Rheumatoid arthritis （RA） is the most common inflammatory arthritis and a major cause of disability. Presently, the clinical therapeutic medicines for inflammatory and arthritic diseases are unsatisfactory due to se...Rheumatoid arthritis （RA） is the most common inflammatory arthritis and a major cause of disability. Presently, the clinical therapeutic medicines for inflammatory and arthritic diseases are unsatisfactory due to severe adverse effects or ineffectiveness. The Guge Fengtong formula （GGFT）, containing the standardized extracts of Dioscoreae Nipponicae Rhizoma, Spatholobi Caulis, and Zingiberis Rhizoma, has long been used for RA treatment in China. However, the detailed anti-inflammatory and anti-arthritic activity of GGFT has not been reported so far. In the present work, we aimed to evaluate the anti-inflammatory and anti-arthritic effects of GGFT using three in vivo animal models and tried to uncover the underlying mechanism of action in RAW 264.7 macrophages. The obtained results indicated that GGFT significantly attenuated ear edema, decreased carrageenan-induced paw edema, reduced the ar- thritis score, and reversed the weight loss of the complete Freund＇s adjuvant （CFA）-injected rats. Additionally, decrease in synovial inflammatory infiltration and synovial lining hyperplasia in the joints and decline of inflammatory factors （TNF-α and IL-1β） in the serum were observed in the GGFT-treated rats. In lipopolysaccharide-activated RAW264.7 macrophages, GGFT reduced the produc- tion of NO, PGE2, and IL-6 and inhibited the expression of iNOS, COX-2, and NF-kB. Our results demonstrated that GGFT possessed considerable anti-inflammatory activity and had potential therapeutic effects on adjuvant induced arthritis in rats, providing experi- mental evidences for its application in the treatment of RA and other inflammatory diseases.展开更多
The present study was designed to characterize the chemical constituents of Guge Fengtong Tablet(GGFTT).Based on the chromatographic retention behavior,fragmentation pathways of chemical components and the published l...The present study was designed to characterize the chemical constituents of Guge Fengtong Tablet(GGFTT).Based on the chromatographic retention behavior,fragmentation pathways of chemical components and the published literatures,a diagnostic ion filtering strategy with electrospray ionization quadrupole time-of-flight tandem mass spectrometry(HPLC-ESI-Q-TOF/MS) was established to identify the multiple bioactive constituents of GGFTT.The rapid identification of forty-seven components,including 18 phenolic acids,8 saponins,14 gingerol-related compounds,and 7 diarylhepatonoids,was accomplished using this newly developed method.The coupling of HPLC-ESI-Q-TOF/MS with the diagnostic ion filtering strategy was useful and efficient for the in-depth structural elucidation of chemical compounds of GGFTT.展开更多
In the present study, we developed and validated a rapid analytical method using high performance liquid chromatography coupled with quadrupole time of flight mass spectrometry(HPLC-Q-TOF/MS) to investigate the metabo...In the present study, we developed and validated a rapid analytical method using high performance liquid chromatography coupled with quadrupole time of flight mass spectrometry(HPLC-Q-TOF/MS) to investigate the metabolic profile of Guge Fengtong tablet(GGFTT), a traditional Chinese medicine. The urine and bile samples were collected with 24 h after oral administration of GGFTT. A total of 34 compounds, including 11 parent compounds and 23 metabolites were unambiguously or tentatively identified. Our results indicated that glucuronidation, oxidation and methylation were the major metabolic pathways of the constituents in GGFTT. In addition, the results of this work also demonstrated the feasibility of HPLC-ESI-Q-TOF/MS for reliable characterization of the in vivo metabolites from herbal preparations.展开更多
