Pub Date : 2024-07-22DOI: 10.2174/0115734072325272240712114444
H. Mouada, T. Lanez
An investigation on the antioxidant activity and ADME properties of some N-phenylalkanehydrazides (NPhs) in comparison with ascorbic acid was carried out. The power of the compounds to scavenge the superoxide anion radical was examined using cyclic voltammetry. Furthermore, molecular docking was used to examine how NPhs bind to the antioxidant enzyme glutathione peroxidase (GPx). Finally, ADME properties were predicted using the SwissADME webserver. The results showed that the studied compounds had significantly higher EC50 values than Vitamin C and displayed spontaneous binding with GPx with binding energy similar to ascorbic acid. Also, substantial values emerged from the predictive analysis of drug-likeness and bioavailability characteristics. First, the EC50 of the compounds under study was determined by assessing the decrease in the anodic current peak intensity; this demonstrated significant radical scavenging activity. Next, the electrostatic way of binding with ROS radical and with antioxidant enzyme was disclosed by the binding free energies; however, the oxygen and nitrogen atoms in the compounds' structures might make many conventional hydrogen bonds with amino acids. Finally, NPh (a) followed all the rules for drug-likeness and bioavailability estimates, making it a promising moiety for synthesising new antioxidant chemicals. The current study is a hybrid of experimental and computational methods that complement each other perfectly.
{"title":"Investigation on the Potential of Some N-phenylalkanehydrazides as Superoxide Anion Radical Scavengers and Glutathione Peroxidase Binders\u0000with ADME Prediction: Comparison with Vitamin C","authors":"H. Mouada, T. Lanez","doi":"10.2174/0115734072325272240712114444","DOIUrl":"https://doi.org/10.2174/0115734072325272240712114444","url":null,"abstract":"\u0000\u0000An investigation on the antioxidant activity and ADME properties of some\u0000N-phenylalkanehydrazides (NPhs) in comparison with ascorbic acid was carried out.\u0000\u0000\u0000\u0000The power of the compounds to scavenge the superoxide anion radical\u0000was examined using cyclic voltammetry. Furthermore, molecular docking was used to examine\u0000how NPhs bind to the antioxidant enzyme glutathione peroxidase (GPx). Finally, ADME properties\u0000were predicted using the SwissADME webserver.\u0000\u0000\u0000\u0000The results showed that the studied compounds had significantly higher EC50 values than\u0000Vitamin C and displayed spontaneous binding with GPx with binding energy similar to ascorbic\u0000acid. Also, substantial values emerged from the predictive analysis of drug-likeness and bioavailability\u0000characteristics.\u0000\u0000\u0000\u0000First, the EC50 of the compounds under study was determined by assessing the decrease\u0000in the anodic current peak intensity; this demonstrated significant radical scavenging activity.\u0000Next, the electrostatic way of binding with ROS radical and with antioxidant enzyme was\u0000disclosed by the binding free energies; however, the oxygen and nitrogen atoms in the compounds'\u0000structures might make many conventional hydrogen bonds with amino acids. Finally,\u0000NPh (a) followed all the rules for drug-likeness and bioavailability estimates, making it a promising\u0000moiety for synthesising new antioxidant chemicals.\u0000\u0000\u0000\u0000The current study is a hybrid of experimental and computational methods that complement\u0000each other perfectly.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"23 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141816045","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-12DOI: 10.2174/0115734072316442240603061608
Parvinder Kaur, Nitin Kumar, Shikha Sharma, B. Banik
Heterocyclic compounds that incorporate nitrogen and sulfur, particularly those within the thiazole family, have garnered significant attention due to their versatile synthetic properties. This interest arises from their abundance of biologically active natural products and their effectiveness as potent agrochemicals and pharmaceuticals. Among these, the thiazolidin-2,4-dione (TZD) motif plays a pivotal role in the biological functions of many important molecules. The adaptability of the TZD scaffold is further heightened by the potential for substitutions at the third and fifth positions, rendering it a widely employed moiety with diverse biological effects. TZD analogs, bearing substitutions at these positions, exhibit a wide spectrum of biological activities, with a notable emphasis on hypoglycemic effects attributed to enhanced insulin resistance through the activation of the PPAR-γ receptor. This manuscript aims to present a comprehensive review of research conducted on TZD derivatives as potential antihyperglycemic agents spanning from 2010 to the current date. The review encompasses insights into their molecular mechanisms. Thiazolidin-based chemicals have received significant attention as hypoglycemic agents and provided information on patents granted for TZD analogs.
