Quercetin is a promising pancreatic lipase inhibitor in reducing fat absorption in vivo

Zhou, Jianfeng; Wang, Wenjun; Yin, Zhong‐Ping; Zheng, Guodong; Chen, Jiguang; Li, Jingen; Chen, Lingli; Zhang, Qingfeng

doi:10.1016/j.fbio.2021.101248

Cited by 36 publications

(40 citation statements)

References 35 publications

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“…Our result showed that the phyto‐compounds of the extracts either directly bind with the free enzyme or with the enzyme‐substrate complex indicating a non‐competitive mode of inhibition. Similar results were also reported recently for the citrus peel extract and phytocompounds of quercetin, isoquercetin, and rutin (Zhou et al, 2021). The plant extracts containing an array of bioactive compounds bind the sites outside the active sites and thereby alter the kinetic parameters potentially through synergistic mechanisms.…”

Section: Discussionsupporting

confidence: 91%

Comparative evaluation of Brassica oleracea , Ocimum basilicum , and Moringa oleifera leaf extracts on lipase inhibition and adipogenesis in 3T3‐L1 adipocytes

Nallamuthu

Jain

Anand

2022

Journal of Food Biochemistry

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The anti-adipogenic effects of alcohol extract of Brassica oleracea (BO), Ocimum basilicum (OB), and Moringa oleifera (MO) leaves on 3T3-L1 pre-adipocyte as well as their lipase inhibitory properties were comparatively evaluated. The polyphenol-rich extracts of MO, BO, and OB leaves were profiled for major bioactive compounds using UPLC-HRMS/MS analysis. Among the three plant extracts, BO had the highest flavonoid content with stronger radical scavenging activity. All extracts exhibited lipase inhibitory activities, dose-dependently and a non-competitive type of inhibition with altered kinetic parameters was observed. In cell culture studies, these plant extracts remarkably inhibited the intracellular triglyceride accumulation in 3T3-L1 cells and the effect was in the decreasing order of BO > OB > MO. The extracts also downregulated the key transcription factors of adipogenesis (PPARγ, C/EPBα, PI3k, p-Akt, and FAS enzyme) as well as modulated the release profile of leptin and adiponectins.Overall, BO extract showed an exceptional inhibitory potential against both adipogenesis and lipase activities among the evaluated plants. Practical applicationsThe present study highlights the anti-adipogenic potential of three local edible plants and herbs, that is, Brassica oleracea (BO), Ocimum basilicum (OB), and Moringa oleifera (MO) leaves, using in vitro models. The results revealed that the BO extract had remarkable activity against adipogenesis in the 3T3-L1 pre-adipocyte differentiation model as well as lipase inhibitory properties. This study elucidates the prospects of natural plant-derived compounds in managing obesity-related health issues. The outcomes of this study would be useful in developing alternative or complementary therapies that are being preferred and largely sought over pharmacological treatments and procedures for controlling and treating abnormal weight gain in humans.

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Section: Discussionsupporting

confidence: 91%

Comparative evaluation of Brassica oleracea , Ocimum basilicum , and Moringa oleifera leaf extracts on lipase inhibition and adipogenesis in 3T3‐L1 adipocytes

Nallamuthu

Jain

Anand

2022

Journal of Food Biochemistry

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“…Only one previous report on lipase-inhibitory activity of C. arborea was available, albeit in the Korean language [ 32 ]. High lipase inhibition in C. arborea might be due to the biological function of kaempferol and quercetin since both were previously reported to be effective lipase inhibitors with IC 50 values of approximately 0.23 mM [ 13 , 33 ]. The former acted as a competitive inhibitor, while the latter was a mixed type, close to a noncompetitive inhibitor [ 13 , 33 ].…”

Section: Discussionmentioning

confidence: 99%

“…High lipase inhibition in C. arborea might be due to the biological function of kaempferol and quercetin since both were previously reported to be effective lipase inhibitors with IC 50 values of approximately 0.23 mM [ 13 , 33 ]. The former acted as a competitive inhibitor, while the latter was a mixed type, close to a noncompetitive inhibitor [ 13 , 33 ]. In addition to its potential to reduce fat absorption, our results indicated that C. arborea is involved in controlling the degradation of cholinergic neurotransmitters through inhibitions of AChE and BChE.…”

Section: Discussionmentioning

confidence: 99%

Impact of Drying Processes on Phenolics and In Vitro Health-Related Activities of Indigenous Plants in Thailand

