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Molecules, Vol. 28, Pages 4953: Electrochemical Disposable Biosensor to Monitor Dabigatran in Point-of-Care Anticoagulation Therapy
riero Dabigatran etexilate, an oral prodrug, is often used to treat complications linked to thrombosis. Dabigatran (DAB, active form) does not need to be monitored. However, there are several conditions, such as reduced renal function, traumatic bleeding, emergency surgery, the need for thrombolytic therapy in acute stroke, or the requirement to use other forms of anticoagulation, where knowing the concentration of DAB in the blood is indispensable. Unfortunately, there are no convenient DAB-specific point-of-care tests available. To solve this problem, two disposable sensors were constructed and optimised in this work...
Source: Molecules - June 23, 2023 Category: Chemistry Authors: Ashwin K. V. Mruthunjaya Ronald C. Chatelier Angel A. J. Torriero Tags: Article Source Type: research

Molecules, Vol. 27, Pages 5488: The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke
Kiseleva Vadim V. Negrebetsky Yuri I. Baukov Ischemic stroke triggers a whole cascade of pathological changes in the brain, one of which is postischemic inflammation. Since in such cases thrombolytic therapy is often not possible, methods that modulate inflammation and affect microglia become particularly interesting. We synthesized 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate calcium(II) (Compound 4) and studied its anti-inflammatory activity in in vitro and in vivo models of inflammation and ischemia. Macrophage cell line RAW 264.7 was treated with lipopolysaccharides (LPS) and Compound 4 at various dosa...
Source: Molecules - August 26, 2022 Category: Chemistry Authors: Denis A. Borozdenko Tatiana A. Shmigol Aiarpi A. Ezdoglian Darya I. Gonchar Natalia. Y. Karpechenko Dmitri N. Lyakhmun Anastasia D. Shagina Elvira A. Cherkashova Daria D. Namestnikova Ilya L. Gubskiy Anastasia A. Chernysheva Nina M. Kiseleva Vadim V. Negr Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3407: Targeted Delivery of Plasminogen Activators for Thrombolytic Therapy: An Integrative Evaluation
Tony Wu In thrombolytic therapy, plasminogen activators (PAs) are still the only group of drug approved to induce thrombolysis, and therefore, critical for treatment of arterial thromboembolism, such as stroke, in the acute phase. Functionalized nanocomposites have attracted great attention in achieving target thrombolysis due to favorable characteristics associated with the size, surface properties and targeting effects. Many PA-conjugated nanocomposites have been prepared and characterized, and some of them has been demonstrated with therapeutic efficacy in animal models. To facilitate future translation, this pape...
Source: Molecules - September 18, 2019 Category: Chemistry Authors: Yunn-Hwa Ma Chih-Hsin Liu Yueh Liang Jyh-Ping Chen Tony Wu Tags: Review Source Type: research

Anti-inflammatory Target of a Novel Thrombolytic Stroke Drug Enzymology
Although ischemic stroke is a major cause of death and disability worldwide, only a small fraction of patients benefit from the current thrombolytic therapy due to a risk of cerebral hemorrhage caused by inflammation. Thus, the development of a new strategy to combat inflammation during thrombolysis is an urgent demand. The small molecule thrombolytic SMTP-7 effectively treats ischemic stroke in several animal models with reducing cerebral hemorrhage. Here we revealed that SMTP-7 targeted soluble epoxide hydrolase (sEH) to suppress inflammation. SMTP-7 inhibited both of the two sEH enzyme activities: epoxide hydrolase (whi...
Source: Journal of Biological Chemistry - December 26, 2014 Category: Chemistry Authors: Matsumoto, N., Suzuki, E., Ishikawa, M., Shirafuji, T., Hasumi, K. Tags: Enzymology Source Type: research

Minocycline Repurposing in Critical Illness: Focus on Stroke.
Abstract Stroke is a devastating disease associated with high morbidity and mortality. Despite the approved indication of systemic thrombolytic therapy in the United States for the acute management of ischemic stroke, its use is limited given a strict eligibility criteria and a risk for hemorrhagic transformation as a feared adverse effect. Many agents have been studied without success for neuroprotection in patients with stroke to reduce vascular injury and improve long-term functional outcomes. Minocycline is a tetracycline antibiotic that shows promise for its neuroprotective effects in multiple animal models a...
Source: Current Topics in Medicinal Chemistry - September 20, 2013 Category: Chemistry Authors: Vivian Liao T, C Forehand C, Hess DC, Fagan SC Tags: Curr Top Med Chem Source Type: research