scholarly journals Biomedical Applications of Scutellaria edelbergii Rech. f.: In Vitro and In Vivo Approach

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3740
Author(s):  
Muddaser Shah ◽  
Waheed Murad ◽  
Najeeb Ur Rehman ◽  
Sobia Ahsan Halim ◽  
Manzoor Ahmed ◽  
...  

In the current study, in vitro antimicrobial and antioxidant activities and in vivo anti-inflammatory and analgesic activities of Scutellaria edelbergii Rech. f. (crude extract and subfractions, i.e., n-hexane, ethyl acetate (EtOAc), chloroform, n-butanol (n-BuOH) and aqueous) were explored. Initially, extraction and fractionation of the selected medicinal plant were carried out, followed by phytochemical qualitative tests, which were mostly positive for all the extracts. EtOAc fraction possessed a significant amount of phenolic (79.2 ± 0.30 mg GAE/g) and flavonoid (84.0 ± 0.39 mg QE/g) content. The EtOAc fraction of S. edelbergii exhibited appreciable antibacterial activity against Gram-negative (Escherichia coli and Klebsiella pneumoniae) strains and significant zones of inhibition were observed against Gram-positive bacterial strains (Bacillus subtilis and Staphylococcus aureus). However, it was found inactive against Candida Albicans and Fusarium oxysporum fungal strains. The chloroform fraction was the most effective with an IC50 value of 172 and 74 µg/mL against DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays, in comparison with standard ascorbic acid 59 and 63 µg/mL, respectively. Moreover, the EtOAc fraction displayed significant in vivo anti-inflammatory activity (54%) using carrageenan-induced assay and significant (55%) in vivo analgesic activity using acetic acid-induced writing assay. In addition, nine known compounds, ursolic acid (UA), ovaul (OV), oleanolic acid (OA), β-sitosterol (BS), micromeric acid (MA), taraxasterol acetate (TA), 5,3′,4′-trihydroxy-7-methoxy flavone (FL-1), 5,7,4′-trihydroxy-6,3′-dimiethoxyflavone (FL-2) and 7-methoxy catechin (FL-3), were isolated from methanolic extract of S. edelbergii. These constituents have never been obtained from this source. The structures of all the isolated constituents were elucidated by spectroscopic means. In conclusion, the EtOAc fraction and all other fractions of S. edelbergii, in general, displayed a significant role as antibacterial, free radical scavenger, anti-inflammatory and analgesic agents which may be due to the presence of these constituents and other flavonoids.

2016 ◽  
Vol 2016 ◽  
pp. 1-13 ◽  
Author(s):  
Junqiao Wang ◽  
Shuzhen Hu ◽  
Shaoping Nie ◽  
Qiang Yu ◽  
Mingyong Xie

It is widely acknowledged that the excessive reactive oxygen species (ROS) or reactive nitrogen species (RNS) induced oxidative stress will cause significant damage to cell structure and biomolecular function, directly or indirectly leading to a number of diseases. The overproduction of ROS/RNS will be balanced by nonenzymatic antioxidants and antioxidant enzymes. Polysaccharide or glycoconjugates derived from natural products are of considerable interest from the viewpoint of potentin vivoandin vitroantioxidant activities recently. Particularly, with regard to thein vitroantioxidant systems, polysaccharides are considered as effective free radical scavenger, reducing agent, and ferrous chelator in most of the reports. However, the underlying mechanisms of these antioxidant actions have not been illustrated systematically and sometimes controversial results appeared among various literatures. To address this issue, we summarized the latest discoveries and advancements in the study of antioxidative polysaccharides and gave a detailed description of the possible mechanisms.


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.


