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Isolation and assessment of the in vitro anti-tumor activity of smenothiazole A and B, chlorinated thiazole-containing peptide/polyketides from the Caribbean sponge, Smenospongia aurea.

Esposito G, Teta R, Miceli R, Ceccarelli LS, Della Sala G, Camerlingo R, Irollo E, Mangoni A, Pirozzi G, Costantino V - Mar Drugs (2015)

Bottom Line: The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds.Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

View Article: PubMed Central - PubMed

Affiliation: The NeaNat Group, Dipartimento di Farmacia, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy. germana.esposito@unina.it.

ABSTRACT
The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds. Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

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Related in: MedlinePlus

Evaluation assays of apoptosis/necrosis by the Annexin-V FITC/PI in four cancer cell lines after 48 h of treatment with smenothiazole A (3) and smenothiazole B (4).
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marinedrugs-13-00444-f006: Evaluation assays of apoptosis/necrosis by the Annexin-V FITC/PI in four cancer cell lines after 48 h of treatment with smenothiazole A (3) and smenothiazole B (4).

Mentions: Smenothiazoles were assayed on the same four cell lines used for MTT assays. The results are reported in Figure 6. For Calu-1 cells, the efficacy of smenothiazoles in these assays was limited, and most cells remained viable even at the highest concentration tested. Smenothiazol A (3) showed mostly a necrotic effect, while the effect of smenothiazol B (4) was borderline, with a percentage of necrotic cells similar to that of apoptotic cells. Better activity was observed on the LC31 primary lung cancer cell line: both compounds showed a clear pro-apoptotic activity, although the slope of the dose-response curve appeared to be different for the two compounds. No effect, either apoptotic or necrotic, was observed for breast MCF-7 cells compared to the control.


Isolation and assessment of the in vitro anti-tumor activity of smenothiazole A and B, chlorinated thiazole-containing peptide/polyketides from the Caribbean sponge, Smenospongia aurea.

Esposito G, Teta R, Miceli R, Ceccarelli LS, Della Sala G, Camerlingo R, Irollo E, Mangoni A, Pirozzi G, Costantino V - Mar Drugs (2015)

Evaluation assays of apoptosis/necrosis by the Annexin-V FITC/PI in four cancer cell lines after 48 h of treatment with smenothiazole A (3) and smenothiazole B (4).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4306946&req=5

marinedrugs-13-00444-f006: Evaluation assays of apoptosis/necrosis by the Annexin-V FITC/PI in four cancer cell lines after 48 h of treatment with smenothiazole A (3) and smenothiazole B (4).
Mentions: Smenothiazoles were assayed on the same four cell lines used for MTT assays. The results are reported in Figure 6. For Calu-1 cells, the efficacy of smenothiazoles in these assays was limited, and most cells remained viable even at the highest concentration tested. Smenothiazol A (3) showed mostly a necrotic effect, while the effect of smenothiazol B (4) was borderline, with a percentage of necrotic cells similar to that of apoptotic cells. Better activity was observed on the LC31 primary lung cancer cell line: both compounds showed a clear pro-apoptotic activity, although the slope of the dose-response curve appeared to be different for the two compounds. No effect, either apoptotic or necrotic, was observed for breast MCF-7 cells compared to the control.

Bottom Line: The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds.Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

View Article: PubMed Central - PubMed

Affiliation: The NeaNat Group, Dipartimento di Farmacia, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy. germana.esposito@unina.it.

ABSTRACT
The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds. Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

Show MeSH
Related in: MedlinePlus