Design, synthesis and antimycobacterial activity of novel nitrobenzamide derivatives

We report herein the design and synthesis of a series of novel nitrobenzamide derivatives. Results reveal that many of them display considerable in vitro antitubercular activity. Four N-benzyl or N-(pyridine-2-yl)methyl 3,5-dinitrobenzamides A6, A11, C1 and C4 have not only the same excellent MIC values of 1500), opening a new direction for further development

Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives

We report herein the design and synthesis of a series of novel Sinefungin (SIN) derivatives, based on the structures of SIN and its analogue EPZ004777. Our results reveal that target compounds 1ad-af, 1ba-bb and 1bf-bh show better activity (IC50 = 4.56–20.16 μM) than EPZ004777 (IC50 = 35.19 μM). Surprisingly, SIN was founded to be not as active (IC50 > 50 μM) as we and other research groups predicted. Interestingly, the intermediates 9a-b and 11b display potent anti-ZIKV potency (IC50 = 6.33–29.98 μM), and compound 9a also exhibits acceptable cytotoxicity (CC50 > 200 μM), suggesting their promising potential to be leads for further development

Energy Demand and Carbon Emission Peak Paths for the Rise of Central China

Energy revolution is essential for the coordinated and sustainable development of economy, society, and the environment, and it should coordinate with regional development strategies. Using the Kaya identity, this study categorizes the energy consumption demand brought by the rise of Central China into production and living demand. Energy demand scenarios for the rise of Central China are constructed considering factors such as gross domestic product, industrial structure, urbanization, energy efficiency, per capita income, and residential energy. Accordingly, the low-carbon development paths under energy revolution are analyzed. Urbanization and industrialization will promote the total energy demand in the five provinces in Central China up to 8.4×108–1.01×109 tce in 2035. Moreover, the establishment of a diversified energy supply system can help achieve low-carbon emission, energy security, and efficient utilization of energy; a carbon emission peak is expected to reach before 2030. China should vigorously develop technologies regarding energy conservation and clean and renewable energies. A multi-energy complementary system should be established in China by optimizing the industrial structure, and the existing energy system should be reformed to realize energy cooperation among regions

Introducing a novel and natural antibiotic for the treatment of oral pathogens: Abelmoschus esculentus green-formulated silver nanoparticles

Nanotechnology can solve many biomedical problems and cause transformation in the field of health and pharmaceuticals. The use of this technology in removing pathogenic bacteria is of great interest. The introduction of a strong antibacterial agent is very important to control pathogenic bacteria, especially strains resistant to antibiotics. The aim of this research was to synthesize silver nanoparticles (AgNPs) with the help of Abelmoschus esculentus aqueous extract and investigate its antibacterial properties against oral pathogens. Our study examined the ability of AgNPs to inhibit the dental bacterial growth and anti-adherence in vitro. The biosynthesized AgNPs@Abelmoschus esculentus were characterized by FT-IR, UV–Vis, and SEM tests. The physical and chemical investigation of the synthesized AgNPs showed that the particles were produced in nano dimensions, spherical shape, and without any impurities. In antibacterial test, the 8 µg/mL exhibited the lowest minimum inhibitory concentrations (MICs) against Porphyromonas gingivalis and Streptococcus mutans (MIC = 8 µg/mL). In vitro adherence of S. mutans was significantly prevented by AgNPs@Abelmoschus esculentus (MIC = 8–16 µg/mL). According to the results, the AgNPs@Abelmoschus esculentus may be good candidates for the oral hygiene agents to prevent periodontopathic conditions and dental caries

Interaction and energy transfer between carbon dots and serum human transferrin

<p>Human serum transferrin has been used as a potential drug carrier to transport anticancer drugs to tumor cells, where transferrin receptors are overexpressed on the surface. Carbon dots are biocompatible, and have potential application to drug delivery. The interaction mechanism of human serum transferrin with carbon dots was investigated by fluorescence spectra, ultraviolet–visible absorption spectroscopy, circular dichroism, at extracellular pH 7.4 and endosomal pH 4.8, at varying temperatures. We observed a quenching of fluorescence of human serum transferrin in the presence of carbon dots by a static quenching mechanism and also analyzed the quenching results using the Stern–Volmer equation and obtained high-affinity binding to human serum transferrin dominated by hydrogen bonds or van der Waals forces. An isoemissive point was seen, indicating that quenching of human serum transferrin depends on the formation of human serum transferrin–carbon dots complex. Binding distance between carbon dots and human serum transferrin substantiated that the photoinduced electron transfer and Föster nonradiative resonance energy transfer mechanism were also involved in the quenching of protein. Furthermore, the circular dichroism also showed that carbon dots changed the secondary structure of human serum transferrin to some extent with decreased <i>α</i>-helix content or peak wavelength red-shifted. This study provides some theoretical foundation for carbon dots as a promising probe to monitor the process of delivering drugs to human serum transferrin in the future.</p