{"title":"Chemistry or Hypoglycaemic Aspect of Thiazolidin-2,4-Dione Insight into\u0000the Structure-activity Relationship","authors":"Parvinder Kaur, Nitin Kumar, Shikha Sharma, B. Banik","doi":"10.2174/0115734072316442240603061608","DOIUrl":"https://doi.org/10.2174/0115734072316442240603061608","url":null,"abstract":"\u0000\u0000Heterocyclic compounds that incorporate nitrogen and sulfur, particularly those within\u0000the thiazole family, have garnered significant attention due to their versatile synthetic properties.\u0000This interest arises from their abundance of biologically active natural products and their effectiveness\u0000as potent agrochemicals and pharmaceuticals. Among these, the thiazolidin-2,4-dione\u0000(TZD) motif plays a pivotal role in the biological functions of many important molecules. The\u0000adaptability of the TZD scaffold is further heightened by the potential for substitutions at the third\u0000and fifth positions, rendering it a widely employed moiety with diverse biological effects. TZD\u0000analogs, bearing substitutions at these positions, exhibit a wide spectrum of biological activities,\u0000with a notable emphasis on hypoglycemic effects attributed to enhanced insulin resistance\u0000through the activation of the PPAR-γ receptor. This manuscript aims to present a comprehensive\u0000review of research conducted on TZD derivatives as potential antihyperglycemic agents spanning\u0000from 2010 to the current date. The review encompasses insights into their molecular mechanisms.\u0000Thiazolidin-based chemicals have received significant attention as hypoglycemic agents and provided\u0000information on patents granted for TZD analogs.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"47 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141353281","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-11DOI: 10.2174/0115734072310948240529112415
Sonia Singh, Khushi Sharma
Cubeb, often referred to as Piper cubeba (Piperaceae), has a long history in traditional herbal medicine, particularly in the management of digestive and respiratory disorders. The plant is a valuable source of essential oils, which are very important economically and are mostly found in its fruits. Recent research has validated many of the traditional applications and their bioactive components, highlighting their antibacterial, antioxidant, anticancer, and anti-inflammatory properties. This article presents a contemporary summary of bioactive compounds and the pharmacological properties of plants. It also explores the potential of plant P. cubeba for future applications in promoting health and nutrition.
{"title":"Unveiling the Potential of Piper cubeba L. f.: A Comprehensive\u0000Review Covering its Phytochemistry, Pharmacology, and Cutting-edge\u0000Applications","authors":"Sonia Singh, Khushi Sharma","doi":"10.2174/0115734072310948240529112415","DOIUrl":"https://doi.org/10.2174/0115734072310948240529112415","url":null,"abstract":"\u0000\u0000Cubeb, often referred to as Piper cubeba (Piperaceae), has a long history in traditional\u0000herbal medicine, particularly in the management of digestive and respiratory disorders. The plant\u0000is a valuable source of essential oils, which are very important economically and are mostly found\u0000in its fruits. Recent research has validated many of the traditional applications and their bioactive\u0000components, highlighting their antibacterial, antioxidant, anticancer, and anti-inflammatory properties.\u0000This article presents a contemporary summary of bioactive compounds and the pharmacological\u0000properties of plants. It also explores the potential of plant P. cubeba for future applications\u0000in promoting health and nutrition.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"95 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141359146","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-07DOI: 10.2174/0115734072316509240530044415
Reshmi Paul, Sourav Nag, Sumanta Mondal, Naresh Panigrahi, Partha Roy, Santosh Kumar Sahoo, Raja S, Abu Mohiuddin
In recent scientific studies, a variety of phytochemicals, including carotenoids, polyphenols, isoprenoids, phytosterols, saponins, and dietetic fibers, besides polysaccharides, have been linked to beneficial health effects, which include reducing the risk of diabetes, obesity, and cancer, cardiovascular diseases, and other conditions. Squash, pumpkin, cucumber, and melons are just a few examples of the Cucurbitaceae family plants that contain cucurbitacins, highly oxygenated tetracyclic triterpenes. Since ancient times, various traditional remedies have been made from plants that contain cucurbitacins. Several cucurbitacins (A, B, C, D, E, F, G, I, J, K, L, O, P, Q, R, S) have an extensive assortment of bioactivities, including hepatoprotective activity, liver protection, anticancer, anti-inflammatory, antiviral, and anti-diabetic properties. Cucurbitacins, for instance, have a well-known anticancer effect. Specific reports suggest that cucurbitacins stimulate apoptosis via the JAK/STAT3 pathway. Through cyclin inhibition, cucurbitacins may inhibit the cell cycle. Besides, they expedite autophagy while preventing cancer cells from migrating and infecting other tissues. Cucurbitacins have been categorized as signal transducers and activators of transcription. It is soundly acknowledged that the plant-based compound cucurbitacin B (CuB) has insecticidal and repellent properties. CuB has been shown to have non-specific toxicity and limited bioavailability in studies evaluating its toxicity and pharmacokinetic characteristics. Hence, we aimed to concentrate on the numerous properties of cucurbitacins in this article, including their chemistry, an analysis of biosynthesis, several types of bioactivities, and studies on their toxicity.
