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1.
Bioorg Chem ; 153: 107802, 2024 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-39244972

RESUMO

The treatment of bladder cancer is limited by low drug efficacy and drug resistance. Hence, this study aimed to screen and identify potential drug precursors and investigate their mechanism of action. A set of camptothecin derivatives showing high anti-tumor potential was selected from early-stage research or literature and synthesized to construct a compound library. A total of 135 compounds were screened in T24 and J82 cells, revealing that FL118 significantly inhibited the proliferation of GC (gemcitabine + cisplatin)-sensitive/insensitive cells. FL118 exhibited excellent penetration and killing ability in organoids and three GC-insensitive patient-derived xenografts. Chemical proteomic and docking calculations were employed to identify binding proteins, indicating that FL118 can bind into H2A.X and its entwined DNA. The results of Cellular thermal shift assay and surface plasmon resonance (Kd = 3.77E-6) support the above findings. Fluorescence localization revealed widespread binding of FL118 within the cell nucleus. Furthermore, WB showed that FL118 increased cellular DNA damage, resulting in significant cell cycle inhibition. The binding of FL118 to H2A.X hindered the damage repair process, leading to apoptosis. Controllable adverse reactions were observed in mice treated with FL118. In conclusion, FL118 may be a superior anti-bladder cancer compound that acts as a molecular glue binding to both H2A.X and DNA. The resistance mediated by the DNA damage repair to DNA damage caused by GC regimen can be reversed by FL118. This distinct mechanism of FL118 has the potential to complement existing mainstream treatment approaches for bladder cancer.

2.
J Agric Food Chem ; 72(38): 20831-20841, 2024 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-39284582

RESUMO

This research adopted the Fischer indole synthesis method to continue constructing a novel drug-like chemical entity based on the guidance of isocryptolepine and obtained four series of derivatives: Y, Da, Db, and Dc. The antimicrobial activity of these derivatives against plant pathogens was further evaluated. The results showed that Dc-2 had the best antifungal effect against Botrytis cinerea, and its EC50 value was up to 1.29 µg/mL. In addition, an in vivo activity test showed that the protective effect of Dc-2 on apples was 82.2% at 200 µg/mL, which was better than that of Pyrimethanil (45.4%). Meanwhile, it was found by scanning electron microscopy and transmission electron microscopy that the compound Dc-2 affected the morphology of mycelia. The compound Dc-2 was found to damage the cell membrane by PI and ROS staining. Through experiments such as leakage of cell contents, it was found that the compound Dc-2 changed the permeability of the cell membrane and caused the leakage of substances in the cell. According to the above studies, compound Dc-2 can be used as a candidate lead compound for further structural optimization and development.


Assuntos
Botrytis , Desenho de Fármacos , Fungicidas Industriais , Doenças das Plantas , Botrytis/efeitos dos fármacos , Botrytis/crescimento & desenvolvimento , Doenças das Plantas/microbiologia , Fungicidas Industriais/farmacologia , Fungicidas Industriais/síntese química , Fungicidas Industriais/química , Relação Estrutura-Atividade , Antibacterianos/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Testes de Sensibilidade Microbiana , Malus/química , Malus/microbiologia , Bactérias/efeitos dos fármacos , Estrutura Molecular
3.
J Agric Food Chem ; 72(36): 19618-19628, 2024 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-39193844

RESUMO

Sophora flavescens, a traditional Chinese herb, produces a wide range of secondary metabolites with a broad spectrum of biological activities. In this study, we isolated six isopentenyl flavonoids (1-6) from the roots of S. flavescens and evaluated their activities against phytopathogenic fungi. In vitro activities showed that kurarinone and sophoraflavanone G displayed broad spectrum and superior activities, among which sophoraflavanone G displayed excellent activity against tested fungi, with EC50 values ranging from 4.76 to 13.94 µg/mL. Notably, kurarinone was easily purified and showed potential activity against Rhizoctonia solani, Botrytis cinerea, and Fusarium graminearum with EC50 values of 16.12, 16.55, and 16.99 µg/mL, respectively. Consequently, we initially investigated the mechanism of kurarinone against B. cinerea. It was found that kurarinone disrupted cell wall components, impaired cell membrane integrity, increased cell membrane permeability, and affected cellular energy metabolism, thereby exerting its effect against B. cinerea. Therefore, kurarinone is expected to be a potential candidate for the development of plant fungicides.


