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Bioisosteric modification on melatonin: synthesis of new naphthalene derivatives, in vitro antioxidant activity and cytotoxicity studies BJPS
Shirinzadeh,Hanif; Ghalia,Mohammed; Tascioglu,Alev; Adjali,Ferial Intissar; Gunesacar,Gulsen; Gurer-Orhan,Hande; Suzen,Sibel.
Melatonin (MLT) is a strong free radical scavenger that protects the body from the deleterious effects of excess oxidants. Synthesis of MLT analogue compounds with antioxidant potency has recently attracted the interest of researchers. In general, the strategy consists of modifying the groups in the different sites of the indole ring or replacing the indole ring with an analogue. As part of our ongoing research, the antioxidant capacity and cytotoxicity of newly synthesized MLT analogue naphthalene derivatives were evaluated. The radical scavenging activity was tested by a 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Most of the synthesized compounds showed significant antioxidant activity in comparison to MLT. The structure-activity relationship was...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Antioxidant; Cytotoxic; Melatonin; MTT; DPPH.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100550
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Comparison of sexual performance and testicular characteristics of melatonin treated Kivircik and Charollais rams during the non-breeding season Arq. Bras. Med. Vet. Zootec.
Cevik,M.; Yilmazer,C.; Kocyigit,A..
ABSTRACT This study was conducted to investigate the effects of melatonin implantation on basic testicular characteristics and reproductive performance of Kivircik and Charollais rams and ewes during the non-breeding season. In this study, 8 Kivircik and 6 Charollais rams were used. Rams were implanted with 54 mg melatonin according to the manufacturer's instructions. At melatonin implantation and at ram introduction the reproductive performance and testicular characteristics were evaluated. Throughout the experimental period, rams were permanently kept outdoors under conditions of natural day length and at ambient temperature. The effects of exogenous melatonin treatments on the reproductive performances of rams and ewes, estrus response, pregnancy rate,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Ram; Melatonin; Fertility; Non-breeding season.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0102-09352017000200278
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Down-Regulation of NFkB, Bax,TGF-β, Smad-2mRNA expression in the Livers of Carbon Tetrachloride Treated Rats using Different Natural Antioxidants BABT
Al-Rasheed,Nouf Mohamed; Fadda,Laila Mohamed; Al-Rasheed,Nawal Mohamed; Ali,Hanaa Mahmoud; Yacoub,Hazar Ibrahim.
The objective of this study is to examine whether silymarin alone or in combination with chlorogenic acid and/ or melatonin plays a modulatory role against apoptotic damage in rats liver induced by of CCl4. The present work revealed that CCl4 induced elevation of in Bax, Smad, TGF-β and NFkBhepatic mRNA expression, administration of silymarin alone down regulates these expressions. Treatment with chlorogenic acid and/ or melatonin along with silymarin produced best results in this concern. Bcl-2 expression was down regulated by CCl4 whereas concurrent treatment of chlorogenic acid and/ or melatonin along with silymarin increased this expression. On conclusion, the use of chlorogenic acid and/ or melatonin potentiates the anti-apoptotic action of silymarin.
Tipo: Info:eu-repo/semantics/article Palavras-chave: CCl4; Silymarin; Chlorogenic acid; Melatonin; MRNA expression.
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132016000100408
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Effect of melatonin administration on subjective sleep quality in chronic obstructive pulmonary disease BJMBR
Nunes,D.M.; Mota,R.M.S.; Machado,M.O.; Pereira,E.D.B.; de Bruin,V.M.S.; de Bruin,P.F.C..
Disturbed sleep is common in chronic obstructive pulmonary disease (COPD). Conventional hypnotics worsen nocturnal hypoxemia and, in severe cases, can lead to respiratory failure. Exogenous melatonin has somnogenic properties in normal subjects and can improve sleep in several clinical conditions. This randomized, double-blind, placebo-controlled study was carried out to determine the effects of melatonin on sleep in COPD. Thirty consecutive patients with moderate to very severe COPD were initially recruited for the study. None of the participants had a history of disease exacerbation 4 weeks prior to the study, obstructive sleep apnea, mental disorders, current use of oral steroids, methylxanthines or hypnotic-sedative medication, nocturnal oxygen...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Chronic obstructive pulmonary disease; Melatonin; Sleep.
