Novel indole and triazole based hybrid molecules exhibit potent anti-adipogenic and antidyslipidemic activity by activating Wnt3a/β-catenin pathway

Rajan, Sujith; Puri, Surendra K.; Kumar, Durgesh; Babu, Madala Hari; Shankar, Kripa; Varshney, Salil; Srivastava, Ankita; Gupta, Abhishek; Reddy, Maddi Sridhar; Gaikwad, Anil Nilkanth

doi:10.1016/j.ejmech.2017.10.034

Cited by 47 publications

(17 citation statements)

References 63 publications

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“…Upregulation of mir-509-5p inversely associated with β-catenin activation,31 β-catenin stimulation enhanced FFAs catabolism, whereas genetic knock out of β-catenin gene reduced oleate oxidation coupled with reduced osteoblast maturation and increased glycolytic metabolism. Diminishing of β-catenin expression in vivo led to an increase in white adipose tissue mass, dyslipidemia, and impaired insulin sensitivity 32,33. So, overexpression of mir-509-5p lead to dyslipidemia by reducing β-catenin expression.…”

Section: Discussionmentioning

confidence: 99%

<p>Potential role of circulating microRNAs (486-5p, 497, 509-5p and 605) in metabolic syndrome Egyptian male patients</p>

Zaki

Abulsoud

Elsisi

et al. 2019

DMSO

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Objective: This study aims to evaluate the expression pattern of circulating microRNAs (miR)-486-5p, miR-497, miR-509-5p, and miR-605 in the serum of metabolic syndrome (MetS) Egyptian male patients. Methods: In this study, the circulating miR-486-5p, miR-497, miR509-5p, and miR-605 were amplified and quantitatively detected by quantitative real-time polymerase chain reaction in sera of 55 MetS male patients in comparison to 20 male controls. The level of fasting plasma glucose and triacylglycerol (TAG) were measured using calorimetric assay. Blood pressure was measured using mercuric sphygmomanometer. Anthropometric measurements were done to each individual. Furthermore, MetS patients were defined according to the criteria proposed by the American Heart Association and divided into three groups according to MetS index. Results: The study was performed on three groups and a control group defined as follows: group 1: 15 MetS patients who fulfilled all diagnostic criteria of MetS; group 2: 20 MetS patients with normal blood pressure; group 3: 20 MetS patients with normal TAG levels.The levels of miRs are expressed as [median (IQR)]. miR-486-5-p and miR-497 expression were elevated in group 1 [31.9(49), p˂ 0.0001; 73.1(42.5), p˂ 0.0001], group 2 [36.4(15.7), p˂ 0.0001; 68.3(54.8), p˂ 0.0001], and group (3) [10.8(18.9), p= 0.0014; 27.5(39.7), p= 0.0012]. MiR-509-5p was elevated in groups 1 and 2 [501(468), p= 0.0001], [309(436), p= 0.0006], respectively, while normally expressed in group 3 [0.93(0.077), p= 0.0001]. miR-605 was elevated in groups 1 and 3 [25.4(20.0), p= 0.0018], [54.8(65.8), p˂ 0.0001], while normally expressed in group 2 [0.84(0.67), p˂ 0.0001]. Conclusion: miRs (486-5p, 497, 509-5p, and 605) serum levels were higher in MetS patients than in healthy control subjects; therefore, these serum miRs can serve as early biomarkers and can be used to follow-up the prognosis of MetS.

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Section: Discussionmentioning

confidence: 99%

<p>Potential role of circulating microRNAs (486-5p, 497, 509-5p and 605) in metabolic syndrome Egyptian male patients</p>

Zaki

Abulsoud

Elsisi

et al. 2019

DMSO

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“…The indole-triazole hybrids were synthesised using the click method and studied for anti-adipogenic properties. 152 In this study, a N-((1-(2,3-difluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)-4-methyl-N-((1tosyl-1H-indol-3-yl)methyl)benzenesulfonamide (125, Fig. 18) was identified as a promising anti-adipogenic agent with an IC 50 of 1.67 µM, which was more potent than that of its parent compound.…”

Section: 23-triazoles As Anti-adipogenic Agentsmentioning

confidence: 99%

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Bozorov

Zhao

Aisa

2019

Bioorganic & Medicinal Chemistry

582

289

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A B S T R A C TThe 1,2,3-triazole ring is a major pharmacophore system among nitrogen-containing heterocycles. These fivemembered heterocyclic motifs with three nitrogen heteroatoms can be prepared easily using 'click' chemistry with copper-or ruthenium-catalysed azide-alkyne cycloaddition reactions. Recently, the 'linker' property of 1,2,3-triazoles was demonstrated, and a novel class of 1,2,3-triazole-containing hybrids and conjugates was synthesised and evaluated as lead compounds for diverse biological targets. These lead compounds have been demonstrated as anticancer, antimicrobial, anti-tubercular, antiviral, antidiabetic, antimalarial, anti-leishmanial, and neuroprotective agents. The present review summarises advances in lead compounds of 1,2,3-triazolecontaining hybrids, conjugates, and their related heterocycles in medicinal chemistry published in 2018. This review will be useful to scientists in research fields of organic synthesis, medicinal chemistry, phytochemistry, and pharmacology. Chemistry: synthesis and properties of the 1,2,3-triazolesThe general synthetic route of 1,2,3-triazoles using click chemistry is described in Scheme 1A. The most popular route to 1,2,3-triazoles is Cu(I)-catalysed Huisgen 1,3-dipolar cycloaddition, which is the https://doi.

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“…[2] More complex polycyclic indole alkaloids, such as vincristine and vinblastine (antitumor agents), [3] have been widely investigated. [4] Triazole-bearing indoles (Figure 1) have also shown wide-ranging biological activities, such as compound A (anti-adipogenic and anti-dyslipidemic activity), [5] molecule B (selective inhibitors and inducers of bacterial biofilms), [6] compound C (antimicrobial activity), [7] and compound D (antifungal agent). [8] In addition, indole-fused oxazinone derivatives are present in a large number of bioactive compounds and some representative members of this family are also depicted in Figure 1.…”

Section: Introductionmentioning

confidence: 99%

Easy installation of 1,2,3-triazoles or iodo-1,2,3-triazoles onto indole-fused oxazinones via CuAAC-based MCR in the presence of 18-crown-6

Mayooufi

Carcenac

Thibonnet

2019

Synthetic Communications

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Novel indole and triazole based hybrid molecules exhibit potent anti-adipogenic and antidyslipidemic activity by activating Wnt3a/β-catenin pathway

Cited by 47 publications

References 63 publications

<p>Potential role of circulating microRNAs (486-5p, 497, 509-5p and 605) in metabolic syndrome Egyptian male patients</p>

<p>Potential role of circulating microRNAs (486-5p, 497, 509-5p and 605) in metabolic syndrome Egyptian male patients</p>

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Easy installation of 1,2,3-triazoles or iodo-1,2,3-triazoles onto indole-fused oxazinones via CuAAC-based MCR in the presence of 18-crown-6

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