Caffeic Acid Derivatives from Bacopa monniera Plants as Inhibitors of Pancreatic Lipase Activity and their Structural Requirements

The methanol extract of whole Bacopa monniera plants inhibited pancreatic lipase activity in vitro. From this extract we have reported the isolation of 11 triterpene glycosides and 5 phenylethanoid- and/or phenylpropanoid- glycosides. In this paper, we describe the effects of the methanol extract and/or its constituents on pancreatic lipase activity and the isolation of an active constituent, desrhamnosyl isoacteoside. In addition, the structural requirements for its inhibitory effects were examined. We also examined the effects on the elevation of plasma triglyceride (TG) levels in olive oil loaded mice. The major active constituents, desrhamnosyl isoacteoside and plantainoside B, reduced plasma TG levels in the mice. The inhibitory effects of B. monniera and its constituents on pancreatic lipase activity and plasma TG level are reported for the first time.

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The Effects of Cordyceps sinensis (Berk.) Sacc. and Gymnema inodorum (Lour.) Decne. Extracts on Adipogenesis and Lipase Activity In Vitro

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2019/5370473 ◽

2019 ◽

Vol 2019 ◽

pp. 1-13 ◽

Cited By ~ 2

Author(s):

Kanokwan Tiamyom ◽

Kittipot Sirichaiwetchakoon ◽

Tanaporn Hengpratom ◽

Sajeera Kupittayanant ◽

Rungrudee Srisawat ◽

...

Keyword(s):

Pancreatic Lipase ◽

Lipase Activity ◽

Lipid Accumulation ◽

Acyl Chain ◽

Principal Component ◽

Cordyceps Sinensis ◽

Dependent Manner ◽

Inhibitory Effects ◽

Ftir Microspectroscopy

This study aimed to investigate the effects of Cordyceps sinensis extract (CSE) and Gymnema inodorum extract (GIE), used alone and combined, on antiadipogenesis in 3T3-L1 cells. Oil Red O staining was used to examine the effects of these extracts on inhibition of intracellular lipid accumulation in 3T3-L1 adipocytes and on lipid droplet morphology. Fourier transform-infrared (FTIR) microspectroscopy was used to examine biomolecular changes in 3T3-L1 adipocytes. The pancreatic lipase assay was used to evaluate the inhibitory effects of CSE and GIE on pancreatic lipase activity. Taken together, the results indicated that CSE, GIE, and their combination suppressed lipid accumulation. The FTIR microspectroscopy results indicated that CSE, GIE, and their combination had inhibitory effects on lipid accumulation in the adipocytes. Compared with the untreated adipocytes, the signal intensity and integrated areas of glycogen and other carbohydrates, the acyl chain of phospholipids, and the lipid/protein ratios of the CSE, GIE, alone, and combined treated adipocytes were significantly lower (p < 0.05). Combination treatment resulted in a synergistic effect on lipid accumulation reduction in the adipocytes. Principal component analysis of the biomolecular changes revealed six distinct clusters in the FTIR spectra of the sample cells. The pancreatic lipase assay results indicated that CSE and GIE inhibited the pancreatic lipase activity in a dose-dependent manner (mean ± standard error of the mean IC50 values, 2312.44 ± 176.55 μg mL−1 and 982.24 ± 44.40 μg mL−1, resp.). Our findings indicated that FTIR microspectroscopy has potential application for evaluation of the effectiveness of medicinal plants and for the development of infrared biochemical obesity markers useful for treating patients with obesity. These results suggested that use of CSE and GIE alone and in combination may be efficacious as a complementary therapy for hyperlipidemia and obesity management. However, clinical trials in animals and humans must first be completed.

