Evaluation method of medicine nature of individual ginsenosides / 中国药理学通报

.Aim To establish the evaluation methods of the med¬icine nature of ginsenosides by eorrelation analysis between med¬icine nature and ginsenoside contents in five Panax herbs with different medicine nature and the measurement of their effects on Na + /K + -ATPase activities.Methods 'Hie contents of ginsen¬osides in Sanqi, red ginseng , ginseng , American ginseng and ginseng leaves in the existing literature were eolleeted.and the medicinal nature was assigned by vector methods.rI1ie medicine nature of ginsenosides and the contribution of ginsenoside to the medicine nature were evaluated through bivariate correlation a- nalysis and grey eorrelation degree respectively.'Hie effects of ginsenosides on the Na+ /K +-ATPase activities of L02 eells and in pig eerebral cortex were measured to evaluate the medicine na¬ture of ginsenosides.Results Correlation results indicated that the order of correlation coefficients of ginsenosides to the warm and hot medicine nature was Rf > R1 > Rg3 > Rg2 > Rbl > Ro, while the order of correlation coefficients of ginsenosides to the eool and eold medicine nature was Rb2 > Re > Rd > Fll.Grey eorrelation degree analysis showed that the contribution of ginsen¬oside to the medicine nature was F11 > Re > Kg2 > Rd > Rb2 >Rbl > Rgl > Rc > Rg3 > R1 > Rf > Ro.The effects of ginsen- osides on Na +/K +-ATPase activities showed that the substance basis of the warm medicine nature was ginsenoside Rbl, Rb3, Rc, Rf, Rg2, Rgl, Rhl, Rg3, R1 and Ro, which increased the activity of Na + /K + -ATPase.While the cold and cool medi- cine nature were ginsenoside Rh2, Rd, Rh2, Re and oleanolic acid, which inhibited the activity of Na+/K

Investigation of Ecological Environment of Mountain Cultivated Panax ginseng and Their Associated Plants / 中国实验方剂学杂志

Objective:To investigate the ecological environment and associated plants of mountain cultivated Panax ginseng were investigated in Xifeng county，Kuandian Manchu autonomous county and Huanren Manchu autonomous county of Liaoning province，in order to provided suggestions on the development of the mountain cultivated P. ginseng in these areas and necessary reference materials for the analysis of ecological suitability of mountain cultivated P. ginseng. Method:The field survey was conducted through sample plot survey in the survey pattern ofbased on representative area-sample plot-quadrat，literature review and data collation， were conducted to record indicators， calculate relevant parameters and make summary. Result:The associated plants were investigated based on 42 samples of mountain cultivated ginseng collected. A total of 95 plant species were identified. The correlation analysis was made on the six main species with an occurrence frequency of higher than 33%， and they were all positively correlated. Asarum heterotropoides var. mandshuricum was the strongest，which was followed by Schisandra chinensis， and Tilia tuan was the strongest in the arbor layer. The survey also found many problems in these areas，such as fewer large-scale planting bases， more scattered households，mixed germplasms，irregular planting techniques，simple planting mode and less sources of economic income generation. Conclusion:Xifeng county，Kuandian county and Huanren county of Liaoning province boast a superior ecological environment and abundant resources of mountain cultivated P. ginseng. The survey gets the whole picture of the ecological environment and associated plants of mountain cultivated P. ginseng in representative areas of Liaoning province，so as to provide the basis for the further development of mountain cultivated P. ginseng cultivation industry and the promotion of mountain cultivated Panax ginseng economy.

