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Our group has seen great promise in using substituted diaryl-hydrazones to alleviate oxidative stress in preeclampsia. Specifically, fluorinated diaryl-hydrazones have shown great efficacy, confirmed via antioxidant assays and animal trials using pregnant mice. In addition to efficient antioxidant properties, these diaryl-hydrazones are also considered non-toxic. While the synthesis of these compounds is relatively simple, it commonly utilizes undesirable solvents and glacial acetic acid as the catalyst; additional solvents are needed for the isolation of the desired products, which negatively affects the green synthesis of the hydrazones. To combat this possible industrial roadblock, we have begun incorporating the use of hydrostatic high pressure (HHP) in the synthesis. The use of HHP allowed us to synthesize substituted diaryl-hydrazones in a 1:1 molar ratio without the need for solvents or acid catalysts. The optimized procedure can produce nearly quantitative yields, leading to an easier isolation of the products. Different HHP methodologies, such as constant high-pressure treatment and cycling (with different number of cycles, holding and decompression times) were applied and cycling was observed to be the most efficient activation for the majority of the reactions. Stability experiments were also conducted with one of the products and observed that although the solid-state storage does not alter the hydrazone, storing it in various solvents may significantly decrease the concentration of the active component which should be considered when performing the biochemical/biological assays. [ABSTRACT FROM AUTHOR]

Anthocyanins are the main plant pigments responsible for the color of flowers, fruits, and vegetative organs of many plants, and are applied also as safe food colorants. They are efficient antioxidants. In this review, the reactivity of anthocyanins and their aglycones, anthocyanidins, in the main antioxidant assays, and their reactions with reactive oxygen and nitrogen species, effects of interactions with other compounds and metal ions on the antioxidant activity of anthocyanins and the electrochemical properties of anthocyanins are presented. Numerous cases of attenuation of oxidative stress at the cellular and organismal levels by anthocyanins are cited. The direct and indirect antioxidant action of anthocyanins, the question of the specificity of anthocyanin action in complex extracts, as well as limitations of cellular in vitro assays and biomarkers used for the detection of antioxidant effects of anthocyanins, are critically discussed. [ABSTRACT FROM AUTHOR]

Cynanchum auriculatum Royle ex Wight (CA) is a traditional medicinal and edible plant in China. This study aimed to isolate and characterize the phenolic compounds of C. auriculatum to identify its main antioxidant constituents. Polyphenols were extracted using an ultrasound-assisted ethanol extraction method, followed by partitioning with ethyl acetate. The ethyl acetate extract was then purified through thin-layer chromatography, silica gel column chromatography, and reverse-phase silica gel column chromatography. Three monomeric compounds—cynandione A (I), 2,5-dihydroxyacetophenone (II), and radix piperacanthone (III)—were identified through their physical and chemical properties, UV and IR spectra, and liquid chromatography–mass spectrometry (LC-MS/MS). Vitamin C (VC) and 2,4-dihydroxyacetophenone were used as controls to evaluate the antioxidant potential of the two most abundant monomers. Antioxidant assays demonstrated that 2,5-dihydroxyacetophenone and cynandione A exhibited strong antioxidant activity at lower concentrations, whereas 2,4-dihydroxyacetophenone showed significantly weaker activity. Furthermore, cynandione A displayed superior cellular antioxidant activity compared to 2,5-dihydroxyacetophenone, indicating its potential as a promising bioactive compound. In conclusion, this study provides valuable insights into the phenolic composition of C. auriculatum and highlights cynandione A as a key antioxidant, paving the way for future research on its therapeutic applications. [ABSTRACT FROM AUTHOR]

Searching for protein sources for fish diet formulations has become essential. So, this investigation evaluated the impacts of kidney bean protein hydrolysate (KPH) (Phaseolus vulgaris L) as a new plant protein source in the diets of Nile tilapia, Oreochromis niloticus (O. niloticus), on the fish growth, hematology, biochemistry, antioxidant status, and tissue histomorphology. Two hundred fingerlings (37.38 ± 0.058 g) were allocated to five experimental treatments (TRTs) in 20 glass tanks for a feeding trial of about 70 days. KPH was supplemented to the diets by five levels: 0, 5, 10, 15, or 20%. A linear increase in the fish growth was observed by dietary KPH supplementation. The final body weight was increased by 6, 12, 15, and 18% for KPH5, KPH10, KPH15, and KPH20, respectively. The red blood cells, hemoglobin, and packed cell volume were increased in the KPH15 and KPH20 groups compared to the KPH0 group. The serum TP and β2-globulin levels were increased in KPH-supplemented TRTs (P < 0.05). Reduced serum MDA levels and increased SOD activity were observed in KPH15 and KPH20 groups (P < 0.01). The best intestinal histomorphometry was seen in the KPH15 group. Histological analysis of the treated groups’ liver and kidney sections revealed a comparatively normal histomorphology. Splenic tissues of the treated groups were normal, with more prevalent lymphoid elements, especially in the KPH10 and KPH15 groups. In conclusion, KPH could be a potential source of protein in Nile tilapia diets with good results for fish growth, blood biochemistry, and antioxidant status. KPH supplementation had no adverse effects on fish organs. The recommended inclusion level was 15% of the diet. [ABSTRACT FROM AUTHOR]

Orange-fleshed non-netted honeydew melon has high nutritional and economic potential, being widely appreciated as a refreshing sweet fruit. Therefore, evaluating commercial samples of such relevant products for the fresh fruit market is of great importance. This study investigated the antioxidant capacity, quality parameters, and chemical composition of honeydew melons from the Brazilian market. The values of pH and °Brix determined for melon samples were 6.5 ± 0.30 and 9.2 ± 0.80 g/100 g (fresh weight), respectively, which agree with the results expected for high-quality melons. The chromatography analysis revealed sucrose (49% of total sugar) as the main sugar, followed by fructose (30%) and glucose (21%). Carotenoids, which are directly linked to the characteristic orange color, showed a total level of 270.59 µg/g (dry weight). Additionally, the higher b* value compared to a* value indicates the highest yellow contribution. Regarding the antioxidant assays, in addition to presenting antioxidant capacity for both methods applied, DPPH and FRAP, levels ranging from 16.40 ± 0.21 µmol ascorbic acid equivalent/g to 56.98 ± 0.80 µmol Trolox equivalent/g (dry weight) were reported in melon extracts. Moreover, the results were higher in terms of FRAP than DPPH. Therefore, the results underscore the evaluated honeydew melons as valuable sources of bioactive compounds, such as carotenoids and phenolics, which contribute to their antioxidant properties. Besides, analyses of color, pH, and total soluble solids content also reflect the quality attributes. [ABSTRACT FROM AUTHOR]

Erectile dysfunction (ED) which is the inability to maintain an erection during sexual activity, is one of the most prevalent sexual dysfunctions, with mild to severe ED affecting an estimated 5-20% of men globally and about 322 million men may be affected globally by 2025.

Background/Objectives: Phloroglucinol (PHL), a phenolic compound extracted from the brown alga Rosenvingea intricata, exhibits potent antioxidant and anticancer properties. This study aims to extract, purify, and characterize PHL, and further develop functionalized zinc oxide nanoparticles (ZnO NPs) loaded with PHL to enhance its therapeutic potential. Methods: PHL was extracted using acetone and purified through Sephadex LH-20 column chromatography, yielding a highly enriched fraction (F-3). The purified compound was characterized by FTIR, HPLC, NMR, and LC-MS. ZnO NPs were synthesized, PEGylated, and conjugated with PHL, forming ZnO-PEG-PHL NPs. Their characterization included DLS, zeta potential, XRD, SEM-EDAX, and encapsulation efficiency studies. Antioxidant assays (DPPH, FRAP, ABTS, RPA) were performed and in vitro cytotoxicity on A549 lung cancer cells were determined to evaluate the therapeutic efficacy of PHL. Results: The purified PHL fraction showed a high phenolic content (45.65 PHL mg/g), which was was confirmed by spectral analysis. The ZnO-PEG-PHL NPs increased in size from 32.36 nm to 46.68 nm, with their zeta potential shifting from −37.87 mV to −26.82 mV. The antioxidant activity was superior for the ZnO-PEG-PHL NPs in all assays, while the in vitro cytotoxicity tests showed an IC50 of 40 µg/mL compared to 60 µg/mL for the ZnO NPs and 70 µg/mL for PHL. Apoptotic studies revealed significant cell cycle arrest and apoptosis induction. Conclusions: The synthesized ZnO-PEG-PHL NPs demonstrated enhanced antioxidant and anticancer properties, making them promising candidates for cancer therapy and antioxidant applications. [ABSTRACT FROM AUTHOR]

