European Journal of Medicinal Chemistry Reports最新文献

Trans-ferulic acid, is one of the many biologically significant bioactive components of Datura. It has wide range of potential applications in the food industry, health, and cosmetics industries. Trans-ferulic acid possess myriad properties like anti-inflammatory, anti-aging, antiangiogenic, anticancer, antimicrobial, and antioxidant properties. To exploit its antioxidant and anti-inflammatory properties, first of all, trans-ferulic acid loaded tragacanth/chitosan nanoparticles (TFA loaded TGCA-NPs) were synthesized by ionic gelation method using tragacanth and chitosan as polymers. Tragacanth used to encapsulate the trans-ferulic acid is a polysaccharide gum, which is used all over the world in industries ranging from the food industry to healthcare systems due to its availability, affordability, non-toxicity, and environmental friendliness. The synthesized nanoparticles were then characterized by using techniques like FTIR, UV–Vis Spectroscopy, SEM and TEM. The particle size of nanoparticles thus obtained ranged from 105 nm to 250 nm. SEM micrograph of nanoparticles showed tiny rod-like structures, which appear to be coated on the polymer. TEM images showed somewhat sphere-shaped nanoparticles with a projecting rod-like structure that might be due to the trans-ferulic acid encapsulation in tragacanth-chitosan polymer. Decent antimicrobial activity of synthesized nanoparticles was observed against pathogenic bacteria named Staphylococcus aureus. Hemocompatibility of trans-ferulic acid loaded tragacanth-chitosan nanoparticles was also examined. The antioxidant activity was evaluated by DPPH radical scavenging assay, in which synthesized nanoparticles showed 41.62 % radical scavenging activity. For in-vitro anti-inflammatory activity Human Red Blood Cell membrane stabilization method (HRBC method) was used, and the results showed higher protection by the synthesized nanoparticles in comparison to the pure trans-ferulic acid and blank nanoparticles.

The emergence of metallic nanoparticles through green synthesis has garnered significant recognition, shaping global research efforts towards eco-friendly practices, often termed as the green revolution. Specifically, the green synthesis of silver nanoparticles (AgNPs) has made considerable strides in the past decade, becoming a prominent fixture in the realm of science and technology. The study explores the synthesis and characterization of silver nanoparticles (AgNPs) using Cassia fistula L. flowers extract through chemical co-precipitation (CM_AgNPs) and green methods (CFF_AgNPs). Characterization techniques, including scanning electron microscopy (SEM), transmission electron microscopy (TEM), attenuated total reflectance fourier-transform infrared (FTIR), and X-ray diffraction (XRD), revealed irregular morphologies with agglomeration, polycrystalline nature, and intrinsic functional groups involved in capping AgNPs. Antioxidant assessment demonstrated superior antioxidative activity (84.48 %) in green-synthesized nanoparticles compared to chemically synthesized ones (75.87 %), and they exhibited dose-dependent anti-inflammatory effects with IC₅₀ values CFF_AgNPs_30.19 μg/mL and CM_AgNPs _34.14 μg/mL respectively. The lower IC₅₀ value of CFF_AgNPs_30.19 μg/mL signifies finer and better activity due to the presence of phytochemicals present in it. Whereas for CM_AgNPs the IC₅₀ value is a 34.14 μg/mL which is solely due to AgNPs. To ensure the promising therapeutic aspects of AgNPs with a careful assessment of their safety profile, cytotoxicity of AgNPs on HEP3B cancer cells was evaluated through MTT assay, lactate dehydrogenase (LDH) release, and reactive oxygen species (ROS) level measurement. In the in vitro cytotoxicity evaluation, HEP3B demonstrated more pronounced dose-dependent adverse effects upon exposure to CFF_AgNPs compared to CM_AgNPs. This study underscores the bioactive potential of Cassia fistula L. mediated AgNPs, suggesting promising applications in biomedicine with environmental sustainability. The findings contribute to the growing interest in green synthesis methods for metallic nanoparticles and their potential benefits in various fields.

