Journal of Advanced Pharmaceutical Technology & Research最新文献

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.

Cisplatin (Cisp), a platinum-based compound, is a potent chemotherapy drug that effectively treats various cancers such as lung, breast, bladder, and hepatocellular carcinoma. However, its clinical application is limited due to its fibroblast damage, which is linked to its ability to produce collagen and other extracellular matrix components essential for tissue healing. Enhancing antioxidant capacity offers a potential strategy to reduce Cisp-induced fibroblast damage. Hesperidin (HSD), a flavonoid from Citrus sp., exhibits various pharmacological properties, including anti-inflammatory and antioxidant effects. This study aims to determine HSD as cytoprotective induced by Cisp using the fibroblast cell lines (NIH-3T3). 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was used to determine antioxidant activity. The viability cell after treatment with HSD, Cisp, and cotreatment HSD-Cisp was evaluated through Mictroculure Tetrazolium Technique (MTT) assay. The evaluation of senescence was performed using the senescence-associated β-galactosidase assay. Gelatin zymography assay was utilized to analyze the activity of matrix metalloproteinases (MMPs). Data were analyzed using one-way ANOVA and Tukey's post hoc test in SPSS (version 20.0). The IC₅₀ of the radical scavenging assay of HSD was found to be 20.967 ± 0.016 µM. HSD showed low cytotoxicity against NIH-3T3 cells, with IC₅₀ values of over 500 µM. HSD showed an antagonistic effect when used as cotreatment HSD with Cisp in NIH-3T3 cells, with a combination index >1. Cotreatment of HSD and Cisp reduces cellular senescence and the expression of MMP-9 and MMP-2. These findings suggest that HSD could be beneficial as a cytoprotective agent, helping to maintain cellular health against chemotherapy.

This study was conducted to evaluate the impact of a combination of Morinda citrifolia fruit extract (MCFE) and Averrhoa bilimbi leaf extract (ABLE) on hair growth in rabbits. The study included seven treatment groups: (1) control group (distilled water), (2) positive control (minoxidil 5%), (3) treatment 1 (MCFE 10%), (4) treatment 2 (ABLE 10%), (5) treatment 3 (MCFE 5% + ABLE 5%), (6) treatment 4 (MCFE 7.5% + ABLE 2.5%), and (7) treatment 5 (MCFE 2.5% + ABLE 7.5%). Hair length measurements were taken on days 7, 14, 21, and 28, and the average daily growth rate was calculated by dividing the change in hair length by the number of days. Hair weight was measured on day 28. Data analysis was conducted using both two-way and one-way ANOVA, and statistical significance was determined at P < 0.05. The treatment group 4 (MCFE 7.5% + ABLE 2.5%) showed a significant difference in hair growth compared to the normal control, positive control, and other treatment groups (P < 0.05). The group exhibited a 19.69 ± 0.38 mm increase in hair length, with a daily growth rate of 0.88 mm/day, and an increase in hair weight of 0.33 ± 0.003 g. The combination of MCFE and ABLE demonstrated potential as an anti-hair loss agent, effectively enhancing both hair length and weight.

Graptophyllum pictum offers therapeutic potential that has received attention from researchers around the world. The purple leaf is native to New Guinea and has been widely distributed, including Indonesia. This study aims to determine the antioxidant activity and potential inhibition of the lipoxygenase (LOX) enzyme in the hexane fraction, ethyl acetate fraction, and water fraction of purple leaf. Samples were extracted by maceration using 96% ethanol, followed by multilevel fractionation using ethyl acetate, hexane, and water solvents. The fractions were determined for their antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl method, and their potential in LOX enzyme inhibition was analyzed using an ultraviolet-vis spectrophotometer. The ethyl acetate fraction showed the highest antioxidant activity with inhibition concentration (IC₅₀) of 17.23 µg/mL; LOX inhibition was also demonstrated by the highest ethyl acetate fraction with IC₅₀ 133.47 µg/mL, followed by the hexane fraction, and then the water fraction. These results suggest purple leaves with ethyl acetate fraction can be a new drug innovation with antioxidant and anti-inflammatory properties, and this study can be used as an evaluation material for further drug development.

