Pub Date : 2023-08-10DOI: 10.2174/1573407219666230810094657
H. Jabbari
Glycosylamine play an important role in living organisms. Most plants store their chemical resources in the form of inactive glycosides, which are broken down and converted into sugar in the body of herbivores by hydrolyzing enzymes. Glycosylamine are obtained from the secondary metabolism of plants and consist of two parts. One part of it contains sugar like glucose and is inactive in most substances, and has a good effect on the solubility of the glycosylamine derivatives and its absorption and even its transfer from one organ to another. The therapeutic effect is related to the second part, which is called aglycan (or aglucan). Glycosylamine derivatives form a large group of valuable medicinal substances, which at the same time include some of the most dangerous and toxic substances in nature. These substances are present in many groups of flowering plants. Glycosides are made in different ways in different metabolic pathways. These materials have a complex and special chemical structure and leave special effects on the human body. Glycosylamine derivatives are called O-glycosid, N-glycosid, S-glycosid in terms of atoms coupling to anomeric carbon. Carbohydrate esterification reaction to prepare new glycosylamine derivatives is one of the most important carbohydrate reactions. The anomeric position of carbohydrates with strong leaving groups is very important for the preparation of glycosides. Preparation of glycosylamine derivatives based on acetylated carbohydrates is the main purpose of this article. Different carbohydrates were acetylated under mild conditions and high yields. The anomeric position was deacetylated by a magnesium oxide heterogeneous catalyst in methanol solvent. In order to prepare new glycosides acetylated/ deacytylated carbohydrate reacted with N-Methyl-(naphtha-2- ylmethoxy)amine. The final product was identified by various spectroscopic methods. Anhydrous sodium acetate (4 g) and α-D-glucose (28 mg, 5 g) were mixed. The mixture was transferred to a 200 ml Round-bottom flask . Acetic acid (260 mg, 25 ml) was added to the reaction mixture. The reaction mixture was heated in a boiling water bath for 2 h until complete dissolution of the glucose. Then 100 ml of ice was added. After 1 hour, White crystals formed and were washed with cold water. And then 1 mol of glucose pentaacetate per 50 ml of methanol was dissolved by a magnetic stirrer. After thatMgO (0.2gr) was added to the reaction mixture. The reaction mixture was refluxed at room temperature within 4-5 hours. After 5 hours, the solvent was removed and separated by chromatography. It is then washed with hexane and crystallized by etherhexane. And the final step reacted with N-Methyl- (naphtha-2-ylmethoxy) amine in order to prepare new glycosylamine derivatives. Magnesium oxide in methanol solvent is one of the best effective catalysts in the deacetylation of the anomer position of acetylated carbohydrates. It is done under ambient temperature and in very easy
{"title":"Synthesis of New Glycosylamine Derivatives based on Carbohydrates","authors":"H. Jabbari","doi":"10.2174/1573407219666230810094657","DOIUrl":"https://doi.org/10.2174/1573407219666230810094657","url":null,"abstract":"\u0000\u0000Glycosylamine play an important role in living organisms. Most plants\u0000store their chemical resources in the form of inactive glycosides, which are broken down and\u0000converted into sugar in the body of herbivores by hydrolyzing enzymes. Glycosylamine are\u0000obtained from the secondary metabolism of plants and consist of two parts. One part of it contains\u0000sugar like glucose and is inactive in most substances, and has a good effect on the solubility of the\u0000glycosylamine derivatives and its absorption and even its transfer from one organ to another. The\u0000therapeutic effect is related to the second part, which is called aglycan (or aglucan). Glycosylamine\u0000derivatives form a large group of valuable medicinal substances, which at the same time include\u0000some of the most dangerous and toxic substances in nature. These substances are present in many\u0000groups of flowering plants. Glycosides are made in different ways in different metabolic pathways.