Article
Biochemistry & Molecular Biology
Jeffrey Y. Jian, Kevin D. McCarty, Jo Ann W. Byl, F. Peter Guengerich, Keir C. Neuman, Neil Osheroff
Summary: Type II topoisomerases generate a covalent enzyme-cleaved DNA complex to perform double-stranded DNA passage. Cleavage complexes are targets for anticancer and antibacterial drugs. Different topoisomerases show preferences for recognizing negative or positive supercoiled DNA substrates. The ability to distinguish supercoil handedness is determined by the forward rate of cleavage and can be enhanced by drugs.
NUCLEIC ACIDS RESEARCH
(2023)
Article
Polymer Science
Daniel A. Palacio, Carla Munoz, Manuel Melendrez, Walter A. Rabanal-Leon, Juliana A. Murillo-Lopez, Manuel Palencia, Bernabe L. Rivas
Summary: This study investigates the use of two cationic polymers, poly[(4-vinylbenzyl) trimethylammonium chloride] and N-alkylated chitosan, for removing nalidixic acid from water. The removal efficiency was studied under different experimental conditions using liquid-phase polymer-based retention (LPR) and a stochastic algorithm provided by Fukui's functions. The results showed that both polymers demonstrated high removal percentages, with alkylated N-chitosan performing better at pH 7 and poly[(4-vinylbenzyl) trimethylammonium chloride] at pH 9. The interaction mechanisms involved electrostatic interactions, π-π interactions, and hydrogen bonding.
Article
Engineering, Environmental
Safa Radmehr, Mina Hosseini Sabzevari, Mehrorang Ghaedi, Mohammad Hossein Ahmadi Azqhandi, Farzaneh Marahel
Summary: This study successfully synthesized NiZrAl-LDH-GO-CS NC and demonstrated its high efficiency and adsorption capacity for the removal of nalidixic acid. Various analytical methods were used to assess the synthesis and adsorption performance of the nanocomposite, ultimately confirming that the ANFIS model performed the best in simulating NA adsorption.
JOURNAL OF ENVIRONMENTAL CHEMICAL ENGINEERING
(2021)
Article
Chemistry, Applied
Giuliana Mosconi, Yadira Salguero, Laura E. Valenti, Ricardo Rojas, Miriam C. Strumia, Cesar G. Gomez, Carla E. Giacomelli
Summary: LDH-AMD were successfully incorporated into PP-based platforms in this study, increasing the surface roughness and antimicrobial activity of the platforms. The Nal-incorporating platforms exhibited strong bactericidal effects on bacterial strains, while the Bz-loaded platform slightly delayed bacterial growth.
REACTIVE & FUNCTIONAL POLYMERS
(2022)
Article
Chemistry, Applied
Giuliana Mosconi, Yadira Salguero, Laura E. Valenti, Ricardo Rojas, Miriam C. Strumia, Cesar G. Gomez, Carla E. Giacomelli
Summary: In this study, polypropylene-based platforms with antimicrobial activity were successfully obtained by incorporating layered double hydroxides nanoparticles and antimicrobial drugs into polyacrylate-photografted polypropylene films. These platforms exhibited high surface antimicrobial concentration and significant antimicrobial activity.
REACTIVE & FUNCTIONAL POLYMERS
(2022)
Article
Multidisciplinary Sciences
Tian Liu, Lingxiao Li, Shuo Wang, Fudan Dong, Shiyi Zuo, Jiaxuan Song, Xin Wang, Qi Lu, Helin Wang, Haotian Zhang, Maosheng Cheng, Xiaohong Liu, Zhonggui He, Bingjun Sun, Jin Sun
Summary: In this study, the authors introduced a hybrid chalcogen bond linker into a docetaxel dimeric prodrug nanoassembly and demonstrated its improved selfassembly, redox-responsivity and antitumor efficacy. The hybrid chalcogen bonds, especially the sulfur-tellurium-sulfur bond, exhibited ultrahigh dual-responsivity to both oxidation and reduction conditions, effectively addressing the heterogeneous tumor microenvironment and promoting the self-assembly of homodimeric prodrugs.