Ano: 2008 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2008001000016
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Effect of melatonin and time of administration on irradiation-induced damage to rat testes BJMBR
Take,G.; Erdogan,D.; Helvacioglu,F.; Göktas,G.; Ozbey,G.; Uluoglu,C.; Yücel,B.; Guney,Y.; Hicsonmez,A.; Ozkan,S..
The effect of ionizing irradiation on testes and the protective effects of melatonin were investigated by immunohistochemical and electron microscopic methods. Eighty-two adult male Wistar rats were divided into 10 groups. The rats in the irradiated groups were exposed to a sublethal irradiation dose of 8 Gy, either to the total body or abdominopelvic region using a 60Co source at a focus of 80 cm away from the skin in the morning or evening together with vehicle (20% ethanol) or melatonin administered 24 h before (10 mg/kg), immediately before (20 mg/kg) and 24 h after irradiation (10 mg/kg), all ip. Caspace-3 immunoreactivity was increased in the irradiated group compared to control (P < 0.05). Melatonin-treated groups showed less apoptosis as...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Testes; Gamma-irradiation; Melatonin; Immunohistochemistry; Electron microscopy.
Ano: 2009 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2009000700006
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Effect of melatonin on the functional recovery from experimental traumatic compression of the spinal cord BJMBR
Schiaveto-de-Souza,A.; da-Silva,C.A.; Defino,H.L.A.; Bel,E.A.Del.
Spinal cord injury is an extremely severe condition with no available effective therapies. We examined the effect of melatonin on traumatic compression of the spinal cord. Sixty male adult Wistar rats were divided into three groups: sham-operated animals and animals with 35 and 50% spinal cord compression with a polycarbonate rod spacer. Each group was divided into two subgroups, each receiving an injection of vehicle or melatonin (2.5 mg/kg, intraperitoneal) 5 min prior to and 1, 2, 3, and 4 h after injury. Functional recovery was monitored weekly by the open-field test, the Basso, Beattie and Bresnahan locomotor scale and the inclined plane test. Histological changes of the spinal cord were examined 35 days after injury. Motor scores were progressively...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Spinal cord injury; Melatonin; Functional recovery.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013000400348
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Effect of Photoperiod and Melatonin on Volume and Cellular Parameters of Testis in Pinealectomized Rats International Journal of Morphology
Akosman,Murat Sirri; Özdemir,Vural; Taskiran,Nihal; Akalan,Mehmet Aydin; Bülbül,Aziz.
Mammalian reproductive axis is regulated by the combination of three fundamental tissues of neuroendocrine system including hypothalamus, hypophysis and gonads. In recent years, pineal gland has been included in this axis. The aim of the present study was to investigate the effect of 12L (Light):12D (Dark) photoperiod and melatonin administration (0.5 mg/kg/day; subcutaneously) on testicular volume and cellular parameters of testis at the pinealectomized (PE) rats. For this aim, twelve adult rats were firstly pinealectomized and then divided into two groups as GI and GII randomly. The GI rats served as control group and received only normal saline, whereas GII rats were the melatonin administered group. It was found that the total testicular volume,...
Tipo: Journal article Palavras-chave: Cavalieri Method; Melatonin; Optical Fractionator; Pinealectomy; Stereology; Testis.
Ano: 2013 URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-95022013000300046
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Effects of hypoxia on epididymal sperm parameters and protective role of ibuprofen and melatonin Biol. Res.
Vargas,Álvaro; Bustos-Obregón,Eduardo; Hartley,Ricardo.
Hypobaric hypoxia is of interest due to an increase of human populations working at high altitude. Testicular damage is related to the physiological response (neoangiogenesis) to increased intrascrotal blood flow as temperature rises. Hypoxia is a stress factor with overproduction of reactive oxygen species (ROS). The effect of hypoxia in mice reproductive parameters is analyzed. Animals were exposed to simulated hypoxia of 4,200 meters above sea level (m.a.s.l.) in a chamber for 33.2 days, both to continuous (HH) or intermittent hypoxia (HI) with an intermittency period of 4 days hypoxia /4 days normoxia (500 m.a.s.l.). The anti-inflammatory drug Ibuprofen was administered to a group of mice to control vasodilation and increased blood flow. Melatonin was...
Tipo: Journal article Palavras-chave: Epididymal sperm; Mouse; Ibuprofen; Melatonin.
