Respiratory syncytial virus(RSV)is a ubiquitous respiratory virus that affects individuals of all ages;however,there is a notable lack of targeted treatments.RSV infection is associated with a range of respiratory sym...Respiratory syncytial virus(RSV)is a ubiquitous respiratory virus that affects individuals of all ages;however,there is a notable lack of targeted treatments.RSV infection is associated with a range of respiratory symptoms,including bronchiolitis and pneumonia.Baicalin(BA)exhibits significant therapeutic effects against RSV infection through mechanisms of viral inhibition and anti-inflammatory action.Nonetheless,the clinical application of BA is constrained by its low solubility and bioavailability.In this study,we prepared BA nanodrugs(BA NDs)with enhanced water solubility utilizing the supramolecular self-assembled strategy,and we further conducted a comparative analysis of this pharmacological activity between free drugs and NDs of BA.Both in vitro and in vivo results demonstrated that BA NDs significantly enhanced the dual effects of viral inhibition and inflammation relief compared to free BA,attributed to prolonged lung retention,improved cellular uptake,and increased targeting affinity.Our study confirms that the nanosizing strategy,a straightforward approach to enhance drug solubility,can also increase biological activity compared to free drugs with the same content,thereby providing a potential ND for RSV treatment.This correlation analysis between the existing forms of drugs and their biological activity offers a novel perspective for research on the active ingredients of traditional Chinese medicine.展开更多
Recombinant human growth hormone(rhGH)has been widely used for the treatment of disorders associated with GH deficiency and multiple clinical indications[1].Accurate determination of biological activity is essential i...Recombinant human growth hormone(rhGH)has been widely used for the treatment of disorders associated with GH deficiency and multiple clinical indications[1].Accurate determination of biological activity is essential in the development,registration,and quality control of rhGH pharmaceutical products[2].However,the existing in vivo bioassay procedure based on somatropin-induced weight gain in rats is complicated,and the use of a rat cell line-based approach(Nb2-11 bioassay),which measures the production of adenosine triphosphate(ATP)as a direct indicator of cell growth,has a low mechanism of action(MOA)relevance.Therefore,novel rhGH bioassays are still needed.To this end,we developed a reporter gene assay(RGA)based on the GH/insulin-like growth factor-1(IGF-1)axis.展开更多
Polycyclic polyprenylated acylphloroglucinols(PPAPs)represent a distinct subclass of specialized metabolites predominantly found in the plant kingdom,particularly within the Guttiferae(Clusiaceae)family.These compound...Polycyclic polyprenylated acylphloroglucinols(PPAPs)represent a distinct subclass of specialized metabolites predominantly found in the plant kingdom,particularly within the Guttiferae(Clusiaceae)family.These compounds exhibit remarkable structural diversity and a wide range of biological activities.Seco-and nor-PPAPs,two unique variants of PPAPs with diverse skeletal structures,have been extensively investigated.As of June 2023,200 compounds have been isolated from four genera,with Hypericum being the primary source.Notably,115 of these compounds were identified in the past four years,indicating a significant increase in research activity.Seco-and nor-PPAPs can be categorized into six main subgroups based on the original PPAP scaffolds.Biological studies have revealed their potential in various therapeutic applications,including anti-cancer,anti-inflammatory,hepatoprotective,anti-Alzheimer’s disease(anti-AD),multidrug resistance(MDR)reversal,anti-depressant,neuroprotective,and immunosuppressive effects.This review provides a comprehensive overview of the occurrence,structures,and bioactivities of natural seco-and nor-PPAPs,offering valuable insights for the further development of PPAPs.展开更多
Rutin,also known as vitamin P,belongs to the flavonoid class of compounds and is widely present in plants.Its ability to bind with albumin in the blood helps maintain capillary permeability,leading to its extensive us...Rutin,also known as vitamin P,belongs to the flavonoid class of compounds and is widely present in plants.Its ability to bind with albumin in the blood helps maintain capillary permeability,leading to its extensive use for cardiovascular protection.This review aimed to provide insights into the development of rutin raw material industry in China and its future applications in various fields,such as medicine,healthcare,food,and animal husbandry.The study began by comparing rutin quality standards across China,the United States and Europe,outlined the industrial extraction processes of rutin,and examined the biological activity and potential medical applications of rutin.展开更多
[Objective] This study aims to screen for the high effective fungicides which could significantly decrease the disease incidence and disease index of rice false smut. [Method] The inhibitory activities of the fungicid...[Objective] This study aims to screen for the high effective fungicides which could significantly decrease the disease incidence and disease index of rice false smut. [Method] The inhibitory activities of the fungicide against mycelial growth of Ustilaginoidea virens were measured to in vitro evaluate the ECho values. And 17 fungicides were sprayed to evaluate the efficacy and effect of the fungicides tested in the field trials on the rice characters, [Result] The results showed that epoxicona- zole, difenoconazole, propiconazole and procloraz exhibited high inhibitory activity against mycelial growth of Ustilaginoidea virens with the ECso values 0.04, 0.07, 0.12 and 0.11 pg/ml, respectively. The results of field trials showed that the efficacy of Wen- quning, and fungicides such as difenoconazole, prochloraz, propiconazole, epoxi- conazole and their mixtures in controlling rice false smut were all 70% or more. [Conclusion] The 17 tested fungicides behaved efficacy in controlling rice false smut and did not cause drug injury on leaves and grains of rice plants, sprayed when flag leaves of rice fully expanded.展开更多
