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Braz. arch. biol. technol ; 62: e19180531, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039123


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.

Ovarian Neoplasms/drug therapy , Plants, Medicinal/drug effects , Chemical Phenomena/drug effects , Antineoplastic Agents/pharmacology , Mass Spectrometry/instrumentation
Rev. bras. farmacogn ; 28(5): 602-609, Sept.-Oct. 2018. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-977727


Abstract Annona leptopetala (R.E.Fr.) H. Rainer, Annonaceae, is used in folk medicine like antitumor and anti-inflammatory. The aim of this study was to determine chemical composition, toxicity and antitumor activity of A. leptopetala leaves volatile oil. Fresh leaves were hydrodistilled and then the volatile oil chemical composition was assessed by gas chromatography and mass spectrometry. Toxicity was assessed using haemolysis, micronucleus and acute toxicity protocols. Antitumor effects were determined in vitro and in vivo, using sulforhodamine B assay and sarcoma 180 murine tumor model, respectively. Spathulenol was the major component identified (12.56%). The volatile oil showed in vitro antitumor activity mainly in leukemia cell line (K-562), with Total growth inhibit (TGI) (concentration producing TGI) of 0.64 µg/ml. In other hand, the volatile oil <250 µg/ml did not inhibit HaCat non-tumor cell line growth. The concentration that produced 50% haemolysis was 372.8 µg/ml. The 50% lethal dose in mice was approximately 447.2 mg/kg intraperitoneally. Sarcoma 180 tumor growth inhibition rates were 59.29% and 58.77% at 100 and 150 mg/kg intraperitoneally, respectively. The volatile oil presented moderate gastrointestinal toxicity and no genotoxicity was observed at 350 mg/kg. Thus, the volatile oil shows antitumor activity with moderate toxicity.

Rev. bras. cancerol ; 64(1): 93-98, Jan/Fev/Mar 2018.
Article in Portuguese | LILACS | ID: biblio-969213


Introdução: Bisfosfonatos são fármacos utilizados para o tratamento de enfermidades ósseas, como a osteoporose e metástases ósseas, em razão do seu mecanismo de ação, que consiste na diminuição do processo de reabsorção do osso. Outros estudos verificaram que bisfosfonatos de alta potência, como o zoledronato, poderiam auxiliar no tratamento de outras enfermidades malignas por causa da promoção de um efeito antiproliferativo. Objetivo: Este estudo in vitro objetivou avaliar a atividade antiproliferativa de zoledronato em diferentes linhagens de células tumorais. Método: Nove linhagens humanas (U251; MCF7; NCI/ADR-RES; 786-0; NCI-H460; PC-3; OVCAR-3; HT29; K-562 e HaCaT) foram submetidas ao tratamento com as concentrações de 0,12; 1,2; 12 e 120 µM de zoledronato e tiveram sua atividade proliferativa avaliada após 48 horas, utilizando-se o corante sulforrodamina B. Resultados: Verificou-se que as concentrações de 12 µM e 120 µM de zoledronato foram eficazes para a redução em 50% e 100%, respectivamente, da proliferação das células 786-0 (carcinoma renal). A maior concentração de zoledronato (120 µM) promoveu um efeito citostático (redução da proliferação celular em 50%) para as células HaCaT (queratinócito humano não tumoral), HT-29 (carcinoma de cólon), NCI-ADR/ RES (adenocarcinoma de ovário com fenótipo de multirresistência) e NCI-H460 (carcinoma pulmonar). Conclusão: Esses resultados sugerem um promissor efeito auxiliar do zoledronato para o tratamento de alguns tipos de tumores; estudos complementares in vitro e in vivo são necessários para a validação dessa hipótese.

