Articles de revues : « Imperative compounds »

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Pant, Bishnu D., Bogdan M. Benin, Nalin Abeydeera, Min-Ho Kim et Songping D. Huang. « Bi₂O₃ nanoparticles exhibit potent broad-spectrum antimicrobial activity and the ability to overcome Ag-, ciprofloxacin- and meropenem-resistance in P. aeruginosa : the next silver bullet of metal antimicrobials ? » Biomaterials Science 10, n^o 6 (2022) : 1523–31. http://dx.doi.org/10.1039/d1bm01844b.

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The rise of antimicrobial resistance (AMR) toward the conventional antibiotics and Ag compounds has made the search for metallodrugs to combat AMR imperative. Bi compounds such as the one reported in this article may emerge as the next silver bullet of metal antimicrobials.

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Lian, Ru, Fang Zhang, Yurong Zhang, Zhongping Wu, Haiying Ye, Chunfang Ni, Xiaobao Lv et Yinlong Guo. « Ion mobility derived collision cross section as an additional measure to support the rapid analysis of abused drugs and toxic compounds using electrospray ion mobility time-of-flight mass spectrometry ». Analytical Methods 10, n^o 7 (2018) : 749–56. http://dx.doi.org/10.1039/c7ay02808c.

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Zhang, Ye-Qing, Zhe Li, Tao Ling, Sergei A. Kulinich et Xi-Wen Du. « Superior gas-sensing performance of amorphous CdO nanoflake arrays prepared at room temperature ». Journal of Materials Chemistry A 4, n^o 22 (2016) : 8700–8706. http://dx.doi.org/10.1039/c6ta01300g.

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Kurniawati, Erna Yovi, Noor Pramono, Syarief Thaufik Hidayat et Endang Mahati. « In Silico Pharmacokinetic and Toxicity Analysis on Clitoria Ternatea Flower ». Jurnal Farmasi Indonesia 20, n^o 2 (30 novembre 2023) : 124–35. http://dx.doi.org/10.31001/jfi.v20i2.2190.

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This study explores the pharmacokinetic and toxicity aspects of Clitoria ternatea, which is well-known in traditional medicine for its promising pharmacological potential. Using computational methods, research seeks to unravel the interaction of active compounds in the human body, predicting not only pharmacokinetic properties but also exploring the correlation between chemical structure and parameters such as lipophilicity and P-glycoprotein substrate status, which improves our understanding of the compound's behaviour. The urgency of this research stems from the need for a safe source of therapeutics. Through in-depth in silico toxicity assessments, potential side effects of compounds are carefully identified, ensuring a comprehensive safety evaluation. This important step lays the foundation for responsible pharmacological development. This research introduces a new perspective on exploring traditional medicinal plants, emphasising the importance of safe therapeutic alternatives. The ultimate goal is to establish a solid foundation to further develop C. ternatea as a valuable resource for pharmacological applications and advance natural medicine. The results revealed many compounds with significant pharmacological potential, which show promise for future natural medicine applications. However, the imperative for additional research and experimental validation underscores our commitment to understanding the pharmacological and toxicological aspects of these compounds.

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Bai, Xinyu, Lin Zhou, Li Zhou, Song Cang, Yuhan Liu, Rui Liu, Jie Liu, Xun Feng et Ronghua Fan. « The Research Progress of Extraction, Purification and Analysis Methods of Phenolic Compounds from Blueberry : A Comprehensive Review ». Molecules 28, n^o 8 (21 avril 2023) : 3610. http://dx.doi.org/10.3390/molecules28083610.

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Blueberry is the source of a variety of bioactive substances, including phenolic compounds, such as anthocyanins, pterostilbene, phenolic acids, etc. Several studies have revealed that polyphenols in blueberry have important bioactivities in maintaining health, such as antioxidant and anti-tumor activities, immune regulation, the prevention of chronic diseases, etc. Therefore, these phenolic compounds in blueberries have been widely used in the field of healthcare, and the extraction, isolation, and purification of phenolic compounds are the prerequisites for their utilization. It is imperative to systematically review the research progress and prospects of phenolic compounds present in blueberries. Herein, the latest progress in the extraction, purification, and analysis of phenolic compounds from blueberries is reviewed, which can in turn provide a foundation for further research and usage of blueberries.

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Alkhaibari, Ibrahim, Hansa Raj KC, Duminduni H. Angappulige, David Gilmore et Mohammad A. Alam. « Novel pyrazoles as potent growth inhibitors of staphylococci, enterococci and Acinetobacter baumannii bacteria ». Future Medicinal Chemistry 14, n^o 4 (février 2022) : 233–44. http://dx.doi.org/10.4155/fmc-2021-0140.

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Background: Methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci and Acinetobacter baumannii cause serious antibiotic-resistant infections. Finding new antibiotics to treat these infections is imperative for combating this worldwide menace. Methods & Results: In this study, the authors designed and synthesized potent antimicrobial agents using 4-trifluoromethylphenyl-substituted pyrazole derivatives. In addition to their potency against planktonic bacteria, potent compounds effectively eradicated S. aureus and Enterococcus faecalis biofilms. Human cells tolerated these compounds with good selectivity factors. Furthermore, the authors provide evidence for the mode of action of compounds based on time-kill kinetics, flow cytometry analysis of propidium iodide-treated bacteria and oxygen uptake studies. Conclusion: This study demonstrated 20 novel compounds with potent antibacterial activity that are tolerated by human cell lines.

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Kathrotiya, Haresh G., et Yogesh T. Naliapara. « Synthesis of Thiophenyl Thiazole Based Novel Quinoxaline Derivatives ». International Letters of Chemistry, Physics and Astronomy 51 (mai 2015) : 115–24. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.51.115.

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A new series of thiophenyl thiazole based novel quinoxaline derivatives 4a-4t have been synthesized by base catalysed condensation reaction. In which 6-substituted 2,3-dichloroquinoxaline 1a and 4-(thiophen-2-yl) thiazol-2-amine 2b reacted in basic condition to afford intermediate 3c which reacts with various aromatic amine to form final compounds. Easy experimental procedure, high yield, and selectivity are the imperative features of this method. The identity of all the compounds has been established by 1H NMR, 13C NMR, FT-IR, and elemental analysis.

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Kathrotiya, Haresh G., et Yogesh T. Naliapara. « Synthesis of Thiophenyl Thiazole Based Novel Quinoxaline Derivatives ». International Letters of Chemistry, Physics and Astronomy 51 (15 mai 2015) : 115–24. http://dx.doi.org/10.56431/p-oioid3.

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A new series of thiophenyl thiazole based novel quinoxaline derivatives 4a-4t have been synthesized by base catalysed condensation reaction. In which 6-substituted 2,3-dichloroquinoxaline 1a and 4-(thiophen-2-yl) thiazol-2-amine 2b reacted in basic condition to afford intermediate 3c which reacts with various aromatic amine to form final compounds. Easy experimental procedure, high yield, and selectivity are the imperative features of this method. The identity of all the compounds has been established by 1H NMR, 13C NMR, FT-IR, and elemental analysis.

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López-Vallejo, Fabian, Rafael Castillo, Lilián Yépez-Mulia et José L. Medina-Franco. « Benzotriazoles and Indazoles Are Scaffolds with Biological Activity against Entamoeba histolytica ». Journal of Biomolecular Screening 16, n^o 8 (5 août 2011) : 862–68. http://dx.doi.org/10.1177/1087057111414902.

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Parasitic infections caused by Entamoeba histolytica are still major threats against public health, especially in developing countries. Although current therapies exist, the problems associated with parasite resistance and negative side effects make it imperative to search for new therapeutic agents. A systematic scaffold analysis reported herein of a public database containing 474 antiamoebic compounds reveals that benzimidazole is the most active scaffold reported thus far. To gain insights into the antiamoebic activity of novel compounds, the authors report herein the biological activity of 12 compounds, including benzotriazole and indazole derivatives, scaffolds not previously tested against E. histolytica. Compounds with the benzotriazole and indazole scaffolds showed low micromolar activity (IC50 = 0.304 and 0.339 µM) and are more active than metronidazole, which is the drug of choice used for the treatment of amebiosis. The novel compounds have similar properties to approved drugs. Compounds with novel scaffolds represent promising starting points of an optimization program against E. histolytica.

