Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biologic...Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biological applications, and have long been utilized as replacements to popular platinum based-drugs. Here, we report a novel series of ruthenium（ll） arene compounds bearing thiosemicarba- zone and isonicotinylhydrazone ligands with potent anticancer activity their structure activity relationships and apoptosis was studied. The cytotoxic activity of the new ruthenium（ll） arene compounds has been evaluated in several cell lines （Molt 4/C8, LI 210, CEM, HL60 and BEL7402）. Among them, ten complexes were found to be excellent in vitro growth inhibitory activity against various cell lines with IC50 in the sub-micromolar range.展开更多
Methicillin-resistant Staphylococcus aureus (MRSA), the most common pathogen in hospital and community environments, can cause serious and even fatal infections. The antibiotics currently used for clinical treatment o...Methicillin-resistant Staphylococcus aureus (MRSA), the most common pathogen in hospital and community environments, can cause serious and even fatal infections. The antibiotics currently used for clinical treatment of MRSA have developed resistance, and there is an urgent need to develop new antimicrobials to treat infections caused by MRSA strains. Quinoline analogues play an important role in the development of antimicrobials. Herein, we discussed the current development of antibacterial activities of quinoline analogues, mainly for anti-MRSA activity, and their structure-activity relationships (SARs) from the perspective of using the quinoline nucleus to search for novel potential anti-MRSA candidates. Additionally, the mechanisms of some representative quinoline analogues against MRSA were clarified. Altogether, this review could provide further insights for the rational development of quinoline-based antibacterial drugs, especially against MRSA.展开更多
Human Notum(hNotum)inhibitors could be used for treating Wnt signalling-associated diseases including colorectal cancer.Herein,two series of chalcone derivatives were designed and synthesized aiming to find selective ...Human Notum(hNotum)inhibitors could be used for treating Wnt signalling-associated diseases including colorectal cancer.Herein,two series of chalcone derivatives were designed and synthesized aiming to find selective and potent hNotum inhibitors.Structure–activity relationship(SAR)studies showed that 2-methoxyl and 5-bromine substitutions on A-ring significantly enhanced anti-hNotum effect,while 4’-ethoxyl and 3’-alkyl substitutions on B-ring were beneficial for hNotum inhibition.Among all tested chalcones,B11 displayed the most potent anti-Notum effect(IC_(50)=3.6 nmol/L),good selectivity,excellent chemical stability and suitable metabolic stability.Further investigations showed that B11 acted as a competitive inhibitor of hNotum,while this agent(5μmol/L)significantly weaken the migration abilities of colorectal cancer cells.Collectively,this study deciphers the SARs of chalcones as hNotum inhibitors and reports a novel and potent hNotum inhibitor with the anti-migration effect on colorectal cancer cells,which offers a promising lead compound to develop novel anti-cancer agents.展开更多
The biological activity against Staphylococcus aureus, and Eschericia coil were investigated implementing three series, the first series was l-phenyl-2-（4＇-X-phenyl）-4-（2,4-dichlorophenyl）-1,3-butadiene, where X ...The biological activity against Staphylococcus aureus, and Eschericia coil were investigated implementing three series, the first series was l-phenyl-2-（4＇-X-phenyl）-4-（2,4-dichlorophenyl）-1,3-butadiene, where X = H, CH3, OCH3, NH2, C1, F, NO2 and COOEt; the second was 3,4-dichlorochalcone series namely 3-（3,4-dichlorophenyl）-l-（4＇-X-phenyl）-2-propen-l-one, where X = H, CH3, OCH3, NH2, CI, F, NO2 and CN; and the third one was 2,4-dichlorochalcone series namely 3-（2,4-dichlorophenyl）-l- （4＇-X-phenyl）-2-propen-l-one, where X = H, CH3, OCH3, NH2, C1, F, NO2 and COOEt. MIC, MBC and the percentage of inhibition （activity） at 20 ~tg/mL, 15 μg/mL and 10μg/mL against Eschericia coli, and at 7.5 lag/mL, 5 μg/mL and 2.5 μg/mL against Staphylococcus aureus, were determined for each compound in the three series. Highest MIC activity against E. coli and S. aureus were given by 2,4-dichlorochalcone series. Butadiene series was similar in behavior to 2,4-dichlorochalcone series in MIC activity against S. aureus. Results of MBC revealed that compounds in the three series exerted high activity against both types of bacteria. Compounds substituted with nitro or nitril exhibited higher activity than other compounds in the three series. Percentage of inhibition of halogenated compounds （4＇-C1 and 4＇-F） was almost equal in every series. Compounds with substituents （4＇-H and 4＇-CH3） showed fluctuation in activity according to the nature of each series.展开更多
Peptides are functional active fragments of proteins which can provide nutrients needed for human growth and development,and they also have unique physiological activity characteristics relative to proteins.Bioactive ...Peptides are functional active fragments of proteins which can provide nutrients needed for human growth and development,and they also have unique physiological activity characteristics relative to proteins.Bioactive peptides contain a great deal of development potential.More specifically,food-derived bioactive peptides have the advantages of a wide variety of sources,unique structures,high efficiency and safety,so they have broad development prospects.This review provides an overview of the current advances regarding the preparation,functional characteristics,and structure–activity relationships of food-derived bioactive peptides.Moreover,the prospects for the future development and application of food-derived bioactive peptides are discussed.This review may provide a better understanding of foodderived bioactive peptides,and some constructive inspirations for further research and applications in the food industry.展开更多
