RESUMEN

Plant cell cultures have become a promising production platform of bioactive compounds for biomedical and cosmetic uses in the last decades. However, the success so far has been limited. The study aimed to evaluate the effectiveness of this unique biotechnology process to obtain a bioactive stem cell extract of Coffea canephora (SCECC) with antioxidant, anti-inflammatory, and regenerative properties. Total phenolic and flavonoid contents were determined in the SCECC by spectrophotometry. The chemical composition of the extracts was characterized by mass spectrometry. Antioxidant activity was evaluated using the colorimetric methods of free radical scavenging 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and the ferric reducing ability of plasma (FRAP). The anti-inflammatory activity was determined in lipopolysaccharide-stimulated RAW 264.7 macrophages through the production of superoxide anion (O2•-), nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and the activity of nuclear factor kappa B (NF-κB). Moreover, the ability of SCECC to stimulate the proliferation and migration of fibroblasts was assessed. Five compounds were tentatively identified, two flavonoids, two phenolic acids, and one sugar. High phenolic content and antioxidant activity were observed in the SCECC. SCECC promoted the proliferation and migration of fibroblasts and suppressed the pro-inflammatory mediators O2•-, NO, TNF-α, and IL-6 in a dose-dependent manner. Moreover, SCECC inhibited the NF-κB transcription factor. Therefore, we obtained evidence that the extract from C. canephora stem cells can be used as a natural agent against skin damage. Hence, it could be of interest in cosmetics for preventing skin aging.

Asunto(s)

RESUMEN

Plant cell cultures have become a promising production platform of bioactive compounds for biomedical and cosmetic uses in the last decades. However, the success so far has been limited. The study aimed to evaluate the effectiveness of this unique biotechnology process to obtain a bioactive stem cell extract of Coffea canephora (SCECC) with antioxidant, anti-inflammatory, and regenerative properties. Total phenolic and flavonoid contents were determined in the SCECC by spectrophotometry. The chemical composition of the extracts was characterized by mass spectrometry. Antioxidant activity was evaluated using the colorimetric methods of free radical scavenging 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and the ferric reducing ability of plasma (FRAP). The anti-inflammatory activity was determined in lipopolysaccharide-stimulated RAW 264.7 macrophages through the production of superoxide anion (O2•-), nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and the activity of nuclear factor kappa B (NF-κB). Moreover, the ability of SCECC to stimulate the proliferation and migration of fibroblasts was assessed. Five compounds were tentatively identified, two flavonoids, two phenolic acids, and one sugar. High phenolic content and antioxidant activity were observed in the SCECC. SCECC promoted the proliferation and migration of fibroblasts and suppressed the pro-inflammatory mediators O2•-, NO, TNF-α, and IL-6 in a dose-dependent manner. Moreover, SCECC inhibited the NF-κB transcription factor. Therefore, we obtained evidence that the extract from C. canephora stem cells can be used as a natural agent against skin damage. Hence, it could be of interest in cosmetics for preventing skin aging.

RESUMEN

Anabolic androgenic steroids lead to cardiac complications and have been shown to exhibit proapoptotic effects in cardiac cells; however, the mechanism involved in those effects is unclear. The aim of this study was to assess whether apoptosis and the activation of caspase-3 (Casp-3) induced by testosterone in high concentrations involves increments in tumor necrosis factor-α (TNF-α) concentrations and angiotensin-converting enzyme (ACE) activity in cardiomyocytes (H9c2) cell cultures. Cardiomyocytes were treated with testosterone (5 × 10(-6) mol/L), doxorubicin (9.2 × 10(-6) mol/L), testosterone + etanercept (Eta; 6.67 × 10(-5) mol/L), testosterone + losartan (Los; 10(-7) mol/L), and testosterone + AC-DEVD-CHO (10(-5) mol/L; Casp-3 inhibitor). Apoptosis was determined by flow cytometry and by the proteolytic activity of Casp-3. We demonstrated that incubation of H9c2 cells for 48 h with testosterone causes the apoptotic death of 60-70% of the cells and co-treatments with Eta, Los, or AC-DEVD-CHO reduced this effect. Testosterone also induces apoptosis (concentration dependent) and increases the proteolytic activity of Casp-3, which were reduced by co-treatments. TNF-α and ACE activities were elevated by testosterone treatment, while co-treatment with Los and Eta reduced these effects. We concluded that an interaction between testosterone, angiotensin II, and TNF-α induced apoptosis and Casp-3 activity in cultured cardiomyocytes, which contributed to the reduced viability of these cells induced by testosterone in toxic concentrations.

