Role and regulation of FOXO3a: new insights into breast cancer therapy
Breast cancer is the most common malignancy in the world, particularly affecting female cancer patients. Enhancing the therapeutic strategies for breast cancer necessitates identifying molecular drug targets that effectively eliminate tumor cells. One of these prominent targets is the forkhead and O3a class (FOXO3a), a member of the forkhead transcription factor subfamily. FOXO3a plays a pivotal role in various cellular processes, including apoptosis, proliferation, cell cycle regulation, and drug resistance. It acts as a tumor suppressor in multiple cancer types, although its specific role in cancer remains unclear. Moreo...
Source: Frontiers in Pharmacology - March 4, 2024 Category: Drugs & Pharmacology Source Type: research
Sinomenine protects against atherosclerosis in apolipoprotein E-knockout mice by inhibiting of inflammatory pathway
Inflammopharmacology. 2024 Mar 2. doi: 10.1007/s10787-024-01437-8. Online ahead of print.ABSTRACTAtherosclerosis, a multifaceted and persistent inflammatory condition, significantly contributes to the progression of cardiocerebrovascular disorders, such as myocardial infarctions and cerebrovascular accidents. It involves the accumulation of cholesterol, fatty deposits, calcium and cellular debris in the walls of arteries, leading to the formation of plaques. Our aim is to investigate the potential of sinomenine to counteract atherosclerosis in mice lacking Apolipoprotein E (ApoE-/-) Mice. We employed the high-fat diet-indu...
Source: Atherosclerosis - March 2, 2024 Category: Cardiology Authors: Zhao Gao Chao Yang Guangwei Zeng Ming Lin Wei Li Mengna Sun Yantao Zhang Beibei Fan Yogesh Kumar Kun Yan Source Type: research
Sinomenine protects against atherosclerosis in apolipoprotein E-knockout mice by inhibiting of inflammatory pathway
Inflammopharmacology. 2024 Mar 2. doi: 10.1007/s10787-024-01437-8. Online ahead of print.ABSTRACTAtherosclerosis, a multifaceted and persistent inflammatory condition, significantly contributes to the progression of cardiocerebrovascular disorders, such as myocardial infarctions and cerebrovascular accidents. It involves the accumulation of cholesterol, fatty deposits, calcium and cellular debris in the walls of arteries, leading to the formation of plaques. Our aim is to investigate the potential of sinomenine to counteract atherosclerosis in mice lacking Apolipoprotein E (ApoE-/-) Mice. We employed the high-fat diet-indu...
Source: Atherosclerosis - March 2, 2024 Category: Cardiology Authors: Zhao Gao Chao Yang Guangwei Zeng Ming Lin Wei Li Mengna Sun Yantao Zhang Beibei Fan Yogesh Kumar Kun Yan Source Type: research
Sinomenine protects against atherosclerosis in apolipoprotein E-knockout mice by inhibiting of inflammatory pathway
AbstractAtherosclerosis, a multifaceted and persistent inflammatory condition, significantly contributes to the progression of cardiocerebrovascular disorders, such as myocardial infarctions and cerebrovascular accidents. It involves the accumulation of cholesterol, fatty deposits, calcium and cellular debris in the walls of arteries, leading to the formation of plaques. Our aim is to investigate the potential of sinomenine to counteract atherosclerosis in mice lacking Apolipoprotein E (ApoE −/−) Mice. We employed the high-fat diet-induced method to induce atherosclerosis in ApoE−/− mice, and the mice were treated ...
Source: Inflammopharmacology - March 2, 2024 Category: Drugs & Pharmacology Source Type: research
Pharmacokinetic Evaluation of the CYP3A4 and CYP2C9 Drug ‐Drug Interaction of Avacopan in 2 Open‐Label Studies in Healthy Participants
AbstractAvacopan, a complement 5a receptor (C5aR) antagonist approved for treating severe active antineutrophil cytoplasmic autoantibody (ANCA)-associated vasculitis, was evaluated in 2 clinical drug-drug interaction studies. The studies assessed the impact of avacopan on the pharmacokinetics (PK) of CYP3A4 substrates midazolam and simvastatin and CYP2C9 substrate celecoxib, and the influence of CYP3A4 inhibitor itraconazole and inducer rifampin on the PKs of avacopan. The results indicated that twice-daily oral administration of 30 mg of avacopan increased the area under the curve (AUC) of midazolam by 1.81-fold and cel...
