Preparation and prodrug studies of quercetin pentabenzensulfonate.
نویسندگان
چکیده
Pentabenzensulfonate (QPBS), a potential prodrug for quercetin, was designed and synthesized in high yield. It possesses better physical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kinetics than its original form. The LogP value (2.04) and the half-life of the hydrolysis value (3.85 h) show that oral bioavailability is improved evidently compared with that of quercetin. These results indicate that QPBS can be considered as a potential prodrug for quercetin.
منابع مشابه
Neuroprotective Effect of Quercetin Nanocrystal in a 6-Hydroxydopamine Model of Parkinson Disease: Biochemical and Behavioral Evidence
Introduction: studies have suggested that free radicals-induced neurodegeneration is one of the many studies of Parkinson Disease (PD). Quercetin as a natural polyphenol has been regarded as a significant player in altering the progression of neurodegenerative diseases by protecting from damages caused by free radicals. Owing to its poor water solubility, preparation of its oral formulation is ...
متن کاملOptimization, preparation and characterization of rutin-quercetin dual drug loaded keratin nanoparticles for biological applications
Objective(s): Response surface methodology (RSM) by central composite design (CCD) was applied to statistically optimize the preparation of Rutin-Quercetin (Ru-Qr) dual drug loaded human hair keratin nanoparticles as well as evaluate the characteristics. Materials and Methods: The effects of three independent parameters, namely, temperature (X1:10-40 C), surfactant (X2: SDS (1), SLS (2), Tween-...
متن کاملPreparation of acrylic-type derivative of ibuprofen and in vitro evaluation studies of its polymeric prodrugs
Acrylic-type polymeric systems having degradable ester bonds linked to ibuprofen were synthesized and evaluated as materials for drug delivery. Ibuprofen, as a non-steroidal anti-inflammatory drug, was linked to 2-hydroxyethyl methacrylate by activated ester methodology in one-pot procedure. The resulting methacrylic derivative of ibuprofen was copolymerized with 2-hydroxyethyl methacrylate and...
متن کاملSynthesis and evaluation of a prodrug of 5-aminosalicylic acid for the treatment of ulcerative colitis
Objective(s): This study is aimed to design and synthesize a prodrug of 5-aminosalicylic acid and evaluate its ameliorative effect on experimental ulcerative colitis (UC).Materials and Methods: 5-Aminosalicylic acid-alanine (5-ASA-ALA) was synthesized and characterized. Its stability study was conducted in rat plasma and in the gastroint...
متن کاملPreparation and evaluation of 99mTc-labeled zidovudine function as an analog of thymidine in the diagnosis of human lung cancer cells
Introduction: Labeled nucleotide detectors provide a basis for measuring cell division. Zidovudine is a prodrug that is phosphorylated by cellular enzymes at the 5ʹ position and converted to active triphosphate. Zidovudine triphosphate interferes with the reverse transcriptase enzyme and lengthens the viral DNA strand. Materials and Methods: Ethyl-2-propynyl acetate and 2-amino-N-propynyl benza...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
دوره 128 12 شماره
صفحات -
تاریخ انتشار 2008