Research Update:Polygala tenuifolia root,Polygala tenuifolia Willd,Polygala sibirica L.

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   Phytochemical info of Polygala tenuifolia root.

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 Definition:Polygala tenuifolia root are majorly composed of
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   Research Update:Polygala tenuifolia root,Polygala tenuifolia Willd,Polygala sibirica L.

  Effect of Polygala tenuifolia Root Extract on Scopolamine-Induced Impairment of Rat Spatial Cognition in an Eight-Arm Radial Maze Task.:Biol Pharm Bull. 2007 Sep;30(9):1727-31.

 The effects of Polygala tenuifolia root fractions and the acyl groups of its constituents on the retrieval process of spatial cognition in rats were studied using an eight-arm radial maze task. Oral administration of a precipitate fraction (PTB) obtained by concentration of the n-BuOH-soluble portion from the extract of the roots significantly decreased the number of total errors (TEs) and that of working memory errors (WMEs) at doses of 100 mg/kg and 200 mg/kg. However, it caused no significant decrease in the number of reference memory errors (RMEs). In addition, the saponin-rich fraction (PTBM) obtained by purification of PTB also showed significant decreases in TEs and WMEs at a dose of 100 mg/kg. Among the cinnamic acid derivatives present as the acyl groups in the P. tenuifolia constituents, sinapic acid (SNPA) significantly decreased TEs and WMEs at doses of 10 to 100 mg/kg. These results indicated that P. tenuifolia extracts, PTB and PTBM, and SNPA had a beneficial effect on the memory impairment induced by dysfunction of the cholinergic system in the brain. The memory improvement in the scopolamine-induced memory impairment seen in the radial maze performance was due to improvement in the short-term memory. A contribution of some constituents other than SNPA to the memory improvement was also suggested.

  Simultaneous determination of phenols in Radix Polygalae by high performance liquid chromatography: Quality assurance of herbs from different regions and seasons.:J Sep Sci. 2007 Aug 22; Li J, Dong X, Jiang Y, Gao Q, Jiang Z, Cheung AW, Duan R, Dong TT, Tu P, Tsim KW.Department of Biology and Center for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong. Fax: +852-2358-1559.

 Radix Polygalae, roots of Polygala tenuifolia or of Polygala sibirica, is a Chinese herbal medicine commonly used to prevent dementia. Reliable chemical markers for quality assurance of this herb are missing. Here, a high performance liquid chromatography method coupled with diode array detection was developed to simultaneously determine nine different phenols in Radix Polygalae, including sibiricose A(5), sibiricose A(6), glomeratose A, tenuifoliside A, glomeratose D, 3',6-di-O-sinapoyl sucrose ester, mangiferin, polygalaxanthone III, and polygalaxanthone XI. By using two different detection wavelengths in the HPLC analysis, the developed method was able to determine the phenols with excellent resolution, precision, and recovery. This established method was therefore applied to determine the amounts of phenols in thirty-two samples from different cultivation regions and harvest seasons in China, and significant variations were revealed. The amounts of phenols in the roots of P. tenuifolia collected in Shanxi and Shannxi Provinces were markedly higher than in roots collected from other Provinces. Moreover, the samples harvested in the spring contained higher contents of phenols than those collected in other seasons.

  Structure analysis of triterpene saponins in Polygala tenuifolia by electrospray ionization ion trap multiple-stage mass spectrometry.:J Mass Spectrom. 2007 Jul;42(7):861-73.Liu J, Yang X, He J, Xia M, Xu L, Yang S.Institute of Medicinal Plants Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

 Eighteen different triterpene saponins isolated from Polygala tenuifolia were investigated by electrospray ionization ion trap multiple-stage mass spectrometry (ESI-ITMS(n)) in positive and negative ion modes. MS(1)-MS(3)/MS(4) spectra of the both modes were analyzed, and they all gave fragments in line and shared common fragmentation patterns. Key fragments from MS(n) spectra of both the modes and their proposed fragmentation pathways were constructed with examples illustrated for the formation of characteristic fragments in the saponins. Two special fragmentation patterns were proposed: (1) the formation of fragments by cleavage of CH(2)O from Delta(12)-14alpha-CH(2)OH of the oleanene-type saponin aglycone in both positive and negative MS(n) (n > or = 2) modes; (2) the occurrence of fragments by cleavage of CO(2) and 3-glucose as the characteristic structure feature of 23-COOH at the oleanene-type saponin aglycones coupled with 3-Glc substitutes in the negative MS(n) (n > or = 2) modes. Peak intensities in MS(n) spectra were also correlated with structural features and fragmentation preferences of the investigated saponins, which are discussed in detail. In general, fragments formed predominantly by cleavages of glycosidic bonds in the positive mode, while selective cleavages of acyl bonds preceded that of glycosidic bonds in negative MS(n) (n > or = 2) mode, both of which could well be applied to the structural analysis of these saponins. Interpretation of MS(n) spectra presented here provided diagnostic key fragment ions important for the structural elucidation of saponins in P.tenuifolia.

  Cerebral protective and cognition-improving effects of sinapic acid in rodents.:Biol Pharm Bull. 2007 Mar;30(3):514-9.

 We previously demonstrated that tenuifoliside B and 3,6'-disinapoylsucrose in Polygalae Radix, the root of Polygala tenuifolia WILLDENOW, inhibited potassium cyanide (KCN)-induced hypoxia and scopolamine-induced memory impairment in mice. Because both ingredients have a common sinapoyl moiety in their structure, we inferred that the sinapoyl moiety could inhibit hypoxia and memory impairment. In the present study to clarify the hypothesis, sinapic acid inhibited KCN-induced hypoxia and scopolamine-induced memory impairment as well as tenuifoliside B and 3,6'-disinapoylsucrose did. In addition, sinapic acid inhibited decompression- or bilateral carotid artery ligation-induced hypoxia (or mortality) and CO2-induced impairment in mice, and basal forebrain lesion-induced cerebral cholinergic dysfunction (decreases in acetylcholine concentration and choline acetyltransferase activity) in rats. These results, taken together, suggest the possibilities that sinapic acid is not only a very important moiety in the pharmacological activities of tenuifoliside B and 3,6'-disinapoylsucrose but also a candidate for a cerebral protective and cognition-improving medicine.

