From the whole plant of Boschniakia rossica (Cham. et Schlech.) Fedtsch. et Flerov., a new phenylpropanoid glycoside (2) was isolated together with fourteen known compounds which include two phenylpropanoid glycosides [rossicaside B (1) and rossicaside A (3)], triandrin (4), boschniakinic acid (5),two iridoid glucosides [boschnaloside(6), 8-epideoxyloganic acid (7)], three triterpenoids [3-epioleanolic acid (8), 3-epiacetyloleanolic acid (9), oleanolic acid (10)], β-sito-sterol (11), and four iridoid aglycones [1,10-bisdeoxy-7,8-dihydrogenipin (12), 7-methyl-octahy-dro-cyclopenta [c]pyran-4-carboxylic acid (13), (1R) and (1S) 1-O-methyl-8-epideoxyloganic acid aglycone (14, 15)].
{"title":"New Phenylpropanoid Glycoside from Boschniakia rossica","authors":"Lie-Chwen Lin, K. Chen","doi":"10.7019/CPJ.200404.0077","DOIUrl":"https://doi.org/10.7019/CPJ.200404.0077","url":null,"abstract":"From the whole plant of Boschniakia rossica (Cham. et Schlech.) Fedtsch. et Flerov., a new phenylpropanoid glycoside (2) was isolated together with fourteen known compounds which include two phenylpropanoid glycosides [rossicaside B (1) and rossicaside A (3)], triandrin (4), boschniakinic acid (5),two iridoid glucosides [boschnaloside(6), 8-epideoxyloganic acid (7)], three triterpenoids [3-epioleanolic acid (8), 3-epiacetyloleanolic acid (9), oleanolic acid (10)], β-sito-sterol (11), and four iridoid aglycones [1,10-bisdeoxy-7,8-dihydrogenipin (12), 7-methyl-octahy-dro-cyclopenta [c]pyran-4-carboxylic acid (13), (1R) and (1S) 1-O-methyl-8-epideoxyloganic acid aglycone (14, 15)].","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"53 1","pages":"77-85"},"PeriodicalIF":0.0,"publicationDate":"2004-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77852451","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
W. Lo, Y. Wu, T. Hsieh, S. Kuo, Honghui Lin, Chung-Yi Chen
Phytochemical investigation of the stems of Michelia compressa was performed by column chromatography. We isolated four aporphines, including (-)-anonaine (1), (-)-norushinsunine (2), (-)-ushinsunine (3), (-)-3-hydroxynornuciferine (4); one oxoaporphine, liriodenine (5); two amides, N-trans-feruloyltyramine (6), N-cis-feruloyltyramine (7); one lignan, (+)-syringaresinol (8); two neolignans, 2R,3S-dihydrodehydroconiferyl alcohol (9), 2S,3R-dihydrodehydroconiferyl alcohol (10); one benzenoid, vanillic acid (11), and two steroids, β-sitosterol (12) and stigmasterol (13) from the methanolic extract. The structures of these compounds were established on the basis of spectroscopic analysis.
{"title":"Chemical Constituents from the Stems of Michelia compressa","authors":"W. Lo, Y. Wu, T. Hsieh, S. Kuo, Honghui Lin, Chung-Yi Chen","doi":"10.7019/CPJ.200404.0069","DOIUrl":"https://doi.org/10.7019/CPJ.200404.0069","url":null,"abstract":"Phytochemical investigation of the stems of Michelia compressa was performed by column chromatography. We isolated four aporphines, including (-)-anonaine (1), (-)-norushinsunine (2), (-)-ushinsunine (3), (-)-3-hydroxynornuciferine (4); one oxoaporphine, liriodenine (5); two amides, N-trans-feruloyltyramine (6), N-cis-feruloyltyramine (7); one lignan, (+)-syringaresinol (8); two neolignans, 2R,3S-dihydrodehydroconiferyl alcohol (9), 2S,3R-dihydrodehydroconiferyl alcohol (10); one benzenoid, vanillic acid (11), and two steroids, β-sitosterol (12) and stigmasterol (13) from the methanolic extract. The structures of these compounds were established on the basis of spectroscopic analysis.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"26 1","pages":"69-75"},"PeriodicalIF":0.0,"publicationDate":"2004-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84511572","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
F. Wu, M. Tsai, Shao‐Wen Sun, Wen-Ying Yu, Po-Huang Lee
Sirolimus (SRL) is a potent immunosuppressant with a long elimination half-life. Steady-state trough concentration (C0 or C24) is a reliable index of its exposure. This study was designed to understand the influence of sampling time on SRL C24. Twenty-seven stable renal transplant recipients with normal liver function who received calcineurin inhibitor (CNI)/SRL/steroid were monitored after administration of SRL tablets or solution. The SRL C24 of eighteen patients was compared with blood concentrations taken at 20 hours after dosing (C20) of nine patients. Both SRL solution and tablets produced a significantly higher dose-adjusted SRL C20 than dose-adjusted SRL C24 (mean ± SD, 3.5±1.8 vs. 2.3±1.0 ng/mL/mg for SRL solution, p＜0.01; 3.5±1.5 vs. 2.6±1.0 ng/mL/mg for SRL tablets, p=0.04) at steady state. The C20 was higher than C24 for SRL solution (mean ± SD, 5.8±2.8 vs. 4.4±2.0 ng/mL, p＜0.01), but not for tablets (mean ± SD, 5.5±3.6 vs. 4.6±2.6 ng/mL, p=0.32). All the SRL levels were within therapeutic range. Although the difference may not be clinically significant when fix-dose SRL is used, sampling time may become significant when SRL-based regimens or adjusted-dose SRL is used.
西罗莫司(SRL)是一种有效的免疫抑制剂，消除半衰期长。稳态谷浓度(C0或C24)是其暴露的可靠指标。本研究旨在了解采样时间对SRL C24的影响。对27例接受钙调磷酸酶抑制剂(CNI)/SRL/类固醇治疗的肝功能正常且稳定的肾移植受者在给予SRL片剂或溶液后进行监测。将18例患者的SRL C24与9例患者给药后20小时的血药浓度(C20)进行比较。SRL溶液和片剂产生的剂量调整SRL C20均显著高于剂量调整SRL C24(平均±SD, SRL溶液3.5±1.8 vs 2.3±1.0 ng/mL/mg, p<0.01;稳定状态下，SRL片为3.5±1.5 vs. 2.6±1.0 ng/mL/mg, p=0.04)。SRL溶液C20高于C24(平均±SD, 5.8±2.8 vs. 4.4±2.0 ng/mL, p<0.01)，片剂C20高于C24(平均±SD, 5.5±3.6 vs. 4.6±2.6 ng/mL, p=0.32)。所有SRL水平均在治疗范围内。虽然当使用固定剂量的SRL时，这种差异在临床上可能不显着，但当使用基于SRL的方案或调整剂量的SRL时，采样时间可能变得显着。
{"title":"The influence of sampling time on sirolimus trough concentrations","authors":"F. Wu, M. Tsai, Shao‐Wen Sun, Wen-Ying Yu, Po-Huang Lee","doi":"10.7019/CPJ.200404.0087","DOIUrl":"https://doi.org/10.7019/CPJ.200404.0087","url":null,"abstract":"Sirolimus (SRL) is a potent immunosuppressant with a long elimination half-life. Steady-state trough concentration (C0 or C24) is a reliable index of its exposure. This study was designed to understand the influence of sampling time on SRL C24. Twenty-seven stable renal transplant recipients with normal liver function who received calcineurin inhibitor (CNI)/SRL/steroid were monitored after administration of SRL tablets or solution. The SRL C24 of eighteen patients was compared with blood concentrations taken at 20 hours after dosing (C20) of nine patients. Both SRL solution and tablets produced a significantly higher dose-adjusted SRL C20 than dose-adjusted SRL C24 (mean ± SD, 3.5±1.8 vs. 2.3±1.0 ng/mL/mg for SRL solution, p＜0.01; 3.5±1.5 vs. 2.6±1.0 ng/mL/mg for SRL tablets, p=0.04) at steady state. The C20 was higher than C24 for SRL solution (mean ± SD, 5.8±2.8 vs. 4.4±2.0 ng/mL, p＜0.01), but not for tablets (mean ± SD, 5.5±3.6 vs. 4.6±2.6 ng/mL, p=0.32). All the SRL levels were within therapeutic range. Although the difference may not be clinically significant when fix-dose SRL is used, sampling time may become significant when SRL-based regimens or adjusted-dose SRL is used.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"139 1","pages":"87-96"},"PeriodicalIF":0.0,"publicationDate":"2004-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80553453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A crucial difference between cancer cells and normal cells is the inability of cancer cells to undergo terminal differentiation. Alteration of methylation enzymes plays a pivotal role in the blockade of terminal differentiation of cancer cells. Elimination of abnormal methylation enzymes is, therefore, a logical approach of cancer therapy. Methylation enzymes play a central role in the regulation of cell replication, differentiation, and apoptosis. When these enzymes are activated, cells enter cell cycle replicating; and when these enzymes become inactive, replicating cells are then diverted into terminal differentiation or apoptosis. The activity of these enzymes in normal stem cells is strictly under the regulation of an exogenous growth factor. Cancer cells, on the other hand, produce a cancer specific endogenous protein factor to lock these enzymes in the active state. Thus, cancer cells keep on dividing. This cancer specific protein factor is an attractive molecular target for cancer therapy, which can be selectively antagonized by CDA-Ⅱ*. CDA-Ⅱ is a preparation derived from fresh human urine. Once abnormal methylation enzymes are corrected by CDA-Ⅱ to become normal enzymes, cancer cells are then induced to undergo terminal differentiation or apoptosis. The action of CDA-Ⅱ is selective on cancer cells, thus the therapy is free of adverse side effects. Better yet, many abnormal behaviors characteristic of cancer cells disappear naturally as a consequence of differentiation induced by CDA-Ⅱ, which include abnormal expression of oncogenes, silencing of suppressor genes, drug resistance, metastasis, telomerase, and tumor markers. CDA-Ⅱ has been approved by the State Drug Administration of China to undergo clinical trial, which is now in the final stage of phase Ⅲ. So far the clinical studies are encouraging. The best clinical result in the application of CDA-Ⅱ was, however, demonstrated by Sano of Japan, who has initiated a very effective protocol by combination therapy with vitamin C, restriction of protein intake, and other nontoxic remedies.
{"title":"Abnormal Methylation Enzymes: A Selective Molecular Target for Differentiation Therapy of Cancer","authors":"M. Liau","doi":"10.7019/CPJ.200404.0057","DOIUrl":"https://doi.org/10.7019/CPJ.200404.0057","url":null,"abstract":"A crucial difference between cancer cells and normal cells is the inability of cancer cells to undergo terminal differentiation. Alteration of methylation enzymes plays a pivotal role in the blockade of terminal differentiation of cancer cells. Elimination of abnormal methylation enzymes is, therefore, a logical approach of cancer therapy. Methylation enzymes play a central role in the regulation of cell replication, differentiation, and apoptosis. When these enzymes are activated, cells enter cell cycle replicating; and when these enzymes become inactive, replicating cells are then