ABSTRACT
Cancer is a long-standing disease, and the use of anticancer drugs can cause many different harmful side effects. Therefore, the quantitative analysis of anticancer drugs is crucial. Among all the analytical techniques that have been utilized for the detection of doxorubicin, electrochemical sensors have drawn exceptional consideration because they are simple, affordable, and highly sensitive. Manganese tetraphenylporphyrin decorated reduced graphene oxide (Mn-TPP/RGO), tetraphenylporphyrin decorated reduced graphene oxide (TPP/RGO), and reduced graphene oxide (RGO) nanostructure based glassy carbon electrodes (GCEs) were fabricated for the detection of doxorubicin (DOX). The synthesized materials were characterized by FTIR, scanning electron microscopy (SEM), ultraviolet-visible spectroscopy (UV/vis), energy dispersive X-ray spectroscopy (EDS), and X-ray diffraction (XRD). Doxorubicin detection was performed using differential pulse voltammetry (DPV), electrochemical impedance spectroscopy (EIS), and cyclic voltammetry (CV). Among the prepared electrodes, Mn-TPP/RGO modified GCE gave an optimum peak current at pH 3. The Mn-TPP/RGO modified electrode showed significant linear response range (0.1-0.6 mM); effective sensitivity (112.09 µA mM-1 cm-2); low detection limit (63.5 µM); and excellent stability, selectivity, repeatability, and reproducibility toward doxorubicin. With differential pulse voltammetry, LoD and sensitivity were 27 µM and 0.174 µA µM-1 cm-2, respectively. Real sample analysis was also performed in human serum, and it depicted reasonable recovery results for spiked doxorubicin.
ABSTRACT
Inhibition of α-glucosidase is one of the important approaches in designing antidiabetic drugs for its role in decrease of the carbohydrates digestion to avoid post-prandial increase in blood sugar levels in diabetic patients. In the present study we designed a novel series of 2-acetylbenzofuran hydrazones (L1-L7) and their metal (II) complexes Cu (II), Co (II), Zn (II) and Mn (II) (8-29) and screened for inhibitory activity against the yeast α-glucosidase. The synthesis of hydrazones incorporated the use of I2 as a catalyst which resulted in excellent yield of 94%. The ligand L3, showed good activity (IC50 = 47.51 ± 0.86 µM) while its metal complex (10) showed potent activity (IC50 = 1.15 ± 0.001 µM) compared to reference acarbose IC50 = 378.25 ± 0.12 µM. Similarly, the Cu (II) complexes with ligands L5 and L6 showed excellent α-glucosidase inhibition (IC50 = 0.15 ± 0.003 12 and 0.21 ± 0.002 µM for 13, respectively) whereas, the metal complexes of Co (II), Mn (II), and Zn (II) showed moderate to poor inhibitory activities against α-glucosidase. The The findings are supported by the ligands and enzyme interactions through molecular docking studies. In conclusion, it is indicated that metal complexes of 2-acetylbenzofuran hydrazones have good potential for research leading to antidiabetic therapies.
Subject(s)
Benzofurans/pharmacology , Coordination Complexes/pharmacology , Glycoside Hydrolase Inhibitors/pharmacology , Hydrazones/pharmacology , Metals, Heavy/pharmacology , alpha-Glucosidases/metabolism , Benzofurans/chemistry , Coordination Complexes/chemical synthesis , Coordination Complexes/chemistry , Dose-Response Relationship, Drug , Glycoside Hydrolase Inhibitors/chemical synthesis , Glycoside Hydrolase Inhibitors/chemistry , Humans , Hydrazones/chemistry , Metals, Heavy/chemistry , Molecular Structure , Structure-Activity RelationshipABSTRACT
With increasing urbanization and industrialization, clean air is becoming a scarce resource. During the present investigation, concentrations of metals (Pb, Ni and Zn) in the atmosphere and their subsequent deposition in the lungs of two common avian species, common myna, Acridotheres tristis (n = 30) and bank myna, A. ginginianus (n = 20), captured from urban areas of Lahore city and semi-urban areas of Pattoki city 80 km away from main city of Lahore were determined. The obtained results were analyzed statistically using Independent sample t test and Pearson's correlation. A comparison of trace metal concentrations in air of both the cities was also carried out. Statistically, significant variations were recorded for Pb (t (7) = - 4.276, p = 0.001) while non-significant differences were observed for both Ni (t (7) = 0.049, p = 0.962) and Zn (t (7) = 1.555, p = 0.146).