  Experimental report on cultivated density of Polygala tenuifolia.:Zhong Yao Cai. 2006 Jul;29(7):652-3. Chinese.Zhao YS, Li ZL, Mao FY, Zhang LP.Institute of Crop Research, Shanxi Academy of Agricultural Sciences, Fenyang, China.

 OBJECTIVE: The proper cultivated density of P. tenuifolia was researched to improve cultural practices in producing region. METHOD: The experiment was determined by the randomized blocks design of three replications. RESULT: There is significance difference for the yield per mu in different cultivated density. CONCLUSION: The proper planted density is 20 cm x 3 cm, i. e. 111 thousand plants per mu.


  Antidepressant principles of the roots of Polygala tenuifolia.:J Nat Prod. 2006 Sep;69(9):1305-9.Cheng MC, Li CY, Ko HC, Ko FN, Lin YL, Wu TS.Medical and Pharmaceutical Industry Technology and Development Center, Taipei County, Taiwan, Republic of China.

 [(125)I]RTI-55-membrane binding assay-guided fractionation and separation of a water-soluble extract of the roots of Polygala tenuifolia gave five new oligosaccharide derivatives, polygalatenosides A-E (1-5). The structures of these new oligosaccharides were established on the basis of spectroscopic evidence. Polygalatenosides A and B (1 and 2) showed significant inhibitory activity, with IC(50) values of 30.0 and 6.04 microM, respectively, in this membrane binding assay and acted as norepinephrine reuptake inhibitors through blocking norepinephrine transport.

  Characterization of anti-neurodegenerative effects of Polygala tenuifolia in Abeta(25-35)-treated cortical neurons.:Biol Pharm Bull. 2006 Sep;29(9):1892-6.

 Although Polygala tenuifolia WILLD (PT) was classically mentioned as an anti-dementia drug in Chinese traditional medicine, basic research showed only enhancement of the cholinergic function. In Alzheimer's disease, neuritic atrophy and synaptic loss occur prior to neuronal death event, and may be the first trigger of the memory impairment. Therefore, we studied effects of Polygala tenuifolia WILLD (PT) on Abeta(25-35)-induced neuronal damage using rat cortical neurons for characterization of activities of PT under Abeta-induced neuronal damage. Treatment with the water extract of PT enhanced axonal length dose-dependently after Abeta(25-35)-induced axonal atrophy. However, dendritic atrophy and synaptic loss induced by Abeta(25-35) were not recovered by treatment with PT extract. In contrast, Abeta(25-35)-induced cell damage was completely inhibited by PT extract. By characterization of PT effects on neuronal morphological plasticity and cell damage, usefulness as well as an insufficiency of PT as an anti-dementia drug was clarified.

  New acylated triterpene saponins from Polygala tenuifolia willd.:J Asian Nat Prod Res. 2006 Sep;8(6):499-503.Li J, Jiang Y, Tu PF.Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100083, China.

 Two new acylated presenegenin glycosides E-onjisaponin H (5) and Z-onjisaponin (6) together with seven known saponins were isolated from the roots of Polygala tenuifolia Willd. Compounds 5 and 6 were obtained as a pair of isomers due to trans and cis-p-methoxycinnamoyl. Their structures were elucidated mainly by 2D-NMR techniques including 1H-1HCOSY, TOCSY, HSQC, HMBC as 3-O-(beta-D-glucopyranosyl) presenegenin 28-[O-beta-D-apiofuranosyl-(1 --> 3)-O-[beta-D-xylopyranosyl-(1 --> 4)]-O-alpha-L-rhamnopyranosyl-(1 --> 2)-O-[alpha-L-rhamnopyranosyl-(1 --> 3)]-4-O-[(E)-p-methoxycinnamoyl]-beta-D-fucopyranosyl] ester (5) and its (Z)-isomer (6).

  Modulation of cytokine expression by traditional medicines: a review of herbal immunomodulators.:Altern Med Rev. 2006 Jun;11(2):128-50. Review.Spelman K, Burns J, Nichols D, Winters N, Ottersberg S, Tenborg M.Clinical Division, Department of Herbal Medicine, Tai Sophia Institute, 7750 Montpelier Road, Laurel, MD 20723, USA. spelman123@earthlink.net.

 Modulation of cytokine secretion may offer novel approaches in the treatment of a variety of diseases. One strategy in the modulation of cytokine expression may be through the use of herbal medicines. A class of herbal medicines, known as immunomodulators, alters the activity of immune function through the dynamic regulation of informational molecules such as cytokines. This may offer an explanation of the effects of herbs on the immune system and other tissues. For this informal review, the authors surveyed the primary literature on medicinal plants and their effects on cytokine expression, taking special care to analyze research that utilized the multi-component extracts equivalent to or similar to what are used in traditional medicine, clinical phytotherapy, or in the marketplace. METHODOLOGY: MEDLINE, EBSCO, and BIOSIS were used to identify research on botanical medicines, in whole or standardized form, that act on cytokine activity through different models, i.e., in vivo (human and animal), ex vivo, or in vitro. RESULTS: Many medicinal plant extracts had effects on at least one cytokine. The most frequently studied cytokines were IL-1, IL-6, TNF, and IFN. Acalypha wilkesiana, Acanthopanax gracilistylus, Allium sativum, Ananus comosus, Cissampelos sympodialis, Coriolus versicolor, Curcuma longa, Echinacea purpurea, Grifola frondosa, Harpagophytum procumbens, Panax ginseng, Polygala tenuifolia, Poria cocos, Silybum marianum, Smilax glabra, Tinospora cordifolia, Uncaria tomentosa, and Withania somnifera demonstrate modulation of multiple cytokines. CONCLUSION: The in vitro and in vivo research demonstrates that the reviewed botanical medicines modulate the secretion of multiple cytokines. The reported therapeutic success of these plants by traditional cultures and modern clinicians may be partially due to their effects on cytokines. Phytotherapy offers a potential therapeutic modality for the treatment of many differing conditions involving cytokines. Given the activity demonstrated by many of the reviewed herbal medicines and the increasing awareness of the broad-spectrum effects of cytokines on autoimmune conditions and chronic degenerative processes, further study of phytotherapy for cytokine-related diseases and syndromes is warranted.