Effects of carboxylic acid collector, benzohydroxamic acid (BHA), sodium hexametaphosphate (SHAP), sodium silicate, and oxalic acid on scheelite flotation were studied through flotation tests, quantum chemical calcula...Effects of carboxylic acid collector, benzohydroxamic acid (BHA), sodium hexametaphosphate (SHAP), sodium silicate, and oxalic acid on scheelite flotation were studied through flotation tests, quantum chemical calculation, and flotation solution computational chemistry. In terms of the calculation results, the relationship between chemical reactions occurring on the scheelite surface and molecular structures of the reagents were analyzed. The results show that BHA and carboxylic acid collectors interact with scheelite in different forms and the recovery of scheelite using sodium oleate as collector declines successively from SHAP, sodium silicate, to oxalic acid. Moreover, it is found that the performance of depressant in scheelite flotation is directly related to the group electronegativity, indicating that the latter is a dominant factor that determines the former. These findings will be helpful to the academic research communities of scheelite flotation.展开更多
A method for the analysis of the relationship between the helical structure and optical activity was proposed by the study of the conformations and X-ray diffraction structures of some cyclic esters prepared by esteri...A method for the analysis of the relationship between the helical structure and optical activity was proposed by the study of the conformations and X-ray diffraction structures of some cyclic esters prepared by esterification of L-(-)-2.3-O-methylidene threitol and L-(+)-2,3-O-isopropplidene threitol with alkanedioyl dichlorides and o-,m-,and p-phthaloyl dichlorides.展开更多
Firstly discovered in 1980s, human immunodeficiency virus （HIV） continues to affect more and more people. However, there is no effective drug available for the therapy of HIV infection. Betulinic acid existing in va...Firstly discovered in 1980s, human immunodeficiency virus （HIV） continues to affect more and more people. However, there is no effective drug available for the therapy of HIV infection. Betulinic acid existing in various medicinal herbs and fruits exhibits multiple biological effects, especially its outstanding anti-HIV activity, which has drawn the attentions of many pharmacists. Among the derivatives of betulinic acid, some compounds exhibited inhibitory activities at the nanomolar concentration, and have entered phase II clinical trials. This paper summarizes the current investigations on the anti-HIV activity of betulinic acid analogues, and provides valuable data for subsequent researches.展开更多
To utilize themultiple functions and give full play of ginsenosides,a variety of ginsenosides with different structures were prepared into liposomes and evaluated for their effect on the stability,pharmacokinetics and...To utilize themultiple functions and give full play of ginsenosides,a variety of ginsenosides with different structures were prepared into liposomes and evaluated for their effect on the stability,pharmacokinetics and tumor targeting capability of liposomes.The results showed that the position and number of glycosyl groups of ginsenosides have significant effect on the in vitro and in vivo properties of their liposomes.The pharmacokinetics of ginsenosides liposomes indicated that the C-3 sugar group of ginsenosides is beneficial to their liposomes for longer circulation in vivo.The C-3 and C-6 glycosyls can enhance the uptake of their liposomes by 4T1 cells,and the glycosyls at C-3 position can enhance the tumor active targeting ability significantly,based on the specific binding capacity to Glut 1 expressed on the surface of 4T1 cells.According to the results in the study,ginsenoside Rg3 and ginsenoside Rh2 are potential for exploiting novel liposomes because of their cholesterol substitution,long blood circulation and tumor targeting capabilities.The results provide a theoretical basis for further development of ginsenoside based liposome delivery systems.展开更多
New series of pyrazolo[1,5-α]pyrimidine derivatives 7a-i,11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines,namely colorectal car...New series of pyrazolo[1,5-α]pyrimidine derivatives 7a-i,11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines,namely colorectal carcinoma（HCT116）,prostate adenocarcinoma（PC-3） and liver carcinoma（HepG-2） using MTT cytotoxicity assay at 100 μg/mL.Some of the tested compounds displayed good anticancer activities against HCT-116 and PC-3 cells.Whereas,compounds 7d and 11 a showed better antitumor activity than the rest of the compounds against both cell lines.A structure-activity relationship（SAR） has been discussed and structures of the newly synthesized compounds were confirmed by different spectral data（MS,IR,^1H NMR and ^13C NMR） and elemental analysis.展开更多
