Synthesis of a New Series of Anthraquinone-Linked Cyclopentanone Derivatives: Investigating the Antioxidant, Antibacterial, Cytotoxic and Tyrosinase Inhibitory Activities of the Mushroom Tyrosinase Enzyme Using Molecular Docking

Drug Design Development and Therapy, Год журнала: 2024, Номер Volume 18, С. 597 - 612

Опубликована: Фев. 1, 2024

Purpose: New bioactive anthraquinone derivatives are investigated for antibacterial, tyrosinase inhibitory, antioxidant cytotoxic activity, and molecular docking. Methods: The compounds were produced using the grindstone method, yielding 69 to 89%. These analyzed IR, 1 H, 13 C NMR elemental mass spectral methods. Additionally, antioxidant, inhibitory activities of all synthesised evaluated. Results: Compound 2 showed remarkable inhibition with an (IC 50 : 13.45 μg/mL), compared kojic acid 19.40 μg/mL). It also exhibited moderate antibacterial respect references BHT ampicillin, respectively. Kinetic analysis revealed that activity compound was non-competitive competitive, whereas low. All (1-8) significantly less active than doxorubicin (LC 0.74± 0.01μg/mL). However, affinity 2Y9X protein lower acid, a docking score (− 8.6 kcal/mol 4.7 kcal/mol), making it more effective. Conclusion: synthesized displayed activities, showing exceptional potency as multitarget agent. Anthraquinone substituent groups may offer potential development treatments. their inspected. Molecular dynamics simulations performed validate results confirm stability compounds. Keywords: anthraquinone, enzyme, docking, binding affinity,

Язык: Английский

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Affinity gel synthesis from the p-aminobenzoic acid derivative 4-amino-2-methylbenzoic acid and purification of polyphenol oxidase from various plant sources

Protein Expression and Purification, Год журнала: 2024, Номер 219, С. 106474 - 106474

Опубликована: Март 20, 2024

Язык: Английский

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Ornamental cabbage (Brassica oleracea var. acephala) responses to phytase enzyme purified from Lactobacillus coryniformis application

Biotechnology and Applied Biochemistry, Год журнала: 2023, Номер 70(3), С. 1407 - 1420

Опубликована: Фев. 13, 2023

In order to increase the quality and yield of ornamental plants, especially potted it is necessary enrich physical properties growing medium ensure continuity medium. achieve this, organic substances that create a serious cost in plant cultivation are added This study was planned assess role inoculation different levels seeds soaking times purified phytase, on growth decorative values cabbage plants under nutrient limiting condition greenhouse. Different doses (E0 : 0 EU, E1 5 E2 10 EU), (W15 15 min, W30 30 W60 60 min), their combinations + E0 , W15 ) phytase enzyme isolated from Lactobacillus coryniformis were applied seeds, they sown plug trays filled with appropriate Seedlings planted plastic pots during period when seedlings had four five true leaves. Treatments microorganism generally improved observed parameters. The application of, especially, highest level increased height, main stem diameter as compared control treatment: distilled water). While number leaves per obtained at times; times. present clarified can concentration time promising biotechnology material for agricultural applications, species.

Язык: Английский

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Recent Advancement in Bioactive Chalcone Hybrids as Potential Antimicrobial Agents in Medicinal Chemistry

Mini-Reviews in Medicinal Chemistry, Год журнала: 2023, Номер 24(2), С. 176 - 195

Опубликована: Июль 27, 2023

Chalcones are flavonoid-related aromatic ketones and enones generated from plants. The chalcones have a wide range of biological activities, such as anti-tumor, calming, antimicrobial activities. In the present review, we focused on recently published original research articles unique antibacterial framework in medicinal chemistry. structurally diverse moieties can be split into simple hybrid chalcones, with both having core pharmacophore 1,3-diaryl-2-propen-1-one. isolated natural sources also synthesized by using various methods. Their structure-activity relationship, mechanisms, list patents summarized this paper. This review article outlines currently chalcone hybrids suggests that derivatives may potential agents future.

Язык: Английский

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The Effects of Apigenin in the Treatment of Diabetic Nephropathy: A Systematic Review of Non-clinical Studies

Mini-Reviews in Medicinal Chemistry, Год журнала: 2023, Номер 24(3), С. 341 - 354

Опубликована: Окт. 15, 2023

Diabetes is one of the important and growing diseases in world. Among most common diabetic complications are renal adverse effects. The use apigenin may prevent development progression diabetes-related injuries. current study aims to review effects treatment nephropathy.

Язык: Английский

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Naringenin, Hesperidin and Quercetin Ameliorate Radiation‐Induced Damage In Rats: In Vivo And In Silico Evaluations

Chemistry & Biodiversity, Год журнала: 2023, Номер 21(2)

Опубликована: Дек. 18, 2023

Abstract In this study, we sought to determine how well naringenin, hesperidin, and quercetin prevented damage brought on by radiotherapy. During the investigation, 48 adult female Sprague Dawley rats were used. Eight groups of eight each formed randomly assigning groups. The normal control group was represented Group 1. 2 those that received a dose 15 Gray (Gy) assigned 3 only Naringenin, whereas 4 quercetine, 5 hesperidin. Rats in 6, 7 8 quarcetin hesperidin at 50 mg/kg daily for one week prior radiotheraphy exposition. After phenolic compounds sacrificed some metabolic enzyme (aldose reductase (AR), sorbitol dehydrogenase (SDH), paraoxonase‐1 (PON1), butyrylcholinesterase (BChE) glutathione S‐transferase (GST)) activity determined eye brain tissues. It found have protective effect against radiation‐induced because their anti‐diabetic antioxidant anti‐inflammatory properties. addition, be superior naringenin terms efficacy. Furthermore, exhibited favorable binding affinity BChE silico compared other enzymes.