Carnation (Dianthus caryophyllus L.) plant is native to the Mediterranean region. However, it is cultivated throughout the world for its beautiful flowers. In Pakistan, its flower yield and quality is very poor due to numerous abiotic stresses including salt stress, which drastically decreases plant growth, flower yield and quality. The aim of the present study was to evaluate foliar application of moringa and mint leaf extracts (0.03% each, separately) to mitigate negative effects of irrigation water salinity (0, 30 and 60 mM NaCl) on carnation plants. Salinity treatments reduced plant height, plant fresh and dry weights, leaf number, root length, number of flower buds, number of flowers, fresh and dry weights of flowers, photosynthetic pigments, i.e. chlorophyll a, chlorophyll b and total chlorophyll, and carotenoid content as well as ascorbic acid content. However, number of branches increased at 30 mM irrigation water salinity level and then decreased at 60 mM, while hydrogen peroxide (H2O2), malondialdehyde (MDA), peroxidase (POD) and catalase (CAT) activities increased with an increase in salinity level. Leaf length, root fresh weight, total phenolic content and superoxide dismutase (SOD) activity in leaves remained unaffected due to the salinity treatments. Over all, performance of mint leaf extract was better that of moringa; however, moringa leaf extract was more effective in improving leaf carotenoids content than mint leaf extract. Both, extracts reduced H2O2 and MDA contents. Leaf length, root length, root fresh weight, fresh weight of flowers and total phenolic content remained unaffected due to foliar application of extracts. Present study revealed that plant extracts especially mint leaf extract had good potential to mitigate negative effects of salt stress in carnation through regulation of metabolic and biochemical capabilities. [ABSTRACT FROM AUTHOR]

Pinus roxburghii and Pinus wallichiana are traditionally plants used for various medicinal purposes worldwide. The present study focused on evaluating the phytochemical compounds and the free radical scavenging potential in various parts of P. roxburghii and P. wallichiana through in vitro and in silico study. Crude extract of the fresh leaves was obtained using methanol while steam distillation method was used for the extraction of the essential oil. The phytochemicals were determined by standard methods. Antioxidant Potential of the phytochemicals was performed using 2,2-diphenyl-1-picrylhydrazyl (DPPH), Hydroxyl radical (OH) inhibition, Ferric ion reducing power (FRAP) and Phosphomolybedenum complex (PMC) assays. The interactions between the total phenolics and flavonoids of the selected plants and virulent target proteins of the pathogenic bacteria were identified, characterized, and examined using Molecular Operating Environment (MOE) software. The fresh leaves of P. roxburghii, exhibited the highest total phenolic (744.6 ± 27.0 mg GAE/100 g) and carotenoid content (21.4 ± 0.4 mg/g) that was significantly varied from other samples. The EO of P. wallichiana, showed the highest total flavonoid content. In P. roxburghii and P. wallichiana, the fresh leaves exhibited the highest percentage of scavenging potential against the DPPH radical. Additionally, the EO from P. roxburghii and P. wallichiana have significant potential to reduce ferric ions, and molybdate ions, respectively) with significant differences. The molecular docking showed a significant interaction of compounds present in these pines leaves with Exotoxin A and Elastase B proteins. The essential oil (EO), hydrosol (HS), and crude extract derived from P. roxburghii and P. wallichiana could be exploited as natural sources of antioxidants, anti-inflammatory agents, and innovative medications against the human pathogen, Pseudomonas aeruginosa.

Background: Finding herbal herbicides with biodegradability and selectivity against weeds is an interesting and vital challenge for human health. The study was considered to analyze the phytochemical profile, phytotoxicity and biological activities of Rindera lanata together with a molecular docking perspective. The study was considered to analyze the phytochemical profile, phytotoxicity and biological activities of Rindera lanata together with a molecular docking perspective. Methods: Aerial parts of R. lanata were successively solvent extracted with the Soxhlet apparatus, followed by maceration. Different chromatography methods were employed to isolate and purify the major compounds of the plant. The compounds were assigned by spectroscopic methods, containing 1D and 2D NMR (Nuclear Magnetic Resonance). Several in vitro antioxidant assays, together with an antimicrobial assay, alongside the allelopathic property on the germination of Cuscuta campestris seeds, were assessed upon the extracts. As a final point, molecular docking was conducted to evaluate the interactions among the identified compounds with 4-hydroxyphenyl pyruvate dioxygenase (HPPD), glutamine synthetase (GS), and acetohydroxyacid synthetase (AHAS). Results: Phytochemical analysis of the extracts led to the identification of a new flavonoid 3, 5, 4’-tri-O-methylquercetin (1), apigenin (2), chrysoeriol (3), luteolin-7-O-glucoside (4) and rutin (5). It was exposed that ethyl acetate extract not only illustrated the highest antioxidant effect in all the in vitro assays but also exhibited the maximum antibacterial effect against Staphylococcus epidermidis. Effectively, it showed conventional allelopathic activity in preventing germination, seedling length and seedling weight growth of C. campestris seeds, as well as a concentration-dependent enhancement (p≤0.05). Docking analysis results indicated that rutin had a good affinity for HPPD, GS and AHAS enzymes, with docking score values of -11.454, -10.422 and -10.152 kJ/mol, respectively. Conclusion: The present study suggested that isolated flavonoids from R. lanata could be used as the lead compounds in the development of natural herbicides for strong bonds in the active region of HPPD, GS and AHAS enzymes.

Stevia rebaudiana Bertoni, a no-calorie natural sweetener, contains a plethora of polyphenols that exert antioxidant properties with potential medicinal significance. Due to the variety of functional groups, polyphenols exhibit varying solubility depending on the nature of the extraction solvents (water, organic, or their mixtures, defined further on as hydroalcoholic extracts). In the present study, we performed a systematic review, following PRISMA guidelines, and meta-analysis, synthesizing all available data from 45 articles encompassing 250 different studies. Our results showed that the total phenolic content (TPC) of hydroalcoholic and aqueous extracts presents higher values (64.77 and 63.73 mg GAE/g) compared to organic extracts (33.39). Total flavonoid content (TFC) was also higher in aqueous and hydroalcoholic extracts; meta-regression analysis revealed that outcomes in different measuring units (mg QE/g, mg CE/g, and mg RUE/g) do not present statistically significant differences and can be synthesized in meta-analysis. Using meta-regression analysis, we showed that outcomes from the chemical-based ABTS, FRAP, and ORAC antioxidant assays for the same extract type can be combined in meta-analysis because they do not differ statistically significantly. Meta-analysis of ABTS, FRAP, and ORAC assays outcomes revealed that the antioxidant activity profile of various extract types follows that of their phenolic and flavonoid content. Using regression meta-analysis, we also presented that outcomes from SOD, CAT, and POX enzymatic antioxidant assays are independent of the assay type (p-value = 0.905) and can be combined. Our study constitutes the first effort to quantitatively and statistically synthesize the research results of individual studies using all methods measuring the antioxidant activity of stevia leaf extracts. Our results, in light of evidence-based practice, uncover the need for a broadly accepted, unified, methodological strategy to perform antioxidant tests, and offer documentation that the use of ethanol:water 1:1 mixtures or pure water can more efficiently extract stevia antioxidant compounds. [ABSTRACT FROM AUTHOR]

ABSTRACT: Orange-fleshed non-netted honeydew melon has high nutritional and economic potential, being widely appreciated as a refreshing sweet fruit. Therefore, evaluating commercial samples of such relevant products for the fresh fruit market is of great importance. This study investigated the antioxidant capacity, quality parameters, and chemical composition of honeydew melons from the Brazilian market. The values of pH and °Brix determined for melon samples were 6.5 ± 0.30 and 9.2 ± 0.80 g/100 g (fresh weight), respectively, which agree with the results expected for high-quality melons. The chromatography analysis revealed sucrose (49% of total sugar) as the main sugar, followed by fructose (30%) and glucose (21%). Carotenoids, which are directly linked to the characteristic orange color, showed a total level of 270.59 µg/g (dry weight). Additionally, the higher b* value compared to a* value indicates the highest yellow contribution. Regarding the antioxidant assays, in addition to presenting antioxidant capacity for both methods applied, DPPH and FRAP, levels ranging from 16.40 ± 0.21 µmol ascorbic acid equivalent/g to 56.98 ± 0.80 µmol Trolox equivalent/g (dry weight) were reported in melon extracts. Moreover, the results were higher in terms of FRAP than DPPH. Therefore, the results underscore the evaluated honeydew melons as valuable sources of bioactive compounds, such as carotenoids and phenolics, which contribute to their antioxidant properties. Besides, analyses of color, pH, and total soluble solids content also reflect the quality attributes.

