanda benth extract in diphenytriazol-treated microsome was more potent than that in BNF-treated microsome (P<0.01). The phase I metabolism of diphenytriazol was markedly inhibited by quercetin and kaempferol, with the inhibition constants (Ki) (12.41 +/-0.26)microg . ml(-1) and (7.97 +/-0.08)microg . ml(-1), respectively.

CONCLUSIONDiphenytriazol demonstrates metabolism-based interaction with flavone compounds in vitro.

Abortifacient Agents ; metabolism ; pharmacology ; Animals ; Drug Interactions ; Female ; Flavones ; metabolism ; pharmacology ; Kaempferols ; metabolism ; pharmacology ; Plant Extracts ; pharmacology ; Quercetin ; metabolism ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Triazoles ; metabolism ; pharmacology

OBJECTIVETo study chemical constituents of Incarvillea arguta and their accelerating PC-12 cell differentiation.

METHODThe constituents were isolated and repeatedly purified on silica gel column chromatography, and were identified on the basis of physicochemical and spectroscopic analysis. The neurotrophic activity of different portion and all purified compounds from I. arguta was determined on the model of PC-12 cell.

RESULTFive compounds were isolated from BuOH portion of alcohol extraction of I. arguta. Their structures were identified as plantarenaloside (I), 5-hydroxy-4', 6 7-trimethoxy-flavone (II), 4', 5-dihydroxy-6, 7-dimethoxyflavone (III), 4', 5-dihydroxy-7-methoxyflavone (IV), 5-dydroxy-4', 7-dimethoxyflavone (V).

CONCLUSIONCompound I is isolated from the plant for the first time and it has neurotrophic activity for PC-12 cell. Compounds II approximately V are isolated from the genus Incarvillea for the first time.

Animals ; Apigenin ; isolation & purification ; pharmacology ; Bignoniaceae ; chemistry ; Cell Transformation, Neoplastic ; drug effects ; Flavones ; isolation & purification ; pharmacology ; PC12 Cells ; Rats

Along with the deep-going researches on mechanism of apoptosis, the apoptosis inducers as anticancer drugs have been the hot points of researches for new drugs. In this paper are reviewed a number of related articles on the progress in cell apoptosis inducers including the derivative anthraquinone, saponin, flavonids and terpines. The mechanisms are analyzed and discussed. The researches into the molecular mechanisms of inducer can provide the theoretical basis for discovering new compound, and can find out the apoptosis inducers with high efficiency and low toxicity. There is hope of developing apoptosis inducers into safe and effectual anticancer drugs.
Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Diterpenes, Abietane ; Emodin ; pharmacology ; Flavones ; pharmacology ; Humans ; Neoplasms ; drug therapy ; metabolism ; pathology ; Phenanthrenes ; pharmacology ; Saponins ; pharmacology

OBJECTIVETo evaluate influence of assemble flavone of rhizome drynaria (AFDR) on the value of the blood serum alkalinity phosphatase (ALP), calcium (Ca), phosphorus (P), creatinine (Cr) and glutamic-pyruvic transaminase (GPT) in rats model with skull defects.

METHODSSixty SD male rats with age of 6-month were feeded for a week and then were randomly divided into control group and AFDR group, with 30 rats in each group. Left and right skull of rats were perforated with electromotive drill and the model of skull defects was made. Injectable bone regeneration vomposite (IBRC) was implanted right skull defects. The rats of control group and AFDR group were respectively lavaged with AFDR and deionized water at the first day after operation. The rats were respectively killed at the 2nd,4th and 8th week and the blood serum ALP, Ca, P, Cr, GPT were detected and analyzed by statistics.

RESULTSAt the 2nd week after operation, blood serum ALP in AFDR group was higher than that of control group. At the 4th week after operation, blood serum Ca, P, and calcium-phosphorus product in AFDR group was higher than that of control group; there was no significant difference in GPT between two groups. At the 8th week after operation, blood serum Cr in AFDR group was lower than that of control group.

CONCLUSIONWhen AFDR is used in the repairing of bone defect for 2-4 weeks, it may affect the level of ALP, Ca, P, and without toxicity to liver and kindey.

