Antiproliferative Effect of Urera baccifera Leaves Against Ovarian Carcinoma Cell Line (OVCAR-3)

Abstract Natural products, especially phytochemicals, have been extensively studies and have exhibited important antiproliferative effects. The American native species Urera baccifera (L.) Gaudich. ex Wedd. (Urticaceae) is widely distributed in Brazil, where it is known as urtiga-vermelha or urtigão. The leaves are popularly used as anti-inflammatory, antirheumatic and in the treatment of gastric disorders. However, the antiproliferative potential of this plant against human tumor cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of U. baccifera leaves extracts and fractions against a panel of human tumor cell lines in vitro besides a chemical evaluation of the most active sample by mass spectrometry (ESI-IT-MSn). The hydroalcoholic extract was inactive while dichloromethane extract showed moderate cytostatic activity against ovarian carcinoma cell line (OVCAR-3, GI50 = 1.5 μg/mL). More, the ethyl acetate and n-butanol fractions did not show important activity against tumour cell while the dichloromethane and hexane fractions showed moderate cytostatic activity against ovarian tumor cell line (OVCAR-3, GI50 = 12.7 and 9.4 μg/mL, respectively). Finally, the chemical profile evaluated by mass spectrometry (ESI-IT-MSn) allowed the detection of flavonoids in the HEU and hydroxylated fatty acid in DEU that can explain partially the biological effects observed. This is the first report of the antiproliferative effects of U. baccifera, and DEU has shown potential as a promising source of bioactive compounds.

Antiproliferative potential of solidagenone isolated of Solidago chilensis

ABSTRACT Plants are considered among the main sources of biologically active chemicals. The species Solidago chilensis Meyen, Asteraceae, is native to the southern parts of South America, where the aerial parts of the plant are commonly used for the treatment of inflammatory conditions. However, the effects of S. chilensis on human cancer cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of the hydroalcoholic and dichloromethane extracts of S. chilensis, as well as their chemical constituents quercitrin and solidagenone against the five human tumor cell lines in vitro. The dichloromethane extract showed a promisor antiproliferative effects in vitro, especially against glioma cell line. Besides, the hydroalcoholic extract and quercitrin were inactive. The diterpene solidagenone showed highly potent antiproliferative effects against breast (MCF-7), kidney (786-0), and prostate cancer (PC-3) cells (total growth inhibition: TGI < 6.25 µg/ml). Solidagenone meets the theoretical physico-chemical criteria for bioavailability of drugs, according to the "Rule of Five" and, by theorical studies, the observed biological effects were probably related to the interaction of the molecule with nuclear receptors and as an enzymatic inhibitor. This study contributes to chemical study and to the identification of antiproliferative molecules in S. chilensis.

Effects of hydroalcoholic extract of Celtis iguanaea on markers of cardiovascular diseases and glucose metabolism in cholesterol-fed rats

ABSTRACT Celtis iguanaea (Jacq.) Sarg., Cannabaceae, is popularly used in the treatment of diabetes mellitus. However, chemical and pharmacological investigations are lacking. In this study, we investigated the effects of the hydroalcoholic extract from C. iguanaea on markers of cardiovascular diseases and the glucose metabolism in cholesterol-fed rats. Therefore, hypercholesterolemic rats (1% cholesterol) were orally treated with C. iguanaea extract (C-150, CI-300, or CI-600 mg/kg) or simvastatin (4 mg/kg) (n = 6) once a day (30 days) with a hypercholesterolemic diet. A control group (C) was given saline. C. iguanaea extract showed significant decreases in serum levels of total cholesterol, LDL-cholesterol, HMG-CoA-reductase, interleukin-1 and 6, TNF-α and IFN-γ when compared to group C (p < 0.001). Hypoglycemic effects were observed along with a decrease of the activity of sucrase (CI-600), maltase (CI-150, CI-300), and an increase in muscle glycogen levels (CI-300). Antioxidant effects were observed in plasma by the decrease of TBARS and increase of nonprotein thiols levels (CI-600). The histopathological analysis showed a significant decrease in the liver fat area for C. iguanaea extract compared to group C (p < 0.001). Our results suggest that the biological effects of C. iguanaea extract could be related to the flavonoids that possibly exert antioxidant, enzymatic inhibitory, and insulin-mimetic effects.

