34 results on '"El-Demerdash, Amr"'
Search Results
2. Synthesis of Some Novel Thiophene Analogues as Potential Anticancer Agents.
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Almatari, Altaf S., Saeed, Ali, Abdel‐Ghani, Ghada E., Abdullah, Mahmood M. S., Al‐Lohedan, Hamad A., Abdel‐Latif, Ehab, and El‐Demerdash, Amr
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- 2024
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3. Synthesis and Molecular Docking of some new Thiazolidinone and Thiadiazole Derivatives as Anticancer Agents.
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Saeed, Ali, Soliman, Ahbarah M., Abdullah, Mahmood M. S., Abdel‐Latif, Ehab, and El‐Demerdash, Amr
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- 2024
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4. Employing acetoacetamide as a key synthon for synthesizing novel thiophene derivatives and assessing their potential as antioxidants and antimicrobial agents.
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Almatari, Altaf S., Saeed, Ali, Abdel‐Ghani, Ghada E., Abdullah, Mahmood M. S., El‐Demerdash, Amr, and Abdel‐Latif, Ehab
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DIAZONIUM compounds ,ANTI-infective agents ,THIOPHENE derivatives ,METHYL iodide ,DIOXANE ,INFRARED spectroscopy ,THIAZOLE derivatives ,HYDRAZINE derivatives - Abstract
The objective of this study is to synthesize novel heterocyclic scaffolds containing a thiophene moiety using easily accessible acetoacetamide as a key synthon. The reaction of acetoacetamide with diazonium salts resulted in the formation of the corresponding thiophene derivatives 4a–c. Additionally, the reaction of acetoacetamide derivative 3 with malononitrile, ethyl cyanoacetate, or 2‐cyanoacetamide, along with elemental sulfur, under refluxing in dioxane containing triethylamine afforded thiophene‐containing derivatives 5a–c. Furthermore, compound 3 reacted with phenyl isothiocyanate in dry dimethylformamide and K2CO3 to yield compound 7. In situ alkylation of the non‐isolable salt 6 was achieved by the addition of methyl iodide, resulting in the formation of methylthio‐thiophene‐2‐carboxamide 8. Compound 7 was employed with numerous alpha‐halogenated reagents in ethanol, affording thiazole derivative 9 and thiophene derivatives 10a and 10b, respectively. Moreover, compound 8 was reacted with hydrazine to produce the 1H‐pyrazole‐4‐carboxamide derivative 11. Additionally, refluxing acetoacetamide derivative 3 with malononitrile and/or ethyl cyanoacetate in dioxane, in the presence of catalytic amount of triethylamine afforded 4‐imino‐3,7‐dimethyl‐4H‐pyrido[1,2‐a]thieno[3,2‐e]pyrimidin‐9(5H)‐one derivatives 12a and 12b. Furthermore, the reactivity of acetoacetamide derivative 3 with 2‐cyanoacetohydrazide was investigated through refluxing the reactants in dioxane, which subsequently yielded the corresponding cyanoacetamide derivative 13. The chemical identity of the newly synthesized compounds was determined by employing infrared spectroscopy (IR), 1H NMR, and 13C NMR techniques. Newly synthesized heterocycles incorporating thiophenes were evaluated for their antioxidant and antimicrobial potentials. Notably, thiophene scaffolds 5a, 10b, 11, and 13 displayed notable antioxidant and antimicrobial activities. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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5. Complete biosynthesis of QS-21 in engineered yeast.
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Liu, Yuzhong, Zhao, Xixi, Gan, Fei, Chen, Xiaoyue, Deng, Kai, Crowe, Samantha A., Hudson, Graham A., Belcher, Michael S., Schmidt, Matthias, Astolfi, Maria C. T., Kosina, Suzanne M., Pang, Bo, Shao, Minglong, Yin, Jing, Sirirungruang, Sasilada, Iavarone, Anthony T., Reed, James, Martin, Laetitia B. B., El-Demerdash, Amr, and Kikuchi, Shingo
- Abstract
QS-21 is a potent vaccine adjuvant and remains the only saponin-based adjuvant that has been clinically approved for use in humans1,2. However, owing to the complex structure of QS-21, its availability is limited. Today, the supply depends on laborious extraction from the Chilean soapbark tree or on low-yielding total chemical synthesis3,4. Here we demonstrate the complete biosynthesis of QS-21 and its precursors, as well as structural derivatives, in engineered yeast strains. The successful biosynthesis in yeast requires fine-tuning of the host’s native pathway fluxes, as well as the functional and balanced expression of 38 heterologous enzymes. The required biosynthetic pathway spans seven enzyme families—a terpene synthase, P450s, nucleotide sugar synthases, glycosyltransferases, a coenzyme A ligase, acyl transferases and polyketide synthases—from six organisms, and mimics in yeast the subcellular compartmentalization of plants from the endoplasmic reticulum membrane to the cytosol. Finally, by taking advantage of the promiscuity of certain pathway enzymes, we produced structural analogues of QS-21 using this biosynthetic platform. This microbial production scheme will allow for the future establishment of a structure–activity relationship, and will thus enable the rational design of potent vaccine adjuvants.QS-21—an FDA-approved vaccine adjuvant—and several structural analogues of QS-21 can be synthesized in engineered yeast strains, and this process is much less laborious compared with the conventional mode of extraction from the Chilean soapbark tree. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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6. Investigating the antiviral therapeutic potentialities of marine polycyclic lamellarin pyrrole alkaloids as promising inhibitors for SARS-CoV-2 and Zika main proteases (Mpro).
