Pub Date : 2024-01-24DOI: 10.2174/0115734072279525231210144617
Arunabh Arandhara, Dipankar Saha, D. J. Deka, Mrinmoy Deka, Bhrigu Kumar Das
The intriguing role of the oxidation system in cardiovascular disease lies in its contribution to chronic and acute increases in intracellular reactive oxygen species (ROS), driving the progression of cardiovascular diseases (CVDs). ROS, produced as by-products of oxidative physiological and metabolic events, act as mediators in various signaling pathways contributing to cardiovascular pathology. The delicate equilibrium between the production of free radicals and antioxidant defense shifts in favor of the former, resulting in redox imbalance and extensive cellular damage. Among CVDs, coronary artery disease (CAD) remains as the leading cause of death globally. Understanding the significance of oxidative damage in the dysfunction of endothelial cells, atherosclerosis, and other pathogenic events and pathways is crucial for preventing and managing CVD. Consequently, it is imperative to comprehend the mechanism/s underlying the pathogenic alterations of CVD due to oxidative damage to develop effective prevention strategies. Many studies have reported bioactive phytochemical/s as potential therapies against CVDs, modulating ROS generation, controlling the CVD-related inflammatory mediators and protecting the vascular system. Therefore, this review provides an update for understanding how the phytoconstituents exhibit preventive roles in oxidative stress-related CVD, thus improving the quality of life of people. This study conducted a thorough literature search on CVD, oxidative imbalance, and phytoconstituents. The search was performed using multiple search engines and the main keywords, and only English publications until June 2023 were included. However, there is a need for more research and clinical trials to fully elucidate the efficacy and safety of these phytochemicals for managing the disease.
{"title":"Redox Imbalance and Cardiovascular Pathogenesis: Exploring the Therapeutic\u0000Potential of Phytochemicals","authors":"Arunabh Arandhara, Dipankar Saha, D. J. Deka, Mrinmoy Deka, Bhrigu Kumar Das","doi":"10.2174/0115734072279525231210144617","DOIUrl":"https://doi.org/10.2174/0115734072279525231210144617","url":null,"abstract":"\u0000\u0000The intriguing role of the oxidation system in cardiovascular disease lies in its contribution\u0000to chronic and acute increases in intracellular reactive oxygen species (ROS), driving the\u0000progression of cardiovascular diseases (CVDs). ROS, produced as by-products of oxidative physiological\u0000and metabolic events, act as mediators in various signaling pathways contributing to\u0000cardiovascular pathology. The delicate equilibrium between the production of free radicals and\u0000antioxidant defense shifts in favor of the former, resulting in redox imbalance and extensive cellular\u0000damage. Among CVDs, coronary artery disease (CAD) remains as the leading cause of\u0000death globally. Understanding the significance of oxidative damage in the dysfunction of endothelial\u0000cells, atherosclerosis, and other pathogenic events and pathways is crucial for preventing\u0000and managing CVD. Consequently, it is imperative to comprehend the mechanism/s underlying\u0000the pathogenic alterations of CVD due to oxidative damage to develop effective prevention strategies.\u0000Many studies have reported bioactive phytochemical/s as potential therapies against CVDs,\u0000modulating ROS generation, controlling the CVD-related inflammatory mediators and protecting\u0000the vascular system. Therefore, this review provides an update for understanding how the phytoconstituents\u0000exhibit preventive roles in oxidative stress-related CVD, thus improving the quality\u0000of life of people. This study conducted a thorough literature search on CVD, oxidative imbalance,\u0000and phytoconstituents. The search was performed using multiple search engines and the main\u0000keywords, and only English publications until June 2023 were included. However, there is a need\u0000for more research and clinical trials to fully elucidate the efficacy and safety of these phytochemicals\u0000for managing the disease.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139600572","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 octahedral Pt(IV) complexes contain either inert or biologically active ligands where the nature of these axial ligands provides additional stability and synergistic biological activity. There are many literature reports from each of the classes mentioning the varied nature of these axial ligands. The targeting, as well as the non-targeting nature of these moieties, exerts additive or synergistic effects of anticancer activity of Pt(II) moieties. Herein, we have discussed the effects of these axially oriented ligands, changes in the non-leaving am(m)ine groups, and changes in the leaving groups on the biological activity. In this review, we have discussed the axial ligands with a focus on the nature of the ligands and alterations in biological activities.
