Pub Date : 2023-05-10DOI: 10.2174/2212796817666230510095530
M. de Cerqueira César, Larissa Rodrigues Souza da Mata, Lais Damásio dos Santos
Hexokinase catalyses the first regulatory step of the glycolytic pathway. We can say without any exaggeration that both hexokinase and glycolysis are involved in the control of brain cells' life and death. To perform these pivotal roles, hexokinase occurs in four different isoforms in mammalian cells. Type I isozyme is best suited for energy generation, introducing glucose in glycolysis. In contrast, Type II and Type III isoforms product is directed to generation of NADPH through the pentose phosphate pathway, utilized in biosynthetic processes. Nevertheless, hexokinase has another unique property to accomplish its multiple functions: the capacity for mitochondrial binding. Linked to its role in apoptosis control, the binding of hexokinase inhibits the action of apoptosis inducers, such as Bax, from initiating the release of intramitochondrial proteins. Akt mediates HKII binding to mitochondria. Overexpression of the phosphatase SHIP2 reduces Akt activity and enhances apoptosis, emphasizing the role of hexokinase in cell death. Furthermore, hexokinase also participates in cellular signaling and functional regulation. Adding complexity to this multidimensional enzyme´s attributes, glycolysis occurs in aerobic or anaerobic situations. “Aerobic glycolysis” participates in the control of cell excitability, in synapse formation and neurite growth. Here we provide an overview of the multiple roles of hexokinase and glycolysis in neuronal metabolic association with astrocytes, oligodendrocytes, and microglia. We also provide an update on the role of hexokinase and glycolysis in microglia activation and in brain aging and neurodegenerative diseases.
{"title":"Hexokinase and glycolysis: Between brain cells life and death","authors":"M. de Cerqueira César, Larissa Rodrigues Souza da Mata, Lais Damásio dos Santos","doi":"10.2174/2212796817666230510095530","DOIUrl":"https://doi.org/10.2174/2212796817666230510095530","url":null,"abstract":"\u0000\u0000Hexokinase catalyses the first regulatory step of the glycolytic pathway. We can say without any exaggeration that both hexokinase and glycolysis are involved in the control of brain cells' life\u0000and death. To perform these pivotal roles, hexokinase occurs in four different isoforms in mammalian\u0000cells. Type I isozyme is best suited for energy generation, introducing glucose in glycolysis. In contrast, Type II and Type III isoforms product is directed to generation of NADPH through the pentose\u0000phosphate pathway, utilized in biosynthetic processes. Nevertheless, hexokinase has another unique\u0000property to accomplish its multiple functions: the capacity for mitochondrial binding. Linked to its\u0000role in apoptosis control, the binding of hexokinase inhibits the action of apoptosis inducers, such as\u0000Bax, from initiating the release of intramitochondrial proteins. Akt mediates HKII binding to mitochondria. Overexpression of the phosphatase SHIP2 reduces Akt activity and enhances apoptosis, emphasizing the role of hexokinase in cell death. Furthermore, hexokinase also participates in cellular\u0000signaling and functional regulation. Adding complexity to this multidimensional enzyme´s attributes,\u0000glycolysis occurs in aerobic or anaerobic situations. “Aerobic glycolysis” participates in the control of\u0000cell excitability, in synapse formation and neurite growth. Here we provide an overview of the multiple roles of hexokinase and glycolysis in neuronal metabolic association with astrocytes, oligodendrocytes, and microglia. We also provide an update on the role of hexokinase and glycolysis in microglia\u0000activation and in brain aging and neurodegenerative diseases.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74552267","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 : 2023-02-27DOI: 10.2174/2212796817666230227112835
Soumia Mouffouk, Chaima Mouffouk, Sara Mouffouk, Hamada Haba
The genus Helianthemum from the Cistaceae family includes about 110 plants, which are well known for their wide therapeutic uses and interesting pharmacological activities. To the best of our knowledge, there are no previous comprehensive and critical reviews on the therapeutic applications, chemical composition, and biological properties of this genus. In this context, the present paper describes a systematic mini-review on the traditional use, phytochemical composition, and pharmacological properties of species belonging to the genus Helianthemum. For this, more than 75 papers covering the period from 1970 to 2022 were collected and analyzed to achieve this review. From 110 species of the genus Helianthemum, only 22 species were studied. Helianthemum species are widely used in folk medicine for the treatment of respiratory, hepatic, renal, psychiatric, and inflammatory diseases. According to the collected information, species from this genus have several pharmacological properties linked to their rich chemical composition, particularly in phenolic compounds and flavonoids. In fact, Helianthemum plants have antioxidant, antimicrobial, anti-inflammatory, analgesic, antidiabetic, insecticide, anticancer, antiulcer, larvicide, chemo, and hepatoprotective activities, justifying their various uses in traditional medicine. Despite the intense use of Helianthemum species in traditional human and veterinary medicine, few studies were conducted on the phytochemical composition and pharmacological activities of the plants constituting this genus. In fact, until now, the emphasis has only been on twenty-two species and the work carried out was not explanatory, especially for certain species. So it will be interesting to broaden the spectrum of the tested biological activities, especially for endemic species in order to understand the possible modes of action and to confirm the toxicity of certain species.
