The objective was to investigate the effect of kinsenoside(Kin) treatments on macrophage polarity and evaluate the resulting protection of chondrocytes to attenuate osteoarthritis(OA) progression.RAW264.7 macrophages ...The objective was to investigate the effect of kinsenoside(Kin) treatments on macrophage polarity and evaluate the resulting protection of chondrocytes to attenuate osteoarthritis(OA) progression.RAW264.7 macrophages were polarized to M1/M2 subtypes then administered with different concentrations of Kin. The polarization transitions were evaluated with quantitative real-time polymerase chain reaction(q RT-PCR), confocal observation and flow cytometry analysis. The mechanism of Kin repolarizing M1 macrophages was evaluated by Western blot. Further, macrophage conditioned medium(CM) and IL-1β were administered to chondrocytes. Micro-CT scanning and histological observations were conducted in vivo on anterior cruciate ligament transection(ACLT) mice with or without Kin treatment. We found that Kin repolarized M1 macrophages to the M2 phenotype. Mechanistically, Kin inhibited the phosphorylation of IκBα, which further reduced the downstream phosphorylation of P65 in nuclear factor-κB(NF-κB) signaling. Moreover, Kin inhibited mitogen-activated protein kinases(MAPK) signaling molecules p-JNK, p-ERK and p-P38. Additionally, Kin attenuated macrophage CM and IL-1β-induced chondrocyte damage. In vivo, Kin reduced the infiltration of M1 macrophages,promoted M2 macrophages in the synovium, inhibited subchondral bone destruction and reduced articular cartilage damage induced by ACLT. All the results indicated that Kin is an effective therapeutic candidate for OA treatment.展开更多
Kinsenoside is a main active component isolated from plants of the genus Anoectochilus,and exhibits many biological activities and pharmacological effects,including hepatoprotective,anti-hyperglycemic,anti-hyperliposi...Kinsenoside is a main active component isolated from plants of the genus Anoectochilus,and exhibits many biological activities and pharmacological effects,including hepatoprotective,anti-hyperglycemic,anti-hyperliposis,anti-inflammatory,vascular protective and anti-osteoporosis effects and so on,which is contributing to its promising potency in disease treatments.This review aims to recapitulate the pharmacological functions of kinsenoside,as well as its source,extraction,identification,quantitative analysis,pharmacokinetics,synthesis and patent information.The data reported in this work can confirm the therapeutic potential of kinsenoside and provide useful information for further new drug development.展开更多
目的:探讨不同干燥温度下金线莲8个黄酮类成分(芦丁、异槲皮苷、山柰酚-3-O-芸香糖苷、水仙苷、槲皮苷、槲皮素、山柰酚和异鼠李素)、6个核苷类成分(胞苷、尿苷、腺嘌呤、鸟苷、β-胸苷和腺苷)、金线莲苷和总黄酮活性成分的含量变化。方...目的:探讨不同干燥温度下金线莲8个黄酮类成分(芦丁、异槲皮苷、山柰酚-3-O-芸香糖苷、水仙苷、槲皮苷、槲皮素、山柰酚和异鼠李素)、6个核苷类成分(胞苷、尿苷、腺嘌呤、鸟苷、β-胸苷和腺苷)、金线莲苷和总黄酮活性成分的含量变化。方法:应用超高效液相色谱方法(UP L C)测定不同干燥温度处理下(45、50、65、80、100、120℃)金线莲黄酮类成分、核苷类成分及金线莲苷含量;应用紫外可见分光光度法(UV-VIS)测定不同干燥温度处理下金线莲中总黄酮含量。结果:不同干燥温度影响金线莲中主要活性成分含量。低温干燥下(45~50℃)金线莲黄酮类成分、总黄酮最高,含量随着温度升高呈现递减的趋势;金线莲总核苷和金线莲苷含量随着温度升高整体上呈现先增加(65℃处理含量达到最高)后减少趋势。结论:45~65℃干燥可有效保留金线莲主要药用活性成分,为金线莲生产加工中温度的选择提供实验依据。展开更多
基金supported by the National Natural Science Foundation of China(No.81672205)National Key R&D Programme(No.2016YFC1102100,China)the Shanghai Science and Technology Development Fund(Nos.18DZ2291200and 18441902700,China)
文摘The objective was to investigate the effect of kinsenoside(Kin) treatments on macrophage polarity and evaluate the resulting protection of chondrocytes to attenuate osteoarthritis(OA) progression.RAW264.7 macrophages were polarized to M1/M2 subtypes then administered with different concentrations of Kin. The polarization transitions were evaluated with quantitative real-time polymerase chain reaction(q RT-PCR), confocal observation and flow cytometry analysis. The mechanism of Kin repolarizing M1 macrophages was evaluated by Western blot. Further, macrophage conditioned medium(CM) and IL-1β were administered to chondrocytes. Micro-CT scanning and histological observations were conducted in vivo on anterior cruciate ligament transection(ACLT) mice with or without Kin treatment. We found that Kin repolarized M1 macrophages to the M2 phenotype. Mechanistically, Kin inhibited the phosphorylation of IκBα, which further reduced the downstream phosphorylation of P65 in nuclear factor-κB(NF-κB) signaling. Moreover, Kin inhibited mitogen-activated protein kinases(MAPK) signaling molecules p-JNK, p-ERK and p-P38. Additionally, Kin attenuated macrophage CM and IL-1β-induced chondrocyte damage. In vivo, Kin reduced the infiltration of M1 macrophages,promoted M2 macrophages in the synovium, inhibited subchondral bone destruction and reduced articular cartilage damage induced by ACLT. All the results indicated that Kin is an effective therapeutic candidate for OA treatment.
文摘Kinsenoside is a main active component isolated from plants of the genus Anoectochilus,and exhibits many biological activities and pharmacological effects,including hepatoprotective,anti-hyperglycemic,anti-hyperliposis,anti-inflammatory,vascular protective and anti-osteoporosis effects and so on,which is contributing to its promising potency in disease treatments.This review aims to recapitulate the pharmacological functions of kinsenoside,as well as its source,extraction,identification,quantitative analysis,pharmacokinetics,synthesis and patent information.The data reported in this work can confirm the therapeutic potential of kinsenoside and provide useful information for further new drug development.
文摘目的:探讨不同干燥温度下金线莲8个黄酮类成分(芦丁、异槲皮苷、山柰酚-3-O-芸香糖苷、水仙苷、槲皮苷、槲皮素、山柰酚和异鼠李素)、6个核苷类成分(胞苷、尿苷、腺嘌呤、鸟苷、β-胸苷和腺苷)、金线莲苷和总黄酮活性成分的含量变化。方法:应用超高效液相色谱方法(UP L C)测定不同干燥温度处理下(45、50、65、80、100、120℃)金线莲黄酮类成分、核苷类成分及金线莲苷含量;应用紫外可见分光光度法(UV-VIS)测定不同干燥温度处理下金线莲中总黄酮含量。结果:不同干燥温度影响金线莲中主要活性成分含量。低温干燥下(45~50℃)金线莲黄酮类成分、总黄酮最高,含量随着温度升高呈现递减的趋势;金线莲总核苷和金线莲苷含量随着温度升高整体上呈现先增加(65℃处理含量达到最高)后减少趋势。结论:45~65℃干燥可有效保留金线莲主要药用活性成分,为金线莲生产加工中温度的选择提供实验依据。