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Um, Gi-Yong, Taehoon Kwon, Seong Hwan Lee, Woong Kim, Jungsoo Kim, Hee Joong Kim et Jin Hong Lee. « The Influence of Styrene Content in Solution Styrene Butadiene Rubber on Silica-Filled Tire Tread Compounds ». Polymers 15, n^o 21 (31 octobre 2023) : 4288. http://dx.doi.org/10.3390/polym15214288.

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In tire tread applications, achieving enhanced abrasion resistance, wet grip, and rolling resistance is crucial for optimizing overall performance. To realize improvements in these attributes for silica-filled tire tread compounds, it becomes imperative to improve the dispersity of silica filler by investigating the effect of each component in the tire tread compound. In this work, we study the effect of styrene content within solution styrene butadiene rubber (SSBR) on the properties of tire tread compounds. A higher styrene segment within SSBR contributes to increased silica dispersion and crosslink density. Thus, tire tread compounds featuring SSBR with increased styrene content not only improve physical and mechanical properties, but also enhance major characteristics tailored for tire tread applications. These findings provide valuable insights into advancing the reinforced performance of tire tread compounds through the strategic utilization of SSBR enriched in styrene content.

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Wang, Shaoyu. « Leveraging budding yeast Saccharomyces cerevisiae for discovering aging modulation substances for functional food ». Functional Foods in Health and Disease 9, n^o 5 (30 mai 2019) : 297. http://dx.doi.org/10.31989/ffhd.v9i5.575.

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Background: Discovery of bioactive substances contained in functional food and the mechanism of their aging modulation are imperative steps in developing better, potent and safer functional food for promoting health and compression of morbidity in the aging population. Budding yeast (Saccharomyces cerevisiae) is invaluable model organism for aging modulation and bioactive compounds discovery. In this paper we have conceptualised a framework for achieving such aim. This framework consists of four components: discovering targets for aging modulation, discovering and validating caloric restriction mimetics, acting as cellular systems for screening natural products or compounds for aging modulation and being a biological factory for producing bioactive compounds according to the roles the yeast systems play. It have been argued that the component of being a biological factory for producing bioactive compounds has much underexplored which also present an opportunity for new active substance discovery and validation for health promotion in functional food industry.Keywords: Aging modulation, budding yeast, functional food, bioactive substances, cell factory

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Stokes, Jonathan M., Carrie Selin, Silvia T. Cardona et Eric D. Brown. « Chemical Inhibition of Bacterial Ribosome Biogenesis Shows Efficacy in a Worm Infection Model ». Antimicrobial Agents and Chemotherapy 59, n^o 5 (23 février 2015) : 2918–20. http://dx.doi.org/10.1128/aac.04690-14.

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ABSTRACTThe development of antibacterial compounds that perturb novel processes is an imperative in the challenge presented by widespread antibiotic resistance. While many antibiotics target the ribosome, molecules that inhibit ribosome assembly have yet to be used in this manner. Here we show that a novel inhibitor of ribosome biogenesis, lamotrigine, is capable of rescuingCaenorhabditis elegansfrom an establishedSalmonellainfection, revealing that ribosome biogenesis is a promising target for the development of new antibiotics.

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Salmerón, Ivan, Sergio Loeza-Serrano, Samuel Pérez-Vega et Severino S. Pandiella. « Headspace gas chromatography (HS-GC) analysis of imperative flavor compounds in Lactobacilli-fermented barley and malt substrates ». Food Science and Biotechnology 24, n^o 4 (août 2015) : 1363–71. http://dx.doi.org/10.1007/s10068-015-0175-z.

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Borcea, Anca-Maria, Gabriel Marc, Ioana Ionuț, Dan C. Vodnar, Laurian Vlase, Felicia Gligor, Andreea Pricopie, Adrian Pîrnău, Brîndușa Tiperciuc et Ovidiu Oniga. « A Novel Series of Acylhydrazones as Potential Anti-Candida Agents : Design, Synthesis, Biological Evaluation and In Silico Studies ». Molecules 24, n^o 1 (6 janvier 2019) : 184. http://dx.doi.org/10.3390/molecules24010184.

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In the context of an increased incidence of invasive fungal diseases, there is an imperative need of new antifungal drugs with improved activity and safety profiles. A novel series of acylhydrazones bearing a 1,4-phenylene-bisthiazole scaffold was designed based on an analysis of structures known to possess anti-Candida activity obtained from a literature review. Nine final compounds were synthesized and evaluated in vitro for their inhibitory activity against various strains of Candida spp. The anti-Candida activity assay revealed that some of the new compounds are as active as fluconazole against most of the tested strains. A molecular docking study was conducted in order to evaluate the binding poses towards lanosterol 14α-demethylase. An in silico ADMET analysis showed that the compounds possess drug-like properties and represent a biologically active framework that should be further optimized as potential hits.

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Venkateskumar, Krishnamoorthy, Subramani Parasuraman, Leow Y. Chuen, Veerasamy Ravichandran et Subramani Balamurgan. « Exploring Antimicrobials from the Flora and Fauna of Marine : Opportunities and Limitations ». Current Drug Discovery Technologies 17, n^o 4 (8 septembre 2020) : 507–14. http://dx.doi.org/10.2174/1570163816666190819141344.

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About 95% of earth living space lies deep below the ocean’s surface and it harbors extraordinary diversity of marine organisms. Marine biodiversity is an exceptional reservoir of natural products, bioactive compounds, nutraceuticals and other potential compounds of commercial value. Timeline for the development of the drug from a plant, synthetic and other alternative sources is too lengthy. Exploration of the marine environment for potential bioactive compounds has gained focus and huge opportunity lies ahead for the exploration of such vast resources in the ocean. Further, the evolution of superbugs with increasing resistance to the currently available drugs is alarming and it needs coordinated efforts to resolve them. World Health Organization recommends the need and necessity to develop effective bioactive compounds to combat problems associated with antimicrobial resistance. Based on these factors, it is imperative to shift the focus towards the marine environment for potential bioactive compounds that could be utilized to tackle antimicrobial resistance. Current research trends also indicate the huge strides in research involving marine environment for drug discovery. The objective of this review article is to provide an overview of marine resources, recently reported research from marine resources, challenges, future research prospects in the marine environment.

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Alqahtani, Leena S., Ahmad Salah Alkathiri, Abdulrahman Alzahrani, Rashed Mohammed Alghamdi, Waad Abdulrahmman Alamri, Mohammad Azhar Kamal, Ahmed Hamdan Aloufi, Ali Saeed Alamri et Qamre Alam. « Structure-Based Virtual Screening of Antiviral Compounds Targeting the Norovirus RdRp Protein ». Advancements in Life Sciences 11, n^o 2 (29 avril 2024) : 488. http://dx.doi.org/10.62940/als.v11i2.2830.

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Background: Human noroviruses (NV) are the primary etiological organisms causing acute gastroenteritis around the world, causing severe morbidity and imposing a significant economic burden. The RNA-dependent RNA polymerase (RdRp) is essential for viral replication and could be a promising target for anti-NV therapeutics. Despite the discovery of a few NV RdRp inhibitors, the majority of these pharmaceuticals have demonstrated limited efficacy in inhibiting viral replication in cellular models.Methods: In this study, computational screening of antiviral compounds was conducted targeting the NV RdRp protein. The assessment was based on binding poses and the key residues of RdRp involved in interactions with compounds.Results: The compounds namely, Ribavirin, BMS806, Dihydromyricetin, R7935788, and LY2784544 were found to bind the RdRp protein with high affinity. Notably, these compounds displayed significantly lower binding affinities compared to the positive control, PPNDS. In addition, these compounds exhibited many RdRp protein binding residues that were also present in the PPNDS.Conclusion: The results presented here suggest that these compounds have the potential to be used as inhibitors of NV RdRp in the development of antiviral medications. Nevertheless, due to the computational nature of this study, it is imperative to do experimental validation.Keywords: Noroviruses; RdRp; Virtual screening; Antiviral Compounds

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Thoda, Christina, et Maria Touraki. « Probiotic-Derived Bioactive Compounds in Colorectal Cancer Treatment ». Microorganisms 11, n^o 8 (27 juillet 2023) : 1898. http://dx.doi.org/10.3390/microorganisms11081898.