diverted into terminal differentiation or apoptosis. The activity of these enzymes in normal stem cells is strictly under the regulation of an exogenous growth factor. Cancer cells, on the other hand, produce a cancer specific endogenous protein factor to lock these enzymes in the active state. Thus, cancer cells keep on dividing. This cancer specific protein factor is an attractive molecular target for cancer therapy, which can be selectively antagonized by CDA-Ⅱ*. CDA-Ⅱ is a preparation derived from fresh human urine. Once abnormal methylation enzymes are corrected by CDA-Ⅱ to become normal enzymes, cancer cells are then induced to undergo terminal differentiation or apoptosis. The action of CDA-Ⅱ is selective on cancer cells, thus the therapy is free of adverse side effects. Better yet, many abnormal behaviors characteristic of cancer cells disappear naturally as a consequence of differentiation induced by CDA-Ⅱ, which include abnormal expression of oncogenes, silencing of suppressor genes, drug resistance, metastasis, telomerase, and tumor markers. CDA-Ⅱ has been approved by the State Drug Administration of China to undergo clinical trial, which is now in the final stage of phase Ⅲ. So far the clinical studies are encouraging. The best clinical result in the application of CDA-Ⅱ was, however, demonstrated by Sano of Japan, who has initiated a very effective protocol by combination therapy with vitamin C, restriction of protein intake, and other nontoxic remedies.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"79 5 1","pages":"57-67"},"PeriodicalIF":0.0,"publicationDate":"2004-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87945149","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
H. Ding, Yaping Chen, Wen-liang Chang, Hang-Ching Lin
An isoflavone, 7, 8, 4'-trihydroxyisoflavone, and a peptide, (+)-3-(4-hydroxybenzyl)-6-iso butylpiperazine-2, 5-dione, together with eight known corn pounds including five isoflavonoids and three but-2-enolides were isolated from the roots of Pueraria lobata. Their structures were established on the basis of spectral evidence.
{"title":"Isoflavonoids and But-2-enolides from the Roots of Pueraria lobata","authors":"H. Ding, Yaping Chen, Wen-liang Chang, Hang-Ching Lin","doi":"10.7019/CPJ.200402.0031","DOIUrl":"https://doi.org/10.7019/CPJ.200402.0031","url":null,"abstract":"An isoflavone, 7, 8, 4'-trihydroxyisoflavone, and a peptide, (+)-3-(4-hydroxybenzyl)-6-iso butylpiperazine-2, 5-dione, together with eight known corn pounds including five isoflavonoids and three but-2-enolides were isolated from the roots of Pueraria lobata. Their structures were established on the basis of spectral evidence.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"399 1","pages":"31-35"},"PeriodicalIF":0.0,"publicationDate":"2004-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76693001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
T. Hsieh, Y. Wu, W. Lo, Sumi C. Chen, S. Kuo, Chung-Yi Chen
The chemical constituents of the leaves of Mahonia japonica were investigated by column chromatography. We isolated eight flavonoids, including quercetin (1), quercetin 3-O-β-D-glucopyranoside (2), quercetin 3-O-β-D-galactopyranoside (3), quercetin 3-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (4), isorhamnetin (5), isorhamnetin 3-O-β-D-glucopyranoside (6), isorhamnetin 3-O-β-D-galactopyranoside (7), and isorhamnetin 3-O-β-D-glucopyranosl-(1→6)-β-D-glucopyranoside (8), and four phenollic carboxylic acids, in cluding caffeic acid (9),p-hydroxy-benzoic acid (10), protocatechuic acid (11), and vanillic acid (12) from the n-BuOH soluble fraction of the methanolic extract. The structures of these com pounds were established by spectroscopic and chemical analysis.
