Antibiotic resistance has become a major public threat across the globe associated with human health. Some bacterial and fungal infections produce bacterial resistance, such as methicillin- resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE) and multidrug-resistant (MDR) species Acinetobacter baumannii etc. Tetrahydrocarbazoles (THCz) are a sub-class of indole alkaloids profoundly present in natural products and biologically active compounds and have displayed potential biological activities in literature. THCz exhibit potential antibacterial activities through major bacterial pathways like cell wall synthesis inhibition and DNA gyrase enzyme inhibition with DNA sliding clamp inhibitors and MreB inhibitors. These THCZ also showed significant in vitro antibacterial activities against bacterial-resistant species, such as MRSA, VRE and Acinetobacter baumannii (MDR) in literature. MTDL (Multi Target Direct ligand) approach has been significantly used for the design of THC motif-based antibacterial agents. In this review article, we collected literature on THCz as a potential antibacterial agent from 2014 to date. The review study of THC core-based derivatives found excellent in vitro antibacterial profiles and revealed that they can play a significant role in drug discovery and the development of new antibiotics against various infectious diseases.
{"title":"Antibacterial Potential of Tetrahydrocarbazoles (THCZ): A Review","authors":"Nitin Kumar, Shalini Sharma, Saurabh Agrawal, Vishesh Verma","doi":"10.2174/0115734072275884240125100455","DOIUrl":"https://doi.org/10.2174/0115734072275884240125100455","url":null,"abstract":"\u0000\u0000Antibiotic resistance has become a major public threat across the globe associated with\u0000human health. Some bacterial and fungal infections produce bacterial resistance, such as methicillin-\u0000resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE)\u0000and multidrug-resistant (MDR) species Acinetobacter baumannii etc. Tetrahydrocarbazoles\u0000(THCz) are a sub-class of indole alkaloids profoundly present in natural products and biologically\u0000active compounds and have displayed potential biological activities in literature. THCz exhibit\u0000potential antibacterial activities through major bacterial pathways like cell wall synthesis inhibition\u0000and DNA gyrase enzyme inhibition with DNA sliding clamp inhibitors and MreB inhibitors.\u0000These THCZ also showed significant in vitro antibacterial activities against bacterial-resistant species,\u0000such as MRSA, VRE and Acinetobacter baumannii (MDR) in literature. MTDL (Multi Target\u0000Direct ligand) approach has been significantly used for the design of THC motif-based antibacterial\u0000agents. In this review article, we collected literature on THCz as a potential antibacterial\u0000agent from 2014 to date. The review study of THC core-based derivatives found excellent in vitro\u0000antibacterial profiles and revealed that they can play a significant role in drug discovery and the\u0000development of new antibiotics against various infectious diseases.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"255 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139799483","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}
Antibiotic resistance has become a major public threat across the globe associated with human health. Some bacterial and fungal infections produce bacterial resistance, such as methicillin- resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE) and multidrug-resistant (MDR) species Acinetobacter baumannii etc. Tetrahydrocarbazoles (THCz) are a sub-class of indole alkaloids profoundly present in natural products and biologically active compounds and have displayed potential biological activities in literature. THCz exhibit potential antibacterial activities through major bacterial pathways like cell wall synthesis inhibition and DNA gyrase enzyme inhibition with DNA sliding clamp inhibitors and MreB inhibitors. These THCZ also showed significant in vitro antibacterial activities against bacterial-resistant species, such as MRSA, VRE and Acinetobacter baumannii (MDR) in literature. MTDL (Multi Target Direct ligand) approach has been significantly used for the design of THC motif-based antibacterial agents. In this review article, we collected literature on THCz as a potential antibacterial agent from 2014 to date. The review study of THC core-based derivatives found excellent in vitro antibacterial profiles and revealed that they can play a significant role in drug discovery and the development of new antibiotics against various infectious diseases.
{"title":"Antibacterial Potential of Tetrahydrocarbazoles (THCZ): A Review","authors":"Nitin Kumar, Shalini Sharma, Saurabh Agrawal, Vishesh Verma","doi":"10.2174/0115734072275884240125100455","DOIUrl":"https://doi.org/10.2174/0115734072275884240125100455","url":null,"abstract":"\u0000\u0000Antibiotic resistance has become a major public threat across the globe associated with\u0000human health. Some bacterial and fungal infections produce bacterial resistance, such as methicillin-\u0000resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE)\u0000and multidrug-resistant (MDR) species Acinetobacter baumannii etc. Tetrahydrocarbazoles\u0000(THCz) are a sub-class of indole alkaloids profoundly present in natural products and biologically\u0000active compounds and have displayed potential biological activities in literature. THCz exhibit\u0000potential antibacterial activities through major bacterial pathways like cell wall synthesis inhibition\u0000and DNA gyrase enzyme inhibition with DNA sliding clamp inhibitors and MreB inhibitors.\u0000These THCZ also showed significant in vitro antibacterial activities against bacterial-resistant species,\u0000such as MRSA, VRE and Acinetobacter baumannii (MDR) in literature. MTDL (Multi Target\u0000Direct ligand) approach has been significantly used for the design of THC motif-based antibacterial\u0000agents. In this review article, we collected literature on THCz as a potential antibacterial\u0000agent from 2014 to date. The review study of THC core-based derivatives found excellent in vitro\u0000antibacterial profiles and revealed that they can play a significant role in drug discovery and the\u0000development of new antibiotics against various infectious diseases.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"171 7","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139859339","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}
The present study investigated the development of kidney stone formation in animal models involving renal tubular stone formation by ethylene glycol and COX-2 selective inhibitor-induced urolithiasis along with the diuretic potentiality by Lipschitz teston Wistar rats. Hemidesmus indicus (H. indicus) R. Br. played a prominent role in various ancient traditional systems of medications and possessed various pharmacological applications. Since the last few decades, urolithiasis has been a major constraint in both livestock and human health. Celecoxib administration increased urinary enzyme excretion but did not affect oxalate or citrate excretion in a urolithiasis model. This research provides a comprehensive account of the ethnobotanical use of H. indicus as an antiurolithiatic and diuretic agent in animal models. The plant material was dried, pulverized into a dry powder, extracted with ethanol, and analyzed for the presence of various secondary metabolites. The anti-urolithic effect of ethanolic extract of H. indicus roots in albino rats was investigated using ethylene glycol (0.75%) and COX -2 selective inhibitor models The experimental data showed the significant effect of H. Indicus root extract (HIEE) as anti-urolithiasis by the prevention of kidney stone formation, also by decreasing crystal nucleation, growth inhibition, decreased aggregation, and crystal retention within the renal tubules. The effect of HIEE supplementation prevents the impairment of renal stone formation, which was also confirmed by the histological findings. HIEE also acts as a potent diuretic, which supports the study. The results indicated that HIEE was effective against experimentally induced urolithiasis, and it also acts as a potent diuretic in treated animals. So, it needs to perform future research on medicinal plants, including in vivo mechanistic and human studies for urolithiasis.
{"title":"Anti Urolithiatic and Diuretic Potentiality of Hemidesmus indicus R. Br.","authors":"Saumya Das, Avijit Mazumder, Smriti Ojha, Deepika Pathak, Himanshu Singh, Pratibha Pandey, Rashmi Saxena Pal","doi":"10.2174/0115734072286989240124112311","DOIUrl":"https://doi.org/10.2174/0115734072286989240124112311","url":null,"abstract":"\u0000\u0000The present study investigated the development of kidney stone formation in animal models involving renal tubular stone formation by ethylene glycol and COX-2 selective inhibitor-induced urolithiasis along with the diuretic potentiality by Lipschitz teston Wistar rats.\u0000\u0000\u0000\u0000Hemidesmus indicus (H. indicus) R. Br. played a prominent role in various ancient\u0000traditional systems of medications and possessed various pharmacological applications. Since the\u0000last few decades, urolithiasis has been a major constraint in both livestock and human health.\u0000Celecoxib administration increased urinary enzyme excretion but did not affect oxalate or citrate\u0000excretion in a urolithiasis model.\u0000\u0000\u0000\u0000This research provides a comprehensive account of the ethnobotanical use of H. indicus as an antiurolithiatic and diuretic agent in animal models.