Objective:To establish a method for directional screening of the cytotoxic components from the medicinal herb of Achnatherum inebrians by a combination of surface plasmon resonance(SPR)biosensor and chromatographic is...Objective:To establish a method for directional screening of the cytotoxic components from the medicinal herb of Achnatherum inebrians by a combination of surface plasmon resonance(SPR)biosensor and chromatographic isolation technology.Methods:Under the guidance of bioactive assessment based on binding abilities between objects and the a-Mannosidase(a-Man)target,the active components from different solvents extracts,different polar extraction parts and fractions were screened orderly and directionally using SPR.Components with a high binding ability to a-Man can be precisely oriented in a narrower fractions range and are easy to isolate.Three human cancer cells were used to evaluate the cytotoxic activity of component with the highest affinity to a-Man.Results:Eight compounds were isolated and identificated from A.inebrians for the first time.Deoxyvasicinone possessed the highest affinity to a-Man among them.Moreover,deoxyvasicinone showed good effects on inhibited proliferation of human hepatoma cells HepG2(IC_(50)=5.7 μmol/L),human breast cancer cells MCF7(IC_(50)=7.21 μmol/L)and human lung cancer cells HCC827(IC_(50)=0.75 μmol/L),respectively.In particular,its inhibitory effect on HCC827 was stronger than the positive drug gefitinib(IC_(50)=1.65 μmol/L).Conclusion:A comprehensive strategy of directional screening potential cytotoxic components from herb based on biomolecular interaction and chromatography was established.Deoxyvasicinone as an effective anti-cancer component was initially isolated from A.inebrians.It is expected that this screening strategy could provide new perspectives for rapid screening and identification of active components from natural plants with the complex matrix.展开更多
With _D-proline as the reducing and capping agent, fluorescent gold nanoclusters were rapidly prepared(_D-Pro@AuNCs) within 10 min at 100℃. In the present of gold nanoparticles, the fluorescence of _DPro@AuNCs was re...With _D-proline as the reducing and capping agent, fluorescent gold nanoclusters were rapidly prepared(_D-Pro@AuNCs) within 10 min at 100℃. In the present of gold nanoparticles, the fluorescence of _DPro@AuNCs was remarkably quenched. Interestingly, based on the electrostatic interaction between anticancer drug Raltitrexed and gold nanoparticles induced fluorescence "turn-on" principle, a high selective assay for detection of Raltitrexed was established with the probe associating the fluorescence emission at 435 nm. The fluorescence intensity of _D-Pro@AuNCs linearly correlated with the concentration of Raltitrexed in the range from 5.0 mmol/L to 40.0 mmol/L(R^2= 0.999) and the limit of detection was 1.9 mmol/L. Further, after Raltitrexed was abdominal injected in rats, a metabolic approach was constructed with the prepared fluorescent probe. It showed great potential of AuNCs-based sensing probes for application in analysis of serum anticancer drugs.展开更多
基金supported by the National Natural Science Foundation of China(No.81573834)the Cultivation Project of Ideological and Political Demonstration Course for Graduate Courses of Minzu University of China(No.GRSKCSZ005)the Foundation of Key Laboratory of Ethnomedicine,Ministry of Education(No.KLEM-ZZ201808).
文摘Objective:To establish a method for directional screening of the cytotoxic components from the medicinal herb of Achnatherum inebrians by a combination of surface plasmon resonance(SPR)biosensor and chromatographic isolation technology.Methods:Under the guidance of bioactive assessment based on binding abilities between objects and the a-Mannosidase(a-Man)target,the active components from different solvents extracts,different polar extraction parts and fractions were screened orderly and directionally using SPR.Components with a high binding ability to a-Man can be precisely oriented in a narrower fractions range and are easy to isolate.Three human cancer cells were used to evaluate the cytotoxic activity of component with the highest affinity to a-Man.Results:Eight compounds were isolated and identificated from A.inebrians for the first time.Deoxyvasicinone possessed the highest affinity to a-Man among them.Moreover,deoxyvasicinone showed good effects on inhibited proliferation of human hepatoma cells HepG2(IC_(50)=5.7 μmol/L),human breast cancer cells MCF7(IC_(50)=7.21 μmol/L)and human lung cancer cells HCC827(IC_(50)=0.75 μmol/L),respectively.In particular,its inhibitory effect on HCC827 was stronger than the positive drug gefitinib(IC_(50)=1.65 μmol/L).Conclusion:A comprehensive strategy of directional screening potential cytotoxic components from herb based on biomolecular interaction and chromatography was established.Deoxyvasicinone as an effective anti-cancer component was initially isolated from A.inebrians.It is expected that this screening strategy could provide new perspectives for rapid screening and identification of active components from natural plants with the complex matrix.
基金the financial support from the National Natural Science Foundation of China (Nos. 21575144, 91732103, 21874138, 21635008, 21621062)
文摘With _D-proline as the reducing and capping agent, fluorescent gold nanoclusters were rapidly prepared(_D-Pro@AuNCs) within 10 min at 100℃. In the present of gold nanoparticles, the fluorescence of _DPro@AuNCs was remarkably quenched. Interestingly, based on the electrostatic interaction between anticancer drug Raltitrexed and gold nanoparticles induced fluorescence "turn-on" principle, a high selective assay for detection of Raltitrexed was established with the probe associating the fluorescence emission at 435 nm. The fluorescence intensity of _D-Pro@AuNCs linearly correlated with the concentration of Raltitrexed in the range from 5.0 mmol/L to 40.0 mmol/L(R^2= 0.999) and the limit of detection was 1.9 mmol/L. Further, after Raltitrexed was abdominal injected in rats, a metabolic approach was constructed with the prepared fluorescent probe. It showed great potential of AuNCs-based sensing probes for application in analysis of serum anticancer drugs.
