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 observe reversal of ventricular remodeling by the protein kinase C inhibitor Scutellarein in spontaneously hypertensive rats (SHRs).

METHODSTwelve SHRs were randomly divided into two groups. Scutellarein and saline (10 mg x kg(-1) x d(-1)) were given by intraperitoneal injection to two groups of rats separately. Systolic blood pressure (SBP) and ventricular weight index (LVW/BW, RVW/BW) were measured. A polarization microscope and an image analyzer system (IAS) were used to observe changes in cardiovascular structure and to count the content of cardiac muscle interstitial collagen.

RESULTSThe pathologic changes in the left ventricle in the Scutellarein group rats (SHR(D)) improved to varying degrees, including hypertrophy of the cardiac muscle and collagen volume fraction.

CONCLUSIONScutellarein can reverse ventricular remodeling, improve myocardial stiffness and protect heart cardiac muscle.

Animals ; Female ; Flavanones ; Flavonoids ; pharmacology ; Hypertension ; physiopathology ; Male ; Protective Agents ; pharmacology ; Protein Kinase C ; antagonists & inhibitors ; Random Allocation ; Rats ; Rats, Inbred SHR ; Ventricular Remodeling ; drug effects

An experiment was conducted using cultivated Glycyrrhiza uralensis in age of one year to study the effects of abscisic acid (ABA) on chemical components content and color of G. uralensis. By using different concentrations of ABA spraying on leaves, the change of the chemical component content was analyzed within 45 d after ABA stimulation, and the effects on quality were studied combined with colorimetric analysis data. It turned out that in some sense the content of glycyrrhizic acid and liquiritin had increased within 45 d, especially for liquiritin. After high concentrations of ABA (3.96 mg · L(-1)) stimulating, the content of glycyrrhizic acid rose 52% while liquiritin up 392% within 30 d. Then they both showed a decline in the content of glycyrrhizic acid and liquiritin on 45 d. Color index values of a* and b* were all significantly higher than that of the control group within 45 d, which meant the color of powders turned toward red and yellow. The conclusion was that ABA (3.96 mg · L(-1)) stimulating could not only improve the quality in the traditional sense through the color of G. uralensis, but also in the modern sense by improving the content of glycyrrhizic acid and liquiritin.
Abscisic Acid ; pharmacology ; Color ; Drugs, Chinese Herbal ; chemistry ; Flavanones ; analysis ; Glucosides ; analysis ; Glycyrrhiza uralensis ; chemistry ; drug effects ; growth & development ; Glycyrrhizic Acid ; analysis ; Plant Growth Regulators ; pharmacology

This paper aimed to study the ability of baicalein to block human cytomegalovirus (HCMV) infection in extravillous cytotrophoblasts (EVT) and its effect on the vasoactive intestinal peptide (VIP) expression in HCMV-infected EVT in vitro. A human trophoblast cell line (HPT-8) was chosen in this study. HCMV with 100 TCID50 was added into culture medium to infect HPT-8 cells, and then HCMV pp65 antigen was assayed by immunofluorescence staining. The infection status was determined by virus titration. Real-time quantitative polymerase chain reaction (qRT-PCR) was used to detect virus DNA load in the infected cells. The expression of VIP mRNA and protein in the infected cells was measured by qRT-PCR, immunocytochemistry and Western blotting. Concentration of VIP secreted in supernatants was determined by ELISA. Red-stained HCMV pp65 antigens were found in infected HPT-8 cells 48 h after infection. HCMV replicated in large quantity in infected HPT-8 cells 4 days after infection, reaching a peak at day 6 post-infection. After treatment with baicalein, virus DNA load in infected HPT-8 cells was decreased (P<0.05), and the levels of VIP mRNA and protein, and the concentration were raised to the normal (P>0.05). Our study suggested that baicalein exerts a positive effect on the VIP expression in HCMV-infected EVT at maternal-fetal interface.
Antiviral Agents ; pharmacology ; Cell Line ; Cytomegalovirus ; drug effects ; physiology ; Flavanones ; pharmacology ; Humans ; Trophoblasts ; cytology ; drug effects ; metabolism ; virology ; Vasoactive Intestinal Peptide ; metabolism ; Virus Inactivation ; drug effects

Flavonoid naringin is widely distributed in various types of plants and is an important component of herbal Drynaria. In previous studies, Drynaria has been demonstrated to have inhibitory effects on inflammatory responses and bone destruction and exert anabolic effects on bone, has been widely used in the clinical treatment. Naringin, was in the stage of experimental yet. The experimental results have confirmed that naringin suppressed inflammation including arthritis by lowering the expression of inflammatory cytokines, and the mechanism can be explained as reducing the expression of NF-κB. Naringin has been shown to increase osteoblast proliferation by increasing the expression of BMP-2, inhibit osteoclast activity by reducing the expression of RANKL. In animal experimental, naringin was useful for osteoporosis, and the mechanisms are in-depth studies. Research in the field of traditional Chinese medicine and orthopedics, naringin as a explicit material structure in the components of Drynaria, has been concerned about the experimental studies, it is not only prosperity the development of traditional Chinese medicine research,but also ready for clinical studies anti-inflammatory and bone effects of naringin in the future.
Animals ; Anti-Inflammatory Agents ; pharmacology ; Bone and Bones ; drug effects ; Flavanones ; pharmacology ; Humans ; Medicine, Chinese Traditional ; Osteoblasts ; drug effects ; Osteoclasts ; drug effects ; Osteoporosis ; drug therapy ; Polypodiaceae ; chemistry