{"title":"Medicinal, pharmacological and biochemical progress on the study of genus Helianthemum: A review","authors":"Soumia Mouffouk, Chaima Mouffouk, Sara Mouffouk, Hamada Haba","doi":"10.2174/2212796817666230227112835","DOIUrl":"https://doi.org/10.2174/2212796817666230227112835","url":null,"abstract":"\u0000\u0000The genus Helianthemum from the Cistaceae family includes about 110 plants, which are well known for their wide therapeutic uses and interesting pharmacological activities. To the best of our knowledge, there are no previous comprehensive and critical reviews on the therapeutic applications, chemical composition, and biological properties of this genus.\u0000\u0000\u0000\u0000In this context, the present paper describes a systematic mini-review on the traditional use, phytochemical composition, and pharmacological properties of species belonging to the genus Helianthemum.\u0000\u0000\u0000\u0000For this, more than 75 papers covering the period from 1970 to 2022 were collected and analyzed to achieve this review.\u0000\u0000\u0000\u0000From 110 species of the genus Helianthemum, only 22 species were studied. Helianthemum species are widely used in folk medicine for the treatment of respiratory, hepatic, renal, psychiatric, and inflammatory diseases. According to the collected information, species from this genus have several pharmacological properties linked to their rich chemical composition, particularly in phenolic compounds and flavonoids. In fact, Helianthemum plants have antioxidant, antimicrobial, anti-inflammatory, analgesic, antidiabetic, insecticide, anticancer, antiulcer, larvicide, chemo, and hepatoprotective activities, justifying their various uses in traditional medicine.\u0000\u0000\u0000\u0000Despite the intense use of Helianthemum species in traditional human and veterinary medicine, few studies were conducted on the phytochemical composition and pharmacological activities of the plants constituting this genus. In fact, until now, the emphasis has only been on twenty-two species and the work carried out was not explanatory, especially for certain species. So it will be interesting to broaden the spectrum of the tested biological activities, especially for endemic species in order to understand the possible modes of action and to confirm the toxicity of certain species.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"85 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87402901","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 : 2023-02-22DOI: 10.2174/2212796817666230222103441
Morteza Vaezi
Unsaturated fatty acids (UFAs) as bioactive compounds possess a wide range of biomedical functions and a lack or shortage of them may cause serious harm to human body health. Biochemically, UFAs have attracted growing interest, and this attention arises not only from biomedical reasons but also economic ones. Among these fatty acids, omega-3 and omega-6 fatty acids are considered the most efficient and safe compounds which can be used for expanding and identification of novel functionalities. They are considered essential membrane components and are associated with a variety of biological processes. For example, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) as polyunsaturated fatty acids (PUFAs) play a central role in the proper functioning of the nervous system like anti-atherogenic properties and improve the functioning of the cardiovascular system. Briefly, understanding the relationship between these properties and potential biomedical applications of UFAs may help to elucidate and facilitate the development of novel pathogenesis strategies regarding their disorders in human health and diseases. This review provides the most suitable functional roles and potential mechanisms of UFAs associated with human health and nutrition.
