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Plant-derived extracellular vesicles (PDEVs) are lipid bilayer nanoparticles, naturally produced by plant cells, with sizes ranging from 50 to 500 nm. Recent studies have highlighted their great potential in the biotechnological and medical fields, due to their natural origin, high biocompatibility and intrinsic therapeutic properties. PDEVs contain a complex biological cargo of proteins, lipids, nucleic acids and secondary metabolites, including antioxidants and anti-inflammatory molecules, making them ideal for biomedical applications such as drug delivery. These vesicles play a key role in intercellular communication and gene regulation, proving to be particularly promising in personalized medicine. Recent studies have highlighted their ability to improve drug stability and bioavailability, optimizing targeted release and minimizing side effects. Despite some challenges, such as compositional variability and the need for standardized protocols, PDEVs are at the gunsight of innovative research aimed at improving their loading capacity and therapeutic specificity. This review aims to provide a comprehensive overview of PDEVs, exploring their structure, isolation methods, functional characteristics, and applications, highlighting their advantages over synthetic nanoparticles and animal-derived extracellular vesicles, leading to an innovative and sustainable solution for the development of new therapeutic approaches. [ABSTRACT FROM AUTHOR]

Background: This research centers on the development and spectroscopic characterization of new quinazolin-4(3H)-one-isoxazole derivatives (5a–e). The aim was to investigate the regioselectivity of the 1,3-dipolar cycloaddition involving arylnitriloxides and N-propargylquinazolin-4(3H)-one, and to assess the antioxidant properties of the synthesized compounds. The synthetic approach started with the alkylation of quinazolin-4(3H)-one using propargyl bromide, followed by a 1,3-dipolar cycloaddition reaction. Methods: The structural identification of the products was performed using various spectroscopic methods, such as IR, 1H, 13C, and HMBC NMR, HRMS, and single-crystal X-ray diffraction. To further examine the regioselectivity of the cycloaddition, Density Functional Theory (DFT) calculations at the B3LYP/6-31G(d) level were employed. Additionally, the antioxidant potential of the compounds was tested in vitro using DPPH (2,2-Diphenyl-1-picrylhydrazyl)radical scavenging assays. The reaction selectively produced 3,5-disubstituted isoxazoles, with the regiochemical outcome being independent of the substituents on the phenyl ring. Results: Theoretical calculations using DFT were in agreement with the experimental results, revealing activation energies of −81.15 kcal/mol for P-1 and −77.32 kcal/mol for P-2, favoring the formation of P-1. An analysis of the Intrinsic Reaction Coordinate (IRC) confirmed that the reaction proceeded via a concerted but asynchronous mechanism. The antioxidant tests demonstrated that the synthesized compounds exhibited significant radical scavenging activity, as shown in the DPPH assay. The 1,3-dipolar cycloaddition of arylnitriloxides with N-propargylquinazolin-4(3H)-one successfully resulted in novel 3,5-disubstituted isoxazoles. Conclusions: The experimental findings were well-supported by theoretical predictions, and the antioxidant assays revealed strong activity, indicating the potential for future biological applications of these compounds. [ABSTRACT FROM AUTHOR]

In this research, we aimed to determine the antioxidant activity of an atomized extract of Cnidoscolus diacanthus (Pax & K. Hoffm.) J.F. Macbr., known in Peru as "huanarpo hembra", and its effect on sex hormone levels. Its phytochemical profile was determined using liquid chromatography–mass spectrometry (LC–MS), while its total phenol content (TPC) and total flavonoids (TFs) were determined using the Folin–Ciocalteu method and the aluminum chloride method. Its antioxidant activity was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH), the radical 2,2-azino-bis-3-ethylbenzthiazolin-6 sulfonic acid (ABTS), and ferric-reducing antioxidant power (FRAP). The biological activity of C. diacanthus and its effect on sexual hormones were determined in Holtzman rats of both sexes. Phytochemical analysis revealed the presence of flavonoids and phenolic compounds in its leaves and stems, mainly rutin, quercetin, chlorogenic acid, and genistein. However, the stem extract contained higher total phenol (464.38 ± 4.40 GAE/g) and flavonoid (369.17 ± 3.16 mg QE/g of extract) contents than the leaf extract (212.38 ± 3.19 mg GAE/g and 121.49 ± 2.69 mg QE/g). For DPPH, ABTS, and FRAP, the Trolox-equivalent antioxidant capacity (TEAC) was 597.20 ± 5.40 µmol/g, 452.67 ± 5.76 µmol/g, and 535.91 ± 1.56 µmol/g, respectively, for the stems, while for the leaves, it was 462.39 ± 3.99 µmol/g, 202.32 ± 5.20 µmol/g, and 198.13 ± 1.44 µmol/g, respectively. In terms of the values for hormonal levels, at a dose of 100 mg/kg of the extract, testosterone levels of 1.430 ng/mL (with the leaf extract) and 1.433 ng/mL (with the stem extract), respectively, were found in the male rats. Regarding estradiol levels, in the female rats, these were 10.425 ng/mL (leaf extract) and 8.775 ng/mL (stem extract), while their levels of luteinizing hormone were 0.320 mIU/mL (leaf extract) and 0.273 mIU/mL (stem extract). For the follicle-stimulating hormone, levels of 0.858 mIU/mL (leaf extract) and 0.840 mIU/mL (stem extract) were found in the female rats, and levels of 0.220 mIU/mL (leaf extract) and 0.200 mIU/mL (stem extract) were found in the male rats. It is concluded that the C. diacanthus stem extract had a greater antioxidant capacity than the leaf extract, while both extracts had a superior effect on the sex hormone levels in the female rats compared to the male rats. [ABSTRACT FROM AUTHOR]

Herein we describe the antioxidant, antimicrobial, antibiofilm, anti-inflammatory and wound-healing potential of aqueous and polysaccharide extracts from three widely appreciated mushrooms: Agrocybe aegerita, Laetiporus sulphureus and Agaricus bisporus. Moreover, we present their detailed phenolic, polysaccharide and protein profiles and ATR-FTIR spectra. The study found that polysaccharide extracts (PEs) from mushrooms had higher total and β-glucan levels than aqueous extracts (AEs), with A. aegerita showing the highest content. L. sulphureus had a higher total protein content, and A. aegerita AE had the highest phenolic content. Our results indicate that all the tested extracts have high potential regarding their bioactive properties, with A. aegerita being the most promising one. Namely, the antibacterial activity assay showed that the development of the skin-infection-causing agent, Staphylococcus aureus, was inhibited with a minimal inhibitory concentration of 4.00 mg/mL and minimal bactericidal concentration of 8.00 mg/mL, while the results regarding wound healing showed that, over the course of 24 h, the A. aegerita extract actively promoted wound closure in the HaCaT keratinocyte cell line model. The anti-inflammatory activity results clearly showed that when we used S. aureus as an inflammation-inducing agent and the A. aegerita aqueous extract in treatment, IL-6 levels reduced to the level of 4.56 pg/mL. The obtained data suggest that the tested mushroom extracts may serve as a source of bioactive compounds, with potential applications in the cosmeceutical, pharmaceutical and food industries. Furthermore, potential skin preparations carefully crafted with mushroom extract may help restore the skin's barrier function, decrease the probability of staph infections and minimize skin irritation. [ABSTRACT FROM AUTHOR]

Background: Cisplatin is one of the most commonly used anticancer agents either alone or in combination. Nephrotoxicity is the most common and distressing side effect of its usage. Many mechanisms have been reported for describing the pathogenesis of cisplatin-nephrotoxicity, including a severe inflammatory response, vascular injury, free radicals generation, toxic metabolites, and apoptotic pathways. Many experimental trials were done to prevent or ameliorate cisplatin nephrotoxicity using neutralizing agents, antioxidant agents, or herbal compounds with variable results. Sex/gender differences have a great role in the process of cisplatin-induced nephrotoxicity. Many experimental studies reported that female rats were more resistant to cisplatin nephrotoxicity than male rats. Many experimental trials were done using a variety of compounds including sex hormones, antioxidants, and plant extracts to discover their preventive effects on cisplatin-induced nephrotoxicity in male and female experimental models with variable results. Conclusion: There is still a need for further studies to discover effective strategies for combating this dangerous side effect of cisplatin treatment and its sexual dimorphism. [ABSTRACT FROM AUTHOR]

