Pub Date : 2023-10-25DOI: 10.2174/0115734072265828231010050909
Navin B. Patel, Pratik N. Maisuria, Akash V. Gujarati, Divyesh K. Patel
Background: One of the most crucial heterocycles is piperazine for the creation of novel medication candidates with a variety of medicinal applications. The piperazine moiety is a cyclic compound with four carbon atoms and two nitrogen atoms in positions 1 and 4. Objective: The objective of this studty is the development of 1-((3,4-dimethoxyphenyl) (substitutedphenyl) substituted -piperazine (A1-A10) analogs via the one-pot synthesis method and evaluation for their preliminary antibacterial, antifungal, antimycobacterial, antioxidant, and antimalarial activity. Methods: Desired piperazine derivatives were obtained in a single step reaction using piperazine, aldehydes, and boronic acid derivatives. The structures of all newly synthesized compounds have been established based on analytical and spectral data. An in silico molecular docking study was carried out for the series. Results: The spectral data using IR, 1 H NMR, and 13C NMR and mass spectra confirmed the structure of the synthesized compounds. Compounds A6 and A10 were found to be the most promising agents for antimalarial activity. A1-A10 showed a higher IC50 value and found less antioxidant activity. Some of the compounds showed higher potency when compared to the standard drugs in this antimicrobial study. Conclusion: The structure-activity study showed that changes in substituents either on aldehyde, piperazine, or boronic acid derivatives can lead to potential active compounds. These facts make the compounds interesting candidates for further evaluation of their efficacy in the treatment of microbial, tubercular and malarial diseases.
{"title":"Synthesis of Piperazine-containing Derivatives and their Antimicrobial, Antimycobacterial, Antimalarial and Antioxidant Activities","authors":"Navin B. Patel, Pratik N. Maisuria, Akash V. Gujarati, Divyesh K. Patel","doi":"10.2174/0115734072265828231010050909","DOIUrl":"https://doi.org/10.2174/0115734072265828231010050909","url":null,"abstract":"Background: One of the most crucial heterocycles is piperazine for the creation of novel medication candidates with a variety of medicinal applications. The piperazine moiety is a cyclic compound with four carbon atoms and two nitrogen atoms in positions 1 and 4. Objective: The objective of this studty is the development of 1-((3,4-dimethoxyphenyl) (substitutedphenyl) substituted -piperazine (A1-A10) analogs via the one-pot synthesis method and evaluation for their preliminary antibacterial, antifungal, antimycobacterial, antioxidant, and antimalarial activity. Methods: Desired piperazine derivatives were obtained in a single step reaction using piperazine, aldehydes, and boronic acid derivatives. The structures of all newly synthesized compounds have been established based on analytical and spectral data. An in silico molecular docking study was carried out for the series. Results: The spectral data using IR, 1 H NMR, and 13C NMR and mass spectra confirmed the structure of the synthesized compounds. Compounds A6 and A10 were found to be the most promising agents for antimalarial activity. A1-A10 showed a higher IC50 value and found less antioxidant activity. Some of the compounds showed higher potency when compared to the standard drugs in this antimicrobial study. Conclusion: The structure-activity study showed that changes in substituents either on aldehyde, piperazine, or boronic acid derivatives can lead to potential active compounds. These facts make the compounds interesting candidates for further evaluation of their efficacy in the treatment of microbial, tubercular and malarial diseases.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"48 3-4","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135112947","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}
Abstract: The existence of the blood-brain barrier (BBB), a densely woven network of blood vessels and endothelial cells designed to prevent the infiltration of foreign substances into the brain, the methods employed in developing treatments for neurodegenerative disorders (NDs) such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Multiple sclerosis, Amyotrophic lateral sclerosis, and others, pose significant challenges and complexities. These illnesses have had a terrible impact on the human population's health. Because early detection of these problems is poor and no good therapy has been established, they have emerged as the biggest lifethreatening healthcare burden worldwide compared to other significant illnesses. Traditional drug delivery techniques do not offer efficient treatment for NDs due to constraints in the BBB design, efflux pumps, and metabolic enzyme expression. Nanotechnology has the potential to significantly enhance ND therapy by utilizing systems that have been bioengineered to engage with living organisms at the cellular range. Compared to traditional techniques, nanotechnological technologies have several potential ways for crossing the BBB and increasing therapeutic efficacy in the brain. The introduction and growth of nanotechnology indicate promising potential for overcoming this issue. Engineered nanoparticles coupled with therapeutic moieties and imaging agents with dimensions ranging from 1-100 nm can improve effectiveness, cellular uptake, selective transport, and drug delivery to the brain due to their changed physicochemical properties. Conjugates of nanoparticles and medicinal plants, or their constituents known as nano phytomedicine, have recently gained importance in developing cutting-edge neuro-therapeutics due to their abundant natural supply, promising targeted delivery to the brain, and lower potential for adverse effects. This study summarizes the common NDs, their prevalence and pathogenesis, and potential herbal nanoformulation for treating NDs.
