3-Epi-betulinic acid 3-O-β-D-glucopyranoside(eBAG)is a pentacyclic triterpene mainly distributed in food and medicinal plants,which exhibits various pharmacological properties.However,whether these functions are attr...3-Epi-betulinic acid 3-O-β-D-glucopyranoside(eBAG)is a pentacyclic triterpene mainly distributed in food and medicinal plants,which exhibits various pharmacological properties.However,whether these functions are attributed to eBAG or additional components in these plants remain unknown.Herein,we report that eBAG exerted an inhibitory activity against hepatocellular carcinoma and esophageal cancer cells.EBAG induced non-apoptotic cell death in hepatocellular carcinoma cells.The eBAG-induced cell death was inhibited by knock-down of autophagy related gene(ATG)5 and ATG7,by administration of 3-methyladenine,a selective autophagy inhibitor that suppresses phosphoinositide 3-kinase(PI3K),and by chloroquine,a classic autophagy flux inhibitor.We demonstrated that eBAG induced an autophagy-mediated cell death.Application of eBAG mimicked cellular bioenergetics depletion leading to the reduction of intracellular ATP,activation of AMP-activated protein kinase(AMPK),and inhibition of mTOR.Co-treatment with compound C,an AMPK inhibitor,abrogated cell death induced by eBAG.We further validated the anti-tumor effect of eBAG in the murine xenograft model of hepatocellular carcinoma and found that eBAG treatment promoted the induction of autophagy and reduction of tumor growth in mice.As a functional food ingredient,eBAG is a potential therapeutic agent for the treatment of hepatocellular carcinoma and esophageal cancer.展开更多
Flower plants are popular all over the world and important sources of ornamental plants,bioactive molecules and nutrients.Flowers have a wide range of biological activities and beneficial pharmacological effects.Flowe...Flower plants are popular all over the world and important sources of ornamental plants,bioactive molecules and nutrients.Flowers have a wide range of biological activities and beneficial pharmacological effects.Flowers and their active ingredients are becoming more and more popular in the preparation of food,drugs and industrial products.This paper summarizes the active ingredients,pharmacological activities and applications in the pharmaceutical and food industries of flower plants in recent years.In addition,the possible molecular mechanism of pharmacological effects of flower plants were also discussed.302 active constituents from 55 species of flower plants were summarized,including flavonoids(115),terpenoids(90),phenylpropanoids(20),alkaloids(13),organic acids(27)and others(37).The pharmacological effects of flower plants are very extensive,mainly including antioxidant,anti-inflammatory,anti-tumor,anti-virus,and hypoglycemic.The mechanisms of anti-inflammatory,anti-tumor and hypoglycemic activities present the characteristics of multi-way and multi-target.Because of its rich nutrients,bioactive ingredients and plant essential oils,and its wide sources,flower plants are widely used in food,beverage,cosmetics and drug research.Flower plants also play an important role in pharmaceutical industry,food industry and other fields.展开更多
Antrodia cinnamomea is extensively used as a traditional medicine to prevention and treatment of liver cancer.However,its comprehensive chemical fingerprint is uncertain,and the mechanisms,especially the potential the...Antrodia cinnamomea is extensively used as a traditional medicine to prevention and treatment of liver cancer.However,its comprehensive chemical fingerprint is uncertain,and the mechanisms,especially the potential therapeutic target for anti-hepatocellular carcinoma(HCC)are still unclear.Using UPLC-Q-TOF/MS,139 chemical components were identified in A.cinnamomea dropping pills(ACDPs).Based on these chemical components,network pharmacology demonstrated that the targets of active components were significantly enriched in the pathways in cancer,which were closely related with cell proliferation regulation.Next,HCC data was downloaded from Gene Expression Omnibus database(GEO).The Cancer Genome Atlas(TCGA)and Dis Ge NET were analyzed by bioinformatics,and 79 biomarkers were obtained.Furtherly,nine targets of ACDP active components were revealed,and they were significantly enriched in PI3 K/AKT and cell cycle signaling pathways.The affinity between these targets and their corresponding active ingredients was predicted by molecular docking.Finally,in vivo and in vitro experiments showed that ACDPs could reduce the activity of PI3 K/AKT signaling pathway and downregulate the expression of cell cycle-related proteins,contributing to the decreased growth of liver cancer.Altogether,PI3 K/AKT-cell cycle appears as the significant central node in anti-liver cancer of A.Cinnamomea.展开更多