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Colorectal cancer (CRC) is a multifactorial disease with increased morbidity and mortality rates globally. Despite advanced chemotherapeutic approaches for the treatment of CRC, low survival rates due to the regular occurrence of drug resistance and deleterious side effects render the need for alternative anticancer agents imperative. Accumulating evidence supports that gut microbiota imbalance precedes the establishment of carcinogenesis, subsequently contributing to cancer progression and response to anticancer therapy. Manipulation of the gut microbiota composition via the administration of probiotic-derived bioactive compounds has gradually attained the interest of scientific communities as a novel therapeutic strategy for CRC. These compounds encompass miscellaneous metabolic secreted products of probiotics, including bacteriocins, short-chain fatty acids (SCFAs), lactate, exopolysaccharides (EPSs), biosurfactants, and bacterial peptides, with profound anti-inflammatory and antiproliferative properties. This review provides a classification of postbiotic types and a comprehensive summary of the current state of research on their biological role against CRC. It also describes how their intricate interaction with the gut microbiota regulates the proper function of the intestinal barrier, thus eliminating gut dysbiosis and CRC development. Finally, it discusses the future perspectives in precision-medicine approaches as well as the challenges of their synthesis and optimization of administration in clinical studies.

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Bianco, Maria da Conceição Avelino Dias, Debora Inacio Leite Firmino Marinho, Lucas Villas Boas Hoelz, Monica Macedo Bastos et Nubia Boechat. « Pyrroles as Privileged Scaffolds in the Search for New Potential HIV Inhibitors ». Pharmaceuticals 14, n^o 9 (2 septembre 2021) : 893. http://dx.doi.org/10.3390/ph14090893.

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Acquired immunodeficiency syndrome (AIDS) is caused by human immunodeficiency virus (HIV) and remains a global health problem four decades after the report of its first case. Despite success in viral load suppression and the increase in patient survival due to combined antiretroviral therapy (cART), the development of new drugs has become imperative due to strains that have become resistant to antiretrovirals. In this context, there has been a continuous search for new anti-HIV agents based on several chemical scaffolds, including nitrogenated heterocyclic pyrrole rings, which have been included in several compounds with antiretroviral activity. Thus, this review aims to describe pyrrole-based compounds with anti-HIV activity as a new potential treatment against AIDS, covering the period between 2015 and 2020. Our research allowed us to conclude that pyrrole derivatives are still worth exploring, as they may provide highly active compounds targeting different steps of the HIV-1 replication cycle and act with an innovative mechanism.

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Samad, Abdul, Moawiah M. Naffaa, Mohammed Afroz Bakht, Manav Malhotra et Majid A. Ganaie. « Target Based Designing of Anthracenone Derivatives as Tubulin Polymerization Inhibiting Agents : 3D QSAR and Docking Approach ». International Journal of Medicinal Chemistry 2014 (17 avril 2014) : 1–15. http://dx.doi.org/10.1155/2014/658016.

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Novel anthracenone derivatives were designed through in silico studies including 3D QSAR, pharmacophore mapping, and molecular docking approaches. Tubulin protein was explored for the residues imperative for activity by analyzing the binding pattern of colchicine and selected compounds of anthracenone derivatives in the active domain. The docking methodology applied in the study was first validated by comparative evaluation of the predicted and experimental inhibitory activity. Furthermore, the essential features responsible for the activity were established by carrying out pharmacophore mapping studies. 3D QSAR studies were carried out for a series of 1,5- and 1,8-disubstituted10-benzylidene-10H-anthracen-9-ones and 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-one derivatives for their antiproliferation activity. Based on the pattern recognition studies obtained from QSAR results, ten novel compounds were designed and docked in the active domain of tubulin protein. One of the novel designed compounds “N1” exhibited binding energy −9.69 kcal/mol and predicted Ki 78.32 nM which was found to be better than colchicine.

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Venkatesan, Arthi, Lavanya Ravichandran et J. Febin Prabhu Dass. « Computational Drug Design against Ebola Virus Targeting Viral Matrix Protein VP30 ». Borneo Journal of Pharmacy 2, n^o 2 (14 novembre 2019) : 71–81. http://dx.doi.org/10.33084/bjop.v2i2.836.

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Ebola viral disease (EVD) is a deadly infectious hemorrhagic viral fever caused by the Ebola virus with a high mortality rate. Until date, there is no effective drug or vaccination available to combat this condition. This study focuses on designing an effective antiviral drug for Ebola viral disease targeting viral protein 30 (VP30) of Ebola virus, highly required for transcription initiation. The lead molecules were screened for Lipinski rule of five, ADMET study following which molecular docking and bioactivity prediction was carried out. The compounds with the least binding energy were analyzed using interaction software. The results revealed that 6-Hydroxyluteolin and (-)-Arctigenin represent active lead compounds that inhibit the activity of VP30 protein and exhibits efficient pharmacokinetics. Both these compounds are plant-derived flavonoids and possess no known adverse effects on human health. In addition, they bind strongly to the predicted binding site centered on Lys180, suggesting that these two lead molecules can be imperative in designing a potential drug for EVD.

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Oztaskin, Necla, Suleyman Goksu, Yeliz Demir, Ahmet Maras et İlhami Gulcin. « Synthesis of Novel Bromophenol with Diaryl Methanes—Determination of Their Inhibition Effects on Carbonic Anhydrase and Acetylcholinesterase ». Molecules 27, n^o 21 (1 novembre 2022) : 7426. http://dx.doi.org/10.3390/molecules27217426.

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In this work, nine new bromophenol derivatives were designed and synthesized. The alkylation reactions of (2-bromo-4,5-dimethoxyphenyl)methanol (7) with substituted benzenes 8–12 produced new diaryl methanes 13–17. Targeted bromophenol derivatives 18–21 were synthesized via the O-Me demethylation of diaryl methanes with BBr3. Moreover, the synthesized bromophenol compounds were tested with some metabolic enzymes such as acetylcholinesterase (AChE), carbonic anhydrase I (CA I), and II (CA II) isoenzymes. The novel synthesized bromophenol compounds showed Ki values that ranged from 2.53 ± 0.25 to 25.67 ± 4.58 nM against hCA I, from 1.63 ± 0.11 to 15.05 ± 1.07 nM against hCA II, and from 6.54 ± 1.03 to 24.86 ± 5.30 nM against AChE. The studied compounds in this work exhibited effective hCA isoenzyme and AChE enzyme inhibition effects. The results show that they can be used for the treatment of glaucoma, epilepsy, Parkinson’s as well as Alzheimer’s disease (AD) after some imperative pharmacological studies that would reveal their drug potential.

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Carvalho, Sarah Fiorelli de, Ana Paula Antunes Correa, Letícia Vanni Ferreira, Marcia Vizzotto et Luis Eduardo Corrêa Antunes. « Production, chemical components, and content of bioactive compounds of strawberry cultivars ». Revista Engenharia na Agricultura - Reveng 29 (21 octobre 2021) : 275–85. http://dx.doi.org/10.13083/reveng.v29i1.10883.

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There are only a few strawberry cultivars available in Brazil and all are imported from North America and Europe. Thus, the introduction of new materials and their evaluation under Brazilian environmental conditions is imperative. The objective of this study was to evaluate the production, chemical components, and concentration of bioactive compounds in strawberry cultivars under edaphoclimatic conditions in the municipality of Pelotas-RS. The experiment was conducted in the field with low tunnels in 2011 and 2012. The experiment in the field was arranged in a completely randomized design, with eight treatments (cultivars), four replications. Each plot consisted of nine plants. The experiment in laboratory was arranged in a completely randomized 8x3 factorial design (8 cultivars and 3 months of harvest) and 4 replications. The variables analyzed were fruit number and fruit mass per plant, production, yield, soluble solid content, titratable acidity, ascorbic acid, anthocyanins, phenolic compounds, and antioxidant activity. Cultivar and harvest month influenced acidity, and the contents of soluble solids, ascorbic acid, and bioactive compounds. Cultivar Camarosa showed higher production, and higher contents of anthocyanin, phenolic compounds, and soluble solids. Cultivars ‘Palomar and ‘Aromas’ stand out for the content of ascorbic acid.

