OBJECTIVE The total steroid saponins(TSSN)isolated from Dioscorea zingiberensis C.H.Wright(D.zingiberensis)has shown a variety of beneficial bioactivities.However,there are no reports about the neuroprotective effects...OBJECTIVE The total steroid saponins(TSSN)isolated from Dioscorea zingiberensis C.H.Wright(D.zingiberensis)has shown a variety of beneficial bioactivities.However,there are no reports about the neuroprotective effects of the TSSN until now.Therefore,we explored the neuroprotective effects of TSSN on rats against transient focal cerebral ischemia-reperfusion(I/R)and the underlying mechanisms.METHODS The healthy adult Sprague-Dawley rats were randomly assigned into six groups.After pre-treatment with the TSSN intragastrically for six days,the rats were subjected to the ischemia injury by the surgery of middle cerebral artery occlusion(MCAO)for 90 min.Some indexes were evaluated and detected.RESULTS As compared to the I/R group,TSSN group of rats,especially given the 30 mg·kg^-1 of TSSN,not only marked reduction in the neurological deficit scores,cerebral infarct volume,and brain edema,but also an increase in neuron survival(Nissl bodies)in the hippocampal cornuammons 1(CA1)and cortex hemisphere of the ipsilateral ischemia.At the same time,the inflammatory cytokines in serum induced by MCAO were significantly alleviated by the TSSN pre-administration.What′s more,the increase of caspase-3 was evidently reduced in the CA1 and cortex of the hemisphere injured brain.Finally,the down-regulating anti-apoptotic Bcl-2 and up-regulating pro-apoptotic Bax proteins were obviously suppressed.CONCLUSION TSSN plays a potential neuroprotective role against a severe injury induced by transient focal cerebral ischemic reperfusion in a rat experimental model,and this role may be mediated by its antiinflammatory and anti-apoptotic actions.展开更多
Sulfydryl-contained(-SH)substances including hydrogen sulfide(H_(2)S),cysteine(Cys),homocysteine(Hcy)and glutathione(GSH)play crucial roles in living systems,and their variations are closely associated with various di...Sulfydryl-contained(-SH)substances including hydrogen sulfide(H_(2)S),cysteine(Cys),homocysteine(Hcy)and glutathione(GSH)play crucial roles in living systems,and their variations are closely associated with various diseases.Herein,we developed a near-infrared intramolecular charge transfer(ICT)based fluorescent probe Y-NBD,achieving detection of Cys/Hcy and H_(2)S with different fluorescent signals(green-red for Cys/Hcy,red for H_(2)S),large Stokes shifts(∼100/105nm or 191 nm)and high signal-background-ratio,but not responding to GSH.Y-NBD was successfully applied to image exogenous/endogenous Cys/Hcy and H_(2)S in various living cancer cells(HeLa,A549,and HepG2)and in zebrafish.It not only visualized the transformation pathway of several thiols in HepG2 cells but also verified that the intestine is the main site for the activation and metabolism of Y-NBD in zebrafish,as well as realized to evaluate the degree of drug-induced liver injury.This work provides a promising tool for imaging Cys/Hcy and H_(2)S in living systems and shows great potency in evaluating drug-induced liver injury and its treatment.展开更多
Dual-state emission(DSE)molecules displayed conspicuous fluorescent performance both in solid and solution states.However,the construction of DSE molecules and the regulation of their emission wavelengths remains a gr...Dual-state emission(DSE)molecules displayed conspicuous fluorescent performance both in solid and solution states.However,the construction of DSE molecules and the regulation of their emission wavelengths remains a great challenge.Based on the structure-function relationship of quinolinonitrile-type fluorophores,this work proposed a feasible strategy for modulating their fluorescent properties into DSE via limiting the torsion angle between the quinoline ring and C=C bond in the range of 4.7°to 30°.Based on this strategy,53 compounds were obtained which displayed tunable emission wavelengths from^(3)97 nm to 740 nm in solid-state and from 360 nm to 672 nm in solution.The feasibility of the strategy was supported by a series of theoretical calculations,optical characterizations,and crystal analysis,suggesting the compounds have great potential in imaging living cells and tissues with desired wavelengths.展开更多
Objective Establishing a fingerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for fingerprint analysis and determin...Objective Establishing a fingerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for fingerprint analysis and determination of four ingredients in G. macrophylla roots from different sources. LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the fingerprint. Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides. Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS. Four secoiridoid glucosides were identified based on their MS data. Conclusion The method is specific and could be served for the quality identification and comprehensive evaluation of G. macrophylla.展开更多
To improve the therapeutic effect of rhaponticin （RHA）, a folate receptor （FR） targeted RHA prodrug was designed and regioselectively synthesized by utilizing a hydrophilic peptide spacer linked to folic acid （FA...To improve the therapeutic effect of rhaponticin （RHA）, a folate receptor （FR） targeted RHA prodrug was designed and regioselectively synthesized by utilizing a hydrophilic peptide spacer linked to folic acid （FA） via a releasable disulfide linker. A series of biological evaluation was investigated in vitro and in vivo. The positive results of biological investigations warrant further preclinical study before this novel targeted chemotherapeutic is considered for clinical investigation.展开更多
Hydrogenation/deuteration of carbon chloride(C–Cl)bonds is of high significance but remains a remarkable challenge in synthetic chemistry,especially using safe and inexpensive hydrogen donors.In this article,a visibl...Hydrogenation/deuteration of carbon chloride(C–Cl)bonds is of high significance but remains a remarkable challenge in synthetic chemistry,especially using safe and inexpensive hydrogen donors.In this article,a visible-light-photocatalytic watersplitting hydrogenation technology(WSHT)is proposed to in-situ generate active H-species(i.e.,Had)for controllable hydrogenation of aryl chlorides instead of using flammable H2.When applying heavy water-splitting systems,we could selectively install deuterium at the C–Cl position of aryl chlorides under mild conditions for the sustainable synthesis of high-valued added deuterated chemicals.Sub-micrometer Pd nanosheets(Pd NSs)decorated crystallined polymeric carbon nitrides(CPCN)is developed as the bifunctional photocatalyst,whereas Pd NSs not only serve as a cocatalyst of CPCN to generate and stabilize H(D)-species but also play a significant role in the sequential activation and hydrogenation/deuteration of C–Cl bonds.This article highlights a photocatalytic-WSHT for controllable hydrogenation/deuteration of low-cost aryl chlorides,providing a promising way for the photosynthesis of high-valued added chemicals instead of the hydrogen evolution.展开更多
Thiophenol(PhSH)is an important raw material for organic synthesis,while its high toxicity to organisms makes it an environmental pollutant.Therefore,it is crucial to accurately detect PhSH and explore its metabolic p...Thiophenol(PhSH)is an important raw material for organic synthesis,while its high toxicity to organisms makes it an environmental pollutant.Therefore,it is crucial to accurately detect PhSH and explore its metabolic process in the living system.Herein,a near-infrared(NIR)fluorescent probe TEM-FB was developed for sensing PhSH with a turn-on fluorescent signal at 719nm and a large Stokes shift(198 nm)based on generating the intramolecular charge transfer(ICT)process.TEM-FB shows high specificity and significant sensitivity towards PhSH(detection limit:10 nmol/L)via the aromatic nucleophilic substitution mechanism.Furthermore,it was successfully applied to image PhSH in multiple cell lines and in zebrafish.Notably,we revealed the oxidative stress process caused by PhSH and demonstrated that the hydrogen peroxide(H_(2)O_(2))in cells would alleviate the poisonousness from exogenous PhSH for the first time.This work provides a promising bioimaging tool for monitoring PhSH in living systems and visualizing the process of oxidative stress induced by PhSH.展开更多
基金National Natural Science Foundation of China(81603267)Fundamental Research Funds for the Central UniversitiesShaanxi Key Laboratory of "Qiyao"Resources and Anti-tumor Activities
文摘OBJECTIVE The total steroid saponins(TSSN)isolated from Dioscorea zingiberensis C.H.Wright(D.zingiberensis)has shown a variety of beneficial bioactivities.However,there are no reports about the neuroprotective effects of the TSSN until now.Therefore,we explored the neuroprotective effects of TSSN on rats against transient focal cerebral ischemia-reperfusion(I/R)and the underlying mechanisms.METHODS The healthy adult Sprague-Dawley rats were randomly assigned into six groups.After pre-treatment with the TSSN intragastrically for six days,the rats were subjected to the ischemia injury by the surgery of middle cerebral artery occlusion(MCAO)for 90 min.Some indexes were evaluated and detected.RESULTS As compared to the I/R group,TSSN group of rats,especially given the 30 mg·kg^-1 of TSSN,not only marked reduction in the neurological deficit scores,cerebral infarct volume,and brain edema,but also an increase in neuron survival(Nissl bodies)in the hippocampal cornuammons 1(CA1)and cortex hemisphere of the ipsilateral ischemia.At the same time,the inflammatory cytokines in serum induced by MCAO were significantly alleviated by the TSSN pre-administration.What′s more,the increase of caspase-3 was evidently reduced in the CA1 and cortex of the hemisphere injured brain.Finally,the down-regulating anti-apoptotic Bcl-2 and up-regulating pro-apoptotic Bax proteins were obviously suppressed.CONCLUSION TSSN plays a potential neuroprotective role against a severe injury induced by transient focal cerebral ischemic reperfusion in a rat experimental model,and this role may be mediated by its antiinflammatory and anti-apoptotic actions.
