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1.
Funct Integr Genomics ; 24(2): 73, 2024 Apr 10.
Artículo en Inglés | MEDLINE | ID: mdl-38598147

RESUMEN

Vitamin C, also known as ascorbic acid, is an essential nutrient that plays a critical role in many physiological processes in plants and animals. In humans, vitamin C is an antioxidant, reducing agent, and cofactor in diverse chemical processes. The established role of vitamin C as an antioxidant in plants is well recognized. It neutralizes reactive oxygen species (ROS) that can cause damage to cells. Also, it plays an important role in recycling other antioxidants, such as vitamin E, which helps maintain the overall balance of the plant's antioxidant system. However, unlike plants, humans cannot synthesize ascorbic acid or vitamin C in their bodies due to the absence of an enzyme called gulonolactone oxidase. This is why humans need to obtain vitamin C through their diet. Different fruits and vegetables contain varying levels of vitamin C. The biosynthesis of vitamin C in plants occurs primarily in the chloroplasts and the endoplasmic reticulum (ER). The biosynthesis of vitamin C is a complex process regulated by various factors such as light, temperature, and plant hormones. Recent research has identified several key genes that regulate vitamin C biosynthesis, including the GLDH and GLDH genes. The expression of these genes is known to be regulated by various factors such as light, temperature, and plant hormones. Recent studies highlight vitamin C's crucial role in regulating plant stress response pathways, encompassing drought, high salinity, and oxidative stress. The key enzymes in vitamin C biosynthesis are L-galactose dehydrogenase (GLDH) and L-galactono-1, 4-lactone dehydrogenase (GLDH). Genetic studies reveal key genes like GLDH and GLDH in Vitamin C biosynthesis, offering potential for crop improvement. Genetic variations influence nutritional content through their impact on vitamin C levels. Investigating the roles of genes in stress responses provides insights for developing resilient techniques in crop growth. Some fruits and vegetables, such as oranges, lemons, and grapefruits, along with strawberries and kiwi, are rich in vitamin C. Guava. Papaya provides a boost of vitamin C and dietary fiber. At the same time, red and yellow bell peppers, broccoli, pineapple, mangoes, and kale are additional sources of this essential nutrient, promoting overall health. In this review, we will discuss a brief history of Vitamin C and its signaling and biosynthesis pathway and summarize the regulation of its content in various fruits and vegetables.


Asunto(s)
Ácido Ascórbico , Verduras , Animales , Humanos , Antioxidantes , Frutas/genética , Reguladores del Crecimiento de las Plantas , Productos Agrícolas/genética , Transducción de Señal
2.
Crit Rev Biotechnol ; : 1-19, 2024 Jan 17.
Artículo en Inglés | MEDLINE | ID: mdl-38232958

RESUMEN

The market size of biosurfactants (BSs) has been expanding at an extremely fast pace due to their broad application scope. Therefore, the re-construction of cell factories with modified genomic and metabolic profiles for desired industrial performance has been an intriguing aspect. Typical mutagenesis approaches generate huge mutant libraries, whereas a battery of specific, robust, and cost-effective high-throughput screening (HTS) methods is requisite to screen target strains for desired phenotypes. So far, only a few specialized HTS assays have been developed for BSs that were successfully applied to obtain anticipated mutants. The most important milestones to reach, however, continue to be: specificity, sensitivity, throughput, and the potential for automation. Here, we discuss important colorimetric and fluorometric HTS approaches for possible intervention on automated HTS platforms. Moreover, we explain current bottlenecks in developing specialized HTS platforms for screening high-yielding producers and discuss possible perspectives for addressing such challenges.

