Article
Biochemistry & Molecular Biology
Lorenza Marinaccio, Azzurra Stefanucci, Giuseppe Scioli, Alice Della Valle, Gokhan Zengin, Angelo Cichelli, Adriano Mollica
Summary: This review provides an overview of the latest advancements in peptide human neutrophil elastase inhibitors isolated from natural sources, including their identification, structures, and mechanisms of action. These inhibitors play a significant role in the development of potent bioactive compounds.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Medicine, Research & Experimental
Paul J. Hanson, Felicia Liu-Fei, Coco Ng, Taylor A. Minato, Chi Lai, Al Rohet Hossain, Rebecca Chan, Bobby Grewal, Harpreet Rai, Jeremy Hirota, Daniel R. Anderson, Stanley J. Radio, Bruce M. McManus
Summary: As the COVID-19 pandemic continues, it becomes evident that the heart is a critical target of injury. This study explored the mechanisms of COVID-19-associated heart damage using tissue samples from 21 COVID-19-positive deceased individuals. The findings suggest that elevated levels of neutrophil extracellular traps (NETs) and von Willebrand factor are defining features of direct and indirect viral-related heart injury.
LABORATORY INVESTIGATION
(2022)
Article
Hematology
Evelien G. G. Sprenkeler, Ines Goetschalckx, Sara Fernandez Hermira, Anton T. J. Tool, Mark Hoogenboezem, Robin van Bruggen, Taco W. Kuijpers
Summary: Activated eosinophils do not form eosinophil extracellular traps (EETs) like neutrophils form neutrophil extracellular traps (NETs) due to the natural absence of neutrophil elastase (NE)-like proteolytic activity in eosinophils.
Review
Biochemistry & Molecular Biology
Katarzyna Jakimiuk, Jakub Gesek, Atanas G. Atanasov, Michal Tomczyk
Summary: Elastase inhibitors can prevent the development of various diseases, and some derivatives of flavonoids can influence its action.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Jessica Basso, Jimin Zhang, Daniel Lasala, Sasha J. Rose, Kuan-Ju Chen, David Cipolla
Summary: This study compares two methods for extracting neutrophil serine proteases (NSPs) and finds that the NP40 cell pellet extraction method is more effective in extracting active NSPs compared to the zymosan stimulation method.
Article
Multidisciplinary Sciences
Qian Ou, Jia-qi Fang, Zhe-sheng Zhang, Zhe Chi, Jie Fang, Di-yan Xu, Kai-zhong Lu, Meng-qing Qian, Da-yong Zhang, Jun-ping Guo, Wei Gao, Na-ru Zhang, Jian-ping Pan
Summary: TcpC is a well-characterized multifunctional virulence factor expressed by uropathogenic Escherichia coli. In addition to its known functions, TcpC also inhibits neutrophil NETosis by promoting the degradation of PAD4 through its E3 ligase functionality, revealing an additional immune evasion mechanism of this bacterially derived virulence factor.
NATURE COMMUNICATIONS
(2021)
Article
Immunology
Yali Sun, Xianfei Ding, Yuqing Cui, Hongyi Li, Dong Wang, Huoyan Liang, Shaohua Liu, Xiaojuan Zhang, Haixu Wang, Tongwen Sun
Summary: This study demonstrates that the administration of Sivelestat in septic rats can improve survival, gut microbiota composition, and associated metabolites, providing new options for sepsis treatment.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Angelique Rivot, Natacha Jugniot, Samuel Jacoutot, Nicolas Vanthuyne, Philippe Massot, Philippe Mellet, Sylvain R. A. Marque, Gerard Audran, Pierre Voisin, Marie Delles, Gilles Devouassoux, Eric Thiaudiere, Abderrazzak Bentaher, Elodie Parzy
Summary: The study suggests using OMRI in mice to evaluate protease activity in the lungs, finding an increase in proteolysis in LPS-induced inflammation. This preclinical detection method may open new avenues for diagnosis and in vivo antiprotease testing.
