Investigation of Cytotoxic Activity on Human Cancer Cell Lines of Arborinine and Furanoacridones Isolated from Ruta graveolens

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.

Ethyl acetate extract fromGlycosmis parvaleaf induces apoptosis and cell-cycle arrest by decreasing expression of COX-2 and altering BCL-2 family gene expression in human colorectal cancer HT-29 cells

“…Chemical examination of the EtOAc extract from the leaves of G. parva led to the identification of the acridone alkaloid and sulfur-containing propanamides as its major active compounds. Arborinine, a main acridone alkaloid found in EtOAC of the leaves of G. parva, has been reported to have potent antiproliferative effects against cervix adenocarcinoma HeLa cells with an IC 50 of 1.84 mM, which was lower than that of cisplatin (12.43 mM) (Rethy et al, 2007), indicating that arborinine possesses higher antiproliferative activity than cisplatin. Additionally, antifungal activities of sulfur-containing propanamides derivative, S-deoxydihydroglyparvin, S-deoxytetrahydroglyparvin, glyparvin-A, and dihydroglyparvin were reported (Chansriniyom et al, 2009;Greger et al, 1993).…”

The interference of piperidinopropionaphthone hydrochloride in mammalian type I and type II DNA topoisomerase reactions

“…On the other hand, the AN and MB were added to the medium and penetration through an intact cell membrane is a condition of their action in MTT assay. A close relationship between cytostatic effect and lipid solubility of a set of alkaloids has been published earlier (31). Therefore, it could be speculated that MB has a limited capacity to enter the cell and interact with the DNA which is reflected in its poor overall antiproliferative property.…”

Extraction of Alkaloids and Oil from Karanja (<i>Pongamia pinnata</i>) Seed

“…The alkaloids which are contained in plant materials naturally exhibit a variety of physical, chemical, biological as well as medicinal properties [23][24][25][26][27][28]. In plant materials alkaloids generally occur partially as free bases and partially as salts which are insoluble in most of the organic solvents.…”