Polygalae Radix has long been used in China for calming the mind, promoting intelligence, communicating the heart and kidney, eliminating phlegm, and reducing swelling. At present, it is used to treat amnesia, insomnia, and malaise. Modern research has revealed that Polygalae Radix mainly contains triterpenoid saponins, xanthone, oligosaccharide esters, etc., with the activities of improving memory, resisting dementia, protecting the brain, relieving cough, and removing phlegm, as well as sedation and hypnosis. The present study reviews the research progress on chemical composition, pharmacological action, quality control, and metabolism of Polygalae Radix in the past 30 years, to provide a theoretical basis for further research and development.
Drugs, Chinese Herbal ; Oligosaccharides ; Plant Roots ; Polygala ; Quality Control

OBJECTIVETo study the chemical constituents from the whole plants of Polygala telephioides.

METHODCompounds were isolated by repeated silica gel and Sephadex LH -20 column chromatography, and their structures were determined by spectral analysis and physicochemical properties.

RESULTSix xanthones were isolated from P. telephioides, and their structures were identified as 1, 3, 7-trihydroxyxanthone (1), 1, 7-dihydroxy-3-methoxyxanthone (2), 1, 3-dihydroxyxanthone (3), 1, 7-dihydroxyxanthone (4), 1-methoxy-2, 3-methylenedioxyxanthone (5) and 1, 7-dimethoxyxanthone (6).

CONCLUSIONAll the compounds were obtained from this plant for the first time.

Plants, Medicinal ; chemistry ; Polygala ; chemistry ; Xanthones ; chemistry ; isolation & purification

P-methoxycinnamic acid and 3,4,5-trimethoxycinnamic acid are the compounds found in Polygalae Radix, the root of Polygala tenuifolia Willdenow, and have been reported to have hepatoprotective and anti-neurodegenerative effects. On the other hand, there are no reports of their effects on gastric lesions. This study examined the inhibitory effects of cinnamic acids, including p-methoxycinnamic acid, 3,4,5-trimethoxycinnamic acid, and 8 compounds (cinnamic acid, 2-(trifluoromethyl) cinnamic acid, 3-(trifluoromethyl) cinnamic acid, trans-4-(trifluoromethyl) cinnamic acid, 4-(dimethylamino) cinnamic acid, 3,4-(methylenedioxy) cinnamic acid and 3,4-dihydroxycinnamic acid), which were selected based on their presence in medicinal herbs and molecular weight, against gastric lesions. Animal models were used to confirm the protective effects on acute gastritis caused by the administration of HCl/EtOH. Gastric acid inhibition was examined by an acid-neutralizing test and the proton pump (H⁺/K⁺-ATPase) inhibiting activity. In addition, antioxidant tests were performed and the gastric emptying rate was determined. The results showed that cinnamic acid, p-methoxycinnamic acid, and 3,4,5-trimethoxycinnamic acid had an inhibitory effect on gastric lesions.
Gastric Acid ; Gastric Emptying ; Gastritis ; Hand ; Models, Animal ; Molecular Weight ; Plants, Medicinal ; Polygala ; Proton Pumps

Nine compounds were isolated from the n-butanol extract of the aerial parts of Polygala sibirica by various column chromatographic methods. Their structures were identified by MS and NMR spectroscopic data as sibiricaxanthone F (1), amentoflavone (2), linarin (3), zigu-glucoside I (4), 3, 6'-disinapoyl sucrose (5), tenuifoliside A (6), 2, 4, 4-trimethyl-3-formyl-6-hy-droxy-2, 5-cyclohexadien-1-one (7), lanierone (8), and aralia cerebroside (9) , respectively. Compounds 2, 3, 4, 7, 8 were isolated from the genus Ploygala for the first time, and compound 9 was firstly isolated from the title plant.
Butanols ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Plant Components, Aerial ; chemistry ; Polygala ; chemistry

OBJECTIVETo analyze the correlation between environmental factors and the lipophilic and hydrophilic constituents of Polygalae Radix.

METHODThe contents of lipophilic constituent were determined by GC-MS and hydrophilic constituents by HPLC. Geographical factors were collected by on-site inspection and climate factors by the local meteorological data. The relationship between the content of the lipophilic and hydrophilic constituents and the factors were analyzed by SPSS 18.0.

RESULTThere was linear relationship between the content of lipophilic constituent and climate factors such as average temperature of July, average temperature of January. There was also linear relationship between hydrophilic constituents and climate factors such as annual average temperature, latitude, annual average rainfall.

CONCLUSIONThe main climate factors that affect liposoluble constituent content were average temperature of July, average temperature of January, and the main climate factors that affect hydrophilic constituent content were annual average temperature, latitude, annual average rainfall. The study would contribute to the quality evaluation and suitability of origin of Polygalae Radix.

