scholarly journals Scrophularia Tenuipes Coss and Durieu: Phytochemical Composition and Biological Activities

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1647
Author(s):  
Zeyneb Chaibeddra ◽  
Salah Akkal ◽  
Houria Ouled-Haddar ◽  
Artur M. S. Silva ◽  
Ammar Zellagui ◽  
...  

Scrophularia tenuipes is an Algerian-Tunisian endemic species, which has not been studied yet. Ethyl acetate (EA) and n-butanol (Bu) fractions obtained from Scrophularia tenuipes were investigated for their health benefit properties, in particular with respect to in vivo/in vitro anti-inflammatory and antioxidant activities, as well as their potential to inhibit key enzymes with impact in diabetes (α-glucosidase and α-amylase). The fractions had a distinct phytochemical composition, of which EA was richer in total phenolic compounds (225 mg GAE/g) and mostly composed of the phenylethanoid acetyl martynoside. Compared to EA, Bu had higher amounts of total flavonoids, and according to the result obtained from UHPLC-DAD-ESI-MSn analysis, harpagoside (iridoid) was its major phytochemical. EA fraction was quite promising with regard to the in vivo (at 200 mg/kg, po) anti-inflammatory effect (62% and 52% for carrageenan-induced rat paw edema and xylene-induced ear edema tests, respectively), while Bu fraction exhibited a stronger antioxidant capacity in all tests (IC50 = 68 µg/mL, IC50 = 18 µg/mL, IC50 = 18 µg/mL and A0.50 = 43 µg/mL for DPPH●, ABTS•+, O2•− scavenging assays and cupric-reducing antioxidant capacity method, respectively). Both fractions also showed a strong effect against α-amylase enzyme (IC50 = 8 µg/mL and 10 µg/mL for EA and Bu fraction, respectively).

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4411 ◽  
Author(s):  
Olympia Kouzi ◽  
Eleni Pontiki ◽  
Dimitra Hadjipavlou-Litina

Indandiones are a relatively new group of compounds presenting a wide range of biological activities. The synthesis of these compounds was performed via a Knoevenagel reaction between an aldehyde and 1,3-indandione and were obtained with a yield up to 54%. IR, 1H-Nucleic Magnetic Resonance (NMR), 13C-NMR, LC/MS ESI+ and elemental analysis were used for the confirmation of the structures of the novel derivatives. Lipophilicity values of compounds were calculated theoretically and experimentally by reversed chromatography method as values RM. The novel derivatives were studied through in vitro and in vivo experiments for their activity as anti-inflammatory and antioxidant agents and as inhibitors of lipoxygenase, trypsin, and thrombin. The inhibition of the carrageenin-induced paw edema (CPE) was also determined for representative structures. In the above series of experiments, we find that all the compounds showed moderate to satisfying interaction with the stable DPPH free radical in relation to the concentration and the time 2-arylidene-1-indandione (10) was the strongest. We observed moderate or very low antioxidant activities for selected compounds in the decolorization assay with ABTS+•. Most of the compounds showed high anti-lipid peroxidation of linoleic acid induced by AAPH.2-arylidene-1-indandione (7) showed a strongly inhibited soybean LOX. Only 2-arylidene-1-indandione (3) showed moderate scavenging activity of superoxide anion, whereas 2-arylidene-1-indandione (8) and 2-arylidene-1-indandione (9) showed very strong inhibition on proteolysis. 2-arylidene-1-indandione (8) highly inhibited serine protease thrombin. 2-arylidene-1-indandiones (7, 8 and 9) can be used as lead multifunctional molecules. The compounds were active for the inhibition of the CPE (30–57%) with 2-arylidene-1-indandione (1) being the most potent (57%). According to the predicted results a great number of the derivatives can cross the Blood–Brain Barrier (BBB), act in CNS and easily transported, diffused, and absorbed. Efforts are conducted a) to correlate quantitatively the in vitro/in vivo results with the most important physicochemical properties of the structural components of the molecules and b) to clarify the correlation of actions among them to propose a possible mechanism of action. Hydration energy as EHYDR and highest occupied molecular orbital (HOMO) better describe their antioxidant profile whereas the lipophilicity as RM values governs the in vivo anti-inflammatory activity. Docking studies are performed and showed that soybean LOX oxidation was prevented by blocking into the hydrophobic domain the substrates to the active site.


