Free Radical Scavenging Capacities and Alleviating Actions of Polysaccharides Extract of Termitomyces le-testui on Methylprednisolone-Induced Immunodepression in RatsRead the full article
Advances in Pharmacological and Pharmaceutical Sciences publishes original research articles and review articles in all areas of experimental and clinical pharmacology, pharmaceutics, medicinal chemistry and drug delivery.
Advances in Pharmacological and Pharmaceutical Sciences maintains an Editorial Board of practicing researchers from around the world, to ensure manuscripts are handled by editors who are experts in the field of study.
Latest ArticlesMore articles
ACE2 : S1 RBD Interaction-Targeted Peptides and Small Molecules as Potential COVID-19 Therapeutics
The COVID-19 pandemic that began in late 2019 continues with new challenges arising due to antigenic drift as well as individuals who cannot or choose not to take the vaccine. There is therefore an urgent need for additional therapies that complement vaccines and approved therapies such as antibodies in the fight to end or slow down the pandemic. SARS-CoV-2 initiates invasion of the human target cell through direct contact between the receptor-binding domain of its Spike protein and its cellular receptor, angiotensin-converting enzyme-2 (ACE2). The ACE2 and S1 RBD interaction, therefore, represents an attractive therapeutic intervention to prevent viral entry and spread. In this study, we developed a proximity-based AlphaScreen™ assay that can be utilized to quickly and efficiently screen for inhibitors that perturb the ACE2 : S1 RBD interaction. We then designed several peptides candidates from motifs in ACE2 and S1 RBD that play critical roles in the interaction, with and without modifications to the native sequences. We also assessed the possibility of reprofiling of candidate small molecules that previously have been shown to interfere with the viral entry of SARS-CoV. Using our optimized AlphaScreen™ assay, we evaluated the activity and specificity of these peptides and small molecules in inhibiting the binding of ACE2 : S1 RBD. This screen identified cepharanthine as a promising candidate for development as a SARS-CoV-2 entry inhibitor.
Effects of pH and Electrolytes on Castor Oil Emulsions with Various Stabilisers Using Khaya senegalensis Gum as an Emulsifier
Dispersed systems such as emulsions are easily destabilised during processing and storage since they are thermodynamically unstable systems. It is for this reason emulsifiers/stabilisers are frequently employed in pharmaceutical emulsion formulations to increase their short- and long-term kinetic stability. This current study seeks to investigate the potential emulsifying property of gums obtained from Khaya senegalensis (family: Meliaceae) trees. Gums were collected, authenticated, oven-dried, milled, filtered, and purified using 96% ethanol. The microbial quality of the gum was assessed following the BP (2013) specifications. The purified gum was free from some selected pathogenic microorganisms, rendering the gum safe for consumption. The emulsifying property was investigated by formulating emulsions using castor oil and employing the dry gum method. The ratios of oil-to-water-to-gum for the formulation of a stable emulsion were determined. The stability of the emulsion was evaluated, and an effort was made to improve the stability by incorporating Tween 80, hydroxypropyl methylcellulose, and xanthan gum. From the results, it can be inferred that Tween 80 (0.5%) was able to stabilise the emulsion. Addition of xanthan gum worsened the creaming. The effects of pH (4.0, 5.5, 7.2, 9.0, and 11.0) and electrolytes (0.1 M of NaCl, KCl, and CaCl2) on the physical stability of oil-in-water emulsions were studied during 12 weeks of storage. Percentage creaming volume and whether there was phase inversion were the criteria used as the evaluation parameter. From the percentage creaming volume data, emulsions formulated with both gums showed the lowest creaming volumes at pH of 7.2, followed by the acidic regions (pH 4.0, 5.5), with the basic regions (pH 9.0, 11.0) recording the highest creaming volumes. The effects of the various electrolytes at a constant concentration of 0.1 M on the o/w emulsions were found in this order NaCl < KCl < CaCl2. This study proves that Khaya senegalensis gum can successfully be employed as an emulsifying agent in pharmaceutical formulations.
Optimization of Growth Conditions and Biological Activities of Nepalese Ganoderma lucidum Strain Philippine
Ganoderma lucidum has been extensively studied for its valuable medicinal importance. In this study, the artificial cultivation of G. lucidum strain Philippine in different culture media, including sawdust substrate, was performed and optimized on the Potato Dextrose Agar (PDA) media. Phytochemical, antibacterial, and antioxidant analyses were performed and compared between the ethanol extracts prepared from two different cultures (fruit from synthetic log culture and mycelia from PDA media culture). Both the 200 mg/mL and 100 mg/mL concentrations of extracts inhibited all the tested bacteria, and the results were promising than the corresponding control using antibiotics. The fruit extract showed higher antioxidant potential (150.6 ± 56.92 mg ascorbic acid equivalent/g extract) than mycelial extract (144.28 ± 81.72 mg ascorbic acid equivalent/g extract). The results indicate that fruiting bodies of G. lucidum cultivated in a complex dust medium possess higher antioxidant properties than mycelia culture, which can be further explored for therapeutic applications.
