The safety of Chuangyuling (CYL) dressing—a multifunctional medicine carrying biomaterial was evaluated in order to provide foundation for the application of CYL as material used in the wound healing. The traditional...The safety of Chuangyuling (CYL) dressing—a multifunctional medicine carrying biomaterial was evaluated in order to provide foundation for the application of CYL as material used in the wound healing. The traditional Chinese medicine (TCM) extract solution was compounded with scaffolds (gelatin and Bletilla hyacinthine gum), and then frozen and dried to form spongy and porous material CYL. According to the standard of biological evaluation of medical devices that was instituted by the ministry of health of China \, the biological evaluation of CYL dressing was conducted. The results showed that all the contents of biological evaluation test consisting of acute toxicity, skin irritation, sensitization and cytotoxicity met the requirement of standards. It was concluded that the biomaterial carrying TCM (CYL dressing) is safe for application of wound healing.展开更多
Protoporphyrinogen oxidase inhibitor has become the focus research field as herbicides.Seven novel N-benzoxazolonyluracils were obtained by cyclization of 6-aminobenzoxazolone derivatives with ethyl 3-dimethylcarbamoy...Protoporphyrinogen oxidase inhibitor has become the focus research field as herbicides.Seven novel N-benzoxazolonyluracils were obtained by cyclization of 6-aminobenzoxazolone derivatives with ethyl 3-dimethylcarbamoylamido-4,4,4-trifluorocrotonate and then methylation or amination, and the reaction yields were between 5900—8600. The chemical structures of the compounds were identified by Elemental Analysis, MS and 1H NMR. Biological results indicate that some compounds exhibit excellent control of broadleaf weeds at post-emergence by low dosage 18.75 ga.i/ha, but are not effective for grass weeds below dosage 37.5 ga.i/ha. In addition, these compounds show no damage at high-dosage 150 ga.i/ha to wheat and corn, but are unsafe to dicotyledonous plants such as cole, soybean and sorghum even at lower dosage 18.75 ga.i/ha.展开更多
Taking the water ecosystem of Small Xingkai Lake as research object,through the survey and analysis of aquatic organism indicators,this paper established an ecosystem integrity evaluation system with the biological in...Taking the water ecosystem of Small Xingkai Lake as research object,through the survey and analysis of aquatic organism indicators,this paper established an ecosystem integrity evaluation system with the biological integrity as the criterion layer. Using the index of biological integrity and comprehensive health index,it evaluated the health status of water ecosystem of Small Xingkai Lake.展开更多
A series of 3-substituted quinazolinones,2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in vitro.The new compounds revealed excellent in vitro ant...A series of 3-substituted quinazolinones,2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in vitro.The new compounds revealed excellent in vitro antifungal activity with broad spectrum.The structure-activity relationships（SARs） of the derivatives were analyzed.Compound 9A2 exhibits better antifungal activity against 5 tested fungi in vitro than fluconazole,especially against Trichophyton rubrum and Microsporum gypseum.This study provides a series of novel lead compounds for the development of non-azole antifungal agents.展开更多
A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which sho...A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which showed the potential for further research as lead compounds.展开更多
3,5-Dimethoxyhomophthalic acid was synthesized in four steps from 3,5-dimethoxycinnamic acid via a series of reactions including cyclization of 3-（3＇,5＇-dimethoxyphenyl）propionic acid to 5,7-dimethoxy-1-indanone a...3,5-Dimethoxyhomophthalic acid was synthesized in four steps from 3,5-dimethoxycinnamic acid via a series of reactions including cyclization of 3-（3＇,5＇-dimethoxyphenyl）propionic acid to 5,7-dimethoxy-1-indanone and oxidative decomposition of methyl-2-hydroxy-2-[5,7-dimethyoxy-1-oxo-1H-inden-2（3H）-ylidene]acetate to 3,5-dimethoxyhomophthalic acid.The synthesized compounds were characterized by elemental analysis,IR,1H NMR,and MS.The biological evaluation experiments of 3,5-dimthoxyhomophthalic acid and the related synthesized compounds were also carried out.Naturally occurring biologically active isocoumarins were prepared in a single step by the condensation of the homophthalic acid with appropriate acid chlorides.展开更多
