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Theophylline, a nitrogen-containing heterocycle, serves as a promising focal point for medicinal researchers aiming to create derivatives with diverse pharmacological applications. In this work, we present an improved synthetic method for a range of theophylline-1,2,4-triazole-S-linked N-phenyl acetamides (4aâg) utilizing ultrasound-assisted synthetic approach. The objective was to assess the effectiveness of synthesized theophylline-1,2,4-triazoles (4aâg) as inhibitors of HCV serine protease and as antibacterial agents against B. subtilis QB-928 and E. coli AB-274. Theophylline-1,2,4-triazoles were obtained in good to excellent yields (69%-95%) in a shorter time than conventional approach. 4-Chlorophenyl moiety containing theophylline-1,2,4-triazole 4c displayed significantly higher inhibitory activity against HCV serine protease enzyme (IC50 = 0.015 ± 0.25 mg) in comparison to ribavirin (IC50 = 0.165 ± 0.053 mg), but showed excellent binding affinity (-7.55 kcal/mol) with the active site of serine protease, better than compound 4c (-6.90 kcal/mol) as well as indole-based control compound 5 (-7.42 kcal/mol). In terms of percentage inhibition of serine protease, 2-chlorophenyl compound 4b showed the maximum percentage inhibition (86%), more than that of the 3,4-dichlorophenyl compound 4c (76%) and ribavirin (81%). 3,4-Dimethylphenyl-based theophylline-1,2,4-triazole 4g showed the lowest minimum inhibitory concentration (MIC = 0.28 ± 0.50 µg/mL) against the B. subtilis bacterial strain as compared to the standard drug penicillin (MIC = 1 ± 1.50 µg/mL). The other 4-methylphenyl theophylline-1,2,4-triazole 4e (MIC = 0.20 ± 0.08 µg/mL) displayed the most potent antibacterial potential against E. coli in comparison to the standard drug penicillin (MIC = 2.4 ± 1.00 µg/mL). Molecular docking studies further helped in an extensive understanding of all of the interactions between compounds and the enzyme active site, and DFT studies were also employed to gain insights into the molecular structure of the synthesized compounds. The results indicated that theophylline-linked triazole derivatives 4b and 4c showed promise as leading contenders in the fight against the HCV virus. Moreover, compounds 4e and 4g demonstrated potential as effective chemotherapeutic agents against E. coli and B. subtilis, respectively. To substantiate these findings, additional in vivo studies and clinical trials are imperative, laying the groundwork for their integration into future drug design and development.
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Transgenic Arabidopsis thaliana (ecotype Columbia) was successfully transformed with the gene fructose-1,6-bisphosphatase (FBPas e) and named as AtFBPase plants. Transgenic plants exhibited stable transformation, integration and significantly higher expressions for the transformed gene. Morphological evaluation of transgenic plants showed increased plant height (35cm), number of leaves (25), chlorophyll contents (28%), water use efficiency (increased from 1.5 to 2.6µmol CO2 µmol-1 H2 O) and stomatal conductance (20%), which all resulted in an enhanced photosynthetic rate (2.7µmolm-2 s-1 ) compared to wild type plants. This study suggests the vital role of FBPase gene in the modification of regulatory pathways to enhance the photosynthetic rate, which can also be utilised for economic crops in future.
