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1.
Molecules ; 28(15)2023 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-37570891

RESUMO

Bismuth-based drugs have been used primarily to treat ulcers caused by Helicobacter pylori and other gastrointestinal ailments. Combined with antibiotics, these drugs also possess synergistic activity, making them ideal for multiple therapy regimens and overcoming bacterial resistance. Compounds based on bismuth have a low cost, are safe for human use, and some of them are also effective against tumoral cells, leishmaniasis, fungi, and viruses. However, these compounds have limited bioavailability in physiological environments. As a result, there is a growing interest in developing new bismuth compounds and approaches to overcome this challenge. Considering the beneficial properties of bismuth and the importance of discovering new drugs, this review focused on the last decade's updates involving bismuth compounds, especially those with potent activity and low toxicity, desirable characteristics for developing new drugs. In addition, bismuth-based compounds with dual activity were also highlighted, as well as their modes of action and structure-activity relationship, among other relevant discoveries. In this way, we hope this review provides a fertile ground for rationalizing new bismuth-based drugs.


Assuntos
Infecções por Helicobacter , Helicobacter pylori , Humanos , Bismuto/farmacologia , Bismuto/uso terapêutico , Antibacterianos/farmacologia , Infecções por Helicobacter/tratamento farmacológico , Quimioterapia Combinada
2.
Andrologia ; 54(3): e14338, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34878673

RESUMO

The objective of this study was to enhance the in vitro sperm quality and in vivo fertility of frozen-thawed equine semen by the addition of l-carnitine (LC) to post-thawed semen. Different concentrations of LC were added to thawed samples to obtain four treatments control and 0.5, 1 and 2 mM LC. In the in vitro experiments, sperm motility and kinematics, membrane integrity and intracellular calcium ion concentration ([Ca2+ ]i ) were investigated, and the antioxidant bioactivity of LC was assessed by measuring hydrogen peroxide and nitrite concentrations (NO2 - ). The fertility rate was assessed via the artificial insemination of mares. The treatment with 1 mM LC increased sperm [Ca2+ ]i (60.6 ± 0.05 AU), reduced nitrite concentration (39.1 ± 14.9 µM/µg protein), increased the sperm straightness percentage (STR: 78.3 ± 5.3%) and increased the pregnancy rate (75%) as compared to the control ([Ca2+ ]i 48.4 ± 0.05 AU, NO2 - concentration 63.1 ± 14.4 µM/µg protein, STR 67.5 ± 7.9%, 12.5% pregnancy rate, p < 0.05). These results suggest that 1 mM LC acts as an antioxidant and stimulator of sperm metabolism in post-thawed equine semen, increasing the fertility rate. Thus, addition of LC might be an alternative to improve the fertility of poor quality post-thawed equine semen.


Assuntos
Preservação do Sêmen , Sêmen , Animais , Antioxidantes/farmacologia , Carnitina/farmacologia , Criopreservação/veterinária , Feminino , Fertilidade , Cavalos , Inseminação Artificial/veterinária , Masculino , Gravidez , Preservação do Sêmen/veterinária , Motilidade dos Espermatozoides , Espermatozoides
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