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Ana Lúcia Tasca Gois Ruiz - One of the best experts on this subject based on the ideXlab platform.
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Antiproliferative Activity and chemical constituents of lonchocarpus cultratus fabaceae
Natural Product Research, 2019Co-Authors: Emanuelle M B M Da Silva Landim, Ana Lúcia Tasca Gois Ruiz, J Carvalho, Armando M Pomini, Lindamir Hernandez Pastorini, Silvana Maria De Oliveira SantinAbstract:The aerial parts of L. cultratus were submitted to a phytopharmacological investigation in order to isolate and identify the major secondary metabolites and evaluate its crude extract, fractions and isolated compounds for Antiproliferative Activity. Seven compounds were isolated and identified as the chalcones 2',4'-dihydroxy-5'-prenylchalcone (1) and isocordoin (2), the flavanone 8-prenylpinocembrin (3), the alkaloid 4-hydroxy-N-methylproline (4), the triterpenes lupeol and lupenone. These compounds were identified by nuclear magnetic resonance of 1H and 13C data in comparison with literature. Hexanic fraction and chalcone 2',4'-dihydroxy-5'-prenylchalcone showed potent results against human cancer cell lines tested.
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Antiproliferative Activity of synthetic fatty acid amides from renewable resources
Bioorganic & Medicinal Chemistry, 2015Co-Authors: Daiane Dos S Santos, Caroline Da Ros Montes Doca, Carolina R L Hack, Tamara G M Treptow, Marieli Oliveira Rodrigues, Debora Barbosa Vendraminicosta, Ana Lúcia Tasca Gois Ruiz, Luciana A Piovesan, João Ernesto De Carvalho, Marcelo Montes G DocaAbstract:Abstract In the work, the in vitro Antiproliferative Activity of a series of synthetic fatty acid amides were investigated in seven cancer cell lines. The study revealed that most of the compounds showed Antiproliferative Activity against tested tumor cell lines, mainly on human glioma cells (U251) and human ovarian cancer cells with a multiple drug-resistant phenotype (NCI-ADR/RES). In addition, the fatty methyl benzylamide derived from ricinoleic acid (with the fatty acid obtained from castor oil, a renewable resource) showed a high selectivity with potent growth inhibition and cell death for the glioma cell line—the most aggressive CNS cancer.
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synthesis and Antiproliferative Activity of 8 hydroxyquinoline derivatives containing a 1 2 3 triazole moiety
European Journal of Medicinal Chemistry, 2014Co-Authors: Luiza Baptista De Oliveira Freitas, Ana Lúcia Tasca Gois Ruiz, João Ernesto De Carvalho, Thiago F Borgati, Rossimiriam Pereira De Freitas, Gabriela M Marchetti, Elaine F F Da Cunha, Teodorico C Ramalho, Rosemeire B AlvesAbstract:Abstract Twelve novel 8-hydroxyquinoline derivatives were synthesized with good yields by performing copper-catalyzed Huisgen 1,3-dipolar cycloaddition (“click” reaction) between an 8- O -alkylated-quinoline containing a terminal alkyne and various aromatic or protected sugar azides. These compounds were evaluated in vitro for their Antiproliferative Activity on various cancer cell types. Protected sugar derivative 16 was the most active compound in the series, exhibiting potent Antiproliferative Activity and high selectivity toward ovarian cancer cells (OVCAR-03, GI 50 −1 ); this derivative was more active than the reference drug doxorubicin (OVCAR-03, GI 50 = 0.43 μg mL −1 ). In structure–Activity relationship (SAR) studies, the physico-chemical parameters of the compounds were evaluated and docking calculations were performed for the α-glucosidase active site to predict the possible mechanism of action of this series of compounds.
