Pancreatic lipase inhibitory constituents from Morus alba leaves and optimization for extraction conditions

Jeong, Jong Youn; Jo, Yang Hee; Kim, Seon Beom; Liu, Qing; Lee, Jin Woo; Mo, Eun Jin; Lee, Ki Yong; Hwang, Bang Yeon; Lee, Mi Kyeong

doi:10.1016/j.bmcl.2015.04.045

Cited by 44 publications

(26 citation statements)

References 31 publications

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“…Among 12 papers included (Birari et al, ; Cha, Song, Kim, & Pan, ; Chatsumpun, Sritularak, & Likhitwitayawuid, ; Jeong, Cho, Kim, & Kim, ; Jeong et al, ; Nakai et al, ; Ray, Samanta, Mitra, & De, ; Shimura et al, ; Sugiyama et al, ; Wikiera et al, ; Won et al, ; Yuda et al, ), seven studies investigated the anti‐lipase activity of chalcone derivatives while five studies mentioned that of xanthine derivatives. The predominant study design was in vitro among all of them with the unique exception of Birari et al (), which was both in vitro and in vivo with no clinical study found .…”

Section: Resultsmentioning

confidence: 99%

Efficacy of chalcone and xanthine derivatives on lipase inhibition: A systematic review

Tam¹,

Mostafa

et al. 2019

Chem Biol Drug Des

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Tam and Mostafa are contributed equally to work.Our review provided efficient candidates of compounds with chalcone scaffold and their characteristics which can be beneficial for discovering further new drugs. Correspondence AbstractLosing weight has significant impact on chronic disease management. Orlistat, a lipase inhibitor, has alternative effect for weight controlling. To find more candidates, we conducted a review of chalcone and xanthine derivatives regarding their anti-lipase activity. Eight databases were searched including PubMed, Scopus, Web of Science (ISI), Virtual Health Library (VHL), System for Information on Grey Literature in Europe (SIGLE), Global Health Library (GHL), EMBASE, and Google Scholar in August 2018. We found chalcone scaffold was more effective on lipase inhibition than xanthine scaffold. Among 19 investigated chalcones, only isoliquiritigenin and licuroside demonstrated an effect on preventing weight gain and increase in the total cholesterol and total triglycerides aside apart from their high activity on inhibiting lipase. Effect and type of inhibition of individual chalcones differed depending on their structure. In addition, very few studies investigated xanthine compounds and their activities were inconsistent. We suggest more studies investigate 206 |

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Section: Resultsmentioning

confidence: 99%

Efficacy of chalcone and xanthine derivatives on lipase inhibition: A systematic review

Tam¹,

Mostafa

et al. 2019

Chem Biol Drug Des

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“…Global or partial demethylation of 4p gave the corresponding Cuspidan B( 19,H L-60 cell inhibitor) [26] and Stemofuran B (20,a nti-inflammatory activity) [27] in 93 %a nd 68 %y ield, respectively.A fter protecting group manipulation, 4q was transferred to Gnetucleistol C [28] (21)i n4 9% yield. Global demethylation of 6bcould afford Wittifuran E(22,pancreatic lipase inhibitor) [29] in 88 %yield.…”

Section: Angewandte Chemiementioning

confidence: 99%

Deconstructive Reorganization: De Novo Synthesis of Hydroxylated Benzofuran

et al. 2020

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An unprecedented deconstructive reorganization strategy for the de novo synthesis of hydroxylated benzofurans from kojic acid‐ or maltol‐derived alkynes is reported. In this reaction, both the benzene and furan rings were simultaneously constructed, whereas the pyrone moiety of the kojic acid or maltol was deconstructed and then reorganized into the benzene ring as a six‐carbon component. Through this strategy, at least one free hydroxyl group was introduced into the benzene ring in a substitution‐pattern tunable fashion without protection–deprotection and redox adjustment. With this method, a large number of hydroxylated benzofuran derivatives with different substitution‐patterns have been prepared efficiently. This methodology has also been shown as the key step in a collective total synthesis of hydroxylated benzofuran‐containing natural products (11 examples).

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“…To develop a ligand-based pharmacophore model, a total of one hundred and thirty-three (133) molecules from diverse scaffolds with PL inhibitory activity evaluated by the same assay method (using the p-nitrophenyl butyrate (p-NPB) as substrate) were selected [13][14][15][16][17][18]. The IC50 values were converted into negative logarithm of the reported inhibitory concentrations (pIC50).…”

Section: Datasetmentioning

confidence: 99%

Ligand Based Pharmacophore Modeling, Virtual Screening and Molecular Docking Studies to Design Novel Pancreatic Lipase Inhibitors

Engels

Divakar

et al. 2017

Int J Pharm Pharm Sci

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Objective: To understand the essential structural features required for pancreatic lipase (PL) inhibitory activity and to design novel chemical entities, ligand-based pharmacophore modeling, virtual screening and docking studies were carried out. Methods:The pharmacophore model was generated based on 133 compounds with PL inhibitory activity using PHASE. An external test set and decoy dataset methods were applied to validate the hypothesis and to retrieve potential PL inhibitors. The generated hypothesis model was further subjected to virtual screening and molecular docking studies. Results:A five point pharmacophoric hypothesis model which consists of three hydrogen bond acceptor sites and two hydrophobic sites was developed. The generated pharmacophore gave significant 3D QSAR (three-dimensional Quantitative Structural Activity Relationship) model with r 2 of 0.9389 and Q 2 value of 0.4016. After database screening, five molecules were found to have better glide scores and binding interactions with the active site amino acid residues. Conclusion:As an outcome of this study, five hit molecules were suggested as potent PL inhibitors as they showed good glide scores as well as binding interactions with required active site amino acids. The five molecules obtained from this study may serve as potential leads for the development of promising anti-obesity agents.

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Pancreatic lipase inhibitory constituents from Morus alba leaves and optimization for extraction conditions

Cited by 44 publications

References 31 publications

Efficacy of chalcone and xanthine derivatives on lipase inhibition: A systematic review

Efficacy of chalcone and xanthine derivatives on lipase inhibition: A systematic review

Deconstructive Reorganization: De Novo Synthesis of Hydroxylated Benzofuran

Ligand Based Pharmacophore Modeling, Virtual Screening and Molecular Docking Studies to Design Novel Pancreatic Lipase Inhibitors

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