Indonesian Journal of Pharmacy
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Anredera cordifolia Extract in Reducing Immunoglobulin E Expression in Wistar Rats Allergic Model
Full text linkAnredera cordifolia (AC), the binahong plant in Indonesia, has been extensively used in herbal medicine since ancient times. AC contains secondary metabolites, such as flavonoids, with anti-oxidative, anti-inflammatory, anti-mutagenic, and anti-carcinogenic properties. Many flavonoid compounds with anti-inflammatory activity can potentially treat nasal inflammation, such as allergic rhinitis. This study aims to determine whether there is a decrease in IgE expression after AC extract administration in the Wistar rats allergic model. The research was conducted on 36 Wistar rats classified into nine groups: control group (K1), negative control group (K2), positive control group (K3), treatment group with hydrogel intranasal AC extract of 2.5% (P1), 5% (P2), and 7.5% (P3), and treatment group with oral AC extract of 25 mg/200 g BW (P4), 50 mg/200 g BW (P5), and 75 mg/200 g BW (P6). Afterward, ELISA examined the expression of IgE. The t-test results for treatment groups applied with hydrogel intranasal AC extract of 2.5% revealed a significant difference in decreasing IgE levels. In conclusion, the finding supports that AC extract exerts its anti-allergy properties by suppressing IgE levels in the Wistar rats allergic model
Extraction Method and Solvent Effect on Antioxidant and Anti-lipase Activities of Nostoc sp. MRB-1 from the Peatlands in Oxbow Hanjalutung Lake, Indonesia
No full textThe increasing utilization of microalgae as a natural resource of bioactive compounds encourages finding efficient and cost-effective ways to extract those compounds. Therefore, the present study aimed to evaluate two solvents and two extraction methods to obtain extracts of microalgae Nostos sp. MRB-1. The extracts were evaluated regarding phenolic content, antioxidant, and anti-lipase activities. The results showed that maceration using ethanol obtained the highest phenolic content (11.77±1.47 GAE mg/g dry extract) and anti-lipase activity with the value of 23.01±1.66% at 0.38 mg/mL. While the extract obtained from the ultrasound using hexane exhibited the highest antioxidant activity with a value of 39.68±0.07% at 0.8 mg/mL. These results demonstrate that maceration using ethanol is more effective for phenolic extraction from microalgae. In microalgae, phenolic content positively correlates with anti-lipase activity, but the opposite was verified, phenolic compounds are not contributors to the antioxidant activity of Nostoc sp. MR-1 extrac
Retrospective Study of COVID-19 Impact on Medication Use
Full text linkThe coronavirus disease 2019 (COVID-19) pandemic shifted the medicine utilization landscape in hospitals globally.The purpose of this study was to assess changes in medication utilization throughout the course of the COVID-19 pandemic. A retrospective, descriptive study on medication use was conducted at a tertiary referral hospital in Malaysia. The study covered two periods: from 1 January 2018, to 31 December 2019 (pre-pandemic phase), and from 1 January 2020 to 31 December 2021 (pandemic phase). The analysis included 266 medicines, and the results indicated that a majority of the medications (n=142, 53.4%) experienced a decline in purchasing trends during the pandemic period (2020-2021). Notably, parenteral medications such as muscle relaxant cisatracurium besylate 2 mg/ml injection (1583.3%), vasopressin 20IU/mL injection (796%), vitamin B and C injection (672.9%,) and oral antipsychotic olanzapine 5mg (534.4%) witnessed an exponential increase in purchases. Conversely, several classes of medicines exhibited a decline in purchasing trends ranging from -45.7% to -73.7%. Notable decreases were observed in peptic ulcer medication, diuretics, and nasal decongestants. This study provides valuable insights into medication utilization trends, offering guidance to healthcare supply chain stakeholders in optimizing logistics operations, ensuring medication availability, and making informed decisions to enhance patient care and resource allocation
Optimization of HPMC and Carbopol 940 as Gelling Agents on The Physical Properties and Stability in Anti-Acne Gel of Binahong Leaves (Anredera cordifolia (Ten.) Steenis Extract
No full textBinahong (Anredera cordifolia (Ten.) steenis) is recognized as a widespread plant species in Indonesia and is known to possess strong antibacterial properties against P. acnes. This study aims to determine the effect and optimum proportion of hydroxypropyl methylcellulose (HPMC) and carbopol 940 as the gelling agent on the physical properties of binahong anti-acne gel. The Simplex Lattice Design (SLD) method was performed to optimize the gel base with Design-Expert® version 13.0.0 with a total run of 8 formulas. The evaluated parameters were organoleptic, homogeneity, pH, viscosity, spreadability, adhesion, stability, and irritation test. The independent variables in SLD were the amount of HPMC and carbopol 940, while the responses included pH, viscosity, spreadability, and adhesion. The optimal formula proposed by SLD is a combination of 1.96% HPMC, and 0.53% carbopol 940 that showed no significant difference when compared to the test results. The optimal formula has a pH of 6, a viscosity of 18,130 cP, a spreadability of 4.7 cm, and an adhesion of 10 second. The optimum formulation proved to be physically stable after three freeze-thaw cycles and showed no irritation after in vivo application
