scholarly journals Antimicrobial Activity, Growth Inhibition of Human Tumour Cell Lines, and Phytochemical Characterization of the Hydromethanolic Extract Obtained fromSapindus saponariaL. Aerial Parts

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Khaled N. Rashed ◽  
Ana Ćirić ◽  
Jasmina Glamočlija ◽  
Ricardo C. Calhelha ◽  
Isabel C. F. R. Ferreira ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Tumor Cell ◽  
Cell Lines ◽  
Antimicrobial Agents ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
Human Colon ◽  
Liver Cells ◽  
Isolation And Identification ◽  
Aerial Parts

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.

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 ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Tumor Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
Human Colon ◽  
Human Tumor Cell Lines ◽  
Derivatives Of ◽  
Ht 29

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.

scholarly journals Isolation, Structure Elucidation, and Antiproliferative Activity of Butanolides and Lignan Glycosides from the Fruit of Hernandia nymphaeifolia

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 4005
Author(s):  
Simayijiang Aimaiti ◽  
Yohei Saito ◽  
Shuichi Fukuyoshi ◽  
Masuo Goto ◽  
Katsunori Miyake ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Optical Rotation ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
2D Nmr ◽  
Significant Activity ◽  
Tumor Cell Lines

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).

scholarly journals Synthesis and Biological Evaluation of Novel Aminochalcones as Potential Anticancer and Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4129 ◽  
Author(s):  
Joanna Kozłowska ◽  
Bartłomiej Potaniec ◽  
Dagmara Baczyńska ◽  
Barbara Żarowska ◽  
Mirosław Anioł
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Antimicrobial Agents ◽  
Human Colon ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Human Colon Cancer ◽  
E Coli ◽  
Almost All ◽  
Ht 29

A series of 18 aminochalcone derivatives were obtained in yields of 21.5–88.6% by applying the classical Claisen-Schmidt reaction. Compounds 4–9, 14 and 16–18 with 4-ethyl, 4-carboxy-, 4-benzyloxy- and 4-benzyloxy-3-methoxy groups were novel, not previously described in the scientific literature. To determine the biological properties of the synthesized compounds, anticancer and antimicrobial activity assays were performed. Antiproliferative potential was evaluated on four different human colon cancer cell lines—HT-29, LS180, LoVo and LoVo/DX —using the SRB assay and compared with green monkey kidney fibroblasts COS7. Anticancer activity was described as the IC50 value. The best results were observed for 2′-aminochalcone (1), 3′-aminochalcone (2) and 4′-aminochalcone (3) (IC50 = 1.43–1.98 µg·mL−1) against the HT-29 cell line and for amino-nitrochalcones 10–12 (IC50 = 2.77–3.42 µg·mL−1) against the LoVo and LoVo/DX cell lines. Moreover, the antimicrobial activity of all derivatives was evaluated on two strains of bacteria: Escherichia coli ATCC10536 and Staphylococcus aureus DSM799, the yeast strain Candida albicans DSM1386 and three strains of fungi: Alternaria alternata CBS1526, Fusarium linii KB-F1 and Aspergillus niger DSM1957. In the case of E. coli ATCC10536 almost all derivatives hindered the bacterial growth (∆OD = 0). Furthermore, the best results were observed in the presence of 4′-aminochalcone (3), that completely limited the growth of all tested strains at the concentration range of 0.25–0.5 mg·mL−1. The strongest bacteriostatic activity was exhibited by novel 3′-amino-4-benzyloxychalcone (14), that prevented the growth of E. coli ATCC10536 with MIC = 0.0625 mg·mL−1.

scholarly journals Identification by High-Throughput Screening of Viridin Analogs as Biochemical and Cell-Based Inhibitors of the Cell Cycle–Regulated Nek2 Kinase

2010 ◽  
Vol 15 (8) ◽  
pp. 918-927 ◽  
Author(s):  
Daniel G. Hayward ◽  
Yvette Newbatt ◽  
Lisa Pickard ◽  
Eilis Byrne ◽  
Guojie Mao ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
High Throughput ◽  
High Throughput Screening ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
Cancer Drug ◽  
Human Tumor Cell ◽  
Cancer Drug Discovery ◽  
Centrosome Separation

Nek2 is a serine/threonine protein kinase that localizes to the centrosome and is implicated in mitotic regulation. Overexpression of Nek2 induces premature centrosome separation and nuclear defects indicative of mitotic errors, whereas depletion of Nek2 interferes with cell growth. As Nek2 expression is upregulated in a range of cancer cell lines and primary human tumors, inhibitors of Nek2 may have therapeutic value in cancer treatment. The authors used a radiometric proximity assay in a high-throughput screen to identify small-molecule inhibitors of Nek2 kinase activity. The assay was based on the measurement of the radiolabeled phosphorylated product of the kinase reaction brought into contact with the surface of wells of solid scintillant-coated microplates. Seventy nonaggregating hits were identified from approximately 73,000 compounds screened and included a number of toxoflavins and a series of viridin/wortmannin-like compounds. The viridin-like compounds were >70-fold selective for Nek2 over Nek6 and Nek7 and inhibited the growth of human tumor cell lines at concentrations consistent with their biochemical potencies. An automated mechanism-based microscopy assay in which centrosomes were visualized using pericentrin antibodies confirmed that 2 of the viridin inhibitors reduced centrosome separation in a human tumor cell line. The data presented show that pharmacological inhibition of Nek2 kinase results in the expected phenotype of disruption to centrosome function associated with growth inhibition and further supports Nek2 as a target for cancer drug discovery.