NATURE COMMUNICATIONS
(2022)
Article
Chemistry, Physical
Marzena Matejczyk, Piotr Ofman, Jozefa Wiater, Renata Swislocka, Pawel Kondzior, Wlodzimierz Lewandowski
Summary: In this study, the toxicity and oxidative stress generation of the antidepressant fluoxetine (FLU), its metabolite nor-fluoxetine (Nor-FLU), the antibiotic nalidixic acid (NA), caffeic acid (CA), and their mixtures were investigated in three different environments: microbial medium (MM), raw wastewaters (RW), and treated wastewaters (TW). The results showed that FLU, Nor-FLU, NA, CA, and their mixtures are toxic and can induce oxidative stress in E. coli strains. The presence of wastewater affected the toxic activity and oxidative stress synthesis of these chemicals and their mixtures. The strongest toxic activity and oxidative stress generation were observed with NA at a concentration of 1 mg/dm(3) and the mixture of FLU (1 mg/dm(3)), Nor-FLU (0.1 mg/dm(3)), and NA (0.1 mg/dm(3)).
Article
Spectroscopy
Malgorzata Kosinska-Pezda, Urszula Maciolek, Lidia Zapala
Summary: Three new solid lanthanide complexes with nalidixic acid were synthesized using a green synthesis method. The complexes were fully characterized and their luminescent properties were investigated. It was concluded that the nalidixate ligands bind to the lanthanide ions through bidentate carboxylate and carbonyl groups, while water molecules are part of the outer coordination sphere. The complexes exhibited characteristic emission of the lanthanide ions upon excitation, depending on the excitation wavelength and/or solvent.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2023)
Article
Chemistry, Analytical
Panpan Xu, Tingting Xu, Mingguang Ma, Xia Qiu, Yue Wang, Yinggui Zhu
Summary: This study presents a method for establishing a highly sensitive and selective NA/S2O8- electrochemiluminescence system using INH as a co-reaction accelerator, and demonstrates that co-reaction accelerators can provide a simple, efficient, and low-cost method for signal amplification. The results show that INH efficiently interacts with S2O8- to promote the production of more oxidant SO4 center dot-, leading to ECL enhancement for the NA/S2O8- system. Under optimal conditions, highly sensitive and selective electrochemiluminescence detection of TEPA was achieved.
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
(2022)
Article
Environmental Sciences
Ji-Hyun Park, Jihyun Kang, Kyung-Seon Bae, Hanbyul Lee, Jihye Kim, Eung-Roh Park, Jeong-Ki Yoon, Soo-Hyung Lee
Summary: The increasing global incidence of quinolone antimicrobial resistance poses a considerable public health concern. The aquatic environment, particularly wastewater treatment plants (WWTPs), serves as a major reservoir for antibiotic-resistant bacteria (ARB) and antibiotic resistance genes (ARGs).
Phenotypic and genotypic analyses of antibiotic resistance demonstrated that quinolone resistance primarily originated from chromosomal mutations in the gyrA, parC, and parE genes, known as quinolone resistance-determining regions (QRDRs). The plasmid-mediated quinolone resistance (PMQR) genes qnrS and qnrB were identified in a portion of the isolates.
Article
Spectroscopy
Jessica Renee Knight, Yingying Wang, Shi Xu, Wei Chen, Clifford E. Berkman, Ming Xian
Summary: A unique reaction between thiols and alkyl sulfonylbenzothiazole was discovered, leading to the development of thiol-triggered fluorescent sensors and prodrugs with tunable release profiles of payloads.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2021)
Article
Biochemistry & Molecular Biology
Yu Imai, Glenn Hauk, Jeffrey Quigley, Libang Liang, Sangkeun Son, Meghan Ghiglieri, Michael F. Gates, Madeleine Morrissette, Negar Shahsavari, Samantha Niles, Donna Baldisseri, Chandrashekhar Honrao, Xiaoyu Ma, Jason J. Guo, James M. Berger, Kim Lewis
Summary: The antimicrobial resistance crisis necessitates the development of new antibiotics. In this study, a novel antimicrobial compound called evybactin was discovered from Photorhabdus noenieputensis, which exhibited potent and selective antibacterial activity against Mycobacterium tuberculosis. Evybactin was found to target DNA gyrase and utilized a promiscuous transporter, BacA, to enter the bacterial cell.
NATURE CHEMICAL BIOLOGY
(2022)
Article
Materials Science, Multidisciplinary
Dongshi Liang, Meiqian Yu, Shuaishuai Huang, Jinglin Wang, Zijin Xu, Daai Li, Zhongyu Li, Huamin Wang
Summary: This study developed a new approach to address the limitations of magnolol as an anti-tumor agent, by creating an acid-responsive polymeric prodrug that can self-assemble into polymeric micelles. In vitro and in vivo studies showed that these micelles released magnolol selectively at an acidic pH, demonstrated superior inhibition of tumor growth, and had increased accumulation in tumor tissues. Pharmacokinetic analysis also showed a longer half-life and extended duration of action for these prodrugs. These findings indicate the potential of this synthesized prodrug as a promising therapeutic option for gastric cancer.
