Lipase Inhibitors for Obesity: A Review

Liu, Tiantian; Liu, Xiaotian; Chen, Qing‐Xi; Shi, Yan

doi:10.1016/j.biopha.2020.110314

Cited by 244 publications

(193 citation statements)

References 82 publications

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“…Lipases present in the digestive system are important in the hydrolysis of glycerides into free fatty acids and glycerol. The most important of these lipases is the pancreatic lipase (PL) which plays an important role in converting the triglycerides found in ingested oils into monoglycerides and free fatty acids [ 52 ]. Hence the inhibition of this enzyme reduces fat absorption and hence represents an excellent strategy to prevent and treat obesity.…”

Section: Antioxidant Activities Of Rhus Coriariamentioning

confidence: 99%

Pharmacological and Antioxidant Activities of Rhus coriaria L. (Sumac)

et al. 2021

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Rhus coriaria L. (Anacardiaceae), commonly known as sumac, is a commonly used spice, condiment, and flavoring agent, especially in the Mediterranean region. Owing to its bountiful beneficial values, sumac has been used in traditional medicine for the management and treatment of many ailments including hemorrhoids, wound healing, diarrhea, ulcer, and eye inflammation. This plant is rich in various classes of phytochemicals including flavonoids, tannins, polyphenolic compounds, organic acids, and many others. By virtue of its bioactive, Rhus coriaria possesses powerful antioxidant capacities that have ameliorative and therapeutic benefits for many common diseases including cardiovascular disease, diabetes, and cancer. This review describes the phytochemical properties of R. coriaria and then focuses on the potent antioxidant capacities of sumac. We then dissect the cellular and molecular mechanisms of sumac’s action in modulating many pathophysiological instigators. We show how accumulating evidence supports the antibacterial, antinociceptive, antidiabetic, cardioprotective, neuroprotective, and anticancer effects of this plant, especially that toxicity studies show that sumac is very safe to consume by humans and has little toxicity. Taken together, the findings we summarize here support the utilization of this plant as an attractive target for drug discovery.

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Section: Antioxidant Activities Of Rhus Coriariamentioning

confidence: 99%

Pharmacological and Antioxidant Activities of Rhus coriaria L. (Sumac)

et al. 2021

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“…Abdominal obesity and increased free fatty acids lead to inflammation and oxidative stress that provoke insulin resistance and β-cells dysfunction [ 48 ]. To avoid ectopic fat accumulation and, therefore, prevent obesity, the treatment should stimulate lipolysis and inhibit the absorption of food triglycerides [ 49 , 50 ]. Hispidin in vitro inactivates pancreatic lipase — an important anti-inflammatory target ( Figure 3 ) that decreases triglyceride absorption in the small intestine.…”

Section: The Effect Of Hispidin On the Metabolic Syndromementioning

confidence: 99%

“… Hispidin as a potential anti-obesity compound (marked green) in the context of metabolic syndrome developing. Adapted from [ 50 , 53 ]. MG—Monoacylglycerol; FA—Fatty acids; ER stress—Endoplasmic reticulum stress.…”

Section: Figurementioning

confidence: 99%

Therapeutic Potential of Hispidin—Fungal and Plant Polyketide

Palkina

Ipatova

Shakhova

et al. 2021

JoF

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There is a large number of bioactive polyketides well-known for their anticancer, antibiotic, cholesterol-lowering, and other therapeutic functions, and hispidin is among them. It is a highly abundant secondary plant and fungal metabolite, which is investigated in research devoted to cancer, metabolic syndrome, cardiovascular, neurodegenerative, and viral diseases. This review summarizes over 20 years of hispidin studies of its antioxidant, anti-inflammatory, anti-apoptotic, antiviral, and anti-cancer cell activity.

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“…Research on lipase inhibition by plant-based products has widely done and some of the research shows obvious inhibitory effects [13]. Yet, due to the low content of active ingredients, complicated in extraction procedures and low recovery rate, which make it cannot be produced in large quantities.…”

Section: Introductionmentioning

confidence: 99%

“…This is a major drawback in commercialization of lipase inhibitors derived from edible plants. One of the suggestion is to study the action mechanism of natural compounds on pancreatic lipase, while the high-activity pancreatic lipase inhibitors are still continuously screened [13]. Thus, this research also emphasis on the reaction mechanism in inhibition of pancreatic lipase by A. malaccensis and A. subintegra leaves crude extract, wherein the activity of pancreatic lipase inhibitor was determined throughout the reaction.…”

Section: Introductionmentioning

confidence: 99%

Kinetic Behaviour of Pancreatic Lipase Inhibition by Ultrasonicated A. malaccensis and A. subintegra Leaves of Different Particle Sizes

Rodhi

Hamzah

Hamid

2020

Bull. Chem. React. Eng. Catal.

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Gallic acid and quercetin equivalent were determined in the crude extract of matured leaves Aquilaria malaccensis and Aquilaria subintegra. The leaves of both Aquilaria species were dried at 60 °C for 24 hours, ground and sieved into particle size of 250, 300, 400, 500, and 1000 µm. Then, each particle size of leaves was soaked in distilled water with a ratio of 1:100 (w/v) for 24 hours and undergoes the pre-treatment method by using ultrasonicator (37 kHz), at the temperature of 60 °C for 30 minutes. The crude extracts were obtained after about 4 hours of hydrodistillation process. The highest concentration of gallic acid and quercetin equivalent was determined in the crude extract from the particle size of 250 µm. The kinetics of pancreatic lipase inhibition was further studied based using the Lineweaver-Burk plot, wherein the concentration of p-NPP as the substrate and pancreatic lipase were varied. Based on the formation of the lines in the plot, the crude leaves extract of both Aquilaria species exhibit the mixed-inhibition on pancreatic lipase, which indicates that in the reaction, the inhibitors were not only attached to the free pancreatic lipase, but also to the pancreatic lipase-(p-NPP) complex. The reaction mechanism was similar to non-competitive inhibition; however the value of dissociation constant, Ki, for both inhibition pathways was different. The inhibition shows an increment in Michaelis-Menten constant (Km) and a reduction in the maximum pancreatic lipase activity (Vm) compared to the reaction without Aquilaria spp. crude extracts (control). This proved that the inhibition occurred in this reaction. Copyright © 2020 BCREC Group. All rights reserved

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Lipase Inhibitors for Obesity: A Review

Cited by 244 publications

References 82 publications

Pharmacological and Antioxidant Activities of Rhus coriaria L. (Sumac)

Pharmacological and Antioxidant Activities of Rhus coriaria L. (Sumac)

Therapeutic Potential of Hispidin—Fungal and Plant Polyketide

Kinetic Behaviour of Pancreatic Lipase Inhibition by Ultrasonicated A. malaccensis and A. subintegra Leaves of Different Particle Sizes

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