The purpose of this study was to develop and evaluate novel antimicrobial Schiff base and their transition metal complexes. Antibiotics that were often used to treat microorganisms are no longer effec-tive against them because of developed resistance. It is believed that newly developed Schiff bases and their transition metal complexes could function well as antimicrobial agents and have considerable pharmacological efficacy. In this report new Schiff base ligand was synthesized by taking the 1:1 stoichio-metric ratio of 2, 4-dinitrophenyl hydrazine and dimethyl tetraphthalate, with ethanol serv-ing as the solvent subsequently its Co(II) and Cd(II) Complexes were created by reacting the synthesized Schiff base ligand with the corresponding metal salts in the form of chlo-rides. All of the target compounds' structures were evaluated using sophisticated analyt-ical techniques, such as elemental analysis, FT-IR, 1H and 13C NMR, and LCMS. In order to determine each compound's biological potential as an antimicrobial agent, its effective-ness was also assessed. The results of the molecular docking studies were found to be com-patible with biological potential. At concentrations of 100–250 ppm, the zones of inhibition were discovered to be between 9–20 mm for ligands and 10-23 mm for complexes. The outcome showed that, in comparison to the Schiff base ligand, metal complexes have supe-rior biological activity. The current study provided a unique method for creating novel and physiolog-ically active Schiff bases and their transition metal complexes. The findings demonstrate that the compounds produced are a promising antimicrobial mediator against contemporary human illnesses. Additionally, it may pave the way for further research on drug-resistant microbes with potential biological applications.
The development of environmentally friendly and efficient protocol for the synthesis of heterocyclic compounds is the current demand of synthetic community. Solvent-free synthesis has emerged as a sustainable approach reducing waste generation, and minimizing environmental impact. In this connection, we have developed a solvent-free method for the construction of five membered heterocycles i.e. isoxazoline and pyrazoline from α, β-unsaturated carbonyl compounds and Hydrazine/hydroxylamine hydrochloride. This protocol involves the [3+2] cycloaddition reaction between α, β-unsaturated carbonyl compounds and hydrazine hydrochloride/hydroxylamine hydrochloride under solvent free conditions to provide the substituted isoxazoline and pyrazoline in excellent yields. The synthesized compounds were characterized through 1H NMR, 13C NMR, Mass spectral data and IR. These newly synthesized compounds were screened for their antihyperglycemic activity using sucrose loaded diabetic model. Isoxazoline derivatives offered potent antihyperglycemic response than correspondence pyrazoline derivatives. Compounds bearing isoxazoline ring II A and II E showed maximum % fall of blood glucose level than control group which was comparable to the standard drug metformin. The newer compounds VIA, VIB, and VIC also evaluated for their anti-hyperglycemic activities, compound VIC showed appreciable response (62.5% antihyperglycemic activity).
Owing to its ever-growing range of pharmacological advantages, sulforaphane, an isothiocyanate from cruciferous vegetables such as broccoli, is becoming increasingly popular. This review aims to provide a thorough understanding and a current update on the application of sulforaphane in cancer treatment. Sulforaphane interacts with many signaling molecules that control various pathways in malignant cells, including angiogenesis, apoptosis, cell cycle arrest, metastasis, and inflammation pathways. This review examines the effects of this isothiocyanate on inflammatory mediators, caspases, MMPs, cytokines, and the proteins Bax and Bcl-2. Furthermore, the advantages of nanotechnology and synergistic effects in sulforaphane applications are also reviewed. As per evidence, sulforaphane is a shining example of how ethno-pharmacological expertise can be used to create modern medications.
The goal of this study was to synthesize the bimetallic nanoparticles using leaf extract of Trifolium alexandrinum, copper sulphate and zinc sulphate and screening their biological and photocatalytic activities. Since growing antibiotic resistance is a significant problem, metallic nanoparticles, which are well-known for their wide biological spectrum, are proving to be an efficient substitute for currently available antibiotics. Leaf extract of T. alexandrinum (TFL) and its bimetallic Cu-Zn (CZS) nanoparticles have been synthesized. Fourier transform infrared spectroscopy, ultraviolet spectroscopy, transmission electron microscopy, field emission scanning electron microscopy, X-ray diffraction and energy dispersive X-ray were used to analyze and characterize the synthesized nanoparticles. The Fourier transform infrared spectroscopy describes the presence of different functional groups in the leaf extract as well as changes in their nature after combining with metal salts. Field emission scanning electron microscopy reveals the formation of nanoparticles in agglomerated form with spherical shape. Transmission electron microscopy images also coincide with the results of scanning electron microscopy. The X-ray diffraction pattern confirms the formation of crystalline nanoparticles with 77% crystallinity with an average size of about 50-150 nm, whereas EDX certifies the presence of different constituent abundances in the form of percentage. Further, the biological potential of the obtained nanoparticles was estimated by evaluating the antimicrobial and anti-angiogenic activities. The maximum value for bacterial inhibition was found to be 21.5 mm and for fungal inhibition this value reaches to 20 mm for 100 µL each. The percentage inhibition on vessel growth rate in TFL/CZS nanoparticle treated groups was obtained as 28% (1 µg) and 85% (10 µg). Percentage degradation for the composite was attained 83%, which was much better than CZS nanoparticles towards the Congo red dye. Results have shown that subjected nanoparticles were proven as excellent biological agents. Moreover, the photocatalytic activity confirms that the novel bimetallic nanoparticles can be used to treat the wastewater at initial level.