3.
Ecotoxicol Environ Saf ; 281: 116616, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38917589

RESUMEN

The urgent need to address the severe environmental risk posed by chromium-contaminated industrial wastewater necessitates the development of eco-friendly cleanup methodologies. Utilizing the Ficus benghalensis plant extracts, the present study aims to develop green zinc oxide nanoparticles for the removal of Cr metal ions from wastewater. The leaves of Ficus benghalensis, often known as the banyan tree, were used to extract a solution for synthesizing ZnO NPs. These nanoparticles were developed with the goal of efficiently eliminating chromium (Cr) from industrial effluents. Batch studies were carried out to assess the efficiency of these synthesized ZnO NPs in treating leather industrial effluent, with aiming for optimal chromium removal. This involved measuring the nanoparticles' capacity to adsorb Cr ions from wastewater samples by comparing chromium levels before and after treatment. Removal efficiency for Cr was estimated through the batches such as optimization of pH, contact time, initial Cr concentration and sorbent dose of ZnO NPs were of the batches. These synthesized ZnO NPs were found to be successful in lowering chromium levels in wastewater to meet permissible limit. The nanoparticles exhibited their highest absorption capacity, reaching 94 % (46 mg/g) at pH 4, with a contact time of 7 hours with the optimum sorbent dose of 0.6 g/L. Hence, the excellent adsorption capabilities of these nanoparticles, together with their environmentally benign manufacturing technique, provide a long-term and efficient solution for chromium-contaminated wastewater treatment. Its novel nature has the potential to significantly improve the safety and cleanliness of water ecosystems, protecting the both i.e. human health and the environment.


Asunto(s)
Cromo , Ficus , Tecnología Química Verde , Extractos Vegetales , Aguas Residuales , Contaminantes Químicos del Agua , Óxido de Zinc , Óxido de Zinc/química , Ficus/química , Cromo/análisis , Cromo/química , Aguas Residuales/química , Contaminantes Químicos del Agua/análisis , Contaminantes Químicos del Agua/química , Extractos Vegetales/química , Tecnología Química Verde/métodos , Residuos Industriales/análisis , Adsorción , Nanopartículas del Metal/química , Eliminación de Residuos Líquidos/métodos , Purificación del Agua/métodos , Nanopartículas/química , Hojas de la Planta/química
4.
J Environ Manage ; 357: 120759, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38554453

RESUMEN

Climate change is increasingly affecting the nutritional content and structural integrity of horticultural crops, leading to challenges such as diminished fruit quality and the exacerbation of fruit cracking. This manuscript systematically explores the multifaceted impacts of these changes, with a particular focus on the nutritional quality and increased incidence of fruit cracking. An exhaustive review of current research identifies the critical role of transcription factors in mediating plant responses to climatic stressors, such as drought, temperature extremes, and saline conditions. The significance of transcription factors, including bHLH, bZIP, DOF, MDP, HD-ZIP, MYB, and ERF4, is highlighted in the development of fruit cracking, underscoring the genetic underpinnings behind stress-related phenotypic outcomes. The effectiveness of greenhouse structures in mitigating adverse climatic effects is evaluated, offering a strategic approach to sustain crop productivity amidst CO2 fluctuations and water scarcity, which are shown to influence plant physiology and lead to changes in fruit development, nutrient dynamics, and a heightened risk of cracking. Moreover, the manuscript delves into advanced breeding strategies and genetic engineering techniques, such as genome editing, to enhance crop resilience against climatic challenges. It also discusses adaptation strategies vital for sustainable horticulture, emphasizing the need to integrate novel genetic insights with controlled environment horticulture to counteract climate change's detrimental effects. The synthesis presented here underscores the urgent need for innovative breeding strategies aimed at developing resilient crop varieties that can withstand climatic uncertainty while preserving nutritional integrity.


