ChemInform Abstract: Structure of Sch 49209: A Novel Antitumor Agent from the Fungus Nattrassia mangiferae.

ChemInform ◽  
2010 ◽  
Vol 25 (32) ◽  
pp. no-no
Author(s):  
M. CHU ◽  
I. TRUUMEES ◽  
M. G. PATEL ◽  
V. P. GULLO ◽  
M. S. PUAR ◽  
...  
1994 ◽  
Vol 59 (5) ◽  
pp. 1222-1223 ◽  
Author(s):  
Min Chu ◽  
Imbi Truumees ◽  
Mahesh G. Patel ◽  
Vincent P. Gullo ◽  
Mohindar S. Puar ◽  
...  

Author(s):  
S.K. Aggarwal ◽  
J. San Antonio

Cisplatin (cis-dichlorodiammineplatinum(II)) a potent antitumor agent is now available for the treatment of testicular and ovarian cancers. It is however, not free from its serious side effects including nephrotoxicity, gastro intestinal toxicity, myelosuppression, and ototoxicity. Here we now report that the drug produces peculiar bloating of the stomach in rats and induces acute ulceration.Wistar-derived rats weighing 200-250 g were administered cisplatin(9 mg/kg) ip as a single dose in 0.15 M NaCl. After 3 days the animals were sacrificed by decapitation. The stomachs were removed, the contents analyzed for pepsin and acidity. The inner surface was examined with a dissecting microscope after a moderate stretching for ulcers. Affected areas were fixed and processed for routine electron microscopy and enzyme cytochemistry.The drug treated animals kept on food and water consistently showed bloating and lesions (Fig. 1) with a frequency of 6-70 ulcers in the rumen section of the stomachs.


Author(s):  
S.K. Aggarwal ◽  
J.M. Fadool

Cisplatin (CDDP) a potent antitumor agent suffers from severe toxic side effects with nephrotoxicity being the major dose-limiting factor, The primary mechanism of its action has been proposed to be through its cross-linking DNA strands. It has also been shown to inactivate various transport enzymes and induce hypocalcemia and hypomagnesemia that may be the underlying cause for some of its toxicities. The present is an effort to study its influence on the parathyroid gland for any hormonal changes that control calcium levels in the body.Male Swiss Wistar rats (Crl: (WI) BR) weighing 200-300 g and of 60 days in age were injected (ip) with cisplatin (7mg/kg in normal saline). The controls received saline injections only. The animals were injected (iv) with calcium (0.5 ml of 10% calcium gluconate/day) and were killed by decapitation on day 1 through 5. Trunk blood was collected in heparinized tubes.


Author(s):  
Gustav Ofosu

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.


Author(s):  
Kenji Ikeda ◽  
Yusuke Kawamura ◽  
Masahiro Kobayashi ◽  
Taito Fukushima ◽  
Yushi Sorin ◽  
...  

Background: Although DC Bead has been useful in treatment of multiple and large hepatocellular carcinoma, loading time of doxorubicin into the DC Bead takes a long time of 30-120 minutes. Epirubicin is also used as an antitumor agent together with DC Bead, but its loading efficiency was not sufficiently elucidated. Methods: To shorten loading time of epirubicin into DC Bead (100-300µm, 300-500µm, 500-700µm), we examined the following three methods after mixing the drug: (a) let stand in room temperature, (b) agitated for 30 seconds with Vortex mixer, and (c) sonicated for 30 seconds with ultrasonic cleaner. After loading of epirubicin by each method, supernatant concentration for epirubicin was assayed at 5, 10, 30, 60, and 120 minutes. Results: Epirubicin loading rates for small bead (100-300µm) at 5 minutes were 82.9 % in group a, 93.8% in group b, and 79.9 % in group c. Similarly, medium bead (300-500µm), 40.1% in group a, 65.7% in group b and 45.5% in group c, respectively. In large-sized bead (500-700µm), loaded rates of epirubicin were 38.8% in group a, 59.0% in group b and 48.0% in group c. Agitation of mixture of epirubicin and DC Bead with Vortex mixer significantly shortened the loading time, but sonication did not affect the time required. Microscopic examination did not lead to any morphological change of microspheres in all the methods. Conclusions: Short time of agitation with Vortex mixer reduced the necessary time for loading of epirubicin in every standard of DC Bead.


2012 ◽  
Vol 20 (2) ◽  
pp. 159-166 ◽  
Author(s):  
L.P. Deng ◽  
J. Dong ◽  
H. Cai ◽  
W. Wang

2010 ◽  
Vol 999 (999) ◽  
pp. 1-9
Author(s):  
D. Santini ◽  
V. Virzi ◽  
M. E. Fratto ◽  
F. Bertoldo ◽  
R. Sabbatini ◽  
...  

2020 ◽  
Vol 17 (1) ◽  
pp. 33-39
Author(s):  
Karen C. Vargas-Castro ◽  
Ana M. Puebla Pérez ◽  
Irma I. Rangel-Salas ◽  
Jorge I. Delgado-Saucedo ◽  
José B. Pelayo-Vázquez ◽  
...  

Background: In the therapy of cancer, several treatments have been designed using nanomaterials, among which gold nanoparticles (AuNPs) have been featured as a promising antitumoral agent. Our research group has developed the synthesis of gold nanoparticles L-AuNPs and D-AuNPs stabilized with zwitterions of imidazolium (L-1 and D-1) derived from L-methionine and D-methionine. Because the stabilizer agent is chiral, we observed through circular dichroism that AuNPs also present chirality; such chirality as well as the fact that the stabilizing agent contains fragments of methionine and imidazolium that are commonly involved in biological processes, opens up the possibility that this system may have biological compatibility. Additionally, the presence of methionine in the stabilizing agent opens the application of this system as a possible antitumor agent because methionine is involved in methylation processes of molecules such as DNA. Objective: The aim of this research is the evaluation of the antitumor activity of gold nanoparticles stabilized with zwitterions of imidazolium (L-AuNPs) derived from L-methionine in the model of BALB/c mice with lymphoma L5178Y. Methods: Taking as a parameter cell density, the evaluation of the inhibitory effect of L-AuNPs was carried out with a series of in vivo tests in BALB/c type mice; three groups of five mice each were formed (Groups 1, 2 and 3); all mice were i.p. inoculated with the lymphoblast murine L5178Y. Group 1 consisted of mice without treatment. In the Groups 2 and 3 the mice were treated with L-AuNPs at 0.3 mg/Kg on days 1, 7 and 14 by orally and intraperitonally respectively. Results: These results show low antitumor activity of these gold nanoparticles (L-NPsAu) but interestingly, the imidazolium stabilizing agent of gold nanoparticle (L-1) displayed promising antitumor activity. On the other hand, the enantiomer of L-1, (D-1) as well as asymmetric imidazole derivate from L-methionine (L-2), do not exhibit the same activity as L-1. Conclusion: The imidazolium stabilizing agent (L-1) displayed promising antitumor activity. Modifications in the structure of L-1 showed that, the stereochemistry (like D-1) and the presence of methionine fragments (like L-2) are determinants in the antitumor activity of this compound.


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