Flavonoids such as baohuoside I and icaritin are the major active compounds in Epimedii Folium(EF)and possess excellent therapeutic effects on various diseases.Encouragingly,in 2022,icaritin soft capsules were approve...Flavonoids such as baohuoside I and icaritin are the major active compounds in Epimedii Folium(EF)and possess excellent therapeutic effects on various diseases.Encouragingly,in 2022,icaritin soft capsules were approved to reach the market for the treatment of hepatocellular carcinoma(HCC)by National Medical Products Administration(NMPA)of China.Moreover,recent studies demonstrate that icaritin can serve as immune-modulating agent to exert anti-tumor effects.Nonetheless,both production efficiency and clinical applications of epimedium flavonoids have been restrained because of their low content,poor bioavailability,and unfavorable in vivo delivery efficiency.Recently,various strategies,including enzyme engineering and nanotechnology,have been developed to increase productivity and activity,improve delivery efficiency,and enhance therapeutic effects of epimedium flavonoids.In this review,the structure-activity relationship of epimedium flavonoids is described.Then,enzymatic engineering strategies for increasing the productivity of highly active baohuoside I and icaritin are discussed.The nanomedicines for overcoming in vivo delivery barriers and improving therapeutic effects of various diseases are summarized.Finally,the challenges and an outlook on clinical translation of epimedium flavonoids are proposed.展开更多
[Objectives] To systematically study the main active components of Fufang Changtai(FFCT) in the treatment of colorectal cancer(CRC), and to explore its mechanism of action. [Methods] The main chemical components of FF...[Objectives] To systematically study the main active components of Fufang Changtai(FFCT) in the treatment of colorectal cancer(CRC), and to explore its mechanism of action. [Methods] The main chemical components of FFCT were analyzed by ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS) combined with automatic analysis platform, and the main pharmacodynamic substances of FFCT were studied by network pharmacology method and its mechanism of action was explored. The binding degree between the active components and the core targets were verified by molecular docking technology. [Results] A total of 86 compounds were identified from FFCT, among which 26 compounds were Ginsenoside Rg3, Ginsenoside Rb1, Astragaloside III, etc. The key target pathway enrichment analysis showed that FFCT played its role in the treatment of CRC mainly through the PI3K-Akt signaling pathway and MAPK signaling pathway. [Conclusions] This study comprehensively identified the FFCT components. Supplemented by network pharmacology and molecular docking technology, it is expected to provide a scientific theoretical basis and an important reference for FFCT therapeutic components identification, key target verification and mechanism of action in the treatment of CRC.展开更多
Moutan Cortex (MC) has been demonstrated to have an inhibitive effect on inflammation and oxidative stress responses in mesangial cells in our previous study. However, little is known about the components of MC contri...Moutan Cortex (MC) has been demonstrated to have an inhibitive effect on inflammation and oxidative stress responses in mesangial cells in our previous study. However, little is known about the components of MC contributing to this benefit. In the present study, cell membrane immobilized chromatography (CMC), a fast and useful method, was presented for screening potential active components of MC. HBZY-1 cells were incubated with MC (200 μg/mL) at the optimal incubation time (90 min). HPLC-DAD analysis and LC/ESI/MS/MS were performed to distinguish the active components and identify its structural ion fragments. The results showed that eight components binding to HBZY-1 cells were mudanoside B, paeoniflorin sulfonate, paeoniflorin, tetragalloyl glucose (isomeride), hexagalloyl glucose, mudanopiside A, and paeonol. In conclusion, our established CMC might be a useful method for screening potential active components in complicated traditional Chinese medicines. These components might be associated with the efficacy of MC on prevention and treatment of diabetic nephropathy.展开更多
This study focuses on the preparation and enzymic hydrolysis of an icariin/bcyclodextrin inclusion complex to efficiently generate icaritin.The physical characteristics of the inclusion complex were evaluated by diffe...This study focuses on the preparation and enzymic hydrolysis of an icariin/bcyclodextrin inclusion complex to efficiently generate icaritin.The physical characteristics of the inclusion complex were evaluated by differential scanning calorimetry(DSC).Enzymatic hydrolysis was optimized for the conversion of icariin/b-cyclodextrin complex to icaritin by Box–Behnken statistical design.The inclusion complex formulation increased the solubility of icariin approximately 17-fold,from 29.2 to 513.5 mg/mL at 60℃.The optimum conditions were predicted by Box–Behnken statistical design as follows:60℃,pH 7.0,the ratio of enzyme/substrate(1:1.1)and reaction time 7 h.Under the optimal conditions the conversion of icariin was 97.91%and the reaction time was decreased by 68%compared with that without b-CD inclusion.Product analysis by melting point,ESI-MS,UV,IR,1H NMR and 13C NMR confirmed the authenticity of icaritin with a purity of 99.3%and a yield of 473 mg of icaritin from 1.1 g icariin.展开更多
基金supported by the National Natural Science Foundation of China(Grant No.:81873196)Sino-German Center for Research Promotion(Project No.:GZ1505)Chinese Scholarship Council,and Science and Technology Planning Projects of Jiaxing City(Project No.:2022AY10014).