\u0000\u0000\u0000\u0000The plant material was dried, pulverized into a dry powder, extracted with ethanol, and\u0000analyzed for the presence of various secondary metabolites. The anti-urolithic effect of ethanolic\u0000extract of H. indicus roots in albino rats was investigated using ethylene glycol (0.75%) and COX\u0000-2 selective inhibitor models\u0000\u0000\u0000\u0000The experimental data showed the significant effect of H. Indicus root extract (HIEE) as\u0000anti-urolithiasis by the prevention of kidney stone formation, also by decreasing crystal nucleation, growth inhibition, decreased aggregation, and crystal retention within the renal tubules. The\u0000effect of HIEE supplementation prevents the impairment of renal stone formation, which was also\u0000confirmed by the histological findings. HIEE also acts as a potent diuretic, which supports the\u0000study.\u0000\u0000\u0000\u0000The results indicated that HIEE was effective against experimentally induced urolithiasis, and it also acts as a potent diuretic in treated animals. So, it needs to perform future research on medicinal plants, including in vivo mechanistic and human studies for urolithiasis.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"47 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139869671","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}
The present study investigated the development of kidney stone formation in animal models involving renal tubular stone formation by ethylene glycol and COX-2 selective inhibitor-induced urolithiasis along with the diuretic potentiality by Lipschitz teston Wistar rats. Hemidesmus indicus (H. indicus) R. Br. played a prominent role in various ancient traditional systems of medications and possessed various pharmacological applications. Since the last few decades, urolithiasis has been a major constraint in both livestock and human health. Celecoxib administration increased urinary enzyme excretion but did not affect oxalate or citrate excretion in a urolithiasis model. This research provides a comprehensive account of the ethnobotanical use of H. indicus as an antiurolithiatic and diuretic agent in animal models. The plant material was dried, pulverized into a dry powder, extracted with ethanol, and analyzed for the presence of various secondary metabolites. The anti-urolithic effect of ethanolic extract of H. indicus roots in albino rats was investigated using ethylene glycol (0.75%) and COX -2 selective inhibitor models The experimental data showed the significant effect of H. Indicus root extract (HIEE) as anti-urolithiasis by the prevention of kidney stone formation, also by decreasing crystal nucleation, growth inhibition, decreased aggregation, and crystal retention within the renal tubules. The effect of HIEE supplementation prevents the impairment of renal stone formation, which was also confirmed by the histological findings. HIEE also acts as a potent diuretic, which supports the study. The results indicated that HIEE was effective against experimentally induced urolithiasis, and it also acts as a potent diuretic in treated animals. So, it needs to perform future research on medicinal plants, including in vivo mechanistic and human studies for urolithiasis.
{"title":"Anti Urolithiatic and Diuretic Potentiality of Hemidesmus indicus R. Br.","authors":"Saumya Das, Avijit Mazumder, Smriti Ojha, Deepika Pathak, Himanshu Singh, Pratibha Pandey, Rashmi Saxena Pal","doi":"10.2174/0115734072286989240124112311","DOIUrl":"https://doi.org/10.2174/0115734072286989240124112311","url":null,"abstract":"\u0000\u0000The present study investigated the development of kidney stone formation in animal models involving renal tubular stone formation by ethylene glycol and COX-2 selective inhibitor-induced urolithiasis along with the diuretic potentiality by Lipschitz teston Wistar rats.\u0000\u0000\u0000\u0000Hemidesmus indicus (H. indicus) R. Br. played a prominent role in various ancient\u0000traditional systems of medications and possessed various pharmacological applications. Since the\u0000last few decades, urolithiasis has been a major constraint in both livestock and human health.\u0000Celecoxib administration increased urinary enzyme excretion but did not affect oxalate or citrate\u0000excretion in a urolithiasis model.\u0000\u0000\u0000\u0000This research provides a comprehensive account of the ethnobotanical use of H. indicus as an antiurolithiatic and diuretic agent in animal models.\u0000\u0000\u0000\u0000The plant material was dried, pulverized into a dry powder, extracted with ethanol, and\u0000analyzed for the presence of various secondary metabolites. The anti-urolithic effect of ethanolic\u0000extract of H. indicus roots in albino rats was investigated using ethylene glycol (0.75%) and COX\u0000-2 selective inhibitor models\u0000\u0000\u0000\u0000The experimental data showed the significant effect of H. Indicus root extract (HIEE) as\u0000anti-urolithiasis by the prevention of kidney stone formation, also by decreasing crystal nucleation, growth inhibition, decreased aggregation, and crystal retention within the renal tubules. The\u0000effect of HIEE supplementation prevents the impairment of renal stone formation, which was also\u0000confirmed by the histological findings. HIEE also acts as a potent diuretic, which supports the\u0000study.\u0000\u0000\u0000\u0000The results indicated that HIEE was effective against experimentally induced urolithiasis, and it also acts as a potent diuretic in treated animals. So, it needs to perform future research on medicinal plants, including in vivo mechanistic and human studies for urolithiasis.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"268 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139809806","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 : 2024-01-31DOI: 10.2174/0115734072282896240115111712
