Enniatin Exerts p53-Dependent Cytostatic and p53-Independent Cytotoxic Activities against Human Cancer Cells

2007 ◽  
Vol 20 (3) ◽  
pp. 465-473 ◽  
Author(s):  
Rita Dornetshuber ◽  
Petra Heffeter ◽  
Majid-Reza Kamyar ◽  
Thomas Peterbauer ◽  
Walter Berger ◽  
...  
2021 ◽  
Vol 45 (11) ◽  
pp. 5176-5183
Author(s):  
Ichraf Slimani ◽  
Serap Şahin-Bölükbaşı ◽  
Mustafa Ulu ◽  
Enes Evren ◽  
Nevin Gürbüz ◽  
...  

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.


2021 ◽  
Vol 16 (2) ◽  
pp. 1934578X2199615
Author(s):  
Lucas Botelho Jerônimo ◽  
Jamile S. da Costa ◽  
Laine C. Pinto ◽  
Raquel C. Montenegro ◽  
William N. Setzer ◽  
...  

This work analyzed the chemical compositions and evaluated the antioxidant and cytotoxic activities of essential oils (EO) of Eugenia patrisii (Epat), Eugenia stipitata (Esti), Myrcia splendens (Mspl), Myrcia sylvatica (Msyl), Psidium guajava (Pgua), and Psidium guineense (Pgui-1 and Pgui-2) from the Brazilian Amazon. Sesquiterpenoids were found in high concentrations in the oils of E. patrisii and M. splendens, which were rich in E-caryophyllene (32.0% and 45.8%); E. stipitata and M. sylvatica, which displayed germacrene D (11.8%) and germacrene B (24.5%); and P. guajava that showed epi-β-bisabolol (16.1%) as the main compound. However, P. guineense samples (Pgui-1 and Pgui-2) were rich in monoterpenoids such as limonene (Pgui-1: 30.2%; Pgui-2 30.4%) and α-pinene (Pgui-1: 22.5%; Pgui-2: 17.7%). The samples showed a weak and moderate antioxidant activities in the DPPH assay, displaying inhibition rates from 11.5% to 38.6% (at 10 mg/mL). All samples were cytotoxic against human cancer cells by the MTT method. Epat oil showed higher activity against melanoma (SKMEL-19, IC505.8 µg/mL), gastric (AGP01, IC503.2 µg/mL), and colon (HCT116, IC506.7 µg/mL). Meanwhile, the samples Pgua and Pgui were more active against breast cancer cells (MCF7, IC5012.4 µg/mL and 11.6 µg/mL, respectively).


2014 ◽  
Vol 82 ◽  
pp. 565-573 ◽  
Author(s):  
Safiye Emirdağ-Öztürk ◽  
Tamer Karayıldırım ◽  
Aysun Çapcı-Karagöz ◽  
Özgen Alankuş-Çalışkan ◽  
Ali Özmen ◽  
...  

ChemInform ◽  
2016 ◽  
Vol 47 (8) ◽  
pp. no-no ◽  
Author(s):  
Byeol Ryu ◽  
Hye Mi Kim ◽  
Jae-Seung Lee ◽  
Yoon Jin Cho ◽  
Myung Sook Oh ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1780 ◽  
Author(s):  
Julio Benites ◽  
Jaime A. Valderrama ◽  
Maryan Ramos ◽  
Maudy Valenzuela ◽  
Angélica Guerrero-Castilla ◽  
...  

A broad range of 3-acyl-2,5-bis(phenylamino)-1,4-benzoquinones were synthesized and their voltammetric values, as well as in vitro cancer cell cytotoxicities, were assessed. The members of this series were prepared from acylbenzoquinones and phenylamines, in moderate to good yields (47–74%), through a procedure involving a sequence of two in situ regioselective oxidative amination reactions. The cyclic voltammograms of the aminoquinones exhibit two one-electron reduction waves to the corresponding radical-anion and dianion, and two quasi-reversible oxidation peaks. The first and second half-wave potential values (E1/2) of the members of the series were sensitive to the push-pull electronic effects of the substituents around the benzoquinone nucleus. The in vitro cytotoxic activities of the 3-acyl-2,5-bis(phenylamino)-1,4-benzoquinones against human cancer cells (bladder and prostate) and non-tumor human embryonic kidney cells were measured using the MTT colorimetric method. The substitution of both aniline groups, by either methoxy (electron donating effect) or fluorine (electron withdrawal effect), decreased the cytotoxicity in the aminoquinones. Among the members of the unsubstituted phenylamino series, two of the 18 compounds showed interesting anti-cancer activities. A preliminary assay, looking for changes in the expression of selected genes, was performed. In this context, the two compounds increased TNF gene expression, suggesting an association with an inflammatory-like response.


Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 566
Author(s):  
Makanjuola Ogunsina ◽  
Pranati Samadder ◽  
Temilolu Idowu ◽  
Mark Nachtigal ◽  
Frank Schweizer ◽  
...  

A major impediment to successful cancer treatment is the inability of clinically available drugs to kill drug-resistant cancer cells. We recently identified metabolically stable l-glucosamine-based glycosylated antitumor ether lipids (GAELs) that were cytotoxic to chemotherapy-resistant cancer cells. In the absence of commercially available l-glucosamine, many steps were needed to synthesize the compound and the overall yield was poor. To overcome this limitation, a facile synthetic procedure using commercially available l-sugars including l-rhamnose and l-glucose were developed and the l-GAELs tested for anticancer activity. The most potent analog synthesized, 3-amino-1-O-hexadecyloxy-2R-(O–α-l-rhamnopyranosyl)-sn- glycerol 3, demonstrated a potent antitumor effect against human cancer cell lines derived from breast, prostate, and pancreas. The activity observed was superior to that observed with clinical anticancer agents including cisplatin and chlorambucil. Moreover, like other GAELs, 3 induced cell death by a non-membranolytic caspase-independent pathway.


2018 ◽  
Vol 5 (1) ◽  
pp. 171510 ◽  
Author(s):  
Haochao Zhang ◽  
Yanling Mu ◽  
Fengling Wang ◽  
Leling Song ◽  
Jie Sun ◽  
...  

Thirty-two gypsogenin derivatives were synthesized and screened for their cytotoxic activities. Their structures were established using IR, 1 H NMR, 13 C NMR, and LC-MS spectroscopic data. In MTT assays nearly all the compounds displayed good cytotoxicity in the low μM range for several human tumour cell lines (A549, LOVO, SKOV3 and HepG2). Low IC 50 values were obtained especially for the carboxamides 7a – 7j , for an oxime derivative 3 and a (2,4-dinitrophenyl)hydrazono derivative 4 . In particular, the IC 50 values of compounds 4 (IC 50  = 2.97 ± 1.13 µΜ) and 7 g (IC 50  = 3.59 ± 2.04 µΜ) against LOVO cells were found to be much lower than those of the other derivatives and parent compound. These compounds were submitted to an extensive biological testing and proved compounds 4 and 7 g to act mainly by an arrest of the tumour cells in the S phase of the cell cycle. In addition, compounds 4 and 7 g triggered the apoptotic pathway in cancer cells, showing high apoptosis ratios.


2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
David Ríos ◽  
Jaime A. Valderrama ◽  
Miriam Cautin ◽  
Milko Tapia ◽  
Felipe Salas ◽  
...  

The reaction of 2-acyl-1,4-naphthoquinones with N,N-dimethylaniline and 2,5-dimethoxyaniline, promoted by catalytic amounts of CeCl3·7H2O under “open-flask” conditions, produced a variety of 2-acyl-3-aminophenyl-1,4-naphthoquinones structurally related to the cytotoxic 2-acetyl-3-phenyl-1,4-naphthoquinone, an inhibitor of the heat shock chaperone protein Hsp90. The members of the 2-acyl-3-aminophenyl-1,4-naphthoquinone series were isolated in good yields (63-98%). The cyclic voltammograms of the 2-acyl-3-aminophenyl-1,4-naphthoquinone exhibit two one-electron reduction waves to the corresponding radical-anion and dianion and two quasireversible oxidation peaks. The first and second half-wave potential values (E1/2) of the members of the series are sensitive to the push-pull electronic effects of the substituents in the naphthoquinone scaffold. Furthermore, the in vitro antiproliferative properties of these new quinones were evaluated on two human cancer cells DU-145 (prostate) and MCF-7 (mammary) and a nontumorigenic HEK-293 (kidney) cell line, using the MTT colorimetric method. Two members, within the series, exhibited interesting cytotoxic activities on human prostate and mammary cancer cells.


2006 ◽  
Vol 164 ◽  
pp. S250-S251 ◽  
Author(s):  
R. Dornetshuber ◽  
P. Heffeter ◽  
R. Kamyar ◽  
W. Berger ◽  
R. Lemmens-Gruber

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