scholarly journals Isolation, Characterization and Antitumour Propirties of the 1,2-Popylenediaminetetraacetate trans-Diaqua-Copper (II)

2000 ◽  
Vol 7 (4) ◽  
pp. 219-224 ◽  
Author(s):  
S. Kamah ◽  
R. Vilaplana ◽  
J. Moreno ◽  
K. Akdi ◽  
G. García-Herdugo ◽  
...  
Keyword(s):  
Antitumour Activity ◽  
Electronic Spectroscopy ◽  
Ovarian Tumour ◽  
Complete Regression ◽  
Sarcoma 180 ◽  
Soluble Compound ◽  
Ft Ir ◽  
Human Ovarian Tumour

A trans-diaquacomplex formed by copper(II) sulphate and the sequestering polyamminopolycarboxylic ligand 1,2-propylenediaminetetraacetic acid (PDTA) has been isolated and characterized by chemical analysis, titrimetry, FT-IR and electronic spectroscopy, Potentiometric and electronic measurements identified the ligand as tetradentate, two nitrogen and two oxygen atoms being bonded to the Cu(II) in planar positions. This octahedral monomeric soluble compound, is an unusual example of a copper (II) substance showing significant in vitro antitumour activity against the human ovarian tumour cells TG (ID50 = 2.29 μM at 48 h) and important in vivo antitumour activity against solid Sarcoma 180 with complete regression of the tumour at a dose of 12.5 mg/Kg body weight.

scholarly journals Synthesis, Characterization and Antitumour Activity of Metal Complexes of 5-Carboxy-2-Thiouracil

1998 ◽  
Vol 5 (1) ◽  
pp. 35-39 ◽  
Author(s):  
Udai P. Singh ◽  
Sudha Singh ◽  
Sukh Mahendra Singh
Keyword(s):  
Metal Complexes ◽  
Room Temperature ◽  
Magnetic Measurements ◽  
Antitumour Activity ◽  
Tumour Cells ◽  
Sarcoma 180 ◽  
X Ray Diffraction ◽  
X Ray

Metal complexes of 5-carboxy-2-thiouracil with Mn(ll), Co(ll), Ni(ll), Cu(ll), Zn(ll) and Cd(ll) ions were synthesized, characterized, and subjected to a screening system for evaluation of antitumour activity against Sarcoma-180 (S-180) tumour cells. The complexes were characterized by elemental analysis, infrared, electronic spectra, room temperature magnetic measurements and powder X-ray diffraction. The antitumour activity results indicate that some complexes have antitumour activity both in vivo and in vitro against S-180 tumour cells.

Cytological changes induced by platinum-thymine in sarcoma-180 cells: Electron microscopy study

1990 ◽  
Vol 48 (3) ◽  
pp. 290-291
Author(s):  
Gustav Ofosu
Keyword(s):  
Mammalian Cells ◽  
Antitumor Agent ◽  
Microscopy Study ◽  
Electron Microscopy Study ◽  
Limiting Factor ◽  
Sarcoma 180 ◽  
Electron Microscopic ◽  
Cytological Changes

Platinum-thymine has been found to be a potent antitumor agent, which is quite soluble in water, and lack nephrotoxicity as the dose-limiting factor. The drug has been shown to interact with DNA and inhibits DNA, RNA and protein synthesis in mammalian cells in vitro. This investigation was undertaken to elucidate the cytotoxic effects of piatinum-thymine on sarcoma-180 cells in vitro ultrastructurally, Sarcoma-180 tumor bearing mice were treated with intraperitoneal injection of platinum-thymine 40mg/kg. A concentration of 60μg/ml dose of platinum-thymine was used in in vitro experiments. Treatments were at varying time intervals of 3, 7 and 21 days for in vivo experiments, and 30, 60 and 120 min., 6, 12, and 24th in vitro. Controls were not treated with platinum-thymine.Electron microscopic analyses of the treated cells in vivo and in vitro showed drastic cytotoxic effect.

scholarly journals A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo

2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Antitumour Activity ◽  
Anticancer Compounds ◽  
Human Cancer Cells ◽  
Cycle Arrest ◽  
Apoptosis Inducer ◽  
Purine Ring

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer.