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Pereira, Florbela, Bedda, Loay, Tammam, Mohamed A., Alabdullah, Abdul Kader, Arafa, Reem, and El-Demerdash, Amr
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- 2024
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7. Discovery of isoflavone phytoalexins in wheat reveals an alternative route to isoflavonoid biosynthesis.
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Polturak, Guy, Misra, Rajesh Chandra, El-Demerdash, Amr, Owen, Charlotte, Steed, Andrew, McDonald, Hannah P., Wang, JiaoJiao, Saalbach, Gerhard, Martins, Carlo, Chartrain, Laetitia, Wilkinson, Barrie, Nicholson, Paul, and Osbourn, Anne
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EMMER wheat ,BIOSYNTHESIS ,PHYTOALEXINS ,WHEATGRASSES ,GENE clusters ,WHEAT ,FOOD crops - Abstract
Isoflavones are a group of phenolic compounds mostly restricted to plants of the legume family, where they mediate important interactions with plant-associated microbes, including in defense from pathogens and in nodulation. Their well-studied health promoting attributes have made them a prime target for metabolic engineering, both for bioproduction of isoflavones as high-value molecules, and in biofortification of food crops. A key gene in their biosynthesis, isoflavone synthase, was identified in legumes over two decades ago, but little is known about formation of isoflavones outside of this family. Here we identify a specialized wheat-specific isoflavone synthase, TaCYP71F53, which catalyzes a different reaction from the leguminous isoflavone synthases, thus revealing an alternative path to isoflavonoid biosynthesis and providing a non-transgenic route for engineering isoflavone production in wheat. TaCYP71F53 forms part of a biosynthetic gene cluster that produces a naringenin-derived O-methylated isoflavone, 5-hydroxy-2′,4′,7-trimethoxyisoflavone, triticein. Pathogen-induced production and in vitro antimicrobial activity of triticein suggest a defense-related role for this molecule in wheat. Genomic and metabolic analyses of wheat ancestral grasses further show that the triticein gene cluster was introduced into domesticated emmer wheat through natural hybridization ~9000 years ago, and encodes a pathogen-responsive metabolic pathway that is conserved in modern bread wheat varieties. Isoflavones are mostly found in the legumes, and little is known about their formation outside of this family. Here, the authors discover an isoflavone synthase gene in wheat, found in a pathogen-induced gene cluster encoding isoflavone biosynthesis. [ABSTRACT FROM AUTHOR]
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- 2023
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8. Signal crosstalk of phytomelatonin during salinity stress tolerance in plants.
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Mishra, Sonal, Bagal, Diksha, Chowdhary, Aksar Ali, Mehrotra, Shakti, Rai, Gyanendra Kumar, Gandhi, Sumit G., Bhau, Brijmohan Singh, El-Demerdash, Amr, and Srivastava, Vikas
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- 2023
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9. Investigating the hepatoprotective potentiality of marine-derived steroids as promising inhibitors of liver fibrosis.
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Tammam, Mohamed A., Pereira, Florbela, Aly, Omnia, Sebak, Mohamed, Diab, Yasser M., Mahdy, Aldoushy, and El-Demerdash, Amr
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- 2023
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10. Elucidation of the pathway for biosynthesis of saponin adjuvants from the soapbark tree.
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Reed, James, Orme, Anastasia, El-Demerdash, Amr, Owen, Charlotte, Martin, Laetitia B. B., Misra, Rajesh C., Kikuchi, Shingo, Rejzek, Martin, Martin, Azahara C., Harkess, Alex, Leebens-Mack, Jim, Louveau, Thomas, Stephenson, Michael J., and Osbourn, Anne
- Published
- 2023
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11. Recent advances in the discovery, biosynthesis, and therapeutic potential of isocoumarins derived from fungi: a comprehensive update.
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Tammam, Mohamed A., Gamal El-Din, Mariam I., Abood, Amira, and El-Demerdash, Amr
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- 2023
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12. Chemical diversity, medicinal potentialities, biosynthesis, and pharmacokinetics of anthraquinones and their congeners derived from marine fungi: a comprehensive update.
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Sebak, Mohamed, Molham, Fatma, Greco, Claudio, Tammam, Mohamed A., Sobeh, Mansour, and El-Demerdash, Amr
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- 2022
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13. Cytotoxic constituents from the wheat plant pathogen Parastagonospora nodorum SN15.
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El-Demerdash, Amr, Borde, Chloé, Genta-Jouve, Gregory, Escargueil, Alexandre, and Prado, Soizic
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PHYTOPATHOGENIC microorganisms ,MARINE natural products ,WHEAT ,NATURAL products ,MICROBIAL products ,ACID derivatives - Abstract
Microbial natural products are continuing to be a promising platform for future drug lead discover. As a part of our ongoing research program on fungal natural product, herein we report metabolites isolated from the fungus Parastagonospora nodorum SN15 a pathogen of wheat and related cereals. Its chemical investigation led to the purification of new isoleucinic acid derivatives (1–2) along with the cis procuramine (4). Their structures were determined based on extensive NMR and the relative configuration by comparison of experimental and predicted NMR chemical shifts. All compounds were evaluated for their cytotoxic activity against a panel of human cell lines and some displayed specific feature towards cancer cells compared to normal immortalised fibroblasts. [ABSTRACT FROM AUTHOR]
- Published
- 2022
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14. COMPARISON OF PHYLOGENIC TREE AND GENE SEQUENCE OF SALMONELLA ENTERITIDIS ISOLATED FROM DIFFERENT BIRDS.