Assuntos
Botrytis , Flavonoides , Fungicidas Industriais , Fusarium , Doenças das Plantas , Raízes de Plantas , Rhizoctonia , Sophora , Botrytis/efeitos dos fármacos , Botrytis/crescimento & desenvolvimento , Sophora/química , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Fusarium/efeitos dos fármacos , Fungicidas Industriais/farmacologia , Fungicidas Industriais/química , Raízes de Plantas/química , Doenças das Plantas/microbiologia , Rhizoctonia/efeitos dos fármacos , Rhizoctonia/crescimento & desenvolvimento , Prenilação , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Sophora flavescens
4.
Bioorg Med Chem ; 112: 117880, 2024 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-39216382

RESUMO

Berberine is a quaternary ammonium isoquinoline alkaloid derived from traditional Chinese medicines Coptis chinensis and Phellodendron chinense. It has many pharmacological activities such as hypoglycemic, hypolipidemic, anti-tumor, antimicrobial and anti-inflammatory. Through structural modifications at various sites of berberine, the introduction of different groups can change berberine's physical and chemical properties, thereby improving the biological activity and clinical efficacy, and expanding the scope of application. This paper reviews the research progress and structure-activity relationships of berberine in recent years, aiming to provide valuable insights for the exploration of novel berberine derivatives.


Assuntos
Berberina , Berberina/química , Berberina/farmacologia , Berberina/análogos & derivados , Relação Estrutura-Atividade , Humanos , Estrutura Molecular , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/síntese química , Animais , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química
5.
Nat Prod Res ; : 1-10, 2024 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-39155512

RESUMO

With the intention of advancing our research on diverse C-20 derivatives of camptothecin (CPT), 38 CPT derivatives bearing sulphonamide and sulfonylurea chemical scaffolds and different substituent groups have been designed, synthesised and evaluated in vitro for cytotoxicity against four tumour cell lines, A-549 (lung carcinoma), KB (nasopharyngeal carcinoma), MDA-MB-231 (triple-negative breast cancer) and KBvin (an MDR KB subiline). As a result, all the synthesised compounds showed promising in vitro cytotoxic activity against the four cancer cell lines tested, and were more potent than irinotecan. Importantly, compounds 12b, 12f, 12j and 13 l possessed better antiproliferative activity against all tested tumour cell lines with IC50 values of 0.0118 - 0.5478 µM, and resulted approximately 3 to 4 times more cytotoxic than topotecan against multidrug-resistant KBvin subline. Convincing evidences are achieved that incorporation of sulphonamide and sulfonylurea motifs into position-20 of camptothecin confers markedly enhanced cytotoxic activity against cancer cell lines.

6.
Angew Chem Int Ed Engl ; 63(39): e202402915, 2024 Sep 23.
Artigo em Inglês | MEDLINE | ID: mdl-38569128

RESUMO

Sustainable carbon dots based on cellulose, particularly carboxymethyl cellulose carbon dots (CMCCDs), were confined in an inorganic network resulting in CMCCDs@SiO2. This resulted in a material exhibiting long afterglow covering a time frame of several seconds also under air. Temperature-dependent emission spectra gave information on thermally activated delayed fluorescence (TADF) and room temperature phosphorescence (RTP) while photocurrent experiments provided a deeper understanding of charge availability in the dark period, and therefore, its availability on the photocatalyst surface. The photo-ATRP initiator, ethyl α-bromophenylacetate (EBPA), quenched the emission from the millisecond to the nanosecond time frame indicating participation of the triplet state in photoinduced electron transfer (PET). Both free radical and controlled radical polymerization based on photo-ATRP protocol worked successfully. Metal-free photo-ATRP resulted in chain extendable macroinitiators based on a reductive mechanism with either MMA or in combination with styrene. Addition of 9 ppm Cu2+ resulted in Mw/Mn of 1.4 while an increase to 72 ppm improved uniformity of the polymers; that is Mw/Mn=1.03. Complementary experiments with kerria laca carbon dots confined materials, namely KCDs@SiO2, provided similar results. Deposition of Cu2+ (9 ppm) on the photocatalyst surface explains better uniformity of the polymers formed in the ATRP protocol.