In Vivo and In Vitro Evaluation of Coated HAp Films with Different Surface Morphology

2007 ◽  
Vol 539-543 ◽  
pp. 710-715
Author(s):  
Kotaro Kuroda ◽  
Ryoichi Ichino ◽  
Masazumi Okido
Keyword(s):  
Bone Formation ◽  
Surface Morphology ◽  
New Bone Formation ◽  
Contact Ratio ◽  
Bone Implant ◽  
Ft Ir ◽  
Mouse Osteoblast ◽  
Surface Morphologies

Hydroxyapatite (HAp) coatings were formed on cp titanium plates and rods by the thermal substrate method in an aqueous solution that included 0.3 mM Ca(H2PO4)2 and 0.7 mM CaCl2. The coating experiments were conducted at 40-140 oC and pH = 8 for 15 or 30 min. The properties for the coated samples were studied using XRD, EDX, FT-IR, and SEM. All the specimens were covered with HAp, which had different surface morphologies such as net-like, plate-like and needle-like. After cleaning and sterilization, all the coated specimens were subjected to in vivo and vitro testing. In the in vitro testing, the mouse osteoblast-like cells (MC3T3-E1) were cultured on the coated and non-coated specimens for up to 30 days. Moreover, the specimens (φ2 x 5 mm) were implanted in rats femoral for up to 8 weeks, the osseoinductivity on them were evaluated. In in vitro evaluations, there were not significant differences between the different surface morphologies. In in vivo evaluations, however, two weeks postimplantation, new bone formed on both the HAp coated and non-coated titanium rods in the cancellous and cortical bone. The bone-implant contact ratio, which was used for the evaluation of new bone formation, was significantly dependent on the surface morphology of the HAp, and the results demonstrated that the needle-like coating appears to promote rapid bone formation.

scholarly journals Overcoming multidrug-resistance in vitro and in vivo using the novel P-glycoprotein inhibitor 1416

2012 ◽  
Vol 32 (6) ◽  
pp. 559-566 ◽  
Author(s):  
Yan Xu ◽  
Feng Zhi ◽  
Guangming Xu ◽  
Xiaolei Tang ◽  
Sheng Lu ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Chemotherapy ◽  
Antitumour Activity ◽  
Multidrug Resistant ◽  
The Novel ◽  
Mice Model ◽  
P Glycoprotein ◽  
Channel Currents

MDR (multidrug-resistance) represents a major obstacle to successful cancer chemotherapy and is usually accomplished by overexpression of P-gp (P-glycoprotein). Much effort has been devoted to developing P-gp inhibitors to modulate MDR. However, none of the inhibitors on the market have been successful. 1416 [1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (phenoprolamine hydrochloride)] is a new VER (verapamil) analogue with a higher IC50 for blocking calcium channel currents than VER. In the present paper, we examined the inhibition effect of 1416 on P-gp both in vitro and in vivo. 1416 significantly enhanced cytotoxicity of VBL (vinblastine) in P-gp-overexpressed human multidrug-resistant K562/ADM (adriamycin) and KBV cells, but had no such effect on the parent K562 and KB cells. The MDR-modulating function of 1416 was further confirmed by increasing intracellular Rh123 (rhodanmine123) content in MDR cells. Human K562/ADM xenograft-nude mice model verified that 1416 potentiates the antitumour activity of VBL in vivo. RT-PCR (reverse transcriptase-PCR) and FACS analysis demonstrated that the expression of MDR1/P-gp was not affected by 1416 treatment. All these observations suggest that 1416 could be a promising agent for overcoming MDR in cancer chemotherapy.

AN ENHANCEMENT OF SOLUBILITY OF PIOGLITAZONE HYDROCHLORIDE USING LIQUISOLID TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 36-39
Author(s):  
S Deshmane ◽  
◽  
K Gandhi ◽  
S. Nagpure ◽  
A. Sawant ◽  
...  
Keyword(s):  
Mathematical Model ◽  
Drug Release ◽  
Dissolution Rate ◽  
In Vivo Study ◽  
Dimethyl Acetamide ◽  
Volatile Liquid ◽  
Ft Ir ◽  
Ir Study

The new mathematical model was developed by studying angle of slide using N, N-dimethyl acetamide, non-volatile liquid vehicle and prepared liquisolid tablets, in which the different concentrations of non-volatile liquid adsorbed over carrier and coating material separately. Both DSC and FT-IR study showed better compatibility and stability. The optimized formulation showed higher drug release during in-vitro and in-vivo study against conventional and marketed preparation. The present work concludes that N, N-dimethyl acetamide enhanced the solubility of pioglitazone HCl with higher dissolution rate through liquisolid technique.

scholarly journals BET bromodomain inhibitor birabresib in mantle cell lymphoma: in vivo activity and identification of novel combinations to overcome adaptive resistance

ESMO Open ◽  
2018 ◽  
Vol 3 (6) ◽  
pp. e000387 ◽  
Author(s):  
Chiara Tarantelli ◽  
Elena Bernasconi ◽  
Eugenio Gaudio ◽  
Luciano Cascione ◽  
Valentina Restelli ◽  
...  
Keyword(s):  
Mantle Cell Lymphoma ◽  
Cell Lines ◽  
Cell Lymphoma ◽  
Antitumour Activity ◽  
Single Agent ◽  
Treatment Strategies ◽  
Bet Inhibitor ◽  
Mantle Cell