{"title":"Efficacy and Biomedical Roles of Unsaturated Fatty Acids as Bioactive Food Components","authors":"Morteza Vaezi","doi":"10.2174/2212796817666230222103441","DOIUrl":"https://doi.org/10.2174/2212796817666230222103441","url":null,"abstract":"\u0000\u0000Unsaturated fatty acids (UFAs) as bioactive compounds possess a wide range of biomedical functions and a lack or shortage of them may cause serious harm to human body health. Biochemically, UFAs have attracted growing interest, and this attention arises not only from biomedical reasons but also economic ones. Among these fatty acids, omega-3 and omega-6 fatty acids are considered the most efficient and safe compounds which can be used for expanding and identification of novel functionalities. They are considered essential membrane components and are associated with a variety of biological processes. For example, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) as polyunsaturated fatty acids (PUFAs) play a central role in the proper functioning of the nervous system like anti-atherogenic properties and improve the functioning of the cardiovascular system. Briefly, understanding the relationship between these properties and potential biomedical applications of UFAs may help to elucidate and facilitate the development of novel pathogenesis strategies regarding their disorders in human health and diseases. This review provides the most suitable functional roles and potential mechanisms of UFAs associated with human health and nutrition.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"81 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84977681","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 : 2023-02-14DOI: 10.2174/2212796817666230214100146
M. Ashtiani, Fariba Nabatchian, M. Davoudi, Negin Davoudi, Reza Afrisham
this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines. Evidence suggests that the Hippo pathway, which regulates organ size, is altered in a few conditions like lung cancer. Achillea wilhelmsii that used in the traditional Iranian medicine to treat a variety of disorders has been proven to contribute to some signaling pathways in cancers. In this regards, this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines. this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines. Hydroalcoholic extract was prepared using a Soxhlet extractor and its antiproliferative activity was studied by MTT assay. Then, the mRNA expressions of large tumour suppressor kinases 1 and 2 (LATS1 and LATS2), Yes1 Associated Transcriptional Regulator (YAP1), and Transcriptional co‑activator with PDZ‑binding motif (TAZ) were measured using real-time PCR. According to MTT, the viability was decreased significantly after 24 hours treatment with A. wilhelmsii at concentrations of 200-1000 µg/ml and after 48 hours treatment at a concentration of 100-1000 µg/ml. While the mRNA levels of LATS1, TAZ, and YAP1 decreased significantly compared to untreated cells, the mRNA expression of LATS2 did not change (P˂ 0.05). Hydroalcoholic extract of A. wilhelmsii might inhibit proliferation of lung cancer cells as well as it could decrease the expression of both oncogenes in them. However, it had suppressing effects on LATS1, which should be considered in further studies. none
{"title":"Hydroalcoholic Extract of Achillea Wilhelmsii Decreases the Expressions of Hippo Signaling Pathway-Associated Oncogenes In the A549 Lung Cancer Cell Line","authors":"M. Ashtiani, Fariba Nabatchian, M. Davoudi, Negin Davoudi, Reza Afrisham","doi":"10.2174/2212796817666230214100146","DOIUrl":"https://doi.org/10.2174/2212796817666230214100146","url":null,"abstract":"\u0000\u0000this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines.\u0000\u0000\u0000\u0000Evidence suggests that the Hippo pathway, which regulates organ size, is altered in a few conditions like lung cancer. Achillea wilhelmsii that used in the traditional Iranian medicine to treat a variety of disorders has been proven to contribute to some signaling pathways in cancers. In this regards, this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines.\u0000\u0000\u0000\u0000this study aimed to evaluate the effect of the hydroalcoholic extract of this plant on viability and mRNA expression of some Hippo signaling pathway-associated oncogenes and suppressors in A549 lung cancer cell lines.\u0000\u0000\u0000\u0000Hydroalcoholic extract was prepared using a Soxhlet extractor and its antiproliferative activity was studied by MTT assay. Then, the mRNA expressions of large tumour suppressor kinases 1 and 2 (LATS1 and LATS2), Yes1 Associated Transcriptional Regulator (YAP1), and Transcriptional co‑activator with PDZ‑binding motif (TAZ) were measured using real-time PCR.