Our group has seen great promise in using substituted diaryl-hydrazones to alleviate oxidative stress in preeclampsia. Specifically, fluorinated diaryl-hydrazones have shown great efficacy, confirmed via antioxidant assays and animal trials using pregnant mice. In addition to efficient antioxidant properties, these diaryl-hydrazones are also considered non-toxic. While the synthesis of these compounds is relatively simple, it commonly utilizes undesirable solvents and glacial acetic acid as the catalyst; additional solvents are needed for the isolation of the desired products, which negatively affects the green synthesis of the hydrazones. To combat this possible industrial roadblock, we have begun incorporating the use of hydrostatic high pressure (HHP) in the synthesis. The use of HHP allowed us to synthesize substituted diaryl-hydrazones in a 1:1 molar ratio without the need for solvents or acid catalysts. The optimized procedure can produce nearly quantitative yields, leading to an easier isolation of the products. Different HHP methodologies, such as constant high-pressure treatment and cycling (with different number of cycles, holding and decompression times) were applied and cycling was observed to be the most efficient activation for the majority of the reactions. Stability experiments were also conducted with one of the products and observed that although the solid-state storage does not alter the hydrazone, storing it in various solvents may significantly decrease the concentration of the active component which should be considered when performing the biochemical/biological assays.

Cynanchum auriculatum Royle ex Wight (CA) is a traditional medicinal and edible plant in China. This study aimed to isolate and characterize the phenolic compounds of C. auriculatum to identify its main antioxidant constituents. Polyphenols were extracted using an ultrasound-assisted ethanol extraction method, followed by partitioning with ethyl acetate. The ethyl acetate extract was then purified through thin-layer chromatography, silica gel column chromatography, and reverse-phase silica gel column chromatography. Three monomeric compounds—cynandione A (I), 2,5-dihydroxyacetophenone (II), and radix piperacanthone (III)—were identified through their physical and chemical properties, UV and IR spectra, and liquid chromatography–mass spectrometry (LC-MS/MS). Vitamin C (VC) and 2,4-dihydroxyacetophenone were used as controls to evaluate the antioxidant potential of the two most abundant monomers. Antioxidant assays demonstrated that 2,5-dihydroxyacetophenone and cynandione A exhibited strong antioxidant activity at lower concentrations, whereas 2,4-dihydroxyacetophenone showed significantly weaker activity. Furthermore, cynandione A displayed superior cellular antioxidant activity compared to 2,5-dihydroxyacetophenone, indicating its potential as a promising bioactive compound. In conclusion, this study provides valuable insights into the phenolic composition of C. auriculatum and highlights cynandione A as a key antioxidant, paving the way for future research on its therapeutic applications.

The process of developing of new drugs is greatly hampered by their inadequate physicochemical, pharmacokinetic, and intrinsic characteristics. In this regard, the selected chloro indolinone, (Z)-6-chloro-3-(2-chlorobenzylidene)indolin-2- one (C1), and nitro indolinone, (Z)-6-chloro-3-(2-nitrobenzylidene)indolin-2- one (C2), were subjected to SwissADME and density function theory (DFT) analysis. For compounds C1 and C2, the BOILED-Egg pharmacokinetic model predicted intestinal absorption, blood-brain barrier (BBB) penetration, and p-glycoprotein interaction. According to the physicochemical analysis, C1 has exceptional drug-like characteristics suitable for oral absorption. Despite only being substrates for some of the major CYP 450 isoforms, compounds C1 and C2 were anticipated to have strong plasma protein binding and efficient distribution and block these isoforms. The DFT study using the B3LYP/6-311G(d,p) approach with implicit water effects was performed to assess the structural features, electronic properties, and global reactivity parameters (GRP) of C1 and C2. The DFT results provided further support for other studies, implying that C2 is more water-soluble than C1 and that both compounds can form hydrogen bonds and (weak) dispersion interactions with other molecules, such as solvents and biomolecules. Furthermore, the GRP study suggested that C1 should be more stable and less reactive than C2. A concentration-dependent 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'- azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity was shown by both C1 and C2. In brief, this finding has provided a strong foundation to explore furtherthe therapeutic potential of these molecules against a variety of human disorders. [ABSTRACT FROM AUTHOR]

This paper presents the results of a study of the effects of the lanthanide ions Ce3+, Pr3+, Nd3+ and Sm3+ on the electronic structure and antioxidant and biological (antimicrobial and cytotoxic) properties of p-coumaric acid (p-CAH2). Structural studies were conducted via spectroscopic methods (FTIR, ATR, UV). Thermal degradation studies of the complexes were performed. The results are presented in the form of TG, DTG and DSC curves. Antioxidant properties were determined via activity tests against DPPH, ABTS and OH radicals. The reducing ability was tested via CUPRAC assays. Minimum inhibitory concentrations (MICs) of the ligand and lanthanide complexes were determined on E. coli, B. subtilis and C. albicans microorganisms. The antimicrobial activity was also determined using the MTT assay. The results were presented as the relative cell viability of C. albicans, P. aeruginosa, E. coli and S. aureus compared to controls and expressed as percentages. In the obtained complexes in the solid phase, lanthanide ions coordinate three ligands in a bidentate chelating coordination mode through the carboxyl group of the acid. Spectroscopic analysis showed that lanthanide ions increase the aromaticity of the pi electron system of the ligand. Thermal analysis showed that the complexes are hydrated and have a higher thermal stability than the ligand. The products of thermal decomposition of the complexes are lanthanide oxides. In the aqueous phase, the metal combines with the ligand in a 1:1 molar ratio. Antioxidant activity tests showed that the complexes have a similar ability to remove free radicals. ABTS and DPPH tests showed that the complexes have twice the ability to neutralise radicals than the ligand, and a much higher ability to remove the hydroxyl radical. The abilities of the complexes and the free ligand to reduce Cu2+ ions in the CUPRAC test are at a similar level. Lanthanide complexes of p-coumaric acid are characterised by a higher antimicrobial capacity than the free ligand against Escherichia coli bacteria, Bacillus subtilis and Candida albicans fungi. [ABSTRACT FROM AUTHOR]

Background/Objectives: Phloroglucinol (PHL), a phenolic compound extracted from the brown alga Rosenvingea intricata, exhibits potent antioxidant and anticancer properties. This study aims to extract, purify, and characterize PHL, and further develop functionalized zinc oxide nanoparticles (ZnO NPs) loaded with PHL to enhance its therapeutic potential. Methods: PHL was extracted using acetone and purified through Sephadex LH-20 column chromatography, yielding a highly enriched fraction (F-3). The purified compound was characterized by FTIR, HPLC, NMR, and LC-MS. ZnO NPs were synthesized, PEGylated, and conjugated with PHL, forming ZnO-PEG-PHL NPs. Their characterization included DLS, zeta potential, XRD, SEM-EDAX, and encapsulation efficiency studies. Antioxidant assays (DPPH, FRAP, ABTS, RPA) were performed and in vitro cytotoxicity on A549 lung cancer cells were determined to evaluate the therapeutic efficacy of PHL. Results: The purified PHL fraction showed a high phenolic content (45.65 PHL mg/g), which was was confirmed by spectral analysis. The ZnO-PEG-PHL NPs increased in size from 32.36 nm to 46.68 nm, with their zeta potential shifting from −37.87 mV to −26.82 mV. The antioxidant activity was superior for the ZnO-PEG-PHL NPs in all assays, while the in vitro cytotoxicity tests showed an IC50 of 40 µg/mL compared to 60 µg/mL for the ZnO NPs and 70 µg/mL for PHL. Apoptotic studies revealed significant cell cycle arrest and apoptosis induction. Conclusions: The synthesized ZnO-PEG-PHL NPs demonstrated enhanced antioxidant and anticancer properties, making them promising candidates for cancer therapy and antioxidant applications.

