Synthesis of gypsogenin and gypsogenic acid derivatives with antitumor activity by damaging cell membranes

2019 ◽  
Vol 43 (47) ◽  
pp. 18898-18914 ◽  
Author(s):  
Guiying Wu ◽  
Haiping Chu ◽  
Jilei Wang ◽  
Yanling Mu ◽  
Jingyong Sun
Keyword(s):  
Antitumor Activity ◽  
Cell Membranes ◽  
Cytotoxic Activities ◽  
Gypsogenic Acid

Forty-five gypsogenin and gypsogenic acid derivatives were synthesized and screened for their cytotoxic activities.

scholarly journals DNA Cleavage, Cytotoxic Activities, and Antimicrobial Studies of Ternary Copper(II) Complexes of Isoxazole Schiff Base and Heterocyclic Compounds

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Vijay Kumar Chityala ◽  
K. Sathish Kumar ◽  
Ramesh Macha ◽  
Parthasarathy Tigulla ◽  
Shivaraj
Keyword(s):  
Antitumor Activity ◽  
Metal Complexes ◽  
Schiff Bases ◽  
Dna Cleavage ◽  
Spectral Studies ◽  
Planar Geometry ◽  
Cytotoxic Activities ◽  
Significant Activity ◽  
Antimicrobial Studies ◽  
Hela Cell Lines

Novel mixed ligand bivalent copper complexes [Cu. L. A. ClO4] and [Cu. L. A] where “L” is Schiff bases, namely 2-((3,4-dimethylisoxazol-5-ylimino)methyl)-4-bromophenol (DMIIMBP)/2-((3,4-dimethylisoxazol-5-ylimino)methyl)-4-chlorophenol (DMIIMCP), and “A” is heterocyclic compound, such as 1,10-phenanthroline (phen)/2,21-bipyridyl (bipy)/8-hydroxyquinoline (oxine)/5-chloro-8-hydroxyquinoline (5-Cl-oxine), have been synthesized. These complexes have been characterized by IR, UV-Vis, ESR, elemental analysis, magnetic moments, TG, and DTA. On the basis of spectral studies and analytical data, five-coordinated square pyramidal/four-coordinated square planar geometry is assigned to all complexes. The ligands and their ternary complexes with Cu(II) have been screened for antimicrobial activity against bacteria and fungi by paper disc method. The antimicrobial studies of Schiff bases and their metal complexes showed significant activity and further it is observed that the metal complexes showed more activity than corresponding Schiff bases. In vitro antitumor activity of Cu(II) complexes was assayed against human cervical carcinoma (HeLa) cancer cells and it was observed that few complexes exhibit good antitumor activity on HeLa cell lines. The DNA cleavage studies have also been carried out on pBR 322 and it is observed that these Cu(II) complexes are capable of cleaving supercoiled plasmid DNA in the presence of H2O2and UV light.

Peptide R18H from BRN2 Transcription Factor POU Domain Displays Antitumor Activity In Vitro and In Vivo and Induces Apoptosis in B16F10-Nex2 Cells

2019 ◽  
Vol 19 (3) ◽  
pp. 389-401 ◽  
Author(s):  
Fernanda F.M. da Cunha ◽  
Katia C.U. Mugnol ◽  
Filipe M. de Melo ◽  
Marta V.S.Q. Nascimento ◽  
Ricardo A. de Azevedo ◽  
...  
Keyword(s):  
Cell Death ◽  
Transcription Factor ◽  
Cytochrome C ◽  
Antitumor Activity ◽  
Chromatin Condensation ◽  
Cytotoxic Activities ◽  
Cytochrome C Release ◽  
Extracellular Medium ◽  
Pou Domain

Background:BRN2 transcription factor is associated with the development of malignant melanoma. The cytotoxic activities and cell death mechanism against B16F10-Nex2 cells were determined with synthetic peptide R18H derived from the POU domain of the BRN2 transcription factor.Objective:To determine the cell death mechanisms and in vivo activity of peptide R18H derived from the POU domain of the BRN2 transcription factor against B16F10-Nex2 cells.Methods:Cell viability was determined by the MTT method. C57Bl/6 mice were challenged with B16F10-Nex2 cells and treated with R18H. To identify the type of cell death, we used TUNEL assay, Annexin V and PI, Hoechst, DHE, and determination of caspase activation and cytochrome c release. Transmission electron microscopy was performed to verify morphological alterations after peptide treatment.Results:Peptide R18H displayed antitumor activity in the first hours of treatment and the EC50% was calculated for 2 and 24h, being 0.76 ± 0.045 mM and 0.559 ± 0.053 mM, respectively. After 24h apoptosis was evident, based on DNA degradation, chromatin condensation, increase of superoxide anion production, phosphatidylserine translocation, activation of caspases 3 and 8, and release of extracellular cytochrome c in B16F10-Nex2 cells. The peptide cytotoxic activity was not affected by necroptosis inhibitors and treated cells did not release LDH in the extracellular medium. Moreover, in vivo antitumor activity was observed following treatment with peptide R18H.Conclusion:Peptide R18H from BRN2 transcription factor induced apoptosis in B16F10-Nex2 and displayed antitumor activity in vivo.

scholarly journals Synthesis, Characterization And Antitumor Activity Of Copper(II) Complexes, [CuL2] [HL1-3=N,N-Diethyl-N'-(R-Benzoyl)Thiourea (R=H, o-Cl and p-NO2)]

2005 ◽  
Vol 3 (3-4) ◽  
pp. 299-316 ◽  
Author(s):  
Wilfredo Hernández ◽  
Evgenia Spodine ◽  
Lothar Beyer ◽  
Uwe Schröder ◽  
Rainer Richter ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Elemental Analysis ◽  
Copper Complexes ◽  
Mammary Adenocarcinoma ◽  
Molar Ratio ◽  
High Yield ◽  
Planar Geometry ◽  
Cytotoxic Activities ◽  
High Accumulation

