Pro-Apoptotic and Pro-Autophagic Properties of Cardenolides from Aerial Parts of Pergularia   tomentosa .
Stefania MartuccielloGaetana PaolellaAntonio Massimiliano RomanelliSilvia SpositoLucia MeolaAntonietta CerulliMilena MasulloSonia PiacenteIvana CaputoPublished in: Molecules (Basel, Switzerland) (2022)
Pergularia tomentosa L., a milkweed tropical plant belonging to the family Asclepiadaceae, is a rich source of unusual cardiac glycosides, characterised by transfused A/B rings and a sugar moiety linked by a double link, generating a dioxanoid structure. In the present report, five cardenolides isolated from the aerial parts of the plant (calactin, calotropin, 12β-hydroxycalactin, 12β,6'-dihydroxycalotropin, and 16α-hydroxycalotropin) were investigated for their biological effects on a human hepatocarcinoma cell line. Cell viability was monitored by an MTT assay. The occurrence of apoptosis was evaluated by detecting caspase-3 activation and chromatin fragmentation. The ability of these compounds to induce autophagy was analysed by monitoring two markers of the autophagic process, LC3 and p62. Our results indicated that all cardenolides had cytotoxic effects, with IC 50 ranging from 0.127 to 6.285 μM. All compounds were able to induce apoptosis and autophagy, calactin being the most active one. Some of them also caused a reduction in cell migration and a partial block of the cell cycle into the S-phase. The present study suggests that selected cardenolides from aerial parts of P. tomentosa , particularly calactin, possess potentially desirable properties for further investigation as anticancer agents.
Keyphrases
- cell death
- cell cycle
- cell cycle arrest
- cell migration
- cell proliferation
- endoplasmic reticulum stress
- endothelial cells
- climate change
- risk assessment
- gene expression
- oxidative stress
- high throughput
- dna damage
- left ventricular
- transcription factor
- induced apoptosis
- protein kinase
- pluripotent stem cells
- mass spectrometry
- heart failure
- induced pluripotent stem cells
- signaling pathway
- atomic force microscopy
- cell wall
- red blood cell
- pi k akt
- high resolution
- single molecule
- water quality