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Broda, Magdalena. « Natural Compounds for Wood Protection against Fungi—A Review ». Molecules 25, n^o 15 (2 août 2020) : 3538. http://dx.doi.org/10.3390/molecules25153538.

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Wood is a renewable, versatile material with multiple applications and the largest terrestrial pool of sequestered carbon. However, it is susceptible to degradation, mainly caused by wood-decaying fungi. Since several traditional wood preservatives have been banned owing to their detrimental effects on humans and the environment, extending the lifespan of wood products using new generation natural preservatives is an imperative from the perspectives of human health and environmental protection. Several natural compounds of plant and animal origin have been tested for their fungicidal properties, including essential oils, tannins, wood extractives, alkaloids, propolis or chitosan; and their enormous potential in wood protection has been shown. Although they are not free of limitations, the potential methods to overcome their drawbacks and enhance their bioactivity already exist, such as co-impregnation with different polymers, cross-linkers, metal chelators or antioxidants. The presence of the discrepancies between laboratory tests and the field performance, as well as legislation-related problems resulting from the lack of standards defining the quality and performance of natural protective formulations, however, create an urgent need for further thorough research and arrangements. The collaboration with other industries interested in the utilisation of natural active compounds will reduce the associated costs, thus, will facilitate the successful implementation of alternative antifungal agents.

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Weber, Christian. « Obstacles and options in the quest for drug candidates against vascular disease ». Thrombosis and Haemostasis 104, n^o 07 (2010) : 1–3. http://dx.doi.org/10.1160/th10-04-0256.

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Summaryhe difficulties in cardiovascular drug development have been exposed by recent clinical trials, which have uncovered various limitations of promising drug candidates. Yet, the imperative to improve medical treatment of atherosclerosis in aging populations afflicted by metabolic disease remains unbroken. Herein alternatives to metabolically active compounds such as glitazones and torcetrapib are introduced and discussed, namely CC chemokine receptor 5 (CCR5) antagonists recently approved for treatment of patients with human immunodeficiency virus-1, interceptors of proatherogenic chemokine interactions, and actively protective pathways. A combination of different strategies may yield improved safety profiles of these therapeutics.

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Martirosyan, Danik, et Alondra Alvarado. « Functional Foods Regulation System : Proposed Regulatory Paradigm by Functional Food Center ». Functional Food Science 3, n^o 11 (30 novembre 2023) : 275. http://dx.doi.org/10.31989/ffs.v3i11.1265.

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In response to the rising demand for functional foods driven by health-conscious consumers, a robust regulatory framework is imperative. The absence of specific guidelines creates uncertainties for both manufacturers and consumers. In response to the rising demand for functional foods driven by health-conscious consumers, a robust regulatory framework is imperative. The absence of specific guidelines creates uncertainties for both manufacturers and consumers. This article discusses the Functional Food Center's pioneering 17-step approval processfor functional foods, emphasizing scientific validation and transparent communication. However, challenges persist within the FDA approval system, including a protracted timeline and the lack of a dedicated category for functional foods. Drawing inspiration from the efficient kosher labeling system, the Functional Food Center could serve as a certification agency. Certified functional foods could display a designated symbol, ensuring credibility and trustworthiness. This approach streamlines the approval process, fostering innovation, ensuring consumer safety, and meeting the evolving health needs of consumers in a transparent, credible, and regulated functional food market.Keywords:Functional Food Classification, Functional Food Regulation, Functional Food Products, Bioactive Compounds, Functional Food Safety, Kosher Labeling Model, Regulatory Paradigm.

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Sayed, Mostafa, Ahmed M. Sayed, Ahmed A. El-Rashedy, Abdelreheem Abdelfatah Saddik, Azhaar T. Alsaggaf, Adel M. Kamal El-Dean, Reda Hassanien et Mostafa Ahmed. « Anti-inflammatory Activity and Computational Biology Study of Indole/Pyrimidine Hybrids ». Current Organic Chemistry 28, n^o 1 (janvier 2024) : 56–64. http://dx.doi.org/10.2174/0113852728289430231227042754.

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Abstract: This research paper embarks on an interdisciplinary exploration encompassing synthetic chemistry, pharmacology, and computational biology. The development of novel anti-inflammatory agents is an imperative endeavor within pharmaceutical research. Pyrimidines and thienopyrimidines are class of heterocyclic compounds that have gained prominence for their diverse pharmacological properties, including potential anti-inflammatory effects. When augmented with an indole moiety, these compounds exhibit structural diversity that can profoundly influence their biological activities. The integration of computational biology specifically molecular docking, plays a crucial role in predicting and understanding the binding interactions between these compounds and select protein targets associated with inflammatory pathways. This computational approach expedites the screening of potential drug candidates and elucidates the molecular underpinnings of their anti-inflammatory actions. Pyrimidine and thienopyrimidines tethering indole scaffold were obtained according to our reported methods. Subsequently, in vivo evaluation of anti-inflammatory is indispensable to gauge the anti-inflammatory potential of these compounds and establish structure-activity relationships. The experimental and computational biology studies of the target indole-pyrimidines hybrids revealed that these compounds can serve as anti-inflammatory agents. This paper can potentially open new avenues for therapeutic strategies against inflammation-associated disorders. The synergy of synthetic innovation, pharmacological evaluation, and computational insights offers a holistic approach to advance our understanding of pyrimidines with an indole moiety as potential agents for mitigating inflammation.

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Dinić, Jelena, Ana Podolski-Renić, Marko Jeremić et Milica Pešić. « Potential of Natural-Based Anticancer Compounds for P-Glycoprotein Inhibition ». Current Pharmaceutical Design 24, n^o 36 (15 février 2019) : 4334–54. http://dx.doi.org/10.2174/1381612825666190112164211.

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Medicinal value of natural products comes from symbiotic and competitive evolution in Earth’s complex biosphere. Billions of years of co-evolutionary interactions among millions of species have produced a large repertoire of defense molecules effective in fighting bacteria, viral, and fungal pathogens. Each species contains millions of different and useful molecules and new research technologies enabled the screening of molecules and complex mixtures from diverse biological sources. Traditional use of plants and other species led to the discovery of many bioactive compounds with various properties. In the last four decades, a large number of them were evaluated for their potential to treat cancer. Penetration of drugs into the cancer cell is necessary for their lethal pharmacological effect through interaction with intracellular target molecules. Increased activity of membrane efflux pumps reduces the intracellular drug accumulation, thereby preventing drug-target interactions. The discovery of the efflux transporter P-glycoprotein (P-gp) in multidrug resistant (MDR) cancer cells prompted the efforts in overcoming drug resistance by P-gp inhibition. The search for nontoxic anticancer agents from natural sources able to overcome MDR has been imperative in the field of drug design and discovery. Herein, we review various natural compounds from diverse sources emphasizing their potential to inhibit P-gp activity and/or expression.

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Subburaj, Saranyadevi. « Role of Natural compounds to target Lung Cancer Stem Cells ». Research Journal of Chemistry and Environment 26, n^o 5 (25 avril 2022) : 202–21. http://dx.doi.org/10.25303/2605rjce202221.

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The innovative information about the molecular study has generated a prototype change in the insight of lung cancer, enlightening the more accurate mark for anticancerous drug design. Lung cancer is an imperative origin of tumor death all over the world and it accounts for ~ 1 in 5 of total tumor-related mortalities. Nonsmall cell lung cancer (NSCLC) is one of the deadliest diseases among cancer types. We mainly focused on the role of natural compounds in targeting NSCLC promising favorable results in tumor dissemination. Numerous studies have shown that drug resistance and relapse in tumor lead to the failure of conventional therapy. The utmost crucial reasons for demise in a tumor comprise the therapy letdown and also a disseminating of tumor cells to reserved positions in which the CSC inside the cancer is recognized as a crucial driver. A cancer stem cell is an erratic distinct inhabitant of tumor cells unveiling significant carcinogenic characteristics composed of self-regeneration and discrepancy ability. Moreover, new beneficial methods targeting these cancer stem cells are deliberated to enhance long-term proven outcomes. Herein, we outlined the cancer stem cells in lung cancer, existing CSC markers and favorable molecules targeting the SC signals in lung growth that might profit the growth of innovative NSCLC therapy.