  Fingerprint of Polygala tenuifolia by high performance liquid chromatography.:Yao Xue Xue Bao. 2006 Feb;41(2):179-83. Chinese.Jiang Y, Zhang N, Cui Z, Tu PF.Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.

 AIM: To study and establish the fingerprint of Polygala tenuifolia by RP-HPLC. METHODS: The fingerprint of P. tenuifolia was built by using Kromasil C18 as column and acetonitrile-0.05% phosphoric acid aqueous in gradient as mobile phase. The flow rate was 1.0 mL x min(-1), and the detecting wavelength was set at 318 nm. Total 14 batches of P. tenuifolia from different habitats were detected, and different commodities and preparative methods were compared. RESULTS: Samples from different habitats were of high similarities, and the qualities of "yuanzhitong" and "yuanzhirou" were better than that of "yuanzhigun", while the fingerprints of P. tenuifolia with different preparative methods have not obvious differences. Moreover, the standard fingerprint of P. tenuifolia was originated from the "Computer Aided Similarity Evaluation" software, and 29 common peaks existed in the fingerprint. Each peak in the fingerprint was separated very well under the above chromatographic condition, with good accuracy, stability and repeatability, satisfied to the requests of fingerprint. CONCLUSION: The RP-HPLC fingerprint method can be used in the quality control of P. tenuifolia.


  Niche characteristics of dominant populations of Sophora davidii community in loess gully region.:Ying Yong Sheng Tai Xue Bao. 2005 Dec;16(12):2231-5. Chinese.Li D, Zhang W, Ren Z.Northwest Sci-Tech University of Agriculture and Forestry, Yangling 712100, China. dengwuli@yahoo.com.cn

 Based on field investigation data and employing Levin and niche proportional similarity formulae, this paper calculated the niche breadth, niche proportional similarity, and niche overlap of 13 dominant species of Sophora davidii community in loess gully region. The results showed that the niche breadth of the dominant populations of Sophora davidii community decreased in order of Sophora davidii (0.964), Artemisia giraldii (0.775), Arteniisia gmelinii (0.664), Thenmeda triandra var. japonica (0.508), Polygala tenuifolia (0.485), Setaria viridis (0.399), Cynodon dactylon (0.393), Bothriochloa ischaemum (0.327), Lespedeza davurica (0.321), Stipa bungeana (0.472), Periploca sepium (0.292), Clemnatis fruticosa (0.251), and Cleistogenes squarrosa (0.234). The niche proportional similarity between Sophora davidii and other species was 0.21-0.76, while the niche overlap was not high, which meant that there was no severe competition between them. It could be concluded that Sophora davidii was the dominant population in the community, with most resources utilization and most adaptability to the ecosystem.

  Effect of Polygala tenuifolia root extract on cerebral ischemia and reperfusion.:Am J Chin Med. 2006;34(1):115-23.Park JH, Kim JS, Jang DS, Lee SM.College of Pharmacy, Sungkyunkwan University, Suwon 440-746, South Korea.

 In this study, the effects of Polygala tenuifolia root extract on brain ischemia/reperfusion injury in Mongolian gerbils were investigated. The gerbils were administered ethanol extract of P. tenuifolia and its four sub-fractions orally 2 hours prior to ischemia, and were subjected to a 20-minute no-flow cerebral ischemia in vivo. Thirty minutes and 72 hours after reperfusion, the brain was removed and the ATP, lactate and lipid peroxide levels were determined, and the neurons in the hippocampal CA1 subfield were examined. In the vehicle-treated ischemic gerbils, the brain ATP levels decreased significantly, but this decrease was prevented by pre-treatment with an n-butanol fraction of P. tenuifolia. In contrast, both the lactate content and lipid peroxidation levels were elevated in the vehicle-treated ischemic animals, but this elevation was inhibited by ethanol extract and n-butanol fraction of P. tenuifolia, respectively. Both the ethanol extract and n-butanol fraction of P. tenuifolia attenuated post-ischemic neuronal necrosis in the hippocampal CA1 subfield. Our findings suggest that both ethanol extract and n-butanol fraction of P. tenuifolia root can reduce brain damage during ischemia and reperfusion, and prevent lipid peroxidation and preserve the energy metabolism.

  Four new phenones from the cortexes of Polygala tenuifolia.:Chem Pharm Bull. 2005 Sep;53(9):1164-6.Jiang Y, Tu P.Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center; Beijing 100083, China

 From the 95% EtOH extract of the cortexes of Polygala tenuifolia, four new phenones and three known xanthones were isolated. The structures of the four new phenones were identified as 4-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-2-hydroxyl-6-methoxybenzophenone (tenuiphenone A, 1), 3,5-di-C-beta-glucopyranosyl-2,4,6,3'-tetrahydroxybenzophenone (tenuiphenone B, 2), 2',4',6'-trihydroxyphenyl-(24Z)-triacontene-1-one (tenuiphenone C, 3), 2',4',6'-trihydroxyphenyl-(26Z)-dotriacontene-1-one (tenuiphenone D, 4) respectively, on the basis of spectroscopic analyses. The isolation of 1 and 2 supplied an evidence for the hypothesis that xanthone was biosynthesized from benzophenone in the plants.

  Xanthone glycosides from Polygala tenuifolia and their conformational analyses.:J Nat Prod. 2005 Jun;68(6):875-9.Jiang Y, Zhang W, Tu P, Xu X.School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing, People's Republic of China.

 Seven xanthone glycosides were isolated from the cortexes of Polygala tenuifolia, and their structures were identified as polygalaxanthones VIII-XI (1-4), sibiricoxanthone B (5), 7-O-methylmangiferin (6), and lancerin (7), on the basis of spectroscopic analyses. Compounds 1-4 are new xanthone glycosides, and compounds 4 and 5 exist as rotamers. To explain this phenomenon, conformational analyses were performed on compounds 4 and 5 and other compounds with similar skeletons that were isolated from P. tenuifolia.