7.
Angew Chem Int Ed Engl ; 63(29): e202404454, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-38683297

RESUMO

Sustainable carbon dots comprising surficial oxime ester groups following homolytic bond cleavage exhibit potential as photoinitiators for traditional free radical photopolymerization. Carbon dots were made following a solvothermal procedure from sustainable furfural available from lignocellulose. Surficial aldehyde moieties reacted with hydroxylamine to the respective oxime while reaction with benzoyl chloride resulted in a biobased Type I photoinitiator comprising sustainable carbon dot (CD-PI). Photoinitiating ability was compared with the traditional photoinitiator (PI) ethyl (2,4,6-trimethyl benzoyl) phenyl phosphinate (TPO-L) by real-time FTIR with UV exposure at 365 nm. Photopolymer composition based on a mixture of urethane dimethacrylate (UDMA) and tripropylene glycol diacrylate (TPGDA) resulted in a similar final conversion of about 70 % using either CD-PI or TPO-L. Nevertheless, it appeared homogeneous in the case of compositions processed with CD-PI, while those made with TPO-L were heterogeneous as shown by two glass transition temperatures. Moreover, the migration rate of CD-PI in the cured samples was lower in comparison with those samples using TPO-L as PI.

8.
J Agric Food Chem ; 72(13): 6988-6997, 2024 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-38506764

RESUMO

Bacterial leaf blight (BLB) caused by Xanthomonas oryzae pv oryzae (Xoo) is extremely harmful to rice production. The traditional control approach is to use bactericides that target key bacterial growth factors, but the selection pressure on the pathogen makes resistant strains the dominant bacterial strains, leading to a decline in bactericidal efficacy. Type III secretion system (T3SS) is a conserved and critical virulence factor in most Gram-negative bacteria, and its expression or absence does not affect bacterial growth, rendering it an ideal target for creating drugs against Gram-negative pathogens. In this work, we synthesized a range of derivatives from cryptolepine and neocryptolepine. We found that compound Z-8 could inhibit the expression of Xoo T3SS-related genes without affecting the growth of bacteria. an in vivo bioassay showed that compound Z-8 could effectively reduce the hypersensitive response (HR) induced by Xoo in tobacco and reduce the pathogenicity of Xoo in rice. Furthermore, it exhibited synergy in control of bacterial leaf blight when combined with the quorum quenching bacterial F20.


Assuntos
Alcaloides , Alcaloides Indólicos , Oryza , Quinolinas , Xanthomonas , Oryza/genética , Sistemas de Secreção Tipo III/genética , Bactérias/metabolismo , Xanthomonas/genética , Doenças das Plantas/prevenção & controle , Doenças das Plantas/microbiologia
9.
Angew Chem Int Ed Engl ; 63(18): e202316431, 2024 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-38012084

RESUMO

Carbon nanomaterials, specifically carbon dots and carbon nitrides, play a crucial role as heterogeneous photoinitiators in both radical and cationic polymerization processes. These recently introduced materials offer promising solutions to the limitations of current homogeneous systems, presenting a novel approach to photopolymerization. This review highlights the preparation and photocatalytic performance of these nanomaterials, emphasizing their application in various polymerization techniques, including photoinduced i) free radical, ii) RAFT, iii) ATRP, and iv) cationic photopolymerization. Additionally, it discusses their potential in addressing contemporary challenges and explores prospects in this field. Moreover, carbon nitrides, in particular, exhibit exceptional oxygen tolerance, underscoring their significance in radical polymerization processes and allowing their applications such as 3D printing, surface modification of coatings, and hydrogel engineering.

