The objectives of this study were to prepare and characterize a novel piperine–succinic acid multicomponent crystal phase and to evaluate the improvement in the solubility and dissolution rate of piperine when prepared in the multicomponent crystal formation. The solid-state characterization of the novel multicomponent crystal was performed by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform-infrared (FT-IR) spectroscopy. Solubility and dissolution rate profiles were evaluated in distilled water. The physical stability was evaluated under high relative humidity (75% and 100% RH). The determination of the single crystal X-ray diffraction structure revealed that this novel multicomponent crystal was a cocrystalline phase of piperine–succinic acid (2:1 molar ratio). The differential scanning calorimetry thermogram of the cocrystal showed a single and sharp endothermic peak at 110.49 °C. The cocrystal resulted in greater solubility and a faster dissolution rate of piperine than intact piperine. This improvement was a result of the formation of a channel structure in the cocrystal. In addition, the cocrystal was stable under a humid condition.
Usnic acid is known for its remarkable antimicrobial activity. The aim of this research was to formulate hydrogel of usnic acid and evaluate the antibacterial activity against Propionibacterium acne. Due to low solubility of usnic acid, solid dispersion was prepared using PVP K-30. In this study, intact usnic acid (UA) and usnic acid-solid dispersion (UA-SD) was formulated in hydrogel using several gelling agents: Aqupec HV-505, sodium alginate and HPMC K 100M. Concentration of each gelling agent was optimized for hydrogel base. All of hydrogel base showed homogenous gel, pH at range 5.37–6.33 and viscosity in range 259.07–10,759.00 cps. Hydrogel was prepared by dispersing 1% intact UA and 3% UA-SD in three different gelling agents. The hydrogel was evaluated for pH, viscosity, stability test for two months and microbiology test. The amount of usnic acid in hydrogel was determined by spectrophotometry UV-Vis. Hydrogel UA showed non-homogenous gel, while hydrogel usnic UA-SD was homogenous. The pH of all hydrogel was in range 5.5–6.4 and viscosity was 2,017.03–3,866.52 cps. All the hydrogel was stable and diameter inhibition of hydrogel was in a range 20–32 mm. The amount of usnic acid in hydrogel was in range 96.9–99.23%. In conclusion, hydrogel UA-SD is promising preparation in handling acne.
To continue the study of Sumatran lichen, six species of the genus Cladonia were screened for phytochemicals and their antibacterial bioactivity. The procedure included sequential extraction (semi polar solvent), antibacterial activity tests using the agar diffusion method, and microdilution to determine the minimum inhibitory concentration (MIC) value of each extract. The study also involved the thin layer chromatography (TLC)-bioautography method and liquid chromatography-mass spectrometry (LC-MS/MS) analysis (in positive mode), which aimed to provide information about the composition and activity of individual components of the extracts that have an antibacterial effect. The test results indicated that all studied Cladonia lichen semipolar extracts had an antibacterial effect, while five of them had very strong bacterial growth inhibition activity (MIC range values 2.5 to 10 mg/mL). Additionally, the identities of compounds found in lichen with broad inhibition, which include the depside and depsidone groups, were confirmed by LC-MS/MS. Based on existing test data, C. scabriuscula, C. crispata, C. rappii, and C. macilenta are potential antibacterial candidates.
Objective: Maize (Zeamays L.) is a crop that has been widely cultivated in Indonesia. Using corn kernels on a large scale will produce much corn cob waste, usually unused. According to the literature search, corn cobs’ phytochemical studies and pharmacological activities still need to be improved. This study aims to determine the content of secondary metabolites (metabolite profiling) and their antityrosinase and anti-aging potential. Methods: Corn cobs were macerated with methanol and fractionated with n-hexane, ethyl acetate, and butanol. The phytochemical profiling approach of the methanol extract was performed by liquid chromatography-mass spectra (LC-MS/MS). Anti-tyrosinase and anti-aging bioactivity were evaluated by thin layer chromatography (TLC)-bioautography and IC50 spectrophotometrically. Results: The evaluation results show that the butanol fraction leads to a potential value (IC50 99.92 µg/ml). Several compounds, especially flavonoid compounds (including catechin; kaempferol 3-arabinofuranoside 7-rhamnoside; 6,8-Di-C-beta-D-arabino pyranosyl apigenin; 5,7-Dihydroxy-8,4’-dimethoxyisoflavone) were identified by LC-MS/MS by comparing the molecular mass of MS/MS data with literature data. Conclusion: Based on this study, it can be concluded that butanol is the fraction that most actively inhibits tyrosinase, elastase, and collagenase enzymes, which means it potentially becomes a new anti-aging candidate.
31 January 2025 in Journal of Multidisciplinary Applied Natural Science
Hyperlipidemia is a major risk factor for cardiovascular diseases. While conventional treatments exist, there is a growing interest in natural remedies with fewer side effects. Ficus elastica has promising medicinal properties, yet its potential as an anti-hyperlipidemic agent remains unexplored. This study aimed to investigate the anti-hyperlipidemic effects of F. elastica using an integrated approach of LC-HRMS-based chemical bioinformatics and in vitro/in vivo experimental validation. The anti-hyperlipidemic potential of F. elastica and its mechanism of action were screened using integrative computational network pharmacology followed by in vitro HMG-CoA reductase inhibition and in vivo lipid-lowering activity in a hyperlipidemia rat model. Network pharmacology analysis identified STAT3, HSP90AA1, and TLR4 as potential core targets involved in lipid and atherosclerosis-related KEGG pathways. Molecular docking simulations revealed high-affinity interactions between F. elastica compounds and the identified targets, notably compound 41 and compound 61. In vitro assay demonstrated that ethanolic extract of F. elastica inhibited HMG-CoA reductase with an IC50 of 297.73 µg/mL. In vivo experiment using a hyperlipidemic rat model showed significant reductions in total cholesterol, triglycerides, and increased HDL levels. The reduction of triglycerides and elevation of HDL level after F. elastica ethanolic extract supplementation is similar to the effect from supplementation of simvastatin. These findings suggest that F. elastica ethanolic extract possesses notable anti-hyperlipidemic properties, likely mediated through multiple molecular targets and pathways. The study highlights the potential of F. elastica ethanolic extract as a promising candidate for anti-hyperlipidemic therapy and underscores the efficacy of integrating computational and experimental approaches in natural product research.