Review
Biochemistry & Molecular Biology
Dahye Yun, So Young Yoon, Soo Jung Park, Yoon Jung Park
Summary: Herbal plants enriched with isoquinoline alkaloids have been used in traditional folk medicine for their anti-inflammatory, antimicrobial, and analgesic effects. These alkaloids induce cell death through cell cycle arrest, apoptosis, and autophagy. The molecular mechanisms of these effects may involve binding to nucleic acids or proteins, enzyme inhibition, and epigenetic modulation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Arkadiusz Orchel, Ewa Chodurek, Marzena Jaworska-Kik, Piotr Paduszynski, Anna Kaps, Elwira Chrobak, Ewa Bebenek, Stanislaw Boryczka, Paulina Borkowska, Janusz Kasperczyk
Summary: In this study, it was found that 30-diethoxyphosphoryl-28-propynoylbetulin displayed the strongest inhibitory effect on growth and induction of cellular death in human breast cancer cells. The compound decreased DNA synthesis, up-regulated p21(WAF1/Cip1) levels, increased cell death, and triggered reactive oxygen species generation and mitochondrial membrane potential loss, ultimately leading to a form of regulated cell demise that exhibits features of necrosis-like morphology and activation of caspases.
Article
Food Science & Technology
Korattuvalappil S. Ravikumar, Haridas Ramya, Thekkuttuparambil A. Ajith, Manzoor A. Shah, Kainoor K. Janardhanan
Summary: The study evaluated the anticancer activity of Fomitopsis pinicola extract, showing significant cytotoxicity and antitumor effects, possibly attributed to the major chemical components identified.
JOURNAL OF FUNCTIONAL FOODS
(2021)
Article
Pharmacology & Pharmacy
Simona Braccini, Giorgia Rizzi, Lorenzo Biancalana, Alessandro Pratesi, Stefano Zacchini, Guido Pampaloni, Federica Chiellini, Fabio Marchetti
Summary: A series of novel diiron complexes were synthesized and evaluated for their anticancer activity, showing potent cytotoxicity against cancer cell lines with remarkable selectivity and good performance in inhibiting cell proliferation. Additionally, these complexes were capable of inducing significant ROS production and had the potential to inhibit the enzyme thioredoxin reductase.
Review
Biochemistry & Molecular Biology
Bruno I. M. Silva, Erika A. Nascimento, Cleber J. Silva, Teresinha G. Silva, Jaciana S. Aguiar
Summary: Monoterpenes have potential anticancer effects, mainly by inducing apoptosis caused by oxidative stress. Additionally, the synergistic effect with conventional chemotherapeutic drugs and improved use in drug delivery systems are important findings.
MOLECULAR BIOLOGY REPORTS
(2021)
Review
Nutrition & Dietetics
Ewa Forma, Magdalena Brys
Summary: Propolis, a natural material produced by honey bees from various botanical sources, has therapeutic activities such as antibacterial, antifungal, and anti-inflammatory effects, with potential benefits in inhibiting cancer cell proliferation and metastasis. Research suggests that propolis can also stimulate apoptosis, influence the tumor microenvironment, and potentially reduce the side effects of chemotherapy and radiotherapy.
Article
Biochemistry & Molecular Biology
Claudia Teixeira, Renato B. Pereira, Nuno F. S. Pinto, Catarina M. M. Coelho, Maria Jose G. Fernandes, Antonio G. Fortes, Maria S. T. Goncalves, David M. Pereira
Summary: Eugenol, the main component of clove essential oil, has shown anticancer activity. By synthesizing a series of derivatives and testing them, three compounds were found to have significant anticancer activity without toxicity towards noncancer cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Chemistry, Medicinal
Nivedita Bhardwaj, Nancy Tripathi, Bharat Goel, Shreyans K. Jain
Summary: During cancer progression, the interconnection between apoptosis and autophagy pathways plays a crucial role in determining the fate of a cell, with Diosgenin emerging as a potential candidate for cancer treatment by modulating these pathways. Numerous proteins involved in autophagy have been targeted for anticancer therapy, with natural compounds like Diosgenin showing promising effects in selectively inducing cytotoxicity in cancer cells.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Maxim E. Zhidkov, Moritz Kaune, Alexey Kantemirov, Polina A. Smirnova, Pavel Spirin, Maria A. Sidorova, Sergey A. Stadnik, Elena Y. Shyrokova, Dmitry N. Kaluzhny, Oleg A. Tryapkin, Tobias Busenbender, Jessica Hauschild, Tina Rohlfing, Vladimir S. Prassolov, Carsten Bokemeyer, Markus Graefen, Gunhild von Amsberg, Sergey A. Dyshlovoy
Summary: We synthesized a library of fascaplysin derivatives and investigated their selectivity, effects on cells, and DNA intercalation. The di- and trisubstituted halogen derivatives showed pronounced selectivity for cancer cells, while modification of cycle C resulted in stronger activity against therapy-resistant cells.