\u0000\u0000\u0000\u0000According to MTT, the viability was decreased significantly after 24 hours treatment with A. wilhelmsii at concentrations of 200-1000 µg/ml and after 48 hours treatment at a concentration of 100-1000 µg/ml. While the mRNA levels of LATS1, TAZ, and YAP1 decreased significantly compared to untreated cells, the mRNA expression of LATS2 did not change (P˂ 0.05).\u0000\u0000\u0000\u0000Hydroalcoholic extract of A. wilhelmsii might inhibit proliferation of lung cancer cells as well as it could decrease the expression of both oncogenes in them. However, it had suppressing effects on LATS1, which should be considered in further studies.\u0000\u0000\u0000\u0000none\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"141 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73640801","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 : 2023-01-02DOI: 10.2174/2212796817666230102092008
Chaima Mouffouk, Soumia Mouffouk, Sara Mouffouk, Hamada Haba
The genus Onopordum (Asteraceae), with about 40 species, is composed of perennials and spermatophyte plants, which are widely used in popular medicine for the treatment of several human diseases. Plants of this genus constitute an interesting source of bioactive molecules with a wide range of pharmacological applications. In this context, the current study describes a critical review of traditional uses, phytochemistry, and pharmacological effects of the genus Onopordum in order to establish a valuable database for future ethnopharmacological surveys on this genus. For this, all bibliographic data covering the period of 1970 to 2022 were collected and analyzed. Only 19 species from the genus Onopordum were studied. They are traditionally used to treat gastric, renal, respiratory, urinary, and gynecological diseases and in the food industry for cheese production. Indeed, it was found that Onopordum species are rich in flavonoids, phenolic compounds, terpenoids, alkaloids, tannins, and steroids. These plants exhibit several interesting biological activities including: antioxidant, antimicrobial, antiproliferative, apoptotic, cytotoxic, antitumor, anticholinergic, larvicidal, analgesic and antipyretic, hypotensive, antiepileptic, and anticonvulsant activities. Furthermore, their hemostatic, anti-inflammatory, and moisturizing properties, increase their usefulness in the cosmetic field. According to the present study, Onoporadum species constitute an important natural source of secondary metabolites with potential therapeutic, cosmetic, and nutritional applications. However, the focus has been only on 19 species and the publications were not very explanatory, Therefore, in-depth pharmacological and phytochemical studies are needed to fully exploit the therapeutic potential and the chemical composition of Onopordum species.
{"title":"Traditional use, phytochemistry and pharmacological properties of the genus Onopordum","authors":"Chaima Mouffouk, Soumia Mouffouk, Sara Mouffouk, Hamada Haba","doi":"10.2174/2212796817666230102092008","DOIUrl":"https://doi.org/10.2174/2212796817666230102092008","url":null,"abstract":"\u0000\u0000The genus Onopordum (Asteraceae), with about 40 species, is composed of\u0000perennials and spermatophyte plants, which are widely used in popular medicine for the treatment of\u0000several human diseases. Plants of this genus constitute an interesting source of bioactive molecules\u0000with a wide range of pharmacological applications.\u0000\u0000\u0000\u0000In this context, the current study describes a critical review of traditional uses, phytochemistry, and pharmacological effects of the genus Onopordum in order to establish a valuable database\u0000for future ethnopharmacological surveys on this genus.\u0000\u0000\u0000\u0000For this, all bibliographic data covering the period of 1970 to 2022 were collected and analyzed.\u0000\u0000\u0000\u0000Only 19 species from the genus Onopordum were studied. They are traditionally used to treat\u0000gastric, renal, respiratory, urinary, and gynecological diseases and in the food industry for cheese production. Indeed, it was found that Onopordum species are rich in flavonoids, phenolic compounds,\u0000terpenoids, alkaloids, tannins, and steroids. These plants exhibit several interesting biological activities including: antioxidant, antimicrobial, antiproliferative, apoptotic, cytotoxic, antitumor, anticholinergic, larvicidal, analgesic and antipyretic, hypotensive, antiepileptic, and anticonvulsant activities.\u0000Furthermore, their hemostatic, anti-inflammatory, and moisturizing properties, increase their usefulness in the cosmetic field.\u0000\u0000\u0000\u0000According to the present study, Onoporadum species constitute an important natural\u0000source of secondary metabolites with potential therapeutic, cosmetic, and nutritional applications.\u0000However, the focus has been only on 19 species and the publications were not very explanatory,\u0000Therefore, in-depth pharmacological and phytochemical studies are needed to fully exploit the therapeutic potential and the chemical composition of Onopordum species.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74354792","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 : 2022-12-21DOI: 10.2174/2212796817666221221151713