{"title":"An Update on the Application of Nano Phytomedicine as an Emerging Therapeutic Tool for Neurodegenerative Diseases","authors":"Md Sadique Hussain, Varunesh Chaturvedi, Saloni Goyal, Sandeep Singh, Reyaz Hassan Mir","doi":"10.2174/0115734072258656231013085318","DOIUrl":"https://doi.org/10.2174/0115734072258656231013085318","url":null,"abstract":"Abstract: The existence of the blood-brain barrier (BBB), a densely woven network of blood vessels and endothelial cells designed to prevent the infiltration of foreign substances into the brain, the methods employed in developing treatments for neurodegenerative disorders (NDs) such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Multiple sclerosis, Amyotrophic lateral sclerosis, and others, pose significant challenges and complexities. These illnesses have had a terrible impact on the human population's health. Because early detection of these problems is poor and no good therapy has been established, they have emerged as the biggest lifethreatening healthcare burden worldwide compared to other significant illnesses. Traditional drug delivery techniques do not offer efficient treatment for NDs due to constraints in the BBB design, efflux pumps, and metabolic enzyme expression. Nanotechnology has the potential to significantly enhance ND therapy by utilizing systems that have been bioengineered to engage with living organisms at the cellular range. Compared to traditional techniques, nanotechnological technologies have several potential ways for crossing the BBB and increasing therapeutic efficacy in the brain. The introduction and growth of nanotechnology indicate promising potential for overcoming this issue. Engineered nanoparticles coupled with therapeutic moieties and imaging agents with dimensions ranging from 1-100 nm can improve effectiveness, cellular uptake, selective transport, and drug delivery to the brain due to their changed physicochemical properties. Conjugates of nanoparticles and medicinal plants, or their constituents known as nano phytomedicine, have recently gained importance in developing cutting-edge neuro-therapeutics due to their abundant natural supply, promising targeted delivery to the brain, and lower potential for adverse effects. This study summarizes the common NDs, their prevalence and pathogenesis, and potential herbal nanoformulation for treating NDs.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"60 8","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135113812","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 : 2023-10-25DOI: 10.2174/0115734072273072231017104102
Vladimir G. Kukes, Vladimir A. Furalyov, Albina А. Gazdanova, Olga K. Parfenova, Dmitry V. Grishin, Nikita G. Sidorov
Objective: To study the cytotoxic effect of palmitic acid on myoblasts in vitro and the influence of this toxicant on the expression of myostatin mRNA in myoblast culture. Methods: To research the protective action against these processes of a compound with antioxidant activity, for which 2-ethyl-6-methyl-3-hydroxypyridine malate (ethoxidol) was chosen. Results: Our studies have shown that palmitic acid has a noticeable cytostatic effect on myoblasts in vitro, significantly suppressing their proliferation: the rate of MTT recovery in myoblasts treated with palmitate was only 9.6% of that rate in control myoblasts. In experiments, it was shown that palmitic acid slightly activated the expression of myostatin mRNA. At the same time, the protective effect of 2-ethyl-6-methyl-3-hydroxypyridine malate was not so pronounced. Conclusion: The results of our research indicate that the activation of myostatin synthesis is not one of the main causes of the development of myodystrophy in obese people or people following a high-lipid diet, while the direct cytotoxic effect of palmitic acid on myoblasts is. It is obvious that the use of antioxidants such as ethoxide has a protective effect on myoblasts in the experiment and may have a certain potential in clinical practice.
