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Structural and mechanistic insights into the precise product synthesis by a bifunctional miltiradiene synthase.
Plant Biotechnol J
January 2023
National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, China.
Selaginella moellendorffii miltiradiene synthase (SmMDS) is a unique bifunctional diterpene synthase (diTPS) that catalyses the successive cyclization of (E,E,E)-geranylgeranyl diphosphate (GGPP) via (+)-copalyl diphosphate (CPP) to miltiradiene, which is a crucial precursor of important medicinal compounds, such as triptolide, ecabet sodium and carnosol. Miltiradiene synthetic processes have been studied in monofunctional diTPSs, while the precise mechanism by which active site amino acids determine product simplicity and the experimental evidence for reaction intermediates remain elusive. In addition, how bifunctional diTPSs work compared to monofunctional enzymes is attractive for detailed research.
View Article and Find Full Text PDFEvaluating the mucoprotective effect of polydeoxyribonucleotide against indomethacin-induced gastropathy via the MAPK/NF-κB signaling pathway in rats.
Eur J Pharmacol
May 2020
Department of Internal Medicine, Kyung Hee University Hospital at Gangdong, College of Medicine, Kyung Hee University, Seoul, 05278, Republic of Korea. Electronic address:
Non-steroidal anti-inflammatory drugs (NSAIDs) cause gastric mucosal damage and gastric ulceration. Among the most commonly used NSAIDs, indomethacin upregulates mucosal tumor necrosis factor-α, which activates nuclear factor-kappa B (NF-κB), and mitogen-activated protein kinases (MAPK) to induce various pro-inflammatory mediators. Polydeoxyribonucleotide (PDRN) is an adenosine A receptor agonist that exerts anti-inflammatory effects.
View Article and Find Full Text PDFRisk of post-stroke pneumonia with proton pump inhibitors, H2 receptor antagonists and mucoprotective agents: A retrospective nationwide cohort study.
PLoS One
January 2020
Department of Neurology, Gangnam Severance Hospital, Yonsei University College of Medicine, Seoul, Korea.
Stroke patients are at high risk of developing pneumonia, which is major cause of post-stroke mortality. Proton pump inhibitors and H2 receptor antagonists are anti-ulcer drugs, which may predispose to the development of pneumonia by suppression of the gastric acid with bactericidal activity. Unlike proton pump inhibitors and H2 receptor antagonists, mucoprotective agents have gastroprotective effects with no or less anti-acid property.
View Article and Find Full Text PDFPreventive effect of ecabet sodium on low-dose aspirin-induced small intestinal mucosal injury: a randomized, double-blind, pilot study.
BMC Gastroenterol
January 2019
Second Department of Internal Medicine, Osaka Medical College, 2-7 Daigaku-Machi, Takatsuki, Osaka, 569-8686, Japan.
Background: We aimed to investigate how high-dose ecabet sodium affects low-dose aspirin-induced small intestinal mucosal injury in healthy volunteers.
Methods: Healthy volunteers were enrolled randomly into one of two groups with the following drug regimens for 2 weeks: group A, low-dose aspirin once per day and group B, low-dose aspirin and 4.0 g of ecabet sodium.
Preparation, Characterization, and Release of Chitosan-Ecabet Electrolyte Complex for the Mucosal Delivery.
J Nanosci Nanotechnol
February 2019
College of Pharmacy, Inje University, Gimhae 50834, Republic of Korea.
Ecabet has a mucosal protection and anti effect only by local action in the gastric mucous layer, due to an extremely poor absorption into the systemic blood circulation. The aim of the present work was to develop chitosan-ecabet electrolyte complex (ChE) for the enhanced mucosal drug delivery. ChEs were prepared with various ecabet-chitosan concentration ratios.
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