In vitro and In vivo Anticancer Activity of Extracts, Fractions, and Eupomatenoid-5 Obtained from Piper regnellii Leaves

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Despite numerous studies with the Piper genus, there are no previous results reporting in vitro or in vivo Piper regnellii (Miq.) C. DC. var. regnellii anticancer activity. The aim of this study was to investigate P. regnellii in vitro and in vivo anticancer activity and further identify its active compounds. In vitro antiproliferative activity was evaluated in 8 human cancer cell lines: melanoma (UACC-62), breast (MCF7), kidney (786-0), lung (NCI-H460), prostate (PC-3), ovary (OVCAR-3), colon (HT29), and leukemia (K-562). Total growth inhibition (TGI) values were chosen to measure antiproliferative activity. Among the cell lines evaluated, eupomatenoid-5 demonstrated better in vitro antiproliferative activity towards prostate, ovary, kidney, and breast cancer cell lines. In vivo studies were carried out with Ehrlich solid tumor on Balb/C mice treated with 100, 300, and 1000 mg/kg of P. regnellii leaves dichloromethane crude extract (DCE), with 30 and 100 mg/kg of the active fraction (FRB), and with 30 mg/kg of eupomatenoid-5. The i.p. administration of DCE, FRB, and eupomatenoid-5 significantly inhibited tumor progression in comparison to control mice (saline). Therefore, this study showed that neolignans of Piper regnellii have promising anticancer activity. Further studies will be undertaken to determine the mechanism of action and toxicity of these compounds.771314821488Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)FAPESP [2008/50836-0

Dihydroflavonols and flavanones from Lonchocarpus atropurpureus roots

From the petroleum extract of Lonchocarpus atropurpureus Benth. roots, 5,2'-dihydroxy-3-methoxy-6,7-(2',2'-dimethylchromene)-8-(3',3'-dimethylallyl)-flavanone and 2',3,5-trihydroxy-6,7-(2',2'-dimethylchromene)-8-(3',3'-dimethylallyl)-flavanone were isolated, together with three known flavonoids and a mixture of two pentacyclic triterpenes. Their molecular structures were determined by spectral analyses (UV, IR, MS and 1D- and 2D-NMR experiments). (C) 1999 Elsevier Science Ltd. All rights reserved.5281681168

Evaluation of the antioxidant and antiproliferative potential of bioflavors

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)alpha-Terpineol is a relatively cheap and abundant aroma compound. It is widely used in food, cosmetics, and household products. Many of its monoterpene counterparts have been applied in antiproliferative assays, leading to promising results in the prevention or even treatment of cancers. However, despite its theoretic potential, no paper reports the evaluation of antiproliferative capacity of this alcohol. Thus, antioxidant potential of three monoterpenoids (carvone, perillyl alcohol, and alpha-terpineol) was measured using two methods: DPPH and ORAC. Also, the antiproliferative effect of these monoterpenoids against nine cancerous cell lines were performed and compared to limonene and doxorubicin. Results showed that all samples tested had very low antioxidant activity in the DPPH assay, but alpha-terpineol (2.72 mu mol Trolox equiv/mu mol) could be compared to commercial antioxidants in the ORAC assay. The antiproliferative results obtained encourage future in vivo studies for alpha-terpineol, since this monoterpenoid presented cytostatic effect against six cell lines, especially for breast adenocarcinoma and chronic myeloid leukemia, in a range of 181-5881 mu M. (C) 2011 Elsevier Ltd. All rights reserved.49716101615Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

Floral scent of Eleocharis elegans (Kunth) Roem. & Schult. (Cyperaceae)

The inflorescences of Eleocharis elegans and Eleocharis sellowiana were investigated by dynamic headspace/GC-MS for the presence of volatiles. No floral volatile was detected in the inconspicuous inflorescences of E. sellowiana but various floral volatiles were produced by the showy inflorescences of E. elegans. The results are discussed in their ecological and evolutionary context. (c) 2005 Elsevier Ltd. All rights reserved.33767567

Antiproliferative activity of the hexanic extract and phloroglucinols from Hypericum brasiliense

Natural products are regarded as major and important sources of molecules used in chemotherapy. Hypericum brasiliense Choisy, Hypericaceae, is an annual bush, native in the southern and southeastern Brazil. This species has been used in Brazilian folk medicine the anti-spasmodic and for the treatment of infectious diseases. H. brasiliense is chemically composed by flavonoids and xanthones. In addition, this species contain phloroglucinols, a class of substances with citotoxity effects against tumor cells lines. On the present study, hexanic extract and derivatives phloroglucinols obtained from H. brasiliense were tested against some human tumor cell lines. Hexanic extract presented a potent antiproliferative activity, with selective action on OVCAR-03 (ovarian), NCI-ADR/RES (ovarian resistant) and UACC-62 (melanoma) tumor cell lines. Uliginosin B was the most active derivative phloroglucinol, presenting selectivity against NCI-ADR/RES (resistant ovarian) and OVCAR-03 (ovarian) tumor cell lines. Analysis of the results suggests that phloroglucinol derivatives with isoprenyl unit closed in the 9' position increases antiproliferative activity. Furthermore, this study contributes to identification of anti-tumor molecules and valorization of Hypericum brasiliense. (C) 2013 Elsevier Editora Ltda. All rights reserved.23584484

Iodine-Catalyzed Aza-Prins Cyclization: Metal-Free Synthesis and Antiproliferative Activity of Hexahydrobenzo[f]isoquinolines

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)A series of hexahydrobenzo[f]isoquinolines were synthesized by an iodine-catalyzed aza-Prins cyclization under metal-free conditions. An aliphatic or an aromatic aldehyde can be used as the carbonyl component in this reaction, which can also be performed efficiently under solvent-free conditions. During this study, we discovered new compounds with moderate antitumor activities.45810761082Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

Chemical Composition and Cytotoxic Activity of Essential Oil from Myrcia laruotteana Fruits

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)The essential oil isolated by hydrodistillation from unripe fruits of Myrcia laruotteana Camb. (Myrtaceae) was analyzed by GC and CG/MS. Forty-four components were identified, representing around 83% of total oil. The major components were a-bisabolol (23.6%) and a-bisabolol oxide B (11.5%). The cytotoxicity of the oil and of a fraction rich in a-bisabolol was tested in vitro against U251 (glioma), UACC-62 (melanoma), MCF-7 (breast), NC1-ADR/RES (ovarian-resistant), 786.0 (kidney), NCI-H460 (lung), PC-3 (prostate), OVCAR-3 (ovarian), HT-29 (colon) and K562 (leukemia) human cancer cells and against VERO (no cancer cell). The oil exhibited antiproliferative activity against all cell lines (TGI 125 mu g/mL). The highest activity of the oil was observed against U251 (TGI 20.46 mu g/mL), 786.0 (TGI 20.74 mu g/mL), UACC-62 (TGI 26.98 mu g/mL) and PC-3 (TGI 27.63 mu g/mL) cell lines. The fraction rich in alpha-bisabol showed a similar activity profile. It was most active against OVCAR-3 (TGI 8.58 mu g/mL) and 786.0 (TGI 8.74 mu g/mL).235SI710Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES