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Article ; Online: Metal Nanoparticles as Emerging Drug Candidates in the Management of Cancers and Microbial Infectious Diseases.

Narayanankutty, Arunaksharan

Recent patents on anti-cancer drug discovery

2023 Volume 18, Issue 3, Page(s) 244–245

MeSH term(s)	Humans ; Communicable Diseases/drug therapy ; Metal Nanoparticles ; Neoplasms/drug therapy ; Nanoparticles
Language	English
Publishing date	2023-03-09
Publishing country	United Arab Emirates
Document type	Editorial
ZDB-ID	2250820-X
ISSN	2212-3970 ; 1574-8928
ISSN (online)	2212-3970
ISSN	1574-8928
DOI	10.2174/157489281803230127124009
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Article ; Online: Natural Products as PI3K/ Akt Inhibitors: Implications in Preventing Hepatocellular Carcinoma.

Narayanankutty, Arunaksharan

Current molecular pharmacology

2021 Volume 14, Issue 5, Page(s) 760–769

Abstract: Hepatocellular carcinoma (HCC) is one of the prominent forms of cancer in developed countries. Globally, the incidence of HCC is well correlated with fatty liver disease and cirrhosis; the underlying chronic inflammation and lipotoxicity are thought to ... ...

Abstract	Hepatocellular carcinoma (HCC) is one of the prominent forms of cancer in developed countries. Globally, the incidence of HCC is well correlated with fatty liver disease and cirrhosis; the underlying chronic inflammation and lipotoxicity are thought to drive the process of HCC. Several biochemical cycles and molecular pathways are associated. The review aims to summarize the role of PI3K/Akt signaling and its downstream effectors in the development of HCC and its progression. Further, the emphasis has been given to the role of natural inhibitors of the PI3K/Akt pathway in HCC prevention, which are under various levels of drug discovery. The required literature were collected from PubMed/Medline databases, as well as Scopus or Web of science. It is evident that various signaling pathways activated by growth factors together with detoxification machinery and biochemical cycles converge to the PI3K/Akt signaling. The pathway plays a key role in the carcinogenesis, metastasis and drug resistance events of HCC cells and provides the growth and survival advantage. Natural products belonging to various classes such as terpenoids, flavonoids, saponins and stilbenoids are proven inhibitors of PI3K signaling and also found to inhibit HCC progression. PI3K/mTOR pathway inhibitors, especially the different phytochemicals, emerged as promising as anti-HCC agents. These molecules are shown to interfere with the PI3K signaling at various stages and therefore the PI3K targeted drugs may be a future for the chemotherapeutic arena.
MeSH term(s)	Biological Products/pharmacology ; Biological Products/therapeutic use ; Carcinoma, Hepatocellular/drug therapy ; Carcinoma, Hepatocellular/prevention & control ; Cell Line, Tumor ; Humans ; Liver Neoplasms/drug therapy ; Liver Neoplasms/prevention & control ; Phosphatidylinositol 3-Kinases ; Proto-Oncogene Proteins c-akt ; TOR Serine-Threonine Kinases
Chemical Substances	Biological Products ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; TOR Serine-Threonine Kinases (EC 2.7.11.1)
Language	English
Publishing date	2021-01-14
Publishing country	United Arab Emirates
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ISSN	1874-4702
ISSN (online)	1874-4702
DOI	10.2174/1874467214666210120152657
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Article ; Online: Pharmacological Potentials and Nutritional Values of Tropical and Subtropical Fruits of India: Emphasis on their Anticancer Bioactive Components.

Narayanankutty, Arunaksharan

Recent patents on anti-cancer drug discovery

2021 Volume 17, Issue 2, Page(s) 124–135

Abstract: Background: Fruits are an important dietary component, which supply vitamins, minerals, as well as dietary fiber. In addition, they are rich sources of various biological and pharmacologically active compounds. Among these, temperate fruits are well ... ...