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Arabidopsis , Arabidopsis/genética , Fructosa-Bifosfatasa/genética , Fructosa-Bifosfatasa/metabolismo , Fructosa/metabolismo , Fotosíntesis/genética , Clorofila/genética , Clorofila/metabolismo , Plantas Modificadas Genéticamente/genética , Plantas Modificadas Genéticamente/metabolismoRESUMEN
Parsley (Petroselinum crispum) is herb with many biological and medicinal benefits for humans. However, growth on zinc (Zn) and cadmium (Cd) contaminated sites might get severely affected due to over accumulation of heavy metals (HM) in different plant tissues. Antioxidants play a crucial role in minimizing the negative effects of HM. The present study investigates the effects of Zn and Cd stress on P. crispum morphological parameters, enzymatic/non-enzymatic antioxidant profiling and metal accumulation in shoot/root. Plants were exposed to different concentrations of Zn (50, 100, 150 and 200 µM) and Cd (10, 20, 40 and 80 µM) along with control (no stress), in soil-less Hoagland's solution. The results showed that Zn and Cd substantially decrease the growth parameters with increased contents of malondialdehyde (MDA), hydrogen peroxide (H2O2), and electrolyte leakage (EL). Non-enzymatic antioxidant activities, like total phenolic contents (TPC) and ferric reducing antioxidant power (FRAP), were induced high in leaves only upon Cd stress and contrarily decreased upon Zn stress. Total flavonoid contents (TFC) were decreased under Zn and Cd stress. Enzymatic antioxidant activities like superoxide dismutase (SOD), catalase (CAT) and ascorbate peroxidase (APX) were also strongly induced upon Cd stress. At the same time, SOD and guaiacol peroxidase (GPX) activity was induced significantly upon Zn stress. Cd uptake and accumulation was notably high in roots as compared to shoots, which suggests P. crispum have a reduced ability to translocate Cd towards aboveground parts (leaves). Additionally, strong induction of antioxidants by P. crispum under Cd stress might indicate the capacity to effectively re-modulate its physiological response. However, further investigations regarding other HMs and experiments at the molecular level are still needed.
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Metales Pesados , Contaminantes del Suelo , Humanos , Antioxidantes/farmacología , Cadmio/farmacología , Petroselinum/metabolismo , Zinc/farmacología , Peróxido de Hidrógeno , Metales Pesados/farmacología , Superóxido Dismutasa/metabolismo , Raíces de Plantas/metabolismo , Estrés OxidativoRESUMEN
With various strains of the novel coronavirus emerging during the last few years, there is a need to reinvent and manage the tourism industry by engaging various stakeholders. Industry and policymakers need to observe the shift and curate tourism-related products and offerings accordingly. In light of the increasing demand for innovations and future directions in the post-COVID-19 period, this article conducts a bibliometric analysis for sustainable tourism studies spanning the years 1990-2021. This paper presents an integrative review of tourism, environment and sustainable tourism to reveal geographical, contextual, and methodological directions for future research. The comprehensive analysis includes contributions on topics and methods, country collaborations, and thematic analysis. The findings are consistent with the Sustainable Development Goals of sustainable production and consumption (SDG-12), with a particular emphasis on sustainable tourism to promote local culture and create jobs (SDG-12.b) and on sustainable growth (SDG-13). The study's findings can be used to inform future policies and directions; for example, the findings indicate that the hospitality industry is facing challenges that necessitate new regulations to address its socioeconomic and environmental impacts.
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COVID-19 , Humanos , Turismo , SARS-CoV-2 , Altruismo , BibliometríaRESUMEN
Cyclopropanes are of great synthetic value in heterocyclic chemistry due to their highly reactive nature. They are widely employed to synthesize various biologically active organic compounds. Generally, vinyl, carbonyl, imine, and alkylidene cyclopropanes are utilized as efficient synthetic precursors in organic synthesis. The Cloke-Wilson rearrangement of these activated cyclopropanes is carried out to achieve the synthesis of diverse heterocyclic scaffolds. Various oxygen, nitrogen, and sulfur-containing heterocyclic compounds have been synthesized employing this rearrangement. With time, Cloke-Wilson rearrangement has evolved into a high yielding enantioselective and diastereoselective approach utilizing integrated novel methods. Our review focuses on the recent approaches for Cloke-Wilson rearrangement to synthesize several five-membered heterocycles and its applicability towards the natural product syntheses reported during 2000-2020.
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Potato is one of the highly consumed vegetable crop grown in different regions across Pakistan that is affected by fungal diseases. The current research was conducted to identify fungal pathogen causing mold-like disease of potato in Khyber Pakhtunkhwa (KP), Pakistan. For molecular identification and characterization of the fungal disease; potato tuber samples were collected followed by culturing on potato dextrose agar (PDA). Based on morphological features, the pathogen was identified as a Penicillium species. This result was obtained in 45 different isolates from potato tubers. Molecular identification was done using ß-tubulin primers and ITS5 sequencing of 13 different isolates that releveled 98% homology with BLAST (GenBank accession no. KX958076) as Penicillium solitum (GenBank accession nos. ON307317; ON307475 and ON310801). Phylogenetic tree was constructed that showed Penicillium solitum prevalence along with Penicillium polonicum and Penicillium citrinum on potato tubers. Based on this, Penicillium solitum based silver nanoparticles (Ag NPs) were synthesized and characterized using UV-visible spectroscopy, Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), energy dispersive X-ray (EDX) and field emission scanning electron microscopy (FE SEM). UV-analysis showed a characteristic peak at 410 nm confirming synthesis of Penicillium solitum based Ag NPs. This was further confirmed by XRD followed by EDX and SEM that showed face cubic crystal structure with Ag as major constituent of 18 nm formed spherical Ag NPs. FTIR showed band stretching of O-H, N-O and C-H of biological origin. Similarly, Penicillium solitum based Ag NPs presented strong anti-bacterial and anti-fungal activity at 0.5 level of significance LSD. According to our knowledge, this is the first report of Penicillium solitum identification in Pakistan, its Ag NPs synthesis and characterization to be used against pathogens of agricultural significance.
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Economic complexity is considered key a driver of social change, structural change, and economic development. Economic complexity is mostly used to capture issues apropos product diversification of exports, trade, technological innovation, human knowledge, and skills. The current study has conducted a detailed bibliometric review of economic complexity, export quality, and trade diversification. In doing so, the authors used the literature up to 2021 to unveil economic complexity's contextual information that witnessed structural change, social change, and trade indicators. The current study is the first integrative review to report the theoretical contribution, future research agendas, and thematic analysis of economic complexity, export quality, and export diversification. Our study, on the subject of economic complexity, export diversification, and import diversification in the period from 1966 to 2021, was carried out by systematically scanning 386 documents, and it is one of the pioneering studies in this field. In addition, economic diversity, development, and economic complexity; export diversification, import diversification, trade openness, and economic growth; energy, environmental Kuznets curve, and economic complexity; and sustainability and economic diversification are the four main research topics of the study. The findings are discussed apropos of economic complexity and exports, methodological aspects of economic complexity, and environmental issues nexus with economic complexity. The current study reports novel findings toward a path for achieving SDG-9 (industry and innovation) and SDG-13 (climate action). The biometric review enables researchers and policymakers to understand export quality, economic complexity, and the trade nexus and report future research directions for achieving sustainable growth in industries and innovation.
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Dióxido de Carbono , Desarrollo Económico , Humanos , Industrias , Invenciones , ClimaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Toxicity studies in appropriate animal models are an integral and very important component of pre-clinical studies in drug development. Brugmansia aurea lagerh. is used for both medicinal and non-medical purposes, including treating skin infections, different types of physical discomfort, inflammation, cough, hallucinations, and evil protection. AIM OF THE STUDY: This study was designed to detect any hazardous effects of B. aurea on animals and find out its LD50. MATERIALS & METHODS: An acute toxicity study was performed to find out the LD50 value and sub-acute toxicity study was performed to find out the toxicity on repeated dose administration till 28 days. Both studies were performed according to the organization of economic cooperation and development (OECD) 425 and 407 respectively. For the acute oral toxicity study, animals were divided into two groups, group I normal control (NC) and group II received a 2000mg/kg dose of B.aurea leaves extract. In the sub-acute toxicity study, male and female animals were divided into eight groups, I-IV for males and V-VIII for females received control, 100, 200 & 400mg/kg B. aurea leaves extract respectively. Hematological and biochemical markers were estimated at the end of each study. RESULTS: Results revealed that no mortality and morbidity were observed in acute oral as well as sub-acute toxicity studies. Oxidative stress markers were increased significantly in all organs of the treatment groups in both studies. Animals significantly decreased their food and water intake in an acute oral toxicity study. A slight difference in renal function tests was observed in the acute oral toxicity study when compared with the normal control group. No significant change in histopathology was observed in both studies on selected organs. CONCLUSION: This study concluded that B. aurea can be safely used for pharmacological purposes.