  Different mechanisms mediated the potentiation uterine smooth muscle caused by Polygala tenuifolia decoction progesterone in virginal rats.:Zhongguo Zhong Yao Za Zhi. 2005 Feb;30(4):295-7, 319. Chinese.Xu JD, Wang W, Qin XM.Department of physiology, Capital University of Medical Science, Beijing 100054, China. xujingdong@163.com

 OBJECTIVE: To research the effects of Polygala tenuifolia decoction on myoelectric activity of uterine smooth muscle and contractile activity of uterine smooth muscle strips of virginal rats. METHOD: To record the effects of P. tenuifolia decoction on myoelectric activity of uterine smooth muscle and contractile activity of uterine smooth muscle strips of virginal rats with biolap 410 biological system. Five blocking agents were used to study their mechanisms respectively. RESULT: Different dosages of water extract of P. tenuifolia (0.02, 0.04, 0.08 g x kg(-1)), could significantly potentiate uterine myoelectric activity and contractile activity of virginal rats. CONCLUSION: The effect of P. tenuifolia on myoelectric activity of uterine smooth muscle and contractile activity of uterine smooth muscle strips in rats may be mainly associated with H1 receptor, L-voltage-dependant calcium channels or prostaglandin synthese, its nothing to M receptor.


  Occupational asthma and rhinitis induced by a herbal medicine, Wonji (Polygala tenuifolia).:J Korean Med Sci. 2005 Feb;20(1):46-9.Park HK, Jeon SG, Kim TB, Kang HR, Chang YS, Kim YK, Cho SH, Min KU, Kim YY.Department of Internal Medicine, Seoul National University College of Medicine, Korea.

 Occupational asthma is induced by many agents, including herbal materials, that are exposed in working places. Although there are a few case reports for occupational allergy induced by herbal materials, there is none for that induced by Wonji (Polygala tenuifolia). This study was conducted to evaluate clinical characteristics and immunologic mechanism of Wonji-induced asthma in a exposed-worker. A patient who complained of asthma and rhinitis symptoms, and who had worked in a herbal manufacturing factory for 8 yr, underwent a skin prick test with crude extract of Wonji under the impression of occupational asthma induced by the agent. The patient had a strong positive response to the extract on the skin prick test. Allergen bronchial challenge to the extract demonstrated a typical dual response. Serum specific IgE level to the extract was higher in the patient than in healthy controls, and ELISA inhibition test revealed complete inhibition of IgE binding with the extract, but no inhibition with Der p 2 or mugwort extracts. Six IgE binding components to the extract (10, 25, 28, 36, 50, and 90 kDa) were detected using SDS-PAGE and immunoblot analysis. These findings suggest that Polygala tenuifolia, a herbal material, can induce IgE-mediated bronchoconstriction in exposed workers.

  Studies on the chemical constituents in root bark of Polygala tenuifolia (II).:Zhongguo Zhong Yao Za Zhi. 2004 Aug;29(8):751-3. Chinese.Yong J, Tu PF.Modern Research Center of Traditional Chinese Medicine, Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100083, China.

 OBJECTIVE: To study the chemical constituents of Polygala tenuifolia. METHOD: Isolations were performed on various chromatography columns and structure elucidations were aided by spectral data and chemical property analyses. RESULT: Four 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). CONCLUSION: Compounds 1 and 2 were isolated from this plant for the first time.

  Polygalae radix extract protects cultured rat granule cells against damage induced by NMDA.:Am J Chin Med. 2004;32(4):599-610.Lee HJ, Ban JY, Koh SB, Seong NS, Song KS, Bae KW, Seong YH.College of Veterinary Medicine and Research Institute of Veterinary Medicine Chungbuk National University, Cheongju, Chungbuk, 361-763, Korea.

 Polygalae Radix (PR) from Polygala tenuifolia (Polygalaceae) is traditionally used in China and Korea, as this herb has a sedative, anti-inflammatory and antibacterial agent. To extend our understanding of the pharmacological actions of PR in the CNS on the basis of its CNS inhibitory effect, the present study examined whether PR has the neuroprotective action against N-methyl-D-aspartate (NMDA)-induced cell death in primarily cultured rat cerebellar granule neurons. PR, over a concentration range of 0.05 to 5 microg/ml, inhibited NMDA (1 mM)-induced neuronal cell death, which was measured by a trypan blue exclusion test and a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) assay. PR (0.5 microg/ml) inhibited glutamate release into medium induced by NMDA (1 mM), which was measured by HPLC. Pre-treatment of PR (0.5 microg/ml) inhibited NMDA (1 mM)-induced elevation of intracellular Ca2+ concentration ([Ca2+]i), which was measured by a fluorescent dye, Fura 2-AM, and generation of reactive oxygen species (ROS). These results suggest that PR prevents NMDA-induced neuronal cell damage in vitro.

  Effect of Polygala tenuifolia root on behavioral disorders by lesioning nucleus basalis magnocellularis in rat.:J Ethnopharmacol. 2004 Nov;95(1):47-55.Chen YL, Hsieh CL, Wu PH, Lin JG.Graduate Institute of Chinese Medical Science, China Medical University, 91 HSue-Hsi Rd., Taichung City, Taiwan.

 We investigated whether an aqueous extract of Polygala tenuifolia Willd (PTW) could improve the rats' memory and behavioral disorders produced by lesioning nucleus basalis magnocellularis (NBM) in rats. The animals were divided into four groups for surgery, and following that they were orally administered PTW extract for 7 and 21 days. Each group consisted of eight male Sprague-Dawley rats and were treated as follows: Control: no surgery (n = 8), PBS: 1M (mol/L) phosphate buffered saline (n = 8), IBO: 0.12 M (n = 8), QUIS: 0.12 M (n = 8). Two 0.5 microL injections were made in the vicinity of the bilateral side of the nucleus basalis magnocellularis (NBM). All rats were tested in the neurological tests and the step-through passive avoidance memory test during pre-surgery, surgery and post-surgery drug treatment. The results suggest that PTW extract has some repairing effects on the memory and behavioral disorders produced by lesioning of the NBM in rats.