Introduction: Antidesma puncticulatum Miq., commonly known as Mao-Luang in Thailand, is a medicinal plant widely renowned for its abundance of bioactive compounds with diverse pharmacological properties. This study investigated the phytochemical components, antioxidant potentials, and α-glucosidase inhibitory activity of ethanolic leaf extracts from 37 cultivars of A. puncticulatum. Methods: The leaves of 37 different varieties of A. puncticulatum were dried, finely ground, and then extracted using ethanol. The phytochemical screening, total amounts of phenolics, flavonoids, and tannins of the extracts were assessed. To evaluate their antioxidant potential, the extracts were subjected to the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2’-azinobis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and the ferric reducing antioxidant power (FRAP) Assays. In addition, standard in vitro methods were used to determine the α-glucosidase-inhibitory activity of the extracts. Results: Five phytochemical classes were detected in high concentrations in all of the extracts. Total phenolics, flavonoids, and tannins contents were in the range of 9.86-26.75 mg gallic acid equivalent (GAE)/g dry extract, 8.10-16.18 mg catechin equivalent (CE)/g dry extract, and 14.83-33.67 mg CE/g dry extract, respectively. According to DPPH, ABTS, and FRAP assay results, the antioxidant activities of the extracts were 5.10-9.07, 0.73-2.12, and 2.06- 4.01 mg ascorbic acid equivalent antioxidative capacity (AEAC)/g crude extract, respectively. Interestingly, the crude extracts from A. puncticulatum were more effective as α-glucosidase inhibitors than acarbose, with IC50 values ranging from 1.26 to 25.07 µg/mL. Conclusion: The ethanolic leaf extracts of A. puncticulatum were potent sources of phytochemicals with antioxidant and antidiabetic properties. Therefore, more research is needed to substantiate their potential applications as therapeutic remedies for diabetes.

The effect of the structure of promising antioxidant agents with prospective medical use, i.e., unsubstituted and para-substituted annelated triazinylacetic acid hydrazides, on their melting points, thermal stabilities, pyrolysis and oxidative decomposition stages and the type of volatiles emitted under heating with the use of DSC and TG/DTG/FTIR/QMS methods was evaluated and discussed. The melting point of the investigated compounds increased with an enhanced number of electrons (directly correlated with their molecular weight). Melting enthalpy values were determined and presented for all the studied compounds. The pyrolysis and oxidative decomposition processes of the analysed molecules consisted of several poorly separated stages, which indicated a multi-step course of the decomposition reactions. It was found that the thermal stability of the tested compounds depended on the type of substituent at the para position of the phenyl moiety or its absence. In both atmospheres used (air and helium), the thermal stability increased in relation to R as follows: -CH3 ≤ -OCH3 < -H < -OC2H5. In an inert atmosphere, it was higher by approx. 8–18 °C than in an oxidative atmosphere. The pyrolysis was connected with the emission of NH3, HCN, HNCO, HCONH2, HCHO, CO2, CO and H2O in the case of all the tested compounds, regardless of the substituent attached. In the case of the derivative containing the para-CH3 group, para-toluidine was an additional emitted aromatic product. In turn, emissions of aniline and alcohol (methanol or ethanol) for compounds with the para-OCH3 and para-OC2H5 groups, respectively, were confirmed. In oxidative conditions, the release of NH3, NO, HCN, HNCO, HCONH2, CO2, H2O and cyanogen (for all the compounds) and para-toluidine (for the para-CH3 derivative), aniline (for para-OCH3, para-OC2H5 and unsubstituted derivatives) and acetaldehyde (for the para-OC2H5 derivative) were clearly observed. No alcohol emissions were recorded for either compound containing the para-OCH3- or para-OC2H5-substitututed phenyl ring. These results confirmed that the pyrolysis and oxidative decomposition of the investigated annelated triazinylacetohydrazides occurred according to the radical mechanism. Moreover, in the presence of oxygen, the reactions of volatiles and residues with oxygen (oxidation) and the combustion process additionally proceeded. [ABSTRACT FROM AUTHOR]

Background: Complementary ozone therapy has been identified as a revolutionary medical technique for a number of goals and ailments. At the present, it has been shown that ozone has medicinal qualities, such as antibacterial, antifungal, and antiparasitic properties. Coronavirus (SARS-CoV-2) is quickly spread over the globe. Cytokine storms and oxidative stress seem to play a substantial role in the most of acute attacks of the disease. The aim of this research was to assess the therapeutic advantages of complementary ozone therapy on the cytokine profile and antioxidant status in COVID-19 patients. Methods: The statistical sample of this study included two hundred patients with COVID-19. One hundred COVID-19 patients (treatment group) received 240 ml of the patient's blood and an equal volume of O2/O3 gas at a concentration of 35–50 μg/ml daily, which gradually increased in concentration, and were kept for 5–10 days and one hundred patients (control group) received standard treatment. The secretion levels of IL-6, TNF-α, IL-1β, IL-10 cytokines, SOD, CAT and GPx were compared between control patients (standard treatment) and standard treatment plus intervention (ozone) before and after treatment. Results: The findings indicated a significant decrease in the level of IL-6, TNF-α, IL-1β in group receiving complementary ozone therapy in compared with control group. Furthermore, a significant increase was found in the level of IL-10 cytokine. Moreover, SOD, CAT and GPx levels revealed a significant increase in complementary ozone therapy group compared to control group. Conclusions: Our results revealed that complementary ozone therapy can be used as a medicinal complementary therapy to reduce and control inflammatory cytokines and oxidative stress status in patients with COVID-19 as revealed its antioxidant and anti-inflammatory effects. [ABSTRACT FROM AUTHOR]

Obesity is a pathophysiological condition, dependent on body fat accumulation, that progressively induces systemic oxidative stress/inflammation leading to a set of associated clinical manifestations, including male infertility. CircRNAs, covalently closed RNA molecules, are key regulators of sperm quality. Recently, we have characterized a complete profile of high-fat diet (HFD) spermatic circRNA cargo, predicting paternal circRNA dependent networks (ceRNETs), potentially involved in sperm oxidative stress and motility anomalies. In the current work, using HFD C57BL6/J male mice, orally treated with a mix of bioactive molecules (vitamin C; vitamin B12; vitamin E; selenium-L-methionine; glutathione-GSH) for 4 weeks, a reversion of HFD phenotype was observed. In addition, the functional action of the proposed formulations on circRNA biogenesis was evaluated by assessing the endogenous spermatic FUS-dependent backsplicing machinery and related circRNA cargo. After that, spermatic viability and motility were also analyzed. Paternal ceRNETs, potentially involved in oxidative stress regulation and sperm motility defects, were identified and used to suggest that the beneficial action of the food supplements here conveniently formulated on sperm motility was likely due to the recovery of circRNA profile. Such a hypothesis was, then, verified by an in vitro assay.