Multi-components in herbal formulae exert holistic effects in synergistic or additive manners. However, appropriate strategies and supportive evidences are still lacking to uncover the synergistic or additive combinat...Multi-components in herbal formulae exert holistic effects in synergistic or additive manners. However, appropriate strategies and supportive evidences are still lacking to uncover the synergistic or additive combinations. The present investigation aimed at seeking a screening strategy to identify the targeted combinations in GuG e FengT ong Tablet(GGFTT), an herbal formula. Two compounds, belonging to different chemical classes, were combined with different concentration ratios and their anti-inflammation effects were investigated. The most significant anti-inflammatory combinations were evaluated by combination index(CI) method(additive effect, CI = 1; synergism, CI < 1; antagonism, CI > 1). The modulating effects of candidate combinations on pro-inflammatory cytokines and MAPKs signaling pathway were also detected. Two combinations, "biochanin A + 6-gingerol"(Bio-6 G) and "genistein + 6-gingerol"(Gen-6 G), showed synergistic effects(CI < 1), and Bio-6 G was selected for further study. Compared with single compound, Bio-6 G could synergistically inhibit the production of pro-inflammatory cytokines(TNF-α, IL-1β, and IL-6) and the activation of MAPKs signaling pathway in LPS-stimulated RAW264.7 cells. The combined results showed that Bio-6 G was a synergistic anti-inflammatory combination in GGFTT. Our results could provide a useful strategy to screen the synergistic combinations in herbal formulae.展开更多
EDITOR'S NOTE:Although Swedish explorer Sven Hedin ventured into Ngarifrom Xinjiang in 1902, the region remains mysterious and unknown to the outside world.This prompted the State Cultural Relics Bureau and the Cu...EDITOR'S NOTE:Although Swedish explorer Sven Hedin ventured into Ngarifrom Xinjiang in 1902, the region remains mysterious and unknown to the outside world.This prompted the State Cultural Relics Bureau and the Cultural Relics to senda team into Ngari along the Lhasa-Ngari-Yecheng(Xinjiang)route. The purpose was toexplore the Zhangzhung Civilization that existed prior to the Guge Kingdom.According to legend, Zada in the Xianquanhe River Valley is the central part ofthe Zhangzhung Kingdom, which was so formidable that the kingdom was divided intoInternal, Central and External Zhangzhung and Internal Zangzhung alone coveredpresent-day Ngari and Ladakh. This writer was one of the team members.展开更多
基金supported by the Project in the National Science&Technology Pillar Program during the Twelfth Five-year Plan Period(No.2012BAI29B07)National Natural Science Foundation of China(No.81202898)
文摘Rheumatoid arthritis （RA） is the most common inflammatory arthritis and a major cause of disability. Presently, the clinical therapeutic medicines for inflammatory and arthritic diseases are unsatisfactory due to severe adverse effects or ineffectiveness. The Guge Fengtong formula （GGFT）, containing the standardized extracts of Dioscoreae Nipponicae Rhizoma, Spatholobi Caulis, and Zingiberis Rhizoma, has long been used for RA treatment in China. However, the detailed anti-inflammatory and anti-arthritic activity of GGFT has not been reported so far. In the present work, we aimed to evaluate the anti-inflammatory and anti-arthritic effects of GGFT using three in vivo animal models and tried to uncover the underlying mechanism of action in RAW 264.7 macrophages. The obtained results indicated that GGFT significantly attenuated ear edema, decreased carrageenan-induced paw edema, reduced the ar- thritis score, and reversed the weight loss of the complete Freund＇s adjuvant （CFA）-injected rats. Additionally, decrease in synovial inflammatory infiltration and synovial lining hyperplasia in the joints and decline of inflammatory factors （TNF-α and IL-1β） in the serum were observed in the GGFT-treated rats. In lipopolysaccharide-activated RAW264.7 macrophages, GGFT reduced the produc- tion of NO, PGE2, and IL-6 and inhibited the expression of iNOS, COX-2, and NF-kB. Our results demonstrated that GGFT possessed considerable anti-inflammatory activity and had potential therapeutic effects on adjuvant induced arthritis in rats, providing experi- mental evidences for its application in the treatment of RA and other inflammatory diseases.
