Metabolic transformation has a profound effect on anti-inflammatory activity of flavonoids such as quercetin: Lack of association between antioxidant and lipoxygenase inhibitory activity

2008 ◽  
Vol 75 (5) ◽  
pp. 1045-1053 ◽  
Author(s):  
Wai Mun Loke ◽  
Julie M. Proudfoot ◽  
Scott Stewart ◽  
Allan J. McKinley ◽  
Paul W. Needs ◽  
...  
Author(s):  
Xiaofan Zhang ◽  
Huiyun Wang ◽  
Yangrong Xu ◽  
Mingzhu Luan ◽  
Fenglan Zhao ◽  
...  

: Oleanolic acid can inhibit edema and exhibit obvious inhibitory activity to inflammatory by activating of the pituitary-adrenal cortical system, inhibiting the synthesis or release of PGs, inhibiting endotoxin-mediated release of HMGB1 by endothelial cells or regulating MAPK, PI3K/Akt/NF-κB/ICAM-1/JAK/STAT signaling pathways, etc. In recent years, an increased number of interesting research work has been carried out on the anti-inflammatory activity and mechanisms of OA derivatives, such as acyloxyimino derivative, 3-acetylated derivatives, novel 3,5-disubstituted isoxazoles derivatives, acetate, ester derivatives and oximes derivatives. The review summaries and highlights the update advances on the anti-inflammatory activity and mechanism of OA and its derivatives.


Author(s):  
Jayashree V ◽  
Bagyalakshmi S ◽  
Manjula Devi K ◽  
Richard Daniel D

<p>ABSTRACT<br />Objective: To study the in vitro anti-inflammatory activity of 4-benzylpiperidine.<br />Methods: This study was conducted to evaluate the in vitro anti-inflammatory activity of 4-benzylpiperidine using in vitro models such as inhibition<br />of albumin denaturation and proteinase inhibitory activity.<br />Results: This study revealed the dose-dependent inhibition of protein denaturation and proteinase inhibitory activity by 4-benzylpiperidine.<br />Conclusion: In the present study, results indicate that the 4-benzylpiperidine possess anti-inflammatory properties. The drug inhibited the heat<br />induced albumin denaturation and proteinase inhibitory activity. It shows dose-dependent significant activity when compared with a standard drug.<br />Hence, this study gives an idea that the 4-benzylpiperidine can be used as a lead compound for designing a potent anti-inflammatory drug which can<br />be used to cure inflammation.<br />Keywords: Anti-inflammatory activity, 4-Benzylpiperidine, Protein denaturation, Proteinase inhibitory activity.</p>


2021 ◽  
Vol 12 (3) ◽  
pp. 3883-3899

Liquisolid approach is a potential method due to the ease in the production process, low cost, and manufacturing process because of their strong flow and compaction properties. The study's main goal is to create a liquisolid powder formulation from the polyherbal extract and evaluate its anti-inflammatory activity. Hibiscus cannabinus, Murraya koenigii, and Tabernaemontana divaricate are used to formulating polyherbal Liquisolid powder formulation to assess their anti-inflammatory action. The formulation is tested for its stability studies and anti-inflammatory activity, both in-vitro and in-vivo. The polyherbal liquisolid powder formulation (F5) has a minimum strength of 1kg/cm 2, while F2 & F6 strength was 4 kg/cm2; FTIR studies showed no interactions between drug and excipients. To confirm the liquisolid powder formulation, further evaluations on friability, hardness, disintegration time, dissolution rate, and Differential scanning calorimetry and X-ray powder diffraction analysis were determined. The polyherbal extract's anti-inflammatory activities were evaluated using the paw edema and cotton pellet method, and the results are found to exhibit its inhibitory activity. The polyherbal extract of Liquisolid powder formulation was evaluated, and it showed a promising inhibitory activity to overcome the inflammation in the test species. Hence it can be used as an alternative therapy for curing inflammation.


2021 ◽  
Vol 15 (1) ◽  
pp. 173-182
Author(s):  
Garima Gupta ◽  
Anjuman Gul Memon ◽  
Brijesh Pandey ◽  
Mohd Sajid Khan ◽  
Mohammed Shariq Iqbal ◽  
...  