Sweety Dahiya, Anil Kumar Chhillar
In the immunocompromised population, Candida species are the most aetiologic agents causing severe nosocomial fungal infections. Candida species, irrespective of being commensals in the human microbiome, are the fourth most prevalent source of potentially fatal yeast infections. Monotherapy is frequently employed to treat invasive fungal infections, but sometimes, patients do not favor the monotherapy treatment regime. It may be because of the reduced susceptibility of the pathogen toward traditional antimycotic drugs. Antimycotic drug combination therapy could be a better choice in such specific circumstances. In our study, we evaluated the interactions of fluconazole with diphenyl diselenide. The antimycotic susceptibilities of Candida species for fluconazole and diphenyl diselenide were determined by broth microdilution assay, and the in-vitro interactions of fluconazole with diphenyl diselenide were studied by using disc diffusion assay and chequerboard assay. The nature of the interactions was assessed by calculating the fractional inhibitory concentration index (FICI). The interactions were also analyzed by the response surface approach. The minimum inhibitory concentrations (MICs) for fluconazole and diphenyl diselenide as determined by the broth microdilution assay against Candida species were 4 μg/ml-512 μg/ml and 1 μg/ml-32 μg/ml, respectively. The FICI values varied from 0.375 to 2. Our finding demonstrated that there is no antagonism interaction between fluconazole and diphenyl diselenide in Candida species. Thus, this innovative combination should be explored in the future.
{"title":"In-vitro Interactions between Fluconazole and Diphenyl Diselenide against Various Candida Species","authors":"Sweety Dahiya, Anil Kumar Chhillar","doi":"10.2174/0115734072282896240115111712","DOIUrl":"https://doi.org/10.2174/0115734072282896240115111712","url":null,"abstract":"\u0000\u0000In the immunocompromised population, Candida species are the most\u0000aetiologic agents causing severe nosocomial fungal infections. Candida species, irrespective of\u0000being commensals in the human microbiome, are the fourth most prevalent source of potentially\u0000fatal yeast infections. Monotherapy is frequently employed to treat invasive fungal infections, but\u0000sometimes, patients do not favor the monotherapy treatment regime. It may be because of the reduced\u0000susceptibility of the pathogen toward traditional antimycotic drugs. Antimycotic drug\u0000combination therapy could be a better choice in such specific circumstances. In our study, we\u0000evaluated the interactions of fluconazole with diphenyl diselenide.\u0000\u0000\u0000\u0000The antimycotic susceptibilities of Candida species for fluconazole and diphenyl\u0000diselenide were determined by broth microdilution assay, and the in-vitro interactions of fluconazole\u0000with diphenyl diselenide were studied by using disc diffusion assay and chequerboard assay.\u0000The nature of the interactions was assessed by calculating the fractional inhibitory concentration\u0000index (FICI). The interactions were also analyzed by the response surface approach.\u0000\u0000\u0000\u0000The minimum inhibitory concentrations (MICs) for fluconazole and diphenyl diselenide\u0000as determined by the broth microdilution assay against Candida species were 4 μg/ml-512 μg/ml\u0000and 1 μg/ml-32 μg/ml, respectively. The FICI values varied from 0.375 to 2.\u0000\u0000\u0000\u0000Our finding demonstrated that there is no antagonism interaction between fluconazole\u0000and diphenyl diselenide in Candida species. Thus, this innovative combination should be\u0000explored in the future.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"101 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140475573","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 : 2024-01-29DOI: 10.2174/0115734072276049231207110314
Sudesh Kumari, Prity Gulia, Pooja Choudhary, N. Sharma, Sweety Dahiya, Aruna Punia, A. K. Chhillar
Screening for novel bioactive compounds has become more critical since drugresistant fungal infections have emerged and ethno-medicinal plants have been embarked as antifungal agents. The emphasis on medicinal plants has recently switched to the study of endophytes and their interactions with the host plant and screening of their antifungal activity. Endophytes are an endosymbiotic group of microorganisms that thrive within plant tissues without causing any symptoms or marking their presence. Endophytes have been looked into as potential resources for producing distinctive bioactive substances. The quest for bioactive natural compounds of endophytes isolated from higher plants is receiving a lot of interest from researchers worldwide, as seen by the recent surge in studies and publications on antifungal potential. This review aims to comprehend the role and applications of endophytes as a promising source of antifungal agents and enlighten on their most common mode of action.