In this review, we retrospect our progress in biological active naphthalimide and analogues as antitumor agents in the past 20 years. On one hand, various derivations in naphthalimide pharmacophores were developed to ...In this review, we retrospect our progress in biological active naphthalimide and analogues as antitumor agents in the past 20 years. On one hand, various derivations in naphthalimide pharmacophores were developed to enhance their DNA binding affinity and antitumor property thereby. Heterocyclic fused naphthalimides, bis-naphthalimides, non-fused substituted naphthalimides and the carboxamide derivatives were synthesized. For example, thio-heterocyclic fused-naphthalimides were designed and evaluated in comparison with their oxo-heterocyclic fused analogues. Extended or created heterocyclebased skeleton were also developed as antitumor agents. On the other hand, we broaden the design strategy of naphthalimide antitumor agents besides DNA intercalation and topo II poison. We have introduced more drug design methods, such as prodrugs, multitarget drugs, computer-aided drug design,photodynamic therapy. For example, we have got naphthalimide derivatives which inhibited topo II and induced LMP by introducing long alkyl chain and polyamines. Several representative compounds were clarified of their antitumor mechanism of action. In all, our research improves the structure diversity of naphthalimide antitumor agents and distinct variances of antitumor targets and mechanism of action.展开更多
A series of trihydrocarbyltin chlorides containing silicon was synthesized. The acaricidal activity was determined and the structure activity relationship was tried to be found out with the hydrophobic parameter.
Demethoxylation was kinetically and spectroscopically studied over three catalysts with different Ru^(0)/Ru^(δ+) ratios.In-situ spectroscopic tests demonstrated that the synergy between Ru^(0)and Ru^(δ+) was crucial...Demethoxylation was kinetically and spectroscopically studied over three catalysts with different Ru^(0)/Ru^(δ+) ratios.In-situ spectroscopic tests demonstrated that the synergy between Ru^(0)and Ru^(δ+) was crucial,and Ru^(0) was in charge of H_(2) activation and adsorption of aromatic ring while Ru^(δ+) adsorbed with O in methoxyl.A Langmuir-Hinshelwood kinetic model was proposed,and ratio of Ru^(0)/Ru^(δ+) was the key in deciding the rate-determining step(RDS):i)desorp-tion of toluene was RDS over catalyst with highRu^(0)ratio;ii)dissociation of H_(2) was RDS over Ru^(δ+) enriched catalyst;iii)demethoxylation was rate-determined by CO water-gas shift (WGS) when Ru^(0)/Ru^(δ+) approached~1.The best perfor-mance was obtained over Ru/NiAl_(2)O_(4)-200,which effectively enabled both C-O bond activation and rapid recovery of adsorption sites for aromatic rings.Finally,in-situ DRIFT studies on methoxy decomposition and CO-WGS unraveled that the electronic composition of Ru was more stable in Ru/NiAl_(2)O_(4)-200 which contributes to its excellence.展开更多
Precisely tuning the spacing of the active centers on the atomic scale is of great significance to improve the catalytic activity and deepen the understanding of the catalytic mechanism,but still remains a challenge.H...Precisely tuning the spacing of the active centers on the atomic scale is of great significance to improve the catalytic activity and deepen the understanding of the catalytic mechanism,but still remains a challenge.Here,we develop a strategy to dilute catalytically active metal interatomic spacing(d_(M-M))with light atoms and discover the unusual adsorption patterns.For example,by elevating the content of boron as interstitial atoms,the atomic spacing of osmium(d_(Os-Os))gradually increases from 2.73 to 2.96?.More importantly,we find that,with the increase in dOs-Os,the hydrogen adsorption-distance relationship is reversed via downshifting d-band states,which breaks the traditional cognition,thereby optimizing the H adsorption and H_2O dissociation on the electrode surface during the catalytic process;this finally leads to a nearly linear increase in hydrogen evolution reaction activity.Namely,the maximum dOs-Os of 2.96?presents the optimal HER activity(8 mV@10 mA cm^(-2))in alkaline media as well as suppressed O adsorption and thus promoted stability.It is believed that this novel atomic-level distance modulation strategy of catalytic sites and the reversed hydrogen adsorption-distance relationship can shew new insights for optimal design of highly efficient catalysts.展开更多
The presence of hydroxyl groups at the C4 and C7 positions in coumarin backbone has been proposed as a potential modification site for providing excellent bioactivity according to previous studies. A series of novel c...The presence of hydroxyl groups at the C4 and C7 positions in coumarin backbone has been proposed as a potential modification site for providing excellent bioactivity according to previous studies. A series of novel coumarin derivatives were rationally designed and synthesized by use of a complex catalytic system for a targeted modification at the above sites. These derivatives were assayed for nematicidal activity. As predicted, the derivatization enhanced the activity of the coumarins against five nematodes.Compounds 7b, 9a, 10 c and 11 c showed significant strong nematicidal broad spectrum activity against all tested nematodes. Compound 10 c was the most effective with the lowest LC50 values against Meloidogyne incognita（5.1 mmol/L）, Ditylenchus destructor（3.7 mmol/L）, Bursaphelenchus mucronatus（6.4 mmol/L）, Bursaphelenchus B. xylophilus（2.5 mmol/L） and Aphelenchoides besseyi（3.1 mmol/L）,respectively. A brief investigation on the structure–activity relationships（SAR） revealed that the targeted modification by a C7 hydroxyl was optimum compared with that of a C4 hydroxyl and that the coupling chain length was crucial for the nematicidal activity.展开更多
Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant,anti-tumor,anti-microbial and anti-inflammatory activities.It is believed that the mechanisms involved in the...Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant,anti-tumor,anti-microbial and anti-inflammatory activities.It is believed that the mechanisms involved in these bioactivities are due to the modulation of immune system.Recently,the pharmacological validation on immunomodulatory of pentacyclic triterpenes derived from higher plants is very limited and several existence review papers related for this group of compound have not been focused for this activity.In this review,we have highlighted several studies on immunomodulatory potential of botanical pentacyclic triterpenes isolated from wide array of different species of medicinal plants and herbs based on various preclinical in vitro and animal models.This review also attempts to discuss on bioactivities of compouns related with their structure-activity relationship.Hence,the evaluation of pentacyclic triterpenes offers a great opportunity to discover adjuvants and novel therapeutic agents that presented beneficial immunomodulatory properties.展开更多
The medicinal part of Aucklandia lappa(Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years ...The medicinal part of Aucklandia lappa(Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years in the following aspects of pharmacological activities,pharmacokinetics,toxicology,structure-activity relationship.Pharmacological activities consist of anti-cancer,anti-inflammatory activity,anti-immunity activity,anti-oxidant activity,antimicrobial activity,spasmolytic activity and so on.The extractive,showing similar pharmacokinetics parameters,may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacromolecules through Michael-addition.However,the poor aqueous solubility,non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class.In order to evaluate the potential effect of the extractive applied in clinical trial,the present review outlines information on pharmacological activities,pharmacokinetics,toxicology,and structure-activity relationship,as well as the future research directions of the extractive for further development and utilization of A.lappa.展开更多
C-glycosylflavonoids are characterized by a bond between the anomeric carbon of a sugar moiety and the C-6 or C-8 position of a flavonoid A ring.These compounds are widespread in nature and have become the subject of ...C-glycosylflavonoids are characterized by a bond between the anomeric carbon of a sugar moiety and the C-6 or C-8 position of a flavonoid A ring.These compounds are widespread in nature and have become the subject of increasing research interest due to their high biological potential.This review focuses on the biological effects of various C-glycosylflavonoids and their structure–activity relationships(SAR)as elucidated over the last 5 years.展开更多
A series of Sn‐incorporated SBA‐15materials with high specific surface areas and highly orderedmesoporous structures were synthesized by a facile one‐pot method and used as catalyst supports.A reference sample was ...A series of Sn‐incorporated SBA‐15materials with high specific surface areas and highly orderedmesoporous structures were synthesized by a facile one‐pot method and used as catalyst supports.A reference sample was also prepared using a conventional impregnation method.The catalystswere characterized using various methods,and their activities in propane dehydrogenation wereinvestigated.The incorporation of Sn into the SBA‐15matrix led to strong interactions between Snspecies and the support,and these helped to maintain the oxidation states of Sn species during thereaction.Substitution with Sn changed the interfacial properties of the Pt species and improved thefunction and effect of the Sn promoter.The catalytic activities and stabilities of the Pt catalysts supportedon Sn‐incorporated SBA‐15were better than those of the impregnated sample.However,thecatalytic performance deteriorated when an excessive amount of Sn was introduced and the interactionsamong Pt,Sn species,and the support became weaker.The Pt/0.5Sn‐SBA‐15catalyst gavethe best propene selectivity,i.e.,98.5%,with a corresponding propane conversion of about43.8%.展开更多
基金supported by National Council for Scientific and Technological Development (CNPq)Coordenao de Aperfeioamento de Pessoal de Nível Superior (CAPES)+1 种基金Oswaldo Cruz Foundation (Fiocruz)Department of Science and Technology,New Delhi,India [No.SR/WOS-A/LS-562/2011) dated 27/03/2012]
文摘Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biological applications, and have long been utilized as replacements to popular platinum based-drugs. Here, we report a novel series of ruthenium（ll） arene compounds bearing thiosemicarba- zone and isonicotinylhydrazone ligands with potent anticancer activity their structure activity relationships and apoptosis was studied. The cytotoxic activity of the new ruthenium（ll） arene compounds has been evaluated in several cell lines （Molt 4/C8, LI 210, CEM, HL60 and BEL7402）. Among them, ten complexes were found to be excellent in vitro growth inhibitory activity against various cell lines with IC50 in the sub-micromolar range.