V. S. Mattaparthi, P. Borah
Resveratrol (RSV), a polyphenolic compound, is reported to have anti-aggregation properties against Amyloid-beta peptides. It is, therefore, significant to understand the mechanism of inhibition of Aβ1-42 peptide aggregation by the RSV at the molecular level. We have used Molecular docking along with Molecular dynamics (MD) simulation techniques to address the role of RSV in the inhibition of Aβ1-42 pep-tide aggregation. To understand the role of Resveratrol on the Aβ1-42 peptide aggregation. In this computational study, we have docked the RSV to Aβ1-42 peptide using Molecular Docking software and then performed MD simulation for the Aβ1-42 peptide monomer Aβ1-42 peptide-RSV complex using the AMBER force field. From the analysis of MD trajectories, we obtained salient structural features and determined the Binding Free Energy(BFE) and Per-residue Energy Decomposition Analysis (PRED) using MM-PBSA/GBSA method. The secondary structure and the conformational analysis obtained from MD trajectories show that the binding of RSV with the Aβ1-42 peptide monomer causes an increase in the helical content in the structure of the Aβ1-42 peptide. The BFE and PRED results show a high binding affinity (GBtotal=-11.07 kcal mol-1; PBtotal= -1.82 kcal mol-1) of RSV with Aβ1-42 peptide. Also, we found the RSV to interact with cru-cial residues (Asp 23 and Lys 28) of the Aβ1-42 peptide. These residues play a signif-icant role in facilitating the formation of toxic amyloid oligomers and amyloid fibrils. The salt bridge interaction between these residues D23–K28 was found to be destabi-lized in the Aβ1-42 peptide when it is complexed with RSV. In summary, it can be concluded that Resveratrol greatly aids the preven-tion of Aβ1-42 peptide aggregation. Therefore, it can be considered a possible drug candidate for therapeutic strategies for Alzheimer’s disease.
{"title":"Insights Into Resveratrol as an Inhibitor Against Aβ1-42 Peptide Aggregation: A Molecu-lar Dynamics Simulation Study","authors":"V. S. Mattaparthi, P. Borah","doi":"10.2174/2212796817666221221151713","DOIUrl":"https://doi.org/10.2174/2212796817666221221151713","url":null,"abstract":"\u0000\u0000Resveratrol (RSV), a polyphenolic compound, is reported to have anti-aggregation properties against Amyloid-beta peptides. It is, therefore, significant to understand the mechanism of inhibition of Aβ1-42 peptide aggregation by the RSV at the molecular level. We have used Molecular docking along with Molecular dynamics (MD) simulation techniques to address the role of RSV in the inhibition of Aβ1-42 pep-tide aggregation.\u0000\u0000\u0000\u0000To understand the role of Resveratrol on the Aβ1-42 peptide aggregation.\u0000\u0000\u0000\u0000In this computational study, we have docked the RSV to Aβ1-42 peptide using Molecular Docking software and then performed MD simulation for the Aβ1-42 peptide monomer Aβ1-42 peptide-RSV complex using the AMBER force field. From the analysis of MD trajectories, we obtained salient structural features and determined the Binding Free Energy(BFE) and Per-residue Energy Decomposition Analysis (PRED) using MM-PBSA/GBSA method.\u0000\u0000\u0000\u0000The secondary structure and the conformational analysis obtained from MD trajectories show that the binding of RSV with the Aβ1-42 peptide monomer causes an increase in the helical content in the structure of the Aβ1-42 peptide. The BFE and PRED results show a high binding affinity (GBtotal=-11.07 kcal mol-1; PBtotal= -1.82 kcal mol-1) of RSV with Aβ1-42 peptide. Also, we found the RSV to interact with cru-cial residues (Asp 23 and Lys 28) of the Aβ1-42 peptide. These residues play a signif-icant role in facilitating the formation of toxic amyloid oligomers and amyloid fibrils. The salt bridge interaction between these residues D23–K28 was found to be destabi-lized in the Aβ1-42 peptide when it is complexed with RSV.\u0000\u0000\u0000\u0000In summary, it can be concluded that Resveratrol greatly aids the preven-tion of Aβ1-42 peptide aggregation. Therefore, it can be considered a possible drug candidate for therapeutic strategies for Alzheimer’s disease.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74632460","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 : 2022-12-20DOI: 10.2174/2212796817666221220100340
