PT. ETFLIN Scientific Society (Sciences of Phytochemistry)
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Nano Liposomal Curcumin as an Adjuvant: Enhancing Cisplatin Anticancer Effects in HeLa Cells
Full text linkCervical cancer, mainly driven by oncogenic HPV infections, remains a global health burden. Cisplatin is standard chemotherapy for advanced cases but is limited by toxicity. Nano liposomal curcumin, with improved bioavailability, may enhance cisplatin’s efficacy. This study investigated the combination’s effect on HeLa cells by analyzing Cyclin E1 and Bcl-2 expression. Nano liposomal curcumin was synthesized using thin-film hydration, yielding stable 32 nm nanoparticles. HeLa cells were divided into control and treatment groups, and varying doses of nano liposomal curcumin with cisplatin were received. Flow cytometry revealed significant reductions in Cyclin E1 (from 18.62 ± 1.45 to 5.79 ± 0.47) and Bcl-2 (from 32.56 ± 0.82 to 28.19 ± 0.30) at the highest dose (p < 0.05). Cell viability decreased to 9% with cisplatin alone and 1% with the combination. These results indicate that nano liposomal curcumin enhances cisplatin’s antiproliferative and pro-apoptotic effects, supporting its potential as an adjuvant to lower cisplatin doses while maintaining efficacy. Further research involving additional molecular markers, in vivo models, and clinical trials is needed to optimize dosing, confirm safety, and evaluate therapeutic potential
The Effect of Poloxamer 188 on the Solubility and Dissolution Behaviors of Piroxicam-PEG 4000 Solid Dispersions
Full text linkPiroxicam (PRX), a non-steroidal anti-inflammatory drug (NSAID), is classified as a biopharmaceutical classification system class II (high permeability and low solubility), which limits its bioavailability. Enhancement of the dissolution rate is a key strategy to enhance the absorption. Solid dispersion systems, particularly when combined with amphiphilic multiple co-block polymers, offer a promising approach to address this challenge. This study aimed to investigate the effect of Poloxamer 188 (P188) and the solid dispersion technique on the solubility and dissolution rate of PRX. Polyethylene glycol (PEG) 4000-based solid dispersions containing PRX were prepared using varying concentrations of Poloxamer 188 surfactant through the fusion method. The solid dispersions were evaluated for saturated solubility in water for 24 hours. Selected formulations were further characterized using thermal analysis and vibrational spectroscopy. The optimized solid dispersion formulation was filled into capsules, and a dissolution assay was carried out to compare its performance with that of pure PRX capsules. The optimized formula, comprising 3% P188 and PEG4000, demonstrated a significant enhancement in saturation solubility parameters (p < 0.05), specifically the Cmax/S0 ratio. Additionally, dissolution testing showed a 22.22% increase in the dissolution rate of the PRX solid dispersion capsules compared to pure PRX capsules. In conclusion, P188-based solid dispersion containing PRX enhanced the solubility and dissolution rate, potentially improving therapeutic efficacy
Formulation and Stability Evaluation of Red Dragon Fruit (Hylocereus polyrhizus) Extract Gel
Full text linkRed dragon fruit (Hylocereus polyrhizus) is known for its strong antioxidant properties and potential anti-aging effects. To enhance its benefits and improve usability, this fruit extract was formulated into a gel preparation. This study aimed to determine the optimal proportions of Carbopol 940 and triethanolamine (TEA) to obtain a gel with desirable physical characteristics. The flesh of red dragon fruit was juiced and concentrated to produce an 8% extract. Three formulations were prepared with varying ratios of Carbopol 940 to TEA: 0.5%:0.3% (F1), 1.2%:0.7% (F2), and 2%:1.2% (F3). The gels were evaluated for physical properties, antioxidant activity, and antibacterial activity. The most promising formula was subjected to stability testing for three cycles under different temperature conditions: cold (3°C), room temperature (27°C), and climatic chamber (40°C, 75% RH). Results showed that formula F2 exhibited a characteristic red color, clear appearance, distinctive oleum rosae aroma, moderately thick and homogeneous consistency, viscosity of 3112.47 ± 177.90 cps, spreading diameter of 5.20 ± 0.20 cm, adhesion time of 18.45 ± 0.89 s, and pH of 5.33 ± 0.02. No significant changes were observed after the stability testing (p > 0.05), indicating that the formulation remained stable under all temperature conditions. F2 also showed higher antioxidant activity than F1 and better antibacterial properties than F3. Its stability and bioactivity support its potential as a promising natural cosmeceutical formulation