基金the National Natural Science Foundation of China(No.32272575)National College Student Innovation and Entrepreneurship Training Program(No.202210459164)for financial support.
文摘Methicillin-resistant Staphylococcus aureus (MRSA), the most common pathogen in hospital and community environments, can cause serious and even fatal infections. The antibiotics currently used for clinical treatment of MRSA have developed resistance, and there is an urgent need to develop new antimicrobials to treat infections caused by MRSA strains. Quinoline analogues play an important role in the development of antimicrobials. Herein, we discussed the current development of antibacterial activities of quinoline analogues, mainly for anti-MRSA activity, and their structure-activity relationships (SARs) from the perspective of using the quinoline nucleus to search for novel potential anti-MRSA candidates. Additionally, the mechanisms of some representative quinoline analogues against MRSA were clarified. Altogether, this review could provide further insights for the rational development of quinoline-based antibacterial drugs, especially against MRSA.
基金financially supported by the National Natural Science Foundation of China(Nos.82104281,81922070,81973286,81801818 and 82273897)Shanghai Municipal Health Commission’s TCM research project(No.2022CX005)+1 种基金Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(No.ZYYCXTD-D-202004)Three-year Action Plan for Shanghai TCM Development and Inheritance Program[No.ZY(2021–2023)-0401]。
文摘Human Notum(hNotum)inhibitors could be used for treating Wnt signalling-associated diseases including colorectal cancer.Herein,two series of chalcone derivatives were designed and synthesized aiming to find selective and potent hNotum inhibitors.Structure–activity relationship(SAR)studies showed that 2-methoxyl and 5-bromine substitutions on A-ring significantly enhanced anti-hNotum effect,while 4’-ethoxyl and 3’-alkyl substitutions on B-ring were beneficial for hNotum inhibition.Among all tested chalcones,B11 displayed the most potent anti-Notum effect(IC_(50)=3.6 nmol/L),good selectivity,excellent chemical stability and suitable metabolic stability.Further investigations showed that B11 acted as a competitive inhibitor of hNotum,while this agent(5μmol/L)significantly weaken the migration abilities of colorectal cancer cells.Collectively,this study deciphers the SARs of chalcones as hNotum inhibitors and reports a novel and potent hNotum inhibitor with the anti-migration effect on colorectal cancer cells,which offers a promising lead compound to develop novel anti-cancer agents.
文摘The biological activity against Staphylococcus aureus, and Eschericia coil were investigated implementing three series, the first series was l-phenyl-2-（4＇-X-phenyl）-4-（2,4-dichlorophenyl）-1,3-butadiene, where X = H, CH3, OCH3, NH2, C1, F, NO2 and COOEt; the second was 3,4-dichlorochalcone series namely 3-（3,4-dichlorophenyl）-l-（4＇-X-phenyl）-2-propen-l-one, where X = H, CH3, OCH3, NH2, CI, F, NO2 and CN; and the third one was 2,4-dichlorochalcone series namely 3-（2,4-dichlorophenyl）-l- （4＇-X-phenyl）-2-propen-l-one, where X = H, CH3, OCH3, NH2, C1, F, NO2 and COOEt. MIC, MBC and the percentage of inhibition （activity） at 20 ~tg/mL, 15 μg/mL and 10μg/mL against Eschericia coli, and at 7.5 lag/mL, 5 μg/mL and 2.5 μg/mL against Staphylococcus aureus, were determined for each compound in the three series. Highest MIC activity against E. coli and S. aureus were given by 2,4-dichlorochalcone series. Butadiene series was similar in behavior to 2,4-dichlorochalcone series in MIC activity against S. aureus. Results of MBC revealed that compounds in the three series exerted high activity against both types of bacteria. Compounds substituted with nitro or nitril exhibited higher activity than other compounds in the three series. Percentage of inhibition of halogenated compounds （4＇-C1 and 4＇-F） was almost equal in every series. Compounds with substituents （4＇-H and 4＇-CH3） showed fluctuation in activity according to the nature of each series.
