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1.
3 Biotech ; 14(4): 94, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38444785

RESUMO

We analyzed here the in silico biological activities of caffeine, (+)-catechin, and theobromine. For this, the PubChem database of the NIH (National Institutes of Health) was used to obtain the SMILE canonical form of the bioactive molecules, and the free software PASS Online (Prediction of Activity Spectra for Substances) from the Way2Drug portal. Also, we conducted an in vitro experiment using a chronic myeloid leukemia (CML) cell line (K562) to confirm some results found in in silico investigation. These cells were exposed to different concentrations of caffeine, (+)-catechin, and theobromine for 72 h. The results found in this in silico study suggested that caffeine, (+)-catechin, and theobromine showed excellent biological properties, such as antioxidant, anti-inflammatory, and anticarcinogenic, as well as protection against cardiovascular, diabetes, neurological, allergic, respiratory, and other therapeutic activities. These findings can be elucidated through the modulation exerted by these bioactive molecules in many biochemical pathways involved in organism homeostasis, such as free radical scavenger action, oxidoreductase inhibitor, membrane permeability inhibitor, and lipid peroxidase inhibitor. In addition, we have found here that caffeine, (+)-catechin, and theobromine have a remarkable anti-inflammatory activity which plays an important role in the therapeutic approach of COVID-19. Moreover, our in vitro findings confirmed the in silico results regarding anticancer activity since these molecules reduce cell proliferation at all tested concentrations. Therefore, since these molecules exhibit important medicinal activities, further investigations should be conducted to reveal new therapies to improve the treatments and prevention of numerous disorders and, consequently, promote human health.

2.
J Food Biochem ; 46(12): e14512, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36332189

RESUMO

Melanoma frequently presents a poor chemotherapy response. In this scenario, investigations for new therapies are essential. Thus, cocoa is highlighted in this area since it presents many biological properties. This study investigated the anticarcinogenic activity of cocoa in melanoma cell lines (A-375 and B16-F10). Melanoma and fibroblast (HFF-1) cell lines were exposed to different concentrations of cocoa seeds (30 to 2000 ug/ml) at 24 and 72 h. Cocoa was also associated with paclitaxel IC50. We conducted viability, proliferation, and oxidative stress analyses. Our findings suggested that cocoa isolated, at almost all concentrations tested, was able to reduce viability and proliferation of B16-F10 cells and proliferation of A-375 cells via oxidative stress increasing. Also, cocoa caused no damage in fibroblast cells. Moreover, cocoa increased paclitaxel activity on A-375 by reducing cell proliferation and increasing oxidative stress. Therefore, the results highlight cocoa as a potent selective adjuvant anticancer agent against melanoma. PRACTICAL APPLICATIONS: In conclusion, more studies should be performed to deeply explore this remarkable action of cocoa as a an promising adjuvant to enhance chemotherapy.


Assuntos
Antineoplásicos , Cacau , Melanoma , Linhagem Celular Tumoral , Melanoma/tratamento farmacológico , Estresse Oxidativo , Paclitaxel/farmacologia
3.
Theriogenology ; 171: 30-37, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34004368

RESUMO

Although prostaglandins are important in the ovulation process, a precise role for prostaglandin F2α (PGF) has not been elucidated. This study aimed to evaluate the regulation of PGF receptor mRNA (PTGFR) in granulosa cells and the local effect of PGF on ovulation and luteinization. In Experiment 1, using samples collected in vivo before (Day 2), during (Day 3) and after (Day 4) follicular deviation, expression of PTGFR in bovine granulosa cells was more abundant in the dominant follicle after deviation than in subordinates (P < 0.05). However, the expression of PTGFR was not regulated (P = 0.1) in preovulatory follicles at different time-points (0, 3, 6, 12 and 24 h) after ovulation induction with GnRH. In Experiment 2, to assess the role of systemic PGF treatment on luteinization and vascularization of preovulatory follicles, flunixin meglumine (FM), a nonsteroidal anti-inflammatory drug, was used to inhibit endogenous prostaglandin synthesis. Cows with preovulatory follicles were induced to ovulate with GnRH (0 h) and allocated to three groups: Control, with no further treatment; FM, treated with 2.2 mg/kg FM im 17 h after GnRH treatment; and FM + PGF, treated with FM 17 h after GnRH, followed by 25 mg dinoprost tromethamine (PGF) 23 h after GnRH treatment. FM injection was able to reduce the concentration of PGF in the follicular fluid (FF) (P < 0.001). However, contrary to our hypothesis, color Doppler ultrasound evaluations revealed decreased vascular flow in FM + PGF group (P < 0.05), and no effect of the treatments on intrafollicular P4 and E2 concentrations 24 h after GnRH. The prostaglandin metabolite (PGFM) concentrations in the FF were greater in cows receiving systemic PGF (P < 0.001), which prompted us to further check its role on ovulation. Therefore, in Experiment 3, in a final attempt to demonstrate the local effect of PGF on ovulation, cows with preovulatory follicles received an intrafollicular injection (IFI) of PBS (Control) or 100 ng/mL purified PGF (PGF group). PGF treatment did not affect the time of ovulation after IFI (66 ± 6.4 and 63 ± 8.5 h for control and PGF, respectively; P > 0.05), further suggesting that it has no direct effect in the ovulatory process. Based on our findings, we concluded that FM decreased PGF synthesis within the follicle, whereas PGF treatment decreased follicular vascularization. In addition, the in vivo model of intrafollicular injection evidenced that PGF alone is not able to locally induce ovulation.