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Ghada, O., El-demerdash, Amr, Mahmoud, E. M., yahia, Nahed, and Roshdy, Heba.
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SALMONELLA enteritidis ,SALMONELLA typhimurium ,SALMONELLA enterica ,SALMONELLA ,MULTIDRUG resistance ,BIRD mortality ,AVIAN anatomy ,BONE marrow - Abstract
Copyright of Egyptian Poultry Science Journal is the property of Egyptian Poultry Science Association and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
- Published
- 2021
15. Investigating the structure--activity relationship of marine natural polyketides as promising SARSCoV- 2 main protease inhibitors.
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El-Demerdash, Amr, Al-Karmalawy, Ahmed A., Aziz, Tarek Mohamed Abdel, Elhady, de Sameh S., Darwishg, Khaled M., and Hassan, Ahmed H. E.
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- 2021
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16. Animal versus human research reporting guidelines impacts: literature analysis reveals citation count bias.
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Wai Kan Yeung, Andy, Dongdong Wang, El-Demerdash, Amr, Horbanczuk, Olaf K., Das, Niranjan, Pirgozliev, Vasil, Lucarini, Massimo, Durazzo, Alessandra, Souto, Eliana B., Santini, Antonello, Devkota, Hari Prasad, Uddin, Md. Sahab, Echeverría, Javier, El Bairi, Khalid, Leszczynski, Paweł, Hiroaki Taniguchi, Jóźwik, Artur, Strzałkowska, Nina, Sieroń, Dominik, and Horbańczuk, Jarosław Olav
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HUMAN experimentation ,CITATION analysis ,ONLINE databases ,LABORATORY animals ,INTERNET searching ,ELECTRONIC journals - Abstract
The present study evaluated for the first time citation-impacts of human research reporting guidelines in comparison to their animal version counterparts. Re-examined and extended also were previous findings indicating that a research reporting guideline would be cited more for its versions published in journals with higher Impact Factors, compared to its duplicate versions published in journals with lower Impact Factors. The two top-ranked reporting guidelines listed in the Equator Network website (http://www.equator-network.org/) were CONSORT 2010, for parallel-group randomized trials; and STROBE, for observational studies. These two guidelines had animal study versions, REFLECT and STROBE-Vet, respectively. Together with ARRIVE, these five guidelines were subsequently searched in the Web of Science Core Collection online database to record their journal metrics and citation data. Results found that association between citation rates and journal Impact Factors existed for CONSORT guideline set for human studies, but not for STROBE or their counterparts set for animal studies. If Impact Factor was expressed in terms of journal rank percentile, no association was found except for CONSORT. Guidelines for human studies were much more cited than animal research guidelines, with the CONSORT 2010 and STROBE guidelines being cited 27.1 and 241.0 times more frequently than their animal version counterparts, respectively. In conclusion, while the journal Impact Factor is of importance, other important publishing features also strongly affect scientific manuscript visibility, represented by citation rate. More effort should be invested to improve the visibility of animal research guidelines. [ABSTRACT FROM AUTHOR]
- Published
- 2021
17. Short‐Cut Bio‐Inspired Synthesis of Tricyclic Guanidinic Motifs of Crambescidins and Batzelladines Marine Alkaloids.
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El‐Demerdash, Amr, Ermolenko, Ludmila, Gros, Emmanuelle, Retailleau, Pascal, Thanh, Binh Nguyen, Gauvin‐Bialecki, Anne, and Al‐Mourabit, Ali
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GUANIDINES ,NATURAL products ,GUANIDINE ,STEREOISOMERS - Abstract
We report a convenient short synthesis of tricyclic guanidine‐containing natural products model featuring four‐component reaction between 2,5‐dimethoxytetrahydrofuran, 2‐aminopyrimidine and two acylacetic or benzoylacetic acids. A synthetic route combining the Robinson–Schöepf bioinspired strategy and biomechanistic analysis of the crambescidin and batzelladine alkaloids family. An application of this strategy to the synthesis of two unnatural stereoisomers of merobatzelladine B is described from the protected guanidine in the form of aminopyrimidine. [ABSTRACT FROM AUTHOR]
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- 2020
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18. Synthesis and biological evaluation of some heterocyclic scaffolds based on the multifunctional N‐(4‐acetylphenyl)‐2‐chloroacetamide.
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Abdel‐Latif, Ehab, Fahad, Mustafa M., El‐Demerdash, Amr, and Ismail, Mohamed A.