{"title":"Pt(IV) Complexes with Biologically Active and Physicochemical Properties\u0000Modifier Ligands","authors":"Sainath Aher, Jinhua Zhu, Xiuhua Liu, Laxmikant Borse","doi":"10.2174/0115734072277494231213044339","DOIUrl":"https://doi.org/10.2174/0115734072277494231213044339","url":null,"abstract":"\u0000\u0000The octahedral Pt(IV) complexes contain either inert or biologically active ligands\u0000where the nature of these axial ligands provides additional stability and synergistic biological activity.\u0000There are many literature reports from each of the classes mentioning the varied nature of\u0000these axial ligands. The targeting, as well as the non-targeting nature of these moieties, exerts\u0000additive or synergistic effects of anticancer activity of Pt(II) moieties. Herein, we have discussed\u0000the effects of these axially oriented ligands, changes in the non-leaving am(m)ine groups, and\u0000changes in the leaving groups on the biological activity. In this review, we have discussed the\u0000axial ligands with a focus on the nature of the ligands and alterations in biological activities.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139600249","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 : 2024-01-24DOI: 10.2174/0115734072273575231207061849
Madhulika Namdeo, J. Veronica, Krishan Kumar, Anjali Anand, R. Maurya
Leishmaniasis is a protozoan disease caused by a parasite from the genus Leishmania. It is known as a neglected tropical disease by WHO and is the second-leading cause of death by parasites after malaria. Chemotherapy is the only effective way to control the disease, but treatment options for leishmaniasis are limited. The majority of the drugs are costly, have serious side effects and necessitate hospitalisation. The lack of an effective vaccine, in addition to the emergence of resistance to currently available drugs, has all been raised as major concerns, especially in endemic areas of developing countries. Phytochemicals might contribute to the development of novel and effective drugs for the treatment of leishmaniasis by providing selectively targeted intervention in parasites. Many phytochemicals (quinones, alkaloids, terpenes, saponins, phenolics) and their derivatives are quite active against diverse groups of pathogens, such as viruses, bacteria, fungi and parasites. To date, many phytochemicals have shown potent anti-leishmanial activity with highly selective mode of action. However, due to a lack of interaction between academician and pharma industries none of them has undergone the clinical assessment. The present review will analyse the most promising phytochemicals and their synthetic compounds, which have shown antileishmal activity in in-vitro and subsequently in animal studies from 2011-2021. These phytochemicals are apigenin, hydroxyflavanone, Epigallocatechin-O-3 gallate, caffeic acid, α-bisabolol, β-caryophyllene, ursolic acid, quinones, which have shown notable anti-leishmanial activities in several independent studies.
{"title":"Emerging Phytochemicals to Treat Leishmaniasis: A Review of\u0000Experimental Studies from 2011 to 2021","authors":"Madhulika Namdeo, J. Veronica, Krishan Kumar, Anjali Anand, R. Maurya","doi":"10.2174/0115734072273575231207061849","DOIUrl":"https://doi.org/10.2174/0115734072273575231207061849","url":null,"abstract":"\u0000\u0000Leishmaniasis is a protozoan disease caused by a parasite from the genus Leishmania.\u0000It is known as a neglected tropical disease by WHO and is the second-leading cause of death by\u0000parasites after malaria. Chemotherapy is the only effective way to control the disease, but\u0000treatment options for leishmaniasis are limited. The majority of the drugs are costly, have serious\u0000side effects and necessitate hospitalisation. The lack of an effective vaccine, in addition to the\u0000emergence of resistance to currently available drugs, has all been raised as major concerns,\u0000especially in endemic areas of developing countries. Phytochemicals might contribute to the\u0000development of novel and effective drugs for the treatment of leishmaniasis by providing\u0000selectively targeted intervention in parasites. Many phytochemicals (quinones, alkaloids,\u0000terpenes, saponins, phenolics) and their derivatives are quite active against diverse groups of\u0000pathogens, such as viruses, bacteria, fungi and parasites. To date, many phytochemicals have\u0000shown potent anti-leishmanial activity with highly selective mode of action. However, due to a\u0000lack of interaction between academician and pharma industries none of them has undergone the\u0000clinical assessment. The present review will analyse the most promising phytochemicals and their\u0000synthetic compounds, which have shown antileishmal activity in in-vitro and subsequently in\u0000animal studies from 2011-2021. These phytochemicals are apigenin, hydroxyflavanone,\u0000Epigallocatechin-O-3 gallate, caffeic acid, α-bisabolol, β-caryophyllene, ursolic acid, quinones,\u0000which have shown notable anti-leishmanial activities in several independent studies.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139600916","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}
Cancer is a global public health issue. Cancer therapy has been hampered by the issue of multidrug resistance, which is one of the leading causes of death worldwide. As a result, the use of natural derived drugs for cancer prevention and therapy has been researched and developed for decades. Alkaloids are plant-derived secondary metabolites that have antiproliferative and anticancer effects on several forms of cancer. Camptothecin and vinblastine, two anticancer medicines derived from alkaloids, have been adequately developed in the past. Alkaloids, a drug lead compounds, derived from natural products, have the advantage of being used by the host, making them suitable for further exploitation. The current review looks at the anticancer potential of numerous naturally occurring alkaloids, as well as the mechanism behind their anticancer effect.
