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1.
Sensors (Basel) ; 23(20)2023 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-37896509

RESUMO

BACKGROUND: With an increasing number of systems for quantifying lameness-related movement asymmetry, between-system comparisons under non-laboratory conditions are important for multi-centre or referral-level studies. This study compares an artificial intelligence video app to a validated inertial measurement unit (IMU) gait analysis system in a specific group of horses. METHODS: Twenty-two reining Quarter horses were equipped with nine body-mounted IMUs while being videoed with a smartphone app. Both systems quantified head and pelvic movement symmetry during in-hand trot (hard/soft ground) and on the lunge (left/right rein, soft ground). Proportional limits of agreement (pLoA) were established. RESULTS: Widths of pLoA were larger for head movement (29% to 50% in-hand; 22% to 38% on lunge) than for pelvic movement (13% to 24% in-hand; 14% to 24% on lunge). CONCLUSION: The between-system pLoAs exceed current "lameness thresholds" aimed at identifying the affected limb(s) in lame horses. They also exceed published limits of agreement for stride-matched data but are similar to repeatability values and "lameness thresholds" from "non-lame" horses. This is encouraging for multi-centre studies and referral-level veterinary practice. The narrower pLoA values for pelvic movement asymmetry are particularly encouraging, given the difficulty of grading hind limb lameness "by eye".


Assuntos
Inteligência Artificial , Coxeadura Animal , Cavalos , Animais , Coxeadura Animal/diagnóstico , Fenômenos Biomecânicos , Movimento , Marcha , Movimentos da Cabeça , Extremidade Superior , Membro Posterior
2.
Bioorg Med Chem ; 23(9): 2270-80, 2015 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-25800433

RESUMO

In the present study, the synthesis of a range of novel 24-amino-25,26,27-trinorlanost-8-ene derivatives including 24-piperadino-trinorlanost-8-enes, 24-piperazino-trinorlanost-8-enes, 24-morpholino-trinorlanost-8-enes, and 24-diethylamino-trinorlanost-8-enes is reported and their cytotoxic and apoptotic potential evaluated in U937 cell lines. Excellent IC50 results for piperidine and 1-(2-hydroxyethyl)piperazine derivatives have been observed (IC50 values of 1.9 µM and 2.7 µM in U937 cells, respectively).


Assuntos
Apoptose/efeitos dos fármacos , Lanosterol , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Lanosterol/análogos & derivados , Lanosterol/síntese química , Lanosterol/química , Lanosterol/farmacologia , Conformação Molecular , Relação Estrutura-Atividade , Células U937
3.
Life Sci ; 92(13): 775-82, 2013 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-23454444

RESUMO

AIMS: The potato glycoalkaloids, α-chaconine, α-solanine and solanidine, along with potato peel extracts were investigated for potential anti-inflammatory effects in vitro. Their potential to reduce two biomarkers of inflammation, cytokine and nitric oxide (NO) productions, were assessed in the stimulated Jurkat and macrophage models, respectively. MAIN METHODS: Cytokine and nitric oxide productions were stimulated in Jurkat and Raw 264.7 macrophages with Concanavalin A (Con A; 25 µg/ml) and lipopolysaccaride (LPS; 1 µg/ml), respectively. Selective concentrations of glycoalkaloids and potato peel extracts were added simultaneously with Con A or LPS for 24h to investigate their potential to reduce inflammatory activity. KEY FINDINGS: α-Chaconine and solanidine significantly reduced interleukin-2 (IL-2) and interleukin-8 (IL-8) productions in Con A-induced Jurkat cells. The potato peel extracts did not influence cytokine production. In LPS-stimulated Raw macrophages, α-solanine, solanidine and two potato peel extracts significantly reduced induced NO production. SIGNIFICANCE: Our findings suggest that sub-cytotoxic concentrations of potato glycoalkaloids and potato peel extracts possess anti-inflammatory effects in vitro and with further investigation may be useful in the prevention of anti-inflammatory diseases.