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In vitro Antidiabetic, anti-obesity and antioxidant proprities of Rosemary extracts

JOURNAL OF ADVANCES IN CHEMISTRY ◽

10.24297/jac.v10i2.5497 ◽

2014 ◽

Vol 10 (2) ◽

pp. 2305-2316 ◽

Cited By ~ 4

Author(s):

Manel Ben Ali ◽

Kais Mnafgui ◽

Abdelfattah Feki ◽

Mohamed Damak ◽

Noureddine Allouche

Keyword(s):

Essential Oil ◽

Ethyl Acetate ◽

Pancreatic Lipase ◽

Antioxidant Properties ◽

Methanolic Extracts ◽

Ic50 Values ◽

Inhibitory Potential ◽

Prevention Of Diabetes ◽

First Time

Diabetes mellitus is a serious health problem worldwide that has adverse and long-lasting consequences for individuals, families, and communities. Hence, this study sought to investigate the inhibitory potential of rosemary extracts on key-enzymes related to diabetes such as α-amylase and pancreatic lipase activities, as well as to assess their antioxidant properties in vitro. The IC50 values of Rosemary essential oil, ethyl acetate and methanolic extracts against α-amylase were 28.36, 34.11 and 30.39 µg/mL respectively, and those against pancreatic lipase were 32.25, 36.64 and 34.07 µg/mL, suggesting strong anti-diabetic and anti-obesity effects of Rosemary. The methanolic extract was found to be the highest in levels of phenolic (282.98 µgGAE/mg extract) and flavonoids (161.05 µg QE /mg extract) contents as well as in the antioxidant activity (IC50 = 15.82 µg/mL) as compared to other extracts ethyl acetate (IC50 = 32.23 µg/mL) and essential oil (IC50 = 96.12 µg/mL).Antioxidant efficacy of Rosemary extracts has been estimated in the stabilization of sunflower oil (SFO) at three different concentrations, i.e. 200 (SFO-200), 500 (SFO-500) and 1000 ppm (SFO-1000). Results showed the highest efficiency of SFO-1000.The results obtained in this study demonstrated for the first time that Rosemary is a potent source of natural inhibitors of α-amylase and pancreatic lipase with powerful antioxidants proprieties that might be used in the food stabilization and the prevention of diabetes and obesity complications as a complementary pharmacological drug.

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In Vitro and In Vivo α-Glucosidase and α-Amylase Inhibitory Effects of the Water Extract of Leaves of Pepper (Capcicum Annuum L. Cultivar Dangjo ) and the Active Constituent Luteolin 7-O-Glucoside

Journal of Food Biochemistry ◽

10.1111/jfbc.12252 ◽

2016 ◽

Vol 40 (5) ◽

pp. 696-703 ◽

Cited By ~ 4

Author(s):

Mi-Sung Park ◽

Ya Xin Zhu ◽

Hyun-Ock Pae ◽

Seong Hoon Park

Keyword(s):

Water Extract ◽

Inhibitory Effects ◽

Active Constituent

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New pregnane glycosides from Caralluma hexagona Lavranos and their in vitro α-glucosidase and pancreatic lipase inhibitory effects

Phytochemistry Letters ◽

10.1016/j.phytol.2020.01.015 ◽

2020 ◽

Vol 36 ◽

pp. 49-57

Author(s):

Akram A. Shalabi ◽

Ali M. El Halawany ◽

Mouchira A. Choucry ◽

Fatma S. El-Sakhawy ◽

Hiroyuki Morita ◽

...

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Effects

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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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Antioxidant and pancreatic lipase inhibitory effects of flavonoids from different citrus peel extracts: An in vitro study

Food Chemistry ◽

10.1016/j.foodchem.2020.126785 ◽

2020 ◽

Vol 326 ◽

pp. 126785 ◽

Cited By ~ 3

Author(s):

Rui Huang ◽

Yu Zhang ◽

Shuyu Shen ◽

Zijian Zhi ◽

Huan Cheng ◽

...