{"title":"Natural Alkaloids and Mechanisms for Anti-cancer Action: A Review","authors":"Prem Mishra, Niranjan Kaushik, Rakhi Mishra, Sameeksha Koul, Sakshi Sagar","doi":"10.2174/0115734072276134231130170407","DOIUrl":"https://doi.org/10.2174/0115734072276134231130170407","url":null,"abstract":"\u0000\u0000Cancer is a global public health issue. Cancer therapy has been hampered by the issue\u0000of multidrug resistance, which is one of the leading causes of death worldwide. As a result, the\u0000use of natural derived drugs for cancer prevention and therapy has been researched and developed\u0000for decades. Alkaloids are plant-derived secondary metabolites that have antiproliferative and\u0000anticancer effects on several forms of cancer. Camptothecin and vinblastine, two anticancer medicines\u0000derived from alkaloids, have been adequately developed in the past. Alkaloids, a drug lead\u0000compounds, derived from natural products, have the advantage of being used by the host, making\u0000them suitable for further exploitation. The current review looks at the anticancer potential of numerous\u0000naturally occurring alkaloids, as well as the mechanism behind their anticancer effect.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139603350","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 : 2024-01-22DOI: 10.2174/0115734072272429231106090645
Nada Hussien Arafa, Mohamed Refaat Shehata, A. S. Mohamed
Obesity is frequently linked to multiple comorbid and chronic illnesses, including non-alcoholic fatty liver disease, type 2 diabetes, cancer, and heart disease. Ovothiol-A is one of the most powerful natural antioxidants found in marine invertebrates like sea urchins. The current study aimed to investigate ovothiol-A's hypolipidemic and hypoglycemic potential in obese rats. All groups get a high-fat diet (HFD) for four weeks except for the control group. The control and HFD groups received distilled water, while the Ovothiol-A groups received two doses of Ovothiol-A (200 and 400 mg/kg orally) concurrent with HFD. Weight gain, glucose, insulin, alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transferase, alkaline phosphatase, total cholesterol, triglycerides, low-density lipoprotein, malondialdehyde, and nitric oxide were all decreased after oral administration of Ovo at either the 200 or 400 mg/kg dose, while levels of high-density lipoprotein (HDL), glutathionereduced, catalase and glutathione-S-transferase increased. Histopathological alterations were less noticeable in the liver tissue of Ovothiol-A groups, with only a few vacuolated or pyknotic nuclei amongst a few dispersed hepatocytes. The current findings indicate that ovothiol-A protects against high-fat diet-induced fatty liver in rats. The anti-obesity mechanism of Ovothiol-A is associated with its hypolipidemic, hypoglycemic, and antioxidant properties.