10.
Nat Rev Chem ; 7(11): 800-812, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37749285

RESUMO

Room-temperature phosphorescent (RTP) materials have enormous potential in many different areas. Additionally, the conversion of natural resources to RTP materials has attracted considerable attention. Owing to their inherent luminescent properties, natural materials can be efficiently converted into sustainable RTP materials. However, to date, only a few reviews have focused on this area of endeavour. Motivated by this lack of coverage, in this Review, we address this shortcoming and introduce the types of natural resource available for the preparation of RTP materials. We mainly focus on the inherent advantages of natural resources for RTP materials, strategies for activating and enhancing the RTP properties of the natural resources as well as the potential applications of these RTP materials. In addition, we discuss future challenges and opportunities in this area of research.

11.
Pest Manag Sci ; 79(12): 5321-5332, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37615260

RESUMO

BACKGROUND: Chemical fungicides are the mainstay of plant disease control in agricultural production, but there are a very limited number of drugs that can effectively control plant diseases. Two series of secondary amine derivatives were synthesized using the diamine skeleton combined with saturated aromatic and aliphatic aldehydes, and their antibacterial and antifungal activities against plant pathogens were determined. In addition, the antimicrobial mechanism of the highly active compound A26 was preliminarily examined against Xanthomonas oryzae (Xoo). RESULTS: Compound A26 exhibited the highest antibacterial potency among all the target compounds, with MIC values of 3.12, 3.12 and 12.5 µg mL-1 against Xoo, Xanthomonas axonopodis pv. Citri and Pseudomonas sollamacearum, respectively. In addition, compound A26 had powerful curative and protective effects against Xoo at 200 µg mL-1 , and was better than the control agent Xinjunan. Preliminary mechanistic studies showed that compound A26 reduced the bacterial pathogenicity by targeting cell membranes and inhibiting the secretion of extracellular polysaccharides. Meanwhile, the toxicity of compound A26 to Human Embryonic Kidney 293 cells and Human Liver-7702 was similar to that of Xinjunan, and it had moderate toxicity according to the World Health Organization classification standard of oral exogenous toxicity, with an LD50 of 245.47 mg kg-1 . CONCLUSION: Secondary amines have efficient and broad-spectrum antibacterial activity against plant pathogenic bacteria and are expected to be a new class of candidate compounds for antibacterial drugs. © 2023 Society of Chemical Industry.


Assuntos
Oryza , Xanthomonas , Humanos , Testes de Sensibilidade Microbiana , Oxidiazóis/química , Antibacterianos/farmacologia , Antibacterianos/química , Poliaminas/farmacologia , Doenças das Plantas
12.
Int J Food Microbiol ; 404: 110318, 2023 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-37454507

RESUMO

Aspergillus flavus, a widespread saprotrophic filamentous fungus, could colonize agricultural crops with aflatoxin contamination, which endangers food security and the agricultural economy. A safe, effective and environmentally friendly fungicide is urgently needed. Pterostilbene, a natural phytoalexin originated from Pterocarpus indicus Willd., Vaccinium spp. and Vitis vinifera L., has been reported to possess excellent antimicrobial activity. More importantly, it is quite safe and healthy. In our screening tests of plant polyphenols for the inhibition of A. flavus, we found that pterostilbene evidently inhibited mycelial growth of Aspergillus flavus (EC50 = 15.94 µg/mL) and the inhibitory effect was better than that of natamycin (EC50 = 22.01 µg/mL), which is a natural product widely used in food preservation. Therefore, we provided insights into the efficacy of pterostilbene suppression on A. flavus growth, aflatoxin B1 biosynthesis and its potential mechanisms against A. flavus in the present study. Here, pterostilbene at concentrations of 250 and 500 µg/mL could effectively inhibit the infection of A. flavus on peanuts. And the biosynthesis of the secondary metabolite aflatoxin B1 was also inhibited. The antifungal effects of pterostilbene are exerted by inducing a large amount of intracellular reactive oxygen species production to bring the cells into a state of oxidative stress, damaging cellular biomolecules such as DNA, proteins and lipids and destroying the integrity of the cell membrane. Taken together, our study strongly supported the fact that pterostilbene could be considered a safe and effective antifungal agent against A. flavus infection.


