Pancreatic lipase inhibitors: The road voyaged and successes

被引:115
作者
Kumar, Ashwani [1 ]
Chauhan, Shilpi [2 ]
机构
[1] Guru Jambheshwar Univ Sci & Technol, Dept Pharmaceut Sci, Hisar, Haryana, India
[2] Lloyd Inst Management & Technol Pharm, Greater Noida, UP, India
关键词
Pancreatic lipase enzyme; Pancreatic lipase inhibitors; Orlistat; Antiobesity therapeutics; Triacylglycerides; MICROWAVE-ASSISTED SYNTHESIS; ALPHA-KETO AMIDE; BIOLOGICAL EVALUATION; BENZIMIDAZOLE DERIVATIVES; TRITERPENOID SAPONINS; IN-VITRO; STREPTOMYCES-TOXYTRICINI; TRIACYLGLYCEROL ANALOGS; CETILISTAT ATL-962; POTENT INHIBITORS;
D O I
10.1016/j.lfs.2021.119115
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
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).
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页数:23
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共 118 条
  • [1] Fluoroquinolones: novel class of gastrointestinal dietary lipid digestion and absorption inhibitors
    Al-Hiari, Yusuf M.
    Kasabri, Violet N.
    Shakya, Ashok K.
    Alzweiri, Muhammad H.
    Afifi, Fatma U.
    Bustanji, Yasser K.
    Al-Masri, Ihab M.
    [J]. MEDICINAL CHEMISTRY RESEARCH, 2014, 23 (07) : 3336 - 3346
  • [2] Computational approaches for the discovery of natural pancreatic lipase inhibitors as antiobesity agents
    Almasri, Ihab M.
    [J]. FUTURE MEDICINAL CHEMISTRY, 2020, 12 (08) : 741 - 757
  • [3] CATALYTIC ACTIVITY AND ASSOCIATION OF PANCREATIC LIPASE
    ANTONOV, VK
    DYAKOV, VL
    MISHIN, AA
    ROTANOVA, TV
    [J]. BIOCHIMIE, 1988, 70 (09) : 1235 - 1244
  • [4] Arabiyat Shereen, 2019, Asian Pac J Cancer Prev, V20, P2503, DOI 10.31557/APJCP.2019.20.8.2503
  • [5] Arabiyat S, 2016, REV ROUM CHIM, V61, P871
  • [6] Addressing the unmet medical need for safe and effective weight loss therapies
    Arbeeny, CM
    [J]. OBESITY RESEARCH, 2004, 12 (08): : 1191 - 1196
  • [7] Synthesis and biological investigation of the β-thiolactone and β-lactam analogs of tetrahydrolipstatin
    Aubry, Sylvain
    Aubert, Genevieve
    Cresteil, Thierry
    Crich, David
    [J]. ORGANIC & BIOMOLECULAR CHEMISTRY, 2012, 10 (13) : 2629 - 2632
  • [8] PREPARATION OF TRIFLUOROMETHYL KETONES AND RELATED FLUORINATED KETONES
    BEGUE, JP
    BONNETDELPON, D
    [J]. TETRAHEDRON, 1991, 47 (20-21) : 3207 - 3258
  • [9] Synthesis of some novel heterocylic compounds derived from 2-[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]acetohydrazide and investigation of their lipase and α-glucosidase inhibition
    Bekircan, Olcay
    Ulker, Serdar
    Mentese, Emre
    [J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2015, 30 (06) : 1002 - 1009
  • [10] Synthesis of Some New 1,2,4-Triazole Derivatives Starting from 3-(4-Chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol with Anti-Lipase and Anti-Urease Activities
    Bekircan, Olcay
    Mentese, Emre
    Ulker, Serdar
    Kucuk, Cagatay
    [J]. ARCHIV DER PHARMAZIE, 2014, 347 (06) : 387 - 397