Advances in Pharmacological Sciences最新文献

The current focus of nanotechnology is to develop environmentally safe methodologies for the formulation of nanoparticles. The phytochemistry of Zingiber officinale inspired us to utilize it for the synthesis of iron nanoparticles. GC-MS analysis revealed the phytochemical profile of ginger. Out of 20 different chemicals, gingerol was found to be the most potent phytochemical with a retention time of 40.48 min. The present study reports a rapid synthesis method for the formation of iron nanoparticles and its potential efficacy as an antibacterial agent and an antioxidant. Because of its antibacterial property, ginger extract was used to coat surgical cotton. Synthesized ginger root iron nanoparticles (GR-FeNPs) were characterized by UV-visible spectroscopy, Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction analysis, and particle size analysis. XRD confirmed the crystalline structure of iron oxide nanoparticles as it showed the crystal plane (2 2 0), (3 1 1), (2 2 2), and (4 0 0). The particle size analyzer (PSA) showed the average size of the particles, 56.2 nm. The antimicrobial activity of the FeNPs was tested against different Gram-positive and Gram-negative bacteria. E. coli showed maximum inhibition as compared with the other organisms. Antioxidant activity proved the maximum rate of free radicals at 160 µg/mL produced by nanoparticles. In addition, the antimicrobial activity of nanocoated surgical cotton was evaluated on the first day and 30^th day after coating, which clearly showed excellent growth inhibition of organisms, setting a new path in the field of medical microbiology. Hence, iron-nanocoated surgical cotton synthesized using green chemistry, which is antimicrobial and cost effective, might be economically helpful and provide insights to the medical field, replacing conventional wound healing treatments, for better prognosis.

Bergapten (5-methoxypsoralen, 5-MOP) is a plant-derived furocoumarin with demonstrated anti-inflammatory action. The present study investigated its effects on allergic inflammation in two related pathways of mast cell degranulation. Compound 48/80 and lipopolysaccharide (LPS) were used to activate the IgE-independent pathway while bovine serum albumin (BSA) was used as allergen for the IgE-dependent pathway. The modulatory effect of bergapten on mast cell degranulation, neutrophil extravasation, protein concentration, lung histopathology, and oxidative stress was assessed. Bergapten at 10, 30, and 100 μg/ml for 15 min stabilized mast cells in rat mesenteric tissue from disruption in vitro and when administered in vivo at 3, 10, and 30 mg kg^-1 for 1 h protected mice from fatal anaphylaxis induced by compound 48/80. Similarly, treatment of LPS-challenged mice with bergapten (3, 10, and 30 mg kg^-1) for 24 h significantly decreased neutrophil infiltration into bronchoalveolar lavage fluid, mean protein concentration, and inflammatory cell infiltration of pulmonary tissues when compared to the saline-treated LPS-challenged control. In addition, lung histology of the bergapten-treated LPS-challenged mice showed significantly less oedema, congestion, and alveolar septa thickening when compared to the saline-treated LPS-challenged disease control. LPS-induced oxidative stress was significantly reduced through increased tissue activities of catalase and superoxide dismutase and reduced malondialdehyde levels on treatment with bergapten. In the triple antigen-induced active anaphylaxis, daily administration of bergapten at 3, 10, and 30 mg kg^-1 for 10 days, respectively, protected previously sensitized and challenged mice against anaphylactic shock. Overall, our study demonstrates the ability of bergapten to attenuate allergic airway-induced hypersensitivity in murine models of inflammation, suggesting its possible therapeutic benefit in this condition.

Clausena anisata is one of the medicinal plants used traditionally for treatment of parasitic infections, irritation (boils, ringworm, and eczema), flatworm infestations, influenza, abdominal cramps, and constipation. Phytochemical screening test of dichloromethane/methanol (1 : 1) roots extract revealed the presence of flavonoids, phytosterols, coumarins, phenols, alkaloids, tannins, terpenoids, and free reducing sugars and the absence of saponins. Silica gel column chromatographic separation of the dichloromethane/methanol (1 : 1) extract afforded a carbazole alkaloid derivative of heptazoline (1) and three coumarins (2-4), including the known coumarins imperatorin (3) and chalepin (4). Structures of the compounds were elucidated by spectroscopic techniques (IR, ¹H NMR, ¹³C NMR, and DEPT-135). Antibacterial activity of the crude extracts and isolated compounds was screened using agar diffusion method against strains of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Bacillus substilis. The results of antibacterial test revealed derivative of heptaphylline (1) and imperatorin (3) exhibited comparable antibacterial activity against S. aureus and B. substilis (14 and 13 mm zone of inhibition, respectively) to that of ciprofloxacin (15 mm zone of inhibition) at a concentration of 20 µg/mL. Chalepin (4) revealed more antibacterial activity against B. substilis (16 mm zone of inhibition) compared to ciprofloxacin (15 mm).

The nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed by medical practitioners in many clinical conditions for the symptomatic treatment of pain and fever. Due to their anti-inflammatory properties, these drugs have been investigated for their anticancer effects in numerous studies. This is because chronic inflammation has long been linked to carcinogenesis. As such, anti-inflammatory drugs are believed to play a role in cancer treatment and prevention. In the past few decades, research has shown that NSAIDs may decrease the risk of certain types of cancer. However, there is also a growing body of research that proves the contrary. Furthermore, NSAIDs are well known for many side effects, including some life-threatening ones. This review will discuss the relationship between chronic inflammation and cancer, the role of NSAIDs in cancer prevention and cancer promotion, and some of the potentially lethal side effects of these drugs.

Spondyloarthritis or spondyloarthropathy (SpA) is a group of related rheumatic disorders, which presents with axial and nonaxial features, affecting structures within the musculoskeletal system, as well as other bodily systems. Both pharmacological and nonpharmacological therapeutic options are available for SpA. For decades, nonsteroidal anti-inflammatory drugs (NSAIDs) have been used as the first-line drugs to treat the disease. Research has shown that other than pain relief, NSAIDs have disease-modifying effects in SpA. However, to achieve these effects, continuous and/or long-term NSAID use is usually required. This review will give an overview of SpA, discuss NSAIDs and their disease-modifying effects in SpA, and highlight some of the important adverse effects of long-term and continuous NSAID use, particularly those related to the gastrointestinal, renal, and cardiovascular systems.

Introduction: Honey bee venom (HBV) has various biological activities such as the inhibitory effect on several types of cancer. Cisplatin is an old and potent drug to treat most of the cancers. Our aim in the present study was to determine antimutagenic and cytotoxic effects of HBV on mammary carcinoma, exclusively and in combination with cisplatin.

Methods: In this study, 4T1 cell line was cultured in RPMI-1640 with 10% fetal bovine serum (FBS), at 37°C in humidified CO₂ incubator. The cell viabilities were examined by the MTT assay. Also, HBV was screened‏ for its antimutagenic activity via the Ames test. The results were assessed by SPSS software version 19 and one-way ANOVA method considering p < 0.05 level of significance.

Results: The results showed that 6 mg/ml of HBV, 20 μg/ml of cisplatin, and 6 mg/ml HBV with 10 μg/ml cisplatin could induce approximately 50% of 4T1 cell death. The concentration 7 mg/ml of HBV with of 62.76% inhibitory rate showed the highest antimutagenic activity in comparison with other treatment groups.

Conclusions: The MTT assay demonstrated that HBV and cisplatin could cause cell death in a dose-dependent manner. The cytotoxic effect of cisplatin also promoted by HBV. Ames test outcomes indicated that HBV could act as a significant mutagenic agent. The antimutagenic activity of HBV was increased considerably in the presence of S9 mix. Therefore, our findings have revealed that HBV can enhance the cytotoxic effect of cisplatin drug and its cancer-preventing effects.

