Pancreatic lipase inhibitors: The road voyaged and successes

Kumar, Ashwani; Chauhan, Shilpi

doi:10.1016/j.lfs.2021.119115

Cited by 93 publications

(49 citation statements)

References 110 publications

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“…Despite its effectiveness, the consumption of orlistat can lead to undesirable gastrointestinal problems, such as flatulence, diarrhea and oily stools. 3 In light of this, it is crucial to find safe and effective alternatives to address this health issue.…”

Section: Introductionmentioning

confidence: 99%

“…To date, many lipase inhibitors from numerous plant species such as polyphenols in tea products and saponins in Japanese yam have been characterised. 3 However, studies revealed that the anti-obesity potential of these bioactive compounds was limited. 4 This was because polyphenols would interact with the protein in protein-rich food, thereby reducing the lipase inhibitory activity.…”

Section: Introductionmentioning

confidence: 99%

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Resin glycosides in aerial parts of Ipomoea batatas are potent lipase inhibitors: potential upcycling of sweet potato by-products to combat obesity

2022

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Resin glycosides in aerial parts of Ipomoea batatas are potent lipase inhibitors: potential upcycling of sweet potato by-products to combat obesity

2022

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“…Changes in eating habits, increased physical activity and taking supplements and medications are among the main approaches to treating this disease. Antiobesity medications generally involve three mechanisms: enhancement of energy expenditure, appetite suppression and inhibition of gastrointestinal enzymes involved in digestion, absorption and metabolism of carbohydrates and fats [ 9 , 10 , 15 , 16 ]. Since pancreatic lipase plays an important role in fat absorption, its inhibition has also been of great interest in drug development [ 15 , 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

Multitarget Action of Xanthones from Garcinia mangostana against α-Amylase, α-Glucosidase and Pancreatic Lipase

et al. 2022

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Digestive enzymes such α-amylase (AA), α-glucosidase (AG) and pancreatic lipase (PL), play an important role in the metabolism of carbohydrates and lipids, being attractive therapeutic targets for the treatment of type 2 diabetes and obesity. Garcinia mangostana is an interesting species because there have been identified xanthones with the potential to inhibit these enzymes. In this study, the multitarget inhibitory potential of xanthones from G. mangostana against AA, AG and PL was assessed. The methodology included the isolation and identification of bioactive xanthones, the synthesis of some derivatives and a molecular docking study. The chemical study allowed the isolation of five xanthones (1–5). Six derivatives (6–11) were synthesized from the major compound, highlighting the proposal of a new solvent-free methodology with microwave irradiation for obtaining aromatic compounds with tetrahydropyran cycle. Compounds with multitarget activity correspond to 2, 4, 5, 6 and 9, highlighting 6 with IC50 values of 33.3 µM on AA, 69.2 µM on AG and 164.4 µM on PL. Enzymatic kinetics and molecular docking studies showed that the bioactive xanthones are mainly competitive inhibitors on AA, mixed inhibitors on AG and non-competitive inhibitors on PL. The molecular coupling study established that the presence of methoxy, hydroxyl and carbonyl groups are important in the activity and interaction of polyfunctional xanthones, highlighting their importance depending on the mode of inhibition.

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“…Pancreatic lipase (PL), a key digestive enzyme responsible for the hydrolysis of dietary triglycerides in the gastrointestinal tract, has gained considerable attention as an important antiobesity target (17). In the past few decades, a variety of edible herbal medicines (HMs) and their constituents have been reported with anti-PL effects (18)(19)(20).…”

Section: Introductionmentioning

confidence: 99%

Discovery and Characterization of the Naturally Occurring Inhibitors Against Human Pancreatic Lipase in Ampelopsis grossedentata

et al. 2022

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Pancreatic lipase (PL) inhibitor therapy has been validated as an efficacious way for preventing and treating obesity and overweight. In the past few decades, porcine PL (pPL) is widely used as the enzyme source for screening the PL inhibitors, which generates a wide range of pPL inhibitors. By contrast, the efficacious inhibitors against human PL (hPL) are rarely reported. This study aims to discover the naturally occurring hPL inhibitors from edible herbal medicines (HMs) and to characterize the inhibitory mechanisms of the newly identified hPL inhibitors. Following the screening of the inhibition potentials of more than 100 HMs against hPL, Ampelopsis grossedentata extract (AGE) displayed the most potent hPL inhibition activity. After that, the major constituents in AGE were identified and purified, while their anti-hPL effects were assayed in vitro. The results clearly showed that two abundant constituents in AGE (dihydromyricetin and iso-dihydromyricetin) were moderate hPL inhibitors, while myricetin and quercetin were strong hPL inhibitors [half-maximal inhibitory concentration (IC50) values were around 1.5 μM]. Inhibition kinetic analyses demonstrated that myricetin and quercetin potently inhibited hPL-catalyzed near-infrared fluorogenic substrate of human pancreatic lipase (DDAO-ol) hydrolysis in a non-competitive inhibition manner, with Ki values of 2.04 and 2.33 μM, respectively. Molecular dynamics simulations indicated that myricetin and quercetin could stably bind on an allosteric site of hPL. Collectively, this study reveals the key anti-obesity constituents in AGE and elucidates their inhibitory mechanisms against hPL, which offers convincing evidence to support the anti-obesity and lipid-lowering effects of this edible herb.

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Pancreatic lipase inhibitors: The road voyaged and successes

Cited by 93 publications

References 110 publications

Resin glycosides in aerial parts of Ipomoea batatas are potent lipase inhibitors: potential upcycling of sweet potato by-products to combat obesity

Resin glycosides in aerial parts of Ipomoea batatas are potent lipase inhibitors: potential upcycling of sweet potato by-products to combat obesity

Multitarget Action of Xanthones from Garcinia mangostana against α-Amylase, α-Glucosidase and Pancreatic Lipase

Discovery and Characterization of the Naturally Occurring Inhibitors Against Human Pancreatic Lipase in Ampelopsis grossedentata

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