Asunto(s)
Cambio Climático , Frutas , Fitomejoramiento , Productos Agrícolas/genética , Horticultura , Factores de Transcripción
5.
Funct Integr Genomics ; 23(3): 212, 2023 Jun 27.
Artículo en Inglés | MEDLINE | ID: mdl-37368046

RESUMEN

In recent years, significant progress has been made in understanding the biosynthetic pathway and regulation of flavonoids through forward genetic approaches. However, there remains a notable gap in knowledge regarding the functional characterization and underlying processes of the transport framework responsible for flavonoid transport. This aspect requires further investigation and clarification to achieve a comprehensive understanding. Presently, there are a total of four proposed transport models associated with flavonoids, namely glutathione S-transferase (GST), multidrug and toxic compound extrusion (MATE), multidrug resistance-associated protein (MRPs), and bilitranslocase-homolog (BTL). Extensive research has been conducted on the proteins and genes related to these transport models. However, despite these efforts, numerous challenges still exist, leaving much to be explored in the future. Gaining a deeper understanding of the mechanisms underlying these transport models holds immense potential for various fields such as metabolic engineering, biotechnological approaches, plant protection, and human health. Therefore, this review aims to provide a comprehensive overview of recent advancements in the understanding of flavonoid transport mechanisms. By doing so, we aim to paint a clear and coherent picture of the dynamic trafficking of flavonoids.


Asunto(s)
Flavonoides , Plantas , Humanos , Transporte Biológico , Plantas/genética , Glutatión Transferasa/genética , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Regulación de la Expresión Génica de las Plantas
6.
J Sep Sci ; 46(14): e2200914, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37249391

RESUMEN

Multimode chromatographic separations are highly desirable in pharmaceutical and environmental sciences. Current study deals with the application of newly developed mixed-mode end capped-immobilized humic acid onto an aminopropyl silica based chromatographic column for separation and identification of six drugs belonging to different therapeutic groups for its applicability in pharmaceutical industries. For this, central composite design was used to evaluate the separation and resolution by optimization of three most effective parameters (acetonitrile%, flow rate, and pH of mobile phase). Second-order quadratic model was used to evaluate their effect on resolution of peaks; the probability value (<0.05) obtained from analysis of variance suggested the best applicability of the model. Desirability function was applied to calculate optimum conditions (44.8% acetonitrile, 1.75 mL/min of flow rate, and 7.5 pH) required to achieve maximum separation with good resolution within 11 min. The method was validated for linearity, precision accuracy, selectivity, and sensitivity. The results revealed a highly precise (coefficient of variance > 1%), linear (R2  = 0.99), and highly selective method. Moreover, the limit of detection/quantification values revealed acceptable sensitivity of the method. The developed column was compared for its efficiency with a commercially available column and found to be highly applicable for industrial applications.


Asunto(s)
Sustancias Húmicas , Cromatografía Líquida de Alta Presión/métodos , Acetonitrilos , Preparaciones Farmacéuticas
7.
Ecotoxicol Environ Saf ; 263: 115231, 2023 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-37429088

RESUMEN

Water contamination can be detrimental to the human health due to higher concentration of carcinogenic heavy metals such as chromium (Cr) in the wastewater. Many traditional methods are being employed in wastewater treatment plants for Cr removal to control the environmental impacts. Such methods include ion exchange, coagulation, membrane filtration, and chemical precipitation and microbial degradation. Recent advances in materials science and green chemistry have led to the development of nanomaterial that possess high specific surface areas and multiple functions, making them suitable for removing metals such as Cr from wastewater. Literature shows that the most efficient, effective, clean, and long-lasting approach for removing heavy metals from wastewater involves adsorbing heavy metals onto the surface of nanomaterial. This review assesses the removal methods of Cr from wastewater, advantages and disadvantages of using nanomaterial to remove Cr from wastewater and potential negative impacts on human health. The latest trends and developments in Cr removal strategies using nanomaterial adsorption are also explored in the present review.


Asunto(s)
Metales Pesados , Contaminantes Químicos del Agua , Humanos , Cromo/análisis , Aguas Residuales , Contaminantes Químicos del Agua/análisis , Adsorción , Concentración de Iones de Hidrógeno
8.
Int J Mol Sci ; 24(3)2023 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-36769327

