RESUMEN
The copper-cobalt metal oxide composite magnesium oxide catalyst loaded with Ru has achieved the aerobic oxidation of 5-hydroxymethylfurfural (HMF) to the bio-based polyester monomer 2,5-furandicarboxylic acid (FDCA) under base-free conditions. Several Ru/Cu-Co-O·MgO catalysts were prepared, with Cu-Co-O being a combination of CuO and Co3O4. The catalyst's activity was boosted by the synergistic interaction between copper and cobalt, as well as an optimal copper-to-cobalt molar ratio. Optimal catalytic activity was observed in the Ru4/Cu1-Co1-O·MgO catalyst, loaded with 4 wt% Ru when copper-to-cobalt molar ratio of 1:1 and magnesium oxide compounding amount of 6 mmol were employed. The inclusion of MgO and the load of Ru not only expanded the specific surface area of the catalyst but also heightened its basicity. Additionally, the presence of loaded Ru improved the catalyst's reducibility at low temperatures. In aqueous solution under oxygen pressure, the conversion rate of HMF achieved 100%, and the yield of FDCA was 86.1%. After five reaction cycles, examining the catalyst and solution revealed that Ru nanoparticles resisted leaching or oxidation, and MgO exhibited only slight dissolution. The green separation of the product was achieved using semi-preparative liquid chromatography, selectively collecting the FDCA-containing solution by exploiting variations in interactions between solutes and the stationary/mobile phases. The subsequent steps involved rotary evaporation and drying, resulting in FDCA powder with a purity exceeding 99%. Notably, this approach eliminated the need to introduce concentrated hydrochloric acid into the system for FDCA separation, providing a novel method for synthesising powdered FDCA.
RESUMEN
Negative-tone photosensitive polyimides (PSPIs) with a low coefficient of thermal expansion (CTE) were prepared by dissolving polyimide precursor-poly(amide ester) (PAE) resins, photoinitiators, photocrosslinkers and other additives in organic solvents. Using triamine as a monomer and dianhydride and diamine as polycondensates, tri-branched structure PAE resins with different molecular weights named PAE-1~5 were prepared. A series of corresponding PSPI films named PSPI-1~5 were prepared from PAE-1~5 resins with the same formulation, respectively. The PSPI-1~5 films prepared from resins of this structure have excellent mechanical, thermal and electrical properties after being thermally cured at 350 °C/2 h in nitrogen. The PSPI-1~5 films' coating solution also show good photolithographic performance and are able to obtain photolithographic patterns with a resolution of about 10 µm after homogenization, exposure and development. Among the PSPI-1~5 films, PSPI-2 has the most excellent lithographic properties with a weight average molecular weight (Mw) of 2.9 × 104 g/mol, a CTE of 41 ppk/°C, a glass transition temperature (Tg) of 343 °C and a 5% weight loss temperature (Td5) of 520 °C, making it suitable for industrial scale-up. The mechanical properties of elongation at breakage of 42.4%, tensile moduli of 3.4 GPa and tensile strength of 153.7 MPa were also measured.
RESUMEN
Currently, near-infrared (NIR) light-emitting materials have been widely used in many fields, such as night vision, bioimaging, and nondestructive analysis. However, it is difficult to achieve multifunction in certain NIR light emitting phosphor. Herein, we propose a new near-infrared phosphor Mg3Ga2GeO8:Cr3+,Ni2+ that can be applied to at least three fields, i.e., identification of compounds, temperature sensing, anticounterfeiting, and other applications. The multifunctional material exhibited efficient broadband emission of 650-1650 nm under 420 nm excitation. The emission intensity of Ni2+ in Mg3Ga2GeO8:Cr3+,Ni2+ is enhanced by two times compared with that of Ni2+ in Mg3Ga2GeO8:Ni2+ due to the energy transfer process. Compared with phosphor single doped with Ni2+, Mg3Ga2GeO8:Cr3+,Ni2+ is more convincing in organic compound recognition because it is based on two emission bands: 600-1100 nm and 1100-1650 nm. As a temperature sensor, Mg3Ga2GeO8:Cr3+,Ni2+ is an ideal temperature-sensing material. This work not only provides a super broadband NIR emitting phosphor with multiple functions but also presents a practical approach for the development of high-efficiency and multifunctional NIR phosphors.