BackgroundThe outcome of patients affected by mantle cell lymphoma (MCL) has improved in recent years, but there is still a need for novel treatment strategies for these patients. Human cancers, including MCL, present recurrent alterations in genes that encode transcription machinery proteins and of proteins involved in regulating chromatin structure, providing the rationale to pharmacologically target epigenetic proteins. The Bromodomain and Extra Terminal domain (BET) family proteins act as transcriptional regulators of key signalling pathways including those sustaining cell viability. Birabresib (MK-8628/OTX015) has shown antitumour activity in different preclinical models and has been the first BET inhibitor to successfully undergo early clinical trials.Materials and methodsThe activity of birabresib as a single agent and in combination, as well as its mechanism of action was studied in MCL cell lines.ResultsBirabresib showed in vitro and in vivo activities, which appeared mediated via downregulation of MYC targets, cell cycle and NFKB pathway genes and were independent of direct downregulation of CCND1. Additionally, the combination of birabresib with other targeted agents (especially pomalidomide, or inhibitors of BTK, mTOR and ATR) was beneficial in MCL cell lines.ConclusionOur data provide the rationale to evaluate birabresib in patients affected by MCL.

scholarly journals Antitumour activity of XR5944 in vitro and in vivo in combination with 5-fluorouracil and irinotecan in colon cancer cell lines

2005 ◽  
Vol 92 (4) ◽  
pp. 722-728 ◽  
Author(s):  
S M Harris ◽  
P Mistry ◽  
C Freathy ◽  
J L Brown ◽  
P A Charlton
Keyword(s):  
Colon Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumour Activity ◽  
Cancer Cell Lines ◽  
Colon Cancer Cell ◽  
Colon Cancer Cell Lines

Mechanism of Action of the Antitumour Effect of K18

1989 ◽  
Vol 17 (2) ◽  
pp. 132-140
Author(s):  
T. Fujii ◽  
K. Niimura ◽  
T. Furusho ◽  
N. Sugita ◽  
M. Oikawa ◽  
...  
Keyword(s):  
Nude Mice ◽  
Immunoglobulin G ◽  
Antitumour Activity ◽  
Inhibitory Effect ◽  
Human Lung Cancer ◽  
Covalently Bonded ◽  
Human Lung Cancer Cells ◽  
Rpmi 8226

K18 is an anticancer drug for oral administration comprising about five molecules of melphalan, an alkylating drug, covalently bonded to human immunoglobulin G. This study measured the in vitro antitumour activity of K18, melphalan and immunoglobulin G on human myeloma cells (RPMI-8226) and the in vivo antitumour effects of K18 and melphalan in BALB/c nude mice bearing human lung cancer cells (LC-10). The relative tumour-inhibitory effect, in vitro, was found to be: immunoglobulin G <K18 <melphalan. This activity of K18 was about half the theoretical value indicating that melphalan molecules are not released easily from the conjugate. K18 showed strong antitumour activity in vivo which continued after stopping administration. On the other hand, the effects of melphalan did not continue after administration was stopped. The distribution of [125I]K18 and [14C]melphalan was examined in BALB/c nude mice 14 days after implantation of LC-10 cells. Radioactivity levels in the major organs showed a transient rapid increase followed by a gradual decline. In tumours, [14C]melphalan levels increased transiently and then decreased, whereas [125I]K18 levels persisted following intravenous administration.

In Vivo and in Vitro Proliferation Kinetics of Sarcoma 180 in Solid Form

1972 ◽  
Vol 58 (5) ◽  
pp. 335-339 ◽  
Author(s):  
Rosella Silvestrini ◽  
Ornella Sanfilippo ◽  
Luigi Lenaz
Keyword(s):  
Double Labelling ◽  
Pulse Labelling ◽  
Sarcoma 180 ◽  
In Vitro Proliferation ◽  
Proliferation Kinetics ◽  
Human Solid Tumors ◽  
A Cell ◽  
Kinetics Of

In order to obtain data for setting up a rapid and relatively inexpensive method for studying the proliferation kinetics of human solid tumors, we have determined the kinetic parameters of an experimental solid tumor (Sarcoma 180). The curve of labelled mitosis after pulse labelling with 3H thymidine and the 3H and 14C thymidine double labelling technic on tumor samples incubated in vitro with the labelled precursors were used. A method of digestion of the tissue with hyaluronidase to obtain a cell suspension is described. This method allows easy identification of cells labelled with 3H or 14C thymidine. The two methods yielded reproducible results, the labelling index being 45%, and the duration of S phase 9.9 hours. The in vitro double labelling method with subsequent hyaluronidase digestion is proposed for studying the proliferation kinetics of solid malignancies.

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