Gliflozins in the Treatment of Non-diabetic Experimental Cardiovascular Diseases
Physiol Res. 2024 Apr 18. Online ahead of print.ABSTRACTA new class of antidiabetic drugs - gliflozins (inhibitors of sodium glucose cotransporter-2; SGLT-2i) stimulate glucose and sodium excretion, thereby contributing to improved glycemic control, weight loss and blood pressure reduction in diabetic patients. Large clinical trials in patients with type 2 diabetes treated with empagliflozin, canagliflozin or dapagliflozin have demonstrated their excellent efficacy in improving many cardiovascular outcomes, including the reduction of death from cardiovascular diseases, non-fatal myocardial infarction or stroke, and hospita...
Source: Physiological Research - April 18, 2024 Category: Physiology Authors: I Van ěčková J Zicha Source Type: research
Canagliflozin inhibits PASMCs proliferation via regulating SGLT1/AMPK signaling and attenuates artery remodeling in MCT-induced pulmonary arterial hypertension
Biomed Pharmacother. 2024 Apr 3;174:116505. doi: 10.1016/j.biopha.2024.116505. Online ahead of print.ABSTRACTPulmonary arterial hypertension (PAH) was a devastating disease characterized by artery remodeling, ultimately resulting in right heart failure. The aim of this study was to investigate the effects of canagliflozin (CANA), a sodium-glucose cotransporter 2 inhibitor (SGLT2i) with mild SGLT1 inhibitory effects, on rats with PAH, as well as its direct impact on pulmonary arterial smooth muscle cells (PASMCs). PAH rats were induced by injection of monocrotaline (MCT) (40 mg/kg), followed by four weeks of treatment with ...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 4, 2024 Category: Drugs & Pharmacology Authors: Xiaojun Chen Xing Yu Guili Lian Huibin Tang Yan Yan Gufeng Gao Bangbang Huang Li Luo Liangdi Xie Source Type: research
Canagliflozin inhibits PASMCs proliferation via regulating SGLT1/AMPK signaling and attenuates artery remodeling in MCT-induced pulmonary arterial hypertension
Biomed Pharmacother. 2024 Apr 3;174:116505. doi: 10.1016/j.biopha.2024.116505. Online ahead of print.ABSTRACTPulmonary arterial hypertension (PAH) was a devastating disease characterized by artery remodeling, ultimately resulting in right heart failure. The aim of this study was to investigate the effects of canagliflozin (CANA), a sodium-glucose cotransporter 2 inhibitor (SGLT2i) with mild SGLT1 inhibitory effects, on rats with PAH, as well as its direct impact on pulmonary arterial smooth muscle cells (PASMCs). PAH rats were induced by injection of monocrotaline (MCT) (40 mg/kg), followed by four weeks of treatment with ...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 4, 2024 Category: Drugs & Pharmacology Authors: Xiaojun Chen Xing Yu Guili Lian Huibin Tang Yan Yan Gufeng Gao Bangbang Huang Li Luo Liangdi Xie Source Type: research
Sensitization of cancer cells to paclitaxel-induced apoptosis by canagliflozin
Biochem Pharmacol. 2024 Mar 19:116140. doi: 10.1016/j.bcp.2024.116140. Online ahead of print.ABSTRACTCancer cells consume more glucose and usually overexpress glucose transporters which have become potential targets for the development of anticancer drugs. It has been demonstrated that selective SGLT2 inhibitors, such as canagliflozin and dapagliflozin, display anticancer activity. Here we demonstrated that canagliflozin and dapagliflozin synergistically enhanced the growth inhibitory effect of paclitaxel in cancer cells including ovarian cancer and oral squamous cell carcinoma cells. Canagliflozin also inhibited glucose u...