RESUMEN
Insufficient attention has been given to the recycling of excess urea despite its potential detrimental effects on soil nutrient equilibrium, geological structure, and crop health. In this study, corncob-derived porous biochar (CPB), which is rich in surface functional groups, was prepared from biomass corncob in two steps as an adsorbent to remove urea from wastewater. Compared with the typical carbonization and activation processes, this process resulted in a higher yield of CPB and an ultrahigh adsorption capacity for urea. Response surface analysis was utilized to determine the optimal carbonization conditions, which were found to be 500 °C for 6 h with a heating rate of 15 °C/min. The exceptional adsorption capability of CPB can be ascribed to its porous structure and significant presence of oxygen-containing functional groups, which facilitate a synergistic interaction of physisorption and chemisorption. This adsorption phenomenon aligns with the Harkins-Jura isotherm model and adheres to pseudo-second order kinetics. CPB demonstrates potential as an adsorbent for the elimination of urea from wastewater in an economical and effective fashion.
RESUMEN
Body weight of chicken is a typical quantitative trait, which shows phenotypic variations due to selective breeding. Despite some QTL loci have been obtained, the body weight of native chicken breeds in different geographic regions varies greatly, its genetic basis remains unresolved questions. To address this issue, we analyzed 117 Chinese indigenous chickens from 10 breeds (Huiyang Bearded, Xinhua, Hotan Black, Baicheng You, Liyang, Yunyang Da, Jining Bairi, Lindian, Beijing You, Tibetan). We applied fixation index (FST) analysis to find selected genomic regions and genes associated with body weight traits. Our study suggests that NELL1, XYLT1, and NCAPG/LCORL genes are strongly selected in the body weight trait of Chinese indigenous chicken breeds. In addition, the IL1RAPL1 gene was strongly selected in large body weight chickens, while the PCDH17 and CADM2 genes were strongly selected in small body weight chickens. This result suggests that the patterns of genetic variation of native chicken and commercial chicken, and/or distinct local chicken breeds may follow different evolutionary mechanisms.
Asunto(s)
Pollos , Animales , Peso Corporal/genética , Pollos/genética , Genómica , Metagenómica , Polimorfismo de Nucleótido Simple , China , Selección Artificial/genéticaRESUMEN
With rapid industrial development, the massive generation of nitrogenous wastewater poses a serious threat to both human beings and the ecosystem. Bio-based adsorbents are considered promising adsorption materials for many applications. However, their complex preparation procedures, large energy consumption, and difficulty of microstructure control hinder their practical applications. In this study, a new corncob-derived porous adsorbent (CPA) with excellent urea adsorption capacity in wastewater was prepared by the one-step hydrothermal process. The effects of the hydrothermal process conditions on the urea adsorption capacity of the CPA were evaluated and optimized using the response surface methodology, and a kinetic analysis of the CPA was also carried out. Our findings showed that the adsorption process of urea by the adsorbent followed the Langmuir isotherm and pseudo-second-order kinetic models. The high adsorption capacity for urea was attributed to the abundant porous structure and the hydrogen bonds formed between the adsorbent and the amine group in urea, which made it more conducive to the adsorption of urea. Therefore, we believe that CPA could be a promising adsorbent for urea removal in wastewater.
