Impact of roasting on the flavan-3-ol composition, sensory-related chemistry, and in vitro pancreatic lipase inhibitory activity of cocoa beans

Pancreatic lipase inhibitory effect of some edible spices in light of percent inhibition, efficacy, reversibility/ irreversibility and effect of pH on inhibition is presented here. Lipase inhibitory activities of methanolic extracts of eighteen spices were evaluated. Extracts of Zanthoxylum armatum, Cinnamomum tamala, Syzygium aromaticum and Myristica fragrans were considered to be of high potency in synthetic substrate assay. Only Syzygium aromaticum showed high potency in natural substrate based lipase assay. Zanthoxylum armatum extract displayed lowest IC50 of 9.0 μg/mL. On dialysis, all extracts lost their lipase inhibitory activity indicating reversible nature of inhibition. pH significantly affected the performance of spice extracts during inhibition of pancreatic lipase. Most of the extracts lost their pancreatic lipase inhibitory activity at pH 3.0 with the exception of Brassica nigra and Cinnamomum tamala. Results showed spice are good source of pancreatic lipase inhibitor and its potential as drug for obesity can be explored by addressing various issues.

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Inhibitory Activities of Polyphenolic Extracts of Bangladeshi Vegetables against α-Amylase, α-Glucosidase, Pancreatic Lipase, Renin, and Angiotensin-Converting Enzyme

Foods ◽

10.3390/foods9070844 ◽

2020 ◽

Vol 9 (7) ◽

pp. 844

Author(s):

Razia Sultana ◽

Adeola M. Alashi ◽

Khaleda Islam ◽

Md Saifullah ◽

C. Emdad Haque ◽

...

Keyword(s):

Angiotensin Converting Enzyme ◽

Pancreatic Lipase ◽

Lipase Activity ◽

Inhibitory Activity ◽

The Other ◽

Converting Enzyme ◽

Inhibitory Activities ◽

Ash Gourd ◽

Better Than

The aim of the study was to determine the in vitro enzyme inhibition activities of aqueous polyphenolic extracts of nine popular Bangladeshi vegetables, namely ash gourd, bitter gourd, brinjal, Indian spinach, kangkong, okra, ridge gourd, snake gourd, and stem amaranth. Polyphenolic glycosides were the major compounds present in the extracts. Inhibition of α-amylase (up to 100% at 1 mg/mL) was stronger than α-glucosidase inhibition (up to 70.78% at 10 mg/mL). The Indian spinach extract was the strongest inhibitor of pancreatic lipase activity (IC50 = 276.77 µg/mL), which was significantly better than that of orlistat (381.16 µg/mL), a drug. Ash gourd (76.51%), brinjal (72.48%), and snake gourd (66.82%) extracts were the most effective inhibitors of angiotensin-converting enzyme (ACE), an enzyme whose excessive activities have been associated with hypertension. Brinjal also had a significantly higher renin-inhibitory activity than the other vegetable extracts. We conclude that the vegetable extracts may have the ability to reduce enzyme activities that have been associated with hyperglycemia, hyperlipidemia, and hypertension.

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Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations

Molecules ◽

10.3390/molecules25204657 ◽

2020 ◽

Vol 25 (20) ◽

pp. 4657

Author(s):

Phuong Thuy Viet Nguyen ◽

Han Ai Huynh ◽

Dat Van Truong ◽

Thanh-Dao Tran ◽

Cam-Van Thi Vo

Keyword(s):

Molecular Dynamics ◽

Molecular Dynamics Simulations ◽

Pancreatic Lipase ◽

Inhibitory Activity ◽

Dynamics Simulation ◽

Stable Complex ◽

Catalytic Active Site ◽

Dynamics Simulations

Inhibition of human pancreatic lipase, a crucial enzyme in dietary fat digestion and absorption, is a potent therapeutic approach for obesity treatment. In this study, human pancreatic lipase inhibitory activity of aurone derivatives was explored by molecular modeling approaches. The target protein was human pancreatic lipase (PDB ID: 1LPB). The 3D structures of 82 published bioactive aurone derivatives were docked successfully into the protein catalytic active site, using AutoDock Vina 1.5.7.rc1. Of them, 62 compounds interacted with the key residues of catalytic trial Ser152-Asp176-His263. The top hit compound (A14), with a docking score of −10.6 kcal⋅mol−1, was subsequently submitted to molecular dynamics simulations, using GROMACS 2018.01. Molecular dynamics simulation results showed that A14 formed a stable complex with 1LPB protein via hydrogen bonds with important residues in regulating enzyme activity (Ser152 and Phe77). Compound A14 showed high potency for further studies, such as the synthesis, in vitro and in vivo tests for pancreatic lipase inhibitory activity.