采用柱层析法研究了日本麻风叶的化学成分。分离得到槲皮素(1)、槲皮素3- o -β- d -葡萄糖苷(2)、槲皮素3- o -β- d -半乳糖糖苷(3)、槲皮素3- o -β- d -葡萄糖苷(1→6)、异鼠李素3- o -β- d -葡萄糖苷(4)、异鼠李素(5)、异鼠李素3- o -β- d -半乳糖糖苷(6)、异鼠李素3- o -β- d -葡萄糖苷(7)、异鼠李素3- o -β- d -葡萄糖苷(1→6)、异鼠李素3- o -β- d -葡萄糖苷(8)、4种酚类羧酸，分别为咖啡酸(9)、对羟基苯甲酸(10)、原儿茶酸(11)、从甲醇提取物的正丁醇可溶部分提取香草酸(12)。通过光谱和化学分析确定了这些化合物的结构。
{"title":"Chemical Constituents from the Leaves of Mahonia japonica","authors":"T. Hsieh, Y. Wu, W. Lo, Sumi C. Chen, S. Kuo, Chung-Yi Chen","doi":"10.7019/CPJ.200402.0017","DOIUrl":"https://doi.org/10.7019/CPJ.200402.0017","url":null,"abstract":"The chemical constituents of the leaves of Mahonia japonica were investigated by column chromatography. We isolated eight flavonoids, including quercetin (1), quercetin 3-O-β-D-glucopyranoside (2), quercetin 3-O-β-D-galactopyranoside (3), quercetin 3-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (4), isorhamnetin (5), isorhamnetin 3-O-β-D-glucopyranoside (6), isorhamnetin 3-O-β-D-galactopyranoside (7), and isorhamnetin 3-O-β-D-glucopyranosl-(1→6)-β-D-glucopyranoside (8), and four phenollic carboxylic acids, in cluding caffeic acid (9),p-hydroxy-benzoic acid (10), protocatechuic acid (11), and vanillic acid (12) from the n-BuOH soluble fraction of the methanolic extract. The structures of these com pounds were established by spectroscopic and chemical analysis.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"9 1","pages":"17-23"},"PeriodicalIF":0.0,"publicationDate":"2004-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86550378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The antiplatelet activity of eight principles isolated from the seed hulls of Arachis hypogaea L. (A. hypogaea) was determined in washed rabbit platelets. Six flavonoids including luteolin, 8-iso- pentenyl luteolin, eriodictyol, chrysoeriol, 8-isopentenyl chrysoeriol and 4', 5-dihydroxy-2”, 2”- dimethylpyrano[5”,6”:7,8]flavone (AHO6) inhibited platelet aggregation induced by arachidonic acid (AA), collagen, U46619, ADP, platelet-activating factor (PAF) and thrombin in a concentration-dependent manner. These flavonoids were most potent against AA-mediated platelet activation. The flavonoids not only suppressed the elevation of intracellular calcium ([Ca(superscript 2+)]i) but also increased cyclic AMP (cAMP) levels in platelets. Concomitantly, the five flavones degraded exogenously added cAMP as cilostamide did in platelet lysates containing adenylate cyclase inhibitor. But they didn't mimic forskolin to convert ATP to cAMP in platelet lysates containing cAMP phosphodiesterase inhibitor. These results indicate that the flavones act as cAMP phosphodiesterase inhibitors, which allows accumulation of intra-platelet cAMP and consequently represses increasing of [Ca(superscript 2+)]i) induced by the aggregation agonists. Furthermore, these flavonoids also affected AA-metabolism-related enzymes. 8-Isopentenyl chrysoeriol decreased malondialdehyde (MDA) and thromboxane B2(TXB2) formation but increased prostaglandin (PG)E2 and F(superscript 2a) formation from AA indicating its inhibitory activity of thromboxane synthase. The other five flavonoids all inhibited the activity of cyclooxygenase, decreasing AA-metabolites including MDA, TXB2, PGE2 and PGF(superscript 2a).
