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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).
Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
These drugs comprise statins, fibrates, niacin, Ezetimibe, and bile acid sequestrants as well as phytosterols and (n − 3) long-chain polyunsaturated fatty acids that can reduce circulating triglycerides and raise HDL-cholesterol (Micallef and Garg, 2008), and Orlistat (Tetrahydrolipstatin) that is derived from Lipstatin (its biosynthesis has been reported by Bai et al., 2014), isolated from Streptomyces toxytricini and acting as a potent and selective inhibitor of human pancreatic lipase. Orlistat is used as drug to treat obesity; as a consequence of inhibiting lipase activity, triglycerides from the diet are not hydrolyzed and therefore excreted unchanged. Phytosterols, omega-3 fatty acids, and Orlistat are not treated here in more detail.
Nutritional Strategies for Patients with Obesity and the Metabolic Syndrome
Published in Jeffrey I. Mechanick, Elise M. Brett, Nutritional Strategies for the Diabetic & Prediabetic Patient, 2006
Robert F. Kushner, Julie L. Roth
Orlistat is a synthetic hydrogenated derivative of a naturally occurring lipase inhibitor, lipostatin, produced by the mold Streptomyces toxytricini. Orlistat is a potent, slowly reversible inhibitor of intestinal lipases that are required for the hydrolysis of dietary fat in the gastrointestinal tract into fatty acids and monoacylglycerols. The drug’s activity takes place in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of these lipases. A therapeutic oral dose of 120 mg TID blocks the digestion and absorption of about 30% of dietary fat. On a diet containing 30% fat, this effect typically results in a caloric deficit of approximately 200 kcal daily. When orlistat therapy is discontinued, fecal fat usually returns to normal concentrations within 48–72 hours [75]. Multiple randomized, 1- to 2-year double-blind placebo-controlled studies have shown that after 1 year, orlistat produces a weight loss of about 9–10% compared with a 4–6% weight loss in the placebo-treated groups [76,77]. Orlistat has been demonstrated to improve diabetic control and insulin sensitivity [78–80], reduce cardiovascular risk factors [81,82], and reduce the incidence of T2DM [83,84]. Since orlistat is minimally (< 1%) absorbed from the gastrointestinal tract, it has no systemic side effects. Tolerability to the drug is related to the malabsorption of dietary fat and subsequent passage of fat in the feces. Six gastrointestinal tract adverse effects have been reported to occur in at least 10% of orlistat-treated patients: oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, and increased defecation. The events are generally experienced early, diminish as patients control their dietary fat intake, and infrequently cause patients to withdraw from clinical trials. In fact, avoidance behavior (decreasing dietary fat to diminish orlistat-induced steatorrhea) contributes to weight loss. It has recently been shown that psyllium mucilloid is helpful in controlling the orlistat-induced glycemic index (GI) side effects when taken concomitantly with the medication [85]. Serum concentrations of the fat-soluble vitamins D and E and β–carotene have been found to be significantly lower in some of the trials, although they generally remain within normal ranges. The manufacturer’s package insert for orlistat recommends that patients using orlistat take a vitamin supplement at bedtime to prevent potential deficiencies.
Consumption of Spinacia Oleracea (spinach) and aerobic exercise controls obesity in rats by an inhibitory action on pancreatic lipase
Published in Archives of Physiology and Biochemistry, 2020
Vandana Panda, Priyanka Shinde, Payal Dande
Orlistat, the reference standard, was first isolated from the bacterium Streptomyces toxytricini and a current drug in the clinical management of obesity is a long-term pancreatic lipase inhibitor. However, this drug produces several side effects including fatty diarrhea, stool urgency, fecal incontinence, allergies, and liver damage (Derosa and Maffioli 2012). Hence, current research focuses on newer pancreatic lipase inhibitors of natural origin with lesser adverse effects for the successful management of obesity. Leaves of mango, pomegranate and Ginkgo biloba, fenugreek seeds, oolong tea and bitter melon among others are reported to possess potent pancreatic lipase inhibitory activity due to the presence of different antioxidant phytoconstituents (Seyedan et al.2015). Hence, it is pertinent to explore natural products from plant/food origin for pancreatic lipase inhibitory action.