Abstract	Background: Fruits are an important dietary component, which supply vitamins, minerals, as well as dietary fiber. In addition, they are rich sources of various biological and pharmacologically active compounds. Among these, temperate fruits are well studied for their pharmacological potentials, whereas tropical/subtropical fruits are less explored for their health impacts. In India, most of the consumed fruits are either tropical or subtropical. Objectives: This mini review aims to provide a health impact of major tropical and sub-tropical fruits of India, emphasizing their anticancer efficacy. In addition, the identified bioactive components from these fruits exhibiting anticancer efficacy are also discussed along with the patent literature published. Methods: The literature was collected from various repositories, including NCBI, ScienceDirect, Eurekaselect, and Web of Science; literature from predatory journals was omitted during the process. Patent literature was collected from google patents and similar patent databases. Results: Tropical fruits are rich sources of various nutrients and bioactive components including polyphenols, flavonoids, anthocyanin, etc. By virtue of these biomolecules, tropical fruits have been shown to interfere with various steps in carcinogenesis, metastasis, and drug resistance. Their mode of action is either by activation of apoptosis, regulation of cell cycle, inhibition of cell survival and proliferation pathways, increased lipid trafficking or inhibiting inflammatory pathways. Several molecules and combinations have been patented for their anticancer and chemoprotective properties. Conclusion: Overall, the present concludes that Indian tropical/ subtropical fruits are nutritionally and pharmacologically active and may serve as a source of novel anticancer agents in the future.
MeSH term(s)	Fruit ; Humans ; Nutritive Value ; Patents as Topic ; Plant Extracts/pharmacology ; Polyphenols
Chemical Substances	Plant Extracts ; Polyphenols
Language	English
Publishing date	2021-11-30
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2250820-X
ISSN	2212-3970 ; 1574-8928
ISSN (online)	2212-3970
ISSN	1574-8928
DOI	10.2174/1574892816666211130165200
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Article ; Online: Inhibitory Potential of Dietary Nutraceuticals on Cellular PI3K/Akt Signaling: Implications in Cancer Prevention and Therapy.

Narayanankutty, Arunaksharan

Current topics in medicinal chemistry

2021 Volume 21, Issue 20, Page(s) 1816–1831

Abstract: Background: The phosphatidyl inositol-3 kinase (PI3K)/protein kinase B (Akt)/mechanistic target of rapamycin (mTOR) signaling has been associated with many cellular physiological events, such as proliferation, maturation, survival, and metabolism. ... ...

Abstract	Background: The phosphatidyl inositol-3 kinase (PI3K)/protein kinase B (Akt)/mechanistic target of rapamycin (mTOR) signaling has been associated with many cellular physiological events, such as proliferation, maturation, survival, and metabolism. Besides its role in normal cells, the pathway is often upregulated in various cancers. Due to its prominent role in the cancer progression events, it is now being considered as a target for cancer therapy and cancer chemoprevention. Objectives: The present review provides a concise outline of the role of the PI3K/Akt/mTOR pathway in carcinogenesis and progression events, including metastasis, drug resistance and stemness. Further, emphasis needs to be placed on the PI3K/Akt/mTOR pathway inhibitory potentials of various food-derived bioactive components in cancer prevention. Methods: Data on the PI3K/Akt/mTOR inhibiting natural products and their bioactive compounds have been obtained from PubMed/Medline, Scopus, Eurekaselect, etc. Findings from the above citation databases from 2000-2021 are included in the manuscript. Results: Numerous compounds from plants have been isolated and identified as anticancer agents; among these, a predominant class is nutraceuticals. The PI3K pathway is the predominant target of these natural products, and many of these drug candidates are under various stages of drug development. These compounds have shown a significant inhibitory effect on the kinase activities of PI3K and Akt, resulting in the abrogation of cancer initiation and progression events. In addition, these compounds have been shown to reverse the resistance to chemotherapeutic drugs and also reduce the population of cancer stem cells. Conclusion: The nutraceuticals are promising candidates as anticancer agents by blocking PI3K signaling cascades. As the PI3K is a central pathway to various receptors signaling, the dietary intervention may prove to be highly effective.
MeSH term(s)	Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Biological Products/pharmacology ; Biological Products/therapeutic use ; Dietary Supplements ; Humans ; Neoplasms/diet therapy ; Neoplasms/prevention & control ; Phosphatidylinositol 3-Kinases/metabolism ; Phosphoinositide-3 Kinase Inhibitors/pharmacology ; Phosphoinositide-3 Kinase Inhibitors/therapeutic use ; Phytotherapy ; Proto-Oncogene Proteins c-akt/antagonists & inhibitors ; Signal Transduction/drug effects ; TOR Serine-Threonine Kinases/antagonists & inhibitors ; TOR Serine-Threonine Kinases/metabolism
Chemical Substances	Antineoplastic Agents ; Biological Products ; Phosphoinositide-3 Kinase Inhibitors ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; TOR Serine-Threonine Kinases (EC 2.7.11.1)
Language	English
Publishing date	2021-12-16
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/1568026621666210716152224
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Article ; Online: Phytochemicals as PI3K/ Akt/ mTOR Inhibitors and Their Role in Breast Cancer Treatment.