Since its discovery in the bacterium Chromobacterium violaceum, violacein-a striking purple pigment-has garnered significant interest due to its promising applications in the food and pharmaceutical industries. Violacein exhibits a range of pharmacological properties, including anti-inflammatory, anticancer, antibacterial, and antiparasitic effects, yet its complete molecular mechanisms are still being elucidated. Its mechanisms of action likely involve complex interactions with cellular receptors, signaling pathways, and specific molecular targets. Given violacein's unique properties and bioactive intermediates, future research holds substantial potential to advance its clinical and industrial applications. Upcoming studies will focus on deepening our understanding of violacein's molecular interactions, conducting clinical trials, and refining drug delivery systems to maximize its therapeutic value. Additionally, obtaining regulatory approval, conducting rigorous safety assessments, and developing efficient biosynthetic methods remain essential steps for violacein's successful integration into food biotechnology and medical applications.
Background: Lung cancer is the predominant cause of cancer-related death globally, attributed to delayed diagnosis and limited therapeutic effectiveness. Natural chemicals provide potential avenues for the development of innovative cancer therapeutics. Objective: This study seeks to investigate the anticancer efficacy of quinovic acid in lung cancer via a network pharmacology approach combined with molecular docking techniques. Methods: A network pharmacology analysis was conducted to discover the proteins targeted by Quinovic acid. The targets were also analysed for potential overlap with genes linked to lung cancer. A Protein-Protein Interaction (PPI) network was constructed to identify pivotal hub genes. Molecular docking simulations were conducted to evaluate the binding affinity of quinovic acid with the indicated targets. Results: Network pharmacology indicates that quinovic acid interacts with a diverse array of proteins, predominantly phosphatases (33.3%) and phosphodiesterases (26.7%). A substantial overlap of 49 genes was identified between quinovic acid targets and lung cancer-associated genes, suggesting potential therapeutic relevance. PPI analysis identified essential hub genes including TP53, EGFR, KRAS, BRAF, and PIK3CA, which are involved in significant signalling pathways such as PI3K-AKT, MAPK, and apoptosis. Computer-simulated ligand binding analyses demonstrated substantial binding affinities of quinovic acid, particularly with BRAF and PIK3CA (-9.2 kcal/mol). Conclusion: The results indicate that quinovic acid may inhibit cancer proliferation by altering many critical oncogenic pathways, rendering it a promising option for lung cancer treatment. Additional experimental validation is necessary to demonstrate its therapeutic effectiveness.
Harmine is a β-carboline alkaloid derived from Peganum harmala, showing a solid antitumor potential in different types of human cancer cells. Unfortunately, the clinical application of this natural alkaloid has been impeded till now by severe toxic side effects, especially neurotoxicity, besides its poor water solubility. Therefore, over the recent years, several semisynthetic derivatives of harmine have been prepared and studied concerning their abilities to inhibit tumor cell proliferation, survival, angiogenesis, migration, and invasion in diverse preclinical models. This review article summarizes the anticancer effects of harmine and its synthetic derivatives, demonstrating their high potential to be developed as novel anticancer drugs to supplement our current therapeutic arsenal in the fight against the globally increasing rate of malignant disorders.
Gastrointestinal cancers continue to pose a significant global health challenge, with millions of new cases diagnosed each year. Despite advancements in treatment, the prognosis for many patients remains poor. This article explores the potential of garcinol, a polyisoprenylated benzophenone found in various Garcinia species, as a therapeutic agent against gastrointestinal malignancies. The objective is to review recent research on garcinol’s anticancer properties, its mechanisms of action, and safety aspects. Garcinol exhibits anticancer effects in esophageal, gastric, colorectal, pancreatic, and liver cancers by inhibiting metastasis, inducing apoptosis, and targeting key molecular pathways in cancer progression. Nanotechnology is explored as a means to enhance garcinol delivery and efficacy. Safety assessments suggest a promising toxicity profile. Garcinol shows significant potential as a natural therapeutic agent for gastrointestinal cancers, and future research is needed on optimizing its delivery, exploring synergistic combinations, and conducting clinical trials to validate its efficacy and safety for clinical applications.