{"title":"Inhibition of Cyclic AMP Phosphodiesterase and Blockage of Arachidonate Metabolism by Antiplatelet Principles from the Seed Hulls of Arachis Hypogaea L.","authors":"W. Tsai, Yun-Lian Lin, Yen-Chen Ho, Y. Kuo","doi":"10.7019/CPJ.200310.0335","DOIUrl":"https://doi.org/10.7019/CPJ.200310.0335","url":null,"abstract":"The antiplatelet activity of eight principles isolated from the seed hulls of Arachis hypogaea L. (A. hypogaea) was determined in washed rabbit platelets. Six flavonoids including luteolin, 8-iso- pentenyl luteolin, eriodictyol, chrysoeriol, 8-isopentenyl chrysoeriol and 4', 5-dihydroxy-2”, 2”- dimethylpyrano[5”,6”:7,8]flavone (AHO6) inhibited platelet aggregation induced by arachidonic acid (AA), collagen, U46619, ADP, platelet-activating factor (PAF) and thrombin in a concentration-dependent manner. These flavonoids were most potent against AA-mediated platelet activation. The flavonoids not only suppressed the elevation of intracellular calcium ([Ca(superscript 2+)]i) but also increased cyclic AMP (cAMP) levels in platelets. Concomitantly, the five flavones degraded exogenously added cAMP as cilostamide did in platelet lysates containing adenylate cyclase inhibitor. But they didn't mimic forskolin to convert ATP to cAMP in platelet lysates containing cAMP phosphodiesterase inhibitor. These results indicate that the flavones act as cAMP phosphodiesterase inhibitors, which allows accumulation of intra-platelet cAMP and consequently represses increasing of [Ca(superscript 2+)]i) induced by the aggregation agonists. Furthermore, these flavonoids also affected AA-metabolism-related enzymes. 8-Isopentenyl chrysoeriol decreased malondialdehyde (MDA) and thromboxane B2(TXB2) formation but increased prostaglandin (PG)E2 and F(superscript 2a) formation from AA indicating its inhibitory activity of thromboxane synthase. The other five flavonoids all inhibited the activity of cyclooxygenase, decreasing AA-metabolites including MDA, TXB2, PGE2 and PGF(superscript 2a).","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"6 1","pages":"335-345"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88483578","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ray-Ling Huang, Quillan Huang, Chieh‐fu Chen, T. Chang, C. Chou
Niu-Chang-Chih, which is the fruiting body of Antrodia camphorata, is a folk medicine that has traditionally been used in Taiwan for treating food and drug poisoning, liver disease, and cancer. By using HBV producing cell line as an in vitro model system, we found that Niu-Chang-Chih displays anti-HBV effects on both wild-type and lamivudine-resistant mutants. The active compounds responsible for the anti-viral activities of Niu-Chang-Chih were further investigated and identified by anti-HBV assay directed fractionation. Specifically, out of the ten pure compounds isolated from Niu-Chang-Chih which includes one biphenyl, four ergostanes, and five lanostanes derivatives, 2,2',5,5'-tetramethoxy-3,4,3',4'-bis(methlylene-dioxy)-6,6'-dimethyl-biphenyl was positively identified as the single active compound responsible for the anti-viral effects on both wild-type and lamivudine-resistant mutant HBV.
{"title":"Anti-viral effects of active compounds from Antrodia camphorata on wild-type and lamivudine-resistant mutant HBV","authors":"Ray-Ling Huang, Quillan Huang, Chieh‐fu Chen, T. Chang, C. Chou","doi":"10.7019/CPJ.200310.0371","DOIUrl":"https://doi.org/10.7019/CPJ.200310.0371","url":null,"abstract":"Niu-Chang-Chih, which is the fruiting body of Antrodia camphorata, is a folk medicine that has traditionally been used in Taiwan for treating food and drug poisoning, liver disease, and cancer. By using HBV producing cell line as an in vitro model system, we found that Niu-Chang-Chih displays anti-HBV effects on both wild-type and lamivudine-resistant mutants. The active compounds responsible for the anti-viral activities of Niu-Chang-Chih were further investigated and identified by anti-HBV assay directed fractionation. Specifically, out of the ten pure compounds isolated from Niu-Chang-Chih which includes one biphenyl, four ergostanes, and five lanostanes derivatives, 2,2',5,5'-tetramethoxy-3,4,3',4'-bis(methlylene-dioxy)-6,6'-dimethyl-biphenyl was positively identified as the single active compound responsible for the anti-viral effects on both wild-type and lamivudine-resistant mutant HBV.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"44 1","pages":"371-379"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73180768","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chuen‐Neu Wang, I. Chen, Yun-Lian Lin, C. Chi, Chieh‐fu Chen, Y. Shiao