A new compound with biological activity had been synthesized by the reaction between 5-（p-chlorophenyl）-2-amino-1,3,4-thiodiazol and aroyl isocyanates.The structure of the target compound was confirmed by IR,UV,1HNM...A new compound with biological activity had been synthesized by the reaction between 5-（p-chlorophenyl）-2-amino-1,3,4-thiodiazol and aroyl isocyanates.The structure of the target compound was confirmed by IR,UV,1HNMR spectrum and elemental analysis.The biological activity tests showed that the target compound had an activity as plant growth regulator,the auxin activity was 26.1% and the cytokinin activity was 41.1%.展开更多
Micro-arc oxidized Cu-incorporated TiO2 coatings （Cu-TiO2） were prepared in the Ca, P, Cu-containing electrolyte to obtain an implant material with superior biological activity and antibacterial property. The surfac...Micro-arc oxidized Cu-incorporated TiO2 coatings （Cu-TiO2） were prepared in the Ca, P, Cu-containing electrolyte to obtain an implant material with superior biological activity and antibacterial property. The surface topography, phase, and element composition of the TiO2 and Cu-TiO2 coatings were characterized by scanning electron microscopy （SEM）, X-ray diffraction （XRD）, and energy-dispersive X-ray spectrometry （EDS）, respectively. Staphylococcus aureus （S. aureus） was selected to evaluate the antibacterial property of the Cu-TiO2 coatings, whereas osteoblastic MG63 cells were cultured on the coatings to investigate the biological activity. The obtained results demonstrated that Cu element was successfully incorporated into the porous nano-structured TiO2 coatings, which did not alter apparently the surface topography and phase composition of the coatings as compared to the Cu-free TiO2 coatings. Moreover, the antibacterial studies suggested that the Cu-incorporated TiO2 coatings could significantly inhibit the adhesion of S. aureus. In addition, the in vitro biological evaluation displayed that the adhesion, proliferation and differentiation of MG63 cells on the Cu-incorporated coatings were enhanced as compared to those on the Cu-free coatings and Ti plates. In conclusion, the innovative Cu-incorporated nano-structured TiO2 coatings on Ti substrate with excellent antibacterial property and biological activity are promising candidates for orthopedic implant.展开更多
BACKGROUND: The proliferation and metastasis of cancers depend on angiogenesis. This property provides the feasibility for the treatment of cancer by inhibition of angiogenesis, and many angiogenic inhibitors have bee...BACKGROUND: The proliferation and metastasis of cancers depend on angiogenesis. This property provides the feasibility for the treatment of cancer by inhibition of angiogenesis, and many angiogenic inhibitors have been demonstrated to effectively inhibit angiogenesis and consequently the growth of solid cancer. As for the newly identified angiogenesis inhibitor, arresten, some studies have found its high activity on restrainting tumor vessel. This study was to assess the anti-angiogenic activity of arresten. METHODS: The arresten gene was obtained from a healthy puerpera's placenta tissue by the reverse transcriptase-polymerase chain reaction (RT-PCR) method, and molecular cloning to prokaryotic expression plasmid pBV220 by recombination strategy. The prokaryotic expression plasmid pBV220/arr was identified by restriction enzyme digestion and sequenced. The pBV220/arr was transformed into E. coli JM109, DH5α, BL21 and BL21 (DE3) by the CaCl_2 transformation method. The arresten expression level was detected by SDS-PAGE. The expressed product was purlfled, re-naturalized and detected for its biological activity of inhibiting the angiogenesis of chorioallantoic membrane (CAM). RESULTS: The arresten gene was cloned and pBV220/arr was constructed. The arresten expression level of protein was highly increased after pBV220/arr was transformed into E. coli BL21 (DE3). SDS-PAGE showed that the expressed arresten proteins were mainly inclusion bodies and had a molecular weight of 26 kDa. The expressed arresten protein showed evident biological activities. CONCLUSIONS: The successful construction of recombinant plasmid pBV220/arr and the effective expression in E. coil have laid a foundation for further study of its anti-angiogenic function and may pave the way for future antitumor application.展开更多
Dimethomorph is a fungicide with high activity against Peronosporomycetes plant pathogens. The present study showed that dimethomorph is effective on controlling the oomycete fungal pathogen Pseudoperonospora cubensis...Dimethomorph is a fungicide with high activity against Peronosporomycetes plant pathogens. The present study showed that dimethomorph is effective on controlling the oomycete fungal pathogen Pseudoperonospora cubensis causing downy mildew on cucumber. The fungicide did not affect zoospores discharge from sporangia of P. cubensis, but it strongly inhibited mycelial growth and sporangial production in vitro and increased lysis of zoospores. Dose of 2 mg L^-1 of dimethomorph was sufficient to inhibit mycelial growth and sporangial production of P. cubensis on leaf disks, 5 mg L^-1 was enough to lyse zoospores of P. cubensis, and 25 mg L^-1 was required to inhibit sporangial production on detached leaves. In whole plant tests, dimethomorph exhibited strong protective and curative activity. Dimethomorph when applied at a dose of 300 mg L^-1 for 1, 3, 5, 7 days before inoculation exhibited 100% efficacy on disease control. On the other hand, efficacies of 67.1 and 31.5% were obtained when the same dose of dimethomorph was applied for 1 and 3 days after inoculation, respectively. So dimethomorph had persistence effect on leaves for 7 days at least and exhibited strong protective and curative activity. Bioassay analyses showed that dimethomorph could be translocated in the xylem system, redistributed in the leaf, and penetrated from the upper surface to the lower surface of the leaf but could not be translocated in phloem system or transferred from the roots to leaves of cucumber plants in sufficient amounts for disease control. The biocharacteristics of dimethomorph make it well suitable for integration of a control programme against downy mildew disease on cucumber and as a component to delay other peronosporomycetes fungicide-resistance development.展开更多