  Tenuigenin treatment decreases secretion of the Alzheimer's disease amyloid beta-protein in cultured cells.:Neurosci Lett. 2004 Aug 26;367(1):123-8.Jia H, Jiang Y, Ruan Y, Zhang Y, Ma X, Zhang J, Beyreuther K, Tu P, Zhang D.Department of Biochemistry, Institute of Mental Health, Peking University, No. 51 Hua Yuan Bai Road, 100083 Beijing, China.

 Amyloid beta-protein (A beta) is a pivotal pathological factor in Alzheimer's disease (AD). Tenuigenin, extracted from the Chinese herb Polygala tenuifolia, seems to ameliorate the reduction in cholinergic function on rat models induced by A beta. To examine this therapeutic effect, we tested whether Tenuigenin could inhibit secretion of A beta in neuroblastoma cells stably transfected with two amyloid precursor protein (APP) constructs: the APP695 cDNA (SH-SY5Y APP695) and the C-terminal 99 amino acid residues of APP plus the signal peptide (SH-SY5Y SPA4CT). Tenuigenin inhibited the secretion of A beta and the C-terminal 99 amino acids of APP (C99) in SH-SY5Y APP695 cells, but did not change the A beta and C99 levels in SH-SY5Y SPA4CT cells. Fluorescence Resonance Energy Transfer (FRET) assays showed that Tenuigenin inhibited the proteolytic activities of BACE1 (beta-secretase) on its substrate in vitro. In addition, Tenuigenin did not demonstrate any cytotoxic effects, nor did it affect APP mRNA expression, holoAPP synthesis or sAPP alpha secretion. Our data suggest that Tenuigenin can inhibit the secretion of A beta in SH-SY5Y APP 695 cells via BACE1 inhibition. Taken together, these results suggest that Tenuigenin may be worthy of future study as an anti-AD drug.


  Anti-stress effects of 3,4,5-trimethoxycinnamic acid, an active constituent of roots of Polygala tenuifolia.:Biol Pharm Bull. 2004 Aug;27(8):1317-9.

 3,4,5-trimethoxycinnamic acid (TMCA) is one of the constituents in roots of Polygala tenuifolia WILLD. Our previous study revealed that oral administration of this compound prolongs sleeping time induced by hexobarbital in mice to exhibit sedative action. In the present study, we investigate the effects of TMCA on the stress induced with repeated cold exposure or intracerebroventricular injection of corticotrophin-releasing hormone (CRH). Both types of stress significantly reduced the sleeping time induced with pentobarbital in rat, which was significantly prolonged by intraperitoneal injection of TMCA. The intracerebroventricular injection of CRH significantly augmented the content of norepinephrine (NE) in locus coeruleus (LC) of rats, which was significantly suppressed by the intracerebroventricular injection of TMCA. These findings suggest that TMCA would exhibit sedative effects by suppressing NE content in LC.

  Cognitive improving and cerebral protective effects of acylated oligosaccharides in Polygala tenuifolia.:Biol Pharm Bull. 2004 Jul;27(7):1081-5.

 We studied the cognitive improving and cerebral protective constituents in the roots of Polygala tenuifolia Willdenow, a well-known Chinese traditional medicine prescribed for amnesia, neurasthenia, palpitation, noctural emission and insomnia. Tenuifoliside B (1), which is one of the acylated oligosaccharides in the roots of P. tenuifolia, showed the cerebral protective effect on potassium cyanide (KCN)-induced anoxia in mice, widely used as an animal model for cerebrovascular disease, and also had an ameliorative effect on the scopolamine-induced impairment of performance in passive avoidance task in rats. Compound 1 significantly enhanced oxotremorine-induced tremors in mice, suggesting that it ameliorated the scopolamine-induced impairment of passive avoidance response by enhancing the cholinergic system. These findings show that compound 1 has cognitive improving and cerebral protective effects.

  PAP 9704, a Korean herbal medicine attenuates methamphetamine-induced hyperlocomotion via adenosine A2A receptor stimulation in mice.:Biol Pharm Bull. 2004 Jun;27(6):906-9. Kwon YS, Nabeshima T, Shin EJ, Chun W, Jhoo JH, Jhoo WK, Wie MB, Jang CG, Chung H, Sung YE, Kim HC.Neurotoxicology program, College of Pharmacy, Kangwon National University, Chunchon, Korea.

 The effect of PAP 9704, a traditional prescription in Korea consisting of Polygala tenuifolia, Acorus gramineus, and Poria cocos at a ratio of 1:1:1 (dry weight), on methamphetamine (MA)-induced hyperlocomotion was examined in mice. The increased locomotor activity induced by MA (1 mg/kg/d, i.p. x 7) was significantly attenuated by co-administration with PAP 9704 (100 or 200 mg/kg/d, p.o. x 7) in a dose dependent manner. Consistently, it was found that the hyperlocomotor activity occurred in parallel with the expression of striatal fos-related antigen immunoreactivity. The adenosine A(2A) receptor antagonist, 1,3,7-trimethyl-8-(3-chlorostyryl)xanthine (0.5 or 1.0 mg/kg, i.p.), significantly reversed the pharmacological action of PAP 9704 in a dose related manner, but the adenosine A(1) receptor antagonist 8-cyclopentyl-1,3-dimethylxanthine (0.5 or 1.0 mg/kg, i.p.) and the A(2B) receptor antagonist alloxazine (1.5 or 3.0 mg/kg, i.p.) did not significantly affect this pharmacological action. Our results suggest that PAP 9704 prevents MA-induced hyperlocomotion, at least in part, via the stimulation of the adenosine A(2A) receptor.

  Studies on chemical constituents in roots of Polygala tenuifolia.:Zhongguo Zhong Yao Za Zhi. 2003 Sep;28(9):828-30. Chinese.Wang H, Tong YX, Ye WC, Zhao SX.Department of Phytochemistry, China Pharmaceutical University, Nanjing 210009, Jiangsu, China.