\u0000These materials have a complex and special chemical structure and leave special effects on the\u0000human body. Glycosylamine derivatives are called O-glycosid, N-glycosid, S-glycosid in terms of\u0000atoms coupling to anomeric carbon. Carbohydrate esterification reaction to prepare new glycosylamine derivatives is one of the most important carbohydrate reactions. The anomeric position of\u0000carbohydrates with strong leaving groups is very important for the preparation of glycosides.\u0000Preparation of glycosylamine derivatives based on acetylated carbohydrates is the main purpose of this\u0000article. Different carbohydrates were acetylated under mild conditions and high yields. The anomeric\u0000position was deacetylated by a magnesium oxide heterogeneous catalyst in methanol solvent. In order\u0000to prepare new glycosides acetylated/ deacytylated carbohydrate reacted with N-Methyl-(naphtha-2-\u0000ylmethoxy)amine. The final product was identified by various spectroscopic methods.\u0000\u0000\u0000\u0000Anhydrous sodium acetate (4 g) and α-D-glucose (28 mg, 5 g) were mixed. The mixture\u0000was transferred to a 200 ml Round-bottom flask . Acetic acid (260 mg, 25 ml) was added to the\u0000reaction mixture. The reaction mixture was heated in a boiling water bath for 2 h until complete\u0000dissolution of the glucose. Then 100 ml of ice was added. After 1 hour, White crystals formed and\u0000were washed with cold water. And then 1 mol of glucose pentaacetate per 50 ml of methanol was\u0000dissolved by a magnetic stirrer. After thatMgO (0.2gr) was added to the reaction mixture. The\u0000reaction mixture was refluxed at room temperature within 4-5 hours. After 5 hours, the solvent was\u0000removed and separated by chromatography. It is then washed with hexane and crystallized by etherhexane. And the final step reacted with N-Methyl- (naphtha-2-ylmethoxy) amine in order to prepare\u0000new glycosylamine derivatives.\u0000\u0000\u0000\u0000Magnesium oxide in methanol solvent is one of the best effective catalysts in the\u0000deacetylation of the anomer position of acetylated carbohydrates. It is done under ambient temperature\u0000and in very easy","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41407933","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 : 2023-08-10DOI: 10.2174/1573407219666230810094839
F. Muneesa M, Y. Bhandary
Curcumin, a polyphenol compound, is reported to exhibit ameliorative effects in acute lung injury and different organ fibrosis models. We have previously demonstrated that curcumin, at a dose of 75 mg/kg, could modulate inflammatory mediators and fibrinolytic system proteins in the inflammatory stage as well as fibroproliferative stage in a mouse model of bleomycin (BLM) induced pulmonary fibrosis. In this study, we investigated the efficacy of the same dose of curcumin in resolving the established fibrotic stage in a mouse model of BLM-induced pulmonary fibrosis. We prepared the fibrosis model by intranasal administration of BLM (2 mg/kg). Curcumin intervention was performed by intraperitoneal injection on 16th to 20th days post BLM exposure. The control group was administered with normal saline. The mice were sacrificed on the 21st day post BLM exposure. Histological analysis of the lung tissue samples indicated that curcumin (75 mg/kg) could not reverse the fibrotic features induced by BLM. We also performed RT-PCR and western blot to examine the molecular changes induced by BLM and curcumin. It was observed that curcumin could neither reduce the expressions of fibrotic markers nor restore the normal expressions of proteins in the fibrinolytic system. Our data suggest that a low dose of curcumin is not effective in ameliorating the fibrotic stage of BLM-induced pulmonary fibrosis. An increased dose or a formulation that increases the bioavailability of curcumin could probably exhibit promising effects against pulmonary fibrosis in the future.
