Article
Chemistry, Medicinal
Jakub Cebula, Krzysztof Fink, Waldemar Goldeman, Bozena Szermer-Olearnik, Anna Nasulewicz-Goldeman, Mateusz Psurski, Monika Cuprych, Anna Kedziora, Bartlomiej Dudek, Gabriela Bugla-Ploskonska, Monika Chaszczewska-Markowska, Michalina Gos, Pawel Migdal, Tomasz M. Goszczynski
Summary: This research identified two promising structural patterns that provide COSAN-based compounds with potent and selective activity against Staphylococcus aureus. Additionally, proper hydrophilic-lipophilic balance was found to be crucial for the selective activity of the tested compounds. These patterns could be useful in the development of metallacarborane-based antibiotics with strong antibacterial properties and low cytotoxicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Krzysztof Smialkowski, Carla Sardo, Zbigniew J. J. Lesnikowski
Summary: The exploitation of metallacarboranes' potential in various fields requires convenient and versatile methods for their functionalization. This study reports the functionalization of cobalt bis(1,2-dicarbollide) at 8,8 '-boron atoms with different heterobifunctional moieties. It also describes an approach to the synthesis of three and four functionalized metallacarboranes simultaneously at boron and carbon atoms.
Review
Biochemistry & Molecular Biology
Lucia Pazderova, Ece Zeynep Tuzun, Dmytro Bavol, Miroslava Litecka, Lukas Fojt, Bohumir Gruner
Summary: The cobalt bis(dicarbollide)(1(-)) anion plays a significant role in material science and medicine due to its unique properties and the availability of synthetic routes for easy modifications. The modification of the dicarbollide cage has been well-established for boron atom substitutions, but there has been limited progress on carbon vertex modifications. Recent developments in metalation reactions on C-H vertices have enabled direct and straightforward cage modifications, leading to new trends in the field. This review provides an overview of these methods and their applications in designing unconventional drugs.
Article
Biochemistry & Molecular Biology
Lukas Fojt, Bohumir Gruner, Jan Nekvinda, Ece Zeynep Tuzun, Ludek Havran, Miroslav Fojta
Summary: This study explores the effect of hydrophilic alkylhydroxy and carboxy groups on the electrochemical signals of cobalta bis(dicarbollide) ions in aqueous buffers. The results show that the location and type of substitution have minimal effect on the electrochemical response, but the intensity of the signals is dependent on concentration.
Article
Chemistry, Analytical
Tatiana Shishkanova, Alla Sinica
Summary: A cobalt bis(dicarbollide) derivative deposited onto the surface of a graphite electrode through an electrochemically oxidized o-phenylenediamine unit (pCB-oPD) is proposed for the detection of catecholamine metabolites, namely homovanillic acid (HVA) and vanillylmandelic acid (VMA). The set of electrochemical techniques makes it possible to evaluate the options of the individual and simultaneous detection of metabolites.
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Lyubov G. Dezhenkova, Anna A. Druzina, Yulia L. Volodina, Nadezhda Dudarova, Natalia A. Nekrasova, Olga B. Zhidkova, Mikhail A. Grin, Vladimir Bregadze
Summary: Novel cobalt bis(dicarbollide)-curcumin conjugates were synthesized and found to be non-cytotoxic against tumor and normal cells. Flow cytometry analysis showed that these conjugates entered the cells in a time-dependent manner.
Article
Biochemistry & Molecular Biology
Ekaterina Bogdanova, Marina Yu Stogniy, Kyrill Yu Suponitsky, Igor B. Sivaev, Vladimir Bregadze
Summary: A series of novel cobalt bis(dicarbollide) based amidines were synthesized by adding primary and secondary amines to a specific compound, leading to different isomer mixtures when reacting with primary vs. secondary amines. Crystal structures of these compounds were determined by X-ray diffraction.
Article
Chemistry, Inorganic & Nuclear
Krzysztof Fink, Jakub Cebula, Zdenek Tosner, Mateusz Psurski, Mariusz Uchman, Tomasz M. Goszczynski
Summary: Cobalt bis(dicarbollide) (COSAN) is a versatile metallacarborane used in drug development. This study comprehensively characterized the interactions between COSAN and DNA, finding that COSAN has no significant effect on DNA structure and can induce cytotoxicity even without DNA presence. These findings confirm the safety and biocompatibility of metallacarboranes and provide new opportunities for drug development.
DALTON TRANSACTIONS
(2023)
Article
Spectroscopy
Karuppiah Nagaraj, Subramaniam Kamalesu, Subramanian Sakthinathan, Te-Wei Chiu, Snehal Lokhandwala, Nikhil M. Parekh, Chelladurai Karuppiah
Summary: This study investigated the binding interaction between a surfactant cobalt(III) complex and DNA, and found that they bind through intercalation. The presence of long aliphatic chains in the ligands as well as the larger π-framework of the ligand also enhance the intercalation.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2023)
Article
Chemistry, Physical
Hikaru Kuroki, Erika Aida, Takuya Komine, Keisuke Matsuoka
Summary: The study demonstrated that surfactants with long EO chains are effective in solubilizing fullerene, while relatively shorter EO chains are more suitable for solubilizing naphthalene. Furthermore, the solubilization site of fullerene in micelles was found to be in the vicinity of EO chains.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Energy & Fuels
J. Rajesh Banu, M. Dinesh Kumar, S. Kavitha, Jeong-Jun Yoon, Gopalakrishnan Kumar, Jeong-Hoon Park
Summary: This study successfully increased the biohydrogen production and solubilization of sea grass by utilizing surfactant induced sonic fission (SSF) method.