RESUMEN

In this work, BTEAC (benzyl triethylammonium chloride) was employed as a phase transfer catalyst in an improved synthesis (up to 88% yield) of S-alkylated bromobenzofuran-oxadiazole scaffolds BF1-9. These bromobenzofuran-oxadiazole structural hybrids BF1-9 were evaluated in vitro against anti-hepatocellular cancer (HepG2) cell line as well as for their in silico therapeutic potential against six key cancer targets, such as EGFR, PI3K, mTOR, GSK-3ß, AKT, and Tubulin polymerization enzymes. Bromobenzofuran structural motifs BF-2, BF-5, and BF-6 displayed the best anti-cancer potential and with the least cell viabilities (12.72 ± 2.23%, 10.41 ± 0.66%, and 13.08 ± 1.08%), respectively, against HepG2 liver cancer cell line, and they also showed excellent molecular docking scores against EGFR, PI3K, mTOR, and Tubulin polymerization enzymes, which are major cancer targets. Bromobenzofuran-oxadiazoles BF-2, BF-5, and BF-6 displayed excellent binding affinities with the active sites of EGFR, PI3K, mTOR, and Tubulin polymerization enzymes in the molecular docking studies as well as in MMGBSA and MM-PBSA studies. The stable bindings of these structural hybrids BF-2, BF-5, and BF-6 with the enzyme targets EGFR and PI3K were further confirmed by molecular dynamic simulations. These investigations revealed that 2,5-dimethoxy-based bromobenzofuran-oxadiazole BF-5 (10.41 ± 0.66% cell viability) exhibited excellent cytotoxic therapeutic efficacy. Moreover, computational studies also suggested that the EGFR, PI3K, mTOR, and Tubulin polymerization enzymes were the probable targets of this BF-5 scaffold. In silico approaches, such as molecular docking, molecular dynamics simulations, and DFT studies, displayed excellent association with the experimental biological data of bromobenzofuran-oxadiazoles BF1-9. Thus, in silico and in vitro results anticipate that the synthesized bromobenzofuran-oxadiazole hybrid BF-5 possesses prominent anti-liver cancer inhibitory effects and can be used as lead for further investigation for anti-HepG2 liver cancer therapy.


Asunto(s)
Antineoplásicos , Neoplasias , Antineoplásicos/química , Catálisis , Proliferación Celular , Receptores ErbB/metabolismo , Glucógeno Sintasa Quinasa 3 beta/metabolismo , Simulación del Acoplamiento Molecular , Estructura Molecular , Oxadiazoles/química , Fosfatidilinositol 3-Quinasas/metabolismo , Relación Estructura-Actividad , Serina-Treonina Quinasas TOR/metabolismo , Tubulina (Proteína)/metabolismo , Ultrasonido , Humanos , Línea Celular Tumoral
9.
Int J Mol Sci ; 24(7)2023 Apr 03.
Artículo en Inglés | MEDLINE | ID: mdl-37047665

RESUMEN

Ring expansion reactions fascinate synthetic chemists owing to their importance in synthesizing biologically active compounds and their efficacy in medicinal chemistry. The present review summarizes a number of synthetic methodologies, including stereoselective and regioselective pathways adopted by scientists, for framing medium- to large-size carbo- and heterocycles involving lactams, lactone, azepine and azulene derivatives via ring expansion of six-membered carbo- and heterocycles that have been reported from 2007-2022. Numerous rearrangement and cycloaddition reactions involving Tiffeneau-Demjanov rearrangement, Aza-Claisen rearrangement, Schmidt rearrangement, Beckmann rearrangement, etc., have been described in this regard.


Asunto(s)
Compuestos Heterocíclicos , Lactamas , Reacción de Cicloadición , Ciclización , Química Farmacéutica , Compuestos Heterocíclicos/química
10.
Molecules ; 28(2)2023 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-36677762