The process of developing of new drugs is greatly hampered by their inadequate physicochemical, pharmacokinetic, and intrinsic characteristics. In this regard, the selected chloro indolinone, (Z)-6-chloro-3-(2-chlorobenzylidene)indolin-2-one (C1), and nitro indolinone, (Z)-6-chloro-3-(2-nitrobenzylidene)indolin-2-one (C2), were subjected to SwissADME and density function theory (DFT) analysis. For compounds C1 and C2, the BOILED-Egg pharmacokinetic model predicted intestinal absorption, blood–brain barrier (BBB) penetration, and p-glycoprotein interaction. According to the physicochemical analysis, C1 has exceptional drug-like characteristics suitable for oral absorption. Despite only being substrates for some of the major CYP 450 isoforms, compounds C1 and C2 were anticipated to have strong plasma protein binding and efficient distribution and block these isoforms. The DFT study using the B3LYP/6-311G(d,p) approach with implicit water effects was performed to assess the structural features, electronic properties, and global reactivity parameters (GRP) of C1 and C2. The DFT results provided further support for other studies, implying that C2 is more water-soluble than C1 and that both compounds can form hydrogen bonds and (weak) dispersion interactions with other molecules, such as solvents and biomolecules. Furthermore, the GRP study suggested that C1 should be more stable and less reactive than C2. A concentration-dependent 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity was shown by both C1 and C2. In brief, this finding has provided a strong foundation to explore further the therapeutic potential of these molecules against a variety of human disorders.

Two new ruthenium(II)-complexes, [Ru(Ang)((benzene)Cl2] (RuB-Ang) and [Ru(Ang)((p-cymene)Cl2] (RuC-Ang), were synthesized using andrographolide (Ang) as a ligand with [RuCl2(arene)]2 (arene = benzene or p-cymene) and characterized by various spectroscopic techniques. These techniques ascertained the formation of the complexes. An assessment of the antioxidant activity of the compounds indicated better scavenging activity against ABTS•+, DPPH•, O2−, NO• and OH− radicals. The cytotoxic activities of RuB-Ang and RuC-Ang have been evaluated against A549 (human lung) and HeLa (human cervical) cancer cell lines. The complexes exhibited superior anticancer activity to cisplatin and was non-toxic towards human umbilical vein endothelial (HUVEC) cells. The morphological changes of the HeLa and A549 cells with the complexes have been studied by AO-EB and DAPI staining methods. The cytotoxic nature of the compounds was RuC-Ang > RuB-Ang > cisplatin > ligand. [ABSTRACT FROM AUTHOR]

Nutrition has crucial effects and a significant role in disease prevention. Recently, nutraceuticals have attracted much attention in scientific research due to their pleiotropic effects and relatively non-toxic behavior. Among the biological effects displayed by plants belonging to the Lamiaceae family, such as antibacterial, anticancer, anti-inflammatory, and anticholinesterase, sage is well known for its antioxidant properties and is a rich source of numerous compounds that are biologically active, amongst them polyphenols, with more than 160 types identified. In this review we summarized some of the significant studies published in the last decade reporting the most employed extraction methods and the different assays that are useful for establishing the antioxidant properties of some sage species. Even though the scientific literature contains plenty of data regarding the antioxidant properties of many sage species, further studies are needed in order to gain a deeper understanding of the mechanism of action and the compounds responsible for their antioxidant activity. Finally, it should be taken into account that the data on the antioxidant properties of sage extracts are often difficult to compare with each other, since a series of variables in the extraction procedures, the type of assay used, and standardization may affect the final result. [ABSTRACT FROM AUTHOR]

Stevia rebaudiana Bertoni, a no-calorie natural sweetener, contains a plethora of polyphenols that exert antioxidant properties with potential medicinal significance. Due to the variety of functional groups, polyphenols exhibit varying solubility depending on the nature of the extraction solvents (water, organic, or their mixtures, defined further on as hydroalcoholic extracts). In the present study, we performed a systematic review, following PRISMA guidelines, and meta-analysis, synthesizing all available data from 45 articles encompassing 250 different studies. Our results showed that the total phenolic content (TPC) of hydroalcoholic and aqueous extracts presents higher values (64.77 and 63.73 mg GAE/g) compared to organic extracts (33.39). Total flavonoid content (TFC) was also higher in aqueous and hydroalcoholic extracts; meta-regression analysis revealed that outcomes in different measuring units (mg QE/g, mg CE/g, and mg RUE/g) do not present statistically significant differences and can be synthesized in meta-analysis. Using meta-regression analysis, we showed that outcomes from the chemical-based ABTS, FRAP, and ORAC antioxidant assays for the same extract type can be combined in meta-analysis because they do not differ statistically significantly. Meta-analysis of ABTS, FRAP, and ORAC assays outcomes revealed that the antioxidant activity profile of various extract types follows that of their phenolic and flavonoid content. Using regression meta-analysis, we also presented that outcomes from SOD, CAT, and POX enzymatic antioxidant assays are independent of the assay type (p-value = 0.905) and can be combined. Our study constitutes the first effort to quantitatively and statistically synthesize the research results of individual studies using all methods measuring the antioxidant activity of stevia leaf extracts. Our results, in light of evidence-based practice, uncover the need for a broadly accepted, unified, methodological strategy to perform antioxidant tests, and offer documentation that the use of ethanol:water 1:1 mixtures or pure water can more efficiently extract stevia antioxidant compounds.

Wrinkles are a common sign of aging and can significantly impact appearance and self-esteem. Natural plant extracts have gained attention for their potential anti-aging properties. In this study, extracts from Canna indica, Acalypha indica and Psidium guajava were incorporated into patches for topical application. The extraction process was carried from the combination of plant leaves for two different solvents (methanol and hexane). The antioxidant assays such as DPPH' radical, superoxide radical, phosphomolybdenum reduction and Fe3+ reducing power assays were carried out for combination of leaves extract. The maximum DPPH radical scavenging activity was 42.16 ± 1.92% and 51.33 ± 1.74% at 120 μg/ml concentration and the IC50 was 57.85 and 63.57 μg/ml concentrations. The maximum superoxide radical scavenging activity was 87.70 ± 1.17% and 97.54 ± 0.78% at 120 μg/ml concentrations and the IC50 was 80.49 and 85.47 μg/ml. The maximum phosphomolybdenum reduction was 38.42 ± 6.33% and 79.90 ± 2.06% at 120 μg/ml concentration and the RC50 was 49.69 and 97.08 μg/ml concentrations. The maximum Fe3+ reduction was 87.19 ± 0.065 and 83.34 ± 1.14% at 120 μg/ml concentrations and the RC50 was 63.74 and 58.19 μg/ml concentrations. The maximum anti-inflammatory activity for hexane and methanol fractions was 51.01 ± 4.79 and 56.96 ± 4.72% at 120 μg/ml concentrations and the IC50 for hexane and methanol fractions was 85.41 and 96.31 μg/ml, respectively. As a result, we concluded that the methanol has better anti-inflammatory and antioxidant properties than hexane. [ABSTRACT FROM AUTHOR]