Implant-associated infection remains a difficult medical problem in orthopedic surgery. Therefore, the development of multifunctional bone implants for treating infection and regenerating lost bone tissue,which may be...Implant-associated infection remains a difficult medical problem in orthopedic surgery. Therefore, the development of multifunctional bone implants for treating infection and regenerating lost bone tissue,which may be a result of infection, is important. In the present study, we report the fabrication of enoxacinloaded poly(lactic-co-glycolic acid)(PLGA) coating on porous magnesium scaffold(Enox-PLGA-Mg) which combine the favorable properties of magnesium, the antibacterial property and the effect of inhibition of osteoclastic bone resorption of enoxacin. The drug loaded PLGA coating of Mg scaffold enables higher drug loading efficiency(52%–56%) than non-coating enoxacin loaded Mg scaffold(Enox-Mg)(4%–5%). EnoxPLGA-Mg exhibits sustained drug release for more than 14 days, and this controlled release of enoxacin significantly inhibits bacterial adhesion and prevented biofilm formation by Staphylococcus epidermidis(ATCC35984) and Staphylococcus aureus(ATCC25923). Biocompatibility tests with Balb/c mouse embryo fibroblasts(Balb/c 3T3 cells) indicate that PLGA-Mg has better biocompatibility than Mg. Finally, we also demonstrate that Enox-PLGA-Mg extract potently inhibited osteoclast formation in vitro. Therefore, EnoxPLGA-Mg has the potential to be used as a multifunctional controlled drug delivery system bone scaffolds to prevent and/or treat orthopedic peri-implant infections.展开更多
基金supported by Henan Provincial Science and Technology Research Project (212102310355)the National Natural Science Foundation of China (82020108024 and 32161143021)。
文摘3-Epi-betulinic acid 3-O-β-D-glucopyranoside(eBAG)is a pentacyclic triterpene mainly distributed in food and medicinal plants,which exhibits various pharmacological properties.However,whether these functions are attributed to eBAG or additional components in these plants remain unknown.Herein,we report that eBAG exerted an inhibitory activity against hepatocellular carcinoma and esophageal cancer cells.EBAG induced non-apoptotic cell death in hepatocellular carcinoma cells.The eBAG-induced cell death was inhibited by knock-down of autophagy related gene(ATG)5 and ATG7,by administration of 3-methyladenine,a selective autophagy inhibitor that suppresses phosphoinositide 3-kinase(PI3K),and by chloroquine,a classic autophagy flux inhibitor.We demonstrated that eBAG induced an autophagy-mediated cell death.Application of eBAG mimicked cellular bioenergetics depletion leading to the reduction of intracellular ATP,activation of AMP-activated protein kinase(AMPK),and inhibition of mTOR.Co-treatment with compound C,an AMPK inhibitor,abrogated cell death induced by eBAG.We further validated the anti-tumor effect of eBAG in the murine xenograft model of hepatocellular carcinoma and found that eBAG treatment promoted the induction of autophagy and reduction of tumor growth in mice.As a functional food ingredient,eBAG is a potential therapeutic agent for the treatment of hepatocellular carcinoma and esophageal cancer.
基金funded by National Key R&D Program of China(2022)Research on Precision Nutrition and Health Food,Department of Science and Technology of Henan Province(CXJD2021006)Key Project in Science and Technology Agency of Henan Province(212102310355).
文摘Flower plants are popular all over the world and important sources of ornamental plants,bioactive molecules and nutrients.Flowers have a wide range of biological activities and beneficial pharmacological effects.Flowers and their active ingredients are becoming more and more popular in the preparation of food,drugs and industrial products.This paper summarizes the active ingredients,pharmacological activities and applications in the pharmaceutical and food industries of flower plants in recent years.In addition,the possible molecular mechanism of pharmacological effects of flower plants were also discussed.302 active constituents from 55 species of flower plants were summarized,including flavonoids(115),terpenoids(90),phenylpropanoids(20),alkaloids(13),organic acids(27)and others(37).The pharmacological effects of flower plants are very extensive,mainly including antioxidant,anti-inflammatory,anti-tumor,anti-virus,and hypoglycemic.The mechanisms of anti-inflammatory,anti-tumor and hypoglycemic activities present the characteristics of multi-way and multi-target.Because of its rich nutrients,bioactive ingredients and plant essential oils,and its wide sources,flower plants are widely used in food,beverage,cosmetics and drug research.Flower plants also play an important role in pharmaceutical industry,food industry and other fields.