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antioxidative and in vitro Antiproliferative Activity of arctium lappa root extracts
BMC Complementary and Alternative Medicine, 2011Co-Authors: Fabricia De Souza Predes, Ana Lúcia Tasca Gois Ruiz, J Carvalho, Mary Ann Foglio, Heidi DolderAbstract:Arctium lappa, known as burdock, is widely used in popular medicine for hypertension, gout, hepatitis and other inflammatory disorders. Pharmacological studies indicated that burdock roots have hepatoprotective, anti-inflammatory, free radical scavenging and Antiproliferative activities. The aim of this study was to evaluate total phenolic content, radical scavenging Activity by DPPH and in vitro Antiproliferative Activity of different A. lappa root extracts. Hot and room temperature dichloromethanic, ethanolic and aqueous extracts; hydroethanolic and total aqueous extract of A. lappa roots were investigated regarding radical scavenging Activity by DPPH, total phenolic content by Folin-Ciocalteau method and Antiproliferative in vitro Activity was evaluated in human cancer cell lines. The hydroethanolic extract analyzed by high-resolution electrospray ionization mass spectroscopy. Higher radical scavenging Activity was found for the hydroethanolic extract. The higher phenolic contents were found for the dichloromethane, obtained both by Soxhlet and maceration extraction and hydroethanolic extracts. The HRESI-MS demonstrated the presence of arctigenin, quercetin, chlorogenic acid and caffeic acid compounds, which were identified by comparison with previous data. The dichloromethane extracts were the only extracts that exhibited Activity against cancer cell lines, especially for K562, MCF-7 and 786-0 cell lines. The hydroethanolic extracts exhibited the strongest free radical scavenging Activity, while the highest phenolic content was observed in Soxhlet extraction. Moreover, the dichloromethanic extracts showed selective Antiproliferative Activity against K562, MCF-7 and 786-0 human cancer cell lines.
João Ernesto De Carvalho - One of the best experts on this subject based on the ideXlab platform.
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Antiproliferative Activity of walnut (Juglans regia L.) proteins and walnut protein hydrolysates
'Mary Ann Liebert Inc', 2017Co-Authors: Carrillo W., Ruiz, Ana Lucia, Gómez-ruiz, José Angel, João Ernesto De CarvalhoAbstract:Proteins from Juglans regia L. were isolated. Then, proteins were hydrolyzed with different enzymes. Antiproliferative Activity of proteins and of the protein hydrolysates of J. regia L. were evaluated using the sulforhodamine B method. Glutelin and prolamin proteins presented a high Antiproliferative Activity against cancer cells PC-3 (prostate) and K-562 (leukemia) with values of 43.9 and 84.4 μg/mL, respectively. The highest inhibitory effect observed was 50% at 0.25 μg/mL concentration in gastrointestinal digestion with pepsin and corolase pp in a dose-dependent manner against cancer cell UACC62 (melanoma). Pepsin hydrolysate showed inhibitory effects against cancer cell UACC62 (melanoma) with a concentration of 71.0 μg/mL. The effects were studied in a dose-dependent manner. The hydrolysate obtained with neutrase enzyme presented inhibitory effects against cancer cell UACC62 (melanoma) at a concentration of 25 μg/mL. Neither proteins nor protein hydrolysates presented cytotoxicity against normal cell assay VERO (epithelial).This study was supported with project number AGL2015-66886-R of Instituto de Investigación en Ciencias de la Alimentación, CIAL (CSIC-UAM), Madrid, Spain, Consolider Ingenio 2010 FUN-C-Food CSD2007-063, CYTED110AC0386 IBEROFUN, and CNPq (Brazil), and project 1373-2014-UTA, Universidad Técnica de Ambato. This work has been reviewed in the English edition by Emilio Labrador. W.C. thanks Comunidad Autónoma de Madrid for the research contract to complete his PhD and CYTED IBERFORUN for the grant of study interchange with Brazil.Peer reviewe
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Antiproliferative Activity of synthetic fatty acid amides from renewable resources
Bioorganic & Medicinal Chemistry, 2015Co-Authors: Daiane Dos S Santos, Caroline Da Ros Montes Doca, Carolina R L Hack, Tamara G M Treptow, Marieli Oliveira Rodrigues, Debora Barbosa Vendraminicosta, Ana Lúcia Tasca Gois Ruiz, Luciana A Piovesan, João Ernesto De Carvalho, Marcelo Montes G DocaAbstract:Abstract In the work, the in vitro Antiproliferative Activity of a series of synthetic fatty acid amides were investigated in seven cancer cell lines. The study revealed that most of the compounds showed Antiproliferative Activity against tested tumor cell lines, mainly on human glioma cells (U251) and human ovarian cancer cells with a multiple drug-resistant phenotype (NCI-ADR/RES). In addition, the fatty methyl benzylamide derived from ricinoleic acid (with the fatty acid obtained from castor oil, a renewable resource) showed a high selectivity with potent growth inhibition and cell death for the glioma cell line—the most aggressive CNS cancer.