This study investigated antipathogenic efficacy of a polyherbal wound-healing formulation Herboheal against three multidrug-resistant strains of gram-negative bacterial pathogens associated with wound infections. Herboheal was evaluated for its quorum-modulatory potential against three different human-pathogenic bacteria, first in vitro through the broth dilution assay and then in vivo in the model host Caenorhabditis elegans. Herboheal at ≥0.1% v/v was able to inhibit (19-55%) in vitro production of quorum sensing-regulated pigments in all these bacteria and seemed to interfere with bacterial quorum sensing by acting as a signal-response inhibitor. This formulation could compromise haemolytic activity of all three bacteria by ∼18-69% and induced their catalase activity by ∼8-21%. Herboheal inhibited P. aeruginosa biofilm formation up to 40%, reduced surface hydrophobicity of P. aeruginosa cells by ∼9%, and also made them (25%) more susceptible to lysis by human serum. Antibiotic susceptibility of all three bacteria was modulated owing to pretreatment with Herboheal. Exposure of these test pathogens to Herboheal (≥0.025% v/v) effectively reduced their virulence towards the nematode Caenorhabditis elegans. Repeated subculturing of P. aeruginosa on the Herboheal-supplemented growth medium did not induce resistance to Herboheal in this mischievous pathogen, and this polyherbal extract was also found to exert a post-extract effect on P. aeruginosa, wherein virulence of the Herboheal-unexposed daughter cultures, of the Herboheal-exposed parent culture, was also found to be attenuated. Overall, this study indicates Herboheal formulation to be an effective antipathogenic preparation and validates its indicated traditional therapeutic use as a wound-care formulation.

Nutraceuticals are the pharmaceutically blended products that possess both nutritional as well as the medicinal value. Such a product is designed to improve the physical health, fight against day-to-day challenges such as stress, increase longevity, etc. Nowadays, emphasis is given to those herbs which are used as food and medicine due to its greater acceptance. Due to dynamic action, the popularity of nutraceuticals among people as well as healthcare providers has been increased over medicines and health supplements. This review documents herbs with a wide variety of therapeutic values such as immunity booster, antidiabetic, anticancer, antimicrobial, and gastroprotective. These herbs could be better options to formulate as nutraceuticals. Several nutraceuticals are described based on their availability as food, chemical nature, and mechanism of action.

The aim of this study was to test antimicrobial activity of ethanol extract of Lavandula stoechas against 22 bacteria and 1 yeast. Also, biochemical composition of the extract was investigated. A wide range of Gram-positive, Gram-negative microorganisms, and multidrug resistant bacteria were selected to test the antimicrobial activity. As a result, the extract is observed to contain fenchone (bicyclo[2.2.1]heptan-2-one, 1,3,3-trimethyl-, (1R)-) and camphor (+)-2-bornanone) as major components and showed antimicrobial activity against all studied microorganisms except Escherichia coli ATCC 25922 and Klebsiella pneumoniae. The results of the study present that L. stoechas is active against MDR strains too.

The extracts of different parts of Nerium oleander L. are used as antidiabetic remedy in the traditional medicinal systems of different parts of the world. Despite these uses in ethnomedicinal system, the antihyperglycemic potentials of oleander stem (NOSE) and root (NORE) extracts have not been pharmacologically evaluated. Therefore, we aimed at evaluating the antidiabetic ethnomedicinal claims of NOSE and NORE, primarily focusing on glucose homeostasis and associated metabolic implications. Alloxan-treated mice with hyperglycaemia (blood glucose >200 mg/dL) were treated with oleander 70% hydromethanolic extracts (200 mg/kg) for 20 consecutive days, and the results were compared with positive control glibenclamide. Blood glucose level was 52-65% lowered (P < 0.001) in oleander treated groups, which was otherwise 4.62 times higher in diabetic mice, compared to control. Insulin resistance was lowered 51-36% irrespective of any significant (P > 0.05) changes in insulin sensitivity throughout the treatments. Improved serum insulin remained associated with lowered glucose level (r _P = -0.847 and -0.772; P < 0.01). Markers of hyperglycaemia-related hepatic glycogen, glycated haemoglobin (HbA1c), hyperlipidaemia, hepatic injury, and diabetic nephropathy were normalized as well. Improvement of systemic intrinsic antioxidant enzymes (catalase and peroxidase) were correlated (r _P = -0.952 to -0.773; P < 0.01) with lower lipid peroxidation by-product malondialdehyde (MDA) in the circulation. Principal component analysis coupled with hierarchical cluster analysis represented shift in metabolic homeostasis in diabetic mice, which was further normalized by oleander and glibenclamide treatment. Additionally, molecular docking studies of the phenolic acids measured by HPLC with intracellular cytoprotective transcription factor nuclear factor erythroid 2-related factor 2 (Nrf2) revealed strong molecular interactions. The results collectively support the ethnomedicine antidiabetic claims of oleander stem and root and suggest that the oleander mediated elevation of systemic antioxidant status is likely responsible for the improved glycaemic control.