The Anti-Inflammatory Activity of Pentacyclic Triterpenes In Vitro

2011 ◽  
Vol 138-139 ◽  
pp. 1174-1178
Author(s):  
Li Ming Bai ◽  
Fan Xu Meng ◽  
Li Jie Zhao ◽  
Ming Zhao

The Anti-inflammatory activity of pentacyclic triterpenes, oleananes (1,2), urasanes (3-11), lupanes (12,13), taraxasteranes (14,15), which isolated from Nerium oleander L, were examined. Ursolic acid (5) showed significant activity and compounds (1, 12) and (14) showed weak to modelate activity toward inhibitory activity on ICAM-1 expression.

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>


Author(s):  
Mingzhu Luan ◽  
Huiyun Wang ◽  
Jiazhen Wang ◽  
Xiaofan Zhang ◽  
Fenglan Zhao ◽  
...  

: In vivo and in vitro studies reveal that ursolic acid (UA) is able to counteract endogenous and exogenous inflammatory stimuli, and has favorable anti-inflammatory effects. The anti-inflammatory mechanisms mainly include decreasing the release of histamine in mast cells, suppressing the activities of lipoxygenase, cyclooxygenase and phospholipase, and reducing the production of nitric oxide and reactive oxygen species, blocking the activation of signal pathway, down-regulating the expression of inflammatory factors, and inhibiting the activities of elastase and complement. These mechanisms can open up new avenues for the scientific community to develop or improve novel therapeutic approaches to tackle inflammatory diseases such as arthritis, atherosclerosis, neuroinflammation, liver diseases, kidney diseases, diabetes, dermatitis, bowel diseases, cancer. The anti-inflammatory activity, the anti-inflammatory mechanism of ursolic acid and its therapeutic applications are reviewed in this paper.


2019 ◽  
Vol 35 (2) ◽  
pp. 870-876
Author(s):  
Husam Hamza Salman ◽  
Huda Salih Abood ◽  
Usama Hamid Ramadhan

This study included the preparation of a series of some new azo compounds by diazo coupling aromatic amines with salicylic acid derivatives. The prepared compounds identified using precise elemental analysis (C.H.N.), the results supported the structure of concerned compounds. The synthesized azo compounds also identified by using infrared spectroscopy and 1H-NMR spectroscopy. Anti-inflammatory activity of the compounds were determined in-vitro by human red blood cell (HRBC) membrane stability method, the compounds showed a significant activity to protection of the cell membrane. Other compounds show moderate to low activity, sodium diclofenac was used as positive control.


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.


2020 ◽  
Vol 11 (4) ◽  
pp. 7317-7322
Author(s):  
Sebastin V ◽  
Gopalakrishnan G ◽  
Sreejith M ◽  
Anoob Kumar K I

Plants of the genus Argyreia have ethnomedicinal importance, and several pharmacological activities are also reported. In this study, the anti-inflammatory activity of different extracts of Argyreia imbricata was evaluated by in vitro and in vivo methods. In both evaluations, standard, Diclofenac sodium was used for comparative evaluation. In this study, extraction of powdered whole plant material was done with different solvents viz., petroleum ether, chloroform, ethyl acetate and methanol by soxhelation. In vitro anti-inflammatory activity of all the prepared extracts was evaluated by stabilization of human red blood cell (HRBC) membrane in different temperature and tonicity conditions. Among the six different concentrations of four tested extracts, the ethyl acetate and methanol extracts (1000μg/ml) showed significant activity in the in vitro evaluation. They were selected for the in vivo evaluation on the paw oedema induced by carrageenan on Wistar albino rats. Two doses, 200mg.kg-1 and 400mg.kg-1 of the test extracts were subjected to evaluation. Both the tested extracts showed the activity, particularly, the methanol extract in the dose of 400mg.kg-1 showed significant activity. Results of this study strongly supported the anti-inflammatory activity of the tested extracts. Further, studies on toxicity, identification, isolation of the active constituents may give useful results.


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.