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BIOSYNTHESIS ,THIOSEMICARBAZONES ,VILSMEIER reagents ,SUBSTITUTION reactions ,ACETAMIDE derivatives ,CONDENSATION reactions - Abstract
The chloroacetamide derivative, 1, was used as a versatile precursor for the synthesis of various types of N‐aryl‐2‐(benzothiazol‐2‐ylthio)acetamide derivatives. The reaction of 1 with 2‐mercaptobenzothiazole followed by condensation reaction of the produced sulfide with phenylhydrazine, 2‐cyanoacetohydrazide, and/or thiosemicarbazide furnished the conforming condensation products, 4, 7, and 10, respectively. Treatment of the phenylhydrazone product, 4, with Vilsmeier formylation reagent (POCl3/DMF) yielded the corresponding 4‐formylpyrazole derivative, 5. The thiosemicarbazone product, 10, was reacted with ethyl bromoacetate to furnish the thiazolin‐4‐one derivative, 11. The substitution reactions of chloroacetamide derivative, 1, with 2‐mercapto‐4,6‐dimethylnicotinonitrile and 6‐amino‐2‐mercaptopyrimidin‐4‐ol, were explored to identify the sulfide products, 14 and 17. Cyclization of 14 into its corresponding thieno[2,3‐b]pyridine compound, 15, was performed using sodium ethoxide. The thiosemicarbazone, 10, and sulfide derivative, 14, were found to be the most potent antibacterial compounds against Escherichia coli and Staphylococcus aureus, exhibiting growth inhibitory activities of 80.8% and 91.7%, respectively. Moreover, the thiosemicarbazone, 10, displayed the most significant antioxidant activity with inhibitory activity of 82.6%, which comes close to the antioxidant activity of L‐ascorbic acid. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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19. Utilization of 5‐Chloro‐2‐(cyanoacetamido)pyridines in the Synthesis of Biologically Active Heterocyclic Hybrids.
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Abdel‐Latif, Ehab, Alashhab, Rabia E., El‐Demerdash, Amr, and Ismail, Mohamed A.
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VITAMIN C ,STAPHYLOCOCCUS aureus ,ESCHERICHIA coli ,DRUG standards ,AMPICILLIN ,PYRIDINE derivatives - Abstract
A simple synthesis for a series of chloropyridine derivatives incorporating heterocyclic hybrids has been accomplished. The key reaction involving employment of 5‐chloro‐2‐(cyanoacetamido)pyridines 3 in the synthesis of chloropyridinyl‐pyridone, chloropyridinyl‐pyrazole, chloropyridinyl‐thiazole and chloropyridinyl‐thiophene hybrids. The newly synthesized heterocycles were evaluated for their antioxidant and antibacterial activities against Gram‐positive and Gram‐negative bacterial strains. 3‐Amino‐N‐(3,5‐dichloropyridin‐2‐yl)‐1H‐pyrazole‐4‐carboxamide (12 b) was found to be the most potent compound against Escherichia coli and Staphylococcus aureus exhibiting inhibition percent of 92.3 % and 100 %, respectively, when compared to the standard drug ampicillin. Moreover, compound 12 b displayed the most significant antioxidant activity with percent inhibition 87.8 % which is close to the antioxidant activity of ascorbic acid. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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20. Berberine, a popular dietary supplement for human and animal health: Quantitative research literature analysis – a review.
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Andy Wai Kan Yeung, Orhan, Ilkay Erdogan, Aggarwal, Bharat Bhushan, Battino, Maurizio, Belwal, Tarun, Bishayee, Anupam, Daglia, Maria, Devkota, Hari Prasad, El-Demerdash, Amr, Balacheva, Aneliya A., Georgieva, Maya G., Guptal, Vijai Kumar, Horbańczuk, Jarosław Olav, Jóźwik, Artur, Mozos, Ioana, Nabavi, Seyed Mohammad, Pittala, Valeria, Feder-Kubis, Joanna, Silva, Ana Sanches, and Sheridan, Helen
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DIETARY supplements ,BERBERINE ,QUANTITATIVE research ,ANIMAL health ,MOLECULAR biology ,ALZHEIMER'S disease ,ISOQUINOLINE alkaloids - Abstract
Berberine is an alkaloid with a wide range of reported beneficial health effects. The current work provides an extensive literature analysis on berberine. Bibliometric data were identified by means of the search string TOPIC=(“berberin*” OR “umbellatine*”), which yielded 5,547 publications indexed in the Web of Science Core Collection electronic database. The VOSviewer software generated bubble maps to visualize semantic terms with citation results. The ratio of original articles to reviews was 13.6:1. The literature has been growing more quickly since the 2010s. Major contributing countries were China, the United States, India, Japan, and South Korea. Most of the publications appeared in journals specialized in pharmacology pharmacy, biochemistry molecular biology, chemistry, and plant science. Some of the frequently mentioned chemicals/chemical classes were alkaloid, palmatine, jatrorrhizine, coptisine, isoquinoline, and sanguinarine. The prevalent medical conditions under investigation included Alzheimer’s disease, cancer, diabetes, and obesity. [ABSTRACT FROM AUTHOR]