INTERNATIONAL JOURNAL OF ENERGY RESEARCH
(2021)
Article
Chemistry, Physical
Zoya Zaheer, Samia A. Kosa, Mohammad Osama, Mohd Akram
Summary: The study investigated the binding capabilities of flurbiprofen drug with a new type of gemini surfactant using spectroscopic methods, revealing significant interaction and a correlation with the chain length and critical micellar concentration of the surfactant.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Biochemistry & Molecular Biology
Anna A. Druzina, Natalia E. Grammatikova, Olga B. Zhidkova, Natalia A. Nekrasova, Nadezhda V. Dudarova, Irina D. Kosenko, Mikhail A. Grin, Vladimir I. Bregadze
Summary: A series of novel conjugates of cobalt bis(dicarbollide) and closo-dodecaborate with curcumin were synthesized and tested for antibacterial activity. One of the conjugates exhibited better activity against Gram-positive microorganisms.
Article
Pharmacology & Pharmacy
Mirella Miranko, Judit Toth, Csilla Bartos, Rita Ambrus, Tivadar Feczko
Summary: This study developed composite powders containing levocetirizine dihydrochloride (LC) for nasal administration using three mucoadhesive polymers and four cyclodextrin species. The LC was in the form of a zwitterion after neutralization and the product exhibited an amorphous state. The average particle size of the microparticles ranged from 2.42 to 3.44 μm, except for those containing a polyvinyl alcohol excipient, which had a larger diameter of 29.80 μm. The spray-dried powder with beta-cyclodextrin showed the highest permeability, while other cyclodextrins and polymer excipients showed similar or slightly higher penetration abilities than LC.
Article
Chemistry, Physical
Larissa dos Santos Silva Araujo, Giuseppe Lazzara, Leonardo Chiappisi
Summary: This study provides a comprehensive overview of the thermodynamics aspects of surfactants and CDs inclusion complexes formation in aqueous environment, emphasizing the assessment of interactions, thermodynamic driving forces, and structural aspects. It also discusses the most common analytical techniques used to gather deep insight into CDs complexes, pointing out the perspectives for the surfactant-cyclodextrin complexes.
ADVANCES IN COLLOID AND INTERFACE SCIENCE
(2021)
Review
Biochemistry & Molecular Biology
Robert Hromadka, Zdenek Kejik, Milan Jakubek, Robert Kaplanek, Viera Sandrikova, Marian Urban, Pavel Martasek, Vladimir Kral
CURRENT MEDICINAL CHEMISTRY
(2019)
Article
Biochemistry & Molecular Biology
Milan Jakubek, Zdenek Kejik, Robert Kaplanek, Veronika Antonyova, Robert Hromadka, Viera Sandrikova, David Sykora, Pavel Martasek, Vladimir Kral
BIOORGANIC CHEMISTRY
(2019)
Article
Chemistry, Inorganic & Nuclear
Miroslava Guricova, Jan Pinc, Juraj Malincik, Jakub Rak, Martin Kuchar, Vilem Bartunek
REVIEWS IN INORGANIC CHEMISTRY
(2019)
Review
Oncology
Jakub Rak, Pavla Pouckova, Jiri Benes, David Vetvicka
ANTICANCER RESEARCH
(2019)
Review
Genetics & Heredity
Veronika Antonyova, Zdenek Kejik, Tereza Brogyanyi, Robert Kaplanek, Martina Pajkova, Veronika Talianova, Robert Hromadka, Michal Masarik, David Sykora, Lucie Miksatkova, Pavel Martasek, Milan Jakubek
Article
Biochemistry & Molecular Biology
Nikita Abramenko, Zdenek Kejik, Robert Kaplanek, Ameneh Tatar, Tereza Brogyanyi, Martina Pajkova, David Sykora, Katerina Vesela, Veronika Antonyova, Petr Dytrych, Masao Ikeda-Saito, Pavel Martasek, Milan Jakubek
Summary: Proton pump inhibitors are important clinically used drugs, but their long-term use may be associated with an increased risk of serious pathological states. The interaction between these drugs and transition metal ions could play a role in their side effects.
CHEMICAL BIOLOGY & DRUG DESIGN
(2021)
Review
Biochemistry & Molecular Biology
Zdenek Kejik, Robert Kaplanek, Michal Masarik, Petr Babula, Adam Matkowski, Petr Filipensky, Katerina Vesela, Jakub Gburek, David Sykora, Pavel Martasek, Milan Jakubek
Summary: Flavonoids, common plant natural products, can suppress ROS-related damage through chelation of transition metal ions, with iron being the most significant. Their interaction with Fe(II) and Fe(III) ions can significantly affect their biological properties. Special biological effects of their iron metallocomplexes, such as the inhibition of iron-containing enzymes, have been discussed in this review.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Engineering, Chemical
Milan Jakubek, Michal Masarik, Tomas Briza, Robert Kaplanek, Katerina Vesela, Nikita Abramenko, Pavel Martasek
Summary: The study found that some PPO herbicides showed significant inhibition of hPPO, while the newly synthesized compounds did not exhibit significant activity. However, a designed model based on determined IC50 values can better predict PPO herbicidal toxicity and improve the design of synthetic inhibitors.