基金supported by the National Natural Science Foundation of China(Nos.22077099 and 22171223)the Innovation Capability Support Program of Shaanxi(Nos.2023-CX-TD-75 and 2022KJXX-32)+4 种基金the Technology Innovation Leading Program of Shaanxi(Program No.2023KXJ-209)the Natural Science Basic Research Program of Shaanxi(Nos.2022JQ-151 and 2023-JC-YB-141)Young Talent Fund of Association for Science and Technology in Shaanxi,China(No.SWYY202206)the Shaanxi Fundamental Science Research Project for Chemistry&Biology(Nos.22JHZ010 and 22JHQ080)the Yan’an City Science and Technology Project(No.2022SLZDCY-002).
文摘Sulfydryl-contained(-SH)substances including hydrogen sulfide(H_(2)S),cysteine(Cys),homocysteine(Hcy)and glutathione(GSH)play crucial roles in living systems,and their variations are closely associated with various diseases.Herein,we developed a near-infrared intramolecular charge transfer(ICT)based fluorescent probe Y-NBD,achieving detection of Cys/Hcy and H_(2)S with different fluorescent signals(green-red for Cys/Hcy,red for H_(2)S),large Stokes shifts(∼100/105nm or 191 nm)and high signal-background-ratio,but not responding to GSH.Y-NBD was successfully applied to image exogenous/endogenous Cys/Hcy and H_(2)S in various living cancer cells(HeLa,A549,and HepG2)and in zebrafish.It not only visualized the transformation pathway of several thiols in HepG2 cells but also verified that the intestine is the main site for the activation and metabolism of Y-NBD in zebrafish,as well as realized to evaluate the degree of drug-induced liver injury.This work provides a promising tool for imaging Cys/Hcy and H_(2)S in living systems and shows great potency in evaluating drug-induced liver injury and its treatment.
基金supported by the National Natural Science Foundation of China(Nos.22077099 and 22171223)The Innovation Capability Support Program of Shaanxi(Nos.2023-CX-TD-75 and 2022KJXX-32)+5 种基金the Scientific and Technological Innovation Team of Shaanxi Province(No.2022TD-36)the Technology Innovation Leading Program of Shaanxi(No.2023KXJ-209)the Natural Science Basic Research Program of Shaanxi(Nos.2023-JC-YB-141 and 2022JQ-151)Young Talent Fund of Association for Science and Technology in Shaanxi,China(No.SWYY202206)the Shaanxi Fundamental Science Research Project for Chemistry&Biology(Nos.22JHZ010 and 22JHQ080)the Yan’an City Science and Technology Project(No.2022SLZDCY-002)。
文摘Dual-state emission(DSE)molecules displayed conspicuous fluorescent performance both in solid and solution states.However,the construction of DSE molecules and the regulation of their emission wavelengths remains a great challenge.Based on the structure-function relationship of quinolinonitrile-type fluorophores,this work proposed a feasible strategy for modulating their fluorescent properties into DSE via limiting the torsion angle between the quinoline ring and C=C bond in the range of 4.7°to 30°.Based on this strategy,53 compounds were obtained which displayed tunable emission wavelengths from^(3)97 nm to 740 nm in solid-state and from 360 nm to 672 nm in solution.The feasibility of the strategy was supported by a series of theoretical calculations,optical characterizations,and crystal analysis,suggesting the compounds have great potential in imaging living cells and tissues with desired wavelengths.