Introduction: Bisphosphonates are used in the treatment of bone diseases such as osteoporosis and bone metastases, because of their ability to inhibit bone resorption. There is evidence that high-potency bisphosphonates, such as zoledronate, are useful in the treatment of other malignancies because they have an antiproliferative effect. Objective:To evaluate the antiproliferative activity of zoledronate in different tumor cell lines. Method: This was an in vitro study in which nine human cell lines (U251, MCF7, NCI/ ADR-RES, 786-0, NCI-H460, PC-3, OVCAR-3, HT29, K-562, and HaCaT) were treated with of 0.12, 1.2, 12, and 120 µM of zoledronate, their proliferative activity being evaluated 48 h later with sulforhodamine B assay. Results: At the 12 µM and 120 µM doses, zoledronate effectively reduced the proliferation of 786-0 (renal carcinoma) cells by 50% and 100%, respectively. At the highest concentration (120 µM), zoledronate had a cytostatic effect (50% reduction in cell proliferation) on HaCaT (non-tumor human keratinocyte), HT-29 (colon carcinoma), NCI-ADR/ RES (multidrug-resistant ovarian adenocarcinoma), and NCI-H460 (lung carcinoma) cells. Conclusion: These results suggest a promising auxiliary effect of zoledronate for the treatment of some tumors. Further in vitro and in vivo studies are needed in order to test that hypothesis.

Introducción: Los bisfosfonatos son fármacos utilizados para el tratamiento de enfermedades óseas, como la osteoporosis y metástasis óseas debido a su mecanismo de acción, que consiste en la disminución del proceso de reabsorción del hueso. Otros estudios observaron que los bisfosfonatos de alta potencia, como el zoledronato, podrían ayudar en el tratamiento de otras enfermedades malignas debido a la promoción de un efecto antiproliferativo. Objetivo: Este estudio in vitro objetivó evaluar la actividad antiproliferativa de zoledronato en diferentes linajes de células tumorales. Método: Los nueve humano linajes (U251, MCF7, NCI / ADR-RES, 786-0, NCI-H460, PC-3, OVCAR-3, HT29, K-562 and HaCaT) se sometieron al tratamiento con las concentraciones de 0,12; 1,2; 12 y 120 µM de zoledronato y tuvieron su actividad proliferativa evaluada después de 48 horas utilizando el colorante sulforrodamina B. Resultados: Se comprobó que las concentraciones de 12 µM y 120 µM de zoledronato fueron efectivas para reducir en un 50% y un 100%, respectivamente, de la proliferación de las células 786-0 (carcinoma renal). La mayor concentración de zoledronato (120 µM) promovió un efecto citostático (reducción de la proliferación celular en un 50%) para las células HaCaT (queratinocito humano no tumoral), HT-29 (carcinoma de colon), NCI-ADR/RES (adenocarcinoma de ovário con fenótipo de multirresistencia) y NCI-H460 (carcinoma pulmonar). Conclusión: Estos resultados sugieren un prometedor efecto auxiliar del zoledronato para el tratamiento de algunos tumores; se requieren más estudios in vitro e in vivo para validar esta hipótesis

Humans , Cell Proliferation/drug effects , Diphosphonates , In Vitro Techniques , Tumor Cells, Cultured/drug effects , Cell Line, Tumor/drug effects
Braz. oral res. (Online) ; 32: e41, 2018. tab, graf
Article in English | LILACS | ID: biblio-889473


Abstract: The aim of this study was to evaluate in vitro the antifungal, antibiofilm and antiproliferative activities of the extract from the leaves of Guapira graciliflora Mart. The phytochemical characterization of the extract was performed using electrospray ionization mass spectrometry (ESI-MS). The antimicrobial activity of the extract and its fractions was evaluated using the broth microdilution method against species of Candida. The inhibition of C. albicans biofilm was evaluated based on the number of colony-forming units (CFU) and metabolic activity (MTT). The antiproliferative activity of the extract and its fraction was evaluated in the presence of human tumor and non-tumor cells, and the cytotoxicity of the extract was determined on the RAW 264.7 macrophage line - both using the sulforhodamine B method. The phytochemical characterization indicated the presence of the flavonoids rutin and kaempferol. The extract and the methanol fraction exhibited moderate antifungal activity against C. albicans, C. krusei, and C. glabrata, and strong activity against C. dubliniensis. In the biofilms at 24 and 48 hours, the concentration of 12500 µg/mL of the extract was the most effective at reducing the number of CFU s/mL (44.4% and 42.9%, respectively) and the metabolic activity of C. albicans cells (34.6% and 52%, respectively). The extract and its fractions had no antiproliferative effect on the tumor lines tested, with mean activity (log GI50) equal to or greater than 1.71 µg/mL. Macrophage cell viability remained higher than 80% for concentrations of the extract of up to 62.5 µg/mL. G. graciliflora has flavonoids in its chemical composition and demonstrates potential antifungal and antibiofilm activity, with no evidence of a significant change in the viability of human tumor and non-tumor cell lines.

