Background Medicinal plant contains multiple bioactive compounds with therapeutic potentials. Due to their availability, affordability, and minimal known side effects, they are widely practiced. Identification, quantification, and establishment of their interaction with physiological enzymes help in the standardization of plant-based medicinal extracts. In this study, gas chromatography/flame ionization detector (GC–FID) and high-performance liquid chromatography (HPLC) analysis were used to determine the bioactive components in the ethanol extract of Newbouldia laevis stem bark. The antioxidant activity of the extract was determined. Enzyme inhibitory potency of the flavonoids’ components was investigated against acetylcholinesterase, butyrylcholinesterase, phospholipase A2, α-glucosidase, and α-amylase. Results Analysis of ethanol extract of N. laevis stem-bark revealed alkaloids (0.37%), tannins (1.82 mg/TEq/g), flavonoids (5.85 mg/QEq), steroids (0.11 mg/10 g) and glycosides (0.08 mg/10 g). The HPLC fingerprint of flavonoids showed high concentrations (mg/100 g) of catechin (47.11), apigenin (15.68), luteolin (18.90), kaempferol (41.54), and quercetin (37.64), respectively. In vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging ability of the extract was exhibited at 150 and 200 mg/mL, respectively. At 300 mg, most in vitro antioxidant potentials (lipid peroxidation, metal chelating ability, hydroxyl, nitric oxide, sulfide oxide radicals scavenging abilities) were obtained. The extract showed varying inhibitory abilities (> 50%) on acetylcholinesterase, butyrylcholinesterase, phospholipase A2, α-glucosidase and α-amylase at 300 mg/mL, IC50 of 129.46, 237.10, 169.50, 251.04 and 243.06 mg/mL, respectively, with inhibition constants (Ki) of 3.92, 1.63, 1.11, 2.95 and 2.11. Results showed an affinity for the targeted enzymes with free energies higher than the standard drugs. Conclusion The results revealed that the N. laevis stem bark possesses antioxidant activity and enzyme inhibitory activity on the physiological enzyme that has been implicated in diabetes. In vitro and in silico inhibition of these physiological enzymes by extract suggests that the stem bark can be effective in ameliorating the complications associated with diabetes mellitus.
Background Recent efforts for the complementary treatment of diabetes have focused on medicinal plants and their bioactive compounds. Tephrosia bracteolata is one of such plants used in the management of diabetes but its anti-diabetic principles are yet to be identified. This study was aimed at identifying the compounds responsible for the antidiabetic activity of the ethylacetate fraction of Tephrosia bracteolata leaves and subsequently, carryout an in silico molecular docking of these compounds against key targets in the pathophysiology of diabetes. Methods The ethylacetate fraction (EAF) of T. bracteolata leaves was fractionated using Silica gel column chromatography to yield 100 fractions. Pooling together of fractions with similar thin layer chromatographic (TLC) mobility profile afforded seven major fractions (SF1- SF7). Preliminary phytochemical studies were carried out on the fractions using standard methods. The antidiabetic activity of the fractions was subsequently evaluated (at a dose of 200 mg/kg) against alloxan- induced diabetes in adult mice. GC-MS analysis was carried out on the fraction with the highest activity. Subsequently, some of the identified active compounds were docked against key targets in the pathology of diabetes using Auto Dock tool. Results Preliminary phytochemical analysis revealed the presence of terpenoids, saponins, steroids, glycosides, flavonoids, tannins and alkaloids in varying proportions in the fractions. The sub-fractions produced varying degrees of significant (p < 0.05) decrease in FBS at 12h and 24h- post-treatment. GC-MS analysis of the most active fraction (SF5) revealed the presence of thirty- six compounds among which are some that have been reported to possess direct or indirect antidiabetic properties. These are Mome-inositol, 2-methoxy-4-vinylphenol, 1-D-thio-glucitol, 4-Piperidinone, Hexadecanoic acid, 9- octadecanoic acid, n- hexadecanoic acid and D- allose. Molecular docking studies (Auto Dock tool) between Mome inositol, 1-D-thio-glucitol and alpha-glucosidase showed that Mome inositol (− 6.7 kcal/mol) had a stronger affinity to the enzyme. Similarly, for sodium glucose co-transporter 2 (SGLT 2), Mome inositol (− 6.5 kcal/mol) had a stronger affinity than 1-D-thio-glucitol. Conclusions The identified compounds in the fraction could be responsible for the observed antidiabetic properties of the fraction of T. bracteolata.
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