{"title":"Study of the Effect of Palmitic Acid on the Expression of Myostatin mRNA and its Cytotoxic Properties in the Culture of Myoblast Cells and the Possibility of Exogenous Regulation","authors":"Vladimir G. Kukes, Vladimir A. Furalyov, Albina А. Gazdanova, Olga K. Parfenova, Dmitry V. Grishin, Nikita G. Sidorov","doi":"10.2174/0115734072273072231017104102","DOIUrl":"https://doi.org/10.2174/0115734072273072231017104102","url":null,"abstract":"Objective: To study the cytotoxic effect of palmitic acid on myoblasts in vitro and the influence of this toxicant on the expression of myostatin mRNA in myoblast culture. Methods: To research the protective action against these processes of a compound with antioxidant activity, for which 2-ethyl-6-methyl-3-hydroxypyridine malate (ethoxidol) was chosen. Results: Our studies have shown that palmitic acid has a noticeable cytostatic effect on myoblasts in vitro, significantly suppressing their proliferation: the rate of MTT recovery in myoblasts treated with palmitate was only 9.6% of that rate in control myoblasts. In experiments, it was shown that palmitic acid slightly activated the expression of myostatin mRNA. At the same time, the protective effect of 2-ethyl-6-methyl-3-hydroxypyridine malate was not so pronounced. Conclusion: The results of our research indicate that the activation of myostatin synthesis is not one of the main causes of the development of myodystrophy in obese people or people following a high-lipid diet, while the direct cytotoxic effect of palmitic acid on myoblasts is. It is obvious that the use of antioxidants such as ethoxide has a protective effect on myoblasts in the experiment and may have a certain potential in clinical practice.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"15 10","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135113692","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}
Background: Alzheimer’s disease (AD) is a complex neurodegenerative condition for which a single protein-targeting medication is not enough to provide a cure. All the medications now available for AD are palliative. FDA has approved five medications for the treatment of AD, i.e., tacrine, donepezil, galantamine, rivastigmine, and memantine. Due to hepatotoxicity, tacrine is no longer utilized in clinical practice. Due to the lack of therapeutic efficiency of single-target medications and the multifaceted etiology of AD, multitarget-directed ligands have been developed. Objectives: The present research focused on incorporating a flavone nucleus into the amino group of 9-amino acridine nucleus to make it an acetylcholinesterase (AChE) and butyryl cholinesterase inhibitor (BuChE) with less toxicity Methods: We designed and synthesized ten flavone-substituted acridine derivatives and evaluated them for in vitro AChE and BuChE inhibitory activity. Molecular modeling studies were conducted using AutoDock Vina with hAChE (PDB ID: 4EY7) and hBuChE (PDB ID: 4TPK). The toxicity profile of the most active novel compound tested on zebrafish larvae for determining the liver and cardiac toxicity and LD50 value of the compound were determined. Results: In vitro AChE and BuChE inhibitory study by Ellman assay showed acceptable results. The compound AF2 showed the highest activity with an IC50 value of 0.99 ± 0.1 µM for AChE and 1.78 ± 0.19 for BuChE. The in vivo acute toxicity studies conducted on zebra fish larvae did not show cardiac and hepatotoxicity, and the LD50 value was found to be 1000 µL Conclusion: The results highlighted the AChE and BuChE inhibitory effects of the novel acridine-flavone hybrids, and they can be promising multitarget-directed ligands for AD.
