Article
Biochemistry & Molecular Biology
Premranjan Kumar, Ob Osahon, David B. Vides, Nicola Hanania, Charles G. Minard, Rajagopal V. Sekhar
Summary: This study reveals that COVID-19 patients of all age groups experience GSH deficiency, increased OxS, and elevated oxidant damage, which worsen with advancing age. The supplementation of GlyNAC, a combination of glycine and N-acetylcysteine, has the potential to improve these defects and combat COVID-19 infection.
Article
Chemistry, Medicinal
Iwan J. P. de Esch, Daniel A. Erlanson, Wolfgang Jahnke, Christopher N. Johnson, Louise Walsh
Summary: The review summarizes successful fragment-to-lead studies published in 2020 and discusses trends and best practices in fragment libraries, target proteins, screening technologies, hit-optimization strategies, and properties of hit fragments and leads. Trends and innovations identified in the review promise to further increase the success of FBDD by developing novel screening fragments, improving screening technologies, using computer-aided design and virtual screening, and combining FBDD with other drug-discovery technologies.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Bart De Geest, Mudit Mishra
Summary: Type 2 diabetes is a redox disease characterized by oxidative stress and chronic inflammation. The cardiac manifestations of the disease, known as diabetic cardiomyopathy, are primarily caused by mitochondrial overproduction of reactive oxygen species. These species are produced due to intracellular hyperglycemia, increased fatty oxidation, and lipotoxicity in cardiomyocytes. The resulting oxidative distress affects various pathways, leading to cell dysfunction and injury. Animal studies have shown that increasing the expression of antioxidant enzymes can attenuate myocardial pathology and improve cardiac function.
Article
Chemistry, Medicinal
Kai S. Yang, Sunshine Z. Leeuwon, Shiqing Xu, Wenshe Ray Liu
Summary: The approval of the combination therapy PAXLOVID has boosted morale in fighting the COVID-19 pandemic. The analysis in the article discusses possible mutations in the M-Pro that could lead to acquired viral resistance to nirmatrelvir and its implications for fighting future drug-resistant viral variants.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Marnix R. van der Kolk, Mathilde A. C. H. Janssen, Floris P. J. T. Rutjes, Daniel Blanco-Ania
Summary: Cyclobutanes, with their unique structure, offer various benefits in medicinal chemistry, such as improving drug candidate properties through replacement of alkenes and larger cyclic systems.
Review
Oncology
Biswa Mohan Sahoo, Bimal Krishna Banik, Preetismita Borah, Adya Jain
Summary: This article introduces the definition and generation pathways of Reactive Oxygen Species (ROS), as well as their role in the development of cancer. ROS can act as tumor-suppressing or tumor-promoting agents, and their increased levels can inhibit tumor growth or induce apoptosis. However, high levels of ROS can also lead to the formation of malignant tumors.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Gennaro Pescitelli
Summary: The exciton chirality method is a well-established approach for assigning the absolute configuration of compounds with multiple chromophores. Its correct application requires a good understanding of molecular conformation, transition dipole moment directions, and the exciton coupling mechanism. These prerequisites can be easily verified through quantum-mechanical calculations.
Article
Biochemistry & Molecular Biology
Grzegorz K. Jakubiak, Kamila Osadnik, Mateusz Lejawa, Tadeusz Osadnik, Marcin Golawski, Piotr Lewandowski, Natalia Pawlas
Summary: Metabolic syndrome is the coexistence of factors that increase the risk for type 2 diabetes and cardiovascular disease, and it is associated with oxidative stress. Among the components of metabolic syndrome, obesity and insulin resistance show the strongest association with oxidative stress.
Review
Plant Sciences
Uttpal Anand, Champa Keeya Tudu, Samapika Nandy, Kumari Sunita, Vijay Tripathi, Gary J. Loake, Abhijit Dey, Jaroslaw Prockow
Summary: This study compiled and emphasized the traditional herbal knowledge and their applications for treating various skin diseases in India, showing great potential in treating human skin disorders. However, further research and clinical evidence are needed to determine the effectiveness of these plant species in skin condition treatment.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Takumi Satoh, Dorit Trudler, Chang-Ki Oh, Stuart A. Lipton
Summary: This article reviews the potential applications of carnosic acid (CA) and carnosol (CS) in rosemary for conditions such as Alzheimer's disease, Parkinson's disease, and COVID-19. It highlights the antioxidant, anti-inflammatory, and neuroprotective effects of CA, as well as its potential to inhibit the NLRP3 inflammasome. The article suggests that CA-related compounds could serve as therapeutics for acute and chronic neurological effects caused by SARS-CoV-2 infection and other neurodegenerative diseases.
