OBJECTIVETo study chemical constituents contained in Phymatopteris hastate and their antioxidant activity.

METHODChemical constituents were separated and purified from P. hastate by using such methods as silica gel, Toyopearl HW-40C and HPLC preparative chromatography. Their structures were identified by spectroscopic methods such as NMR. Furthermore, 1, 1-diphenyl-2-picryl-hydrazyl(DPPH) method was used to assess the antioxidant activity of each compound.

RESULTFourteen compounds were separated and identified as 4-O-beta-D-glucopyranosyl-ethyl-trans-caffeicate (1), kaempferlo-7-O-alpha-L-rhamnopyranside (2), kaempferol-3, 7-di-O-alpha-L-rhamnopyranoside (3), kaempferol-3-O-alpha-L-arabinofuranosyl-7-O-alpha-L-rhamnopyranoside (4), juglanin (5), naringin (6), naringenin-7-O-beta-D-glucopyranoside (7), trans-caffeic acid (8), trans-caffeic acid-3-O-beta-D-glucopyranoside (9), trans-cinnamic acid-4-O-beta-D- glucopyranoside (10), trans-melilotoside (11), cis-melilotoside (12), ethyl chlorogenate (13), protocatechuic acid (14). The antioxidation experiment showed an obvious antioxidant activity in compounds 1-9, 13-14.

CONCLUSIONAll of the compounds were separated from this genus for the first time. Among them, compound 1 was not seen in literature reports and assumed to be a new artifact derived from compound 9 and ethanol. Compounds 1-9, 13-14 showed a remarkable antioxidant activity.

Antioxidants ; pharmacology ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; analysis ; pharmacology ; Flavanones ; analysis ; Kaempferols ; analysis ; Magnetic Resonance Spectroscopy

The objective of this study was to investigate the protection by naringenin against doxorubicin-induced oxidative damage in normal blood cells. Inhibiting effects of naringenin, doxorubicin and naringenin combined with doxorubicind on K562 cells and polymorphonuclear leukocytes were detected with MTT method, the level of reactive oxygen species (ROS) and lipid peroxidation (MDA), the activity of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) were examined with spectrophotometric method in the K562 cells and polymorphonuclear leukocytes. The results indicated that the proliferation of K562 cells was not inhibited by the cytotoxicity of doxorubicin in combination of naringenin with doxorubicin. As compared with the doxorubicin, the addition of naringenin after doxorubicin for 1 hour, the levels of reactive oxygen species (ROS) and lipid peroxidation (MDA) obviously decreased, the activity of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) obviously increased in the polymorphonuclear leukocytes, but these were not changed obviously in K562 cells. It is concluded naringenin can protect against doxorubicin-induced oxidative damage in normal blood cells. The mechanism of naringenin may be elevating activities of antioxidant enzyme and degrading oxidative production level in normal blood cells, and meanswhile decreasing level of oxidative products.
Antioxidants ; pharmacology ; Doxorubicin ; adverse effects ; Erythrocytes ; drug effects ; Flavanones ; pharmacology ; Humans ; Oxidative Stress ; Reactive Oxygen Species ; metabolism ; Superoxide Dismutase ; metabolism

Flavonoids are a widely distributed group of phytochemicals having benzo-pyrone nucleus, and more than 4,000 different flavonoids have been described and categorized into flavonols, flavones, flavanones, isoflavones, catechins and anthocyanidins. Flavonoids occurs naturally in fruits, vegetables, nuts, and beverages such as coffee, tea, and red wine, as well as in medical herbs. Flavonoids are responsible for the different colors of plant parts and are important constituents of the human diet. Flavanoids have different pharmacological activities, such as antioxidant, anti-allergic, antibacterial, anti-inflammatory, antimutagenic and anticancer activity. Naringenin belongs to the flavanones and is mainly found in fruits (grapefruit and oranges) and vegetables. Pharmacologically, it has anticancer, antimutagenic, anti-inflammatory, antioxidant, antiproliferative and antiatherogenic activities. Naringenin is used for the treatments of osteoporosis, cancer and cardiovascular diseases, and showed lipid-lowering and insulin-like properties. In the present review, detailed pharmacological and analytical aspects of naringenin have been presented, which revealed the impressive pharmacological profile and the possible usefulness in the treatment of different types of diseases in the future. The information provided in this communication will act as an important source for development of effective medicines for the treatment of various disorders.
Anti-Inflammatory Agents ; chemistry ; pharmacology ; Antineoplastic Agents ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Flavanones ; chemistry ; pharmacology ; Humans ; Isoflavones ; chemistry ; pharmacology ; Neoplasms ; drug therapy

OBJECTIVETo compare the effects of 8-prenylnaringenin (PNG) and naringenin (NG) on the activity and apoptosis of osteoclasts cultured in vitro, in order to study physiological activity of 8-prenyl perssad.