Ano: 2011 URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602011000200008
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Effects of Ischemia/Reperfusion on ß Cells of Pancreas and Protective Effects of Melatonin Treatment International Journal of Morphology
Yildirim,Ayse  ; Tuncer,Mehmet Cudi; Pamukçu,Özlem  ; Aktas  ,Ayfer  ; Akkus,Murat  .
Oxygen free radicals are considered to be important components involved in the pathophysiological tissue alterations observed during ischemia-reperfusion (I/R). In this study, we investigated the putative protective effects of melatonin treatment on pancreatic I/R injury. Sprague Dawley male rats were subjected to 30 min of pancreatic pedicle occlusion followed by 90 min reperfusion. Melatonin (10 mg/kg. s.c) was administrated 30 min prior to ischemia or I/R application. At the end of the reperfusion periods, rats were decapitated. Pancreatic samples were taken for transmission electron microscopy. The results indicated that ischemia created b cell damage as evidenced by dilatation between the nucleus inner and outer membrane and degeneration on islets of...
Tipo: Journal article Palavras-chave: Pancreas; SS cells; Melatonin; Ischemia; Reperfusion.
Ano: 2009 URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-95022009000200036
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Effects of melatonin on DNA damage induced by cyclophosphamide in rats BJMBR
Ferreira,S.G.; Peliciari-Garcia,R.A.; Takahashi-Hyodo,S.A.; Rodrigues,A.C.; Amaral,F.G.; Berra,C.M.; Bordin,S.; Curi,R.; Cipolla-Neto,J..
The antioxidant and free radical scavenger properties of melatonin have been well described in the literature. In this study, our objective was to determine the protective effect of the pineal gland hormone against the DNA damage induced by cyclophosphamide (CP), an anti-tumor agent that is widely applied in clinical practice. DNA damage was induced in rats by a single intraperitoneal injection of CP (20 or 50 mg/kg). Animals received melatonin during the dark period for 15 days (1 mg/kg in the drinking water). Rat bone marrow cells were used for the determination of chromosomal aberrations and of formamidopyrimidine DNA glycosylase enzyme (Fpg)-sensitive sites by the comet technique and ofXpf mRNA expression by qRT-PCR. The number (mean ± SE) of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Melatonin; Cyclophosphamide; Chromosomal aberration; DNA fragmentation; Comet assay; Xpf expression.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013000300278
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Effects of melatonin on the ovarian response to pinealectomy or continuous light in female rats: similarity with polycystic ovary syndrome BJMBR
Prata Lima,M.F.; Baracat,E.C.; Simões,M.J..
The current study was conducted to investigate the relationship between melatonin and chronic anovulation. Adult (3-4 months old) female Wistar rats were submitted to pinealectomy: group I: pinealectomized ovariectomized melatonin-treated (N = 10); group II: pinealectomized ovariectomized placebo-treated (N = 12); group III: pinealectomized light-treated placebo-treated(N = 10) or maintained under continuous light; group IV: maintained under continuous light, ovariectomized melatonin-treated (N = 22); group V: maintained under continuous light, ovariectomized placebo-treated (N = 10); group VI: maintained under continuous light placebo-treated (N = 10). In order to assess ovarian modifications, unilateral ovariectomy was performed during the fourth month...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Melatonin; Polycystic ovary syndrome; Pineal body; Anovulation.
Ano: 2004 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2004000700007
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Effects of Melatonin on Tibia Bone Defects in Rats International Journal of Morphology
Koparal,M; Irtegün,S; Alan,H; Deveci,E; Gülsün,B; Pektanç,G.
The aim of this study was to evaluate the effects of melatonin healing in a tibial bone defect model in rats by means of histopathological and immunohistochemistry analysis. Twenty one male Wistar albino rats were used in this study. In each animal, bone defects (6 mm length ) were created in the tibias. The animals were divided into three groups. In group 1 control group (rats which tibial defects). Group 2 melatonin (10 mg/kg) + 14 days in the tibial defect group) was administered intraperitoneally to rats. Group 3 melatonin (10 mg/kg) + 28 days in the tibial defect group) was administered intraperitoneally to rats. Histopathological analysis of samples was performed to evaluate the process of osteoblastic activity, matrix formation, trabecular bone...
Tipo: Journal article Palavras-chave: Tibial defects; Melatonin; Osteonectin; Osteopontin.