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synthesis and Antiproliferative Activity of 8 hydroxyquinoline derivatives containing a 1 2 3 triazole moiety
European Journal of Medicinal Chemistry, 2014Co-Authors: Luiza Baptista De Oliveira Freitas, Ana Lúcia Tasca Gois Ruiz, João Ernesto De Carvalho, Thiago F Borgati, Rossimiriam Pereira De Freitas, Gabriela M Marchetti, Elaine F F Da Cunha, Teodorico C Ramalho, Rosemeire B AlvesAbstract:Abstract Twelve novel 8-hydroxyquinoline derivatives were synthesized with good yields by performing copper-catalyzed Huisgen 1,3-dipolar cycloaddition (“click” reaction) between an 8- O -alkylated-quinoline containing a terminal alkyne and various aromatic or protected sugar azides. These compounds were evaluated in vitro for their Antiproliferative Activity on various cancer cell types. Protected sugar derivative 16 was the most active compound in the series, exhibiting potent Antiproliferative Activity and high selectivity toward ovarian cancer cells (OVCAR-03, GI 50 −1 ); this derivative was more active than the reference drug doxorubicin (OVCAR-03, GI 50 = 0.43 μg mL −1 ). In structure–Activity relationship (SAR) studies, the physico-chemical parameters of the compounds were evaluated and docking calculations were performed for the α-glucosidase active site to predict the possible mechanism of action of this series of compounds.
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Synthesis and differential Antiproliferative Activity of Biginelli compounds against cancer cell lines: Monastrol, oxo-monastrol and oxygenated analogues.
Bioorganic chemistry, 2006Co-Authors: Dennis Russowsky, Rômulo Faria Santos Canto, Sérgio Augusto Antunes Sanches, Marcelo G. Montes D’oca, Ângelo De Fátima, Ronaldo A. Pilli, Luciana K. Kohn, Márcia Aparecida Antônio, João Ernesto De CarvalhoAbstract:Abstract The synthesis and differential Antiproliferative Activity of monastrol ( 1a ), oxo-monastrol ( 1b ) and eight oxygenated derivatives 3a , b – 6a , b on seven human cancer cell lines are described. For all evaluated cell lines, monastrol ( 1a ) was shown to be more active than its oxo-analogue, except for HT-29 cell line, suggesting the importance of the sulfur atom for the Antiproliferative Activity. Monastrol ( 1a ) and the thio-derivatives 3a , 4a and 6a displayed relevant Antiproliferative properties with 3,4-methylenedioxy derivative 6a being approximately more than 30 times more potent than monastrol ( 1a ) against colon cancer (HT-29) cell line.
Ling Peng - One of the best experts on this subject based on the ideXlab platform.
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n aryltriazole ribonucleosides with potent Antiproliferative Activity against drug resistant pancreatic cancer
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Yang Liu, Yi Xia, Yuting Fan, Alain Maggiani, Palma Rocchi, Juan L Iovanna, Ling PengAbstract:Novel N-aryltriazole nucleosides were synthesized via Cu-mediated C-N cross-coupling reaction starting with 3-aminotriazole ribonucleoside and various boronic acids. Two of them exhibited potent apoptosis-related Antiproliferative Activity against the drug-resistant pancreatic cancer cell line MiaPaCa-2, with an increased potency compared to gemcitabine, the reference treatment for pancreatic cancer. A preliminary SAR study suggests that the appended N-aryl moiety and the substituent at its para-position, as well as the ribose sugar component, contribute considerably to the observed Antiproliferative Activity.