Author(s):  
HITESH MALHOTRA ◽  
MANJUSHA CHOUDHARY

Objective: The objective of the study was to establish the anti-inflammatory and anti-arthritic potential of various fractions of Eclipta prostrata Linn. Methods: The four fractions, i.e., n-butanol, ethyl acetate, chloroform, and n-hexane from hydro-alcoholic extract were obtained. First, the fractions were evaluated through in vitro models, and then they were evaluated by in vivo anti-inflammatory model, i.e., carrageenan-induced paw edema model. Further, two active fractions were evaluated for the anti-arthritic activity using formaldehyde induced arthritis model. Results: The fractions at a dose of 100 and 200 mg/kg showed an anti-inflammatory activity, but the ethyl acetate and chloroform fraction will show maximum anti-inflammatory potential. Hence, they are further evaluated for anti-arthritic potential where they show significant activity. Conclusion: From the results, it is concluded that the ethyl acetate and chloroform fraction show significant anti-arthritic activity.


2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Xiu E. Feng ◽  
Tai Gang Liang ◽  
Jie Gao ◽  
De Peng Kong ◽  
Rui Ge ◽  
...  

Increasing evidence has demonstrated that heme oxygenase-1 (HO-1) is a key enzyme triggered by cellular stress, exhibiting cytoprotective, antioxidant, and anti-inflammatory abilities. Previously, we prepared a series of novel active halophenols possessing strong antioxidant activities in vitro and in vivo. In the present study, we demonstrated that these halophenols exhibited significant protective effects against H2O2-induced injury in EA.hy926 cells by inhibition of apoptosis and ROS and TNF-αproduction, as well as induction of the upregulation of HO-1, the magnitude of which correlated with their cytoprotective actions. Further experiments which aimed to determine the mechanistic basis of these actions indicated that the halophenols induced the activation of Nrf2, Erk1/2, and PI3K/Akt without obvious effects on the phosphorylation of p38, JNK, or the expression of PKC-δ. This was validated with the use of PD98059 and Wortmannin, specific inhibitors of Erk1/2 and PI3K, respectively. Overall, our study is the first to demonstrate that the cytoprotective actions of halophenols involve their antiapoptotic, antioxidant, and anti-inflammatory abilities, which are mediated by the upregulation of Nrf2-dependent HO-1 expression and reductions in ROS and TNF-αgeneration via the activation of Erk1/2 and PI3K/Akt in EA.hy926 cells. HO-1 may thus be an important potential target for further research into the cytoprotective actions of halophenols.


2020 ◽  
Author(s):  
Gervason Moriasi ◽  
Elias Nelson ◽  
Epaphrodite Twahirwa

Abstract Oxidative stress is a critical etiologic factor and driver of inflammatory responses, witnessed in chronic and persistent conditions. The current anti-oxidative stress and anti-inflammatory drugs are associated with detrimental effects, high dependence, high costs, inaccessibility, among other drawbacks; therefore, a need for alternatives is imperative. Despite the remarkable potential of medicinal plants, there are scanty empirical studies on their pharmacologic efficacy. The Phytexponent is an alcoholic polyherbal preparation of Allium sativum, Triticum repens, Echinacea purpurea, Viola tricolor and Matricaria chamomilla. In complementary medicine, the Phytexponent is used to boost immunity, to treat inflammatory disorders, oxidative stress, blood pressure, diabetes, stress/depression, among other conditions. However, there is no sufficient scientific data to support these healing claims. Therefore, in the current study evaluated the in vitro anti-inflammatory, antioxidant activities and qualitative phytochemical composition of the Phytexponent. The in vitro anti-inflammatory activities were evaluated using the inhibition of protein denaturation and the human erythrocyte (HRBC) membrane stabilization techniques. Antioxidant activities were evaluated by the 1,1-diphenyl-picryl-1-hydrazyl (DPPH) radical scavenging-, the hydroxyl radical scavenging- and catalase activities. Qualitative phytochemical screening was performed using standard procedures. The results showed a significantly higher percentage inhibition of heat-induced- and hypotonicity induced HRBC hemolysis by the Phytexponent at concentrations of 50 % and 100 %, compared with the percentage inhibitions of etanercept (p<0.05). No significant differences in percentage inhibitions of protein denaturation were observed among concentrations of 12.5 %,25.0 %,50.0 %,100.0 % of the Phytexponent and etanercept (25 mg/ml) (p˃0.05). Furthermore, the Phytexponent demonstrated high antioxidant activities against the DPPH- (IC50=0.00733%) and the hydroxyl- (IC50 = 0.716 %) radicals in vitro.The Phytexponent recorded significantly higher catalase activities at concentrations of 1 % and 0.1 % than those recorded by ascorbic acid at similar concentrations. Qualitative phytochemical screening revealed the presence of phenols, flavonoids, tannins, among other antioxidant associated phytochemicals. The bioactivities of the Phytexponent reported herein, were attributed to the presence of these phytochemicals. Further studies to establish specific mode(s) through which the Phytexponent exerts in vitro anti-inflammatory and antioxidant effects are encouraged. Moreover, in vivo anti-inflammatory and antioxidant activities should be done to determine the replicability of these findings in vivo. Bioassay-guided isolation of compounds responsible for the reported bioactivities herein should be done.


Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
YS Kim ◽  
JW Hwang ◽  
SE Kim ◽  
BI You ◽  
NJ Jeon ◽  
...  

2019 ◽  
Vol 18 (2) ◽  
pp. 233-240
Author(s):  
Wilfred O Obonga ◽  
Charles O Nnadi ◽  
Chinonye C Chima ◽  
Sunday N Okafor ◽  
Edwin O Omeje

This study evaluated the antioxidant and anti-inflammatory properties of Marantochloa leucantha (Marantaceae). The in vitro antioxidant activity of the extracts and solvent fractions was evaluated by 1,1-diphenyl- 2-picrylhydrazyl (DPPH) radical scavenging and ferric reducing antioxidant potential (FRAP) assay models and in vivo anti-inflammatory activity by the rat paw edema model. The phytochemical screening indicated the presence of tannins, terpenoids, steroids, flavonoids, reducing sugar and phenolics. The antioxidant assay showed that all the extracts exhibited high antioxidant activity comparable with ascorbic and gallic acid controls. In DPPH model, a 250 μg/ml EtOAc fraction of the leaves showed antioxidant activity of 93.9 ± 1.7 % (EC50 0.82 μg/ml) and a 1000 μg/ml of same stem fraction produced 91.9 ± 0.3 % activity (EC50 1.38 μg/ml). In the FRAP model, EtOAc fraction exhibited 31.1±0.7 and 92.0 ± 2.2 μM Fe2+/g of dried leaves and stem, respectively at 1000 μg/ml FeSO4 equivalent. The anti-inflammatory potential of the plant showed that the crude stem extract and fractions at 200 - 600 mg/kg exhibited significant (p < 0.01) dose-related inhibition of paw edema in rats. A 200 mg/kg EtOAc fraction showed 18.8 % inhibition compared to 31 % observed in diclofenac-treated rats in 2 h post albumin challenge. These findings validated the folkloric use of this plant in the treatment of diseases associated to the oxidative stress and could further provide promising lead compounds with potent antioxidant and anti-inflammatory activities Dhaka Univ. J. Pharm. Sci. 18(2): 233-240, 2019 (December)


2020 ◽  
Vol 16 (7) ◽  
pp. 1144-1159
Author(s):  
Sang-Eun Hong ◽  
Jong Hun An ◽  
Seong-Lan Yu ◽  
Jaeku Kang ◽  
Chang Gyo Park ◽  
...  

Oxidative stress is one of the principal causes of hypoxia-induced kidney injury. The ceria nanoparticle (CNP) is known to exhibit free radical scavenger and catalytic activities. When zirconia is attached to CNPs (CZNPs), the ceria atom tends to remain in a Ce3+ form and its efficacy as a free radical scavenger thus increases. We determined the effectiveness of CNP and CZNP antioxidant activities against hypoxia-induced acute kidney injury (AKI) and observed that these nanoparticles suppress the apoptosis of hypoxic HK-2 cells by restoring autophagy flux and alleviating mitochondrial damage. In vivo experiments revealed that CZNPs effectively attenuate hypoxia-induced AKI by preserving renal structures and glomerulus function. These nanoparticles can successfully diffuse into HK-2 cells and effectively counteract reactive oxygen species (ROS) to block hypoxia-induced AKI. This suggests that these particles represent a novel approach to controlling this condition.


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