{"title":"Cucurbitacin: Unveiling its Role as Phytomolecule in Health Benefits","authors":"Reshmi Paul, Sourav Nag, Sumanta Mondal, Naresh Panigrahi, Partha Roy, Santosh Kumar Sahoo, Raja S, Abu Mohiuddin","doi":"10.2174/0115734072316509240530044415","DOIUrl":"https://doi.org/10.2174/0115734072316509240530044415","url":null,"abstract":"\u0000\u0000In recent scientific studies, a variety of phytochemicals, including carotenoids,\u0000polyphenols, isoprenoids, phytosterols, saponins, and dietetic fibers, besides polysaccharides,\u0000have been linked to beneficial health effects, which include reducing the risk of diabetes, obesity,\u0000and cancer, cardiovascular diseases, and other conditions. Squash, pumpkin, cucumber, and\u0000melons are just a few examples of the Cucurbitaceae family plants that contain cucurbitacins,\u0000highly oxygenated tetracyclic triterpenes. Since ancient times, various traditional remedies have\u0000been made from plants that contain cucurbitacins. Several cucurbitacins (A, B, C, D, E, F, G, I, J,\u0000K, L, O, P, Q, R, S) have an extensive assortment of bioactivities, including hepatoprotective\u0000activity, liver protection, anticancer, anti-inflammatory, antiviral, and anti-diabetic properties.\u0000Cucurbitacins, for instance, have a well-known anticancer effect. Specific reports suggest that\u0000cucurbitacins stimulate apoptosis via the JAK/STAT3 pathway. Through cyclin inhibition,\u0000cucurbitacins may inhibit the cell cycle. Besides, they expedite autophagy while preventing\u0000cancer cells from migrating and infecting other tissues. Cucurbitacins have been categorized as\u0000signal transducers and activators of transcription. It is soundly acknowledged that the plant-based\u0000compound cucurbitacin B (CuB) has insecticidal and repellent properties. CuB has been shown to\u0000have non-specific toxicity and limited bioavailability in studies evaluating its toxicity and\u0000pharmacokinetic characteristics. Hence, we aimed to concentrate on the numerous properties of\u0000cucurbitacins in this article, including their chemistry, an analysis of biosynthesis, several types\u0000of bioactivities, and studies on their toxicity.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" 26","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141375360","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-07DOI: 10.2174/0115734072303357240528095424
A. Varlamova, S. Khalikov, I. Arkhipov, M. Arisov, K. Sadov, Michael M. Ilyin
Due to the fact that animal parasitic diseases often occur in the form of mixed infections, it is necessary to use complex drugs with a combination of active substances that act against different classes of helminths. Fenbendazole has a wide spectrum of nematocidal action and is less effective against cestodes. Considering that sheep are often infected with both gastro-intestinal nematodes and cestodes, a complex drug based on fenbendazole, niclosamide with polyvinylpyrrolidone polymer, was developed using mechanochemical technology in order to increase its solubility and bioavailability and reduce the dosages and side effects. This study aimed to evaluate the influence of mechanochemical technology on the efficacy of complex solid dispersions of anthelmintics against cestodoses and nematodoses. The influence of different types of mills (roller and planetary mills), levels of energy intensity (20, 40, 60 g), and component ratio (2:20:78; 3:30:67; 4:40:56) during mechanochemical processing was studied on the anthelmintic efficacy of complex solid dispersions of fenbendazole, niclosamide, and polyvinylpyrrolidone in laboratory models of trichinellosis and hymenolepiosis of white mice, and on sheep naturally infected with helminths. The efficacy of complex solid dispersions obtained in the planetary mill was higher than the activity of dispersions obtained in a roller mill. It showed 87.5, 96.36, 83.77, and 99.39% efficacy, respectively, against experimental trichinellosis, hymenolepiosis of white mice, gastrointestinal nematode infection and monieziosis of sheep at a ratio of 2:20:78. The basic drug – fenbendazole demonstrated 31.37 and 22.77% activity against experimental trichinellosis and gastro-intestinal nematode infection of sheep. The basic drug, niclosamide, showed 36.37% efficacy against hymenolepiosis in mice and 28.31% against monieziosis in sheep. It was established that with an increase in the energy intensity level of the planetary mill (20, 40, and 60 g), the decrease in the efficacy of solid dispersion occurred from 73.90 to 59.12% against T. spiralis and from 92.73% to 79.81% against H. nana. The use of mechanochemical technology for the production of solid dispersions of fenbendazole and niclosamide with polyvinylpyrrolidone makes it possible to increase the anthelmintic efficacy by 2.7–3 times compared to the activity of basic substances. It was noted that the complex solid dispersions of anthelmintics obtained in a planetary mill had 7.51–10.17% greater activity in comparison with the samples obtained in a roller mill. The most optimal ratio of active substances was 2:20:78 at a 20 g level of energy intensity of the planetary mill.
