Article
Chemistry, Multidisciplinary
Reham S. Ibrahim, Rahma S. R. Mahrous, Rasha M. Abu EL-Khair, Samir A. Ross, Abdallah A. Omar, Hoda M. Fathy
Summary: Selective factor Xa inhibitors effectively block the coagulation cascade and have become crucial in both preventing and treating thromboembolic diseases, especially in COVID-19 patients. Ten flavonoids were isolated from licorice root extract, with liquirtin showing the most potent FXa inhibitory activity. This study also utilized the QikProp module for ADMET predictions on the screened compounds.
Article
Biochemistry & Molecular Biology
M. Prabhahar, K. Gomathi, S. Prakash, S. Sendilvelan, M. Saravana Kumar, G. O. Jijina, Edwin Geo Varuvel, A. Haiter Lenin
Summary: Bread has been converted into functional herbal bread by infusing it with extracts of Glycyrrhiza glabra. The study found that the extract has high antioxidant potency and antidiabetic effects, and the fortified bread reduces the glycaemic index, making it suitable for diabetic people and diet watchers.
BIOINORGANIC CHEMISTRY AND APPLICATIONS
(2022)
Article
Chemistry, Medicinal
Felix F. Lillich, Sabine Willems, Xiaomin Ni, Whitney Kilu, Carmen Borkowsky, Mirko Brodsky, Jan S. Kramer, Steffen Brunst, Victor Hernandez-Olmos, Jan Heering, Simone Schierle, Roxane- Kestner, Franziska M. Mayser, Moritz Helmstaedter, Tamara Goebel, Lilia Weizel, Dmitry Namgaladze, Astrid Kaiser, Dieter Steinhilber, Waltraud Pfeilschifter, Astrid S. Kahnt, Anna Proschak, Apirat Chaikuad, Stefan Knapp, Daniel Merk, Ewgenij Proschak
Summary: The synergistic effect of dual partial PPAR agonist/sEH inhibitor shows promise in combating metabolic syndrome, while avoiding the adverse effects of full PPAR activation. Through structure-activity relationship studies and crystal structure analysis, successful optimization of the designed drug was achieved, resulting in compounds with potential application in patients with MetS.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Shaza H. H. Aly, Ahmed M. M. Elissawy, Abdulla M. A. Mahmoud, Fatma Sa'eed El-Tokhy, Sherif S. Abdel Mageed, Hadia Almahli, Sara T. T. Al-Rashood, Faizah A. A. Binjubair, Mahmoud A. El Hassab, Wagdy M. M. Eldehna, Abd El-Nasser B. Singab
Summary: In this study, flavonoid-rich fractions of Glycyrrhiza glabra roots and Sophora japonica leaves were prepared and their compositions were analyzed. The wound healing potential of these fractions was evaluated, and it was found that the topical application of the fractions significantly increased wound healing and reduced oxidative stress. Molecular docking studies also revealed that the major compounds in the fractions could efficiently bind to proteins related to wound healing. Therefore, Glycyrrhiza glabra roots and Sophora japonica leaves may serve as a rich source of bioactive metabolites with antioxidant, anti-inflammatory, and wound healing properties.
Article
Agriculture, Dairy & Animal Science
Laya Pourazadi, Mohsen Sharafi, Mohammad Amir Karimi Torshizi, Abdolhossein Shahverdi, AliReza Alizadeh
Summary: This study investigated the effects of pioglitazone on aged broiler breeder roosters and found that pioglitazone supplementation improved sperm motility, mitochondrial activity, and apoptosis rates. These improvements were associated with the receptor-independent actions of pioglitazone, and the mechanism of action of pioglitazone was not affected by the PPAR-γ receptor in broiler breeder roosters.
Article
Agricultural Engineering
Saimijiang Yaermaimaiti, Tao Wu, Haji Akber Aisa
Summary: This study isolated bioactive phenolic compounds with strong antioxidant and antimicrobial activities from the fruits of Cordia dichotoma, some of which also showed moderate antiviral activity. These compounds, including newly discovered ones, could potentially serve as preservatives in the food industry due to their potent bioactivity.
INDUSTRIAL CROPS AND PRODUCTS
(2021)
Article
Plant Sciences
Janice Mani, Joel Johnson, Holly Hosking, Beatriz E. Hoyos, Kerry B. Walsh, Paul Neilsen, Mani Naiker
Summary: This study selected five native Australian plants for screening, with Kakadu plum flesh extract showing the highest total phenolic content and antioxidant capacity. Extracts from Gumbi gumbi and Kakadu plum seeds exhibited significant cell inhibition in multiple cancer cell lines, indicating potential for further research.