文摘Flavonoids such as baohuoside I and icaritin are the major active compounds in Epimedii Folium(EF)and possess excellent therapeutic effects on various diseases.Encouragingly,in 2022,icaritin soft capsules were approved to reach the market for the treatment of hepatocellular carcinoma(HCC)by National Medical Products Administration(NMPA)of China.Moreover,recent studies demonstrate that icaritin can serve as immune-modulating agent to exert anti-tumor effects.Nonetheless,both production efficiency and clinical applications of epimedium flavonoids have been restrained because of their low content,poor bioavailability,and unfavorable in vivo delivery efficiency.Recently,various strategies,including enzyme engineering and nanotechnology,have been developed to increase productivity and activity,improve delivery efficiency,and enhance therapeutic effects of epimedium flavonoids.In this review,the structure-activity relationship of epimedium flavonoids is described.Then,enzymatic engineering strategies for increasing the productivity of highly active baohuoside I and icaritin are discussed.The nanomedicines for overcoming in vivo delivery barriers and improving therapeutic effects of various diseases are summarized.Finally,the challenges and an outlook on clinical translation of epimedium flavonoids are proposed.
基金Supported by Key Project of National Clinical Research Base of Traditional Chinese Medicine (JD2022SZXZD01)Open Project of Jiangsu Health Development Research Center (JSHD2021014&JSHD2021040)+1 种基金National Natural Science Foundation of China (81573620)Jiangsu Province Six Talent Summit Innovation Team Funding Project (SWYY-CXTD-004)。
文摘[Objectives] To systematically study the main active components of Fufang Changtai(FFCT) in the treatment of colorectal cancer(CRC), and to explore its mechanism of action. [Methods] The main chemical components of FFCT were analyzed by ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS) combined with automatic analysis platform, and the main pharmacodynamic substances of FFCT were studied by network pharmacology method and its mechanism of action was explored. The binding degree between the active components and the core targets were verified by molecular docking technology. [Results] A total of 86 compounds were identified from FFCT, among which 26 compounds were Ginsenoside Rg3, Ginsenoside Rb1, Astragaloside III, etc. The key target pathway enrichment analysis showed that FFCT played its role in the treatment of CRC mainly through the PI3K-Akt signaling pathway and MAPK signaling pathway. [Conclusions] This study comprehensively identified the FFCT components. Supplemented by network pharmacology and molecular docking technology, it is expected to provide a scientific theoretical basis and an important reference for FFCT therapeutic components identification, key target verification and mechanism of action in the treatment of CRC.
文摘Moutan Cortex (MC) has been demonstrated to have an inhibitive effect on inflammation and oxidative stress responses in mesangial cells in our previous study. However, little is known about the components of MC contributing to this benefit. In the present study, cell membrane immobilized chromatography (CMC), a fast and useful method, was presented for screening potential active components of MC. HBZY-1 cells were incubated with MC (200 μg/mL) at the optimal incubation time (90 min). HPLC-DAD analysis and LC/ESI/MS/MS were performed to distinguish the active components and identify its structural ion fragments. The results showed that eight components binding to HBZY-1 cells were mudanoside B, paeoniflorin sulfonate, paeoniflorin, tetragalloyl glucose (isomeride), hexagalloyl glucose, mudanopiside A, and paeonol. In conclusion, our established CMC might be a useful method for screening potential active components in complicated traditional Chinese medicines. These components might be associated with the efficacy of MC on prevention and treatment of diabetic nephropathy.
基金supported by the National Natural Science Foundation of China(No.30973944/H2805)the foundation for high-level talent on six areas of Jiangsu province.
文摘This study focuses on the preparation and enzymic hydrolysis of an icariin/bcyclodextrin inclusion complex to efficiently generate icaritin.The physical characteristics of the inclusion complex were evaluated by differential scanning calorimetry(DSC).Enzymatic hydrolysis was optimized for the conversion of icariin/b-cyclodextrin complex to icaritin by Box–Behnken statistical design.The inclusion complex formulation increased the solubility of icariin approximately 17-fold,from 29.2 to 513.5 mg/mL at 60℃.The optimum conditions were predicted by Box–Behnken statistical design as follows:60℃,pH 7.0,the ratio of enzyme/substrate(1:1.1)and reaction time 7 h.Under the optimal conditions the conversion of icariin was 97.91%and the reaction time was decreased by 68%compared with that without b-CD inclusion.Product analysis by melting point,ESI-MS,UV,IR,1H NMR and 13C NMR confirmed the authenticity of icaritin with a purity of 99.3%and a yield of 473 mg of icaritin from 1.1 g icariin.