Development and Validation of the Quantification Method for Hydroxychloroquine in Volumetric Absorptive Microsampling (VAMS) Using High-Performance Liquid Chromatography-Photodiode Array
Hydroxychloroquine is an antimalarial drug used for systemic lupus erythematosus, rheumatoid arthritis, and malaria treatment. However, hydroxychloroquine has several side effects such as ocular toxicity, neurotoxicity, gastrointestinal disorder, and also severe toxicity such as cardiotoxicity. Therefore, therapeutic drug monitoring of high dose or long-term use of hydroxychloroquine is needed. This study aims to obtain an optimum and validated analysis and preparation method for hydroxychloroquine in volumetric absorptive microsampling (VAMS) using the high-performance liquid chromatography–photodiode array detector based on the Food and Drug Administration guidelines (2018). Hydroxychloroquine quantification was performed using HPLC-PDA with Waters Sunfire™ C18 (5 µm; 250 × 4,6 mm) column. Mobile phase consists of acetonitrile-diethylamine 1% (65 : 35, v/v) (isocratic elution) and delivered at a flow rate of 0.8 mL/min throughout the 12 minutes run. Sample in VAMS is extracted by liquid-liquid extraction with ammonia 1% and n-hexane-ethyl acetate (50 : 50 v/v) as a extraction solvent. This method has successfully qualified the Food and Drug Administration (2018) parameters, with 2 ng/mL of LLOQ, range of calibration curve 2–6500 ng/mL, and coefficient of correlation 0.9993–0.9997.
Antiaging and Antioxidant Bioactivities of Asteraceae Plant Fractions on the Cellular Functions of the Yeast Schizosaccharomyces pombe
Research on antioxidants has been gaining worldwide attention because of their essential applications for medicinal purposes. In this study, we conducted bioprospecting of six Asteraceae plants as the source of antiaging and antioxidant agents. Water and chloroform fractions from Ageratum conyzoides L., Dichrocephala integrifolia (L.f.) Kuntze, Galinsoga parviflora (Cav.), Mikania micrantha Kunth, Sphagneticola trilobata (L.) Pruski, and Synedrella nodiflora L. were collected and assayed for their in vitro antioxidant activities and potential antiaging properties using the yeast Schizosaccharomyces pombe as the model organism. Based on the in vitro assay, the water fractions of S. trilobata showed a strong antioxidant activity. Interestingly, all treatment solutions promoted the stress tolerance phenotype of S. pombe to strong H2O2-induced oxidative stress conditions. Moreover, compared with the treatments without plant extract/fraction, all extract and fraction treatments, except the chloroform fractions of A. conyzoides, promoted yeast cell longevity. Strong induction of mitochondria activity was found following the treatments with the extracts and fractions of S. nodiflora, D. integrifolia, and M. micrantha and likely mimicked the calorie restriction-induced lifespan. Interestingly, S. nodiflora water fractions significantly upregulated the mRNA transcripts of the Pap1-mediated core environmental stress response, namely, ctt1 gene in S. pombe. These data indicated that the fractions of Asteraceae plants had potential antioxidant and antiaging activities through various cellular modulations. S. nodiflora water fraction has been shown to have antioxidant and antiaging activities in S. pombe, by modulating stress tolerance response, inducing mitochondrial activity, and increasing the ctt1 gene expression. Compounds analysis identified that S. nodiflora water fraction contained some primarily compounds including oxyphyllacinol, valine, and sugiol.
Wound-Healing Potential of Cucurbita moschata Duchesne Fruit Peel Extract in a Rat Model of Excision Wound Repair
Background and Aim. Pumpkin (Cucurbita moschata Duchesne) is a medicinal plant with different pharmacological effects such as antioxidant, antidiabetic, hepatoprotective, and anticancer effects. In the present study, we aimed to investigate wound-healing activity of pumpkin fruit peel in a rat model of excision wound repair. Materials and Methods. Hydroalcoholic extractions of pumpkin fruit peel were obtained and used to prepare two different cold cream-based formulations, namely, 10% and 20% pumpkin peel extracts (PPEs). These formulations, phenytoin cream, and cold cream were topically used once daily for 14 days to compare their wound-healing effects in a rat model of excision wound repair. Wound sizes were monitored at different intervals. Skin tissue samples were subject to H&E staining for histopathological analysis. Blood samples were also taken on day 14 to measure serum levels of nitrite. Results. Both 10% and 20% PPE formulations resulted in a significant reduction of wound sizes compared to positive and negative controls. Wound closure rate was estimated to be higher in 20% PPE-treated rats. According to histopathological analysis, treatment with 20% PPE improved parameters associated with efficient wound repair, including better regeneration of epidemic layer, higher density of dermis collagen fibers, and lower presence of inflammatory cells. Also, both formulations lowered serum concentrations of nitrite. Conclusion. Given the obtained data from our study, the hydroalcoholic extract of Cucurbita moschata Duchesne fruit peel is proposed to be effective in accelerating the process of excision wound repair partly due to its antioxidant effect in terms of decreasing nitrite concentration.