{"title":"The Inefficiency of Low-concentration Curcumin Intervention in Ameliorating\u0000Chronic-stage Pulmonary Fibrosis","authors":"F. Muneesa M, Y. Bhandary","doi":"10.2174/1573407219666230810094839","DOIUrl":"https://doi.org/10.2174/1573407219666230810094839","url":null,"abstract":"\u0000\u0000Curcumin, a polyphenol compound, is reported to exhibit ameliorative\u0000effects in acute lung injury and different organ fibrosis models. We have previously demonstrated\u0000that curcumin, at a dose of 75 mg/kg, could modulate inflammatory mediators and fibrinolytic system proteins in the inflammatory stage as well as fibroproliferative stage in a mouse model of bleomycin (BLM) induced pulmonary fibrosis. In this study, we investigated the efficacy of the same\u0000dose of curcumin in resolving the established fibrotic stage in a mouse model of BLM-induced\u0000pulmonary fibrosis.\u0000\u0000\u0000\u0000We prepared the fibrosis model by intranasal administration of BLM (2 mg/kg). Curcumin intervention was performed by intraperitoneal injection on 16th to 20th days post BLM exposure. The control group was administered with normal saline. The mice were sacrificed on the 21st\u0000day post BLM exposure.\u0000\u0000\u0000\u0000Histological analysis of the lung tissue samples indicated that curcumin (75 mg/kg) could\u0000not reverse the fibrotic features induced by BLM. We also performed RT-PCR and western blot to\u0000examine the molecular changes induced by BLM and curcumin. It was observed that curcumin\u0000could neither reduce the expressions of fibrotic markers nor restore the normal expressions of proteins in the fibrinolytic system.\u0000\u0000\u0000\u0000Our data suggest that a low dose of curcumin is not effective in ameliorating the fibrotic stage of BLM-induced pulmonary fibrosis. An increased dose or a formulation that increases\u0000the bioavailability of curcumin could probably exhibit promising effects against pulmonary fibrosis\u0000in the future.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45879288","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 : 2023-08-07DOI: 10.2174/1573407219666230807150426
Swati Wadhawan, Vishal Kumar Biswkarma, A. Chaudhary, Priya Masand
Alzheimer’s disease (AD) is the most common neurodegenerative and progressive disorder that results in damage to memory and alters thinking and behavior, which represent critical problems the world’s aging population is faced with. Clinical symptoms of AD include cognitive decline, loss of memory, emotional and behavioral changes, loss of motor coordination, and mental impairments. Yet, neither a universally accepted diagnosis with respect to its pathogenesis nor an ideal therapy is available for the management of AD. The existing drugs cause many complications and adverse effects. Herbal drugs, supported by an abundance of traditional knowledge, may fulfill the need as they can target the pathogenesis of AD at various destinations, both at the cellular and molecular levels. In recent years, herbal drugs and formulations have been evaluated in preclinical setups, especially involving rat and mouse models of AD, which have shown their memoryenhancing, neuroprotective, and antioxidant activities. Several herbal drugs and phytochemicals have been evaluated for their effectiveness as antioxidative agents to prevent the occurrence of oxidative stress and ROS formation during AD pathogenesis and exhibit antiapoptotic properties by downregulating caspase-3, DNA fragmentation, NF-κB, interleukin-1 β (IL1β), and TNF levels. In this paper, we have primarily reviewed herbal remedies that have been recently evaluated as alternative treatments for AD in a preclinical setup, and discussed the role of herbal medicines in the management of AD and advances in their knowledge.
阿尔茨海默病(AD)是一种最常见的神经退行性和进行性疾病，它会导致记忆损伤，改变思维和行为，这是世界人口老龄化面临的关键问题。阿尔茨海默病的临床症状包括认知能力下降、记忆丧失、情绪和行为改变、运动协调能力丧失和精神障碍。然而，对于阿尔茨海默病的发病机制，既没有普遍接受的诊断，也没有理想的治疗方法。现有的药物引起许多并发症和不良反应。在丰富的传统知识的支持下，草药可能会满足这一需求，因为它们可以在细胞和分子水平上针对阿尔茨海默病的发病机制。近年来，草药及其制剂已在临床前研究中进行了评估，特别是在大鼠和小鼠AD模型中，显示出其增强记忆、神经保护和抗氧化活性。一些草药和植物化学物质已被评估其作为抗氧化剂的有效性，以防止AD发病过程中氧化应激的发生和ROS的形成，并通过下调caspase-3、DNA片段化、NF-κB、白细胞介素-1 β (il -1 β)和TNF水平表现出抗凋亡特性。在本文中，我们主要回顾了最近被评估为阿尔茨海默病临床前替代治疗方法的草药，并讨论了草药在阿尔茨海默病管理中的作用及其知识进展。
{"title":"A Critical Review Based on Preclinical Studies of Medicinal Plants for the\u0000Management of Alzheimer’s Disease","authors":"Swati Wadhawan, Vishal Kumar Biswkarma, A. Chaudhary, Priya Masand","doi":"10.2174/1573407219666230807150426","DOIUrl":"https://doi.org/10.2174/1573407219666230807150426","url":null,"abstract":"\u0000\u0000Alzheimer’s disease (AD) is the most common neurodegenerative and progressive disorder that results in damage to memory and alters thinking and behavior, which represent critical\u0000problems the world’s aging population is faced with. Clinical symptoms of AD include cognitive\u0000decline, loss of memory, emotional and behavioral changes, loss of motor coordination, and mental\u0000impairments. Yet, neither a universally accepted diagnosis with respect to its pathogenesis nor an\u0000ideal therapy is available for the management of AD. The existing drugs cause many complications\u0000and adverse effects. Herbal drugs, supported by an abundance of traditional knowledge, may fulfill\u0000the need as they can target the pathogenesis of AD at various destinations, both at the cellular and\u0000molecular levels. In recent years, herbal drugs and formulations have been evaluated in preclinical\u0000setups, especially involving rat and mouse models of AD, which have shown their memoryenhancing, neuroprotective, and antioxidant activities. Several herbal drugs and phytochemicals\u0000have been evaluated for their effectiveness as antioxidative agents to prevent the occurrence of oxidative stress and ROS formation during AD pathogenesis and exhibit antiapoptotic properties by\u0000downregulating caspase-3, DNA fragmentation, NF-κB, interleukin-1 β (IL1β), and TNF levels. In\u0000this paper, we have primarily reviewed herbal remedies that have been recently evaluated as alternative treatments for AD in a preclinical setup, and discussed the role of herbal medicines in the\u0000management of AD and advances in their knowledge.