{"title":"Design, Synthesis, Evaluation, and Toxicity Studies of Novel Acridine Derivatives in Zebra Fish Larvae","authors":"Remya R.S, Ramalakshmi Natarajan, Nalini Nagarajan","doi":"10.2174/0115734072256561231008183612","DOIUrl":"https://doi.org/10.2174/0115734072256561231008183612","url":null,"abstract":"Background: Alzheimer’s disease (AD) is a complex neurodegenerative condition for which a single protein-targeting medication is not enough to provide a cure. All the medications now available for AD are palliative. FDA has approved five medications for the treatment of AD, i.e., tacrine, donepezil, galantamine, rivastigmine, and memantine. Due to hepatotoxicity, tacrine is no longer utilized in clinical practice. Due to the lack of therapeutic efficiency of single-target medications and the multifaceted etiology of AD, multitarget-directed ligands have been developed. Objectives: The present research focused on incorporating a flavone nucleus into the amino group of 9-amino acridine nucleus to make it an acetylcholinesterase (AChE) and butyryl cholinesterase inhibitor (BuChE) with less toxicity Methods: We designed and synthesized ten flavone-substituted acridine derivatives and evaluated them for in vitro AChE and BuChE inhibitory activity. Molecular modeling studies were conducted using AutoDock Vina with hAChE (PDB ID: 4EY7) and hBuChE (PDB ID: 4TPK). The toxicity profile of the most active novel compound tested on zebrafish larvae for determining the liver and cardiac toxicity and LD50 value of the compound were determined. Results: In vitro AChE and BuChE inhibitory study by Ellman assay showed acceptable results. The compound AF2 showed the highest activity with an IC50 value of 0.99 ± 0.1 µM for AChE and 1.78 ± 0.19 for BuChE. The in vivo acute toxicity studies conducted on zebra fish larvae did not show cardiac and hepatotoxicity, and the LD50 value was found to be 1000 µL Conclusion: The results highlighted the AChE and BuChE inhibitory effects of the novel acridine-flavone hybrids, and they can be promising multitarget-directed ligands for AD.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"26 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135619499","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 : 2023-10-11DOI: 10.2174/0115734072255749230928060834
Remya R.S, Barath R, Ruban R, Jaitharasan V
Background: Cancer is a leading cause of death worldwide and is anticipated to reach 28,4 million fresh cases globally by 2040. Despite all the progress made in cancer prevention, diagnosis, and treatment, mortality by cancer is in second place. Objectives: The design of novel 2-substituted benzimidazole modelled by QSAR study. Molecular docking studies on the novel derivatives and synthesis characterization and evaluation of the anticancer activity of the novel derivatives against breast cancer cell line MCF 7. Methods: We designed 10 novel benzimidazole derivatives modeled by 2D QSAR. From the ten compounds by applying insilico tools of ADME properties and toxicity and through molecular docking on Tyrosine Kinase (PDB ID: 2SRC). Compound 2AD showed the highest dock score of -9.5 kcal/mol followed by 2 BD and 2GD (-9.3kcal/mol) Molecular dynamic simulation studies were conducted using CABSflex an online molecular dynamic simulation tool. Six compounds were selected for synthesis. The synthesized compounds were characterized and the invitro pharmacological activity was tested on MCF-7 cell line by MTT assay. Results: The compounds 2AD and 2GD showed good percentage inhibition on MCF-7 cell line withIC50 values of 2.757 µg/ml and 2.875 µg/ml respectively. Conclusion: The novel 2-substituted benzimidazole derivatives are good lead compounds for cancer therapy. Optimization of these compounds will be providing more target-specific anticancer agents.
