To investigate the effects of leonurine(Leo) on abdominal aortic constriction(AAC)-induced cardiac hypertrophy in rats and its mechanism. A rat model of pressure overload-induced cardiac hypertrophy was established by AAC method. After 27-d intervention with high-dose(30 mg·kg~(-1)) and low-dose(15 mg·kg~(-1)) Leo or positive control drug losartan(5 mg·kg~(-1)), the cardiac function was evaluated by hemodynamic method, followed by the recording of left ventricular systolic pressure(LVSP), left ventricular end-diastolic pressure(LVESP), as well as the maximum rate of increase and decrease in left ventricular pressure(±dp/dt_(max)). The degree of left ventricular hypertrophy was assessed based on heart weight index(HWI) and left ventricular mass index(LVWI). Myocardial tissue changes and the myocardial cell diameter(MD) were measured after hematoxylin-eosin(HE) staining. The contents of angiotensin Ⅱ(AngⅡ) and angiotensin Ⅱ type 1 receptor(AT1 R) in myocardial tissue were detected by ELISA. The level of Ca~(2+) in myocardial tissue was determined by colorimetry. The protein expression levels of phospholipase C(PLC), inositol triphosphate(IP3), AngⅡ, and AT1 R were assayed by Western blot. Real-time quantitative PCR(qRT-PCR) was employed to determine the mRNA expression levels of β-myosin heavy chain(β-MHC), atrial natriuretic factor(ANF), AngⅡ, and AT1 R. Compared with the model group, Leo decreased the LVSP, LVEDP, HWI, LVWI and MD values, but increased ±dp/dt_(max) of the left ventricle. Meanwhile, it improved the pathological morphology of myocardial tissue, reduced cardiac hypertrophy, edema, and inflammatory cell infiltration, decreased the protein expression levels of PLC, IP3, AngⅡ, AT1 R, as well as the mRNA expression levels of β-MHC, ANF, AngⅡ, AT1 R, c-fos, and c-Myc in myocardial tissue. Leo inhibited AAC-induced cardiac hypertrophy possibly by influencing the RAS system.
Angiotensin II/metabolism* ; Animals ; Cardiomegaly/genetics* ; Gallic Acid/analogs & derivatives* ; Hypertrophy, Left Ventricular/pathology* ; Myocardium/pathology* ; Rats

The extracting technology of salidroside, tyrosol, crenulatin and gallic acid from Rhodiolae Crenulatae Radix et Rhizoma was optimized. With extraction rate of salidroside, tyrosol, crenulatin and gallic acid as indexes, orthogonal test was used to evaluate effect of 4 factors on extracting technology, including concentration of solvent, the dosage of solvent, duration of extraction, and frequency of extraction. The results showed that, the best extracting technology was to extract in 70% alcohol with 8 times the weight of herbal medicine for 2 times, with 3 hours once. High extraction rate of salidroside, tyrosol, crenulatin and gallic acid were obtained with the present technology. The extracting technology was stable and feasible with high extraction rate of four compounds from Rhodiolae Crenulatae Radix et Rhizoma, it was suitable for industrial production.
Chemical Fractionation ; methods ; Chemistry, Pharmaceutical ; methods ; Coumarins ; isolation & purification ; Drugs, Chinese Herbal ; isolation & purification ; Gallic Acid ; isolation & purification ; Glucosides ; isolation & purification ; Phenols ; isolation & purification ; Phenylethyl Alcohol ; analogs & derivatives ; isolation & purification ; Rhizome ; chemistry ; Rhodiola ; chemistry