G. Perin, Daniela H. Mailahn, D. R. Araújo, P. Nobre, C. A. Fonseca, Filipe Penteado, E. Lenardão, C. Luchese, E. A. Wilhelm
We report the synthesis and antioxidant evaluation of 1-organoselanyl-naphthalen-2-ols. The title compounds were selectively prepared through the selenofunctionalization of 2-naphthol derivatives using benzeneseleninic acids as a selenium source. We aimed at synthesizing 1-organoselanyl-naphthalen-2-ol by functionalizing 2-naphthol with arylseleninic acids using glycerol as the solvent and further evaluating the pharmacological activity. The products were synthesized at 70 °C using glycerol as a solvent in an oil bath. Reactive species (RS) tests, DPPH radical scavenging activity assay, and ABTS+ radical scavenging activity assay were performed. A statistical analysis of the data was performed. A total of fifteen 1-organoselanyl-naphthalen-2-ols were selectively obtained in yields of 58-95% in 0.25-48 h of reaction. Additionally, all the synthesized seleno-derivatives exhibited antioxidant activity, as revealed by their ability to scavenge DPPH and ABTS+ radicals and reduce the reactive species (RS) levels. The synthesis of 1-arylselanyl-naphthalen-2-ols was developed under mild reaction conditions using benzeneseleninic acid derivatives in reactions with 2-naphthol. All synthesized 2-naphthol derivatives exhibited antioxidant activity, as revealed by their DPPH and ABTS+ radical scavenging activity and reduced RS levels.
{"title":"Benzeneseleninic acid promoting the selenofunctionalization of 2-naphthol derivatives: Synthesis and antioxidant activity of 1-organoselanyl-naphthalen-2-ols","authors":"G. Perin, Daniela H. Mailahn, D. R. Araújo, P. Nobre, C. A. Fonseca, Filipe Penteado, E. Lenardão, C. Luchese, E. A. Wilhelm","doi":"10.2174/2212796817666221220100340","DOIUrl":"https://doi.org/10.2174/2212796817666221220100340","url":null,"abstract":"\u0000\u0000We report the synthesis and antioxidant evaluation of 1-organoselanyl-naphthalen-2-ols. The title compounds were selectively prepared through the selenofunctionalization of 2-naphthol derivatives using benzeneseleninic acids as a selenium source.\u0000\u0000\u0000\u0000We aimed at synthesizing 1-organoselanyl-naphthalen-2-ol by functionalizing 2-naphthol with arylseleninic acids using glycerol as the solvent and further evaluating the pharmacological activity.\u0000\u0000\u0000\u0000The products were synthesized at 70 °C using glycerol as a solvent in an oil bath. Reactive species (RS) tests, DPPH radical scavenging activity assay, and ABTS+ radical scavenging activity assay were performed. A statistical analysis of the data was performed.\u0000\u0000\u0000\u0000A total of fifteen 1-organoselanyl-naphthalen-2-ols were selectively obtained in yields of 58-95% in 0.25-48 h of reaction. Additionally, all the synthesized seleno-derivatives exhibited antioxidant activity, as revealed by their ability to scavenge DPPH and ABTS+ radicals and reduce the reactive species (RS) levels.\u0000\u0000\u0000\u0000The synthesis of 1-arylselanyl-naphthalen-2-ols was developed under mild reaction conditions using benzeneseleninic acid derivatives in reactions with 2-naphthol. All synthesized 2-naphthol derivatives exhibited antioxidant activity, as revealed by their DPPH and ABTS+ radical scavenging activity and reduced RS levels.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"56 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72942595","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 : 2022-12-08DOI: 10.2174/2212796817666221208115047
P. Shakib, A. Manouchehri, A. Marzban, H. Esmaeil Lashgarian, A. Alhameedawi
Acinetobacter baumannii is an opportunistic bacterium capable of causing nosocomial infections resistant to a wide range of antibiotics. Herbal medicines could become the source of novel therapies for antibiotic-resistant bacteria. This review paper aimed to survey the effectiveness of medicinal plants in treating infections caused by A. baumannii. The relevant data was obtained by systematically searching PubMed, ISI Web of Science, Scopus, Science Direct, and Google Scholar databases with the specific keywords of medicinal plants (including extracts and essential oils) and bacterial infections (including A. baumannii). The present review identified 23 studies published between 2009 and 2021 that discussed the effectiveness of medicinal plants in inhibiting the growth of A. baumannii. In these studies, 28 medicinal plants were found effective against infection caused by A. baumannii in vivo. The results of this review indicated that to develop a therapeutic strategy for treating bacterial infections, especially A. baumannii, based on medicinal plants, extensive studies were required to determine their cytotoxicity and therapeutic dosage before they could be used as an alternative to antibiotics.
