Empagliflozin and colchicine in patients with reduced left ventricular ejection fraction following ST-elevation myocardial infarction: a randomized, double-blinded, three-arm parallel-group, controlled trial
ConclusionThis study showed that neither the combination treatment of empagliflozin 10 mg/day with colchicine nor the monotherapy of empagliflozin 25 mg/day was superior to empagliflozin 10 mg/day in terms of changes in clinical, inflammatory, and echocardiographic outcome parameters in patients with recent MI with reduced LVEF over 3 months. Further studies are warranted to confirm the findings.Trial registrationClinical trial ID: IRCT20111206008307N39. Registration date: 27 October 2022.https://www.irct.ir/trial/66216 (Source: European Journal of Clinical Pharmacology)
Source: European Journal of Clinical Pharmacology - October 28, 2023 Category: Drugs & Pharmacology Source Type: research
The discovery of water-soluble indazole derivatives as potent microtubule polymerization inhibitors
Eur J Med Chem. 2023 Oct 18;262:115870. doi: 10.1016/j.ejmech.2023.115870. Online ahead of print.ABSTRACTTaking a previously discovered indazole derivative 1 as a lead, systematic structural modifications were performed with an indazole core at the 1- and 6-positions to improve its aqueous solubility. Among the designed indazole derivatives, 6-methylpyridin-3-yl indazole derivative 8l and 1H-indol-4-yl indazole derivative 8m exhibited high potency in the low nanomolar range against A549, Huh-7, and T24 cancer cells, including Taxol-resistant variant cells (A549/Tax). As a hydrochloride salt, 8l exhibited much improved aque...
Source: European Journal of Medicinal Chemistry - October 27, 2023 Category: Chemistry Authors: Ying-Jie Cui Yi Zhou Xi-Wu Zhang Bao-Kai Dou Chen-Chen Ma Jing Zhang Source Type: research
The discovery of water-soluble indazole derivatives as potent microtubule polymerization inhibitors
Eur J Med Chem. 2023 Oct 18;262:115870. doi: 10.1016/j.ejmech.2023.115870. Online ahead of print.ABSTRACTTaking a previously discovered indazole derivative 1 as a lead, systematic structural modifications were performed with an indazole core at the 1- and 6-positions to improve its aqueous solubility. Among the designed indazole derivatives, 6-methylpyridin-3-yl indazole derivative 8l and 1H-indol-4-yl indazole derivative 8m exhibited high potency in the low nanomolar range against A549, Huh-7, and T24 cancer cells, including Taxol-resistant variant cells (A549/Tax). As a hydrochloride salt, 8l exhibited much improved aque...
Source: European Journal of Medicinal Chemistry - October 27, 2023 Category: Chemistry Authors: Ying-Jie Cui Yi Zhou Xi-Wu Zhang Bao-Kai Dou Chen-Chen Ma Jing Zhang Source Type: research
Design, synthesis and biological evaluation of novel dihydroquinolin-4(1H)-one derivatives as novel tubulin polymerization inhibitors
Eur J Med Chem. 2023 Oct 15;262:115881. doi: 10.1016/j.ejmech.2023.115881. Online ahead of print.ABSTRACTA series of novel dihydroquinolin-4(1H)-one derivatives targeting colchicine binding site on tubulin were designed, synthesized and evaluated as anticancer agents. The most potent compound 6t showed remarkable antiproliferative activities against four cancer cell lines with IC50 values among 0.003-0.024 μM and tubulin polymerization inhibitory activity (IC50 = 3.06 μM). Further mechanism studies revealed that compound 6t could induce K562 cells apoptosis and arrest at the G2/M phase. Meanwhile, 6t significantly inhibi...
Source: European Journal of Medicinal Chemistry - October 26, 2023 Category: Chemistry Authors: Yuchen Tan Han Hu Wenjian Zhu Tao Wang Tian Gao Hongqi Wang Jian Chen Jinyi Xu Shengtao Xu Huajian Zhu Source Type: research
Localized delivery of anti-inflammatory agents using extracellular matrix-nanostructured lipid carriers hydrogel promotes cardiac repair post-myocardial infarction
In conclusion, ECM-NLC hydrogel is a potential platform for sustained and localized delivery of biomolecules into the heart, and loading appropriate medicines further increases the therapeutic efficacy of ECM-NLC hydrogel for cardiovascular diseases.PMID:37883909 | DOI:10.1016/j.biomaterials.2023.122364 (Source: Biomaterials)
Source: Biomaterials - October 26, 2023 Category: Materials Science Authors: Xinming Wang Hongpeng Shi Shixing Huang Yecen Zhang Xiaojun He Qiang Long Bei Qian Yiming Zhong Zhaoxi Qi Qiang Zhao Xiaofeng Ye Source Type: research
Localized delivery of anti-inflammatory agents using extracellular matrix-nanostructured lipid carriers hydrogel promotes cardiac repair post-myocardial infarction
In conclusion, ECM-NLC hydrogel is a potential platform for sustained and localized delivery of biomolecules into the heart, and loading appropriate medicines further increases the therapeutic efficacy of ECM-NLC hydrogel for cardiovascular diseases.PMID:37883909 | DOI:10.1016/j.biomaterials.2023.122364 (Source: Biomaterials)
Source: Biomaterials - October 26, 2023 Category: Materials Science Authors: Xinming Wang Hongpeng Shi Shixing Huang Yecen Zhang Xiaojun He Qiang Long Bei Qian Yiming Zhong Zhaoxi Qi Qiang Zhao Xiaofeng Ye Source Type: research
