Xanthones with pancreatic lipase inhibitory activity from the pericarps ofGarcinia mangostanaL. (Guttiferae)

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.

Download Full-text

Anti-Obesity and Gut Microbiota Modulation Effect of Secoiridoid-Enriched Extract from Fraxinus mandshurica Seeds on High-Fat Diet-Fed Mice

Molecules ◽

10.3390/molecules25174001 ◽

2020 ◽

Vol 25 (17) ◽

pp. 4001

Author(s):

Sen Guo ◽

Haoan Zhao ◽

Zhongxiao Ma ◽

Shanshan Zhang ◽

Mingrou Li ◽

...

Keyword(s):

Gut Microbiota ◽

Pancreatic Lipase ◽

Inhibitory Activity ◽

High Fat Diet ◽

Obese Mice ◽

Modulation Effect ◽

Fraxinus Mandshurica ◽

High Fat ◽

Stress Injury ◽

Phytochemical Study

Previously we conducted a phytochemical study on the seeds of Fraxinus excelsior and isolated nine secoiridoid compounds with adipocyte differentiation inhibitory activity and peroxisome proliferator activated receptor alpha (PPARα) activation effects. However, the bioactive constituents and functions of Fraxinus mandshurica seeds have not been studied. In the present study, we investigated the secoiridoid compounds in F. mandshurica seed extract (FM) using column chromatography, 1H-NMR, 13C-NMR and HPLC-DAD methods. The pancreatic lipase inhibitory activities of isolated compounds were evaluated in vitro. Additionally, the anti-obesity and gut microbiota modulation effect of FM on high-fat diet-induced obesity in C57BL/6 mice were also studied in vivo. The results showed that 19 secoiridoids were isolated from FM and identified. The total content of secoiridoids in FM reached 181.35 mg/g and the highest content was nuzhenide (88.21 mg/g). All these secoiridoid compounds exhibited good pancreatic lipase inhibitory activity with inhibition rate ranged from 33.77% to 70.25% at the concentration of 100 μM. After obese mice were administrated with FM at 400 mg/kg.bw for 8 weeks, body weight was decreased by 15.81%. Moreover, FM could attenuate the lipid accumulation in serum and liver, relieve the damage in liver and kidney, and extenuate oxidative stress injury and inflammation caused by obesity in mice. FM could also modulate the structural alteration of gut microbiota in obese mice, increasing the proportion of anti-obesity gut microbiota (Bacteroidetes, Bacteroidia, S24-7 and Allobaculum), and reducing the proportion of obesogenic gut microbiota (Firmicutes and Dorea). This study suggests that F. mandshurica seeds or their secoiridoids may have potential for use as a dietary supplement for obesity management.

Download Full-text

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.

Download Full-text

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.

Download Full-text

Oleanane-type triterpene oligoglycosides with pancreatic lipase inhibitory activity from the pericarps of Sapindus rarak

Phytochemistry ◽

10.1016/j.phytochem.2009.06.015 ◽

2009 ◽

Vol 70 (9) ◽

pp. 1166-1172 ◽

Cited By ~ 44

Author(s):

Toshio Morikawa ◽

Yuanyuan Xie ◽

Yasunobu Asao ◽

Masaki Okamoto ◽

Chihiro Yamashita ◽

...

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity

Download Full-text

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.

Download Full-text