- Published
- 2020
21. Dietary natural products and their potential to influence health and disease including animal model studies.
- Author
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Wai Kan Yeung, Andy, Aggarwal, Bharat Bhushan, Barreca, Davide, Battino, Maurizio, Belwal, Tarun, Horbańczuk, Olaf K., Berindan-Neagoe, Ioana, Bishayee, Anupam, Daglia, Maria, Devkota, Hari Prasad, Echeverría, Javier, El-Demerdash, Amr, Orhan, Ilkay Erdogan, Godfrey, Keith M., Gupta, Vijai Kumar, Horbańczuk, Jarosław O., Modliński, Jacek A., Huber, Lukas A., Huminiecki, Lukasz, and Jóźwik, Artur
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BIOACTIVE compounds ,NATURAL products ,FOOD science ,ANIMAL models in research ,CITATION analysis ,BIBLIOMETRICS - Abstract
Although biological and pharmacological effects of dietary natural products have been intensively studied, there has been no bibliometric analysis performed on this research field up to now. The current study has aimed to identify and analyze the manuscripts on dietary natural products and their potential to influence health and disease including studies using animal models. Data, including words from titles and abstracts, publication and citation data, have been extracted from Web of Science database and analyzed by the VOSviewer software. Our search has yielded 1,014 manuscripts. The ratio of original articles to reviews was identified to be 1.5:1. Over half of the manuscripts have been published since 2010. The manuscripts have been contributed by 4,301 authors from 1,445 organizations in 76 countries/territories and published in 499 journals. The results from the current study point out that scientific research focusing on the potential of dietary natural products to affect health and disease status (including animal model studies) is expanding, and suggests an increasing significance of this scientific area. With the progressive development and improvement of animal studies, it should be expected that animal models of different human diseases (especially civilization ones) would be an integral part of the research for the evaluation of pharmaceuticals originated from dietary natural products like plants or plant materials. Moreover, natural products can also be fed to animals to improve the quality of animal products, with numerous resulting functional effects. [ABSTRACT FROM AUTHOR]
- Published
- 2018
22. Unguiculins A-C: cytotoxic bis-guanidine alkaloids from the French Polynesian sponge, Monanchora n. sp.
- Author
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El-Demerdash, Amr, Moriou, Céline, Martin, Marie-Thérèse, Petek, Sylvain, Debitus, Cécile, and Al-Mourabit, Ali
- Abstract
Two new acyclic bis-guanidine alkaloids, unguiculins B-C (2–3), were isolated from a French Polynesian sponge Monanchora n. sp. together with the known compound unguiculin A (1). Their structures were established by spectroscopic data interpretation and comparison with the literature. Unguiculins A-C displayed antiproliferative and cytotoxic efficacy against several human cancer cells with IC
50 values in the micromolar range. [ABSTRACT FROM AUTHOR]- Published
- 2018
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23. Batzella, Crambe and Monanchora: Highly Prolific Marine Sponge Genera Yielding Compounds with Potential Applications for Cancer and Other Therapeutic Areas.
- Author
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El-Demerdash, Amr, Atanasov, Atanas G., Bishayee, Anupam, Abdel-Mogib, Mamdouh, Hooper, John N. A., and Al-Mourabit, Ali
- Abstract
Pyrroloquinoline and guanidine-derived alkaloids present distinct groups of marine secondary metabolites with structural diversity that displayed potentialities in biological research. A considerable number of these molecular architectures had been recorded from marine sponges belonging to different marine genera, including Batzella, Crambe, Monanchora, Clathria, Ptilocaulis and New Caledonian starfishes Fromia monilis and Celerina heffernani. In this review, we aim to comprehensively cover the chemodiversity and the bioactivities landmarks centered around the chemical constituents exclusively isolated from these three marine genera including Batzella, Crambe and Monanchora over the period 1981-2017, paying a special attention to the polycyclic guanidinic compounds and their proposed biomimetic landmarks. It is concluded that these marine sponge genera represent a rich source of novel compounds with potential applications for cancer and other therapeutic areas. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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24. Lycopene: total-scale literature landscape analysis of a valuable nutraceutical with numerous potential applications in the promotion of human and animal health.
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Yeung, Andy Wai Kan, Choudhary, Neeraj, Tewari, Devesh, El-Demerdash, Amr, Tomczyk, Michał, Das, Niranjan, Pirgozliev, Vasil, Lucarini, Massimo, Durazzo, Alessandra, Souto, Eliana B., Santini, Antonello, Devkota, Hari Prasad, Uddin, Md. Sahab, Echeverría, Javier, Dongdong Wang, Ren-You Gan, Brnčić, Mladen, Kalfin, Reni E., De, Ronita, and Cenanovic, Merisa
- Subjects
LYCOPENE ,ANIMAL health ,BETA carotene ,CAROTENES ,CARDIOVASCULAR diseases ,PROSTATE cancer ,FUNCTIONAL foods - Abstract
Lycopene intake from tomatoes and other food sources has multiple potential health benefits. This report aimed to evaluate the current research literature on lycopene concerning human and animal health. The electronic Web of Science Core Collection database was searched with (lycopene*) AND (health* OR illness* OR disease* OR medic* OR pharma* OR drug* OR therap*). The resulted 3972 papers were analyzed with the aid of bibliometric software. Besides the United States, the lycopene papers received global contributions, particularly from China, Italy, India, and Spain. Examples of frequently mentioned chemicals/chemical classes were carotenoid, beta carotene, alpha carotene, beta cryptoxanthin, and alpha tocopherol. Examples of frequently mentioned medical conditions were prostate cancer, cardiovascular disease, and obesity. Published scientific articles reveal the diverse potential of lycopene in prompting human and animal health, and the knowledge on the bioactivities of this phytochemical is expected to further grow in the future. [ABSTRACT FROM AUTHOR]
- Published
- 2022
25. Quercetin: total-scale literature landscape analysis of a valuable nutraceutical with numerous potential applications in the promotion of human and animal health - a review.