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47555651","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 : 2023-08-07DOI: 10.2174/1573407219666230807150030
Sonia Singh, Bhupesh C. Semwal, Himanshu Sharma, D. Sharma
Inflammation is a part of the biological response of body tissues against harmful stimuli, such as damaged cells, pathogens, irradiations, and toxic compounds. Numerous treatments, including anti-inflammatory drugs that treat the condition of inflammation, are available for its management. Because of the severe adverse effects associated with synthetic medications, phytotherapy may be a promising and effective approach to treating inflammation. The therapeutic potential of herbs is due to their capacity to target a variety of inflammatory mediators, including chemokines, cytokines, nitric oxide, lipoxygenase, nuclear factor kappa-B, and arachidonic acid. Furthermore, nanomedicine may be a valuable and effective formulation approach for overcoming the drawbacks of phytoconstituents, such as their low bioavailability, high first-pass metabolism, and poor stability. The current manuscript provides a thorough description of many phytoconstituents and herbal plants that have great potential for treating inflammation-related diseases, as well as information on their limitations, drug formulations, and regulatory issues.
{"title":"Impact of Phytomolecules with Nanotechnology on the Treatment of\u0000Inflammation","authors":"Sonia Singh, Bhupesh C. Semwal, Himanshu Sharma, D. Sharma","doi":"10.2174/1573407219666230807150030","DOIUrl":"https://doi.org/10.2174/1573407219666230807150030","url":null,"abstract":"\u0000\u0000Inflammation is a part of the biological response of body tissues against harmful stimuli,\u0000such as damaged cells, pathogens, irradiations, and toxic compounds. Numerous treatments, including anti-inflammatory drugs that treat the condition of inflammation, are available for its management. Because of the severe adverse effects associated with synthetic medications, phytotherapy\u0000may be a promising and effective approach to treating inflammation. The therapeutic potential of\u0000herbs is due to their capacity to target a variety of inflammatory mediators, including chemokines,\u0000cytokines, nitric oxide, lipoxygenase, nuclear factor kappa-B, and arachidonic acid. Furthermore,\u0000nanomedicine may be a valuable and effective formulation approach for overcoming the drawbacks\u0000of phytoconstituents, such as their low bioavailability, high first-pass metabolism, and poor stability. The current manuscript provides a thorough description of many phytoconstituents and herbal\u0000plants that have great potential for treating inflammation-related diseases, as well as information on\u0000their limitations, drug formulations, and regulatory issues.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47741183","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 : 2023-07-26DOI: 10.2174/1573407219666230726164538
H. Tuli, D. Aggarwal, M. Chaudhary, Nandini Bajaj, Deepika Sharma, S. Upadhyay, V. Garg, H. Abdulabbas, Isha Rani
Curcumin is a natural compound obtained from Curcuma longa that possesses a vast therapeutic potential for disease treatment. It is a potent anticancer, anti-inflammatory, antioxidant, and anti-aging phytochemical as evident from numerous studies. Curcumin's anti-inflammatory and antioxidant properties are thought to be more potent than its other biological actions. Curcumin's anti-inflammatory properties can lead to an improvement in symptoms and make it a viable candidate for the treatment and prevention of pro-inflammatory disorders. The goal of this review is to analyse curcumin's anti-inflammatory properties and mechanisms in the treatment of various disorders. The effect of different curcumin-based nanoformulations on anti-inflammatory potential is also reviewed, as the therapeutic use of curcumin is influenced by its solubility, bioavailability, and pharmacokinetic profile. The literature searched during the last ten years using keywords such as curcumin, anti-inflammatory mechanisms, cytokines, and nanoformulations from multiple databases, such as PubMed, Science Direct, Scopus, and others. The quality research and review articles containing the aforementioned keywords were chosen for this review article. This review focuses on the anti-inflammatory properties of curcumin against a variety of inflammatory disorders that arise over the course of various illnesses. It also emphasises the importance of developing alternative nanoformulations to address the limitations of curcumin usage. Further, it will aid the scientific community's understanding of curcumin and its anti-inflammatory mechanisms, prompting them to devise innovative treatment options.
