Assessment of selegiline and trilostane combined therapy efficacy for canine pituitary-dependent hypercortisolism treatment: A pilot randomized clinical trial

Carvalho, Guilherme Luiz Carvalho de; Meirelles, Luana; Silva, Carolina Castilhos da; Neto, Waldemir Santiago; Furtado, Priscila Viau; Machado, Letícia Rocha; Martins, Francisco Sávio de Moura; Mello, Fabíola Peixoto da Silva; Valle, Stella de Faria; Pöppl, Álan Gomes

doi:10.1016/j.rvsc.2022.06.020

Cited by 2 publications

(1 citation statement)

References 49 publications

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“…Due to different efficacy, it was withdrawn for human use in the United States in the 1990s. However, it was approved for treating Cushing’s syndrome in pets such as dogs and cats 11 , 12 . The identified potent h 3β-HSD2 and r 3β-HSD1 inhibitors of curcumin analogues such as DMC and BDMC may be potential food additives for therapeutic purposes and further preclinical studies are needed.…”

Section: Discussionmentioning

confidence: 99%

Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking

Qiao

et al. 2023

Journal of Enzyme Inhibition and Medicinal Chemistry

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Curcuminoids are functional food additives, and the effect on gonadal hormone biosynthesis remains unclear. Gonads contain 3β-hydroxysteroid dehydrogenase isoforms, h 3β-HSD2 (humans) and r3β-HSD1 (rats), which catalyse pregnenolone into progesterone. The potency and mechanisms of curcuminoids to inhibit 3β-HSD activity were explored. The inhibitory potency was bisdemethoxycurcumin (IC 50 , 1.68 µM) >demethoxycurcumin (3.27 µM) > curcumin (13.87 µM) > tetrahydrocurcumin (109.0 µM) > dihydrocurcumin and octahydrocurcumin on KGN cell h 3β-HSD2, while that was bisdemethoxycurcumin (1.22 µM) >demethoxycurcumin (2.18 µM) > curcumin (4.12 µM) > tetrahydrocurcumin (102.61 µM) > dihydrocurcumin and octahydrocurcumin on testicular r 3β-HSD1. All curcuminoids inhibited progesterone secretion by KGN cells under basal and forskolin-stimulated conditions at >10 µM. Docking analysis showed that curcuminoids bind steroid-active site with mixed or competitive mode. In conclusion, curcuminoids inhibit gonadal 3β-HSD activity and de-methoxylation of curcumin increases inhibitory potency and metabolism of curcumin by saturation of carbon chain losses inhibitory potency.

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Section: Discussionmentioning

confidence: 99%

Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking

Qiao

et al. 2023

Journal of Enzyme Inhibition and Medicinal Chemistry

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Structure-activity relationship and docking analysis of nature flavonoids as inhibitors of human and rat gonadal 3β-hydroxysteroid dehydrogenases for therapeutic purposes

Ren,

Yu,

et al. 2024

The Journal of Steroid Biochemistry and Molecular Biology

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Assessment of selegiline and trilostane combined therapy efficacy for canine pituitary-dependent hypercortisolism treatment: A pilot randomized clinical trial

Cited by 2 publications

References 49 publications

Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking

Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking

Structure-activity relationship and docking analysis of nature flavonoids as inhibitors of human and rat gonadal 3β-hydroxysteroid dehydrogenases for therapeutic purposes

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