基金supported by the National Natural Science Foundation of China(U1905202,31972017,and 31771922)the National Key R&D Program of China(2018YFD0901006)+2 种基金the Fujian Major Project of Provincial Science&Technology Hall,China(2020NZ010008)the Open Project of the Key Laboratory of Refrigeration and Conditioning Aquatic Products Processing,Ministry of Agriculture and Rural Affairs,China(KLRCAPP2021-03)the Quanzhou Science&Technology Project,China(2019C085R)。
文摘Peptides are functional active fragments of proteins which can provide nutrients needed for human growth and development,and they also have unique physiological activity characteristics relative to proteins.Bioactive peptides contain a great deal of development potential.More specifically,food-derived bioactive peptides have the advantages of a wide variety of sources,unique structures,high efficiency and safety,so they have broad development prospects.This review provides an overview of the current advances regarding the preparation,functional characteristics,and structure–activity relationships of food-derived bioactive peptides.Moreover,the prospects for the future development and application of food-derived bioactive peptides are discussed.This review may provide a better understanding of foodderived bioactive peptides,and some constructive inspirations for further research and applications in the food industry.
基金financially supported by the National Natural Science Foundation of China(No.51074037)
文摘Effects of carboxylic acid collector, benzohydroxamic acid (BHA), sodium hexametaphosphate (SHAP), sodium silicate, and oxalic acid on scheelite flotation were studied through flotation tests, quantum chemical calculation, and flotation solution computational chemistry. In terms of the calculation results, the relationship between chemical reactions occurring on the scheelite surface and molecular structures of the reagents were analyzed. The results show that BHA and carboxylic acid collectors interact with scheelite in different forms and the recovery of scheelite using sodium oleate as collector declines successively from SHAP, sodium silicate, to oxalic acid. Moreover, it is found that the performance of depressant in scheelite flotation is directly related to the group electronegativity, indicating that the latter is a dominant factor that determines the former. These findings will be helpful to the academic research communities of scheelite flotation.
文摘A method for the analysis of the relationship between the helical structure and optical activity was proposed by the study of the conformations and X-ray diffraction structures of some cyclic esters prepared by esterification of L-(-)-2.3-O-methylidene threitol and L-(+)-2,3-O-isopropplidene threitol with alkanedioyl dichlorides and o-,m-,and p-phthaloyl dichlorides.
基金This research was supported by the National Natural Science Foundation of China （No. 81273537）, Scientific Research Fund of Education Department of Hunan Province （No. 17A190）, the Key Project of Science and Technology Department of Hunan Province （No. 2016DK2001）, and the Key Disciplines of Hunan Province and the Zhengxing Scholar Program of the University of South China.
文摘Firstly discovered in 1980s, human immunodeficiency virus （HIV） continues to affect more and more people. However, there is no effective drug available for the therapy of HIV infection. Betulinic acid existing in various medicinal herbs and fruits exhibits multiple biological effects, especially its outstanding anti-HIV activity, which has drawn the attentions of many pharmacists. Among the derivatives of betulinic acid, some compounds exhibited inhibitory activities at the nanomolar concentration, and have entered phase II clinical trials. This paper summarizes the current investigations on the anti-HIV activity of betulinic acid analogues, and provides valuable data for subsequent researches.
基金supported by the National Natural Science Foundation of China (No. 82074277 and 81773911)the Development Project of Shanghai Peak Disciplines-Integrated Medicine (No. 20180101)
文摘To utilize themultiple functions and give full play of ginsenosides,a variety of ginsenosides with different structures were prepared into liposomes and evaluated for their effect on the stability,pharmacokinetics and tumor targeting capability of liposomes.The results showed that the position and number of glycosyl groups of ginsenosides have significant effect on the in vitro and in vivo properties of their liposomes.The pharmacokinetics of ginsenosides liposomes indicated that the C-3 sugar group of ginsenosides is beneficial to their liposomes for longer circulation in vivo.The C-3 and C-6 glycosyls can enhance the uptake of their liposomes by 4T1 cells,and the glycosyls at C-3 position can enhance the tumor active targeting ability significantly,based on the specific binding capacity to Glut 1 expressed on the surface of 4T1 cells.According to the results in the study,ginsenoside Rg3 and ginsenoside Rh2 are potential for exploiting novel liposomes because of their cholesterol substitution,long blood circulation and tumor targeting capabilities.The results provide a theoretical basis for further development of ginsenoside based liposome delivery systems.