{"title":"Anti-Inflammatory Potential of Curcumin: From Chemistry and Mechanistic Insight to Nanoformulations","authors":"H. Tuli, D. Aggarwal, M. Chaudhary, Nandini Bajaj, Deepika Sharma, S. Upadhyay, V. Garg, H. Abdulabbas, Isha Rani","doi":"10.2174/1573407219666230726164538","DOIUrl":"https://doi.org/10.2174/1573407219666230726164538","url":null,"abstract":"\u0000\u0000Curcumin is a natural compound obtained from Curcuma longa that possesses a vast therapeutic potential for disease treatment. It is a potent anticancer, anti-inflammatory, antioxidant, and anti-aging phytochemical as evident from numerous studies. Curcumin's anti-inflammatory and antioxidant properties are thought to be more potent than its other biological actions. Curcumin's anti-inflammatory properties can lead to an improvement in symptoms and make it a viable candidate for the treatment and prevention of pro-inflammatory disorders.\u0000\u0000\u0000\u0000The goal of this review is to analyse curcumin's anti-inflammatory properties and mechanisms in the treatment of various disorders. The effect of different curcumin-based nanoformulations on anti-inflammatory potential is also reviewed, as the therapeutic use of curcumin is influenced by its solubility, bioavailability, and pharmacokinetic profile.\u0000\u0000\u0000\u0000The literature searched during the last ten years using keywords such as curcumin, anti-inflammatory mechanisms, cytokines, and nanoformulations from multiple databases, such as PubMed, Science Direct, Scopus, and others. The quality research and review articles containing the aforementioned keywords were chosen for this review article.\u0000\u0000\u0000\u0000This review focuses on the anti-inflammatory properties of curcumin against a variety of inflammatory disorders that arise over the course of various illnesses. It also emphasises the importance of developing alternative nanoformulations to address the limitations of curcumin usage. Further, it will aid the scientific community's understanding of curcumin and its anti-inflammatory mechanisms, prompting them to devise innovative treatment options.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49132602","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 : 2023-07-20DOI: 10.2174/1573407219666230720103734
A. Adhikari, D. Shrestha, Sushma Thapa, Tamlal Pokhrel, Bishnu Bahadur Sinjali, J. Baral
The use of medicinal plants as supplemental or alternative medicine is widespread around the world. For the development of new drugs, studies on these medicinal plants that include pharmacological and toxicological assessments are crucial. This work aimed to find the total phenolic and flavonoid content, antioxidant, antibacterial, and antidiabetic potential of the traditionally used medicinal plant Mimosa rubicaulis Lam. The in vitro antidiabetic potential of methanolic extract and its fractions of the roots of M. rubicaulis were performed via enzyme (α-glucosidase and α-amylase) inhibition assays. Antioxidant and anti-inflammatory activities were carried out using 2,2 Diphenyl-1-picrylhydrazyl (DPPH), and reactive oxygen species (ROS) inhibiting methods. Well diffusion method is applied for antibacterial activity. Autodock vina was used for molecular docking. The crude extract reported the highest inhibition activity against α-glucosidase with an IC50 value of 10.29 ± 0.35 μg/mL compared to the standard acarbose IC50 value of 5.653 ± 0.29 µg/mL. Similarly, the ethyl acetate (EA) fraction disclosed significant inhibition against α-amylase with an IC50 value of 108.7 ± 0.66 μg/mL compared to the standard drug’s IC50 value of 6.01 ± 0.14 µg/mL. Likewise, the EA fraction showed the maximum antioxidant activity with an IC50 value of 11.89 ± 1.05μg/mL among the crude extract and its fractions. Mimosa rubicaulis was found to have α-glucosidase and α-amylase inhibition, anti-inflammatory, and antibacterial activity. To the best of our knowledge, this is the first report of α-glucosidase and α-amylase inhibition activity of this plant. Further studies on this plant are required to isolate potent compounds.