{"title":"Endophytes: Untapped Source of Antifungal Agents","authors":"Sudesh Kumari, Prity Gulia, Pooja Choudhary, N. Sharma, Sweety Dahiya, Aruna Punia, A. K. Chhillar","doi":"10.2174/0115734072276049231207110314","DOIUrl":"https://doi.org/10.2174/0115734072276049231207110314","url":null,"abstract":"\u0000\u0000Screening for novel bioactive compounds has become more critical since drugresistant\u0000fungal infections have emerged and ethno-medicinal plants have been embarked as antifungal\u0000agents. The emphasis on medicinal plants has recently switched to the study of endophytes\u0000and their interactions with the host plant and screening of their antifungal activity. Endophytes\u0000are an endosymbiotic group of microorganisms that thrive within plant tissues without causing\u0000any symptoms or marking their presence. Endophytes have been looked into as potential resources\u0000for producing distinctive bioactive substances. The quest for bioactive natural compounds\u0000of endophytes isolated from higher plants is receiving a lot of interest from researchers worldwide,\u0000as seen by the recent surge in studies and publications on antifungal potential. This review\u0000aims to comprehend the role and applications of endophytes as a promising source of antifungal\u0000agents and enlighten on their most common mode of action.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"67 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140485842","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 : 2024-01-26DOI: 10.2174/0115734072275982231230073813
Taylor H. Díaz-Herrera, María Leonor Caldas Martínez, E. Coy-Barrera
Infectious diseases are considered a global public health problem, with viruses being the predominant infectious agents afflicting the human population. The most used control alternatives are the search and development of vaccines and drugs. Nevertheless, their efficacy has limitations related to the immune response stimulation, resistance mechanisms, costeffort ratio, development, and production. An alternative to these drawbacks is the search for compounds isolated from plants with antiviral and/or virucidal properties. The genus Phyllanthus is a plant group producing compounds that gathers an antiviral and virucidal spectrum on different biological models. However, there is no complete review of their properties against viruses in cell models. To compile and analyse the more relevant information on the antiviral and virucidal activity in cell models, phytochemical composition, and generalities of the genus Phyllanthus. The information was assembled from a general search for articles in various databanks, and the information was organized, tabulated, and discussed. The taxonomic classification of the genus Phyllanthus showed discrepancies between different authors and publications. The antiviral and virucidal effects of Phyllanthus naturallyoccurring compounds on cell models showed a broad spectrum and a high chemical diversity mainly related to phenols and polyphenols. Antiviral and virucidal properties of Phyllanthus-derived compounds showed promising results as controlling agents against viral infections in different cell models, particularly in the viral replication and translation processes. Further studies are required to elucidate the specific mechanisms involved in these natural alternatives to expand their efficient and effective applications.