基金supported by the National Key Research Project of China(2019YFC1606400)CAMS Innovation Fund for Medical Sciences(2019-I2M-5-055,China)+4 种基金Major Public Welfare Projects in Henan Province(201300110200,China)National Key Research Project of Hebei Province(20375502D,China)Natural Science Foundation of Hebei Province(H2019206212,China)High-level Talent Funding Project of Hebei Province(A201905006,China)Fund of National R&D Center for Edible Fungus Processing Technology,Henan University(20200109,China)。
文摘Antrodia cinnamomea is extensively used as a traditional medicine to prevention and treatment of liver cancer.However,its comprehensive chemical fingerprint is uncertain,and the mechanisms,especially the potential therapeutic target for anti-hepatocellular carcinoma(HCC)are still unclear.Using UPLC-Q-TOF/MS,139 chemical components were identified in A.cinnamomea dropping pills(ACDPs).Based on these chemical components,network pharmacology demonstrated that the targets of active components were significantly enriched in the pathways in cancer,which were closely related with cell proliferation regulation.Next,HCC data was downloaded from Gene Expression Omnibus database(GEO).The Cancer Genome Atlas(TCGA)and Dis Ge NET were analyzed by bioinformatics,and 79 biomarkers were obtained.Furtherly,nine targets of ACDP active components were revealed,and they were significantly enriched in PI3 K/AKT and cell cycle signaling pathways.The affinity between these targets and their corresponding active ingredients was predicted by molecular docking.Finally,in vivo and in vitro experiments showed that ACDPs could reduce the activity of PI3 K/AKT signaling pathway and downregulate the expression of cell cycle-related proteins,contributing to the decreased growth of liver cancer.Altogether,PI3 K/AKT-cell cycle appears as the significant central node in anti-liver cancer of A.Cinnamomea.
基金supported by the Key National Basic Research Program of China (Grant No. 2012CB619101)the National Natural Science Foundation of China (No. 81190133)+3 种基金the National Natural Science Foundation for the Youth of China (Grant Nos. 81401852 and 31500777)the Doctoral Innovation Fund Projects from Shanghai Jiao Tong University School of Medicine (No. BXJ201430)the Natural Science Foundation of Shanghai (No. 14ZR1424000)"Chen Guang" Project supported by Shanghai Municipal Education Commission and Shanghai Education Development Foundation (No. 14CG14)
文摘Implant-associated infection remains a difficult medical problem in orthopedic surgery. Therefore, the development of multifunctional bone implants for treating infection and regenerating lost bone tissue,which may be a result of infection, is important. In the present study, we report the fabrication of enoxacinloaded poly(lactic-co-glycolic acid)(PLGA) coating on porous magnesium scaffold(Enox-PLGA-Mg) which combine the favorable properties of magnesium, the antibacterial property and the effect of inhibition of osteoclastic bone resorption of enoxacin. The drug loaded PLGA coating of Mg scaffold enables higher drug loading efficiency(52%–56%) than non-coating enoxacin loaded Mg scaffold(Enox-Mg)(4%–5%). EnoxPLGA-Mg exhibits sustained drug release for more than 14 days, and this controlled release of enoxacin significantly inhibits bacterial adhesion and prevented biofilm formation by Staphylococcus epidermidis(ATCC35984) and Staphylococcus aureus(ATCC25923). Biocompatibility tests with Balb/c mouse embryo fibroblasts(Balb/c 3T3 cells) indicate that PLGA-Mg has better biocompatibility than Mg. Finally, we also demonstrate that Enox-PLGA-Mg extract potently inhibited osteoclast formation in vitro. Therefore, EnoxPLGA-Mg has the potential to be used as a multifunctional controlled drug delivery system bone scaffolds to prevent and/or treat orthopedic peri-implant infections.