NLRP12-associated autoinflammatory disease: much more than the FCAS phenotype
CONCLUSIONS: In conclusion, the disease can cause effects on various tissues, especially the musculoskeletal and gastrointestinal systems, apart from FCAS symptoms. We think that a patient who can be defined as syndrome of undifferentiated recurrent fever should also be evaluated genetically in terms of NLRP12 previously.PMID:37877365 | DOI:10.55563/clinexprheumatol/kzggp3 (Source: Clinical and Experimental Rheumatology)
Source: Clinical and Experimental Rheumatology - October 25, 2023 Category: Rheumatology Authors: Ferhat Demir Bet ül Sözeri Source Type: research
NLRP12-associated autoinflammatory disease: much more than the FCAS phenotype
CONCLUSIONS: In conclusion, the disease can cause effects on various tissues, especially the musculoskeletal and gastrointestinal systems, apart from FCAS symptoms. We think that a patient who can be defined as syndrome of undifferentiated recurrent fever should also be evaluated genetically in terms of NLRP12 previously.PMID:37877365 | DOI:10.55563/clinexprheumatol/kzggp3 (Source: Clinical and Experimental Rheumatology)
Source: Clinical and Experimental Rheumatology - October 25, 2023 Category: Rheumatology Authors: Ferhat Demir Bet ül Sözeri Source Type: research
Colchicine promotes atherosclerotic plaque stability independently of inflammation
bioRxiv. 2023 Oct 3:2023.10.03.560632. doi: 10.1101/2023.10.03.560632. Preprint.ABSTRACTAtherosclerosis is a chronic inflammatory disease which is driven in part by the aberrant trans -differentiation of vascular smooth muscle cells (SMCs). No therapeutic drug has been shown to reverse detrimental SMC-derived cell phenotypes into protective phenotypes, a hypothesized enabler of plaque regression and improved patient outcome. Herein, we describe a novel function of colchicine in the beneficial modulation of SMC-derived cell phenotype, independent of its conventional anti-inflammatory effects. Using SMC fate mapping in an ad...
Source: Atherosclerosis - October 24, 2023 Category: Cardiology Authors: Weizhen Li Alexander Lin Michael Hutton Harkirat Dhaliwal James Nadel Julie Rodor Sergey Tumanov Tiit Örd Matthew Hadden Michal Mokry Barend M Mol Gerard Pasterkamp Matthew P Padula Carolyn L Geczy Yogambha Ramaswamy Judith C Sluimer Minna U Kaikkonen Ro Source Type: research
Colchicine promotes atherosclerotic plaque stability independently of inflammation
bioRxiv. 2023 Oct 3:2023.10.03.560632. doi: 10.1101/2023.10.03.560632. Preprint.ABSTRACTAtherosclerosis is a chronic inflammatory disease which is driven in part by the aberrant trans -differentiation of vascular smooth muscle cells (SMCs). No therapeutic drug has been shown to reverse detrimental SMC-derived cell phenotypes into protective phenotypes, a hypothesized enabler of plaque regression and improved patient outcome. Herein, we describe a novel function of colchicine in the beneficial modulation of SMC-derived cell phenotype, independent of its conventional anti-inflammatory effects. Using SMC fate mapping in an ad...
Source: Atherosclerosis - October 24, 2023 Category: Cardiology Authors: Weizhen Li Alexander Lin Michael Hutton Harkirat Dhaliwal James Nadel Julie Rodor Sergey Tumanov Tiit Örd Matthew Hadden Michal Mokry Barend M Mol Gerard Pasterkamp Matthew P Padula Carolyn L Geczy Yogambha Ramaswamy Judith C Sluimer Minna U Kaikkonen Ro Source Type: research
Targeting residual inflammatory risk: The next frontier for atherosclerosis treatment and prevention
Vascul Pharmacol. 2023 Oct 21:107238. doi: 10.1016/j.vph.2023.107238. Online ahead of print.ABSTRACTInflammation and hyperlipidemia act synergistically to drive atherosclerotic progression. Multiple randomized trials now demonstrate that "lower is better" not only for LDLC, but also for hsCRP. Recent data among statin treated patients indicates that residual inflammatory risk is a stronger determinant of recurrent events than residual cholesterol risk. Based on trial data demonstrating a 31% reduction in events with minimal side effects, low-dose colchicine (0.5 mg daily) has been approved by the United States Food and Dru...
Source: Atherosclerosis - October 23, 2023 Category: Cardiology Authors: Paul M Ridker Source Type: research
Targeting residual inflammatory risk: The next frontier for atherosclerosis treatment and prevention
Vascul Pharmacol. 2023 Oct 21:107238. doi: 10.1016/j.vph.2023.107238. Online ahead of print.ABSTRACTInflammation and hyperlipidemia act synergistically to drive atherosclerotic progression. Multiple randomized trials now demonstrate that "lower is better" not only for LDLC, but also for hsCRP. Recent data among statin treated patients indicates that residual inflammatory risk is a stronger determinant of recurrent events than residual cholesterol risk. Based on trial data demonstrating a 31% reduction in events with minimal side effects, low-dose colchicine (0.5 mg daily) has been approved by the United States Food and Dru...
Source: Vascular Pharmacology - October 23, 2023 Category: Drugs & Pharmacology Authors: Paul M Ridker Source Type: research