Evaluating the Impact of a Modified UCMS Protocol with a Psychological Stress Device on Neurobiological and Behavioral Responses in Rats
Full text linkThe antidepressant effect of drugs can be tested using various methods, including unpredictable chronic mild stress (UCMS). Although the initial UCMS protocol involved administering stressors for 21 days, many modifications have been made, one of which is shortening the duration of the stressors to 10-15 days. This study aims to modify the UCMS model to increase the stress response in male Wistar rats. UCMS protocol in this study did not use predator odor (2,5-dihydro-2,4,5-trimethylthiazoline) as in the previous protocol, but a psychological stress device (PSD) was used instead. Forty male Wistar rats (150-200 grams) were given UCMS treatment for 10 and 15 days. Sucrose consumption, coat score, body weight, and serum corticosterone levels were measured. Immunohistochemical examination of 5-HT1A receptors, TNF-α, NOX2, and NF-ĸB were performed in the hippocampus part of the brain. All data were analyzed using the Mann-Whitney test. UCMS treatment for 10 and 15 days reduced sucrose consumption and body weight and increased the coat score. UCMS treatment increased corticosterone levels, decreased 5-HT1A receptor expression, and increased TNF-α, NOX2, and NF-ĸB expression. The primary behavioral response during PSD was head dip as a preparatory behavior for jumping. Modifying the UCMS model using a PSD can increase the stress response
Design and Evaluation of The Floating Oral In Situ Gelling System of Levofloxacin Hemihydrate to Dysphagia Patients
Full text linkPediatric, geriatric, and dysphagia patients often experience difficulty swallowing solid preparations and discomfort when administered by injection. Levofloxacin is marketed as available in tablet and injection forms, such as in Indonesia. This study aims to develop an aqueous dispersion formulation for a floating oral gelling system of levofloxacin hemihydrate with sustained release delivery. HPMC and sodium alginate were combined as polymers to form an in situ gel system in an acidic environment. The optimization was performed based on the simplex lattice mixture design method. The effect of variations in the concentration of both polymers influenced the viscosity of the formula. The optimum formula was 0.378% sodium alginate and 0.122% HPMC. The drug release mechanism of the optimum formula followed the Korsmeyer-Peppas model. The kinetic mechanism of drug release fits into 2-compartment. The developed formulation offers augmented gastric retention of levofloxacin hemihydrate, leading to improved efficacy
VALIDATION OF HPLC METHOD FOR TIMOLOL MALEATE DETERMINATION IN NANO-POLYMERIC FORMULA
No full textIn this study, a sensitive, selective, and precise HPLC method for the detection of timolol maleate (TM), one of the anti-haemangioma ß-blockers, in nano-polymeric formulation was developed. Chromatographic separation was achieved using a mobile phase of 10 mM ammonium acetate buffer pH=3.5: acetonitrile (80:20, v/v) in isocratic mode of elution at a flow rate of 1.0 ml/min on Luna Phenomenex C18 ODS column (150mm x 4.6mm, 5μm). Validation has been performed on the method's system suitability, selectivity, linearity, accuracy, precision, and robustness. The results showed that the precision and uniformity values of the nanoparticle samples were within an acceptable range for both between and within days. The retention time of timolol maleate was observed to be around 6.8 minutes in the absence of any peak intervention. The standard curve exhibited a strong linear relationship, and the recovery values satisfied the specified range criteria consistently over a period of three consecutive days. After different ways of making sample preparations, which should affect the amount of contained drug, the employed technique successfully determined the percentage of drugs encapsulation in a nanopolymer formulation with dependable outcomes. The penetration profile of the nanoparticle formula and free drugs on mouse skin membranes was successfully determined utilizing the same approach that had previously undergone an extra verification step. The improved and validated method has proven its reliability and suitability in measuring the amount of timolol maleate in nano-polymer products to evaluate the efficiency of encapsulation and its penetration profile, which is a crucial factor in building drug delivery systems utilizing nanotechnology
Unveiling Metabolite Compounds and Anti-Inflammatory Properties from Chromolaena odorata in Three Geothermal Areas