Light is often considered the primary factor leading to the regeneration failure of Korean pines (Pinus koraiensis) under the forest canopy. However, studies on the effect of light on Korean pines mainly focus on the use of an artificial sunshade net to control shade; field studies on the canopy are extremely scarce, and the current experimental results are contradictory. For a deeper understanding of the relationship between light conditions and understory Korean pine trees, the conditions of low, middle, high and full light (control) under the forest were tested at 18 years of age. The photosynthetic pigments, chlorophyll fluorescence, non-structural carbohydrate metabolism, antioxidant enzyme activity, and nutrient concentrations of current-year needles from Korean pine trees were measured. From June to September, light intensity and quality decreased under full light, but following leaf fall, understory light conditions improved slightly. As the light conditions improved, the photosynthetic pigments in the needles decreased, but Car/Chl were highest in the needles under full light. All light conditions had a positive correlation with glucose concentrations and Rubisco activity. Full-light needles had the highest APX activity, DPPH scavenging capacity, and proline concentration, as well as higher NPQ and lower Fv/Fm readings. This indicated that full-light Korean pine trees were stressed and inhibited photosynthesis to some extent, while the understory light environment may alleviate stress. The conservative strategy of storing more starch and using less glucose in understory Korean pine trees may be one of the reasons for the observed differences in growth rates among Korean pine trees under varying light conditions. Overall, this study implies that understory light during the growing season is not always unfavorable to 18-year-old Korean pine trees; this means that 18-year-old Korean pine trees still have shade tolerance to some extent and are capable of living under a canopy of deciduous trees. [ABSTRACT FROM AUTHOR]

There is a rising demand for packaged food in the twenty-first century. Fresh food products are prone to spoilage, moisture loss, physical damage, microbial decay, and biochemical changes. These are the principal reasons for the quality loss and decreased shelf-life, necessitating the usage of packing films. The packaging films are currently made from different synthetic polymers including polypropylene, polyethylene, and other types of artificial polymers. However, it would be better to use soy protein as a justifiable antibacterial film in packaging. Soy Protein Isolate (SPI) is cheap and widely available for different uses in the food industry. Soy-based films made from renewable resources are a better option than synthetic-based films. They have strong mechanical characteristics and they are transparent in the presence of other additions like acids, nanoparticles, and natural substances. Furthermore, the production technique (compression molding and solution casting) for SPI film in the absence or presence of additives is simple and economically beneficial. Chemicals derived from plants such as essential oils and plant extracts are also useful to add antioxidant and antibacterial properties to films and coatings resulting in SPI. This paper was focused on the application of soy protein-based coatings and films, as well as coatings incorporated with nano-materials (nano-bioactive chemicals or essential oils), in food models to extend shelf life, as reported in recent years. [ABSTRACT FROM AUTHOR]

The beauty industry is actively searching for solutions to prevent skin aging. Some of the crucial elements protecting cells from the aging process are telomere shortening, telomerase expression, cell senescence, and homeostasis of the redox system. Modification of these factors using natural antioxidants is an appealing way to support healthy skin aging. Therefore, in this study, we sought to investigate the antiaging efficacy of a specific combination of four botanical extracts (pomegranate, sweet orange, Cistanche and Centella asiatica) with proven antioxidant properties. To this end, normal human dermal fibroblasts were used as a cell model and the following studies were performed: cell proliferation was established by means of the MTT assay and the intracellular ROS levels in stress-induced premature senescence fibroblasts; telomere length measurement was performed under standard cell culture conditions using qPCR and under oxidative stress conditions using a variation of the Q-FISH technique; telomerase activity was examined by means of Q-TRAP; and AGE quantification was completed by means of ELISA assay in UV-irradiated fibroblasts. As a result, the botanical blend significantly reversed the H2O2-induced decrease in cell viability and reduced H2O2-induced ROS. Additionally, the presence of the botanical ingredient reduced the telomere shortening rate in both stressed and non-stressed replicating fibroblasts, and under oxidative stress conditions, the fibroblasts presented a higher median and 20th percentile telomere length, as well as a lower percentage of short telomeres (<3 Kbp) compared with untreated fibroblasts. Furthermore, the ingredient transiently increased relative telomerase activity after 24 h and prevented the accumulation of UVR-induced glycated species. The results support the potential use of this four-component plant-based ingredient as an antiaging agent. [ABSTRACT FROM AUTHOR]

The potentiality of coenzyme Q10 (CoQ10), D‐Aspartic acids (D‐Asp), Maca or vitamin C, as antioxidant agents, to reduce negative impacts of high ambient temperature on semen quality, oxidative capacity and fertility of Muscovy ducks was investigated. Seventy‐five Muscovy males (34‐wk of age) were distributed randomly into five experimental groups of fifteen ducks each. The first group was fed a basal diet without supplementation and served as a control. The other four groups were fed a basal diet supplemented with 400 mg CoQ10, 400 mg D‐Asp, 500 mg Maca and 200 mg vitamin C (ascorbic acid) per kg diet for 17 consecutive weeks under high ambient temperature conditions. The dietary inclusion of antioxidants significantly maintains better semen variables and a higher fertility rate either for fresh or preserved semen. Among the tested antioxidants, the Maca group showed the best status and outperformed the others in terms of motility, viability, sperm cell concentration, intact acrosome and membrane integrity percentages, total proteins, total antioxidants capacity, glutathione peroxidase, superoxide dismutase (SOD), malondialdehyde (MDA), testosterone, and the fertility rate for the fresh semen, as well as, forward motility, SOD and MDA for the preserved semen. The CoQ10 showed similar results to Maca in some measurements. Conversely, the basal diet had the poorest performance in all examined variables. The dietary incorporation of antioxidants (Maca or CoQ10) enhances fresh and preserved semen quantity and quality, as well as the fertility rate of Muscovy males under high ambient temperature conditions. [ABSTRACT FROM AUTHOR]

This work evaluated the phytochemical composition of olive seed extracts from different cultivars ('Cobrançosa', 'Galega', and 'Picual') and their antioxidant capacity. In addition, it also appraised their potential antineurodegenerative properties on the basis of their ability to inhibit enzymes associated with neurodegenerative diseases: acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase (TYR). To achieve this goal, the phenolic composition of the extracts was determined through high-performance liquid chromatography coupled with photodiode-array detection and electrospray ionization/ion trap mass spectrometry (HPLC-DAD-ESI/MSn). The antioxidant capacity was assessed by two different methods (ABTS•+ and DPPH•), and the antineurodegenerative potential by the capacity of these extracts to inhibit the aforementioned related enzymes. The results showed that seed extracts presented a high content of phenolic compounds and a remarkable ability to scavenge ABTS•+ and DPPH•. Tyrosol, rutin, luteolin-7-glucoside, nüzhenide, oleuropein, and ligstroside were the main phenolic compounds identified in the extracts. 'Galega' was the most promising cultivar due to its high concentration of phenolic compounds, high antioxidant capacity, and remarkable inhibition of AChE, BChE, and TYR. It can be concluded that olive seed extracts may provide a sustainable source of bioactive compounds for medical and industrial applications. [ABSTRACT FROM AUTHOR]

Presbycusis or Age-related hearing loss (ARHL) is a sensorineural hearing loss that affects communication, leading to depression and social isolation. Currently, there are no effective treatments against ARHL. It is known that cocoa products have high levels of polyphenol content (mainly flavonoids), that are potent anti-inflammatory and antioxidant agents with proven benefits for health. The objective is to determine the protective effect of cocoa at the cellular and molecular levels in Presbycusis. For in vitro study, we used House Ear Institute-Organ of Corti 1 (HEI-OC1), stria vascularis (SV-k1), and organ of Corti (OC-k3) cells (derived from the auditory organ of a transgenic mouse). Each cell line was divided into a control group (CTR) and an H2O2 group (induction of senescence by an oxygen radical). Additionally, every group of every cell line was treated with the cocoa polyphenolic extract (CPE), measuring different markers of apoptosis, viability, the activity of antioxidant enzymes, and oxidative/nitrosative stress. The data show an increase of reactive oxidative and nitrogen species (ROS and RNS, respectively) in senescent cells compared to control ones. CPE treatment effectively reduced these high levels and correlated with a significant reduction in apoptosis cells by inhibiting the mitochondrial-apoptotic pathway. Furthermore, in senescence cells, the activity of antioxidant enzymes (Superoxide dismutase, SOD; Catalase, CAT; and Glutathione peroxidase, GPx) was recovered after CPE treatment. Administration of CPE also decreased oxidative DNA damage in the auditory senescent cells. In conclusion, CPE inhibits the activation of senescencerelated apoptotic signaling by decreasing oxidative stress in auditory senescent cells. [ABSTRACT FROM AUTHOR]

Reactive oxygen species (ROS) are a common hallmark of many degenerative diseases, developing in all those cases where a failure of physiological antioxidant mechanisms occurs (in particular, antioxidant enzymes and the glutathione system), or in case of exposure to an extremely high level of oxidants. In this regard, antioxidant natural extracts are promising compounds as preventive or therapeutic agents against ROS-dependent degenerations. In this study, a deep investigation of hazelnut (Corylus avellana) extract has been performed in terms of mass spectroscopy, evaluation of phenolic content, and antioxidant capacity. Then, nanostructured lipid carriers (NLCs) have been exploited for encapsulation of the hazelnut extracts in order to achieve prolonged bioactivity, increased stability, and targeting through a sustainable delivery approach. The hazelnut extract-loaded NLCs (NE_NLCs) have been deeply characterized for their stability, production yield, and encapsulation efficiency. Moreover, NE_NLCs showed optimal cytocompatibility on human dermal fibroblast (HDF) cells, as well as excellent antioxidant activity, upon pro-oxidant stimulus on HDF cells.