基金supported by a project of the National Science&Technology Pillar Program during the Twelfth Five-year Plan Period(No.2012BAI29B07)the National Natural Science Foundation of China(No.81202898)
文摘The present study was designed to characterize the chemical constituents of Guge Fengtong Tablet(GGFTT).Based on the chromatographic retention behavior,fragmentation pathways of chemical components and the published literatures,a diagnostic ion filtering strategy with electrospray ionization quadrupole time-of-flight tandem mass spectrometry(HPLC-ESI-Q-TOF/MS) was established to identify the multiple bioactive constituents of GGFTT.The rapid identification of forty-seven components,including 18 phenolic acids,8 saponins,14 gingerol-related compounds,and 7 diarylhepatonoids,was accomplished using this newly developed method.The coupling of HPLC-ESI-Q-TOF/MS with the diagnostic ion filtering strategy was useful and efficient for the in-depth structural elucidation of chemical compounds of GGFTT.
基金supported by National Science&Technology Pillar Program During the Twelfth Five-year Plan Period(2012BAI29B07)National Natural Science Foundation of China(81202898)
文摘In the present study, we developed and validated a rapid analytical method using high performance liquid chromatography coupled with quadrupole time of flight mass spectrometry(HPLC-Q-TOF/MS) to investigate the metabolic profile of Guge Fengtong tablet(GGFTT), a traditional Chinese medicine. The urine and bile samples were collected with 24 h after oral administration of GGFTT. A total of 34 compounds, including 11 parent compounds and 23 metabolites were unambiguously or tentatively identified. Our results indicated that glucuronidation, oxidation and methylation were the major metabolic pathways of the constituents in GGFTT. In addition, the results of this work also demonstrated the feasibility of HPLC-ESI-Q-TOF/MS for reliable characterization of the in vivo metabolites from herbal preparations.
基金supported by a project in the National Science&Technology Pillar Program during the Twelfth Five-year Plan Period(No.2012BAI29B07)the National Natural Science Foundation of China(Nos.81202898 and 81473343)a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘Multi-components in herbal formulae exert holistic effects in synergistic or additive manners. However, appropriate strategies and supportive evidences are still lacking to uncover the synergistic or additive combinations. The present investigation aimed at seeking a screening strategy to identify the targeted combinations in GuG e FengT ong Tablet(GGFTT), an herbal formula. Two compounds, belonging to different chemical classes, were combined with different concentration ratios and their anti-inflammation effects were investigated. The most significant anti-inflammatory combinations were evaluated by combination index(CI) method(additive effect, CI = 1; synergism, CI < 1; antagonism, CI > 1). The modulating effects of candidate combinations on pro-inflammatory cytokines and MAPKs signaling pathway were also detected. Two combinations, "biochanin A + 6-gingerol"(Bio-6 G) and "genistein + 6-gingerol"(Gen-6 G), showed synergistic effects(CI < 1), and Bio-6 G was selected for further study. Compared with single compound, Bio-6 G could synergistically inhibit the production of pro-inflammatory cytokines(TNF-α, IL-1β, and IL-6) and the activation of MAPKs signaling pathway in LPS-stimulated RAW264.7 cells. The combined results showed that Bio-6 G was a synergistic anti-inflammatory combination in GGFTT. Our results could provide a useful strategy to screen the synergistic combinations in herbal formulae.
文摘EDITOR'S NOTE:Although Swedish explorer Sven Hedin ventured into Ngarifrom Xinjiang in 1902, the region remains mysterious and unknown to the outside world.This prompted the State Cultural Relics Bureau and the Cultural Relics to senda team into Ngari along the Lhasa-Ngari-Yecheng(Xinjiang)route. The purpose was toexplore the Zhangzhung Civilization that existed prior to the Guge Kingdom.According to legend, Zada in the Xianquanhe River Valley is the central part ofthe Zhangzhung Kingdom, which was so formidable that the kingdom was divided intoInternal, Central and External Zhangzhung and Internal Zangzhung alone coveredpresent-day Ngari and Ladakh. This writer was one of the team members.
