更新于：2024-11-01

Lipase x CLPS

更新于：2024-11-01

基本信息

关联

项与 Lipase x CLPS 相关的药物

H-0506B

靶点

CLPS x Lipase

作用机制

CLPS抑制剂 [+1]

在研机构-

原研机构

Forskarpatent i Syd AB

在研适应症-

非在研适应症

肥胖

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 Lipase x CLPS 相关的临床结果

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100 项与 Lipase x CLPS 相关的转化医学

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0 项与 Lipase x CLPS 相关的专利（医药）

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274

项与 Lipase x CLPS 相关的文献（医药）

2023-10-01·EFSA Journal

Appethyl® and reduction of body weight: evaluation of a health claim pursuant to Article 13(5) of Regulation (EC) No 1924/2006

Article

作者: Vinceti, Marco ; Turck, Dominique ; Maciuk, Alexandre ; Bresson, Jean‐Louis ; Naska, Androniki ; Bohn, Torsten ; Siani, Alfonso ; Hirsch‐Ernst, Karen Ildico ; McArdle, Harry J ; Bresson, Jean-Louis ; Knutsen, Helle Katrine ; Castenmiller, Jacqueline ; Hirsch-Ernst, Karen Ildico ; Pentieva, Kristina ; Thies, Frank ; Mangelsdorf, Inge ; Fiolet, Thibault ; De Henauw, Stefaan ; Tsabouri, Sophia

Following an application from Greenleaf Medical AB, submitted for authorisation of a health claim pursuant to Article 13(5) of Regulation (EC) No 1924/2006 via the Competent Authority of Sweden, the EFSA Panel on Nutrition, Novel Foods and Food allergens (NDA) was asked to deliver an opinion on the scientific substantiation of a health claim related to Appethyl® and reduction of body weight. Appethyl® is an aqueous extract from spinach leaves standardised by the manufacturing process and its lipase/colipase inhibition capacity in vitro. The Panel considers that the food is sufficiently characterised. A reduction in body weight is a beneficial physiological effect for overweight/obese individuals. The applicant identified a total of three human intervention studies that investigated the effects of Appethyl® on body weight as being pertinent to the claim. In weighing the evidence, the Panel took into account that Appethyl® (5 g/day for 12 weeks) had no effect on body weight as compared to placebo under minimal dietary counselling and moderate physical activity, and that no beneficial physiological effects are to be expected for the target population of overweight/obese individuals from the weight loss that could be attributed to the intervention with Appethyl® under predefined energy restriction and moderate physical activity. The Panel also considered that the effect of Appethyl® (5 g/day for 24 weeks) on body weight maintenance after initial weight loss shown in one study has not been replicated in different settings, which questions the external validity of the results, and that no evidence was provided for a plausible mechanism by which daily consumption of Appethyl® could exert a sustained effect on body weight in humans. The Panel concludes that a cause-and-effect relationship has not been established between the consumption of Appethyl® and a reduction of body weight under the conditions of use proposed by the applicant.

2022-02-01·Journal of Colloid and Interface Science2区 · 化学

Balanced lipase interactions for degradation-controlled paclitaxel release from lipid cubic phase formulations

2区 · 化学

Article

作者: Verma, Vivek ; Murray, David ; Hudson, Sarah P ; Thompson, Damien ; Soulimane, Tewfik ; Dully, Michele ; Bhattacharya, Shayon

Lipid cubic phase (LCP) formulations enhance the intestinal solubility and bioavailability of hydrophobic drugs by reducing precipitation and facilitating their mass transport to the intestinal surface for absorption. LCPs with an ester linkage connecting the acyl chain to the glycerol backbone (monoacylglycerols), are susceptible to chemical digestion by several lipolytic enzymes including lipases, accelerating the release of hydrophobic agents from the lipid bilayers of the matrix. Unlike regular enzymes that transform soluble substrates, lipolytic enzymes act at the interface of water and insoluble lipid. Therefore, compounds that bind to this interface can enhance or inhibit the activity of enzymes to varying extent. Here, we explore how the lipolysis rate can be tuned by the interfacial interaction of porcine pancreatic lipase with monoolein LCPs containing a known lipase inhibitor, tetrahydrolipstatin. Release of the Biopharmaceutical Classification System (BCS) class IV drug, paclitaxel, from the inhibitor-modified LCP was examined in the presence of lipase and its effectors colipase and calcium. By combining experimental dynamic digestion studies, thermodynamic measurements and molecular dynamics simulations of the competitive inhibition of lipase by tetrahydrolipstatin, we reveal the role and mode of action of lipase effectors in creating a precisely-balanced degradation-controlled LCP release system for the poorly soluble paclitaxel drug.

2021-04-01·Life Sciences3区 · 医学

Pancreatic lipase inhibitors: The road voyaged and successes

3区 · 医学

Review

作者: Kumar, Ashwani ; Chauhan, Shilpi

Human pancreatic lipase (triacylglycerol acyl hydrolase EC3.1.1.3) is the most widely studied member of the human lipase superfamily related to carboxyl esterase. It is secreted from the acinar cell of pancreas and has strong preference for triacylglycerides over cholesterol esters, phospholipids, and galactolipids. Apart from the hydrolysis of triacylglycerides, pancreatic lipase may cause the hydrolysis of retinyl esters in vivo. So, it is very much evidenced that pancreatic lipase with its cofactor colipase has prominent role in efficient digestion of dietary fat. Hence, the modulation of human pancreatic lipase may represent a new insight in the discovery of a number of therapeutics that can inhibit the absorption of fat in body and can be used in obesity and other related metabolic disorders. Even, the only Food and drug administration (FDA) approved antiobesity drug, orlistat, is also an inhibitor of pancreatic lipase. This review summarizes studies about structure, mechanistic approach of pancreatic lipase enzyme while emphasizing on the various synthetic pancreatic lipase inhibitors with their structure activity relationship (SAR).