Dysregulated HGF/c-Met signalling has been associated with many human cancers,poor clinical outcomes,and even resistance acquisition to some approved targeted therapies.As such,c-Met kinase has emerged as an attractiv...Dysregulated HGF/c-Met signalling has been associated with many human cancers,poor clinical outcomes,and even resistance acquisition to some approved targeted therapies.As such,c-Met kinase has emerged as an attractive target for anticancer drug discovery.展开更多
Advancements in screening technologies employing small organisms have enabled deep profiling of compounds in vivo.However,current strategies for phenotyping of behaving animals,such as zebrafish,typically involve tedi...Advancements in screening technologies employing small organisms have enabled deep profiling of compounds in vivo.However,current strategies for phenotyping of behaving animals,such as zebrafish,typically involve tedious manipulations.Here,we develop and validate a fully automated in vivo screening system(AISS)that integrates microfluidic technology and computer-vision-based control methods to enable rapid evaluation of biological responses of non-anesthetized zebrafish to molecular gradients.Via precise fluidic control,the AISS allows automatic loading,encapsulation,transportation and immobilization of single-larva in droplets for multi-organ imaging and chemical gradients generation inaccessible in previous systems.Using this platform,we examine the cardiac sensitivity of an antipsychotic drug with multiple concentration gradients,and reveal dramatic diversity and complexity in the accurate chemical regulation of cardiac functions in vivo.This proposed system expands the arsenal of tools available for in vivo screening and facilitates comprehensive profiling of pharmaceuticals.展开更多
The Hydrobios in Dongping Lake, Shandong Province, mainly includes phytoplankton, zooplankton, benthic animals, fishes and hydrophytic vascular plants. Nitrogen and phosphorus are the restrictive factors for the growt...The Hydrobios in Dongping Lake, Shandong Province, mainly includes phytoplankton, zooplankton, benthic animals, fishes and hydrophytic vascular plants. Nitrogen and phosphorus are the restrictive factors for the growth and propagation of hydrophyta, therefore the key to the prevention and control of eutrophication in lakes lies in the control of the contents of the two elements in the water. Artificial fishing of algae can reduce the concentrations of trophic substances such as nitrogen and phosphorus in the water bodies, and biological measures may decrease the contents of these trophic substances in the bottom sediments and the water bodies, thereby playing an active role in modifying the eutrophication of the lake.展开更多
First Ni(Ⅱ)ternary complex using the quinolone antibacterial agent enoxacin(HEn)as ligand and 1,10-phenanthroline as co-ligand has been synthesized and characterized.It is a mononuclear structure,in which enoxacin ac...First Ni(Ⅱ)ternary complex using the quinolone antibacterial agent enoxacin(HEn)as ligand and 1,10-phenanthroline as co-ligand has been synthesized and characterized.It is a mononuclear structure,in which enoxacin acts as a bidentate ligand bound to the metal through the ketone oxygen and a carboxylate oxygen atom.The complex exhibited good binding propensity to human and bovine serum albumin proteins having relatively high binding constants(6.40×10^(4) and 7.12×10^(4),respectively).The investigation of the interaction of the complex with calf-thymus(CT)DNA has been performed with UV and circular dichroism(CD)spectroscopies,indicating that they bind to CT DNA probably by the intercalative binding mode.The binding constant(K_(b))of the complex with CT DNA calculated with UV is 2.03×10^(5),which is higher than that of free enoxacin drug(2.09×10^(4))and even higher than that of typical intercalation indicator(1.23×10^(5))of ethidium bromide(EB).Fluorescence competitive studies with EB have revealed that the complex exhibited the ability to displace the DNA-bound EB using the intercalative binding site.In addition,the antimicrobial activity showed that the complex exhibited a little bit good inhibition(MIC=1.843μg•mL^(-1))against B.subtilis than free HEn.展开更多
