METHODS: Mangosteen peel extract was formulated into amorphous solid dispersions using polyvinylpyrrolidone K30 at a 1:3 polymer ratio via solvent evaporation and fluidized bed drying methods. Solubility enhancement was evaluated under standardized conditions, and α-glucosidase inhibitory activity was assessed through IC50 determination. Comparative analysis against acarbose and quercetin standards was performed.
RESULTS: Solvent evaporation achieved 2.1-fold solubility enhancement, while fluidized bed drying yielded 1.8-fold improvement. The mangosteen peel extract demonstrated superior α-glucosidase inhibition (IC50 = 20.13 ± 0.02 μg/mL) compared to acarbose (IC50 = 379.75 ± 0.57 μg/mL) but remained less potent than quercetin (IC50 = 2.97 ± 0.05 μg/mL). When normalized to equivalent α- mangostin concentrations, fluidized bed drying preserved inhibitory activity more effectively (IC50 = 112.87 ± 0.06 μg/mL) than solvent evaporation (IC50 = 1238.48 ± 0.51 μg/mL).
DISCUSSION: The manufacturing method significantly influenced both solubility and biological activity. Solvent evaporation maximized solubility enhancement but compromised enzyme inhibitory potency, whereas fluidized bed drying maintained superior inhibitory activity despite moderate solubility improvement. This trade-off suggests that formulation strategy selection should prioritize the desired therapeutic outcome.
CONCLUSION: Amorphous solid dispersion successfully enhanced both solubility and α-glucosidase inhibitory activity of mangosteen peel extract. Fluidized bed drying represents the optimal manufacturing approach for preserving enzyme inhibition while achieving meaningful solubility enhancement, positioning α-mangostin as a promising candidate for natural antidiabetic drug development.
METHODS: Health-related quality of life was captured using the EuroQol-5 Dimension-3 Level (EQ-5D-3L), with data collected at baseline and throughout the trial. Multilevel mixed-effects linear regression with random effects estimated health-related quality of life over time, capturing variation between hospital sites and individuals, and a fixed-effects linear model estimated the impact of cardiovascular and gastrointestinal events.
RESULTS: Patients were followed for a median of 5 years (interquartile range 3.4-6.0). The average baseline EQ-5D score of 0.930 (SD 0.104) remained relatively unchanged over the trial period with no evidence of statistically significant differences in EQ-5D score between randomized treatment groups. The largest decrement in the year of an event was estimated for stroke (-0.107, P
METHOD: This research commenced with retrieving protein structures from the RCSB database, generating the formation of ligands using the ChemDraw Professional software, conducting molecular docking with the Autodock Vina software, and performing molecular dynamics simulations using the Amber software, along with the evaluation of RMSD values and intermolecular hydrogen bonds. Free energy, electrostatic interactions, and Van der Waals interaction were calculated using MM/GBSA. Acarbose, used as a positive control, and maltose are simulated together with test compound that has the best free energy. The forcefields used for molecular dynamics simulations are ff19SB, gaff2, and tip3p.
Materials and Methods: Crude methanolic fraction of E. suberosa (Roxb) bark and its respective fractions were screened for the presence of different phytochemicals with different reagents. On the basis of increasing order of polarity, different organic solvents were used to obtain different fractions. Enzymatic studies were performed on crude methanolic extract of the plant. All the assays were performed under standard in vitro conditions.
Results: The phytochemical analysis shows the presence of alkaloids, phenols, triterpenoids, phytosterols, and flavonoids. Phenolic compounds and flavonoids are the major constituents of the plant. In anticholinesterase assay, the percent inhibition of standard drug (eserine) was 91.27 ± 1.17 and the half maximal inhibitory concentration (IC50) was 0.04 ± 0.0001. For α-glucosidase inhibition, the IC50 value for Dichloromethane fraction was 8.45 ± 0.13, for Methanol fraction it was 64.24 ± 0.15, and for aqueous fraction it was 42.62 ± 0.17 as compared with standard IC50 that is 37.42 (acarbose). Furthermore, results show that all fractions have potential against anti-urease enzyme, but DCM fraction of crude aqueous extract has significant IC50 value (45.26 ± 0.13) than other fractions.
Conclusion: Keeping in view all the results, it is evident that the plant can be used in future for formulating effective drugs against many ailments. Secondary metabolites and their derivatives possess different biological activities, for example, .g. flavonoids in cancer, asthma, and Alzheimer. Furthermore, the extracts of this plant can be used in their crude form, which is an addition to the complementary and alternative treatment strategies.