Indonesian Journal of Pharmacy
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Phytochemical Profile and Bioactivity of the Methanolic Leaf and Root Extracts of South African Bulbine frutescens
Get PDFBulbine frutescens is an indigenous succulent medicinal plant in South Africa. The plant is commonly used traditionally for the treatment of skin related ailments. B. frutescens has been reported to possess antioxidant, anti-viral and antimicrobial properties. To date, most studies have been conducted on the leaves, while limited reports have been documented on the roots, as well as comparative analyses between both plant parts. The aim of this study was to determine the phytochemical content, antioxidant and antibacterial activities in the leaves and roots of B. frutescens. Methanolic extracts of each plant part were assessed on the phytochemical analysis, antioxidant (DPPH, hydrogen peroxide, metal chelating) and antibacterial activity against S. aureus and E. coli. The results from the phytochemical screening showed that the leaves contained more phytochemical groups than the roots. The roots displayed higher total phenolics (991.7 ± 54.1 mg GAE/g), total flavonoid (285.8 ± 60.6 mg QE/g) and total tannin contents (1698.75 ± 28.15 mg GAE/g) than the leaves. The roots also showed a stronger antioxidant activity in DPPH (3.43 ± 0.16 mg/ml) and metal chelating (0.54 ± 0.01 mg/ml) assays, compared to the leaves, which only showed a higher scavenging power against hydrogen peroxide radicals (1.48 ± 0.02 mg/ml) than the roots. Both plant parts showed intermediate zones of inhibition (10-19 mm) against both bacterial strains, with the exception of the leaves which had a 20.67 ± 0.67 mm inhibition against S. aureus. These results validate the uses of both leaves and roots of B. frutescens in traditional medicine and further suggests for the application of the roots in pharmaceutical and cosmetic industries.Bulbine frutescens is an indigenous succulent medicinal plant in South Africa. The plant is commonly used traditionally for the treatment of skin related ailments. B. frutescens has been reported to possess antioxidant, anti-viral and antimicrobial properties. To date, most studies have been conducted on the leaves, while limited reports have been documented on the roots, as well as comparative analyses between both plant parts. The aim of this study was to determine the phytochemical content, antioxidant and antibacterial activities in the leaves and roots of B. frutescens. Methanolic extracts of each plant part were assessed on the phytochemical analysis, antioxidant (DPPH, hydrogen peroxide, metal chelating) and antibacterial activity against S. aureus and E. coli. The results from the phytochemical screening showed that the leaves contained more phytochemical groups than the roots. The roots displayed higher total phenolics (991.7 ± 54.1 mg GAE/g), total flavonoid (285.8 ± 60.6 mg QE/g) and total tannin contents (1698.75 ± 28.15 mg GAE/g) than the leaves. The roots also showed a stronger antioxidant activity in DPPH (3.43 ± 0.16 mg/ml) and metal chelating (0.54 ± 0.01 mg/ml) assays, compared to the leaves, which only showed a higher scavenging power against hydrogen peroxide radicals (1.48 ± 0.02 mg/ml) than the roots. Both plant parts showed intermediate zones of inhibition (10-19 mm) against both bacterial strains, with the exception of the leaves which had a 20.67 ± 0.67 mm inhibition against S. aureus. These results validate the uses of both leaves and roots of B. frutescens in traditional medicine and further suggests for the application of the roots in pharmaceutical and cosmetic industries
Formulation and Evaluation of Luliconazole nanosponge gel using Experimental design
Get PDFDifferent approaches are being in the practice for the topical application of antifungal drugs, although in a few cases, they have been found less efficient because of their poor cutaneous availability and permeability. Luliconazole (LUL) is one of the antifungal medications that is being used for the treatment of various superficial infections. The poor permeability of LUL is regarded to be a factor for its reduced efficacy. Hence, the current study aimed to develop a nanosponge hydrogel that would improve dermal availability and permeability. A set of nanosponge formulations (L1-L18) were designed with the help of central composite design (Design Expert 13, state ease Inc., Minneapolis, MN, USA). L1-L18 was prepared by using the emulsion solvent evaporation technique. The nanosponges were characterized for drug-excipient compatibility (FTIR, P-XRD, and DSC), and particle