Environment ; Hydrophobic and Hydrophilic Interactions ; Polygala ; chemistry ; Quality Control ; Rain ; Regression Analysis ; Seasons ; Temperature

OBJECTIVETo study the chemical constituents of Polygala tenuifolia.

METHODIsolations were performed on various chromatography columns and structure elucidations were aided by spectral data and chemical property analyses.

RESULTFour compounds were isolated from the roots of P. tenuifolia. Their structures were identified as sibiricose A5 (1), sibiricose A6 (2), tenuifoliside A (3) and 3',6-disinapoyl sucrose (4).

CONCLUSIONCompounds 1 and 2 were isolated from this plant for the first time.

Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Polygala ; chemistry ; Sucrose ; analogs & derivatives ; chemistry ; isolation & purification

OBJECTIVETo investigate the chemical constituents of the aerial parts of Polygala sibirica systematically.

METHODSThe chemical constituents were isolated by various column chromatographic methods. The structures were identified by spectral data.

RESULTTen compounds were isolated and identified as 6-hydroxy-1, 2, 3, 7-tetramethoxy xanthone (1); 1, 2, 3, 6, 7-heptamethoxy xanthone (2); 1, 7-didydroxy-2, 3-methylenedioxy xanthone (3); 1, 7-dihydroxy-2, 3-dimethoxy xanthone (4); 1, 3, 7-trihydroxy-2-methoxy xanthone (5); 1, 6, 7-trihydroxy-2, 3-dimethoxy xanthone (6); alpha-spinasterol (7); alpha-spinasterolic-3-O-beta-D-glucoside (8); squalene (9) and polygital (10).

CONCLUSIONCompounds 1-10 were isolated from this species for the first time.

Plant Components, Aerial ; chemistry ; Plant Extracts ; chemistry ; Polygala ; chemistry ; Xanthones ; chemistry

OBJECTIVETo establish the method for quantitative determination of sibricose A5 and sibricose A6 in Polygalae Radix by HPLC.

METHODThe ultrasonic extracting method was applied in sample pre-treatment. The HPLC procedure was performed on the chromatographic column of Agela Promosil C18 (4.6 mm x 250 mm, 5 microm), the mobile phase was acetonitrile-0.1% phosphoric acid water solution (10:90). The detection wavelength was 330 nm and flow velocity was 1 mL x min(-1). The column temperature was 30 degrees C.

RESULTThe method has good linearity in the ranges of 0.0087-0.0694 g x L(-1) (r = 0.9993) for sibricose A5, 0.0090-0.0723 g x L(-1) (r=0.9991) for sibricose A6. The average recoveries of sibricose A5 and sibricose A6 were 101.7%, 97.87%, with the RSD of 1.7%, 1.6%, respectively.

CONCLUSIONThe method was simple, quick accurate and reliable. It is appropriate for the quantitative determination of sibricose A5 and sibricose A6 in Polygalae Radix.

Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Polygala ; chemistry ; Polysaccharides ; analysis ; chemistry ; isolation & purification

AIMTo study the chemical constituents of Polygala aureocauda Dunn..

METHODSChemical compounds were isolated by column chromatography and their structures were determined mainly by spectroscopic means (UV, IR, MS, 1HNMR, 13CNMR, HMQC, HMBC).

RESULTSThree compounds were isolated and identified as 3-hydroxy-1,4-dimethoxyxanthone (I), 1, 7-dihydroxy-2, 3-methylendioxyxanthone (II), 7-hydroxy-1-methoxy-2, 3-methylendioxyxanthone (III).

CONCLUSIONCompounds I-III were isolated from Polygala aureocauda Dunn. for the first time, whereas compound I is a new xanthone.

Molecular Conformation ; Molecular Structure ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Polygala ; chemistry ; Xanthones ; chemistry ; isolation & purification

OBJECTIVE: This study was to investigate in vivo antidopaminergic activities of polygalasaponins which included in the roots of Polygalae tenuifolia, one of the natural plants prescribed to treat psychotic disorders in traditional medicine. METHODS: The chemical separations were conducted by chromatographies with various columns and the chemical structures were identified using spectroscopy, NMR and so on. The apomorphine-induced stereotyped behaviors and climbing behaviors in mice as animal models of psychotic disorders were applied to explore the antidopaminergic activity. RESULTS: The active compounds with antidopaminergic effects in the roots of Polygalae tenuifolia were identified as polygalasaponin A-D. The polygalasaponins showed to suppress the apomorphine-induced stereotyped behaviors and climbing behaviors in dose-related fashions. CONCLUSION: This study suggests that polygalasaponins might have antipsychotic activities. The natural products need to be explored extensively as sources of new medications in psychiatric fields. Further explorations for chemical and pharmacological properties of polygalasaponins are required.
Animals ; Apomorphine ; Biological Products ; Chromatography ; Magnetic Resonance Spectroscopy ; Medicine, Traditional ; Mice* ; Models, Animal ; Polygala* ; Psychotic Disorders ; Stereotyped Behavior