scholarly journals Anti-inflammatory and NF-κB inhibitory activity of aerial parts of Cestrum diurnum

2020 ◽  
Author(s):  
Amina Khatun ◽  
Mahmudur Rahman ◽  
Lutfun Nesa ◽  
Chung Yeng Looi ◽  
Won Fen Wong ◽  
...  

Abstract Background Cestrum diurnum L. (Solanaceae) is used in various traditional medicine for pain and related disorders. The Malayali tribe of Tamil Nadu in India use the leaf in joint pain. In the Chinese traditional medicine it is used for the treatment of burns and swellings. Present study was designed to evaluate its traditional use in pain and inflammation. Methods Methanol extract of the aerial parts of C. diurnum was tested by carrageenan induced paw oedema and formalin induced paw licking test in mice at the oral doses of 150 and 300 mg/kg body weight. NF-κB inhibitory activity was evaluated by TNF-α induced NF-κB activation assay in RAW 264.7 macrophage cells at the concentration of 100 µg/ml. Results The extract, at the doses of 150 and 300 mg/kg, showed significant inhibition (p < 0.05) of carrageenan induced paw oedema and the effect persisted throughout the entire experimental period of 3 h with the highest activity (50% inhibition) at 3rd h. In formalin induced paw licking test, the extract exhibited significant (p < 0.05) inhibition of paw licking, both in the early and late phase of the experiment at the aforementioned dose levels. At the concentration of 100 µg/ml, the extract did not inhibit the nuclear translocation of NF-κB. Rather, the extract was found to downregulate NF-κB p65 protein expression. Conclusions The present work supports the folkloric use of the plant for its analgesic and anti-inflammatory action which might involve downregulation of NF-κB p65 protein expression and/or inhibition of autacoid (histamine, serotonin, prostaglandin) synthesis.

2007 ◽  
Vol 2 (11) ◽  
pp. 1934578X0700201 ◽  
Author(s):  
Sabrin R. M. Ibrahim ◽  
Jihan M. Badr ◽  
Khalid A. El Sayed ◽  
Diaa T. A. Youssef

A re-investigation of the methanolic extract of the aerial parts of Tanacetum santolinoides has resulted in the isolation of a new sesquiterpene, tanacetonic acid (1), along with three known methoxylated flavonoids. The structure of the isolated compounds was secured based on their IR, UV, 1D and 2D (1H-1H COSY, HSQC and HMBC) NMR spectroscopic and FAB mass spectral characteristics. The new sesquiterpene showed a significant cytotoxic activity when tested using the brine shrimp bioassay, while the three flavonoids demonstrated anti-inflammatory effects in the rat paw oedema test.


2020 ◽  
Vol 11 (SPL4) ◽  
pp. 2063-2067
Author(s):  
Alekhya V ◽  
Ganapaty S ◽  
Deepan T

To assess phytochemical with pharmacological studies of Hibiscus hispidissimus griff belong to family malavaceae. Preliminary phytochemical analysis reveals the presence of steroids, triterpenes, saponins, steroidal saponins and phenols. Evaluation of anti-inflammatory, anti-microbial with antioxidant action were performed on aerial parts of methanolic extract of Hibiscus hispidissimus. Invitro antioxidant activity was performed by 2, 2 -diphenyl- 1- picrylhydrazyl (DPPH) assay, hydroxy radical scavenging method and superoxide radical scavenging activity.The results of invitro antioxidant study reveal that % inhibition of H. hispidissimus  was higher compared to ascorbic acid. Anti-inflammatory studies were performed using carrageenan-induced rat paw oedema animal model, for anti-inflammatory studies, the extracts were compared with standards like indomethacin, and it shows a remarkable zone of inhibition ranging from 58.97 to 71.73 respectively. The anti-bacterial and antifungal activity of plant extracts were studied for the occurrence of inhibition zones. The activity was performed by the cup plate method. Ethanolic extract of H. Hispidissimus  shows significant anti-bacterial effect against S. Aureus, B. Subtilis, P. Vulgaris and E. coli using ciprofloxacin (50µg/ml) as standard.The extracts show remarkable inhibition of zone of inhibition, and results were compared with that of standard drugs against the organism tested. In conclusion, the ethanolic extract of H. hispidissimus  shows  significant antioxidant, anti-inflammatory and anti-bacterial properties.


2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Xue-yan Zhang ◽  
Jing Cheng ◽  
Ping Zhao ◽  
Ke-li Chen ◽  
Juan Li