[Display omitted] • A series of novel 25 arylaminonaphthols have been synthesized. • Biological evaluations of arylaminonaphthols revealing promising results in both antioxidant activity and BChE inhibition. • Theoretical calculations have been employed to understand the structure and properties of the synthesized compounds. • QSAR study has been used to establish relationships between chemical structures and biological activities. • Molecular docking has been performed to predict the binding interactions between arylaminonaphthols and the target enzymes. • Further research can focus on optimizing the chemical structures of the compounds to enhance their efficacy. A completely green protocol was developed for the synthesis of a series of arylaminonaphthol derivatives in the presence of N -ethylethanolamine (NEEA) as a catalyst under ultrasonic irradiation and solventless conditions. The major assets of this methodology were the use of non-toxic organic medium, available catalyst, mild reaction condition, and good to excellent yield of desired products. All of the synthesized products were screened for their in vitro antioxidant activity using DPPH, ABTS, and Ferric-phenanthroline assays and it was found that most of them are potent antioxidant agents. Also, their butyrylcholinesterase inhibitory activity has been investigated in vitro. All tested compounds exhibited potential inhibitory activity toward BuChE when compared to standard reference drug galantamine, however, compounds 4r , 4u , 4 g and 4x gave higher butyrylcholinesterase inhibitory with IC 50 values of 14.78 ± 0.65 µM, 16.18 ± 0.50 µM, 20.00 ± 0.50 µM, and 20.28 ± 0.08 µM respectively. On the other hand, we employed density functional theory (DFT), calculations to analyze molecular geometry and global reactivity descriptors, and MESP analysis to predict electrophilic and nucleophilic attacks. A quantitative structure–activity relationship (QSAR) investigation was conducted on the antioxidant and butyrylcholinesterase properties of 25 arylaminonaphthol derivatives, resulting in robust and satisfactory models. To evaluate their anti-Alzheimer's activity, compounds 4 g , 4q , 4r , 4u , and 4x underwent docking simulations at the active site of the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), revealing why these compounds displayed superior activity, consistent with the biological findings. [ABSTRACT FROM AUTHOR]

Agarwood is a fragrant dark resin produced in plants belonging to the family Thyme-laeaceae and which has a high economic value. The unique fragrance and medicinal applications intensify the value of agarwood. The wild populations of agarwood trees are highly threatened by high economic demand. Therefore, it is worthwhile to develop an artificial agarwood induction technology for the countries that rely on agarwood from the natural habitat of the plants. Fungal induction of agarwood has been shown to be an efficient method. Interestingly, most of the fungi known from agarwood are endophytic. In this paper, we supplement and update the bioactivity of fungi associated with agarwood and their ability to induce agarwood formation. According to the existing literature, 59 endophytic fungal strains of 16 genera induce agarwood production, most of which belong to Fusarium (28 identified strains). Hence, Fusarium is a good candidate for further studies on fungal induced agarwood production. [ABSTRACT FROM AUTHOR]

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The potential employment of 18 commercial Tunisian essential oils (EOs) as natural food preservatives was investigated. Their antimicrobial activity was evaluated against two food-borne bacteria (Escherichia coli O157:H7 and Klebsiella pneumoniae) by the agar-well diffusion method and, subsequently, by determining the minimum inhibitory concentration (MIC); while their antioxidant activity was assayed by the DPPH test. Also, the main volatile constituents and inorganic elements were elucidated and discussed in relation to the biological activities. Excluding the wormwood EO, all EOs inhibited the growth of at least one reference strain. In particular, spearmint, sage and rosemary EOs had the lowest MICs against E. coli O157:H7 (0.09, 0.09, 0.07 mg mL−1, respectively); whereas sage EO was effective against K. pneumoniae at 0.41 mg mL−1. All EOs displayed also a promising antioxidant activity. Specifically, spearmint, bigroot geranium, and sage EOs showed the lowest IC50 values (0.024, 0.046 and 0.052 mg mL−1), and a behavior similar to that of butylated hydroxytoluene. EOs exhibited variegated and peculiar element profiles. Among minerals, Mg and K were in the range 1.72–14.12 mg Kg−1 and 0.57–20.90 mg Kg−1; while Cu and Fe were generally the most abundant trace essential metals (0.07–1.02 mg Kg−1 0.20–2.98 mg Kg−1, respectively). Very low and safe levels of heavy metals were also revealed. A statistical correlation analysis pointed out a significant positive correlation between some elements (K, Cu, and Fe) and the biological activities displayed. In conclusion, the selected Tunisian EOs had a marked potential applicability as antibacterial and antioxidant additive in food industry. [ABSTRACT FROM AUTHOR]

Background: A large number of chemical compounds exert their antioxidant effects by activation of key transcriptional regulatory mechanisms, such as the transcription factor Nrf2. The aim of this study was to evaluate the activation of the Keap1-Nrf2 pathway by both the n-butanol extract obtained from the inner bark of Tabebuia rosea (Bertol) DC and specioside isolated from this extract. Methods: The antioxidant activity of the extract and specioside isolated from the inner bark of T. rosea were evaluated using the oxygen radical absorbance capacity (ORAC) and the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH) techniques, whereas their effects on the viability of HepG2 cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The effects of the compound and the extract on activating the Keap1-Nrf2 pathway were evaluated using a Nrf2 Transcription Factor Assay kit. Induction of the Nrf2-mediated antioxidant response genes HMOX-1 and NQO1 was evaluated by real-time PCR. The protective effects against H 2O 2-induced oxidative stress in HepG2 cells was determined as the percent protection using the MTT method. Results: Both the n-butanol extract and specioside exhibited activity at low concentrations without affecting cellular viability, since the cell viability was greater than 80% after 24 hours of exposure at each tested concentration. In addition, Nrf2 dissociated from Keap1 after treatment with the n-butanol extract at a concentration of 0.25 µg/mL after 4 hours of exposure. An increase in the Nrf2 level in the cytoplasm after 4 hours of exposure to 2 μM specioside was observed. Nrf2 levels stabilized in the nucleus 12 hours after stimulation with both specioside and the extract. After 6 hours of stimulation, both the extract and specioside induced the expression of HMOX-1 and NQO1. Conclusion: The n-butanol extract from the inner bark of T. rosea and specioside produced protective effects against H 2O 2-induced oxidative stress in HepG2 cells.

Background: A large number of chemical compounds exert their antioxidant effects by activation of key transcriptional regulatory mechanisms, such as the transcription factor Nrf2. The aim of this study was to evaluate the activation of the Keap1-Nrf2 pathway by both the n-butanol extract obtained from the inner bark of Tabebuia rosea (Bertol) DC and specioside isolated from this extract. Methods: The antioxidant activity of the extract and specioside isolated from the inner bark of T. rosea were evaluated using the oxygen radical absorbance capacity (ORAC) and the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH) techniques, whereas their effects on the viability of HepG2 cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The effects of the compound and the extract on activating the Keap1-Nrf2 pathway were evaluated using a Nrf2 Transcription Factor Assay kit. Induction of the Nrf2-mediated antioxidant response genes HMOX-1 and NQO1 was evaluated by real-time PCR. The protective effects against H 2O 2-induced oxidative stress in HepG2 cells was determined as the percent protection using the MTT method. Results: Both the n-butanol extract and specioside exhibited activity at low concentrations without affecting cellular viability, since the cell viability was greater than 80% after 24 hours of exposure at each tested concentration. In addition, Nrf2 dissociated from Keap1 after treatment with the n-butanol extract at a concentration of 0.25 µg/mL after 4 hours of exposure. An increase in the Nrf2 level in the cytoplasm after 4 hours of exposure to 2 μM specioside was observed. Nrf2 levels stabilized in the nucleus 12 hours after stimulation with both specioside and the extract. After 6 hours of stimulation, both the extract and specioside induced the expression of HMOX-1 and NQO1. Conclusion: The n-butanol extract from the inner bark of T. rosea and specioside produced protective effects against H 2O 2-induced oxidative stress in HepG2 cells.