{"title":"Phyllanthus-derived Naturally-occurring Products: An Overview of Their\u0000Effects against Viruses in Cell Models","authors":"Taylor H. Díaz-Herrera, María Leonor Caldas Martínez, E. Coy-Barrera","doi":"10.2174/0115734072275982231230073813","DOIUrl":"https://doi.org/10.2174/0115734072275982231230073813","url":null,"abstract":"\u0000\u0000Infectious diseases are considered a global public health problem, with\u0000viruses being the predominant infectious agents afflicting the human population. The most used\u0000control alternatives are the search and development of vaccines and drugs. Nevertheless, their\u0000efficacy has limitations related to the immune response stimulation, resistance mechanisms, costeffort ratio, development, and production. An alternative to these drawbacks is the search for\u0000compounds isolated from plants with antiviral and/or virucidal properties. The genus Phyllanthus\u0000is a plant group producing compounds that gathers an antiviral and virucidal spectrum on different biological models. However, there is no complete review of their properties against viruses in\u0000cell models.\u0000\u0000\u0000\u0000To compile and analyse the more relevant information on the antiviral and virucidal\u0000activity in cell models, phytochemical composition, and generalities of the genus Phyllanthus.\u0000\u0000\u0000\u0000The information was assembled from a general search for articles in various databanks,\u0000and the information was organized, tabulated, and discussed.\u0000\u0000\u0000\u0000The taxonomic classification of the genus Phyllanthus showed discrepancies between\u0000different authors and publications. The antiviral and virucidal effects of Phyllanthus naturallyoccurring compounds on cell models showed a broad spectrum and a high chemical diversity\u0000mainly related to phenols and polyphenols.\u0000\u0000\u0000\u0000Antiviral and virucidal properties of Phyllanthus-derived compounds showed promising results as controlling agents against viral infections in different cell models, particularly in\u0000the viral replication and translation processes. Further studies are required to elucidate the specific mechanisms involved in these natural alternatives to expand their efficient and effective applications.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"44 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140494236","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 : 2024-01-26DOI: 10.2174/0115734072278257231224171735
S. K. Panday, Munish Kumar
4-Substituted- 5-oxo-prolinates (pyroglutamates) are important components in various natural products, e.g. (-)-bulgecinine, (-)-anatoxin, salinosporamide, as well as ACE inhibitors. These also act as important intermediates in the synthesis of many of the bioactive molecules. Due to these reasons, the synthesis of 4-substituted-(2S)-5-oxo-prolinates has received much attention over the globe in the last three decades. However, most of the synthetic strategies available in the literature describe either the use of expensive lithium enolate-derived lowtemperature chemistry or the rigorous reaction conditions, and therefore, a simple, environmentfriendly, and cost-effective approach was truly demanding. In our ongoing research program, we required different 4-substituted pyroglutamates as intermediates, and with that very basic objective, we were looking for an alternate strategy which should be simple, requiring cheap reagents and consequently, in the process, it was thought to attempt proline catalyzed aldol/alkylation reactions on pyroglutamates, and the idea provided excellent outcome. Herein we wish to report the L-proline catalyzed asymmetric functionalization at C-4 of (2S)-5-oxoproline methyl ester, which furnished desired products at room temperature at the same time, not requiring expensive reagents and, therefore, in turn, cost-effective. This new strategy explored for synthesizing 4-substituted pyroglutamates could be useful for researchers across the globe working in the area and requiring substitution at C-4 of pyroglutamates for synthesizing bioactive molecules/natural products.
{"title":"Environment-friendly Simple, and Straightforward Approach Towards the C-4 functionalization of (2S)-5-oxoproline Methyl Ester","authors":"S. K. Panday, Munish Kumar","doi":"10.2174/0115734072278257231224171735","DOIUrl":"https://doi.org/10.2174/0115734072278257231224171735","url":null,"abstract":"\u0000\u00004-Substituted- 5-oxo-prolinates (pyroglutamates) are important components\u0000in various natural products, e.g. (-)-bulgecinine, (-)-anatoxin, salinosporamide, as well as\u0000ACE inhibitors.\u0000\u0000\u0000\u0000These also act as important intermediates in the synthesis of many of the bioactive molecules.\u0000Due to these reasons, the synthesis of 4-substituted-(2S)-5-oxo-prolinates has received\u0000much attention over the globe in the last three decades. However, most of the synthetic strategies\u0000available in the literature describe either the use of expensive lithium enolate-derived lowtemperature\u0000chemistry or the rigorous reaction conditions, and therefore, a simple, environmentfriendly,\u0000and cost-effective approach was truly demanding.