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Extractos Vegetales , Hojas de la Planta , Ratas , Masculino , Femenino , Animales , Pruebas de Toxicidad Aguda , Extractos Vegetales/toxicidad , Dosificación Letal Mediana , Pruebas de Toxicidad SubagudaRESUMEN
This paper investigates the effect of the supply chain disruption, greener energy consumption, and economic growth on carbon emissions in advanced economies and emerging markets from 1997 to 2021 using panel quantile autoregressive distributed lags (QARDL) and the panel quantile regression (QR). The results of the two models confirm, on the one hand, the validity of the environmental Kuznets curve (EKC) hypothesis and, on the other hand, the role of renewable energy consumption in mitigating carbon emissions in advanced and developing economies. Furthermore, the finding shows that the supply chain disruption for the long run is positive at all quantiles, indicating the evidence of association at the extreme low and high quantiles than at the intermediate quantile. In addition, the effect of the supply chain decreases at the lower quantile. It turns negative at the upper 90th quantile in the short run, indicating that the supply chain disruption reduces the environmental degradation under the bearish market conditions. In the future, the increasing supply chain disruptions due to the Russia-Ukraine conflict and further COVID-19 worldwide can consider sluggish economic growth and play an essential role in promoting renewable energy abundance and reducing CO2 emissions. Practical implications are reported in the lens of carbon neutrality and structural changes.
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COVID-19 , Desarrollo Sostenible , Humanos , Dióxido de Carbono/química , Desarrollo Económico , Energía Renovable , CarbonoRESUMEN
Climate change and global warming have been driven by a rise in carbon dioxide (CO2) concentrations in recent decades, posing a danger to environmental sustainability. Thus, this research scrutinizes the effects of two types of energy (coal and geothermal) and natural resources on CO2 emissions in 10 newly industrialized countries (NICs). The study also considers the role of financial globalization using a data between 1990 and 2019. This research applied a fresh nonparametric econometric technique termed "method of moments quantile regression (MMQR)." This approach is resistant to outliers and produces an asymmetric connection between variables. Furthermore, the long-run estimators (AMG and CCEMG) are employed as a robustness check. The findings reveal that natural resources, coal, and economic growth contribute to the degradation of the environment in the NICs in all quantiles (0.1-0.90). However, geothermal energy aids in enhancing environmental sustainability at all quantile distributions (0.1-0.90). Our findings are robust with alternative methods (AMG and CCEMG). The research's outcomes have the potential to help NICs nations design policies. Finally, based on the research results, a policy framework is proposed to solve the objectives of SDGs 7 and 13.
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Energía Geotérmica , Desarrollo Sostenible , Dióxido de Carbono/análisis , Recursos Naturales , Desarrollo Económico , Carbón Mineral , Energía RenovableRESUMEN
Novel azomethines derived from acefylline tethered triazole hybrids (7a-k) have been synthesized and evaluated against human liver cancer cell line (Hep G2) using MTT assay. The synthesized series of azomethines exhibited promising efficacy against liver cancer cell line. Screening of the synthesized series identified compound 7d with the least cell viability value (11.71 ± 0.39%) as the most potent anticancer agent in contrast to the reference drug acefylline (cell viability = 80 ± 3.87%). In this study, the potentials of the novel agents (7a-k) to inhibit liver cancer proteins were assessed. Subsequently, the structure-activity relationship of the potential drug candidates was assessed via ADME/T molecular screening. The cytotoxic potential of these derivatives was also investigated by hemolysis and thrombolysis. Their hemolytic and thrombolytic studies showed that all of these drugs had very low cytotoxicity and moderate clot lysis activity. Compound 7g (0.26% hemolysis) and 7k (52.1% clot lysis) were the least toxic and moderate thrombolytic agents respectively.