Evaluation of Total Flavonoid Content, Xanthine Oxidase Inhibition, and Uric Acid Inhibitory Activity In Vitro and In Vivo of Ethanol Extract of Sida rhombifolia
Full text linkSecondary metabolites content in Sida rhombifolia L. (SR) are believed to inhibit the xanthine oxidase (XO) enzyme, which is responsible for converting hypoxanthine and xanthine into uric acid. This study aimed to compare flavonoid levels, XO inhibitory activity, and the reduction of uric acid levels of sidaguri herb, stem, leaves, and root extract both in vitro and in vivo. The research results showed that the highest total flavonoid content in SR was found in the leaves, at 21.29±0.08 mg/QE/g extract. The IC50 values were as follows: roots (EESRR 1096.07±1.07 ppm), stems (EESRS 561.62±7.01 ppm), leaves (EESRL 101.84±0.63 ppm), and herbs (EESRH 104.70±3.50 ppm). EESR can inhibit the XO enzyme and has potential as an anti-hyperuricemia agent. The best total flavonoid content and IC50 values were observed in EESRL, which are 21.29±0.08 mg/QE/g and 101.84±0.63 ppm, respectively. EESRL at a dose of 400 mg/kg BW has the equivalent ability to reduce blood uric acid levels in mice when compared to the positive control group. Based on these findings, it can be concluded that EESRL has significant potential as a natural XO inhibitor and can be considered a promising candidate for the development of anti-hyperuricemia treatments
Enhanced Ability of Agarwood Leaves (Aquilaria malaccensis Lam.) Ointment as Wound Healing to Heal Second-Degree Burns in Rats
Full text linkAgarwood leaves (Aquilaria malaccensis Lam.) contain chemical substances such as alkaloids, flavonoids, and triterpenoids that contribute to the healing process of burns. This study aims to evaluate the wound healing activity of spray-dried extract from agarwood leaves formulated into an ointment for second-degree burns. The method involves extracting agarwood leaves through the decoction method, followed by spray drying, and subsequent evaluation of the extract. The prepared extract was then formulated into an ointment and tested for wound healing activity on 24 white rats of the Sprague-Dawley strain, divided into four groups, each consisting of 6 rats: negative control (ointment base), positive control (Betadine®), formula 1 (agarwood leaves extract ointment with 20% extract concentration - ALO-20), and formula 2 (agarwood leaves extract ointment with 30% extract concentration - ALO-30). Second-degree burns were induced by exposing the rats' backs to ferrous metal for 3 seconds and treating them for 14 days. Observations were made by assessing changes in burn diameter and scab formation. In this study, ALO-30 demonstrated superior activity. Scab formation was faster on day 3, and the burn diameter was reduced by day 7. The results indicated that ALO-30 led to a quicker reduction in wound diameter compared to ALO-20 and the negative control. Agarwood leaves extract ointment with a concentration of 30% (ALO-30) exhibited a more effective wound healing effect than the ointment with a 20% concentration (ALO-20)
Characterizations of Swelling Granule of Clove Leaf (Syzygium aromaticum L.) Ethanol Extract