scholarly journals New Dammarane-type Saponins from Gynostemma pentaphyllum

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1375 ◽  
Author(s):  
Po-Yen Chen ◽  
Chih-Chao Chang ◽  
Hui-Chi Huang ◽  
Li-Jie Zhang ◽  
Chia-Ching Liaw ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Gynostemma Pentaphyllum ◽  
Antiproliferative Effects ◽  
Aerial Parts

Six new dammarane-type saponins, gypenosides CP1-6 (16), along with 19 known compounds 7–25, were isolated and characterized from the aerial parts of Gynostemma pentaphyllum. Among these compounds, eight dammarane-type saponins, 2, 5, 6, 7, 11, 12, 13, and 15, exhibited the greatest antiproliferative effects against two human tumor cell lines (A549 and HepG2).

scholarly journals Antimicrobial Activity of Essential Oils againstStreptococcus mutansand their Antiproliferative Effects

2012 ◽  
Vol 2012 ◽  
pp. 1-12 ◽  
Author(s):  
Lívia Câmara de Carvalho Galvão ◽  
Vivian Fernandes Furletti ◽  
Salete Meyre Fernandes Bersan ◽  
Marcos Guilherme da Cunha ◽  
Ana Lúcia Tasca Góis Ruiz ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Tumor Cell ◽  
Essential Oils ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Human Tumor ◽  
Gas Chromatography Mass Spectrometry ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

This study aimed to evaluate the activity of essential oils (EOs) againstStreptococcus mutansbiofilm by chemically characterizing their fractions responsible for biological and antiproliferative activity. Twenty EO were obtained by hydrodistillation and submitted to the antimicrobial assay (minimum inhibitory (MIC) and bactericidal (MBC) concentrations) againstS. mutansUA159. Thin-layer chromatography and gas chromatography/mass spectrometry were used for phytochemical analyses. EOs were selected according to predetermined criteria and fractionated using dry column; the resulting fractions were assessed by MIC and MBC, selected as active fractions, and evaluated againstS. mutansbiofilm. Biofilms formed were examined using scanning electron microscopy. Selected EOs and their selected active fractions were evaluated for their antiproliferative activity against keratinocytes and seven human tumor cell lines. MIC and MBC values obtained for EO and their active fractions showed strong antimicrobial activity. Chemical analyses mainly showed the presence of terpenes. The selected active fractions inhibitedS. mutansbiofilm formation (P<0.05) did not affect glycolytic pH drop and were inactive against keratinocytes, normal cell line. In conclusion, EO showed activity at low concentrations, and their selected active fractions were also effective against biofilm formed byS. mutansand human tumor cell lines.

scholarly journals Synthesis of Novel Methyl 7-[(Hetero)arylamino]thieno[2,3-b]pyrazine-6-carboxylates and Antitumor Activity Evaluation: Effects in Human Tumor Cells Growth, Cell Cycle Analysis, Apoptosis and Toxicity in Non-Tumor Cells

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4823
Author(s):  
Juliana M. Rodrigues ◽  
Ricardo C. Calhelha ◽  
António Nogueira ◽  
Isabel C. F. R. Ferreira ◽  
Lillian Barros ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Tumor Cell ◽  
Cell Line ◽  
Tumor Cells ◽  
Cell Lines ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
African Green Monkey Kidney ◽  
Cell Lung Carcinoma ◽  
Cell Cycle Profile

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.

scholarly journals Two-Dimensional PCA Highlights the Differentiated Antitumor and Antimicrobial Activity of Methanolic and Aqueous Extracts ofLaurus nobilisL. from Different Origins

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Maria Inês Dias ◽  
João C. M. Barreira ◽  
Ricardo C. Calhelha ◽  
Maria-João R. P. Queiroz ◽  
M. Beatriz P. P. Oliveira ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Aqueous Extracts ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Methanolic Extracts

Natural matrices are important sources of new antitumor and antimicrobial compounds. Species such asLaurus nobilisL. (laurel) might be used for this purpose, considering its medicinal properties. Herein,in vitroactivity against human tumor cell lines, bacteria, and fungi was evaluated in enriched phenolic extracts. Specifically, methanol and aqueous extracts of wild and cultivated samples ofL. nobiliswere compared considering different phenolic groups. Principal component analysis (PCA) was applied to understand how each extract acts differentially against specific bacteria, fungi, and selected human tumor cell lines. In general, the extract type induced the highest differences in bioactivity of laurel samples. However, from the PCA biplot, it became clear that wild laurel samples were higher inhibitors of tumor cell lines (HeLa, MCF7, NCI-H460, and HCT15). HepG2 had the same response to laurel from wild and cultivated origin. It was also observed that methanolic extracts tended to have higher antimicrobial activity, except againstA. niger, A. fumigatus, andP. verrucosum. The differences in bioactivity might be related to the higher phenolic contents in methanolic extracts. These results allow selecting the extract type and/or origin with highest antibacterial, antifungal, and antitumor activity.

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