Narayanankutty, Arunaksharan

Recent patents on anti-cancer drug discovery

2020 Volume 15, Issue 3, Page(s) 188–199

Abstract: Background: Breast cancer is the predominant form of cancer in women; various cellular pathways are involved in the initiation and progression of breast cancer. Among the various types of breast cancer that differ in their growth factor receptor status, ...

Abstract	Background: Breast cancer is the predominant form of cancer in women; various cellular pathways are involved in the initiation and progression of breast cancer. Among the various types of breast cancer that differ in their growth factor receptor status, PI3K/Akt signaling is a common pathway where all these converge. Thus, the PI3K signaling is of great interest as a target for breast cancer prevention; however, it is less explored. Objective: The present review is aimed to provide a concise outline of the role of PI3K/Akt/mTOR pathway in breast carcinogenesis and its progression events, including metastasis, drug resistance and stemness. The review emphasizes the role of natural and synthetic inhibitors of PI3K/Akt/m- TOR pathway in breast cancer prevention. Methods: The data were obtained from PubMed/Medline databases, Scopus and Google patent literature. Results: PI3K/Akt/mTOR signaling plays an important role in human breast carcinogenesis; it acts on the initiation and progression events associated with it. Numerous molecules have been isolated and identified as promising drug candidates by targeting the signaling pathway. Results from clinical studies confirm their application in the treatment of human breast cancer alone and in combination with classical chemotherapeutics as well as monoclonal antibodies. Conclusion: PI3K/mTOR signaling blockers have evolved as promising anticancer agents by interfering breast cancer development and progression at various stages. Natural products and bioactive components are emerging as novel inhibitors of PI3K signaling and more research in this area may yield numerous drug candidates.
MeSH term(s)	Antineoplastic Agents, Phytogenic/pharmacology ; Antineoplastic Combined Chemotherapy Protocols/therapeutic use ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Female ; Humans ; Molecular Targeted Therapy ; Patents as Topic ; Phosphatidylinositol 3-Kinases/metabolism ; Phosphoinositide-3 Kinase Inhibitors/therapeutic use ; Phytochemicals/pharmacology ; Proto-Oncogene Proteins c-akt/antagonists & inhibitors ; TOR Serine-Threonine Kinases/antagonists & inhibitors
Chemical Substances	Antineoplastic Agents, Phytogenic ; Phosphoinositide-3 Kinase Inhibitors ; Phytochemicals ; MTOR protein, human (EC 2.7.1.1) ; TOR Serine-Threonine Kinases (EC 2.7.1.1) ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1)
Language	English
Publishing date	2020-09-11
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2250820-X
ISSN	2212-3970 ; 1574-8928
ISSN (online)	2212-3970
ISSN	1574-8928
DOI	10.2174/1574892815666200910164641
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Article ; Online: Toll-like Receptors as a Novel Therapeutic Target for Natural Products Against Chronic Diseases.

Narayanankutty, Arunaksharan

Current drug targets

2019 Volume 20, Issue 10, Page(s) 1068–1080

Abstract: Toll-like receptors (TLR) are one among the initial responders of the immune system which participate in the activation inflammatory processes. Several different types of TLR such as TLR2, TLR4, TLR7 and TLR9 have been identified in various cell types, ... ...