RESUMEN

Allenes with two carbon-carbon double bonds belong to a unique class of unsaturated hydrocarbons. The central carbon atom of allene is sp hybridized and forms two σ-bonds and two π-bonds with two terminal sp2 hybridized carbon atoms. The chemistry of allenes has been well documented over the last decades. They are more reactive than alkenes due to higher strain and exhibit significant axial chirality, thus playing a vital role in asymmetric synthesis. Over a variety of organic transformations, allenes specifically undergo classical metal catalyzed cycloaddition reactions to obtain chemo-, regio- and stereoselective cycloadducts. This review briefly describes different types of annulations including [2+2], [2+2+1], [3+2], [2+2+2], [4+2], [5+2], [6+2] cycloadditions using titanium, cobalt, rhodium, nickel, palladium, platinum, gold and phosphine catalyzed reactions along with a mechanistic study of some highlighted protocols. The synthetic applications of these reactions towards the synthesis of natural products such as aristeromycin, ent-[3]-ladderanol, waihoensene(-)-vindoline and (+)-4-epi-vindoline have also been described.

11.
Molecules ; 28(15)2023 Jul 26.
Artículo en Inglés | MEDLINE | ID: mdl-37570621

RESUMEN

Simmons-Smith cyclopropanation is a widely used reaction in organic synthesis for stereospecific conversion of alkenes into cyclopropane. The utility of this reaction can be realized by the fact that the cyclopropane motif is a privileged synthetic intermediate and a core structural unit of many biologically active natural compounds such as terpenoids, alkaloids, nucleosides, amino acids, fatty acids, polyketides and drugs. The modified form of Simmons-Smith cyclopropanation involves the employment of Et2Zn and CH2I2 (Furukawa reagent) toward the total synthesis of a variety of structurally complex natural products that possess broad range of biological activities including anticancer, antimicrobial and antiviral activities. This review aims to provide an intriguing glimpse of the Furukawa-modified Simmons-Smith cyclopropanation, within the year range of 2005 to 2022.


Asunto(s)
Alcaloides , Productos Biológicos , Productos Biológicos/química , Alcaloides/química , Ciclización , Nucleósidos , Ciclopropanos/química
12.
Molecules ; 28(11)2023 May 26.
Artículo en Inglés | MEDLINE | ID: mdl-37298842

RESUMEN

The Corey-Seebach reagent plays an important role in organic synthesis because of its broad synthetic applications. The Corey-Seebach reagent is formed by the reaction of an aldehyde or a ketone with 1,3-propane-dithiol under acidic conditions, followed by deprotonation with n-butyllithium. A large variety of natural products (alkaloids, terpenoids, and polyketides) can be accessed successfully by utilizing this reagent. This review article focuses on the recent contributions (post-2006) of the Corey-Seebach reagent towards the total synthesis of natural products such as alkaloids (lycoplanine A, diterpenoid alkaloids, etc.), terpenoids (bisnorditerpene, totarol, etc.), polyketide (ambruticin J, biakamides, etc.), and heterocycles such as rodocaine and substituted pyridines, as well and their applications towards important organic synthesis.


Asunto(s)
Alcaloides , Productos Biológicos , Policétidos , Indicadores y Reactivos , Terpenos
13.
Molecules ; 28(6)2023 Mar 17.
Artículo en Inglés | MEDLINE | ID: mdl-36985698

RESUMEN

Sharpless asymmetric dihydroxylation is an important reaction in the enantioselective synthesis of chiral vicinal diols that involves the treatment of alkene with osmium tetroxide along with optically active quinine ligand. Sharpless introduced this methodology after considering the importance of enantioselectivity in the total synthesis of medicinally important compounds. Vicinal diols, produced as a result of this reaction, act as intermediates in the synthesis of different naturally occurring compounds. Hence, Sharpless asymmetric dihydroxylation plays an important role in synthetic organic chemistry due to its undeniable contribution to the synthesis of biologically active organic compounds. This review emphasizes the significance of Sharpless asymmetric dihydroxylation in the total synthesis of various natural products, published since 2020.