{"title":"Antioxidant, Antibacterial, α-Amylase, and α-Glucosidase Inhibition, and Anti-inflammatory Activities of Mimosa rubicaulis Lam","authors":"A. Adhikari, D. Shrestha, Sushma Thapa, Tamlal Pokhrel, Bishnu Bahadur Sinjali, J. Baral","doi":"10.2174/1573407219666230720103734","DOIUrl":"https://doi.org/10.2174/1573407219666230720103734","url":null,"abstract":"\u0000\u0000The use of medicinal plants as supplemental or alternative medicine is widespread around the world. For the development of new drugs, studies on these medicinal plants that include pharmacological and toxicological assessments are crucial.\u0000\u0000\u0000\u0000This work aimed to find the total phenolic and flavonoid content, antioxidant, antibacterial, and antidiabetic potential of the traditionally used medicinal plant Mimosa rubicaulis Lam.\u0000\u0000\u0000\u0000The in vitro antidiabetic potential of methanolic extract and its fractions of the roots of M. rubicaulis were performed via enzyme (α-glucosidase and α-amylase) inhibition assays. Antioxidant and anti-inflammatory activities were carried out using 2,2 Diphenyl-1-picrylhydrazyl (DPPH), and reactive oxygen species (ROS) inhibiting methods. Well diffusion method is applied for antibacterial activity. Autodock vina was used for molecular docking.\u0000\u0000\u0000\u0000The crude extract reported the highest inhibition activity against α-glucosidase with an IC50 value of 10.29 ± 0.35 μg/mL compared to the standard acarbose IC50 value of 5.653 ± 0.29 µg/mL. Similarly, the ethyl acetate (EA) fraction disclosed significant inhibition against α-amylase with an IC50 value of 108.7 ± 0.66 μg/mL compared to the standard drug’s IC50 value of 6.01 ± 0.14 µg/mL. Likewise, the EA fraction showed the maximum antioxidant activity with an IC50 value of 11.89 ± 1.05μg/mL among the crude extract and its fractions.\u0000\u0000\u0000\u0000Mimosa rubicaulis was found to have α-glucosidase and α-amylase inhibition, anti-inflammatory, and antibacterial activity. To the best of our knowledge, this is the first report of α-glucosidase and α-amylase inhibition activity of this plant. Further studies on this plant are required to isolate potent compounds.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43426010","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 : 2023-07-18DOI: 10.2174/1573407219666230718125630
R. Kebbab, Aida basseddik, Walid Boussebaa, E. Nabti, K. Houali
In recent years, medicinal plants have received considerable attention due to the search for novel bioactive compounds. In this optic, we have been interested in Artemisia judaica subsp. Sahariensis, a Saharan species widely used in phytotherapy by the Tuaregs of the Ahaggar. This study aims to evaluate and optimize the biological activities of this plant in order to valorize its bioactive compounds. For this purpose, an extraction with methanol (70%) was carried out, then a liquid-liquid fractionation, using solvents with increasing polarity: diethyl ether, ethyl acetate, n-butanol and water. We realized an analysis of phenols, flavonoids and evaluation of antioxidant and antimicrobial activities in addition to the UPLC-ESI-MS/MS analysis of the fractions. The reducing effect was proportional to the solvent polarity. The crude extract gave the best reducing power (17.55±3.06µg/mL), better phenols and flavonoids contents (20.35±0.5 mgGAE/gTDM), (10.35±0.56 mgGAE/gTDM) respectively compared to its fractions. The DPPH (2,2-Diphenyl-1-Picrylhydrazyl) radical scavenging assay showed that the ethyl acetate fraction was the most active with the lowest IC50 value (inhibitory concentration to 50% of DPPH) (41.43±0.24 µg/ml) followed by n-butanol (58.53±0.20 µg/mL), diethyl ether (135.07±6.18 µg/mL) and aqueous (226.41±1.51 µg/mL) fractions (p<0.0001). Moreover, hydromethanolic extract gave an IC50 value of 114.05±3.37 µg/mL. The antimicrobial effect was observed on all clinical multi-resistant bacteria tested except Klebsiella pneumoniae, which was resistant. The most important effect was observed by the ethyl acetate fraction against the fungal strain Candida albicans. Various phenolic acids and flavonoids (flavones, flavonols, flavanones) were detected and could be responsible for these bioactivities. We can conclude that liquid-liquid extraction with solvents of increasing polarity plays a major role in optimizing the biological activity of this plant, which contains polyphenols and can therefore be valued as a source of natural antioxidants and antimicrobials.