Review
Biochemistry & Molecular Biology
Nikita Abramenko, Frederic Vellieux, Petra Tesarova, Zdenek Kejik, Robert Kaplanek, Lukas Lacina, Barbora Dvorankova, Daniel Rosel, Jan Brabek, Adam Tesar, Milan Jakubek, Karel Smetana
Summary: Estrogens may have a protective effect against COVID-19 by influencing the cardiovascular/pulmonary/immune system, reducing cytokine storms, and directly inhibiting viral replication. In addition to natural hormones, phytestrogens and synthetic molecules may also have anti-viral activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Zdenek Kejik, Robert Kaplanek, Petr Dytrych, Michal Masarik, Katerina Vesela, Nikita Abramenko, David Hoskovec, Martina Vasakova, Jarmila Kralova, Pavel Martasek, Milan Jakubek
Summary: Designing optimal adjuvant therapy is crucial in treating non-small-cell lung carcinoma. Standard methods may not be effective in cases with high level of CTCs, thus alternative therapeutic strategies like low-toxicity natural agents may be considered when standard methods fail. This review discusses NSCLC therapy strategies and potential options for treatment beyond standard methods.
Article
Biochemistry & Molecular Biology
Veronika Antonyova, Zdenek Kejik, Tereza Brogyanyi, Robert Kaplanek, Katerina Vesela, Nikita Abramenko, Tomas Ocelka, Michal Masarik, Adam Matkowski, Jakub Gburek, Renata Abel, Andrean Goede, Robert Preissner, Petr Novotny, Milan Jakubek
Summary: Predicting and studying the effects of non-psychotropic cannabinoids on DNA methylation is crucial for assessing the safety of these products. Researchers found that these cannabinoids can interfere with TET enzymes, affecting methylation patterns, possibly through chelating ferrous ions.
BIOORGANIC CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
Jindriska Leischner Fialova, Katerina Honigova, Martina Raudenska, Lucie Miksatkova, Renata Zobalova, Jiri Navratil, Jana Smigova, Taraka Ramji Moturu, Tomas Vicar, Jan Balvan, Katerina Vesela, Nikita Abramenko, Zdenek Kejik, Robert Kaplanek, Jaromir Gumulec, Daniel Rosel, Pavel Martasek, Jan Brabek, Milan Jakubek, Jiri Neuzil, Michal Masarik
Summary: Mitochondria play a crucial role in cellular growth and function, and recent studies have challenged the notion that they are not involved in cancer growth. This study shows that pentamethinium salts, originally designed as mitochondrial probes, have a strong inhibitory effect on cancer cell proliferation and migration by interfering with mitochondrial respiration and causing oxidative stress. These findings suggest that pentamethinium salts could be potential novel anti-cancer agents.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Medicine, Research & Experimental
Tereza Brogyanyi, Robert Kaplanek, Zdenek Kejik, Bozena Hosnedlova, Veronika Antonyova, Nikita Abramenko, Katerina Vesela, Pavel Martasek, Martin Vokurka, Des R. Richardson, Milan Jakubek
Summary: This study tested novel iron chelators for their cytotoxicity against pancreatic cancer cells, showing high toxicity and selectivity. The mechanism of action of the chelators may be associated with mitophagy induction.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Veronika Antonyova, Ameneh Tatar, Tereza Brogyanyi, Zdenek Kejik, Robert Kaplanek, Frederic Vellieux, Nikita Abramenko, Alla Sinica, Jan Hajduch, Petr Novotny, Bettie Sue Masters, Pavel Martasek, Milan Jakubek
Summary: In this study, we synthesized a series of pyrrolopyrrole derivatives and found that the basic pyrrolo[3,2-b]pyrrole derivative 1 exhibited strong inhibitory activity against TET1 protein. Furthermore, derivative 1 showed potent anticancer activity and exclusive mitochondrial localization.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Veronika Talianova, Zdenek Kejik, Robert Kaplanek, Katerina Vesela, Nikita Abramenko, Lukas Lacina, Karolina Strnadova, Barbora Dvorankova, Pavel Martasek, Michal Masarik, Magdalena Houdova Megova, Petr Busek, Jana Krizova, Lucie Zdrazilova, Hana Hansikova, Erik Vlcak, Vlada Filimonenko, Aleksi Sedo, Karel Smetana, Milan Jakubek
Summary: IL-6 signaling plays a crucial role in the pathogenesis of serious diseases such as chronic inflammation and cancer. Two newly designed bis-pentamethinium salts compounds showed potential in binding IL-6 receptor and inhibiting mitochondrial metabolism in cancer cells.
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)