{"title":"2D QSAR Modelling, Docking, Synthesis and Evaluation of 2-substituted Benzimidazole Derivatives as Anti-breast Cancer Agents","authors":"Remya R.S, Barath R, Ruban R, Jaitharasan V","doi":"10.2174/0115734072255749230928060834","DOIUrl":"https://doi.org/10.2174/0115734072255749230928060834","url":null,"abstract":"Background: Cancer is a leading cause of death worldwide and is anticipated to reach 28,4 million fresh cases globally by 2040. Despite all the progress made in cancer prevention, diagnosis, and treatment, mortality by cancer is in second place. Objectives: The design of novel 2-substituted benzimidazole modelled by QSAR study. Molecular docking studies on the novel derivatives and synthesis characterization and evaluation of the anticancer activity of the novel derivatives against breast cancer cell line MCF 7. Methods: We designed 10 novel benzimidazole derivatives modeled by 2D QSAR. From the ten compounds by applying insilico tools of ADME properties and toxicity and through molecular docking on Tyrosine Kinase (PDB ID: 2SRC). Compound 2AD showed the highest dock score of -9.5 kcal/mol followed by 2 BD and 2GD (-9.3kcal/mol) Molecular dynamic simulation studies were conducted using CABSflex an online molecular dynamic simulation tool. Six compounds were selected for synthesis. The synthesized compounds were characterized and the invitro pharmacological activity was tested on MCF-7 cell line by MTT assay. Results: The compounds 2AD and 2GD showed good percentage inhibition on MCF-7 cell line withIC50 values of 2.757 µg/ml and 2.875 µg/ml respectively. Conclusion: The novel 2-substituted benzimidazole derivatives are good lead compounds for cancer therapy. Optimization of these compounds will be providing more target-specific anticancer agents.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"2014 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253935","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}
Background:: Lack of control in voluntary movements, resting tremor, postural instability, and stiffness are the hallmarks of Parkinson's disease (PD). Objective:: The current work's objective is to assess naringin isolated from Citrus aurantium L. peels as an anti-parkinsonism agent in rats. Methods:: The HPLC and LC-ESI-MS analysis of Citrus aurantium L. peels methanol extract was done. The behavioral, biochemical, genetic, and histopathological analysis were evaluated in parkinsonism rats. Results:: Fourteen phenolics and nine flavonoids were found in the extract, according to the HPLC analysis, while LC-ESI-MS analysis revealed the presence of twenty-six flavonoids. The dominant flavonoid subclasses were 4 aglycones, 11 monoglycosides, 5 diglycosides, and 6 polymethoxy flavonoids, beside 4 coumarines, 4 alkaloids and a limonin triterpene. Adenosine A2A receptor (A2AR) gene expression, malondialdehyde (MDA), interleukin-6 (IL-6), caspase-3 (Cas-3) and DNA fragmentation levels significantly increased in rotenone-treated rats. Dopamine (DA), norepinephrine (NE), serotonin (5-HT), reduced glutathione (GSH), succinate, and lactate dehydrogenase (SDH &LDH) levels all significantly decreased. Treatment with naringin and A2AR antagonists enhanced the animals’ behavior and improved all the selected parameters. The brain hippocampal features confirmed our results. Conclusion:: Naringin could be considered a nutraceutical agent by attenuating the neurodegeneration associated with PD via blocking adenosine A2AR. conclusion: Naringin could be considered as a nutraceutical agent by attenuating the neurodegeneration associated with PD via blocking adenosine A2AR
{"title":"Gene Expression, Oxidative Stress, and Neurotransmitters in Rotenoneinduced Parkinson’s Disease in Rats: Role of Naringin from Citrus aurantium via Blocking Adenosine A2A Receptor","authors":"Yomna Ahmed, Asmaa Fathy Aboul Naser, Marwa Elbatanony, Amel El-Feky, Wagdy khalil, Manal Hamed","doi":"10.2174/0115734072268296231002060839","DOIUrl":"https://doi.org/10.2174/0115734072268296231002060839","url":null,"abstract":"Background:: Lack of control in voluntary movements, resting tremor, postural instability, and stiffness are the hallmarks of Parkinson's disease (PD). Objective:: The current work's objective is to assess naringin isolated from Citrus aurantium L. peels as an anti-parkinsonism agent in rats. Methods:: The HPLC and LC-ESI-MS analysis of Citrus aurantium L. peels methanol extract was done. The behavioral, biochemical, genetic, and histopathological analysis were evaluated in parkinsonism rats. Results:: Fourteen phenolics and nine flavonoids were found in the extract, according to the HPLC analysis, while LC-ESI-MS analysis revealed the presence of twenty-six flavonoids. The dominant flavonoid subclasses were 4 aglycones, 11 monoglycosides, 5 