- Author
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Wai Kan Yeung, Andy, Choudhary, Neeraj, Tewari, Devesh, El-Demerdash, Amr, Horbanczuk, Olaf K., Das, Niranjan, Pirgozliev, Vasil, Lucarini, Massimo, Durazzo, Alessandra, Souto, Eliana B., Santini, Antonello, Devkota, Hari Prasad, Uddin, Md. Sahab, Echeverría, Javier, Dongdong Wang, Ren-You Gan, Brnčić, Mladen, Kalfin, Reni E., Tzvetkov, Nikolay T., and Jóźwik, Artur
- Subjects
ANIMAL health ,QUERCETIN ,ALZHEIMER'S disease ,FUNCTIONAL foods - Abstract
Numerous investigations on quercetin have revealed that it effectively treats and prevents different diseases, acting as an anti-inflammatory, anti-bacterial, anti-proliferative, anti-atherogenic, anticoagulative, antioxidant, antidiabetic agent, etc. This work aimed to analyze the present research literature on quercetin in the context of human and animal health. The Web of Science Core Collection electronic database was searched with (quercetin*) AND (health* OR illness* OR disease* OR medic* OR pharma* OR drug* OR therap*). The resulted 15685 papers were bibliometrically evaluated with the aid of VOSviewer software. Besides the United States, the quercetin papers received global contributions, particularly from Asian countries such as China, India, and South Korea. Examples of frequently mentioned chemicals/chemical classes were flavonoid, kaempferol, rutin, polyphenol, and catechin. Examples of frequently mentioned medical conditions were cancer, Alzheimer's disease, and atherosclerosis. There are numerous reported beneficial effects of quercetin on human and animal health, which warrants further research for corroboration, understanding mechanism of action, and practical application. [ABSTRACT FROM AUTHOR]
- Published
- 2021
26. Apple polyphenols in human and animal health.
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Wai Kan Yeung, Andy, Tzvetkov, Nikolay T., El-Demerdash, Amr, Horbanczuk, Olaf K., Das, Niranjan, Pirgozliev, Vasil, Lucarini, Massimo, Durazzo, Alessandra, Souto, Eliana B., Santini, Antonello, Devkota, Hari Prasad, Uddin, Md. Sahab, Echeverría, Javier, Dongdong Wang, Ren-You Gan, Brnčić, Mladen, Kalfin, Reni E., Tancheva, Lyubka P., Tewari, Devesh, and Berindan-Neagoe, Ioana
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PLANT polyphenols ,ANIMAL health ,APPLE varieties ,POLYPHENOLS ,CARDIOVASCULAR diseases ,PHENOLS ,ALZHEIMER'S disease - Abstract
Apples contain substantial amounts of polyphenols, and diverse phenolics - mainly flavonoids and phenolic acids, have been identified in their flesh and skins. This work aimed to analyze the overall landscape of the research literature published to date on apple phenolic compounds in the context of human and animal health. The Web of Science Core Collection electronic database was queried with (apple* polyphenol*) AND (health* OR illness* OR disease* OR medic* OR pharma*) to identify relevant papers covering these words and their derivatives in the titles, abstracts, and keywords. The resulted 890 papers were bibliometrically analyzed. The VOSviewer software was utilized to produce term maps that illustrate how the frequent phrases fared in terms of publication and citation data. The apple polyphenol papers received global contributions, particularly from China, Italy, the United States, Spain, and Germany. Examples of frequently mentioned chemicals/chemical classes are quercetin, anthocyanin, catechin, epicatechin, and flavonol, while examples of frequently mentioned medical conditions are cardiovascular disease, atherosclerosis, diabetes, Alzheimer's disease, and obesity. The potential health benefits of apple polyphenols on humans and animals are diverse and warrant further study. [ABSTRACT FROM AUTHOR]
- Published
- 2021
27. Marine Brominated Tyrosine Alkaloids as Promising Inhibitors of SARS-CoV-2.
- Author
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El-Demerdash, Amr, Hassan, Afnan, Abd El-Aziz, Tarek Mohamed, Stockand, James D., and Arafa, Reem K.
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SARS-CoV-2 ,TYROSINE ,VACCINE hesitancy ,MOLECULAR dynamics ,PROTEIN-tyrosine kinases ,ISOQUINOLINE alkaloids ,PROTEIN-protein interactions ,MARINE toxins - Abstract
There have been more than 150 million confirmed cases of SARS-CoV-2 since the beginning of the pandemic in 2019. By June 2021, the mortality from such infections approached 3.9 million people. Despite the availability of a number of vaccines which provide protection against this virus, the evolution of new viral variants, inconsistent availability of the vaccine around the world, and vaccine hesitancy, in some countries, makes it unreasonable to rely on mass vaccination alone to combat this pandemic. Consequently, much effort is directed to identifying potential antiviral treatments. Marine brominated tyrosine alkaloids are recognized to have antiviral potential. We test here the antiviral capacity of fourteen marine brominated tyrosine alkaloids against five different target proteins from SARS-CoV-2, including main protease (M
pro ) (PDB ID: 6lu7), spike glycoprotein (PDB ID: 6VYB), nucleocapsid phosphoprotein (PDB ID: 6VYO), membrane glycoprotein (PDB ID: 6M17), and non-structural protein 10 (nsp10) (PDB ID: 6W4H). These marine alkaloids, particularly the hexabrominated compound, fistularin-3, shows promising docking interactions with predicted binding affinities (S-score = −7.78, −7.65, −6.39, −6.28, −8.84 Kcal/mol) for the main protease (Mpro ) (PDB ID: 6lu7), spike glycoprotein (PDB ID: 6VYB), nucleocapsid phosphoprotein (PDB ID: 6VYO), membrane glycoprotein (PDB ID: 6M17), and non-structural protein 10 (nsp10) (PDB ID: 6W4H), respectively, where it forms better interactions with the protein pockets than the native interaction. It also shows promising molecular dynamics, pharmacokinetics, and toxicity profiles. As such, further exploration of the antiviral properties of fistularin-3 against SARS-CoV-2 is merited. [ABSTRACT FROM AUTHOR]- Published
- 2021
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28. Bioactive Bromotyrosine Derivatives from the Pacific Marine Sponge Suberea clavata (Pulitzer-Finali, 1982).