2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Maria Lúcia da Silva Cordeiro ◽  
Ana Raquel Carneiro Ribeiro ◽  
Luciana Fentanes Moura de Melo ◽  
Lucas Felipe da Silva ◽  
Gabriel Pereira Fidelis ◽  
...  

Commiphora leptophloeos is widely used in folk medicine without any scientific basis. Considering this, the aim of this study was to evaluate the chemical profile and the antioxidant activity of C. leptophloeos leaf extracts using in vitro and in vivo assays. Six extracts were obtained from fresh leaves using a serial extraction (nonpolar to polar solvents). These extracts were first evaluated with the presence of phytochemical compounds using the methods thin layer chromatography (TLC), ultrahigh performance liquid chromatography (UHPLC-DAD), and high performance liquid chromatography, both with diode array detection (HPLC-DAD). Based on the compounds identified, it was used some bioinformatics tools in order to identify possible pathway and gene targets. After that, the antioxidant capacity from these extracts was analysed by in vitro assays and in vivo assays using Caenorhabditis elegans model. Phytochemical analyses showed the presence of polyphenols, such as rutin, vitexin, and quercetin diglycosides in all extracts, especially in ethanol extract (EE) and methanol extract (EM). Bioinformatics analysis showed these polyphenols linked to antioxidant pathways. Furthermore, EE and EM displayed a high antioxidant capacity in DPPH and superoxide radical scavenging assays. They also had no effect on cell viability for 3T3 nontumour cell. However, for B16-F10 tumour cell lines, these extracts had toxicity effect. In vivo assays using C. elegans N2 showed that EE was not toxic, and it did not affect its viability nor its development. Besides, EE increased worm survival under oxidative stress and reduced intracellular reactive oxygen species (ROS) levels by 50%. Thus, C. leptophloeos EE displayed an important in vitro and in vivo antioxidant capacity. The EE extract has polyphenols, suggesting that these compounds may be responsible for a myriad of biological activities having this potential to be used in various biotechnological applications.


2020 ◽  
Vol 3 (1) ◽  
pp. 47
Author(s):  
Nadezhda Petkova ◽  
Manol Ognyanov ◽  
Blaga Inyutin ◽  
Petar Zhelev ◽  
Panteley Denev

Crab apple (Malus baccata (L.) Borkh.) was mainly distributed in Europe as an ornamental plant, but the nutritional properties of its edible fruits were not fully revealed. The aim of the current study was to characterize the phytochemical composition of ripen carb apple fruits and to evaluate their nutritional and antioxidant potentials. The fruits were assayed for moisture and ash content, proteins, lipids, carbohydrates, titratable acidity (TA), pH, total phenolic compounds and natural pigments. Among the analyzed carbohydrates cellulose was found in the highest content (6% dw), followed by sugars (sucrose, glucose and fructose) and 1.8 % dw uronic acids. The total chlorophylls and carotenoids contents in their fruits were 6.51 and 4.80 μg/g fw, respectively. Total monomeric anthocyanins were not detected. The highest content of total phenolic compounds (2.67 mg GAE/g fw) was found in 95 % ethanol extract from fruits, while the total flavonoids were relatively low – 0.1 mg QE/g fw. DPPH assay (17.27 mM TE/g fw) and FRAP assay (14.34 mM TE/g fw) demonstrated in vitro antioxidant activities of crabapple. Malus baccata fruits were evaluated as a rich source of dietary fibers and phenolic compounds with significant antioxidant potential that could be used in human nutrition.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 991
Author(s):  
Melanie S. Matos ◽  
José D. Anastácio ◽  
Cláudia Nunes dos Santos

