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1.
Nutrients ; 15(20)2023 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-37892513

RESUMO

Monosodium glutamate (MSG) is the sodium salt of glutamic acid (GLA), used as a flavour enhancer. MSG is considered a controversial substance. It is incriminated in disturbing the antioxidant system, but also has beneficial effects, as GLA metabolism plays a crucial role in homeostasis. This study highlights which positive or negative aspects of MSG sub-chronic consumption are better reflected in subjects potentially affected by advanced age. Daily doses of MSG were administered to four groups of two-year-old Wistar rats for 90 days: (I) 185 mg/kg bw, (II) 1500 mg/kg bw, (III) 3000 mg/kg bw and (IV) 6000 mg/kg bw, compared to a MSG non-consumer group. Aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, direct and total bilirubin, total cholesterol, triglycerides, creatinine and urea levels were analysed; stomach, liver and kidney samples were subjected to histopathological analysis. Although, in most cases, there were no statistical differences, interesting aspects of the dose-effect relationship were observed. After MSG sub-chronic consumption, the positive aspects of GLA seem to be reflected better than the negative ones. The hormesis effect, with low-level reactive oxygen species' protective effects and GLA metabolism, may represent the hypothesis of a potential defence mechanism triggered by MSG sub-chronic consumption in ageing rats.


Assuntos
Antioxidantes , Glutamato de Sódio , Ratos , Humanos , Animais , Pré-Escolar , Ratos Wistar , Glutamato de Sódio/farmacologia , Antioxidantes/farmacologia , Rim/metabolismo , Fígado/metabolismo
2.
Molecules ; 28(10)2023 May 16.
Artigo em Inglês | MEDLINE | ID: mdl-37241864

RESUMO

Glutamic acid is a non-essential amino acid involved in multiple metabolic pathways. Of high importance is its relationship with glutamine, an essential fuel for cancer cell development. Compounds that can modify glutamine or glutamic acid behaviour in cancer cells have resulted in attractive anticancer therapeutic alternatives. Based on this idea, we theoretically formulated 123 glutamic acid derivatives using Biovia Draw. Suitable candidates for our research were selected among them. For this, online platforms and programs were used to describe specific properties and their behaviour in the human organism. Nine compounds proved to have suitable or easy to optimise properties. The selected compounds showed cytotoxicity against breast adenocarcinoma, lung cancer cell lines, colon carcinoma, and T cells from acute leukaemia. Compound 2Ba5 exhibited the lowest toxicity, and derivative 4Db6 exhibited the most intense bioactivity. Molecular docking studies were also performed. The binding site of the 4Db6 compound in the glutamine synthetase structure was determined, with the D subunit and cluster 1 being the most promising. In conclusion, glutamic acid is an amino acid that can be manipulated very easily. Therefore, molecules derived from its structure have great potential to become innovative drugs, and further research on these will be conducted.


Assuntos
Antineoplásicos , Neoplasias da Mama , Humanos , Feminino , Ácido Glutâmico/farmacologia , Relação Estrutura-Atividade , Glutamina , Simulação de Acoplamento Molecular , Antineoplásicos/farmacologia , Antineoplásicos/química , Aminoácidos/farmacologia , Estrutura Molecular , Ensaios de Seleção de Medicamentos Antitumorais , Proliferação de Células , Linhagem Celular Tumoral
3.
Saudi Pharm J ; 30(9): 1327-1344, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36249938

RESUMO

Effective communication between pharmacists and patients is essential for therapeutic success. The pharmacist's perspective may differ from that of the patient in terms of effective communication. Our study aimed to assess the communication efficiency in the pharmacist-patient relationship from the pharmacists' perspective. We hypothesize that the community pharmacist's perspective can lead to relevant aspects of patient-centred communication and their profession. A cross-sectional study was conducted through an online questionnaire addressed to pharmacists. A number of 506 questionnaires were collected, evaluated, analyzed and interpreted. The questionnaire focused on the following main issues: degree of job satisfaction, essential skills of a pharmacist working in a community pharmacy, different aspects of pharmacist-patient communication, shared decision-making, patient monitoring plan and other elements related to a patient under treatment (healthy lifestyle, receptivity to counselling, loyalty and appreciation of pharmaceutical services). The pharmacist's efficiency in communication with the patient and professional education were also targeted in the study. There are no significant differences between job satisfaction in women compared to men. However, the job satisfaction increases with the average age. Caregiver, communicator and life-long learner were identified as essential skills of a pharmacist. Pharmacists participating in the study generally perceive themselves as good communicators with the patient. Nevertheless, many particular aspects of communication with patients can be greatly improved. The lack of training in the spirit of the "patient-centred communication" concept has been identified. Still, more than a third of the respondents are missing the need for professional training. A periodic evaluation of the efficiency of pharmacist-patient communication in the community pharmacy is necessary. The degree of subjectivity of the pharmacist from this perspective and self-sufficiency would be significantly diminished if the pharmacists had access to the results of the periodic evaluations.

