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Anticancer activity evaluation of kuanoniamines A and C isolated from the marine sponge Oceanapia sagittaria, collected from the Gulf of Thailand.

Kijjoa A, Wattanadilok R, Campos N, Nascimento MS, Pinto M, Herz W - Mar Drugs (2007)

Bottom Line: Kuanoniamine A was found to be a potent growth inhibitor of all the tumour and a non-tumour cell lines while kuanoniamine C was less potent but showed high selectivity toward the estrogen dependent (ER+) breast cancer cell line.Kuanoniamine A has shown to be a more potent inhibitor of DNA synthesis than kuanoniamine C.Kuanoniamine A was also found to cause an extensive reduction of the MCF-7 cells in G2/M phase as well as an increase in the apoptotic cells.

View Article: PubMed Central - PubMed

Affiliation: ICBAS-Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto, 4099-003 Porto, Portugal. ankijjoa@icbas.up.pt

ABSTRACT
The pyridoacridine alkaloids kuanoniamines A and C were isolated together with 24 alpha-methylcholestanol, p-hydroxybenzaldehyde, p-hydroxybenzoic acid, phenylacetic acid and 3-formylindole from the ethyl acetate extract of the marine sponge Oceanapia sagittaria (Sollas), collected from the Gulf of Thailand. Kuanoniamines A and C were evaluated for their effect on the growth of five human tumour and a non-tumour cell lines, as well as on the proliferation of human lymphocytes. Kuanoniamine A was found to be a potent growth inhibitor of all the tumour and a non-tumour cell lines while kuanoniamine C was less potent but showed high selectivity toward the estrogen dependent (ER+) breast cancer cell line. Kuanoniamine A has shown to be a more potent inhibitor of DNA synthesis than kuanoniamine C. Kuanoniamine A was also found to cause an extensive reduction of the MCF-7 cells in G2/M phase as well as an increase in the apoptotic cells.

No MeSH data available.


Related in: MedlinePlus

Time and dose-dependent curves of kuanoniamine A (6) and kuanoniamine C (7) in DNA synthesis of MCF-7 cells determined by [3H]-thymidine incorporation assay. Results are the mean ± SEM of four replicates from a representative experiment.
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f2-md502006: Time and dose-dependent curves of kuanoniamine A (6) and kuanoniamine C (7) in DNA synthesis of MCF-7 cells determined by [3H]-thymidine incorporation assay. Results are the mean ± SEM of four replicates from a representative experiment.

Mentions: As both kuanoniamine A (6) and kuanoniamine C (7) were found to be potent inhibitors of the MCF-7 cells, we have selected this breast cancer cell line to further characterize the growth inhibitory effect of the two compounds. We first evaluated their capacity to interfere with the biosynthesis of DNA by exposing the exponential growing MCF-7 cells to a range of increasing concentrations of kuanoniamine A (6) and kuanoniamine C (7), below and above their GI50 (0.04 – 86.51 μM and 0.03 – 66.84 μM, respectively) for 6, 12, 24 and 48 h and the DNA synthesis was quantified by thymidine incorporation (Figure 2). The dose-response curve showed that kuanoniamine A (6) dramatically affected DNA synthesis, even at concentrations as low as 0.08 μM, which were associated with a decrease in thymidine incorporation of more than 60% when compared with untreatead control cells. It was also found that the effect on DNA synthesis was mainly dependent on the concentration of kuanoniamine A (6) rather than on the exposure time. On the contrary, the effect of kuanoniamine C (7) was found to be dependent either on the concentration or the exposure time. Although an inhibition of DNA synthesis was also observed with kuanoniamine C (7), an interesting stimulatory effect was detected at low concentrations and exposure periods of 6 and 12 h. A maximum stimulation of 130% was reached after 6 h of treatment with 0.26 and 0.52 μM. This biphasic effect in DNA synthesis of ER (+) MCF-7 cells, expressed by a stimulatory effect at low concentrations and an inhibitory effect at high concentrations, resembles the behaviour described for phytoestrogens on ER (+) breast cancer cells [16, 17].