diglycosides, and 6 polymethoxy flavonoids, beside 4 coumarines, 4 alkaloids and a limonin triterpene. Adenosine A2A receptor (A2AR) gene expression, malondialdehyde (MDA), interleukin-6 (IL-6), caspase-3 (Cas-3) and DNA fragmentation levels significantly increased in rotenone-treated rats. Dopamine (DA), norepinephrine (NE), serotonin (5-HT), reduced glutathione (GSH), succinate, and lactate dehydrogenase (SDH &LDH) levels all significantly decreased. Treatment with naringin and A2AR antagonists enhanced the animals’ behavior and improved all the selected parameters. The brain hippocampal features confirmed our results. Conclusion:: Naringin could be considered a nutraceutical agent by attenuating the neurodegeneration associated with PD via blocking adenosine A2AR. conclusion: Naringin could be considered as a nutraceutical agent by attenuating the neurodegeneration associated with PD via blocking adenosine A2AR","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"41 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136357867","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}
Introduction: Memecylon umbellatum is a perennial plant of the Melastomataceae family that grows in abundance in the Western Ghats and has been used traditionally to treat cancer and inflammatory conditions. background: Memecylon umbellatum is a perennial plant of the Melastomataceae family grows in abundance in the Western Ghats and has been used traditionally to treat cancer and inflammatory conditions. Methods: From the literature survey, it was found that no substantial work has been carried out to identify the bioactive compounds by HPTLC method and to screen the antioxidant and anticancer activity of M. umbellatum. Hence, an effort has been made to carry out the phytochemical investigation by HPTLC method and to screen the antioxidant activity by ABTS assay, DPPH assay, Nitric oxide antioxidant assay, Iron chelating activity and Total antioxidant activity. objective: From the literature survey it was found that no substantial work has been carried out to identify the bioactive compounds by HPTLC method and to screen the antioxidant and anticancer activity of M. umbellatum. Hence an effort has been made to carry out the phytochemical investigation by HPTLC method and to screen the antioxidant activity and anticancer activity Results: Total phenolics and flavonoids were carried out by using suitable methods. MCF-7 as well as MDA-MB-231 cells were used to test anticancer activities in vitro. Cell cycle analysis demonstrated that ethyl acetate extract caused G0/G1 phase arrest in MCF-7 cells. HPTLC analysis led to the identification of Lupeol from ethyl acetate extract. Conclusion: The anticancer activity of ethyl acetate extract of M. umbellatum was significant. The antioxidant and anticancer activity may attributed to Lupeol, Phenolic compounds and Flavonoids. conclusion: The antioxidant and anticancer activity may attributed to Lupeol, Phenolic compounds and Flavonoids.
{"title":"Evaluation of Antioxidant and Anticancer Activities of Memecylon umbellatum in Breast Carcinoma and Lupeol and Beta-sitosterol Quantified by HPTLC","authors":"Shilpee Chaudhary, Chandrashekar Kodangala Subraya, Sreedhara Ranganath Karkala, Vasudev Pai, Aswatha Ram Holavanna Halli Nanjundaiah, Aravinda Pai","doi":"10.2174/0115734072268707230921102959","DOIUrl":"https://doi.org/10.2174/0115734072268707230921102959","url":null,"abstract":"Introduction: Memecylon umbellatum is a perennial plant of the Melastomataceae family that grows in abundance in the Western Ghats and has been used traditionally to treat cancer and inflammatory conditions. background: Memecylon umbellatum is a perennial plant of the Melastomataceae family grows in abundance in the Western Ghats and has been used traditionally to treat cancer and inflammatory conditions. Methods: From the literature survey, it was found that no substantial work has been carried out to identify the bioactive compounds by HPTLC method and to screen the antioxidant and anticancer activity of M. umbellatum. Hence, an effort has been made to carry out the phytochemical investigation by HPTLC method and to screen the antioxidant activity by ABTS assay, DPPH assay, Nitric oxide antioxidant assay, Iron chelating activity and Total antioxidant activity. objective: From the literature survey it was found that no substantial work has been carried out to identify the bioactive compounds by HPTLC method and to screen the antioxidant and anticancer activity of M. umbellatum. Hence an effort has been made to carry out the phytochemical investigation by HPTLC method and to screen the antioxidant activity and anticancer activity Results: Total phenolics and flavonoids were carried out by using suitable methods. MCF-7 as well as MDA-MB-231 cells were used to test anticancer activities in vitro. Cell cycle analysis demonstrated that ethyl acetate extract caused G0/G1 phase arrest in MCF-7 cells. HPTLC analysis led to the identification of Lupeol from ethyl acetate extract. Conclusion: The anticancer activity of ethyl acetate extract of M. umbellatum was significant. The antioxidant and anticancer activity may attributed to Lupeol, Phenolic compounds and Flavonoids. conclusion: The antioxidant and anticancer activity may attributed to Lupeol, Phenolic compounds and Flavonoids.