Asunto(s)
Productos Biológicos , Hidroxilación , Productos Biológicos/química , Alquenos , Estereoisomerismo
14.
Molecules ; 28(24)2023 Dec 10.
Artículo en Inglés | MEDLINE | ID: mdl-38138522

RESUMEN

The Petasis reaction, also called the Petasis Borono-Mannich reaction, is a multicomponent reaction that couples a carbonyl derivative, an amine and boronic acids to yield substituted amines. The reaction proceeds efficiently in the presence or absence of a specific catalyst and solvent. By employing this reaction, a diverse range of chiral derivatives can easily be obtained, including α-amino acids. A broad substrate scope, high yields, distinct functional group tolerance and the availability of diverse catalytic systems constitute key features of this reaction. In this review article, attention has been drawn toward the recently reported methodologies for executing the Petasis reaction to produce structurally simple to complex aryl/allyl amino scaffolds.

15.
BMC Plant Biol ; 22(1): 2, 2022 Jan 03.
Artículo en Inglés | MEDLINE | ID: mdl-34979911

RESUMEN

BACK GROUND: MYB Transcription factors (TFs) are most imperative and largest gene family in plants, which participate in development, metabolism, defense, differentiation and stress response. The MYB TFs has been studied in various plant species. However, comprehensive studies of MYB gene family in the sweet cherry (Prunus avium L.) are still unknown. RESULTS: In the current study, a total of 69 MYB genes were investigated from sweet cherry genome and classified into 28 subfamilies (C1-C28 based on phylogenetic and structural analysis). Microcollinearity analysis revealed that dispersed duplication (DSD) events might play an important role in the MYB genes family expansion. Chromosomal localization, the synonymous (Ks) and nonsynonymous (Ka) analysis, molecular characteristics (pI, weight and length of amino acids) and subcellular localization were accomplished using several bioinformatics tools. Furthermore, the members of distinct subfamilies have diverse cis-acting regions, conserved motifs, and intron-exon architectures, indicating functional heterogeneity in the MYB family. Moreover, the transcriptomic data exposed that MYB genes might play vital role in bud dormancy. The quantitative real-time qRT-PCR was carried out and the expression pattern indicated that MYB genes significantly expressed in floral bud as compared to flower and fruit. CONCLUSION: Our comprehensive findings provide supportive insights into the evolutions, expansion complexity and functionality of PavMYB genes. These PavMYB genes should be further investigated as they seem to be brilliant candidates for dormancy manipulation in sweet cherry.


Asunto(s)
Flores/crecimiento & desarrollo , Frutas/crecimiento & desarrollo , Proteínas de Plantas/genética , Prunus avium/genética , Factores de Transcripción/genética , Flores/genética , Frutas/genética , Familia de Multigenes , Proteínas de Plantas/metabolismo , Prunus avium/crecimiento & desarrollo , Prunus avium/metabolismo , Factores de Transcripción/metabolismo
16.
Ecotoxicol Environ Saf ; 242: 113892, 2022 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-35863217

RESUMEN

Rhamnolipid biosurfactants are multifunctional compounds that can play an indispensable role in biotechnological, biomedical, and environmental bioremediation-related fields, and have attracted significant attention in recent years. Herein, a novel strain Pseudomonas sp. S1WB was isolated from an oil-contaminated water sample. The biosurfactants produced by this strain have capabilities to reduce surface tension (SFT) at 32.75 ± 1.63 mN/m and emulsified 50.2 ± 1.13 % in liquid media containing 1 % used engine oil (UEO) as the sole carbon source. However, the lowest SFT reduction (28.25 ± 0.21), highest emulsification index (60.15 ± 0.07), and the maximum yields (900 mg/L) were achieved under optimized conditions; where, the glucose/urea and glycerol/urea combinations were found efficient carbon and nitrogen substrates for improved biosurfactants production. Biosurfactants product was characterized using ultra-high performance liquid chromatography-mass spectrometry (UHPLC- MS) and detected various di- rhamnolipids congeners. In addition, the di-rhamnolipids produced by S1WB strain was found highly stable in terms of surface activity and EI indices at different environmental factors i.e. temperature, pH and various NaCl concentrations, where, emulsifying property was found high stable till 30 days of incubation. Moreover, the stain was capable to degrade hydrocarbon at 42.2 ± 0.04 %, and the Gas chromatography- mass spectrometry (GC-MS) profile showed the majority of peak intensities of hydrocarbons have been completely degraded compared to control.