Review
Chemistry, Medicinal
Fatima Noor, Muhammad Tahir ul Qamar, Usman Ali Ashfaq, Aqel Albutti, Ameen S. S. Alwashmi, Mohammad Abdullah Aljasir
Summary: The use of natural products, specifically medicinal plants, in medicine has proven to be crucial due to their ability to interact with cellular targets involved in diseases. Network pharmacology has emerged as a systematic paradigm in drug discovery, providing a comprehensive understanding of the bioactive components found in medicinal plants.
Article
Chemistry, Applied
Min Guo, Ying-Zhong Liang, Xiu-Ming Cui, Lin-Jiao Shao, Yin-Fei Li, Xiao-Yan Yang
Summary: A new chamigrane sesquiterpene, albocimea A (1), and one known compound, 6-hydroxy-8-methoxy-3S,5-dimethylisochroman (2), were isolated from the rice fermentation of the fungus Antrodiella albocinnamomea. The structure of the new compound was elucidated through spectroscopic analysis and ECD calculations. Cytotoxicity tests on both compounds against five human cancer cell lines revealed no significant cytotoxicity.
NATURAL PRODUCT RESEARCH
(2023)
Review
Chemistry, Medicinal
Seyedeh Roya Alizadeh, Mohammad Ali Ebrahimzadeh
Summary: More studies are needed to develop new drugs that can overcome drug resistance and minimize side effects. Quercetin, a natural flavonoid, has shown diverse biological activities, but its poor solubility and bioavailability limit its applicability. Researchers have been exploring the modification of quercetin by designing and synthesizing novel derivatives to overcome these limitations. The physico-chemical properties of quercetin's molecular scaffold make it attractive for drug development, and the investigation of its derivatives' activities, chemical structure-activity relationship, and mechanism of action is crucial. Quercetin-based molecules have the potential to contribute to the discovery of medications for various diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Murat Ozdal, Sumeyra Gurkok
Summary: Nanoparticles show promising antimicrobial properties by bypassing bacterial drug resistance mechanisms, inhibiting biofilm formation, and disrupting important molecular mechanisms. When used in combination with appropriate antibiotics, nanoparticles may exhibit synergy and help prevent the global bacterial resistance crisis. Additionally, nanoparticles with enhanced biocompatibility and biodegradability enable the development of a wide range of medical products.
Article
Chemistry, Medicinal
Lingling Dong, Hongling Du, Minyue Zhang, Haiting Xu, Xiulan Pu, Qiyan Chen, Ruifeng Luo, Yichen Hu, Yitao Wang, He Tu, Jinming Zhang, Fei Gao
Summary: The study showed that Rhein had therapeutic effects on ulcerative colitis by inhibiting the production of pro-inflammatory cytokines, alleviating UC-associated symptoms, and modulating the PI3K/Akt/mTOR signaling pathway and gut microbiota.
PHYTOTHERAPY RESEARCH
(2022)
Article
Chemistry, Medicinal
Thanigaimalai Pillaiyar, Stefan Laufer
Summary: This article highlights the kinases associated with coronavirus infections and their inhibitors with antiviral and potentially anti-inflammatory, cytokine-suppressive, or antifibrotic activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Roya Abka-Khajouei, Latifa Tounsi, Nasim Shahabi, Anil Kumar Patel, Slim Abdelkafi, Philippe Michaud
Summary: Alginate is a hydrogel derived from brown algae with a wide range of applications. Its structural, physical, and chemical properties are influenced by the arrangement of monomers.
Review
Biochemistry & Molecular Biology
Monica Emanuelli, Davide Sartini, Elisa Molinelli, Roberto Campagna, Valentina Pozzi, Eleonora Salvolini, Oriana Simonetti, Anna Campanati, Annamaria Offidani
Summary: The skin is constantly exposed to reactive oxygen species (ROS) and oxidative stress may play a role in skin diseases, including melanoma. Melanocytes are more susceptible to oxidative stress due to their melanin production process.
Article
Chemistry, Medicinal
Wenhao Dai, Dirk Jochmans, Hang Xie, Hang Yang, Jian Li, Haixia Su, Di Chang, Jiang Wang, Jingjing Peng, Lili Zhu, Yong Nian, Rolf Hilgenfeld, Hualiang Jiang, Kaixian Chen, Leike Zhang, Yechun Xu, Johan Neyts, Hong Liu
Summary: A series of peptidomimetic aldehydes were designed and synthesized to target 3C(pro) of EV71 and SARS-CoV-2. Compound 18p showed potent antiviral and enzyme inhibitory activity, as well as good pharmacokinetic properties.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Parnian Baharlouei, Azizur Rahman
Summary: Chitin and chitosan, abundant polymers in nature, have gained attention for their favorable properties and enormous potential biomedical applications. They can be used in drug delivery systems, cancer treatment, wound dressings, and more, making them important in the medical field.