Article
Biochemistry & Molecular Biology
Jeong Ho Kim, Yeong Jun Ban, Aizhamal Baiseitova, Marie Merci Nyiramana, Sang Soo Kang, Dawon Kang, Ki Hun Park
Summary: This study explored anti-inflammatory phytochemicals from B. chinensis by isolating iridal-type triterpenoids with inhibitory effects on pro-inflammatory enzyme HNE and anti-inflammatory activities. The compounds displayed reversible noncompetitive inhibition against HNE and significant anti-inflammatory effects by suppressing pro-inflammatory cytokine expressions through the NF-κB pathway. This is the first report indicating iridal-type triterpenoids as responsible phytochemicals for the anti-inflammatory effects of B. chinensis.
Article
Biochemistry & Molecular Biology
Xiaojie Chu, Zehua Sun, Du-San Baek, Wei Li, John W. Mellors, Steven D. Shapiro, Dimiter S. Dimitrov
Summary: The study identified two high-affinity, specific, and noncompetitive anti-NE antibodies from human libraries, which can effectively inhibit NE enzymatic activity and have potential for antibody-based immunotherapy for cancer and inflammatory diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Yingjun Cui, Mengyi Zhang, Honglei Xu, Tingrong Zhang, Songming Zhang, Xiuhe Zhao, Peng Jiang, Jing Li, Baijun Ye, Yuanjun Sun, Mukuo Wang, Yangping Deng, Qing Meng, Yang Liu, Qiang Fu, Jianping Lin, Liang Wang, Yue Chen
Summary: Acute lung injury/acute respiratory distress syndrome (ALI/ARDS) is a common complication in COVID-19. The natural macrocyclic peptide CTL-A has been identified as a potential elastase inhibitor for preventing ALI/ARDS. The first total synthesis of CTL-A was achieved in 24 steps, and preliminary structure-activity relationships were elucidated. In vivo studies using an ALI mouse model demonstrated that CTL-A effectively alleviated acute lung injury, outperforming the approved elastase inhibitor sivelestat. The findings highlight the potential of CTL-A as a candidate for COVID-19 pathogenesis.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Thomas C. Harper, Elaine M. Oberlick, Tomas J. Smith, Duncan E. Nunes, Mark-Anthony Bray, Seonmi Park, Corey D. Driscoll, Sarah F. Mowbray, Christophe Antczak
Summary: Researchers improved the differentiation of human pluripotent stem cell-derived neutrophils by deleting GATA1 and CYBB molecules, making them more similar to primary neutrophils. These improved neutrophils can be used as a more accurate model to study various diseases, including COVID-19.
Article
Biochemistry & Molecular Biology
Ik Soo Lee, Yu-Ri Lee, Jea Heon Sim, Ki Mo Kim, Young Sook Kim
Summary: 1-O-acetylbritannilactone (ABL), a natural sesquiterpene lactone, was isolated from the flowers of Inula britannica during a search for natural inflammatory inhibitors. ABL exhibited significant inhibitory effects on human neutrophil elastase (HNE) and the production of nitric oxide and prostaglandin E-2. The anti-inflammatory effects of ABL were confirmed using a zebrafish larval model.
Article
Biochemistry & Molecular Biology
Beata Donarska, Marta Switalska, Joanna Wietrzyk, Wojciech Plazinski, Magdalena Mizerska-Kowalska, Barbara Zdzisinska, Krzysztof Z. Laczkowski
Summary: A series of 3,3-diethylazetidine-2,4-dione based thiazoles were synthesized as new human neutrophil elastase inhibitors, exhibiting high inhibitory activity and stability, as well as broad-spectrum antiproliferative activity against various cancer cell lines. These findings suggest their potential in cancer treatment and other immunoreactive diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Ramachandran Vidhya, Velmurugan Ilavarasi Anbumani, Ampasala Dinakara Rao, Carani Venkatraman Anuradha
Summary: In this study, potential dietary phytochemicals that can target the active site of HNE were identified using computational methods and in vitro inhibition assay. Troxerutin (TX) showed the best binding efficacy with HNE among the hit candidates, indicating its potential as a safe and affordable therapy for inflammatory diseases.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