The title compound N-（2,6-difluorobenzoyl）-N＇-[5-（4-trifluoromethylphenyl）-1,3,4-thiadiazol-2-yl]urea（C17H9F5N4O2S,Mr = 428.34） has been synthesized by the reaction of 2-amino-5-（4-trifluoromethylphenyl）-1,3,...The title compound N-（2,6-difluorobenzoyl）-N＇-[5-（4-trifluoromethylphenyl）-1,3,4-thiadiazol-2-yl]urea（C17H9F5N4O2S,Mr = 428.34） has been synthesized by the reaction of 2-amino-5-（4-trifluoromethylphenyl）-1,3,4-thiadiazole with 2,6-difluorobenzoyl isocyanate,and its crystal structure was determined by single-crystal X-ray diffraction.The crystal belongs to monoclinic,space group P21/n with a = 10.7316（13）,b = 10.5617（13）,c = 16.037（2） ,β = 106.408（2）°,V = 1743.6（4） 3,Z = 4,Dc = 1.632 g/cm3,μ = 0.260 mm-1,F（000） = 864,the final R = 0.0599 and wR = 0.1420 for 3467 observed reflections with I〉 2σ（I）.The urea group,which adopts a planar configuration mediated by the intramolecular N-H...O hydrogen bond,is nearly coplanar with the thiadiazole and 4-trifluoromethylbenzene rings.The title compound was found to exhibit good fungicidal activity against Rhizoctonia solani and Botrytis cinerea.展开更多
A novel compound, (HGly) 4[HPMo 12 O 40 ] 2·22H 2O, was synthesized and characterized by means of elemental analysis, IR and X ray diffraction. The compound crystallized in a monoclinic space group ...A novel compound, (HGly) 4[HPMo 12 O 40 ] 2·22H 2O, was synthesized and characterized by means of elemental analysis, IR and X ray diffraction. The compound crystallized in a monoclinic space group Cc with a =4 0060(0 8) nm, b =1 2527(0 3) nm, c =1 9930(0 4) nm, β =96 36(3)°, V =9 940(3) nm 3, Z =2, R 1=0 0576, wR 2 =0 1746. The anti tumor activity of this compound was tested in two human tumor cell lines in vitro .展开更多
To express recombinant arresten in Escherichia coli (E.Coli) and investigate its biological activity, prokaryotic expression vector of human arresten gene was constructed by gene engineering. Human arresten gene was a...To express recombinant arresten in Escherichia coli (E.Coli) and investigate its biological activity, prokaryotic expression vector of human arresten gene was constructed by gene engineering. Human arresten gene was amplified from recombinant plasmid pGEMArr by polymerase chain reaction (PCR), and inserted into prokaryotic expression vector pRSET containing T7 promoter. Restriction analysis and DNA sequencing verified that the arresten gene was correctly cloned into the expression vector. The recombinant plasmid pRSETAt was subsequently transformed into E.coli BL21 (DE3), and the target gene was expressed under induction of IPTG. SDS-PAGE analysis revealed that the recombinant protein with a molecular weight of 29 kD (1 kD=0.992 1 ku) amounted to 29 % of the total bacterial proteins. After purification and renaturation, the recombinant protein could significantly suppress the proliferation of human umbilical vein endothelial cells (HUVECs). These results suggested that the expression of a biologically active form of human arresten in the pRSET expression system laid a foundation for further study on the mechanistic insight into arresten action on angiogenesis and the development of powerful anti-cancer drugs.展开更多
The novel title compound 4-chlorobenzaldehyde （2-trifluoromethyl-5,6,7,8- tetrahydro- benzo[4,5]thieno[2,3-d]pyrimidin-4-yl）hydrazone monohydrate （C18H14C1F3N4S.H20, Mr = 428.86） has been synthesized by a condensa...The novel title compound 4-chlorobenzaldehyde （2-trifluoromethyl-5,6,7,8- tetrahydro- benzo[4,5]thieno[2,3-d]pyrimidin-4-yl）hydrazone monohydrate （C18H14C1F3N4S.H20, Mr = 428.86） has been synthesized by a condensation reaction of 4-chlorobenzaldehyde with （2-trifuoromethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl）hydrazine, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to monoclinic, space group P21/c with a = 7.4252（7）, b = 26.344（2）, c = 10.3095（9） A, /3 = 109.407（2）~, V= 1902.0（3） A3, Z = 4, Dc = 1.498 g/cm^3, p = 0.356 mm-1, F（000） = 880, the final R = 0.0564 and wR = 0.1681 for 2343 observed reflections with I 〉 2o（/）. X-ray diffraction analysis reveals that the title hydrazone molecule is nearly planar except for the cyclohexene and trifluoromethyl moieties. In the crystal packing, the molecules form stacks by a three-dimensional framework, which results from intermolecular N（3）-H（3）...O（1）, O（1）-H（1B）...N（2）, O（1）- H（1B）...N（4） and O（1）-H（1A）...F（1） hydrogen bonds via water molecules together with π-π stacking interactions. Molecular geometry of the title compound in the ground state optimized by B3LYP functional with 6-311G＊＊ basis sets indicates that the calculations are in agreement with the experimental data. The preliminary bioassay suggested that the title compound exhibits relatively good fungicidal activity against Fusarium oxysporium fsp.vasinfectum and Dothiorella gregaria.展开更多
The title compound 2-（1-（3-bromo-1-（3-chloropyridin-2-yl）-1H-pyrazole-5-carbonyl）piperidin-4-yl）-N-isopropylthiazole-4-carboxamide（C21H22Br Cl N6O2 S,Mr = 536.04） has been synthesized,and its structure was cha...The title compound 2-（1-（3-bromo-1-（3-chloropyridin-2-yl）-1H-pyrazole-5-carbonyl）piperidin-4-yl）-N-isopropylthiazole-4-carboxamide（C21H22Br Cl N6O2 S,Mr = 536.04） has been synthesized,and its structure was characterized by IR spectra,1H-NMR,13C-NMR,EA,and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic system,space group P/c with a = 15.146（3）,b = 11.573（2）,c = 26.937（5） A,β = 103.64（3）°,V = 1839.0（6） A^3,Z = 4,Dc = 1.557 g/cm^3,μ（Mo Ka） = 0.71073 mm^-1,F（000） = 2192,R = 0.0601 and w R = 0.1392.There exist one intramolecular hydrogen bond at N–H···N and four intermolecular weak interactions at O（2）···H（1）,Cl（1）···H（12）,O（1）···Cl（1） and S（1）···O（2）.Bioassay results indicated that the title compound had good fungicidal and antiviral activities against tobacco mosaic virus.展开更多
Five new solid complexes were synthesized about transition metals with Schiff base（ L, C18H23NO2 ） derived from adamantaneamine and o-vanillin, and characterized by elemental analysis, molar conductance, infrared sp...Five new solid complexes were synthesized about transition metals with Schiff base（ L, C18H23NO2 ） derived from adamantaneamine and o-vanillin, and characterized by elemental analysis, molar conductance, infrared spectra, UV-vis spectra, thermal analysis. Their chemical formula are [ML2]（ClO4）2 （ M= Mn, Co, Ni, Cu, Zn）, and the coordination numbers are four, The antibacterial activity of Schiff base ligand and its complexes was studied.展开更多