Konjac glucomannan(KGM)is recognized as a safe material for its health-promoting benefits and thus widely used in various fields including pharmaceutical industry.In recent decades,the combination of collagen and KGM ...Konjac glucomannan(KGM)is recognized as a safe material for its health-promoting benefits and thus widely used in various fields including pharmaceutical industry.In recent decades,the combination of collagen and KGM attracts more attentions for biomedical purpose,especially the hybrid films of collagen-KGM or collagen-KGM-polysaccharide.In this study,to further and deeply develop the intrinsic values of both collagen and KGM as biomaterials,a novel kind of composite hydrogel comprising collagen and KGM at a certain ratio was fabricated under mild conditions via fibrillogenesis process of the aqueous blends of collagen and KGM that experienced deacetylation simultaneously.The chemical composition,microcosmic architectures,swelling behavior,biodegradation and dynamic mechanic properties of such resulted composite hydrogels were systematically investigated.Biologic experiments,including cell culture in vitro and hypodermic implantation in vivo,were also conducted on these collagen/KGM composite hydrogels to evaluate their biologic performances.The relevant results prove that,based on collagen self-assembly behavior,this synthesis strategy is efficient to construct a composite hydrogel of collagen/KGM with improved mechanical properties,biodegradability,excellent biocompatibility and bioactivity,which are promising for potential biomedical applications such as tissue engineering and regenerative medicine.展开更多
Non-alcoholic fatty liver disease(NAFLD),a type of liver disease for which no treatment is currently approved,remains a major concern worldwide.It is manifested as simple hepatocyte steatosis and can develop into infl...Non-alcoholic fatty liver disease(NAFLD),a type of liver disease for which no treatment is currently approved,remains a major concern worldwide.It is manifested as simple hepatocyte steatosis and can develop into inflam-mation,fibrosis,cirrhosis and liver cancer in severe cases.However,due to the lack of appropriate in vitro drug testing platforms,an in-depth understanding of the therapeutic activity of ginsenoside Rb_(1) in NAFLD remains challenging.Here,we proposed a NAFLD model on a liver organoids(LOs)-on-a-chip platform to evaluate the therapeutic effect of ginsenoside Rb_(1) in a dynamic,multi-condition and high-throughput manner.This platform allowed us to reshape certain features such as multicellular types and liver-specific functions of the physiology of the human-relative liver.Free fatty acids(FFAs)-induced LOs displayed typical pathological characteristics of NAFLD progression,including steatosis,oxidative stress,lipid peroxidation,inflammation and fibrosis.With ginsenoside Rb_(1) intervention,these pathological features can be significantly improved,which may provide new insights into the potential mechanisms of NAFLD progression and treatment and suggest the clinical implications for humans.The proposed system enables the formation,differentiation,and function of LOs to serve as a scalable,high-throughput and sensitive drug testing model,to potentially expedite the NAFLD drug discovery.展开更多
文摘The safety of Chuangyuling (CYL) dressing—a multifunctional medicine carrying biomaterial was evaluated in order to provide foundation for the application of CYL as material used in the wound healing. The traditional Chinese medicine (TCM) extract solution was compounded with scaffolds (gelatin and Bletilla hyacinthine gum), and then frozen and dried to form spongy and porous material CYL. According to the standard of biological evaluation of medical devices that was instituted by the ministry of health of China \, the biological evaluation of CYL dressing was conducted. The results showed that all the contents of biological evaluation test consisting of acute toxicity, skin irritation, sensitization and cytotoxicity met the requirement of standards. It was concluded that the biomaterial carrying TCM (CYL dressing) is safe for application of wound healing.
文摘Protoporphyrinogen oxidase inhibitor has become the focus research field as herbicides.Seven novel N-benzoxazolonyluracils were obtained by cyclization of 6-aminobenzoxazolone derivatives with ethyl 3-dimethylcarbamoylamido-4,4,4-trifluorocrotonate and then methylation or amination, and the reaction yields were between 5900—8600. The chemical structures of the compounds were identified by Elemental Analysis, MS and 1H NMR. Biological results indicate that some compounds exhibit excellent control of broadleaf weeds at post-emergence by low dosage 18.75 ga.i/ha, but are not effective for grass weeds below dosage 37.5 ga.i/ha. In addition, these compounds show no damage at high-dosage 150 ga.i/ha to wheat and corn, but are unsafe to dicotyledonous plants such as cole, soybean and sorghum even at lower dosage 18.75 ga.i/ha.
文摘Taking the water ecosystem of Small Xingkai Lake as research object,through the survey and analysis of aquatic organism indicators,this paper established an ecosystem integrity evaluation system with the biological integrity as the criterion layer. Using the index of biological integrity and comprehensive health index,it evaluated the health status of water ecosystem of Small Xingkai Lake.