Abstract	Toll-like receptors (TLR) are one among the initial responders of the immune system which participate in the activation inflammatory processes. Several different types of TLR such as TLR2, TLR4, TLR7 and TLR9 have been identified in various cell types, each having distinct ligands like lipids, lipoproteins, nucleic acids and proteins. Though its prime concern is xenobiotic defences, TLR signalling has also recognized as an activator of inflammation and associated development of chronic degenerative disorders (CDDs) including obesity, type 2 diabetes mellitus (T2DM), fatty liver disease, cardiovascular and neurodegenerative disorders as well as various types of cancers. Numerous drugs are in use to prevent these disorders, which specifically inhibit different pathways associated with the development of CDDs. Compared to these drug targets, inhibition of TLR, which specifically responsible for the inflammatory insults has proven to be a better drug target. Several natural products have emerged as inhibitors of CDDs, which specifically targets TLR signalling, among these, many are in the clinical trials. This review is intended to summarize the recent progress on TLR association with CDDs and to list possible use of natural products, their combinations and their synthetic derivative in the prevention of TLR-driven CDD development.
MeSH term(s)	Biological Products/pharmacology ; Biological Products/therapeutic use ; Chronic Disease/drug therapy ; Gene Expression Regulation/drug effects ; Humans ; Molecular Targeted Therapy ; Signal Transduction/drug effects ; Toll-Like Receptors/metabolism
Chemical Substances	Biological Products ; Toll-Like Receptors
Language	English
Publishing date	2019-02-26
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2064859-5
ISSN	1873-5592 ; 1389-4501
ISSN (online)	1873-5592
ISSN	1389-4501
DOI	10.2174/1389450120666190222181506
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: PI3K/ Akt/ mTOR Pathway as a Therapeutic Target for Colorectal Cancer: A Review of Preclinical and Clinical Evidence.

Narayanankutty, Arunaksharan

Current drug targets

2019 Volume 20, Issue 12, Page(s) 1217–1226

Abstract: Background: Phosphoinositide 3-kinase (PI3Ks) is a member of intracellular lipid kinases and involved in the regulation of cellular proliferation, differentiation and survival. Overexpression of the PI3K/Akt/mTOR signalling has been reported in various ... ...

Abstract	Background: Phosphoinositide 3-kinase (PI3Ks) is a member of intracellular lipid kinases and involved in the regulation of cellular proliferation, differentiation and survival. Overexpression of the PI3K/Akt/mTOR signalling has been reported in various forms of cancers, especially in colorectal cancers (CRC). Due to their significant roles in the initiation and progression events of colorectal cancer, they are recognized as a striking therapeutic target. Objective: The present review is aimed to provide a detailed outline on the role of PI3K/Akt/mTOR pathway in the initiation and progression events of colorectal cancers as well as its function in drug resistance. Further, the role of PI3K/Akt/mTOR inhibitors alone and in combination with other chemotherapeutic drugs, in alleviating colorectal cancer is also discussed. The review contains preclinical and clinical evidence as well as patent literature of the pathway inhibitors which are natural and synthetic in origin. Methods: The data were obtained from PubMed/Medline databases, Scopus and Google patent literature. Results: PI3K/Akt/mTOR signalling is an important event in colorectal carcinogenesis. In addition, it plays significant roles in acquiring drug resistance as well as metastatic initiation events of CRCs. Several small molecules of natural and synthetic origin have been found to be potent inhibitors of CRCs by effectively downregulating the pathway. Data from various clinical studies also support these pathway inhibitors and several among them are patented. Conclusion: Inhibitors of the PI3K/mTOR pathway have been successful for the treatment of primary and metastatic colorectal cancers, rendering the pathway as a promising clinical cancer therapeutic target.
MeSH term(s)	Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Colorectal Neoplasms/drug therapy ; Colorectal Neoplasms/metabolism ; Drug Resistance, Neoplasm/drug effects ; Gene Expression Regulation, Neoplastic/drug effects ; Humans ; Phosphatidylinositol 3-Kinases/metabolism ; Proto-Oncogene Proteins c-akt/metabolism ; Signal Transduction/drug effects ; Small Molecule Libraries/pharmacology ; Small Molecule Libraries/therapeutic use ; TOR Serine-Threonine Kinases/metabolism ; Up-Regulation
Chemical Substances	Antineoplastic Agents ; Small Molecule Libraries ; MTOR protein, human (EC 2.7.1.1) ; TOR Serine-Threonine Kinases (EC 2.7.1.1) ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1)
Language	English
Publishing date	2019-08-19
Publishing country	United Arab Emirates
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2064859-5
ISSN	1873-5592 ; 1389-4501
ISSN (online)	1873-5592
ISSN	1389-4501
DOI	10.2174/1389450120666190618123846
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Article ; Online: Phytochemicals and Nanoparticles in the Modulation of PI3K/Akt/mTOR Kinases and its Implications in the Development and Progression of Gastrointestinal Cancers: A Review of Preclinical and Clinical Evidence.