{"title":"Ovothiol-A Mitigates High-Fat Diet-Induced Non-alcoholic Fatty Liver\u0000Disease in Rats","authors":"Nada Hussien Arafa, Mohamed Refaat Shehata, A. S. Mohamed","doi":"10.2174/0115734072272429231106090645","DOIUrl":"https://doi.org/10.2174/0115734072272429231106090645","url":null,"abstract":"\u0000\u0000Obesity is frequently linked to multiple comorbid and chronic illnesses,\u0000including non-alcoholic fatty liver disease, type 2 diabetes, cancer, and heart disease. Ovothiol-A\u0000is one of the most powerful natural antioxidants found in marine invertebrates like sea urchins.\u0000\u0000\u0000\u0000The current study aimed to investigate ovothiol-A's hypolipidemic and hypoglycemic\u0000potential in obese rats.\u0000\u0000\u0000\u0000All groups get a high-fat diet (HFD) for four weeks except for the control group. The\u0000control and HFD groups received distilled water, while the Ovothiol-A groups received two doses\u0000of Ovothiol-A (200 and 400 mg/kg orally) concurrent with HFD.\u0000\u0000\u0000\u0000Weight gain, glucose, insulin, alanine aminotransferase, aspartate aminotransferase,\u0000gamma-glutamyl transferase, alkaline phosphatase, total cholesterol, triglycerides, low-density\u0000lipoprotein, malondialdehyde, and nitric oxide were all decreased after oral administration of Ovo\u0000at either the 200 or 400 mg/kg dose, while levels of high-density lipoprotein (HDL), glutathionereduced, catalase and glutathione-S-transferase increased. Histopathological alterations were less\u0000noticeable in the liver tissue of Ovothiol-A groups, with only a few vacuolated or pyknotic nuclei\u0000amongst a few dispersed hepatocytes.\u0000\u0000\u0000\u0000The current findings indicate that ovothiol-A protects against high-fat diet-induced\u0000fatty liver in rats. The anti-obesity mechanism of Ovothiol-A is associated with its hypolipidemic,\u0000hypoglycemic, and antioxidant properties.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139609393","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 : 2024-01-22DOI: 10.2174/0115734072285630240110115046
Saranya Selvaraj, Yasuri Amarasekara, Inoka C. Perera, L. Weerasinghe
Globally, the number of cancer cases and death rates are increasing, making it necessary to develop new and improved medications for the treatment of cancer.Owing to a broad range of physio-chemical properties, Antimicrobial Peptides (AMPs) possessing tumoricidal properties and Anticancer Peptides (ACPs) are promising alternatives for enhanced cancer therapy. Recently, biopharmaceuticals have changed the rules of radiation therapy and chemotherapy by introducing peptide therapy for cancer treatments. However, several limitations obstruct the clinical efficacy of peptide-based cancer therapies, which include limited target specificity, oral intake, and half-life payloads. The integration of theranostic nanomaterials could be facilitated as a transformative strategy to address these challenges and enhance the potential of peptide-based cancer therapy. Increasing applications of recent times of peptide-nano hybrids have addressed the crucial issues related to conventional peptide-based drug therapy by enhancing the druggability. This review aims to explore the impact of nano-formulated peptides as an anticancer agent, highlighting the involvement of nanotechnology as an enabling tool.
{"title":"Theranostic Nanomaterials to Overcome the Challenges in Peptide-based\u0000Cancer Therapy","authors":"Saranya Selvaraj, Yasuri Amarasekara, Inoka C. Perera, L. Weerasinghe","doi":"10.2174/0115734072285630240110115046","DOIUrl":"https://doi.org/10.2174/0115734072285630240110115046","url":null,"abstract":"\u0000\u0000Globally, the number of cancer cases and death rates are increasing, making it necessary to develop new and improved medications for the treatment of cancer.Owing to a broad\u0000range of physio-chemical properties, Antimicrobial Peptides (AMPs) possessing tumoricidal\u0000properties and Anticancer Peptides (ACPs) are promising alternatives for enhanced cancer therapy. Recently, biopharmaceuticals have changed the rules of radiation therapy and chemotherapy\u0000by introducing peptide therapy for cancer treatments. However, several limitations obstruct the\u0000clinical efficacy of peptide-based cancer therapies, which include limited target specificity, oral\u0000intake, and half-life payloads. The integration of theranostic nanomaterials could be facilitated as\u0000a transformative strategy to address these challenges and enhance the potential of peptide-based\u0000cancer therapy. Increasing applications of recent times of peptide-nano hybrids have addressed\u0000the crucial issues related to conventional peptide-based drug therapy by enhancing the druggability. This review aims to explore the impact of nano-formulated peptides as an anticancer agent,\u0000highlighting the involvement of nanotechnology as an enabling tool.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139606433","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}
