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1.
Exp Parasitol ; 135(2): 307-13, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23891943

RESUMO

Leishmaniasis' treatment is based mostly on pentavalent antimonials or amphotericin B long-term administration, expensive drugs associated with severe side effects. Considering these aforementioned, the search for alternative effective and safe leishmaniasis treatments is a necessity. This work evaluated a neolignan, licarin A anti-leishmanial activity chemically synthesized by our study group. It was observed that licarin A effectively inhibited Leishmania (Leishmania) major promastigotes (IC50 of 9.59 ± 0.94 µg/mL) growth, by inducing in these parasites genomic DNA fragmentation in a typical death pattern by apoptosis. Additionally, the neolignan proved to be even more active against intracellular amastigotes of the parasite (EC50 of 4.71 ± 0.29 µg/mL), and significantly more effective than meglumine antimoniate (EC50 of 216.2 ± 76.7 µg/mL) used as reference drug. The antiamastigote activity is associated with an immunomodulatory activity, since treatment with licarin A of the infected macrophages induced a decrease in the interleukin (IL)-6 and IL-10 production. This study demonstrates for the first time the antileishmanial activity of licarin A and suggests that the compound may be a promising in the development of a new leishmanicidal agent.


Assuntos
Antiprotozoários/farmacologia , Fatores Imunológicos/farmacologia , Leishmania major/efeitos dos fármacos , Leishmaniose Cutânea/tratamento farmacológico , Lignanas/farmacologia , Anfotericina B/farmacologia , Animais , Antiprotozoários/toxicidade , Apoptose , Citocinas/metabolismo , Fragmentação do DNA , Feminino , Fatores Imunológicos/toxicidade , Concentração Inibidora 50 , Leishmania major/genética , Lignanas/toxicidade , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/imunologia , Macrófagos Peritoneais/parasitologia , Meglumina/farmacologia , Meglumina/toxicidade , Antimoniato de Meglumina , Camundongos , Camundongos Endogâmicos BALB C , Óxido Nítrico/metabolismo , Compostos Organometálicos/farmacologia , Compostos Organometálicos/toxicidade
2.
Int J Mol Sci ; 12(7): 4550-73, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21845096

RESUMO

Seaweeds are an important source of bioactive metabolites for the pharmaceutical industry in drug development. Many of these compounds are used to treat diseases like cancer, acquired immune-deficiency syndrome (AIDS), inflammation, pain, arthritis, as well as viral, bacterial, and fungal infections. This paper offers a survey of the literature for Gracilaria algae extracts with biological activity, and identifies avenues for future research. Nineteen species of this genus that were tested for antibacterial, antiviral, antifungal, antihypertensive, cytotoxic, spermicidal, embriotoxic, and anti-inflammatory activities are cited from the 121 references consulted.


Assuntos
Gracilaria/metabolismo , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Bactérias/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Vírus de DNA/efeitos dos fármacos , Fungos/efeitos dos fármacos , Gracilaria/química , Humanos , Sistema Nervoso/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Vírus de RNA/efeitos dos fármacos
3.
Theriogenology ; 127: 1-6, 2019 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-30611013

RESUMO

The determination of specific reproductive parameters, which allow the early selection of high genetic merit boars from different lines, is critical as it may avoid the high maintenance costs of keeping unfertile males in the production system. The aim of this work was to evaluate body and testicular measurements during the pre-pubertal phase, and associate them with reproductive characteristics, such as precocity and libido, and seminal characteristics during puberty in two different lines. Two pure breeds used in the crossing of female lines (FL) and two crossbred terminal lines (TL) were evaluated through body and testicular biometrical measures and seminal characteristics. Terminal line boars presented greater body weights and testicular measures (P < 0.01) compared to FL animals throughout the pre-pubertal period. TL males had their first collection at 24.0 ±â€¯0.3 weeks, while their FL counterparts started about one week later (25.0 ±â€¯0.3 weeks, P < 0.05) and age of selection presented a two-week delay in FL males (29.0 ±â€¯0.7 versus 27.0 ±â€¯0.6 weeks). Overall, 57% of FL boars were selected up to 31 weeks of age, while 90% of TL males were selected during the same period (P < 0.05). It was observed that genotype did not affect the seminal characteristics evaluated: volume, concentration, number of total spermatozoa, number of viable spermatozoa or sperm motility and kinetics. However, TL crossbred males showed higher percentage of normal spermatozoa and lower percentage of tail and head defects (P < 0.05). Sperm concentration in the 28th week was positively correlated with body weight in the 1st (r = 0.58, P < 0.001) and 15th (r = 0.39, P < 0.05) weeks of age. Moreover, sperm concentration in the 28th week was also correlated with right testicle length (RTL) in the 3rd week (r = 0.40, P < 0.05), and right testicle width (RTW) at week 15 (r = 0.36, P < 0.05). There was a negative correlation between RTW at week 15 and age of selection (r = -0.32, P < 0.05). Therefore, body and testicular measurements in the pre-pubertal period may predict semen concentration and can be used as early classification criteria for the selection of boars from different lines, without the risk of culling high value boars.


Assuntos
Espermatozoides/fisiologia , Suínos/fisiologia , Animais , Peso Corporal , Genótipo , Masculino , Análise do Sêmen/veterinária , Maturidade Sexual , Suínos/anatomia & histologia , Suínos/genética , Testículo/anatomia & histologia
4.
J Steroid Biochem Mol Biol ; 103(3-5): 227-30, 2007 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17321129

RESUMO

Hapten derivatives of 25-hydroxyvitamin D(3) and 1alpha,25-dihydroxyvitamin D(3) were synthesized using the Wittig-Horner approach. Both haptens bearing a carboxylic group at the side chain that can be linked to a protein for raising antibodies of potential utility for the determination of 25-hydroxyvitamin D(3), 1alpha,25-dihydroxyvitamin D(3) and 1alpha-hydroxylated vitamin D(3) analogues.


Assuntos
Calcifediol/síntese química , Haptenos/química , Vitamina D/análogos & derivados , Calcifediol/química , Calcifediol/imunologia , Calcifediol/metabolismo , Haptenos/imunologia , Estrutura Molecular , Vitamina D/síntese química , Vitamina D/química , Vitamina D/imunologia , Vitamina D/metabolismo
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