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1

Cytotoxicity and inhibitory properties against topoisomerase II of doxorubicin and its formamidine derivatives

100%
Kik K., Studzian K., Wasowska-Lukawska M., Oszczapowicz I., Szmigiero L.
Acta Biochimica Polonica
|
2009
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tom 56
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nr 1
135-142
 This work was undertaken to compare cytotoxicity, DNA damaging properties and effect on DNA cleavage by topoisomerase II of the anthracycline drug doxorubicin (DOX) and its two derivatives with a formamidino group containing a cyclic amine moiety such as morpholine (DOXM) or hexamethyleneimine (DOXH). The tetrazolium dye colorimetric assay was used to determine the cytotoxic activity of anthracyclines toward L1210 leukemia cells. DNA damage was measured by alkaline elution technique. The effect of anthracyclines on DNA cleavage was studied in a cell-free system containing supercoiled pBR322 DNA and purified human topoisomerase II. The cytotoxicity data and the results of studies on the mechanism of DNA break formation by anthracyclines at the cellular level and in the cell-free system showed that the presence of the formamidino group in the doxorubicin molecule reduced its ability to stimulate DNA cleavage by DNA topoisomerase II. Conclusion: DNA topoisomerase II is not a primary cellular target for DOXM or DOXH. An advantageous feature of formamidinoanthracyclines is their mechanism of cytotoxic action which is not related to the inhibition of DNA topoisomerase II. Therefore this class of anthracyclines seems to be a good source for selection of an anticancer drug directed toward cancer cells with the developed multidrug resistance attributed to the presence of altered DNA topoisomerase II.
2

Alpha-1-acute phase globulin in the blood of tunicamycin-injected rats. Isolation of the non-glycosylated form, its inhibitory properties and synthesis in liver slices

84%
Koj A., Bereta J., Dubin A., Kurdowska A., Chindemi P., Regoeczi E.
Folia Histochemica et Cytobiologica
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1986
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tom 24
|
nr 1
3

Studies on the inhibitory properties of leaf ethanolic extracts obtained from Ficus (Moraceae) species against Aeromonas spp. strains

84%
Pekala-Safinska A., Tkachenko H., Kurhaluk N., Buyun L., Osadowski Z., Honcharenko V., Prokopiv A.
Journal of Veterinary Research
|
2021
|
tom 65
|
nr 1
4
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In vitro control of tomato (Solanum lycopersicon L.) fruit rot caused by fungi using two plant extracts

67%
Okey E. N., Akwaji P. I., Akpan J. B., Umana E. J., Bassey G. A.
International Letters of Natural Sciences
|
2016
|
tom 52
The inhibitory properties of the ethanolic and methanolic leaf extracts of Vernonia amygdalina and Cola acuminata on the fungal pathogens isolated from infected tomato fruits were investigated. The pathogens were Fusarium moniliformes and Rhizopus stolonifer. Various concentrations of the extracts ranging from 10, 20, 30, 40, 50, 60, 70, 80, 90 and 100% were separately added to PDA media. The fungal pathogens were separately inoculated into the media and incubated for seven days. Antifungal effects of these extracts on the mycelia growth of the pathogens were significant at P<0.05 for all treatments at higher concentrations. At 10-50% concentration, ethanolic and methanolic extracts of Vernonia amygdalina and Cola acuminata had no significant effect on the mycelia growth of Fusarium moniliformes and Rhizopus stolonifer after seven days observation period. At 60-100% concentrations, the two pathogens were completely inhibited by ethanolic extracts of Vernonia amygdalina and Cola acuminata. Methanolic extracts of Vernonia amygdalina and Cola acuminata inhibited completely Fusarium moniliformes and Rhizopus stolonifer at 80-100% concentrations. The in vitro inhibitory effects of these extracts at higher concentrations indicated that they can be used for the control of tomato fruit rot. It may be necessary to use them in prolonging the shelf-life of fresh tomato fruit and some other fruits.
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