Assuntos
Aflatoxinas , Aspergillus flavus , Aspergillus flavus/metabolismo , Aflatoxina B1 , Antifúngicos/farmacologia , Antifúngicos/metabolismo
13.
Angew Chem Int Ed Engl ; 62(27): e202301242, 2023 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-36916463

RESUMO

A sustainable photocatalyst for use with multiple purpose comprising demethylated lignin (Fe3 O4 @D-wood) was made by treatment of wood and iron oxide. Characterization followed by XRD, UV/Vis, photo-current studies, and electrochemical measurements. This material became subject of photocatalytic explorations for water treatment and material synthesis by radical photopolymerization. Exposure of Fe3 O4 @D-wood with artificial sunlight showed an improved activity considering photochemical oxidation of organic pollutants in the presence of H2 O2 . The efficient generation of reactive radicals brought this system also to photopolymerization. Here, radicals based on reactive oxygen species (ROS) generated in the catalytic cycle can be seen as the dominating species to initiate radical polymerization. A mixture of UDMA and TPGDA showed good reactivity with cumene hydroperoxide (CHP). Photocatalyst used for water treatment facilitates reuse for photopolymerization.

14.
Pest Manag Sci ; 79(8): 2748-2761, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36914877

RESUMO

BACKGROUND: The unreasonable use of chemical fungicides causes common adverse consequences that not only affect the environment, but also cause resistance and resurgence problems of plant pathogens, which are extremely harmful to human health, the economy, and the environment. Based on the rich biological activities of boron-based compounds, 82 phenylboronic acid derivatives were selected and their antifungal activities against six agricultural plant pathogens were determined. Combined with transcriptomics tools, the mechanism of action of compound A49 (2-chloro-5-trifluoromethoxybenzeneboronic acid) against Botrytis cinerea Pers (B. cinerea) was studied. RESULTS: The EC50 values of compounds A24, A25, A30, A31, A36, A41, A49 and B23 against all six fungi were under 10 µg/mL. Compound A49 displayed significant activity against B. cinerea (EC50 = 0.39 µg/mL), which was better than that of commercial fungicide boscalid (EC50 = 0.55 µg/mL). A49 not only inhibited the germination of B. cinerea spores, but also caused abnormal cell morphology, loss of cell membrane integrity, enhanced cell membrane permeability, and accumulation of intracellular reactive oxygen species. Further findings showed that A49 reduced cellular antioxidant activity, and peroxidase and catalase activities. Transcriptomic results indicated that A49 could degrade intracellular redox processes and alter the metabolism of some amino acids. Meanwhile, A49 showed obvious activity in vivo and low cytotoxicity to mammal cells. CONCLUSION: The boron-containing small molecule compounds had high efficiency and broad-spectrum antifungal activities against six plant pathogens, and are expected to be candidate compounds for a new class of antifungal drugs. © 2023 Society of Chemical Industry.


Assuntos
Antifúngicos , Fungicidas Industriais , Humanos , Antifúngicos/farmacologia , Antifúngicos/química , Boro , Fungicidas Industriais/farmacologia , Fungicidas Industriais/química , Botrytis , Relação Estrutura-Atividade
15.
Pest Manag Sci ; 79(6): 2135-2146, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36721354

RESUMO

BACKGROUND: The resistance of traditional chemical fungicides to plant pathogenic fungi and the threats to the safety of humans and the environment highlight an urgent need to find safe and efficient alternatives to chemical fungicides. Owing to the wide spectrum of antifungal activities, low persistence and nontoxicity to mammals and aquatic life, essential oils have considerable potential as low-risk pesticides. In this study, the essential oil and the main components of Angelica sinensis (Oliv.) Diels (Danggui) were extracted, analyzed by GC-MS, and evaluated for their antifungal activities against six plant pathogenic fungi. RESULTS: 3-butylidenephthalide (3-BPH) showed the best antifungal activity against Fusarium graminearum with an EC50 value of 14.35 µg mL-1 . The antifungal mechanistic studies revealed that 3-BPH induced the generation of endogenous ROS to cause lipid peroxidation of the cell membrane and inhibited the biosynthesis of ergosterol, thereby causing the cell membrane damaged to exert its fungicidal activity. Significantly, 3-BPH could reduce deoxynivalenol production compared to the control. CONCLUSION: This study demonstrated the potent fungicidal activity of natural phthalide compound 3-BPH and highlighted its potential as an alternative agent to control F. graminearum. © 2023 Society of Chemical Industry.