Article
Biochemistry & Molecular Biology
Ganesh Kumar Raut, Genji Sukumar, Moumita Chakrabarti, Jolly Janette Mendonza, Srihari Pabbaraja, B. Jagan Mohan Reddy, Ramakrishna Sistla, Sai Balaji Andugulapati, Manika Pal Bhadra
Summary: Polyphenols are natural compounds with anti-tumorigenic effects. This study designed and synthesized a compound that interferes with the cell cycle progression in aggressive prostate cancer. Further experiments showed that the compound inhibits the viability of prostate cancer cells and induces apoptosis through oxidative stress. In a mouse model, the compound showed no toxicity and reduced the tumor burden.
Article
Chemistry, Medicinal
Surendar Chitti, Sravani Pulya, Adinarayana Nandikolla, Tarun Kumar Patel, Karan Kumar Banot, Sankaranarayanan Murugesan, Balaram Ghosh, Venkata Gowri Chandra Sekhar Kondapalli
Summary: This study synthesized and evaluated 18 spirochromanone derivatives for their anticancer activity. The most potent compounds, Csp 12 and Csp 18, exhibited strong anticancer activity and showed higher selectivity towards MCF-7 cells compared to B16F10 cells.
FUTURE MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Mohamed A. El-Atawy, Mai S. Alsubaie, Mohammed L. Alazmi, Ezzat A. Hamed, Demiana H. Hanna, Hoda A. Ahmed, Alaa Z. Omar
Summary: "The preparation of N,N-diarylurea and N,N-diarylthiourea derivatives successfully revealed their therapeutic effects on human MCF-7 cancer cells. Among them, Diarylthiourea (compound 4) showed the highest efficacy with the most effective IC50 value (338.33±1.52 μM) and no cytotoxic effects on normal human lung cells (wi38 cells)."
Article
Biochemistry & Molecular Biology
Irina Tolmacheva, Yulia Beloglazova, Mikhail Nazarov, Olga Gagarskikh, Victoria Grishko
Summary: Multidrug resistance (MDR) is a common occurrence in cancer treatment, where cancer cells become resistant to chemotherapy drugs due to overexpression of ATP-binding cassette efflux transporters, including P-glycoprotein (P-gp). A new semi-synthetic derivative, MK, was found to have the highest cytotoxicity against cancer cells, but it was not identified as a P-gp inhibitor or substrate. Further studies suggest that the cytotoxic effect of MK on cancer cells may be induced through the ROS-mediated mitochondrial pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Maria Schroder, Maria Petrova, Zlatina Vlahova, Georgi M. Dobrikov, Ivaylo Slavchev, Evdokia Pasheva, Iva Ugrinova
Summary: The successful design of antitumour drugs often involves combining different biologically active subunits to affect multiple cellular regulatory pathways, leading to higher efficacy. In this study, two ferrocene derivatives, DK-164 and CC-78, were tested for their cytotoxic potential on lung cancer cell lines. DK-164 showed selective cytotoxicity towards cancer cells, while CC-78 exhibited higher cytotoxicity without selectivity. The different cellular mechanisms induced by these compounds in lung cancer cells provide insights into the specific functions of functional groups in ferrocene compounds and can guide the design of new antitumour drugs.
Article
Medicine, Research & Experimental
Shabeeba M. Ashraf, Susobhan Mahanty, Krishnan Rathinasamy
Summary: Securinine effectively inhibits the proliferation of cervical, breast, and lung cancer cells while inducing minimal toxicity in non-malignant HEK cells. It disrupts microtubule organization in both interphase and mitotic phases, as well as inhibits tubulin assembly. Additionally, securinine induces a mitochondrial-dependent ROS response in cancer cells and leads to apoptosis through a p53-dependent pathway in MCF-7 cells.