Schiff base metal complexes are of great importance in pharmaceutical science owing to their unique chemical properties, which enable them to exhibit diverse biological activities such as anti-bacterial,anti-oxidant, ...Schiff base metal complexes are of great importance in pharmaceutical science owing to their unique chemical properties, which enable them to exhibit diverse biological activities such as anti-bacterial,anti-oxidant, anti-inflammatory, and anti-tumor properties. Furthermore, Schiff base metal complexes can serve as reagents and catalysts in chemical reactions. This review aims to provide an overview of our recently published studies on Cu(Ⅱ) and Pd(Ⅱ) complexes derived from proline Schiff base ligands. We also discuss the potential applications of these metal complexes in the fields of antibacterial and chiral resolution.展开更多
The title compound N-cyanosulfoximine derivative containing 1,2,3-thiadiazole （C6HsN4OS2, Mr = 216.28） has been synthesized using 4-（chloromethyl）-5-methyl-1,2,3-thiadiazole as the starting material, and its struc...The title compound N-cyanosulfoximine derivative containing 1,2,3-thiadiazole （C6HsN4OS2, Mr = 216.28） has been synthesized using 4-（chloromethyl）-5-methyl-1,2,3-thiadiazole as the starting material, and its structure was characterized by IR, 1H NMR, HRMS, elemental analysis and single-crystal X-ray diffraction. The crystal of the title compound belongs to orthorhombic, space group Pna21 with a = 14.730（6）, b = 5.478（2）, c = 22.619（9） A, Z = 8, V = 1825.0（13） A3, Dc = 1.574 g/cm3,/a = 0.547 mm-1, F（000） = 896, R = 0.0767 and wR （I〉 2o（/）） = 0.2064. X-ray analysis indicates that in this crystal double enantiomers are found as the basically asymmetrical unit and interactions between S（1）...N（3）, S（3）...N（4） and S（3）...N（7） are observed. This kind of interactions extends the molecules into a one-dimensional double chain. The preliminary biological test showed that the title compound had insecticidal activity against Myzus persicae in a certain degree and also presented moderate potential bioactivity against tobacco mosaic virus （TMV）.展开更多
The title compound diethyl 2-（3,4-dichloroisothiazol-5-yl）-4-（trifluoromethyl）-4,5- dihydrothiazol-4-yl-3-methylbenzoate （C15H9C12F3N202S2, Mr = 441.26） was prepared from methyl 3,4-dichloroisothiazole-5-carboxy...The title compound diethyl 2-（3,4-dichloroisothiazol-5-yl）-4-（trifluoromethyl）-4,5- dihydrothiazol-4-yl-3-methylbenzoate （C15H9C12F3N202S2, Mr = 441.26） was prepared from methyl 3,4-dichloroisothiazole-5-carboxylate as the starting material by four steps of reaction. Its structure was characterized by IR, 1H-NMR, 13C-NMR, EA and single-crystal X-ray diffraction. The crystal of the title compound belongs to the monoclinic system, space group P2dc with a = 8.8437（18）, b = 16.128（3）, c = 12.305（3） A, β = 91.68（3）°, V= 1754.4（6） A3, Z = 4, Dc = 1.671 g/cm3,μ（MoKa） = 0,71073 mm^-1, F（000） = 888, R = 0.0384 and wR = 0.0778. Weak π-π interactions occur between the isothiazole rings and phenyl rings of adjacent molecules to form a one-dimensional chain and stabilize the crystal structure. Bioassay indicates that the title compound has good activity against the fungi and TMV tested.展开更多
A novel compound,2-（anthracen-9-yl）-5-p-tolyl-1,3,4-oxadiazole（C23H16N2O）,has been synthesized by the condensation of 4-methylbenzohydrazide and anthracene-9-carbaldehyde in an ethanol solution with chloramine-T.T...A novel compound,2-（anthracen-9-yl）-5-p-tolyl-1,3,4-oxadiazole（C23H16N2O）,has been synthesized by the condensation of 4-methylbenzohydrazide and anthracene-9-carbaldehyde in an ethanol solution with chloramine-T.The compound was characterized by 1H-NMR,13C-NMR,MS and single-crystal X-ray diffraction.The crystal belongs to the triclinic system,space group P with a = 7.7817（4）,b = 8.8544（5）,c = 12.4726（8） ,β = 92.8520（10）°,Z = 2,V = 826.58（8） 3,Dc = 1.352 g/cm3,Mr = 336.38,λ（MoKα） = 0.71073 ,μ = 0.084 mm-1,F（000） = 352,R = 0.0381 and wR = 0.1099.The dihedral angle between anthracene skeleton and phenyl ring is 64.19°.A total of 6354 unique reflections were collected,of which 3172 with I 〉 2σ（I） were observed.X-ray analysis indicated an offset face-to-face π-π stacking interaction between anthracene skeletons and an offset face-to-face π-π stacking interaction between phenyl ring planes.The novel compound molecules are connected through the offset face-to-face π-π stacking interactions to generate a three-dimensional network.The preliminary bioassay results showed that the novel compound exhibited significant insect growth inhibitory activity against Spodoptera litura Fabricius larvae.展开更多
The title compound diethyl 1,4-dihydro-2,6-dimethyl-4-（4-methyl-1,2,3-thiadiazol- 5-yl） pyridine-3,5-dicarboxylate （C16H21N3O4S, Mr = 351.42） was prepared by the Hantszch reaction with 4-methyl-1,2,3-thiadiazole-5...The title compound diethyl 1,4-dihydro-2,6-dimethyl-4-（4-methyl-1,2,3-thiadiazol- 5-yl） pyridine-3,5-dicarboxylate （C16H21N3O4S, Mr = 351.42） was prepared by the Hantszch reaction with 4-methyl-1,2,3-thiadiazole-5-formaldehyde, ethyl acetoacetate and ammonium acetate in the presence of aluminum chloride in alcohol, and its structure was characterized by IR spectra, 1H-NMR, EA, and single-crystal X-ray diffraction. The crystal of the title compound belongs to monoclinic system, space group P21/n with α= 11.300（2）, b = 12.771（3）, c = 12.826（3） ？, β = 96.55（3）o, V = 1839.0（6） ？3, Z = 4, Dc = 1.296 g/cm3, μ（MoKa） = 0.71073 mm-1, F（000） = 744, R = 0.0981 and wR = 0.1994. X-ray diffraction result shows that the torsion angles of N（1）–C（2）– C（3）–C（4） and C（2）–C（3）–C（4）–C（8） are 178.9（3）° and –130.3（3）°, respectively. All rings in the title compound are non-planar. The bioassay results indicate that the title compound has good fungicidal activity, good antivirus activity against tobacco mosaic virus and certain extent of insecticidal activity against Mythimna separata.展开更多
基金supported by the National Natural Science Foundation of China(Grant No.:82474195)the Postgraduate Research&Practice Innovation Program of Jiangsu Province,China(Grant No.:021093002882)+2 种基金the Youth Medical Innovation Research Project of China(Grant No.:P24021887623)Taizhou Science and Technology Support Project,China(Grant No.:TS202420)grants from Nanjing Medical University,China(Grant Nos.:TZKY20230104 and 2024KF0292).