{"title":"Optimization of Antioxidant and Antimicrobial Activities by Fractionation of Artemisia judaica subsp. sahariensis Crude Extract from Ahaggar (Algerian Arid Region): UPLC-ESI-MS/MS Analysis of Fractions","authors":"R. Kebbab, Aida basseddik, Walid Boussebaa, E. Nabti, K. Houali","doi":"10.2174/1573407219666230718125630","DOIUrl":"https://doi.org/10.2174/1573407219666230718125630","url":null,"abstract":"\u0000\u0000In recent years, medicinal plants have received considerable attention due to the search for novel bioactive compounds. In this optic, we have been interested in Artemisia judaica subsp. Sahariensis, a Saharan species widely used in phytotherapy by the Tuaregs of the Ahaggar.\u0000\u0000\u0000\u0000This study aims to evaluate and optimize the biological activities of this plant in order to valorize its bioactive compounds.\u0000\u0000\u0000\u0000For this purpose, an extraction with methanol (70%) was carried out, then a liquid-liquid fractionation, using solvents with increasing polarity: diethyl ether, ethyl acetate, n-butanol and water. We realized an analysis of phenols, flavonoids and evaluation of antioxidant and antimicrobial activities in addition to the UPLC-ESI-MS/MS analysis of the fractions.\u0000\u0000\u0000\u0000The reducing effect was proportional to the solvent polarity. The crude extract gave the best reducing power (17.55±3.06µg/mL), better phenols and flavonoids contents (20.35±0.5 mgGAE/gTDM), (10.35±0.56 mgGAE/gTDM) respectively compared to its fractions. The DPPH (2,2-Diphenyl-1-Picrylhydrazyl) radical scavenging assay showed that the ethyl acetate fraction was the most active with the lowest IC50 value (inhibitory concentration to 50% of DPPH) (41.43±0.24 µg/ml) followed by n-butanol (58.53±0.20 µg/mL), diethyl ether (135.07±6.18 µg/mL) and aqueous (226.41±1.51 µg/mL) fractions (p<0.0001). Moreover, hydromethanolic extract gave an IC50 value of 114.05±3.37 µg/mL. The antimicrobial effect was observed on all clinical multi-resistant bacteria tested except Klebsiella pneumoniae, which was resistant. The most important effect was observed by the ethyl acetate fraction against the fungal strain Candida albicans. Various phenolic acids and flavonoids (flavones, flavonols, flavanones) were detected and could be responsible for these bioactivities.\u0000\u0000\u0000\u0000We can conclude that liquid-liquid extraction with solvents of increasing polarity plays a major role in optimizing the biological activity of this plant, which contains polyphenols and can therefore be valued as a source of natural antioxidants and antimicrobials.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49507240","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 : 2023-07-18DOI: 10.2174/1573407219666230718105347
B. Chopra, N. Saini, Ashwani Kumar Dhingra
Piperazine is the heterocyclic nucleus and exhibits significant biological potential such as antipsychotic, antidepressant, antihistamine, anticancer, anti-anginal, cardioprotective, antiviral, and anti-inflammatory activity. As a result, it had been considered a crucial structural component in the majority of the therapeutic medications that were already on the market. Other issues that limit its use include solubility, limited bioavailability, cost-effectiveness, and a mismatch between the drug's pharmacokinetic and pharmacodynamic profiles. Literature describes structural modification in the piperazine moiety to create novel derivatives or analogues to solve the issues with currently marketed medications. Nature provides various bioactive components having piperazine nuclei in their core structure. The present review describes the potential of the piperazine nucleus present in natural bioactive components. So the study concludes that it is vital to concentrate on the structural characteristics of this scaffold, which opens the way for future research and may benefit pharmaceutical companies as well as medicinal chemists.