Assuntos
Angelica sinensis , Fungicidas Industriais , Fusarium , Óleos Voláteis , Animais , Angelica sinensis/química , Antifúngicos/farmacologia , Antifúngicos/química , Fungos , Fungicidas Industriais/farmacologia , Mamíferos , Plantas
16.
J Agric Food Chem ; 71(5): 2301-2312, 2023 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-36706432

RESUMO

A series of quinoline derivatives were designed and synthesized by the structural simplification of cryptolepine and evaluated for their fungicidal activity against six phytopathogenic fungi. Most of these compounds exhibited remarkable activities against Botrytis cinereain vitro. Among them, compounds A18 and L01 showed superior antifungal activity. Significantly, compared to cryptolepine, compound A18 exhibited broad-spectrum inhibitory activities against B. cinerea, Sclerotinia sclerotiorum, Rhizoctonia solani, Phytophthora capsica, Magnaporthe oryzae, and Fusarium graminearum with the respective EC50 values of 0.249, 1.569, 3.915, 0.505, 0.246, and 4.999 µg/mL. Compound L01 displayed the best antifungal activity against B. cinerea with an EC50 value of 0.156 µg/mL. Preliminary mechanistic studies showed that compound A18 could inhibit spore germination, affect the permeability of the cell membrane, increase the content of reactive oxygen species, and affect the morphology of hyphae and cells. Moreover, compound A18 showed excellent in vivo protective effect against B. cinerea, which was more potent than pyrimethanil and equitant to cryptolepine. These results evidenced that compound A18 displayed superior fungicidal activities and could be a potential fungicidal candidate against plant fungal diseases.


Assuntos
Fungicidas Industriais , Quinolinas , Antifúngicos/farmacologia , Fungicidas Industriais/química , Quinolinas/farmacologia , Alcaloides Indólicos/farmacologia , Botrytis , Relação Estrutura-Atividade , Fungos
17.
J Antibiot (Tokyo) ; 76(3): 131-182, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-36707717

RESUMO

Epidemic diseases of crops caused by fungi deeply affected the course of human history and processed a major restriction on social and economic development. However, with the enormous misuse of existing antimicrobial drugs, an increasing number of fungi have developed serious resistance to them, making the diseases caused by pathogenic fungi even more challenging to control. Drug repurposing is an attractive alternative, it requires less time and investment in the drug development process than traditional R&D strategies. In this work, we screened 600 existing commercially available drugs, some of which had previously unknown activity against pathogenic fungi. From the primary screen at a fixed concentration of 100 µg/mL, 120, 162, 167, 85, 102, and 82 drugs were found to be effective against Rhizoctonia solani, Sclerotinia sclerotiorum, Botrytis cinerea, Phytophthora capsici, Fusarium graminearum and Fusarium oxysporum, respectively. They were divided into nine groups lead compounds, including quinoline alkaloids, benzimidazoles/carbamate esters, azoles, isothiazoles, pyrimidines, pyridines, piperidines/piperazines, ionic liquids and miscellaneous group, and simple structure-activity relationship analysis was carried out. Comparison with fungicides to identify the most promising drugs or lead structures for the development of new antifungal agents in agriculture.