Aims The creation and testing of new Schiff base-based antibacterial organotin (IV) complexes were the objectives of this investigation. Background Due to developed resistance, antibiotics that were once often used to treat microorganisms are no longer effective against them. It is thought that organotin compounds synthesized from Schiff bases have significant pharmacological effectiveness and work well as antibacterial agents. Methods Thiocarbohydrazide and dehydroacetic acid were condensed to create the Schiff base, followed by processing with dialkyltin (IV) dichloride to synthesize the final product. Modern analytical techniques were used to clarify the compounds' probable structural details. The crystalline nature of the produced compounds was tested using PXRD. Results All of the compounds were thermally stable up to 300°C. All of the synthesized complexes showed potent antibacterial activity in the range of 250 to 400 µg/ml. Furthermore, the computational biology research showed that, in contrast to ligands, which had a binding energy of -7.3 to -7.4 kcal/mol, complexes interacted well with dihydropteroate synthase and DNA gyrase. Conclusion The current study offered a unique technique for synthesizing diorganotin (IV) derivatives of N-substituted Schiff bases that are physiologically active. The results show that the chemicals created are promising antibacterial mediators against diseases that affect humans in the modern world. It might also open the door to future studies on drug-resistant microorganisms that could have biological uses.
In recent times, there have been notable advancements in comprehending the potential anti-cancer effects of chrysin (CH), a naturally occurring flavonoid compound found abundantly in various plant sources like honey, propolis, and certain fruits and vegetables. This active compound has garnered significant attention due to its promising therapeutic qualities and minimal toxicity. CH’s ability to combat cancer arises from its multifaceted mechanisms of action, including the initiation of apoptosis and the inhibition of proliferation, angiogenesis, metastasis, and cell cycle progression. CH also displays potent antioxidant and anti-inflammatory properties, effectively counteracting the harmful molecules that contribute to DNA damage and the development of cancer. Furthermore, CH has exhibited the potential to sensitize cancer cells to traditional chemotherapy and radiotherapy, amplifying the effectiveness of these treatments while reducing their negative impact on healthy cells. Hence, in this current review, the composition, chemistry, mechanisms of action, safety concerns of CH, along with the feasibility of its nanoformulations. To conclude, the recent investigations into CH’s anti-cancer effects present a compelling glimpse into the potential of this natural compound as a complementary therapeutic element in the array of anti-cancer approaches, providing a safer and more comprehensive method of combating this devastating ailment.
In recent years, Web phishing attacks have evolved, eroding customer trust in online services. Traditional blacklist-based approaches struggle to detect sophisticated phishing websites, including newly deployed ones. Researchers are turning to machine learning techniques for early detection but facing limitations in feature selection and parameter tuning. This paper presents an innovative approach that combines Particle Swarm Optimization (PSO) with feature selection techniques, including correlation and mutual information, and tree-based feature selection. The goal is to accurately differentiate between legitimate and phishing websites by identifying relevant features. A comprehensive dataset of diverse website features is used, and correlation and mutual information methods are used to assess feature importance. A tree-based feature selection algorithm refines the feature set, and PSO optimizes the parameters by exploring the feature space. Thorough experimentation is needed to fine-tune features and parameters for accurate detection. Experimental results show the superiority of the proposed approach, eliminating irrelevant features and improving efficiency and classification performance through PSO optimization. Integrating PSO with feature selection provides a robust framework, addressing tuning challenges and improving accuracy.
Cucurbitacins constitute a group of cucumber-derived dietary lipids, highly oxidized tetracyclic triterpenoids, with potential medical uses. These compounds are known to interact with a variety of recognized cellular targets to impede the growth of cancer cells. Accumulating evidence has suggested that inhibition of tumor cell growth via induction of apoptosis, cell-cycle arrest, anti-metastasis and anti-angiogenesis are major promising chemo-preventive actions of cucurbitacins. Cucurbitacins may be a potential choice for investigations of synergism with other drugs to reverse cancer cells' treatment resistance. The detailed molecular mechanisms underlying these effects include interactions between cucurbitacins and numerous cellular targets (Bcl-2/Bax, caspases, STAT3, cyclins, NF-κB, COX-2, MMP-9, VEGF/R, etc.) as well as control of a variety of intracellular signal transduction pathways. The current study is focused on the efforts undertaken to find possible molecular targets for cucurbitacins in suppressing diverse malignant processes. The review is distinctive since it presents all potential molecular targets of cucurbitacins in cancer on one common podium.
