Detection and characterization of simvastatin and its metabolites in rat tissues and biological fuids using MALDI high resolution mass spectrometry approach
Simvastatin (SV) is a hypolipidemic agent, and it is the 2nd most widely prescribed lipid-lowering
drug. Here, the detection and characterization of SV and its metabolites was studied in selected
organs/tissues (lung, liver, brain, heart and kidney) and biological samples (blood, urine and feces)
of rats. MALDI Orbitrap MS was used as a high-resolution mass analyzer. 2,5-Dihydroxybenzoic acid
(DHB) and 1,5-diaminonaphthalene (DAN) were used as matrices. Several sample loading methods
onto the MALDI plate were attempted and dried droplet method was found to be superior. Two
diferent cell disruption methods, pulverization and homogenization, were also evaluated for the
optimum sensitivity in MALDI. Pulverization allowed the detection of more metabolites in all organs
except the liver, where homogenization led to the detection of more metabolites. Altogether, 13
metabolites were detected, and one metabolite tentatively identifed as a reduced product is being
reported for the frst time. SV and its metabolites were distributed to all the tissues studied except the
brain. Overall, the results implied that the pulverized samples were more uniform and larger in surface
area, resulting in their more efcient and complete extraction during sample preparation. As shown
in the present study, MALDI Orbitrap MS is a useful tool to study drug and metabolite detection and
characterization.
Cancer remains the leading cause of human morbidity universally. Hence, we
sought to assess the in vitro antiproliferative activity of new isatin-based conjugates (5a–s)
against three…
Simvastatin (SV) is a semisynthetic derivative of lovastatin (LV), which is biosynthetically
produced from the fungus Aspergillus terreus and has a high log p value (log p = 4.39)and thus…
Simvastatin (SV) is a hypolipidemic agent, and it is the 2nd most widely prescribed lipid-lowering
drug. Here, the detection and characterization of SV and its metabolites was studied in…