Amyloid β protein (Aβ) elicits a toxic effect on neurons in vitro and in vivo and has been proposed to play an important role in the pathogenesis of Alzheimer’s disease (AD). Previous studies have shown that aggregated Aβ can induce caspase-dependent apoptosis by oxidative stress in cultured neurons. Uncaria rhynchophylla (miq.) Jacks., a traditional Chinese herbal medicine, has been used in combination with other herbs for the treatment of cognitive disorders. The major components responsible for the neuroprotective effect remains unclear In the present study, 23 fractions (UR-EAs) and 24 subfractions (UR-EA-As and UR-EA-Bs) were isolated from the ethyl acetate extracts of Uncaria hirsuta Haviland, a Taiwanese Uncaria. Five fractions, UR-EA-8, -16, -17, -18 and -19, and 5 subfractions, UR-EA-A567, -B3, -B8, -B9 and -BlO, and a pure compound, catechin, purified from UR-EA-19, were identified as neuroprotective components. The neuroprotective mechanism of UR-EA-A567, -B3 and -B9 were studied. All three fractions reduced Aβ-induced cytochome c release and nucleus condensation suggesting that Aβ-induced apoptosis was inhibited by the fractions. Nevertheless, three fractions had distinct effects on the activity of caspases. UR-EA-A567 abrogated Aβ-induced activation of caspase 2, 3, and 8. UR-EA-B3 reduced Aβ-induced activation of caspase 2 and 3, and promoted Aβ-induced activation of caspase 9. In contrast, UR-EA-B9 enhanced the Af3-induced activation of caspase 2, 3, 8, and 9. These results indicate that these fractions affect different targets in the apoptotic pathway. Moreover, UR-EAB9 possessed antioxidant capacity, whereas UR-EA-A567 and -B3 lacked this activity, implying that antioxidative activity may not play a role to protect neurons against Aβ-mediated toxicity for UR-EA-A567 and -B3. However, three fractions were able to eliminate reactive oxygen species (ROS) induced by Af3. Moreover, antioxidants such as epigallocatechin and probucol facilitated the caspase-dependent neuroprotective effects of UR-EA-A567. These results indicate that ROS elimination is essential for neurorpotection. Our results demonstrate that the neuroprotective mechanisms of Uncaria hirsuta Haviland on Af3-induced toxicity is mediated by abrogating the activation of the caspase cascade. The inhibition of the caspase cascade in combination with antioxidative activity will further eliminate Aβ-mediated neurotoxicity.
{"title":"The Neuroprotective Effects of Uncaria Hirsute Haviland on Amyloid β Protein-induced Toxicity in Rat Cortical Neurons","authors":"Chuen‐Neu Wang, I. Chen, Yun-Lian Lin, C. Chi, Chieh‐fu Chen, Y. Shiao","doi":"10.7019/CPJ.200310.0319","DOIUrl":"https://doi.org/10.7019/CPJ.200310.0319","url":null,"abstract":"Amyloid β protein (Aβ) elicits a toxic effect on neurons in vitro and in vivo and has been proposed to play an important role in the pathogenesis of Alzheimer’s disease (AD). Previous studies have shown that aggregated Aβ can induce caspase-dependent apoptosis by oxidative stress in cultured neurons. Uncaria rhynchophylla (miq.) Jacks., a traditional Chinese herbal medicine, has been used in combination with other herbs for the treatment of cognitive disorders. The major components responsible for the neuroprotective effect remains unclear In the present study, 23 fractions (UR-EAs) and 24 subfractions (UR-EA-As and UR-EA-Bs) were isolated from the ethyl acetate extracts of Uncaria hirsuta Haviland, a Taiwanese Uncaria. Five fractions, UR-EA-8, -16, -17, -18 and -19, and 5 subfractions, UR-EA-A567, -B3, -B8, -B9 and -BlO, and a pure compound, catechin, purified from UR-EA-19, were identified as neuroprotective components. The neuroprotective mechanism of UR-EA-A567, -B3 and -B9 were studied. All