基金supported by the Shandong Natural Science Foundation(No.ZR2012HQ026)the Foundation of Sichuan Provincial Health Department(No.110480)
文摘A series of 3-substituted quinazolinones,2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in vitro.The new compounds revealed excellent in vitro antifungal activity with broad spectrum.The structure-activity relationships（SARs） of the derivatives were analyzed.Compound 9A2 exhibits better antifungal activity against 5 tested fungi in vitro than fluconazole,especially against Trichophyton rubrum and Microsporum gypseum.This study provides a series of novel lead compounds for the development of non-azole antifungal agents.
基金financially supported by the Natural Science Foundation of Jiangsu Province(No.BK2009303)the National Natural Science Foundation of China(No.30973609)+1 种基金Fundamental Research Funds for the Central Universities(No.JKZ2011004)Specialized Research Fund for the Doctoral Program of Higher Education(No.20100096110007)
文摘A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which showed the potential for further research as lead compounds.
基金Supported by Higher Education Commission of Pakistan,the National Basic Research Program of China(No.2003CB114402)the National Natrual Science Foundation of China(No.20672062)the Tianjin Natural Science Foundation(No.07JCYBJC01200).
文摘3,5-Dimethoxyhomophthalic acid was synthesized in four steps from 3,5-dimethoxycinnamic acid via a series of reactions including cyclization of 3-（3＇,5＇-dimethoxyphenyl）propionic acid to 5,7-dimethoxy-1-indanone and oxidative decomposition of methyl-2-hydroxy-2-[5,7-dimethyoxy-1-oxo-1H-inden-2（3H）-ylidene]acetate to 3,5-dimethoxyhomophthalic acid.The synthesized compounds were characterized by elemental analysis,IR,1H NMR,and MS.The biological evaluation experiments of 3,5-dimthoxyhomophthalic acid and the related synthesized compounds were also carried out.Naturally occurring biologically active isocoumarins were prepared in a single step by the condensation of the homophthalic acid with appropriate acid chlorides.
基金This work was supported by the Fundamental Research Funds for the Central Universities(Nos.31920170193 and 31920200026).
文摘Dysregulated HGF/c-Met signalling has been associated with many human cancers,poor clinical outcomes,and even resistance acquisition to some approved targeted therapies.As such,c-Met kinase has emerged as an attractive target for anticancer drug discovery.
基金supported by the National Natural Science Foundation of China(82372088)the National Natural Science Foundation of Guangdong Province(2021A1515010266)+2 种基金the Shenzhen Science and Technology Program(202206193000001,20220816161126002)the Foundation of Guangdong Provincial Key Laboratory of Sensor Technology and Biomedical Instrument(2020B1212060077)2021 Foshan Science and Technology Innovation Team for Young-Top Talents(2120001010795).
文摘Advancements in screening technologies employing small organisms have enabled deep profiling of compounds in vivo.However,current strategies for phenotyping of behaving animals,such as zebrafish,typically involve tedious manipulations.Here,we develop and validate a fully automated in vivo screening system(AISS)that integrates microfluidic technology and computer-vision-based control methods to enable rapid evaluation of biological responses of non-anesthetized zebrafish to molecular gradients.Via precise fluidic control,the AISS allows automatic loading,encapsulation,transportation and immobilization of single-larva in droplets for multi-organ imaging and chemical gradients generation inaccessible in previous systems.Using this platform,we examine the cardiac sensitivity of an antipsychotic drug with multiple concentration gradients,and reveal dramatic diversity and complexity in the accurate chemical regulation of cardiac functions in vivo.This proposed system expands the arsenal of tools available for in vivo screening and facilitates comprehensive profiling of pharmaceuticals.
文摘The Hydrobios in Dongping Lake, Shandong Province, mainly includes phytoplankton, zooplankton, benthic animals, fishes and hydrophytic vascular plants. Nitrogen and phosphorus are the restrictive factors for the growth and propagation of hydrophyta, therefore the key to the prevention and control of eutrophication in lakes lies in the control of the contents of the two elements in the water. Artificial fishing of algae can reduce the concentrations of trophic substances such as nitrogen and phosphorus in the water bodies, and biological measures may decrease the contents of these trophic substances in the bottom sediments and the water bodies, thereby playing an active role in modifying the eutrophication of the lake.
基金The authors thank the financial support by Jiangsu National Science Foundation(No.BK2009239)The project was also funded by the Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources(Guangxi Normal University)the Ministry of Education of China(No.CMEMR2013-B02).