文摘Respiratory syncytial virus(RSV)is a ubiquitous respiratory virus that affects individuals of all ages;however,there is a notable lack of targeted treatments.RSV infection is associated with a range of respiratory symptoms,including bronchiolitis and pneumonia.Baicalin(BA)exhibits significant therapeutic effects against RSV infection through mechanisms of viral inhibition and anti-inflammatory action.Nonetheless,the clinical application of BA is constrained by its low solubility and bioavailability.In this study,we prepared BA nanodrugs(BA NDs)with enhanced water solubility utilizing the supramolecular self-assembled strategy,and we further conducted a comparative analysis of this pharmacological activity between free drugs and NDs of BA.Both in vitro and in vivo results demonstrated that BA NDs significantly enhanced the dual effects of viral inhibition and inflammation relief compared to free BA,attributed to prolonged lung retention,improved cellular uptake,and increased targeting affinity.Our study confirms that the nanosizing strategy,a straightforward approach to enhance drug solubility,can also increase biological activity compared to free drugs with the same content,thereby providing a potential ND for RSV treatment.This correlation analysis between the existing forms of drugs and their biological activity offers a novel perspective for research on the active ingredients of traditional Chinese medicine.
基金supported by the first batch of grants from the State Key Laboratory of Drug Regulatory Science,China(Grant No.:2023SKLDRS0108).
文摘Recombinant human growth hormone(rhGH)has been widely used for the treatment of disorders associated with GH deficiency and multiple clinical indications[1].Accurate determination of biological activity is essential in the development,registration,and quality control of rhGH pharmaceutical products[2].However,the existing in vivo bioassay procedure based on somatropin-induced weight gain in rats is complicated,and the use of a rat cell line-based approach(Nb2-11 bioassay),which measures the production of adenosine triphosphate(ATP)as a direct indicator of cell growth,has a low mechanism of action(MOA)relevance.Therefore,novel rhGH bioassays are still needed.To this end,we developed a reporter gene assay(RGA)based on the GH/insulin-like growth factor-1(IGF-1)axis.
基金supported by the National Natural Science Foundation for Distinguished Young Scholars(No.81725021)the National Natural Science Foundation of China(Nos.82003633,32100321,and 32300335)+1 种基金the National Natural Science Foundation of Hubei Province(Nos.2023AFB791 and 2023AFB530)the Knowledge Innovation Project of Wuhan Science and Technology Bureau(No.2023020201020534).
文摘Polycyclic polyprenylated acylphloroglucinols(PPAPs)represent a distinct subclass of specialized metabolites predominantly found in the plant kingdom,particularly within the Guttiferae(Clusiaceae)family.These compounds exhibit remarkable structural diversity and a wide range of biological activities.Seco-and nor-PPAPs,two unique variants of PPAPs with diverse skeletal structures,have been extensively investigated.As of June 2023,200 compounds have been isolated from four genera,with Hypericum being the primary source.Notably,115 of these compounds were identified in the past four years,indicating a significant increase in research activity.Seco-and nor-PPAPs can be categorized into six main subgroups based on the original PPAP scaffolds.Biological studies have revealed their potential in various therapeutic applications,including anti-cancer,anti-inflammatory,hepatoprotective,anti-Alzheimer’s disease(anti-AD),multidrug resistance(MDR)reversal,anti-depressant,neuroprotective,and immunosuppressive effects.This review provides a comprehensive overview of the occurrence,structures,and bioactivities of natural seco-and nor-PPAPs,offering valuable insights for the further development of PPAPs.
基金Supported by the Scientific and Technological Research Project Foundation of Henan Provincial Scientific and Technological Department(242102310530,242102310119,252102310498)the Zhumadian Science and Technology Innovation Youth Special Project(QNZX202413)+1 种基金the Henan Provincial Medical Science and Technology Tackling Program(LHGJ20241009,LHGJ20241006)the Key Scientific Research Project of Higher Education Institutions in Henan Province(25B180015,25B230006)。
文摘Rutin,also known as vitamin P,belongs to the flavonoid class of compounds and is widely present in plants.Its ability to bind with albumin in the blood helps maintain capillary permeability,leading to its extensive use for cardiovascular protection.This review aimed to provide insights into the development of rutin raw material industry in China and its future applications in various fields,such as medicine,healthcare,food,and animal husbandry.The study began by comparing rutin quality standards across China,the United States and Europe,outlined the industrial extraction processes of rutin,and examined the biological activity and potential medical applications of rutin.
基金Supported by Agricultural S&T Innovation:Genetic Structure Analysis and Parasitism Fitness of U.virens in Anhui Province(14B1148)Special Fund for Talent Development:Pesticide Innovation and High-efficient Application Technology(13C1109)~~
文摘[Objective] This study aims to screen for the high effective fungicides which could significantly decrease the disease incidence and disease index of rice false smut. [Method] The inhibitory activities of the fungicide against mycelial growth of Ustilaginoidea virens were measured to in vitro evaluate the ECho values. And 17 fungicides were sprayed to evaluate the efficacy and effect of the fungicides tested in the field trials on the rice characters, [Result] The results showed that epoxicona- zole, difenoconazole, propiconazole and procloraz exhibited high inhibitory activity against mycelial growth of Ustilaginoidea virens with the ECso values 0.04, 0.07, 0.12 and 0.11 pg/ml, respectively. The results of field trials showed that the efficacy of Wen- quning, and fungicides such as difenoconazole, prochloraz, propiconazole, epoxi- conazole and their mixtures in controlling rice false smut were all 70% or more. [Conclusion] The 17 tested fungicides behaved efficacy in controlling rice false smut and did not cause drug injury on leaves and grains of rice plants, sprayed when flag leaves of rice fully expanded.