Assuntos
Anti-Infecciosos , Fungicidas Industriais , Fusarium , Humanos , Fungicidas Industriais/química , Reposicionamento de Medicamentos , Antifúngicos/farmacologia , Relação Estrutura-Atividade , Anti-Infecciosos/farmacologia
18.
J Agric Food Chem ; 70(39): 12297-12309, 2022 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-36149871

RESUMO

The inhibitory effect of tavaborole on the invasion of Botrytis cinerea in grapes and tomatoes, as well as the potential mechanism involved, was discovered in this study. Our findings showed that tavaborole inhibited Botrytis cinerea spore germination and mycelial expansion in vitro and that the control efficiency in vivo on fruit decay was dose-dependent, which was effective in reducing disease severity and maintaining the organoleptic quality of the fruit, such as reducing weight loss and retaining fruit hardness and titratable acid contents during storage. Furthermore, the precise mechanism of action was investigated further. Propidium iodide staining revealed that Botrytis cinerea treated with tavaborole lost membrane integrity. For further validation, cytoplasmic malondialdehyde accumulation and leakage of cytoplasmic constituents were determined. Notably, the inhibitory effect was also dependent on inhibiting the activities of aminoacyl-tRNA synthetases involved in the aminoacyl-tRNA biosynthesis pathway in Botrytis cinerea. The above findings concluded that tavaborole was effective against Botrytis cinerea infection in postharvest fruit, and a related mechanism was also discussed, which may provide references for the drug repurposing of tavaborole as a postharvest fungicide.


Assuntos
Frutas , Fungicidas Industriais , Compostos de Boro , Botrytis , Compostos Bicíclicos Heterocíclicos com Pontes , Fungicidas Industriais/farmacologia , Ligases , Malondialdeído , Doenças das Plantas , Propídio/farmacologia , RNA de Transferência/farmacologia
19.
J Agric Food Chem ; 70(37): 11782-11791, 2022 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-36067412

RESUMO

In this work, a series of derivatives with disulfide bonds containing pyridine, pyrimidine, thiophene, thiazole, benzothiazole, and quinoline were designed and synthesized based on the various biological activities of allicin disulfide bond functional groups. The antimicrobial activities of the target compounds were determined, and the structure-activity relationships were discussed. Among them, compound S8 demonstrated the most potent antifungal activity in vitro against Monilinia fructicola (M. fructicola), with an EC50 value of 5.92 µg/mL. Furthermore, an in vivo bioassay revealed that compound S8 exhibited equivalent curative and higher protective effects as the positive drug thiophanate methyl at a concentration of 200 µg/mL. The preliminary mechanism experiments showed that compound S8 could inhibit the growth of M. fructicola' s hyphae in a time- and concentration-dependent manner, and compound S8 could induce the shrinkage of hyphae, disrupt the integrity of the plasma membrane, and cause the damage and leakage of cell contents. More than that, compound S5 also demonstrated an excellent antibacterial effect on Xanthomonas oryzae (X. oryzae), with a MIC90 value of 1.56 µg/mL, which was superior to the positive control, thiodiazole copper.


Assuntos
Oryza , Quinolinas , Xanthomonas , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Benzotiazóis/farmacologia , Cobre/farmacologia , Dissulfetos/farmacologia , Testes de Sensibilidade Microbiana , Oryza/microbiologia , Doenças das Plantas/microbiologia , Piridinas/farmacologia , Pirimidinas/farmacologia , Quinolinas/farmacologia , Relação Estrutura-Atividade , Ácidos Sulfínicos , Tiofanato , Tiofenos/farmacologia
20.
Angew Chem Int Ed Engl ; 61(40): e202208180, 2022 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-35882626

RESUMO

Sustainable carbon dots (CDs) based on furfuraldehyde (F-CD) resulted in a photosensitive material after pursuing the Alder-Longo reaction. The porphyrin moiety formed connects the F-CDs in a covalent organic network. This heterogeneous material (P-CD) was characterized by XPS indicating incorporation of the respective C, N and O moieties. Time resolved fluorescence including global analysis showed contribution of three linked components to the overall dynamics of the excited state. Electrochemical and photonic properties of this heterogeneous material facilitated photopolymerization in a photo-ATRP setup where either CuBr2 /TPMA, FeBr3 /Br- or a metal free reaction setup activated controlled polymerization. Chain extension experiments worked in all three cases showing end group fidelity for activation of controlled block copolymerization using MMA and styrene as monomers. Traditional radical polymerization using a diaryl iodonium salt as co-initiator failed.

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