METHODOsteoclasts were separated from long-limb bones of newly born rabbits, cultured in alpha-MEM containing 10% FBS, and then added with PNG and NG with the concentration of 1 x 10(-5) mol x L(-1). They were stained with TRAP and determined for enzymatic activity with TRAP after 4 d, and analyzed by toluidine blue staining after 7 d. The apoptotic osteoclasts were analyzed by Annexin V-FITC staining after 2, 4, 8, 12, 24, 36, and 48 hours, to observe their apoptosis. Their total RNAs were extracted, and analyzed for TRAP and Cathepsin K expressions by Real-time RT-PCR.

RESULTCompared with the control group, both of the PNG group and the NG group showed much less osteoclasts (TRAP positive cells), lower TRAP activity and TRAP and Cathepin K (CTSK) expression, and smaller number of bone resorption pits and areas. The PNG group show lower indexes than the NG group. Additionally, the PNG group reached the apoptotic peak of osteoclasts at 12 h after drug administration, whereas the NG group reached after 24 h. And the former had more apoptotic cells than the latter.

CONCLUSION8-PNG is much more active than NG in inhibiting the resorption of osteoclasts and inducing apoptosis of osteoclasts. Their only difference lies in 8-prenyl perssad, which is proved to be able to enhance the anti-bone resorption activity of 8-prenylnarigenin.

Acid Phosphatase ; metabolism ; Animals ; Bone Resorption ; prevention & control ; Cathepsin K ; metabolism ; Cells, Cultured ; Flavanones ; pharmacology ; Osteoclasts ; drug effects ; Rabbits

OBJECTIVETo isolatate and elucidate the antioxidant constituents from acetone extract of Scutellaria rehderiana.

METHODChemical constituents were isolated by several column chromatographies and their structures were elucidated on the basis of standard compounds and spectral analysis.

RESULTFive compounds, oroxylin A, wogonin, baicalein, ganhuangenin, ganhuangemin were isolated from acetone extract of S. rehderiana. Baicalin was obtained from methanol extract of S. rehderiana.

CONCLUSIONGanhuangemin was isolated from the plant for the first time. Baicalein and ganhuangenin have stronger antioxidant activity than that of BHT (butylated hydroxytoluene).

Antioxidants ; chemistry ; isolation & purification ; pharmacology ; Flavanones ; chemistry ; isolation & purification ; pharmacology ; Flavonoids ; chemistry ; isolation & purification ; pharmacology ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Scutellaria ; chemistry

This study investigated the inhibitory effect of eight natural flavonoids in Chinese herb Scutellariae Radix on huamn cytochrome P450 1 A(CYP1 A), a key cancer chemo-preventive target. In this study, phenacetin was used as a probe substrate for CYP1 A, while human liver microsomes and recombinant human CYP1 A enzymes were used as enzyme sources. Liquid chromatography-tandem mass spectrometry was used to monitor the formation rates of acetaminophen, the O-deethylated metabolite of phenacetin. The dose-dependent inhibition curves were depicted based on the changes of the formation rates of acetaminophen, while the IC_(50) were determined. Inhibition kinetic analyses and docking simulations were used to investigate the inhibition modes and mechanism of wogonin(the most potent CYP1 A inhibitor in this herb), while the inhibition constants(K_i) of wogonin against both CYP1 A1 and CYP1 A2 were determined. Among all tested flavonoids, wogonin, 7-methoxyflavanone and oroxylin A displayed a strong inhibitory effect on CYP1 A(IC_(50)<1 μmol·L~(-1)), baicalein exhibited a moderate inhibitory effect on CYP1 A(IC_(50) between 1-10 μmol·L~(-1)), and baicalin, scutellarein and wogonoside displayed a very weak inhibitory effect on CYP1 A(IC_(50) between 10-25 μmol·L~(-1)), but scutellarin displayed a negligible inhibitory effect on CYP1 A(IC_(50)>100 μmol·L~(-1)). Further investigations demonstrated that wogonin had a weak inhibitory effect on other human CYP enzymes, suggesting that it could be used as a lead compound for the development of specific inhibitors of CYP1 A. Furthermore, the inhibition kinetic analyses clearly demonstrated that wogonin could strongly inhibit phenacetin O-deethylation in both CYP1 A1 and CYP1 A2 in a competitive manner, with K_i values at 0.118 and 0.262 μmol·L~(-1), respectively. Molecular docking demonstrated that wogonin could strongly interact with CYP1 A1 and CYP1 A2 via hydrophobic and π-π interactions, as well as Ser120 and Ser116 in CYP1 A1 via hydrogen-bonding. In conclusion, this study found that some flavonoids in Scutellariae Radix displayed a strong inhibitory effect on CYP1 A, while wogonin is the most potent CYP1 A inhibitor with a relatively high selectivity towards CYP1 A over other human CYPs.
Chromatography, Liquid ; Cytochrome P-450 CYP1A1 ; antagonists & inhibitors ; Cytochrome P-450 Enzyme Inhibitors ; pharmacology ; Flavanones ; pharmacology ; Flavonoids ; pharmacology ; Humans ; Molecular Docking Simulation ; Scutellaria baicalensis ; chemistry