基金Supported by Major Programs in Education Bureau of Wuhan City(2008K013)~~
文摘A new compound with biological activity had been synthesized by the reaction between 5-（p-chlorophenyl）-2-amino-1,3,4-thiodiazol and aroyl isocyanates.The structure of the target compound was confirmed by IR,UV,1HNMR spectrum and elemental analysis.The biological activity tests showed that the target compound had an activity as plant growth regulator,the auxin activity was 26.1% and the cytokinin activity was 41.1%.
基金supported by the Shanghai Science and Technology R&D Fund(Nos.0952nm04400,07JC14057 and 08ZR1421600)the National Basic Research Fund(No. 2005CB623901)the National Natural Science Foundation of China(Nos.30700170,30973041 and 81271959)
文摘Micro-arc oxidized Cu-incorporated TiO2 coatings （Cu-TiO2） were prepared in the Ca, P, Cu-containing electrolyte to obtain an implant material with superior biological activity and antibacterial property. The surface topography, phase, and element composition of the TiO2 and Cu-TiO2 coatings were characterized by scanning electron microscopy （SEM）, X-ray diffraction （XRD）, and energy-dispersive X-ray spectrometry （EDS）, respectively. Staphylococcus aureus （S. aureus） was selected to evaluate the antibacterial property of the Cu-TiO2 coatings, whereas osteoblastic MG63 cells were cultured on the coatings to investigate the biological activity. The obtained results demonstrated that Cu element was successfully incorporated into the porous nano-structured TiO2 coatings, which did not alter apparently the surface topography and phase composition of the coatings as compared to the Cu-free TiO2 coatings. Moreover, the antibacterial studies suggested that the Cu-incorporated TiO2 coatings could significantly inhibit the adhesion of S. aureus. In addition, the in vitro biological evaluation displayed that the adhesion, proliferation and differentiation of MG63 cells on the Cu-incorporated coatings were enhanced as compared to those on the Cu-free coatings and Ti plates. In conclusion, the innovative Cu-incorporated nano-structured TiO2 coatings on Ti substrate with excellent antibacterial property and biological activity are promising candidates for orthopedic implant.
基金This work was supported by a grant from Science and Technology Fund of Shanxi Province, China (No. 042082).
文摘BACKGROUND: The proliferation and metastasis of cancers depend on angiogenesis. This property provides the feasibility for the treatment of cancer by inhibition of angiogenesis, and many angiogenic inhibitors have been demonstrated to effectively inhibit angiogenesis and consequently the growth of solid cancer. As for the newly identified angiogenesis inhibitor, arresten, some studies have found its high activity on restrainting tumor vessel. This study was to assess the anti-angiogenic activity of arresten. METHODS: The arresten gene was obtained from a healthy puerpera's placenta tissue by the reverse transcriptase-polymerase chain reaction (RT-PCR) method, and molecular cloning to prokaryotic expression plasmid pBV220 by recombination strategy. The prokaryotic expression plasmid pBV220/arr was identified by restriction enzyme digestion and sequenced. The pBV220/arr was transformed into E. coli JM109, DH5α, BL21 and BL21 (DE3) by the CaCl_2 transformation method. The arresten expression level was detected by SDS-PAGE. The expressed product was purlfled, re-naturalized and detected for its biological activity of inhibiting the angiogenesis of chorioallantoic membrane (CAM). RESULTS: The arresten gene was cloned and pBV220/arr was constructed. The arresten expression level of protein was highly increased after pBV220/arr was transformed into E. coli BL21 (DE3). SDS-PAGE showed that the expressed arresten proteins were mainly inclusion bodies and had a molecular weight of 26 kDa. The expressed arresten protein showed evident biological activities. CONCLUSIONS: The successful construction of recombinant plasmid pBV220/arr and the effective expression in E. coil have laid a foundation for further study of its anti-angiogenic function and may pave the way for future antitumor application.
基金funded by BASF (China)CorporationNational 973 Program of China(2006CB101907)863 Program of China(2008AA10Z414).
文摘Dimethomorph is a fungicide with high activity against Peronosporomycetes plant pathogens. The present study showed that dimethomorph is effective on controlling the oomycete fungal pathogen Pseudoperonospora cubensis causing downy mildew on cucumber. The fungicide did not affect zoospores discharge from sporangia of P. cubensis, but it strongly inhibited mycelial growth and sporangial production in vitro and increased lysis of zoospores. Dose of 2 mg L^-1 of dimethomorph was sufficient to inhibit mycelial growth and sporangial production of P. cubensis on leaf disks, 5 mg L^-1 was enough to lyse zoospores of P. cubensis, and 25 mg L^-1 was required to inhibit sporangial production on detached leaves. In whole plant tests, dimethomorph exhibited strong protective and curative activity. Dimethomorph when applied at a dose of 300 mg L^-1 for 1, 3, 5, 7 days before inoculation exhibited 100% efficacy on disease control. On the other hand, efficacies of 67.1 and 31.5% were obtained when the same dose of dimethomorph was applied for 1 and 3 days after inoculation, respectively. So dimethomorph had persistence effect on leaves for 7 days at least and exhibited strong protective and curative activity. Bioassay analyses showed that dimethomorph could be translocated in the xylem system, redistributed in the leaf, and penetrated from the upper surface to the lower surface of the leaf but could not be translocated in phloem system or transferred from the roots to leaves of cucumber plants in sufficient amounts for disease control. The biocharacteristics of dimethomorph make it well suitable for integration of a control programme against downy mildew disease on cucumber and as a component to delay other peronosporomycetes fungicide-resistance development.