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"30 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136360869","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 : 2023-10-04DOI: 10.2174/0115734072275416230927074446
Sameer Ranjan Sahoo, Arun Pradhan
Background:: The rising interest in natural pigments as alternatives is a result of the expanding usage of synthetic colorants and the negative consequences that go along with them. Noble natural pigments with higher stability and productivity are becoming popular in the food industry, and their diverse biological characteristics make them valuable for pharmaceutical applications. Microbes, especially gram-negative and positive bacteria, are considered attractive sources for replacing synthetic dyes. Prodigiosin, a tripyrrole red pigment produced as secondary metabolites by these bacteria, exhibits unusual properties and has potential as an effective proapoptotic agent against cancer and multi-drug resistant cells. Objective:: This review aims to highlight the characteristics of prodigiosin and explore its potential applications as a therapeutic drug. Results:: The review investigates the biosynthetic cluster genes of prodigiosin identified using the EZ-Tn5 transposon approach in different bacteria, including the pig gene cluster in Serratia sp., red gene cluster in S. coelicolor, and hap gene cluster in Hahella chejuensis. It is also described compound nature for producing host survival physiology. Prodigiosin has a common pyrrolyl Promethean structure and is a member of the tripyrrole family. Numerous tri-pyrrole derivatives have been used in antibiotics and have demonstrated promise as pro-apoptotic agents against cancer and drug-resistant cells. Conclusion:: Prodigiosin is an intriguing subject for investigating biosynthesis and exploitation through biotechnological methods due to its distinctive properties and potential as a medicinal medication. Future investigation and bioengineering on producing strains may synthesize functional derivatives with diverse applications.
{"title":"Prodigiosin: An In-depth Exploration of a Bioactive Compound from Serratia sp.","authors":"Sameer Ranjan Sahoo, Arun Pradhan","doi":"10.2174/0115734072275416230927074446","DOIUrl":"https://doi.org/10.2174/0115734072275416230927074446","url":null,"abstract":"Background:: The rising interest in natural pigments as alternatives is a result of the expanding usage of synthetic colorants and the negative consequences that go along with them. Noble natural pigments with higher stability and productivity are becoming popular in the food industry, and their diverse biological characteristics make them valuable for pharmaceutical applications. Microbes, especially gram-negative and positive bacteria, are considered attractive sources for replacing synthetic dyes. Prodigiosin, a tripyrrole red pigment produced as secondary metabolites by these bacteria, exhibits unusual properties and has potential as an effective proapoptotic agent against cancer and multi-drug resistant cells. Objective:: This review aims to highlight the characteristics of prodigiosin and explore its potential applications as a therapeutic drug. Results:: The review investigates the biosynthetic cluster genes of prodigiosin identified using the EZ-Tn5 transposon approach in different bacteria, including the pig gene cluster in Serratia sp., red gene cluster in S. coelicolor, and hap gene cluster in Hahella chejuensis. It is also described compound nature for producing host survival physiology. Prodigiosin has a common pyrrolyl Promethean structure and is a member of the tripyrrole family. Numerous tri-pyrrole derivatives have been used in antibiotics and have demonstrated promise as pro-apoptotic agents against cancer and drug-resistant cells. Conclusion:: Prodigiosin is an intriguing subject for investigating biosynthesis and exploitation through biotechnological methods due to its distinctive properties and potential as a medicinal medication. Future investigation and bioengineering on producing strains may synthesize functional derivatives with diverse applications.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"200 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135647382","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 : 2023-10-01DOI: 10.2174/1573407219666230503094421