Full text linkCloves, scientifically known as Syzygium aromaticum L., hold promise as a potential antiulcer remedy due to their rich composition of compounds, including high levels of phenolic compounds such as eugenol, eugenol acetate, and gallic acid. To improve bioavailability in the gastric environment, this study focuses on optimizing and evaluating a swelling granule system derived from clove leaf extract. The granules were produced using wet granulation with Carbopol, HPMC, and their combination as polymer matrices. Results indicated favorable properties in the swelling granules, with the optimal composition of 210 mg Carbopol, 36 mg PVP, and 404 mg Avicel pH 101. These granules exhibited a uniform particle size distribution, with 90.1% below 149 µm and 9.9% distributed across mesh numbers 100, 80, and 40. The formula with Carbopol polymer showed superior flow rate, compressibility, and swelling capacity compared to other formulations. The interaction between Carbopol's C=O groups and HPMC's hydroxyl groups significantly influenced parameters, especially swelling capacity. Thus, when combining polymers, potential chemical or physical reactions should be considered. The wet granulation process effectively preserved secondary metabolite levels from clove leaf. Further tests are recommended to evaluate the granulation's effectiveness as a delivery system for clove leaf extract
Effects of Methanolic Leaf Extract and Fractions of Irvingia Gabonensis on Hematological Parameters in Wistar Rats with Splenomegaly
Full text linkSplenomegaly is a medical condition characterized by an enlargement of the spleen, an organ located in the upper left part of the abdomen, beneath the ribcage. The spleen plays various essential roles in the body, including filtering blood, removing old or damaged blood cells, and helping the immune system by producing and storing immune cells. Splenomegaly causes negative haematological effects. It is very common in Africa and Asia. The aim of this study is to investigate the effect of methanol leaf extract and fractions of Irvingia gabonensis on haematological parameters in splenomegaly-induced Wistar rats. Extraction and fractionation of the plant were carried out through standard procedure using methanol, hexane, butanol and ethyl acetate. A qualitative phytochemical evaluation of the plant was done. The effects of the extract and fractions of Irvingia gabonensis were investigated using a rat model. The presence of various phytochemicals like alkaloids, flavonoids, steroids, terpenoids, and tannins was observed in the extract and fractions of the plant. The methanolic extract and ethylacetate fraction significantly caused the normalization of PCV, HB, and RBC post-treatment. The findings from this study suggest that Irvingia gabonensis could be researched further for the management of splenomegaly and also the isolation of phytochemicals responsible for these effects
Formulation and Characterization of Resveratrol-Loaded Nanostructured Lipid Carriers (NLC) with Mesua ferrea Seed Oil as Liquid Lipid
Full text linkNanostructured
Lipid Carriers (NLCs) are colloidal drug delivery systems composed of both
solid and liquid lipids. They enhance drug loading capacity, regulate the
release of poorly water-soluble drugs, and are suitable for targeted delivery.
Resveratrol, a polyphenol with promising anticancer properties, faces
challenges due to its low water solubility, poor bioavailability, and chemical
instability, resulting in rapid metabolism and excretion. Therefore, it is
crucial to develop a delivery system that safeguards resveratrol during its
transit through the body. This study aimed to develop and characterize
resveratrol-loaded NLCs using the nano-precipitation method followed by
ultrasonication, incorporating Mesua ferrea seed oil as the liquid
lipid. The NLCs were evaluated for particle size, morphology (TEM), zeta
potential, drug entrapment efficiency, drug loading, and in vitro drug release.
The resulting NLCs demonstrated stability and homogeneity, with a particle size
of 181.6 ± 12.4 nm, a polydispersity index (PDI) of 0.135 ± 0.09, drug
entrapment efficiency of 82.76 ± 12.2%, and drug loading capacity of 42.94 ±
7.5%. They exhibited sustained drug release, achieving 84.56% release within 24
h. These findings suggest that the developed NLCs can effectively enhance
the incorporation and controlled release of poorly water-soluble drugs like
resveratrol, offering potential advantages over conventional delivery systems
Characterization, In Silico Antimalarial, Antiinflammatory, Antioxidant, and ADMET Assessment of Neonauclea excelsa Merr.