{"title":"Influence of Parameters of Mechanochemical Processing on the Efficacy of Complex Solid Dispersion of Anthelmintics","authors":"A. Varlamova, S. Khalikov, I. Arkhipov, M. Arisov, K. Sadov, Michael M. Ilyin","doi":"10.2174/0115734072303357240528095424","DOIUrl":"https://doi.org/10.2174/0115734072303357240528095424","url":null,"abstract":"\u0000\u0000Due to the fact that animal parasitic diseases often occur in the form\u0000of mixed infections, it is necessary to use complex drugs with a combination of active substances\u0000that act against different classes of helminths. Fenbendazole has a wide spectrum of nematocidal\u0000action and is less effective against cestodes. Considering that sheep are often infected with\u0000both gastro-intestinal nematodes and cestodes, a complex drug based on fenbendazole,\u0000niclosamide with polyvinylpyrrolidone polymer, was developed using mechanochemical\u0000technology in order to increase its solubility and bioavailability and reduce the dosages and side\u0000effects.\u0000\u0000\u0000\u0000This study aimed to evaluate the influence of mechanochemical technology on the efficacy\u0000of complex solid dispersions of anthelmintics against cestodoses and nematodoses.\u0000\u0000\u0000\u0000The influence of different types of mills (roller and planetary mills), levels of energy\u0000intensity (20, 40, 60 g), and component ratio (2:20:78; 3:30:67; 4:40:56) during mechanochemical\u0000processing was studied on the anthelmintic efficacy of complex solid dispersions of fenbendazole,\u0000niclosamide, and polyvinylpyrrolidone in laboratory models of trichinellosis and hymenolepiosis\u0000of white mice, and on sheep naturally infected with helminths.\u0000\u0000\u0000\u0000The efficacy of complex solid dispersions obtained in the planetary mill was higher than\u0000the activity of dispersions obtained in a roller mill. It showed 87.5, 96.36, 83.77, and 99.39% efficacy,\u0000respectively, against experimental trichinellosis, hymenolepiosis of white mice, gastrointestinal\u0000nematode infection and monieziosis of sheep at a ratio of 2:20:78. The basic drug –\u0000fenbendazole demonstrated 31.37 and 22.77% activity against experimental trichinellosis and\u0000gastro-intestinal nematode infection of sheep. The basic drug, niclosamide, showed 36.37% efficacy\u0000against hymenolepiosis in mice and 28.31% against monieziosis in sheep. It was established\u0000that with an increase in the energy intensity level of the planetary mill (20, 40, and 60 g), the decrease\u0000in the efficacy of solid dispersion occurred from 73.90 to 59.12% against T. spiralis and\u0000from 92.73% to 79.81% against H. nana.\u0000\u0000\u0000\u0000The use of mechanochemical technology for the production of solid dispersions\u0000of fenbendazole and niclosamide with polyvinylpyrrolidone makes it possible to increase the\u0000anthelmintic efficacy by 2.7–3 times compared to the activity of basic substances. It was\u0000noted that the complex solid dispersions of anthelmintics obtained in a planetary mill had\u00007.51–10.17% greater activity in comparison with the samples obtained in a roller mill. The most\u0000optimal ratio of active substances was 2:20:78 at a 20 g level of energy intensity of the planetary\u0000mill.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" 84","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141374794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-06DOI: 10.2174/0115734072301970240528053901
Kaushal Arora, Prabhakar Kumar Verma
In this study, a new series of 2-amino-6-(substituted)pyrimidin-4-yl-2Hchromen- 2-one analogues (S1-S15) was prepared by using the Knovengeal condensation method and evaluated for antimicrobial as well as antioxidant activity. To ensure the progress and confirmation of the reactions, TLC was employed. The melting points (MP) were ascertained utilising a Sunbim-made sonar melting point device produced in India. To confirm the chemical structures of these compounds, we employed a range of techniques, including FT-IR, MS, 1H-NMR, and Elemental analysis. The antimicrobial and antifungal activity was evaluated using the tube dilution method, and a DPPH assay was used to assess antioxidant activity. Within the series, S1 demonstrated strong antibacterial efficacy against S. Aureus, with a minimum inhibitory concentration value of 16.26μg/ml, while compound S7 displayed significant potential against B. subtilis and E. coli, with a MIC value of 17.34μg/ml. For antifungal activity, compounds S7 and S11 are the most potent against A. niger, showing a minimum inhibitory concentration of 17.34μg/ml. In the evaluation of antioxidant activity, it was observed that compounds S2 and S4 displayed outstanding antioxidant properties, with IC50 values of 13.33μg/ml and 43.13μg/ml. The newly created derivatives exhibited robust antimicrobial and antioxidant characteristics upon assessment through designated methodologies, surpassing the efficacy of conventional drugs in the comparative analysis. Notably, compounds S1, S2, S7, S4, and S11 exhibited even greater activity than the reference drugs. Their structure-activity relationship was also discussed.