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Antineoplásicos , Neoplasias Hepáticas , Humanos , Ensayos de Selección de Medicamentos Antitumorales , Línea Celular Tumoral , Hemólisis , Reposicionamiento de Medicamentos , Estructura Molecular , Proliferación Celular , Triazoles/farmacología , Antineoplásicos/farmacología , Relación Estructura-Actividad , Relación Dosis-Respuesta a DrogaRESUMEN
Background: Taxus wallichiana is an evergreen tree species found in the Himalayan region of Pakistan. The tree possesses important secondary metabolites such as Taxol that has been implicated in treating breast, ovarian and colon cancer. Therefore keeping in view the importance of this plant species, silver nanoparticles were synthesized using Taxus wallichiana aqueous leaf extract and evaluated for their anti-bacterial and anti-cancer properties. Methods: Silver (Ag) nanoparticles (NPs) were characterized for their optical, morphological and structural features using techniques such as UV-visible spectroscopy, X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) and were evaluated for their antibacterial activity and anti-cancer activity using U251 cell line. Results: The study showed that the UV-absorbance peak of Ag2O NPs at 450 nm shifted to 410 nm, affirming the formation of leaf extract Ag NPs. Similarly structural studies revealed the crystalline nature of the cubic structure of the Ag crystal with an average crystallite size of 29 nm. FTIR analysis exhibited the existence of different functional elements including O-H and N-H and phenolic groups. Non-spherical glomerular shaped Taxus wallichiana Ag NPs were observed from SEM studies and EDX profile showed Ag as the main element along with constituent of biological origin. The synthesized Ag NPs showed significant antibacterial activity against Salmonella typhi, and Staphylococcus aureus. The cytotoxic activity of Ag NPs on U251 brain cancer cells showed a synergistic effect with 10 ug/mL concentration after 48 and 72 h incubation based on cell viability assay indicating promising glioblastoma drug potential.
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Nanopartículas del Metal , Taxus , Nanopartículas del Metal/uso terapéutico , Plata/farmacología , Espectroscopía Infrarroja por Transformada de Fourier , Antibacterianos/farmacología , Extractos Vegetales/farmacologíaRESUMEN
Dryopteris ramosa (family; Dryopteridaceae) has been reported for its medicinal importance in cancer, gastrointestinal disorders, and infections. The present study aimed to investigate the detailed phytochemical profile of D. ramosa and its cytotoxic potential using various cancer cell lines. The phytochemical profile of D. ramosa methanolic extract and its fractions were established by employing UHPLC-MS/MS and Global Natural Product Social (GNPS) molecular networking. Moreover, the cytotoxic activity of extract and fractions was evaluated against human liver (HepG-2) and prostate cancer (PC-3) cells using MTT assay. Overall, 18 compounds including flavonoids, flavonoid O-glycosides, isoflavone di-C-glycoside, flavanol, flavanone, rotenoid, phloroglucinol derivative, coumarin derivative, benzofuranone, abietic acid, and phenolic acid were observed as the major phytochemical bioactive constituents in the extract and fractions of D. ramosa. In MTT assay, chloroform fraction showed highest anti-proliferative activity against liver cancer cells (IC50 = 53.49 µg/mL) followed by n-hexane fraction (IC50 = 55.36 µg/mL), D. ramosa extract (IC50 = 85.67 µg/mL) and ethyl acetate (IC50 = 125.00 µg/mL) fraction. However, n-hexane and chloroform fractions presented maximum cytotoxic effect against prostate cancer cells with respective IC50 values of 214.53 and 281.47 µg/mL. Moreover, all the tested samples showed negligible toxicity against non-cancer (BHK-21) cells. The results indicated that D. ramosa is rich in flavonoids, phloroglucinol derivative, and phenolic acids and showed positive results in cytotoxic studies, especially against liver cancer. Therefore, it can be considered safe for the development of anticancer drugs, especially against liver cancer.