RESUMEN
Background: Plastic bronchitis (PB) is a rare and severe lung disease. It can be triggered by influenza virus infection, which is a common respiratory infection in children. Bronchoscopy can aid in the early detection and treatment of PB. However, the outcomes and risk for PB development in pediatric patients with influenza virus infection are not fully understood. Methods: Data from 321 children diagnosed with influenza virus pneumonia who underwent bronchoscopy examinations between 1st January, 2009 and 31st December, 2020 were retrospectively analyzed to assess the outcomes and risk factors associated with PB development. Results: This study included 97 girls and 224 boys with influenza virus pneumonia with a median age of 42 months. Among them, 36 patients (11.2%) were categorized as having PB based on bronchoscopy findings. PB patients had significantly longer fever durations (p=0.010) and higher risks of developing severe conditions including respiratory failure (p<0.001), acute respiratory distress syndrome (p<0.001), and air-leak syndrome (p<0.001) compared to non-PB patients. Conventional treatment including the use of neuraminidase inhibitors and antibiotics did not differ between the PB and non-PB patients, but PB patients required more anti-inflammatory treatment (p=0.019) and ventilator support (p<0.001). Combined univariate and multivariate analyses suggested that radiographic findings, including mediastinal emphysema (p=0.012) and lung consolidation (p=0.012), as well as increased levels of neutrophils (p=0.026), aspartate aminotransferase (p=0.004), and lactate dehydrogenase (p<0.001), were identified as risk factors for PB development in patients with influenza virus pneumonia. Although PB patients required more intensive care and had longer hospital stays, they all recovered well after treatment. Conclusion: Influenza virus infection is linked to PB development in children. Identifying risk factors and early intervention such as bronchoscopy can improve the prognosis of children with PB.
RESUMEN
Poly (hexamethylene succinate) (PHS) is a biobased and biodegradable polyester. In this research, two fully biobased high-molecular-weight poly (hexamethylene succinate-co-2,5-furandicarboxylate) (PHSF) copolyesters with low hexamethylene furandicarboxylate (HF) unit contents (about 5 and 10 mol%) were successfully synthesized through a two-step transesterification/esterification and polycondensation method. The basic thermal behavior, crystal structure, isothermal crystallization kinetics, melting behavior, thermal stability, and tensile mechanical property of PHSF copolyesters were studied in detail and compared with those of PHS. PHSF showed a decrease in the melt crystallization temperature, melting temperature, and equilibrium melting temperature while showing a slight increase in the glass transition temperature and thermal decomposition temperature. PHSF copolyesters displayed the same crystal structure as PHS. Compared with PHS, PHSF copolyesters showed the improved mechanical property. The presence of about 10 mol% of HF unit increased the tensile strength from 12.9 ± 0.9 MPa for PHS to 39.2 ± 0.8 MPa; meanwhile, the elongation at break also increased from 498.5 ± 4.78% to 1757.6 ± 6.1%.
RESUMEN
INTRODUCTION: Lobaplatin is a new platinum-based cytotoxic chemotherapeutic agent. Endostar is an endogenous angiogenic inhibitor with implicated anti-tumor activity. This study was to investigate the efficacy and safety of thoracic perfusion of lobaplatin combined with endostar in the treatment of malignant pleural effusions (MPE). METHODS: We searched the databases of Pubmed, the Cochrane Library, Embase, WanFang Data, and CNKI to select the studies regarding the efficacy and safety of lobaplatin combined with endostar to treat MPE. A total of 10[3-12] randomized controlled trials with 651 patients were included. RESULTS: The objective response rate (P < .001, odds ratio = 4.08) and disease control rate (P < .001, odds ratio = 3.69) of lobaplatin combined with endostar were significantly higher than lobaplatin alone. In addition, lobaplatin combined with endostar remarkably promoted the quality of life of patients (P < .001, odds ratio = 3.93) compared with lobaplatin alone. Lobaplatin combined with endostar also promoted the quality of life of patients (P < .05, odds ratio = 2.56) compared with cisplatin combined with endostar. At the same time, the leukopenia rate (P < .05, odds ratio = .40) and the incidence of nausea and vomiting (P < .05, odds ratio = .38) of lobaplatin combined with endostar were significantly lower than that of cisplatin combined with endostar. CONCLUSIONS: The efficacy of lobaplatin combined with endostar was superior to lobaplatin alone. The safety was higher than cisplatin combined with endostar through thoracic perfusion in treating MPE, which indicated that lobaplatin combined with endostar could be the effective agent for controlling MPE.