Inflammation is a crucial and complex process that reestablishes the physiological state after a noxious stimulus. In pathological conditions the inflammatory state may persist, leading to chronic inflammation and causing tissue damage. Sesquiterpene lactones (SLs) are composed of a large and diverse group of highly bioactive plant secondary metabolites, characterized by a 15-carbon backbone structure. In recent years, the interest in SLs has risen due to their vast array of biological activities beneficial for human health. The anti-inflammatory potential of these compounds results from their ability to target and inhibit various key pro-inflammatory molecules enrolled in diverse inflammatory pathways, and prevent or reduce the inflammatory damage on tissues. Research on the anti-inflammatory mechanisms of SLs has thrived over the last years, and numerous compounds from diverse plants have been studied, using in silico, in vitro, and in vivo assays. Besides their anti-inflammatory potential, their cytotoxicity, structure–activity relationships, and pharmacokinetics have been investigated. This review aims to gather the most relevant results and insights concerning the anti-inflammatory potential of SL-rich extracts and pure SLs, focusing on their effects in different inflammatory pathways and on different molecular players.


Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4399
Author(s):  
Norhasnida Zawawi ◽  
Pei Juin Chong ◽  
Nurul Nadhirah Mohd Tom ◽  
Nurkhairina Solehah Saiful Anuar ◽  
Salma Malihah Mohammad ◽  
...  

Honey is a well-known natural sweetener and is rich in natural antioxidants that prevent the occurrence of oxidative stress, which is responsible for many human diseases. Some of the biochemical compounds in honey that contribute to this property are vitamins and phenolic compounds such as phenolic acids and flavonoids. However, the extent to which these molecules contribute towards the antioxidant capacity in vitro is inconsistently reported, especially with the different analytical methods used, as well as other extrinsic factors that influence these molecules’ availability. Therefore, by reviewing recently published works correlating the vitamin, total phenolic, and flavonoid content in honey with its antioxidant activities in vitro, this paper will establish a relationship between these parameters. Based on the literature, vitamins do not contribute to honey’s antioxidant capacity; however, the content of phenolic acids and flavonoids has an impact on honey’s antioxidant activity.


2009 ◽  
Vol 6 (2) ◽  
pp. 227-231 ◽  
Author(s):  
S. A. Adesegun ◽  
A. Fajana ◽  
C. I. Orabueze ◽  
H. A. B. Coker

The antioxidant activities of crude extract ofPhaulopsis fascisepalaleaf were evaluated and compared with α-tocopherol and BHT as synthetic antioxidants and ascorbic acid as natural-based antioxidant.In vitro, we studied its antioxidative activities, radical-scavenging effects, Fe2+-chelating ability and reducing power. The total phenolic content was determined and expressed in gallic acid equivalent. The extract showed variable activities in all of thesein vitrotests. The antioxidant effect ofP. fascisepalawas strongly dose dependent, increased with increasing leaf extract dose and then leveled off with further increase in extract dose. Compared to other antioxidants used in the study, α-Tocopherol, ascorbic acid and BHT,P. fascisepalaleaf extract showed less scavenging effect on α,α,-diphenyl-β-picrylhydrazyl (DPPH) radical and less reducing power on Fe3+/ferricyanide complex but better Fe2+-chelating ability. These results revealed thein vitroantioxidant activity ofP.fascisepala.Further investigations are necessary to verify these activitiesin vivo.


2017 ◽  
Vol 313 (4) ◽  
pp. L710-L721 ◽  
Author(s):  
Yunbo Ke ◽  
Olga V. Oskolkova ◽  
Nicolene Sarich ◽  
Yufeng Tian ◽  
Albert Sitikov ◽  
...  