Background: A large number of chemical compounds exert their antioxidant effects by activation of key transcriptional regulatory mechanisms, such as the transcription factor Nrf2. The aim of this study was to evaluate the activation of the Keap1-Nrf2 pathway by both the n-butanol extract obtained from the inner bark of Tabebuia rosea (Bertol) DC and specioside isolated from this extract. Methods: The antioxidant activity of the extract and specioside isolated from the inner bark of T. rosea were evaluated using the oxygen radical absorbance capacity (ORAC) and the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH) techniques, whereas their effects on the viability of HepG2 cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The effects of the compound and the extract on activating the Keap1-Nrf2 pathway were evaluated using a Nrf2 Transcription Factor Assay kit. Induction of the Nrf2-mediated antioxidant response genes HMOX-1 and NQO1 was evaluated by real-time PCR. The protective effects against H 2O 2-induced oxidative stress in HepG2 cells was determined as the percent protection using the MTT method. Results: Both the n-butanol extract and specioside exhibited activity at low concentrations without affecting cellular viability, since the cell viability was greater than 80% after 24 hours of exposure at each tested concentration. In addition, Nrf2 dissociated from Keap1 after treatment with the n-butanol extract at a concentration of 0.25 µg/mL after 4 hours of exposure. An increase in the Nrf2 level in the cytoplasm after 4 hours of exposure to 2 μM specioside was observed. Nrf2 levels stabilized in the nucleus 12 hours after stimulation with both specioside and the extract. After 6 hours of stimulation, both the extract and specioside induced the expression of HMOX-1 and NQO1. Conclusion: The n-butanol extract from the inner bark of T. rosea and specioside produced protective effects against H 2O 2-induced oxidative stress in HepG2 cells.

Presbycusis or Age-related hearing loss (ARHL) is a sensorineural hearing loss that affects communication, leading to depression and social isolation. Currently, there are no effective treatments against ARHL. It is known that cocoa products have high levels of polyphenol content (mainly flavonoids), that are potent anti-inflammatory and antioxidant agents with proven benefits for health. The objective is to determine the protective effect of cocoa at the cellular and molecular levels in Presbycusis. For in vitro study, we used House Ear Institute-Organ of Corti 1 (HEI-OC1), stria vascularis (SV-k1), and organ of Corti (OC-k3) cells (derived from the auditory organ of a transgenic mouse). Each cell line was divided into a control group (CTR) and an H2O2 group (induction of senescence by an oxygen radical). Additionally, every group of every cell line was treated with the cocoa polyphenolic extract (CPE), measuring different markers of apoptosis, viability, the activity of antioxidant enzymes, and oxidative/nitrosative stress. The data show an increase of reactive oxidative and nitrogen species (ROS and RNS, respectively) in senescent cells compared to control ones. CPE treatment effectively reduced these high levels and correlated with a significant reduction in apoptosis cells by inhibiting the mitochondrial-apoptotic pathway. Furthermore, in senescence cells, the activity of antioxidant enzymes (Superoxide dismutase, SOD; Catalase, CAT; and Glutathione peroxidase, GPx) was recovered after CPE treatment. Administration of CPE also decreased oxidative DNA damage in the auditory senescent cells. In conclusion, CPE inhibits the activation of senescence-related apoptotic signaling by decreasing oxidative stress in auditory senescent cells.

Background/Aim: Ischemia is a common issue in fracture healing due to vascular injury, compartment syndrome, and long-term tourniquet use. With ischemia-reperfusion injury, normal tissue repair can become complicated. In our study, we aimed to investigate the effect of edaravone on fracture union in a rat fracture model complicated with ischemia. Methods: We conducted our study on forty-four rats divided into four study groups and a control group, as follows: Group 1- Fracture, Group 2- Fracture-ischemia, Group 3- Fracture-ischemia-edaravone, Group 4- Fracture-edaravone, and Group 5- Control group. The control group comprised the contralateral intact tibia of the rats in Group 1 that were not complicated with ischemia and were not given edaravone treatment. The effects of edaravone on fracture healing were evaluated histologically, radiologically, and biomechanically. Results: There were no differences between the groups in terms of biomechanical and radiological indices, except for hardness values in the control subjects (Group 5), which were significantly higher than those of the other groups (P<0.05 for all). Similarly, in terms of histological evaluations of fracture healing between groups, group 3 has better improvement fracture healing scores than group 2 (P=0.042), and Group 4 has better improvement fracture healing scores than group 1 (P=0.049). Conclusion: These findings suggest that the administration of edaravone, independent of ischemia, had positive results on histopathological fracture healing. [ABSTRACT FROM AUTHOR]

Hepatitis B virus (HBV) infection is a leading risk factor for hepatocellular carcinoma (HCC), contributing to cancer development through direct genomic integration and chronic inflammation. N-acetylcysteine (NAC), known for its antioxidant properties, is widely utilized in cancer prevention. However, clinical evidence regarding its protective effect against HCC in HBV carriers remains sparse. In this retrospective cohort study spanning 2008 to 2018, we utilized Taiwan's National Health Insurance Research Database (NHIRD) to include 1,061,174 chronic HBV carriers. Participants were stratified into NAC users and non-users using Propensity Score Matching. We assessed the incidence of HCC in both cohorts, examining the relationship between NAC usage duration and HCC incidence, and evaluating the dose-response effect. NAC users exhibited a significantly lower risk of developing HCC (adjusted hazard ratio [aHR]: 0.38; 95% confidence interval [CI]: 0.36-0.40; P < 0.0001). A dose-response relationship was evident, with higher cumulative defined daily doses (cDDDs) of NAC correlating with reduced HCC risk, revealing a significant trend (P < 0.0001). Notably, a daily NAC intensity of > 1.4 DDDs was associated with a decreased risk of HCC in HBV patients. Our results demonstrate that the use of NAC, in a dose-dependent manner, is intricately linked with a diminished incidence of HCC in individuals chronically infected with the HBV., Competing Interests: None., (AJCR Copyright © 2024.)

Over loading of iron oxide nanoparticles can causes the liver injury through overproduction of free radicals. Zataria multiflora Boiss. (Lamiaceae) has been used for many years in folk medicine due to its antioxidant and antibacterial activities. This study evaluates -for the first time- the effect of Z. multiflora essential oil (EO) against iron oxide nanoparticles hepatotoxicity in rat model. Male Wistar rats were divided randomly into 4 groups; control group (C), non-treated control group (NT), treatment groups, nanoparticles plus Z. multiflora EO at 100 and 200 mg/kg b.w. In following, the liver and blood tissue were collected for estimating antioxidant / oxidative stress parameters including lipid peroxidation (LP), glutathione (GSH), glutathione-S-transferase (GST), and liver enzyme asparate transaminase (AST) and also histopathological examinations. Iron oxide nanoparticles toxicity produced a significant increase in the levels of LP, ferric reducing ability of plasma (FRAP), and AST activity concomitant with decrease in the levels of GSH and GST activity compared to the control group. However, in the treatment groups received Z. multiflora EO, the levels of LP and AST activity reduced together with increasing in GSH content and GST activity were significantly reported. Histopathological studies also supported the biochemical assessments indicating hepatic improvements induced by nanoparticles. Z. multiflora EO protected the liver from injuries induced by iron oxide nanoparticles which can be correlated with its antioxidant activities. This can be a valuable candidate in modulating the oxidative hepatic injuries.