E. Plotnikov, Maria S Tretayakova, Konstantin S. Brazovskii, M. Belousov, A. Artamonov, S. Stuchebrov, A. Gogolev, M. Larkina, E. Sukhikh
The study aimed to assess the radiosensitizing effect of lithium ascorbate on tumor cells. Cancer cells radioresistance is an important factor restraining the success of X-ray therapy. Radiosensitizing drugs make tumor cells more sensitive to ionizing radiation and improve the effectiveness of radiotherapy. Although many chemical substances can potentiate the cytotoxic effects of X-ray radiation, their clinical applications are limited due to possible adverse reactions. Recently, several approaches have been proposed to develop new radiosensitizers that are highly effective and feature low toxicity. Among new enhancers of X-ray therapy, ascorbic acid, and its derivates demonstrate very low toxicity along with a wide therapeutic range. Lithium ascorbate is a promising X-ray therapy enhancer, but its mechanism of action is unknown. This research focuses on the radiosensitizing properties of lithium ascorbate and its effects on both tumor and normal irradiated cells. The viability of the radiosensitized cells was evaluated by fluorescence flow cytometry using Annexin V-FITC Apoptosis Detection Kit and Cellular ROS Assay Kit (Abcam, UK). The test cell cultures included normal human mononuclear and Jurkat cells. Lithium ascorbate sensitizes normal human mononuclear and Jurkat cells towards ionizing radiation. The combined cytotoxic effect of X-ray irradiation (3 Gy) and lithium ascorbate (1,2 mmol/L) substantially exceeds the effects of the individual factors, i.e. synergetic action appears. The major types of cell death were late apoptosis and necrosis caused by excessive production of reactive oxygen species. Lithium ascorbate in combination with X-ray irradiation exhibited the cytotoxic effect on both normal and cancer lymphoid cells by activating reactive oxygen species (ROS)-induced apoptosis. These findings indicate that lithium ascorbate is a promising substance to develop a new radiosensitizing drug.
{"title":"Radiosensitizing Effects of Lithium Ascorbate on Normal and Tumor\u0000Lymphoid Cells under X-ray Irradiation","authors":"E. Plotnikov, Maria S Tretayakova, Konstantin S. Brazovskii, M. Belousov, A. Artamonov, S. Stuchebrov, A. Gogolev, M. Larkina, E. Sukhikh","doi":"10.2174/1573407219666230503094421","DOIUrl":"https://doi.org/10.2174/1573407219666230503094421","url":null,"abstract":"\u0000\u0000The study aimed to assess the radiosensitizing effect of lithium ascorbate on tumor cells.\u0000\u0000\u0000\u0000Cancer cells radioresistance is an important factor restraining the success of X-ray\u0000therapy. Radiosensitizing drugs make tumor cells more sensitive to ionizing radiation and improve\u0000the effectiveness of radiotherapy. Although many chemical substances can potentiate the cytotoxic\u0000effects of X-ray radiation, their clinical applications are limited due to possible adverse reactions.\u0000Recently, several approaches have been proposed to develop new radiosensitizers that are highly\u0000effective and feature low toxicity. Among new enhancers of X-ray therapy, ascorbic acid, and its\u0000derivates demonstrate very low toxicity along with a wide therapeutic range. Lithium ascorbate is a\u0000promising X-ray therapy enhancer, but its mechanism of action is unknown. This research focuses\u0000on the radiosensitizing properties of lithium ascorbate and its effects on both tumor and normal irradiated\u0000cells.\u0000\u0000\u0000\u0000The viability of the radiosensitized cells was evaluated by fluorescence flow cytometry\u0000using Annexin V-FITC Apoptosis Detection Kit and Cellular ROS Assay Kit (Abcam, UK). The\u0000test cell cultures included normal human mononuclear and Jurkat cells.\u0000\u0000\u0000\u0000Lithium ascorbate sensitizes normal human mononuclear and Jurkat cells towards ionizing\u0000radiation. The combined cytotoxic effect of X-ray irradiation (3 Gy) and lithium ascorbate (1,2\u0000mmol/L) substantially exceeds the effects of the individual factors, i.e. synergetic action appears.\u0000The major types of cell death were late apoptosis and necrosis caused by excessive production of\u0000reactive oxygen species.\u0000\u0000\u0000\u0000Lithium ascorbate in combination with X-ray irradiation exhibited the cytotoxic effect\u0000on both normal and cancer lymphoid cells by activating reactive oxygen species (ROS)-induced\u0000apoptosis. These findings indicate that lithium ascorbate is a promising substance to develop a new\u0000radiosensitizing drug.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44976101","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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