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Pancu, Daniel Florin, Alexandra Scurtu, Ioana Gabriela Macasoi, Daniela Marti, Marius Mioc, Codruta Soica, Dorina Coricovac, Delia Horhat, Marioara Poenaru et Cristina Dehelean. « Antibiotics : Conventional Therapy and Natural Compounds with Antibacterial Activity—A Pharmaco-Toxicological Screening ». Antibiotics 10, n^o 4 (7 avril 2021) : 401. http://dx.doi.org/10.3390/antibiotics10040401.

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Antibiotics are considered as a cornerstone of modern medicine and their discovery offers the resolution to the infectious diseases problem. However, the excessive use of antibiotics worldwide has generated a critical public health issue and the bacterial resistance correlated with antibiotics inefficiency is still unsolved. Finding novel therapeutic approaches to overcome bacterial resistance is imperative, and natural compounds with antibacterial effects could be considered a promising option. The role played by antibiotics in tumorigenesis and their interrelation with the microbiota are still debatable and are far from being elucidated. Thus, the present manuscript offers a global perspective on antibiotics in terms of evolution from a historical perspective with an emphasis on the main classes of antibiotics and their adverse effects. It also highlights the connection between antibiotics and microbiota, focusing on the dual role played by antibiotics in tumorigenesis. In addition, using the natural compounds with antibacterial properties as potential alternatives for the classical antibiotic therapy is discussed.

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Frye, Stephen V. « Drug discovery in academic institutions ». Hematology 2013, n^o 1 (6 décembre 2013) : 300–305. http://dx.doi.org/10.1182/asheducation-2013.1.300.

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Abstract Although academic science has always provided a fundamental understanding of the biological and clinical basis of disease, the opportunity and imperative for academics to contribute more directly to the discovery of new medicines continues to grow. Embedding medicinal chemists with cancer biologists creates collaborative opportunities for drug discovery and the design and synthesis of chemical biology tool compounds (chemical probes) to better elucidate the role of specific proteins and pathways in biology and disease. Two case studies are presented here: (1) the discovery of inhibitors of mer kinase to treat acute lymphoblastic leukemia in children and (2) the discovery of chemical probes targeting epigenetic regulators. These case studies provide lessons in target selection strategies, the requirement for iterative optimization of lead compounds (useful drugs/probes rarely come directly from a screen), and the value of mutually dependent collaborations between medicinal chemists and cancer biologists.

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Kittner, Kai, et Birgit Awiszus. « The Process of Co-Extrusion – An Analysis ». Key Engineering Materials 491 (septembre 2011) : 81–88. http://dx.doi.org/10.4028/www.scientific.net/kem.491.81.

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This paper provides an analysis of a co-extrusion process. The compound consists of the sleeve material, aluminum, and the core material, magnesium. It is imperative to produce impeccable compounds without cracks in the interface. Therefore, a simple indicating value for damaging effects during the process is necessary. In the numerical simulation the compound quality is noticeable by the current macro mechanical criterion of axial strain difference. A statistical analysis verifies this criterion as an adequate quality criterion. By means of this criterion it is possible to define a stable process window for the co-extrusion process.

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Wang, Li, Hui Lu et Yuanying Jiang. « Natural Polyketides Act as Promising Antifungal Agents ». Biomolecules 13, n^o 11 (24 octobre 2023) : 1572. http://dx.doi.org/10.3390/biom13111572.

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Invasive fungal infections present a significant risk to human health. The current arsenal of antifungal drugs is hindered by drug resistance, limited antifungal range, inadequate safety profiles, and low oral bioavailability. Consequently, there is an urgent imperative to develop novel antifungal medications for clinical application. This comprehensive review provides a summary of the antifungal properties and mechanisms exhibited by natural polyketides, encompassing macrolide polyethers, polyether polyketides, xanthone polyketides, linear polyketides, hybrid polyketide non-ribosomal peptides, and pyridine derivatives. Investigating natural polyketide compounds and their derivatives has demonstrated their remarkable efficacy and promising clinical application as antifungal agents.

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Beteck, Richard M., Ronnett Seldon, Audrey Jordaan, Digby F. Warner, Heinrich C. Hoppe, Dustin Laming et Setshaba D. Khanye. « New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis ». Molecules 24, n^o 9 (4 mai 2019) : 1740. http://dx.doi.org/10.3390/molecules24091740.

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Co-infection of malaria and tuberculosis, although not thoroughly investigated, has been noted. With the increasing prevalence of tuberculosis in the African region, wherein malaria is endemic, it is intuitive to suggest that the probability of co-infection with these diseases is likely to increase. To avoid the issue of drug-drug interactions when managing co-infections, it is imperative to investigate new molecules with dual activities against the causal agents of these diseases. To this effect, a small library of quinolone-thiosemicarbazones was synthesised and evaluated in vitro against Plasmodium falciparum and Mycobacterium tuberculosis, the causal agents of malaria and tuberculosis, respectively. The compounds were also evaluated against HeLa cells for overt cytotoxicity. Most compounds in this series exhibited activities against both organisms, with compound 10, emerging as the hit; with an MIC90 of 2 µM against H37Rv strain of M. tuberculosis and an IC50 of 1 µM against the 3D7 strain of P. falciparum. This study highlights quinolone-thiosemicarabazones as a class of compounds that can be exploited further in search of novel, safe agents with potent activities against both the causal agents of malaria and tuberculosis.

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Cooney, Louise N., Kevin D. O’Shea, Hannah J. Winfield, Michael M. Cahill, Larry T. Pierce et Florence O. McCarthy. « Bisindolyl Maleimides and Indolylmaleimide Derivatives—A Review of Their Synthesis and Bioactivity ». Pharmaceuticals 16, n^o 9 (22 août 2023) : 1191. http://dx.doi.org/10.3390/ph16091191.

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The evolution of bisindolyl maleimides and indolyl maleimide derivatives and their unique biological activities have stimulated great interest in medicinal chemistry programs. Bisindolylmaleimide (BIM)-type compounds arise from natural sources such as arcyriarubin and are biosynthetically related to indolocarbazoles. BIMs are commonly the immediate synthetic precursors of indolocarbazoles, lacking a central bond between the two aromatic units and making them more flexible and drug-like. Synthetic endeavours within this class of compounds are broad and have led to the development of both remarkably potent and selective protein kinase inhibitors. Clinical BIM examples include ruboxistaurin and enzastaurin, which are highly active inhibitors of protein kinase C-β. While BIMs are widely recognised as protein kinase inhibitors, other modes of activity have been reported, including the inhibition of calcium signalling and antimicrobial activity. Critically, structural differences can be used to exploit new bioactivity and therefore it is imperative to discover new chemical entities to address new targets. BIMs can be highly functionalised or chemically manipulated, which provides the opportunity to generate new derivatives with unique biological profiles. This review will collate new synthetic approaches to BIM-type compounds and their associated bioactivities with a focus on clinical applications.

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Sun, Shuang-Shuang, Shi-Wei Ma, Jun Li, Qin Zhang et Guang-Zhou Zhou. « Review on the Antiviral Organic Agents against Fish Rhabdoviruses ». Fishes 8, n^o 1 (16 janvier 2023) : 57. http://dx.doi.org/10.3390/fishes8010057.

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Fish rhabdoviruses are harmful single-stranded RNA viruses with high mortality rates which cause considerable economic losses in aquaculture. It is imperative to explore and develop new antiviral compounds against them. In recent years, in addition to inorganic antiviral substances, more than 50 different organic compounds have been confirmed to be effective in the prevention and treatment of rhabdovirus infection and its dissemination in fish. The main types of extracts or agents and their trial designs are here considered for review. This review reveals the reported antiviral activities of extracts from organisms, proteins, lipids, polysaccharides, nucleic acids, coumarin derivatives, arctigenin derivatives, and other antiviral organic molecules against fish rhabdoviruses, respectively. Additionally, their antiviral mechanisms of action include direct virucidal effects, inhibiting virus-induced host cell apoptosis, the blocking of the viral replication cycle, affecting gene expression and innate antiviral immune responses, and so on. This review also gives perspectives on how to comprehensively explore the potential applications of the candidate molecules, which lay the foundation for the future development of new compounds or strategies for the prevention and control of fish rhabdoviruses in aquaculture.

