Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog
Background: The major triterpene glycoside of the sea cucumber Psolus patagonicus and its desulfated analog were tested for their antiproliferative, cytotoxic and hemolytic activities, and their effect on NF-κB activation. Methods: The antiproliferative action of glycosides 1 and 2 were determined o...
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todo:paper_00093157_v55_n1_p60_Careaga2023-10-03T14:08:38Z Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog Careaga, V.P. Bueno, C. Muniain, C. Alché, L. Maier, M.S. Antiproliferation Cytotoxicity Nuclear factor-kappa B Psolus patagonicus Sea cucumber Triterpene glycosides aglycone antineoplastic agent glycoside hydroxyl group I kappa B alpha immunoglobulin enhancer binding protein patagonicoside a triterpene derivative tumor necrosis factor alpha unclassified drug animal cell article cancer inhibition cell proliferation cell viability chronic inflammation controlled study disease association drug activity drug cytotoxicity drug effect drug isolation drug mechanism drug screening hemolysis human human cell IC 50 immunofluorescence mouse nonhuman priority journal protein degradation Psolus patagonicus sea cucumber staining structure activity relation tumor cell line Western blotting Background: The major triterpene glycoside of the sea cucumber Psolus patagonicus and its desulfated analog were tested for their antiproliferative, cytotoxic and hemolytic activities, and their effect on NF-κB activation. Methods: The antiproliferative action of glycosides 1 and 2 were determined on 3 tumor cell lines. Their effect on the activation of NF-κB was evaluated by indirect immunofluorescence assay staining and the concomitant IκBα degradation was studied by Western blot. Results: Both compounds were able to suppress the growth of 3 tumor cell lines (Hep3B, MDA-MB231 and A549) and induced the activation of NF-κB, a key player linking chronic inflammation and cancer, concomitant with IκBα degradation in the A549 tumor cell line. Compounds 1 and 2 showed hemolytic activity with half maximal inhibitory concentration (IC50) values around 80 μM. Conclusions: Both glycosides showed low cytotoxic activity in A549 tumor cells in comparison with sea cucumber triterpene glycosides containing a linear tetrasaccharide chain. This could be a result of the uncommon presence of two 12α- and 17α-hydroxyl groups and a Δ7 double bond in the aglycone moiety. This aglycone functionalization may be related to their low membranolytic activity. Although glycosides 1 and 2 exert an antiproliferative effect, their mechanisms of action do not involve inhibition of NF-κB. Recently, it has been shown that diverse and new mechanisms of action are responsible for the antitumor and cytotoxic activities of marine compounds. Therefore, more extensive studies are needed to establish a mechanism of action and to deduce a clear structure-activity relationship of sea cucumber triterpene glycosides. Copyright © 2008 S. Karger AG. Fil:Careaga, V.P. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Bueno, C. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Alché, L. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Maier, M.S. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00093157_v55_n1_p60_Careaga |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Antiproliferation Cytotoxicity Nuclear factor-kappa B Psolus patagonicus Sea cucumber Triterpene glycosides aglycone antineoplastic agent glycoside hydroxyl group I kappa B alpha immunoglobulin enhancer binding protein patagonicoside a triterpene derivative tumor necrosis factor alpha unclassified drug animal cell article cancer inhibition cell proliferation cell viability chronic inflammation controlled study disease association drug activity drug cytotoxicity drug effect drug isolation drug mechanism drug screening hemolysis human human cell IC 50 immunofluorescence mouse nonhuman priority journal protein degradation Psolus patagonicus sea cucumber staining structure activity relation tumor cell line Western blotting |
| spellingShingle |
Antiproliferation Cytotoxicity Nuclear factor-kappa B Psolus patagonicus Sea cucumber Triterpene glycosides aglycone antineoplastic agent glycoside hydroxyl group I kappa B alpha immunoglobulin enhancer binding protein patagonicoside a triterpene derivative tumor necrosis factor alpha unclassified drug animal cell article cancer inhibition cell proliferation cell viability chronic inflammation controlled study disease association drug activity drug cytotoxicity drug effect drug isolation drug mechanism drug screening hemolysis human human cell IC 50 immunofluorescence mouse nonhuman priority journal protein degradation Psolus patagonicus sea cucumber staining structure activity relation tumor cell line Western blotting Careaga, V.P. Bueno, C. Muniain, C. Alché, L. Maier, M.S. Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog |
| topic_facet |
Antiproliferation Cytotoxicity Nuclear factor-kappa B Psolus patagonicus Sea cucumber Triterpene glycosides aglycone antineoplastic agent glycoside hydroxyl group I kappa B alpha immunoglobulin enhancer binding protein patagonicoside a triterpene derivative tumor necrosis factor alpha unclassified drug animal cell article cancer inhibition cell proliferation cell viability chronic inflammation controlled study disease association drug activity drug cytotoxicity drug effect drug isolation drug mechanism drug screening hemolysis human human cell IC 50 immunofluorescence mouse nonhuman priority journal protein degradation Psolus patagonicus sea cucumber staining structure activity relation tumor cell line Western blotting |
| description |
Background: The major triterpene glycoside of the sea cucumber Psolus patagonicus and its desulfated analog were tested for their antiproliferative, cytotoxic and hemolytic activities, and their effect on NF-κB activation. Methods: The antiproliferative action of glycosides 1 and 2 were determined on 3 tumor cell lines. Their effect on the activation of NF-κB was evaluated by indirect immunofluorescence assay staining and the concomitant IκBα degradation was studied by Western blot. Results: Both compounds were able to suppress the growth of 3 tumor cell lines (Hep3B, MDA-MB231 and A549) and induced the activation of NF-κB, a key player linking chronic inflammation and cancer, concomitant with IκBα degradation in the A549 tumor cell line. Compounds 1 and 2 showed hemolytic activity with half maximal inhibitory concentration (IC50) values around 80 μM. Conclusions: Both glycosides showed low cytotoxic activity in A549 tumor cells in comparison with sea cucumber triterpene glycosides containing a linear tetrasaccharide chain. This could be a result of the uncommon presence of two 12α- and 17α-hydroxyl groups and a Δ7 double bond in the aglycone moiety. This aglycone functionalization may be related to their low membranolytic activity. Although glycosides 1 and 2 exert an antiproliferative effect, their mechanisms of action do not involve inhibition of NF-κB. Recently, it has been shown that diverse and new mechanisms of action are responsible for the antitumor and cytotoxic activities of marine compounds. Therefore, more extensive studies are needed to establish a mechanism of action and to deduce a clear structure-activity relationship of sea cucumber triterpene glycosides. Copyright © 2008 S. Karger AG. |
| format |
JOUR |
| author |
Careaga, V.P. Bueno, C. Muniain, C. Alché, L. Maier, M.S. |
| author_facet |
Careaga, V.P. Bueno, C. Muniain, C. Alché, L. Maier, M.S. |
| author_sort |
Careaga, V.P. |
| title |
Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog |
| title_short |
Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog |
| title_full |
Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog |
| title_fullStr |
Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog |
| title_full_unstemmed |
Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog |
| title_sort |
antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from psolus patagonicus and its desulfated analog |
| url |
http://hdl.handle.net/20.500.12110/paper_00093157_v55_n1_p60_Careaga |
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