Ubiquitously present in plant life, coumarins, as a class of phenolic compounds, have multiple applications—in everyday life, in organic synthesis, in medicine and many others. Coumarins are well known for their broad spectrum of physiological effects. The specific structure of the coumarin scaffold involves a conjugated system with excellent charge and electron transport properties. The antioxidant activity of natural coumarins has been a subject of intense study for at least two decades. Significant research into the antioxidant behavior of natural/semi-synthetic coumarins and their complexes has been carried out and published in scientific literature. The authors of this review have noted that, during the past five years, research efforts seem to have been focused on the synthesis and examination of synthetic coumarin derivatives with the aim to produce potential drugs with enhanced, modified or entirely novel effects. As many pathologies are associated with oxidative stress, coumarin-based compounds could be excellent candidates for novel medicinal molecules. The present review aims to inform the reader on some prominent results from investigations into the antioxidant properties of novel coumarin compounds over the past five years. [ABSTRACT FROM AUTHOR]

Introduction: Local anesthetics are widely recognized pharmaceutical compounds with various clinical effects. Recent research indicates that they positively impact the antioxidant system and they may function as free radical scavengers. We hypothesize that their scavenging activity is influenced by the lipophilicity of the environment.Methods: We assessed the free radical scavenging capacity of three local anesthetics (lidocaine, bupivacaine, and ropivacaine) using ABTS, DPPH, and FRAP antioxidant assays. We also employed quantum chemistry methods to find the most probable reaction mechanism. The experiments were conducted in an aqueous environment simulating extracellular fluid or cytosol, and in a lipophilic environment (n-octanol) simulating cellular membranes or myelin sheets.Results: All local anesthetics demonstrated ABTS˙+ radical scavenging activity, with lidocaine being the most effective. Compared to Vitamin C, lidocaine exhibited a 200-fold higher half-maximal inhibitory concentration. The most thermodynamically favorable and only possible reaction mechanism involved hydrogen atom transfer between the free radical and the -C-H vicinal to the carbonyl group. We found that the antioxidant activity of all tested local anesthetics was negligible in lipophilic environments, which was further confirmed by quantum chemical calculations.Conclusion: Local anesthetics exhibit modest free radical scavenging activity in aqueous environments, with lidocaine demonstrating the highest activity. However, their antioxidant activity in lipophilic environments, such as cellular membranes, myelin sheets, and adipose tissue, appears to be negligible. Our results thus show that free radical scavenging activity is influenced by the lipophilicity of the environment.

Secondary metabolites have been shown to possess a range of biological functions. Flavonoids, due to their ability to scavenge ROS, are famous antioxidants. The plants of Artemisia species are rich sources of flavonoids; however, the amount of these metabolites is less. In the current study, the flavonoid content was detected and then enhanced by genetically modifying the Artemisia carvifolia Buch with Agrobacterium tumefaciens strain GV3101 carrying rol A gene. The transformation of rol A gene was confirmed with PCR and the gene copy number was confirmed by Southern blot analysis. The HPLC analysis revealed the presence of catechin (3.19 ug/mg DW) and geutisic acid (2.22 ug/mg DW) in transformed plants, unlike wild-type plants. In transformed plants, all detected flavonoids (vanillic acid, rutin, catechine, gallic acid, syringic acid, caffeic acid, coumaric acid, geutisic acid, ferulic acid, and cinnamic acid) were increased up to several folds. Real-time qPCR revealed the higher expression levels of the genes for flavonoid biosynthesis enzymes phenylalanine ammonia-lyase (PAL) and chalcone synthase (CHS) in plants transformed with rol A genes, as the expression levels were increased up to 9–20-fold and 2–6-fold, respectively. The rol A transgenic lines T3 and T5 carrying two copies of rol A gene, particularly showed higher expression of both PAL and CHS gene, with the highest expression in T3 line. The transgenic lines demonstrated an average increase of 1.4-fold in the total phenolic content and 1–2-fold in the total flavonoid content as compared to wild-type plants. Total antioxidant capacity and total reducing power were increased up to an average of 1–2-fold and 1.5–2-fold respectively, along with increased free radical scavenging ability. Furthermore, the rol A gene transgenics were found to have much greater cytotoxic capacity than the A. carvifolia wild-type plant against the MCF7, HeLA, and HePG2 cancer cell lines. Current findings show that the rol A gene effectively increases the flavonoid content of A. carvifolia Buch, boosting the plant's capacity as an antioxidant and an anticancer. This is the first-ever report, demonstrating the genetic transformation of Artemisia carvifolia Buch with rol A gene. [ABSTRACT FROM AUTHOR]

Nutrition has crucial effects and a significant role in disease prevention. Recently, nutraceuticals have attracted much attention in scientific research due to their pleiotropic effects and relatively non-toxic behavior. Among the biological effects displayed by plants belonging to the Lamiaceae family, such as antibacterial, anticancer, anti-inflammatory, and anticholinesterase, sage is well known for its antioxidant properties and is a rich source of numerous compounds that are biologically active, amongst them polyphenols, with more than 160 types identified. In this review we summarized some of the significant studies published in the last decade reporting the most employed extraction methods and the different assays that are useful for establishing the antioxidant properties of some sage species. Even though the scientific literature contains plenty of data regarding the antioxidant properties of many sage species, further studies are needed in order to gain a deeper understanding of the mechanism of action and the compounds responsible for their antioxidant activity. Finally, it should be taken into account that the data on the antioxidant properties of sage extracts are often difficult to compare with each other, since a series of variables in the extraction procedures, the type of assay used, and standardization may affect the final result.

In the present work, complexes of cobalt(II), copper(II), and zinc(II), 2-amino-4-methylpyrimidineand, and 2,3-diaminopyridine were successfully prepared and characterized using elemental analysis, UV-visible, and FTIR spectroscopy, as well as magnetic susceptibility measurements, molar conductance, TGA analysis, and X-ray diffraction. From elemental and spectral data, the formulae [M(L1)(L2)Cl2(H2O)] (where L1 = AMPY (2-amino-4-methylpyrimidine) and L2 = DAPY(2,3-diaminopyridine)) and M = Co(II) (2), Cu(II) (2), and Zn(II)) for the metal complexes have been proposed. The geometric structures of the mixed-ligand complexes were found to be octahedral around the metal ions, and the XRD patterns showed monoclinic crystal systems with space group P21. The mode of bonding was pentacoordinate for Cu and hexacoordinate for Zn and Co. Different features may result from the fact that not all molecules have the same electron distribution. For example, Zn and Co have larger electron densities in at least one of the chlorides in the HOMO compared with pentacoordinate Cu, which has a small electron distribution on the chloride. Thermal analysis indicated that all metal complexes are stable up to about 88 °C with thermodynamically favored overlapped chemical reactions. Excellent antibacterial and antifungal activity was shown by the three synthesized forms of the complexes. The Zn(II) complex had a high level of antioxidant activity with a DPPH scavenging of 91.5%, whereas the Cu(II) complex had a low level of antioxidant potential (16.5%). The docking tests also showed that all compounds had good binding energy levels (7.2–7.9 kcal mol−1). For this reason, all molecules can easily fit in the receptor protein's catalytic sites. However, the Co(II) complex is shown to be more active. [ABSTRACT FROM AUTHOR]

The following article discusses the antioxidant properties of mandelic acid and its hydroxy and methoxy derivatives. The antioxidant capacity of these compounds is determined by DPPH, FRAP, CUPRAC and ABTS. The mechanisms underlying the antioxidant properties are described by BDE, IP, PDE, ETE and PA calculation method values and referenced to experimental data. Thermochemistry, HOMO/LUMO energies, dipole moments, charge distribution, IR, RAMAN, NMR frequencies, binding lengths and angles were calculated using the B3LYP method and the 6-311++G(d,p) basis set. The structure of mandelic acid and its derivatives was determined experimentally using IR and RAMAN spectroscopy. [ABSTRACT FROM AUTHOR]