Sirichai

Kittibunchakul

Thangsiri

et al. 2022

Plants

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Thailand has vast areas of tropical forests with many indigenous plants, but limited information is available on their phytochemical profile and in vitro inhibitions of enzymatic and nonenzymatic reactions. This study investigated phenolic profiles using liquid chromatography–electrospray ionization tandem mass spectrometry (LC–ESI-MS/MS), antioxidant activities, and in vitro inhibitory activities of 10 indigenous plants on key enzymes related to obesity (lipase), diabetes (α-amylase and α-glucosidase), and Alzheimer’s disease (cholinesterases and β-secretase). The nonenzymatic anti-glycation reaction was also investigated. The 10 indigenous plants were Albizia lebbeck (L.) Benth, Alpinia malaccensis (Burm.) Roscoe, Careya arborea Roxb., Diplazium esculentum (Retz.) Swartz, Kaempferia roscoeana Wall., Millettia brandisiana Kurz., Momordica charantia, Phyllanthus emblica L., Zingiber cassumunar Roxb, and Zingiber citriodorum J. Mood & T. Theleide. Preparations were made by either freeze-drying or oven-drying processes. Results suggested that the drying processes had a minor impact on in vitro inhibitions of enzymatic and nonenzymatic reactions (<4-fold difference). P. emblica was the most potent antioxidant provider with high anti-glycation activity (>80% inhibition using the extract concentration of ≤6 mg/mL), while D. esculentum effectively inhibited β-secretase activity (>80% inhibition using the extract concentration of 10 mg/mL). C. arborea exhibited the highest inhibitory activities against lipase (47–51% inhibition using the extract concentration of 1 mg/mL) and cholinesterases (>60% inhibition using the extract concentration of 2 mg/mL), while Mi. brandisiana dominantly provided α-amylase and α-glucosidase inhibitors (>80% inhibition using the extract concentration of ≤2 mg/mL). Information obtained from this research may support usage of the oven-drying method due to its lower cost and easier preparation step for these studied plant species and plant parts. Furthermore, the information on in vitro inhibitions of enzymatic and nonenzymatic reactions could be used as fundamental knowledge for further investigations into other biological activities such as cell culture or in vivo experiments of these health-beneficial plants.

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“…l ‐Carnitine, procyanidins B2, l ‐arginine and N ‐acetyl‐cysteine ameliorated T‐2 toxin‐induced cytotoxicity by regulating oxidative stress 13‐16 . Quercetin, tea polyphenols, and rutin are the most widely used plant‐derived active ingredients that possess antioxidant, anti‐inflammatory, and anti‐tumor properties 17‐20 . The protective mechanisms of these three antioxidants against T‐2 toxin are mainly related to cell stress.…”

Section: Introductionmentioning

confidence: 99%

“…[13][14][15][16] Quercetin, tea polyphenols, and rutin are the most widely used plant-derived active ingredients that possess antioxidant, anti-inflammatory, and anti-tumor properties. [17][18][19][20] The protective mechanisms of these three antioxidants against T-2 toxin are mainly related to cell stress. For example, quercetin protects porcine ovarian granulosa cells against T-2 toxin by improving the response to cellular stress.…”

Section: Introductionmentioning

confidence: 99%

Protective mechanisms of three antioxidants against T‐2 toxin‐induced muscle protein deterioration in shrimp

Huang

Sun

et al. 2022

J Sci Food Agric

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BACKGROUND: Quercetin (Q), tea polyphenols (TP), and rutin (R) are widely used plant-derived active ingredients. They possess antioxidant, anti-inflammatory, and anti-tumor properties, and can reduce the muscle damage caused by mycotoxins. However, few studies have examined the protective mechanisms of quercetin, tea polyphenols, and rutin on muscle quality. To elucidate their protective mechanisms, shrimp were exposed to both T-2 toxin and these three antioxidants for 20 days in a doseescalating trial. The changes in the protein composition of shrimp muscle were measured. The target proteins associated with T-2 and antioxidants were screened and identified by non-labeled quantitative proteomics. RESULTS:The T-2 toxin induced abnormal expression of 21 target proteins, leading to the deterioration of muscle proteins in shrimp. The three antioxidants ameliorated the T-2 toxin-induced damage to muscle proteins by increasing the sarcoplasmic and myofibrillar protein content and decreasing the alkali-soluble protein content. Quercetin had the strongest protective effect. The protective processes of these antioxidants involved the upregulation of target proteins involved in carbohydrate metabolism (enolase, malate dehydrogenase), protein translation (elongation factor 1-alpha and eukaryotic translation initiation factor 2 subunit alpha), and cytoskeleton component (actin 2, fast-type skeletal muscle actin 1). Quercetin regulated the largest number of target proteins, making it the best protective agent against T-2 toxin. CONCLUSION:The T-2 toxin (4.80-24.30 mg/kg feed) induced changes in target proteins and muscle composition of shrimp, leading to a deterioration in muscle proteins. Quercetin (2.00-32.00 g/kg feed) had significant protective effects against this deterioration in muscle protein in shrimp.

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Quercetin is a promising pancreatic lipase inhibitor in reducing fat absorption in vivo

Cited by 36 publications

References 35 publications

Comparative evaluation of Brassica oleracea , Ocimum basilicum , and Moringa oleifera leaf extracts on lipase inhibition and adipogenesis in 3T3‐L1 adipocytes

Comparative evaluation of Brassica oleracea , Ocimum basilicum , and Moringa oleifera leaf extracts on lipase inhibition and adipogenesis in 3T3‐L1 adipocytes

Impact of Drying Processes on Phenolics and In Vitro Health-Related Activities of Indigenous Plants in Thailand

Protective mechanisms of three antioxidants against T‐2 toxin‐induced muscle protein deterioration in shrimp

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