scholarly journals Oxaliplatin Analogues with Carboxy Derivatives of Boldine with Enhanced Antioxidant Activity

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Marco Mellado ◽  
Carlos Jara ◽  
David Astudillo ◽  
Joan Villena ◽  
Patricio G. Reveco ◽  
...  

A new oxaliplatin analog [Pt(dach)(L5)] (1) was synthesized and characterized as a continuation of a study of the previously reported [Pt(dach)(L6)] (2), where dach = (1R,2R)-diaminocyclohexane, L5 = 3-carboxyboldine, and L6 = 3-carboxypredicentrine. Compounds1and2exhibited a substantially enhanced antioxidant activity compared to oxaliplatin (130 and 30 times for1and 13 and 4 times for2using the DPPH and FRAP assays, resp.). In addition,1and2exhibited cytotoxic activity in the same range as oxaliplatin toward the two human tumor cell lines (MCF-7 and HT-29) studied and two to four times lower activity in the human colon nontumor cell line (CCD-841). Preadministration of L5 or L6 to the colon tumor (HT-29) and the colon nontumor (CCD-841) cell lines prior to oxaliplatin addition increased the viability of the nontumor cell line to a greater extent than that of the tumor cell line.

2019 ◽  
Vol 74 (1) ◽  
pp. 107-114 ◽  
Author(s):  
Ana Clara Sabbione ◽  
Fredrick Onyango Ogutu ◽  
Adriana Scilingo ◽  
Miao Zhang ◽  
María Cristina Añón ◽  
...  

1985 ◽  
Vol 122 (1) ◽  
pp. 21-29 ◽  
Author(s):  
Alain Zweibaum ◽  
Mo�se Pinto ◽  
Guillemette Chevalier ◽  
Elisabeth Dussaulx ◽  
Nicole Triadou ◽  
...  

2014 ◽  
Vol 22 (3) ◽  
pp. 1049-1062 ◽  
Author(s):  
Carla Fernandes ◽  
Kamonporn Masawang ◽  
Maria Elizabeth Tiritan ◽  
Emília Sousa ◽  
Virgínia de Lima ◽  
...  

2005 ◽  
Vol 100 (3) ◽  
pp. 323-332 ◽  
Author(s):  
Alessandra Russo ◽  
Venera Cardile ◽  
Laura Lombardo ◽  
Luca Vanella ◽  
Angelo Vanella ◽  
...  

1986 ◽  
Vol 488 (1 Membrane Path) ◽  
pp. 579-581 ◽  
Author(s):  
G. ESPOSITO ◽  
E. BOMBARDIERI ◽  
M. G. COCCIOLO ◽  
C. LINDI ◽  
M. VALTOLINA ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 4005
Author(s):  
Simayijiang Aimaiti ◽  
Yohei Saito ◽  
Shuichi Fukuyoshi ◽  
Masuo Goto ◽  
Katsunori Miyake ◽  
...  

Seven new butanolides, peltanolides A–G (1–7), and two lignan glucosides, peltasides A (8) and B (9), along with eleven known compounds, 10–20, were isolated from a crude CH3OH/CH2Cl2 (1:1) extract of the fruit of Hernandia nymphaeifolia (Hernandiaceae). The structures of 1–9 were characterized by extensive 1D and 2D NMR spectroscopic and HRMS analysis. The absolute configurations of newly isolated compounds 1–9 were determined from data obtained by optical rotation and electronic circular dichroism (ECD) exciton chirality methods. Butanolides and lignan glucosides have not been isolated previously from this genus. Several isolated compounds were evaluated for antiproliferative activity against human tumor cell lines. Lignans 15 and 16 were slightly active against chemosensitive tumor cell lines A549 and MCF-7, respectively. Furthermore, both compounds displayed significant activity (IC50 = 5 µM) against a P-glycoprotein overexpressing multidrug-resistant tumor cell line (KB-VIN) but were less active against its parent chemosensitive cell line (KB).


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Khaled N. Rashed ◽  
Ana Ćirić ◽  
Jasmina Glamočlija ◽  
Ricardo C. Calhelha ◽  
Isabel C. F. R. Ferreira ◽  
...  

The hydromethanolic extract ofSapindus saponariaL. aerial parts was investigated for antimicrobial activity (against several Gram-positive and Gram-negative bacteria and fungi) and capacity to inhibit the growth of different human tumor cell lines as also nontumor liver cells. The evaluated extract was further characterized in terms of phytochemicals using UV,1H-NMR,13C-NMR, and MS spectroscopic tools. The extract has shown a significant antimicrobial activity on all tested bacterial and fungal species. The best activity was achieved againstBacillus cereusandStaphylococcus aureusamong bacteria and against all threePenicilliumspecies tested. It also revealed cytotoxicity against human colon (HCT-15), cervical (HeLa), breast (MCF-7), and lung (NCI-H460) carcinoma cell lines, with HeLa being the most susceptible tumor cell line. The extract was not toxic for nontumor liver cells. Chromatographic separation of the extract resulted in the isolation and identification of stigmasterol, oleanolic acid, luteolin, luteolin 8-C-β-glucoside (orientin), luteolin 6-C-β-glucoside (isoorientin), luteolin 7-O-β-glucuronide, and rutin. The results of the present findings may be useful for the discovery of novel antitumor and antimicrobial agents from plant origin.


Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4823
Author(s):  
Juliana M. Rodrigues ◽  
Ricardo C. Calhelha ◽  
António Nogueira ◽  
Isabel C. F. R. Ferreira ◽  
Lillian Barros ◽  
...  

Several novel methyl 7-[(hetero)arylamino]thieno[2,3-b]pyrazine-6-carboxylates were synthesized by Pd-catalyzed C–N Buchwald–Hartwig cross-coupling of either methyl 7-aminothieno[3,2-b]pyrazine-6-carboxylate with (hetero)arylhalides or 7-bromothieno[2,3-b]pyrazine-6-carboxylate with (hetero)arylamines in good-to-excellent yields (50% quantitative yield), using different reaction conditions, namely ligands and solvents, due to the different electronic character of the substrates. The antitumoral potential of these compounds was evaluated in four human tumor cell lines: gastric adenocarcinoma (AGS), colorectal adenocarcinoma (CaCo-2), breast carcinoma (MCF7), and non-small-cell lung carcinoma (NCI-H460) using the SRB assay, and it was possible to establish some structure–activity relationships. Furthermore, they did not show relevant toxicity against a non-tumor cell line culture from the African green monkey kidney (Vero). The most promising compounds (GI50 ≤ 11 µM), showed some selectivity either against AGS or CaCo-2 cell lines without toxicity at their GI50 values. The effects of the methoxylated compounds 2b (2-OMeC6H4), 2f and 2g (3,4- or 3,5-diOMeC6H3, respectively) on the cell cycle profile and induction of apoptosis were further studied in the AGS cell line. Nevertheless, even for the most active (GI50 = 7.8 µM) and selective compound (2g) against this cell line, it was observed that a huge number of dead cells gave rise to an atypical distribution on the cell cycle profile and that these cells were not apoptotic, which points to a different mechanism of action for the AGS cell growth inhibition.


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