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Background: In the present study we investigated the combination effects of anthracycline antibiotic, doxorubicin, with methylxanthine fractions isolated from Bancha and Pu-erh tea leaves, against MCF-7 and MDA-MB-231 breast cancer cell lines.Methods: Neutral red uptake assay was used for assessment of cytotoxicity effects and fractional effect analysis and combination index for evaluation of the combination effects.Results: Doxorubicin was used in varying concentrations by a double dilution method, whereas the methylxanthine fractions were in fixed concentrations – 100, 200, 400 or 600 ?g/ml. Results have shown that methylxanthine fraction isolated from Bancha has synergic effects with doxorubicin, while methylxanthines from Pu-erh displayed antagonistic effects.Conclusions: ?he obtained results lead us to suspect, that even minor differences in the composition of natural products can lead to significant differences in the biological activity of the product.
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Caffeine (CA) is a methylxanthine alkaloid widely used in anti-inflammatory drug associations due to itsvasoconstricting properties. Although CA is acknowledged to interact with a plethora of macromolecules inhuman organism, there was to the best of our knowledge, no survey regarding its possible interactions withcommon inflammation-related targets. Henceforth, this work was concerned in the investigation of CA possibleinteractions with cyclooxygenases-1 and -2 (COX-1 and COX-2), as well as prostaglandin H2 synthase-1and leukotriene A4 hydrolase through in silico approaches. CA molecule was studied as a ligand whereas theligand-macromolecules docking models were created through AutoDock Vina tools. Results showcased that,although the thermodynamic features of the best scoring models did not render enough information to affirmstable interaction between CA and the analyzed macromolecules, more studies are needed to shed light on thepossible role of methylxanthines towards inflammation targets.
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A study was conducted to evaluate the effect of chlorogenic acid (ChA) added pre-cooling and its combination with caffeine added during warming on cooled-stored boar semen parameters. Ten ejaculates were diluted in commercial extender with or without 4.5mg/ml ChA and stored at 15°C. After 0, 24 and 72 hours of storage, aliquots of these doses were taken and incubated at 37°C in the presence or absence of 8.0mM caffeine. Semen quality was evaluated after 10 and 120 minutes of incubation. The ChA increased (P <0.01) the sperm motility, viability, acrosomal integrity and the percentage of spermatozoa with high mitochondrial activity (PMHA), however, decreased (P <0.01) the malondialdehyde (MDA) concentration. Caffeine increased (P<0.05) the sperm motility, viability, PMHA and the MDA concentration and reduced (P <0.05) the acrosome integrity. When associated (ChA+caffeine), there was an increase (P <0.05) in sperm motility and viability, PMHA and acrosome integrity. The addition of ChA to the dilution medium improves the quality of the swine inseminating doses. The addition of caffeine during re-warming is only recommended when the semen is stored for prolonged periods (72h), and the inseminating dose should be used immediately after its addition.(AU)
O objetivo deste estudo foi avaliar os efeitos da adição de ácido clorogênico (ChA) antes do resfriamento e sua combinação com cafeína adicionada durante o reaquecimento sobre a qualidade do sêmen suíno resfriado. Dez ejaculados foram diluídos em diluidor comercial com adição ou não de 4,5mg/mL de ChA e armazenados a 15°C. Após zero, 24 e 72 horas de armazenamento, 10mL foram retirados e incubados a 37°C na presença ou ausência de 8,0mM de cafeína. A qualidade seminal foi avaliada após 10 e 120 minutos de incubação. O ChA aumentou (P<0,01) a motilidade, a viabilidade, a integridade acrosomal e a porcentagem de espermatozoides com alta atividade mitocondrial (PMHA), entretanto diminuiu (P<0,01) a concentração de malondialdeído (MDA). A cafeína aumentou (P<0,05) a motilidade, a viabilidade, a PMHA e a concentração de MDA e reduziu a integridade acrossomal. Quando associados (ChA+cafeína), houve aumento (P<0,05) na motilidade, na PMHA, na viabilidade e na integridade acrossomal. Conclui-se que a adição de ChA ao meio de diluição melhora a qualidade das doses inseminantes de suínos. A adição de cafeína durante o reaquecimento só é recomendada ao sêmen adicionado de ChA quando esse for armazenado por períodos prolongados (72h), devendo a dose inseminante ser utilizada imediatamente após sua adição.(AU)