Article
Pharmacology & Pharmacy
Xuezhi Zhuo, Vito Fodera, Per Larsson, Zarah Schaal, Christel A. S. Bergstrom, Korbinian Lobmann, Aleksei Kabedev
Summary: Our previous work demonstrated that beta-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70 % indomethacin remains stable for over 12 months. We further investigated the stabilization mechanisms by testing five other drug molecules and using experimental techniques and molecular dynamics simulations. The results showed that steric confinement, hydrogen bonding, and the glass transition temperature of the drug molecule play important roles in stabilizing ASDs with high drug loadings.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Sebastian Schmidt, Ulrike Holzgrabe
Summary: The binding of drugs to plasma proteins, such as human serum albumin (HSA), is crucial for determining pharmacokinetic parameters. This study investigated the enantioselective binding of S- and R-ketamine to HSA. It was found that ketamine has weak affinity to HSA, with no significant differences in binding behavior between the individual enantiomers and the racemate. The aromatic ring and N-methyl group were identified as the most strongly involved structural moieties in the binding of ketamine to HSA.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Yuchen Zhao, Han Wang, Lin Jin, Ziwei Zhang, Lianghu Liu, Mengqi Zhou, Xianzheng Zhang, Lingling Zhang
Summary: Interleukins (ILs) are important for communication between immune cells and non-immune cells, but dysregulation of ILs expression is a characteristic of autoinflammatory diseases. Drugs targeting ILs have significant clinical benefits, but may also cause adverse reactions. Fusion protein technology, with its ability to enhance therapeutic efficacy, has been explored for developing anti-inflammatory drugs. This review discusses the efficacy of fusion protein drugs developed with ILs or their receptors in treating autoinflammatory diseases, highlighting the potential of this technology in future anti-inflammatory drug development.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Serena Bertoni, Elena Simone, Stefano Sangiorgi, Beatrice Albertini, Nadia Passerini
Summary: This study investigated the correlation between the structure and release properties of solid lipid microparticles (MPs) with different liquid additives. The additives accelerated the conversion of the unstable alpha-form of tristearin to the stable beta-polymorph and caused structural modifications in the MPs. The presence of additives prolonged the drug release in water and resulted in higher release profiles in biorelevant media. The findings suggest that the release behavior can be influenced by the polymorphism and supramolecular-level structural modification of lipid formulations containing crystal modifiers.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Juulia Jarvinen, Ahmed B. Montaser, Santosh Kumar Adla, Jukka Leppanen, Marko Lehtonen, Kati-Sisko Vellonen, Tuomo Laitinen, Aaro Jalkanen, William F. Elmquist, Juri Timonen, Kristiina M. Huttunen, Jarkko Rautio
Summary: This study attempted to alter the brain distribution pattern of Palbociclib by creating and assessing two novel prodrugs. Although the prodrug design did not significantly improve Palbociclib brain delivery, the study provides valuable insights for future prodrug development and drug delivery strategies targeting specific transporters.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Review
Pharmacology & Pharmacy
Miao Wang, Xinyu Ma, Shiyu Zong, Yaqiong Su, Rui Su, Hong Zhang, Yang Liu, Chunliu Wang, Ye Li
Summary: This article discusses the potential and limitations of nasal administration in central nervous system drug delivery. Nasal gel viscosity can alleviate the impact of nasal mucociliary clearance on drug delivery, and materials such as gellan gum, chitosan, carbomer, cellulose, and poloxamer can be used to prepare nasal gels.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Bjarke Strom Larsen, Eric Kissi, Liebert Parreiras Nogueira, Natalja Genina, Ingunn Tho
Summary: This study investigates the influence of drug load and polymer molecular weight on the structure of 3D printed tablets. The results show that drug load and polymer molecular weight have a significant impact on the porosity and size of the tablets, while the effect of drug load on the total porosity of the tablets is minimal.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Zhentao Qiao, Fuhang Wang, Dongjian Han, Yuansong Zhuang, Qingjiao Jiang, Yi Zhang, Miaomiao Liu, Quanxu An, Zhiwei Wang, Deliang Shen
Summary: In this study, it was demonstrated that periadventitial delivery of rapamycin-fibrin glue (RPM-FG) can inhibit intimal hyperplasia (IH) in a rat carotid artery injury model without compromising re-endothelialization. This provides a promising direction for the future development of a safe, effective, and minimally invasive perivascular drug delivery method to treat vascular disease.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Neele Puhlmann, Rodrigo Vidaurre, Klaus Kuemmerer
Summary: Active pharmaceutical ingredients and their metabolites and transformation products are pollutants that can harm human and environmental health. Designing greener APIs is an effective strategy to address this issue. The drug discovery and development process can incorporate environmental parameters to achieve this design, and this process is highly flexible.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)