Assuntos
Dinoprosta , Progesterona , Animais , Bovinos , Dinoprosta/farmacologia , Feminino , Hormônio Liberador de Gonadotropina/farmacologia , Luteinização , Folículo Ovariano , Ovulação
4.
Braz. J. Vet. Res. Anim. Sci. (Online) ; 58: e175001, 2021. ilus, graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1344777

RESUMO

This study aimed to evaluate the role of prostaglandin F2α (PGF) on ovulation. In Experiment 1, cows were randomly allocated to two treatments to receive 150 µg of d-Cloprostenol (PGF Group, n = 12) or 2 mL of NaCl 0.9% (Control Group, n = 11) and CIDRs, were removed 4 days later. No cow ovulated in Control and PGF groups. In Experiment 2, cows were randomly separated into two experimental groups to receive 4 injections of 150 µg of d-Cloprostenol (n = 9) or 2 mL of NaCL 0.9% (n = 9). In this experiment, ovulation was not observed in any cows. In Experiment 3, ovariectomized cows receive three injections of 300µg of PGF analog (PGF Group, n = 5), 100µg of Lecirelin (GnRH Group, n = 5) or 2 mL of PBS (Control Group, n = 4). The LH concentration was higher (P <0.0001) in cows from the GnRH group than in the PGF and Control groups. In experiment 4, cows with preovulatory follicles (>11.5 mm) were treated with Saline (Control Group, n = 6); Lecirelin (GnRH Group, n = 7) or Cloprostenol Sodium (PGF Group, n = 6). There was a significant increase in the vascular area of follicles from 0 to 24 h in GnRH and PGF treatments. In conclusion, PGF was not able to induce ovulation in cows with high or low plasma progesterone concentration. Additionally, PGF alone was not able to induce LH release and follicle luteinization, but increased follicular vascularization.(AU)


O objetivo deste estudo foi avaliar o papel da prostaglandina F2α (PGF) na ovulação. No Experimento 1, as vacas foram alocadas aleatoriamente em dois tratamentos para receber 150 µg de d-Cloprostenol (Grupo PGF, n = 12) ou 2 mL de NaCl 0,9% (Grupo Controle, n = 11) e os CIDR, foram removidos 4 dias depois. Nenhuma vaca ovulou nos grupos Controle e PGF. No Experimento 2, as vacas foram separadas aleatoriamente em dois grupos experimentais para receber 4 injeções de 150 µg de d-Cloprostenol (n = 9) ou 2 mL de NaCL 0,9% (n = 9). Não foi observada ovulação em nenhum dos animais deste experimento. No Experimento 3, vacas ovariectomizadas receberam três injeções de 300µg de análogo de PGF (Grupo PGF, n = 5), 100µg de Lecirelina (Grupo GnRH, n = 5) ou 2 mL de PBS (Grupo Controle, n = 4). A concentração de LH foi maior (P <0,0001) nas vacas do grupo GnRH do que nos grupos PGF e Controle. No Experimento 4, vacas com folículos pré-ovulatórios (> 11,5 mm) foram tratadas com solução salina (Grupo Controle, n = 6), Lecirelina (Grupo GnRH, n = 7) ou Cloprostenol Sódico (Grupo PGF, n = 6). Houve um aumento significativo na área vascular dos folículos de 0 a 24h nos tratamentos com GnRH e PGF. Em conclusão, a PGF não foi capaz de induzir ovulação em vacas com alta ou baixa concentração plasmática de progesterona. Além disso, a PGF sozinha não foi capaz de induzir a liberação de LH e a luteinização do folículo, mas aumentou a vascularização folicular.(AU)


Assuntos
Animais , Feminino , Bovinos , Prostaglandinas Sintéticas , Bovinos/embriologia , Bovinos/fisiologia , Hormônio Luteinizante , Dinoprosta/análise , Ovulação , Hipófise
5.
Radiol Bras ; 49(1): 6-11, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26929454

RESUMO

OBJECTIVE: To determine the rates of diagnostic underestimation at stereotactic percutaneous core needle biopsies (CNB) and vacuum-assisted biopsies (VABB) of nonpalpable breast lesions, with histopathological results of atypical ductal hyperplasia (ADH) or ductal carcinoma in situ (DCIS) subsequently submitted to surgical excision. As a secondary objective, the frequency of ADH and DCIS was determined for the cases submitted to biopsy. MATERIALS AND METHODS: Retrospective review of 40 cases with diagnosis of ADH or DCIS on the basis of biopsies performed between February 2011 and July 2013, subsequently submitted to surgery, whose histopathological reports were available in the internal information system. Biopsy results were compared with those observed at surgery and the underestimation rate was calculated by means of specific mathematical equations. RESULTS: The underestimation rate at CNB was 50% for ADH and 28.57% for DCIS, and at VABB it was 25% for ADH and 14.28% for DCIS. ADH represented 10.25% of all cases undergoing biopsy, whereas DCIS accounted for 23.91%. CONCLUSION: The diagnostic underestimation rate at CNB is two times the rate at VABB. Certainty that the target has been achieved is not the sole determining factor for a reliable diagnosis. Removal of more than 50% of the target lesion should further reduce the risk of underestimation.