Antiproliferative effects of pinostrobin and 5,6-dehydrokavain isolated from leaves of Alpinia zerumbet

Abstract Natural products are a major source of drugs for the treatment of cancer. The species Alpinia zerumbet (Pers.) B.L. Burtt & R.M. Sm, Zingiberaceae, is widely distributed in Brazil where it is known as "colônia". The leaves are commonly used in the treatment of hypertension and dyspepsia, however, the effects of A. zerumbet extracts and isolated substances on human cancer cells remain to be elucidated. This study was designed to identify the chemical constituents of hydroalcoholic and dichloromethane extracts from A. zerumbet leaves and to investigate their in vitro antiproliferative activity. The isolated phytochemicals included kaempferol, dihydro-5,6-dehydrokavain, 5,6-dehydrokavain, and pinostrobin. The hydroalcoholic extract inhibited cellular proliferation only at high concentrations, while the dichloromethane extract showed a moderate antiproliferative effect against leukemia and lung tumor cell lines. 5,6-Dehydrokavain showed potent cytostatic activity against glioblastoma cells and a moderate effect on all other tumor cell lines. Pinostrobin showed potent activity against leukemia and breast tumor cell lines and moderate cytostatic effect against ovarian cell. Furthermore, this is the first report on the isolation of kaempferol and pinostrobin from A. zerumbet leaves. Moreover, the purification process described in this study was effective. These results suggest that A. zerumbet leaves are a promising source of anticancer compounds.

Analysis of the frequency and degree of temporomandibular disorder in patients with head and neck cancer undergoing radiotherapy / Análise da frequência e grau de disfunção temporomandibular em pacientes com câncer de cabeça e pescoço submetidos à radioterapia

Abstract Introduction: Head and neck cancer is responsible for an increasing incidence of primary malignant neoplasm cases worldwide. Radiotherapy is one of the treatments of choice for this type of cancer, but it can cause adverse effects, such as temporomandibular disorder. The objective of this study was to characterize the degree and frequency of temporomandibular disorder in patients with head and neck cancer undergoing radiotherapy. Method: This research was quantitative, descriptive and exploratory. The sample consisted of 22 patients that answered assessment questions and the Helkimo anamnestic questionnaire, modified by Fonseca (1992). The data were collected from May to October 2014, and statistically analyzed using the Chi-square test, with a significance level of p ≤ 0.05. Results: Of the 22 patients, 86.4 % were male, with a mean age of 58.86 ± 9.41 years. Temporomandibular disorder was present in 31.8% of the subjects, based on the assessment prior to radiotherapy, and in 59.1% in the post-treatment assessment. Among all questions, the most frequent was "Do you use only one side of the mouth to chew?" with 22.7% "yes" answers, both at the first assessment and at the post treatment. Conclusion: According to the results of this study, temporomandibular disorder is a disease that is present with a high prevalence in people diagnosed with head and neck cancer undergoing radiotherapy.

Resumo Introdução: O câncer de cabeça e pescoço é responsável por uma crescente incidência de neoplasias malignas primárias no mundo. A radioterapia é um dos tratamentos de escolha para este tipo de câncer, porém pode causar efeitos adversos, como a Disfunção Temporomandibular. O objetivo deste estudo foi caracterizar o grau e a frequência da Disfunção Temporomandibular em pacientes com câncer de cabeça e pescoço submetidos à radioterapia. Método: A pesquisa é quantitativa, descritiva e exploratória. A amostra foi composta por 22 pacientes que responderam a uma ficha de avaliação e ao questionário de anamnese de Helkimo modificado por Fonseca (1992). Os dados foram coletados entre maio e outubro de 2014 e analisados estatisticamente através do teste de Qui-Quadrado, com um nível de significância de p ≤ 0,05. Resultados: Dos 22 pacientes, 86,4% eram do sexo masculino, com idade média 58.86 ± 9.41 anos. A Disfunção Temporomandibular esteve presente em 31,8% dos indivíduos na avaliação prévia à radioterapia, e em 59,1% na avaliação pós-tratamento. Entre todas as questões, a que mais apresentou incidência foi "Você usa apenas um lado da boca para mastigar?", com 22,7% respostas "sim", tanto na avaliação inicial como na final. Conclusão: De acordo com os resultados do presente estudo, a Disfunção Temporomandibular é uma patologia presente e com grande prevalência em pessoas que foram diagnosticadas com câncer de cabeça e pescoço que foram submetidas ao tratamento radioterápico.