4.
Pharmaceutics ; 14(8)2022 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-36015376

RESUMO

The emergence of bacterial resistance has motivated researchers to discover new antibacterial agents. Nowadays, fluoroquinolones keep their status as one of the essential classes of antibacterial agents. The new generations of fluoroquinolones are valuable therapeutic tools with a spectrum of activity, including Gram-positive, Gram-negative, and atypical bacteria. This review article surveys the design of fluoroquinolone hybrids with other antibacterial agents or active compounds and underlines the new hybrids' antibacterial properties. Antibiotic fluoroquinolone hybrids have several advantages over combined antibiotic therapy. Thus, some challenges related to joining two different molecules are under study. Structurally, the obtained hybrids may contain a cleavable or non-cleavable linker, an essential element for their pharmacokinetic properties and mechanism of action. The design of hybrids seems to provide promising antibacterial agents helpful in the fight against more virulent and resistant strains. These hybrid structures have proven superior antibacterial activity and less susceptibility to bacterial resistance than the component molecules. In addition, fluoroquinolone hybrids have demonstrated other biological effects such as anti-HIV, antifungal, antiplasmodic/antimalarial, and antitumor activity. Many fluoroquinolone hybrids are in various phases of clinical trials, raising hopes that new antibacterial agents will be approved shortly.

5.
Pharmaceutics ; 13(8)2021 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-34452252

RESUMO

The evolution of the class of antibacterial quinolones includes the introduction in therapy of highly successful compounds. Although many representatives were withdrawn due to severe adverse reactions, a few representatives have proven their therapeutical value over time. The classification of antibacterial quinolones into generations is a valuable tool for physicians, pharmacists, and researchers. In addition, the transition from one generation to another has brought new representatives with improved properties. In the last two decades, several representatives of antibacterial quinolones received approval for therapy. This review sets out to chronologically outline the group of approved antibacterial quinolones since 2000. Special attention is given to eight representatives: besifloxacin, delafoxacin, finafloxacin, lascufloxacin, nadifloxacin and levonadifloxacin, nemonoxacin, and zabofloxacin. These compounds have been characterized regarding physicochemical properties, formulations, antibacterial activity spectrum and advantageous structural characteristics related to antibacterial efficiency. At present these new compounds (with the exception of nadifloxacin) are reported differently, most often in the fourth generation and less frequently in a new generation (the fifth). Although these new compounds' mechanism does not contain essential new elements, the question of shaping a new generation (the fifth) arises, based on higher potency and broad spectrum of activity, including resistant bacterial strains. The functional groups that ensured the biological activity, good pharmacokinetic properties and a safety profile were highlighted. In addition, these new representatives have a low risk of determining bacterial resistance. Several positive aspects are added to the fourth fluoroquinolones generation, characteristics that can be the basis of the fifth generation. Antibacterial quinolones class continues to acquire new compounds with antibacterial potential, among other effects. Numerous derivatives, hybrids or conjugates are currently in various stages of research.

6.
Adv Pharm Bull ; 8(4): 529-534, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30607326

RESUMO

Through doping, we understand the use by athletes of substances prohibited by the antidoping agencies in order to gain a competitive advantage. Since sport plays an important role in physical and mental education and in promoting international understanding and cooperation, the widespread use of doping products and methods has consequences not only on health of the athletes, but also upon the image of sport. Thus, doping in sports is forbidden for both ethical and medical reasons. Narcotics and analgesics, anabolic steroids, hormones, selective androgen receptor modulators are among the most frequently utilized substances. Although antidoping controls are becoming more rigorous, doping and, very importantly, masking doping methods are also advancing, and these are usually one step ahead of doping detection techniques. Depending on the sport practiced and the physical attributes it requires, the athletes will look for one or more of the following benefits of doping: recovering from an injury, increasing body recovery capacity after training, increasing muscle mass and strength, decreasing fat tissue, increasing endurance. Finally, when we look once again at a doping scandal, amazed at how much animosity against those caught can exist; the question is: is it really such a disaster as presented by the media or a silent truth under our eyes, but which many of us have refused to accept?

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