Article
Biochemistry & Molecular Biology
Yukiko Matsuo, Asuka Yamashiro, Kanae Ootomo, Mika Nakagawa, Hiroko Tsuchihashi, Niro Inaba, Yoshihiro Mimaki
Summary: Scilla species are used as medicinal plants containing lanosterol-type triterpene glycosides. Phytochemical investigation of Scilla peruviana bulbs led to the isolation of 17 compounds, including new rearranged pentacyclic-lanosterol glycosides and homoisoflavanone glycosides. Among them, some compounds showed significant pancreatic lipase inhibitory activity in vitro and one compound reduced serum triglyceride levels in mice in a dose-dependent manner.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Bilal Ahmad, Emily P. Friar, Muhammad Sufyan Vohra, Nasar Khan, Christopher J. Serpell, Michelle D. Garrett, Jason Siau Ee Loo, Isabel Lim Fong, Eng Hwa Wong
Summary: This study investigates the anti-obesity effects of hydroxylated polymethoxyflavones (HPMFs) and explores their mechanism of action. It demonstrates that two HPMFs, 3' OH-TetMF and 4' OH-TetMF, have anti-obesity effects by inhibiting pancreatic lipase activity, suppressing adipogenesis-related gene expression, promoting lipid breakdown, and reducing adipokine secretion. These findings suggest that HPMFs have potential in the treatment of obesity.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Food Science & Technology
Mahsa Nayebhashemi, Somayeh Enayati, Mozhgan Zahmatkesh, Hamid Madanchi, Samaneh Saberi, Ehsan Mostafavi, Esmat Mirbzadeh Ardakani, Mohammad Azizi, Vahid Khalaj
Summary: Inhibition of lipid absorption is an effective strategy in obesity treatment. Pancreatic Lipase inhibitor (PLI) peptides, as novel anti-obesity agents, were expressed in Saccharomyces boulardii using a yeast surface display system. The recombinant probiotics showed dose-dependent PL inhibition in vitro and significant weight loss and reduced serum lipids in a rat model of obesity, indicating their potential application in treating obesity.
JOURNAL OF FUNCTIONAL FOODS
(2023)
Article
Biochemistry & Molecular Biology
Ginson George, Prashant S. Auti, Pracheta Sengupta, Nisha Yadav, Atish T. Paul
Summary: A series of novel indole-thiazolidinedione hybrid analogues were synthesized and evaluated for their potential pancreatic lipase (PL) inhibition. Among them, 7r exhibited the highest activity with an IC50 of 2.67 μM. Enzyme inhibition kinetics study suggested a competitive mode of inhibition by the analogues, which was further confirmed by fluorescence spectroscopy. Molecular docking and molecular dynamics study supported the in vitro results. Moreover, 7r showed potential antioxidant activity and no cytotoxic effect on RAW 264.7 cells. In vivo pharmacological evaluation demonstrated the anti-obesity effect of 7r. Overall, the synthesized analogue 7r exerted a comparable anti-obesity effect to orlistat.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Xinyi Wang, Xin Ai, Zehui Zhu, Mingxin Zhang, Fei Pan, Zichen Yang, Ou Wang, Liang Zhao, Lei Zhao
Summary: Peptides derived from sesame could potentially inhibit the activity of pancreatic lipase, reducing triglyceride absorption and preventing obesity.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Review
Chemistry, Analytical
Silvia Rocha, Ana T. Rufino, Marisa Freitas, Artur M. S. Silva, Felix Carvalho, Eduarda Fernandes
Summary: Obesity is a concerning epidemic, and pancreatic lipase has been explored as an alternative for weight loss by reducing fat absorption. This review aims to understand and summarize the methodologies and experimental conditions used to evaluate pancreatic lipase catalytic activity.
CRITICAL REVIEWS IN ANALYTICAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Tian-Tian Liu, Xiao-Tian Liu, Gui-Li Huang, Long Liu, Qing-Xi Chen, Qin Wang
Summary: The dramatic increase in obesity has led to a growing interest in lipase inhibitors as effective anti-obesity drugs. In this study, a lipase inhibitor called Fu Brick Theophylline (FBT) was screened using enzyme molecular dynamics. The study analyzed and discussed the mechanism of lipase inhibitors in combating obesity at the cellular and animal model levels. The results showed that FBT had a strong inhibitory effect on lipase and could reduce the generation of reactive oxygen species (ROS) and expression of inflammatory factors during cell differentiation. Animal models further confirmed that FBT effectively reduced the degree of fatty liver and improved mitochondrial membrane damage. This study provides a theoretical basis for the screening and clinical treatment of lipase inhibitors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Bilal Ahmad, Emily P. Friar, Emerald Taylor, Muhammad Sufyan Vohra, Christopher J. Serpell, Michelle D. Garrett, Jason Siau Ee Loo, Isabel Lim Fong, Eng Hwa Wong
Summary: In this study, the anti-obesity effects of two flavones (PMF and TMF) were evaluated through inhibition of pancreatic lipase and inhibition of adipogenesis. Both flavones competitively inhibited pancreatic lipase activity and reduced lipid accumulation in adipocytes. They also downregulated the expression of adipogenic and lipogenic genes and upregulated the expression of lipolytic genes. Overall, PMF was found to be a more potent inhibitor of both pancreatic lipase activity and adipogenesis compared to TMF. These findings suggest that PMF and TMF have anti-obesity activities and should be further investigated.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Chemistry, Applied
Yuying Wang, Lihang Chen, Huimin Liu, Jiahan Xie, Wandi Yin, Zhenghang Xu, Huijing Ma, Wenzhuo Wu, Mingzhu Zheng, Meihong Liu, Jingsheng Liu
Summary: This study identified novel pancreatic lipase (PL) inhibitors, cyanidin-3-O-glucoside (C3G) and catechin, extracted from black rice and adzuki bean coat extracts. The combination of C3G and catechin showed a synergistic effect in inhibiting PL, and molecular docking analysis revealed that these polyphenols formed interactions with PL amino acid residues. These findings suggest that C3G and catechin have potential for developing food supplements to prevent obesity.
