During the pathogensis of rheumatoid arthritis(RA),activated RA fibroblast-like synoviocytes(RA-FLSs)combines similar proliferative features as tumor and inflammatory features as osteoarthritis,which eventually leads ...During the pathogensis of rheumatoid arthritis(RA),activated RA fibroblast-like synoviocytes(RA-FLSs)combines similar proliferative features as tumor and inflammatory features as osteoarthritis,which eventually leads to joint erosion.Therefore,it is imperative to research and develop new compounds,which can effectively inhibit abnormal activation of RA-FLSs and retard RA progression.Neohesperidin(Neo)is a major active component of flavonoid compounds with anti-inflammation and anti-oxidant properties.In this study,the anti-inflammation,anti-migration,anti-invasion,anti-oxidant and apoptosis-induced effects of Neo on RAFLSs were explored to investigate the underlying mechanism.The results suggested that Neo decreased the levels of interleukin IL-1β,IL-6,IL-8,TNF-α,MMP-3,MMP-9 and MMP-13 in FLSs.Moreover,Neo blocked the activation of the MAPK signaling pathway.Furthermore,treatment with Neo induced the apoptosis of FLSs,and inhibited the migration of FLSs.It was also found that Neo reduced the accumulation of reactive oxygen species(ROS)induced by TNF-α.Taken together,our results highlighted that Neo may act as a potential and promising therapeutic drug for the management of RA.展开更多
Objective: To compare the pharmacokinetics of naringin and neohesperidin after oral administration of Zhishi total flavonoid glycosides(ZSTFG) extracted from Aurantii Fructus Immaturus in normal and gastrointestinal m...Objective: To compare the pharmacokinetics of naringin and neohesperidin after oral administration of Zhishi total flavonoid glycosides(ZSTFG) extracted from Aurantii Fructus Immaturus in normal and gastrointestinal motility disorders(GMD) mice.Methods: ZSTFG was orally given to normal and GMD mice induced by atropine or dopamine. The plasma samples were incubated with β-glucuronidase/sulfatase, the total(free + conjugated) naringenin and hesperitin were extracted with acetonitrile. The validated HPLC-MS/MS method was successfully applied to the pharmacokinetic study.Results: The results showed that, compared with the normal group, AUC0–∞, AUC0–tand Cmaxfor total naringenin and hesperitin were significantly higher(P < 0.01 or P < 0.05), while CLZ/F for total naringenin and hesperitin was significantly lower(P < 0.01) in the GMD group. Tmax, t1/2 z, MRT0-t, and MRT0-∞for naringenin were longer(P < 0.01) in the GMD group than those in the normal group.Conclusion: The results showed that there were significant differences in pharmacokinetic parameters of naringenin and hesperitin between normal and GMD groups. It was suggested that the absorption of naringenin and hesperitin was increased, and the elimination processes of naringenin and hesperitin were slower in the GMD group than the normal group. The data are of value for further pharmacological studies of ZSTFG and would be useful to provide a reference for improving the therapeutic regimen of ZSTFG in clinical trials.展开更多
Bitter is generally undesirable,although it is an important part of flavor.Bitter substances exhibit diverse health-promoting activities,which is in line with the famous Chinese saying‘a good medicine tastes bitter’...Bitter is generally undesirable,although it is an important part of flavor.Bitter substances exhibit diverse health-promoting activities,which is in line with the famous Chinese saying‘a good medicine tastes bitter’.Naringin(NAG)and neohesperidin(NHP),two important flavanones that give bitterness to citrus fruits,show various pharmacological activities.Interestingly,their hydrogenation products,i.e.naringin dihydrochalcone(NDC)and neohesperidin dihydrochalcone(NHDC),undergo a dramatic taste shift from bitter to intensely sweet,which can be 300 and 1000 times sweeter than sucrose,respectively.Such sweeteners not only provide a sweet taste without the burden of increased calorie intake and glycemia,but also may exert multiple bioactivities.This review summarizes common dietary bitter and sweet compounds with sensory scores.Taste conversions induced by structural changes from bitter NAG and NHP to sweet NDC and NHDC are particularly discussed.In addition,the taste-sensing mechanisms,pharmacological characteristics,dietary distribution,synthesis,and food industry applications of these bitter–sweet interchangeable compounds are outlined.In conclusion,the bitter NAG and NHP are promising therapeutic candidates for management of diverse etiologically complex diseases while their corresponding dihydrochalcones NDC and NHDC are promising sweeteners,which might be a blessing for those who need to control sugar intake.展开更多
[目的]综述胡柚皮化学成分、药理作用的研究进展,推进胡柚皮中药开发和临床应用。[方法]检索1994至2024年中国知网、万方、PubMed、Web of Science和Google Scholar等数据库中胡柚皮化学成分、药理活性及临床应用相关的研究报道,归纳总...[目的]综述胡柚皮化学成分、药理作用的研究进展,推进胡柚皮中药开发和临床应用。[方法]检索1994至2024年中国知网、万方、PubMed、Web of Science和Google Scholar等数据库中胡柚皮化学成分、药理活性及临床应用相关的研究报道,归纳总结胡柚皮的研究现状。[结果]现代研究表明,胡柚皮中含有多种生理活性成分,包括黄酮类化合物、柠檬苦素类化合物、香豆素类化合物、挥发油类化合物、酚酸类化合物、果胶、膳食纤维、类胡萝卜素等,具有抗氧化、抗菌、降血脂、降血糖、调节免疫、调节胃肠运动、保肝护肝、止咳祛痰等药理作用。目前胡柚皮的临床研究较少,偶有应用胡柚皮治疗呼吸系统疾病与运动系统疾病的文献报道。[结论]胡柚皮具有丰富的功能性化学成分、广泛的药理作用和一定的药用价值,随着研究的不断深入,胡柚皮在传统医药、临床应用及保健食品等方面的开发和利用将有着广阔的前景。展开更多
基金supported by the National Natural Science Foundation of China(No.81672161).
