Explore chapters and articles related to this topic
Sulfonamides
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Natasha E. Holmes, M. Lindsay Grayson
The degree of sulfonamide protein binding influences the rate of renal excretion of these drugs (see section 5d, Excretion). The protein-bound drug does not penetrate into some body compartments, such as the subarachnoid space, but this may not apply if the meninges are inflamed. Madsen et al. (1963) compared the sulfonamide concentration and the antibacterial activity in serum of two long-acting sulfonamides (sulfadimethoxine and sulfamethoxypyridazine) with sulfadiazine. These authors found that these three sulfonamides all produced about the same antibacterial activity in the serum. There appeared to be a close correlation between the total sulfonamide concentration and the antibacterial activity regardless of the degree of protein binding. The highly protein-bound long-acting sulfonamides also penetrated well into extravascular fluids and exudates, particularly when these were of a high protein content. There are many considerations in assessing the effect of protein binding on antibacterial activity (Rolinson, 1980). A protein-bound drug is essentially without antibacterial effect and is nondiffusible, but this is only a temporary state, because when a protein-bound drug dissociates, the drug is available again in active form. The free unbound plasma levels of a drug dictate the free levels in extravascular fluids. The level of free drug after therapeutic doses and how this relates to the MIC of the organism are important factors in determining therapeutic efficacy.
Novel curcumin nanoformulation induces apoptosis, and reduces migration and angiogenesis in liver cancer cells
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2023
Steve Harakeh, Saber H. Saber, Rajaa Al-Raddadi, Turki Alamri, Soad Al-Jaouni, Mohammed Qari, Yousef Qari, Shafiul Haque, Ayat Zawawi, Soad S. Ali, Zakaria Y. Abd Elmageed, Shaker Mousa
It has been known that primary cancer cells metastasise to distant organs through degradation of extracellular matrix and promoting cell migration, invasion, and angiogenesis [46]. Different approaches, including nanoformulation, have been undertaken to inhibit cancer metastasis and recurrence. Our results show that treatment of LC with 2.5 to 10 µg/ml of Cur-NPs inhibited cell migration and angiogenesis as evidenced by the results from wound-healing assay and chicken embryo model. Arya et al. reported comparable results of anti-migratory and anti-invasive property when pancreatic cells were treated with PLGA chitosan/PEG curcumin NPs compared to cells treated with native curcumin [42]. The chick embryo and its chorioallantois membrane have been used as an accepted model although its reported limitations for evaluating drug delivery loaded in nanoparticles [47,48]. An investigation performed by de Carvalho et al. examined the effect of curcumin-loaded nanoformulations and their different coating agents using a chick embryo model. They found that curcumin NPs coated with P80, PEG, EUD and CS reduce angiogenic and teratogenic effects in the treated chick embryos [49]. In addition, a study conducted by Dragostin et al. revealed that treatment of chick embryo with chitosan-sulfadimethoxine (CLC) and chitosan-sulfisoxazole (CLD) NPs exerted an antiangiogenic effect [50].
Metabolic map of the antiviral drug podophyllotoxin provides insights into hepatotoxicity
Published in Xenobiotica, 2021
Dongxue Sun, Xiaoxia Gao, Qiao Wang, Kristopher W. Krausz, Zhongze Fang, Youbo Zhang, Cen Xie, Frank J. Gonzalez
The bile samples were separated and analysed using a Waters Acquity UPLC system coupled to a Waters Synapt HDMS Q-TOF mass spectrometer under the following conditions: capillary volts 3 kV, sample cone 40 V, source temperature 150 °C, desolvation temperature 400 °C, cone and desolvation gas flow 50 and 900 L/h, respectively. Data were acquired in centroid mode in both positive and negative electrospray ionization modes, using sulfadimethoxine as the Lock Mass. Mass range acquired was 50–900 Amu at 0.3 second scans. Chromatography was carried out using a Waters Acquity BEH C18 column (2.1 × 50 mm) under acidic conditions using water (A) and acetonitrile (B) containing 0.1% formic acid. The following gradient was used: initial conditions 98% (A) for 0.5 min, to 80% (A) at 6.5 minutes, to 70% (A) at 8.0 min, to 1% (A) at 8.5 min, held for one min, and returned to the initial conditions for two min for column equilibration. Total run time was 11.5 min. Column temperature was maintained at 40 °C. All samples were injected at 5 µL.
Functional assessment of rat pulmonary flavin-containing monooxygenase activity
Published in Xenobiotica, 2019
Yildiz Yilmaz, Gareth Williams, Nenad Manevski, Markus Walles, Stephan Krähenbühl, Gian Camenisch
Benzydamine hydrochloride, benzydamine N-oxide maleate, NADPH, sulfadimethoxine (SDM) and 1-aminobenzotriazole were purchased from Sigma-Aldrich (Poole, UK). HPLC grade water and acetonitrile were purchased from VWR (Leicestershire, UK). Sprague-Dawley rat (pool of 299) lung microsomes were obtained from Xenotech (Kansas City, MO). Lung microsomes were not further characterized with regard to CYP and FMO protein content.