scholarly journals Antiproliferative Activity of Flavonoids fromCroton sphaerogynusBaill. (Euphorbiaceae)

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Kátia Pereira dos Santos ◽  
Lucimar B. Motta ◽  
Deborah Y. A. C. Santos ◽  
Maria L. F. Salatino ◽  
Antonio Salatino ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Rain Forest ◽  
Room Temperature ◽  
Southeastern Brazil ◽  
Atlantic Rain Forest ◽  
Moderate Activity ◽  
Etoh Extract ◽  
Weak Activity ◽  
Mcf 7

Croton sphaerogynusis a shrub from the Atlantic Rain Forest in southeastern Brazil. A lyophilized crude EtOH extract from leaves ofC. sphaerogynus, obtained by maceration at room temperature (seven days), was suspended in methanol and partitioned with hexane. The purified MeOH phase was fractionated over Sephadex LH-20 yielding five fractions (F1–F5) containing flavonoids, as characterized by HPLC-DAD and HPLC-MS analyses. The antiproliferative activity of the crude EtOH extract, MeOH and hexane phases, and fractionsF1–F5was evaluated onin vitrocell lines NCI-H460 (nonsmall cell lung), MCF-7 (breast cancer), and U251 (glioma). The MeOH phase showed activity (mean log GI500.54) higher than the hexane phase and EtOH extract (mean log GI501.13 and 1.19, resp.).F1exhibited activity against NCI-H460 (nonsmall cell lung) (GI501.2 μg/mL), which could be accounted for the presence of flavonoids and/or diterpenes.F4showed moderate activity (mean log GI501.05), whileF5showed weak activity (mean log GI501.36). It is suggested that the antiproliferative activity of the crude EtOH extract and MeOH phase is accounted for a synergistic combination of flavonoids and diterpenes.

scholarly journals Model Amphipathic Peptide Coupled with Tacrine to Improve Its Antiproliferative Activity

2020 ◽  
Vol 22 (1) ◽  
pp. 242
Author(s):  
Sara Silva ◽  
Cláudia Alves ◽  
Diana Duarte ◽  
Ana Costa ◽  
Bruno Sarmento ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis ◽  
Drug Repurposing ◽  
Parent Drug ◽  
Ache Inhibitor ◽  
Amphipathic Peptide ◽  
Reference Drug ◽  
Mcf 7

Drug repurposing and drug combination are two strategies that have been widely used to overcome the traditional development of new anticancer drugs. Several FDA-approved drugs for other indications have been tested and have demonstrated beneficial anticancer effects. In this connection, our research group recently reported that Tacrine, used to treat Alzheimer’s Disease, inhibits the growth of breast cancer MCF-7 cells both alone and in combination with a reference drug. In this view, we have now coupled Tacrine with the model amphipathic cell-penetrating peptide (CPP) MAP, to ascertain whether coupling of the CPP might enhance the drug’s antiproliferative properties. To this end, we synthesized MAP through solid-phase peptide synthesis, coupled it with Tacrine, and made a comparative evaluation of the parent drug, peptide, and the conjugate regarding their permeability across the blood-brain barrier (BBB), ability to inhibit acetylcholinesterase (AChE) in vitro, and antiproliferative activity on cancer cells. Both MAP and its Tacrine conjugate were highly toxic to MCF-7 and SH-SY5Y cells. In turn, BBB-permeability studies were inconclusive, and conjugation to the CPP led to a considerable loss of Tacrine function as an AChE inhibitor. Nonetheless, this work reinforces the potential of repurposing Tacrine for cancer and enhances the antiproliferative activity of this drug through its conjugation to a CPP.

Feeding Ecology of Thoropa Miliaris (Anura, Cycloramphidae) in Four Areas of Atlantic Rain Forest, Southeastern Brazil

2006 ◽  
Vol 40 (4) ◽  
pp. 520-525 ◽  
Author(s):  
Carla C. Siqueira ◽  
Monique Van Sluys ◽  
Cristina V. Ariani ◽  
Carlos F. D. Rocha
Keyword(s):  
Feeding Ecology ◽  
Rain Forest ◽  
Southeastern Brazil ◽  
Atlantic Rain Forest

New binuclear Ni(ii) metallates containing ONS chelators: synthesis, characterisation, DNA binding, DNA cleavage, protein binding, antioxidant activity, antimicrobial and in vitro cytotoxicity