文摘During the pathogensis of rheumatoid arthritis(RA),activated RA fibroblast-like synoviocytes(RA-FLSs)combines similar proliferative features as tumor and inflammatory features as osteoarthritis,which eventually leads to joint erosion.Therefore,it is imperative to research and develop new compounds,which can effectively inhibit abnormal activation of RA-FLSs and retard RA progression.Neohesperidin(Neo)is a major active component of flavonoid compounds with anti-inflammation and anti-oxidant properties.In this study,the anti-inflammation,anti-migration,anti-invasion,anti-oxidant and apoptosis-induced effects of Neo on RAFLSs were explored to investigate the underlying mechanism.The results suggested that Neo decreased the levels of interleukin IL-1β,IL-6,IL-8,TNF-α,MMP-3,MMP-9 and MMP-13 in FLSs.Moreover,Neo blocked the activation of the MAPK signaling pathway.Furthermore,treatment with Neo induced the apoptosis of FLSs,and inhibited the migration of FLSs.It was also found that Neo reduced the accumulation of reactive oxygen species(ROS)induced by TNF-α.Taken together,our results highlighted that Neo may act as a potential and promising therapeutic drug for the management of RA.
基金Jiangxi Qingfeng Pharmaceutical Co., Ltd. for financial support
文摘Objective: To compare the pharmacokinetics of naringin and neohesperidin after oral administration of Zhishi total flavonoid glycosides(ZSTFG) extracted from Aurantii Fructus Immaturus in normal and gastrointestinal motility disorders(GMD) mice.Methods: ZSTFG was orally given to normal and GMD mice induced by atropine or dopamine. The plasma samples were incubated with β-glucuronidase/sulfatase, the total(free + conjugated) naringenin and hesperitin were extracted with acetonitrile. The validated HPLC-MS/MS method was successfully applied to the pharmacokinetic study.Results: The results showed that, compared with the normal group, AUC0–∞, AUC0–tand Cmaxfor total naringenin and hesperitin were significantly higher(P < 0.01 or P < 0.05), while CLZ/F for total naringenin and hesperitin was significantly lower(P < 0.01) in the GMD group. Tmax, t1/2 z, MRT0-t, and MRT0-∞for naringenin were longer(P < 0.01) in the GMD group than those in the normal group.Conclusion: The results showed that there were significant differences in pharmacokinetic parameters of naringenin and hesperitin between normal and GMD groups. It was suggested that the absorption of naringenin and hesperitin was increased, and the elimination processes of naringenin and hesperitin were slower in the GMD group than the normal group. The data are of value for further pharmacological studies of ZSTFG and would be useful to provide a reference for improving the therapeutic regimen of ZSTFG in clinical trials.
基金supported by the SanNongJiuFang Project of Zhejiang Province(No.2022SNJF083)the National Agricultural Science and Technology Modernization Project between Zhejiang University and Changshan County(No.588970-Y12202)+1 种基金the Key Research and Development Program of Zhejiang Province(No.2021C02001)the Serving Local Economic Development Project of Shandong(Linyi)Institute of Modern Agriculture,Zhejiang University,China.
文摘Bitter is generally undesirable,although it is an important part of flavor.Bitter substances exhibit diverse health-promoting activities,which is in line with the famous Chinese saying‘a good medicine tastes bitter’.Naringin(NAG)and neohesperidin(NHP),two important flavanones that give bitterness to citrus fruits,show various pharmacological activities.Interestingly,their hydrogenation products,i.e.naringin dihydrochalcone(NDC)and neohesperidin dihydrochalcone(NHDC),undergo a dramatic taste shift from bitter to intensely sweet,which can be 300 and 1000 times sweeter than sucrose,respectively.Such sweeteners not only provide a sweet taste without the burden of increased calorie intake and glycemia,but also may exert multiple bioactivities.This review summarizes common dietary bitter and sweet compounds with sensory scores.Taste conversions induced by structural changes from bitter NAG and NHP to sweet NDC and NHDC are particularly discussed.In addition,the taste-sensing mechanisms,pharmacological characteristics,dietary distribution,synthesis,and food industry applications of these bitter–sweet interchangeable compounds are outlined.In conclusion,the bitter NAG and NHP are promising therapeutic candidates for management of diverse etiologically complex diseases while their corresponding dihydrochalcones NDC and NHDC are promising sweeteners,which might be a blessing for those who need to control sugar intake.
文摘[目的]综述胡柚皮化学成分、药理作用的研究进展,推进胡柚皮中药开发和临床应用。[方法]检索1994至2024年中国知网、万方、PubMed、Web of Science和Google Scholar等数据库中胡柚皮化学成分、药理活性及临床应用相关的研究报道,归纳总结胡柚皮的研究现状。[结果]现代研究表明,胡柚皮中含有多种生理活性成分,包括黄酮类化合物、柠檬苦素类化合物、香豆素类化合物、挥发油类化合物、酚酸类化合物、果胶、膳食纤维、类胡萝卜素等,具有抗氧化、抗菌、降血脂、降血糖、调节免疫、调节胃肠运动、保肝护肝、止咳祛痰等药理作用。目前胡柚皮的临床研究较少,偶有应用胡柚皮治疗呼吸系统疾病与运动系统疾病的文献报道。[结论]胡柚皮具有丰富的功能性化学成分、广泛的药理作用和一定的药用价值,随着研究的不断深入,胡柚皮在传统医药、临床应用及保健食品等方面的开发和利用将有着广阔的前景。