Asunto(s)
Derrame Pleural Maligno , Inhibidores de la Angiogénesis/uso terapéutico , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapéutico , Cisplatino/uso terapéutico , Ciclobutanos , Endostatinas , Humanos , Compuestos Organoplatinos , Perfusión , Derrame Pleural Maligno/tratamiento farmacológico , Derrame Pleural Maligno/patología , Calidad de Vida , Ensayos Clínicos Controlados Aleatorios como Asunto , Proteínas RecombinantesRESUMEN
Public concerns on microplastic (MP) pollution and its prevalence in urban runoff have grown exponentially. Huge amounts of MPs are transported from urban environments via surface runoff to different environment compartments, including rivers, lakes, reservoirs, estuaries, and oceans. The global concentrations of MPs in urban runoff range from 0 to 8580 particles/L. Understanding the sources, abundance, composition and characteristics of MPs in urban runoff on a global scale is a critical challenge because of the existence of multiple sources and spatiotemporal heterogeneity. Additionally, dynamic processes in the mobilization, aging, fragmentation, transport, and retention of MPs in urban runoff have been largely overlooked. Furthermore, the MP flux through urban runoff into rivers, lakes and even oceans is largely unknown, which is very important for better understanding the fate and transport of MPs in urban environments. Here, we provide a critical review of the global occurrence, transport, retention process, and sinks of MPs in urban runoff. Relevant policies, regulations and measures are put forward. Future global investigations and mitigation efforts will require us to address this issue cautiously, cooperating globally, nationally and regionally, and acting locally.
Asunto(s)
Microplásticos , Contaminantes Químicos del Agua , Plásticos , Monitoreo del Ambiente , Contaminantes Químicos del Agua/análisis , RíosRESUMEN
Microplastic (MP), an emerging contaminant, is globally prevalent and poses potential environmental threats and ecological risks to both aquatic and terrestrial ecosystems. When MPs enter into natural environments, they may serve as artificial substrates for microbial colonization and plastisphere formation, providing new ecological niches for microorganisms. Recent studies of the plastisphere have focused on aquatic ecosystems. However, our understanding of the soil plastisphere e.g. its formation process, microbial ecology, co-transport of organic pollutants and heavy metals, and effects on biogeochemical processes is still very limited. This review summarizes latest methods used to explore the soil plastisphere, assesses the factors influencing the microbial ecology of the soil plastisphere, and sheds light on potential ecological risks caused by the soil plastisphere. The formation and succession of soil plastisphere communities can be driven by MP characteristics and soil environmental factors. The soil plastisphere may affect a series of ecological processes, especially the co-transport of environmental contaminants, biodegradation of MPs, and soil carbon cycling. We aim to narrow the knowledge gap between the soil and aquatic plastisphere, and provide valuable guidance for future research on the soil plastisphere in MP-contaminated soils.
