Chlorogenic acid methyl ester exerts strong anti-inflammatory effectsviainhibiting the COX-2/NLRP3/NF-κB pathway

2018 ◽  
Vol 9 (12) ◽  
pp. 6155-6164 ◽  
Author(s):  
Lang Zhang ◽  
Ya Fan ◽  
Hanwen Su ◽  
Li Wu ◽  
Yuying Huang ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Chlorogenic Acid ◽  
Acid Methyl Ester ◽  
Acid Methyl ◽  
Cox 2 ◽  
Anti Inflammatory

In vivoandin vitrostudies show that chlorogenic acid methyl ester (CME) has been proven to be a potential nutraceutical for preventing inflammation.

scholarly journals PPARα/γ, adiponectin and GLUT4 overexpression induced by moronic acid methyl ester influenced on glucose and triglycerides levels of experimental diabetic mice

2021 ◽  
Author(s):  
Samuel Estrada-Soto ◽  
Litzia Cerón-Romero ◽  
Gabriel Navarrete-Vázquez ◽  
Edgar Rosales-Ortega ◽  
Jaime H. Gómez-Zamudio ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Acid Methyl Ester ◽  
Control Group ◽  
Oral Glucose ◽  
Acute Administration ◽  
Diabetic Mice ◽  
Ppar Γ ◽  
Acid Methyl

The current study aimed to determine the antidiabetic and antidyslipidemic activities of moronic acid methyl ester (1) by in vivo, in vitro, in silico and molecular biology studies. Compound 1 was evaluated to establish its dose-dependent antidiabetic and antihyperglycemic (50 mg/kg) activities, in diabetic and normoglycemic male CD1 mice, respectively. Also, compound 1 was subjected to a sub-acute study (50 mg/kg/day for eight days) to determine blood biochemical profiles and the expression of PTP-1B, GLUT4, PPAR-α, PPAR-γ, adiponectin, IL-1β, and MCP1 in adipose tissue of animals after treatment. Different doses in acute administration of 1 decreased glycemia (p < 0.05), compared with vehicle, showing greater effectiveness in the range 50-160 mg/kg. Also, the oral glucose tolerance test (OGTT) showed that 1 induced a significant antihyperglycemic action by opposing the hyperglycemic peak (p < 0.05). Moreover, 1 subacute administration decrease glucose and triglycerides levels after treatment (p < 0.05); while the expression of PPAR-α and γ, adiponectin and GLUT4 displayed an increase (p< 0.05) compared with the diabetic control group. In conclusion, compound 1 showed antihyperglycemic, antidiabetic and antidyslipidemic effects in normal and diabetic mice, probably due to insulin sensitization through increase mRNA expression of GLUT4, PPAR-α, PPAR-γ and adiponectin genes.

scholarly journals Bioactive Variability and In Vitro and In Vivo Antioxidant Activity of Unprocessed and Processed Flour of Nine Cultivars of Australian lupin Species: A Comprehensive Substantiation

Antioxidants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 282 ◽  
Author(s):  
Kishor Mazumder ◽  
Afia Nabila ◽  
Asma Aktar ◽  
Asgar Farahnaky
Keyword(s):  
Antioxidant Activity ◽  
Methyl Ester ◽  
Bioactive Compounds ◽  
Antioxidant Activities ◽  
Acid Methyl Ester ◽  
Heat Processing ◽  
Acid Methyl ◽  
Ms Analysis

The aim of this present investigation was to analyze bioactive compounds, as well as demonstrate the antioxidant activities of nine cultivars of Australian lupin species accompanied by observing the effect of domestic heat processing on their antioxidant activities adopting in vivo and in vitro approaches. Gas chromatography mass spectroscopy (GC-MS) analysis was performed for profiling bioactive compounds present in lupin cultivars. Multiple assay techniques involving quantification of polyphenolics, flavonoids and flavonol, electron transfer (ET) based assay, hydrogen atom transfer (HAT)-based assay and in vivo assays were performed. The major compounds found were hexadecanoic acid methyl ester, 9,12-octadecadienoic acid methyl ester, methyl stearate, lupanine,13-docosenamide and 11-octadecenoic acid (Z)- methyl ester. Mandelup was found to show excellent antioxidant activity. Moreover, Jurien, Gunyidi and Barlock had strong antioxidant activity. Both positive and negative impacts of heat processing were observed on antioxidant activity. Heating and usage of excess water during processing were the key determinants of loss of antioxidants. Negligible loss of antioxidant activity was observed in most of the assays whereas inhibition of both lipid peroxidation (33.53%) and hemolysis of erythrocytes (37.75%) were increased after processing. In addition, in vitro and in vivo antioxidant assays are found to show statistically significant (* p < 0.05 and ** p < 0.01) results, which are supported by the presence of a number of antioxidant compounds in GC-MS analysis.

