Triazene metabolism. III. In vitro cytotoxicity towards M21 cells and in vivo antitumour activity of the proposed metabolites of the antitumour 1-aryl-3,3-dimethyltriazenes

1984 ◽  
Vol 62 (4) ◽  
pp. 396-402 ◽  
Author(s):  
Douglas J. Kohlsmith ◽  
Keith Vaughan ◽  
Stephen J. Luner
Keyword(s):  
Cell Line ◽  
Chemical Stability ◽  
Active Metabolite ◽  
Melanoma Cell Line ◽  
Antitumour Activity ◽  
Metabolic Activation ◽  
In Vitro Cytotoxicity ◽  
Structural Analogues

In vitro cytotoxicity of a series of antitumour triazenes towards the M21 melanoma cell line has been studied. Dimethyltriazenes are structural analogues of 5-(3,3-dimethyl-1-triazeno-)imidazole-4-carboxamide (Dacarbazine) and are inactive, which is consistent with the requirement for metabolic activation. Monomethyltriazenes and hydroxymethyltriazenes, the proposed metabolites of the dimethyltriazenes, are cytotoxic to the M21 cell line. A new series of 4-hydroxy-1,2,3-benzotriazines has been tested for in vitro cytotoxicity. A series of monoalkyltriazenes (Ar∙N=N∙NHR) has been tested for antitumour activity against the P388 lymphoma in vivo. Only monomethyltriazenes had significant antitumour activity, which supports the hypothesis that the monomethyltriazene is the active metabolite of the antitumour dimethyltriazenes. The activity of monomethyltriazenes in vivo is correlated with the chemical stability and t1/2 measurements in pH 7.5 phosphate buffer.

scholarly journals CARMUSTINE LOADED NANOSIZE LIPID VESICLES SHOWED PREFERENTIAL CYTOTOXICITY AND INTERNALIZATION IN U87MG CELL LINE ALONG WITH IMPROVED PHARMACOKINETIC PROFILE IN MICE: A STRATEGY FOR TREATMENT OF GLIOMA

2020 ◽  
pp. 240-248
Author(s):  
BHABANI SANKAR SATAPATHY ◽  
JNANRANJAN PANDA
Keyword(s):  
Electron Microscopy ◽  
Cell Line ◽  
Drug Loading ◽  
Lipid Vesicles ◽  
Pharmacokinetic Profile ◽  
In Vitro Cytotoxicity ◽  
Pharmacokinetic Data ◽  
Transmission Electron

Objective: Successful treatment of glioma still remains a tough challenge. The present study aims at the development and evaluation of carmustine loaded nanosize phospholipid vesicles (CNLVs) for the treatment of glioma. Methods: The experimental NLVs were developed by conventional lipid layer hydration technique and were characterized by different in vitro tools such as diffraction light scattering (DLS), zeta potential, field emission scanning electron microscopy (FESEM), cryo-transmission electron microscopy (cryo-TEM), in vitro drug loading capacity, drug release study etc. In vitro cytotoxicity and cellular uptake of the optimized drug-loaded NLVs were carried out in U87MG human glioblastoma cell line. In vivo pharmacokinetic study was conducted in Swiss albino mice. Results: DLS data showed an average vesicle diameter of 92 nm with narrow size distribution. Optimized CNLVs were spherical in shape with a smooth surface as depicted from FESEM data. Cryo-TEM study confirmed formation of unilamellar vesicles with intact outer bilayer. A reasonable drug loading of 7.8 % was reported for the optimized CNLVs along with a sustained release of CS over a 48 h study period. In vitro cytotoxicity assay revealed a considerable higher toxicity of CNLVs than free drugs in the U87MG cells. Confocal microscopy showed a satisfactory internalization of the optimized drug-loaded NLVs in the tested cell line. Pharmacokinetic data demonstrated an enhanced mean residence time of optimized CNLVs in blood than free drug. Conclusion: Results depicted the potential of experimental CNLVs for the treatment of glioma after further in vivo tests.

Correlation of the in vitro cytotoxicity of ethyldeshydroxysparsomycin and cisplatin with the in vivo antitumour activity in murine L1210 leukaemia and two resistant L1210 sublcones

1993 ◽  
Vol 31 (4) ◽  
pp. 289-294 ◽  
Author(s):  
H. P. Hofs ◽  
D. J. T. Wagener ◽  
V. de Valk-Bakker ◽  
H. van Rennes ◽  
A. J. van Zeist ◽  
...  
Keyword(s):  
Antitumour Activity ◽  
In Vitro Cytotoxicity

scholarly journals Cholesterol-Based Nanovesicles Enhance the In Vitro Cytotoxicity, Ex Vivo Intestinal Absorption, and In Vivo Bioavailability of Flutamide

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1741
Author(s):  
Mohamed A. Ali ◽  
Magdy I. Mohamed ◽  
Mohamed A. Megahed ◽  
Tamer M. Abdelghany ◽  
Khalid M. El-Say
Keyword(s):  
Prostate Cancer ◽  
Adverse Effects ◽  
Cell Line ◽  
Oral Bioavailability ◽  
Ex Vivo ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Rabbit Intestine

