Bioanalytical method for the quantification of the monastrol derivative anticancer candidate LaSOM 65 in pre-clinical pharmacokinetic investigations

Abstract

95%), after which they were subjected to chromatography under the isocratic elution of an acetonitrile:water (45:55, ν/ν) solution with detection at 303 nm. The method was linear (r² > 0.98) over the concentration range (0.05-2 µg mL-1) with intra- and inter-day precision ranging from 9.6% to 13.6% and 4.3% to 5.4%, respectively. The accuracy of the method ranged from 85% to 113.6%, and it showed sufficient sensitivity to determine pharmacokinetic parameters of LaSOM 65 after intravenous administration to Wistar rats.]]>

Influence of Experimental Cryptococcal Meningitis in Wistar Rats on Voriconazole Brain Penetration Assessed by Microdialysis

“…VRC protein binding was determined by ultrafiltration. The procedures used were the same previously described by our research group (40). To perform this step, plasma samples from healthy (n ϭ 3) and C. neoformans-infected (n ϭ 3) Wistar rats were used.…”

Monastrol: Unveiling the Mechanisms, Efficacy, and Therapeutic Potential – A Comprehensive Review

“…Since monastrol has weak activity and lacks typical drug traits, it is not the best drug option for cancer treatments. Due to its low solubility in water, monastrol requires other methods to be administered to the body (Torres et al, 2014). One method, the use of mesoporous silica nanoparticles, involves the use of nanocarriers synthesized from ammonia, ethanol, tetraethyl orthosilicate, and Polysorbate 80 to store hydrophobic drugs such as monastrol to transport it within the body (Zhang et al, 2016).…”

Pyridine-based, microwave-assisted one-pot synthetic protocol for the synthesis of ethyl 3-substituted-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates

“…anti-hypertensive, antibacterial, antitumor, antiviral and anticancer, are comparatively less explored [5,6]. It is worth noting that a very limited number of reports are available for thiolated-5-carboxyuracil (4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid) [7,8] and its ester derivatives (Monastrol [9] and LaSOM-65 [10]; Fig. 1), despite their promising biological results [4,11].…”