Chemistry, Medicinal

Review Biochemistry & Molecular Biology

Revisiting the Oxidation of Flavonoids: Loss, Conservation or Enhancement of Their Antioxidant Properties

Herna Speisky, Fereidoon Shahidi, Adriano Costa de Camargo, Jocelyn Fuentes

Summary: Flavonoids have the ability to act as antioxidants, but their phenolic moieties are easily oxidized, compromising their antioxidant capacity. However, the oxidation of certain flavonoids can actually enhance their antioxidant properties. This apparent paradox is due to the pro-oxidant and/or electrophilic character of the oxidation-derived metabolites, which activate the cell's endogenous antioxidant capacity or prevent the activation of pro-oxidant pathways.

ANTIOXIDANTS (2022)

Article Chemistry, Medicinal

The Boron Advantage: The Evolution and Diversification of Boron's Applications in Medicinal Chemistry

Katia Messner, Billy Vuong, Geoffrey K. Tranmer

Summary: This review discusses the history of boron's early use in drugs and the use of boron functional groups in medicinal chemistry. It highlights critical developments from these functional groups and showcases the application of boron in prodrugs, softdrugs, and nanocarriers.

PHARMACEUTICALS (2022)

Review Plant Sciences

A comprehensive review of ethnopharmacology, phytochemistry, pharmacology, and pharmacokinetics of Schisandra chinensis (Turcz.) Baill. and Schisandra sphenanthera Rehd. et Wils.

Ke Yang, Jing Qiu, Zecheng Huang, Ziwei Yu, Wenjun Wang, Huiling Hu, Yu You

Summary: Schisandra chinensis and Schisandra sphenanthera, known as bei-wuweizi and nan-wuweizi in Chinese respectively, are highly similar plants with traditional uses in Chinese medicine for treating various conditions. They have similar chemical compositions and pharmacological activities, with potential drug interactions due to their inhibitory effects on CYP3A and P-gp. Further research is needed to explore their traditional uses and differences for clinical applications.

JOURNAL OF ETHNOPHARMACOLOGY (2022)

Review Biochemistry & Molecular Biology

Oxidative Stress Is a Key Modulator in the Development of Nonalcoholic Fatty Liver Disease

Yuanqiang Ma, Gyurim Lee, Su-Young Heo, Yoon-Seok Roh

Summary: This review summarizes the relationship between oxidative stress and the development of nonalcoholic fatty liver disease (NAFLD), and discusses the potential role of antioxidants as therapeutic agents for NAFLD.

ANTIOXIDANTS (2022)

Review Plant Sciences

A systematic review on botany, processing, application, phytochemistry and pharmacological action of Radix Rehmnniae

Minmin Li, Huajuan Jiang, Yule Hao, Kequn Du, Hongling Du, Chuan Ma, He Tu, Yao He

Summary: Radix Rehmanniae (RR) is a traditional Chinese herbal medicine with clinical value and rich resources. It has multiple pharmacological actions and can be used to treat various diseases. RR can be processed into two different products, which have significant changes in properties, taste, efficacy, clinical application, chemical composition, and pharmacological action.

JOURNAL OF ETHNOPHARMACOLOGY (2022)

Article Chemistry, Medicinal

An AI-based Prediction Model for Drug-drug Interactions in Osteoporosis and Paget's Diseases from SMILES

Truong Nguyen Khanh Hung, Nguyen Quoc Khanh Le, Ngoc Hoang Le, Le Van Tuan, Thuan Phuoc Nguyen, Cao Thi, Jiunn-Horng Kang

Summary: Osteoporosis and Paget's disease are common bone diseases in the elderly, and drug-drug interactions are potential issues in combination therapy. This study develops an AI-based machine-learning model to predict the outcomes of interactions between drugs used for osteoporosis and Paget's treatment, offering a time and cost-saving approach to determine the best combination of medications in clinical practice.