Candida/drug effects , Plant Extracts/pharmacology , Biofilms/drug effects , Nyctaginaceae/chemistry , Cell Proliferation/drug effects , Antifungal Agents/pharmacology , Microbial Sensitivity Tests , Cell Survival/drug effects , Biofilms/growth & development , Lethal Dose 50 , Antifungal Agents/isolation & purification
Braz. J. Pharm. Sci. (Online) ; 53(3): e00251, 2017. tab, graf
Article in English | LILACS | ID: biblio-889402


ABSTRACT The triterpene lupeol (1) and some of its esters are secondary metabolites produced by species of Celastraceae family, which have being associated with cytotoxic activity. We report herein the isolation of 1, the semi-synthesis of eight lupeol esters and the evaluation of their in vitro activity against nine strains of cancer cells. The reaction of carboxylic acids with 1 and DIC/DMAP was used to obtain lupeol stearate (2), lupeol palmitate (3) lupeol miristate (4), and the new esters lupeol laurate (5), lupeol caprate (6), lupeol caprilate (7), lupeol caproate (8) and lupeol 3',4'-dimethoxybenzoate (9), with high yields. Compounds 1-9 were identified using FT-IR, 1H, 13C-NMR, CHN analysis and XRD data and were tested in vitro for proliferation of human cancer cell activity. In these assays, lupeol was inactive (GI50> 250µg/mL) while lupeol esters 2 -4 and 7 - 9 showed a cytostatic effect. The XRD method was a suitable tool to determine the structure of lupeol and its esters in solid state. Compound 3 showed a selective growth inhibition effect on erythromyeloblastoid leukemia (K-562) cells in a concentration-dependent way. Lupeol esters 4 and 9 showed a selective cytostatic effect with low GI50 values representing promising prototypes for the development of new anticancer drugs.

Triterpenes/analysis , Celastraceae/classification , Biological Products , Chemoprevention/statistics & numerical data
Rev. bras. farmacogn ; 25(4): 369-374, July-Aug. 2015. tab, graf
Article in English | LILACS-Express | LILACS | ID: lil-763197


AbstractIn this study, antiproliferative and antioxidant activities of crude extracts (hexane, ethyl acetate and methanol) from leaves and stem of Chresta sphaerocephala DC., Asteraceae, were investigated. Antiproliferative activity was tested in vitro against ten human cancer cells and against VERO (no cancer cell). Antioxidant activities were determined using DPPH and ORAC-FL assays and the total phenolic content was estimated by Folin–Ciocalteu method. Hexane and ethyl acetate extracts (leaves and stem) exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 50.40 and 250 µg/ml. For VERO cell, TGI values were >250 µg/ml for all extracts, except to hexane extract of the stem (TGI 80.92 µg/ml). In an initial evaluation, ethyl acetate and methanol extracts (leaves and stem) have shown levels of phenolic compounds between 6.94 and 30.96 mg GAE/kg in Folin–Ciocalteu assay, DPPH free-radical scavenging activity with SC50 in the range of 75.22 and 400 µg/ml and antioxidant capacity between 290.08 and 1088 µmol TE/g of extract in ORAC-FL assay. HPLC-DAD and ESI-MS analysis allowed the identification of flavonoids in the methanol extract from the leaves of C. sphaerocephala. Three steroids and nine triterpenoids were identified in the bioactive hexane extracts using HRGC.