Drug Design, Discovery and Therapy
Emerging Insights and Innovations in Acridine Derivatives: A Review
Acridine derivatives represent a promising class of compounds in anticancer drug development owing to their versatile mechanisms of action and synthetic flexibility. These compounds can intercalate between DNA base pairs disrupting vital cellular processes such as DNA replication and transcription which underscores their potential as potent anticancer agents. This intercalation not only inhibits tumor growth but also enhances cancer cell sensitivity to other therapeutic interventions improving overall treatment efficacy. The synthesis of acridine derivatives involves several named reactions and synthetic schemes such as the Ullmann Bernthsen and Friedlander syntheses. These methods allow for the production of derivatives with specific substitution patterns and biological activities enabling researchers to optimize pharmacological properties like bioavailability and target specificity. Recent research has produced acridine derivatives with enhanced cytotoxicity and improved selectivity against various cancer types. Notable examples include spiro compounds and 39-disubstituted acridines which have shown potent antitumor activities in preclinical studies paving the way for further development and clinical evaluation. Acridine derivatives hold significant promise in the fight against cancer offering novel avenues for therapeutic innovation and advancement in oncology. Interdisciplinary efforts integrating synthetic chemistry pharmacology and molecular biology will be essential to fully harness their therapeutic potential and address the complex challenges of cancer treatment.
Plants as Medicine for Autism: Reviewing the Evidence for Phytopharmaceuticals for ASD
A complicated neural developmental condition autism spectrum disorder (ASD) is marked by difficulties with social interaction communication and repetitive behaviours. There is increasing interest in complementary and alternative medicines including medicinal plants to treat the symptoms of ASD as incidence rates rise globally. This thorough analysis looks at the available data supporting a range of plant-based ASD control strategies. We assess important therapeutic herbs including Curcuma longa (turmeric) Bacopa monnieri Ginkgo biloba Cannabis sativa and Camellia sinensis (green tea) and talk about their bioactive components possible modes of action and clinical results. Several plants have neuroprotective anti-inflammatory and antioxidant qualities that may work against the underlying pathophysiological mechanisms of ASD. The body of data is still small even if certain clinical studies yield encouraging results especially in the areas of behaviour modification and symptom treatment. The diverse character of ASD small sample sizes and methodological problems are study challenges. We also talk about the restrictions and security issues surrounding herbal remedies. Potential directions for phytopharmaceutical design for ASD in the future such as combination therapy enhanced delivery strategies and the requirement for more extensive carefully planned clinical studies. The potential of medicinal plants in treating ASD is highlighted in this review but it also emphasizes the urgent need for further thorough study to confirm their efficacy and safety.
Intranasal Sodium Valproate: A New Frontier in Epilepsy Therapy
Epilepsy a prevalent neurological disorder affects approximately 1% of the Indian population presenting a significant challenge in clinical management. Noninvasive treatment options are actively being explored with nose-to-brain drug delivery emerging as a promising approach for effective epilepsy control. This comprehensive review delves into the potential of intranasal nanotherapy focusing on its applicability in managing epilepsy. A key component of this review is an in-depth analysis of sodium valproate (SVS) a widely prescribed antiepileptic drug known for its effectiveness in treating epilepsy as well as various mental health conditions such as bipolar disorder and migraine. The review examines the chemical structure pharmacological properties and diverse therapeutic uses of SVS highlighting its role as a GABA amplifier. Special attention is given to emerging nanoparticle-based intranasal formulations which show promise for enhanced brain delivery and improved therapeutic outcomes in epilepsy treatment. Furthermore it discusses the associated compounds in SVS and their potential impact on its pharmacological profile including possible side effects drug interactions and adverse effects. The importance of precise dosing and rigorous medical monitoring is emphasized to minimize risks. Detailed analyses of the anatomy of the nasal cavity drug deposition mechanisms and mucociliary clearance are carried out to illustrate the challenges in optimizing drug delivery via this route. The unique pharmacokinetic and pharmacodynamic features of divalproex sodium a formulation of valproic acid are explored with insights into its absorption distribution metabolism and excretion (ADME) characteristics. The review also highlights its broad-spectrum antiepileptic effects and regulation of the GABAergic system offering a comprehensive understanding of its therapeutic efficacy. The findings underscore the potential of intranasal nanotherapies as an innovative and effective strategy for epilepsy management.
Murraya koenigii: A Source of Bioactive Compounds for Inflammation and Pain Management
Curry leaf or Murraya koenigii is the popular name for a tiny tropical tree in the Rutaceae family. Its fragrant leaves a mainstay of Indian cooking have led to its widespread cultivation in tropical and subtropical areas. Murraya koenigii has important therapeutic qualities and has been used for a long time in Ayurvedic medicine to treat a variety of illnesses.
The main goal of this work is to identify the bioactive compounds of Murraya koenigii for the treatment of inflammation and pain management.
To provide a comprehensive analysis of Murraya koenigii as a source of bioactive compounds for the management of inflammation and pain.
A comprehensive literature review was conducted using databases such as PubMed Scopus and Web of Science. The studies were selected based on the robustness of their phytochemical analyses focusing on bioactive compounds with documented anti-inflammatory properties.
Curry leaf (Murraya koenigii) has gained attention for its bioactive compounds with potent analgesic and anti-inflammatory properties. Its alkaloids flavonoids and phenolic compounds effectively inhibit pro-inflammatory cytokines and key enzymes such as COX-2 and iNOS reducing inflammation and pain.
Murraya koenigii's anti-inflammatory and analgesic qualities make it a promising medicinal agent. Subsequent investigations have to focus on the isolation and characterization of certain bioactive substances comprehend their mechanisms of action and assess their safety and efficiency in clinical trials. Incorporating Murraya koenigii into conventional medicine may improve patient outcomes and provide effective treatment options for individuals with inflammation- and pain-related disorders.
Synthesis and In-vitro Cytotoxicity Activity of 1,3,4-oxadiazol-2-amine Derivatives and Inhibition of Human MAO-A Enzyme: A Molecular Docking Approach
Hybridizing 134-oxadiazole with other anticancer heterocyclic pharmacophores improves the capacity of novel drug candidates to overcome drug resistance. In this study we designed and synthesized a new series of oxadiazole derivatives based on these biological implications as part of our continuous interest in designing and developing novel therapeutic medicines.
The final derivatives of substituted N-134-oxadiazol-2-amine were achieved through the conventional synthesis method and the physicochemical and spectroscopic results validated the newly synthesized compounds' structural integrity. The docking studies revealed that compound AL45 (-11.1 k/cal) showed similar binding affinity of standard molecule clorgyline towards the targeted protein and these molecules showed 2 conventional hydrogen bonds with Tyr 407 and Met 445 amino acid residues. The entire 10 synthesized compounds were evaluated for their cytotoxicity by in-vitro MTT assay using MCF-7 and A549 cell lines.
The A549 cell line showed the most promising sensitivity towards all the synthesized molecules but the compounds AL41 (32.35 ± 0.11 nM) AL45 (24.37 ± 0.253 nM) and AL49 (37.45 ± 0.041 nM) were most promising derivatives. The MCF-7 cell line showed sensitivity towards the following derivatives such as AL41 (29.32 ± 0.861 nM) AL45 (24.85± 0.846 nM) AL49 (33.93 ± 0.333 nM) and AL43 (27.27 ± 0.423 nM).
These compounds showed promise in inhibiting the proliferation of tumor cells. These chemicals also demonstrated a higher docking score and inhibition of the human MAO-A enzyme. In addition the in-silico ADMET screening revealed that all the designed compounds have low toxicity and adequate pharmacokinetic properties.