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Inclán, Mario, Neus Torres Hernández, Alejandro Martínez Serra, Gonzalo Torrijos Jabón, Salvador Blasco, Cecilia Andreu, Marcel lí del Olmo, Beatriz Jávega, José-Enrique O’Connor et Enrique García-España. « Antimicrobial Properties of New Polyamines Conjugated with Oxygen-Containing Aromatic Functional Groups ». Molecules 28, n^o 22 (20 novembre 2023) : 7678. http://dx.doi.org/10.3390/molecules28227678.

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Antibiotic resistance is now a first-order health problem, which makes the development of new families of antimicrobials imperative. These compounds should ideally be inexpensive, readily available, highly active, and non-toxic. Here, we present the results of our investigation regarding the antimicrobial activity of a series of natural and synthetic polyamines with different architectures (linear, tripodal, and macrocyclic) and their derivatives with the oxygen-containing aromatic functional groups 1,3-benzodioxol, ortho/para phenol, or 2,3-dihydrobenzofuran. The new compounds were prepared through an inexpensive process, and their activity was tested against selected strains of yeast, as well as Gram-positive and Gram-negative bacteria. In all cases, the conjugated derivatives showed antimicrobial activity higher than the unsubstituted polyamines. Several factors, such as the overall charge at physiological pH, lipophilicity, and the topology of the polyamine scaffold were relevant to their activity. The nature of the lipophilic moiety was also a determinant of human cell toxicity. The lead compounds were found to be bactericidal and fungistatic, and they were synergic with the commercial antifungals fluconazole, cycloheximide, and amphotericin B against the yeast strains tested.

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Gawor, Andrzej, Anna Ruszczynska, Marian Czauderna et Ewa Bulska. « Determination of Selenium Species in Muscle, Heart, and Liver Tissues of Lambs Using Mass Spectrometry Methods ». Animals 10, n^o 5 (7 mai 2020) : 808. http://dx.doi.org/10.3390/ani10050808.

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Identification and quantification of the selenium species in biological tissues is imperative, considering the need to properly understand its metabolism and its importance in various field of sciences, especially nutrition science. Although a number of studies deals with the speciation of selenium, speciation analysis is still far from being a routine task, and so far strongly depends on the type of the samples. We present a study aimed to examine speciation analysis of Se in tissues of livers, muscles, and hearts obtained from lambs, namely in liver, muscle, and heart. The studied lambs were fed with the diet enriched with an inorganic (as sodium selenate) and organic chemical form of Se (as Se-enriched yeast) compounds with simultaneous addition of fish oil (FO) and carnosic acid (CA). The first part of the work was focused on the optimization of the extraction procedure of selenium compounds from tissues. Next, hyphenated high performance liquid chromatography and inductively coupled plasma mass spectrometry (HPLC–ICP–MS) was used for the identification of five seleno-compounds—Se-methionine (SeMet), Se-cystine (SeCys2), Se-methyl-Se-cysteine (SeMetSeCys), and Se(IV) and Se(VI). Verification of the identified seleno-compounds was achieved using triple-quadrupole mass spectrometer coupled to high performance liquid chromatography (HPLC–ESI–MS/MS). The applied procedure allowed for quantitative analysis of SeMet, SeCys2, and SeMetSeCys, in biological tissues. The developed analytical protocol is feasible for speciation analysis of small molecular seleno-compounds in animals samples.

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Gonçalves, A. Pedro, Kevin McCluskey, N. Louise Glass et Arnaldo Videira. « The Fungal Cell Death Regulator czt-1 Is Allelic to acr-3 ». Journal of Fungi 5, n^o 4 (6 décembre 2019) : 114. http://dx.doi.org/10.3390/jof5040114.

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Fungal infections have far-reaching implications that range from severe human disease to a panoply of disruptive agricultural and ecological effects, making it imperative to identify and understand the molecular pathways governing the response to antifungal compounds. In this context, CZT-1 (cell death-activated zinc cluster transcription factor) functions as a master regulator of cell death and drug susceptibility in Neurospora crassa. Here we provide evidence indicating that czt-1 is allelic to acr-3, a previously described locus that we now found to harbor a point mutation in its coding sequence. This nonsynonymous amino acid substitution in a low complexity region of CZT-1/ACR-3 caused a robust gain-of-function that led to reduced sensitivity to acriflavine and staurosporine, and increased expression of the drug efflux pump abc-3. Thus, accumulating evidence shows that CZT-1 is an important broad regulator of the cellular response to various antifungal compounds that appear to share common molecular targets.

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Kuvad, Ranjan P., Kiran S. Chudasama, Vibhuti M. Jhala et Vrinda S. Thaker. « Standardization of leaf age for radical scavenging activity in Terminalia arjuna ». Journal of Applied and Natural Science 6, n^o 1 (1 juin 2014) : 76–80. http://dx.doi.org/10.31018/jans.v6i1.378.

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Terminalia arjuna is one of the many such plant that used in indigenous system of medicine for curing different diseases. For effective formulation of herbal drug selection of proper age of the plant is imperative. In the present study, the T. arjuna plant (leaves) was collected from the Botanical garden of Saurashtra University. The leaves were grouped in to various size and growth analysis was performed. Each extract homogenized in methanol and was used for chlorophyll estimation and antioxidant activities. Radical scavenging activity of the methanol extract of different stages leaves were determined using a stable free radical 2, 2-diphenyl-1-picryl hydrazyl (DPPH), using Micro plate assay. Further the phenolic compounds were separated by Reverse phase high pressure liquid chromatography analysis (RP-HPLC). At the leaf stage when maximum antioxidant activity was observed, phenol like Gallic acid showed distinct peak. The role of phenolic compounds in antioxidant activities is discussed.

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Wei, Qiang, et Yi-han Zhang. « Flavonoids with Anti-Angiogenesis Function in Cancer ». Molecules 29, n^o 7 (31 mars 2024) : 1570. http://dx.doi.org/10.3390/molecules29071570.

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The formation of new blood vessels, known as angiogenesis, significantly impacts the development of multiple types of cancer. Consequently, researchers have focused on targeting this process to prevent and treat numerous disorders. However, most existing anti-angiogenic treatments rely on synthetic compounds and humanized monoclonal antibodies, often expensive or toxic, restricting patient access to these therapies. Hence, the pursuit of discovering new, affordable, less toxic, and efficient anti-angiogenic compounds is imperative. Numerous studies propose that natural plant-derived products exhibit these sought-after characteristics. The objective of this review is to delve into the anti-angiogenic properties exhibited by naturally derived flavonoids from plants, along with their underlying molecular mechanisms of action. Additionally, we summarize the structure, classification, and the relationship between flavonoids with their signaling pathways in plants as anti-angiogenic agents, including main HIF-1α/VEGF/VEGFR2/PI3K/AKT, Wnt/β-catenin, JNK1/STAT3, and MAPK/AP-1 pathways. Nonetheless, further research and innovative approaches are required to enhance their bioavailability for clinical application.

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Onukwuli, Chimezie O., Chisom E. I. zuchukwu et Okechukwu Paul-Chima Ugwu. « Exploring Phytochemicals for Diabetes Management : Mechanisms, Efficacy, and Future Directions ». NEWPORT INTERNATIONAL JOURNAL OF RESEARCH IN MEDICAL SCIENCES 5, n^o 2 (20 mars 2024) : 7–17. http://dx.doi.org/10.59298/nijrms/2024/5.2.0717.