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Chemical Constituents of the Bulbs of Scilla peruviana and Their Pancreatic Lipase Inhibitory Activity

International Journal of Molecular Sciences ◽

10.3390/ijms22031262 ◽

2021 ◽

Vol 22 (3) ◽

pp. 1262

Author(s):

Yukiko Matsuo ◽

Asuka Yamashiro ◽

Kanae Ootomo ◽

Mika Nakagawa ◽

Hiroko Tsuchihashi ◽

...

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity ◽

Chemical Constituents ◽

Serum Triglyceride ◽

2D Nmr ◽

Triterpene Glycosides ◽

Dependent Manner ◽

Concentration Dependent Manner ◽

Phytochemical Investigation

Scilla species are used as medicinal plants and contain lanosterol-type triterpene glycosides. The phytochemical investigation of the bulbs of Scilla peruviana led to the isolation of 17 compounds, including three new rearranged pentacyclic-lanosterol glycosides (1–3) and two new homoisoflavanone glycosides (12 and 13). The structures of the undescribed compounds were determined by extensive spectroscopic analyses, including two-dimensional (2D) NMR. Among the triterpene glycosides, 2, 3, and 6 showed significant pancreatic lipase inhibitory activity in a concentration-dependent manner in vitro. The oral administration of scillascilloside D-2 (6) reduced serum triglyceride levels in a dose-dependent manner in soybean oil-loaded mice.

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Pancreatic Lipase Inhibitory Activity of Cassiamin A, a Bianthraquinone from Cassia siamea

Natural Product Communications ◽

10.1177/1934578x1300800216 ◽

2013 ◽

Vol 8 (2) ◽

pp. 1934578X1300800 ◽

Cited By ~ 2

Author(s):

Dilip Kumar ◽

Aniket Karmase ◽

Sneha Jagtap ◽

Ruchi Shekhar ◽

Kamlesh K Bhutani

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity ◽

Enzyme Inhibitors ◽

Etoac Extract ◽

Cassia Siamea ◽

Bioassay Guided Fractionation ◽

Pancreatic Lipase Inhibition ◽

Lipase Inhibition ◽

Indian Medicinal Plants

In continuation towards the discovery of potential antiobesity lead(s) from natural products, we have screened n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of 33 Indian medicinal plants (200 extracts) for in vitro pancreatic lipase inhibitory activity. Of the screened extracts, the EtOAc extract of Cassia siamea roots showed 74.3±1.4% enzyme inhibition at 250 μg/mL concentration. Bioassay guided fractionation of the active extract afforded 6 known compounds viz. chrysophanol (1), physcion (2), emodin (3), cassiamin A (4), friedelin (5) and cycloart-25-en-3β,24-diol (6). These compounds were further evaluated for pancreatic lipase inhibitory activity. Cassiamin A (4), a bianthraquinone, was found to be most active with an IC50 value of 41.8±1.2 μM and compounds 2 and 5 were found to be moderate enzyme inhibitors. Results indicate the antiobesity potential of C. siamea through pancreatic lipase inhibition.

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BIOLOGICAL ACTIVITIES OF NOVEL IN VITRO RAISED STEVIA PLANT

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i8.19117 ◽

2017 ◽

Vol 10 (8) ◽

pp. 240 ◽

Cited By ~ 1

Author(s):

Neeta Raj Sharma ◽

Vineet Meshram ◽

Mahiti Gupta

Keyword(s):

Pancreatic Lipase ◽

Staphylococcus Epidermidis ◽

Inhibitory Activity ◽

Inhibitory Concentration ◽

Methanolic Extract ◽

Biological Activities ◽

Gram Negative Bacteria ◽

Herbal Formulation ◽

Further Development

Objective: This communication explores a lead fraction from methanolic extract of novel Stevia species raised under in vitro conditions for its various biological activities.Methods: The dried Stevia leaves were crushed in methanol to get the polar extract. This methanol extract was tested for pancreatic lipase and alpha-amylase inhibitory activity using quantitative plate assays. Antibacterial property of the extract was also evaluated against Staphylococcus epidermidis, Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. Further, the antioxidant potential was evaluated using 1,1-diphenyl-2-picrylhydrazyl.Results: The methanolic extract inhibited pancreatic lipase with IC50 of 5.74 μg/ml in a similar manner to a well-known anti-obesity drug in the market orlistat. The methanolic extract also showed a better pancreatic α-amylase inhibitory activity (IC50=88 μg/ml) than acarbose. Further, the lead fraction exhibited 88.48% antioxidant activity. It also exhibited broad spectrum antimicrobial activity against the spectrum of Gram-positive and Gram-negative bacteria tested under laboratory conditions with a minimal inhibitory concentration ranging from 1.95 to 31.25 μg/ml.Conclusion: Thus, this study signifies the vast potential of the lead fraction from a novel Stevia species for further development into a herbal formulation for prevention of various infectious and non-infectious diseases.