OBJECTIVETo investigate the effects of Drynaria fortunei J. Smith naringin (DFSN) on proliferation and differentiation of human periodontal ligament cells (hPDLC).

METHODSCultured human periodontal ligament cells were treated with DFSN at different concentrations. Cell proliferation was determined by MTT method; cell differentiation was evaluated through the examination of alkaline phosphate (ALP) activities.

RESULTSDFSN in a concentration ranged from 0.01 mu mol/L to 10 mu mol/L showed a promoting effect on proliferation of hPDLC (P< 0.05), and it also promoted ALP activities of hPDLC (P<0.05).

CONCLUSIONDrynaria fortunei J. Smith naringin can promotes the proliferation and differentiation of human periodontal ligament cells.

Cell Differentiation ; drug effects ; Cell Proliferation ; drug effects ; Cells, Cultured ; Drugs, Chinese Herbal ; pharmacology ; Flavanones ; isolation & purification ; pharmacology ; Humans ; Osteoblasts ; cytology ; Periodontal Ligament ; cytology ; Polypodiaceae ; chemistry

OBJECTIVETo develop a simple, reliable approach for evaluating the quality of Huangqin (Scutellaria baicalensis).

METHODTo determine the DPPH free radical scavenging activity and assay of four bioactive components: baicalin, baicalein, wogonin and wogonin-7-O-glucuronide by HPLC.

RESULTThe correlative relationship between DPPH free radical scavenging activity and baicalin content was obtained.

CONCLUSIONBioassay of DPPH free radical scavenging activity could be used as one of the methods for quality evaluation of Chinese drug Huangqin.

Biphenyl Compounds ; Flavanones ; Flavonoids ; chemistry ; isolation & purification ; pharmacology ; Free Radical Scavengers ; pharmacology ; Free Radicals ; Molecular Structure ; Picrates ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Quality Control ; Scutellaria baicalensis ; chemistry

Apoptosis ; drug effects ; Cell Line, Tumor ; Drug Synergism ; Flavanones ; administration & dosage ; pharmacology ; Humans ; Multiple Myeloma ; pathology ; Thalidomide ; administration & dosage ; analogs & derivatives ; pharmacology

Baicalein, a flavonoid compound extracted from dried roots of traditional Chinese medicine Scutellaria baicalensis, has been widely applied as an antioxidant and anti-inflammatory agent. With continuous studies on its mechanisms, recent findings suggest that baicalein has some effect on neuroprotection and improvement of clinical symptoms in neurodegenerative diseases such as Parkinson's disease. Recent studies showed that its neuroprotective efficacy is closely related to such functions as antiinflammatory, antioxidative stress, protecting chondriosome, inhibiting glutamate neurotoxicity, promoting nerve growth and inhibiting alpha-synuclein protein-aggregate activities. The aim of this article is to summarize the neuroprotective effects of baicalein in Parkinson's disease.
Flavanones ; pharmacology ; therapeutic use ; Humans ; Mitochondria ; drug effects ; metabolism ; Nerve Growth Factor ; metabolism ; Neuroprotective Agents ; pharmacology ; therapeutic use ; Oxidative Stress ; drug effects ; Parkinson Disease ; drug therapy ; metabolism ; pathology