Critical adverse effects and frequent administration, three times per day, limit the use of flutamide (FLT) as a chemotherapeutic agent in the treatment of prostate cancer. Therefore, our research aimed to develop new cholesterol-based nanovesicles for delivering FLT to malignant cells in an endeavor to maximize its therapeutic efficacy and minimize undesired adverse effects. Draper–Lin small composite design was used to optimize the critical quality attributes of FLT-loaded niosomes and ensure the desired product quality. The influence of the selected four independent variables on mean particle size (Y1), zeta potential (Y2), drug entrapment efficiency (Y3), and the cumulative drug release after 24 h (Y4) was examined. The optimized nanovesicles were assessed for their in vitro cytotoxicity, ex-vivo absorption via freshly excised rabbit intestine as well as in vivo pharmacokinetics on male rats. TEM confirmed nanovescicles’ spherical shape with bilayer structure. Values of dependent variables were 748.6 nm, −48.60 mV, 72.8% and 72.2% for Y1, Y2, Y3 and Y4, respectively. The optimized FLT-loaded niosomes exerted high cytotoxic efficacy against human prostate cancer cell line (PC-3) with an IC50 value of 0.64 ± 0.04 µg/mL whilst, it was 1.88 ± 0.16 µg/mL for free FLT. Moreover, the IC50 values on breast cancer cell line (MCF-7) were 0.27 ± 0.07 µg/mL and 4.07 ± 0.74 µg/mL for FLT-loaded niosomes and free FLT, respectively. The permeation of the optimized FLT-loaded niosomes through the rabbit intestine showed an enhancement ratio of about 1.5 times that of the free FLT suspension. In vivo pharmacokinetic study displayed an improvement in oral bioavailability of the optimized niosomal formulation with AUC and Cmax values of 741.583 ± 33.557 μg/mL × min and 6.950 ± 0.45 μg/mL compared to 364.536 ± 45.215 μg/mL × min and 2.650 ± 0.55 μg/mL for the oral FLT suspension. With these promising findings, we conclude that encapsulation of FLT in cholesterol-loaded nanovesicles enhanced its anticancer activity and oral bioavailability which endorse its use in the management of prostate cancer.

Inhibition of metastatic potential of B16-F10 melanoma cell line in vivo and in vitro by biflorin

Life Sciences ◽  
2013 ◽  
Vol 93 (5-6) ◽  
pp. 201-207 ◽  
Author(s):  
Adriana Andrade Carvalho ◽  
Patrícia Marçal da Costa ◽  
Luciana Gregório Da Silva Souza ◽  
Telma Leda G. Lemos ◽  
Ana Paula Negreiros Nunes Alves ◽  
...  
Keyword(s):  
Cell Line ◽  
Melanoma Cell ◽  
Melanoma Cell Line ◽  
Metastatic Potential

scholarly journals An In Vitro-In Vivo Evaluation of the Antiproliferative and Antiangiogenic Effect of Flavone Apigenin against SK-MEL-24 Human Melanoma Cell Line

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Alexandra Ghiƫu ◽  
Ioana Zinuca Pavel ◽  
Stefana Avram ◽  
Brigitta Kis ◽  
Daliana Minda ◽  
...  
Keyword(s):  
Cell Line ◽  
Melanoma Cell ◽  
Melanoma Cell Line ◽  
Human Melanoma ◽  
Human Melanoma Cell Line ◽  
Human Melanoma Cell ◽  
Cell Growth And Migration ◽  
Vitro Effect

One of the most important class of natural compounds with successful preclinical results in the management of cancer is the flavonoids. Due to the plethora of biological activities, apigenin (4 ′ ,5,7 trihydroxyflavone) is a main representant of the flavone subclass. Although the antiproliferative and antiangiogenic effects of apigenin were studied on a significant number of human and murine melanoma cell lines, in order to complete the data existing in the literature, the aim of this study is to evaluate the in vitro effect of apigenin on SK-MEL-24 human melanoma cell line as well as in vivo on tumor angiogenesis using the aforementioned cell line on the chorioallantoic membrane assay. Results have shown that in the range of tested doses, the phytocompound presents significant antiproliferative, cytotoxic, and antimigratory potential at 30 μM, respectively, 60 μM. Moreover, the phytocompound in both tested concentrations limited melanoma cell growth and migration and induced a reduced angiogenic reaction limiting melanoma cell development.

Chitosan-Coated Lipid-Core Nanocapsules Functionalized with Gold-III and Bevacizumab Induced In Vitro Cytotoxicity against C6 Cell Line and In Vivo Potent Antiangiogenic Activity

2020 ◽  
Vol 37 (6) ◽  
Author(s):  
Aline de Cristo Soares Alves ◽  
Vladimir Lavayen ◽  
Fabrício Figueiró ◽  
Danieli Rosane Dallemole ◽  
Amanda de Fraga Dias ◽  
...  
Keyword(s):  
Cell Line ◽  
In Vitro Cytotoxicity ◽  
Lipid Core ◽  
Antiangiogenic Activity ◽  
C6 Cell Line
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