Asunto(s)

RESUMEN

RESUMO No Brasil, a família Malvaceae está representada por aproximadamente 200 espécies e algumas foram descritas como gastroproteroras. Pavonia alnifolia A.St.-Hil. (Malvaceae) foi selecionada após uma abordagem quimiossistemática, considerando-se sua potencial capacidade em prevenir lesões gástricas. Assim, a atividade gastroprotetora do extrato etanólico de caules de P. alnifolia foi avaliada utilizando o modelo de indução aguda da lesão gástrica por etanol acidificado em camundongos. Além disso, foram quantificados o teor de flavonóides, pelo método de cloreto de alumínio, e de polifenóis, pelo método Folin-Ciocalteu, uma vez que a relação desses componentes com a proteção gástrica foi evidenciada. Os ensaios apontaram redução acentuada das lesões gástricas em camundongos tratados com o extrato da planta em todas as doses ensaiadas (10, 100 e 300 mg/kg). Esse efeito pode estar relacionado com a presença de polifenóis, cujo teor encontrado foi 74,3 ± 7,5 µg equivalente de pirogalol/mg do material vegetal examinado e 82,7 ± 7,1 µg equivalente de pirogalol /mg da amostra no extrato preparado por percolação e teor de flavonoides totais, que por sua vez apresentou um resultado de 17,1 ± 1,4 µg/mg de extrato. O extrato apresentou proteção da mucosa gástrica e este efeito pode estar relacionado à presença dos polifenóis e flavonóides encontrados

ABSTRACT Gastro protective activity of the Pavonia alnifolia A.St.-Hil. extract. In Brazil, the Malvaceae family is represented by at about 200 species. Some of those species are known as gastro protective ones. The Pavonia alnifolia A.St.-Hil (Malvaceae) was selected after a chemosystematic approach. The gastro preventive activity of the ethanol extract of stems Pavonia alnifolia was evaluated through the use of the Ethanol:chlroridric acid model on mice. The quantification of the total flavonoids (aluminum chloride method) and total polyphenols (Folin-Ciocalteu method) was also performed since the relation of those components with gastric protection has been previously highlighted. The tests showed a significant reduction of the ulcer formation in the mice treated with the plant extract (10, 100 and 300 mg/kg). This effect may be related to the presence of polyphenols whose content was found to be 74.3 ± 7.5 µg/mg of vegetal material and 82.7 ± 7.1 µg/mg of crude extract and flavonoids, which in turn showed a content of 17.1 ± 1.4 µg/mg dry extract

Asunto(s)

RESUMEN

Há poucas informações sobre o efeito tóxico in vivo do extrato etanólico das folhas de Carica papaya (ECP). Portanto, esse estudo caracteriza quimicamente ECP por meio de HPLC-RP e avalia a atividade antimutagênica e citotóxica da fração aquosa de ECP422 Antimutagenic activity of Carica papaya L.Rev Ciênc Farm Básica Apl., 2011;32(3):419-423(CA), empregando ensaio do micronúcleo (MN). O extrato tem predominância de substâncias polares, entre elas a rutina. O ensaio do MN foi realizado em ratos Wistar. Grupos: Controle Negativo (CN), veículo; Controle Positivo (CP40), ciclofosfamida (40 mg/Kg i.p.), 24 horas; Grupo tratado (CA), ECP (500 mg/Kg, p.p.) 24h; Grupo Tratado (CACP40), CA (500 mg/Kg, p.o.) 48, 36 e 24 horas , a última dose de ECP foi administrada junto com ciclofosfamida (40 mg/Kg, i.p.). O índice de MN para CN e CA foi de 3,2 ± 1,79 e 1,6 ± 0,5, e razão PCE/NCE foi de 1,38 ± 0,52 e 1,13 ± 0,28, respectivamente, indicando baixa toxicidade. Por outro lado o índice de MN foi de 20 ± 4,9 para CP40 e 3,0 ± 1,6 para o CACP40, indicando efeito antimutagênico de ECP. Este estudo sugere que ECP possui efeito antimutagênico e baixa toxicidade e que a rutina pode estar envolvida nesse efeito.

There is little information about in vivo toxic effects of the ethanolic extract of leaves of Carica papaya L. (ECP). Therefore, in this study ECP was characterized chemically by HPLC-RP and the antimutagenic and cytotoxic activities of an aqueous solution of ECP (CA) were assessed by the micronucleus (MN) bioassay. The extract consisted mainly of polar substances, one of which was rutin. The MN test was performed on groups of Wistar rats, as follows: negative control (NC) - vehicle; positive control (CP40) - cyclophosphamide (40 mg/kg, ip), 24h; extract-treated (CA) - ECP (500 mg/kg, po), 24h; extract + cyclophosphamide-treated (CACP40) - ECP (500 mg/kg, po), 48, 36 and 24 h, plus cyclophosphamide (40 mg/kg, ip), 24h. The MN index was 3.2 ± 1.79 and 1.6 ± 0.5, for NC and CA, and the PCE-to-NCE ratio was 1.38 ± 0.52 and 1.13 ± 0.28, respectively, indicating low cytotoxicity of CA. CP40 showed a high MN index of 20 ± 4.9, but CACP40 only 3.0 ± 1.6, the same as NC, indicating an antimutagenic effect. The study suggests that ECP has low toxicity and possesses an antimutagenic protective effect in which rutin may be involved.