Язык: Английский

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Some pyrroles as inhibitors of the pentose phosphate pathways enzymes: An in vitro and molecular docking study

Journal of Molecular Recognition, Год журнала: 2024, Номер 37(3)

Опубликована: Март 21, 2024

Abstract Glucose‐6‐phosphate dehydrogenase (G6PD) and 6‐phosphogluconate (6PGD) are pentose phosphate pathway enzymes. Compounds with a heterocyclic pyrrole ring system containing this atom can be derivatized various functional groups into highly effective bioactive agents. In study, derivatives on these enzyme's activity were investigated. The IC 50 values of different concentrations for G6PD found in the range 0.022–0.221 mM K i 0.021 ± 0.003–0.177 6PGD 0.020–0.147, 0.013 0.002–0.113 0.030 mM. 2‐acetyl‐1‐methylpyrrole ( 1g ) showed best inhibition value addition, silico molecular docking experiments performed to elucidate how 1a – g interact binding sites target study's findings could used create innovative therapeutics that treatment many diseases, especially cancer manifestations.

Язык: Английский

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Unveiling the Molecular Mechanism of Diosmetin and its Impact on Multifaceted Cellular Signaling Pathways

Protein and Peptide Letters, Год журнала: 2024, Номер 31(4), С. 275 - 289

Опубликована: Апрель 1, 2024

Background: Diosmetin is an O-methylated flavone and the aglycone part of flavonoid glycosides diosmin that occurs naturally in citrus fruits. Pharmacologically, diosmetin reported to exhibit anticancer, antimicrobial, antioxidant, oestrogenic, anti-inflammatory activities. Objective: This comprehensive review was aimed critically explore diverse pharmacological activities exhibited by diosmetin. Along with that, this can also identify potential research areas elucidation multifactorial underlying signaling mechanism action different diseases. Methods: A collection evidence insights obtained from scientific journals books physical libraries electronic platforms like Google Scholar PubMed. The time frame selected year 1992 July 2023. Results: delves into diosmetin's impact on cellular pathways its various Due ability modulate reduce oxidative stress, it be suggested as a versatile therapeutic agent for mitigating stressassociated pathogenesis. Conclusion: amalgamation underscores promising role multifaceted agent, highlighting drug development clinical applications.

Язык: Английский

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Identification of dilated cardiomyopathy‐linked key genes by bioinformatics methods and evaluating the impact of tannic acid and monosodium glutamate in rats

Biotechnology and Applied Biochemistry, Год журнала: 2024, Номер unknown

Опубликована: Сен. 25, 2024

Abstract Dilated cardiomyopathy (DCM) is the most common type of myocardial dysfunction, affecting mostly young adults, but its therapeutic diagnosis and biomarkers for prognosis are lacking. This study aimed to investigate possible effect food additive monosodium glutamate (MSG) tannic acid (TA), a phenolic compound, on key molecular actors responsible DCM. DCM‐related publicly available microarray datasets (GSE120895, GSE17800, GSE19303) were downloaded from comprehensive Gene Expression Omnibus (GEO) database, analyzed identify differentially expressed genes (DEGs). By integrating DEGs gene‐disease validity curation results, overlapping screened identified as hub genes. Protein‐protein interaction (PPI) network ontology analysis performed make sense biological data. Finally, mRNA expression changes in heart tissues rats treated with MSG TA measured by qPCR method. Six upregulated ( IGF1, TTN, ACTB, LMNA, EDN1 , NPPB ) between DCM healthy control samples results revealed that levels these involved development increased significantly rat exposed MSG. In contrast, this increase was remarkably alleviated treatment. Our provide new insights into critical mechanisms should be focused future studies. Moreover, may play role formation, used promising agent

Язык: Английский

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Rapid identification of chemical components in Xuelian granule by UHPLC-Q-orbitrap-HRMS based on enzyme activity in vitro

BMC Complementary Medicine and Therapies, Год журнала: 2023, Номер 23(1)

Опубликована: Июль 5, 2023

Abstract Background Xuelian granule (XL), a traditional Chinese medicine (TCM) formula, has been used for the treatment of diabetic nephropathy long time as hospital preparation. Because active ingredients in XL that can help to treat are still unclear, which limits interpretation its pharmacological mechanism, further development and subsequent study on material basis efficacy. Methods In this study, screening method based inhibition activity against aldose reductase (AR) was employed activity-directed chemical analysis using ultra-high performance liquid chromatography combined with quadrupole-orbitrap high resolution mass spectrometry (UHPLC-Q-orbitrap-HRMS) technique. Results A total 178 compounds, including 46 terpenes, 47 organic acids, 25 flavonoids, 29 phenylethanoid glycosides, 31 other types, were tentatively identified from might responsible AR activity. Conclusion This is first systematic, rapid, accurate qualitative XL. research provides scientific experimental researches pharmacodynamics quality control

Язык: Английский

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