Planta Med 2019; 85(18): 1530
DOI: 10.1055/s-0039-3400039
Main Congress Poster
Poster Session 2
© Georg Thieme Verlag KG Stuttgart · New York

Further insights in the antiproliferative activity of cardenolides from the aerial parts of Pergularia tomentosa

M Masullo
1   Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy;
,
H Hossaini
2   Department of Biology, University of Jiroft, Jiroft, Iran;
,
A Cerulli
1   Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy;
,
S Martucciello
3   Dipartimento di Chimica e Biologia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy;
,
M Ayyari
2   Department of Biology, University of Jiroft, Jiroft, Iran;
4   Department of Horticultural Science, Faculty of Agriculture, Tarbiat Modares University, Tehran, Iran
,
C Pizza
1   Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy;
,
S Piacente
1   Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy; Department of Chemistry and Biology, University of Salerno, Fisciano, Italy;
› Author Affiliations
Further Information

Publication History

Publication Date:
20 December 2019 (online)

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Pergularia tomentosa (Asclepiadaceae) is a milkweed tropical plant used in traditional medicine for the treatment of several diseases such as bronchitis, constipation and skin diseases [1]-[3]. Previously we reported the occurrence of cardiac glycosides with trans fused A/B rings of the steroidal skeleton and with a single sugar, linked to the 2α- and 3β-positions of the aglycone by hemiketal and acetal functions respectively [1],[3],[4]. Isolated cardenolides inhibited cell viability of PC3, Hela, Calu-1, MCF-7, and U251MG cell lines exhibiting IC50 values ranging from 0.2 to 8.0 μM [4]. Herein, the ability of the isolated compounds to inhibit cell viability of Hepg2 (liver hepatocellular carcinoma) cell line has been evaluated. Of all tested compounds, calotropin and calactin showed the highest activity with IC50 values of 0.83 µM and 0.11 µM, respectively. Chemically, these compounds differ in the stereochemistry of C-3ʹ of the sugar linked to the aglycone. With the aim to deeper explore their ability to inhibit cancer progression, the effects on cellular migration and proliferation were also investigated. Our results showed that calotropin and calactin at 1μM inhibited cell migration (wound healing assay) and proliferation (fase S entry) of the Hepg2 cancer cell line. They induced apoptosis associated with activation of caspase-3 and increased p53 expression, more than 35% and 45%, respectively, when compared with staurosporine used as positive control. Moreover reduction of GRP78, a general ER-stress marker was also observed. These findings suggest that selected compounds from P. tomentosa are potential leads to be explored as anti-cancer agents.

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Fig. 1
 

  • References

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