文摘First Ni(Ⅱ)ternary complex using the quinolone antibacterial agent enoxacin(HEn)as ligand and 1,10-phenanthroline as co-ligand has been synthesized and characterized.It is a mononuclear structure,in which enoxacin acts as a bidentate ligand bound to the metal through the ketone oxygen and a carboxylate oxygen atom.The complex exhibited good binding propensity to human and bovine serum albumin proteins having relatively high binding constants(6.40×10^(4) and 7.12×10^(4),respectively).The investigation of the interaction of the complex with calf-thymus(CT)DNA has been performed with UV and circular dichroism(CD)spectroscopies,indicating that they bind to CT DNA probably by the intercalative binding mode.The binding constant(K_(b))of the complex with CT DNA calculated with UV is 2.03×10^(5),which is higher than that of free enoxacin drug(2.09×10^(4))and even higher than that of typical intercalation indicator(1.23×10^(5))of ethidium bromide(EB).Fluorescence competitive studies with EB have revealed that the complex exhibited the ability to displace the DNA-bound EB using the intercalative binding site.In addition,the antimicrobial activity showed that the complex exhibited a little bit good inhibition(MIC=1.843μg•mL^(-1))against B.subtilis than free HEn.
基金The present study was supported by the National Natural Science Foundation of China(Grants 51373105 and 51203103)Sichuan Province Key Research and Development Project(2018SZ0046).
文摘Konjac glucomannan(KGM)is recognized as a safe material for its health-promoting benefits and thus widely used in various fields including pharmaceutical industry.In recent decades,the combination of collagen and KGM attracts more attentions for biomedical purpose,especially the hybrid films of collagen-KGM or collagen-KGM-polysaccharide.In this study,to further and deeply develop the intrinsic values of both collagen and KGM as biomaterials,a novel kind of composite hydrogel comprising collagen and KGM at a certain ratio was fabricated under mild conditions via fibrillogenesis process of the aqueous blends of collagen and KGM that experienced deacetylation simultaneously.The chemical composition,microcosmic architectures,swelling behavior,biodegradation and dynamic mechanic properties of such resulted composite hydrogels were systematically investigated.Biologic experiments,including cell culture in vitro and hypodermic implantation in vivo,were also conducted on these collagen/KGM composite hydrogels to evaluate their biologic performances.The relevant results prove that,based on collagen self-assembly behavior,this synthesis strategy is efficient to construct a composite hydrogel of collagen/KGM with improved mechanical properties,biodegradability,excellent biocompatibility and bioactivity,which are promising for potential biomedical applications such as tissue engineering and regenerative medicine.
基金supported by the Tianjin Synthetic Biotechnology Innovation Capacity Improvement Projects(TSBICIP-CXRC-008)Major Project of Haihe Laboratory of Synthetic Biology(E2M9560201)+1 种基金National Natural Science Foundation of China(32301210&31200035)the China Postdoctoral Science Foundation(No.2022M713330).
文摘Non-alcoholic fatty liver disease(NAFLD),a type of liver disease for which no treatment is currently approved,remains a major concern worldwide.It is manifested as simple hepatocyte steatosis and can develop into inflam-mation,fibrosis,cirrhosis and liver cancer in severe cases.However,due to the lack of appropriate in vitro drug testing platforms,an in-depth understanding of the therapeutic activity of ginsenoside Rb_(1) in NAFLD remains challenging.Here,we proposed a NAFLD model on a liver organoids(LOs)-on-a-chip platform to evaluate the therapeutic effect of ginsenoside Rb_(1) in a dynamic,multi-condition and high-throughput manner.This platform allowed us to reshape certain features such as multicellular types and liver-specific functions of the physiology of the human-relative liver.Free fatty acids(FFAs)-induced LOs displayed typical pathological characteristics of NAFLD progression,including steatosis,oxidative stress,lipid peroxidation,inflammation and fibrosis.With ginsenoside Rb_(1) intervention,these pathological features can be significantly improved,which may provide new insights into the potential mechanisms of NAFLD progression and treatment and suggest the clinical implications for humans.The proposed system enables the formation,differentiation,and function of LOs to serve as a scalable,high-throughput and sensitive drug testing model,to potentially expedite the NAFLD drug discovery.
