ChemInform Abstract: ANTITUMOR ACTIVITY OF 1,2-DIAMINOCYCLOHEXANE-PLATINUM COMPLEXES AGAINST SARCOMA-180 ASCITES FORM

1979 ◽  
Vol 10 (19) ◽  
Author(s):  
Y. KIDANI ◽  
K. INAGAKI ◽  
M. IIGO ◽  
A. HOSHI ◽  
K. KURETANI
1978 ◽  
Vol 21 (12) ◽  
pp. 1315-1318 ◽  
Author(s):  
Yoshinori Kidani ◽  
Kenji Inagaki ◽  
Masaaki Iigo ◽  
Akio Hoshi ◽  
Kazuo Kuretani

1980 ◽  
Vol 2 (1) ◽  
pp. 99-112 ◽  
Author(s):  
R. Megirian ◽  
C. L. Astry ◽  
R. P. Spoor ◽  
L. D. Loose

1985 ◽  
Vol 108 (2) ◽  
pp. 113-115 ◽  
Author(s):  
Sheryl L. Doran ◽  
Abdul R. Khokhar ◽  
Miles P. Hacker

1993 ◽  
Vol 71 (6) ◽  
pp. 880-885 ◽  
Author(s):  
S. Hanessian ◽  
J.-Y. Gauthier ◽  
K. Okamoto ◽  
A.L. Beauchamp ◽  
T. Theophanides

Acyclic vicinal polyol complexes related to cisplatin were synthesized from D-mannitol by stereocontrolled manipulation of the hydroxy groups. Controlled cleavage of a 3,4-diazido hexitol gave the corresponding D-threitol and D-xylitol analogs, which were converted to their diamino platinum complexes. The antitumor activity of these compounds is reported.


2013 ◽  
Vol 16 (11) ◽  
pp. 1004-1012 ◽  
Author(s):  
Ivaneliza Simionato Assis ◽  
Mariane Bonatti Chaves ◽  
Marcia Luciane Lange Silveira ◽  
Regina Maria Miranda Gern ◽  
Elisabeth Wisbeck ◽  
...  

2015 ◽  
Vol 70 (5-6) ◽  
pp. 129-137 ◽  
Author(s):  
Aline L. Xavier ◽  
João Carlos L.R. Pita ◽  
Monalisa T. Brito ◽  
Déborah R.P. Meireles ◽  
Josean F. Tavares ◽  
...  

Abstract The chemical composition, antitumor activity and toxicity of the essential oil from Lippia microphylla leaves (OEL) were investigated. The major constituents were thymol (46.5%), carvacrol (31.7%), p-cymene (9%), and γ-terpinene (2.9%). To evaluate the toxicity of OEL in non-tumor cells, the hemolytic assay with Swiss mice erythrocytes was performed. The concentration producing 50% hemolysis (HC50) was 300 μg/mL. Sarcoma 180 tumor growth was inhibited in vivo 38% at 50 mg/kg, and 60% at 100 mg/kg, whereas 5-FU at 50 mg/kg caused 86% inhibition. OEL displays moderate gastrointestinal and hematological toxicity along with causing some alteration in liver function and morphology. However, the changes were considered reversible and negligible in comparison to the effects of several anticancer drugs. In summary, OEL displays in vivo antitumor activity and a moderate toxicity, which suggests further pharmacological study.


Author(s):  
Soumita Goswami ◽  
Souvik Debnath ◽  
Saumen Karan ◽  
Tapan Kumar Chatterjee

 Objective: PITC-2 was isolated from the methanolic root extract of tissue cultured medicinal plant Pluchea indica (L.) Less. PITC-2 is a thiophene derivative which is 2-(Prop-1-ynyl)-5(5,6-dihydroxyhexa-1,3-diynyl)-thiophene. The main objective of the study is to evaluate the in vivo antitumor activity of PITC 2 against sarcoma-180 cancer cell in Swiss albino mice.Methods: The antitumor activity was evaluated by treatment with PITC-2 at a dose of 2.5 and 5 mg/kg b.w for 21 days on sarcoma-180 mice model. Cell viability was studied using 3-(4, 5- dimethylthiazol -2-yl)-2, 5-diphenyl tetrazolium bromide assay and cell apoptosis, G1 cell cycle arrest and reduction in tumor cell proliferation were evaluated by histopathological analysis and Bcl-2, cyclic-D1, and Ki-67 protein expression through immunohistochemistry study.Results: Precisely, PITC-2 had a cytotoxic effect on various in vitro cancer cells. Significant decreases in solid tumor volume and weight along with increase lifespan also observed. The histopathological and immunohistopathological examination indicates that PITC-2 induces apoptosis, typical morphological changes and suppresses tumor cell proliferation along with G1 cell cycle arrest through the downregulation of the intratumoral expression of Bcl-2, cyclic D1, and Ki-67 and thus highlighting antiproliferative and apoptotic properties against sarcoma-180 in vivo solid tumor model.Conclusion: The present results clearly demonstrate that PITC-2 significantly inhibits sarcoma-180 cell growth in a dose-dependent manner in in vivo mice model. Besides this, the study reveals a comprehensive perception of the possible mechanism behind the antitumor activity of PITC-2 by significant changes in the morphological, hematological, biochemical parameters in sarcoma-180 cells.


1999 ◽  
Vol 380 (11) ◽  
pp. 1287-1294 ◽  
Author(s):  
Daniel Kushev ◽  
Galina Gorneva ◽  
Svetoslav Taxirov ◽  
Nadejda Spassovska ◽  
Konstantin Grancharov

Abstract New platinum(II) complexes of cyclopentanecarboxylic acid hydrazide (cpcah) were prepared, characterized by elemental analysis, IR and 1H NMR spectra, and evaluated for in vitro cytotoxicity in Friend leukemia (FL) and A2780 ovarian tumor cells, induction of apoptosis in FL cells, as well as for in vivo antitumor activity toward murine L1210 leukemia and Lewis lung carcinoma. The spectral analyses indicated a cissquare planar structure of the complexes with hydrazide ligand coordinated via the NH2 group. The compounds exerted significantly lower in vitro and in vivo toxicities as compared with those of cisplatin (cis-diamminedichloroplatinum(II), DDP). On the other hand, the complex [Pt(NH3)(cpcah)Cl2] exhibited antitumor activity against L1210 leukemia in mice comparable to that of cisplatin, resulting at a dose of 42 mg/kg (administered 3 times) in a T/C (mean survival time) of 280%. This compound displayed an in vitro macromolecular synthesis inhibition pattern similar to that of DDP. At concentrations close to the cytostatic ones (10–20 μM) this complex, as well as DDP, was able to induce apoptosis in FL cells as shown by neutral comet assay and morphological analysis. We concluded that there is a correlation between the ability of platinum complexes to induce apoptosis and their antitumor activity.


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