Article
Food Science & Technology
Teresa Del Castillo-Santaella, Juan Jose Hernandez-Morante, Jesus Suarez-Olmos, Julia Maldonado-Valderrama, Jorge Pena-Garcia, Carlos Martinez-Cortes, Horacio Perez-Sanchez
Summary: The study found that silibinin(A) and glutathione-disulphide (GSSG) can inhibit pancreatic-lipase activity, showing potential for combating obesity. Further research will help validate the suitability of these compounds.
JOURNAL OF FUNCTIONAL FOODS
(2021)
Article
Biochemistry & Molecular Biology
Lavanya Prabhakar, Davis G. Dicky John, Satya Ranjan Singh, Ayaluru Murali
Summary: Obesity is a global crisis and the compound BC010 from the brown algae Cystophora fibrosa has been identified as a potential drug candidate for inhibiting obesity by inhibiting pancreatic lipase.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Sanjay Kottekad, Sudip Roy, Usharani Dandamudi
Summary: Pancreatic lipase (PL) inhibitors were investigated using molecular docking and binding energy calculations. Most compounds bound at the catalytic site, while some bound at the non-catalytic site. Tannins preferred the non-catalytic site, while flavonoids and furan-flavonoids had strong interactions with catalytic residues. 55 potent PL inhibitors were identified and 14 bioactive compounds were predicted.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Na Li, Xi Liu, Jing Zhang, Yan-Zhi Lang, Lu Lu, Jia Mi, You-Long Cao, Ya-Mei Yan, Lin-Wu Ran
Summary: This study demonstrates that anthocyanins from Lycium ruthenicum fruits have preventive effects in high-fat-diet induced obese mice. Anthocyanins regulate the diversity of gut microbiota, decrease the ratio of Firmicutes to Bacteroidota, increase the abundance of Akkermansia, and reduce the abundance of Faecalibaculum to prevent obesity.
Article
Biochemistry & Molecular Biology
Peng-Chao Huo, Qing Hu, Sheng Shu, Qi-Hang Zhou, Rong-Jing He, Jie Hou, Xiao-Qing Guan, Dong-Zhu Tu, Xu-Dong Hou, Peng Liu, Nan Zhang, Zhi-Guo Liu, Guang-Bo Ge
Summary: In this study, a series of chalcone-like compounds were designed, synthesized, and evaluated as potent and reversible pancreatic lipase (PL) inhibitors. Among them, compound B13 showed the most potent PL inhibition activity and excellent stability in gastrointestinal fluids and metabolic stability in human liver preparations. These findings suggest that chalcone-like compounds are promising candidates for developing novel anti-obesity agents targeting PL, with B13 serving as a potential lead compound.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Nutrition & Dietetics
Xiao-Ya Qin, Xu-Dong Hou, Guang-Hao Zhu, Yuan Xiong, Yun-Qing Song, Liang Zhu, Dong-Fang Zhao, Shou-Ning Jia, Jie Hou, Hui Tang, Guang-Bo Ge
Summary: This study discovers human pancreatic lipase inhibitors from edible herbal medicines, specifically from Ampelopsis grossedentata extract. The study identifies and characterizes the inhibitory mechanisms of these inhibitors, which offer support for their anti-obesity and lipid-lowering effects. The study also highlights the importance of finding effective inhibitors against human pancreatic lipase.
FRONTIERS IN NUTRITION
(2022)
Article
Chemistry, Medicinal
Ga Young Lee, Jang Hoon Kim, Seung-Kook Choi, Young Ho Kim
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2015)
Article
Chemistry, Medicinal
Dae Sik Jang, Ga Young Lee, Yun Mi Lee, Young Sook Kim, Hang Sun, Dong-Hee Kim, Jin Sook Kim
CHEMICAL & PHARMACEUTICAL BULLETIN
(2009)
Article
Pharmacology & Pharmacy
Dae Sik Jang, Ga Young Lee, Young Sook Kim, Yun Mi Lee, Chan-Sik Kim, Jeong Lim Yoo, Jin Sook Kim
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2007)