Asunto(s)

RESUMEN

A espécie vegetal Alpinia zerumbet (Pers.) B.L.Burtt & R.M. Sm. é popularmente empregada para o tratamento de diversas enfermidades, entre elas a hipertensão. Avaliar a composição química, a atividade antihipertensiva e ação na hipertrofia cardíaca do óleo essencial das folhas de Alpinia zerumbet (OEAZ) em ratos foram os objetivos deste estudo. O OEAZ, obtido por hidrodestilação em aparelho Clevenger, teve sua composição química analisada em cromatografia gasosa acoplada à espectrometria de massas (CG-EM). Foram identificados 14 constituintes, sendo terpinen-4-ol (37,45 por cento) o majoritário, seguido pelos óxido de cariofileno (7,56 por cento), trans-hidrato de sabineno (6,61 por cento) e 1,8-cineol (4,02 por cento). A avaliação cardiovascular foi feita após o tratamento crônico de ratos espontaneamente hipertensos (SHR) e seus respectivos controles, ratos Wistar-Kyoto (WKY). Os dados hemodinâmicos revelaram redução da pressão arterial média (PAM) no grupo tratado (SHRP: 160 ± 7 mm Hg; p<0,01) em relação ao não tratado (SHR: 180 ± 5 mm Hg). A relação entre peso do ventrículo esquerdo e peso corporal (VE/PC) do SHRP (2,50 ± 0,03 mg g-1; p<0,01) mostrou-se inferior ao SHR (2,61 ± 0,01 mg g-1), confirmando a redução da hipertrofia cardíaca (HC). Os dados de PAM e VE/PC dos animais SHRP foram estatisticamente diferentes quando comparados com os ratos controle (WKY: 116 ± 2 mm Hg e WKYP: 119 ± 4 mm Hg; p<0,05; WKY: 2,15 ± 0,04 mg g-1 e WKYP: 2,17 ± 0,04 mg g-1 ; p<0,01), indicando não ter havido normalização dos mesmos. Conclui-se que o tratamento crônico com OEAZ foi capaz de determinar redução, mas não a normalização, da PAM e da HC de ratos SHR, provavelmente pela presença dos componentes terpinen-4-ol e 1,8-cineol. Estudos com doses maiores ou período de tratamento superior são necessários para avaliar a possibilidade de o OEAZ normalizar os parâmetros analisados (PAM e HC).

Alpinia zerumbet (Pers.) B.L. Burtt & R.M.Sm. is traditionally employed to treat several diseases such as hypertension. The aim of this study was to evaluate the chemical composition, the anti-hypertensive activity and the capacity to reduce cardiac hypertrophy of the essential oil of A. zerumbet leaves (EOAZ) in rats. EOAZ was obtained through hydrodistillation in Clevenger apparatus and its chemical composition was analyzed by gas chromatography-mass spectrometry (GC-MS). Several constituents (14) were identified, terpen-4-ol (37.45 percent) being the major component, followed by caryophyllene oxide (7.56 percent), trans-sabinene hydrate (6.61 percent) and 1,8-cineol (4.02 percent). The cardiovascular effect was investigated after chronic treatment with spontaneously hypertensive rats (SHR) and their respective controls, Wistar-Kyoto rats (WKY). The treated group showed a lower mean arterial pressure (MAP) (SHRP: 160 ± 7 mm Hg; p<0.01) than the untreated group (SHR: 180 ± 5 mm Hg). The ratio of left ventricle-to-body weight (LV/BW) for SHRP was lower (2.504 ± 0.03 mg g-1; p<0.01) than that for SHR (2.162 ± 0.01 mg g-1), confirming the cardiac hypertrophy (CH) reduction. There were significant differences in MAP and CH between SHRP animals and control rats (WKY: 116 ± 2 mm Hg and WKYP: 119 ± 4 mm Hg; p<0.05. WKY: 2.152 ± 0.04 mg g-1 and WKYP: 2.168 ± 0.04 mg g-1; p<0.01), indicating that these values were not normalized. Those data showed that the chronic treatment with EOAZ reduces MAP and CH in SHR probably due to the presence of the compounds terpinen-4-ol and 1,8-cineol. Studies with higher doses or longer treatment periods are necessary to evaluate whether EOAZ can reduce the analyzed parameters (MAP and CH) to normal values.