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In the realm of global health diplomacy, diabetes mellitus undoubtedly poses a significant challenge. Furthermore, there is a pressing need to explore alternative and complementary therapies. Phytochemicals, which are naturally occurring bioactive compounds found in plants, exhibit distinct biochemical properties, rendering them promising candidates for diabetes management. This review focuses on the potential of various classes of phytochemicals, including polyphenols, alkaloids, terpenoids, organosulfur compounds, and polysaccharides, in diabetes management. Each class demonstrates unique mechanisms of action, contributing to therapeutic effects such as enhancing insulin sensitivity, reducing carbohydrate digestion and glucose absorption, regulating antioxidant stress, inflammation, and glucose metabolism. While successful preclinical trials provide valuable insights, further rigorous clinical trials are imperative to ascertain the therapeutic efficacy, optimal dosage, bioavailability, and potential interactions with concomitant medications. Understanding the functional pathways of plant-derived substances is crucial, as it enables the formulation of precise strategies for incorporating them as dietary supplements for individuals with diabetes mellitus. Keywords: Phytochemicals, diabetes mellitus, insulin sensitivity, glucose metabolism, oxidative stress, and inflammation.

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Ullah, Tariq Saiff, Syeda S. Firdous, Ansar Mehmood, Javaid Q. Swati, Muhammad Usman et Abdul N. Khalid. « Detection of bioactive compounds and amino acids from fruiting bodies of Morchella tridentina ». Acta Scientiarum Polonorum Hortorum Cultus 21, n^o 1 (28 février 2022) : 103–14. http://dx.doi.org/10.24326/asphc.2022.1.9.

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Morels are well known due to their nutritional and food value since ancient human history. In this study, biochemical and proteomic analyses were carried out on the ascocarp of Morchella tridentina Bres. For this, several ascocarp of M. tridentina were collected from different sites of Neelum Valley Azad Jammu and Kashmir, Pakistan. Identification was confirmed by phylogenetic sequencing using nuclear ribosomal DNA bar-coding technique along with morph-anatomical analysis. During the biochemical analysis, different bioactive compounds used in drugs to treat cancer, heart diseases, edema (veprisinium, visnagin, and bumetanide), and breast cancer (petunidin) were identified. Cerulinin, daidzein, guanthidin and okanin (imperative compounds) were also detected. Furthermore, protein analysis by FTICR/MS/Orbitrap revealed the presence of 921 proteins belonging to 171 protein groups having 165 unique peptide sequences. The study shows that this morel could be used as a source of bioactive substances to develop anticancer, antifungal, and antiviral drugs in the future. This fruitful addition of M. tridentina in Mycota of Pakistan increases the number of morels to three.

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Tahir, Rana Adnan, Farwa Hassan, Abdul Kareem, Umer Iftikhar et Sheikh Arslan Sehgal. « Ligand-Based Pharmacophore Modeling and Virtual Screening to Discover Novel CYP1A1 Inhibitors ». Current Topics in Medicinal Chemistry 19, n^o 30 (3 janvier 2020) : 2782–94. http://dx.doi.org/10.2174/1568026619666191112104217.

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Background: Cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) is an imperative enzyme due to its immersion in the biotransformation of a wide range of drugs and other xenobiotics. The involvement of enzymes in drug metabolism indicates an effective drug target for the development of novel therapeutics. The discovery of CYP1A1 specific inhibitors would be of particular relevance for the clinical pharmacology. Method: In the current work, in silico approaches were utilized to identify the novel potential compounds through a diverse set of reported inhibitors against CYP1A1. A dataset of reported compounds against CYP1 belongs to 10 different classes (alkaloids, coumarins, flavonoids, natural compounds, synthetic inhibitors, drugs, MBI’s, PAHs, naphthoquinone and stilbenoids) was retrieved and utilized for the comparative molecular docking analyses followed by pharmacophore modeling. The total eleven novel compounds were scrutinized on the basis of the highest binding affinities and least binding energy values. Result: ZINC08792486 compound attained the highest gold fitness score of 90.11 against CYP1A1 among all the scrutinized molecules. Conclusion: It has been elucidated that the residues Phe-224, Gly-316 and Ala-317 were conserved in all ligand-receptor interactions and critical for the development of effective therapies. The ADMET property analyses also predict better absorption and distribution of the selected hits that may be used in the future for in vitro validations and drug development.

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Bianco, Maria da Conceição Avelino Dias, Debora Inacio Leite, Frederico Silva Castelo Branco, Nubia Boechat, Elisa Uliassi, Maria Laura Bolognesi et Monica Macedo Bastos. « The Use of Zidovudine Pharmacophore in Multi-Target-Directed Ligands for AIDS Therapy ». Molecules 27, n^o 23 (3 décembre 2022) : 8502. http://dx.doi.org/10.3390/molecules27238502.

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The concept of polypharmacology embraces multiple drugs combined in a therapeutic regimen (drug combination or cocktail), fixed dose combinations (FDCs), and a single drug that binds to different targets (multi-target drug). A polypharmacology approach is widely applied in the treatment of acquired immunodeficiency syndrome (AIDS), providing life-saving therapies for millions of people living with HIV. Despite the success in viral load suppression and patient survival of combined antiretroviral therapy (cART), the development of new drugs has become imperative, owing to the emergence of resistant strains and poor adherence to cART. 3′-azido-2′,3′-dideoxythymidine, also known as azidothymidine or zidovudine (AZT), is a widely applied starting scaffold in the search for new compounds, due to its good antiretroviral activity. Through the medicinal chemistry tool of molecular hybridization, AZT has been included in the structure of several compounds allowing for the development of multi-target-directed ligands (MTDLs) as antiretrovirals. This review aims to systematically explore and critically discuss AZT-based compounds as potential MTDLs for the treatment of AIDS. The review findings allowed us to conclude that: (i) AZT hybrids are still worth exploring, as they may provide highly active compounds targeting different steps of the HIV-1 replication cycle; (ii) AZT is a good starting point for the preparation of co-drugs with enhanced cell permeability.

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Pinto, Diana, Ana Sofia Ferreira, Julián Lozano-Castellón, Emily P. Laveriano-Santos, Rosa M. Lamuela-Raventós, Anna Vallverdú-Queralt, Cristina Delerue-Matos et Francisca Rodrigues. « Exploring the Impact of In Vitro Gastrointestinal Digestion in the Bioaccessibility of Phenolic-Rich Chestnut Shells : A Preliminary Study ». Separations 10, n^o 9 (28 août 2023) : 471. http://dx.doi.org/10.3390/separations10090471.

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Chestnut shells (CS), the principal by-product of the chestnut processing industry, contain high concentrations of flavonoids and other polyphenols with huge interest for the nutraceuticals field. Nonetheless, the bioaccessibility and bioactivity of phytochemicals can be influenced by their digestibility, making it imperative to evaluate these activities prior to application of CS as a nutraceutical ingredient. This work aims to appraise the effects of in vitro simulated gastrointestinal digestion on the bioaccessibility, bioactivity, and metabolic profiling of CS. An increase in the total phenolic and flavonoid contents, antioxidant/antiradical properties, radical scavenging capacity, and inhibition on acetylcholinesterase activity was evidenced during in vitro simulated digestion. Metabolomic profiling by LC-ESI-LTQ-Orbitrap-MS revealed changes during the simulated digestion, particularly in phenolic compounds (46% of total compounds annotated), lipids (22%), phenylpropanoids (9%), organic acids (7%), carbohydrates (5%), nucleosides (5%), amino acids (4%), and alcohols (1%). Phenolic acids (gallic acid, syringic acid, and hydroxyphenylacetic acid) and flavonoids (epicatechin) were the major polyphenolic classes identified. The heatmap-positive correlations highlighted that the bioactivity of CS is closely related to the phenolic compounds and their bioaccessibility. These findings suggest the reuse of CS as a potential nutraceutical ingredient with antioxidant and neuroprotective effects, encouraging the use of appropriate extraction and/or encapsulation techniques to enhance the bioaccessibility of phenolic compounds.

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Wei, Grace, et Danik Martirosyan. « Hair loss : A review of the role of food bioactive compounds ». Bioactive Compounds in Health and Disease 2, n^o 5 (30 mai 2019) : 94. http://dx.doi.org/10.31989/bchd.v2i5.610.