The present work has reported a green chemistry‐based approach for the synthesis of crystalline metal oxide nanoparticle using plant extract to reduce metal ions. It demonstrated the efficient synthesis of Zinc oxide nanoparticles (ZnO NPs) using aqueous leaf extract of Thryallis glauca (Cav.) Kuntze with a focus on minimizing toxic reactants and byproducts. The physicochemical characterizations by standard methods and the mechanism of action were presented. The UV–Vis absorption peak of the annealed ZnO NPs appeared at a 359 nm wavelength. The calculated direct band‐gap energy was 3.6 eV. The peak at 567 nm in the visible region in the photoluminescence spectra indicated surface defects from oxygen vacancy, and the vibrational peak also indicated it at 582 cm−1 in Raman spectra. FTIR spectroscopy showed the possible involvement of proteins, aromatic compounds, and alcohols as reducing agents in the reaction. X‐ray diffraction analysis revealed that pure crystalline ZnO NPs have structural properties as hexagonal wurtzite below 50 nm size. Antioxidant analysis by DPPH assay illustrated an excellent free radical scavenging activity. The prepared ZnO NPs tested against pathogenic Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis did not show any antibacterial activity. Highlights: Renewable, eco‐friendly plant material was used to synthesize Zinc Oxide nanoparticles (NPs).Synthesis of thermally stable, pure crystalline NPs with good optical properties.The synthesized NPs showed excellent free radical scavenging activity.ZnO NPs exhibited antibacterial resistance at the test concentrations. [ABSTRACT FROM AUTHOR]

Vegetables are one of the most preferred food commodities and can be consumed either raw or as processed due to their health-promoting nutrients. In the present work, analysis of pharmacognostical standards, antioxidant capacity, and separation of phytocompounds through thin layer chromatography (TLC) from cabbage, cauliflower, pea, carrot, and potato peels were carried out. Microscopic analysis revealed the presence of wood fibers, trichomes, crystals, and annular xylem vessels in the vegetable peels. Physicochemical analysis showed that all the vegetable peel samples which were analysed have low (7.08%-10%) moisture content. The total ash content of vegetable peels varied in cauliflower peels (1.95±0.58) to the peels of pea (19.86±1.9). The content of acid insoluble ash varied from 1.46±0.63 to 3.09±0.59 in cauliflower and pea. Potato peel has the lowest water-soluble ash content (1.16±1.90) as compared to other peels. The highest pH value was found in the peels of pea (7), while the lowest pH was found in the peels of cabbage (4). Among all extracts, the petroleum ether extract has shown the greatest yield (5.6±0.45). The fluorescence analysis showed various colours like green, brown, pale green, and yellow under different chemical treatments. Different types of pri-secondary metabolites were detected in small, moderate, and high amounts and notified to provide numerous health benefits to humans. In case of DPPH assay, aqueous extract of cauliflower has shown the low value of IC50 (24.82 µg/ml) in comparison to standard, suggested the higher antioxidant activity of the extract. Among all the extracts, aqueous and methanol extracts of cauliflower have shown the better reducing and total antioxidant activity in comparison to standard. TLC profiling of methanolic extract of cabbage and cauliflower peels revealed the presence of different compounds of varying Rf values. Above results indicate that the food waste consists of valuable components and may be utilized as noticeable and cheap source in pharmaceuticals for the treatment of several life-threatening diseases.

Aconitum chasmanthum Stapf ex Holmes, an essential and critically endangered medicinal plant from Kashmir Himalayas, was studied for its antioxidant and antifungal properties. The shade-dried powdered rhizome was extracted sequentially with hexane, ethyl acetate, and methanol. These subsequent fractions were evaluated for total phenolic content (TPC); total flavonoid content (TFC); antioxidant assays, such as 1,1-diphenyl 1-2-picryl-hydrazyl (DPPH); ferric-reducing antioxidant power (FRAP); superoxide radical scavenging (SOR); hydroxyl radical scavenging (OH) and antifungal activity using the poisoned food technique. Highest TPC (5.26 ± 0.01 mg/g) and TFC (2.92 ± 0.04 mg/g) were reported from methanolic extracts. The highest values of radical scavenging activities were also observed in methanolic extracts with IC50 values of 163.71 ± 2.69 μg/mL in DPPH, 173.69 ± 4.91 μg/mL in SOR and 159.64 ± 2.43 μg/mL in OH. The chemical profile of ethyl acetate extract was tested using HR-LCMS. Methanolic extracts also showed a promising inhibition against Aspergillus niger (66.18 ± 1.03), Aspergillus flavus (78.91 ± 1.19) and Penicillium notatum (83.14 ± 0.97) at a 15% culture filtrate concentration with minimum inhibitory concentration (MIC) values of 230 μg/mL, 200 μg/mL and 190 μg/mL, respectively. Overall, the methanolic fractions showed significant biological potential, and its pure isolates might be used to construct a potential new medicinal source. [ABSTRACT FROM AUTHOR]

Ubiquitously present in plant life, coumarins, as a class of phenolic compounds, have multiple applications—in everyday life, in organic synthesis, in medicine and many others. Coumarins are well known for their broad spectrum of physiological effects. The specific structure of the coumarin scaffold involves a conjugated system with excellent charge and electron transport properties. The antioxidant activity of natural coumarins has been a subject of intense study for at least two decades. Significant research into the antioxidant behavior of natural/semi-synthetic coumarins and their complexes has been carried out and published in scientific literature. The authors of this review have noted that, during the past five years, research efforts seem to have been focused on the synthesis and examination of synthetic coumarin derivatives with the aim to produce potential drugs with enhanced, modified or entirely novel effects. As many pathologies are associated with oxidative stress, coumarin-based compounds could be excellent candidates for novel medicinal molecules. The present review aims to inform the reader on some prominent results from investigations into the antioxidant properties of novel coumarin compounds over the past five years.

Oleaster (Olea europaea var. sylvestris) is a wild olive tree distributed in the Mediterranean area. It is known to possess several biological activities due to their richness in polyphenols. However, enhanced autophagic activity in human cells by using this plant has not been studied before. The objective of the present study was to determine the phytochemical composition of the fruits paste from Tunisian Oleaster, and evaluate its antioxidant activity using the DPPH• and ABTS•+ methods as well as the evaluation of its effect on autophagy activity. The extraction conditions were optimized using response surface methodology (RSM) leading to the best phenolic extract yield. It was noted that ethyl acetate extract presented the highest amount of total phenols and the best solvent for extraction of phenolic compounds. After optimization, the ethyl acetate extract was fractionated into 15 fractions by silica gel column chromatography. The most phenolic components in the fifth and sixth fractions (F5 and F6) were identified using UPLC-ESI(-)-HRMS analysis. Accordingly, F6 was the richer fraction in polyphenols. In vitro antioxidant activity evaluation showed that F6 exhibited a strong ability to scavenge DPPH and ABTS radicals. Furthermore, this fraction was also the most effective to induce autophagic activity in Human foreskin fibroblasts (HFF) cells. These results could be presumably due to the presence of oleuropein aglycon in this fraction which is absent in fraction F5. Oleaster fruits paste would be used as a natural source of bioactive compounds useful in various pharmaceutical drugs. [ABSTRACT FROM AUTHOR]

Background: C. vespertiliomis extracts were evaluated for antiproliferative and apoptosis effect on breast cancer (MCF7) cells. Methods and results: The leaves extracts were analysed for its antiproliferative effect on breast cancer (MCF7) cells and normal epithelial breast (MCF 10A) cells using Sulforhodamine B (SRB) assay. The selective extract was evaluated for its ability to induce apoptosis using Annexin V-FITC apoptosis staining and the expression of molecular genes using qualitative reverse transcription-polymerase chain reaction (RT-PCR) against MCF7 cells. Gas chromatography–mass spectrometry (GC–MS) was used to identify the compounds from the selective extract. The findings showed that dichloromethane fraction (CV-Dcm) extract had high antiproliferative effect against MCF7 cells (IC50 = 24 µg/mL, selective index (SI) = 8.17). The percentages of apoptosis cells in CV-Dcm-treated MCF7 cells was 58.8%. The CV-Dcm extract induced downregulation of PCNA level. The apoptotic genes were also triggered in both extrinsic and intrinsic signaling pathways, affecting a 1.5-fold increase in BAX, 1.4-fold increase in cytochrome c, 1.3-fold increase in caspase-8, 1.7-fold increase in caspase-3 and 0.5-fold-decrease in BCL-2. Treated MCF7 cells also activated P53-dependent apoptotic death pathway. Conclusions: The present work strongly suggests that high efficacy of CV-Dcm extract was attributed to its antiproliferative and apoptosis-inducing activation in MCF7 cells, most likely due to its favourable compounds. [ABSTRACT FROM AUTHOR]