Asunto(s)
Petróleo , Biodegradación Ambiental , Carbono , Glucolípidos/química , Hidrocarburos/metabolismo , Petróleo/metabolismo , Pseudomonas/metabolismo , Tensoactivos/química , Urea
17.
Int J Mol Sci ; 23(18)2022 Sep 19.
Artículo en Inglés | MEDLINE | ID: mdl-36142889

RESUMEN

Furan-oxadiazole structural hybrids belong to the most promising and biologically active classes of oxygen and nitrogen containing five member heterocycles which have expanded therapeutic scope and potential in the fields of pharmacology, medicinal chemistry and pharmaceutics. A novel series 5a-j of benzofuran-oxadiazole molecules incorporating S-alkylated amide linkage have been synthesized using ultrasonic irradiation and screened for bacterial tyrosinase inhibition activity. Most of the synthesized furan-oxadiazole structural motifs exhibited significant tyrosinase inhibition activity in the micromolar range, with one of the derivatives being more potent than the standard drug ascorbic acid. Among the tested compounds, the scaffold 5a displayed more tyrosinase inhibition efficacy IC50 (11 ± 0.25 µM) than the ascorbic acid IC50 (11.5 ± 0.1 µM). Compounds 5b, 5c and 5d efficiently inhibited bacterial tyrosinase with IC50 values in the range of 12.4 ± 0.0-15.5 ± 0.0 µM. The 2-fluorophenylacetamide containing furan-oxadiazole compound 5a may be considered as a potential lead for tyrosinase inhibition with lesser side effects as a skin whitening and malignant melanoma anticancer agent.


Asunto(s)
Antineoplásicos , Benzofuranos , Amidas , Antineoplásicos/farmacología , Ácido Ascórbico , Benzofuranos/farmacología , Quimioinformática , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Furanos , Simulación del Acoplamiento Molecular , Estructura Molecular , Monofenol Monooxigenasa/metabolismo , Nitrógeno , Oxadiazoles/farmacología , Oxígeno , Relación Estructura-Actividad , Ultrasonido
18.
Int J Mol Sci ; 23(17)2022 Aug 29.
Artículo en Inglés | MEDLINE | ID: mdl-36077199

RESUMEN

Ultraviolet-C (UV-C) radiation significantly impacts living organisms. UV-C radiation can also be used as a pest management tool. Therefore, this study was designed to investigate the effect of UV-C radiation on the physiology and gene expression level of Plutella xylostella, a destructive vegetable pest. Results showed that, after exposure to UV-C radiation for 3, 6, 12, and 24 h, the activity of SOD (superoxide dismutase) and CAT (catalase) of P. xylostella increased, while the activity of PPO (polyphenol oxidase), POD (peroxidase), AChE (acetylcholinesterase), CarE (carboxylesterase), and ACP (acid phosphatase) decreased with increased exposure time. Correlation coefficient analyses indicated that the activity of CAT correlated positively, while PPO and CarE correlated negatively, with exposure time. Gene regulation analysis via qRT-PCR confirmed a significant increase in regulation in CAT, CarE, and PPO-related genes. We also investigated the effect of UV-C exposure on the virulence of Cordyceps fumosorosea against P. xylostella. Here, results indicated that when the fungal treatment was applied to larvae before UV-C radiation, the virulence of C. fumosorosea was significantly reduced. However, this decline in virulence of C. fumosorosea due to UV-C exposure remained only for one generation, and no effect was observed on secondary infection. On the other hand, when larvae were exposed to UV-C radiation before fungal application, the mortality rate significantly increased as the exposure time to UV-C radiation increased. From the current study, it could be concluded that UV-C exposure suppressed the immunity to P. xylostella, which later enhanced the virulence of entomopathogenic fungi. Moreover, the study also suggested that UV irradiation is an effective pest management tool that could be incorporated into pest management strategies, which could help reduce pesticide application, be economically beneficial for the farmer, and be environmentally safe.