Ano: 2016 URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-95022016000200053
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Evolution of circadian organization in vertebrates BJMBR
Circadian organization means the way in which the entire circadian system above the cellular level is put together physically and the principles and rules that determine the interactions among its component parts which produce overt rhythms of physiology and behavior. Understanding this organization and its evolution is of practical importance as well as of basic interest. The first major problem that we face is the difficulty of making sense of the apparently great diversity that we observe in circadian organization of diverse vertebrates. Some of this diversity falls neatly into place along phylogenetic lines leading to firm generalizations: i) in all vertebrates there is a "circadian axis" consisting of the retinas, the pineal gland and the...
Tipo: Info:eu-repo/semantics/other Palavras-chave: Circadian rhythms; Evolution; Vertebrates; Pineal; SCN; Retina; Melatonin.
Ano: 1997 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X1997000300003
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Ghost protein damage by peroxynitrite and its protection by melatonin BJMBR
Di Mascio,P.; Dewez,B.; Garcia,C.R.S..
We have studied the effect of peroxynitrite (ONOO-) on the membrane cytoskeleton of red blood cells and its protection by melatonin. Analysis of the protein fraction of the preparation by SDS-PAGE revealed a dose-dependent (0-600 µM ONOO-) disappearance at pH 7.4 of the main proteins: spectrin, band 3, and actin, with the concomitant formation of high-molecular weight aggregates resistant to reduction by ß-mercaptoethanol (2%) at room temperature for 20 min. These aggregates were not solubilized by 8 M urea. Incubation of the membrane cytoskeleton with ONOO- was characterized by a marked depletion of free sulfhydryl groups (50% at 250 µM ONOO-). However, a lack of effect of ß-mercaptoethanol suggests that, under our conditions, aggregate formation is not...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Peroxynitrite; Melatonin; Spectrin; Protein; Ghost; Thiols.
Ano: 2000 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000100002
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Indole ring oxidation by activated leukocytes prevents the production of hypochlorous acid BJMBR
Ximenes,V.F.; Paino,I.M.M.; Faria-Oliveira,O.M.M. de; Fonseca,L.M. da; Brunetti,I.L..
Hypochlorous acid (HOCl) released by activated leukocytes has been implicated in the tissue damage that characterizes chronic inflammatory diseases. In this investigation, 14 indole derivatives, including metabolites such as melatonin, tryptophan and indole-3-acetic acid, were screened for their ability to inhibit the generation of this endogenous oxidant by stimulated leukocytes. The release of HOCl was measured by the production of taurine-chloramine when the leukocytes (2 x 10(6) cells/mL) were incubated at 37ºC in 10 mM phosphate-buffered saline, pH 7.4, for 30 min with 5 mM taurine and stimulated with 100 nM phorbol-12-myristate acetate. Irrespective of the group substituted in the indole ring, all the compounds tested including indole,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Leukocytes; Myeloperoxidase; Hypochlorous acid; Indole ring; Melatonin; Indole-3-acetic acid.
Ano: 2005 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005001100003
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Influence of melatonin on the development of functional nicotinic acetylcholine receptors in cultured chick retinal cells BJMBR
Sampaio,L.F.S.; Hamassaki-Britto,D.E.; Markus,R.P..
The influence of melatonin on the developmental pattern of functional nicotinic acetylcholine receptors was investigated in embryonic 8-day-old chick retinal cells in culture. The functional response to acetylcholine was measured in cultured retina cells by microphysiometry. The maximal functional response to acetylcholine increased 2.7 times between the 4th and 5th day in vitro (DIV4, DIV5), while the Bmax value for [125I]-alpha-bungarotoxin was reduced. Despite the presence of alpha8-like immunoreactivity at DIV4, functional responses mediated by alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors were observed only at DIV5. Mecamylamine (100 µM) was essentially without effect at DIV4 and DIV5, while dihydro-ß-erythroidine (10-100 µM) blocked...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Retina; Development; Nicotinic acetylcholine receptors; Alpha-bungarotoxin; Melatonin; Microphysiometry.
Ano: 2005 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005000400015
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Influence of the pineal gland on the physiology, morphometry and morphology of pancreatic islets in rats BJB
LIMA,L. M. B. de; REIS,L. C. dos; LIMA,M. A. de.