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In the present work, complexes of cobalt(II), copper(II), and zinc(II), 2-amino-4-methylpyrimidineand, and 2,3-diaminopyridine were successfully prepared and characterized using elemental analysis, UV-visible, and FTIR spectroscopy, as well as magnetic susceptibility measurements, molar conductance, TGA analysis, and X-ray diffraction. From elemental and spectral data, the formulae [M(L1)(L2)Cl2(H2O)] (where L1 = AMPY (2-amino-4-methylpyrimidine) and L2 = DAPY(2,3-diaminopyridine)) and M = Co(II) (2), Cu(II) (2), and Zn(II)) for the metal complexes have been proposed. The geometric structures of the mixed-ligand complexes were found to be octahedral around the metal ions, and the XRD patterns showed monoclinic crystal systems with space group P21. The mode of bonding was pentacoordinate for Cu and hexacoordinate for Zn and Co. Different features may result from the fact that not all molecules have the same electron distribution. For example, Zn and Co have larger electron densities in at least one of the chlorides in the HOMO compared with pentacoordinate Cu, which has a small electron distribution on the chloride. Thermal analysis indicated that all metal complexes are stable up to about 88 °C with thermodynamically favored overlapped chemical reactions. Excellent antibacterial and antifungal activity was shown by the three synthesized forms of the complexes. The Zn(II) complex had a high level of antioxidant activity with a DPPH scavenging of 91.5%, whereas the Cu(II) complex had a low level of antioxidant potential (16.5%). The docking tests also showed that all compounds had good binding energy levels (7.2–7.9 kcal mol−1). For this reason, all molecules can easily fit in the receptor protein’s catalytic sites. However, the Co(II) complex is shown to be more active.

The present research work depicts a cinch and economical synthesis of silver nanoparticles (AgNPs) phytofabricated utilizing leaf extract of Simarouba glauca and aerial extract of Celastrus paniculatus. Fourier transform infrared spectroscopy (FTIR) analysis displayed the synthesized AgNPs capped with bio-constituents existent in these medicinal plants marked by their functional groups. The morphological features of prepared NPs were characterized by employing X-ray Diffraction (XRD), Scanning Electron Microscope with Energy Dispersive spectra (SEM–EDX) and Transmission Electron Microscope (TEM) analysis illustrated their spherical shape and ~ 40 nm particle size. Green synthesized AgNPs were assessed for their antioxidant potential by free radical scavenging assays; and antibacterial efficacy. The phytofabricated AgNPs were found to induce cell growth arrest in MCF-7 and HT-29 cell lines with an IC50 value of 70.84 ± 0.67 and 158.24 ± 0.89 µg/mL for AgNPs prepared using S. glauca (Ag-SG) while 207.19 ± 0.64 and 221.22 ± 0.57 µg/mL for AgNPs synthesized using C. paniculatus (Ag-CP) in dose-proportional relation. The same samples could not effectively prohibit the growth of immortalized normal human breast epithelial cell lines (MCF-10A). The cytotoxicity induced by apoptosis was further confirmed by fluorescent images. The synthesized nanoparticles also demonstrated less hemolysis efficiency and are evidenced by SEM images. The analyses indicate the potent antioxidant and antiproliferative capacity of stable green synthesized AgNPs derived from the mentioned exorbitant curative herbs. [ABSTRACT FROM AUTHOR]

In this research, supercritical CO2 extraction is applied to extract bioactive compounds from Lamium album (white dead nettle, Lamiaceae). Extraction was performed at various temperatures (40, 50, and 60 °C) using methanol as co-solvent at a constant flow rate of CO2, methanol, and pressure. The collected extracts were characterized in terms of antioxidant capacity by using DPPH, ABTS and FRAP in vitro antioxidant activity assays, whereas the Folin–Ciocalteu procedure was employed to estimate the total phenols content (TPC). On the other hand, phenolic compounds in the extracts were quantitated by liquid chromatography coupled with a photodiode array detector (UPLC-PDA) and confirmed with a mass detector (TQD). The extracts have shown high TPC ranged between 234.17 to 650.17 mg GAE/g extract. DPPH scavenging of the extracts was estimated and obtained EC50 values ranged from 0.12 to 0.37 mg/mL of solution. The ABTS radical scavenging activity ranged from 43.20 to 44.53 µg TE/g. The FRAP value was found within the range of 19.48 to 44.74 µmol TE/g of extract. Differences between extraction conditions were observed. In this research, 50 °C/250 bar was efficient for the TPC, DPPH, ABTS, and FRAP assays; moreover, statistically, TPCs and FRAP assay showed significant differences between the conditions at α = 0.05. The identification of phenolic compounds in the obtained extract of Lamium album flowers, using UPLC/PDA, revealed that chrysin, pinostrobin, myricetin, and trans-3-hydroxycinnamic acid were the significant molecules present, which may be responsible for the high content of polyphenols and antioxidant activity. The results obtained indicated that SC-CO2 could be considered an alternative method for extracting bioactive compounds of Lamium album. High antioxidant activity and the presence of various bioactive compounds indicate the potential of this plant from the Lamiaceae family and the possibility of its application in various industries, including agriculture, food technology, or pharmacy. [ABSTRACT FROM AUTHOR]

Poor drug solubility and oral bioavailability is a significant challenge with many effective drug candidates. Pluronic micelles are effective solutions for improved solubility, stability, and delivery of the hydrophobic drug to the right area, at the right time, and in the right amount. Solubilization of three drugs, namely curcumin (CUR), quercetin (QCN), and lamotrigine (LTG), were explored using Pluronics with varying molecular characteristics. All the drugs showed better solubility in Pluronic solutions. The tendency of augmentation in solubility was QCN>CUR>LTG. Results showed better solubilization of drugs in Pluronics which form micelles and have low CMTs. With an objective to enhance the oral bioavailability of drugs, the drug‐loaded Pluronic P123 nanomicelles (PLC for CUR, PLQ for QCN, and PLL for LTG) have been prepared and characterized using UV‐VIS, DLS, SANS, CPT, and TEM measurements. The drug‐loaded P123 nanomicelles having particle sizes range from 18 to 22.5 nm and spherical in shapes. In the in‐vitro release study, CUR and QCN showed slow release,while LTG exhibited a faster release profile. The PLC and PLQ assessed their anti‐oxidant potential had confirmed the oxidation resistance more significantly than the free drug. Considering the pharma uses of CUR, QCN, and LTG drugs and observing the application of Pluronics in drug delivery systems, the present work facilitates insight into the possible formulations of these drugs. [ABSTRACT FROM AUTHOR]

Aconitum chasmanthum Stapf ex Holmes, an essential and critically endangered medicinal plant from Kashmir Himalayas, was studied for its antioxidant and antifungal properties. The shade-dried powdered rhizome was extracted sequentially with hexane, ethyl acetate, and methanol. These subsequent fractions were evaluated for total phenolic content (TPC); total flavonoid content (TFC); antioxidant assays, such as 1,1-diphenyl 1-2-picryl-hydrazyl (DPPH); ferric-reducing antioxidant power (FRAP); superoxide radical scavenging (SOR); hydroxyl radical scavenging (OH) and antifungal activity using the poisoned food technique. Highest TPC (5.26 ± 0.01 mg/g) and TFC (2.92 ± 0.04 mg/g) were reported from methanolic extracts. The highest values of radical scavenging activities were also observed in methanolic extracts with IC50 values of 163.71 ± 2.69 μg/mL in DPPH, 173.69 ± 4.91 μg/mL in SOR and 159.64 ± 2.43 μg/mL in OH. The chemical profile of ethyl acetate extract was tested using HR-LCMS. Methanolic extracts also showed a promising inhibition against Aspergillus niger (66.18 ± 1.03), Aspergillus flavus (78.91 ± 1.19) and Penicillium notatum (83.14 ± 0.97) at a 15% culture filtrate concentration with minimum inhibitory concentration (MIC) values of 230 μg/mL, 200 μg/mL and 190 μg/mL, respectively. Overall, the methanolic fractions showed significant biological potential, and its pure isolates might be used to construct a potential new medicinal source.

