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1.
J Pak Med Assoc ; 72(4): 654-657, 2022 Apr.
Article in English | MEDLINE | ID: mdl-35614596

ABSTRACT

Objective: To identify the most common allergy type among patients visiting an urban allergy centre. METHODS: The descriptive cross-sectional study was conducted at the Allergy Centre of the National Institute of Health, Islamabad, Pakistan, from December 2019 to June 2020, and comprised subjects of either gender aged 20-50 years. Skin prick test was used to determine the skin reactivity for 11 common allergen extracts. Patients with a wheal diameter >3mm were considered positive. Data was analysed using SPSS 22. RESULTS: Of the 100 patients, 55(55%) were males and 45(45%) were females. The overall mean age was 34.03±8.16 years. Majority of the respondents 93(93%) were sensitive to aeroallergen, 7(7%) to food allergens, and 2(2%) exhibited sensitivity against both types of allergens. Poly-sensitisation was found among 86(86%) respondents. Conclusion: Aeroallergens were found to be the main triggering factor for allergies compared to the food allergens.


Subject(s)
Food Hypersensitivity , Hypersensitivity , Adult , Allergens , Cross-Sectional Studies , Female , Food Hypersensitivity/epidemiology , Humans , Hypersensitivity/epidemiology , Incidence , Male , Skin Tests
2.
Molecules ; 25(20)2020 Oct 14.
Article in English | MEDLINE | ID: mdl-33066366

ABSTRACT

Background: Fear, stress, and anxiety-like behaviors originate from traumatic events in life. Stress response is managed by endocannabinoids in the body by limiting the uncontrolled retrieval of aversive memories. Pharmacotherapy-modulating endocannabinoids, especially anandamide, presents a promising tool for treating anxiety disorders. Here, we investigated the effect of kaempferol, a flavonoid, in the extinction of fear related memories and associated anxiety-like behavior. Methods: The ability of kaempferol to inhibit fatty-acid amide hydrolase (FAAH, the enzyme that catabolizes anandamide) was assessed in vitro using an enzyme-linked immunosorbent assay (ELISA) kit. For animal studies (in vivo), the extinction learning was evaluated using contextual fear conditioning (CFC, a behavioral paradigm based on ability to learn and remember aversive stimuli). Furthermore, an elevated plus-maze (EPM) model was used for measuring anxiety-like behavior, while serum corticosterone served as a biochemical indicator of anxiety. Lastly, the interaction of kaempferol with FAAH enzyme was also assessed in silico (computational study). Results: Our data showed that kaempferol inhibited the FAAH enzyme with an IC50 value of 1 µM. In CFC, it reduced freezing behavior in rats. EPM data demonstrated anxiolytic activity as exhibited by enhanced number of entries and time spent in the open arm. No change in blood corticosterone levels was noted. Our computational study showed that Kaempferol interacted with the catalytic amino acids (SER241, PHE192, PHE381, and THR377) of FAAH enzyme Conclusion: Our study demonstrate that kaempferol facilitated the extinction of aversive memories along with a reduction of anxiety. The effect is mediated through the augmentation of endocannabinoids via the inhibition of FAAH enzyme.


Subject(s)
Amidohydrolases/antagonists & inhibitors , Enzyme Inhibitors/pharmacology , Extinction, Psychological/drug effects , Fear/drug effects , Kaempferols/pharmacology , Amidohydrolases/chemistry , Amidohydrolases/metabolism , Animals , Anti-Anxiety Agents/pharmacology , Behavior, Animal/drug effects , Catalytic Domain , Computer Simulation , Conditioning, Classical/drug effects , Corticosterone/blood , Dose-Response Relationship, Drug , Elevated Plus Maze Test , Endocannabinoids/metabolism , Kaempferols/administration & dosage , Kaempferols/chemistry , Molecular Docking Simulation , Rats, Wistar
3.
ACS Omega ; 9(28): 31056-31080, 2024 Jul 16.
Article in English | MEDLINE | ID: mdl-39035877

ABSTRACT

Recent advancements in chemical graph theory have facilitated a deeper understanding of the relationship between chemical structures and their underlying graphs based upon classical graph theory principles. Quantitative structure-property relationship (QSPR) analysis stands out as a powerful tool for probing chemical graphs. Topological indices, graph invariants assigning numerical values to graphs, play a pivotal role in statistically correlating physical properties, chemical reactivity, and biological activity across diverse chemical structures. The cactus graph (CG) represents a noteworthy family of connected graphs distinguished by the absence of common vertices between cycles. In this study, we focus on establishing the expressions of Zagreb and reverse Zagreb indices in terms of known parameters for cactus graphs. Subsequently, we leverage these indices to conduct QSPR analysis, employing linear and multilinear regression models to investigate the relationship between the properties of chemical structures adorned with cactus-like graphs and the corresponding Zagreb and reverse Zagreb indices.