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Background: The impact that hair loss has on an individual's psychological wellness, and subsequent quality of life, is widespread and long lasting. The current standard treatments for hair loss include surgery and medications, ranging from over-the-counter treatments to corticosteroid injections and immunosuppressants. Unfortunately, these current treatments are either expensive, invasive, or have extremely negative side effects. Recently, the role of vitamins, minerals, and functional foods with their associated bioactive compounds, have gained increasing recognition as a potential means to address this issue. Some of these compounds have been shown to decrease the risk of specific forms of hair loss, particularly alopecia, a form of balding that results due from an autoimmune disorder. These include experimental studies using black raspberry extract and egg yolks as well as epidemiological studies using Mediterranean diets and various micronutrients. Other compounds have been shown to promote hair growth on a more general scale, including in vivo studies using rice bran extract and mouse models using red ginseng oil and annurca apple polyphenols. This review identifies key hair growth promoting vitamins, minerals, and functional foods, as well as summarizes the relevant mechanisms of action of these compounds that have been elucidated. Knowledge regarding the effects of these nutriceuticals on reducing hair loss is rapidly expanding. However, it is imperative that further research be done in order to delineate mechanisms of actions for all compounds related to managing and treating hair loss and subsequently integrate these dietary modifications into clinical treatment recommendations for hair loss.Keywords: Hair loss, alopecia, berry extract, mediterranean diet, rice bran, ginseng, annurca apple, thuja orientalis, marine supplement, honey, egg yolk, functional foods, bioactive compounds

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Malkar, Radhika S., et Ganapati D. Yadav. « Development of Green and Clean Processes for Perfumes and Flavors Using Heterogeneous Chemical Catalysis ». Current Catalysis 9, n^o 1 (10 septembre 2020) : 32–58. http://dx.doi.org/10.2174/2211544708666190613163523.

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Background: In this review, different heterogeneous catalysts based on acid, base, metal and enzymes are discussed for the synthesis of industrially relevant perfumes and flavor compounds. These molecules are mainly produced by a variety of reaction pathways such as esterification, isomerization, hydration, alkylation, hydrogenation, oxidation, etc. All these reactions are discussed thoroughly for the synthesis of vital aromatic compounds. The review also summarizes various recent technologies applied for designing new catalysts to obtain the maximum yield of the desired product. Overall, this review highlights the green, clean and eco-friendly processes which can be industrially accepted for the synthesis of perfumes, flavors and fragrances. Objective: The objective of the current review was to emphasize on the synthesis of industrially important perfumes and flavor molecules such as α-terpineol, cyclohexyl esters, thymol, raspberry ketone, etc. using heterogeneous catalysts. Results: Three hundred and eight papers are reported in this review, the majority of which are on heterogeneous catalysis for the synthesis of molecules which impart flavor or possess perfumery characteristics. Among all, the preparation of esters is highlighted as they represent an imperative functional group in aroma chemicals. Conclusion: The review confirms the need for heterogeneous catalysis in pollution-free and costeffective synthesis of flavor and perfumery compounds.

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Miniyar, Pankaj, Anand Mahajan, Dattatray Anuse, Ashish Kumar, Mahesh Barmade, Dhiman Sarkar, Manisha Arkile et Vijay Khedkar. « Recursive Partitioning Analysis and Anti-Tubercular Screening of 3- Aminopyrazine-2-Carbohydrazide Derivatives ». Letters in Drug Design & ; Discovery 16, n^o 11 (23 octobre 2019) : 1264–75. http://dx.doi.org/10.2174/1570180816666190329222636.

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Background: Treating tuberculosis is a challenge due to the development of drug resistance. Hence, it is imperative to develop novel leads having high potency and efficacy to curb drug resistance. Methods: The present research work is focused on microwave-assisted synthesis of novel twenty-six 3-amino-N’-benzylidenepyrazine-2-carbohydrazide derivatives (3a-z), where, lyophilization technique was used for isolation of the major intermediate, 3-aminopyrazin-2-carbohydrazide. All synthesized compounds were subjected for anti-tubercular screening against Mycobacterium tuberculosis H37Ra by using XTT Reduction Menadione Assay (XRMA) protocol. Results: Out of 26 synthesized compounds, four N’-substitutedbenzaldehyde-3-amino-pyrazine-2- carbohydrazide derivatives viz. 3i, 3j 3v and 3z showed significant activity against M. tuberculosis H37Ra. The compounds 3i, 3j, 3v and 3z showed 99, 98, 92 and 87 % inhibition respectively as compared to 94% inhibition shown by the standard drug rifampicin. The MIC and IC50 values were in the range of 24.3-110 and 5.9-20.8 µg/ml respectively. Conclusion: A classification model called Recursive Partitioning (RP) based on binary Quantitative Structure-Activity Relationship (QSAR) was derived for the establishment of structure-activity relationship (SAR). The predictions derived on the basis of RP model were found to be in agreement with anti-tubercular screening data.

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Pan, Bowen, Sumei Li, Junwei Xiao, Xin Yang, Shouxia Xie, Ying Zhou, Jian Yang et Ying Wei. « Dual Inhibition of HIV-1 and Cathepsin L Proteases by Sarcandra glabra ». Molecules 27, n^o 17 (29 août 2022) : 5552. http://dx.doi.org/10.3390/molecules27175552.

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The COVID-19 pandemic continues to impose a huge threat on human health due to rapid viral mutations. Thus, it is imperative to develop more potent antivirals with both prophylactic and treatment functions. In this study, we screened for potential antiviral compounds from Sarcandra glabra (SG) against Cathepsin L and HIV-1 proteases. A FRET assay was applied to investigate the inhibitory effects and UPLC-HRMS was employed to identify and quantify the bioactive components. Furthermore, molecular docking was carried out to get a glimpse of the binding of active compounds to the proteases. Our results showed that the SG extracts (SGW, SG30, SG60, and SG85) inhibited HIV-1 protease with an IC50 of 0.003~0.07 mg/mL and Cathepsin L protease with an IC50 of 0.11~0.26 mg/mL. Fourteen compounds were identified along with eight quantified from the SG extracts. Chlorogenic acid, which presented in high content in the extracts (12.7~15.76 µg/mg), possessed the most potent inhibitory activity against HIV-1 protease (IC50 = 0.026 mg/mL) and Cathepsin L protease (inhibition: 40.8% at 0.01 mg/mL). Thus, SG extracts and the active ingredients could potentially be used to prevent/treat viral infections, including SARS-CoV-2, due to their dual-inhibition functions against viral proteases.

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Adinortey, Cynthia A., Gabriel B. Kwarko, Russell Koranteng, Daniel Boison, Issaka Obuaba, Michael D. Wilson et Samuel K. Kwofie. « Molecular Structure-Based Screening of the Constituents of Calotropis procera Identifies Potential Inhibitors of Diabetes Mellitus Target Alpha Glucosidase ». Current Issues in Molecular Biology 44, n^o 2 (21 février 2022) : 963–87. http://dx.doi.org/10.3390/cimb44020064.

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Diabetes mellitus is a disorder characterized by higher levels of blood glucose due to impaired insulin mechanisms. Alpha glucosidase is a critical drug target implicated in the mechanisms of diabetes mellitus and its inhibition controls hyperglycemia. Since the existing standard synthetic drugs have therapeutic limitations, it is imperative to identify new potent inhibitors of natural product origin which may slow carbohydrate digestion and absorption via alpha glucosidase. Since plant extracts from Calotropis procera have been extensively used in the treatment of diabetes mellitus, the present study used molecular docking and dynamics simulation techniques to screen its constituents against the receptor alpha glucosidase. Taraxasterol, syriogenin, isorhamnetin-3-O-robinobioside and calotoxin were identified as potential novel lead compounds with plausible binding energies of −40.2, −35.1, −34.3 and −34.3 kJ/mol against alpha glucosidase, respectively. The residues Trp481, Asp518, Leu677, Leu678 and Leu680 were identified as critical for binding and the compounds were predicted as alpha glucosidase inhibitors. Structurally similar compounds with Tanimoto coefficients greater than 0.7 were reported experimentally to be inhibitors of alpha glucosidase or antidiabetic. The structures of the molecules may serve as templates for the design of novel inhibitors and warrant in vitro assaying to corroborate their antidiabetic potential.

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