基金National Science and Technology Ministry "Significant new drugs creation" special science and Technology Major (20082X09101-016)
文摘Objective Establishing a fingerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for fingerprint analysis and determination of four ingredients in G. macrophylla roots from different sources. LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the fingerprint. Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides. Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS. Four secoiridoid glucosides were identified based on their MS data. Conclusion The method is specific and could be served for the quality identification and comprehensive evaluation of G. macrophylla.
基金supported by the National Scientific Foundation of China(No81001622)
文摘To improve the therapeutic effect of rhaponticin （RHA）, a folate receptor （FR） targeted RHA prodrug was designed and regioselectively synthesized by utilizing a hydrophilic peptide spacer linked to folic acid （FA） via a releasable disulfide linker. A series of biological evaluation was investigated in vitro and in vivo. The positive results of biological investigations warrant further preclinical study before this novel targeted chemotherapeutic is considered for clinical investigation.
基金supported by the National Natural Science Foundation of China(21972094,51701127,21401190)China Postdoctoral Science Foundation(2017M612709)+5 种基金Guangdong Special Support ProgramPengcheng Scholar ProgramShenzhen Peacock Plan(KQJSCX20170727100802505,KQTD2016053112042971)Educational Commission of Guangdong Province(2016KTSCX126)Foundation for Distinguished Young Talents in Higher Education of Guangdong(2018KQNCX221)Shenzhen Innovation Program(JCYJ20170818142642395).
文摘Hydrogenation/deuteration of carbon chloride(C–Cl)bonds is of high significance but remains a remarkable challenge in synthetic chemistry,especially using safe and inexpensive hydrogen donors.In this article,a visible-light-photocatalytic watersplitting hydrogenation technology(WSHT)is proposed to in-situ generate active H-species(i.e.,Had)for controllable hydrogenation of aryl chlorides instead of using flammable H2.When applying heavy water-splitting systems,we could selectively install deuterium at the C–Cl position of aryl chlorides under mild conditions for the sustainable synthesis of high-valued added deuterated chemicals.Sub-micrometer Pd nanosheets(Pd NSs)decorated crystallined polymeric carbon nitrides(CPCN)is developed as the bifunctional photocatalyst,whereas Pd NSs not only serve as a cocatalyst of CPCN to generate and stabilize H(D)-species but also play a significant role in the sequential activation and hydrogenation/deuteration of C–Cl bonds.This article highlights a photocatalytic-WSHT for controllable hydrogenation/deuteration of low-cost aryl chlorides,providing a promising way for the photosynthesis of high-valued added chemicals instead of the hydrogen evolution.
基金supported by the National Natural Science Foundation of China(Nos.22077099 and 22171223)the Technology Innovation Leading Program of Shaanxi(No.2020TG-031)+3 种基金the Innovation Capability Support Program of Shaanxi(Nos.2023-CXTD-75 and 2022KJXX-32)the Natural Science Basic Research Program of Shaanxi(No.2023-JC-YB-141)Young Talent Fund of Association for Science and Technology in Shaanxi,China(No.SWYY202206)the Natural Science Basic Research Plan in Shaanxi Province of China(Nos.2022JQ-151 and 2022JQ-125).
文摘Thiophenol(PhSH)is an important raw material for organic synthesis,while its high toxicity to organisms makes it an environmental pollutant.Therefore,it is crucial to accurately detect PhSH and explore its metabolic process in the living system.Herein,a near-infrared(NIR)fluorescent probe TEM-FB was developed for sensing PhSH with a turn-on fluorescent signal at 719nm and a large Stokes shift(198 nm)based on generating the intramolecular charge transfer(ICT)process.TEM-FB shows high specificity and significant sensitivity towards PhSH(detection limit:10 nmol/L)via the aromatic nucleophilic substitution mechanism.Furthermore,it was successfully applied to image PhSH in multiple cell lines and in zebrafish.Notably,we revealed the oxidative stress process caused by PhSH and demonstrated that the hydrogen peroxide(H_(2)O_(2))in cells would alleviate the poisonousness from exogenous PhSH for the first time.This work provides a promising bioimaging tool for monitoring PhSH in living systems and visualizing the process of oxidative stress induced by PhSH.