 OBJECTIVE: To study the chemical constituents from the roots of Polygala tenuifolia. METHOD: Column chromatographic techniques were employed for isolation and purification of chemical constituents of the plant and the structures were elucidated by spectroscopic analysis. RESULT: Five chemical constituents were isolated and elucidated as 4-C-beta-glucopyranosyl-1,3,6-trihydroxy-7-methoxyxanthone (1), 4-C-[beta-D-apiofuranosyl-(1-->6)-beta-D-glucopyranosyl]-1,3,6- trihydroxy-7-methoxyxanthone (2), presenegenin (3), presenegenin-3-O-beta-D-glycopyranoside (4) and daucosterol (5), respectively. CONCLUSION: Compounds 1,3,4 and 5 were isolated from this plant for the first time. Compound 1 is a new natural product.

  Structural characteristics and spectroscopic profiles of xanthones from Polygala.:Beijing Da Xue Xue Bao. 2004 Feb;36(1):94-8. Review. Chinese.Jiang Y, Tu PF.Modern Research Center of TCM, Peking University School of Pharmaceutical Sciences, Beijing 100083, China. jiangy02@163.com

 Through studies of xanthones from Polygla tenuifolia, one of the main medicinal plants of Polygala, the structural characteristics and spectroscopic rules (including IR, UV, (1)H NMR and (13)C NMR data) of xanthones from Polygala were summarized, combined with the reference reports of this type of compounds from the other plants of Polygala. It is helpful to the structure elucidation of xanthones.


  Tenuifoliose Q, a new oligosaccharide ester from the root of Polygala tenuifolia Willd.:J Asian Nat Prod Res. 2003 Dec;5(4):279-83.Jiang Y, Tu PF.Modern Research Center of TCM, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100083, China.

 From the cortexes of Polygala tenuifolia Willd., a new oligosaccharide ester, tenuifoliose Q (1), was isolated together with three known compounds. The structure of 1 was elucidated by spectroscopic and physiochemical analysis as an oligosaccharide esterified with acetic, benzoic and p-hydroxycinnamoyl acid.

  Induction of NGF synthesis in astrocytes by onjisaponins of Polygala tenuifolia,:Phytomedicine. 2003 Mar;10(2-3):106-14.

 The effect of Ren-shen-yang-rong-tang in Chinese on nerve growth factor (NGF) secretion from the cultured rat astrocytes was examined in vitro. When rat embryo astrocytes were cultured in the presence of NYT for 24 h, the amount of NGF in the medium was significantly increased in a dose dependent manner. Among 14 kinds of component herbs in NYT, the roots of Polygala tenuifolia and roots of Panax ginseng extracts increased NGF levels from the astrocytes. Saponin fraction from the roots of P. tenuifolia enhanced the production of NGF, however phenolic glycoside fraction showed no effect. Onjisaponins A, B, E, F and G as major saponins of the root of P. tenuifolia strongly increased the NGF level, whereas ginsenosides Rb1 and Rg1 did not affect the NGF level. Onjisaponin F also induced ChAT mRNA level in rat basal forebrain cells. These results indicate the possibility that NYT and/or onjisaponins in P. tenuifolia may have potential therapeutic effects for the treatment of Alzheimer disease patients.

  Studies on chemical constituents of fat oil of Polygala tenuifolia.:Zhong Yao Cai. 2000 Jan;23(1):35-7. Chinese.Sun X, Shi S, Yang G.Department of Pharmaceutical Science of Shanxi Medical University, Taiyuan 030001.

 OBJECTIVE: To study the chemical constituents of fat oil from root of Polygala tenuifolia Willd. METHOD: The components were separated and identified by gas chromatograpy-mass spectrometry and elucidated on the standard mass spectral data and the percentages were determined by gas chromatographic area normalization method. RESULT: Eighteen constituents were separated and sixteen of them were identified. CONCLUSION: The major components of the fat oil were established first time as oleic acid, linoleic acid, palmitic acid, eicosenoic acid and stearic acid, which make up 87.0%, 7.31%, 3.27%, 1.07%, 0.91% of fat oil respectively.

  Novel cognitive improving and neuroprotective activities of Polygala tenuifolia Willdenow extract, BT-11.:J Neurosci Res. 2002 Nov 1;70(3):484-92.Park CH, Choi SH, Koo JW, Seo JH, Kim HS, Jeong SJ, Suh YH. Department of Pharmacology, College of Medicine, National Creative Research Initiative Center for Alzheimer's Dementia and Neuroscience Research Institute, MRC, Seoul National University, Seoul, South Korea.

 We carried out this study to search a new active constituent that had cognitive enhancing activity and low side effects from natural source. We found that the extract of dried root of Polygala tenuifolia Willdenow (BT-11, 10 mg/kg, i.p.) could significantly reverse scopolamine-induced cognitive impairments in rat, using a passive avoidance and a water maze test. We also investigated the effects of BT-11 on neurotoxicity induced by glutamate (Glu) and toxic metabolites of amyloid precursor protein (APP) such as amyloid beta protein (A beta) and C-terminal fragment of APP (CT) in primary cultured neurons of rat. The pretreatment of BT-11 (0.5, 3, and 5 micro g/ml) significantly reduced cell death induced by Glu (1 mM), A beta (10 micro M) and CT105 (10 micro M) in a dose-dependent manner. In addition, BT-11 inhibited acetylcholinesterase (AChE) activity in a dose-dependent and non-competitive manner (IC(50) value; 263.7 micro g/ml). Our novel findings suggest the possibility that this extract may have some protective effects against neuronal death and cognitive impairments in Alzheimer's disease (AD), or other neurodegenerative diseases related to excitotoxicity and central cholinergic dysfunction.

  Xanthone O-glycosides from Polygala tenuifolia.:Phytochemistry. 2002 Aug;60(8):813-6. Jiang Y, Tu PF.Modern Research Center of TCM, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Haidian District, Beijing 100083, People's Republic of China.

 Four xanthone O-glycosides, polygalaxanthones IV-VII were isolated from the roots of Polygala tenuifolia Willd., together with eight known compounds. The structures of the four xanthone O-glycosides were established as 6-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-1-hydroxy-3,7-dimethoxyxanthone (polygalaxanthone IV), 6-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-1,3-dihydroxy-7-methoxyxanthone (polygalaxanthone V), 6-O-(beta-D-glucopyranosyl)-1,2,3,7-tetramethoxyxanthone (polygalaxanthone VI), and 3-O-[alpha-D-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl]-1,6-dihydroxy-2,7-dimethoxyxanthone (polygalaxanthone VII), respectively, on the basis of analysis of spectroscopic evidence.