- Author
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Moriou, Céline, Lacroix, Damien, Petek, Sylvain, El-Demerdash, Amr, Trepos, Rozenn, Leu, Tinihauarii Mareva, Florean, Cristina, Diederich, Marc, Hellio, Claire, Debitus, Cécile, Al-Mourabit, Ali, and Baker, Bill J.
- Abstract
Chemical investigation of the South-Pacific marine sponge Suberea clavata led to the isolation of eight new bromotyrosine metabolites named subereins 1–8 (2–9) along with twelve known co-isolated congeners. The detailed configuration determination of the first representative major compound of this family 11-epi-fistularin-3 (11R,17S) (1) is described. Their chemical characterization was achieved by HRMS and integrated 1D and 2D NMR (nuclear magnetic resonance) spectroscopic studies and extensive comparison with literature data. For the first time, a complete assignment of the absolute configurations for stereogenic centers C-11/17 of the known members (11R,17S) 11-epi-fistularin-3 (1) and 17-deoxyfistularin-3 (10) was determined by a combination of chemical modifications, Mosher's technology, and ECD spectroscopy. Consequently, the absolute configurations of all our new isolated compounds 2–9 were determined by the combination of NMR, Mosher's method, ECD comparison, and chemical modifications. Interestingly, compounds 2–7 were obtained by chemical transformation of the major compound 11-epi-fistularin-3 (1). Evaluation for acetylcholinesterase inhibition (AChE), DNA methyltransferase 1 (DNMT1) modulating activity and antifouling activities using marine bacterial strains are also presented. [ABSTRACT FROM AUTHOR]
- Published
- 2021
- Full Text
- View/download PDF
29. Comprehensive Virtual Screening of the Antiviral Potentialities of Marine Polycyclic Guanidine Alkaloids against SARS-CoV-2 (COVID-19).
- Author
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El-Demerdash, Amr, Metwaly, Ahmed M., Hassan, Afnan, Abd El-Aziz, Tarek Mohamed, Elkaeed, Eslam B., Eissa, Ibrahim H., Arafa, Reem K., Stockand, James D., and Medina-Franco, José L.
- Subjects
COVID-19 ,SARS-CoV-2 ,COVID-19 pandemic ,GUANIDINES ,GUANIDINE ,BLOOD proteins ,ALKALOIDS ,ISOQUINOLINE alkaloids - Abstract
The huge global expansion of the COVID-19 pandemic caused by the novel SARS-corona virus-2 is an extraordinary public health emergency. The unavailability of specific treatment against SARS-CoV-2 infection necessitates the focus of all scientists in this direction. The reported antiviral activities of guanidine alkaloids encouraged us to run a comprehensive in silico binding affinity of fifteen guanidine alkaloids against five different proteins of SARS-CoV-2, which we investigated. The investigated proteins are COVID-19 main protease (M
pro ) (PDB ID: 6lu7), spike glycoprotein (PDB ID: 6VYB), nucleocapsid phosphoprotein (PDB ID: 6VYO), membrane glycoprotein (PDB ID: 6M17), and a non-structural protein (nsp10) (PDB ID: 6W4H). The binding energies for all tested compounds indicated promising binding affinities. A noticeable superiority for the pentacyclic alkaloids particularly, crambescidin 786 (5) and crambescidin 826 (13) has been observed. Compound 5 exhibited very good binding affinities against Mpro (ΔG = −8.05 kcal/mol), nucleocapsid phosphoprotein (ΔG = −6.49 kcal/mol), and nsp10 (ΔG = −9.06 kcal/mol). Compound 13 showed promising binding affinities against Mpro (ΔG = −7.99 kcal/mol), spike glycoproteins (ΔG = −6.95 kcal/mol), and nucleocapsid phosphoprotein (ΔG = −8.01 kcal/mol). Such promising activities might be attributed to the long ω-fatty acid chain, which may play a vital role in binding within the active sites. The correlation of c Log P with free binding energies has been calculated. Furthermore, the SAR of the active compounds has been clarified. The Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) studies were carried out in silico for the 15 compounds; most examined compounds showed optimal to good range levels of ADMET aqueous solubility, intestinal absorption and being unable to pass blood brain barrier (BBB), non-inhibitors of CYP2D6, non-hepatotoxic, and bind plasma protein with a percentage less than 90%. The toxicity of the tested compounds was screened in silico against five models (FDA rodent carcinogenicity, carcinogenic potency TD50 , rat maximum tolerated dose, rat oral LD50 , and rat chronic lowest observed adverse effect level (LOAEL)). All compounds showed expected low toxicity against the tested models. Molecular dynamic (MD) simulations were also carried out to confirm the stable binding interactions of the most promising compounds, 5 and 13, with their targets. In conclusion, the examined 15 alkaloids specially 5 and 13 showed promising docking, ADMET, toxicity and MD results which open the door for further investigations for them against SARS-CoV-2. [ABSTRACT FROM AUTHOR]- Published
- 2021
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30. Cover Feature: Short‐Cut Bio‐Inspired Synthesis of Tricyclic Guanidinic Motifs of Crambescidins and Batzelladines Marine Alkaloids (Eur. J. Org. Chem. 35/2020).