scholarly journals Comparison of in vitro and in vivo phototoxicity tests with S-(−)-10,11-dihydroxyfarnesic acid methyl ester produced by Beauveria bassiana KACC46831

2014 ◽  
Vol 2 (5) ◽  
pp. 659-663
Author(s):  
MIN-A KIM ◽  
HYEONG-U SON ◽  
CHEOL-SIK YOON ◽  
SUNG-HEE NAM ◽  
YOUNG-CHEOL CHOI ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Beauveria Bassiana ◽  
Acid Methyl Ester ◽  
Acid Methyl

Anti-angiogenic activity of para-coumaric acid methyl ester on HUVECs in vitro and zebrafish in vivo

Phytomedicine ◽  
2018 ◽  
Vol 48 ◽  
pp. 10-20 ◽  
Author(s):  
He-Zhong Zhang ◽  
Chong-Yong Li ◽  
Jia-Qi Wu ◽  
Rui-Xue Wang ◽  
Ping Wei ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Acid Methyl Ester ◽  
Coumaric Acid ◽  
Angiogenic Activity ◽  
Acid Methyl

2,5-disubstituted-4-thiazolidinones: Synthesis, anti-inflammatory, free radical scavenging potentials and structural insights through molecular docking

2021 ◽  
Vol 18 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A Chawla ◽  
Rohit Bhatia ◽  
Shamsher Singh
Keyword(s):  
Free Radicals ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Assay Method ◽  
Acidic Group ◽  
Active Compounds ◽  
Cox 2 ◽  
Anti Inflammatory

: The present work reports synthesis and screening of fifteen 2,5-disubstituted-4-thiazolidinones with different substitutions of varied arylidene groups at imino. The structures of the compounds were confirmed by spectral characterization. The compounds were subjected to in vivo anti-inflammatory and in vitro antioxidant activities. The derivatives possessed remarkable activities quite close to standard drugs used. Unlike conventional non-selective NSAIDs, the synthesized compounds did not contain any acidic group, thereby ensuring a complete cure from ulcers. To further substantiate the claim for safer derivatives, the active compounds were docked against the cyclooxygenase (COX)-2 enzyme. It was found that 4-fluorophenylimino substituent at 2- position and 3-nitro moiety on a 5-benzylidene nucleus of the 4-thiazolidinone derivative fitted in the COX-2 binding pocket. The compounds exhibited remarkable activity in scavenging free radicals, as depicted by the DPPH assay method. The structure-activity relationship was also established in the present work with respect to the nature and position of the substituents. The active compounds were evaluated for drug-like nature under Lipinski’s rule of five, and the toxicity behaviour of active compounds was predicted using ADMETlab software. The compounds have the potential to target degenerative disorders associated with inflammation and the generation of free radicals.

scholarly journals Natural Products from Scorzonera aristata (Asteraceae)

2010 ◽  
Vol 5 (5) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Manuela Jehle ◽  
Johanna Bano ◽  
Ernst P. Ellmerer ◽  
Christian Zidorn
Keyword(s):  
Natural Products ◽  
Methyl Ester ◽  
Chlorogenic Acid ◽  
Caffeic Acid ◽  
Acid Methyl Ester ◽  
Quinic Acid ◽  
The South ◽  
Caffeic Acid Derivatives ◽  
Aerial Parts ◽  
Acid Methyl

The aerial parts of Scorzonera aristata Ramond ex DC., collected in the South Tyrolean Dolomites, yielded the flavonoids quercetin 3- O-glucoside, rutin, and isoorientin, and the caffeic acid derivatives chlorogenic acid, 4,5-dicaffeoyl quinic acid, and 3,5-dicaffeoyl quinic acid. Sub-aerial parts contained caffeic acid methyl ester, 3,5-dicaffeoyl quinic acid, and the triterpenes 3α-hydroxyolean-5-ene, lupeol, and magnificol. Chemosystematic implications of the isolated compounds are discussed briefly.

scholarly journals Synthesis and Antiproliferative Evaluation of Novel Hybrids of Dehydroabietic Acid Bearing 1,2,3-Triazole Moiety