This study is to investigate the effect of ethyl gallate on invasion capabilities and its mechanism of breast cancer MDA-MB-231 cells. Using cell adhesion and transwell assay, separately, the effects of ethyl gallate on the invasion of MDA-MB-231 cells were measured. The Akt-NF-κB signal pathway protein expressions were analyzed with Western blot. Also, the mRNA levels of MMP-9 and MMP-2 were analyzed by RT-PCR. Ethyl gallate inhibited the abilities of motility, adhesion and invasion of breast cancer MDA-MB-231 cells in vitro (P<0.05), inhibited the mRNA levels of MMP-9, MMP-2, phosphorylation of AKt and protein expression of NF-κB. It is concluded that ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt and protein expression of NF-κB.
Breast Neoplasms ; pathology ; Cell Adhesion ; drug effects ; Cell Line, Tumor ; Cell Movement ; drug effects ; Gallic Acid ; analogs & derivatives ; pharmacology ; Humans ; Matrix Metalloproteinase 2 ; metabolism ; Matrix Metalloproteinase 9 ; metabolism ; NF-kappa B ; metabolism ; Phosphorylation ; Proto-Oncogene Proteins c-akt ; metabolism ; RNA, Messenger ; Signal Transduction

OBJECTIVETo study the anti-cataract effect of gigantol combined with syringic acid and their action mechanism.

METHODH202-induced lens oxidative injury in vitro rat model was establish to observe the impact of gigantol combined with syringic acid on lens transparency under a dissecting microscope. D-galactose-induced cataract rat model was established to observe the impact of gigantol combined with syringic acid on lens transparency under a slit-lamp. UV spectrophotometry was adopted to detect the inhibitory activity of gigantol combined with syringic acid against AR. Molecular docking method was used to detect binding sites, binding types and pharmacophores of gigantol combined with syringic acid in prohibiting aldose reductase.

RESULTBoth in vitro and in vivo experiments showed a good anti-sugar cataract activity in the combination of gigantol and syringic acid and a better collaborative effect than single component-gigantol and syringic acid and positive control drug Catalin. Molecular docking and dynamic simulation showed their collaborative AR-inhibiting amino acid residue was Asn160 and the major acting force was Van der Waals' force, which formed common pharmacophores.

CONCLUSIONGigantol combined with syringic acid shows good anti-cataract, their action mechanism is reflected in their good collaborative inhibitory effect on AR.

Aldehyde Reductase ; antagonists & inhibitors ; Animals ; Bibenzyls ; Cataract ; drug therapy ; enzymology ; Drug Synergism ; Female ; Gallic Acid ; analogs & derivatives ; pharmacology ; Guaiacol ; analogs & derivatives ; pharmacology ; Humans ; In Vitro Techniques ; Lens, Crystalline ; drug effects ; enzymology ; Male ; Rats ; Rats, Wistar

OBJECTIVETo study the dissolution rate of active components of different extracting solvents of Danggui Chishao drug pair.

METHODThe dissolution rates of phenolic acids (ferulic acid, vanillic acid and gallic acid), monoterpenes (gallic acid, peoniflorin, albiflorin, hydroxypeoniflorin and galloylpaeoniflorin) and phthalates (senkyunolide and ligustilide) contained in Danggui Chishao drug pair were determined by quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MS) and ultra high performance liquid chromatography in combination with triple-quadrupole mass spectrometry (UPLC-TQ-MS).

RESULTThe dissolution rates of phenolic acids and monoterpenes decreased with the increase in alcohol concentration, on the contrary the rates of phthalates increased. The relative dissolution rates of most active components were relatively high in water and low concentration alcohol than other solvents.

CONCLUSIONLiquid chromatography-mass spectrometry is practical for comprehensive multi-component assessment on traditional Chinese medicine preparation processes and can provide reference for optimization of processing parameters.

