scholarly journals In Vitro Pancreatic Lipase Inhibition by Marine Fungi Purpureocillium lilacinum Associated with Stylissa sp. Sponge as Anti-obesity Agent

2021 ◽  
Vol 29 (1) ◽  
pp. 76-86
Author(s):  
Wendi Nurul Fadillah ◽  
Nampiah Sukarno ◽  
Dyah Iswantini ◽  
Min Rahminiwati ◽  
Novriyandi Hanif ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Pancreatic Lipase ◽  
Metabolite Identification ◽  
Molecular Characteristics ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Purpureocillium Lilacinum ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

This study aimed to evaluate the potential of marine fungus Purpureocillium lilacinum isolated from an Indonesian marine sponge Stylissa sp. as an anti-obesity agent through pancreatic lipase inhibition assay. The fungus was identified as P. lilacinum through morphological and molecular characteristics. The fungal extract’s inhibition activity and kinetics were evaluated using spectrophotometry and Lineweaver-Burk plots. Ethyl acetate and butanol were used for extraction. Both extracts showed pancreatic lipase inhibition in a concentration-dependent manner. Both crude extracts were then fractionated once. All fractionated extracts showed inhibitory activity above 50%, with the highest activity found in fraction 5 of ethyl acetate at 93.41% inhibition. The best fractionated extract had an IC50value of 220.60 µg.mL-1. The most active fraction of P. lilacinum had a competitive-type inhibitor behavior as shown by the value of Vmax not significantly changing from 388.80 to 382.62 mM pNP.min-1, and the Michaelis-Menten constant (KM) increased from 2.02 to 5.47 mM in the presence of 500 µg.mL-1 fractionated extract. Metabolite identification with LC-MS/MS QTOF suggested that galangin, kaempferol, and quercetin were responsible for the observed lipase inhibition.

scholarly journals In Vitro Antioxidant Capacity and Neuronal Cell Toxicity of Roots of Ostericum koreanum Maximowicz

2011 ◽  
Vol 8 (3) ◽  
pp. 1451-1455
Author(s):  
Ramalingam Mahesh ◽  
Hyo Won Jung ◽  
Jun Hong Park ◽  
Yong-Ki Park
Keyword(s):  
Cell Viability ◽  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Neuronal Cell ◽  
Ethyl Acetate Fraction ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ostericum Koreanum

Ostericum koreanummaximowicz (Umbelliferae), a medicinal herb in Korean Oriental Medicine, has been applied to treat cold, headache, neuralgia and arthralgia. The ethyl acetate fraction ofO. koreanumroot was subjected toin vitroantioxidant activity with different methods for free radical scavenging activities. In addition, the cell viability and nitric oxide release assays were performed here for the first time in neuroblastoma (Neuro-2a) cell cultures. Among all the tested methods, the ethyl acetate fraction was expressed very active, exhibiting a good Trolox equivalent values and IC50, comparable to that of the commercial antioxidants, Trolox and ascorbic acid, respectively. The results showed that there was a reduction of cell viability by the fraction in a concentration dependent manner. These results suggest thatO. koreanumshows good antioxidant activitiesin vitroby inhibiting free radicals. These findings provide a rationale for thein vivotesting. Also, the major constituents behind the antioxidant mechanisms of this fraction warrant further study.

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

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.

scholarly journals Synthesis, Drug Likeness and In-vitro Screening of Some Novel Quinazolinone Derivatives for Anti-Obesity Activity

2021 ◽  
pp. 81-92
Author(s):  
Pratik G. Modh ◽  
Laxman J. Patel
Keyword(s):  
Pancreatic Lipase ◽  
Synthesis Method ◽  
Proton Nmr ◽  
Lipolytic Enzyme ◽  
Coupling Reactions ◽  
Lipinski’S Rule ◽  
High Yields ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