2011 ◽  
Vol 6 (10) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Shivraj H. Nile ◽  
Chandrahasy N. Khobragade

The methanolic extract of Tephrosia purpurea (Leguminosae) shoots was evaluated in-vitro for its anti-inflammatory and xanthine oxidase inhibitory activity. Anti-inflammatory activity was measured by the Diene-conjugate, HET-CAM and β-glucuronidase methods. The enzyme inhibitory activity was tested against isolated cow milk xanthine oxidase. The average anti-inflammatory activity of T. purpurea shoot extract in the concentration range of 1-2 μg/mL in the reacting system revealed significant anti-inflammatory activities, which, as recorded by the Diene-conjugate, HET-CAM and β-glucuronidase assay methods, were 45.4, 10.5, and 70.5%, respectively. Screening of the xanthine oxidase inhibitory activity of the extract in terms of kinetic parameters revealed a mixed type of inhibition, wherein the Km and Vmax values in the presence of 25 to 100 μg/mL shoot extract was 0.20 mM/mL and 0.035, 0.026, 0.023 and 0.020 μg/min, while, for the positive control, the Km and Vmax values were 0.21 mM/mL and 0.043 μg/min, respectively. These findings suggest that T. purpurea shoot extract may possess constituents with good medicinal properties that could be exploited to treat the diseases associated with oxidative stress, xanthine oxidase enzyme activity and inflammation.


2020 ◽  
Vol 21 (2) ◽  
pp. 149-157
Author(s):  
Zahra Iqbal ◽  
Ausaf Ahmad ◽  
Ziyaul Haque ◽  
Mohammed S. Khan ◽  
Mohd S. Khan ◽  
...  

Background: Flavonol derivative and phenolic acids derived from the plants function as free radical scavengers, reducing agents, and quenchers for the formation of singlet oxygen. Flavonoids and phenolic constituents also play an important role in various human diseases and disorders primarily through modulation of inflammatory responses. Objective: To estimate the Flavonol Derivatives (FD) and phenolic acids (PA) in Capsicum annuum (CA) and other important phytochemicals having an anti-inflammatory effect. Method: In the present study, FD and PA were estimated in CA and in vitro anti-inflammatory activity (pilot study) was determined and correlation was established. Results: The results were found to be significant using RP-HPLC. FD and PA were found to be 0.0659±0.0058 and 0.0862±0.0.0134 mg/gram dry weight, respectively. For in vitro anti-inflammatory activity, the inhibition of albumin denaturation and antiproteinase activity was found to be maximum in Quercetin (QE) with 98.230±1.589% and 59.906±1.529%, respectively. Heat-induced hemolysis of erythrocytes was found to be maximum in salicylic acid (SA) (71.830±2.838%). Hypotonicity-induced hemolysis showed significant activity with QE (76.770±3.475%). Lipoxygenase and cyclooxygenase inhibition was found to be maximum in QE with 56.930±4.069% and 61.660±3.135%, respectively. Conclusion: A strong positive correlation of 0.9 was observed between the extract of CA and standard QE and SA against the anti-inflammatory activity. Therefore, the role of FD and PA has been postulated to be an active phytochemical of CA accountable for its anti-inflammatory activity. However further work is desirable to fully elucidate the phytochemicals responsible for their anti-inflammatory activity and to develop better herbal drug formulations.


Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1323 ◽  
Author(s):  
Maria Stefania Lepanto ◽  
Luigi Rosa ◽  
Rosalba Paesano ◽  
Piera Valenti ◽  
Antimo Cutone

Lactoferrin (Lf), a cationic glycoprotein able to chelate two ferric irons per molecule, is synthesized by exocrine glands and neutrophils. Since the first anti-microbial function attributed to Lf, several activities have been discovered, including the relevant anti-inflammatory one, especially associated to the down-regulation of pro-inflammatory cytokines, as IL-6. As high levels of IL-6 are involved in iron homeostasis disorders, Lf is emerging as a potent regulator of iron and inflammatory homeostasis. Here, the role of Lf against aseptic and septic inflammation has been reviewed. In particular, in the context of aseptic inflammation, as anemia of inflammation, preterm delivery, Alzheimer’s disease and type 2 diabetes, Lf administration reduces local and/or systemic inflammation. Moreover, Lf oral administration, by decreasing serum IL-6, reverts iron homeostasis disorders. Regarding septic inflammation occurring in Chlamydia trachomatis infection, cystic fibrosis and inflammatory bowel disease, Lf, besides the anti-inflammatory activity, exerts a significant activity against bacterial adhesion, invasion and colonization. Lastly, a critical analysis of literature in vitro data reporting contradictory results on the Lf role in inflammatory processes, ranging from pro- to anti-inflammatory activity, highlighted that they depend on cell models, cell metabolic status, stimulatory or infecting agents as well as on Lf iron saturation degree, integrity and purity.


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