Pyridazinone is a unique template that is associated with several pharmacogical activities. A new class of pyridazinone derivatives containing cyclic/acyclic amine moiety was synthesized and evaluated for their in vitro cytotoxic activity against HEP3BPN 11 (liver), MDA 453 (breast) and HL60 (leukemia) cancer cells. Three derivatives 4a (76.78±0.7 against HEP3BPN 11), 4b (71.55±0.88 against HL60), and 4e (79.04±0.2 against HEP3BPN 11 & 73.09±01 against MDA 453) showed promising anticancer activity were further tested for their potential to inhibit the proangiogenic cytokines involved in tumor progression. Free radical scavenging activities of these compounds were demonstrated using 2,2-diphenyl-1-picryl hydrazine (DPPH), OH and superoxide anion radicals. [ABSTRACT FROM AUTHOR]

Silver nanoparticles (AgNPs) were biosynthesized using the cell free supernatant of putative probiotic Lactobacillus paracasei A26. Several biological activities of biogenic AgNPs were investigated in respect to in vitro anti-oxidant and anti-tumor potentials. Anti-oxidant potentials were screened in terms of free radical scavenging activity against two free radicals, 2, 2-Diphenyl-1-picrylhydrazyl (DPPH) and resazurin dye. AgNPs exhibited a potent scavenging activity against resazurin dye (91±0.046%) with an EC50 concentration of 146.823 μg/ml, while scavenging of DPPH was significantly (P≤0.05) reduced to 72.330±0.114% using a higher EC50 concentration of 176.12 μg/ml. The anti-tumor potentials of biogenic AgNPs were studied in relation to the cytotoxicity against two human breast cancer cell lines (CAL-51 and MCF7), using crystal violet dye assay. The viability of AgNPs-treated cancerous cells was significantly decreased in a time- and concentration manner, as compared to insignificant cytotoxic effects against the normal cell line. However, the anti-proliferative activity of AgNPs did not exceed the value of 63.85±0.019% in both cancer cell lines. CAL-51 cells were the most sensitive to the introduced AgNPs, with a maximum decrease in viability of 49.889±0.021% being reached using an IC50 value of 98.65μg/ml for 48h exposure time. The inhibition percentage was increased to 60.13±0.005% when the used IC50 value was significantly declined to 40.73μg/ml with an exposure time expanded to 72h. MCF7 cells showed lower sensitivity than CAL-51 cells, but with a similar inhibition trend of 59.523±0.01% with an IC50 concentration of 66.54 μg/ml for 48h which was increased to 63.857±0.019% when the IC50 was reduced to 62.63 μg/ml and the exposure time expanded to 72h. The morphological changes of AgNPs-treated cells were apparent at 72h exposure time, with cells showing apoptotic-like features such as shrinkage and losing of regular fusiform shape. Moreover, cells became detached to surfaces and from each other. [ABSTRACT FROM AUTHOR]

Abstract Mitochondria are critically involved in reactive oxygen species (ROS)-dependent lung diseases, such as lung fibrosis, asbestos, chronic airway diseases and lung cancer. Mitochondrial DNA (mtDNA) encodes mitochondrial proteins and is more sensitive to oxidants than nuclear DNA. Damage to mtDNA causes mitochondrial dysfunction, including electron transport chain impairment and mitochondrial membrane potential loss. Furthermore, damaged mtDNA also acts as a damage-associated molecular pattern (DAMP) that drives inflammatory and immune responses. In this review, crosstalk among alveolar epithelial cells, alveolar macrophages and mitochondria is examined. ROS-related transcription factors and downstream cell signaling pathways are also discussed. We conclude that targeting oxidative stress with antioxidant agents, such as thiol molecules, polyphenols and superoxide dismutase (SOD), and promoting mitochondrial biogenesis should be considered as novel strategies for treating lung diseases that currently have no effective treatment options.

A series of novel chalcone derivatives was designed, synthesized and evaluated as multifunctional agents for the treatment of AD. Among of these synthesized compounds, compound TM-2 was a selective BuChE inhibitor (IC 50 = 2.6 μM) and selective MAO-B inhibitor (IC 50 = 5.3 μM), which were supported by docking study. Compound TM-2 also showed good antioxidant activity, and was a selective metal chelator, as well as a neuroprotectant. Moreover, compound TM-2 could significantly inhibit self-induced and Cu2+-induced A β 1-42 aggregation with 70.2% and 80.7% inhibition rate, respectively, and could disaggregate Cu2+-induced A β 1-42 aggregation (73.5%), the further TEM images observed provided rational explanation. Besides, compound TM-2 displayed good PAMPA-BBB permeability and conformed to the Lipinski's rule of five. Further, compound TM-2 presented precognitive effect on scopolamine-induced memory impairment in vivo assay. Therefore, compound TM-2 might be a promising multifunctional hit compound for the treatment of AD, and the further structure optimization are in progress. Image 1 • TM-2 was a selective BuChE inhibitor and selective MAO-B inhibitor. • TM-2 showed good antioxidant activity and selective metal chelator. • TM-2 could inhibit/disaggregate self/Cu2+-induced A β 1-42 aggregation. • TM-2 displayed good PAMPA-BBB permeability. • TM-2 presented precognitive effect in vivo assay. [ABSTRACT FROM AUTHOR]

To discover multifunctional agents for the treatment of Alzheimer's disease (AD), a series of chalcone- O -carbamate derivatives was designed and synthesized based on the multitarget-directed ligands strategy. The in vitro biological activities were evaluated including AChE/BChE inhibition, MAO-A/MAO-B inhibition, antioxidant activities, Aβ 1-42 aggregation inhibition, metal-chelating properties and neuroprotective effects against H 2 O 2 -induced PC12 cell injury. The results showed compounds 5b and 5h indicated highly selective BChE inhibitory activity with IC 50 values of 3.1 μM and 1.2 μM, respectively and showed highly selective MAO-B inhibitory potency with IC 50 values of 1.3 μM and 3.7 μM, respectively. In addition, compounds 5b and 5h could inhibit self-induced Aβ 1-42 aggregation with 63.9% and 53.1% inhibition percent rate, respectively. Particularly, compound 5b was a potent antioxidant agent and neuroprotectant, as well as a selective metal chelator by chelating Cu2+ and Al3+. Moreover, compound 5b could inhibit and disaggregate Cu2+-induced Aβ 1-42 aggregation, which was further supported by the TEM images. Furthermore, compounds 5b and 5h could cross the blood-brain barrier (BBB) in vitro and conformed to the Lipinski's rule of five. Finally, the in vivo assay exhibited that compound 5b could improve scopolamine-induced cognitive impairment. Taken together, these results revealed that compound 5b might be a potential multifunctional agent for the treatment of AD, and deserved to do further structure optimization. Image 1 • Compound 5b was a reversible competition BChE inhibitor (IC 50 = 3.1 μM) and selective MAO-B inhibitor (IC 50 = 1.3 μM). • Compound 5b showed good antioxidant activity and neuroprotective effect. • Compound 5b was a selective metal chelator, and could significantly inhibit and decompose Cu2+-induced A β 1-42 aggregation. • Compound 5b could cross PAMPA-BBB and conformed to the Lipinski's rule. • Compound 5b could improve scopolamine-induced memory impairment. [ABSTRACT FROM AUTHOR]