Full text linkIn our study, we identified the phytoconstituents and carried out antimalarial, anti-inflammatory, antioxidant, and ADMET assessments of Neonauclea excelsa. The phytochemicals were detected and quantified followed by identification via GC-MS. The antimalaria, anti-inflammatory, and antioxidant assessments were done by molecular docking (MD) and molecular dynamics simulation (MDS) while ADMET by ADMET predictions. Saponins (27.33% ±1.20) and terpenes (8.33% ±0.73) were detected while alkaloids, steroids, glycosides, and flavonoids were absent. Exactly 29 compounds were identified with squalene being the most abundant (32.41%). Compound II exhibited the lowest BA (-6.4 kcal/mol) and Ki (20.12 µM), interacting with dihydrofolate reductase-thymidylate synthase. IV exhibited the lowest respective BA and Ki interacting with Plasmodium falciparum hexose transporter protein 1 (-6.2 kcal/mol and 28.20 µM), cyclo-oxygenase-2 (-7.2 kcal/mol and 5.21 µM), and myeloperoxidase (-7.4 kcal/mol and 3.71 µM). Compound VII had the lowest respective BA and Ki interacting with inducible nitric oxide synthase (-8.0 kcal/mol and 1.35 µM), xanthine oxidase (-7.2 kcal/mol and 5.21 µM), and cytochrome p450 21A2 (-7.0 kcal/mol and 7.30 µM). The MDS showed various cluster mobilities and residue fluctuations up to 5.26, 2.96, 5.10, 3.51, 5.02, 4.65, and 6.18 Å for dihydrofolate reductase-thymidylate synthase, Plasmodium falciparum hexose transporter protein 1, inducible nitric oxide synthase (INOS), cyclo-oxygenase-2 (COX2), xanthine oxidase (XO), cytochrome p450 21A2, and myeloperoxidase, respectively. Additionally, these compounds demonstrated good pharmacological properties with minimal toxicity. Conclusively, the identified compounds might be significant contributors to the antimalarial, anti-inflammatory, and antioxidant activity of N. excelsa and are good sources of novel antimalarial, anti-inflammatory, and antioxidant drugs
Bioactive Compounds of Rosa canina L. and Their Effect on Tumor Necrosis Factor-α and Interleukin-1β Activity in Diabetes-Induced Rats
Full text linkThe ethnopharmacological significance of Rosa canina, or dog rose, transcends diverse cultures, with traditional applications in treating various diseases. This study investigates the potential pharmacological application of Rosa canina for diabetes treatment, aiming to assess its antidiabetic properties through in vitro, in vivo, and in silico analyses targeting pro-cytokines. Biochemical profiling utilizing HPLC, and phenolic content analyses were conducted to reveal the antioxidant properties of Rosa canina. In diabetic rats, root extracts influenced the expression of TNF-α and IL-1β, with an exploration of DNA-binding and protective activities. DPPH scavenging and iron chelating activities were measured, identifying significant IC50 values. The chromatographic analysis identified various compounds, with Kaempferol 3-O-glucoside and Rutin exhibiting high inhibitory activity against TNF-alpha. In silico analyses highlighted inhibitory activities by molecular docking against TNF-α and IL-1β (PDB IDs 2AZ5 and 9ILB, respectively) and their drug potential based on ADMET properties. The obtained results have demonstrated a significant decrease in blood glucose levels in mice through the reduction of TNF-α and IL-1β mediated diabetic processes, facilitated by the Rosa canina extract. In conclusion, this study exploring the effects of Rosa canina extracts on diabetic rats have provided valuable insights into its potential therapeutic benefits. The observed reductions in blood glucose levels, improvements in lipid profiles, and modulation of antioxidant activity highlight its promising role in managing diabetes-related complications. Further research is warranted to elucidate the underlying mechanisms and optimize the dosage regimens for harnessing the full therapeutic potential of Rosa canina extracts in diabetes management