In vitro targeted screening and molecular docking of stilbene, quinones, and flavonoid on 3T3-L1 pre-adipocytes for anti-adipogenic actions

Bedi, Onkar; Aggarwal, Savera; Trehanpati, Nirupma; Ramakrishna, Gayatri; Grewal, Ajmer Singh; Krishan, Pawan

doi:10.1007/s00210-020-01919-w

Cited by 12 publications

(8 citation statements)

References 35 publications

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“…Further, molecular docking studies were performed to investigate interactions of the pharmacological agents' arbutin (ARB), purpurin (PUR), quercetin (QR), and pterostilbene (PTS) with the beta-ketoacyl reductase (KR) and thioesterase (TE) domains of fatty acid synthase (FAS) enzyme. All compounds displayed significant binding interactions with KR and TE domains of the FAS enzyme, supporting in vitro studies that significantly decreased the adipocyte differentiation and stimulatory effect on fatty acid uptake in 3T3-L1 adipocytes [71].…”

Section: In Silico Methods May Provide the Basis For Elucidating The ...supporting

confidence: 70%

Alternative Methods as Tools for Obesity Research: In Vitro and In Silico Approaches

Pamplona

Zoehler²,

Shigunov³

et al. 2022

Life

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The study of adipogenesis is essential for understanding and treating obesity, a multifactorial problem related to body fat accumulation that leads to several life-threatening diseases, becoming one of the most critical public health problems worldwide. In this review, we propose to provide the highlights of the adipogenesis study based on in vitro differentiation of human mesenchymal stem cells (hMSCs). We list in silico methods, such as molecular docking for identification of molecular targets, and in vitro approaches, from 2D, more straightforward and applied for screening large libraries of substances, to more representative physiological models, such as 3D and bioprinting models. We also describe the development of physiological models based on microfluidic systems applied to investigate adipogenesis in vitro. We intend to identify the main alternative models for adipogenesis evaluation, contributing to the direction of preclinical research in obesity. Future directions indicate the association of in silico and in vitro techniques to bring a clear picture of alternative methods based on adipogenesis as a tool for obesity research.

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Section: In Silico Methods May Provide the Basis For Elucidating The ...supporting

confidence: 70%

Alternative Methods as Tools for Obesity Research: In Vitro and In Silico Approaches

Pamplona

Zoehler²,

Shigunov³

et al. 2022

Life

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show abstract

“…We found that low concentrations of arbutin reduced serum lipids, whereas reversed at high concentrations. Previous studies have shown that arbutin significantly reduced adipocyte differentiation and promoted fatty acid uptake in 3T3-L1 adipocytes (35). The polyjuice decoction containing arbutin decreased the total cholesterol, triglyceride, VLDL, and LDL in diabetic rats (36).…”

Section: Discussionmentioning

confidence: 85%

Arbutin improves gut development and serum lipids via Lactobacillus intestinalis

Chen

et al. 2022

Front. Nutr.

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Arbutin has been widely studied in whitening, anti-inflammatory, and antioxidant. However, the interaction between arbutin and intestinal microbes has been rarely studied. Thus, mice were treated with arbutin concentrations of 0, 0.1, 0.2, 0.4, and 1 mg/ml. We found that arbutin promoted gut development such as villus length, villus areas, and villus length/crypt depth (L/D). Total cholesterol (TC), high-density lipoprotein (HDL), and low-density lipoprotein (LDL) were significantly reduced by low concentrations of arbutin. Importantly, we analyzed the microbial composition in the control and 0.4 mg/ml arbutin group and found that the abundance of Lactobacillus intestinalis (L. intestinalis) was highest and enhanced in arbutin. Further, mice were fed with oral antibiotics and antibiotics + 0.4 mg/ml arbutin and then we transplanted fecal microbes from oral 0.4 mg/ml arbutin mice to mice pretreated with antibiotics. Our results showed that arbutin improves gut development, such as villus width, villus length, L/D, and villus areas. In addition, L. intestinalis monocolonization was carried out after a week of oral antibiotics and increased villus length, crypt depth, and villus areas. Finally, in vitro arbutin and L. intestinalis co-culture showed that arbutin promoted the growth and proliferation of L. intestinalis. Taken together, our results suggest that arbutin improves gut development and health of L. intestinalis. Future studies are needed to explore the function and mechanism of L. intestinalis affecting gut development.

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“…Quercetin significantly inhibited the level of tumor suppressor (Schwingel et al, 2014). Quercetin-induced apoptosis can also be induced by inhibition of FASN in HepG2 cells (Bedi et al, 2020), but the exact mechanism is unclear and remains to be further investigated in depth afterward.…”

Section: Apoptosis-related Factorsmentioning

confidence: 98%

“…On oxaliplatin‐induced hepatotoxicity in mice, quercetin nanoemulsion mainly reduced the immunopositivity of apoptosis marker caspase‐3 and decreasing neutrophil migration as measured by peroxidase (MPO) activity (Schwingel et al, 2014). Quercetin‐induced apoptosis can also be induced by inhibition of FASN in HepG2 cells (Bedi et al, 2020), but the exact mechanism is unclear and remains to be further investigated in depth afterward.…”

Section: Antiliver Steatosis Property Of Quercetinmentioning

confidence: 99%

Quercetin as a protective agent for liver diseases: A comprehensive descriptive review of the molecular mechanism

Zhao

Wang

Deng

et al. 2021

Phytotherapy Research

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Quercetin is the major representative of the flavonoid subgroup of flavones, with good pharmacological activities for the treatment of liver diseases, including liver steatosis, fatty hepatitis, liver fibrosis, and liver cancer. It can significantly influence the development of liver diseases via multiple targets and multiple pathways via antifat accumulation, anti‐inflammatory, and antioxidant activity, as well as the inhibition of cellular apoptosis and proliferation. Despite extensive research on understanding the mechanism of quercetin in the treatment of liver diseases, there are still no targeted therapies available. Thus, we have comprehensively searched and summarized the different targets of quercetin in different stages of liver diseases and concluded that quercetin inhibited inflammation of the liver mainly through NF‐κB/TLR/NLRP3, reduced PI3K/Nrf2‐mediated oxidative stress, mTOR activation in autophagy, and inhibited the expression of apoptotic factors associated with the development of liver diseases. In addition, quercetin showed different mechanisms of action at different stages of liver diseases, including the regulation of PPAR, UCP, and PLIN2‐related factors via brown fat activation in liver steatosis. The compound inhibited stromal ECM deposition at the liver fibrosis stage, affecting TGF1β, endoplasmic reticulum stress (ERs), and apoptosis. While at the final liver cancer stage, inhibiting cancer cell proliferation and spread via the hTERT, MEK1/ERK1/2, Notch, and Wnt/β‐catenin‐related signaling pathways. In conclusion, quercetin is an effective liver protectant. We hope to explore the pathogenesis of quercetin in different stages of liver diseases through the review, so as to provide more accurate targets and theoretical basis for further research of quercetin in the treatment of liver diseases.

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In vitro targeted screening and molecular docking of stilbene, quinones, and flavonoid on 3T3-L1 pre-adipocytes for anti-adipogenic actions

Cited by 12 publications

References 35 publications

Alternative Methods as Tools for Obesity Research: In Vitro and In Silico Approaches

Alternative Methods as Tools for Obesity Research: In Vitro and In Silico Approaches

Arbutin improves gut development and serum lipids via Lactobacillus intestinalis

Quercetin as a protective agent for liver diseases: A comprehensive descriptive review of the molecular mechanism

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