Aim: A series of novel quinazolinone derivates was synthesized and assessed for their ability to inhibitory action on pancreatic lipase. The cyclization of quinazolinone-4(3H)-one derivatives was achieved, whereas carbon-carbon cross coupling reactions were carried out on cyclized quinazolinone-4(3H)-one. This synthesis method afforded corresponding 2, 3 and 6 substituted quinazolin-4(3H)-ones (3a to 3m) with moderate to high yields. Methods: Benzamide derivatives (1a-1b) were synthesized from anthranilic acid using acid-amine reaction, followed by cyclization using catalytic p-toluene sulfonic acid and oxidation using (diacetoxyiodo)benzene to give bromo substituted quinazolin-4(3H)-ones (2a-2b), which were cross coupled to suitable boronic acid using Suzuki-Miyaura condition to obtain desired compound (3a-3m). All synthesized compounds were characterized by FTIR, proton NMR, LC-MS analysis, checked for their drug likeness, absorption and evaluated for in vitro pancreatic lipase inhibition activity. Results: Analytical interpretation of all compounds with infrared, proton NMR and LC-MS spectroscopy confirmed their correct structure. All compounds (3a-3m) show good absorption and have reasonably good molecular properties except 3c and 3m which violate two criteria for Lipinski’s rule. Whereas, Compounds 3l and 3m showed IC50 value of 13.13±0.84 µg/mL and 13.80±1.27 µg/mL respectively comparable to the Orlistat (12.72±0.97µg/mL), a US FDA approved drug for the treatment of obesity. Conclusion: Pancreatic lipase is an important lipolytic enzyme, synthesized and secreted through pancreas, plays an important role in dietary trigycerol absorption and metabolism. Therefore, reducing fat absorption through pancreatic lipase inhibition is a promising strategy to treat obesity. Based upon our findings, compounds 3l and 3m can be further developed as potent anti-obesity agents.

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

2013 ◽  
Vol 8 (2) ◽  
pp. 1934578X1300800 ◽  
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.

scholarly journals Phytochemical Evaluation of Lythrum Salicaria Extracts and Their Effects on Guinea-Pig Ileum

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Tímea Bencsik ◽  
Loránd Barthó ◽  
Viktor Sándor ◽  
Nóra Papp ◽  
Rita Benkó ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Guinea Pig ◽  
Ethyl Acetate ◽  
Water Extract ◽  
Lythrum Salicaria ◽  
Dependent Manner ◽  
Guinea Pig Ileum ◽  
Concentration Dependent Manner ◽  
Ethanol In Water

n-Hexane, chloroform, ethyl acetate and 50% ethanol in water extracts prepared from the air-dried flowering parts of Lythrum salicaria L. were tested for in vitro pharmacological properties on Guinea-pig ileum, which is suitable for detecting a whole range of neuronal and smooth muscle effects. UHPLC-MS was used to evaluate polyphenol components of the extracts. In the ileum, the most prominent response (46.4% related to 0.5 μM histamine) of the extracts causing smooth muscle contractions were triggered by the 50% ethanol in water extract in a concentration-dependent manner. Atropine, indomethacin and PPADS plus suramin significantly reduced the contractile response caused by this extract. The strongest inhibition was due to atropine. The results suggest that L. salicaria extracts have a moderate muscarinic receptor agonist effect in Guinea-pig ileum and that prostanoids and purinoceptor mechanisms are involved to some extent. Therefore diluted extracts of L. salicaria p.o. could be used as a mild stimulant of gastrointestinal motility. The 50% ethanol in water extract was rich in polyphenols. n-Hexane, chloroform and ethyl acetate extracts failed to contain catechin, caffeic acid, quercetin-3-D-galactoside and rutin, but they all showed spasmogenic effects, and, therefore we do not think that these compounds could be involved in the spasmogenic activity.

Antioxidant Activity of Fruits of Perillafrutescens

2014 ◽  
Vol 644-650 ◽  
pp. 5262-5265
Author(s):  
Jing Rong Song ◽  
Gang Lv
Keyword(s):  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Dependent Manner ◽  
Scavenging Activity ◽  
Concentration Dependent Manner ◽  
Dpph Method

The antioxidant activities of extracts and residuum of Perillafrutescens fruits from supercritical CO2 extraction were determined in vitro. The residuum was extracted in turn with water, propyl alcohol and ethyl acetate. The antioxidant activities of the extracts were assayed with antioxidant capacity in linoleic acid model system, reducing powers, radical scavenging activity using 1,1-diphenyl-2-picrylhy-drazyl (DPPH) method. The results show that the ethyl acetate extract of Perillafrutescens possesses strongest DPPH radical scavenging activity and reducing power in a concentration-dependent manner.

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