Keyword(s):

Pancreatic Lipase ◽

In Vitro Study ◽

Vitro Study ◽

Inhibitory Effects ◽

Citrus Peel

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IN VITRO ANTI-OBESITY EFFECT OF MACROLICHENS HETERODERMIA LEUCOMELOS AND RAMALINA CELASTRI BY PANCREATIC LIPASE INHIBITORY ASSAY

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i5.13560 ◽

2017 ◽

Vol 9 (5) ◽

pp. 137

Author(s):

Rashmi Shivanna ◽

Hengameh Parizadeh ◽

Rajkumar H. Garampalli

Keyword(s):

Ethyl Acetate ◽

Pancreatic Lipase ◽

Methanol Extract ◽

Well Being ◽

Inhibitory Effect ◽

Potential Effect ◽

Protective Role ◽

Treatment Of Obesity ◽

Molecular Sequencing

Objective: Obesity is a chronic disorder caused by an imbalance between energy intake and expenditure in which excessive fat will be deposited in adipose tissue and poses a risk to the health and well-being of humans. Agents which inhibit pancreatic lipase play an important role in the treatment of obesity. The aim of this study was to assess the potential effect of macro lichens Heterodermia leucomelos (L.) Poelt a foliose lichen and Ramalina celastri (Sprengel) Krog and Swinscow a fruticose lichen in the treatment of obesity.Methods: In vitro anti-obesity inhibitory effect of macro lichens were evaluated by using chicken pancreatic lipase activity. Lipase was extracted from the chicken pancreas. Different concentrations from 5-25 mg/ml of methanol and ethyl acetate extracts of lichens Heterodermia leucomelos and Ramalina celastri was incubated with pancreas lipase.Results: With the increase in the concentration of extracts the higher inhibition of the enzyme was observed. Solvent methanol showed good activity compared to ethyl acetate. Percentage of inhibition ranged from 19.7-69.8 and 20.0-86.6 % in the methanol extract of Heterodermia leucomelos and Ramalina celastri respectively. Comparatively lichen Ramalina celastri in methanol extract showed maximum inhibition of 86.6 %, whereas ethyl acetate showed an inhibition of 63.0% at 25 mg/ml against enzyme lipase.Conclusion: In the present study, the inhibitory activity of lichen indicates its protective role in treating obesity. Molecular sequencing of this lichen helps in future to determine the various metabolic pathways that are responsible for the production of novel compounds.

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Inhibitory Activity of Benzophenones from Anemarrhena asphodeloides on Pancreatic Lipase

Natural Product Communications ◽

10.1177/1934578x1300800419 ◽

2013 ◽

Vol 8 (4) ◽

pp. 1934578X1300800 ◽

Cited By ~ 2

Author(s):

Yang Hee Jo ◽

Seon Beom Kim ◽

Jong Hoon Ahn ◽

Qing Liu ◽

Bang Yeon Hwang ◽

...

Keyword(s):

Pancreatic Lipase ◽

Lipase Activity ◽

Soluble Fraction ◽

Significant Inhibition ◽

Dietary Fats ◽

Lipid Absorption ◽

Vitro Assay ◽

Key Enzyme ◽

Anemarrhena Asphodeloides

Pancreatic lipase is a key enzyme for lipid absorption by hydrolysis of total dietary fats. Therefore, inhibition of pancreatic lipase is suggested to be an effective therapy in the regulation of obesity. The EtOAc-soluble fraction of Anemarrhena asphodeloides rhizomes significantly inhibited pancreatic lipase activity as assessed using porcine pancreatic lipase as an in vitro assay system. Further fractionation of the EtOAc-soluble fraction of A. asphodeloides led to the isolation of a new benzophenone glycoside, zimoside A (1), together with the eleven known compounds iriflophenone (2), 2,4′,6-trihydroxy-4-methoxybenzophenone (3), foliamangiferoside A (4), (2,3-dihydroxy-4-methoxyphenyl)(4-hydroxyphenyl)-methanone (5), 1,4,5,6,-tetrahydroxyxanthone (6), isosakuranetin (7), 4-hydroxybenzoic acid (8), 4-hydroxyacetophenone (9), vanillic acid (10), tyrosol (11) and 5-hydroxymethyl-2-furaldehyde (12). Among the isolated compounds, 3, 5 and 10 showed significant inhibition of pancreatic lipase activity.

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