Evaluation of Brazilian plants on cancer chemoprevention targets in vitro.

Cancer is a leading cause of death worldwide. Cancer chemoprevention is one of the promising strategies to decrease its incidence and both plant extracts and natural products may constitute sources of new chemoprevention agents. Some Brazilian species popularly used to treat inflammatory conditions were selected for evaluation for cancer chemoprevention. A total of 32 extracts/fractions from Hancornia speciosa, Davilla elliptica, Jacaranda caroba, Mansoa hirsuta, Remija ferrugina, Solanum paniculatum and Xyris pterygoblephara, along with a mixture of ursolic and oleanolic acids obtained from J. caroba and a dihydroisocoumarin isolated from aerial parts of X. pterygoblephara were tested for their cancer chemoprevention activity [inhibition of 12-O-tetradecanoyl-13-acetate (TPA)-mediated NF-kappaB activation, ornithine decarboxylase (ODC) and cyclooxygenase-1 (COX-1); induction of antioxidant response element (ARE)]. Several extracts/fractions were active in more than one assay and those from H. speciosa, M. hirsuta and J. caroba mediated strong responses with NF-kappaB, COX-1 and ARE, respectively.

Antiviral activity of Solanum paniculatum extract and constituents.

Solanum species are traditionally employed as antiherpes and anticancer agents in different countries. S. paniculatum has widespread ethnomedical uses in Brazil, including the treatment of viral infections. This paper reports on the isolation of neotigogenin (1) and the new compound delta25(27)-tigogenin-3-O-beta-D-glucopyranoside (2), obtained as a mixture of R and S diastereoisomers at C22 from an ethanol extract of S. paniculatum leaves, along with the determination of their cytotoxicity against Vero cells and antiviral effect against human herpes virus type 1 (HHV-1), murine encephalomyocarditis virus (EMCv), and vaccinia virus strain Western Reserve (VACV-WR). The extract of S. paniculatum inhibited HHV-1 replication [EC50 = (298.0 +/- 11.2) microg/ml] and showed no effect on EMCv and VACV-WR. On its turn, 1 was inactive against the assayed strains but presented high cytotoxicity [CC50 = (2.03 +/- 0.03) microg/ml], whereas 2 exhibited significant antiherpes [EC50 = (170.8 +/- 1.7) microg/ml] and antivaccinia virus effects [EC50 = (177.0 +/- 3.3) microg/ml], with low cytotoxicity (CC50 > 400 microg/ml). The results corroborate Solanum paniculatum as a source of cytotoxic and antiviral compounds.

Mechanism of endothelium-dependent vasodilation induced by a proanthocyanidin-rich fraction from Ouratea semiserrata.

The vasodilator effects of Ouratea semiserrata stem hydroethanolic extract (OSE) and its ethyl acetate fraction (OSR) were evaluated in endothelium-intact aortic rings. OSR produced a more potent vasodilatation (IC(50) = 3.5 +/- 0.8 microg/ml) than OSE (IC(50) > 30 microg/ml). OSR also presented a higher content of total proanthocyanidins (21.8 +/- 1.5 %) in comparison to OSE (6.5 +/- 0.4 %), suggesting that compounds of this class play a role in the vasorelaxing activity. The vasodilatation mechanism of OSR was further investigated. In endothelium-intact aortic rings, its vasorelaxing effect was completely abolished by L-NAME (300 microM), a nitric oxide (NO) synthase inhibitor, but not by a muscarinic antagonist (atropine, 1 microM) nor by a cyclo-oxygenase inhibitor (indomethacin, 10 microM). The OSR vasodilator effect was completely abolished in endothelium-denuded vessels. Furthermore, OSR did not change the vasodilatation produced by SIN-1, an NO donor, in endothelium-denuded vessels. These findings led us to conclude that OSR, a proanthocyanidin rich fraction of O. semiserrata, induces vasodilatation by a mechanism dependent on endothelium-derived factors, likely NO.