Abstract
The cytotoxic effects of a series of furanoacridones isolated from Ruta graveolens L. (Rutaceae) and of two further acridone alkaloids (arborinine and evoxanthine) were investigated by means of the MTT assay, using the human cell lines HeLa, MCF7 and A431. Arborinine proved best in inhibiting the proliferation of all three cell lines. The cytotoxic potency of the furacridone alkaloids was a function of their lipid solubility, which was determined by means of PAMPA. The capacity of the most effective furanoacridones to induce apoptosis was demonstrated by flow cytometric cell cycle analysis and by staining with ethidium bromide and acridine orange. This finding was reinforced by determining the apoptosis-regulating factors Bcl-2 and Bax, which were revealed by means of RT-PCR to change dose-dependently. The data presented here indicate that naturally occurring furanoacridones can be regarded as excellent starting structures for the potential development of new anticancer agents.
| Original language | English |
|---|---|
| Pages (from-to) | 41-48 |
| Number of pages | 8 |
| Journal | Planta Medica |
| Volume | 73 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Jan 2007 |
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Keywords
- Acridone alkaloids
- Apoptosis
- Cytotoxicity
- Ruta graveolens L.
- Rutaceae
ASJC Scopus subject areas
- Plant Science
- Drug Discovery
- Organic Chemistry
- Pharmacology
Cite this
Investigation of cytotoxic activity on human cancer cell lines of arborinine and furanoacridones isolated from Ruta graveolens. / Réthy, B.; Zupkó, I.; Minorics, Renáta; Hohmann, J.; Ocsovszki, I.; Falkay, G.
In: Planta Medica, Vol. 73, No. 1, 01.2007, p. 41-48.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Investigation of cytotoxic activity on human cancer cell lines of arborinine and furanoacridones isolated from Ruta graveolens
AU - Réthy, B.
AU - Zupkó, I.
AU - Minorics, Renáta
AU - Hohmann, J.
AU - Ocsovszki, I.
AU - Falkay, G.
PY - 2007/1
Y1 - 2007/1
N2 - The cytotoxic effects of a series of furanoacridones isolated from Ruta graveolens L. (Rutaceae) and of two further acridone alkaloids (arborinine and evoxanthine) were investigated by means of the MTT assay, using the human cell lines HeLa, MCF7 and A431. Arborinine proved best in inhibiting the proliferation of all three cell lines. The cytotoxic potency of the furacridone alkaloids was a function of their lipid solubility, which was determined by means of PAMPA. The capacity of the most effective furanoacridones to induce apoptosis was demonstrated by flow cytometric cell cycle analysis and by staining with ethidium bromide and acridine orange. This finding was reinforced by determining the apoptosis-regulating factors Bcl-2 and Bax, which were revealed by means of RT-PCR to change dose-dependently. The data presented here indicate that naturally occurring furanoacridones can be regarded as excellent starting structures for the potential development of new anticancer agents.
AB - The cytotoxic effects of a series of furanoacridones isolated from Ruta graveolens L. (Rutaceae) and of two further acridone alkaloids (arborinine and evoxanthine) were investigated by means of the MTT assay, using the human cell lines HeLa, MCF7 and A431. Arborinine proved best in inhibiting the proliferation of all three cell lines. The cytotoxic potency of the furacridone alkaloids was a function of their lipid solubility, which was determined by means of PAMPA. The capacity of the most effective furanoacridones to induce apoptosis was demonstrated by flow cytometric cell cycle analysis and by staining with ethidium bromide and acridine orange. This finding was reinforced by determining the apoptosis-regulating factors Bcl-2 and Bax, which were revealed by means of RT-PCR to change dose-dependently. The data presented here indicate that naturally occurring furanoacridones can be regarded as excellent starting structures for the potential development of new anticancer agents.
KW - Acridone alkaloids
KW - Apoptosis
KW - Cytotoxicity
KW - Ruta graveolens L.
KW - Rutaceae
UR - http://www.scopus.com/inward/record.url?scp=33847771282&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33847771282&partnerID=8YFLogxK
U2 - 10.1055/s-2006-951747
DO - 10.1055/s-2006-951747
M3 - Article
C2 - 17109253
AN - SCOPUS:33847771282
VL - 73
SP - 41
EP - 48
JO - Planta Medica
JF - Planta Medica
SN - 0032-0943
IS - 1
ER -