Asunto(s)
Plásticos , Suelo , Biodegradación Ambiental , Ecosistema , Microplásticos , Suelo/químicaRESUMEN
Introduction: Surgeons have widely regarded sternotomy (ST) as the standard surgical method for thymectomy. Minimally invasive methods for thymectomy, including video-assisted and robot-assisted thoracoscopic surgery (RATS), have been explored. There are some studies have researched and compared the outcomes of patients after robotic and sternotomy procedure. Methods: We searched the databases of Pubmed, the Cochrane Library, Embase and selected the studies on the efficacy and safety of RATS or ST for thymectomy. Meta-analysis was performed for operation time, operation blood loss, postoperative drainage time, operative complications and hospitalization time. Results: A total of 16 cohort studies with 1,089 patients were included. Compared to ST, RATS is an appropriate alternative for thymectomy which reduced operation blood loss [standardized mean difference (SMD) = -1.82, 95% confidence interval (95% CI): (-2.64, -0.99), p = 0.000], postoperative drainage time [SMD = -2.47, 95% Cl: (-3.45, -1.48), p = 0.000], operative complications [odds ratio (OR) = 0.31, 95% Cl: (0.18, 0.51), p = 0.000] and hospitalization time [SMD = -1.62, 95% Cl: (-2.16, -1.07), p = 0.000]. Conclusions: This meta-analysis based on cohort studies shows that RATS has more advantages over ST. Therefore, RATS is a more advanced and suitable surgical method for thymectomy.
RESUMEN
Periphytic biofilms have been widely used in wastewater purification and water ecological restoration, and artificial substrates have been progressively used for periphyton immobilisation to substitute natural substrates. However, there is insufficient knowledge regarding the interaction network structure and microbial functions in biofilm communities on artificial substrates, which are essential attribute affecting their applications in biofilm immobilisation. This study compared the community structure, co-occurrence network, and metabolic functions of bacterial and microeukaryotic periphytic biofilms during a 35-day indoor cultivation on artificial substrates, such as artificial carbon fibre (ACF) and polyvinyl chloride (PVC), and natural substrates, such as pebble and wood. Results demonstrated that different types of artificial substrates could affect the community composition and functional diversity of bacterial and microeukaryotic biofilms. The bacterial and microeukaryotic community on ACF and PVC showed significantly higher Simpson index compared to those on wood. Bacterial networks on artificial substrates were more complex than those on natural substrates, while the keystone species on natural substrates were more abundant, indicating that the bacterial communities on artificial substrates had stronger stability and resistance to external interference. Furthermore, the functional metabolic profiles predicted showed the abilities of bacterial communities to metabolise nitrogen and carbon sources colonised on artificial substrates were stronger than those on natural substrates. These findings demonstrated that artificial substrates could be special niches for microbial colonisation, possibly altering microbial compositions, interactions, and functions. Therefore, this study provides a powerful theoretical basis for choosing suitable artificial substrates for microbial aggregation and immobilisation technology.
RESUMEN
Concerns are growing about the increasing amounts of microplastics (MPs) and their ecological impacts, especially the influences of "plastisphere" in the freshwater ecosystems. Although the microbial structure and composition of biofilms are investigated, knowledge of their microbial functions remains limited. Herein, we investigated the functional diversity of carbon metabolism in biofilms colonizing one inert (glass) and two MPs as polyvinyl chloride (PVC) and polyethylene terephthalate (PET) substrates incubated for 44 days in situ in the Niushoushan River, the Qinhuai River, and Donghu Lake. 2D confocal laser scanning microscopy images visualized distinct micro-structures and biofilm compositions on three substrates. BIOLOG ECO microplates indicated variation on carbon utilization capacities of biofilms of inert and MPs in three freshwater ecosystems. Biofilms on PET showed lower capacities and carbon metabolism rates than those on glass and PVC, indicating the presence of substrate-specific functional diversity. The Shannon-Wiener diversity, Simpson diversity and Shannon evenness indices for the Niushoushan River and Donghu Lake were ordered as glass > PVC > PET. Besides to MPs-specific factors, environmental factors including nutrient (i.e., TN and TP) and turbidity largely shaped biofilm carbon metabolism. Overall findings demonstrated that as specific niches, MPs influenced microbial-mediated carbon cycling in the freshwater ecosystems and MPs-promoted microbial communities posed ecological significance.