Consumption of Bt Maize Pollen Containing Cry1Ie Does Not Negatively Affect Propylea japonica (Thunberg) (Coleoptera: Coccinellidae)

Propylea japonica (Thunberg) (Coleoptera: Coccinellidae) are prevalent predators and pollen feeders in East Asian maize fields. They are therefore indirectly (via prey) and directly (via pollen) exposed to Cry proteins within Bt-transgenic maize fields. The effects of Cry1Ie-producing transgenic maize pollen on the fitness of P. japonica was assessed using two dietary-exposure experiments in the laboratory. In the first experiment, survival, larval developmental time, adult fresh weight, and fecundity did not differ between ladybirds consuming Bt or non-Bt maize pollen. In the second experiment, none of the tested lethal and sublethal parameters of P. japonica were negatively affected when fed a rapeseed pollen-based diet containing Cry1Ie protein at 200 μg/g dry weight of diet. In contrast, the larval developmental time, adult fresh weight, and fecundity of P. japonica were significantly adversely affected when fed diet containing the positive control compound E-64. In both experiments, the bioactivity of the Cry1Ie protein in the food sources was confirmed by bioassays with a Cry1Ie-sensitive lepidopteran species. These results indicated that P. japonica are not affected by the consumption of Cry1Ie-expressing maize pollen and are not sensitive to the Cry1Ie protein, suggesting that the growing of Bt maize expressing Cry1Ie protein will pose a negligible risk to P. japonica

The effect of intravenous lidocaine on postoperative cognitive dysfunction: a systematic review and meta-analysis

Abstract Background Postoperative cognitive dysfunction (POCD) has been reported as a significant complication in elderly patients. Various methods have been proposed for reducing the incidence and severity of POCD. Intravenous lidocaine administration has been reported in the literature to reduce POCD, but the effect of lidocaine remains controversial. Methods We screened Medline, Embase, Cochrane Library, and China National Knowledge Infrastructure (up to April 2022) databases following a search strategy for intravenous lidocaine on POCD. We also screened related bibliographies on lidocaine for POCD. Ten articles comprising 1517 patients were selected and analyzed. We divided the postoperative follow-up period as follows: short term (90 days). Outcomes We found that lidocaine could attenuate the overall incidence of POCD, especially in the short term. There were no differences between lidocaine and placebo on the overall severity of POCD. Conclusion Lidocaine administered intravenously could attenuate the overall incidence of POCD and its severity in the short term

Effect of Phosphorus, Iron, Zinc, and Their Combined Deficiencies on Photosynthetic Characteristics of Rice (<i>Oryza sativa</i> L.) Seedlings

Combined elemental deficiencies are more complex and insidious physiological metabolic responses than single elemental stresses. To determine the effects of phosphorus (P), iron (Fe), zinc (Zn), and their deficient combinations on photosynthetic characteristics of rice seedlings, we investigated their effects on dry weight, chlorophyll (Chl) content, rapid photosynthetic carbon assimilation CO2 responses, and Chl fluorescence in four-week-old rice (CB9 and BJ1 cultivars) seedlings. The results showed that the dry matter, maximum carboxylation efficiency (Vc,max), and maximum electron transfer efficiency (Jmax) of seedlings were all reduced to different degrees under the element deficiency treatments. JIP-test analysis showed that the decrease in the concentration of active PSII reaction centers (RC/ABS) under -Zn treatment was the main reason for the inhibition of performance index PIABS. The -P treatment reduced RC/ABS and inhibited electron transfer (ψEo). Primary photochemical reactions (φPo) of -P-Zn treated seedlings were also inhibited compared to the -P treatment. The -Fe and -Fe-Zn treatments inhibited photosynthesis most severely, which not only reduced RC/ABS but also severely inhibited φPo and ψEo. Notably, the -P-Fe and -P-Fe-Zn treatments of the CB9 improved the RC/ABS, alleviating the limitation of Fe deficiency. These results help enhance the understanding of the complex relationship between nutrient balance and photosynthesis, especially for P, Fe, Zn, and their combined deficiency