Journal of Advanced Pharmaceutical Technology & Research最新文献

Cordyline fruticosa (L.) A. Chev. (CF) is an ornamental plant known for its therapeutic properties, particularly its antimicrobial activity. This study attempted to identify bioactive compounds in the CF leaf extract and assess their antibacterial and antifungal efficacy against Streptococcus mutans and Candida albicans, which are key contributors to early childhood caries (ECC). CF leaves were extracted using the maceration technique with 70% methanol. Phytochemical and gas chromatography-mass spectrometry (GC-MS) screening were performed to identify secondary metabolites and chemical compounds. S. mutans and C. albicans were isolated from supragingival plaque samples of paediatric patients with severe ECC. The minimum inhibitory concentration (MIC) was determined through serial dilution and ELISA spectrophotometry. Phytochemical screening verified the existence of phenolic compounds, flavonoids, saponins, triterpenoids, and alkaloids. GC-MS identified 17 chemical compounds. The MIC was 6.25% for S. mutans and 1.56% for C. albicans. The extract exhibited significant antimicrobial activity, with a stronger inhibitory effect against C. albicans than S. mutans. The CF leaf extract demonstrates antibacterial and antifungal potential and may serve as a cariogenic antimicrobial agent. Further toxicological studies are needed to confirm its safety for clinical applications.

[This corrects the article on p. 24 in vol. 16, PMID: 40177513.].

Vegetable fermentation extract (VFE) shows potential as a preventive agent to inhibit nonalcoholic fatty liver disease (NAFLD). This study identified bioactive compounds of VFE and explored the mechanism of VFE against NAFLD. Metabolite profiling was analysed using Liquid chromatography-tandem mass spectrometry (LC-MS/MS). The bioactive compounds were screened using the Lipinski Rule of 5, toxicity, and biological activity prediction, followed by network pharmacology and molecular docking. Of the 24 bioactive compounds identified, 8 compounds passed the screening process. Twenty-four genes from network pharmacology were involved in the NAFLD mechanism, including those related to insulin signaling, inflammation, and lipid metabolism. Kaempferol, apigenin, and N-(p-coumaroyl) serotonin showed a good binding affinity with CCR2, AKT, IL-6, and PPAR-γ compared to simvastatin and metformin. Bioactive compounds from VFE were predicted to ameliorate NAFLD.

Traditional Indonesian medicine has long been recognized for its curative qualities, although concerns remain over the efficacy and safety of medicinal herbs. The application of computational methods in novel drug discovery is one of the promising new insights offered by recent technical advancements. This study attempts to find putative anticancer chemicals in two extensively used plants in Southeast Asia, Curcuma longa and Phyllanthus urinaria, using a computational technique. AKT1, a model protein implicated in the development of cancer cells, was used in this investigation. In these two plants, 28 different chemicals were found. We use strict selection standards, like Lipinski's rule of five, to ensure the identification of potential candidates. The findings demonstrated that 24 compounds had comparable binding affinities to the reference ligands, indicating encouraging therapeutic potential. Subsequent investigation showed that the compounds' chemical structures differed and that their similarities to the reference ligand were <10%. However, for both plant-derived drugs, the amino acid binding patterns revealed remarkable similarities that went above 50% similarity, suggesting that both may be useful.

Herbal medicine can be used as an alternative treatment to alleviate allergy symptoms in individuals with urticaria. The herbal remedy comprised four plant components, including Allium ascalonicum, Acanthus ilicifolius, Bambusa blumeana, and Rhinacanthus nasutus, in equal amounts. It was administered to impacted areas of the skin affected by allergies. Nevertheless, the disadvantages of herbal products include their limited ability to penetrate the skin. Microemulsion (ME) is a topical medication delivery device that enhances drug absorption into the skin. This work aims to develop and optimize a ME containing an herbal remedy extract. The construction methods utilized were pseudo-ternary phase diagrams and mixture design using system engineering software. Data were calculated and reported as means ± standard. Statistical significance was indicated when P < 0.05. The optimal herbal ME consisted of 4%-5% isopropyl myristate, 35%-45% Smix, and 46%-58% water. The stability studies demonstrated consistent physical properties and a low level of viscosity. The pH, particle size, polydispersity index, and zeta potential readings have remained stable after storage under nine heating and cooling cycles. The ME exhibited sustained release of rhinacanthin-C, with a steady release rate of 10.34% ± 0.03% from 0.5 h to 20.21% ± 0.11% at 8 h. The Kae-Lom-Pid proves to be suited for MEs and can serve as a model for pharmaceutical development.