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discovery of novel arylethynyltriazole ribonucleosides with selective and effective antiviral and Antiproliferative Activity
Journal of Medicinal Chemistry, 2009Co-Authors: Jinqiao Wan, Yang Liu, Yi Xia, Palma Rocchi, Juan L Iovanna, Menghua Wang, Jianhua Yao, Johan Neyts, Ling PengAbstract:Novel ethynyltriazole ribonucleosides were synthesized using a simple and efficient two-step procedure involving Sonogashira coupling and subsequent ammonolysis. Compounds 2f and 3o inhibited hepatitis C virus (HCV) replication efficiently, whereas compound 3f demonstrated potent apoptosis-induced Antiproliferative Activity against pancreatic cancer MiaPaCa-2 cells both in vitro and in vivo. Most interestingly, the notable selective antiviral and Antiproliferative activities were achieved respectively for 2f and 3f by modulating the ribose sugar moiety into deprotected and protected forms while retaining a similar trifluoromethylphenylethynyltriazole as the nucleobase. Preliminary structure−Activity relationship study revealed that not only the ribose moiety but also the CF3 group at the p-position of the phenyl ring and the rigid triple bond functionality contributed critically to the observed antiviral Activity of 2f against HCV and Antiproliferative Activity of 3f against pancreatic cancer. These two c...
Adam Opolski - One of the best experts on this subject based on the ideXlab platform.
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synthesis and Antiproliferative Activity of some 5 substituted 2 2 4 dihydroxyphenyl 1 3 4 thiadiazoles
European Journal of Medicinal Chemistry, 2006Co-Authors: Joanna Matysiak, Marta Switalska, Iwona Jaroszewicz, Anna Nasulewicz, Marzena Pelczynska, Adam OpolskiAbstract:Abstract A series of new 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles has been synthesised and evaluated for their Antiproliferative Activity. The compounds were prepared by the reaction of the sulphinylbis(2,4-dihydroxythiobenzoyl) (STB) wit hydrazides or carbazates. The panel substitution included alkyl, alkoxy, aryl and heteroaryl derivatives. The structures of compounds were identified from the elemental, IR, 1 H NMR and MS spectra analysis. The highest Antiproliferative Activity against the cells of human cancer lines for 2-(2,4-dihydroxyphenyl)- 5- (4-methoxybenzyloxy)-1,3,4-thiadiazole was found with ID 50 values comparable (HCV29T and SW707) or significantly lower (T47D) than for cisplatin applied as the reference compound. The influence of 5-substiution type of 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles on Antiproliferative Activity is discussed.
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Synthesis and Antiproliferative Activity in vitro of 2-aminobenzimidazole derivatives.
Farmaco, 2004Co-Authors: Nawrocka W, Joanna Wietrzyk, Anna Nasulewicz, Marzena Pelczynska, B. Sztuba, M. W. Kowalska, H. Liszkiewicz, Adam OpolskiAbstract:A novel series of Schiff bases 1–11, the derivatives of 2-aminobenzimidazole and substituted aromatic aldehydes, has been synthesised. Compounds 1–11 reduced by NaBH4 formed 2-benzylaminobenzimidazoles 12–21. 2-(o-Bromobenzylamino)benzimidazole (15) acylated by cinnamoyl chloride gave 2-(o-bromobenzylamino)-1-cinnamoylbenzimidazole (22). Long heating of 15 and 19 with p-nitrocinnamoyl or cinnamoyl chloride led to the formation of pyrimido[1,2-a]benzimidazol-4-ones 23 and 24. The structures of 1–24 were identified by the results of elemental analysis and their IR, 1H NMR and MS spectra. Among the compounds 1–24 evaluated for their Antiproliferative Activity in vitro, 16, 19, 20 and 22 exhibited cytotoxic Activity against the cells of human cancer cell lines, namely SW707 (rectal), HCV29T (bladder), A549 (lung) and T47D (breast cancer).
