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

DEVELOPMENT AND VALIDATION OF ANALYTICAL METHODOLOGY BY HPLC-IR FOR EVALUATION OF ARTEMISININ ON Artemisa annua L.

The aim of this work was to develop and validate an analytical methodology for determination of artemisinin used as antimalaric. The method was based on high performace liquid chromatography, using a CN column with mobile phase composed of methanol : H(2)O 50: 50 (V/V). The results showed that the method presented linearity from 50 to 1500 mu g/mL. It was considered selective, accurate, precise according to the specific resolution from ANVISA, the Brazilian regulatory agency.32nd Annual Meeting of the Sociedade-Brasileira-de-Quimica : MAY 30-JUN 02, 2009 : Fortaleza, BRAZIL : Soc Brasileira Quim :32487587

Hypertriglyceridemic waist phenotype in primary health care: comparison of two cutoff points

Marina Augusta Dias Braz,1 Jallyne Nunes Vieira,1 Flayane Oliveira Gomes,1 Priscilla Rafaella da Silva,1 Ohanna Thays de Medeiros Santos,1 Ilanna Marques Gomes da Rocha,2 Iasmin Matias de Sousa,2 Ana Paula Trussardi Fayh2 1Faculdade de Ciências da Saúde do Trairi, Universidade Federal do Rio Grande do Norte (UFRN), Santa Cruz, 2Department of Nutrition, Centro de Ciências da Saúde, UFRN, Natal, Rio Grande do Norte, Brazil Objective: We aimed to evaluate the prevalence of hypertriglyceridemic waist (HTGW) phenotype among users of primary health care using two different cutoff points used in the literature. Methods: We evaluated adults and elderly individuals of both sexes who attended the same level of primary health care. HTGW phenotype was determined with measurements of waist circumference (WC) and triglyceride levels and compared using cutoff points proposed by the National Cholesterol Education Program – NCEP/ATP III (WC ≥102 cm for men and ≥88 cm for women; triglyceride levels ≥150 mg/dL for both sexes) and by Lemieux et al (WC ≥90 cm for men and ≥85 cm for women; triglyceride levels ≥177 mg/dL for both). Results: Within the sample of 437 individuals, 73.7% was female. The prevalence of HTGW phenotype was high and statistically different with the use of different cutoff points from the literature. The prevalence was higher using the NCEP/ATP III criteria compared to those proposed by Lemieux et al (36.2% and 32.5%, respectively, p<0.05). Individuals with the presence of the phenotype also presented alterations in other traditional cardiovascular risk markers. Conclusion: The HTGW phenotype identified high prevalence of cardiovascular risk in the population, with higher cutoff points from the NCEP/ATP III criteria. The difference in frequency of risk alerts us to the need to establish cutoff points for the Brazilian population. Keywords: abdominal obesity, cardiovascular disease, dyslipidemia, cardiovascular ris

Evaluation of wound healing properties of Arrabidaea chica Verlot extract

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Ethnopharmacological relevance: Arrabidaea chica Verlot. (Bignoniaceae), popularly known as Crajiru, has been traditionally used as wound healing agent. Aim of the study: Investigate in vitro and in vivo healing properties of Arrabidaea chica leaves extract (AC). Materials and methods: AC was evaluated in vitro in fibroblast growth stimulation (0.25-250 mu g/mL) and collagen production stimulation (250 mu g/mL.) assays. Allantoin (0.25-250 mu g/mL) and vitamin C (25 mu g/mL) were used as controls respectively. DPPH and Folin-Ciocalteau assays were used for antioxidant evaluation, using trolox (0.25-250 mu g/mL) as reference antioxidant. To study wound healing properties in rats, AC (100 mg/mL, 200 mu L/wound/day) was topically administered during 10 days and wound area was evaluated every day. Allantoin (100 mg/mL, 200 mu L/wound/day) was used as standard drug. After treatment, wound sites were removed for histopathological analysis and total collagen determination. Results: AC stimulated fibroblast growth in a concentration dependent way (EC(50) = 30 mu g/mL), increased in vitro collagen production and demonstrated moderate antioxidant capacity. In vivo, AC reduced wound size in 96%. whereas saline group showed only 36% wound healing. Conclusion: AC efficiency seems to involve fibroblast growing stimulus and collagen synthesis both in vitro and in vivo, beyond moderate scavenging activity, corroborating Crajiru folk use. (c) 2008 Elsevier Ireland Ltd. All rights reserved.1183361366CPQBA/UNICAMPFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

Antiproliferative properties of polyketides isolated from Virola sebifera leaves

An activity-guided fractionation of Virola sebifera Aubl. methylene chloride-soluble fraction provided novel 3,5-dihydro-2-(1'-oxo-3'-hexadecenyl)-2-cyclohexen-1-one (3), two known lignans (1, 2) and dehydro hexadecanoyl resorcinol (4). Isolation and purification were conducted with the application of column chromatography and structures were assigned by spetral analysis (1D and 2D NMR, HREIMS). Compounds 1-4 were evaluated for cytotoxic activities against human tumour cell lines UACC62 (melanoma), MCF-7 (breast), NCI 460 (lung, non-small cells), OVCAR03 (ovarian), PC-03 (prostate), HT-29 (colon), 786-0 (renal) and NCI-ADR (breast expressing phenotype multiple drugs resistance) in vitro. The new polyketide (3) showed selectivity against human OVCAR03 and NCI-ADR cell lines, ranging from 2 to 4 mu g/mL. Copyright (c) 2007 John Wiley & Sons, Ltd.22112713