4-Butyrolactone ; analogs & derivatives ; chemistry ; Benzoates ; chemistry ; Benzofurans ; chemistry ; Bridged-Ring Compounds ; chemistry ; Chromatography, Liquid ; Drugs, Chinese Herbal ; chemistry ; Gallic Acid ; chemistry ; Glucosides ; chemistry ; Hydroxybenzoates ; chemistry ; Mass Spectrometry ; Monoterpenes ; chemistry ; Phthalic Acids ; chemistry ; Solvents ; chemistry ; Vanillic Acid ; chemistry

To study the chemical constituents of Alchornea trewioides, silica gel column chromatography, Sephadex LH-20, reverse phase ODS column chromatography, MCI and semi-preparative HPLC were used to separate the 95% EtOH extract of the root of Alchornea trewioides. The structures were elucidated on the basis of spectroscopic studies including ESI-TOF-MS, 1H NMR, 13C NMR, HSQC and HMBC. Eight phenolic acids were obtained and identified as 1-O-galloyl-6-O-vanilloyl-beta-glucose (1), gallic acid (2), ethyl gallate (3), syringic acid (4), glucosyringic acid (5), erigeside C (6), 3, 4-dimethoxyphenyl-(6'-O-alpha-L-rhamnosyl)-beta-D-glucopyranoside (7) and 3, 4, 5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside (8). Among them, compound 1 is a new compound, compounds 4-8 are isolated from the genus Alchornea for the first time, and the others are isolated from the plant for the first time.
Benzoates ; chemistry ; isolation & purification ; Euphorbiaceae ; chemistry ; Gallic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; Glucose ; analogs & derivatives ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Hydroxybenzoates ; chemistry ; isolation & purification ; Molecular Structure ; Phenols ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry

To study the chemical constituents of Bauhinia glauca subsp. pernervosa, eleven phenolic acids were isolated from a 95% ethanol extract by using a combination of various chromatographic techniques including column chromatography over silica gel, ODS, MCI, Sephadex LH-20, and semi-preparative HPLC. By spectroscopic techniques including 1H NMR, 13C NMR, 2D NMR, and HR-ESI-MS, these compounds were identified as isopropyl O-beta-(6'-O-galloyl)-glucopyranoside (1), ethyl O-beta-(6'-O-galloyl)-glucopyranoside (2), 3, 4, 5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside (3), 3, 4, 5-trimethoxyphenyl-beta-D-glucopyranoside (4), gallic acid (5), methyl gallate (6), ethyl gallate (7), protocatechuic acid (8), 3, 5-dimethoxy-4-hydroxybenzoic acid (9), erigeside C (10) and glucosyringic acid (11). Among them, compound 1 is a new polyhydroxyl compound; compounds 2, 10, and 11 were isolated from the genus Bauhinia for the first time, and the other compounds were isolated from the plant for the first time. Compounds 6 and 8 showed significant protein tyrosine phosphatase1B (PTP1B) inhibitory activity in vitro with the IC50 values of 72.3 and 54.1 micromol x L(-1), respectively.
Bauhinia ; chemistry ; Benzoates ; chemistry ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Gallic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Glucosides ; chemistry ; isolation & purification ; pharmacology ; Hydroxybenzoates ; chemistry ; isolation & purification ; pharmacology ; Phenols ; chemistry ; isolation & purification ; pharmacology ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 ; metabolism

OBJECTIVETo develop an HPLC method for determination of gallic acid, hydroxysafflor yellow A, cinnamic aldehyde and piperine in Tibetan medicine Dangzuo, and to compare the content of four active components in Dangzuo of different Tibetan regions.

METHODThe separation was carried out on a Waters XTerra RP-C18 column ( 4.6 mm x 250 mm, 5 microm). The mobile phases were methanol and water, all contained 0.1% glacial acetic acid, for gradient elution. The gradient program was as follows: 0-22.5 min, methanol was changed from 5% to 50%; 22.5-40 min, changed to 80% 80:20. The flow rate was 1.0 mL x min(-1). The detection wavelength was 270 nm. The reference wavelength was 500 nm.