Regulatory effects of Poria on substance and energy metabolism in cold-deficiency syndrome compared with heat-deficiency syndrome in rats / 中国天然药物

Recent studies have revealed that the property of drug is mainly associated with the body's substance and energy metabolism. The present study aimed to evaluate the drug property of Poria, called Fuling (FL) in traditional Chinese medicine (TCM), in terms of its effects on the substance and energy metabolism in rat models of cold-deficiency and heat-deficiency syndromes, compared with Aconiti Lateralis Radix Praeparaia, called Fuzi (FZ) in TCM, with hot property, and Anemarrhenae Rhizoma, called Zhimu (ZM) in TCM, with cold property, as reference drugs, respectively. The appearance score, toe and rectal temperatures of the animals treated were assessed at different time points. Several indices in vivo correlated with substance and energy metabolism (glucokinas, phosphoglycerate kinase, cytochrome c reductase, cytochrome c oxydase, and Na-K-ATPase), endocrine system (triiodothyronine, thyroxine, and 17-hydroxycorticosteroid), nervous system (acetylcholin esterase), and cyclic nucleotide system were determined. The changes in appearance score and indices in vivo suggested the successful establishment of cold-deficiency and heat-deficiency syndrome models. FZ reversed the decreased levels of indices (substance and energy metabolism and endocrine system) and alleviated the syndrome of cold-deficiency model, and ZM showed obviously therapeutic effect on heat-deficiency syndrome (appearance score, substance and energy metabolism, and endocrine system). FL could alleviate cold-deficiency syndrome and raise the decreased levels of glucokinas, phosphoglycerate kinase, cytochrome c reductase and triiodothyronine in cold-deficiency model, but had no significant effect on heat-deficiency syndrome. Drug property of FL was inferred as trending to "flat and warm", which still need further study. It was advisable to adopt both cold-deficiency and heat-deficiency models to study the drugs with "flat" property.

Regulatory effects of Poria on substance and energy metabolism in cold-deficiency syndrome compared with heat-deficiency syndrome in rats / 中国天然药物

Recent studies have revealed that the property of drug is mainly associated with the body's substance and energy metabolism. The present study aimed to evaluate the drug property of Poria, called Fuling (FL) in traditional Chinese medicine (TCM), in terms of its effects on the substance and energy metabolism in rat models of cold-deficiency and heat-deficiency syndromes, compared with Aconiti Lateralis Radix Praeparaia, called Fuzi (FZ) in TCM, with hot property, and Anemarrhenae Rhizoma, called Zhimu (ZM) in TCM, with cold property, as reference drugs, respectively. The appearance score, toe and rectal temperatures of the animals treated were assessed at different time points. Several indices in vivo correlated with substance and energy metabolism (glucokinas, phosphoglycerate kinase, cytochrome c reductase, cytochrome c oxydase, and Na-K-ATPase), endocrine system (triiodothyronine, thyroxine, and 17-hydroxycorticosteroid), nervous system (acetylcholin esterase), and cyclic nucleotide system were determined. The changes in appearance score and indices in vivo suggested the successful establishment of cold-deficiency and heat-deficiency syndrome models. FZ reversed the decreased levels of indices (substance and energy metabolism and endocrine system) and alleviated the syndrome of cold-deficiency model, and ZM showed obviously therapeutic effect on heat-deficiency syndrome (appearance score, substance and energy metabolism, and endocrine system). FL could alleviate cold-deficiency syndrome and raise the decreased levels of glucokinas, phosphoglycerate kinase, cytochrome c reductase and triiodothyronine in cold-deficiency model, but had no significant effect on heat-deficiency syndrome. Drug property of FL was inferred as trending to "flat and warm", which still need further study. It was advisable to adopt both cold-deficiency and heat-deficiency models to study the drugs with "flat" property.

Advance and prospect in studies on anaphylactoid reaction of traditional Chinese medicine injections / 中国中药杂志

Because of the rapid action and high bioavailability, traditional Chinese medicine injections (TCMIs) had been widely used in clinical critical field. In recent years, with the increasing reports of clinical adverse reaction, more and more attention was paid to them, and acute allergic reaction was the main adverse reaction. Acute allergic reaction included type-I anaphylaxis reaction and anaphylactoid reaction, the latter had been found in a variety of TCMIs and accounted for 77% of adverse reaction. But the mechanism of anaphylactoid reaction was not completely understood, the standard animal model for TCMIs was not established, and the technical guidance for anaphylactoid reaction was not formulated. Thus the three aspects included mechanism, evaluation index and evaluation methods of TCMIs for anaphylactoid were reviewed. Five ways including direct stimulating pathway, complement pathway, coagulation pathway, kallikrein-kinin pathway and acute allergic pathway were the main mechanism of anaphylactoid reaction; whole animal model and cell model were the main evaluation methods; the occurrence index and effect index were reviewed for the evaluation index analysis.