Assuntos
Anti-Inflamatórios/farmacologia , Diosgenina/farmacologia , Células Jurkat/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Solanina/análogos & derivados , Animais , Linhagem Celular , Concanavalina A/imunologia , Humanos , Interleucina-2/imunologia , Interleucina-8/imunologia , Células Jurkat/imunologia , Lipopolissacarídeos/imunologia , Macrófagos/imunologia , Camundongos , Óxido Nítrico/imunologia , Solanina/farmacologia , Solanum tuberosum/química
4.
Biochimie ; 95(3): 496-503, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22561884

RESUMO

The cytotoxic effects of the oxidised derivatives of the phytosterols, stigmasterol and ß-sitosterol, have previously been shown to be similar but less potent than those of the equivalent cholesterol oxides in the U937 cell line. The objective of the present study was to compare the cytotoxic effects of the oxidised derivatives of synthetic mixtures of campesterol and dihydrobrassicasterol in both the U937 and HepG2 cell lines. The parent compounds consisted of a campesterol: dihydrobrassicasterol mix at a ratio of 2:1 (2CMP:1DHB) and a dihydrobrassicasterol:campesterol mix at a ratio of 3:1 (3DHB:1CMP). The 2CMP:1DBH oxides were more cytotoxic in the U937 cells than the 3DBH:1CMP oxides but the difference in cytotoxicity was less marked in the HepG2 cells. The order of toxicity of the individual oxidation products was found to be similar to that previously observed for cholesterol, ß-sitosterol and stigmasterol oxidation products in the U937 cell line. There was an increase in apoptotic nuclei in U937 cells incubated with the 7-keto and 7ß-OH derivatives of both 2CMP:1DHB and 3DHB:1CMP and also in the presence of 3DHB:1CMP-3ß,5α,6ß-triol and 2CMP:1DHB-5ß,6ß-epoxide. An additional oxidation product synthesised from 2CMP:1DHB, 5,6,22,23-diepoxycampestane, was cytotoxic but did not induce apoptosis. These results signify the importance of campesterol oxides in the overall paradigm of phytosterol oxide cytotoxicity.


Assuntos
Colesterol/análogos & derivados , Citotoxinas/síntese química , Citotoxinas/toxicidade , Fitosteróis/síntese química , Fitosteróis/toxicidade , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Técnicas de Química Sintética , Colesterol/síntese química , Colesterol/química , Colesterol/toxicidade , Citotoxinas/química , Células Hep G2 , Humanos , Oxirredução , Fitosteróis/química , Células U937
5.
J Agric Food Chem ; 60(23): 5952-61, 2012 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-22594485

RESUMO

The ability of phytosterol compounds to reduce plasma serum cholesterol levels in humans is well investigated. However, phytosterols are structurally similar to cholesterol with a double bond at the C5-6 position and are therefore susceptible to oxidation. Much research has been carried out on the biological effects of cholesterol oxidation products (COPs) in vitro. In contrast, there is less known about phytosterol oxidation products (POPs). From previous studies, it is apparent that oxidized derivatives of the phytosterols, ß-sitosterol and stigmasterol, are cytotoxic in vitro but are less potent than their COP counterparts. In the present study, the cytotoxic and apoptotic potential of oxidized derivatives of dihydrobrassicasterol (DHB) including 5α,6α-epoxyergostan-3ß-ol (α-epoxide), 5ß,6ß-epoxyergostan-3ß-ol (ß-epoxide), ergost-5-en-7-on-3ß-ol (7-keto), ergost-5-ene-3ß,7ß-diol (7-ß-OH), and ergostane-3ß,5α,6ß-triol (triol) were evaluated in the U937 and HepG2 cell lines. In general, 7-keto, 7-ß-OH, and triol derivatives had a significant cytotoxic impact on U937 and HepG2 cells. The oxides appear to be more toxic toward U937 cells. In line with previous findings, the POPs investigated in this study were less potent than the equivalent COPs. The results add to the body of data on the toxicity of individual POPs.


Assuntos
Apoptose/efeitos dos fármacos , Fitosteróis/química , Sitosteroides/química , Estigmasterol/química , Caspase 3/genética , Caspase 3/metabolismo , Caspase 7/genética , Caspase 7/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Colesterol/química , Fragmentação do DNA/efeitos dos fármacos , Células Hep G2 , Humanos , Oxirredução/efeitos dos fármacos , Fitosteróis/farmacologia , Sitosteroides/farmacologia , Estigmasterol/farmacologia , Células U937
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