4.
Macromol Biosci ; : e2400288, 2024 Sep 25.
Article in English | MEDLINE | ID: mdl-39319685

ABSTRACT

The study aimed to develop thiolated pluronic-based self-emulsifying drug delivery system (SNEDDS) targeted delivery of Rifampicin coated by arginine for enhanced drug loading, mucoadhesion, muco penetration, site-specific delivery, stabilized delivery against intracellular mycobacterium tuberculosis (M. tb), decreased bacterial burden and production by intracellular targeting. Oleic oil, PEG 200 and Tween 80 are selected as oil, co-surfactant and surfactant based on solubilizing capacity and pseudo ternary diagram region. Coating of thiolated polymer on SNEDDS with ligand arginine (Arg-Th-F407 SNEDDDS) decreased bacterial burden and production by intracellular targeting in macrophages. Formulation are evaluated through scanning electron microscope (SEM), EDAX analysis, diffraction laser scattering (DLS), Fourier transform infrared (FTIR) spectroscopy, and thermal analysis (DSC & TGA). Hydrodynamic diameter of thiolated polymeric SNEDDS (Th-F407 SNEDDS) and Arg-Th-F407 SNEDDS is observed to be 148.4 and 188.5 nm with low PDI of 0.4 and 0.3, respectively. Invitro drug release study from Arg-Th-F407 SNEDDS indicates 80% sustained release in 72 h under controlled conditions. Arg-Th-F407 SNEDDDS shows excellent capability of killing M.tb strains in macrophages even at low dose as compared to traditional rifampicin (RIF) and is found biocompatible, non-cytotoxic, and hemocompatible. Therefore, Arg-Th-F407 SNEDDDS of RIF proved ideal for targeting and treating M.tb strains within macrophages.

5.
J Trauma Inj ; 36(1): 39-48, 2023 Mar.
Article in English | MEDLINE | ID: mdl-39381675

ABSTRACT

Purpose: Sports offer several health benefits but are not free of injury risk. Activity dynamics vary across sports, impacting the injury profile and thereby influencing healthcare resource utilization and health outcomes. The purpose of this study was to investigate sports-related major trauma cases and compare differences across sports and activity groups. Methods: A retrospective case notes review of sports-related major traumas over a 5-year period was conducted. Demographic, hospital episode-related, and health outcome-related data were analyzed, and differences were compared across sports and activity groups. The Glasgow Outcome Scale (GOS) at discharge was used as the primary outcome measure and the length of hospital stay as the secondary outcome measure. Results: In total, 76% of cases had good recovery at discharge (GOS, 5), 19% had moderate disability (GOS, 4), and 5% had severe disability (GOS, 3). The mean length of hospital stay was 11.2 days (range, 1-121 days). The most severely injured body region was the limbs (29.1%) and vertebral/spinal injuries were most common (33%) in terms of location. A significant difference (P<0.05) existed in GOS across sports groups, with motor sports having the lowest GOS. However, no significant differences (P>0.05) were found in other health-outcome variables or injury patterns across sports or activity groups, although more competitive sports cases (67%) required admission than recreational sports cases (33%). Conclusions: Spinal injuries are the most frequent sports injuries, bear the worst health outcomes, and warrant better preventive measures. Head injuries previously dominated the worst outcomes; this change is likely due to better preventive and management modalities. Competitive sports had a higher injury frequency than recreational sports, but no difference in health outcomes or injury patterns.