size, polydispersibility index, zeta potential, entrapment efficiency (EE), and in vitro drug release; further optimized. The optimized nanosponge formulation (L18) was taken to produce six hydrogels (LF1-LF6) of LUL by varied proportions of the gelling agent. In this process, initially, the gel was constituted with Carbopol 934/ sodium CMC/HPMC. Later, attained hydrogel texture was evaluated for its viscosity, swelling, and membrane permeability, followed by in vitro drug release, and antifungal efficacy study. The nanosponge formulations (L1-L17) had an average particle size of 109±0.45 to 386±0.34 nm, entrapment efficiency of 35.45±0.46- 89.65±0.37 % with 84.67±0.54 -99.65±0.48 % of drug release for 8 h. The formulation L18 was predicted with better responses in particle size, EE, and drug release i.e., 378±0.25 nm, 84.65±0.45%, and of 96.18±0.54%, respectively for 8 h. Out of six formulated nanosponge gels (LF1-LF6), LF2 showed an optimal viscosity (25.69 ±0.45 pa.S), pH (6.87±0.56) and % drug release (80.65 ±0.64%) in 8 h. Drug release was governed by non-fickian diffusion mechanisms and zero-order. Developed nanosponge hydrogel was found as stable and had a high rate of permeation with better retention which can be effective enough in topical applications
Network Pharmacology and Molecular Mechanism of Traditional Indonesian Medicine in Hypertension Treatment
Get PDFScientific herbal formulations are used clinically to treat hypertension, but their functional molecular mechanisms remain to be elucidated. This study was identified the molecular pathways by which scientific herbal remedies for treating hypertension work. The identified compounds were then excluded by measuring oral bioavailability and drug similarity. The network was created using Cytoscape version 3.8, and the predicted target information was obtained from a number of databases, including SwissTarget Prediction, STRING, Online Mendelian Inheritance in Man (OMIM), and Kyoto Encyclopedia of Genes and Genomes (KEGG). The decoction’s method for lowering hypertension was then clarified using an enrichment analysis. It was discovered that bioavailability and drug similarity metrics existed for a total of 44 identified substances. The results of pathway analysis using KEGG revealed that the potential targets were correlated antihypertensive mechanism of herbal medicine such as the HIF-1 signaling pathway, Relaxin signaling pathway, PI3K signaling pathway, and MAPK signaling pathway. Scientific herbal formulas' pressure-lowering mechanisms include those related to vascular endothelium and atherosclerosis, which involve several signaling pathways such as the HIF-1 signaling pathway, the Relaxin signaling pathway, the PI3K signaling pathway, and the MAPK signaling pathway
Gut Microbiota Dynamics and Phenotypic Changes Induced by Tetracycline in Drosophila melanogaster
Get PDFGut microbiota plays a crucial role in both physiological and pathological processes in humans and animals. Antibiotics, designed to combat bacterial infections, can induce alterations in the composition and abundance of the gut microbiota over prolonged exposure. This study addresses the limited understanding of the connections between gut microbiota and phenotypic profiles of metazoan species. We investigated the impact of early-life exposure to tetracycline in wild-type D. melanogaster, which were fed a standard diet, comparing them to a control group not exposed to tetracycline. The primary objective was to examine the consequences of early-life tetracycline exposure on gut microbiota and its implications for phenotypic profiles, including survival, locomotor activity, and reproduction in adult flies. Results revealed a significant reduction in lactic acid bacteria in adult flies exposed to tetracycline. However, tetracycline exhibited no interference with fly development, allowing them to maintain a normal lifespan. In adult flies, tetracycline significantly decreased the lifespan on day 35 at a concentration of 1000 µg/mL and reduced locomotion on day 27 at concentrations of 10 µg/mL and 1000 µg/mL. Remarkably, tetracycline did not impact the reproductive capabilities of the flies. This study demonstrates that while tetracycline led to a decline in lactic acid bacteria, locomotion, and lifespan in adult flies, it did not disrupt their development or reproductive processes
Formulation and Hair Growth Activity Test of Cinnamon Essential Oil (Cinnamomum burmannii) Nanoemulsion-Based Serum