Triterpenes constituents from male flowers of Eucommia ulmoides / 中国中药杂志

Nine triterpenes compounds were isolated from the male flowers of Eucommia ulmoides by recrystallization and chromatographic techniques over silica gel, Sephadex LH-20, and RP-18 gel. Their chemical structures were identified on the basis of spectral analysis and as 3-oxo-12-en-ursane-28-O-α-L-arabinofuranosyl (1 --> 6) -β-D-glucopyranoside (1), 2α, 3β-dihydroxyurs-12-en-28-oic acid(28 --> 1) -β-D-glucopyranosyl ester (2), ursolic acid (3), α-amyrin (4), uvaol (5), ursolic acid acetate (6), 3-O-acetate oleanoic acid (7), betulinic acid (8), and betulinol (9). Compound 1 was a new compound, and compounds 2, 4-7 were isolated from the Eucommiu genus for the first time. Cytotoxic activity was tested for all the compounds against K562 and HepG2 cells. The results showed that only compound 3, exhibited cytotoxic activity.

Cytotoxic constituents from the leaves of Broussonetia papyrifera / 中国天然药物

AIM@#To investigate the chemical constituents from the leaves of Broussonetia papyrifera.@*METHODS@#The chemical constituents were isolated and purified by macroporous adsorptive resin D101, silica gel, and ODS column chromatography and preparative HPLC. Their structures were elucidated on the basis of 1D and 2D NMR analyses. In addition, their cytotoxic activity against human hepatoma carcinoma cells (HepG-2) were evaluated by the MTT method. Furthermore, RP-HPLC and colorimetric methods were used for the analysis of cosmosiin and total flavonoids.@*RESULTS@#A new lignan, together with five known compounds were obtained, and their structures were characterized as (+)-pinoresinol-4'-O-β-D-glucopyranosyl-4″-O-β-D-apiofuranoside (1), cosmosiin (2), luteolin-7-O-β-D-glucopyranoside (3), liriodendrin (4), 3, 5, 4'-trihydroxy-bibenzyl-3-O-β-D-glucoside (5), and apigenin-6-C-β-D-glucopyranside (6). Furthermore, RP-HPLC and colorimetric methods were established for the analysis of cosmosiin and total flavonoids.@*CONCLUSION@#Compound 1 was a new lignan, and compounds 5 and 6 were isolated for the first time from the title plant. Compounds 1, 4 and 6 showed definite activities against HepG-2, while the other compounds didn't show inhibitory effects. The optimal harvest time of B. papyrifera (L.) Vent. is September.

Splitted fractions and unoverlapping analysis of chemical constituents of Poria cocos / 中国中药杂志

With the combined applications of steam distillation, water extraction and alcohol precipitation, liquid-liquid extraction and column chromatography over macroporous resin, a splitted-fractions method of the chemical constituents of Poria cocos was established. The unoverlapping property of the fractions of P. cocos was qualitatively analysed by using principal component analysis and cluster analysis. With angle cosine, squared euclidean distance and the overlapping analysis of peak area of crude herbs, the unoverlapping property of the fractions of P. cocos was half-quantitatively analysed. The chemical components of P. cocos was divided into the fractions of polysaccharide, petroleum ether, ethyl acetate, alcohol eluate from macroporous resin and water eluate from macroporous resin. Non similarity degree among each chemical fraction was above 80% and main chemical components were identified. The established method for splitting fractions of P. cocos has good stability and repeatability and all chemical components in P. cocos could be completely divided into six fractions. It is the first time that the author half-quantitatively analyse the unoverlapping property of the chemical fractions of P. cocos.