Obesity is increasingly a leading cause of dyslipidemia and metabolic syndrome, which are known to be comorbidities of various diseases. A study was conducted to evaluate the effects of different concentrations of exopolysaccharide from goat milk kefir (EPS-GMK) on the activity of key enzymes involved in fat cell formation in 3T3-L1 adipocyte cells. The study used six groups, including two control groups (negative and positive) and four treatment groups with varying concentrations of EPS-GMK (25, 50, 75, and 100 µg/ml). The results showed that EPS-GMK has a significant inhibitory effect on the activity of key enzymes involved in fat cell formation. The findings suggest that EPS-GMK could be a valuable component in developing anti-obesity functional foods. This study aims to analyze the effects of EPS-GMK on the 3T3-L1 adipocyte cells' phosphoenolpyruvate carboxykinase, Glucose-6-Phosphate Dehydrogenase, and Lipoprotein lipase administration. This study applied different doses of EPS-GMK to 3T3-L1 adipocytes with four replications. The doses used were P1 (25 g/ml), P2 (50 g/ml), P3 (75 g/ml), and P4 (100 g/ml). The study also included two control groups, negative control and positive control. This study utilized a completely randomized design for maximum efficacy. The experimental material was 3T3-L1 adipocyte cells, each sample containing adipocyte model cells. One hundred six cells per well were induced with DMI on 24 culture plates. Statistical variance analysis was used to determine the significance between the mean values. The study results revealed that EPS-GMK concentrations between 25 and 100 g/mL could potentially reduce adipogenesis enzyme activity. According to this study, EPS-GMK has the potential and feasibility of being used as an anti-obesity agent.

To date, the specific impact of hypoglycemia on insulin resistance in skeletal muscle is unclear. This study aimed to investigate the correlation between hypoglycemia in individuals with Type 2 Diabetes Mellitus by assessing peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α) and Akt levels in both skeletal muscle tissue and blood plasma. A true experimental-design study was conducted at the Laboratory of Animal Clinical Study, Faculty of Veterinary, Universitas Syiah Kuala, from October to December 2022. The study utilized 24 male rats (Rattus norvegicus) and the rates were categorized into the following groups: control (K1), streptozocin-induced diabetic without hypoglycemia (K2), streptozocin-induced diabetic with mild hypoglycemia (K3), and streptozocin-induced diabetic with severe hypoglycemia (K4). The rats were euthanized a minimum of 30 min after hypoglycemia was confirmed. W Quadriceps femoris muscle and 2 ml of heart blood were collected. PGC-1α and protein kinase B/Akt were examined using enzyme-linked immunosorbent assay. This study demonstrates that PGC-1α and Akt levels in skeletal muscle and plasma are influenced by hypoglycemia severity in rats, with lower levels associated with more severe hypoglycemia, though no significant differences were observed between mild and severe hypoglycemia groups. A positive correlation was found between PGC-1α and Akt levels in skeletal muscle and plasma, suggesting interdependency. Control group plasma levels were 2.48 ± 0.53 ng/ml for PGC-1α and 11.26 ± 1.21 ng/ml for Akt. Even mild episodes of hypoglycemia can lead to a substantial deterioration of insulin resistance in skeletal muscle.

