Antitumoral and Anticholinesterasic Activities 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 antiproliferative and anticholinesterase activities and quantification of the alkaloids of seven species among the genus found in Mato Grosso do Sul region in Brazil. METHODS: Concentrations of alkaloids were measured spectrophotometrically. The extracts were submitted to antiproliferative activity against ten cell lines. The anticholinesterase activity of the extracts was developed using brain structures of male Wistar rats: cerebral cortex, hippocampus, hypothalamus and striatum by the Ellman method. RESULTS: Alkaloids from Psychotria and Palicourea species were quantified which showed values of 47.6 to 21.9 µg/g. 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 present work showed for the first time, anticholinesterasic and antiproliferative activities of extracts of Palicourea and Psychotria seem to be mainly associated with the levels of alkaloids in the leaves of these species.

Anti-inflammatory, Antioxidant and Antiproliferative Activities from Trichilia silvatica (C.DC).

BACKGROUND: Trichilia silvatica, popularly known as "catiguá-branco", is distributed in Brazil (Mato Grosso do Sul), and members of this genus are commonly used for the treatment of rheumatism (arthritis). The aim of this research was to investigate the anti-inflammatory, antioxidant and antiproliferative activities of the methanolic extract of the leaves (MEL-TS) and bark (MEB-TS) of T. silvatica. We also evaluated the concentration of phenolic compounds, flavonoids, flavonol, and condensed tannins by liquid chromatography - photodiode array (LC/PDA) analysis. METHODS: The MEL-TS and MEB-TS revealed the presence of caffeic acid in both extracts by LC/PDA. The samples were evaluated for antioxidant activity using free-radical scavenging and lipoperoxidation assays. The anti-inflammatory effects were studied in carrageenan-induced paw edema, pleurisy and zymosan-induced arthritis. RESULTS: The MEL-TS and MEB-TS showed the total phenolic concentration (270.8 ± 17.10 mg gallic acid equivalents GAE/g extract and 278.8 ± 25.13 mg GAE/ g extract, respectively), and flavonoids in MEL-TS (209.30 ± 2.91 mg quercetin equivalents QE/ g extract). In the lipoperoxidation assay, exhibited moderate antioxidant activity with IC50 values ≤ 35.32 µg/mL. Both extracts inhibited oedema induced by carrageenan at 2 h and 4 h, inhibited leukocyte migration at 6 h post administration, and did not impact zymosan-induced arthritis. Finally, MEL-TS was particularly effective against prostate cell line (GI50 ≤ 0.22 µg/mL). CONCLUSION: Overall, the results indicated that T. silvatica reduce migration leukocytes activity, edema formation in these models of experimental arthritis could explain the popular use for treatment of inflammatory processes (rheumatism).