Subject(s)
Animals , Male , Semen Preservation/veterinary , Caffeine , Cryopreservation/veterinary , Chlorogenic Acid , Sus scrofa , Sperm Motility , AntioxidantsABSTRACT
Background: Bronchial Asthma is one of the worldwide health problems associated with increased morbidity and also mortality. Bronchial Asthma is a disease of airways that is characterized by increased responsiveness of the trachea-bronchial tree. Anti asthmatic drugs are associated with adverse effects which can affect the compliance and course of treatment. Monitoring adverse drug reactions in asthma will play a vital role in alerting physicians about the possibility and circumstances of such events, thereby protecting the user population from avoidable harm.Methods: The study was conducted in 500 bronchial asthma patients (250 patients in Beta 2 agonist group (Salbutamol) and 250 patients in Methylxanthine group (Deriphyllin) who fulfilled the study criteria and were observed for three months at Madras Medical College and Rajiv Gandhi Government General Hospital, Chennai. Their prescriptions were collected and analysed. Adverse drug reactions(ADRs) in each group were collected and evaluated. The causality assessment was done by WHO-UMC assessment scale and severity by using Modified Hartwig-Seigel severity assessment scale.Results: Total 38% of patients taking anti-asthma drugs were encountered adverse drug reactions and were more common in elderly females (61 to 70 years). Adverse Drug Reactions were more common in Methylxanthine group (48%) compared to Beta 2 agonist group (28%). Headache (38%) was the commonest ADR in Methylxanthine group and Tremors (31%) in Beta 2 agonist group. Most of ADRs were mild (95 %), manageable and comes under possible (60 %) category of WHO causality assessment scale.Conclusions: Treatment of Bronchial Asthma is mainly based on Beta 2 agonist and Methylxanthine group. So, occurrence of ADR is much common. Our study offers a representative idea of the ADR profile of anti asthmatic drugs. Constant vigil in detecting ADRs and subsequent dose adjustments can make therapy with anti asthmatic drugs safer and more effective. This, in turn, will improve compliance.
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Objetivou-se avaliar a teofilina como agente capacitante substituto ou associado à heparina sobre a reação acrossômica dos espermatozoides e o desenvolvimento de embriões produzidos in vitro. O experimento foi realizado com quatro touros e três tratamentos, totalizando 12 grupos experimentais. O sêmen dos touros foi avaliado nos tratamentos descritos a seguir: tratamento 1 (HEP): heparina - 10µg/mL; tratamento 2 (TEO): teofilina - 5mM; tratamento 3 (HEP + TEO): heparina (10µg/mL) + teofilina (5mM), por zero, seis, 12 e 18 horas, corados com trypan blue/Giemsa para avaliação da reação acrossômica. Para a produção dos embriões, os agentes capacitantes foram adicionados aos meios de fertilização. Na análise espermática, a taxa de reação acrossômica verdadeira foi maior (P<0,05) no tempo zero hora, enquanto para espermatozoides mortos, as maiores taxas (P<0,05) foram nos tempos de 12h (84,46±5,82) e 18h (86,75±4,19). A taxa de embriões produzidos (37,97±13) e a taxa de eclosão (33,50±14) foram maiores (P<0,05) para o tratamento HEP. Não foi observada diferença (P>0,05) entre touros na análise de reação acrossômica nem na PIVE. A utilização da teofilina foi tão eficiente quanto a da heparina na indução da reação acrossômica, no entanto resultou em menores taxas de produção embrionária.(AU)
The sperm capacitating process should take special attention during in vitro embryo production (IVEP) once that affects the success of embryo production. The study aimed to evaluate theophylline as substitute capacitating agent or in combination with heparin on the sperm acrosome reaction and development of embryos produced in vitro. The experiment was carried out using 4 bulls and 3 treatments, establishing 12 experimental groups. Each bull was evaluated in the following treatments: Treatment 1 (HEP): Heparin - 10mg/mL; Treatment 2 (THEO): Theophylline - 5mM; Treatment 3 (HEP + THEO), Heparin (10mg/mL) + Theophylline (5mM). The semen of bulls was incubated in each treatment for 0, 6, 12 and 18h, stained with Trypan blue / Giemsa and analyzed by electron microscopy for assessment of acrosome reaction. Using sperm of same bulls, capacitating agents were added to the fertilization media, for IVEP. In sperm analysis, the true acrosome reaction rate was higher (P<0.05) in time 0h, while sperm dead rates were highest (P<0.05) at 12h (84.46±5, 82), and 18h (86.75±4.19). The produced embryos rate (37.97±13) and hatching rate (33.50±14) were larger (P<0.05) for HEP treatment. There was no difference (P>0.05) between bulls in acrosome reaction analysis neither for IVEP. The use of theophylline was as effective as heparin in the induction of the acrosome reaction, although it resulted in lower embryo production rates.(AU)
Subject(s)
Animals , Male , Cattle , Acrosome Reaction , Heparin , Semen , Spermatozoa , Theophylline/therapeutic useABSTRACT
Objective To discuss the protective effect of doxofylline on radical surgery for esophageal cancer.Methods Under elective general anesthesia, 60 cases, 35 males and 25 females, aged 45-70 years, BMI 20-30 kg/m2, ASA physical status Ⅰ or Ⅱ, FEV1%>50%, underwent radical surgery for esophageal cancer at middle and distal parts.Random number table was employed to divide these patients into two groups: doxofylline group (group D) and control group (group C) with 30 cases in each.After a routing intravenous induction in the two groups, mechanical ventilation was conducted after bronchial intubation with double channel catheter on the right side.The intravenous injection of doxofylline 4 mg/kg in group D was administrated 30 min after bronchial intubation with double channel catheter.Equal normal saline was instilled to the patients in group C.Blood samples were taken from radial artery to detect the levels of TNF-α, IL-6, IL-10, MDA and SOD at four time points: 10 min (T0) before the one-lung ventilation, 60 min after OLV (T1), after two-lung ventilation (T2) and the end of the operation (T3).Meanwhile, the blood and breath at these time points were tested.The occurrence of OLV, blood loss volumes, fluid input quantities, urine volumes, postoperative hyoxemia and pulmonary inflammation were observed.Results Compared with T0, the activity of SOD in serum and PaO2 in the two groups at T1-T3 decreased (P＜0.05).The concentrations of TNF-α, IL-6, IL-10 and MDA increased significantly (P＜0.05).Compared with group C, the activity of SOD activities and PaO2 in group D at T1-T3 increased while concentrations of TNF-α, IL-6, IL-10 and MDA decreased significantly (P＜0.05).The occurrence rates of postoperative hyoxemia and pulmonary inflammation in group D were obviously lower than those in group C (P＜0.05).Conclusion Doxofylline can suppress patients' inflammatory response and oxidative stress response after OLV and reduce the incidence rates of postoperative hyoxemia and pulmonary inflammation as well as alleviate lung injury triggered by radical surgery for esophageal cancer.
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In food restriction, hypoglycemic episodes can be more severe and persistent. This study assessed the influence of acute exercise and caffeine on the insulin-induced hypoglycemia in freely-fed or malnourished (50% food restriction) young rats. At the age of 60 days, rats under overnight fasting received an insulin injection to cause an episode of hypoglycemia. In some animals, hypoglycemia was preceded by an acute session of exercise, in others, caffeine was orally given 15 minutes after insulin injection; or exercise and caffeine were combined. Blood samples were collected at regular intervals for five hours after insulin injection. A beneficial effect of both exercise or caffeine on the hypoglycemic episode in the malnourished rats was found. In the control rats, the association of exercise+caffeine was more beneficial than either intervention alone. It is discussed that exercise and caffeine, alone or combined, can be used as exogenous anti-hypoglycemic resources, but considering the nutritional status of the subject.
Na restrição alimentar, os episódios de hipoglicemia podem ser mais severos e persistentes. Este trabalho avaliou a influência do exercício agudo e da cafeína sobre a hipoglicemia induzida por insulina em ratos jovens alimentados livremente ou desnutridos (50% de restrição alimentar) desde o nascimento. Aos 60 dias de idade, os ratos em jejum noturno receberam injeção de insulina para causar um episódio de hipoglicemia. Em alguns animais, a hipoglicemia foi precedida por sessão aguda de exercício; em outros foi administrada a cafeína via oral, 15 min. após a injeção de insulina; ou foi associada a exercício e cafeína. Amostras de sangue foram coletadas em intervalos regulares por 5h desde a aplicação da insulina. Registrou-se efeito benéfico do exercício e da cafeína isolados sobre o episódio hipoglicêmico nos ratos desnutridos. Nos ratos controle, a associação de exercício+cafeína teve efeito benéfico mais acentuado do que as intervenções separadas. É discutido que exercício físico e cafeína, isolados ou combinados, podem ser explorados como recursos anti-hipoglicêmicos exógenos, levando-se em consideração porém o estado nutricional do indivíduo.