No full textBaldness can result from hair loss, which can also affect a person's mental health. It is preferable to use natural hair growth products in place of synthetic ones because of their limits. It is possible for cinnamon essential oil (CEO) to promote hair growth. CEO's cinnamaldehyde molecule is irritative and has low stability, which is why it was encapsulated in a nanoemulsion system. The goal of this research is to create the ideal CEO nanoemulsion serum, which will meet all requirements, actively promote hair growth, and not irritate users when used. In this study, the formula was optimized using D-optimal design and the spontaneous nano emulsification method was utilized to generate the nanoemulsion. Characteristics of the cinnamon oil nanoemulsion serum (CEONS) included pH, viscosity, organoleptic, droplet size and polydispersity index, and stability. For 28 days, the Tanaka method was used to study the hair growth activity test in terms of the weight and length of the male rabbits' hair. An in vivo cutaneous acute irritation test was used to evaluate the safety of the product. Propylene glycol (34.905%), CEO (12.686%), and cremophor RH 40 (52.408%) made up the ideal CEONS formula. The substance has a colourless, transparent, clear, and distinct scent. It also has a little viscous viscosity, with a pH range of 5.1 to 5.196, is non-irritating, and is stable. With a mean hair length of 2.4 cm ± 0.308 and a hair weight of 1.36 ± 0.16 g, the ideal CEONS droplet size was 44.31 ± 0.3024 with a PDI value of 0.25 ± 0.004. This droplet size was also able to accelerate hair development. According to the study's findings, CEO has greater hair growth activity than traditional oils and can be combined to create CEONS
Pharmacological Activities, Isolated Compounds, Toxicity, and Potential for New Drug Discovery from the Genus Leea
Get PDFThe genus Leea is a genus of medicinal plants. Half of this genus species are traditionally used to treat various ailments. This genus also holds promise for molecules that have the potential to be used as drugs or lead compounds in the discovery of a new drug. So far, 66 compounds have been isolated from this genus, 46 known to have pharmacological activity. Antioxidant, antimicrobial, anti-inflammatory and anticancer are the pharmacological activities most frequently found in these compounds. Although the toxicity studies are still limited to chronic toxicity tests showing low toxicity potential. The fact that various pharmacological activities and low potential make toxicity makes this plant worthy of continued study. The potential to possibility drugs from this genus is also huge
Hesperidin Enhanced the Antimigratory Activity and Senescence-Mediated G2/M Arrest Effect of PGV-1 Against T47D Luminal Breast Cancer Cells
Get PDFLuminal breast cancer cells exhibit proliferative and metastatic characteristics. Exploration of the effective treatment with minimum side effects is necessary. This study aimed to confirm the combination treatment of a potent anticancer candidate PGV-1 and hesperidin on luminal breast cancer cells, T47D, covering its cytotoxic and anti-migratory activities. PGV-1 showed much stronger cytotoxicity with an IC50 value of 2 μM than that of hesperidin (200 μM) as evaluated by trypan blue exclusion assay, but the combination of the two compounds exhibited a synergistic effect. Propidium iodide (PI) staining with flow cytometry proved that the combination treatment increased the cell population in the G2/M phase. Additionally, the combination treatment increased senescent cells as shown in senescence associated β-galactosidase (SA-β-gal) assay which might correlate to its antiproliferative properties. In addition, the scratch wound healing assay showed that the combination also inhibited cell migration significantly. Molecular docking of the two compounds demonstrated potential interaction with their protein targets in cell cycle machinery, i.e. KIF1, CDK1, TOP2A, CA12, ESR1, FN1, and TYMS. Altogether, these findings strengthen the evidence of anti-cancer properties enhancement of PGV-1 in luminal breast cancer through combining the compound with hesperidin
Validation of An HPLC Method for the Determination of Some Β-Lactams Antibiotics Using A Green Analytical Technique
Get PDFGreen analytical chemistry (GAC) primary goal is to develop environmental and health-friendly analytical methods by reduction or replacement of hazardous substances from analytical procedures. In this research, the application of GAC to quantify five β-lactams antibiotics (cefuroxime sodium, cefaclor, ertapenem sodium, ampicillin sodium and sulbactam sodium) by high-performance liquid chromatography (HPLC) using photodiode arrays (PDA) detector was developed. To achieve this, ethanol was used as a green replacement for methanol and acetonitrile, common solvents in chromatographic procedures. Several chromatographic conditions were investigated to accomplish the optimal conditions. The method validation followed the ICH Q2 (R1) guideline, and the developed method was successfully applied for quantifying some pharmaceutical products