Fatma U Afifi - One of the best experts on this subject based on the ideXlab platform.
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chemodiversity and Antiproliferative Activity of the essential oil of schinus molle growing in jordan
Chemistry & Biodiversity, 2019Co-Authors: Nour H Aboalhaija, Oriana Awwad, Enam A Khalil, Reem Abbassi, Ismail F Abaza, Fatma U AfifiAbstract:The leaves and unripe and fully-grown fruits of Schinus molle were collected from three geographical regions of Jordan: Amman (the Mediterranean), Madaba (Irano-Turanean), and Sahab (Saharo-Arabian). The hydrodistilled volatile oils of fresh and dried leaves and fruits were analyzed by gas chromatography-mass spectrometry (GC/MS). The actual composition of the emitted volatiles was determined using Solid Phase Micro-Extraction (SPME). α- and β-Phellandrenes were the major components in all the analyzed samples. Quantitative differences were observed in the obtained essential oils (0.62-5.25 %). Additionally, cluster analysis was performed. Biologically, the Antiproliferative Activity of the essential oil, ethanol, and water extracts of the fruits and leaves was screened on Caco2, HCT116, MCF7, and T47D cell lines. The essential oil and ethanol extracts exhibited a dose-dependent inhibition of cell growth with IC50 ranging between 21 and 65 μg/mL. The water extract did not exhibit any Antiproliferative Activity against the investigated cell lines.
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volatile oil composition and Antiproliferative Activity of laurus nobilis origanum syriacum origanum vulgare and salvia triloba against human breast adenocarcinoma cells
Nutrition Research, 2010Co-Authors: Jelnar Z Alkalaldeh, Rana Abudahab, Fatma U AfifiAbstract:Medicinal plants and culinary herbs have gained importance in the last decade as cytotoxic and antitumor agents. We hypothesized that some of the commonly used spices with reported antimicrobial Activity might have Antiproliferative Activity. In the present study, selected spices used in Jordan were chemically analyzed and investigated for their Antiproliferative Activity to the adenocarcinoma of breast cell line (MCF7). The composition of the essential oils of Laurus nobilis L, Origanum syriacum L, Origanum vulgare L, and Salvia triloba L was analyzed by gas chromatography-mass spectrometry. The Antiproliferative activities of the hydrodistilled volatile oils and the crude ethanol and water extracts were evaluated using the sulphorhodamine B assay. 1,8-Cineol was the major constituent in the hydrodistilled oils of both plants, L nobilis and S triloba, with concentrations of 40.91% and 45.16%, respectively. The major constituent of O syriacum was the carvacrol (47.10%), whereas that of O vulgare was trans-sabinene hydrate (27.19%). The ethanol crude extracts of O syriacum, L nobilis, and S triloba showed Antiproliferative Activity to MCF7 with IC(50) values 6.40, 24.49, and 25.25 microg/mL, respectively. However, none of the hydrodistilled essential oils of the tested plant species or their aqueous extracts demonstrated cytotoxic Activity.
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Antiproliferative Activity of selected medicinal plants of jordan against a breast adenocarcinoma cell line mcf7
Scientia Pharmaceutica, 2007Co-Authors: Rana Abudahab, Fatma U AfifiAbstract:76 ethanolic extracts of medicinal herbs from the Jordanian flora, belonging to 67 species and 34 families, were evaluated for their Antiproliferative Activity on a breast cancer cell line (MCF7). The cells were cultured in RPMI 1640 medium and incubated with the extracts for 72 hours. Sulphorhodamine B (SRB) assay was used to test cytotoxicity. From the tested crude extracts, Inula graveolens, Salvia dominica, Conyza canadiensis and Achillea santolina showed potent Antiproliferative Activity and the Activity resided in the chloroform/ethanolic extracts. The most active plant was I. graveolens with an IC50 of 3.83 μg/ml. Phytochemical screening indicated the presence of flavonoids, terpenoids, and phenolics in all active extracts. These results indicate the possible potential use of medicinal plants from the Jordanian flora as antineoplastic agents.