scholarly journals Activity-Guided Characterization of COX-2 Inhibitory Compounds in Waltheria indica L. Extracts

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7240
Author(s):  
Michael Termer ◽  
Christophe Carola ◽  
Andrew Salazar ◽  
Cornelia M. Keck ◽  
Juergen Hemberger ◽  
...  

Inflammation is the body’s response to infection or tissue injury in order to restore and maintain homeostasis. Prostaglandin E2 (PGE-2) derived from arachidonic acid (AA), via up-regulation of cyclooxygenase-2 (COX-2), is a key mediator of inflammation and can also be induced by several other factors including stress, chromosomal aberration, or environmental factors. Targeting prostaglandin production by inhibiting COX-2 is hence relevant for the successful resolution of inflammation. Waltheria indica L. is a traditional medicinal plant whose extracts have demonstrated COX-2 inhibitory properties. However, the compounds responsible for the activity remained unknown. For the preparation of extracts with effective anti-inflammatory properties, characterization of these substances is vital. In this work, we aimed to address this issue by characterizing the substances responsible for the COX-2 inhibitory activity in the extracts and generating prediction models to quantify the COX-2 inhibitory activity without biological testing. For this purpose, an extract was separated into fractions by means of centrifugal partition chromatography (CPC). The inhibitory potential of the fractions and extracts against the COX-2 enzyme was determined using a fluorometric COX-2 inhibition assay. The characterizations of compounds in the fractions with the highest COX-2 inhibitory activity were conducted by high resolution mass spectrometry (HPLC-MS/MS). It was found that these fractions contain alpha-linolenic acid, linoleic acid and oleic acid, identified and reported for the first time in Waltheria indica leaf extracts. After analyzing their contents in different Waltheria indica extracts, it could be demonstrated that these fatty acids are responsible for up to 41% of the COX-2 inhibition observed with Waltheria indica extract. Additional quantification of secondary metabolites in the extract fractions revealed that substances from the group of steroidal saponins and triterpenoid saponins also contribute to the COX-2 inhibitory activity. Based on the content of compounds contributing to COX-2 inhibition, two mathematical models were successfully developed, both of which had a root mean square error (RMSE) = 1.6% COX-2 inhibitory activity, demonstrating a high correspondence between predicted versus observed values. The results of the predictive models further suggested that the compounds contribute to COX-2 inhibition in the order linoleic acid > alpha linolenic acid > steroidal saponins > triterpenoid saponins. The characterization of substances contributing to COX-2 inhibition in this study enables a more targeted development of extraction processes to obtain Waltheria indica extracts with superior anti-inflammatory properties.

2021 ◽  
Author(s):  
Masoomeh Zeinalzadegan ◽  
Maryam Nejadmansouri ◽  
Mohammad-Taghi Golmakani ◽  
Gholam Reza Mesbahi ◽  
David Julian McClements ◽  
...  

2020 ◽  
Vol 98 (3) ◽  
Author(s):  
Yeqing Q Li ◽  
Yumeng M Xi ◽  
Zedong D Wang ◽  
Hanfang F Zeng ◽  
Zhaoyu Han

Abstract Feed intake is a major factor in maintaining the balance between ruminal fermentation and the microbial community of dairy cows. To explore the relationship among feed intake, microbial metabolism, and ruminal fermentation, we examined the combined signatures of the microbiome and metabolome in dairy cows with different feed intake levels. Eighteen dairy cows were allocated to high feed intake (HFI), medium feed intake (MFI), and low feed intake (LFI) groups according to their average daily feed intake. 16S rDNA sequencing results revealed that the relative abundance of Firmicutes in the HFI group was significantly higher than that in the MFI and LFI groups (P < 0.05). The ratio of Bacteroidetes to Firmicutes was significantly lower in the HFI group than in the MFI and LFI groups (P < 0.05). The relative abundance of Lachnospiraceae_unclassified, Veillonellaceae_unclassified, and Saccharofermentants was significantly higher in the HFI group than in the LFI and MFI groups (P < 0.05). The relative abundance of Erysipelotrichaceae_unclassified and Butyrivibrio was significantly higher in the HFI group than in the MFI and LFI groups (P < 0.05). Ultra high performance liquid chromatography-mass spectrometry revealed five key pathways, including the linoleic acid metabolism pathway, alpha-linolenic acid metabolism, arginine and proline metabolism, glutathione metabolism, and valine, leucine, and isoleucine biosynthesis, which are closely related to energy and amino acid metabolism. Linoleic acid, glutamate, alpha-linolenic acid, l-methionine, and l-valine levels were significantly lower in the HFI group than in the MFI and LFI groups (q < 0.05), while the relative content of glutamate was significantly lower in the MFI group than in the LFI group (q < 0.05). Stearic acid content was significantly higher in the HFI group than in the LFI group (q < 0.05). Our findings provide insight into the rumen microbiome of dairy cows with different feed intake and the metabolic pathways closely associated with feed intake in early-lactating cows. The candidates involved in these metabolic pathways may be useful for identifying variations in feed intake. The signatures of the rumen microbiome and metabolome in dairy cows may help make decisions regarding feeding.