鲍曼不动杆菌是一种机会性细菌，能够引起对多种抗生素耐药的医院感染。草药可能成为治疗耐抗生素细菌的新疗法的来源。本文综述了药用植物对鲍曼不动杆菌感染的治疗效果。通过系统检索PubMed、ISI Web of Science、Scopus、Science Direct、谷歌Scholar等数据库，以药用植物(包括提取物和精油)和细菌感染(包括鲍曼不对称杆菌)为特定关键词获取相关数据。本综述确定了2009年至2021年间发表的23项研究，这些研究讨论了药用植物抑制鲍曼不整虫生长的有效性。在这些研究中，发现28种药用植物在体内对鲍曼不动杆菌感染有效。本综述的结果表明，为了开发一种基于药用植物治疗细菌感染的治疗策略，特别是鲍曼不动杆菌，在将其作为抗生素的替代品之前，需要进行广泛的研究，以确定其细胞毒性和治疗剂量。
{"title":"A Systematic Review Study on the Effectiveness of Medicinal Plants against Acinetobacter baumannii","authors":"P. Shakib, A. Manouchehri, A. Marzban, H. Esmaeil Lashgarian, A. Alhameedawi","doi":"10.2174/2212796817666221208115047","DOIUrl":"https://doi.org/10.2174/2212796817666221208115047","url":null,"abstract":"\u0000\u0000Acinetobacter baumannii is an opportunistic bacterium capable of causing nosocomial infections resistant to a wide range of antibiotics. Herbal medicines could become the source of novel therapies for antibiotic-resistant bacteria. This review paper aimed to survey the effectiveness of medicinal plants in treating infections caused by A. baumannii.\u0000\u0000\u0000\u0000The relevant data was obtained by systematically searching PubMed, ISI Web of Science, Scopus, Science Direct, and Google Scholar databases with the specific keywords of medicinal plants (including extracts and essential oils) and bacterial infections (including A. baumannii).\u0000\u0000\u0000\u0000The present review identified 23 studies published between 2009 and 2021 that discussed the effectiveness of medicinal plants in inhibiting the growth of A. baumannii. In these studies, 28 medicinal plants were found effective against infection caused by A. baumannii in vivo.\u0000\u0000\u0000\u0000The results of this review indicated that to develop a therapeutic strategy for treating bacterial infections, especially A. baumannii, based on medicinal plants, extensive studies were required to determine their cytotoxicity and therapeutic dosage before they could be used as an alternative to antibiotics.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90523079","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 : 2022-12-05DOI: 10.2174/2212796817666221205164816
I. Zhigacheva, Natalya I. Kricunova, M. Rasulov
Germanium is a biologically active trace element, and it is present in almost all or-gans and tissues. Its biological activity was revealed in the 20th century. However, the study on the possibility of using germanium for medical purposes was first undertaken by the Japanese sci-entist Dr. Kazuhiko Asai in 1940. In 1965, academician M.G.Voronkov and colleagues synthe-sized tricyclic esters of triethanolamine germanium with the general formula XGe(OCH2CH2)3N and studied their biological activity. However, the adaptogenic properties of these compounds have not been sufficiently studied. In this regard, there is an urgent need to study the adaptogen-ic properties of these drugs. As the resistance of the organism to stress factors primarily depends on energy metabolism, the aim of our work was to study the influence of stress and 1- (germatran-1-il) –oxyethylamine (GM) on the functional state of mitochondria. The functional state of mitochondria was studied as per the rate of mitochon-dria respiration by the level of lipid peroxidation and fatty acid composition of mitochondrial membranes by chromatography technique. It was shown that the drug in concentrations of 10-5, 10-6, and 10-11M reduced the intensity of LPO in the membranes of "aged" mitochondria. This can serve as evidence re-garding the presence of anti-stress properties in the drug. Injection of GM at a dose of 10-5 mol/kg to rats prevented the activation of LPO in the membranes of the liver mitochondria in conditions of acute hypobaric hypoxia. To restrict lipid peroxidation, GM prevented changes in the content of C18 and C22 fatty acids in mitochondrial membranes, which probably contributed to maintaining the bioenergetic characteristics of mitochondria at the control level. It is assumed that the anti-stress activity of the drug is associated with its antioxidant properties and its effect on the complex I of the mitochondrial respiratory chain.