{"title":"A profound insight into the structural modification of natural bioactive compounds containing piperazine moiety: a comprehensive review..","authors":"B. Chopra, N. Saini, Ashwani Kumar Dhingra","doi":"10.2174/1573407219666230718105347","DOIUrl":"https://doi.org/10.2174/1573407219666230718105347","url":null,"abstract":"\u0000\u0000Piperazine is the heterocyclic nucleus and exhibits significant biological potential such as antipsychotic, antidepressant, antihistamine, anticancer, anti-anginal, cardioprotective, antiviral, and anti-inflammatory activity. As a result, it had been considered a crucial structural component in the majority of the therapeutic medications that were already on the market. Other issues that limit its use include solubility, limited bioavailability, cost-effectiveness, and a mismatch between the drug's pharmacokinetic and pharmacodynamic profiles. Literature describes structural modification in the piperazine moiety to create novel derivatives or analogues to solve the issues with currently marketed medications. Nature provides various bioactive components having piperazine nuclei in their core structure. The present review describes the potential of the piperazine nucleus present in natural bioactive components. So the study concludes that it is vital to concentrate on the structural characteristics of this scaffold, which opens the way for future research and may benefit pharmaceutical companies as well as medicinal chemists.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44001340","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 : 2023-07-06DOI: 10.2174/1573407219666230706145617
O. Onaolapo, A. Olofinnade, A. Onaolapo
Several concerns regarding the safety of sodium benzoate/ascorbic acid combination have been highlighted in various scientific investigations. However, there is a dearth of scientific literature on its effect on the brain. This study investigated the effects of dry-feed added sodium benzoate/ascorbic acid combination on neurobehaviour, oxidative stress, and inflammatory cytokines in mice Adult male mice were assigned into ten groups of 10 mice each. One group was fed a standard diet, three groups were fed a diet containing sodium benzoate (NaB) at 125 mg/kg with ascorbic acid (AA) at 100, 200, or 300 mg/kg of feed, another three groups were fed NaB at 250 mg/kg with AA at 100, 200, or 300 mg/kg of feed, respectively, and the last three groups were fed NaB at 500 mg/kg with AA at 100, 200 or 300 mg/kg, respectively. Behavioural tests were assessed, following which animals were sacrificed, and their brains were homogenised for the assessment of biochemical parameters. The result showed a decrease in body weight, self-grooming, total antioxidant capacity, inflammatory cytokines, mixed response with food intake, locomotor activity, Y maze spatial working memory, and anxiety-related behaviours and an increase in rearing and radial arm maze spatial working memory. Dry-feed added NaB/AA altered behavioural, oxidative stress, and inflammatory markers in mice. It was found that both beneficial and deleterious effects might be possible, depending on the concentrations ingested in food. However, further investigations are required to ascertain its effects on humans.
{"title":"Graded Effects of Dry-Feed Added Sodium Benzoate/Ascorbic Acid Combination on Neurobehaviour, Oxidative Stress, and Markers of Inflammation in Mice","authors":"O. Onaolapo, A. Olofinnade, A. Onaolapo","doi":"10.2174/1573407219666230706145617","DOIUrl":"https://doi.org/10.2174/1573407219666230706145617","url":null,"abstract":"\u0000\u0000Several concerns regarding the safety of sodium benzoate/ascorbic acid combination have been highlighted in various scientific investigations. However, there is a dearth of scientific literature on its effect on the brain. This study investigated the effects of dry-feed added sodium benzoate/ascorbic acid combination on neurobehaviour, oxidative stress, and inflammatory cytokines in mice\u0000\u0000\u0000\u0000Adult male mice were assigned into ten groups of 10 mice each. One group was fed a standard diet, three groups were fed a diet containing sodium benzoate (NaB) at 125 mg/kg with ascorbic acid (AA) at 100, 200, or 300 mg/kg of feed, another three groups were fed NaB at 250 mg/kg with AA at 100, 200, or 300 mg/kg of feed, respectively, and the last three groups were fed NaB at 500 mg/kg with AA at 100, 200 or 300 mg/kg, respectively. Behavioural tests were assessed, following which animals were sacrificed, and their brains were homogenised for the assessment of biochemical parameters.\u0000\u0000\u0000\u0000The result showed a decrease in body weight, self-grooming, total antioxidant capacity, inflammatory cytokines, mixed response with food intake, locomotor activity, Y maze spatial working memory, and anxiety-related behaviours and an increase in rearing and radial arm maze spatial working memory.\u0000\u0000\u0000\u0000Dry-feed added NaB/AA altered behavioural, oxidative stress, and inflammatory markers in mice. It was found that both beneficial and deleterious effects might be possible, depending on the concentrations ingested in food. However, further investigations are required to ascertain its effects on humans.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43475808","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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