Asunto(s)
Microplásticos , Contaminantes Químicos del Agua , Biopelículas , Plásticos , Ríos , Contaminantes Químicos del Agua/análisisRESUMEN
As an artificial type of microbial carrier, plastic debris has been widely detected in freshwater habitats, and the potential impacts of the plastisphere (biofilms colonized on plastics) in aquatic ecosystems have drawn increasing attention. Distinct community compositions and structures of biofilms in plastic and natural substrates have been recorded in freshwater environments. However, the microbial metabolic functioning of the plastisphere was underestimated, especially in freshwater environments. In this study, the effects of substrate types on the carbon metabolic functions of biofilms were studied by in situ cultivation of biofilms on plastics (polyvinyl chloride, PVC and polyethylene, PE) and natural substrate (cobblestone) for 44 days in two rivers (the Niushoushan River and the Qinhuai River) and two lakes (Donghu Lake and Xuanwu Lake). Biofilms on plastics showed higher biomasses than those on natural substrates in all ecosystems. Variations in the micro-structure and compactness of biofilms developed under different substrates were observed from scanning electron microscope and confocal laser scanning microscope image analyses. The carbon metabolic activities of the biofilms evaluated by BIOLOG EcoPlate were different between plastics (PVC and PE) and natural substrate (cobblestone) in the four freshwater ecosystems. In the Niushoushan River, PE-associated biofilms had different capacity in using carbon sources from cobblestone-associated biofilms as illustrated by the Shannon-Wiener diversity index and Shannon evenness index. Additionally, the metabolic functional diversity profiles of biofilms on PVC were significantly different from those on cobblestone in the other three aquatic ecosystems. Moreover, results from variation partitioning analysis suggested that the impact of environmental factors (contribution: 21%) on microbial carbon metabolic functions was much greater than that of substrate types (contribution: 6%). These findings illustrated distinct microbial functions of biofilms inhabited on plastics, and environmental factors play a decisive role in the differentiation and specificity of carbon metabolism of the plastisphere. This study offers new insights that plastics serving as artificial microbial niches have the ability to affect the microbial-mediated carbon cycling process in aquatic ecosystems.
Asunto(s)
Carbono , Plásticos , Biopelículas , Ecosistema , RíosRESUMEN
Remediation of soil heavy metal by biochar has been extensively studied. However, few studies focused on the role of biochar on the co-immobilization of cadmium (Cd(II)) and arsenate (As(V)) and related soil nutrient availability. Remediation tests were conducted with three types of pristine and ferric trichloride (FeCl3) modified biochar (rice, wheat, and corn straw biochar) in Cd-As co-contaminated soil, with application rates of 1, 5, and 10% (w/w) and the incubation of 1, 7, 10, and 15 days. Using TCLP (Toxicity Characteristic Leaching Procedure) method, 10% of FeCl3 modified corn-straw derived biochar (FCB) had the highest immobilization efficiency of Cd(II) (63.21%) and As(V) (95.10%) after 10 days of the incubation. Iron-modified biochar immobilized higher fractions of water-soluble (F1) and surface-absorbed (F2) metal fractions than pristine biochar. For FCB amendment, Cd was mostly presented in the organic matter (OM) and sulfides associated (F4) and residual (F5) fractions (88.52%), as was found in the Fe-Al (oxides and hydroxides) (F3), F4, and F5 fractions (75.87%). FCB amendment increased soil pH values and available iron contents (p < 0.05), while no changes in soil available phosphorus content (p > 0.05). This study showed that FCB application reduces the environmental mobility of metals in Cd-As contaminated soil, while it also increases soil pH and available nutrient mobility, improving soil environmental quality and reducing remediation costs.