Optimization of Spray Drying Process of Mangiferin Extract from Mango Leaf (Mangifera indica L.) and Encapsulation for Diabetes Treatment
No full textMangiferin is known as a major compound in mango leaves with various pharmacological effects such as antioxidant, antiviral, cancer, diabetes,... However, the poor solubility of mangiferin limits its pharmaceutical applications. Thus, this work’s major goal was to optimize the parameters of the spray-drying process in order to improve the dissolution of mangiferin in Mangiferin indica L. leaf extract and capsule formulation for diabetes treatment. Fourteen experiments were designed with Design Expert software and optimized process formulas with BC Pharsoft OPT software. Three independent variables were selected for surveying namely the ratio of mangiferin to excipients (X1), the ratio of maltodextrin in spray fluid composition (X2), and inlet air temperature (X3). The dissolution of mangiferin was shown as the percentage of this compound released within 5 minutes (Y1), 15 minutes (Y2), 30 minutes (Y3), and the percentage of hygroscopicity at 25oC (Y4). The results showed that the optimized spray drying process and formula which included the ratio of mangiferin and maltodextrin in the spray drying solution being 8.30% and 9.63%, respectively, the inlet air temperature of 156.26oC, blowing speed of 50 m3/s, pump flow of 3 mL/min possessed the dissolution of mangiferin in spray drying powder of 91.89 ± 2.43% at 30 minutes, the percentage hygroscopicity of 0.13 ± 0.13% at 25oC. The cause-effect relations and optimization of Mangiferin indica L leaf extract powder formulation were investigated and reported for the first time. The spray-dried powder capsule released more than 90% active ingredients in 30 minutes and showed significant hypoglycemic effects in inhibiting the α-glucosidase enzyme (IC 50 of 36.94 µg/mL equivalent to mangiferin in comparison with the commercial drug Glucobay (acarbose 176.09 µg/mL). In summary, the capsules containing the optimized formula of mangiferin spray-dried powder from Mangifera indica L. leaf extract have been successfully prepared and had potential antidiabetic effects in in-vitro settings
Validating the Instrument of Parents' Knowledge and Attitudes towards Giving Antibiotic for Children in two Hospitals at South Sulawesi
Get PDFTo translate, adapt and validate the instrument of Parents' Knowledge and Attitudes towards giving Antibiotics for Children. Participants were recruited from two hospitals in South Sulawesi, one private and one government hospital. The study started with the translation of the instrument from English to Indonesian (forward and backward translation). Next, the translation result was tested on 40 participants. The final stage was validation involving 300 participants. The analysis used known group validity, construct validity, product-moment correlation, and factor analysis. Internal consistency between items used Cronbach Alpha. A total of 300 participants (200 in private hospitals and 100 in government hospitals). From the participants, 113 participants were outpatients and 187 were inpatients. In the adaptation stage, some vocabulary changes were made to sentences that were not understood by participants in instrument items using words easily understood by the participants. For example, in the knowledge domain, the word "pathogen" was changed to ‘disease-causing bacteria’. In the validation stage, the significance value was 5%, and the r-table value was 0.113. Based on the validity test on 14 items in the knowledge domain, the r-count value was 0.256-0.589, while on 12 items in the attitude domain, the r-count value was 0.375-0.662. The Kaiser-Meyer-Olkin (KMO) value was 0.793. From 14 question items in the knowledge domain, 3 factors were formed. Cronbach alpha value of each domain was >0.6, knowledge (0.759) and attitude (0.744). Instrument reliability for outpatient and inpatient care was 0.768 and 0.752 for knowledge, 0.740 and 0.744 for attitude, respectively. The results of this study indicate that the instrument of Parents' Knowledge and Attitudes towards giving Antibiotics to Children is reliable and valid. This instrument can be used for both outpatients and inpatients