\u0000\u0000\u0000\u0000In our ongoing research program, we required different 4-substituted pyroglutamates as\u0000intermediates, and with that very basic objective, we were looking for an alternate strategy which\u0000should be simple, requiring cheap reagents and consequently, in the process, it was thought to\u0000attempt proline catalyzed aldol/alkylation reactions on pyroglutamates, and the idea provided excellent\u0000outcome.\u0000\u0000\u0000\u0000Herein we wish to report the L-proline catalyzed asymmetric functionalization at C-4 of\u0000(2S)-5-oxoproline methyl ester, which furnished desired products at room temperature at the\u0000same time, not requiring expensive reagents and, therefore, in turn, cost-effective.\u0000\u0000\u0000\u0000This new strategy explored for synthesizing 4-substituted pyroglutamates could be\u0000useful for researchers across the globe working in the area and requiring substitution at C-4 of\u0000pyroglutamates for synthesizing bioactive molecules/natural products.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"10 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140494150","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}
The aim of the study is to assess Neuro-pharmacological activity of Coleus Forskohlii for anti-compulsive activity in Swiss albino mice Obsessive-Compulsive Disorder (OCD) is a common psychiatric illness characterized by obsessions or compulsions that significantly disrupt or impair daily functioning. Coleus forskohlii, a significant medicinal crop, has forskolin in its roots. It is utilized extensively as food and medicine all over the world. Coleus forskohlii has reputed medicinal uses, which includes antidepressant, anti-aggregant, cAMP-genic, anticancer etc. This study used mice models of marble burying and nestlet shredding to assess the potential efficacy of Coleus forskohlii against obsessive-compulsive disorder. 8-OH-DPAT induced-compulsive checking can demonstrate OCD-like repetitive and obsessive behaviour as well as neurotransmitter imbalance (serotonin). Each group had five mice, and the therapy was administered to the animals for a total of 15 days. On days 1, 7, and 14, the marble burying test was assessed for 30 minutes, and on days 2, 8 and 15, the nestlet shredding test was assessed for 30 minutes. The T-maze paradigm was used to assess anti-OCD activity. The brain histology and morphometry were also performed. When compared to the control group, treatments with Coleus forskohlii (50 and 100 mg/kg, p.o.) significantly enhanced performance on both behaviour tests. The SAB score is dramatically increased following administration of 8-OH-DPAT (2 mg/kg, i.p.) group. Coleus forskohlii (50 and 100 mg/kg, p.o.) and fluoxetine (15 mg/kg, p.o.) groups showed significantly lowered results. Animals treated with 8-OH-DPAT showed a considerable reduction serotonin level. Following Coleus forskholii administration, the histology of the brain tissues showed normal morphological structure with no toxicity or abnormalities. The combination of all these finding points to Coleus forskohlii delivered a possible therapeutic option for the treatment of OCD. The identification and anti-compulsive properties of the components from Coleus forskohlii should be the main aim of future study.
{"title":"Neuro-pharmacological Assessment of Coleus forskohlii for Anti-compulsive\u0000Activity in Swiss Albino Mice","authors":"Sagarika Majhi, Manvi Singh, Iti Chauhan, Madhu Verma, Raj Kumari","doi":"10.2174/0115734072278540231229120913","DOIUrl":"https://doi.org/10.2174/0115734072278540231229120913","url":null,"abstract":"\u0000\u0000The aim of the study is to assess Neuro-pharmacological activity of Coleus Forskohlii for anti-compulsive activity in Swiss albino mice\u0000\u0000\u0000\u0000Obsessive-Compulsive Disorder (OCD) is a common psychiatric illness characterized by obsessions or compulsions that significantly disrupt or impair daily functioning. Coleus forskohlii, a significant medicinal crop, has forskolin in its roots. It is utilized extensively as food and medicine all over the world. Coleus forskohlii has reputed medicinal uses, which includes antidepressant, anti-aggregant, cAMP-genic, anticancer etc.\u0000\u0000\u0000\u0000This study used mice models of marble burying and nestlet shredding to assess the potential efficacy of Coleus forskohlii against obsessive-compulsive disorder. 8-OH-DPAT induced-compulsive checking can demonstrate OCD-like repetitive and obsessive behaviour as well as neurotransmitter imbalance (serotonin).\u0000\u0000\u0000\u0000Each group had five mice, and the therapy was administered to the animals for a total of 15 days. On days 1, 7, and 14, the marble burying test was assessed for 30 minutes, and on days 2, 8 and 15, the nestlet shredding test was assessed for 30 minutes. The T-maze paradigm was used to assess anti-OCD activity. The brain histology and morphometry were also performed.