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1.
Int Immunopharmacol ; 100: 108113, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34530203

RESUMO

Postmenopausal osteoporosis is a chronic population health hazard systemic metabolic disease caused by excessive bone resorption and reduced bone formation. The activity between osteoblast and osteoclast, with their mutual effects, influence the procedure of normal bone remodeling. Over-activated osteoclast differentiation and function play a crucial role in excessive bone resorption. Hence, therapy strategies targeting osteoclast activity may promote the bone mass preservation and delay the osteoporosis process. Natural compound (anethole) is emerging as potential therapeutics for various metabolic diseases. The purpose of this study is to investigate the potential effects of anethole on RANKL-induced osteoclast formation and function in vitro and in vivo. Here, in vitro TRAP staining assay was performed to investigate the inhibitory effect of anethole on osteoclast differentiation. Bone pits resorption assay revealed that osteoclast-mediated bone resorption was inhibited by anethole. At mRNA and protein levels, anethole significantly reduced the expression of osteoclast-specific genes expression in a concentration- or time-dependent manner, including NFATc1, MMP-9, DC-STAMP, c-F, TRAP, CTR, Cathepsin K, and V-ATPase d2. Furthermore, intracellular signaling transduction assay indicated that anethole inhibited osteoclast formation via blocking ERK and AKT signaling. GSK3ß, the downstream signal of AKT, is simultaneously suppressed with anethole treatment. Based on ovariectomized (OVX) mice model, micro-CT and histological staining results suggested that anethole prevented estrogen deficiency-induced bone mass loss and increased osteoclast activity in vivo. In conclusion, our results show significant indications that anethole exhibits an osteoprotective effect and may be potential for the treatment of osteoporosis.


Assuntos
Derivados de Alilbenzenos/farmacologia , Anisóis/farmacologia , Reabsorção Óssea/metabolismo , Osteogênese/efeitos dos fármacos , Osteoporose/metabolismo , Receptor Ativador de Fator Nuclear kappa-B/metabolismo , Animais , Densidade Óssea/efeitos dos fármacos , Reabsorção Óssea/tratamento farmacológico , Diferenciação Celular/efeitos dos fármacos , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Feminino , Glicogênio Sintase Quinase 3 beta/metabolismo , Humanos , Camundongos , Camundongos Endogâmicos C57BL , NF-kappa B/metabolismo , Osteoblastos/metabolismo , Osteoporose/etiologia , Ovariectomia/efeitos adversos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos
2.
Org Biomol Chem ; 19(5): 988-992, 2021 02 07.
Artigo em Inglês | MEDLINE | ID: mdl-33459332

RESUMO

A copper-catalyzed one-pot amine-alkylation of quinones with amines and alkanes in the presence of di-tert-butyl peroxide (DTBP) was developed via a radical reaction process. Various alkanes and aromatic or aliphatic amines with diverse structures and electronic properties are suitable substrates, and the chirality of amines can be maintained for the transformation. This method has high step and atom economy for straightforward access to aminated and alkylated quinones from readily available starting materials.

3.
J Hazard Mater ; 392: 122322, 2020 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-32097856

RESUMO

Flotation is an effective and clean separation technology to realize the recovery of metal in waste printed circuit boards (WPCBs). The flotation kinetic of metal and non-metal components was concerned in this study. In addition, the loading of bubbles, the collision and shedding of particles and bubbles were used to assist in proving the particle dynamics results. By analyzing the force on the particles, the load of bubbles on particles was analyzed, and the appropriate volume ratio of bubbles to particles was 1.5-8.0, depending on the particle density. Moreover, Clift model and Schiller-Naumann model has high fitting accuracy for the final bubble velocity. In addition, metal particles have greater settling velocity, which results in shorter collision time with bubbles. In the process of bubble-particle rising, the shedding probability gradually decreases, and the shedding probability of metal particles is much higher than that of non-metal particles. The results of flotation kinetics show that the removal of impurity particles represented by silicon mainly occurs in the initial stage of flotation process. The loss of copper increases with flotation time and collector dosage. This study reveals the flotation kinetics of particles from the perspectives of bubble loading, bubble-particle collision and shedding.

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