2017 ◽  
Vol 41 (7) ◽  
pp. 2543-2560 ◽  
Author(s):  
G. Kalaiarasi ◽  
Ruchi Jain ◽  
H. Puschman ◽  
S. Poorna Chandrika ◽  
K. Preethi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Dna Binding ◽  
Protein Binding ◽  
Hela Cell ◽  
Antiproliferative Activity ◽  
Dna Cleavage ◽  
In Vitro Cytotoxicity ◽  
Hela Cell Lines ◽  
Mcf 7

Four new binuclear nickel(ii) metallates showed promising antiproliferative activity against MCF-7 and HeLa cell lines and were much less toxic against HaCaT.

New Species of Brachycephalus (Anura: Brachycephalidae) from the Atlantic Rain Forest in São Paulo State, Southeastern Brazil

2009 ◽  
Vol 43 (2) ◽  
pp. 212-219 ◽  
Author(s):  
Ana C. R. Alves ◽  
Ricardo J. Sawaya ◽  
Sérgio Fdos Reis ◽  
Célio F. B. Haddad
Keyword(s):  
New Species ◽  
Rain Forest ◽  
Sao Paulo ◽  
Southeastern Brazil ◽  
Atlantic Rain Forest ◽  
São Paulo ◽  
Paulo State ◽  
São Paulo State

scholarly journals Checklist of ferns and lycophytes from the Parque Estadual Turístico do Alto Ribeira, Iporanga, São Paulo, Brazil

Check List ◽  
2015 ◽  
Vol 11 (6) ◽  
pp. 1791 ◽  
Author(s):  
Frederico Fregolente Faracco Mazziero ◽  
Paulo Henrique Labiak ◽  
Mateus Luis Barradas Paciencia
Keyword(s):  
Rain Forest ◽  
Conservation Status ◽  
Sao Paulo ◽  
Southeastern Brazil ◽  
Atlantic Rain Forest ◽  
São Paulo ◽  
Floristic Survey ◽  
Paulo State ◽  
São Paulo State ◽  
Ferns And Lycophytes

We present the floristic survey of ferns and lycophytes from the “Parque Estadual Turístico do Alto Ribeira” (PETAR), a remnant of Atlantic Rain Forest of Southeastern Brazil, in São Paulo state. Besides a complete list of species, we also provide information on habit, geographic distribution, and conservation status. Among the 237 taxa, there are 235 species, one variety and one hybrid, distributed in 29 families and 74 genera. Ferns are represented by 223 taxa, whereas the lycophytes were represented by 14. The most representative families are Polypodiaceae (31 spp.), Pteridaceae (29 spp.) and Dryopteridaceae (28 spp.). The most diverse genera are Thelypteris (23 spp.), Asplenium (19 spp.), Elaphoglossum and Blechnum (10 spp. each). Noteworthy is the presence of Ctenitis anniesii, Dicksonia sellowiana, Elaphoglossum iguapense, E. prestonii, E. strictum, Thelypteris concinna, T. araucariensis and T. hatschbachii, all of them considered as endangered species in São Paulo state.

scholarly journals Synthesis, Crystal Structure, and Biological Activity ofcis/transAmide Rotomers of (Z)-N′-(2-Oxoindolin-3-ylidene)formohydrazide

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Hatem A. Abdel-Aziz ◽  
Hazem A. Ghabbour ◽  
Wagdy M. Eldehna ◽  
Maha M. Qabeel ◽  
Hoong-Kun Fun
Keyword(s):  
Crystal Structure ◽  
Human Tumor ◽  
Cancer Cell Line ◽  
Monoclinic Space Group ◽  
Moderate Activity ◽  
Standard Drug ◽  
X Ray ◽  
H Nmr ◽  
Mcf 7