基金supported by the Natural Science Foundation of Hubei Province (No. 2008CDB016)the Research Project for Innovative Research Team of Hubei University for Nationalities
文摘The title compound N-（2,6-difluorobenzoyl）-N＇-[5-（4-trifluoromethylphenyl）-1,3,4-thiadiazol-2-yl]urea（C17H9F5N4O2S,Mr = 428.34） has been synthesized by the reaction of 2-amino-5-（4-trifluoromethylphenyl）-1,3,4-thiadiazole with 2,6-difluorobenzoyl isocyanate,and its crystal structure was determined by single-crystal X-ray diffraction.The crystal belongs to monoclinic,space group P21/n with a = 10.7316（13）,b = 10.5617（13）,c = 16.037（2） ,β = 106.408（2）°,V = 1743.6（4） 3,Z = 4,Dc = 1.632 g/cm3,μ = 0.260 mm-1,F（000） = 864,the final R = 0.0599 and wR = 0.1420 for 3467 observed reflections with I〉 2σ（I）.The urea group,which adopts a planar configuration mediated by the intramolecular N-H...O hydrogen bond,is nearly coplanar with the thiadiazole and 4-trifluoromethylbenzene rings.The title compound was found to exhibit good fungicidal activity against Rhizoctonia solani and Botrytis cinerea.
基金Supported by National Natural Science Foundation of China(No.2 0 1710 10 ) .
文摘A novel compound, (HGly) 4[HPMo 12 O 40 ] 2·22H 2O, was synthesized and characterized by means of elemental analysis, IR and X ray diffraction. The compound crystallized in a monoclinic space group Cc with a =4 0060(0 8) nm, b =1 2527(0 3) nm, c =1 9930(0 4) nm, β =96 36(3)°, V =9 940(3) nm 3, Z =2, R 1=0 0576, wR 2 =0 1746. The anti tumor activity of this compound was tested in two human tumor cell lines in vitro .
基金This project was supported by grants from the National Natural Science Foundation of China ( No.30271242,30371396).
文摘To express recombinant arresten in Escherichia coli (E.Coli) and investigate its biological activity, prokaryotic expression vector of human arresten gene was constructed by gene engineering. Human arresten gene was amplified from recombinant plasmid pGEMArr by polymerase chain reaction (PCR), and inserted into prokaryotic expression vector pRSET containing T7 promoter. Restriction analysis and DNA sequencing verified that the arresten gene was correctly cloned into the expression vector. The recombinant plasmid pRSETAt was subsequently transformed into E.coli BL21 (DE3), and the target gene was expressed under induction of IPTG. SDS-PAGE analysis revealed that the recombinant protein with a molecular weight of 29 kD (1 kD=0.992 1 ku) amounted to 29 % of the total bacterial proteins. After purification and renaturation, the recombinant protein could significantly suppress the proliferation of human umbilical vein endothelial cells (HUVECs). These results suggested that the expression of a biologically active form of human arresten in the pRSET expression system laid a foundation for further study on the mechanistic insight into arresten action on angiogenesis and the development of powerful anti-cancer drugs.
基金supported by the National Natural Science Foundation of China (No.21262012)the Natural Science Foundation of Hubei Province (No.2011CDB087)+1 种基金the Scientific Research Fund of Hubei Provincial Education Department (No.Q20122909)the Project of Team Research for Excellent Mid-Aged & Young Teachers of Higher Education of Hubei Province, China (No.T201006)
文摘The novel title compound 4-chlorobenzaldehyde （2-trifluoromethyl-5,6,7,8- tetrahydro- benzo[4,5]thieno[2,3-d]pyrimidin-4-yl）hydrazone monohydrate （C18H14C1F3N4S.H20, Mr = 428.86） has been synthesized by a condensation reaction of 4-chlorobenzaldehyde with （2-trifuoromethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl）hydrazine, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to monoclinic, space group P21/c with a = 7.4252（7）, b = 26.344（2）, c = 10.3095（9） A, /3 = 109.407（2）~, V= 1902.0（3） A3, Z = 4, Dc = 1.498 g/cm^3, p = 0.356 mm-1, F（000） = 880, the final R = 0.0564 and wR = 0.1681 for 2343 observed reflections with I 〉 2o（/）. X-ray diffraction analysis reveals that the title hydrazone molecule is nearly planar except for the cyclohexene and trifluoromethyl moieties. In the crystal packing, the molecules form stacks by a three-dimensional framework, which results from intermolecular N（3）-H（3）...O（1）, O（1）-H（1B）...N（2）, O（1）- H（1B）...N（4） and O（1）-H（1A）...F（1） hydrogen bonds via water molecules together with π-π stacking interactions. Molecular geometry of the title compound in the ground state optimized by B3LYP functional with 6-311G＊＊ basis sets indicates that the calculations are in agreement with the experimental data. The preliminary bioassay suggested that the title compound exhibits relatively good fungicidal activity against Fusarium oxysporium fsp.vasinfectum and Dothiorella gregaria.
基金funded in part by the National Natural Science Foundation of China(21372132)NFFTBS(No.J1103306)
文摘The title compound 2-（1-（3-bromo-1-（3-chloropyridin-2-yl）-1H-pyrazole-5-carbonyl）piperidin-4-yl）-N-isopropylthiazole-4-carboxamide（C21H22Br Cl N6O2 S,Mr = 536.04） has been synthesized,and its structure was characterized by IR spectra,1H-NMR,13C-NMR,EA,and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic system,space group P/c with a = 15.146（3）,b = 11.573（2）,c = 26.937（5） A,β = 103.64（3）°,V = 1839.0（6） A^3,Z = 4,Dc = 1.557 g/cm^3,μ（Mo Ka） = 0.71073 mm^-1,F（000） = 2192,R = 0.0601 and w R = 0.1392.There exist one intramolecular hydrogen bond at N–H···N and four intermolecular weak interactions at O（2）···H（1）,Cl（1）···H（12）,O（1）···Cl（1） and S（1）···O（2）.Bioassay results indicated that the title compound had good fungicidal and antiviral activities against tobacco mosaic virus.
文摘Five new solid complexes were synthesized about transition metals with Schiff base（ L, C18H23NO2 ） derived from adamantaneamine and o-vanillin, and characterized by elemental analysis, molar conductance, infrared spectra, UV-vis spectra, thermal analysis. Their chemical formula are [ML2]（ClO4）2 （ M= Mn, Co, Ni, Cu, Zn）, and the coordination numbers are four, The antibacterial activity of Schiff base ligand and its complexes was studied.