{"title":"Design, Synthesis, In vitro Antimicrobial and Antioxidant Evaluation of\u0000Novel Pyrimidine Derivatives","authors":"Kaushal Arora, Prabhakar Kumar Verma","doi":"10.2174/0115734072301970240528053901","DOIUrl":"https://doi.org/10.2174/0115734072301970240528053901","url":null,"abstract":"\u0000\u0000In this study, a new series of 2-amino-6-(substituted)pyrimidin-4-yl-2Hchromen-\u00002-one analogues (S1-S15) was prepared by using the Knovengeal condensation method\u0000and evaluated for antimicrobial as well as antioxidant activity.\u0000\u0000\u0000\u0000To ensure the progress and confirmation of the reactions, TLC was employed. The melting\u0000points (MP) were ascertained utilising a Sunbim-made sonar melting point device produced in India.\u0000To confirm the chemical structures of these compounds, we employed a range of techniques, including\u0000FT-IR, MS, 1H-NMR, and Elemental analysis. The antimicrobial and antifungal activity was\u0000evaluated using the tube dilution method, and a DPPH assay was used to assess antioxidant activity.\u0000\u0000\u0000\u0000Within the series, S1 demonstrated strong antibacterial efficacy against S. Aureus, with a minimum inhibitory concentration value of 16.26μg/ml, while compound S7 displayed significant potential against B. subtilis and E. coli, with a MIC value of 17.34μg/ml. For antifungal activity, compounds S7 and S11 are the most potent against A. niger, showing a minimum inhibitory concentration of 17.34μg/ml. In the evaluation of antioxidant activity, it was observed that compounds S2 and S4 displayed outstanding antioxidant properties, with IC50 values of 13.33μg/ml and 43.13μg/ml.\u0000\u0000\u0000\u0000The newly created derivatives exhibited robust antimicrobial and antioxidant characteristics\u0000upon assessment through designated methodologies, surpassing the efficacy of conventional\u0000drugs in the comparative analysis. Notably, compounds S1, S2, S7, S4, and S11 exhibited even\u0000greater activity than the reference drugs. Their structure-activity relationship was also discussed.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"22 46","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141380174","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-04DOI: 10.2174/0115734072310728240528071149
Mahmoud N. M. Yousif
{"title":"Recent Advances in Chemistry and Biological Activity of Sulphonamides","authors":"Mahmoud N. M. Yousif","doi":"10.2174/0115734072310728240528071149","DOIUrl":"https://doi.org/10.2174/0115734072310728240528071149","url":null,"abstract":"<jats:sec>\u0000<jats:title/>\u0000<jats:p/>\u0000</jats:sec>","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"242 3‐5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141386748","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-20DOI: 10.2174/0115734072320056240513054917
Sonia Singh, Aman Gupta, Mahima Varshney
Skin cancer has become the fifth most frequently reported form of cancer worldwide, imposing significant economic and public health challenges. Over the course of the last ten years, there has been a significant increase in the application of Nanoparticles (NPs) as a method of therapeutic administration to target skin cancer. The information has been gathered from many online databases, such as Scopus, Pubmed, Science Direct, and Web of Science, among others. An analysis of research articles that focused on the therapeutic effect of nanoformulations on skin cancer was included as part of the criteria for selecting the study. Nanoparticles have the potential to change the pharmacokinetics of the drug, increase the drug’s half-life by lowering immunogenicity, increase its bioavailability, decrease drug metabolism, and improve the solubility of poorly water-soluble drugs. The distribution of NP-based treatments to the skin requires special consideration due to the fact that the skin acts as both a physical and immunologic barrier. In addition, specialized technologies must take into consideration not only the target but also the channel of administration in order to be effective. The purpose of this review article was to provide an overview of many types of NPs, address the current landscape of NPs for skin cancer prevention and treatment, and provide a description of the application of NP-based technologies for drug delivery targeting the skin.