Source: Biochemical Pharmacology - March 21, 2024 Category: Drugs & Pharmacology Authors: Haoning Huang Fan-Lu Kung Yu-Wen Huang Chun-Chien Hsu Jih-Hwa Guh Lih-Ching Hsu Source Type: research
Synthetic approaches and clinical application of small-molecule inhibitors of sodium-dependent glucose transporters 2 for the treatment of type 2 diabetes mellitus
Eur J Med Chem. 2024 Mar 18;269:116343. doi: 10.1016/j.ejmech.2024.116343. Online ahead of print.ABSTRACTSodium-dependent glucose transporters 2 (SGLT2) inhibitors are a class of small-molecule drugs that have gained significant attention in recent years for their potential clinical applications in the treatment of type 2 diabetes mellitus (T2DM). These inhibitors function by obstructing the kidneys' ability to reabsorb glucose, resulting in a rise in the excretion of glucose in urine (UGE) and subsequently lowering blood glucose levels. Several SGLT2 inhibitors, such as Dapagliflozin, Canagliflozin, and Empagliflozin, hav...
Source: European Journal of Medicinal Chemistry - March 21, 2024 Category: Chemistry Authors: Tong Xie Li-Jie Zhao Source Type: research
Sensitization of cancer cells to paclitaxel-induced apoptosis by canagliflozin
Biochem Pharmacol. 2024 Mar 20;223:116140. doi: 10.1016/j.bcp.2024.116140. Online ahead of print.ABSTRACTCancer cells consume more glucose and usually overexpress glucose transporters which have become potential targets for the development of anticancer drugs. It has been demonstrated that selective SGLT2 inhibitors, such as canagliflozin and dapagliflozin, display anticancer activity. Here we demonstrated that canagliflozin and dapagliflozin synergistically enhanced the growth inhibitory effect of paclitaxel in cancer cells including ovarian cancer and oral squamous cell carcinoma cells. Canagliflozin also inhibited gluco...
Source: Biochemical Pharmacology - March 21, 2024 Category: Drugs & Pharmacology Authors: Haoning Huang Fan-Lu Kung Yu-Wen Huang Chun-Chien Hsu Jih-Hwa Guh Lih-Ching Hsu Source Type: research
Synthetic approaches and clinical application of small-molecule inhibitors of sodium-dependent glucose transporters 2 for the treatment of type 2 diabetes mellitus
Eur J Med Chem. 2024 Mar 18;269:116343. doi: 10.1016/j.ejmech.2024.116343. Online ahead of print.ABSTRACTSodium-dependent glucose transporters 2 (SGLT2) inhibitors are a class of small-molecule drugs that have gained significant attention in recent years for their potential clinical applications in the treatment of type 2 diabetes mellitus (T2DM). These inhibitors function by obstructing the kidneys' ability to reabsorb glucose, resulting in a rise in the excretion of glucose in urine (UGE) and subsequently lowering blood glucose levels. Several SGLT2 inhibitors, such as Dapagliflozin, Canagliflozin, and Empagliflozin, hav...
Source: European Journal of Medicinal Chemistry - March 21, 2024 Category: Chemistry Authors: Tong Xie Li-Jie Zhao Source Type: research
Adherence to newer second ‐line oral antidiabetic drugs among people with type 2 diabetes—A systematic review
The adherence to newer second-line oral antidiabetic drugs among people with type 2 diabetes was investigated in this study. A systematic literature search was performed in six databases. A total of 14948 records was retrieved from the databases of which 7 articles were included. The reported medication possession ratio (MPR) and treatment discontinuation was extracted from the articles, and these findings were visualised in figures and summarized in a narrative synthesis. The findings indicate that the adherence to the newer second-line OADs may be better than that of older OADs, but a study directly comparing older and n...