To investigate the influence of the pineal gland through melatonin secretion on the physiological and morphological parameters of pancreatic islets, we studied the plasma biochemistry and morphological and morphometric characteristics of the endocrine pancreas of male Wistar rats. The animals were distributed into five groups of ten rats each: NC - normal control group; NS - sham-operated group; Px (25) - pinealectomised group, studied 15-25 days after surgery; Px (70) - pinealectomised group, studied 60-70 days after surgery; ALX - alloxan monohydrate-treated group. Data are analyzed statistically by ANOVA and by the Kruskal-Wallis test. Although there was no significant difference in plasma glucose or insulin levels between the Px (25), Px (70) and NC...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Pinealectomy; Melatonin; Pancreatic islet; Rat; Morphology.
Ano: 2001 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0034-71082001000200018
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Long-term melatonin treatment reduces ovarian mass and enhances tissue antioxidant defenses during ovulation in the rat BJMBR
Chuffa,L.G.A.; Amorim,J.P.A.; Teixeira,G.R.; Mendes,L.O.; Fioruci,B.A.; Pinheiro,P.F.F.; Seiva,F.R.F.; Novelli,E.L.B.; Mello Júnior,W.; Martinez,M.; Martinez,F.E..
Melatonin regulates the reproductive cycle, energy metabolism and may also act as a potential antioxidant indoleamine. The present study was undertaken to investigate whether long-term melatonin treatment can induce reproductive alterations and if it can protect ovarian tissue against lipid peroxidation during ovulation. Twenty-four adult female Wistar rats, 60 days old (± 250-260 g), were randomly divided into two equal groups. The control group received 0.3 mL 0.9% NaCl + 0.04 mL 95% ethanol as vehicle, and the melatonin-treated group received vehicle + melatonin (100 µg·100 g body weight-1·day-1) both intraperitoneally daily for 60 days. All animals were killed by decapitation during the morning estrus at 4:00 am. Body weight gain and body mass index...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Melatonin; Ovary mass; Lipid peroxidation; Antioxidant defenses; Superoxide dismutase.
Ano: 2011 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2011000300007
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Melatonin and N-acetyl-serotonin cross the red blood cell membrane and evoke calcium mobilization in malarial parasites BJMBR
Hotta,C.T.; Markus,R.P.; Garcia,C.R.S..
The duration of the intraerythrocytic cycle of Plasmodium is a key factor in the pathogenicity of this parasite. The simultaneous attack of the host red blood cells by the parasites depends on the synchronicity of their development. Unraveling the signals at the basis of this synchronicity represents a challenging biological question and may be very important to develop alternative strategies for therapeutic approaches. Recently, we reported that the synchrony of Plasmodium is modulated by melatonin, a host hormone that is synthesized only during the dark phases. Here we report that N-acetyl-serotonin, a melatonin precursor, also releases Ca2+ from isolated P. chabaudi parasites at micro- and nanomolar concentrations and that the release is blocked by 250...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Malaria; Plasmodium; Calcium; Melatonin; Circadian rhythm; Host-parasite interaction.
Ano: 2003 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003001100016
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Melatonin in maturation media fails to improve oocyte maturation, embryo development rates and DNA damage of bovine embryos Scientia Agricola
Takada,Luciana; Martins Junior,Alicio; Mingoti,Gisele Zoccal; Balieiro,Julio César Carvalho; Coelho,Lia Alencar.
Melatonin (MEL) acts as a powerful scavenger of free radicals and direct gonadal responses to melatonin have been reported in the literature. Few studies, however, have evaluated the effect of MEL during in vitro maturation (IVM) on bovine embryos. This study tested the addition of MEL to maturation medium (MM) with no gonadotropins on nuclear maturation and embryo development rates and the incidence of DNA damage in resulting embryos. Cumulus-oocyte complexes were aspirated from abattoir ovaries and cultured in MM (TCM-199 medium supplemented with 10% fetal calf serum - FCS) at 39ºC and 5% CO2 in air. After 24 hours of culture in MM with 0.5 µg mL-1 FSH and 5.0 µg mL-1 LH; 10-9 M MEL) or 10-9 M MEL, 0.5 µg mL-1 FSH and 5.0 µg mL-1 LH, the oocytes were...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Comet assay; Embryos; Gonadotropins; In vitro fertilization; Melatonin.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-90162010000400003
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