皮肤癌已成为全球第五大高发癌症，给经济和公共卫生带来了巨大挑战。在过去十年中，纳米粒子（NPs）作为一种针对皮肤癌的治疗方法的应用显著增加。这些信息是从 Scopus、Pubmed、Science Direct 和 Web of Science 等许多在线数据库中收集的，对侧重于纳米制剂对皮肤癌的治疗效果的研究文章进行分析是选择研究的标准之一。纳米颗粒有可能改变药物的药代动力学，通过降低免疫原性延长药物的半衰期，增加生物利用度，降低药物代谢，以及提高水溶性差的药物的溶解度。由于皮肤既是物理屏障，又是免疫屏障，因此需要特别考虑将基于 NP 的治疗分配到皮肤上。此外，专门的技术不仅要考虑目标，还要考虑给药渠道，这样才能有效。这篇综述文章的目的是概述多种类型的 NPs，探讨当前 NPs 在皮肤癌预防和治疗中的应用前景，并介绍基于 NP 的皮肤靶向给药技术的应用。
{"title":"Application of Nanotechnology as a Novel Approach to the Treatment of\u0000Skin Cancer","authors":"Sonia Singh, Aman Gupta, Mahima Varshney","doi":"10.2174/0115734072320056240513054917","DOIUrl":"https://doi.org/10.2174/0115734072320056240513054917","url":null,"abstract":"\u0000\u0000Skin cancer has become the fifth most frequently reported form of cancer worldwide,\u0000imposing significant economic and public health challenges. Over the course of the last ten years,\u0000there has been a significant increase in the application of Nanoparticles (NPs) as a method of\u0000therapeutic administration to target skin cancer. The information has been gathered from many\u0000online databases, such as Scopus, Pubmed, Science Direct, and Web of Science, among others.\u0000An analysis of research articles that focused on the therapeutic effect of nanoformulations on skin\u0000cancer was included as part of the criteria for selecting the study. Nanoparticles have the potential\u0000to change the pharmacokinetics of the drug, increase the drug’s half-life by lowering immunogenicity,\u0000increase its bioavailability, decrease drug metabolism, and improve the solubility of poorly\u0000water-soluble drugs. The distribution of NP-based treatments to the skin requires special consideration\u0000due to the fact that the skin acts as both a physical and immunologic barrier. In addition,\u0000specialized technologies must take into consideration not only the target but also the channel of\u0000administration in order to be effective. The purpose of this review article was to provide an overview\u0000of many types of NPs, address the current landscape of NPs for skin cancer prevention and\u0000treatment, and provide a description of the application of NP-based technologies for drug delivery\u0000targeting the skin.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"58 19","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141121809","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-15DOI: 10.2174/0115734072294675240502065442
Mohsin Ali Khan, Anwar Khan, Akhlak Ahmed Khan, Simrah, Mohd. Aamir Mirza, Kamran Javed Naquvi, Devendra Kumar
Nowadays, cancer treatment is currently limited to surgery, chemotherapy, and radiation, which carry the risk of damaging the normal tissue of the body and incomplete removal of the cancerous cells from the body. Thus, the Nano technique offers a great means to target therapies directly on cancerous cells and neoplasm. Moreover, because nano-based formulations of polyphenolic curcumin show a major effect on cancer and tumour cells, nanoparticles have a tendency to overcome the hydrophobic nature of curcumin to improve its stability and bioavailability in vitro and in vivo. It is apparent from the studies that Curcumin has shown anticancer effects by regulating various immunomodulators, which include cytokines, reactive oxygen species, and cyclooxygenase-2 (COX-2). It also takes part in the downregulation of growth factors, protein kinases, oncogenic molecules, and various signalling pathways, such as nuclear factor kappalight- chain enhancer of activated B cells (NF-κB), c-Jun N-terminal kinase (JNK), and signal transducer and activator of transcription 3 (STAT3) signalling. According to recent studies and clinical trials, nano curcumin shows a major effect on cancerous cells. In this article, the authors summarised the mechanism of nano curcumin in various metastatic cancers and the most recent clinical trials performed.