Anticancer activity evaluation of kuanoniamines A and C isolated from the marine sponge Oceanapia sagittaria, collected from the Gulf of Thailand.

Kijjoa A, Wattanadilok R, Campos N, Nascimento MS, Pinto M, Herz W - Mar Drugs (2007)

Time and dose-dependent curves of kuanoniamine A (6) and kuanoniamine C (7) in DNA synthesis of MCF-7 cells determined by [3H]-thymidine incorporation assay. Results are the mean ± SEM of four replicates from a representative experiment.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2365692&req=5

f2-md502006: Time and dose-dependent curves of kuanoniamine A (6) and kuanoniamine C (7) in DNA synthesis of MCF-7 cells determined by [3H]-thymidine incorporation assay. Results are the mean ± SEM of four replicates from a representative experiment.
Mentions: As both kuanoniamine A (6) and kuanoniamine C (7) were found to be potent inhibitors of the MCF-7 cells, we have selected this breast cancer cell line to further characterize the growth inhibitory effect of the two compounds. We first evaluated their capacity to interfere with the biosynthesis of DNA by exposing the exponential growing MCF-7 cells to a range of increasing concentrations of kuanoniamine A (6) and kuanoniamine C (7), below and above their GI50 (0.04 – 86.51 μM and 0.03 – 66.84 μM, respectively) for 6, 12, 24 and 48 h and the DNA synthesis was quantified by thymidine incorporation (Figure 2). The dose-response curve showed that kuanoniamine A (6) dramatically affected DNA synthesis, even at concentrations as low as 0.08 μM, which were associated with a decrease in thymidine incorporation of more than 60% when compared with untreatead control cells. It was also found that the effect on DNA synthesis was mainly dependent on the concentration of kuanoniamine A (6) rather than on the exposure time. On the contrary, the effect of kuanoniamine C (7) was found to be dependent either on the concentration or the exposure time. Although an inhibition of DNA synthesis was also observed with kuanoniamine C (7), an interesting stimulatory effect was detected at low concentrations and exposure periods of 6 and 12 h. A maximum stimulation of 130% was reached after 6 h of treatment with 0.26 and 0.52 μM. This biphasic effect in DNA synthesis of ER (+) MCF-7 cells, expressed by a stimulatory effect at low concentrations and an inhibitory effect at high concentrations, resembles the behaviour described for phytoestrogens on ER (+) breast cancer cells [16, 17].

Bottom Line: Kuanoniamine A was found to be a potent growth inhibitor of all the tumour and a non-tumour cell lines while kuanoniamine C was less potent but showed high selectivity toward the estrogen dependent (ER+) breast cancer cell line.Kuanoniamine A has shown to be a more potent inhibitor of DNA synthesis than kuanoniamine C.Kuanoniamine A was also found to cause an extensive reduction of the MCF-7 cells in G2/M phase as well as an increase in the apoptotic cells.

View Article: PubMed Central - PubMed

Affiliation: ICBAS-Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto, 4099-003 Porto, Portugal. ankijjoa@icbas.up.pt

ABSTRACT
The pyridoacridine alkaloids kuanoniamines A and C were isolated together with 24 alpha-methylcholestanol, p-hydroxybenzaldehyde, p-hydroxybenzoic acid, phenylacetic acid and 3-formylindole from the ethyl acetate extract of the marine sponge Oceanapia sagittaria (Sollas), collected from the Gulf of Thailand. Kuanoniamines A and C were evaluated for their effect on the growth of five human tumour and a non-tumour cell lines, as well as on the proliferation of human lymphocytes. Kuanoniamine A was found to be a potent growth inhibitor of all the tumour and a non-tumour cell lines while kuanoniamine C was less potent but showed high selectivity toward the estrogen dependent (ER+) breast cancer cell line. Kuanoniamine A has shown to be a more potent inhibitor of DNA synthesis than kuanoniamine C. Kuanoniamine A was also found to cause an extensive reduction of the MCF-7 cells in G2/M phase as well as an increase in the apoptotic cells.

No MeSH data available.


Related in: MedlinePlus