{"title":"Adaptogenic Properties of 1-(Germatran-1-il)-Oxyethylamine","authors":"I. Zhigacheva, Natalya I. Kricunova, M. Rasulov","doi":"10.2174/2212796817666221205164816","DOIUrl":"https://doi.org/10.2174/2212796817666221205164816","url":null,"abstract":"\u0000\u0000Germanium is a biologically active trace element, and it is present in almost all or-gans and tissues. Its biological activity was revealed in the 20th century. However, the study on the possibility of using germanium for medical purposes was first undertaken by the Japanese sci-entist Dr. Kazuhiko Asai in 1940. In 1965, academician M.G.Voronkov and colleagues synthe-sized tricyclic esters of triethanolamine germanium with the general formula XGe(OCH2CH2)3N and studied their biological activity. However, the adaptogenic properties of these compounds have not been sufficiently studied. In this regard, there is an urgent need to study the adaptogen-ic properties of these drugs.\u0000\u0000\u0000\u0000As the resistance of the organism to stress factors primarily depends on energy metabolism, the aim of our work was to study the influence of stress and 1- (germatran-1-il) –oxyethylamine (GM) on the functional state of mitochondria.\u0000\u0000\u0000\u0000The functional state of mitochondria was studied as per the rate of mitochon-dria respiration by the level of lipid peroxidation and fatty acid composition of mitochondrial membranes by chromatography technique.\u0000\u0000\u0000\u0000It was shown that the drug in concentrations of 10-5, 10-6, and 10-11M reduced the intensity of LPO in the membranes of \"aged\" mitochondria. This can serve as evidence re-garding the presence of anti-stress properties in the drug. Injection of GM at a dose of 10-5 mol/kg to rats prevented the activation of LPO in the membranes of the liver mitochondria in conditions of acute hypobaric hypoxia. To restrict lipid peroxidation, GM prevented changes in the content of C18 and C22 fatty acids in mitochondrial membranes, which probably contributed to maintaining the bioenergetic characteristics of mitochondria at the control level.\u0000\u0000\u0000\u0000It is assumed that the anti-stress activity of the drug is associated with its antioxidant properties and its effect on the complex I of the mitochondrial respiratory chain.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87692807","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 : 2022-11-21DOI: 10.2174/2212796817666221121155138
D. Tanini, A. Capperucci
The development of novel small molecules with effective catalytic antioxidant properties is highly sought after. A wide array of structurally diverse selenium- and tellurium-containing glutathione peroxidase mimics have been studied over the past two decades. Within this arena, organotellurium compounds generally exhibit higher catalytic properties with respect to selenium-containing analogues. Different mechanisms accounting for the thiol-peroxidase-like activity of various classes of organotellurium derivatives have been proposed. This review document develops this area and provides an overview of the catalytic mechanisms proposed for the various classes of tellurium-containing thiol-peroxidase-like-catalysts.
{"title":"Tellurium-containing thiol-peroxidase-like antioxidants and their catalytic mechanism","authors":"D. Tanini, A. Capperucci","doi":"10.2174/2212796817666221121155138","DOIUrl":"https://doi.org/10.2174/2212796817666221121155138","url":null,"abstract":"\u0000\u0000The development of novel small molecules with effective catalytic antioxidant properties is highly sought after. A wide array of structurally diverse selenium- and tellurium-containing glutathione peroxidase mimics have been studied over the past two decades. Within this arena, organotellurium compounds generally exhibit higher catalytic properties with respect to selenium-containing analogues. Different mechanisms accounting for the thiol-peroxidase-like activity of various classes of organotellurium derivatives have been proposed. This review document develops this area and provides an overview of the catalytic mechanisms proposed for the various classes of tellurium-containing thiol-peroxidase-like-catalysts.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"69 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73776340","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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