目前，癌症的治疗方法仅限于手术、化疗和放疗，但这些方法都有可能损伤人体正常组织，而且不能完全清除体内的癌细胞。因此，纳米技术为直接针对癌细胞和肿瘤的治疗提供了一个很好的手段。此外，由于多酚姜黄素的纳米制剂对癌细胞和肿瘤细胞有重大作用，因此纳米颗粒有克服姜黄素疏水性的趋势，以提高其在体外和体内的稳定性和生物利用度。研究表明，姜黄素通过调节各种免疫调节剂（包括细胞因子、活性氧和环氧化酶-2 (COX-2)）而显示出抗癌作用。它还参与下调生长因子、蛋白inkinases、致癌分子和各种信号通路，如活化 B 细胞的核因子 kappalight-chain 增强子（NF-κB）、c-Jun N 端激酶（JNK）和信号转导和激活转录 3（STAT3）信号。根据最近的研究和临床试验，纳米姜黄素对癌细胞有重大作用。在本文中，作者总结了纳米姜黄素在各种转移性癌症中的作用机制以及最新的临床试验。
{"title":"Anti-carcinogenic Potential of Nano-curcumin -“Killing Cancerous Cells”","authors":"Mohsin Ali Khan, Anwar Khan, Akhlak Ahmed Khan, Simrah, Mohd. Aamir Mirza, Kamran Javed Naquvi, Devendra Kumar","doi":"10.2174/0115734072294675240502065442","DOIUrl":"https://doi.org/10.2174/0115734072294675240502065442","url":null,"abstract":"\u0000\u0000Nowadays, cancer treatment is currently limited to surgery, chemotherapy, and radiation,\u0000which carry the risk of damaging the normal tissue of the body and incomplete removal of\u0000the cancerous cells from the body. Thus, the Nano technique offers a great means to target therapies\u0000directly on cancerous cells and neoplasm. Moreover, because nano-based formulations of\u0000polyphenolic curcumin show a major effect on cancer and tumour cells, nanoparticles have a tendency\u0000to overcome the hydrophobic nature of curcumin to improve its stability and bioavailability\u0000in vitro and in vivo. It is apparent from the studies that Curcumin has shown anticancer effects by\u0000regulating various immunomodulators, which include cytokines, reactive oxygen species, and\u0000cyclooxygenase-2 (COX-2). It also takes part in the downregulation of growth factors, protein\u0000kinases, oncogenic molecules, and various signalling pathways, such as nuclear factor kappalight-\u0000chain enhancer of activated B cells (NF-κB), c-Jun N-terminal kinase (JNK), and signal\u0000transducer and activator of transcription 3 (STAT3) signalling. According to recent studies and\u0000clinical trials, nano curcumin shows a major effect on cancerous cells. In this article, the authors\u0000summarised the mechanism of nano curcumin in various metastatic cancers and the most recent\u0000clinical trials performed.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"138 41","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140976376","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-13DOI: 10.2174/0115734072297726240430040317
Joice Barbosa do Nascimento, José Walber Gonçalves Castro, Maria Inácio da Silva, José Jonas Ferreira Viturino, Mariana Pereira da Silva, Ana Cecilia Calixto Donelardy, Johnatan Wellisson da Silva Mendes, Fabíola Fernandes Galvão Rodrigues, José Galberto Martins da Costa
The present study aimed to investigate the chemical profile and evaluate the antibacterial and antibiotic-modulating activity of the methanolic extract and ethyl acetate of the stem bark of C. quercifolius against standard and multiresistant strains. The Minimum Inhibitory Concentration was determined by the microdilution method, and the modulating potential of the extracts on aminoglycoside and β-lactam antibiotics was evaluated. The classes of secondary metabolites identified from qualitative chemical prospecting were flavones, flavonols, xanthones, flavonones, flavonols, catechins and leucoanthocyanidins. The assays showed inhibition only for Klebsiella pneumoniae-producing extended-spectrum β- lactamase, Klebsiella pneumoniae carbapenemase and Escherichia coli ATCC 25922 with MICs of 256, 512 and 512 μg/mL, respectively. The extracts, when associated with gentamicin and amoxicillin, showed synergism against all standard and multiresistant strains, with the exception of Klebsiella pneumoniae carbapenemase and Klebsiella pneumoniae producing extendedspectrum β-lactamase, respectively. When combined with amikacin, they also demonstrated synergism against multidrug-resistant strains; however, only the ethyl acetate extract had a synergistic effect against E. coli ATCC 25922. The association of penicillin with methanolic extract showed synergism only for Klebsiella pneumoniae producing