RESULTThe linear ranges of gallic acid, hydroxysafflor yellow A, cinnamic aldehyde and piperine were 0.040-0.640 microg (r = 0.999 8), 0.090-1.440 microg (r = 0.999 9), 0.031-0.500 microg (r = 0.999 9 ) and 0.092-41.477 microg (r = 0.998 9), respectively. The average recoveries (n = 6) were 97.42% (RSD 1.9%), 97.55% (RSD 2.9%), 98.69% (RSD 0.96%) and 96.72% (RSD 4.0%), respectively. The content ranges of gallic acid, hydroxysafflor yellow A, cinnamic aldehyde and piperine in Dangzuo samples of different Tibetan regions were 0.11341.69 mg x g(-1), 0.889-1.51 mg x g(-1), 0.000-40.606 mg x g(-1) and 1.96-2.73 mg x g(-1), respectively.

CONCLUSIONThe method is a simple and effective for quality control of Tibetan medicine Dangzuo.

Acrolein ; analogs & derivatives ; analysis ; isolation & purification ; Alkaloids ; analysis ; isolation & purification ; Benzodioxoles ; analysis ; isolation & purification ; Chalcone ; analogs & derivatives ; analysis ; isolation & purification ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Gallic Acid ; analysis ; isolation & purification ; Medicine, Tibetan Traditional ; Piperidines ; analysis ; isolation & purification ; Plant Components, Aerial ; chemistry ; Plant Extracts ; analysis ; isolation & purification ; Polyunsaturated Alkamides ; analysis ; isolation & purification ; Quality Control ; Quinones ; analysis ; isolation & purification ; Reference Standards ; Spectrophotometry, Ultraviolet ; methods

OBJECTIVETo investigate the chemical constituents of the branches and leaves of Polyalthia nemoralis.

METHODThe compounds were isolated and purified by silica gel, macroporous adsorption resin and Sephadex LH-20 column chromatographic methods. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.

RESULTFourteen compounds were isolated and identified as syringic acid (1), 3-methoxy-4-hydroxycinnamic acid (2), vanillic acid (3), 4-hydroxybenzoic acid (4), mauritianin (5), (+)-xylopinidine (6), (+)-oblongine(7), (+)-tembetarine (8), eythritol (9), D-mannitol (10), ethyl-beta-D-glucopyranoside (11), (+)-magnoflorine (12), stepharanine (13), (2S, 4R)-4-hydroxy-2-piperidine-carboxylic acid (14), respectively.

CONCLUSIONAll the compounds were isolated from the genus Polyalthia for the first time; compounds 6 and 13 showed inhibitation activities against multi tumor cell lines.

Alkaloids ; chemistry ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Aporphines ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Survival ; drug effects ; Chromatography, Agarose ; methods ; Coumaric Acids ; chemistry ; isolation & purification ; pharmacology ; Gallic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Humans ; Kaempferols ; chemistry ; isolation & purification ; pharmacology ; Parabens ; chemistry ; isolation & purification ; pharmacology ; Plant Extracts ; chemistry ; isolation & purification ; pharmacology ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Polyalthia ; chemistry ; Vanillic Acid ; chemistry ; isolation & purification ; pharmacology

Six compounds were isolated from the roots of Pithecellobium lucidum by various chromatograhic techniques such as column chromatography on silica gel and Sephadex LH-20, and preparative HPLC, and their structures were elucidated as julibroside A2 (1), 3-[ (2-acetamido-2-deoxy-beta-D-glucopyranosyl) oxy] -16alpha-hydroxyolean-12-en-28-oic acid (2), galloyl acid (3), ethyl gallate (4), (+)-catechin (5), (-)-gallocatechin gallate (6) on the basis of spectrascopic data analysis. Compounds 1-6 were isolated from Pithecellobium lucidum for the first time. Compound 2 showed selective cytoxic activity against the human cell lines A2780 with an IC50 value of 1.72 micromol x L(-1).
Catechin ; analogs & derivatives ; chemistry ; isolation & purification ; toxicity ; Cell Line ; Fabaceae ; chemistry ; Gallic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; toxicity ; Humans ; Inhibitory Concentration 50 ; Oleanolic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; Plant Extracts ; chemistry ; toxicity ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Saponins ; chemistry ; isolation & purification ; toxicity ; Triterpenes ; chemistry ; isolation & purification ; toxicity