Interest in nanotechnology is increasing day by day. Silver and iron nanoparticles of the chloroform extract of Psephellus pyrrhoblepharus were prepared for this study by green synthesis method. The characterisation of the nanoparticles was carried out with some methods like the Fourier Transform Infrared Spectroscopy (FTIR), Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), X-ray Diffraction Analysis (XRD), zeta potential and particle size. The antioxidant activities and total phenolic capacities of nanoparticles and three different extracts of P. pyrrhoblepharus (chloroform, methanol:water (1:1) and n-hexane) were compared. Silver nanoparticles were the most active ones by antioxidant activities and total phenolic capacity. Although the iron nanoparticles showed activity, they did not show a successful activity as silver nanoparticles. This research is essential because it contains the first nanoparticle studies prepared from the plant P. pyrrhoblepharus. [ABSTRACT FROM AUTHOR]

In this study, four new mixed-ligand saccharin complexes with 2-[[(2-Aminophenyl)imino]methyl]-6-methoxy phenol Schiff base and metal saccharinates (nickel, copper, zinc and cadmium) have been prepared and characterized with various methods including elemental analysis, FT-IR spectroscopy, UV-visible absorption spectroscopy, NMR spectroscopy, QTOF-LC/MS spectroscopy. All methods have confirmed the inclusion of the Schiff base obtained by condensation of o-phenylendiamine and o-vanillin into the metal saccharinates. Besides, DPPH scavenging activities and metal chelating abilities of all complexes have been determined and compared to well-known antioxidant standards (Butylated hydroxyanisole, Butylated hydroxytoluene and α-Tocopherol) along with starting metal saccharinates. According to the results, nickel complex has exhibited the best DPPH scavenging activity, while copper complex has the highest ferrous ion chelating ability. [ABSTRACT FROM AUTHOR]

Plants belonging to the genus Artemisia L. have been used for medicinal purposes since ancient times. These aromatic plants produce and accumulate a wide range of potent secondary metabolites, many of which have shown antioxidant, antiparasitic, antimicrobial, anti-inflammatory, and even anticancer activities. Enhanced biosynthesis of these compounds is a prerequisite for comprehensive studies of their therapeutic properties and cost-efficient use. Transformation of plants with Agrobacterium rhizogenes native root locus (rol) genes is a promising approach to increase the biosynthesis of plant secondary metabolites. The aim of the present study was to evaluate the effects of A. rhizogenes -mediated transformation on the flavonoid contents in hairy roots of medicinal herb A. tilesii Ledeb. Transgenic A. tilesii hairy root lines were analyzed for stable integration of the rolB and rolC transgenes into the plant genome, total flavonoid contents, antioxidant activities of extracts, and the spatiotemporal expression of two flavonoid biosynthetic genes, phenylalanine ammonialyase (PAL) and chalcone synthase (CHS). The flavonoid contents of A. tilesii directly correlated with the antiradical activity and reducing power of their respective lines, with the greatest antioxidant activity found in the plants with the highest level of total flavonoids. Furthermore, all hairy root lines demonstrated altered expression of plant native PAL and CHS genes. Most importantly, A. rhizogenes -mediated transformation enhanced the biosynthesis of natural antioxidants in A. tilesii , producing almost twice the amount of flavonoids than controls. These findings provide an opportunity for the identification of the bioactive molecules in A. tilesii extracts and their potential health benefits. • Agrobacterium rol genes enhance flavonoid biosynthesis in Artemisia tilesii Ledeb. • Flavonoid contents of A. tilesii directly correlate with antioxidant activity. • Development of A. tilesii hairy roots affects expression of native PAL and CHS genes. [ABSTRACT FROM AUTHOR]

Objective: To explore the new sources of novel bioactive compounds having pharmaceutical and agricultural interest and to search the endophytic actinobacteria from medicinal plants. Methods: NAF-1 an endophyte actinobacteria was isolated from leaves of medicinal plant Aloe vera collected in Marrakesh, Morocco using Bennett agar as selective medium. NAF-1 was tested for its antimicrobial activity against five pathogenic bacteria such as Staphylococcus aureus PIC 53156, Micrococcus luteus ATCC381, Bacillus subtilis ATCC 14579, Pseudomonas aeruginosa DSM 50090 and Escherichia coli ATCC 8739 and four human clinic fungi belonging to the Candida, Aspergillus and Microsporum genera. Several antioxidant activities were studied such as DPPH free radical scavenging, β -carotene and linoleic acid and reducing power assays. The total of phenol and flavonoid was also calculated. Using Artemia salina shrimp assay, the cytotoxicity of NAF-1 crude extract was determined. Results: The results revealed that the actinobacteria showed a high activity (≥20 mm) against only Gram positive bacteria but it had a moderate activity (between 13 and 15 mm) against Human clinic fungi. The isolate also exhibited a LD50 of 14.20 μg/mL in the cytotoxicity assay. The result showed that the crude extract presented an interesting free radical-scavenging activity with IC50 value of (5.58 ± 0.26) μg/mL and a high value of phenolic and flavonoid compounds with (15.41 ± 0.18) μg GAE/mg extract and (11.41± 0.06) μg QE/mg extract respectively. Moreover, the taxonomic position of our endophyte actinobacteria using the morphological and physiological criteria and using 16S rRNA gene sequence (polyphasic approach) showed that the NAF-1 isolate was similar to Streptomyces hydrogenans which was never described as an endophyte actinobacteria. Conclusions: This isolated strain appears promising resources of bioactive agents and can be exploited to produce therapeutic agents active against pathogenic disease.

This study reports the effect of an acetone extract of Evernia prunastri on the micronucleus distribution of human lymphocytes and effect on cholinesterase activity. Furthermore, the antioxidant activity (estimated via DPPH, ABTS, TRP and CUPRAC assays), as well as total phenolic compounds (TPC) and antibacterial activity (against two Gram-positive and three Gram-negative bacteria) were determined. Chemical profiling of four E. prunastri extracts (acetone, diethyl ether, ethyl acetate and dichloromethane) was realized by GC–MS and HPLC analysis. In addition, the activity concentrations of 40K, 137Cs, 226Ra and 232Th were established.

In this research, supercritical CO2 extraction is applied to extract bioactive compounds from Lamium album (white dead nettle, Lamiaceae). Extraction was performed at various temperatures (40, 50, and 60 °C) using methanol as co-solvent at a constant flow rate of CO2, methanol, and pressure. The collected extracts were characterized in terms of antioxidant capacity by using DPPH, ABTS and FRAP in vitro antioxidant activity assays, whereas the Folin–Ciocalteu procedure was employed to estimate the total phenols content (TPC). On the other hand, phenolic compounds in the extracts were quantitated by liquid chromatography coupled with a photodiode array detector (UPLC-PDA) and confirmed with a mass detector (TQD). The extracts have shown high TPC ranged between 234.17 to 650.17 mg GAE/g extract. DPPH scavenging of the extracts was estimated and obtained EC50 values ranged from 0.12 to 0.37 mg/mL of solution. The ABTS radical scavenging activity ranged from 43.20 to 44.53 µg TE/g. The FRAP value was found within the range of 19.48 to 44.74 µmol TE/g of extract. Differences between extraction conditions were observed. In this research, 50 °C/250 bar was efficient for the TPC, DPPH, ABTS, and FRAP assays; moreover, statistically, TPCs and FRAP assay showed significant differences between the conditions at α = 0.05. The identification of phenolic compounds in the obtained extract of Lamium album flowers, using UPLC/PDA, revealed that chrysin, pinostrobin, myricetin, and trans-3-hydroxycinnamic acid were the significant molecules present, which may be responsible for the high content of polyphenols and antioxidant activity. The results obtained indicated that SC-CO2 could be considered an alternative method for extracting bioactive compounds of Lamium album. High antioxidant activity and the presence of various bioactive compounds indicate the potential of this plant from the Lamiaceae family and the possibility of its application in various industries, including agriculture, food technology, or pharmacy.