Recently, it has become obvious that renin-angiotensin system (RAS) plays an important role in cancer progression through angiotensin converting enzyme (ACE), involving activation and upregulation of multiple oncogenic molecules. Accordingly, suppression of ACE and its subsequent downstream cascades has received considerable attention as a possible way to combat oncological diseases. In this book chapter, the role of a several plant-derived phenolic acids (Ellagic acid, Gallic acid, Caffeic acid) on inhibition of ACE is demonstrated, and involvement of this action in chemopreventive and chemotherapeutic properties of these natural compounds is discussed, with a special focus on antiangiogenic and antiinflammatory activities.
In parallel to the continuous rise of new cancer cases all over the world, the interest of scientific community in natural anticancer agents has steadily been increased. In the past decades, numerous phytochemicals have been shown to possess a strong anticancer potential in preclinical conditions. One of such interesting compounds, derived from different plants such as ginkgo, hinoki, and St. John`s wort, is amentoflavone. In this review article, a wide range of anticancer properties of this natural biflavone are described, revealing its ability to suppress the malignant growth and lead tumor cells to apoptotic death, besides impeding also angiogenic and metastatic processes. Therefore, amentoflavone can be considered a potential lead compound for the development of novel anticancer drug candidates, definitely deserving further in vivo studies and also initiation of clinical trials. It is expected that this plant biflavone might be important, either alone or in combination with the current standard chemotherapeutics, in providing some alleviation for the continuous rise of global cancer burden.
The increased demands of metal and metal-based nanoparticles result in environmental contamination as they require using various toxic solvents and high-energy methods. These methods include physical (ultrasonication, photoirradiation, radiolysis, etc.), chemical (sol-gel, chemical reduction, reverse micelles, etc.) and biological or green synthesis methods (microbial, plant, algae, etc.). Due to increases in the importance of the environment, sustainable energy and natural resources, the approaches of green synthesis are taken as the best routes for synthesizing nanoparticles. Green chemistry is regarded as interdisciplinary area and is an integration of physical chemistry, analytical chemistry, microbiology, biotechnology, toxicology and engineering. The aim of developing green chemistry is to prevent pollution and damage to the environment in the early stages of nanoparticle synthesis, which cover all aspects and types of precautions to be taken for the environment. This chapter throws light on the biological methods used to synthesize green nanoparticles, their characterization and various important application. Along with it, this chapter gives a brief introduction to the environmental and health problems originating from the use of nanoparticles synthesized by physical and chemical methods.
Chinese native medicine Scutellaria baicalensis Georgi, also referred to as Chinese skullcap or Huang-Qin, is frequently used to treat cancer, viral infections, and seizures. This plant's abundance of flavones (wogonoside) and their related aglycones (wogonin) is responsible for many of its pharmacologic effects. A significant ingredient in S. baicalensis that has been the subject of the most research is wogonin. Numerous preclinical investigations revealed that wogonin suppresses tumor growth by cell cycle arrest, stimulating cell death and preventing metastasis. This review focuses on a complete overview of published reports that suggest chemopreventive action of wogonin and the mechanistic insights behind these neoplastic activities. It also emphasizes the synergistic improvements made by wogonin in chemoprevention. The factual data in this mini-review stimulate additional research on chemistry and toxicological profile of wogonin to confirm its safety issues. This review will encourage researchers to generalize the merits of wogonin to be used as potential compound for cancer treatment.
Increasing rates of cancer incidence and the toxicity concerns of existing chemotherapeutic agents have intensified the research to explore more alternative routes to combat tumor. Luteolin, a flavone found in numerous fruits, vegetables, and herbs, has exhibited a number of biological activities, such as anticancer and anti-inflammatory. Luteolin inhibits tumor growth by targeting cellular processes such as apoptosis, cell-cycle progression, angiogenesis and migration. Mechanistically, luteolin causes cell death by downregulating Akt, PLK-1, cyclin-B1, cyclin-A, CDC-2, CDK-2, Bcl-2, and Bcl-xL, while upregulating BAX, caspase-3, and p21. It has also been reported to inhibit STAT3 signaling by the suppression of STAT3 activation and enhanced STAT3 protein degradation in various cancer cells. Therefore, extensive studies on the anticancer properties of luteolin reveal its promising role in chemoprevention. The present review describes all the possible cellular interactions of luteolin in cancer, along with its synergistic mode of action and nanodelivery insight.