extended-spectrum β-lactamase and S. aureus ATCC 29213, while the ethyl acetate extracts demonstrated synergism against S. aureus and Klebsiella pneumoniae producing extended-spectrum β-lactamase. It was found that C. quercifolius extracts have antibacterial potential against gramnegative bacteria. However, the need for additional research using specific methods against bacteria carrying different resistance mechanisms, especially gram-positive ones, is highlighted, with the aim of elucidating their mechanism of action. The species was found to have substances with potential against Gram-negative bacteria. However, the need for additional research using specific methods against bacteria carrying different resistance mechanisms, especially Gram-positive ones, is highlighted, with the aim of elucidating their mechanism of action.
{"title":"Chemical Profile with Antibacterial and Modulatory Activity of Extracts from the Stem Bark of Cnidoscolus quercifolius Pohl.","authors":"Joice Barbosa do Nascimento, José Walber Gonçalves Castro, Maria Inácio da Silva, José Jonas Ferreira Viturino, Mariana Pereira da Silva, Ana Cecilia Calixto Donelardy, Johnatan Wellisson da Silva Mendes, Fabíola Fernandes Galvão Rodrigues, José Galberto Martins da Costa","doi":"10.2174/0115734072297726240430040317","DOIUrl":"https://doi.org/10.2174/0115734072297726240430040317","url":null,"abstract":"\u0000\u0000The present study aimed to investigate the chemical profile and evaluate the\u0000antibacterial and antibiotic-modulating activity of the methanolic extract and ethyl acetate of the\u0000stem bark of C. quercifolius against standard and multiresistant strains.\u0000\u0000\u0000\u0000The Minimum Inhibitory Concentration was determined by the microdilution method,\u0000and the modulating potential of the extracts on aminoglycoside and β-lactam antibiotics was\u0000evaluated.\u0000\u0000\u0000\u0000The classes of secondary metabolites identified from qualitative chemical prospecting\u0000were flavones, flavonols, xanthones, flavonones, flavonols, catechins and leucoanthocyanidins.\u0000The assays showed inhibition only for Klebsiella pneumoniae-producing extended-spectrum β-\u0000lactamase, Klebsiella pneumoniae carbapenemase and Escherichia coli ATCC 25922 with MICs\u0000of 256, 512 and 512 μg/mL, respectively. The extracts, when associated with gentamicin and\u0000amoxicillin, showed synergism against all standard and multiresistant strains, with the exception\u0000of Klebsiella pneumoniae carbapenemase and Klebsiella pneumoniae producing extendedspectrum\u0000β-lactamase, respectively. When combined with amikacin, they also demonstrated synergism\u0000against multidrug-resistant strains; however, only the ethyl acetate extract had a synergistic\u0000effect against E. coli ATCC 25922. The association of penicillin with methanolic extract\u0000showed synergism only for Klebsiella pneumoniae producing extended-spectrum β-lactamase and\u0000S. aureus ATCC 29213, while the ethyl acetate extracts demonstrated synergism against S. aureus\u0000and Klebsiella pneumoniae producing extended-spectrum β-lactamase.\u0000\u0000\u0000\u0000It was found that C. quercifolius extracts have antibacterial potential against gramnegative\u0000bacteria. However, the need for additional research using specific methods against bacteria\u0000carrying different resistance mechanisms, especially gram-positive ones, is highlighted, with\u0000the aim of elucidating their mechanism of action.\u0000\u0000\u0000\u0000The species was found to have substances with potential against Gram-negative bacteria. However, the need for additional research using specific methods against bacteria carrying different resistance mechanisms, especially Gram-positive ones, is highlighted, with the aim of elucidating their mechanism of action.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"105 28","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140986021","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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