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4191 ◽  
Author(s):  
Fang-Yao Li ◽  
Lin Huang ◽  
Qian Li ◽  
Xiu Wang ◽  
Xian-Li Ma ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Parent Compound ◽  
Acid Methyl Ester ◽  
Normal Liver ◽  
Dehydroabietic Acid ◽  
In Vitro Cytotoxicity ◽  
Human Carcinoma ◽  
Normal Liver Cell ◽  
Acid Methyl

To discover novel potent cytotoxic diterpenoids, a series of hybrids of dehydroabietic acid containing 1,2,3-triazole moiety were designed and synthesized. The target compounds were characterized by means of FT-IR, 1H NMR, 13C NMR, ESI-MS and elemental analysis techniques. The in vitro cytotoxicity of these compounds was evaluated by standard MTT (methyl thiazolytetrazolium) assay against CNE-2 (nasopharynx), HepG2 (liver), HeLa (epithelial cervical), BEL-7402 (liver) human carcinoma cell lines and human normal liver cell (HL-7702). The screening results revealed that most of the hybrids showed significantly improved cytotoxicity over parent compound DHAA. Among them, [1-(3-fluorobenzyl)-1H-1,2,3-triazole-4-yl]dehydroabietic acid methyl ester (3c), and [1-(2-nitrobenzyl)-1H-1,2,3-triazole-4-yl]dehydroabietic acid methyl ester (3k) displayed better antiproliferative activity with IC50 (50% inhibitory concentration) values of 5.90 ± 0.41 and 6.25 ± 0.37 µM toward HepG2 cells compared to cisplatin, while they exhibited lower cytotoxicity against HL-7702. Therefore, the 1,2,3-triazole-hybrids could be a promising strategy for the synthesis of antitumor diterpenoids and it also proved the essential role of 1,2,3-triazole moiety of DHAA in the biological activity.

scholarly journals Characterization of Phenolic Constituents from Prunus cerasifera Ldb Leaves

2020 ◽  
Vol 2020 ◽  
pp. 1-5
Author(s):  
Wei Liu ◽  
Muhammad Farrukh Nisar ◽  
Chunpeng Wan
Keyword(s):  
Methyl Ester ◽  
Ethyl Acetate ◽  
Chlorogenic Acid ◽  
Acid Methyl Ester ◽  
Chemical Compositions ◽  
Preparative Hplc ◽  
Caffeoylquinic Acid ◽  
Prunus Cerasifera ◽  
Acid Methyl ◽  
Phenolic Constituents

To elucidate the chemical compositions of Prunus cerasifera Ldb leaves, the methanol extracts were firstly fractionated by ethyl acetate and n-butanol, respectively. The phenolic acid-rich fractions (ethyl acetate extracts) were further isolated by various chromatographic columns (CC) including MCI macroporous resin, normal-phase silica gel, Sephadex gel LH-20, octadecyl silane (ODS), and preparative HPLC to yield the phenolic compounds. The isolated compounds were analyzed by 1H-nuclear magnetic resonance (1H-NMR), 13C-NMR, and electrospray ionization mass spectral (ESI-MS) spectroscopy. Eleven phenolic acids were identified as p-coumaric acid (1), caffeic acid (2), ferulic acid (3), chlorogenic acid (4), 3-O-caffeoylquinic acid (5), 5-O-coumaroylquinic acid (6), 3-O-caffeoylquinic acid methyl ester (7), chlorogenic acid methyl ester (8), 3-O-caffeoyl-5-O-coumaroylquinic acid or 3-O-coumaroyl-5-O-caffeoylquinic acid (9), gallic acid (10), and protocatechuic acid (11). The current study pioneers to identify and report all the phenolic constituents from P. cerasifera Ldb leaves.

scholarly journals Rationally synthesized coumarin based pyrazolines ameliorate carrageenan induced inflammation through COX-2/pro-inflammatory cytokine inhibition

MedChemComm ◽  
2019 ◽  
Vol 10 (3) ◽  
pp. 421-430 ◽  
Author(s):  
Priyanka Chandel ◽  
Anoop Kumar ◽  
Nishu Singla ◽  
Anshul Kumar ◽  
Gagandeep Singh ◽  
...  
Keyword(s):  
Inflammatory Cytokine ◽  
Cytokine Inhibition ◽  
Cox 2 ◽  
Anti Inflammatory

In the present work, coumarin based pyrazolines (7a–g) have been synthesized and investigated for their in vitro and in vivo anti-inflammatory potential.

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