  Behavioural pharmacology of polygalasaponins indicates potential antipsychotic efficacy.:Pharmacol Biochem Behav. 2002 Jan-Feb;71(1-2):191-5. Chung IW, Moore NA, Oh WK, O'Neill MF, Ahn JS, Park JB, Kang UG, Kim YS.Department of Neuropsychiatry, College of Medicine, Chungbuk National University, 62 Kaeshin-Dong, Hungdok-Gu, Cheongju, Chungbuk 361-711, South Korea.

 Polygalasaponins were extracted from a plant (Polygala tenuifolia Willdenow) that has been prescribed for hundreds of years to treat psychotic illnesses in Korean traditional medicine. Previous in vitro binding studies suggested a potential mechanism for its antipsychotic action, as polygalasaponin was shown to have an affinity for both dopamine and serotonin receptors [Psychopharmacol. Bull. 31 (1995) 139.]. In the present study we have investigated the functional in vivo actions of this material in tests that are predictive of dopamine and serotonin antagonist activities. Polygalasaponin (25-500 mg/kg) was shown to produce a dose-related reduction in the apomorphine-induced climbing behaviour (minimum effective dose [ED(min)] 25 mg/kg ip, 250 mg/kg sc and po), the 5-hydroxytryptamine (5-HTP)-induced serotonin syndrome (ED(min) 50 mg/kg ip) and the MK-801-induced hyperactivity (ED(min) 25 mg/kg ip) in mice. This compound also reduced the cocaine-induced hyperactivity (ED(min) 25 mg/kg ip) in rats. These results demonstrated that polygalasaponin has dopamine and serotonin receptor antagonist properties in vivo. This might suggest its possible utility as an antipsychotic agent.

  Onjisaponins, from the root of Polygala tenuifolia Willdenow, as effective adjuvants for nasal influenza and diphtheria-pertussis-tetanus vaccines.:Vaccine. 2001 Sep 14;19(32):4824-34.

 Active substances from hot water extracts from 267 different Chinese medicinal herbs were screened for mucosal adjuvant activity with influenza HA vaccine in mice. The extract from the root of Polygala tenuifolia was found to contain potent mucosal adjuvant activity. The active substances were purified and identified as onjisaponins A, E, F, and G. When each onjisaponin (10 microg) was intranasally (i.n.) inoculated with influenza vaccine (10 microg) in mice, serum hemagglutination-inhibiting (HI) antibody titers increased 3-14 times over control mice administered vaccine alone after 4 weeks. When each onjisaponin (10 microg) was i.n. inoculated with the vaccine (10 microg) followed by i.n. vaccination of the vaccine alone after 3 weeks, serum HI antibody titers increased 27-50 fold over those mice given i.n. vaccinations without onjisaponins. These same conditions also significantly increased nasal anti-influenza virus IgA antibody titers. Two inoculations with onjisaponin F (1 microg) and influenza HA vaccine (1 microg) at 3 weeks intervals, significantly increased serum HI antibody and nasal anti-influenza virus IgA and IgG antibody titers after only 1 week over mice given HA vaccine alone after the secondary vaccination. Intranasal vaccination with onjisaponin F inhibited proliferation of mouse adapted influenza virus A/PR/8/34 in bronchoalveolar lavages of infected mice. Separate intranasal vaccinations with onjisaponins A, E, F, and G (10 microg) each and diphtheria-pertussis-tetanus (DPT) vaccine (10 microg) of mice followed by i.n. vaccination with DPT vaccine alone after 4 weeks showed significant increases in serum IgG and nasal IgA antibody titers after 2 weeks following secondary vaccination over mice vaccinated with DPT vaccine alone. All onjisaponins showed little hemolytic activity at concentrations up to 100 microg/ml. The results of this study suggest that onjisaponins may provide safe and potent adjuvants for intranasal inoculation of influenza HA and DPT vaccines.

  Inhibitory effect of interleukin-1alpha-induced apoptosis by Polygala tenuifolia in Hep G2 cells.:Immunopharmacol Immunotoxicol. 2000 Aug;22(3):531-44.Koo HN, Jeong HJ, Kim KR, Kim JC, Kim KS, Kang BK, Kim HM, Kim JJ.Department of Oriental Pharmacy, College of Pharmacy, Wonkwang University, Chonbuk, South Korea.

 A human hepatoma cell line, Hep G2 cells are reliable for the study of alcohol-induced hepatotoxicity. In this study, we investigated the effect of an aqueous extract of Polygala tenuifolia WILLDENOW (Polygalaceae) roots (PTAE) on ethanol (EtOH)-induced cytotoxicity in Hep G2 cells. PTAE (0.01-1 microg/ml) dose-dependently inhibited the EtOH-induced interleukin-1alpha (IL-1alpha) secretion. PTAE (0.01-1 microg/ml) also inhibited the EtOH- and IL-1alpha-induced cytotoxicity. Furthermore, we found that PTAE inhibited the IL-1alpha-induced apoptosis of Hep G2 cells. These results suggest that PTAE may prevent the EtOH-induced cytotoxicity through inhibition of the apoptosis of Hep G2 cells.

  Effect of Polygala tenuifolia root extract on the tumor necrosis factor-alpha secretion from mouse astrocytes.:J Ethnopharmacol. 1998 Jul;61(3):201-8.Kim HM, Lee EH, Na HJ, Lee SB, Shin TY, Lyu YS, Kim NS, Nomura S.Department of Oriental Pharmacy, College of Pharmacy, Wonkwang University, Iksan, Chonbuk, South Korea.

 We investigated whether an aqueous extract of Polygala tenuifolia root (PTAE) inhibits secretion of tumor necrosis factor-alpha (TNF-alpha) from primary cultures of mouse astrocytes. PTAE dose-dependently inhibited the TNF-alpha secretion by astrocytes stimulated with substance P (SP) and lipopolysaccharide (LPS). Interleukin-1 (IL-1) has been shown to elevate TNF-alpha secretion from LPS-stimulated astrocytes while having no effect on astrocytes in the absence of LPS. We therefore also investigated whether IL-1 mediated inhibition of TNF-alpha secretion from primary astrocytes by PTAE. Treatment of PTAE to astrocytes stimulated with both LPS and SP decreased IL-1 secretion to the level observed with LPS alone. Moreover, incubation of astrocytes with IL-1 antibody abolished the synergistic co-operative effect of LPS and SP. These results suggest that PTAE may inhibit TNF-alpha secretion by inhibiting IL-1 secretion and that PTAE has an anti-inflammatory activity on the central nervous system curing some pathological disease states.

