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Mitigation of Obesity: A Phytotherapeutic Approach
Published in Amit Baran Sharangi, K. V. Peter, Medicinal Plants, 2023
A.B. Sharangi, Suddhasuchi Das
The best way to manage obesity is to impede fat absorption down the gastrointestinal tract directly by developing inhibitors for digestion of nutrient and assimilation. Enzymatic break down of any dietary fat by the action of pancreatic lipase is very much essential to be absorbed in human intestine This is the vital indicator for the anti-obesity potential of natural products (Marrelli et al., 2013). Pancreatic lipase hydrolyzes triglyceride to mono-glyceride and fatty acids for absorption of dietary triglyceride. A derivative of the naturally-occurring lipase inhibitor, tetrahydrolipstatin (orlistat), is isolated from Streptomyces toxytricini (Zhu et al., 2014). To block the absorption of dietary fat, a synthetic drug is designed to take action through a covalent bond to the active site serine of pancreatic lipase (Mulzer et al., 2006; Tsujita et al., 2006).
An Overview of Molecular Nutrition
Published in Nicole M. Farmer, Andres Victor Ardisson Korat, Cooking for Health and Disease Prevention, 2022
Vincent W. Li, Catherine Ward, Delaney K. Schurr
Once in the stomach, gastric lipase, amongst other digestive enzymes, is released. However, gastric lipase is responsible for only the initial and minimal breakdown of ingested fats. The large majority of fat digestion does not occur in the stomach, but later on in the small intestine. Once released from the food matrix, fat is now bound to bile salts to undergo its main form of digestion in the small intestine. Pancreatic lipase works to break down triglyceride fats into monoglycerides and fatty acids. The efficient activity of the lipase is dependent on the presence of bile salts on fat droplets. Multiple bile salts with the complexed triglyceride components spontaneously form micelles. Micelles then enter enterocytes where the bile is broken down and chylomicrons are packaged and extruded from the basolateral enterocyte wall to enter the lymphatics. This is the mechanism for absorption of triglycerides which represent 90% of dietary fat. Dietary cholesterol undergoes a similar process except it requires a transport protein in order to enter the enterocyte. Lastly, MCTs, such as coconut oil, when extruded from the enterocyte go directly into the blood stream, by passing the lymphatic system. Therefore, MCTs are suspected of having a favorable metabolic profile.
The digestive system
Published in Laurie K. McCorry, Martin M. Zdanowicz, Cynthia Y. Gonnella, Essentials of Human Physiology and Pathophysiology for Pharmacy and Allied Health, 2019
Laurie K. McCorry, Martin M. Zdanowicz, Cynthia Y. Gonnella
Intact triglycerides are too large to be absorbed. Therefore, pancreatic lipase acts on the lipid droplets to hydrolyze the triglyceride molecules into monoglycerides and free fatty acids. These constituent molecules are water-insoluble and would tend to float on the surface of the aqueous chyme. Therefore, they must be transported to the absorptive surface. This process is carried out by micelles, which are sphere-like structures formed by the amphipathic bile salts. The bile salts associate with each other such that the polar region of the molecules orient outward, making them water-soluble. The nonpolar region faces inward, away from the surrounding water. The monoglycerides and free fatty acids are carried in this interior region of the micelle. Upon reaching the brush border of the absorptive cells, the monoglycerides and free fatty acids leave the micelles and enter the cells by simple diffusion. Because they are nonpolar, these molecules move passively through the lipid bilayer of the cell membrane. This process takes place primarily in the jejunum and proximal ileum. The bile salts are absorbed in the distal ileum by way of either passive diffusion or secondary active transport.
Rationale utilization of phospholipid excipients: a distinctive tool for progressing state of the art in research of emerging drug carriers
Published in Journal of Liposome Research, 2023
Koilpillai Jebastin, Damodharan Narayanasamy
Oral LBDDS are premised on the principle of delivering an API to the GIT in a non-aqueous solution. Slow drug dissolution from solid dosage forms, which is frequent with poorly water-soluble medications, is avoided by providing the drug in a solubilized condition. LBDDS are subjected to GI processing after gastric emptying, which includes dispersion, digestion, and bile mixing (Porter et al. 2007). Drug products containing triglycerides (TG) are disseminated in the stomach after ingestion, where gastric lipase begins lipid digestion. Mechanical mixing in the stomach, together with amphiphilic moieties derived from the LBDDS or initial lipid digestion, aids in the emulsification of lipids before they enter the duodenum (Figure 9). The presence of exogenous lipids in the latter is the stimulus that causes the gallbladder to secrete bile fluid and the pancreas to secrete pancreatic fluid. Pancreatic lipase and its cofactor co-lipase complete the breakdown of ingested glycerides into di-glyceride, monoglyceride, and fatty acid in the small intestine (Dahan and Hoffman 2008, Bolko et al. 2014).
Anti-obesity, anti-hyperglycaemic, anti-antipyretic and analgesic activities of Globularia alypum extracts
Published in Archives of Physiology and Biochemistry, 2022
Tiss Mohamed, Zoubeida Souiy, Lotfi Achour, Khaled Hamden
Previous studies have reported that lipase is main enzyme for lipids absorption, being responsible for hydrolysis of e the major of total fat in diet (Elsbaey et al. 2019, Abdin et al. 2019, Quiroga et al. 2013). Inhibition of pancreatic lipase is a promising way to combat obesity, hyperlipidaemia and others diseases (Ben Abdallah Kolsi et al. 2015, Panda et al. 2018, Kalaivani et al. 2019, Spínola et al. 2020). Some drugs such as orlistat have this purpose, but side effects of this drug have encouraged search for healthier alternatives such as those present in natural plant compounds (Hamden et al. 2013, Hamden et al. 2017, Abdin et al. 2019, Hamden et al. 2019). Phenolic compounds from fruits, vegetables have been main target of research to find natural substitutes to decrease obesity (Oliveira et al. 2018, Lenquiste et al. 2019).
Strong inhibitory activities and action modes of lipopeptides on lipase
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Mei-chun Chen, Tian-tian Liu, Jie-ping Wang, Yan-ping Chen, Qing-xi Chen, Yu-jing Zhu, Bo Liu
Dietary and lifestyle modifications such as calorie restriction and physical exercises are the common strategies adopted to control body weight; further, these methods have limited anti-obesity effects4. It has previously been reported that lipase inhibition is a potential strategy for counteracting obesity. Digestive lipase hydrolyses non-absorbable dietary triglycerides to smaller absorbable molecules of monoglycerides and free fatty acids, which are absorbed by the intestine. Inhibiting digestive lipase can reduce intestinal fat absorption5–7. Human pancreatic lipase is the main enzyme in intestinal digestion of dietary fats in the human digestive system. To date, a wide variety of natural products have been used as pancreatic lipase inhibitors, which originate from plants and metabolites of microorganisms. These include lipstatin, panclicins, saponins, polyphenols, flavonoids, caffeine, chitin, chitosan, etc5. The lipase inhibitor orlistat is the only one obesity-treatment drug currently available in the market, which reduces intestinal fat absorption via inhibition of pancreatic lipase; however, it has been reported to cause certain side effects, e.g. oily stools, oily spotting, and flatulence1,8. Some polyphenol compounds have been reported to have potential adverse effects on microorganisms and animal at high concentrations9,10. Thus, there is still a need to explore safe and effective anti-obesity drugs.