Background: Nigella sativa (NS), an herbaceous medicinal plant recognized for its diverse beneficial applications as a spice and traditional medicine. Objective: The present study was targeted to explore the antioxidant potential of Nigella sativa in response to colchicine-induced mutation. The stress condition brought due to mutation may affect the medicinal value (anti-inflammatory activity) of the plant. Method: Nigella sativa seeds were imperiled to colchicine treatment at various concentrations viz. 0.00625, 0.0125, 0.025, 0.05 and 0.1% subjected for analysis. Result: The colchicine treated plant (polyploid/ mutant) at 0.025% concentrations showed significant variation at morpho-physiological and biochemical level with respect to control (p value < 0.05). At the morphological level, the plant showed enlargement of shoot length (33.760±2.295mm), root length (13.546±1.535 mm), and leaf area (22.836±1.524 mm2). The analysis of seeds showed enhanced seeds per pod (49.333±4.163), weight of seeds (2.810±0.010g), length (3.133±0.089mm), and width (1.123±0.044mm) when compared with control. The physiological parameters also showed significant enhancement for stomatal index (35.456±4.751%), chlorophyll A (9.053±0.865 µg/gfw), chlorophyll B (4.990±0.763 µg/gfw), and total carotene content (773.190±5.906 µg/gfw). However, the fresh weight/ dry weight ratio (10.738±3.031) was found to be deprived. Furthermore, biochemical parameters viz. total flavonoid (seeds 1.973±0.134; plant 1.703 ± 0.064 mg eqv QE/g of tissue), total phenolic (seeds 15.690±1.495; plant 8.220±0.070 mg eqv GA/g of tissue), total carotene (seeds nil; plant 773.190±5.906 µg/gfw), and total antioxidant (seeds 0.445±0.102; plant 0.386±0.010 mM eqv AA/g tissue) were significantly elevated at 0.025% of colchicine treatment. When the in vitro anti-inflammatory activity was targeted, a significant escalation was observed for inhibition of albumin denaturation (97.466±2.835%), proteinase inhibitory activity (62.290±6.475%), heat-induced hemolysis (89.873±3.533%), hypotonicity induced hemolysis (92.572±3.527%), anti-lipoxygenase activity (96.010±3.098%), and cyclooxygenase inhibitory activity (68.296±3.920%) at 500µg/mL concentration of extract. Conclusion: Thus, it can be concluded that 0.025% of colchicine can induce significant (p value < 0.05) mutation in the Nigella sativa plant, which may lead to alterations at morpho-physiological and biochemical levels. Such treatment induces stress in the plant and leads to elevated antioxidant levels. This in turn elevates the therapeutic potential of the plant. Hence, our study is a novel and open-ended finding to explore various other medical properties of the plant with respect to colchicine-induced mutation.


2021 ◽  
Vol 14 (12) ◽  
pp. 1323
Author(s):  
Juan Martín-López ◽  
Sandra Codony ◽  
Clara Bartra ◽  
Christophe Morisseau ◽  
María Isabel Loza ◽  
...  

The pharmacological inhibition of soluble epoxide hydrolase (sEH) has been suggested as a potential therapy for the treatment of pain and inflammatory diseases through the stabilization of endogenous epoxyeicosatrienoic acids. Numerous potent sEH inhibitors (sEHI) have been developed, however many contain highly lipophilic substituents limiting their availability. Recently, a new series of benzohomoadamantane-based ureas endowed with potent inhibitory activity for the human and murine sEH was reported. However, their very low microsomal stability prevented further development. Herein, a new series of benzohomoadamantane-based amides were synthetized, fully characterized, and evaluated as sEHI. Most of these amides were endowed with excellent inhibitory potencies. A selected compound displayed anti-inflammatory effects with higher effectiveness than the reference sEHI, TPPU.


Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3750
Author(s):  
Xiao-Yan Liu ◽  
You-Bo Zhang ◽  
Xiu-Wei Yang ◽  
Yan-Fang Yang ◽  
Wei Xu ◽  
...  

The dried vine stems of Spatholobus suberectus are commonly used in traditional Chinese medicine for treating gynecological and cardiovascular diseases. In this study, five new compounds named spasuberol A (2), homovanillyl-4-oxo-nonanoate (5), spasuberol C (6), spasuberoside A (14), and spasuberoside B (15), together with ten known compounds (1, 3, 4, 7–13), were isolated from the dried vine stems of S. suberectus. Their chemical structures were analyzed using spectroscopic assays. This is the first study interpreting the detailed structural information of 4. The anti-inflammatory activity of these compounds was evaluated by reducing nitric oxide overproduction in RAW264.7 macrophages stimulated by lipopolysaccharide. Compounds 1 and 8–10 showed strong inhibitory activity with half maximal inhibitory concentration (IC50) values of 5.69, 16.34, 16.87, and 6.78 μM, respectively, exhibiting higher activity than the positive drug l-N6-(1-iminoethyl)-lysine (l-NIL) with an IC50 value of 19.08 μM. The IC50 values of inhibitory activity of compounds 2 and 4–6 were 46.26, 40.05, 45.87, and 28.29 μM respectively, which were lower than l-NIL, but better than that of positive drug indomethacin with an IC50 value of 55.44 μM. Quantitative real-time polymerase chain reaction analysis revealed that assayed compounds with good anti-inflammatory activity, such as 1, 6, 9, and 10 at different concentrations, can reduce the messenger RNA (mRNA) expression of some pro-inflammatory cytokines such as tumor necrosis factor α (TNF-α), nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX-2). The anti-inflammatory activity and the possible mechanism of the compounds mentioned in this paper were studied preliminarily.


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