MATERIALS & DESIGN
(2023)
Article
Chemistry, Medicinal
Huajian Zhu, Lixue Lu, Wenjian Zhu, Yuchen Tan, Yiping Duan, Jie Liu, Wencai Ye, Zheying Zhu, Jinyi Xu, Shengtao Xu
Summary: A series of NQO1 selectively activated prodrugs were designed and synthesized, and among them, compound 32j exhibited strong antitumor activity by inducing cell apoptosis through interfering with apoptosis-related protein expression.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Afif F. Bandak, Tim R. Blower, Karin C. Nitiss, Viraj Shah, John L. Nitiss, James M. Berger
Summary: The ATPase domains of the enzyme are not required for DNA strand passage, but their loss elevates the enzyme's propensity for DNA damage. The unstructured C-terminal domains and cleavage-prone mutations enhance strand passage activity and sensitivity to the chemotherapeutic agent etoposide. In ATPase-less enzymes, the presence of CTD or mutations promote even greater levels of DNA cleavage.
NUCLEIC ACIDS RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Jimmy Gouyau, Raphael E. Duval, Ariane Boudier, Emmanuel Lamouroux
Summary: Gold nanoparticles exhibit weak antibacterial activity, while silver nanoparticles show high antibacterial activity against Escherichia coli but not against Staphylococcus aureus.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Fatima Zahra Marhoume, Rachida Aboufatima, Younes Zaid, Youness Limami, Raphael E. Duval, Jawad Laadraoui, Anass Belbachir, Abderrahmane Chait, Abdallah Bagri
Summary: The plant extract Rubia tinctorum has been found to prevent the formation of kidney stones in experimental studies, demonstrating antioxidant effects and polyphenol composition that inhibit the deposition of calcium oxalate in urine. Co-administration of Rubia tinctorum extracts prevents changes in serum and urinary biochemical markers and protects kidney tissue damage associated with urolithiasis. The ethanolic extract of Rubia tinctorum shows superior preventive effects compared to the ethyl acetate extract, attributed to its stronger antioxidant effect due to a higher content of polyphenols.
Article
Plant Sciences
Amal Ghorbel, Jawhar Fakhfakh, Vincent Brieudes, Maria Halabalaki, Stephane Fontanay, Raphael E. Duval, Khaled Mliki, Sami Sayadi, Noureddine Allouche
Summary: The essential oil and aqueous extract from Thymus algeriensis Boiss. & Reut exhibit different levels of antioxidant and antibacterial activities, with the former being more effective in antibacterial screening and the latter showing the strongest antioxidant activity. Phenolic compounds are the main components in the aqueous extract.
JOURNAL OF ESSENTIAL OIL BEARING PLANTS
(2021)
Article
Microbiology
Nour Mammari, Emmanuel Lamouroux, Ariane Boudier, Raphael E. Duval
Summary: The emergence of multidrug-resistant bacteria is a major public health issue. Nanotechnologies, particularly metal-based nanoparticles (NPs), offer potential solutions for the development of effective antimicrobial agents. Inducing oxidative stress through NPs represents a valuable and powerful strategy to combat multidrug-resistant bacteria.
Meeting Abstract
Infectious Diseases
M. Pagonendji, G. Ionela, E. Charpentier, A. Sausy, A. Lefaou, R. Duval, J. Hubschen
INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES
(2022)
Article
Biochemistry & Molecular Biology
Bianca Johansen, Raphael E. Duval, Jean-Christophe Sergere
Summary: This study investigates the potential antibacterial synergy between a combination of terpinen-4-ol and alpha-terpineol and standard tea tree oil, and suggests that it could be a valuable weapon against ESKAPE pathogens.