three fractions reduced Aβ-induced cytochome c release and nucleus condensation suggesting that Aβ-induced apoptosis was inhibited by the fractions. Nevertheless, three fractions had distinct effects on the activity of caspases. UR-EA-A567 abrogated Aβ-induced activation of caspase 2, 3, and 8. UR-EA-B3 reduced Aβ-induced activation of caspase 2 and 3, and promoted Aβ-induced activation of caspase 9. In contrast, UR-EA-B9 enhanced the Af3-induced activation of caspase 2, 3, 8, and 9. These results indicate that these fractions affect different targets in the apoptotic pathway. Moreover, UR-EAB9 possessed antioxidant capacity, whereas UR-EA-A567 and -B3 lacked this activity, implying that antioxidative activity may not play a role to protect neurons against Aβ-mediated toxicity for UR-EA-A567 and -B3. However, three fractions were able to eliminate reactive oxygen species (ROS) induced by Af3. Moreover, antioxidants such as epigallocatechin and probucol facilitated the caspase-dependent neuroprotective effects of UR-EA-A567. These results indicate that ROS elimination is essential for neurorpotection. Our results demonstrate that the neuroprotective mechanisms of Uncaria hirsuta Haviland on Af3-induced toxicity is mediated by abrogating the activation of the caspase cascade. The inhibition of the caspase cascade in combination with antioxidative activity will further eliminate Aβ-mediated neurotoxicity.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"1 1","pages":"319-334"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84871495","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hui-Hung Wang, Yuh-Lian Lin, J. Liao, Chieh‐fu Chen
Jujubae Fructus (JF), the dried fruit of Ziziphus jujuba Mill., is mainly used as a tonic and sedative in traditional Chinese medicine. This study examined the anti-amnesic effects of JF on scopolamine (1mg/kg,i.p.)-and β-amyIoid peptide (25-35) (3nmol/mouse, i.c.v.)-induced amnesia in the step-through passive avoidance tasks in mice. The results showed that the water extract of JF (0.15-0.5g/kg, i.p.) administered immediately after the training trial significantly attenuated both scopolamine- and β-amyloid peptide (25-35)-induced amnesia. Using scopolamine-induced amnesia as a bioassay for further isolation of the active principle(s), we found that the anti-amnesic active principle(s) existed in the ethyl acetate fraction when the water extract or 85% ethanol extract of JF was partitioned into ethyl acetate and water fractions. Therefore, the present study demonstrated for the first time that JF contains anti-amnesic principle(s), which can attenuate scopolamine- and β-amyloid peptide (25-35)-induced amnesia.
{"title":"The Anti-Amnesic Effects of the Water Extract of Jujubae Fructus","authors":"Hui-Hung Wang, Yuh-Lian Lin, J. Liao, Chieh‐fu Chen","doi":"10.7019/CPJ.200310.0361","DOIUrl":"https://doi.org/10.7019/CPJ.200310.0361","url":null,"abstract":"Jujubae Fructus (JF), the dried fruit of Ziziphus jujuba Mill., is mainly used as a tonic and sedative in traditional Chinese medicine. This study examined the anti-amnesic effects of JF on scopolamine (1mg/kg,i.p.)-and β-amyIoid peptide (25-35) (3nmol/mouse, i.c.v.)-induced amnesia in the step-through passive avoidance tasks in mice. The results showed that the water extract of JF (0.15-0.5g/kg, i.p.) administered immediately after the training trial significantly attenuated both scopolamine- and β-amyloid peptide (25-35)-induced amnesia. Using scopolamine-induced amnesia as a bioassay for further isolation of the active principle(s), we found that the anti-amnesic active principle(s) existed in the ethyl acetate fraction when the water extract or 85% ethanol extract of JF was partitioned into ethyl acetate and water fractions. Therefore, the present study demonstrated for the first time that JF contains anti-amnesic principle(s), which can attenuate scopolamine- and β-amyloid peptide (25-35)-induced amnesia.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"51 1","pages":"361-369"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82251713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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