Antitumoral and anticholinesterasic activity of the seven species from Rubiaceae.

BACKGROUND: The genus Psychotria and Palicourea are reported as a source of alkaloids and iridoids, which exhibit biological activities. This study aimed to evaluate the antiproliferative, anticholinesterase and LC/MS potential of the methanolic extract of seven species among the genus found in Mato Grosso do Sul region in Brazil.

METHODS: The extracts were submitted to antiproliferative activity against ten human tumor cell lines. The anticholinesterase activity of the extracts (1 mg/mL) was developed using brain structures of male Wistar rats: cerebral cortex, hippocampus, hypothalamus and striatum by the Ellman method.

RESULTS: The LC/MS was performed to identify the alkaloids present in the extracts, identifying strictosidinic acid, strictosidine, strictosamide, miriantosine, raucaffricine, calycanthine, croceaine A and B, brachycerine and bufotenine. Regarding the antiproliferative potential, Palicourea crocea demonstrated selectivity against the 786-0 cell line (GI50: 22.87 μg/mL). Psychotria leiocarpa inhibited cell growth against OVCAR-3 (GI50: 3.28 μg/mL), K-562 (GI50: 5.26 μg/mL), HaCaT (GI50: 27.20 μg/mL), PC-3 (GI50: 34.92 μg/mL), MCF-7 (GI50: 35.80 μg/mL) and P. capillacea showed activity against OVCAR-3 (GI50: 2.33 μg/ml) and U251 (GI50: 16.66 μg/ml). The effect of acetylcholinesterase inhibition was more effective in the hippocampus, demonstrating inhibition for Paliourea crocea, Psychotria deflexa, P. brachybotrya and P. leiocarpa of 70%, 57%, 50% and 40%, respectively, followed by P. poeppigiana and P. capillacea, inhibiting 21%, compared to the control.

CONCLUSION: Herein, the anticholinesterasic and antiproliferative activity of extracts produced from species of Psychotria and Palicourea genus with anticholinesterasic and antiproliferative activity is reported.