Source: Clinical Pharmacology in Drug Development - March 1, 2024 Category: Drugs & Pharmacology Authors: Shichang Miao,
Pirow Bekker,
Danielle Armas,
Mary Lor,
Yanyan Han,
Kenneth Webster,
Ashit Trivedi Tags: Original Article Source Type: research
Screening of 16 major drug glucuronides for time-dependent inhibition of nine drug-metabolizing CYP enzymes - detailed studies on CYP3A inhibitors
In conclusion, we identified several glucuronide metabolites with CYP inhibitory properties. Based on detailed experiments, the inactivation of CYP3A by carvedilol may cause clinically significant drug-drug interactions.PMID:38423227 | DOI:10.1016/j.ejps.2024.106735 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 29, 2024 Category: Drugs & Pharmacology Authors: Helin ä Kahma Marie-No ëlle Paludetto Mikko Neuvonen Mika Kurkela Anne M Filppula Mikko Niemi Janne T Backman Source Type: research
Screening of 16 major drug glucuronides for time-dependent inhibition of nine drug-metabolizing CYP enzymes - detailed studies on CYP3A inhibitors
In conclusion, we identified several glucuronide metabolites with CYP inhibitory properties. Based on detailed experiments, the inactivation of CYP3A by carvedilol may cause clinically significant drug-drug interactions.PMID:38423227 | DOI:10.1016/j.ejps.2024.106735 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 29, 2024 Category: Drugs & Pharmacology Authors: Helin ä Kahma Marie-No ëlle Paludetto Mikko Neuvonen Mika Kurkela Anne M Filppula Mikko Niemi Janne T Backman Source Type: research
Screening of 16 major drug glucuronides for time-dependent inhibition of nine drug-metabolizing CYP enzymes - detailed studies on CYP3A inhibitors
In conclusion, we identified several glucuronide metabolites with CYP inhibitory properties. Based on detailed experiments, the inactivation of CYP3A by carvedilol may cause clinically significant drug-drug interactions.PMID:38423227 | DOI:10.1016/j.ejps.2024.106735 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 29, 2024 Category: Drugs & Pharmacology Authors: Helin ä Kahma Marie-No ëlle Paludetto Mikko Neuvonen Mika Kurkela Anne M Filppula Mikko Niemi Janne T Backman Source Type: research
Molecules, Vol. 29, Pages 1016: Design, Synthesis and Evaluation of Antioxidant and NSAID Derivatives with Antioxidant, Anti-Inflammatory and Plasma Lipid Lowering Effects
Rekka
Amides containing methyl esters of γ-aminobutyric acid (GABA), L-proline and L-tyrosine, and esters containing 3-(pyridin-3-yl)propan-1-ol were synthesized by conjugation with 3,5-di-tert-butyl-4-hydroxybenzoic, an NSAID (tolfenamic acid), or 3-phenylacrylic (cinnamic, (E)-3-(3,4-dimethoxyphenyl)acrylic and caffeic) acids. The rationale for the conjugation of such moieties was based on the design of structures with two or more molecular characteristics. The novel compounds were tested for their antioxidant, anti-inflammatory and hypolipidemic properties. Several compounds were potent antioxidants, c...
Source: Molecules - February 26, 2024 Category: Chemistry Authors: Panagiotis Theodosis-Nobelos Gabriel Marc Eleni A. Rekka Tags: Article Source Type: research
Colonic spider naevi in a middle-aged man
Introduction A 59-year-old man was seen in outpatient clinic with a 1-year history of abdominal cramping and non-bloody diarrhoea. His only medical history comprised hypercholesterolaemia and oesophagogastric reflux, for which he took simvastatin and lansoprazole. He did not show cutaneous spider naevi and there was no history of liver disease or use of oestrogen or hormone replacement medications. CT of the abdomen and pelvis showed a long segment of moderate sigmoid colonic wall thickening (figure 1A) with perifocal fat stranding and free fluid in keeping with acute sigmoiditis. Feeding vessels were patent with no eviden...
Source: Gut - February 23, 2024 Category: Gastroenterology Authors: Hunter, H., Johnston, A. J., Said, W., Wong, N. A. Tags: GUT Snapshot, Gut Editor ' s quiz: GI snapshot Source Type: research
Skeletal muscle mitochondrial capacity in patients with statin-associated muscle symptoms (SAMS)
CONCLUSIONS: NIRS in the forearm cannot differentiate between confirmed and unconfirmed SAMS, but further research is needed to assess the usability of NIRS as a diagnostic tool for SAMS.TRIAL REGISTRATION NUMBER: NCT03653663.PMID:38388189 | DOI:10.1136/openhrt-2023-002551 (Source: Atherosclerosis)
Source: Atherosclerosis - February 22, 2024 Category: Cardiology Authors: Laura A Mangone Beth A Taylor Robert Schmelzer Sung Gi Noh Michael C White Oh Sung Kwon Paul D Thompson Source Type: research
Cancers, Vol. 16, Pages 853: Statin-Sensitive Akt1/Src/Caveolin-1 Signaling Enhances Oxidative Stress Resistance in Rhabdomyosarcoma
o Sampaolesi
Stefano Gastaldello
Matteo Cassandri
Francesco Marampon
Alessandro Fanzani
Identifying the molecular mechanisms underlying radioresistance is a priority for the treatment of RMS, a myogenic tumor accounting for approximately 50% of all pediatric soft tissue sarcomas. We found that irradiation (IR) transiently increased phosphorylation of Akt1, Src, and Cav1 in human RD and RH30 lines. Synthetic inhibition of Akt1 and Src phosphorylation increased ROS levels in all RMS lines, promoting cellular radiosensitization. Accordingly, the elevated activation of the Akt1/Src/Cav1 pathway, as detected in two ...
Source: Cancers - February 20, 2024 Category: Cancer & Oncology Authors: Silvia Codenotti Leonardo Sandrini Delia Mandracchia Luisa Lorenzi Giovanni Corsetti Maura Poli Michela Asperti Valentina Salvi Daniela Bosisio Eugenio Monti Stefania Mitola Luca Triggiani Michele Guescini Enrico Pozzo Maurilio Sampaolesi Stefano Gastalde Tags: Article Source Type: research
Simvastatin-loaded 3D aerogel scaffolds promote bone regeneration
CONCLUSION: The PLCL/gelatin aerogel scaffold, when loaded with Simvastatin, demonstrates a more pronounced potential in enhancing osteoblast proliferation and osteogenic differentiation. We hypothesize that this scaffold could serve as a promising material for addressing bone defects.PMID:38363602 | DOI:10.3233/BME-230068 (Source: Bio-Medical Materials and Engineering)
Source: Bio-Medical Materials and Engineering - February 16, 2024 Category: Materials Science Authors: Lai Linfeng Zhou Xiaowei Chen Xueqin Zhu Xianfeng Source Type: research
