Pancreatic lipase inhibitors from natural sources
Human pancreatic lipase[edit]
Pancreatic lipase, also known as pancreatic triacylglycerol lipase or steapsin is a lipolytic enzyme synthesized and released in the pancreatic juice by the pancreas, plays an essential role in digestion and absorption of triglycerides from the gut.
It that breaks down fat molecules obtained from diet. It mainly responsible for the hydrolysis of ester linkages of triglycerides in order to convert them to monoglycerides and free fatty acids.[1]
Pancreatic enzymes inhibitors[edit]
They are agents that limit diet lipids digestion and fats absorption from intestine.[2] The only FDA approved pharmacological agent works as a potent pancreatic lipase inhibitor & one of the best-selling drugs is orlistat (Xenical).[2]
Orlistat hydrogenated derivative of lipstatin derived from Streptomyces toxytricini that increases fecal fat excretion in dose dependent manner, thus inhibit approximately 25-30% of calories ingested as fat. It's one of the best-selling drugs over the world for there effectiveness in the treatment of human obesity.[2]
Orlistat has unpleasant GI side effects (like oily stools, oily spotting, and flatulence) that make researchers tend to find more reliable to use agents and here we will discuss there tendencies to find pancreatic lipase inhibitors from natural sources that work locally with less systemic side effects.
Obesity and Pancreatic lipase inhibitors[edit]
Obesity is a metabolic disorder, caused by an imbalance between the energy intake and expenditure.
Obesity and central obesity are strongly related to increase morbidity and mortality rate, cardiovascular complications (hypertension, HF, Afib, stroke for example), dyslipidemia and type 2 diabetes mellitus. So several pharmacological and non-pharmacological strategies have been implemented to find treatments for this critical problem.[2]
The elevation in plasma triglycerides is considered the major contributor for the development of obesity and its complications. Thus, the inhibition of diet lipids absorption is such a rate limiting step in prevention of human obesity and this can occur by the inhibiting of the enzyme responsible for the hydrolysis of diet fat and therefore inhibits there absorption.[2]
Medicinal plants with pancreatic lipase inhibitory effect.[edit]
In this article we will discuss some natural sources tested in-vitro for there ability to inhibit pancreatic lipase enzyme that secreted from pancreas and here we are with some of them:
Anthemis palaestina Boiss[edit]
A.palaestina is one of the most potent plant extracts that shows dose dependent pancreatic lipase inhibitory effect ranging from 20-56%. By this result we can consider these plants as a promising agents for the treatment of hypertriglyceridemia and an adjunctive method to treat human obesity. In Addition to anti-PL effect of this plant, it was previously reported that A.plaestina has antioxidant activity.[2][not in citation given]
Further studies are needed, using animal models, to verify the inhibitory activities of these plant in-vivo.
Salvia spinosa[edit]
S.spinosa belongs to Lamiaceae family and it's also consider potent plants extract that has anti-PL activity ranging from 5-55% in dose dependent manner.[citation needed]
It's also such a promising materials for the treatment of hypertriglyceridemia and an adjunctive method to treat human obesity.[citation needed] However, Further studies are needed using animal models to verify the inhibitory activities of these plant in-vivo.
Rosemary, Rosmarinus officinalis[edit]
Rosemary has been used for a wide range of disease as antispasmodic,anti-inflammatory,antimicrobial,anticarcinogenic,a reliever of respiratory symptoms and a stimulator of hair growth.[2][not in citation given]
Rosemary methanolic extracts and pure compounds was recently studied for both hormone sensitive lipase (HSL) and pancreatic lipase (PL).This would provide promising strategy in combating both obesity and hyperglycemia and their complications[2][not in citation given]
Rosemary methanolic extract exhibited a significant inhibitory activity on both enzymes.[citation needed] The rosemary extract was more effective against PL than that of HSL.[citation needed] They[who?] also studied the effect of pure compounds {rosmarinic acid (RA), chlorogenic acid (CA), caffeic acid (CaA) and gallic acid (GA)} on PL and HSL and the conclusion of this study is that all tested compounds were able to inhibit both PL and HSL in dose dependent manner with highest potency of GA towards PL and HSL.[citation needed]
However, further studies are needed to determine whether these in vitro findings would correlate with the in-vivo effects.
Gingko biloba L. (Ginkgoaceae)[edit]
G. biloba has been used for medical purposes as dietary supplement or phytomedicine. It has a cardiovascular, neuroprotective and cerebrovascular effects. The plant extract of Ginkgo biloba after investigation showed a fat mass reduction, hypolipidaemic effect, and a potential weight reduction effect.[citation needed]
The extract have different types of active compounds, the most important ones are terpene trilactones (TTLs) and flavonol glycosides. These active compounds have antioxidant effects, inhibition of platelet aggregation and thromboxane & fatty acid synthase inhibition activity which is the target for the treatment of obesity.[citation needed]
An in vitro study done to evaluate the inhibitory effect of G. biloba against PL, the study was computer-aided molecular docking of TTLs, into the binding pocket of PL in order to reach to conclusions about terpenes/PL-binding energetics. The results were the anti-lipase activity of the methanolic extract of G.biloba leaves revealed a potent PL inhibition activity in a concentration-dependent manner.[2][not in citation given]
Berberine and Dihydroberberine[edit]
Berberine (BBR) is an isoquinoline alkaloid found in Hydrastis canadensis, Berberis and Cortex phellodendri. BBR was found to help diabetes and serum lipid profile by reducing serum cholesterol, triglyc-erides, and LDL-cholesterol.[citation needed]
An in vitro study done to evaluate its inhibitory effect by computer-aided molecular docking of BBR and HBBR into the binding pocket of PL. It showed that it has a potential hypolipidemic effects and fat-mass reduction activities.[2][not in citation given]
Willd(candle nut/buah keras), and fruits of Archidendron jiringa[edit]
In a study of 98 plants from malaysia to evaluate the antipancreatic lipase activity of their methanolic exracts the above two plants showed the highest antilipase activity which is 100% and are equivalent to 0.11mcg of orlistat/ml.[2][not in citation given]
Cudrania tricuspidata[edit]
In a study of an in-vitro screening for procine pancreatic lipase inhibiton activity using ethanol exracts of each plants,Cudrania tricuspidata showed anti-lipase activity at concentration (50-250mg/kg).[citation needed]In addition,this plant extract decrease triglycerol levels at concentration 50mg/kg and delay lipid absorption at higher concentrations.[citation needed]
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- ↑ Hansen, Werner E. (March 1987). "Effect of Dietary Fiber on Pancreatic Lipase Activity in Vitro". Pancreas. 2 (2): 195–198. doi:10.1097/00006676-198703000-00012. ISSN 0885-3177.
- ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 Klein, Samuel (December 2004). "Long-Term Pharmacotherapy for Obesity". Obesity Research. 12 (S12): 163S–166S. doi:10.1038/oby.2004.283. ISSN 1071-7323.