Asunto(s)
Arsénico/aislamiento & purificación , Cadmio/aislamiento & purificación , Carbón Orgánico , Hierro , Contaminantes del Suelo/aislamiento & purificación , SueloRESUMEN
A group of 3'-epi-neoponkoranol analogs with different hydrophobic substituents attached at 3'-position of side chain moiety were designed and synthesized in order to further improve the inhibitory activities against α-glucosidases. Biological evaluation of these compounds revealed that sulfonium salts attached with ortho-substituted benzyl groups showed best α-glucosidase inhibitory activities. The most potent compound 10i showed greater inhibitory activities than all natural products. Moreover, docking studies on 10i with ntMGAM presented a new binding mode, indicating that amino residue Asp542 should be the key interacting point for strong inhibitory activity of small molecules against α-glucosidase enzymes. The strongest α-glucosidase inhibitory activity of 10i could be rationalized by van der Waals interactions between the 3'-attached substituent and particularly the ortho-substituted trifluoromethyl on benzyl group with the adjacent hydrophobic amino residues. Cytotoxicity evaluation assay demonstrated a high level of safety profile of the synthesized sulfonium salts against normal cell line. The enzyme kinetic studies showed a fully competitive inhibition of these sulfonium salts on each α-glucosidase.
Asunto(s)
Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Alcoholes del Azúcar/química , Alcoholes del Azúcar/farmacología , Tiofenos/química , Tiofenos/farmacología , alfa-Glucosidasas/metabolismo , Compuestos de Bencilo/síntesis química , Compuestos de Bencilo/química , Compuestos de Bencilo/farmacología , Línea Celular , Diseño de Fármacos , Inhibidores de Glicósido Hidrolasas/síntesis química , Humanos , Simulación del Acoplamiento Molecular , Relación Estructura-Actividad , Alcoholes del Azúcar/síntesis química , Tiofenos/síntesis químicaRESUMEN
A novel synthetic approach to construct various 3,6-anhydrohexosides via an intramolecular cyclization of corresponding triflates is described. The nucleophilic attack from C3 p-methoxybenzylated hydroxyl to C6 trifluoromethanesulfonate on triflate structures triggered the cyclization reaction to provide 3,6-anhydrohexosides in excellent yields, making the strategy more efficient with respect to the reported protocols. By applying this methodology, a concise first total synthesis of natural product isolated from leaves of Sauropus rostratus was accomplished.
Asunto(s)
Productos Biológicos/síntesis química , Glicósidos/síntesis química , Phyllanthus/química , Productos Biológicos/química , Catálisis , Técnicas Químicas Combinatorias , Cristalografía por Rayos X , Ciclización , Glicósidos/química , Conformación Molecular , Estructura Molecular , Hojas de la Planta/química , EstereoisomerismoRESUMEN
A series of novel hybrids from natural product oridonin and nitrogen mustards were designed and synthesized to obtain more efficacious and less toxic antitumor agents. The antiproliferative evaluation showed that most conjugates were more potent than their parent compounds oridonin and clinically used nitrogen mustards against four human cancer cell lines (K562, MCF-7, Bel-7402, and MGC-803). Furthermore, the representative compounds 16a-c exhibited antiproliferative activities against the multidrug resistant cell lines (SW620/AD300 and NCI-H460/MX20). It was shown that the most effective compound 16b possesses a strong inhibitory activity with an IC50 value 21-fold lower than that of oridonin in MCF-7 cells and also exhibits selective cytotoxicity toward the cancer cells. Intriguingly, compound 16b has been demonstrated to significantly induce apoptosis and affect cell cycle progression in human hepatoma Bel-7402 cells.
RESUMEN
In an effort to develop novel potent antitubercular drugs, thirty-one oridonin derivatives were designed and prepared. All the compounds obtained were screened for their in vitro activities against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Among them, thirteen compounds showed significant inhibitory activity against M. phlei with MICs less than 2 µg/mL. Compounds 2k, 8d, 10c, 10d containing trans-cinnamic acid moiety were the most potent (MIC=0.5 µg/mL), comparable to the well-known antitubercular drug streptomycin. The preliminary structure-activity relationships (SARs) were also analyzed.