Molecular recognition between pancreatic lipase and natural and synthetic inhibitors

Bello, Martiniano; Basilio-Antonio, Lucia; Fragoso-Vázquez, Jonathan; Avalos-Soriano, Anaguiven; Correa‐Basurto, José

doi:10.1016/j.ijbiomac.2017.01.150

Cited by 30 publications

(15 citation statements)

References 60 publications

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“…The same results were observed in a previous study and were described as pancreatitis [17] . It was also found that there were dilated ducts with retained secretion in 30 mg and 40 mg/kg treated groups.…”

Section: Discussionsupporting

confidence: 91%

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Effect of Orlistat on the pancreas of the female albino rat: Histological and Histochemical study

Abdelwahab

Ali

Mahmoud

2017

Journal of Medical Histology

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Introduction: Orlistat is the only FDA approved drug for long term management of obesity. It reduces the absorption of dietary fat by inhibiting lipase enzyme. Many cases of pancreatitis were clinically reported in people who used orlistat. Aim of The work:The aim of the present study is to shed a light on the possible deleterious effect of orlistat on the normal pancreatic tissue, and the molecular mechanisms beyond these changes. Materials & Methods: Thirty six female albino rats were divided into 4 groups: Control Group I (a) without treatment &I (b) received only1 ml fish oil. Group II received 30 mg/kg/day of orlistat dissolved in 1ml of fish oil orally for 8 weeks. Group III, received 40 mg/kg/day of orlistat .Group IV (a) & (b) withdrawal groups. Pancreas was dissected out and processed for histological and immunohistochemical study for CASPASE, TNF, INOS and INSULIN. Results: Orlistat caused variable degrees of pancreatic tissue degeneration, dilatation of pancreatic ducts with retained secretion, fatty degeneration and congestion. Inflammatory cells infiltration observed in both pancreatic acini and islets of Langerhan,s only with high dose (40mg/kg). Positive immunoreactivity for activated caspase 3 and iNOS being more evident in high dose and decrease in immunoreactivity for anti-insulin antibody. immunoreactivity for TNF-α had been shown in high dose. These effects disappear after low dose withdrawal only. Conclusion: Orlistat may induce inflammation, fatty degeneration and impaired insulin production in the pancreas. These effects are dose dependent, and it should be taken in consideration while prescribing orlistat as a treatment for obesity.

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Section: Discussionsupporting

confidence: 91%

“…Orlistat (Xenical; Roche, Basel, Switzerland), an inhibitor of pancreatic lipases that limits the intestinal absorption of dietary fat, has proven effective in augmenting weight loss [13] . Currently, orlistat is the only FDA (Food and Drug Administration) approved drug for long term management of obesity [14] .…”

Section: Discussionmentioning

confidence: 99%

Effect of Orlistat on the pancreas of the female albino rat: Histological and Histochemical study

Abdelwahab

Ali

Mahmoud

2017

Journal of Medical Histology

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“…Inter-lobular massive adipocytes were detected also in the stressed group. The same results were reported in a previous study and were recorded as pancreatitis (Bello et al 2017).…”

Section: Discussionsupporting

confidence: 89%

Impact of chronic exercise on counteracting chronic stress-induced functional and morphological pancreatic changes in male albino rats

Elbassuoni

Hafez

2019

Cell Stress and Chaperones

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Chronic stress has been linked to many diseases resulted from dysfunction of both the nervous system and peripheral organ systems. Yet, the effects of chronic stress on the pancreas have received relatively little attention. This work aims to investigate the influence of chronic stress exposure on both the endocrine and exocrine pancreatic function and morphology and its possible mechanism of action, and also to evaluate the impact of chronic exercise with moderate intensity on ameliorating the stressinduced pancreatic changes. Forty adult male albino rats were used and divided into four groups: control group, exercised group (3 weeks of swimming exercise), stressed group (3 weeks of immobilization stress), and stressed group practicing exercise (3 weeks of exercise, concomitant with 21 daily sessions of stress). On the final day of the experiment, all rats were sacrificed. Biochemical, immunohistochemical, and histological studies were conducted. The results showed that chronic immobilization stress produced hyperglycemia, hyperinsulinemia, and increased homeostatic model assessment of insulin resistance index (HOMA-IR) with increasing exocrine pancreatic injury markers by increasing oxidative and inflammatory status of the pancreatic tissue. Histological study showed the injurious effect of stress on the morphology of pancreatic tissue. Physical exercise protected the pancreas from the negative effects of stress through its antiinflammatory and anti-oxidative effects, evidenced by increasing pancreatic interleukin 10 and total antioxidant capacity and decreasing pancreatic tumor necrosis factor-alpha, and malondialdehyde with ameliorating most of the histological changes induced by stress exposure. Physical exercise effectively counteracts chronic stressinduced pancreatic changes through different mechanisms.

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“…They concluded that both structural calcium and colipase contributed to the pancreatic lipase energetic stability of the heterodimer association, decreased confirmation fluctuation, and impacted the thermodynamic ligand-protein complex. Moreover, using inhibitors, such as green tea polyphenols and orlistat, enhanced the dissociation of the heterodimer (Bello et al 2017;Mohammad et al 2010).…”

Section: Pancreatic Lipase Inhibitionmentioning

confidence: 99%

Plant Products and Their Inhibitory Activity Against Pancreatic Lipase

Bajes

Almasri

Bustanji

2020

Rev. Bras. Farmacogn.

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Imbalance in metabolism can lead to many health complications, and obesity is one of the alarming ones in the new world. Modern lifestyle has reduced physical activity and increased intake of various processed, unhealthy, fattening, and fast food. Many approaches have been followed to reduce lipid absorption through the gastrointestinal tract, including herbal plants and drugs. However, due to the side effects associated with drugs, more researches have been navigating towards the discovery of natural substances to substitute synthetic ones. Natural substances have been isolated and identified to inhibit pancreatic lipase, a key enzyme of lipid metabolism; however, only a few have been tested in clinical studies. The aim of this review is to provide relevant information on natural substances derived from plants and algae that have the potential to be anti-obesity agents, with attention to some medicinal plants from Jordan. As a consequence of the information presented in this mini review, several natural compounds have demonstrated to reduce lipid metabolism and absorption, which makes them potential anti-obesity agents.

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Molecular recognition between pancreatic lipase and natural and synthetic inhibitors

Cited by 30 publications

References 60 publications

Effect of Orlistat on the pancreas of the female albino rat: Histological and Histochemical study

Effect of Orlistat on the pancreas of the female albino rat: Histological and Histochemical study

Impact of chronic exercise on counteracting chronic stress-induced functional and morphological pancreatic changes in male albino rats

Plant Products and Their Inhibitory Activity Against Pancreatic Lipase

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