Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties
Само за регистроване кориснике
2010
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
In the present investigations five new derivatives of betulinic and betulonic acid were synthesized and the effect of this structural variations on anticancer activity was studied and discussed. The antiproliferative activity of betulinic and betulonic acid derivatives was studied against eight tumor cell lines of different histogenic origin. The derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. The apoptotic mode of cell death on colon cancer cell line HT-29 was induced by the most active compounds 5, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl (3-O-acetyl)betulinate, and 9, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl betulonate. Treatment of HT-29 cells with 5 and 9 induced apoptosis, as observed by dye exclusion test (trypan blue) and by the appearance of a typical ladder pattern in the DNA fragmentation assay and FITC annexin V assay. Cell cycle perturbations caused by compound 5 are also presented.
Кључне речи:
Betulinic acid / Betulonic acid / Antitumoral activity / Apoptosis / Cell cycleИзвор:
European Journal of Medicinal Chemistry, 2010, 45, 8, 3346-3353Издавач:
- Elsevier
DOI: 10.1016/j.ejmech.2010.04.018
ISSN: 02235234
PubMed: 20472329
WoS: 000279521800011
Scopus: 2-s2.0-77954315717
Институција/група
IHTMTY - JOUR AU - Kommera, Harish AU - Kaluđerović, Goran N. AU - Kalbitz, Jutta AU - Dräger, Birgit AU - Paschke, Reinhard PY - 2010 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/3179 AB - In the present investigations five new derivatives of betulinic and betulonic acid were synthesized and the effect of this structural variations on anticancer activity was studied and discussed. The antiproliferative activity of betulinic and betulonic acid derivatives was studied against eight tumor cell lines of different histogenic origin. The derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. The apoptotic mode of cell death on colon cancer cell line HT-29 was induced by the most active compounds 5, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl (3-O-acetyl)betulinate, and 9, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl betulonate. Treatment of HT-29 cells with 5 and 9 induced apoptosis, as observed by dye exclusion test (trypan blue) and by the appearance of a typical ladder pattern in the DNA fragmentation assay and FITC annexin V assay. Cell cycle perturbations caused by compound 5 are also presented. PB - Elsevier T2 - European Journal of Medicinal Chemistry T1 - Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties VL - 45 IS - 8 SP - 3346 EP - 3353 DO - 10.1016/j.ejmech.2010.04.018 ER -
@article{ author = "Kommera, Harish and Kaluđerović, Goran N. and Kalbitz, Jutta and Dräger, Birgit and Paschke, Reinhard", year = "2010", abstract = "In the present investigations five new derivatives of betulinic and betulonic acid were synthesized and the effect of this structural variations on anticancer activity was studied and discussed. The antiproliferative activity of betulinic and betulonic acid derivatives was studied against eight tumor cell lines of different histogenic origin. The derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. The apoptotic mode of cell death on colon cancer cell line HT-29 was induced by the most active compounds 5, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl (3-O-acetyl)betulinate, and 9, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl betulonate. Treatment of HT-29 cells with 5 and 9 induced apoptosis, as observed by dye exclusion test (trypan blue) and by the appearance of a typical ladder pattern in the DNA fragmentation assay and FITC annexin V assay. Cell cycle perturbations caused by compound 5 are also presented.", publisher = "Elsevier", journal = "European Journal of Medicinal Chemistry", title = "Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties", volume = "45", number = "8", pages = "3346-3353", doi = "10.1016/j.ejmech.2010.04.018" }
Kommera, H., Kaluđerović, G. N., Kalbitz, J., Dräger, B.,& Paschke, R.. (2010). Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties. in European Journal of Medicinal Chemistry Elsevier., 45(8), 3346-3353. https://doi.org/10.1016/j.ejmech.2010.04.018
Kommera H, Kaluđerović GN, Kalbitz J, Dräger B, Paschke R. Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties. in European Journal of Medicinal Chemistry. 2010;45(8):3346-3353. doi:10.1016/j.ejmech.2010.04.018 .
Kommera, Harish, Kaluđerović, Goran N., Kalbitz, Jutta, Dräger, Birgit, Paschke, Reinhard, "Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties" in European Journal of Medicinal Chemistry, 45, no. 8 (2010):3346-3353, https://doi.org/10.1016/j.ejmech.2010.04.018 . .