  Hoelen (Poria Cocos Wolf) and ginseng (Panax Ginseng C. A. Meyer), the ingredients of a Chinese prescription DX-9386, individually promote hippocampal long-term potentiation in vivo.:Biol Pharm Bull. 1995 Apr;18(4):518-22.

 DX-9386 is a traditional Chinese medicinal prescription consisting of ginseng (Panax Ginseng C. A. Meyer), polygala (Polygala Tenuifolia Willdenew), acorus (Acorus Gramineus Soland) and hoelen (Poria Cocos Wolf). We recently found that oral administration of the prescription at a dose of 500 mg/kg intensified the formation of long-term potentiation (LTP) in the dentoff gyrus of anesthetized rats. To evaluate the individual contribution of separate ingredients in DX-9386 towards the observed biological activity, we investigated their direct influence upon LTP formation in vivo. A single oral administration of hoelen and ginseng (250 and 500 mg/kg) significantly increased the spike amplitude evoked by a subthreshold tetanic stimulation at time intervals up to 30 min after tetanus. Only minor effects of polygala (500 mg/kg) and no influence of acorus up to 500 mg/kg were observed. No drugs affected the basal spike amplitude induced by a test stimulus. In addition, we ascertained that DX-9386 was also active at a dose of 250 mg/kg. Taken together, these results indicate that hoelen and ginseng are the active components of DX-9386 with regard to the enhancement of hippocampal LTP.


  Xanthone C-glycoside and acylated sugar from Polygala tenuifolia.:Chem Pharm Bull. 1994 Nov;42(11):2305-8.

 A new xanthone C-glycoside, polygalaxanthone III (1), and a new acylated sugar, tenuifoliside E (2) were isolated from the roots of Polygala tenuifolia. Their structures were characterized as 4-C-[beta-D-apiofuranosyl-(1-->6)-beta-D-glucopyranosyl]-1, 3,6-trihydroxy-7-methoxyxanthone (1) and beta-D-(1-O-acetyl-3-O-feruloyl-6-O-sinapoyl)-fructofuranosy l-alpha-D-(2,4,6- O-triacetyl)glucopyranoside (2), respectively, on the basis of chemical and spectral evidence including two dimensional nuclear magnetic resonance (2D-NMR) studies.

  Isolation and identification of tetrahydrocolumbamine as a dopamine receptor ligand from Polygala tenuifolia Willd.:Yao Xue Xue Bao. 1994;29(12):887-90.Shen XL, Witt MR, Dekermendjian K, Nielsen M.Department of Biochemistry, St. Hans Hospital, Roskilde, Denmark.

 The isolation and purification of a dopamine receptor ligand, tetrahydrocolumbamine from Polygala tenuifolia Willd is described. Tetrahydrocolumbamine was shown to inhibit the binding of [3H]-SCH23390 and [3H]-spiroperidol to rat striatum membranes in vitro with IC50 values of 0.75 +/- 0.08 mumol.L-1 and 0.92 +/- 0.10 mumol.L-1, respectively. The compound inhibited the binding of [3H]-prazosin (IC50 value of 46 mumol.L-1), while it did not change the binding of the ligands, [3H]-QNB and [3H]-muscimol to rat cortex in vitro. Scatchard plot analysis showed a mixture of competitive and non-competitive inhibition by the compound on both [3H]-SCH23390 and [3H]-spiroperidol binding to membranes from rat striatum.

  Studies on the alkaloidal components of Polygala tenuifolia willd.:Zhongguo Zhong Yao Za Zhi. 1993 Nov;18(11):675-7, 702-3. Chinese.Jin BY, Park J.Department of Pharmacy, Yanbian Medical College, Yengi.

 1-Carbobutoxy-beta-carboline, N9-formylharman, 1-carboethoxy-beta-carboline, 1-carbomethoxy-beta-carboline, perlolyrine, harman and norharman were isolated from the rhizoma of Polygala lenuifolia. The structures were elucidated on the basis of spectroscopic studies and chemical evidence, 1-carbobutoxy-beta-carboline has not been seported before.

  Observation on propagating experiments with Polygala tenuifolia Willd seed.:Zhongguo Zhong Yao Za Zhi. 1989 Aug;14(8):463-4, 510. Chinese.Xue H.

 This paper reports the harvesting and storing of Polygala tenuifolia seed, the operating process and method of seed propagation both in the laboratory and in the field, the relationship between Palygala tenuifolia seed germination, seed treatment and temperature and humidity, and the importance of suitable conditions and climatic factors in the sexual propagation of the seed.

  Screening of the wormicidal Chinese raw drugs on Clonorchis sinensis.:Am J Chin Med. 1981 Winter;9(4):277-84. Rhee JK, Woo KJ, Baek BK, Ahn BJ.

 The wormicidal effect on Clonorchis sinensis in boiled water extracts of 223 species (vegetable origin 206, animal origin 10, mineral origin 7) of raw drugs prescribed in Oriental medicine was observed in vitro. The wormicidal substances were detected from 31 of the above-mentioned species. The wormicidal substances extracted from Platycodon grandiflorum (radix), Schizandra chinensis (fruit), Polygala tenuifolia (herb) and Aster tataricus (radix) were most effective. Those from Smilax glabra (radix), Pueraria thunbergiana (flower, radix), Polygala tenuifolia (radix), Scutellaria baicalensis (radix), Prunus mume (fruit), Glycyrrhiza uralensis (radix), Angelica koreana (radix), Phytolacca esculenta (radix) and Cyrtomium fortunei (rhizoma) were effective. The rest of the raw drugs were less effective.


  Scientific References:

  1.Research Update:Polygala tenuifolia root,Polygala tenuifolia Willd,Polygala sibirica L