Brusatol,a triterpene lactone compound mainly from Brucea javanica,sensitizes a broad spectrum of cancer cells.It is known as a specific inhibitor of nuclear factor-erythroid 2-related factor 2(Nrf2)pathway.In this re...Brusatol,a triterpene lactone compound mainly from Brucea javanica,sensitizes a broad spectrum of cancer cells.It is known as a specific inhibitor of nuclear factor-erythroid 2-related factor 2(Nrf2)pathway.In this review,we provide a comprehensive overview on the antitumor effect and molecular mechanisms of brusatol in vitro and in vivo.This review also covers pharmacokinetics studies,modification of dosages forms of brusatol.Increasing evidences have validated the value of brusatol as a chemotherapeutic agent in cancers,which may contribute to drug development and clinical application.展开更多
Objective:The purpose of this study was to investigate the inhibitory effect of brusatol,a nigakilactone extracted from Brucea javanica,on lung cancer for development of therapeutic drugs.We explored the effects of br...Objective:The purpose of this study was to investigate the inhibitory effect of brusatol,a nigakilactone extracted from Brucea javanica,on lung cancer for development of therapeutic drugs.We explored the effects of brusatol on the proliferation,migration,and invasion of lung cancer PC-9 cells in vitro and analyzed the mechanisms involved.Materials and Methods:MTT assay was used to determine the effect of brusatol on the proliferative capacity of PC-9 and H1975 cells in vitro.The half-maximal inhibitory concentrations(IC_(50))were calculated and used as a reference for subsequent experiments.Variations in the number and size of tumor cell clusters were monitored by the colony formation assay as evidence for the effect of brusatol on cell proliferation.The effect of brusatol on the migration and invasion of PC-9 cells was evaluated using wound healing and transwell assays,respectively.Apoptosis in lung cancer cells was detected using the Annexin V-FITC/propidium iodide assay.The correlated anticancer mechanism was detected using Western blotting.Results:The IC_(50)values of brusatol acting on PC-9 and H1975 cells were 1.58±0.30μM and 31.34±2.72μM,respectively,according to the MTT experiment.In addition,brusatol suppressed PC-9 cell proliferation,migration,and invasion,as well as induced apoptosis,which may be related to the downregulation of epidermal growth factor receptor(EGFR),β-catenin,Akt,and STAT3 expression.Conclusions:Brusatol showed potent anticancer activity against lung cancer PC-9 cells,inhibiting the proliferative capacity and metastatic potential of PC-9 cells.Its anticancer effect may be related to the downregulation of EGFR,β-catenin,Akt,and STAT3.展开更多
In the pathological changes of psoriasis vulgaris,excessive proliferation of keratinocytes,proliferation of microvessels,infiltration of a large number of inflammatory cells,and great shortening of epidermal replaceme...In the pathological changes of psoriasis vulgaris,excessive proliferation of keratinocytes,proliferation of microvessels,infiltration of a large number of inflammatory cells,and great shortening of epidermal replacement time,are the manifestations of Qi and Yin depletion,and they all correspond with pathological changes of nutrient Qi and blood deficiency caused by excessive loss.The treatment of psoriasis should focus on cold straight fire,convergence and fixation.Therefore,it is feasible to treat psoriasis with hoop in theory,and it is found that"cold hoop confining medicine"may be more suitable for the treatment of psoriasis vulgaris in the gradual progress of the experiment.The research could provide theoretical basis for the application of cold hoop confining medicine represented by brusatol in psoriasis vulgaris and related diseases.展开更多
基金supported by National Natural Science Foundation of China(81872767)。
文摘Brusatol,a triterpene lactone compound mainly from Brucea javanica,sensitizes a broad spectrum of cancer cells.It is known as a specific inhibitor of nuclear factor-erythroid 2-related factor 2(Nrf2)pathway.In this review,we provide a comprehensive overview on the antitumor effect and molecular mechanisms of brusatol in vitro and in vivo.This review also covers pharmacokinetics studies,modification of dosages forms of brusatol.Increasing evidences have validated the value of brusatol as a chemotherapeutic agent in cancers,which may contribute to drug development and clinical application.
基金the National Key R and D Program of China(2021YFE0202000)the National Natural Science Foundation of China(81773888)+1 种基金the Natural Science Foundation of Guangdong Province(2020A1515010605)the Special Funds for the Cultivation of Guangdong College Students’Scientific and Technological Innovation(pdjh2020b0483)。
文摘Objective:The purpose of this study was to investigate the inhibitory effect of brusatol,a nigakilactone extracted from Brucea javanica,on lung cancer for development of therapeutic drugs.We explored the effects of brusatol on the proliferation,migration,and invasion of lung cancer PC-9 cells in vitro and analyzed the mechanisms involved.Materials and Methods:MTT assay was used to determine the effect of brusatol on the proliferative capacity of PC-9 and H1975 cells in vitro.The half-maximal inhibitory concentrations(IC_(50))were calculated and used as a reference for subsequent experiments.Variations in the number and size of tumor cell clusters were monitored by the colony formation assay as evidence for the effect of brusatol on cell proliferation.The effect of brusatol on the migration and invasion of PC-9 cells was evaluated using wound healing and transwell assays,respectively.Apoptosis in lung cancer cells was detected using the Annexin V-FITC/propidium iodide assay.The correlated anticancer mechanism was detected using Western blotting.Results:The IC_(50)values of brusatol acting on PC-9 and H1975 cells were 1.58±0.30μM and 31.34±2.72μM,respectively,according to the MTT experiment.In addition,brusatol suppressed PC-9 cell proliferation,migration,and invasion,as well as induced apoptosis,which may be related to the downregulation of epidermal growth factor receptor(EGFR),β-catenin,Akt,and STAT3 expression.Conclusions:Brusatol showed potent anticancer activity against lung cancer PC-9 cells,inhibiting the proliferative capacity and metastatic potential of PC-9 cells.Its anticancer effect may be related to the downregulation of EGFR,β-catenin,Akt,and STAT3.
基金Supported by National Science Foundation for Young Scholars(81704090)Key Projects of Chongqing Municipal Science and Technology Commission(cstc2017jcyjbx0044).
文摘In the pathological changes of psoriasis vulgaris,excessive proliferation of keratinocytes,proliferation of microvessels,infiltration of a large number of inflammatory cells,and great shortening of epidermal replacement time,are the manifestations of Qi and Yin depletion,and they all correspond with pathological changes of nutrient Qi and blood deficiency caused by excessive loss.The treatment of psoriasis should focus on cold straight fire,convergence and fixation.Therefore,it is feasible to treat psoriasis with hoop in theory,and it is found that"cold hoop confining medicine"may be more suitable for the treatment of psoriasis vulgaris in the gradual progress of the experiment.The research could provide theoretical basis for the application of cold hoop confining medicine represented by brusatol in psoriasis vulgaris and related diseases.
