Ruthenium complexes as inhibitors of human islet amyloid polypeptide aggregation, an effect that prevents beta cell apoptosis

Ma, Lijuan; Fu, Yuanting; Yu, Liu; Li, Xiaoling; Zheng, Wenjie; Chen, Tianfeng

doi:10.1039/c4ra15152f

Cited by 20 publications

(16 citation statements)

References 51 publications

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“…Although several Aβ aggregation inhibitors have been reported, still, the interaction between Aβ and its inhibitors is unclear. The phenolic groups present in the novel compounds such as curcumin can interact with the aromatic residues in amyloid fibrils unsettling peptide π–π piling whereas the hydroxyl groups can play the role of β‐sheet breakers through competitive hydrogen bonding .…”

Section: Resultsmentioning

confidence: 99%

Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease

et al. 2016

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Neurodegeneration, a complex disease state, comprises several pathways that contribute to cell death. Conventional approach of targeting only one of these pathways has not been proven to be entirely successful and has demanded a hypothetical change as to how researchers design and develop new drugs. In this study, effects of a series of α, β-unsaturated carbonyl-based tetralone derivatives against Alzheimer's disease (AD) were investigated. Moreover, their activity toward amyloid β-induced cytotoxicity was also studied. Six compounds including 3f, 3o, 3u, 3ae, 3af, and 3ag were discovered to be most protective against Aβ-induced neuronal cell death in PC12 cells. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against MAO-B, AChE, and self-induced Aβ aggregation. The compound 3f exhibited best AChE (IC = 0.045 ± 0.02 μm) inhibitory potential in addition to potent inhibition of MAO-B (IC = 0.88 ± 0.12 μm). Furthermore, compound 3f disassembled the Aβ fibrils produced by self-induced Aβ aggregation by 78.2 ± 4.8%. Collectively, these findings suggest that some compounds from this series have potential to be promising multifunctional agents for AD treatment.

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Section: Resultsmentioning

confidence: 99%

Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease

et al. 2016

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“…These data demonstrate the difference between the smooth brils and granular aggregates, and the results were similar to previous study. 41 More importantly, the heights of granular aggregates became lower with time, revealing disaggregation.…”

Section: Morphological Analysismentioning

confidence: 99%

Binuclear ruthenium complexes inhibit the fibril formation of human islet amyloid polypeptide

Gong

2017

RSC Adv.

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“…Lijuan et al . explored Ru complexes, [Ru(bpy) 3 ](ClO 4 ) 2 (bpy=2,2′‐dipyridyl), [Ru(pip) 3 ](ClO 4 ) 2 (pip=2‐phenylimidazo[4, 5‐ f ][1, 10]phenanthroline) and [Ru(phtpy)(phen)Cl]ClO 4 (phtpy=2,6‐bis(2‐pyridyl)‐4‐phenylpyridine, phen=1,10‐phenanthroline) as inhibitors of human islet amyloid polypeptide (hIAPP) aggregation and associated cytotoxicity …”

Section: Introductionmentioning

confidence: 99%

Ru(II)‐p‐cymene Thiosemicarbazone Complexes as Inhibitors of Amyloid β (Aβ) Peptide Aggregation and Aβ‐Induced Cytotoxicity

Haribabu

Ranade

Bhuvanesh³

et al. 2017

ChemistrySelect

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The reaction of [RuCl2(η6‐p‐cymene)]2 with indole based thiosemicarbazone ligands (L1‐L3) yielded monometallic ruthenium(II) complexes, [RuCl(η6‐p‐cymene)(L)]Cl (1–3). The complexes were characterized by analytical and various spectroscopic (UV‐visible, FT‐IR, 1H & 13C NMR and mass) tools. The solid state structure of complex 2 determined by single crystal X‐ray diffraction analysis showed a piano stool geometry around the metal. The Ru(II)‐p‐cymene complexes with N‐substituted thiosemicarbazone were evaluated for their potential to inhibit aggregation of Aβ peptide and associated cytotoxicity. Results of turbidity assay revealed that complexes 1 and 2 exhibited 70 and 60% inhibition of Aβ peptide aggregation respectively. All the tested compounds were nontoxic to neuronal cells. Interestingly complexes 1 and 2 showed attenuation of Aβ induced cytotoxicity due to flexible alkyl substitution at terminal nitrogen of thiosemicarbazone moiety.

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Ruthenium complexes as inhibitors of human islet amyloid polypeptide aggregation, an effect that prevents beta cell apoptosis

Abstract: Herein we show that ruthenium complexes could inhibit fibrosis of hIAPP and protect the hIAPP-induced cell damage by suppressing ROS generation, indicating the application potential of the complexes in treatment of T2DM by targeting hIAPP.

Cited by 20 publications

References 51 publications

Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease

Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease

Binuclear ruthenium complexes inhibit the fibril formation of human islet amyloid polypeptide

Ru(II)‐p‐cymene Thiosemicarbazone Complexes as Inhibitors of Amyloid β (Aβ) Peptide Aggregation and Aβ‐Induced Cytotoxicity

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