文摘New series of pyrazolo[1,5-α]pyrimidine derivatives 7a-i,11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines,namely colorectal carcinoma（HCT116）,prostate adenocarcinoma（PC-3） and liver carcinoma（HepG-2） using MTT cytotoxicity assay at 100 μg/mL.Some of the tested compounds displayed good anticancer activities against HCT-116 and PC-3 cells.Whereas,compounds 7d and 11 a showed better antitumor activity than the rest of the compounds against both cell lines.A structure-activity relationship（SAR） has been discussed and structures of the newly synthesized compounds were confirmed by different spectral data（MS,IR,^1H NMR and ^13C NMR） and elemental analysis.
基金the financial supports from the National Natural Science Foundation of China(No.20536010)National Key Project for Basic Research(No.2003CB114400)the Program of Shanghai Subject Chief Scientist and the Science and Technology Foundation of Shanghai
文摘In this review, we retrospect our progress in biological active naphthalimide and analogues as antitumor agents in the past 20 years. On one hand, various derivations in naphthalimide pharmacophores were developed to enhance their DNA binding affinity and antitumor property thereby. Heterocyclic fused naphthalimides, bis-naphthalimides, non-fused substituted naphthalimides and the carboxamide derivatives were synthesized. For example, thio-heterocyclic fused-naphthalimides were designed and evaluated in comparison with their oxo-heterocyclic fused analogues. Extended or created heterocyclebased skeleton were also developed as antitumor agents. On the other hand, we broaden the design strategy of naphthalimide antitumor agents besides DNA intercalation and topo II poison. We have introduced more drug design methods, such as prodrugs, multitarget drugs, computer-aided drug design,photodynamic therapy. For example, we have got naphthalimide derivatives which inhibited topo II and induced LMP by introducing long alkyl chain and polyamines. Several representative compounds were clarified of their antitumor mechanism of action. In all, our research improves the structure diversity of naphthalimide antitumor agents and distinct variances of antitumor targets and mechanism of action.
文摘A series of trihydrocarbyltin chlorides containing silicon was synthesized. The acaricidal activity was determined and the structure activity relationship was tried to be found out with the hydrophobic parameter.
基金supported financially by the National Key Research and Development Program of China(No.2022YFA1504900)the NSFC of China(No.22072041,21832002)the Science and Technology Commission of Shanghai Municipality(10dz2220500).
文摘Demethoxylation was kinetically and spectroscopically studied over three catalysts with different Ru^(0)/Ru^(δ+) ratios.In-situ spectroscopic tests demonstrated that the synergy between Ru^(0)and Ru^(δ+) was crucial,and Ru^(0) was in charge of H_(2) activation and adsorption of aromatic ring while Ru^(δ+) adsorbed with O in methoxyl.A Langmuir-Hinshelwood kinetic model was proposed,and ratio of Ru^(0)/Ru^(δ+) was the key in deciding the rate-determining step(RDS):i)desorp-tion of toluene was RDS over catalyst with highRu^(0)ratio;ii)dissociation of H_(2) was RDS over Ru^(δ+) enriched catalyst;iii)demethoxylation was rate-determined by CO water-gas shift (WGS) when Ru^(0)/Ru^(δ+) approached~1.The best perfor-mance was obtained over Ru/NiAl_(2)O_(4)-200,which effectively enabled both C-O bond activation and rapid recovery of adsorption sites for aromatic rings.Finally,in-situ DRIFT studies on methoxy decomposition and CO-WGS unraveled that the electronic composition of Ru was more stable in Ru/NiAl_(2)O_(4)-200 which contributes to its excellence.
基金financially sponsored by the National Natural Science Foundation of China(Grant Nos.22075223,22179104)the State Key Laboratory of Advanced Technology for Materials Synthesis and Processing(Wuhan University of Technology)(2022-ZD-4)。
文摘Precisely tuning the spacing of the active centers on the atomic scale is of great significance to improve the catalytic activity and deepen the understanding of the catalytic mechanism,but still remains a challenge.Here,we develop a strategy to dilute catalytically active metal interatomic spacing(d_(M-M))with light atoms and discover the unusual adsorption patterns.For example,by elevating the content of boron as interstitial atoms,the atomic spacing of osmium(d_(Os-Os))gradually increases from 2.73 to 2.96?.More importantly,we find that,with the increase in dOs-Os,the hydrogen adsorption-distance relationship is reversed via downshifting d-band states,which breaks the traditional cognition,thereby optimizing the H adsorption and H_2O dissociation on the electrode surface during the catalytic process;this finally leads to a nearly linear increase in hydrogen evolution reaction activity.Namely,the maximum dOs-Os of 2.96?presents the optimal HER activity(8 mV@10 mA cm^(-2))in alkaline media as well as suppressed O adsorption and thus promoted stability.It is believed that this novel atomic-level distance modulation strategy of catalytic sites and the reversed hydrogen adsorption-distance relationship can shew new insights for optimal design of highly efficient catalysts.