基金the National Key R&D Program of China(No.2022YFA1302900)the National Natural Science Foundation of China (Nos.82130105, 92253305, 82121005, and 22177124)supported by the Lingang Laboratory (Nos.LG-GG-202204–02 and LG202103–04–01)。
文摘Schiff base metal complexes are of great importance in pharmaceutical science owing to their unique chemical properties, which enable them to exhibit diverse biological activities such as anti-bacterial,anti-oxidant, anti-inflammatory, and anti-tumor properties. Furthermore, Schiff base metal complexes can serve as reagents and catalysts in chemical reactions. This review aims to provide an overview of our recently published studies on Cu(Ⅱ) and Pd(Ⅱ) complexes derived from proline Schiff base ligands. We also discuss the potential applications of these metal complexes in the fields of antibacterial and chiral resolution.
基金funded in part by the National Natural Science Foundation of China(21372132)Nataliya P.Belskaya thanks Russian State Task of Ministry Education and Science No.4.560.2014K.Kalinina A.Tatiana thanks RFBF№13-03-00137
文摘The title compound N-cyanosulfoximine derivative containing 1,2,3-thiadiazole （C6HsN4OS2, Mr = 216.28） has been synthesized using 4-（chloromethyl）-5-methyl-1,2,3-thiadiazole as the starting material, and its structure was characterized by IR, 1H NMR, HRMS, elemental analysis and single-crystal X-ray diffraction. The crystal of the title compound belongs to orthorhombic, space group Pna21 with a = 14.730（6）, b = 5.478（2）, c = 22.619（9） A, Z = 8, V = 1825.0（13） A3, Dc = 1.574 g/cm3,/a = 0.547 mm-1, F（000） = 896, R = 0.0767 and wR （I〉 2o（/）） = 0.2064. X-ray analysis indicates that in this crystal double enantiomers are found as the basically asymmetrical unit and interactions between S（1）...N（3）, S（3）...N（4） and S（3）...N（7） are observed. This kind of interactions extends the molecules into a one-dimensional double chain. The preliminary biological test showed that the title compound had insecticidal activity against Myzus persicae in a certain degree and also presented moderate potential bioactivity against tobacco mosaic virus （TMV）.
基金funded in part by the Tianjin Natural Science Foundation(No.14JCYBJC20400)the"111"Project of Ministry of Education of China(No.B06005)NFFTBS(No.J1103306)
文摘The title compound diethyl 2-（3,4-dichloroisothiazol-5-yl）-4-（trifluoromethyl）-4,5- dihydrothiazol-4-yl-3-methylbenzoate （C15H9C12F3N202S2, Mr = 441.26） was prepared from methyl 3,4-dichloroisothiazole-5-carboxylate as the starting material by four steps of reaction. Its structure was characterized by IR, 1H-NMR, 13C-NMR, EA and single-crystal X-ray diffraction. The crystal of the title compound belongs to the monoclinic system, space group P2dc with a = 8.8437（18）, b = 16.128（3）, c = 12.305（3） A, β = 91.68（3）°, V= 1754.4（6） A3, Z = 4, Dc = 1.671 g/cm3,μ（MoKa） = 0,71073 mm^-1, F（000） = 888, R = 0.0384 and wR = 0.0778. Weak π-π interactions occur between the isothiazole rings and phenyl rings of adjacent molecules to form a one-dimensional chain and stabilize the crystal structure. Bioassay indicates that the title compound has good activity against the fungi and TMV tested.
基金Supported by the National Natural Science Foundation of China (10874047)Natural Science Foundation of Guangdong Province (04300531)
文摘A novel compound,2-（anthracen-9-yl）-5-p-tolyl-1,3,4-oxadiazole（C23H16N2O）,has been synthesized by the condensation of 4-methylbenzohydrazide and anthracene-9-carbaldehyde in an ethanol solution with chloramine-T.The compound was characterized by 1H-NMR,13C-NMR,MS and single-crystal X-ray diffraction.The crystal belongs to the triclinic system,space group P with a = 7.7817（4）,b = 8.8544（5）,c = 12.4726（8） ,β = 92.8520（10）°,Z = 2,V = 826.58（8） 3,Dc = 1.352 g/cm3,Mr = 336.38,λ（MoKα） = 0.71073 ,μ = 0.084 mm-1,F（000） = 352,R = 0.0381 and wR = 0.1099.The dihedral angle between anthracene skeleton and phenyl ring is 64.19°.A total of 6354 unique reflections were collected,of which 3172 with I 〉 2σ（I） were observed.X-ray analysis indicated an offset face-to-face π-π stacking interaction between anthracene skeletons and an offset face-to-face π-π stacking interaction between phenyl ring planes.The novel compound molecules are connected through the offset face-to-face π-π stacking interactions to generate a three-dimensional network.The preliminary bioassay results showed that the novel compound exhibited significant insect growth inhibitory activity against Spodoptera litura Fabricius larvae.
基金supported by the National Key Technology Research and Development Program(2011BAE06B02)
文摘The title compound diethyl 1,4-dihydro-2,6-dimethyl-4-（4-methyl-1,2,3-thiadiazol- 5-yl） pyridine-3,5-dicarboxylate （C16H21N3O4S, Mr = 351.42） was prepared by the Hantszch reaction with 4-methyl-1,2,3-thiadiazole-5-formaldehyde, ethyl acetoacetate and ammonium acetate in the presence of aluminum chloride in alcohol, and its structure was characterized by IR spectra, 1H-NMR, EA, and single-crystal X-ray diffraction. The crystal of the title compound belongs to monoclinic system, space group P21/n with α= 11.300（2）, b = 12.771（3）, c = 12.826（3） ？, β = 96.55（3）o, V = 1839.0（6） ？3, Z = 4, Dc = 1.296 g/cm3, μ（MoKa） = 0.71073 mm-1, F（000） = 744, R = 0.0981 and wR = 0.1994. X-ray diffraction result shows that the torsion angles of N（1）–C（2）– C（3）–C（4） and C（2）–C（3）–C（4）–C（8） are 178.9（3）° and –130.3（3）°, respectively. All rings in the title compound are non-planar. The bioassay results indicate that the title compound has good fungicidal activity, good antivirus activity against tobacco mosaic virus and certain extent of insecticidal activity against Mythimna separata.