Chia seed (Salvia hispanica L.) gum is a mucoadhesive, biodegradable polymer with sustained release properties. The objective of this study was to compare different formulations of glipizide-loaded microparticles using chia seed mucilage and sodium alginate, focusing on sustained release and mucoadhesive properties. The present study aimed to comparatively evaluate various eco-friendly formulations of glipizide-loaded microparticles prepared using chia seed mucilage and sodium alginate. Gum was extracted from chia seeds and lyophilized, and preformulation studies were performed according to established protocols. Microparticles were formulated using the ionic gelation method, with sodium alginate as a copolymer and zinc chloride as a cross-linking agent. The prepared microparticles were evaluated using scanning electron microscopy (SEM) for size and particle aggregation, and Fourier Transform infrared spectroscopy (FTIR) for drug-polymer interaction, entrapment efficiency, swelling index, and in vitro drug release. The % yield of chia seed mucilage was 27.35%. The pH of the mucilaginous suspension was 4.67 ± 0.50. The moisture content value was 14.56 % ± 0.50. The values of Carr's index and Hausner's ratio were 22.58 ± 1.89 and 1.38 ± 0.05, respectively. FTIR spectra showed no interaction between pure glipizide and chia seed mucilage, confirming no possible change in glipizide's pharmacology. SEM studies have confirmed the shape of the microparticles to be spherical, with average sizes ranging from 1235.18 ± 8.7 to 1423.25 ± 9.5 µm, and the drug entrapment efficiency ranged from 64.25 ± 2.52 to 81.82 ± 7.56%. The release of glipizide from the microparticles was sustained, and the Higuchi and Korsmeyer-Peppas models were found to be the best-fit kinetic models. The promising copolymer blend of chia seed mucilage and sodium alginate was used for the development of sustained-release dosage forms. A copolymer blend with a ratio of 1:1 produced glipizide-loaded microparticles with sustained release profiles and good mucoadhesive ability, along with a high percentage of drug entrapment efficiency.
{"title":"Formulation and Evaluation of Glipizide-loaded Mucoadhesive Microparticle Using Salvia hispanica Seeds Mucilage as Co-polymer","authors":"Smriti Ojha, Stutu Tripathi, Shivendra Mani Tripathi, Sudhanshu Mishra","doi":"10.2174/0115734072282524240101065517","DOIUrl":"https://doi.org/10.2174/0115734072282524240101065517","url":null,"abstract":"\u0000\u0000Chia seed (Salvia hispanica L.) gum is a mucoadhesive, biodegradable polymer\u0000with sustained release properties.\u0000\u0000\u0000\u0000The objective of this study was to compare different formulations of glipizide-loaded\u0000microparticles using chia seed mucilage and sodium alginate, focusing on sustained release and\u0000mucoadhesive properties.\u0000\u0000\u0000\u0000The present study aimed to comparatively evaluate various eco-friendly\u0000formulations of glipizide-loaded microparticles prepared using chia seed mucilage and sodium\u0000alginate.\u0000\u0000\u0000\u0000Gum was extracted from chia seeds and lyophilized, and preformulation studies were performed according to established protocols. Microparticles were\u0000formulated using the ionic gelation method, with sodium alginate as a copolymer and zinc\u0000chloride as a cross-linking agent. The prepared microparticles were evaluated using scanning\u0000electron microscopy (SEM) for size and particle aggregation, and Fourier Transform infrared\u0000spectroscopy (FTIR) for drug-polymer interaction, entrapment efficiency, swelling index, and in\u0000vitro drug release.\u0000\u0000\u0000\u0000The % yield of chia seed mucilage was 27.35%. The pH of the mucilaginous suspension\u0000was 4.67 ± 0.50. The moisture content value was 14.56 % ± 0.50. The values of Carr's index and\u0000Hausner's ratio were 22.58 ± 1.89 and 1.38 ± 0.05, respectively. FTIR spectra showed no\u0000interaction between pure glipizide and chia seed mucilage, confirming no possible change in\u0000glipizide's pharmacology. SEM studies have confirmed the shape of the microparticles to be\u0000spherical, with average sizes ranging from 1235.18 ± 8.7 to 1423.25 ± 9.5 µm, and the drug\u0000entrapment efficiency ranged from 64.25 ± 2.52 to 81.82 ± 7.56%. The release of glipizide from\u0000the microparticles was sustained, and the Higuchi and Korsmeyer-Peppas models were found to\u0000be the best-fit kinetic models.\u0000\u0000\u0000\u0000The promising copolymer blend of chia seed mucilage and sodium alginate was\u0000used for the development of sustained-release dosage forms. A copolymer blend with a ratio of\u00001:1 produced glipizide-loaded microparticles with sustained release profiles and good\u0000mucoadhesive ability, along with a high percentage of drug entrapment efficiency.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139608987","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 : 2024-01-19DOI: 10.2174/0115734072271233231113070640
Swati Sharma
The present review describes the biological essence of pyridazine scaffold. Around 142 biologically potential pyridazine entities are gathered in a pile from documented literature. Some of them are commercially available drugs, few are naturally occurring pyridazine compounds, and a wide variety of compounds containing pyridazine moiety are biologically tested, and some are under clinical trials. Rather than collecting large quantities of data, an attempt is made to compile valuable entities. However, efforts have been made to compile the maximum literature in brief. The main motto of this review is to provide a combination of therapeutically active pyridazine containing compounds for further drug design, discovery, and development to contribute to future medicinal chemistry. Our approach is to bring the most biologically potent pyridazine derivatives to medicinal chemists, biologists, pharmacists, and organic chemists. The present work encompasses the literature from 2000-2022 from different and authentic sources. The work is divided according to the bioactive nature of pyridazine nucleus.