Article
Chemistry, Multidisciplinary
Mina Maddah, Roodabeh Bahramsoltani, Nafiseh Hoseini Yekta, Roja Rahimi, Rasoul Aliabadi, Mahdi Pourfath
Summary: The study evaluated the in silico interaction of main licorice components against SARS-CoV-2 infection, and identified six licorice compounds as promising antiviral phytochemicals. Molecular dynamics simulations showed glycyrrhizic acid to have the highest affinity to all targets. The results suggest licorice as a promising substance with potential antiviral properties in SARS-CoV-2 infection, particularly glycyrrhizic acid.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Biology
Keisuke Kitakaze, Hanif Ali, Raiki Kimoto, Yasuhiro Takenouchi, Hironobu Ishimaru, Atsushi Yamashita, Natsuo Ueda, Tamotsu Tanaka, Yasuo Okamoto, Kazuhito Tsuboi
Summary: Human GDE7 is found to possess cPA-producing activity in both living cells and cell-free system, with the active site directed towards the luminal side of the ER. GDE7 suppresses the PPAR gamma pathway, suggesting that cPA functions as an intracellular lipid mediator. These findings help to better understand the biological role of GDE7 and its product, cPA.
COMMUNICATIONS BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Marina Naldi, Gloria Brusotti, Gabriella Massolini, Vincenza Andrisano, Caterina Temporini, Manuela Bartolini
Summary: A combination of techniques was used to isolate phytochemicals with anticholinesterase activity from Phyllanthus muellarianus. Magnoflorine and nitidine were identified as active components from different subfractions and showed potent inhibitory effects on cholinesterases. Nitidine demonstrated comparable potency to the commercial anti-Alzheimer drug galanthamine and also showed weak antiaggregating activity against amyloid-beta self-aggregation.
Article
Multidisciplinary Sciences
Kaustubh Wagh, Diana A. Stavreva, Rikke A. M. Jensen, Ville Paakinaho, Gregory Fettweis, R. Louis Schiltz, Daniel Wustner, Susanne Mandrup, Diego M. Presman, Arpita Upadhyaya, Gordon L. Hager
Summary: Using single-molecule tracking and machine learning, researchers found that histone H2B and multiple chromatin-bound transcriptional regulators have two distinct low-mobility states. Ligand activation increases the binding ability of steroid receptors in the lowest-mobility state. The results reveal common pathways for transcription activation in mammalian cells.
Article
Pharmacology & Pharmacy
Lei Ma, Yuling Lian, Junyuan Tang, Fangyuan Chen, Hui Gao, Zhi Zhou, Ning Hou, Wei Yi
Summary: This study identified FN as a potential anti-diabetic and anti-NAFLD drug, which exerts its effects through promoting beneficial protein expression, inhibiting inflammatory genes, and blocking key phosphorylation reactions. FN has the potential to be a candidate drug for clinical use in the future.
PHARMACOLOGICAL RESEARCH
(2021)
Review
Pharmacology & Pharmacy
Yusaku Miyamae
Summary: PPARγ is a nuclear receptor superfamily member that regulates the transcription of various genes involved in lipid and glucose metabolism, inflammation, and cell proliferation. Its functions are primarily controlled by binding of small molecule ligands to the ligand-binding domain, which contains a large cavity that can be occupied by different classes of compounds.
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2021)
Article
Food Science & Technology
Hongkun Xue, Jiaqi Tan, Xiaohan Zhu, Qian Li, Jintian Tang, Xu Cai
Summary: An effective method for selecting active compounds from cranberry was established using counter-current fractionation and bioassay-guided separation. The compound delphinidin-3-glucoside (D3G) showed the highest alpha-glucosidase inhibitory activity. D3G was found to interact with alpha-glucosidase through hydrophobic interactions, leading to changes in the enzyme's secondary structure, providing new insights into their interaction.
LWT-FOOD SCIENCE AND TECHNOLOGY
(2021)
Article
Chemistry, Medicinal
Hiroyuki Kojima, Ryota Yanagi, Eri Higuchi, Mami Yoshizawa, Tomoyuki Shimodaira, Misaki Kumagai, Tatsuhiro Kyoya, Miyu Sekine, Daichi Egawa, Nami Ohashi, Hiroaki Ishida, Keiko Yamamoto, Toshimasa Itoh
Summary: This article presents a screening approach using HDX-MS to identify covalent modifiers. HDX-MS was able to differentiate between true covalent ligands and PAINS. The study identified ligands for PPAR gamma and vitamin D receptor and discovered iodoacetic acid as a novel covalent modifier for stabilizing PPAR gamma-LBD.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
