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Total 71 results found since Jan 2013.

Metformin derivatives - Researchers' Friends or Foes?
Biochem Pharmacol. 2023 Aug 15:115743. doi: 10.1016/j.bcp.2023.115743. Online ahead of print.ABSTRACTMetformin has been used for ages to treat diabetes mellitus due to its safety profile and low cost. However, metformin has variable pharmacokinetics in patients, and due to its poor oral absorption, the therapeutic doses are relatively high, causing unpleasant gastrointestinal adverse effects. Therefore, novel derivatives of metformin have been synthesized during the past decades. Particularly, after the mid-2000s, when organic cation transporters were identified as the main metformin carriers, metformin derivatives have be...
Source: Biochemical Pharmacology - August 17, 2023 Category: Drugs & Pharmacology Authors: Sema Tuna Torunoglu Agnieszka Zajda Janne Tampio Magdalena Markowicz-Piasecka Kristiina M Huttunen Source Type: research

Tracking contaminants of concern in wet-weather sanitary sewer overflows
The objective was to identify the risks posed by sewage contaminants to aquatic biota in the receiving waters, to aid in prioritising management actions. Twelve organic contaminants were identified in influents across the four sites under rainfall ingress diluted conditions, with measurements showing that the highest concentrations were restricted to the anti-inflammatory acetaminophen and the diabetes medication metformin. Lesser contaminants included theobromine, ibuprofen, sucralose, and three benzotriazoles (mainly 1-H benzotriazole). An assessment of the toxicity of the identified organic chemicals indicated that none...
Source: Environmental Science and Pollution Research International - August 15, 2023 Category: Environmental Health Authors: Colin H Besley Graeme E Batley Michele Cassidy Source Type: research

Inhibition of multiple uptake transporters in cardiomyocytes/mitochondria alleviates doxorubicin-induced cardiotoxicity
In conclusion, our study clarified the role of multiple transporters, especially OCTN2, in DOX uptake in cardiomyocytes/mitochondria; metformin alleviated DOX-induced cardiotoxicity without compromising its antitumor efficacy by selective inhibition of multiple transporters mediated DOX accumulation in myocardium/mitochondria.PMID:37453608 | DOI:10.1016/j.cbi.2023.110627
Source: Chemico-Biological Interactions - July 15, 2023 Category: Molecular Biology Authors: Yaodong Yi Hengbin Zhang Mingyang Chen Binxin Chen Yingchun Chen Ping Li Hui Zhou Zhiyuan Ma Huidi Jiang Source Type: research

Photocatalytic and Electrochemical Borylation and Silylation Reactions
Chem Rec. 2023 Jun 26:e202300172. doi: 10.1002/tcr.202300172. Online ahead of print.ABSTRACTDue to their high versatility borylated and silylated compounds are inevitable synthons for organic chemists. To escape the classical hydroboration/hydrosilylation paradigm, chemists turned their attention to more modern and green methods such as photoredox chemistry and electrosynthesis. This account focuses on novel methods for the generation of boryl and silyl radicals to forge C-B and C-Si bonds from our group.PMID:37358334 | DOI:10.1002/tcr.202300172
Source: Chemical Record - June 26, 2023 Category: Chemistry Authors: Tony Biremond Margaux Riomet Philippe Jubault Thomas Poisson Source Type: research

In vitro validation of an in vivo phenotyping drug cocktail for major drug transporters in humans
CONCLUSION: The inhibition of hOCT2 in vitro by sitagliptin is in agreement with the borderline inhibition of renal metformin elimination observed clinically, supporting a dose reduction of sitagliptin in the cocktail.PMID:37142000 | DOI:10.1016/j.ejps.2023.106459
Source: European Journal of Pharmaceutical Sciences - May 4, 2023 Category: Drugs & Pharmacology Authors: Chih-Hsuan Hsin Annett Kuehne Yi Gu Gabriele Jedlitschky Yohannes Hagos Dirk Gr ündemann Uwe Fuhr Source Type: research

Strong inhibition of organic cation transporter 2 by flavonoids and attenuation effects on cisplatin-induced cytotoxicity
In this study, we aimed to identify flavone derivatives with strong inhibitory effects on OCT2 transport. Among the 80 flavonoids tested, 24 showed moderate to strong inhibitory effects against OCT2 transport activity. The IC50 values were less than 5 μM for 10 flavonoids. All 10 compounds alleviated cisplatin-induced cytotoxicity in cells expressing OCT2, even though the magnitude of the effects varied depending on the functional moieties in each position. Multiple factor analysis revealed that the methyl group at the R1 position and methoxy group at the R6 position of the flavonol backbone are important for OCT2 inhibit...
Source: Chemico-Biological Interactions - April 21, 2023 Category: Molecular Biology Authors: Kwang-Hee Shin Kyeong-Ryoon Lee Min-Ji Kang Yoon-Jee Chae Source Type: research