{"title":"Pyridazine (1,2-Diazine): A Versatile Pharmacophore Known for its Utility in Biological Systems","authors":"Swati Sharma","doi":"10.2174/0115734072271233231113070640","DOIUrl":"https://doi.org/10.2174/0115734072271233231113070640","url":null,"abstract":"\u0000\u0000The present review describes the biological essence of pyridazine scaffold. Around\u0000142 biologically potential pyridazine entities are gathered in a pile from documented literature.\u0000Some of them are commercially available drugs, few are naturally occurring pyridazine compounds,\u0000and a wide variety of compounds containing pyridazine moiety are biologically tested,\u0000and some are under clinical trials. Rather than collecting large quantities of data, an attempt is\u0000made to compile valuable entities. However, efforts have been made to compile the maximum\u0000literature in brief. The main motto of this review is to provide a combination of therapeutically\u0000active pyridazine containing compounds for further drug design, discovery, and development to\u0000contribute to future medicinal chemistry. Our approach is to bring the most biologically potent\u0000pyridazine derivatives to medicinal chemists, biologists, pharmacists, and organic chemists. The\u0000present work encompasses the literature from 2000-2022 from different and authentic sources.\u0000The work is divided according to the bioactive nature of pyridazine nucleus.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139613499","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}
One of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has shown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site— PLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues. The nano-precipitation process was used to make FNS-NPs. The independent variables (stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the point prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs composition was further transformed into a gel formulation. The prepared topical gel formulation (FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies. Optimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI, 71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and the excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content, viscosity, pH, and spreadability. According to the release and permeation investigation findings, FNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before. In a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel showed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth. These findings imply that the innovative formulation that has been developed has several beneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata
{"title":"Optimization and Transfollicular Delivery of Finasteride Loaded PLGA Nanoparticles Laden Carbopol Gel for Treatment of Hair Growth Stimulation","authors":"Mounika Kuchukuntla, Venkatesan Palanivel, Ananthula Madhubabu","doi":"10.2174/0115734072269998240101043601","DOIUrl":"https://doi.org/10.2174/0115734072269998240101043601","url":null,"abstract":"\u0000\u0000One of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has\u0000shown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site—\u0000PLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues.\u0000\u0000\u0000\u0000The nano-precipitation process was used to make FNS-NPs. The independent variables\u0000(stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the\u0000point prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs\u0000composition was further transformed into a gel formulation. The prepared topical gel formulation\u0000(FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry\u0000(DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies.\u0000\u0000\u0000\u0000Optimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI,\u000071.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and\u0000the excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content,\u0000viscosity, pH, and spreadability. According to the release and permeation investigation findings,\u0000FNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before.\u0000In a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel\u0000showed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth.\u0000\u0000\u0000\u0000These findings imply that the innovative formulation that has been developed has several\u0000beneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140503486","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 : 2024-01-18DOI: 10.2174/0115734072272233231119161319
Vinay Kumar, Chanchal Sharma, M. Taleuzzaman, Kandasamy Nagarajan, Anzarul Haque, Mamta Bhatia, Sumayya Khan, Mohammad Ayman A. Salkini, pankaj bhatt