6.
Front Nutr ; 9: 1005341, 2022.
Article in English | MEDLINE | ID: mdl-36304231

ABSTRACT

Background: Ethnopharmacological relevance: Brugmansia, a genus of the Solanaceae family, has historically been utilized in many different parts of the world as an anti-inflammatory for treating skin infections, wounds, and bodily aches and pains. The current study aimed to investigate the potential benefits of a methanolic extract of Brugmansia aurea in the management of diabetes and underlying complications in alloxanized-induced diabetic rats. Materials and methods: Animals were divided into nine groups (n = 6). Four groups received different standard oral hypoglycemic agents; three groups received 100, 200, and 400 mg/kg of B. aurea leaf extract for six consecutive weeks, and the remaining two were normal and disease control groups. All groups received alloxan (150 mg/kg) except for the normal control. Only those animals whose glucose levels were raised to 200 mg/dl were selected for the study. After a 6-week dosage period, various biochemical parameters, as well as HbA1c, antioxidant profile, oral glucose tolerance test (OGTT), insulin sensitivity, histopathology, and insulin resistance, were measured and compared with the untreated diabetic group. Results: Brugmansia aurea leaf extract at a dose of 400 mg/kg showed potent antidiabetic activity by reducing blood glucose levels (p < 0.001) after 6 weeks of treatment. OGTT data showed that B. aurea exhibited significant (p < 0.001) glucose tolerance by significantly reducing blood glucose levels in just 2 h post-treatment. Other tests showed that plant extract significantly increased (p < 0.001) insulin sensitivity and decreased (p < 0.001) insulin resistance. The biochemical profile showed reduced triglyceride and cholesterol, while the antioxidant profile showed restoration of antioxidant enzymes in the pancreas, kidney, and liver tissues of treated rats. Conclusion: The present study indicated that crude extracts of B. aurea increase insulin sensitivity and reduce hyperlipidemia in diabetic rats, which rationalizes the traditional medicinal use of this plant as an antidiabetic agent.

7.
Drug Des Devel Ther ; 15: 2679-2694, 2021.
Article in English | MEDLINE | ID: mdl-34188447

ABSTRACT

BACKGROUND: Alzheimer's disease (AD) is a neurodegenerative illness described predominantly by dementia. Even though Alzheimer's disease has been known for over a century, its origin remains a mystery, and researchers are exploring many therapy options, including the cholinesterase technique. A decreased acetylcholine ACh neurotransmitter level is believed to be among the important factors in the progression of Alzheimer's disease. METHODS: In continuation of synthesizing potential anti-Alzheimer agents and known appreciative pharmacological potential of amide-containing compounds, this study presents the synthesis of two novel amide-based transition metal zinc (II) complexes, AAZ7 and AAZ8, attached with a heterocyclic pyridine ring, which was synthesized and characterized by Fourier transform infrared spectroscopy (FT-IR), elemental analysis, 1H_NMR, and 13C_NMR. FT-IR spectroscopic records showed the development of bidentate ligand as Δν value was decreased in both complexes when compared with the free ligand. Both of the synthesized complexes were analyzed for acetylcholinesterase and butyrylcholinesterase inhibitory potential along with the antioxidizing activity. RESULTS: Importantly, the complex of AAZ8 exhibited more potent activity giving IC50 values of 14 µg/mL and 18µg/mL as AChE and BChE cholinesterase inhibitors, respectively, when compared with standard positive control galantamine. Interestingly, AAZ8 also displayed promising antioxidant potential by showing IC50 values of 35 µg/mL for DPPH and 29 µg/mL for ABTS in comparison with positive control ascorbic acid. CONCLUSION: Herein, we report two new amide carboxylate zinc (II) complexes which were potentially analyzed for various biological applications like acetylcholinesterase (AChE), butyrylcholinesterase (BChE) inhibitory potentials, and antioxidant assays. Computational docking studies also simulated results to understand the interactions. Additionally, thermodynamic parameters utilizing molecular dynamic simulation were performed to determine the ligand protein stability and flexibility that supported the results. Studies have shown that these compounds have the potential to be good anti-Alzheimer candidates for future studies due to inhibition of cholinesterase enzymes and display of free radical scavenging potential against DPPH as well as ABTS free radicals.


Subject(s)
Alzheimer Disease/drug therapy , Antioxidants/pharmacology , Cholinesterase Inhibitors/pharmacology , Acetylcholinesterase/drug effects , Alzheimer Disease/physiopathology , Amides/chemical synthesis , Amides/chemistry , Amides/pharmacology , Animals , Antioxidants/chemical synthesis , Antioxidants/chemistry , Butyrylcholinesterase/drug effects , Carboxylic Acids/chemical synthesis , Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/chemistry , Electrophorus , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology , Horses , Inhibitory Concentration 50 , Molecular Docking Simulation , Pyridines/chemical synthesis , Pyridines/chemistry , Pyridines/pharmacology , Zinc/chemistry
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