Narayanankutty, Arunaksharan / Nambiattil, Sreelakshmi / Mannarakkal, Sreeshna

Recent patents on anti-cancer drug discovery

2022 Volume 18, Issue 3, Page(s) 307–324

Abstract: Background: Gastrointestinal cancer are the major form of cancer in developing countries, which comprises gastric cancer (GC), hepatic cancer (HCC), colorectal cancers (CRC), etc.; they account for a large number of cancer-related deaths globally. ... ...

Abstract	Background: Gastrointestinal cancer are the major form of cancer in developing countries, which comprises gastric cancer (GC), hepatic cancer (HCC), colorectal cancers (CRC), etc.; they account for a large number of cancer-related deaths globally. Gastrointestinal cancers generally have a multifactorial origin, where both genetic and dietary factors play prominent roles. PI3K/Akt signaling is the prime signaling pathway associated with the Phosphoinositide-3 kinase/protein kinase B signaling pathway. Objectives: The present review aims to summarize the role of the PI3K/Akt signaling pathway on the different events of gastrointestinal cancers, such as proliferation, survival, metastasis, angiogenesis, drug resistance and stem cell properties. Methods: Literature collection has been done using the appropriate keywords from Pub- Med/Medline, Scopus, Web of science, or Eurekaselect. The details of individual types of cancers were selected by giving respective keywords. Results: PI3K signaling pathway is important in various gastrointestinal carcinogenesis and progression events; the pathway is involved in proliferation, survival, metastasis, and drug resistance. Several natural phytochemicals and their derivatives have been shown to inhibit PI3K signaling and its downstream regulatory elements, subsequently resulting in anticancer and anti-metastatic activity. Although numerous preclinical evidences are available, conclusive clinical reports are lacking on the anticancer aspects of PI3K inhibitors in gastric cancer. Conclusion: Phytochemicals are promising drug candidates for targeting the PI3K/mTOR pathway in various gastrointestinal cancer treatments. However, there is a need for extensive clinical studies to ascertain the commercial value of anticancer therapeutic compounds against cancers of the stomach, liver, and intestine.
MeSH term(s)	Humans ; Proto-Oncogene Proteins c-akt/metabolism ; Phosphatidylinositol 3-Kinases/metabolism ; Stomach Neoplasms/drug therapy ; TOR Serine-Threonine Kinases ; Gastrointestinal Neoplasms/drug therapy ; Nanoparticles
Chemical Substances	Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; TOR Serine-Threonine Kinases (EC 2.7.11.1) ; MTOR protein, human (EC 2.7.1.1)
Language	English
Publishing date	2022-03-09
Publishing country	United Arab Emirates
Document type	Review ; Journal Article
ZDB-ID	2250820-X
ISSN	2212-3970 ; 1574-8928
ISSN (online)	2212-3970
ISSN	1574-8928
DOI	10.2174/1574892817666220606104712
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Article: A High-Fructose Diet Formulated with Thermally Oxidized Monounsaturated Fat Aggravates Metabolic Dysregulation in Colon Epithelial Tissues of Rats

Narayanankutty, Arunaksharan / Kuzhivelil, Balu T. / Raghavamenon, Achuthan C.

Journal of the American Nutrition Association. 2022 Jan. 2, v. 41, no. 1

2022

Abstract: Various epidemiological and clinical studies have indicated a positive association of colon cancer with high sugar and thermally oxidized fats consumption. The present study evaluated the effects of fresh and thermally oxidized coconut (CO) and mustard ... ...