OBJETIVO: Determinar o grau de subestimação diagnóstica de biópsias mamárias percutâneas estereotáxicas por agulha grossa (core biopsy) e assistidas a vácuo (mamotomia) em lesões não palpáveis, com resultados histopatológico de hiperplasia ductal atípica (HDA) ou carcinoma ductal in situ (CDIS) e que foram submetidas a exérese cirúrgica posteriormente. Como objetivo secundário, atribuiu-se a frequência de HDA e CDIS nos casos biopsiados. MATERIAIS E MÉTODOS: Foram revisados, retrospectivamente, 40 casos biopsiados com diagnóstico de HDA ou CDIS, entre fevereiro de 2011 e julho de 2013, e que posteriormente foram submetidos a cirurgia, cujo laudo histopatológico estava registrado no sistema interno de informações. Os resultados das biópsias foram comparados aos da cirurgia e a taxa de subestimação foi calculada de acordo com equações matemáticas específicas. RESULTADOS: A taxa de subestimação diagnóstica da core biopsy foi 50% para HDA e 28,57% para CDIS, e da mamotomia foi 25% para HDA e 14,28% para CDIS. As HDAs representaram 10,25% do total de casos biopsiados, enquanto 23,91% foram CDIS. CONCLUSÃO: A taxa de subestimação diagnóstica é cerca de duas vezes maior na core biopsy em relação à mamotomia. A certeza do alvo atingido não é o único determinante para um diagnóstico preciso. Remover mais que 50% da lesão alvo poderá diminuir o risco de subestimação diagnóstica.

6.
Radiol. bras ; 49(1): 6-11, Jan.-Feb. 2016. tab, graf
Artigo em Português | LILACS | ID: lil-775177

RESUMO

Abstract Objective: To determine the rates of diagnostic underestimation at stereotactic percutaneous core needle biopsies (CNB) and vacuum-assisted biopsies (VABB) of nonpalpable breast lesions, with histopathological results of atypical ductal hyperplasia (ADH) or ductal carcinoma in situ (DCIS) subsequently submitted to surgical excision. As a secondary objective, the frequency of ADH and DCIS was determined for the cases submitted to biopsy. Materials and Methods: Retrospective review of 40 cases with diagnosis of ADH or DCIS on the basis of biopsies performed between February 2011 and July 2013, subsequently submitted to surgery, whose histopathological reports were available in the internal information system. Biopsy results were compared with those observed at surgery and the underestimation rate was calculated by means of specific mathematical equations. Results: The underestimation rate at CNB was 50% for ADH and 28.57% for DCIS, and at VABB it was 25% for ADH and 14.28% for DCIS. ADH represented 10.25% of all cases undergoing biopsy, whereas DCIS accounted for 23.91%. Conclusion: The diagnostic underestimation rate at CNB is two times the rate at VABB. Certainty that the target has been achieved is not the sole determining factor for a reliable diagnosis. Removal of more than 50% of the target lesion should further reduce the risk of underestimation.


Resumo Objetivo: Determinar o grau de subestimação diagnóstica de biópsias mamárias percutâneas estereotáxicas por agulha grossa (core biopsy) e assistidas a vácuo (mamotomia) em lesões não palpáveis, com resultados histopatológico de hiperplasia ductal atípica (HDA) ou carcinoma ductal in situ (CDIS) e que foram submetidas a exérese cirúrgica posteriormente. Como objetivo secundário, atribuiu-se a frequência de HDA e CDIS nos casos biopsiados. Materiais e Métodos: Foram revisados, retrospectivamente, 40 casos biopsiados com diagnóstico de HDA ou CDIS, entre fevereiro de 2011 e julho de 2013, e que posteriormente foram submetidos a cirurgia, cujo laudo histopatológico estava registrado no sistema interno de informações. Os resultados das biópsias foram comparados aos da cirurgia e a taxa de subestimação foi calculada de acordo com equações matemáticas específicas. Resultados: A taxa de subestimação diagnóstica da core biopsy foi 50% para HDA e 28,57% para CDIS, e da mamotomia foi 25% para HDA e 14,28% para CDIS. As HDAs representaram 10,25% do total de casos biopsiados, enquanto 23,91% foram CDIS. Conclusão: A taxa de subestimação diagnóstica é cerca de duas vezes maior na core biopsy em relação à mamotomia. A certeza do alvo atingido não é o único determinante para um diagnóstico preciso. Remover mais que 50% da lesão alvo poderá diminuir o risco de subestimação diagnóstica.

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