Prostaglandins (PG), the products of cyclooxygenase-mediated conversion of arachidonic acid, become upregulated in many situations including allergic response, inflammation, and injury, and exhibit a variety of biological activities. Previous studies described barrier-enhancing and anti-inflammatory effects of PGE2 and PGI2 on vascular endothelial cells (EC). Yet, the effects of other PG members on EC barrier and inflammatory activation have not been systematically analyzed. This study compared effects of PGE2, PGI2, PGF2α, PGA2, PGJ2, and PGD2 on human pulmonary EC. EC permeability was assessed by measurements of transendothelial electrical resistance and cell monolayer permeability for FITC-labeled tracer. Anti-inflammatory effects of PGs were evaluated by analysis of expression of adhesion molecule ICAM1 and secretion of soluble ICAM1 and cytokines by EC. PGE2, PGI2, and PGA2 exhibited the most potent barrier-enhancing effects and most efficient attenuation of thrombin-induced EC permeability and contractile response, whereas PGI2 effectively suppressed thrombin-induced permeability but was less efficient in the attenuation of prolonged EC hyperpermeability caused by interleukin-6 or bacterial wall lipopolysaccharide, LPS. PGD2 showed a modest protective effect on the EC inflammatory response, whereas PGF2α and PGJ2 were without effect on agonist-induced EC barrier dysfunction. In vivo, PGE2, PGI2, and PGA2 attenuated LPS-induced lung inflammation, whereas PGF2α and PGJ2 were without effect. Interestingly, PGD2 exhibited a protective effect in the in vivo model of LPS-induced lung injury. This study provides a comprehensive analysis of barrier-protective and anti-inflammatory effects of different prostaglandins on lung EC in vitro and in vivo and identifies PGE2, PGI2, and PGA2 as prostaglandins with the most potent protective properties.


2021 ◽  
Vol 18 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A Chawla ◽  
Rohit Bhatia ◽  
Shamsher Singh

: 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.


2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100
Author(s):  
Pei-Ling Yen ◽  
Sen-Sung Cheng ◽  
Chia-Cheng Wei ◽  
Huan-You Lin ◽  
Vivian Hsiu-Chuan Liao ◽  
...  

The in vitro and in vivo antioxidant activities and its potential to protect against amyloid-β toxicity of essential oils from Zelkova serrata (Thunb.) Makino were investigated in the model organism Caenorhabditis elegans. The results revealed that the essential oil of Z. serrata heartwood exhibited great radical scavenging activities and high total phenolic content. In vivo assays showed significant inhibition of oxidative damage in wild-type C. elegans under juglone-induced oxidative stress and heat shock. Based on results from both in vitro and in vivo assays, the major compound in essential oil of heartwood, (-)-(1 S, 4 S)-7-hydroxycalamenene (1 S, 4 S-7HC), may contribute significantly to the observed antioxidant activity. Further evidence showed that 1 S, 4 S-7HC significantly delayed the paralysis phenotype in amyloid beta-expressing transgenic C. elegans. These findings suggest that 1 S, 4 S-7HC from the essential oil of Z. serrata heartwood has potential as a source for antioxidant or Alzheimer's disease treatment.


2020 ◽  
Vol 88 (2) ◽  
pp. 26
Author(s):  
Anca Zanfirescu ◽  
Georgiana Nitulescu ◽  
Gheorghe Stancov ◽  
Denise Radulescu ◽  
Cosmin Trif ◽  
...  

Medicinal plants hold a significant place as alternative treatments available for inflammatory diseases, with many phytoconstituents being frequently tested in vitro for their biological activities. In the current study, we investigated the in vivo anti-inflammatory properties of a novel active gel formulation, combining Achillea millefolium and Taxodium distichum essential oils with extracts of Aesculus hippocastanum seeds and Plantago lanceolata leaves. The toxicity of the obtained extracts and volatile oils was determined using the invertebrate model based on Daphnia magna. Anti-inflammatory potential was evaluated by the plethysmometric method on Wistar rats, expressed as the inhibition of the inflammatory oedema (%IIO), while the antinociceptive response was determined on NMRI mice, according to the tail-flick latency method. The tested gel’s efficacy was similar to the 5% diclofenac standard (maximal %IIO of 42.01% vs. 48.70%, respectively), with the anti-inflammatory effect being observed sooner than for diclofenac. Our active gel also produced a significant prolongation of tail-flick latencies at both 60 and 120 min, comparable to diclofenac. Consequently, we can imply that the active constituents present in vivo anti-inflammatory properties, and the prepared gel may be suited for use as an alternative treatment of topical inflammatory conditions.


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