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El‐Demerdash, Amr, Ermolenko, Ludmila, Gros, Emmanuelle, Retailleau, Pascal, Thanh, Binh Nguyen, Gauvin‐Bialecki, Anne, and Al‐Mourabit, Ali
- Subjects
ALKALOIDS ,BIOMIMETIC synthesis ,SPONGES (Invertebrates) - Published
- 2020
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31. Chemical Diversity and Biological Activities of Meroterpenoids from Marine Derived-Fungi: A Comprehensive Update.
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El-Demerdash, Amr, Kumla, Decha, and Kijjoa, Anake
- Abstract
Meroterpenoids are a class of hybrid natural products, partially derived from a mixed terpenoid pathway. They possess remarkable structural features and relevant biological and pharmacological activities. Marine-derived fungi are a rich source of meroterpenoids featuring structural diversity varying from simple to complex molecular architectures. A combination of a structural variability and their myriad of bioactivities makes meroterpenoids an interesting class of naturally occurring compounds for chemical and pharmacological investigation. In this review, a comprehensive literature survey covering the period of 2009–2019, with 86 references, is presented focusing on chemistry and biological activities of various classes of meroterpenoids isolated from fungi obtained from different marine hosts and environments. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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32. Chemical Diversity and Biological Activities of Marine Sponges of the Genus Suberea: A Systematic Review.
- Author
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El-Demerdash, Amr, Atanasov, Atanas G., Horbanczuk, Olaf K., Tammam, Mohamed A., Abdel-Mogib, Mamdouh, Hooper, John N. A., Sekeroglu, Nazim, Al-Mourabit, Ali, and Kijjoa, Anake
- Abstract
Marine natural products (MNPs) continue to be in the spotlight in the global drug discovery endeavor. Currently, more than 30,000 structurally diverse secondary metabolites from marine sources have been isolated, making MNPs a profound, renewable source to investigate novel drug compounds. Marine sponges of the genus Suberea (family: Aplysinellidae) are recognized as producers of bromotyrosine derivatives, which are considered distinct chemotaxonomic markers for the marine sponges belonging to the order Verongida. This class of compounds exhibits structural diversity, ranging from simple monomeric molecules to more complex molecular scaffolds, displaying a myriad of biological and pharmacological potentialities. In this review, a comprehensive literature survey covering the period of 1998–2018, focusing on the chemistry and biological/pharmacological activities of marine natural products from marine sponges of the genus Suberea, with special attention to the biogenesis of the different skeletons of halogenated compounds, is presented. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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33. Chemistry and Biological Activities of the Marine Sponges of the Genera Mycale (Arenochalina), Biemna and Clathria.
- Author
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El-Demerdash, Amr, Tammam, Mohamed A., Atanasov, Atanas G., Hooper, John N. A., Al-Mourabit, Ali, and Kijjoa, Anake
- Abstract
Over the past seven decades, particularly since the discovery of the first marine-derived nucleosides, spongothymidine and spongouridine, from the Caribbean sponge Cryptotethya crypta in the early 1950s, marine natural products have emerged as unique, renewable and yet under-investigated pools for discovery of new drug leads with distinct structural features, and myriad interesting biological activities. Marine sponges are the most primitive and simplest multicellular animals, with approximately 8900 known described species, although more than 15,000 species are thought to exist worldwide today. These marine organisms potentially represent the richest pipeline for novel drug leads. Mycale (Arenochalina) and Clathria are recognized marine sponge genera belonging to the order Poecilosclerida, whereas Biemna was more recently reclassified, based on molecular genetics, as a new order Biemnida. Together, these sponge genera contribute to the production of physiologically active molecular entities with diverse structural features and a wide range of medicinal and therapeutic potentialities. In this review, we provide a comprehensive insight and up-to-date literature survey over the period of 1976–2018, focusing on the chemistry of the isolated compounds from members of these three genera, as well as their biological and pharmacological activities, whenever available. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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34. Bioactive Bromotyrosine-Derived Alkaloids from the Polynesian Sponge Suberea ianthelliformis.
- Author
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Moriou, Céline, Al-Mourabit, Ali, El-Demerdash, Amr, Toullec, Jordan, Petek, Sylvain, Debitus, Cécile, Lecchini, David, Besson, Marc, Soulet, Stéphanie, and Schmitt, Nelly
- Abstract
Herein, we describe the isolation and spectroscopic identification of eight new tetrabrominated tyrosine alkaloids
2 –9 from the Polynesian spongeSuberea ianthelliformis , along with known major compound psammaplysene D (1 ),N ,N -dimethyldibromotyramine, 5-hydroxy xanthenuric acid, and xanthenuric acid. Cytotoxicity and acetylcholinesterase inhibition activities were evaluated for some of the isolated metabolites. They exhibited moderate antiproliferative activity against KB cancer cell lines, but psammaplysene D (1 ) displayed substantial cytotoxicity as well as acetylcholinesterase inhibition with IC50 values of 0.7 μM and 1.3 μM, respectively. [ABSTRACT FROM AUTHOR]- Published
- 2018
- Full Text
- View/download PDF
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