Alzheimer's disease (AD) is the most prevalent type of dementia, negatively affecting the overall quality of life. Targeting the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway, a regulator of protective genes, offers potential AD therapies. Inhibiting Kelch-like ECH-associated protein 1 (Keap1), which suppresses Nrf2, may help reduce neuronal damage. Rhizophora mucronata, a mangrove known for its anti-inflammatory and antioxidant properties, contains rutin, which is a promising potential AD therapy. The study aimed to explore the potential of rutin, a compound from R. mucronata leaves, to inhibit the Keap1-Nrf2. The study analyzed the metabolomic profile of R. mucronata leaves and evaluated their compound, rutin, as AD therapeutic potential via the Keap1-Nrf2 pathway using in silico molecular docking. R. mucronata was extracted using 96% ethanol. Metabolomic analysis employed liquid chromatography-high resolution mass spectrometry (LC-HRMS). The in silico simulations used BIOVIA Discovery Studio and AutoDock Tool 1.5.7 for docking rutin and donepezil with the Keap1. Docking results were evaluated based on binding energy scores and inhibition constant. HRMS identified hundreds of compounds, with quercetin and rutin as major flavonoids. Molecular docking indicated rutin and donepezil had a binding energy of -6.97 ± 0.16 kcal/mol and -7.63 ± 0.04 kcal/mol, respectively. Their amino acid interaction was similar. R. mucronata leaf extract, particularly rutin, showed promise as an AD therapeutic agent through the Keap1-Nrf2 pathway, warranting further research.

Staphylococcus aureus is a common bacterium causing various infections. The irrational use of antibiotics can lead to resistance, prompting the exploration of alternative treatments, such as herbal plants like cassava and pirdot leaves. To evaluate the antibacterial effectiveness of a combination of cassava leaf and pirdot leaf extracts against S. aureus. Antibacterial activity was tested using the different concentration ratios of cassava and pirdot leaf extracts (80:20, 50:50, and 30:70), with chloramphenicol (30 µg) as the positive control and DMSO (10%) as the negative control. "The inhibition zones for the various concentrations were as follows: 80% cassava and 20% pirdot (14.14 ± 1.69 mm), 50% cassava and 50% pirdot (26.47 ± 2.15 mm), and 30% cassava and 70% pirdot (22.73 ± 1.57 mm). The positive control (chloramphenicol) showed an inhibition zone of 43.59 ± 1.03 mm. Statistical analysis (Kruskal-Wallis, P = 0.0001) indicated significant differences among all treatment groups, followed by Dunn's test for pairwise comparisons. The inhibition zones for the various concentrations were as follows: 80% cassava and 20% pirdot (14.14 ± 1.69 mm), 50% cassava and 50% pirdot (26.47 ± 2.15 mm), and 30% cassava and 70% pirdot (22.73 ± 1.57 mm). The positive control (chloramphenicol) had an inhibition zone of 43.59 ± 1.03 mm. Statistical analysis (Kruskal-Wallis, P = 0.0001) indicated significant differences between the treatment groups.

Moringa oleifera (MO) has been explored for anticancer drug development. However, conventional extract formulations face limitations in drug delivery. Nanoparticles offer a promising alternative due to their small size, enhancing drug selectivity, efficacy, and safety. Therefore, this study aimed to characterize polyvinyl alcohol-based MO nanoparticles (NpMO) and assess their cytotoxicity and anticancer potential. Moreover, NpMO was synthesized using ultrasonication and characterized by its size, functional groups, and surface morphology. Then, an MTT assay was conducted in Vero and HeLa cells, each divided into a control group and five treatment groups (PV1-5 and PL1-5). The treatment groups received NpMO with various doses: 12.5 µg/mL, 25 µg/mL, 50 µg/mL, 100 µg/mL, and 200 µg/mL. The results were represented as OD values and percentage of viable cells, with statistical analysis performed using SPSS version 27. We found that Vero cell viability remained high at 96%, 95%, 93%, 90%, and 82.3% in PV groups, indicating no significant difference between control and PV1-PV4 groups with statistical analysis. Meanwhile, HeLa cell viability decreased to 98%, 92%, 78%, 69%, and 50.2%, with PL5 showing the lowest viability percentage. Statistical analysis confirmed a significant difference between PL5 and the other PL groups. In conclusion, NpMO showed minimal toxicity to Vero cells (>50% viability up to 200 µg/mL) but significantly reduced HeLa cell viability at 50-200 µg/mL, with the strongest effect at 200 µg/mL, indicating a potential anticancer activity.