For a new drug delivery system of 5-fluorouracil, we prepared prodrugs possessing certain desired properties. The prodrugs, 1-(N-4-chlorophenyl-N-methylcarbamoyl)-5-fluorouracil and 1-(N-2,4-dichlorophenyl-N-methylcarbamoyl)-5-fluorouracil, contain high serum albumin binding potency and a comparably long half life in the bloodstream in vivo to Tegafur. These two prodrugs are expected to be retained in the bloodstream as a polymeric complex with albumin and to circulate in the body for a long time, like a polymeric prodrug.

Download full-text PDF

Source
http://dx.doi.org/10.1248/bpb.16.876DOI Listing

Publication Analysis

Top Keywords

serum albumin
8
albumin binding
8
binding potency
8
synthesis vitro
4
vitro vivo
4
vivo stability
4
stability 5-fluorouracil
4
prodrugs
4
5-fluorouracil prodrugs
4
prodrugs possess
4

Similar Publications

Introduction: In chronic kidney disease (CKD) patients, elevated parathyroid hormone (PTH) is linked to cardiovascular mortality and morbidity. Levels of PTH are influenced by serum phosphate (P) and calcium (Ca), but little is known about the impact of magnesium (Mg) on PTH. Hence, this study investigated the relationship between PTH and Mg in peritoneal dialysis (PD) patients and non-dialysis patients from three hospitals in China.

View Article and Find Full Text PDF

Oligonucleotide therapeutics, including antisense oligonucleotides and small interfering RNA, offer promising avenues for modulating the expression of disease-associated proteins. However, challenges such as nuclease degradation, poor cellular uptake, and unspecific targeting hinder their application. To overcome these obstacles, spherical nucleic acids have emerged as versatile tools for nucleic acid delivery in biomedical applications.

View Article and Find Full Text PDF

[Meta-analysis of the efficacy of the Fuzheng Huayu formula in the treatment of hepatitis B-associated liver fibrosis or cirrhosis].

Zhonghua Gan Zang Bing Za Zhi

December 2024

Center of Hepatology and Department of Infectious Disease, Jinling Hospital (General Hospital of Eastern Theater Command) Affiliated to School of Medicine, Nanjing University, Nanjing210002, China.

To systematically evaluate the efficacy of Fuzheng Huayu (FZHY) tablets/capsules on hepatitis B-associated liver fibrosis or cirrhosis based on randomized controlled trials (RCTs) in order to provide more accurate evidence-based medicine for clinical rational drug use. Randomized controlled clinical trial research reports related to the treatment of hepatitis B-associated liver fibrosis or cirrhosis with FZHY published in SCI and statistical source core journals were retrieved from databases such as PubMed, Cochrane Library, and China National Knowledge Infrastructure (CNKI). RevMan 5.

View Article and Find Full Text PDF

Gender differences in systemic inflammatory and nutritional index following radical surgery for advanced gastric cancer.

Zhong Nan Da Xue Xue Bao Yi Xue Ban

August 2024

Department of Gastrointestinal Surgery, General Surgery, Xiangya Hospital, Central South University, Changsha 410008.

Objectives: Albumin-globulin ratio (AGR), prognostic nutritional index (PNI), and platelet-to-lymphocyte ratio (PLR) have been validated as prognostic factors for gastric cancer (GC). However, significant gender differences exist in albumin levels and inflammatory cell counts, and further research is required to understand how these differences influence GC prognosis. This study aims to investigate the prognostic impact of nutritional and inflammatory indicators on GC patients undergoing radical surgery, as well as the influence of gender on these indicators' prognostic value.

View Article and Find Full Text PDF

Regulatory role of the mTOR signaling pathway in autophagy and mesangial proliferation in IgA nephropathy.

Zhong Nan Da Xue Xue Bao Yi Xue Ban

August 2024

Department of Nephrology, Second Xiangya Hospital, Central South University, Changsha 410011.

Objectives: IgA nephropathy (IgAN) is the most common primary glomerular disease in China, but its pathogenesis remains unclear. This study aims to explore the regulatory role of the mammalian target of rapamycin (mTOR) signaling pathway in autophagy and mesangial proliferation during renal injury in IgA.

Methods: The activity of mTOR and autophagy was evaluated in kidney samples from IgAN patients and in an IgAN mouse model induced by oral bovine serum albumin and carbon tetrachloride (CCl4) injection.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!