MOLECULAR INFORMATICS (2022)

Article Chemistry, Medicinal

Discovery and Mechanism of SARS-CoV-2 Main Protease Inhibitors

Sarah Huff, Indrasena Reddy Kummetha, Shashi Kant Tiwari, Matthew B. Huante, Alex E. Clark, Shaobo Wang, William Bray, Davey Smith, Aaron F. Carlin, Mark Endsley, Tariq M. Rana

Summary: This study identifies a class of compounds targeting the SARS-CoV-2 main protease that can inhibit viral replication. The compounds were found through medicinal chemistry and rational drug design strategies and offer a potential framework for the development of future COVID-19 treatments.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Superoxide Radicals in the Execution of Cell Death

Junichi Fujii, Takujiro Homma, Tsukasa Osaki

Summary: Superoxide is a primary oxygen radical that plays a role in cellular defense. Hydrogen peroxide, produced as a result, can exacerbate diseases. Ferroptosis, induced by lipid peroxides in the presence of free iron, is associated with many diseases. Radical electrons, from mitochondrial complexes and enzymatic reactions, cause lipid peroxidation. GPX4 reduces lipid peroxides, and other antioxidants indirectly protect against ferroptosis. Low molecular weight compounds neutralize radical electrons, suppressing ferroptosis. Early removal of radical electrons is important for protection against ferroptosis and oxidative stress-related diseases.

ANTIOXIDANTS (2022)

Review Biochemistry & Molecular Biology

Male Infertility and Oxidative Stress: A Focus on the Underlying Mechanisms

Robert John Aitken, Joel R. Drevet, Aron Moazamian, Parviz Gharagozloo

Summary: Reactive oxygen species (ROS) play a critical role in defining the functional competence of human spermatozoa. Adequate levels of ROS promote sperm capacitation, while excessive ROS generation leads to oxidative stress, disrupting fertilizing capacity and DNA integrity. Understanding the mechanisms of oxidative stress is essential for developing effective antioxidant strategies.

ANTIOXIDANTS (2022)

Article Biochemistry & Molecular Biology

Cytotoxic effect, enzyme inhibition, and in silico studies of some novel N-substituted sulfonyl amides incorporating 1,3,4-oxadiazol structural motif

Ozcan Gulec, Cuneyt Turkes, Mustafa Arslan, Yeliz Demir, Yesim Yeni, Ahmet Hacimuftuoglu, Ergun Ereminsoy, Omer Irfan Kufrevioglu, Sukru Beydemir

Summary: This study discovered novel multi-target AChEIs and hCAIs that are highly potent and may have good oral bioavailability and brain penetration. Compounds 6a, 6d, and 6h showed high selectivity for the target enzymes, were orally bioavailable, and had a preference for distribution in the brain.

MOLECULAR DIVERSITY (2022)

Article Chemistry, Medicinal

Synthesis, biological evaluation, and in silico study of novel library sulfonates containing quinazolin-4(3H)-one derivatives as potential aldose reductase inhibitors

Feyzi Sinan Tokali, Yeliz Demir, Ibrahim Hakki Demircioglu, Cuneyt Turkes, Erbay Kalay, Kivilcim Sendil, Sukru Beydemir

Summary: A series of novel sulfonates were designed and synthesized to inhibit aldose reductase (ALR2), with one compound showing higher inhibitor activity and the need for further molecular modification to improve as an ALR2 inhibitor. Experimental and in silico study results suggest the potential of these quinazolin-4(3H)-one ring derivatives for drug development against ALR2.

DRUG DEVELOPMENT RESEARCH (2022)

Review Chemistry, Medicinal

The current drug discovery landscape for trypanosomiasis and leishmaniasis: Challenges and strategies to identify drug targets

Fernando Altamura, Rishi Rajesh, Carolina M. C. Catta-Preta, Nilmar S. Moretti, Igor Cestari

Summary: Human trypanosomiasis and leishmaniasis, caused by protozoan parasites, have become globally distributed tropical diseases due to human migration, climate change, and anthropogenic disturbance. The current chemotherapy for these diseases has limited efficacy and drug resistance is a growing concern. This review discusses the limitations of available drugs and highlights promising leads from current drug-based clinical trials. It also examines the challenges in target-based drug discovery and the advantages and limitations of modern research tools.