The copper (II) complexes (CuL2) were prepared by reaction ofCu(CH3COO)2with the corresponding derivatives of acylthioureas in a Cu:HL molar ratio of 1:2. Acylthiourea ligands, N,N-diethyl-N'-(R-benzoyl) thiourea (HL1-3) [R=H, o-Cl and p-NO2] were synthesized in high yield (78-83%) and characterized by elemental analysis, infrared spectroscopy,1H and13C NMR spectroscopy. The complexes CuL2were characterized by elemental analysis, IR, FAB(+)-MS, magnetic susceptibility measurements, EPR and cyclic voltammetry. The crystal structure of the complex Cu(L2)2shows a nearly square-planar geometry with two deprotonated ligands (L) coordinated to CuIIthrough the oxygen and sulfur atoms in acisarrangement. The antitumor activity of the copper(II) complexes with acylthiourea ligands was evaluatedin vitroagainst the mouse mammary adenocarcinoma TA3 cell line. These complexes exhibited much higher cytotoxic activity (IC50values in the range of 3.9-6.9 μM) than their corresponding ligands (40-240 μM), which indicates that the coordination of the chelate ligands around the CuIIenhances the antitumor activity and, furthermore, this result confirmed that the participation of the nitro and chloro substituent groups in the complex activities is slightly relevant. The high accumulation of the complexes Cu(L2)2and Cu(L3)2in TA3 tumor cells and the much faster binding to cellular DNA than Cu(L1)2are consistent with thein vitrocytotoxic activities found for these copper complexes.

Structural and functional effects of benzimidazole/thioether–copper complexes with antitumor activity on cell membranes and molecular models

2016 ◽  
Vol 156 ◽  
pp. 98-104 ◽  
Author(s):  
Ivan Castillo ◽  
Mario Suwalsky ◽  
María José Gallardo ◽  
Valentina Troncoso ◽  
Brenda N. Sánchez-Eguía ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Copper Complexes ◽  
Cell Membranes ◽  
Molecular Models

Photoreceptor disk membrane substructures by means of the complementary freeze-fracture-replica methods

1978 ◽  
Vol 36 (2) ◽  
pp. 156-157
Author(s):  
A. Tonosaki ◽  
M. Yamasaki ◽  
H. Washioka ◽  
J. Mizoguchi
Keyword(s):  
Cell Membranes ◽  
Freeze Fracture ◽  
Purple Membrane ◽  
Remarkable Case ◽  
Single Face ◽  
Disk Membrane ◽  
Associated Proteins ◽  
Photoreceptor Membranes

A vertebrate disk membrane is composed of 40 % lipids and 60 % proteins. Its fracture faces have been classed into the plasmic (PF) and exoplasmic faces (EF), complementary with each other, like those of most other types of cell membranes. The hypothesis assuming the PF particles as representing membrane-associated proteins has been challenged by serious questions if they in fact emerge from the crystalline formation or decoration effects during freezing and shadowing processes. This problem seems to be yet unanswered, despite the remarkable case of the purple membrane of Halobacterium, partly because most observations have been made on the replicas from a single face of specimen, and partly because, in the case of photoreceptor membranes, the conformation of a rhodopsin and its relatives remains yet uncertain. The former defect seems to be partially fulfilled with complementary replica methods.

Introduction to Cell Membranes at Molecular Resolution

1978 ◽  
Vol 36 (3) ◽  
pp. 497-502
Author(s):  
R.J. Barrnett
Keyword(s):  
Cell Membranes ◽  
International Federation ◽  
Mountain Range ◽  
Cellular Membranes ◽  
Short History ◽  
Biological Organization ◽  
Macromolecular Assemblies ◽  
The Past

This subject, is like observing the panorama of a mountain range, magnificent towering peaks, but it doesn't take much duration of observation to recognize that they are still in the process of formation. The mountains consist of approaches, materials and methods and the rocky substance of information has accumulated to such a degree that I find myself concentrating on the foothills in the foreground in order to keep up with the advance; the edifices behind form a wonderous, substantive background. It's a short history for such an accumulation and much of it has been moved by the members of the societies that make up this International Federation. My panel of speakers are here to provide what we hope is an interesting scientific fare, based on the fact that there is a continuum of biological organization from biochemical molecules through macromolecular assemblies and cellular membranes to the cell itself. Indeed, this fact explains the whole range of towering peaks that have emerged progressively during the past 25 years.

664: CXCL12/CXCR4 Trans-Activation of HER2 in Lipid Rafts of Prostate Cancer Cell Membranes Promotes Bone Metastasis

2007 ◽  
Vol 177 (4S) ◽  
pp. 223-223
Author(s):  
Sreenivasa R. Chinni ◽  
Hamilto Yamamoto ◽  
Zhong Dong ◽  
Aaron Sabbota ◽  
Sanaa Nabha ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Bone Metastasis ◽  
Lipid Rafts ◽  
Cancer Cell ◽  
Cell Membranes ◽  
Prostate Cancer Cell

710: TNF-Related Apoptosis Inducing Ligand (TRAIL/APO-2L): A Novel Mechanism for BCG-Induced Antitumor Activity

2004 ◽  
Vol 171 (4S) ◽  
pp. 188-189
Author(s):  
Aaron T. Ludwig ◽  
Jill M. Moore ◽  
Yi Luo ◽  
Xiaohong Chen ◽  
Michael A. O’Donnell ◽  
...  
Keyword(s):  
Antitumor Activity
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