Source: Pharmacology Research and Perspectives - March 7, 2024 Category: Drugs & Pharmacology Authors: Nynne Sophie Holdt ‐Caspersen,
Claus Dethlefsen,
Peter Vestergaard,
Ole Hejlesen,
Stine Hangaard,
Morten Hasselstrøm Jensen Tags: REVIEW Source Type: research
IDF23-0543 Canagliflozin improves renal phenotype and restores beta-cell identity in an early-onset T2D model
(Source: Diabetes Research and Clinical Practice)
Source: Diabetes Research and Clinical Practice - March 1, 2024 Category: Endocrinology Authors: A.I. Popescu, P. Ray, R.C. Bunn, J.L. Fowlkes, K.M. Thrailkill Tags: Other Complications Source Type: research
Implication of M2 macrophage on NLRP3 inflammasome signaling in mediating the neuroprotective effect of Canagliflozin against methotrexate-induced cognitive impairment
This study aimed to investigate CANA's protective effect against MTX-induced cognitive impairment, highlighting the possible involvement of TLR4/ NF-κB crosstalk with NLRP3 inflammasome activation and macrophage polarization. Forty-eight Male Wistar rats were divided into 4 groups; (1) received saline orally for 30 days and intravenously on days 8 and 15. (2) received Canagliflozin (CANA; 20 mg/kg/day; p.o.) for 30 days. (3) received MTX (75 mg/kg, i.v.) on day 8 and 15, then they were injected with four i.p. injections of leucovorin (LCV): the first dose was 6 mg/ kg after 18 h, and the remaining doses were 3 mg/kg after...
Source: International Immunopharmacology - February 20, 2024 Category: Allergy & Immunology Authors: Lobna H Khedr Rania M Rahmo Omar M Eldemerdash Engy M Helmy Felopateer A Ramzy George H Lotfy Habiba A Zakaria Marine M Gad Marina M Youhanna Manar H Samaan Nevert W Thabet Reem H Ghazal Mostafa A Rabie Source Type: research
Canagliflozin protects against hyperglycemia-induced cerebrovascular injury by preventing blood-brain barrier (BBB) disruption via AMPK/Sp1/adenosine A2A receptor
Eur J Pharmacol. 2024 Feb 8:176381. doi: 10.1016/j.ejphar.2024.176381. Online ahead of print.ABSTRACTDiabetes mellitus causes brain microvascular endothelial cell (MEC) damage, inducing dysfunctional angiogenic response and disruption of the blood-brain barrier (BBB). Canagliflozin is a revolutionary hypoglycemic drug that exerts neurologic and/or vascular-protective effects beyond glycemic control; however, its underlying mechanism remains unclear. In the present study, we hypothesize that canagliflozin ameliorates BBB permeability by preventing diabetes-induced brain MEC damage. Mice with high-fat diet/streptozotocin-ind...
Source: European Journal of Pharmacology - February 10, 2024 Category: Drugs & Pharmacology Authors: Zhiyi Liu Wei Hua Sinan Jin Yueying Wang Yuxin Pang Benshuai Wang Nan Zhao Jiping Qi Yuejia Song Source Type: research
Selective sodium-glucose cotransporter-2 inhibitors in the improvement of hemoglobin and hematocrit in patients with type 2 diabetes mellitus: a network meta-analysis
ConclusionBased on the existing studies, we concluded that SGLT2i could increase hematocrit and hemoglobin levels in patients with T2DM, and canagliflozin 100mg had the best effect on the improvement of hematocrit, while canagliflozin 200mg had the best effect on the improvement of hemoglobin.Systematic review registrationhttps://www.crd.york.ac.uk/PROSPERO/#loginpage, identifier PROSPERO (CRD42023477103). (Source: Frontiers in Endocrinology)
Source: Frontiers in Endocrinology - February 1, 2024 Category: Endocrinology Source Type: research
Canagliflozin regulates metabolic reprogramming in diabetic kidney disease by inducing fasting-like and aestivation-like metabolic patterns
Conclusions/interpretationIn conclusion, our study shows that CANA ameliorates DKD by inducing fasting-like and aestivation-like metabolic patterns. Furthermore, DKD was ameliorated by glycine supplementation, and the beneficial effects of glycine were probably due to the activation of the AMPK/mTOR pathway.Graphical Abstract (Source: Diabetologia)
Source: Diabetologia - January 18, 2024 Category: Endocrinology Source Type: research