Herbal Phytoconstituents, also known as traditional medicines are considered to be harmless with no side effects. Herbal medicines have a global market value of 60 billion and have become increasingly popular in Western communities. Recent studies indicate that many herbal formulations in the market today have not been tested for quality and efficacy. The research outcomes suggest that, a proper quality check is necessary with novel analytical techniques to ensure product's safety. Thus, the impurities and their limits in herbal formulations should be examined as per pharmacopeial standards guidelines. The present review article emphasizes the importance of impurity profiling in herbal formulations and its significant role in natural product quality control. This article also suggests utilizing simple, precise and accurate, analytical methods to eliminate impurities, adulteration and combined synthetic chemicals in herbal products. In conclusion, implementing stricter regulations and creating public awareness about natural product safety measures can eradicate these adulterations since herbal formulations are in high demand in the commercial market after COVID-19.

Diabetes mellitus (Type 2) is a major world health problem spreading speedily throughout the world. It is a chronic illness that necessitates long-term therapy and care. Therefore, the therapy to treat and manage the disease should not only be safe and effective but should also be affordable. In countries like India, the cost of the therapy must be economical so that it can be easily afforded by common people. This review article mainly focuses on the novel drug dapagliflozin, a SGLT-2 inhibitor, and discusses its various aspects. It acts independently of the insulin pathway by inhibiting the reuptake of glucose in the renal tubules, allowing glycosuria to take place. This helps decrease blood glucose levels. Dapagliflozin is effective as both, monotherapy and combination therapy depending on the severity of the case as indicated by multiple studies. Since, only one daily dose is sufficient, this may be a more reasonable option for many low-income group patients. Many new medications are in development but dapagliflozin could be the major turning factor in managing T2DM along with metformin, sulfonylurea, insulin, pioglitazone, and DPP-4 inhibitors as mono or combination therapy.

Medicinal plants are considered as one of the main sources of biologically active molecules for various diseases, in addition to their traditional applications. Worldwide, interest on medicinal plants having nutritional value and used as food, is increasing day by day as these can prevent or delay the occurrence of chronic diseases. Further exploration of such plants require a thorough updated information on that plant species to ascertain what is known and what can be done. Medicago polymorpha, also known as Medicago denticulata is an annual dicotyledonous weed of family Fabaceae, which is found as a weed in agricultural lands, road sides and other disturbed areas. Herein, we have compiled the information related to traditional uses, chemical constituents, pharmacological activities and metal nanoparticles of M. polymorpha available in Scopus database, which will be a ready reference for the researchers working on this plant to further explore it. The plant contains a wide range of secondary metabolites and has been scientifically studied for its analgesic, antioxidant, hepatoprotective, antimicrobial, cytotoxic, anthelmintic, antiamnesic, antidiarrhoeal, antifungal, antidiabetic, and immunomodulatory activities.

Curcumin is a well-known phenolic compound obtained from Curcuma Longa L. It is used popularly as an antioxidant, anti-inflammatory, antispasmodic, antithrombotic, anticancer as well as immune-modulator. In the last couple of years, few studies showed the usefulness of curcumin against Helicobacter pylori along with the potential to restore gastric damage. However, limited solubility, poor alkaline pH stability and flow property have rendered the industrial application of curcumin. The current research focuses to address this limitation by modifying the flow property using coating and two-step glidant mixing process and then converted into dosage form. Furthermore; to have reproducible and reliable results, flow property was investigated by the advance methodology-powder flow tester (PFT). Initially, curcumin powder was coated with HPMC and further mixed with glidant Sodium Stearyl Fumarate by two methods viz. one-step and two-steps mixing operation. Both blends were investigated for various parameters viz. flow function test, wall friction test and bulk density. We found that a two-step glidant mixing operation to coated curcumin enhanced powder to flow significantly more than one-step. In the lateral stage, both blends were converted into gastroretentive tablets by using the direct compression method. Tablets prepared by using a two-step blend process showed more satisfactory results than one-steps with floating time of 24 h and 21 h respectively. Coating, two-step glidant mixing and PFT were found unique combined approach to prepare the direct compression tablet of curcumin, as it enables the industry to overcome production problems and ensure high-quality products.

