For many decades, the thiazole moiety has been an important heterocycle in the world of chemistry. The thiazole ring consists of sulfur and nitrogen in such a fashion that the pi (π) electrons are free to move from one bond to other bonds rendering aromatic ring properties. On account of its aromaticity, the ring has many reactive positions where donor–acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing a thiazole ring, when entering physiological systems, behave unpredictably and reset the system differently. These molecules may activate/stop the biochemical pathways and enzymes or stimulate/block the receptors in the biological systems. Therefore, medicinal chemists have been focusing their efforts on thiazole-bearing compounds in order to develop novel therapeutic agents for a variety of pathological conditions. This review attempts to inform the readers on three major classes of thiazole-bearing molecules: Thiazoles as treatment drugs, thiazoles in clinical trials, and thiazoles in preclinical and developmental stages. A compilation of preclinical and developmental thiazole-bearing molecules is presented, focusing on their brief synthetic description and preclinical studies relating to structure-based activity analysis. The authors expect that the current review may succeed in drawing the attention of medicinal chemists to finding new leads, which may later be translated into new drugs.
Diabetic patients wound healing is slower than the healthy individuals. Three citrus peel extracts; Lemon (Citrus limon), Grapes fruits (Citrus paradise) and Orange (Citrus sinensis) promote wound healing in experimental animals. This study investigated the effect of oral treatment with citrus peel extracts on wound repair of the skin of diabetic rats. The extracts were estimated for vitamin C and total carotenoid contents prior to animal study. Diabetes mellitus was induced in rats by intraperitoneal injection of a single dose of streptozotocin (STZ, 75 mg kg(-1) b.wt.). One week after diabetes induction, full thickness excision wounds were made in hyperglycemic rats and were divided groups, each containing 6 rats. The different test group animals were treated with different citrus peel extract orally at the dose of 400 mg kg(-1) body weight daily for 12 days. The blood glucose, body weight and rate of wound closure of each rat were measured every 3rd day during the experimental period. At the end of experiment, granular tissues of wounds were removed and estimated for hydroxylproline and total protein content. The results showed significant reduction in blood glucose and time to wound closure. Tissue growth and collagen synthesis were significantly higher as determined by total protein and hydroxyl proline content. From our experimental data, we propose that oral administration of citrus peel extracts has a therapeutic potential in the treatment of chronic wounds in diabetes.
Objective This work attempted to isolate, identify, and correlate the composition of essential oils (EOs) and pharmacological properties of two imported Amomum subulatum fruit samples. These samples were collected from Indian and KSA local supermarkets to ensure consistency in their therapeutic effects. Methods EOs were extracted from Indian and KSA A. subulatum fruit samples using a hydro-distillation method and identified by gas chromatography-mass spectrometry (GC–MS). Antimicrobial activity against gram-negative bacteria ( Pseudomonas aeruginosa , Escherichia coli , and Acinetobacter baumannii ) was determined using minimum inhibitory (MIC) and minimum bactericidal concentration methods. Antioxidant and anti-inflammatory activities were determined using a 2,2-diphenyl-1-picrylhydrazyl-induced free radical assay, and a bovine albumin inhibitory assay, respectively. These analyses were performed to evaluate the pharmacological activities of the substances. Results GC–MS retention times of both samples demonstrated 56 bioactive ingredients with different percentages. The principal bioactive compounds in the Indian and Saudi Arabian EO samples were 1,8-cineole (44.24% and 46.22%, respectively), α-terpineol (7.47% and 7.04%, respectively), terpinen-4-ol (5.01% and 4.83%, respectively), geraniol D (4.05% and 3.54%, respectively), and β-pinene (3.38% and 3.98%, respectively). Superior antimicrobial activity against the selected strains was observed for both samples, with an MIC range of 0.5%–1%. Antioxidant assays demonstrated moderate activity in both samples. Moreover, the Indian and Saudi Arabian samples exhibited IC 50 values of 53.12% and 55.26 μg/mL, respectively, in albumin denaturation inhibition assays. This indicated an outstanding anti-inflammatory potential comparable to ibuprofen. Conclusions The composition of EOs from both samples exhibited similar qualitative but different quantitative variability. No major variations in the pharmacological properties of EOs were observed. More studies are essential for further validation of our study findings.
Diabetic wound (DW) is a secondary application of uncontrolled diabetes and affects about 42.2% of diabetics. If the disease is left untreated/uncontrolled, then it may further lead to amputation of organs. In recent years, huge research has been done in the area of wound dressing to have a better maintenance of DW. These include gauze, films, foams or, hydrocolloid-based dressings as well as polysaccharide- and polymer-based dressings. In recent years, scaffolds have played major role as biomaterial for wound dressing due to its tissue regeneration properties as well as fluid absorption capacity. These are three-dimensional polymeric structures formed from polymers that help in tissue rejuvenation. These offer a large surface area to volume ratio to allow cell adhesion and exudate absorbing capacity and antibacterial properties. They also offer a better retention as well as sustained release of drugs that are directly impregnated to the scaffolds or the ones that are loaded in nanocarriers that are impregnated onto scaffolds. The present review comprehensively describes the pathogenesis of DW, various dressings that are used so far for DW, the limitation of currently used wound dressings, role of scaffolds in topical delivery of drugs, materials used for scaffold fabrication, and application of various polymer-based scaffolds for treating DW.
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