Asunto(s)
Cordyceps , Mariposas Nocturnas , Acetilcolinesterasa , Animales , Larva/microbiología , Mariposas Nocturnas/microbiología
19.
Molecules ; 27(3)2022 Feb 02.
Artículo en Inglés | MEDLINE | ID: mdl-35164286

RESUMEN

Ultrasound- and microwave-assisted green synthetic strategies were applied to furnish benzofuran-oxadiazole 5a-g and benzofuran-triazole 7a-h derivatives in good to excellent yields (60-96%), in comparison with conventional methods (36-80% yield). These synthesized derivatives were screened for hemolysis, thrombolysis and anticancer therapeutic potential against an A549 lung cancer cell line using an MTT assay. Derivatives 7b (0.1%) and 5e (0.5%) showed the least toxicity against RBCs. Hybrid 7f showed excellent thrombolysis activity (61.4%) when compared against reference ABTS. The highest anticancer activity was displayed by the 5d structural hybridwith cell viability 27.49 ± 1.90 and IC50 6.3 ± 0.7 µM values, which were considerably lower than the reference drug crizotinib (IC50 8.54 ± 0.84 µM). Conformational analysis revealed the spatial arrangement of compound 5d, which demonstrated its significant potency in comparison with crizotinib; therefore, scaffold 5d would be a promising anticancer agent on the basis of cytotoxicity studies, as well as in silico modeling studies.


Asunto(s)
Antineoplásicos/farmacología , Benzofuranos/farmacología , Oxadiazoles/farmacología , Triazoles/farmacología , Células A549 , Antineoplásicos/síntesis química , Antineoplásicos/química , Benzofuranos/síntesis química , Benzofuranos/química , Supervivencia Celular/efectos de los fármacos , Técnicas de Química Sintética , Hemólisis/efectos de los fármacos , Humanos , Microondas , Simulación del Acoplamiento Molecular , Neoplasias/tratamiento farmacológico , Oxadiazoles/síntesis química , Oxadiazoles/química , Triazoles/síntesis química , Triazoles/química
20.
Molecules ; 27(15)2022 Jul 26.
Artículo en Inglés | MEDLINE | ID: mdl-35897953

RESUMEN

Piperazine-based dithiocarbamates serve as important scaffolds for numerous pharmacologically active drugs. The current study investigates the design and synthesis of a series of dithiocarbamates with a piperazine unit as well as their biological activities. Under ultrasound conditions, the corresponding piperazine-1-carbodithioates 5a-5j were synthesized from monosubstituted piperazine 2 and N-phenylacetamides 4a-4j in the presence of sodium acetate and carbon disulfide in methanol. The structures of the newly synthesized piperazines were confirmed, and their anti-lung carcinoma effects were evaluated. A cytotoxic assay was performed to assess the hemolytic and thrombolytic potential of the synthesized piperazines 5a-5j. The types of substituents on the aryl ring were found to affect the anticancer activity of piperazines 5a-5j. Piperazines containing 2-chlorophenyl (5b; cell viability = 25.11 ± 2.49) and 2,4-dimethylphenyl (5i; cell viability = 25.31 ± 3.62) moieties demonstrated the most potent antiproliferative activity. On the other hand, piperazines containing 3,4-dichlorophenyl (5d; 0.1%) and 3,4-dimethylphenyl (5j; 0.1%) rings demonstrated the least cytotoxicity. The piperazine with the 2,5-dimethoxyphenyl moiety (5h; 60.2%) showed the best thrombolytic effect. To determine the mode of binding, in silico modeling of the most potent piperazine (i.e., 5b) was performed, and the results were in accordance with those of antiproliferation. It exhibits a similar binding affinity to PQ10 and an efficient conformational alignment with the lipophilic site of PDE10A conserved for PQ10A.


Asunto(s)
Antineoplásicos , Piperazinas , Antineoplásicos/química , Supervivencia Celular , Simulación por Computador , Piperazina/farmacología , Piperazinas/química , Relación Estructura-Actividad
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