Article
Biochemistry & Molecular Biology
Marwa Roumani, Armelle Ropars, Christophe Robin, Raphael E. Duval, Jean-Pol Frippiat, Michel Boisbrun, Romain Larbat
Summary: Resistance to conventional treatments calls for the discovery of new therapeutic molecules. Plant specialized metabolites like phenolamides in tomato plants have potential antioxidant, antimicrobial, and anti-inflammatory properties. This study investigated whether three major phenolamides found in Tuta absoluta-infested tomato leaves have antimicrobial, cytotoxic, and/or anti-inflammatory properties. The results showed that these phenolamides exhibited varying degrees of antibacterial activity and were able to counteract the pro-inflammatory effect on cells. Extracts from healthy tomato leaves could also reduce inflammation. These findings suggest that phenolamides from tomato leaves could serve as alternatives to conventional drugs.
Article
Infectious Diseases
Nassifatou Koko Tittikpina, Gilbert Kirsch, Raphael Emmanuel Duval, Patrick Chaimbault, Claus Jacob
Summary: This study found that Daniellia oliveri has valuable antibacterial activities and can effectively treat intertrigo and candidiasis. The main compounds of this plant include terpenes, phytosterols, phenolic compounds, and fatty acids.
Review
Pharmacology & Pharmacy
Hicham Wahnou, Ibtissam Youlyouz-Marfak, Bertrand Liagre, Vincent Sol, Mounia Oudghiri, Raphael Emmanuel Duval, Youness Limami
Summary: Prostate cancer is a major concern worldwide, and current treatments have limitations and side effects. Photodynamic therapy (PDT) is a promising alternative that uses light-activated photosensitizers to induce tumor cell death. There are synthetic and natural photosensitizers, and combining PDT with other therapies is being explored. This review provides an overview of conventional treatments, principles of PDT, different types of photosensitizers, and ongoing research on combination therapy for prostate cancer. PDT has the potential to be a more effective and less invasive treatment option, and research aims to improve its selectivity and efficacy.
Review
Biochemistry & Molecular Biology
Maxime Mourer, Jean-Bernard Regnouf-de-Vains, Raphael E. Duval
Summary: Since the discovery of polyphenolic resins 150 years ago, research on calix[n]arenes has advanced, leading to their wide range of applications in the field of therapeutics. Specifically, calix[4]arenes offer multiple possibilities for precise structure tuning and are being used for the development of new antibacterial active ingredients.
Review
Oncology
Hicham Wahnou, Bertrand Liagre, Vincent Sol, Hicham El Attar, Rukset Attar, Mounia Oudghiri, Raphael Emmanuel Duval, Youness Limami
Summary: Conventional therapies for colorectal cancer have side effects, but natural compounds like polyphenols are being explored as potential therapeutic agents. However, there are challenges for their use, so researchers are developing novel approaches using nanoparticles as a drug delivery system. This review discusses recent advances in the use of polyphenols-based nanoparticles for the treatment of colorectal cancer.
Review
Microbiology
Nour Mammari, Raphael E. Duval
Summary: The increased spread and persistence of bacterial drug-resistant phenotypes is a concern, but nanotechnology shows promise in combating antibiotic-resistant bacterial infections by improving therapeutic efficacy and reducing side effects. Various nanomaterials, such as metal-based nanoparticles, have intrinsic antibacterial properties and can be used for photothermal therapy and photodynamic therapy to kill bacteria and reduce drug resistance.
Review
Infectious Diseases
Ariane Boudier, Nour Mammari, Emmanuel Lamouroux, Raphael E. Duval
Summary: Amphotericin B is an antifungal molecule widely used in clinical practice, with both prooxidant and antioxidant properties. Inorganic nanoparticles, sharing similar properties, can act as carriers of Amphotericin B to enhance its antimicrobial activity.
Review
Oncology
Salma Benayad, Hicham Wahnou, Riad El Kebbaj, Bertrand Liagre, Vincent Sol, Mounia Oudghiri, El Madani Saad, Raphael Emmanuel Duval, Youness Limami
Summary: With its potential to inhibit cancer development, piperine, a natural compound, shows promise in cancer prevention and treatment.
Review
Biochemistry & Molecular Biology
Youness Limami, Aline Pinon, Hicham Wahnou, Mounia Oudghiri, Bertrand Liagre, Alain Simon, Raphael Emmanuel Duval
Summary: Ursolic acid (UA) has emerged as a promising candidate for multitargeted cancer therapy due to its ability to inhibit cell proliferation, induce apoptosis, suppress angiogenesis, inhibit metastasis, and modulate the tumor microenvironment. It shows promising activity against various cancer types and targets key signaling pathways involved in cancer development and progression. However, its low bioavailability poses a challenge that needs to be addressed.
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