Alkaline Phosphatase ; blood ; Animals ; Calcium ; blood ; Flavones ; pharmacology ; Male ; Phosphorus ; blood ; Polypodiaceae ; chemistry ; Rats ; Rats, Sprague-Dawley ; Skull ; injuries ; surgery

OBJECTIVETo study on the chemical constituents of Lobelia chinensis.

METHODThe coloumn chromatographic techniques were applied to isolate constituents, and their structures were elucidated by means of spectral data analysis.

RESULTSixteen compounds were isolated and identified as daucosterol (1), diosmetin (2), apigenin (3), chrysoeriol (4), loteolin (5), hesperidin (6), loteolin-7-O-beta-D-glucoside (7), apigenin-7-O-beta-D-glucoside (8), linarin (9), diosmin(10), 5,7-dimethoxy-8- hydroxycoumarin (11), palmitinic acid (12), lacceroic acid (13), stearic acid (14), beta-sitosterol (15), daucosterol (16).

CONCLUSIONAll of these compouds were obtained from L. chinensis for the first time.

Apigenin ; analysis ; Cholestenones ; analysis ; Flavones ; Flavonoids ; analysis ; Glycosides ; analysis ; Hesperidin ; analysis ; Lobelia ; chemistry ; Plant Extracts ; pharmacology ; Sitosterols ; analysis

Renal tubular injury in patients with diabetic kidney disease(DKD) may be accompanied by glomerular and microvascular diseases. It plays a critical role in the progression of renal damage in DKD, and is now known as diabetic tubulopathy(DT). To explore the multi-targeted therapeutic effects and pharmacological mechanisms in vivo of total flavones of Abelmoschus manihot(TFA), an extract from traditional Chinese medicine for treating kidney disease, in attenuating DT, the authors randomly divided all rats into four groups: a normal control group(normal group), a DT model group(model group), a DT model+TFA-treated group(TFA group) and a DT model+rosiglitazone(ROS)-treated group(ROS group). The DT rat model was established based on the DKD rat model by means of integrated measures. After successful modeling, the rats in the four groups were continuously given double-distilled water, TFA suspension, and ROS suspension, respectively by gavage every day. After 6 weeks of treatment, all rats were sacrificed, and the samples of their urine, blood, and kidneys were collected. The effects of TFA and ROS on various indicators related to urine and blood biochemistry, renal tubular injury, renal tubular epithelial cell apoptosis and endoplasmic reticulum stress(ERS), as well as the activation of the protein kinase R-like endoplasmic reticulum kinase(PERK)-eukaryotic translation initiation factor 2α(eIF2α)-activating transcription factor 4(ATF4)-C/EBP homologous protein(CHOP) signaling pathway in the kidney of the DT model rats were investigated. The results indicated that hypertrophy of renal tubular epithelial cells, renal tubular hyperplasia and occlusion, as well as interstitial extracellular matrix and collagen deposition occurred in the DT model rats. Moreover, significant changes were found in the expression degree and the protein expression level of renal tubular injury markers. In addition, there was an abnormal increase in tubular urine proteins. After TFA or ROS treatment, urine protein, the characteristics of renal tubular injury, renal tubular epithelial cell apoptosis and ERS, as well as the activation of the PERK-eIF2α-ATF4-CHOP signaling pathway in the kidney of the DT model rats were improved to varying degrees. Therein, TFA was superior to ROS in affecting the pathological changes in renal tubule/interstitium. In short, with the DT model rats, this study demonstrated that TFA could attenuate DT by multiple targets through inhibiting renal tubular ERS-induced cell apoptosis in vivo, and its effect and mechanism were related to suppressing the activation of the PERK-eIF2α-ATF4-CHOP signaling pathway in the kidney. These findings provided preliminary pharmacological evidence for the application of TFA in the clinical treatment of DT.
Rats ; Animals ; Abelmoschus ; Reactive Oxygen Species/metabolism* ; Flavones/pharmacology* ; Endoplasmic Reticulum Stress ; Diabetic Nephropathies/drug therapy* ; Apoptosis ; Diabetes Mellitus