基金the National Natural Science Foundation of China(Nos.31070386,21302195 and 31300290)135 Key Cultivation Program of the Chinese Academy of Sciencesthe Province-Academy Cooperation Program of Henan Province of China(No.102106000021)for financial support
文摘The presence of hydroxyl groups at the C4 and C7 positions in coumarin backbone has been proposed as a potential modification site for providing excellent bioactivity according to previous studies. A series of novel coumarin derivatives were rationally designed and synthesized by use of a complex catalytic system for a targeted modification at the above sites. These derivatives were assayed for nematicidal activity. As predicted, the derivatization enhanced the activity of the coumarins against five nematodes.Compounds 7b, 9a, 10 c and 11 c showed significant strong nematicidal broad spectrum activity against all tested nematodes. Compound 10 c was the most effective with the lowest LC50 values against Meloidogyne incognita（5.1 mmol/L）, Ditylenchus destructor（3.7 mmol/L）, Bursaphelenchus mucronatus（6.4 mmol/L）, Bursaphelenchus B. xylophilus（2.5 mmol/L） and Aphelenchoides besseyi（3.1 mmol/L）,respectively. A brief investigation on the structure–activity relationships（SAR） revealed that the targeted modification by a C7 hydroxyl was optimum compared with that of a C4 hydroxyl and that the coupling chain length was crucial for the nematicidal activity.
文摘Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant,anti-tumor,anti-microbial and anti-inflammatory activities.It is believed that the mechanisms involved in these bioactivities are due to the modulation of immune system.Recently,the pharmacological validation on immunomodulatory of pentacyclic triterpenes derived from higher plants is very limited and several existence review papers related for this group of compound have not been focused for this activity.In this review,we have highlighted several studies on immunomodulatory potential of botanical pentacyclic triterpenes isolated from wide array of different species of medicinal plants and herbs based on various preclinical in vitro and animal models.This review also attempts to discuss on bioactivities of compouns related with their structure-activity relationship.Hence,the evaluation of pentacyclic triterpenes offers a great opportunity to discover adjuvants and novel therapeutic agents that presented beneficial immunomodulatory properties.
基金supported by Special Financial Grant from the China Postdoctoral Science Foundation (No.2015T81140)National Natural Science Foundation of China Youth Fund Project (No.81503467)。
文摘The medicinal part of Aucklandia lappa(Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years in the following aspects of pharmacological activities,pharmacokinetics,toxicology,structure-activity relationship.Pharmacological activities consist of anti-cancer,anti-inflammatory activity,anti-immunity activity,anti-oxidant activity,antimicrobial activity,spasmolytic activity and so on.The extractive,showing similar pharmacokinetics parameters,may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacromolecules through Michael-addition.However,the poor aqueous solubility,non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class.In order to evaluate the potential effect of the extractive applied in clinical trial,the present review outlines information on pharmacological activities,pharmacokinetics,toxicology,and structure-activity relationship,as well as the future research directions of the extractive for further development and utilization of A.lappa.
文摘C-glycosylflavonoids are characterized by a bond between the anomeric carbon of a sugar moiety and the C-6 or C-8 position of a flavonoid A ring.These compounds are widespread in nature and have become the subject of increasing research interest due to their high biological potential.This review focuses on the biological effects of various C-glycosylflavonoids and their structure–activity relationships(SAR)as elucidated over the last 5 years.
基金supported by the Science & Technology Support Plan Projects of Sichuan Province (2016GZ0371)National Natural Science Foun-dation of China (NNSFC,21476145,21506111)~~
文摘A series of Sn‐incorporated SBA‐15materials with high specific surface areas and highly orderedmesoporous structures were synthesized by a facile one‐pot method and used as catalyst supports.A reference sample was also prepared using a conventional impregnation method.The catalystswere characterized using various methods,and their activities in propane dehydrogenation wereinvestigated.The incorporation of Sn into the SBA‐15matrix led to strong interactions between Snspecies and the support,and these helped to maintain the oxidation states of Sn species during thereaction.Substitution with Sn changed the interfacial properties of the Pt species and improved thefunction and effect of the Sn promoter.The catalytic activities and stabilities of the Pt catalysts supportedon Sn‐incorporated SBA‐15were better than those of the impregnated sample.However,thecatalytic performance deteriorated when an excessive amount of Sn was introduced and the interactionsamong Pt,Sn species,and the support became weaker.The Pt/0.5Sn‐SBA‐15catalyst gavethe best propene selectivity,i.e.,98.5%,with a corresponding propane conversion of about43.8%.