Determination of plasma protein binding rate of arctiin and arctigenin with ultrafiltration / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the plasma protein binding rate of arctiin and arctigenin.</p><p><b>METHOD</b>The ultrafiltration combined with HPLC was employed to determine the plasma protein binding rate of arctiin and arctigenin as well as rat plasma and healthy human plasma proteins.</p><p><b>RESULT</b>The plasma protein binding rate of arctiin with rat plasma at the concentrations of 64. 29, 32.14, 16.07 mg x L(-1) were (71.2 +/- 2.0)%, (73.4 +/- 0.61)%, (78.2 +/- 1.9)%, respectively; while the plasma protein binding rate of arctiin with healthy human plasma at the above concentrations were (64.8 +/- 3.1)%, (64.5 +/- 2.5)%, (77.5 +/- 1.7)%, respectively. The plasma protein binding rate of arctigenin with rat plasma at the concentrations of 77.42, 38.71, 19.36 mg x L(-1) were (96.7 +/- 0.41)%, (96.8 +/- 1.6)%, (97.3 +/- 0.46)%, respectively; while the plasma protein binding rate of arctigenin with normal human plasma at the above concentrations were (94.7 +/- 3.1)%, (96.8 +/- 1.6)%, (97.9 +/- 1.3)%, respectively.</p><p><b>CONCLUSION</b>The binding rate of arctiin with rat plasma protein was moderate, which is slightly higher than the binding rate of arctiin with healthy human plasma protein. The plasma protein binding rates of arctigenin with both rat plasma and healthy human plasma are very high.</p>

Plasma pharmacokinetics and tissue distribution of arctiin and its main metabolite in rats by HPLC-UV and LC-MS.

The pharmacokinetic profile of arctiin, the major active lignan in fruits of Arctium lappa L., was investigated. Its main meta"bolite arctigenin was identified by an LC-MS method, and an HPLC-UV technique was developed for the simultaneous quantification of the metabolite and arctiin in plasma and organs. Chromatographic separation was performed on an Agilent™ C18 HPLC column with acetonitrile and water by linear gradient elution. Arctiin and arctigenin were identified on-line by LC-MS. The pharmacokinetics and tissue distribution of arctiin and arctigenin were determined for the first time by using a simple, selective, and accurate HPLC method. The AUC0-t values of arctigenin were larger compared with arctiin after oral administration of arctiin. The concentration of the metabolite was significantly higher than the concentration of arctiin in the stomach and small intestine in rats after oral administration of arctiin, indicating that the stomach and small intestine were the major organs of arctiin metabolism. These findings could provide support for the clinical studies conducted with Fructus Arctii.

Synthesis of (-)-arctigenin derivatives and their anticancer activity.

The natural dibenzylbutyrolactone type lignanolide (-)-arctigenin, which was prepared from fructus arctii, showed obvious anticancer activity. The synthesis of four new (-)-arctigenin derivatives and their anticancer bioactivities were examined. The structures of the four new synthetic derivatives were elucidated.

Prediagnostic methods for the hemolysis of herbal medicine injection.

ETHNOPHARMACOLOGICAL RELEVANCE: The Xue-Sai-Tong injection, a traditional Chinese medicine injection with total saponins extracted from Sanchi Ginseng, has been used for more than half a hundred years to treat coronary artery disease. The study is to establish a prediagnostic method for the hemolytic adverse effect of herbal medicine injection by taking Xue-Sai-Tong injection as an example. MATERIALS AND METHODS: A new method named "fuzzy dissemination" was established to identify the hemolytic ginsenosides in Xue-Sai-Tong injection on the basis of fuzzy changes of individual ginsenosides in the injections altered by re-adding the fractions prepared from the total saponins and statistic analysis between hemolytic degrees and individual ginsenosides. Related substances test, safety tests and fingerprints of the injections in different batches were tested. RESULTS: HD(50), P(50) and interactions on hemolysis of individual ginsenosides were examined. Experiment indicated that the content of Rg(1), Rg(2), M(51) (an unknown ingredient with retention time at 51 min in HPLC) and M(70) in Xue-Sai-Tong injection showed a significant positive correlation with hemolytic degree, and the content of R(1), Re, Rb(1) and Rd showed a significant negative correlation with hemolytic activity. Furthermore HD(50) of injection exhibits superiority to other tests for the hemolysis of injections. Abnormal hemolysis in some batches of injections was observed, but there were no significant differences among injections of different batches in related substances test, safety test and fingerprints. CONCLUSIONS: This is an original method to analyze active ingredients of a complicated integrity instead of studying on individual ingredients, it showed that the interactions of some individual ginsenosides and some unknown micro-ingredients in Xue-Sai-Tong injection were the major factors causing hemolysis, and this method could also be utilized in research of corresponding aspects. HD(50) of injection can reflect the changes of hemolytic property of injections caused by not only the change of active constituents of injection, but also the auxiliary materials. Thus it was recommended as an index for the hemolytic prediagnosis of the injections in practice.