The study aimed to assess the neuroprotective effect of Boswellia serrata against 3-NP-induced experimental Huntington’s disease. Previous studies have shown Boswellia to have sedative, analgesic, and anti-tumour effects. Boswellia serrata yields four pentacyclic triterpene acids and boswellic acid, a bioactive substance that prevents leukotriene biogenesis. The potential neuroprotective effect of Boswellia serrata against 3-nitro propionic acid (3-NP)-induced Huntington's disease (HD) was examined at oral doses of 45 mg/kg, 90 mg/kg, and 180 mg/kg. In this study, HD was induced by 3-NP at a dose of 10 mg/kg in Wistar rats. The study used 56 Wistar rats (8 per group) for biochemical (inflammatory markers, acetylcholinesterase activity) and behavioural (elevated plus maze, Y-maze, open-field, tail suspension tests, etc.) assessments. Additionally, a histological examination of the brain was carried out. In addition, the analysis of Boswellia serrata extract was performed by different analytical techniques, like UV spectrophotometer, FTIR, and HPLC methods. In the brain, succinate dehydrogenase is a mitochondrial enzyme irreversibly inhibited by 3-NP. Administration of 3-NP resulted in HD with altered behavioural and motor changes in rats. Treatment with Boswellia serrata resulted in remarkable protection of rats against 3-NP-induced behaviour and motor deficits in a dose-dependent manner. Moreover, in rats administered with 3-NP, Boswellia serrata improved memory performance and lowered levels of inflammatory biomarkers. These results have also been supported by histopathological analysis. Acetyl-11-keto-p-boswellic acid was found to be the main active component of Boswellia serrata extract. Boswellia serrata at a dose of 180 mg/kg exhibited better protection compared to the other doses against HD induced by 3-NP. More detailed studies based on molecular targets are needed for the Boswellia serrata to transition from the bench to the bedside for use as an adjuvant in HD patients.
{"title":"Neuroprotective Effect of Boswellia serrata against 3-NP Induced Experimental\u0000Huntington’s Disease","authors":"Vinay Kumar, Chanchal Sharma, M. Taleuzzaman, Kandasamy Nagarajan, Anzarul Haque, Mamta Bhatia, Sumayya Khan, Mohammad Ayman A. Salkini, pankaj bhatt","doi":"10.2174/0115734072272233231119161319","DOIUrl":"https://doi.org/10.2174/0115734072272233231119161319","url":null,"abstract":"\u0000\u0000The study aimed to assess the neuroprotective effect of Boswellia serrata\u0000against 3-NP-induced experimental Huntington’s disease.\u0000\u0000\u0000\u0000Previous studies have shown Boswellia to have sedative, analgesic, and anti-tumour\u0000effects. Boswellia serrata yields four pentacyclic triterpene acids and boswellic acid, a bioactive\u0000substance that prevents leukotriene biogenesis.\u0000\u0000\u0000\u0000The potential neuroprotective effect of Boswellia serrata against 3-nitro propionic acid\u0000(3-NP)-induced Huntington's disease (HD) was examined at oral doses of 45 mg/kg, 90 mg/kg,\u0000and 180 mg/kg. In this study, HD was induced by 3-NP at a dose of 10 mg/kg in Wistar rats. The\u0000study used 56 Wistar rats (8 per group) for biochemical (inflammatory markers, acetylcholinesterase\u0000activity) and behavioural (elevated plus maze, Y-maze, open-field, tail suspension tests,\u0000etc.) assessments. Additionally, a histological examination of the brain was carried out. In addition,\u0000the analysis of Boswellia serrata extract was performed by different analytical techniques,\u0000like UV spectrophotometer, FTIR, and HPLC methods.\u0000\u0000\u0000\u0000In the brain, succinate dehydrogenase is a mitochondrial enzyme irreversibly inhibited\u0000by 3-NP. Administration of 3-NP resulted in HD with altered behavioural and motor changes\u0000in rats. Treatment with Boswellia serrata resulted in remarkable protection of rats against\u00003-NP-induced behaviour and motor deficits in a dose-dependent manner. Moreover, in rats\u0000administered with 3-NP, Boswellia serrata improved memory performance and lowered levels of\u0000inflammatory biomarkers. These results have also been supported by histopathological analysis.\u0000Acetyl-11-keto-p-boswellic acid was found to be the main active component of Boswellia serrata\u0000extract.\u0000\u0000\u0000\u0000Boswellia serrata at a dose of 180 mg/kg exhibited better protection compared to the\u0000other doses against HD induced by 3-NP. More detailed studies based on molecular targets are\u0000needed for the Boswellia serrata to transition from the bench to the bedside for use as an adjuvant\u0000in HD patients.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139616009","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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