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Improvement of Health-Promoting Functionality of Rye Bread by Fortification with Free and Microencapsulated Powders from Amelanchier alnifolia Nutt

Antioxidants ◽

10.3390/antiox9070614 ◽

2020 ◽

Vol 9 (7) ◽

pp. 614 ◽

Cited By ~ 2

Author(s):

Sabina Lachowicz ◽

Michał Świeca ◽

Ewa Pejcz

Keyword(s):

Antioxidant Activity ◽

Pancreatic Lipase ◽

Inhibitory Activity ◽

In Vitro Digestion ◽

Antioxidant Compounds ◽

Overall Acceptability ◽

Rye Bread ◽

Functional Additive ◽

Berry Fruits

This study established the appropriate amounts of a functional Saskatoon berry fruit powder in fortified rye bread acceptable to consumers and determined the potential relative bioaccesibility of bioactive compounds exhibiting antioxidant activity, and enzymatic in vitro inhibitory activity against lipoxygenase, cyclooxigenase-1, cyclooxigenase-2, acetylcholinesterase, pancreatic lipase α-glucosidase, and α-amylase, as well as the relative digestibility of nutrients. The content of polyphenolic compounds and antioxidant capability were strongly, positively correlated with the content of the functional additive. The highest phenolics content and antioxidant activity were determined in the products enriched with the powders microencapsulated with maltodextrin (an increase by 91% and 53%, respectively, compared with the control). The highest overall acceptability was shown for the products with 3% addition of the functional additive, regardless of its type. The simulated in vitro digestion released phenols (with the highest bioaccessibility shown for anthocyanins) and enhanced the antioxidant activity of rye bread. In turn, the microencapsulation contributed to the improvement in the relative bioaccesibility of antioxidant compounds. Bread fortification led to an increased inhibitory activity against α-amylase, α-glucosidase, and lipoxygenase. Furthermore, the additive microencapsulated with maltodextrin and inulin improved the capacity to inhibit the activities of pancreatic lipase and cyclooxigenase-2. The results presented allowed concluding that the powders from Saskatoon berry fruits, especially microencapsulated ones, may be a promising functional additive dedicated for the enrichment of rye bread.

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Pancreatic lipase inhibitory activity of taraxacum officinale in vitro and in vivo

Nutrition Research and Practice ◽

10.4162/nrp.2008.2.4.200 ◽

2008 ◽

Vol 2 (4) ◽

pp. 200 ◽

Cited By ~ 45

Author(s):

Jian Zhang ◽

Min-Jung Kang ◽

Myung-Jin Kim ◽

Mi-Eun Kim ◽

Ji-Hyun Song ◽

...

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity ◽

Taraxacum Officinale

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Pancreatic Lipase Inhibitory Alkaloids of Murraya koenigii Leaves

Natural Product Communications ◽

10.1177/1934578x0900400814 ◽

2009 ◽

Vol 4 (8) ◽

pp. 1934578X0900400 ◽

Cited By ~ 10

Author(s):

Rahul Birari ◽

Somendu Kumar Roy ◽

Anubha Singh ◽

Kamlesh Kumar Bhutani

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity ◽

Murraya Koenigii ◽

Etoac Extract ◽

Inhibitory Potential ◽

Pancreatic Lipase Inhibitors ◽

First Time ◽

Carbazole Alkaloids

In the continuing search for newer pancreatic lipase inhibitors from plants, a total of 63 extracts from 21 different plants were screened to study their pancreatic lipase (PL) inhibitory activity in vitro. All three extracts (DCM, EtOAc and MeOH) of Murraya koenigii (L.) Spreng leaves (Rutaceae) exhibited antilipase activity greater than 80%. Further, bioactivity guided fractionation of the EtOAc extract led to the isolation of four alkaloids, namely mahanimbin, koenimbin, koenigicine and clausazoline-K, with IC50 values of 17.9 μM, 168.6 μM, 428.6 μM and ≤500 μM, respectively. This study reports for the first time the PL inhibitory potential of carbazole alkaloids from plants.

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