Thiazolidinedione (TZD) plays a crucial role in activating PPAR-γ receptor, which helps to inhibit insulin-resistant diabetes mellitus through binding with DNA by forming a complex with retinoid receptors. TZD derivatives are the sulphur and nitrogen containing heterocyclic compounds that have a massive impact in synthetic chemistry for their plethora of pharmacological activities. TZD helps to improve insulin resistance and lowering the blood glucose level through oxidation of carbohydrate in case of type II diabetes mellitus. TZD scaffold is a pentacyclic sulphur-containing compound with two carbonyl groups and an alpha hydrogen offering a huge possibility in structural modification of this biologically active molecule, here N-3 & C-5 positions are the most versatile site for structural modification in TZD nucleus. In this review, we focus on a brief description of its antidiabetic activity with its mechanism of action, structure activity relationship and various synthetic approach of the main pharmacophore TZD and hope it will help to develop idea about this moiety for future researchers.

Ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) that significantly increases the risk of developing colorectal cancer (CRC). The overall prevalence of UC-induced CRC is on the rise due to the rapidly increasing frequency of UC. It is widely acknowledged that chronic inflammation that persists for a long period is a significant contributing factor to the development of CRC in individuals with UC. The activation of various proinflammatory pathways, such as nuclear factor kappa B (NF-κB), interleukin-6/signal transducer and activator of transcription 3 (IL-6/STAT3), cyclooxygenase-2/prostaglandin E2 (COX-2/PGE2), and interleukin-23/T-helper 17 (IL-23/Th17), and gut microbiota contributes to the initiation and progression of tumorigenesis by a different mechanism, such as triggering the production of inflammatory mediators, increasing the expression of antiapoptotic genes, and stimulating cell proliferation as well as angiogenesis. Managing this risk and finding potential nutraceutical interventions, such as Dillenia indica (DI), is of significant interest. This review delves into the literature concerning the mechanism correlated to the development of CRC in UC individuals and investigates the potential of DI, as a nutraceutical in managing this rapid risk of UC-CRC. By examining the different mechanisms involved in UC-induced CRC, we aim to provide insight into the therapeutic promise of DI in mitigating these mechanisms.

Aminoalcohols were converted into the corresponding enantiomeric phenylsulfonamide sulfamates. These compounds proved to be inhibitors of carbonic anhydrase II. Interestingly, a sulfamate derived from (S)-tryptophan was no inhibitor at all while its (R) configurated enantiomer was an excellent inhibitor of carbonic anhydrase II (CA II). A rationale can be deduced from molecular modeling studies. The sulfamates derived from (R) or (S) proline held very low inhibition constants for this enzyme as K_i = 0.77 μM and 0.70 μM, respectively.

This study investigate the development and optimization of a mesoporous silica-loaded gel formulated with Rosmarinus officinalis extract, aiming to amplify wound healing capabilities by harnessing the plant's known therapeutic properties alongside the sophisticated drug delivery advantages of mesoporous silica. The formulation process entailed encapsulating the Rosmarinus officinalis extract within mesoporous silica particles before their incorporation into a gel matrix, with particular attention paid to the variable concentrations of Poloxamer 407 and HPMC K15 M to evaluate their effect on the gel's Spreadability and drug release profile. Employing a comprehensive full factorial experimental design analyzed through Design-Expert software, inclusive of ANOVA and 3D surface plotting, the investigation identified batch RF7 as the prime formulation, composed of 14 % w/v Poloxamer 407 and 1 % w/v HPMC K15 M. RF7 precisely matched the predicted Spreadability with an experimental value of 13.6 gm.cm/sec and showcased a promising Cumulative % drug release at 10 h of 87.93 %, closely aligning with a predicted 89.94 %, marking a minimal percentage error of −2.01 %. The study further validated RF7 efficacy through stability and in-vitro antibacterial activity assessments, where it demonstrated significant zones of inhibition against E. coli (22.5 ± 0.87 mm) and S. Aureus (23.4 ± 1.15 mm), nearly paralleling or outperforming the Rosmarinus officinalis extract itself and a marketed standard, Candiderma Plus. These findings, supported by rigorous statistical validation, underscore RF7 enhanced wound healing potential, marrying natural therapeutic virtues with cutting-edge drug delivery technology for a promising advancement in wound care solutions.