2019 ◽  
Vol 16 (1) ◽  
Author(s):  
Sally A. V. Draycott ◽  
Ge Liu ◽  
Zoe C. Daniel ◽  
Matthew J. Elmes ◽  
Beverly S. Muhlhausler ◽  
...  

2020 ◽  
Author(s):  
Khaled R. A. Abdellatif ◽  
Eman K. A. Abdelall ◽  
Heba A. H. Elshemy ◽  
El‐Shaymaa El‐Nahass ◽  
Maha M. Abdel‐Fattah ◽  
...  

2008 ◽  
Vol 52 (No. 7) ◽  
pp. 203-213 ◽  
Author(s):  
D. Schneideroá ◽  
J. Zelenka ◽  
E. Mrkvicová

We studied the effect of different levels of linseed oils made either of the flax cultivar Atalante with a high content of &alpha;-linolenic acid (612 g/kg) or of the cultivar Lola with a predominating content of linoleic acid (708 g/kg) in a chicken diet upon the fatty acid pattern in meat. Cockerels Ross 308 were fed the diets containing 1, 3, 5 or 7 per cent of oil in the last 15 days of fattening. Breast meat (BM) and thigh meat (TM) without skin of 8 chickens from each dietary group were used for analyses. The relative proportions of fatty acids were expressed as percentages of total determined fatty acids. When feeding Atalante oil, the proportions of n-6 fatty acids were highly significantly lower while those of n-3 fatty acids were higher; the ratio of n-6/n-3 polyunsaturated fatty acids in meat was narrower (<i>P</i> < 0.001) than in chickens fed oil with a low content of &alpha;-linolenic acid. In BM and TM, the relative proportions of &alpha;-linolenic and &gamma;-linolenic acids were nearly the same, the proportion of linoleic acid in BM was lower, and the proportions of the other polyunsaturated fatty acids in BM were higher than in TM. In BM, the ratio of n-6/n-3 polyunsaturated fatty acids was significantly (<i>P</i> < 0.001) more favourable than that found in TM. The relative proportions of total saturated and monounsaturated fatty acids in meat decreased and those of polyunsaturated fatty acids increased significantly (<i>P</i> < 0.01) in dependence on the increasing level of dietary oils. When feeding Atalante oil, a significant increase in the proportion of linoleic acid in BM but not in TM was observed. The proportions of the other n-6 fatty acids decreased and those of all determined n-3 fatty acids, with the exception of docosahexaenoic acid, significantly increased with the increasing level of oil in the diet. When feeding Lola oil, its increasing content in the diet increased the relative proportion of linoleic acid as well as its elongation to &gamma;-linolenic acid; however, the proportions of arachidonic and adrenic acid did not change significantly (<i>P</i> > 0.05). The proportion of &alpha;-linolenic acid increased in both BM and TM. The proportion of eicosapentaenoic and clupanodonic acids in BM significantly decreased. The ratio of n-6 to n-3 polyunsaturated fatty acids ranged from 0.9 to 13.6 and from 1.0 to 17.2 in BM and TM, respectively. An increase in the level of Lola oil in the diet by 1% caused that the n-6/n-3 polyunsaturated fatty acid ratio extended by 1.00 and 1.19 units in BM and TM, respectively. Dependences of n-6/n-3 ratio on the level of Atalante oil were expressed by equations of convex parabolas with minima at the level of oil 5.8 and 5.9% for BM and TM, respectively. By means of the inclusion of linseed oil with a high content of &alpha;-linolenic acid in the feed mixture it would be possible to produce poultry meat as a functional food with a very narrow ratio of n-6/n-3 polyunsaturated fatty acids.


2005 ◽  
Vol 85 (3) ◽  
pp. 413-416 ◽  
Author(s):  
F. B. Cavalieri ◽  
G. T. Santos ◽  
M. Matsushita ◽  
H. V. Petit ◽  
L. P. Rigolon ◽  
...  

Cows were fed whole flaxseed or calcium salts of soybean oil as a fat source. Cows fed flaxseed had lower (P < 0.01) milk yield and higher (P < 0.01) percentages of fat and protein than cows fed calcium salts. Feeding whole flaxseed and calcium salts of soybean oil increased, respectively, the concentrations of alpha-linolenic acid and conjugated linoleic acid in milk. Key words: Flaxseed, fatty acids, fat supplement


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