\u0000\u0000\u0000\u0000When compared to the control group, treatments with Coleus forskohlii (50 and 100 mg/kg, p.o.) significantly enhanced performance on both behaviour tests. The SAB score is dramatically increased following administration of 8-OH-DPAT (2 mg/kg, i.p.) group. Coleus forskohlii (50 and 100 mg/kg, p.o.) and fluoxetine (15 mg/kg, p.o.) groups showed significantly lowered results. Animals treated with 8-OH-DPAT showed a considerable reduction serotonin level. Following Coleus forskholii administration, the histology of the brain tissues showed normal morphological structure with no toxicity or abnormalities.\u0000\u0000\u0000\u0000The combination of all these finding points to Coleus forskohlii delivered a possible therapeutic option for the treatment of OCD.\u0000\u0000\u0000\u0000The identification and anti-compulsive properties of the components from Coleus forskohlii should be the main aim of future study.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"66 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140493666","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 : 2024-01-25DOI: 10.2174/0115734072283885231220071717
Amine Ez-Zoubi, Naoufal Elhachlafi, Y. Ez zoubi, Hicham Zarroual, Wafae Moustaid, Riham Sghyar, Farah Abdellah
This paper aimed to investigate, for the first time, the possibility of increasing the antibacterial activities of thymol (TH) by developing an encapsulating agent based on chitosan-grafted cyclodextrin. For this purpose, β-cyclodextrin was monosubstituted at position 6 via propargyl bromide, and chitosan’s amine groups were converted to azide functions. After alkylation and diazotization reactions, the grafting of β-cyclodextrin onto the chitosan (CSβCD) was realized via click chemistry alkyne–azide cycloaddition. The incorporation of TH into chitosan-grafted β-cyclodextrin (TH/CS-βCD) was performed by the freeze-drying method, and the encapsulation efficiency was investigated based on various mass ratios (TH:CS-βCD). The optimized inclusion complex was then thoroughly examined by scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC). The antibacterial activity was assessed against Escherichia coli, Staphylococcus aureus, and Bacillus subtilis using broth-microdilution assay. Fourier transform infrared spectroscopy analysis demonstrated the successful grafting of β-cyclodextrin onto chitosan since the optimum mass ratio between TH and CS-βCD was 1:8 (w:w), corresponding to 78 ± 3.42% of encapsulation efficiency, while SEM, XRD, TGA and DSC confirmed the establishment of TH/CS-βCD inclusion complexes. The in vitro investigation showed that TH/CS-βCD exhibited higher antibacterial properties compared to TH in free form.
{"title":"Chitosan-grafted Cyclodextrin via Click Chemistry as an Encapsulating\u0000Agent to Enhance the Antibacterial Activity of Thymol","authors":"Amine Ez-Zoubi, Naoufal Elhachlafi, Y. Ez zoubi, Hicham Zarroual, Wafae Moustaid, Riham Sghyar, Farah Abdellah","doi":"10.2174/0115734072283885231220071717","DOIUrl":"https://doi.org/10.2174/0115734072283885231220071717","url":null,"abstract":"\u0000\u0000This paper aimed to investigate, for the first time, the possibility of increasing the antibacterial activities of thymol (TH) by developing an encapsulating agent based\u0000on chitosan-grafted cyclodextrin. For this purpose, β-cyclodextrin was monosubstituted at position 6 via propargyl bromide, and chitosan’s amine groups were converted to azide functions.\u0000After alkylation and diazotization reactions, the grafting of β-cyclodextrin onto the chitosan (CSβCD) was realized via click chemistry alkyne–azide cycloaddition.\u0000\u0000\u0000\u0000The incorporation of TH into chitosan-grafted β-cyclodextrin (TH/CS-βCD) was performed by the freeze-drying method, and the encapsulation efficiency was investigated based on\u0000various mass ratios (TH:CS-βCD). The optimized inclusion complex was then thoroughly examined by scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC).\u0000\u0000\u0000\u0000The antibacterial activity was assessed against Escherichia coli, Staphylococcus aureus,\u0000and Bacillus subtilis using broth-microdilution assay. Fourier transform infrared spectroscopy\u0000analysis demonstrated the successful grafting of β-cyclodextrin onto chitosan since the optimum\u0000mass ratio between TH and CS-βCD was 1:8 (w:w), corresponding to 78 ± 3.42% of encapsulation efficiency, while SEM, XRD, TGA and DSC confirmed the establishment of TH/CS-βCD\u0000inclusion complexes.\u0000\u0000\u0000\u0000The in vitro investigation showed that TH/CS-βCD exhibited higher antibacterial\u0000properties compared to TH in free form.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"113 7","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139596738","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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