2-Aminothiazole derivatives bear three nucleophilic centers, i.e. endocyclic N, exocyclic NH2 , and S atom in the ring system. In addition to these centers there are π-electrons in the ring system which can also expectedly be involved in some sort of coordination. To the best of our knowledge the solid state coordination chemistry of such ligands has not been fully presented in the literature. These ligands (2-amino-4-methylthiazole and 2-amino- 5-methylthiazole) were coupled with CoCl2 under aerobic conditions to form tetrahedral complexes, bis(2-amino-4- methylthiazole)dichlorocobalt(II) (1) and bis(2-amino-5-methylthiazole)dichlorocobalt(II) (2). Reaction of 2-amino- 5-methylthiazole with AgNO3 led to an expected two-coordinated, bis(2-amino-5-methylthiazole)silver(I) nitrate (3) as crystalline material. In all complexes the coordination behavior of the aminothiazole derivatives was identical, coordinating to the metal center through endocyclic N atom. The structures of these complexes were confirmed by single-crystal X-ray analysis. Compounds (1–3) were screened for their antimicrobial potency against gram-negative (E. sakazkii, E. coli, K. pneumoniae) and a gram-positive bacteria (S. aurus). Additionally, their role as enzyme inhibitors (acetylcholinesterase, AChE, and butyrylcholinesterase, BChE) and their free radical scavenging ability (2,2-Diphenyl- 1-picrylhydrazyl, DPPH, and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid, ABTS) were studied. These ligands bear additional nucleophilic centers (S and NH2) and can be involved in secondary interactions as confirmed by their solid-state structures. These interactions make the molecules biologically important and thus play a pivotal role in establishing the supramolecular network. We report here the coordination chemistry and selected biological applications of complexes 1–3. [ABSTRACT FROM AUTHOR]

The novel approach in the treatment of complex multifactorial diseases, such as neurodegenerative disorders and cancer, requires a development of efficient multi-targeting oriented drugs. Since oxidative stress significantly contributes to the pathogenesis of cancer and neurodegenerative disorders, potential drug candidates should possess good antioxidant properties. Due to promising biological activities shown for structurally related (1,3-thiazol-2-yl)hydrazones, a focused library of 12 structurally related benzylidene-based (1,3-selenazol-2-yl)hydrazones was designed as potential multi-targeting compounds. Monoamine oxidases (MAO) A/B inhibition properties of this class of compounds have been investigated. Surprisingly, the p-nitrophenyl-substituted (1,3-selenazol-2-yl)hydrazone 4 showed MAO B inhibition in a nanomolar concentration range (IC50 = 73 nM). Excellent antioxidant properties were confirmed in a number of different in vitro assays. Antiproliferative activity screening on a panel of six human solid tumor cell lines showed that potencies of some of the investigated compounds was comparable or even better than that of the positive control 5-fluorouracil. In-silico calculations of ADME properties pointed to promising good pharmacokinetic profiles of investigated compounds. Docking studies suggest that some compounds, compared to positive controls, have the ability to strongly interact with targets relevant to cancer such as 5′-nucleotidase, and to neurodegenerative diseases such as the small conductance calcium-activated potassium channel protein 1, in addition to confirmation of inhibitory binding at MAO B.

Graphical abstract Abstract The use of antioxidants is the most effective means to protect the organism against cellular damage caused by oxidative stress. In this context, organotellurides have been described as promising antioxidant agents for decades. Herein, a series of N -functionalized organotellurium compounds has been tested as antioxidant and presented remarkable activities by three different in vitro chemical assays. They were able to reduce DPPH radical with IC 50 values ranging from 5.08 to 19.20 µg mL−1, and some of them also reduced ABTS + radical and TPTZ-Fe3+ complex in ABTS + and FRAP assays, respectively. Initial structure-activity relationship discloses that the nature of N -substituent strongly influenced both activity and cytotoxicity of the studied compounds. Furthermore, radical scavenging activities of N -functionalized organotellurides have been compared with those of their selenilated congeners, demonstrating that the presence of tellurium atom has an essential role in antioxidant activity. [ABSTRACT FROM AUTHOR]

Electrospinning process of nanofibers specially derivatives of cellulose presents high behest for developing several kinds of novel drug delivery systems (DDSs) due to their specific characteristics, the simplicity, beneficial and impressive top-down fabricating procedure. Moreover, the novel techniques of therapeutic agents for entrapment into core–shell nanofibers including single, coaxial and triaxial applied for DDSs. Recently, biodegradable polymers including derivatives of cellulose, hybrid materials, artificial and natural polymers have been remarkably considered. The acetate ester of cellulose (cellulose acetate (CA)), has been widely used due to biodegradability, chemical persistence, biocompatibility, and thermal constancy for DDSs. This article submits an overview of CA electrospinning techniques, applications, and its usage as a carrier for therapeutic agents in DDSs. Furthermore, in this study, we aimed to summarize the classification of therapeutic agents comprising antimicrobial agents incorporated CA fibers, antibacterial nanoparticles incorporated CA fibers, antioxidant agents loaded CA nanofibers, systematic and anti-inflammatory agents containing CA nanofibers. Our study has been concluded that CA electrospun nanofibers could be potentially applied as biocompatible and biodegradable for DDSs specifically in purpose-designed transdermal or wound dressing patches. [ABSTRACT FROM AUTHOR]

Green synthesis of nanoparticles has fuelled the use of biomaterials to synthesise a variety of metallic nanoparticles. The current study investigates the use of xylanases of Aspergillus niger L3 (NEA) and Trichoderma longibrachiatum L2 (TEA) to synthesise silver nanoparticles (AgNPs). Characterisation of AgNPs was carried out using UV–Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), and transmission electron microscopy, while their effectiveness as antimicrobial, antioxidant, catalytic, anticoagulant, and thrombolytic agents were determined. The colloidal AgNPs was brownish with surface plasmon resonance at 402.5 and 410 nm for NEA‐AgNPs and TEA‐AgNPs, respectively; while FTIR indicated that protein molecules were responsible for the capping and stabilisation of the nanoparticles. The spherical nanoparticles had size of 15.21–77.49 nm. The nanoparticles significantly inhibited the growth of tested bacteria (63.20–88.10%) and fungi (82.20–86.10%), and also scavenged DPPH (37.48–79.42%) and hydrogen peroxide (20.50–96.50%). In addition, the AgNPs degraded malachite green (78.97%) and methylene blue (25.30%). Furthermore, the AgNPs displayed excellent anticoagulant and thrombolytic activities using human blood. This study has demonstrated the potential of xylanases to synthesise AgNPs which is to the best of our knowledge the first record of such. The present study underscores the relevance of xylanases in nanobiotechnology. [ABSTRACT FROM AUTHOR]

Over loading of iron oxide nanoparticles can causes the liver injury through overproduction of free radicals. Zataria multiflora Boiss. (Lamiaceae) has been used for many years in folk medicine due to its antioxidant and antibacterial activities. This study evaluates -for the first time- the effect of Z. multiflora essential oil (EO) against iron oxide nanoparticles hepatotoxicity in rat model. Male Wistar rats were divided randomly into 4 groups; control group (C), non-treated control group (NT), treatment groups, nanoparticles plus Z. multiflora EO at 100 and 200 mg/kg b.w. In following, the liver and blood tissue were collected for estimating oxidative stress/antioxidant parameters including lipid peroxidation (LP), glutathione (GSH), glutathione-S-transferase (GST), and liver enzyme asparate transaminase (AST) and also histopathological examinations. Iron oxide nanoparticles toxicity produced a significant increase in the levels of LP, ferric reducing ability of plasma (FRAP), and AST activity concomitant with decrease in the levels of GSH and GST activity compared to the control group. However, in the treatment groups received Z. multiflora EO, the levels of LP and AST activity reduced together with increasing in GSH content and GST activity were significantly reported. Histopathological studies also supported the biochemical assessments indicating hepatic improvements induced by nanoparticles. Z. multiflora EO protected the liver from injuries induced by iron oxide nanoparticles which can be correlated with its antioxidant activities. This can be a valuable candidate in modulating the oxidative hepatic injuries. [ABSTRACT FROM AUTHOR]