Asunto(s)

RESUMEN

The vasodilator effect of the ethanolic extract of leaves from Hancornia speciosa Gomes (HSE) was evaluated in superior mesenteric artery rings. HSE produced a concentration-dependent vasodilation (IC50 = 10.8 +/- 4.0 microg/mL) in arterial rings pre-contracted with phenylephrine, which was completely abolished in endothelium-denuded vessels. Endothelium-dependent vasodilation induced by HSE was strongly reduced by L-NAME (100 microM), a nitric oxide (NO) synthase inhibitor, but neither by atropine, a muscarinic receptor antagonist (1 microM), nor by indomethacin (10 microM), a cyclooxygenase inhibitor. In rings pre-contracted with 80 mM KCl, the vasodilator effect of HSE was shifted to the right and was completely abolished in the presence of L-NAME (100 microM). Similar effects were obtained in mesenteric rings pre-contracted with phenylephrine in the presence of KCl 25 mM alone or in addition to 100 microM L-NAME. In addition, BaCl2 (1 mM) dramatically reduced the vasodilation induced by HSE. Together, these findings led us to conclude that HSE induces an endothelium-dependent vasodilation in rat mesenteric artery, by a mechanism dependent on NO, on the activation of potassium channels and endothelium-derived hyperpolarizing factor release. Rutin, identified as a major peak in the HPLC fingerprint obtained for HSE, might contribute for the observed vasodilator effect, since it was able to induce an endothelium-dependent vasodilation in rat superior mesenteric arteries.

Asunto(s)

RESUMEN

We have investigated the hypoglycemic effect induced by the starch obtained from the unripe fruits of Solanum lycocarpum (Solanaceae). Per os administration of the starch (1000 or 2000 mg/kg, twice daily for 7 days, N = 6) did not change glycemia levels of nondiabetic female Swiss mice weighing 25-30 g. In streptozotocin-induced diabetic mice, similar treatment with the starch did not change the elevated glycemia 3 h after the last dose (diabetic treated with saline = 288 17/309 18; starch 1000 mg/kg = 295 +/- 33; starch 2000 mg/kg = 258 +/- 37; N = 5). In animals fasted for 15 h, per os administration of glucose (600 mg/kg) significantly increased glycemia 1 h later. Previous (-30 min) treatment of the animals with the starch (1000 or 2000 mg/kg; N = 5) did not change the increase of glycemia. Per os administration of the starch (1000 or 2000 mg kg-1 day-1, twice daily for 7 days) did not induce body weight gain or loss. The chemical analysis of the starch indicated the presence of glycoalkaloids, a finding that represents a reason for concern since many of these substances are generally toxic. In interviews with 56 diabetic patients, 29 medicinal plants were reported as useful in their treatment of diabetes and S. lycocarpum was the sixth most frequently mentioned. All patients interviewed reported that they also used insulin or oral hypoglycemic drugs. The results of the present study do not provide evidence for a hypoglycemic effect associated with the polysaccharide fraction of S. lycocarpum in either normal or hyperglycemic mice. These data demonstrate the need for adequate pharmacological investigation of the natural products widely used in folk medicine.

Asunto(s)

RESUMEN

We have investigated the hypoglycemic effect induced by the starch obtained from the unripe fruits of Solanum lycocarpum (Solanaceae). Per os administration of the starch (1000 or 2000 mg/kg, twice daily for 7 days, N = 6) did not change glycemia levels of nondiabetic female Swiss mice weighing 25-30 g. In streptozotocin-induced diabetic mice, similar treatment with the starch did not change the elevated glycemia 3 h after the last dose (diabetic treated with saline = 288 ± 17/309 ± 18; starch 1000 mg/kg = 295 ± 33; starch 2000 mg/kg = 258 ± 37; N = 5). In animals fasted for 15 h, per os administration of glucose (600 mg/kg) significantly increased glycemia 1 h later. Previous (-30 min) treatment of the animals with the starch (1000 or 2000 mg/kg; N = 5) did not change the increase of glycemia. Per os administration of the starch (1000 or 2000 mg kg-1 day-1, twice daily for 7 days) did not induce body weight gain or loss. The chemical analysis of the starch indicated the presence of glycoalkaloids, a finding that represents a reason for concern since many of these substances are generally toxic. In interviews with 56 diabetic patients, 29 medicinal plants were reported as useful in their treatment of diabetes and S. lycocarpum was the sixth most frequently mentioned. All patients interviewed reported that they also used insulin or oral hypoglycemic drugs. The results of the present study do not provide evidence for a hypoglycemic effect associated with the polysaccharide fraction of S. lycocarpum in either normal or hyperglycemic mice. These data demonstrate the need for adequate pharmacological investigation of the natural products widely used in folk medicine

Asunto(s)