The immune system's principal functions are to preserve health and defend against dangerous invaders (antigens). Parijoto fruit (Medinilla speciosa) is a plant that can potentially have immunomodulatory activity because it contains flavonoid and terpenoid compounds. The aim of this research is to ascertain the total flavonoid and phytochemical content of the parijoto fruit fraction, as well as its potential in vitro immunomodulatory activity. The extraction of powdered parijoto fruit was conducted using 70% ethanol, followed by the separation into n-hexane, ethyl acetate, and water fraction. The phytochemical content was analyzed with gas chromatography (GC)-mass spectrometry. The total flavonoid contents were determined by colorimetric analysis. In addition, the immunomodulatory activity assay was conducted in vitro to evaluate the phagocytic activity (phagocytic capacity [PC] and phagocytic index) of macrophages and the proliferation of lymphocytes (stimulation index [SI]). The GC results showed that parijoto fruit extract contains 9,12-Octadecadienoic acid-, and phthalic acid. The ethyl acetate fraction exhibited the greatest total flavonoid concentration at 7.4094 ± 0.49 mg QE/g sample. In vitro, immunomodulatory tests showed that all fractions could significantly increase macrophage phagocytic activity compared to control cells. The highest value of PC and phagocytic index was found in the n-hexane phase with a concentration of 750 g/mL of 82.75 ± 0.87 and a concentration of 500 g/mL of 6.62 ± 0.19, respectively. The ethyl acetate fraction exhibited the most significant SI for lymphocyte proliferation, recorded at a concentration of 750 g/mL with a value of 8.70 ± 1.01. The ethyl acetate fraction's SI >3 value in the lymphocyte proliferation test suggests that it exhibits lymphocyte proliferation activity. The parijoto fruit may enhance the phagocytic role of macrophages and promote lymphocyte proliferation, indicating its potential as an immunomodulatory therapy.

Vitamin K consumption needs to be monitored in people taking warfarin since it can impact the anticoagulation response. Vegetables are the primary nutritional source of Vitamin K1, in the form of Vitamin K1. The aim of this study was to measure the level of Vitamin K1 in various vegetables that were commercially sold in three major Bandung markets and were ingested by patients using warfarin at Hasan Sadikin Central General Hospital Bandung. High-performance liquid chromatography with an ultraviolet detector set at 245 nm was the analytical technique. One hundred percent methanol was used as the mobile phase, and it was isocratically eluted at a flow rate of 0.6 mL/min with a T3 column maintained at 25°C. The results indicated that the following Vitamin K1 levels were found in lettuce: 38.4391 ± 15.2650-64.4419 ± 19.0315 µg/100 g, in napa cabbage: 56.7445 ± 0.1569-273.2828 ± 8.3061 µg/100 g, in cabbage: 27.9531 ± 1.7487-217.0457 ± 7.2201 µg/100 g, and in spinach: 305.2868 ± 3.3058-970.7098 ± 14.1167 µg/100 g. The highest Vitamin K1 level was in spinach and the lowest was in lettuce.

Voriconazole (VOR) is a triazole antifungal agent; it blocks the synthesis of ergosterol, available in the market orally and intravenously, but, not without various side effects. The aim of this study is development and characterization of VOR oleogel for the topical treatment of skin fungal infection to avoid the drug's systemic side effects that are associated with oral and IV routes. The gelator Span 60 (S) was added at different concentrations to different oils (oleic OO, grapeseed GO, and sesame oil SO) to obtain the minimum gelation concentration, the prepared formulas were subjected to various evaluation tests, and the optimum formula was checked for antifungal effect, and subjected to viscosity, and texture analysis. The optimized formula, Span60 with SO 14SSO, showed 100% drug release, good antifungal activity, and acceptable transition temperature. The study of viscosity demonstrated the pseudo-plastic shear thinning behavior. A Fourier-transform infrared study showed that the drug and excipients did not significantly interact. 14SSO might be a promising topical treatment option for skin fungal infections.