Full text linkOne of the medicinal plants commonly used as traditional medicine due to its anti-inflammatory properties is Chromolaena odorata (L). As invasive plants have the ability to tolerate heat in extreme heat conditions, the underlying processes that explain their anti-inflammatory actions remain unclear. This study investigates the potential targets of C. odorata from three geothermal areas (Ie-Brôuk, Ie-Jue, and Ie-Seu’um) in Aceh Province, as anti-inflammatory using network pharmacology and molecular docking. C. odorata was extracted using an ethanol solvent and further analyzed using gas chromatography-mass spectroscopy. The antioxidant capacity of each plant was examined using 2,2-diphenyl-1-picrylhydrazyl-hydrate (DPPH)-scavenging with dose-response models. Next, the structure of metabolite compounds was characterized using cluster analysis with the FragFP descriptor. Targets for the identified compounds were predicted, and protein-protein interaction networks were constructed. To better understand the biological roles of intersecting genes, pathway enrichment analyses were performed using Gene Ontology and the KEGG pathway. The results showed that ethanolic extract of C. odorata from Ie-Seu'um, Ie-Jue, and Ie-Brouk had DPPH-scavenging values of 46.84, 44.79, and 95.78 ppm, respectively. From network pharmacology perspective, this study highlights the intricate molecular interactions involved, focusing on inhibitory protein kinases and their associated genes. The molecular docking analysis underscores the therapeutic potential of C. odorata ethanolic extracts, especially those from the Ie-Brôuk area, which contain active compounds such as sakuranin, lupeol, and β-stigmasterol has highest binding-free energy value. This study offers insightful information about the anti-inflammatory properties of C. odorata, paving the way for further research and potential therapeutic applications
The Potency of Soil Actinomycetes Extracts as Antibiofilm Agents against Enterococcus faecalis
No full textBackground. Enterococcus faecalis is a bacterium often found in root canal infections. Its virulence and biofilm formation can cause persistent apical periodontitis. Actinomycetes are Gram-positive bacteria known to produce a wide variety of novel biologically active compounds, including antibacterial, antitumor, immunosuppressive agents, and enzyme inhibitors. This study aimed to determine the potency of Actinomycetes extracts from Gunungkidul and Pontianak soil, Indonesia, as antibiofilm agents against E. faecalis and to identify the possible related primary compounds present in the active extracts.
Materials and Methods. Actinomycetes extracts, Streptomyces sp. GMR22 (from Gunungkidul) and Streptomyces sp. ACT214 (from Pontianak) were tested for its antibacterial and antibiofilm activity against E. faecalis through microbroth dilution assay and scanning electron microscopy (SEM) imaging. Primary compounds present in the active extracts were analyzed using untargeted liquid chromatography-tandem high-resolution mass spectrometry (LC-HRMS).
Results. Streptomyces sp. ACT214 demonstrated potent antibacterial activity with a minimum inhibitory concentration (MIC) of 1,250 ppm and a minimum bactericidal concentration (MBC) of 5,000 ppm. Otherwise, GMR22 did not reach MIC or MBC at the highest concentration tested (5,000 ppm). Streptomyces sp. ACT214 also exhibited concentration-dependent antibiofilm effects, fully preventing E. faecalis biofilm formation at 582 ppm (MBIC90) and disrupting biofilm formation under SEM observation. In contrast, GMR22 showed a lower inhibition effect.
Conclusion. This result suggests that Actinomycetes extract from Pontianak soil, Indonesia has potential as an antibiofilm agent against E. faecalis. As a potential source of new antibiotic compounds, these soil Actinomycetes extracts warrant further exploration as alternative treatments targeting E. faecalis biofilm in recalcitrant apical periodontitis cases
Study of Formyl and Phenyl Substituted Styrylpyrazolines: Synthesis, In Vitro Antibacterial Evaluation¸ and Molecular Docking against DNA Gyrase
No full textBacterial resistance to most antibiotics remains a persistent challenge, urging the need for the development of novel antibacterial agents. Styrylpyrazoline derivatives have shown diverse biological activity, including as an antibacterial. This study synthesized and evaluated styrypyrazolines 2a and 2b for their antibacterial activity against Gram-positive and Gram-negative bacteria (Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa). The in vitro evaluation was performed using disc diffusion and microdilution methods. The result revealed that both compounds have the highest inhibition against S. aureus. Moreover, the presence of formyl group (-CHO) on styrylpyrazoline 2a enhanced its inhibitory activity against P. aeruginosa. Neither compound showed significant inhibition against B. subtilis or S. epidermidis. Molecular docking of both compounds against DNA gyrase subunit B was performed to further investigate their antibacterial mechanism. It was revealed that both compounds are able to interact with the receptor within the ATP-binding pocket. Similar to ciprofloxacin, compound 2a formed hydrogen bonds with the Asp81 residue, showing its potential as a DNA gyrase inhibitor. While compound 2b formed aromatic-hydrogen bridging with Pro87 residue. This study suggests that styrypyrazolines 2a and 2b possess promising antibacterial activity. However, their potency is lower than the reference drug. Thus, further modification of the structure is necessary to enhance their potency as antibacterial agents.
Keywords: styrylpyrazoline, antibacterial, DNA gyrase, dockin