A new hexenol glycoside from leaves of Smallanthus sonchifolius.

A new hexenol glycoside with two known compounds was isolated from the leaves of Smallanthus sonchifolius. The structure of the new compound was elucidated as Z-hex-3-en-1-ol O-alpha-L-arabinopyransyl (1''-2')-beta-D-glucopyranoside (1) on the basis of spectroscopic analysis and chemical evidence. The two known compounds were identified as ent-15ß-hydroxy-kaur-16-en-19-oic acid (2) and ent-18-hydroxy-kaur-16-en-19-oic acid (3) by comparison of their spectral data with the reported data. Compounds 2 and 3 were isolated for the first time from the title plant.

New compounds from leaves of Smallanthus sonchifolius.

A new octadecatrienoic acid and a new benzyl glycoside, along with a known compound, were isolated from the leaves of Smallanthus sonchifolius. The structures of the two new compounds were elucidated as 13(R)-hydroxy-octadeca-(9E,11E,15Z)-trienoic acid (1) and benzyl alcohol 7-O-alpha-L-arabinopyranosyl(1" --> 2')-beta-D-glucopyranoside (2) on the basis of spectroscopic analysis and chemical evidence. The known compound was identified as 13(R)-hydroxy-octadeca-(9Z,11E,15Z)-trienoic acid (3) by comparison of its spectral data with that reported. Compound 3 was isolated for the first time from the title plant.

Saponins of polygalacic acid type from Platycodon grandiflorum / 药学学报

<p><b>AIM</b>To isolate triterpene saponins of polygalacic acid type from the roots of Platycodon grandiflorum (Jacq.) A. DC and to identify their structures.</p><p><b>METHODS</b>The compounds were separated by means of extraction, chromatography on silica gel, MPLC and HPLC, and their structures were elucidated on the basis of spectral analyses (FAB-MS, IR, 1H NMR, 13C NMR etc.).</p><p><b>RESULTS</b>Three triterpene saponins were isolated from the roots of Platycodon grandiflorum. They were identified as 3-O-beta-D-laminaribiosyl polygalacic acid (I), 3-O-beta-D-glucopyranosyl polygalacic acid (II), polygalacin D (III), separately.</p><p><b>CONCLUSION</b>Compound I is a new compound, compounds II, III are known triterpene saponins. The compound I and II were isolated from the plant for the first time, which is also the monodesmoside from the plant for the first time.</p>

Study on chemical constituents from Opuntia dillenii / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical composition of Opuntia dillenii.</p><p><b>METHOD</b>Many kinds of chromatography methods were used in the isolation procedure, while the structures of isolated compounds were determined on the aids of NMR and MS spectral analysis.</p><p><b>RESULT</b>A new compound, together with five known compounds, was isolated form the 80% ethanolic extract of its stems.</p><p><b>CONCLUSION</b>The new compound was characterized as opuntioside. Four compounds were obtained for the first from the genus Opuntia, and they were daucosterol, p-hydroxybenzoicacid, L-(-)-malic acid, (E)-ferulic acid. Opuntiol was also separated for the first from the plant.</p>