Biologically and chemically useful hydrazinoimidazolines were evaluated as antioxidant and antihaemolytic agents. 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH•), galvinoxyl radical (GOR), nitric oxide (NO) and hydrogen peroxide (H2O2) scavenging assays, ferric ions reducing power assay, and ex vivo model of rat erythrocytes exposed to 2,2′-azobis(2-methylpropionamidine)dihydrochloride (AAPH) or H2O2 were used. The most potent DPPH• scavengers proved to be hydrazinoimidazolines 3, 2, and 4, revealing excellent antiradical effects - superior or comparable to that of all antioxidant standards used. Moreover, these molecules showed strong NO neutralising potencies - better to that of ascorbic acid (AA) (3), 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox) (3 and 2), butylated hydroxytoluene (BHT) (3 and 2), and butylated hydroxyanisole (BHA) (3, 2, and 4). Compound 4 was also effective in GOR scavenging. The excellent scavenger of GOR, NO, and H2O2 proved to be structure 5, with the potency superior or comparable to the majority of antioxidant standards used. In turn, compound 9 was effective in H2O2 and GOR neutralisation. All hydrazinoimidazolines revealed the reducing power that is higher than BHT. Moreover, the protective effects of most test compounds on oxidatively stressed erythrocytes were observed. Some structure-activity relationships were disclosed. A significance of the primary hydrazino group on antioxidant effects was confirmed. The most likely DPPH• and GOR scavenging mechanisms for test compounds were propound. Among all the investigated molecules, hydrazinoimidazolines 5, 3, 2, 4, and 9, due to their excellent or good antiradical activities, can represent promising antioxidant candidates with prospective utility for prevention of diseases related to reactive oxygen/nitrogen species. [ABSTRACT FROM AUTHOR]

Background: Tabebuia rosea (Bertol.) DC. is a neotropical tree used in traditional medicine in the Northern coast of Colombia as well as Latin America for infectious diseases treatment. Few studies have evaluated the biological activity of this species. Objective: The objective of this study is to determine the antioxidant, anti-inflammatory, and antiproliferative potential of leaf and inner bark extracts from T. rosea. Materials and Methods: The antioxidant activity was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) methods. The anti-inflammatory activity was evaluated in lipopolysaccharide-stimulated murine macrophages. In vitro antiproliferative effect was determined in HepG2, HeLa, MCF-7, and B16F10 cell lines. Results: The highest DPPH radical scavenging activity was observed for T. rosea ethyl acetate leaf extract (IC50 of 157.5 ± 2.4 μg/mL). This extract also induced the best antioxidant activity as determined by ORAC (11,112.2 ± 1,255.3 μmol TE/g of extract). Moreover, T. rosea leaf n-hexane, chloroform, and aqueous extracts, in addition to inner bark aqueous extract did inhibit nitric oxide production by over 90%. In addition, inner bark extracts markedly inhibited prostaglandins E2 and tumor necrosis factor alpha (>90%). The best antiproliferative activity was displayed by the inner bark chloroform extract against HepG2 (selectivity index [SI] = 5.50) and B16F10 (SI = 3.18) cell lines. Conclusion: These results demonstrate the potential biological activity of T. rosea extracts. [ABSTRACT FROM AUTHOR]

The present study was designed to investigate the immunomodulatory effects of Aloe vera, Curcuma longa, Echinacea purpurea, Lavandula officinalis, Origanum vulgare, Panax ginseng, and Rheum officinale extracts on leukocytes purified from rainbow trout (Oncorhynchus mykiss) head kidney. The cells were cultured in a medium containing increasing doses of extracts; afterwards, they were tested for reactive oxygen species production after stimulation with phorbol myristate acetate (PMA) and proliferation in the presence or absence of phytohemagglutinin from Phaseolus vulgaris (PHA-P). After a 2-h exposure, the extracts of L. officinalis, O. vulgare, and R. officinale strongly reduced the oxidative burst activity of PMA-stimulated leukocytes, in a dose-dependent manner (P ≤ 0.05). A. vera, C. longa, E. purpurea, and P. ginseng extracts reduced this response with lower efficacy and especially at lower concentrations. On the contrary, the highest concentration of ginseng extract stimulated the respiratory burst of leukocytes compared to untreated control cells. After a 72-h exposure, the extracts of L. officinalis, R. officinale, C. longa, E. purpurea, and P. ginseng had a clear dose-dependent stimulatory effect on leukocyte proliferation (P ≤ 0.05). The results suggest that these medicinal plants can be considered as reliable sources of new antioxidants or immunostimulants to be used in aquaculture. [ABSTRACT FROM AUTHOR]

Global production of the two major poultry products, meat and eggs, has increased quickly. This, in turn, indicates both the relatively low cost and the customers' desire for these secure and high-quality products. Natural feed additives have become increasingly popular to preserve and enhance the health and productivity of poultry and livestock. We consume a lot of polyphenols, which are a kind of micronutrient. These are phytochemicals with positive effects on cardiovascular, cognitive, anti-inflammatory, detoxifying, anti-tumor, anti-pathogen, a catalyst for growth, and immunomodulating functions, among extra health advantages. Furthermore, high quantities of polyphenols have unknown and occasionally unfavorable impacts on the digestive tract health, nutrient assimilation, the activity of digestive enzymes, vitamin and mineral assimilation, the performance of the laying hens, and the quality of the eggs. This review clarifies the numerous sources, categories, biological functions, potential limitations on usage, and effects of polyphenols on poultry performance, egg composition, exterior and interior quality traits. [ABSTRACT FROM AUTHOR]

This in vitro study aimed to evaluate the aesthetic compromise generated in adhesive interface of ceramic laminate veneer luted after tooth bleaching and the use of antioxidant agents. Thus, the chromatic coordinates and whitening index (WI D) were evaluated, comparing whiteness changes (ΔWI D) results to perceptibility and acceptability thresholds. In total, 88 bovine enamel samples (7 × 8 × 4 mm; n = 8) were submitted to the ceramic laminate veneer luting protocol according to surface treatment (unbleached and bleached enamel), antioxidant agents (control; 10% ascorbic acid and 10% α-tocopherol), and luting periods (after 24 h and after 14 days). To lute IPS e.max ceramic restorations (7 × 8 × 0.6 mm), Tetric N-Bond Universal adhesive system and Variolink Aesthetic LC resin cement were used. An ultraviolet–visible spectrophotometer (UV–VIS) was utilized to measure CIE L*a*b* coordinates prior to and after UV-B artificial accelerated aging for 252, 504, and 756 h. L*, a*, and b* axes were evaluated separately, and the whitening stability (Δ WI D) effect was assessed by varying the whiteness index for dentistry (WI D). The 50:50% visual threshold was used to evaluate ΔWI D values (whiteness perceptibility [WPT] and whiteness acceptability [WAT]). Color parameters changes (Δ L* Δ a* Δ b*), WI D , and ΔWI D data were subjected to 2-way repeated measures ANOVA followed by Tukey's test (α = 0.05). Different UV-aging periods influenced the chromatic coordinates, WI D, and ΔWI D of the ceramic restorations regardless of the bleaching treatment, antioxidant solutions and luting periods (P <.05). In general, ΔWI D values after UV-aging periods were above perceptibility and acceptability thresholds (WPT = 0.72 and WAT = 2.62, respectively) for all experimental groups (P <.05). Unbleached and 10% ascorbic acid-treated enamels luted after 14 days of the antioxidant action exhibited lower Δ L* and Δ b* values, while control group showed lower Δ a* values. All experimental groups showed similar performance on ΔWI D compared to the control group, regardless of the UV-aging period analyzed (P >.05). α-tocopherol is a suitable antioxidant solution to be used 24 h post enamel bleaching not compromising clinical acceptability of ceramic laminate veneers. The adhesive interface of ceramic laminate veneers may appear darker after the use of antioxidant agents affecting the clinical acceptability of the restorations. • Effect of antioxidant agents (AA) and bleaching treatment (BT) was evaluated on aesthetic parameters of ceramic veneers. • Different UV-aging periods influenced the Δ L*, Δ a*, Δ b*, WI D , and ΔWI D of the ceramic restorations. • ΔWI D values after UV-aging periods were above perceptibility (PT) and acceptability (AT) thresholds. • BLE-αT-24H group presented similar aesthetic parameters compared to the control group. • α-tocopherol is a suitable AA to be used 24 h after BT considering the PT and AT thresholds. [ABSTRACT FROM AUTHOR]