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Background: Ethnopharmacological relevance: Brugmansia, a genus of the Solanaceae family, has historically been utilized in many different parts of the world as an anti-inflammatory for treating skin infections, wounds, and bodily aches and pains. The current study aimed to investigate the potential benefits of a methanolic extract of Brugmansia aurea in the management of diabetes and underlying complications in alloxanized-induced diabetic rats. Materials and methods: Animals were divided into nine groups (n = 6). Four groups received different standard oral hypoglycemic agents; three groups received 100, 200, and 400 mg/kg of B. aurea leaf extract for six consecutive weeks, and the remaining two were normal and disease control groups. All groups received alloxan (150 mg/kg) except for the normal control. Only those animals whose glucose levels were raised to 200 mg/dl were selected for the study. After a 6-week dosage period, various biochemical parameters, as well as HbA1c, antioxidant profile, oral glucose tolerance test (OGTT), insulin sensitivity, histopathology, and insulin resistance, were measured and compared with the untreated diabetic group. Results: Brugmansia aurea leaf extract at a dose of 400 mg/kg showed potent antidiabetic activity by reducing blood glucose levels (p < 0.001) after 6 weeks of treatment. OGTT data showed that B. aurea exhibited significant (p < 0.001) glucose tolerance by significantly reducing blood glucose levels in just 2 h post-treatment. Other tests showed that plant extract significantly increased (p < 0.001) insulin sensitivity and decreased (p < 0.001) insulin resistance. The biochemical profile showed reduced triglyceride and cholesterol, while the antioxidant profile showed restoration of antioxidant enzymes in the pancreas, kidney, and liver tissues of treated rats. Conclusion: The present study indicated that crude extracts of B. aurea increase insulin sensitivity and reduce hyperlipidemia in diabetic rats, which rationalizes the traditional medicinal use of this plant as an antidiabetic agent.
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This study adopts a very effective high-performance liquid chromatography (HPLC) technique for the quantitative determination of rosmarinic acid (RA) and PCR-based amplification of biosynthetic key regulators in Isodon rugosus, Daphne mucronata, and Viburnum grandiflorum from the lower Himalayan regions. Rosmarinic acid is engaged in a variety of biological processes and has significant industrial significance. In this study, it was identified from crude methanolic extract using thin-layer chromatography with a standard, and its content was quantified using HPLC without interrupting spikes using a mixture of methanol and deionized water containing acetonitrile (70:30 v/v) and acetic acid (0.1% v/v) at UV 310 nm absorption. We used RT-PCR to identify cDNAs encoding PAL, C4H, and RAS, and Image J's semi-quantitative analysis to quantify the expression levels of genes involved in RA production from chosen plant material. The highest levels of PAL, C4H, and RAS were detected, by band intensity, in the leaves and flowers of I. rugosus, which also exhibited a substantial quantity of RA. However, in V. grandiflorum and D. mucronata the transcript of the given genes was low. The concentration of RA ranged from 187.7 to 21.2 mg g-1 for I. rugosus, 17.42 to 5.42 mg g-1 for V. grandiflorum, and 15.19 mg g-1 for D. mucronata. This study demonstrated that the method for quantifying RA from a crude methanolic extract was effective, indicating that I. rugosus might be used as an indigenous alternative source of RA.
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Metanol , Fenilalanina , Cinamatos , Extractos Vegetales/química , Acetatos , Acetonitrilos , Agua , Cromatografía Líquida de Alta Presión , Ácido RosmarínicoRESUMEN
Silver nanoparticles have received much attention, due to their wide range of biological applications as an alternative therapy for disease conditions utilizing the nanobiotechnology domain for synthesis. The current study was performed to examine the antioxidant, anticancer, antibacterial, and antifungal potential of biosynthesized silver nanoparticles (TpAgNPs) using plant extract. The TpAgNPs were produced by reacting the Tradescantia pallida extract and AgNO3 solution in nine various concentration ratios subjected to bioactivities profiling. According to the current findings, plant extract comprising phenolics, flavonoids, and especially anthocyanins played a critical role in the production of TpAgNPs. UV-visible spectroscopy also validated the TpAgNP formation in the peak range of 401-441 nm. Further, the silver ion stabilization by phytochemicals, face-centered cubic structure, crystal size, and spherical morphology of TpAgNPs were analyzed by FTIR, XRD, and SEM. Among all TpAgNPs, the biosynthesized TpAgNP6 with a medium concentration ratio (5:10) and the plant extract had effective antioxidant potentials of 77.2 ± 1.0% and 45.1 ± 0.5% free radical scavenging activity, respectively. The cytotoxic activity of TpAgNP6 in comparison to plant extract for the rhabdomyosarcoma cell line was significantly the lowest with IC50 values of 81.5 ± 1.9 and 90.59 ± 1.6 µg/ml and cell viability % of 24.3 ± 1.62 and 27.4 ± 1.05, respectively. The antibacterial and antifungal results of TpAgNPs revealed significant improvement in comparison to plant extract, i.e., minimum inhibition concentration (MIC) 64 µg/ml against Gram-negative Pseudomonas aeruginosa while, in the case of antifungal assay, TpAgNP6 was active against Candida parapsilosis. These TpAgNPs play a crucial role in determining the therapeutic potential of T. pallida due to their biological efficacy.