Ginsenoside-Ro enhances cell proliferation and modulates Th1/Th2 cytokines production in murine splenocytes / 药学学报

<p><b>AIM</b>To study the effects of ginsenoside-Ro on cell proliferation and cytokine production in murine splenocytes.</p><p><b>METHODS</b>The effect of ginsenoside-Ro on murine splenocytes proliferation was studied using [3H] thymidine incorporation assay. Effects of ginsenoside-Ro on the production of cytokines interleukin-2 (IL-2), interferon-gamma (IFN-gamma) and interleukin-4 (IL-4) from murine splenocytes were detected by ELISA method. Effects of ginsenoside-Ro on mRNA level of Th1 cytokine IFN-gamma and Th2 cytokine IL-4 were evaluated by reverse transcription polymerase chain reaction (RT-PCR) analysis.</p><p><b>RESULTS</b>Ginsenoside-Ro showed no mitogenic effect on unstimulated murine splenocytes. It enhanced the proliferation of Con A-induced murine splenocytes and the production of IL-2 at concentrations of 1-10 micromol x L(-1). Moreover, ginsenoside-Ro increased the production and expression of Th2 cytokine IL-4 and decreased the production and expression of Th1 cytokine IFN-gamma in Con A-induced murine splenocytes at concentrations of 2-10 micromol x L(-1).</p><p><b>CONCLUSION</b>Ginsenoside-Ro showed immunomodulatory effects by regulating the production and expression of Th1/Th2 cytokines in murine splenocytes.</p>

Studies on dihydroflavonol glycosides from rhizome of Smilax glabra / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents from the rhizomes of Smilax glabra.</p><p><b>METHOD</b>The compounds were isolated by column chromatography with silica gel, Diaion HP-20 and ODS as packing materials, and HPLC. Their structures were determined on the basis of their spectral evidence.</p><p><b>RESULT</b>5 dihydro-flavonol glycosides were identified as: astilbin (1), neoastilbin (2), isoastilbin (3), neoisoastilbin (4), (2R, 3R)-taxifolin-3'-O-beta-D-pyranglucoside (5).</p><p><b>CONCLUSION</b>Compounds 2, 4, 5 were isolated from this plant for the first time.</p>

Study on the chemical constituents of the roots of commercial ginseng / 中国中药杂志

<p><b>OBJECTIVE</b>To isolate and elucidate the constituents from the roots of Commercial Ginseng.</p><p><b>METHOD</b>Column chromatography and HPLC were used to isolate chemical constituents. Physico-chemical characters and spectr-oscopic analysis were employed for structural identification.</p><p><b>RESULT</b>Sixteen compounds were identified as: notoginsenoside-R2(1), ginsenoside-Rg2(2), 20 (R)-Rg2 (3), ginsenoside-Rg1 (4), -Rf(5), -Re(6), -Rd(7), -Rc(8), -Rb1(9), -Rb2(10), -Rb3(11), -Ra3(12), -Ra2(13), -Ra1 (14), notoginsenoside-R4(15) and ginsenoside -Ro(16).</p><p><b>CONCLUSION</b>Compound 1 was obtained from the plant for the first time.</p>

The isolation and identification of a new alpha-pyrone from Opuntia dillenii / 药学学报

<p><b>AIM</b>To study the chemical composition of Opuntia dillenii Haw.</p><p><b>METHODS</b>Many kinds of chromatography methods were used to separate the chemical constituents. Their structures were determined by NMR and MS spectral analysis.</p><p><b>RESULTS</b>A new compound, together with five known compounds, were isolated from the 80% ethanolic extract of the stems.</p><p><b>CONCLUSION</b>The new compound was identified as 4-ethoxyl-6-hydroxymethyl-alpha-pyrone. Compounds 1, 3, 4 and 5 were obtained for the first time from the genus of Opuntia, and they were: 3-O-methyl isorhamnein, 1-heptanecanol, vanillic acid, isorhamnetin-3-O-beta-D-rutinoside. Ruin was isolated from this plant for the first time.</p>