DRUG DEVELOPMENT RESEARCH (2022)

Article Chemistry, Medicinal

Therapeutic strategies to overcome cisplatin resistance in ovarian cancer

Mengdi Song, Mingxiao Cui, Kehai Liu

Summary: This review discusses the chemotherapeutic drugs and phytochemicals developed to overcome cisplatin-resistance ovarian cancer (CROC), highlighting the significance of combination therapy and the use of a nanoparticle delivery system in reversing cisplatin resistance.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation

Tianyu Wang, Shi Cai, Yao Cheng, Wanheng Zhang, Minmin Wang, Huiyong Sun, Binghua Guo, Zheng Li, Yibei Xiao, Sheng Jiang

Summary: Compound 17 is a bifunctional inhibitor that can block the interactions between PD-1 and PD-L1, promoting internalization and degradation of PD-L1. It effectively suppresses tumor growth in vivo by activating antitumor immunity.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Review Chemistry, Medicinal

Antimicrobial peptides, conventional antibiotics, and their synergistic utility for the treatment of drug-resistant infections

Yiyun Zhu, Weijing Hao, Xia Wang, Jianhong Ouyang, Xinyi Deng, Haining Yu, Yipeng Wang

Summary: Antimicrobial peptides (AMPs), also known as host defense peptides (HDPs), are important immune defense molecules in multicellular organisms. AMPs have great potential as new generation antimicrobial agents and can be used in combination with conventional antibiotics to kill drug-resistant pathogens and improve therapeutic effects.

MEDICINAL RESEARCH REVIEWS (2022)

Review Biochemistry & Molecular Biology

Dietary Polyphenol, Gut Microbiota, and Health Benefits

Xiaofei Wang, Yue Qi, Hao Zheng

Summary: Polyphenols, important secondary metabolites produced by plants, have multiple health benefits. Most dietary polyphenols are not absorbed in the gastrointestinal tract, but are transformed into bioactive metabolites by gut microbiota in the large intestine. Dietary polyphenols can modulate the composition of gut microbes, which in turn catabolize polyphenols to release bioactive metabolites.

ANTIOXIDANTS (2022)

Article Chemistry, Medicinal

DYRK1A inhibitors for disease therapy: Current status and perspectives

Tong Liu, Yuxi Wang, Jiaxing Wang, Changyu Ren, Hao Chen, Jifa Zhang

Summary: DYRK1A, a conserved protein kinase, plays essential roles in various biological processes and is associated with Down syndrome, neurodegenerative diseases, cancer, and diabetes. The development of DYRK1A inhibitors has seen a rapid increase in recent years, providing new directions for future therapeutic research.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Bioactive Phytochemicals and Quenching Activity of Radicals in Selected Drought-Resistant Amaranthus tricolor Vegetable Amaranth

Umakanta Sarker, Shinya Oba, Sezai Ercisli, Amine Assouguem, Amal Alotaibi, Riaz Ullah

Summary: This study evaluated the phytochemicals and antioxidant activity of drought-resistant amaranth, revealing their abundance in nutrients and antioxidant profiles, which make them suitable for the production of drinks and beneficial for promoting health and nourishing communities in drought-prone areas.

ANTIOXIDANTS (2022)

Review Biochemistry & Molecular Biology

Heme Oxygenase-1: An Anti-Inflammatory Effector in Cardiovascular, Lung, and Related Metabolic Disorders

Stefan W. Ryter

Summary: The heme oxygenase-1 (HO-1) enzyme and its reaction products have beneficial effects in human diseases, including cardiovascular disease, metabolic conditions, and acute and chronic diseases of the liver, kidney, or lung. Modulating the HO-1 pathway, such as regulating HO-1 expression or using reaction products, has therapeutic potential in inflammatory conditions.

ANTIOXIDANTS (2022)

Review Biochemistry & Molecular Biology

Role of NRF2 in Ovarian Cancer

Giovanni Tossetta, Sonia Fantone, Eva Montanari, Daniela Marzioni, Gaia Goteri

Summary: This review summarizes the role of NRF2 in ovarian cancer, focusing on its function in drug resistance, natural and synthetic modulators of NRF2, and its protective function in normal ovarian preservation.

ANTIOXIDANTS (2022)