Abstract	Various epidemiological and clinical studies have indicated a positive association of colon cancer with high sugar and thermally oxidized fats consumption. The present study evaluated the effects of fresh and thermally oxidized coconut (CO) and mustard oils (MO) along with a high-sugar diet in the rat colon mucosa. The animals were fed with a modified diet containing high-fructose and different edible oils as fatty acids sources over a period of 30 weeks. Further, the development of insulin resistance and hyperglycemia were estimated biochemically. The changes in the redox status were estimated in terms of reduced glutathione (GSH), antioxidant enzymes and thiobarbituric acid reactive substances (TBARS). Changes in the expression of genes associated with inflammation and cell proliferation were evaluated by qPCR. The animals fed with high-fructose developed hyperglycemia and insulin resistance over 30 weeks. These animals had diminished GSH level, SOD activity and a concomitant increase in the TBARS level in the colon epithelial tissues. In addition, the expression of pro-inflammatory cytokines (IL-6 and TNF-α) was elevated while P53 and PPARγ were down-regulated. This heightened body metabolic dysregulation and associated oxidative damage and inflammation in the colon were exacerbated by thermally oxidized edible oils incorporated in the diet, with a more prominent effect was observed with TMO. Feeding high-fructose diet with TMO increases the oxidative and inflammatory damages in the colon epithelium of Wistar rats. Therefore, the study cautions the prolonged consumption of thermally oxidized monounsaturated fat-rich edible oils, especially by individuals with type 2 diabetes.
Keywords	cell proliferation ; coconuts ; colon ; colorectal neoplasms ; glutathione ; high fructose diet ; hyperglycemia ; inflammation ; insulin resistance ; interleukin-6 ; mucosa ; noninsulin-dependent diabetes mellitus ; oxidation ; rats ; sugars
Language	English
Dates of publication	2022-0102
Size	p. 38-49.
Publishing place	Taylor & Francis
Document type	Article
ISSN	2769-707X
DOI	10.1080/07315724.2020.1846145
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Synthesis of Bis-Chalcones and Evaluation of Its Effect on Peroxide-Induced Cell Death and Lipopolysaccharide-Induced Cytokine Production.

Tom, Alby / Jacob, Jisha / Mathews, Manoj / Rajagopal, Rajakrishnan / Alfarhan, Ahmed / Barcelo, Damia / Narayanankutty, Arunaksharan

Molecules (Basel, Switzerland)

2023 Volume 28, Issue 17

Abstract: Plant secondary metabolites are important sources of biologically active compounds with wide pharmacological potentials. Among the different classes, the chalcones form integral pharmacologically active agents. Natural chalcones and bis-chalcones exhibit ...

Abstract	Plant secondary metabolites are important sources of biologically active compounds with wide pharmacological potentials. Among the different classes, the chalcones form integral pharmacologically active agents. Natural chalcones and bis-chalcones exhibit high antioxidant and anti-inflammatory properties in various experiments. Studies are also underway to explore more biologically active bis-chalcones by chemical synthesis of these compounds. In this study, the effects of six synthetic bis-chalcones were evaluated in intestinal epithelial cells (IEC-6); further, the anti-inflammatory potentials were studied in lipopolysaccharide-induced cytokine production in macrophages. The synthesized bis-chalcones differ from each other first of all by the nature of the aromatic cores (functional group substitution, and their position) and by the size of a central alicycle. The exposure of IEC-6 cells to peroxide radicals reduced the cell viability; however, pre-treatment with the bis-chalcones improved the cell viability in these cells. The mechanism of action was observed to be the increased levels of glutathione and antioxidant enzyme activities. Further, these bis-chalcones also inhibited the LPS-stimulation-induced inflammatory cytokine production in RAW 264.7 macrophages. Overall, the present study indicated the cytoprotective and anti-inflammatory abilities of synthetic bis-chalcones.
MeSH term(s)	Antioxidants/pharmacology ; Chalcones/pharmacology ; Lipopolysaccharides/pharmacology ; Cell Death ; Peroxides ; Cytokines
Chemical Substances	Antioxidants ; Chalcones ; Lipopolysaccharides ; Peroxides ; Cytokines
Language	English
Publishing date	2023-08-30
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules28176354
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