pancreatic lipase

3,4,5-Trihydroxycinnamic acid decyl ester, an effective inhibitor of lipid absorption and accumulation, exhibits anti-obesity properties and acts as a pancreatic lipase inhibitor, with an EC50 of approximately 0.9 μM.

1. Gypsogenin-3-O-glucuronide (Methyl gypsogenin 3-O-beta-D-glucuronopy) shows inhibitory activity toward pancreatic lipase with IC5 value of .29 mM, and the free carboxylic acid groups in position 28 within its chemical structures are required for enhancement of pancreatic lipase inhibition.

hPL-IN-1 is a potent reversible pancreatic lipase (PL) inhibitor (IC50=1.86 μM) that can be used to study obesity-related diseases.

Pancreatic lipase Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) with an IC50 of 2.13 μM and human carboxylesterase 1A (hCES1A) with an IC50 of 0.055 μM.

hPL-IN-2 is a potent, reversible and non-competitive inhibitor of Pancreatic lipase (IC50: 1.63 μM) that can be used to investigate obesity-related diseases.

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Phloracetophenone (1-(2,4,6-Trihydroxyphenyl)ethanone) has antiobesity and hypolipidemic effects, may be partly mediated by delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

Oleic acid (Glycon Wo) is a natural product, a common monounsaturated fatty acid found in a variety of animal and vegetable fats and oils. Palmitic acid is a Na+/K+ ATPase activator.

Cetilistat (ATL-962) is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes.

Sanggenon C is a flavanone Diels-Alder adduct compound isolated from the root bark of Morus alba. Sanggenon C can inhibit NF-κB activity, inhibit the expression of inducible nitric oxide synthase in RAW264.7 cells, and inhibit tumor necrosis factor-α-stimulated cell adhesion and vascular cell adhesion molecule-1 expression; Sanggenon C also has antioxidant and anti-inflammatory effects, and also has the effect of inhibiting pancreatic lipase. [1,2]

Cetilistat impurity 1 is an impurity of Cetilistat, which is an inhibitor of pancreatic lipase. It inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM and 5.95 nM, respectively.

Benastatin C is a polyketide synthase-derived benastatin found in [Streptomyces] with diverse biological activities. It inhibits glutathione S-transferase (GST; IC50 = 24 μg ml for the rat liver enzyme) and the esterase activity of isolated porcine pancreatic lipase (IC50 = 10 μg ml). Benastatin C also increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.

Gastrin-releasing peptide (GRP) is a neuropeptide that stimulates gastrin release. It binds to (Ki = 300 nM) and stimulates amylase secretion in rat pancreatic AR42J cells (EC50 = 0.3 nM). GRP increases proliferation of human liver carcinoma HepG2 and MHCC97H cells but does not affect the proliferation of normal HL-7702 liver cells at a concentration of 1 nM. In vivo, GRP (0.35 nmol/kg/h) increases both pancreatic exocrine secretion and pancreatic polypeptide (PP) release in rats. It dose-dependently stimulates gastrin, pancreatic amylase, lipase, bilirubin, and acid output and induces gallbladder contraction in humans when administered at doses ranging from 1 to 27 pmol/kg per hour.

Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.

Neotheaflavin (from black tea) inhibits pancreatic lipase.

Lalistat 2 is a selective inhibitor of lysosomal acid lipase with IC50 of 152 nM and exhibits no inhibition of human pancreatic lipase or bovine milk lipoprotein lipase (up to 10 μM).

3-O-Methylgalangin (GALANGIN-3-METHYLETHER) has antibacterial activity, it has inhibitory effects on Pseudomonas aeruginosa. GALANGIN-3-METHYLETHER has hypolipidemic activity, the action is due to the inhibition of pancreatic lipase.

Escin Ib inhibits gastric emptying, at least in part, mediated by capsaicin-sensitive sensory nerves, to stimulate the synthesis and/or release of dopamine, to act through central dopamine2 receptor, which in turn causes the release of PGs.

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg kg) decreases serum cholesterol levels and total bod......

Echitamine chloride, the predominant monoterpene indole alkaloid found in Alstonia scholaris, exhibits significant anti-tumor activity by inducing DNA fragmentation and apoptosis. Furthermore, it effectively inhibits pancreatic lipase, with an inhibition concentration (IC 50) of 10.92 µM [1] [2].

Ciwujianoside C4, a saponin derivative, has been demonstrated to increase pancreatic lipase activity in vitro [1].

Ciwujianoside C1, a saponin derived from the leaves of Acanthopanax senticosus, exhibits in vitro inhibition of pancreatic lipase activity [1].

Acanthopanaxoside A, a triterpenoid saponin, demonstrates inhibitory activity against pancreatic lipase [1].

5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8), extracted from Dendrobium infundibulum (D. infundibulum), shows no inhibitory effects on α-glucosidase and pancreatic lipase [1].