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Hydrazones of theophylline-7-acetic acid 5a-g have been synthesized using ultrasonic irradiation as well as conventional heating system and analyzed for their anticancer characteristics against human lung cancer cell line (A549). Compound 5g with cell viability 33.19±0.49% (100 µg/µL) compared to the starting reference drug acefylline having cell viability 86.32±11.75% (100 µg/µL) was found to be the most active anticancer agent among all. The synthesized derivatives were also exposed to hemolytic and thrombolytic studies to determine their cytotoxic profile and results revealed their low toxicity and moderate clot lysis activity.
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Antineoplásicos , Neoplasias Pulmonares , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Línea Celular Tumoral , Hemólisis , Humanos , Hidrazonas/farmacología , Neoplasias Pulmonares/tratamiento farmacológico , Relación Estructura-Actividad , Teofilina/análogos & derivadosRESUMEN
This study aimed to synthesize the silver nanoparticles (SNPs) and loaded chitosan nanoparticles (LCNPs) using Euphorbia prostata based on their anticandidal activity. Antioxidant capacity and the total phenolic and total flavonoid content of plant samples and synthesized nanoparticles (NPs) were also evaluated. SNPs and LCNPs were prepared, respectively using chemical reduction of silver salt solution and ionotropic gelation method. The anticandidal activity was assessed by broth micro-dilution method and the antioxidant activity was determined using free-radical scavenging assays. The synthesized NPs after the optimization process were found to be spherical with sizes ranging from 12 to 100 nm. Spectroscopic analysis of NPs showed the appearance of peaks in prescribed wavelength ranging between 402 and 493 nm. The synthesized NPs showed potent anticandidal activity compared to the free extract. The SNPs formulations NpEPM 7.5 and NpEPMR 7.5, showed significantly low MIC values ranging between 2 and 128 µg/mL. In the case of LCNPs, NpEPM (4:1) and NpEPME (4:1) also showed lower MIC values ranging from 32 to 256 µg/mL. The plant samples as well as NPs showed antioxidant potential. In addition, plant extracts and NPs possess the potent biological potential and can be further investigated through in vivo experiments.
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Quitosano , Euphorbia , Nanopartículas del Metal , Antioxidantes/farmacología , Quitosano/farmacología , Plata/farmacologíaRESUMEN
Phenol is the most common organic pollutant in many industrial wastewaters that may pose a health risk to humans due to its widespread application as industrial ingredients and additives. In this study, waste green tea leaves (WGTLs) were modified through chemical activation/carbonization and used as an adsorbent in the presence of ultrasound (cavitation) to eliminate phenol in the aqueous solution. Different treatments, such as cavitation, adsorption, and sono-adsorption were investigated to remove the phenol. The scanning electron microscope (SEM) morphology of the adsorbent revealed that the structure of WGTLs was porous before phenol was adsorbed. A Fourier Transform Infrared (FTIR) analysis showed an open chain of carboxylic acids after the sono-adsorption process. The results revealed that the sono-adsorption process is more efficient with enhanced removal percentages than individual processes. A maximum phenol removal of 92% was obtained using the sono-adsorption process under an optimal set of operating parameters, such as pH 3.5, 25 mg L-1 phenol concentration, 800 mg L-1 adsorbent dosage, 60 min time interval, 30 ± 2 °C temperature, and 80 W cavitation power. Removal of chemical oxygen demand (COD) and total organic carbon (TOC) reached 85% and 53%. The Freundlich isotherm model with a larger correlation coefficient (R2, 0.972) was better fitted for nonlinear regression than the Langmuir model, and the sono-adsorption process confirmed the pseudo-second-order reaction kinetics. The findings indicated that WGTLs in the presence of a cavitation effect prove to be a promising candidate for reducing phenol from the aqueous environment.