(Z)-N′-(2-Oxoindolin-3-ylidene)formohydrazide (2) was synthesized by the reaction of (Z)-3-hydrazonoindolin-2-one (1) with formic acid under reflux. The structure of2was characterized by IR, Mass,1H NMR, and X-ray crystal structure determination. Interestingly, compound2appeared in DMSO-d6ascisandtransamide rotomers in 25% and 75%, respectively. The X-ray analysis showed theZgeometrical isomer of2around –C=N– forcisandtransamide rotomers. The crystal of2belongs to monoclinic, space groupP21/c, witha=4.5206(1) Å,b=22.4747(7) Å,c=17.3637(5) Å,β=103.752(1)°,Z=8,V=1713.57(8) Å3,Dc=1.467 Mg m−3,μ=0.11 mm−1,F(000)=784,R=0.047, andwR=0.123for 3798 observed reflections withI>2σ(I). Compound2exhibited a moderate activity in its antimicrobial evaluation againstE. coliandP. aeruginosaand a good activity againstS. aureusclose to that of the standard drug ciprofloxacin. Thein vitroanticancer activity of2was evaluated against two human tumor cell lines, namely, HepG2 hepatocellular carcinoma and MCF-7 breast cancer. HepG2 cancer cell line was more susceptible to compound2than MCF-7.

scholarly journals THE CYTOTOXIC EFFECT OF CHELIDONIUM MAJUS IN VITRO

2015 ◽  
Vol 8 (2) ◽  
Author(s):  
Vladimíra Tomečková ◽  
Veronika Tkáčová ◽  
Peter Urban ◽  
Marek Stupák
Keyword(s):  
Tumor Cells ◽  
Hela Cells ◽  
Antiproliferative Activity ◽  
Cytotoxic Effect ◽  
Lymphoblastic Leukemia ◽  
Mammary Adenocarcinoma ◽  
Chelidonium Majus ◽  
Mcf 7 ◽  
Lipophilic Substances

The effect of aqueous and ether Chelidonium majus haulms extract on cervical HeLa tumor cells, mammary adenocarcinoma MCF 7 tumor cells and acute lymphoblastic leukemia CEM tumor cells in vitro have been studied. The purpose of this research was to compare the effect of aqueous and ether Chelidonium majus haulms extract on selected tumor cells. Colorimetric MTT assay have been used for the study of the antiproliferative effect of aqueous and ether haulms extract of Chelidonium majus on cell viability in vitro. The results of the experiments have shown the cytotoxic effect of the aqueous and the ether Chelidonium majus haulms extract on the individual tumor cells. The aqueous Chelidonium majus haulms extract was the most effective on CEM cells, it was less effective on MCF 7 cells and it was the least effective on HeLa cells. The ether haulms extract of Chelidonium majus was the most effective at all of studied concentrations on CEM cells and MCF 7 cells in comparison with HeLa cells, where it was significantly effective only at the highest concentration. Aqueous and ether haulms extract of Chelidonium majus tested in vitro indicated their cytotoxic activity. Both haulms extract of Chelidonium majus were more efficient on CEM cells. It is assumed that higher antiproliferative activity of ether haulms extract of Chelidonium majus is the result of higher antiproliferative activity of lipophilic substances. The lipophilic substances pass through membrane and bind to various proteins and change their biological activity.

scholarly journals Synthesis of new 3-(substituted-phenyl)-N-(2-hydroxy-2-(substituted-phenyl)ethyl)-N-methylthiophene-2-sulfonamide derivatives as antiproliferative agents

2018 ◽  
Vol 9 (1) ◽  
pp. 13-21 ◽  
Author(s):  
Chandrakant Pawar ◽  
Dattatraya Pansare ◽  
Devanand Shinde
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
1H Nmr ◽  
13C Nmr ◽  
Antiproliferative Activity ◽  
Positive Control ◽  
Antiproliferative Agents ◽  
Ic50 Values ◽  
Mcf 7

In the present work, we report the synthesis of a series of 3-(substituted phenyl)-N-(2-hydroxy-2-(substituted-phenyl)ethyl)-N-methylthiophene-2-sulfonamide derivatives through Suzuki and Buchwald reaction. We have optimized methodology for targets from milligram to multi-gram scale. The newly synthesized compounds were characterized by 1H NMR, 19F NMR, 13C NMR, LC-MS techniques and purity was further checked by HPLC. The compounds were evaluated for their in-vitro antiproliferative activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines by CCK-8 assay. The preliminary bioassay suggests that most of the compounds show antiproliferation with different degrees and 5-fluorouracil was used as positive control. Among these compounds 2d, 2g, 2i, 4e, 4h and 4k are most active compared to the standard. All the synthesized compounds show IC50 values from 1.82-9.52 µM in different cell lines. Amongst these, compounds 2d, 2g, 2i, 4e, 4h and 4k were most potent, with IC50 values ranging from 1.82-4.28 µM in different cell lines.

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