Objectives. The Selaginella moellendorffii prescription (SMP) consists of S. moellendorffii Herba (SM), Smilacis glabrae Rhizoma (SGR), and Plantaginis Semen (PS). It has been commonly used to treat hyperuricemia and acute gouty arthritis as a hospital preparation. This study was aimed at investigating the best compatibility ratio of SMP on hyperuricemia and gouty arthritis and getting better insight of the possible mechanism. Methods. In vitro, anti-inflammatory activity of SMP was evaluated by lipopolysaccharide (LPS) induced RAW264.7 cells. The release of nitric oxide (NO) was screened by Griess assay, and NF-κB p65 and NLRP3 proteins expression was examined by immunofluorescence assay. Then, the levels of creatinine (Cr), blood urea nitrogen (BUN), and uric acid (UA) were detected in mice induced by potassium oxonate, and the paw oedema, inflammatory mediators, and histological examination were analyzed in rats induced by monosodium urate (MSU). HPLC method was employed to investigate the chemical profile of this preparation. Results. In vitro, SMP-3 (the ratio of SMP:SGR:PS was 3:1:1) exhibited the most potent anti-NO production activity without obvious toxicity. This anti-inflammatory effect was associated with suppression of NF-κB p65 nuclear translocation and NLRP3 protein expression. In animal experiments, the levels of BUN and Cr in SMP-3 group were lower than other extract groups, and the level of UA was also remarkably decreased by SMP-3 in hyperuricemic mice (P<0.01). Besides, SMP-3 extract was able to prevent the paw edema, reduce gouty joint inflammatory features, and decrease the levels IL-1β, PGE-2, IL-8, and NO in gouty arthritis rats. Furthermore, 6-C-β-D-xylopyranosyl-8-C-β-D-glucopyranosyl, apigenin, and astilbin were identified from SMP-3 extract. Conclusions. In summary, SMP-3 may be a potential therapeutic agent for the prevention of hyperuricemic and gout.


1991 ◽  
Vol 19 (03n04) ◽  
pp. 223-231 ◽  
Author(s):  
J. S. Mossa ◽  
M. Tariq ◽  
A. Mohsin ◽  
A. M. Ageel ◽  
M. A. Al-Yahya ◽  
...  

The decoction of the aerial part of Calotropis procera is commonly used in Saudi Arabian traditional medicine for the treatment of variety of diseases including fever, joint pain, muscular spasm and constipation. The present investigation was undertaken to confirm its claimed activity in traditional medicine. The ethanol extract of the plant was tested on laboratory animals for its antipyretic, analgesic, anti-inflammatory, antibacterial, purgative and muscle relaxant activities. The results of this study showed a significant antipyretic, analgesic and neuromuscular blocking activity. On smooth muscle of guinea pig ileum, the extract produced contractions which was blocked by atropine supporting its use in constipation. The extract failed to produce significant anti-inflammatory and antibacterial activities. Our phytochemical studies on the aerial parts of C. procera showed the presence of alkaloids, cardiac glycosides, tannins, flavonoids, sterols and/or triterpenes. However, the chemical constituents responsible for the pharmacological activities remains to be investigated. The safety evaluation studies revealed that the use of extract in single high doses (up to 3g/kg) does not produce any visible toxic symptoms or mortality. However, prolong treatment (90 days) causes significantly higher mortality as compared to control group.


Author(s):  
Shuping Sun ◽  
Yunyan Du ◽  
Chuanliu Yin ◽  
Xiaoguo Suo ◽  
Rui Wang ◽  
...  

Abstract Background Chloranthus serratus (Chloranthaceae) has been used to treat bruises, rheumatoid and bone pain. However, the anti-inflammatory mechanisms of C. serratus in vitro have not been fully elucidated. The present study aimed to explore the anti-inflammatory activity and potential mechanisms of C. serratus’s separated part of water (CSSPW) in lipopolysaccharide (LPS)-induced RAW264.7 cells. Methods The concentrations of CSSPW were optimized by CCK-8 method. Nitric oxide (NO) content was detected by one-step method. The levels of inflammatory cytokines were determined by enzyme-linked immunosorbent assay (ELISA). Gene expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) was detected by real-time quantitative PCR (qPCR). Immunofluorescence and DCFH-DA fluorescent probes were used to detect p65 nuclear translocation and reactive oxygen species (ROS) content, respectively. Western blotting was used to assay the protein expression of mitogen-activated protein kinases (MAPK), nuclear factor-kappa B (NF-κB) and nuclear transcription factor E2 related factor 2/haem oxygenase-1 (Nrf2/HO-1) pathways. Results The final concentrations of 15 ng/mL, 1.5 μg/mL and 150 μg/mL were selected as low, medium and high doses of CSSPW, respectively. CSSPW treatment significantly reduced the generation of NO, tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6), prostaglandinE2 (PGE2), iNOS mRNA and COX-2 mRNA in response to LPS stimulation. Furthermore, the protein expression of the MAPK and NF-κB pathways was suppressed by CSSPW treatment, as well as p65 nuclear translocation and ROS production. In contrast, the protein expression of the Nrf2/HO-1 pathway was markedly upregulated. Conclusions CSSPW exerts its anti-inflammatory effect via downregulating the production of pro-inflammatory mediators, inhibiting the activation of NF-κB and MAPK pathways, as well as activating Nrf2/HO-1 pathway in LPS-induced RAW264.7 cells.


Author(s):  
Madièye Sene ◽  
Daouda Ndiaye ◽  
Abdoulaye Gassama ◽  
Firmin Sylva Barboza ◽  
Mbaye Diagne Mbaye ◽  
...  

Combretum glutinosum Perr. Ex DC (COMBRETACEAE) is a traditional medicinal plant, widely distributed in Senegal and Africa. The aim of that study was to investigate the analgesic and anti-inflammatory activities of two triterpenes, betulonic acid (DN7) and cabraleone (DN12), isolated from the leaves of Combretum glutinosum. Experiments were performed in acetic acid-induced contortions in mice and carrageenan rat paw oedema. DN7 (3 mg/kg, per os) and DN12 (3 mg/kg, per os) significantly prevent contortions in mice. The number of contortions is respectively 30±10 and 32±7 versus 72.6±6.64 in control group (p<0.05, n=5). DN7 (3 mg/kg, per os) significantly prevented the increased rat paw oedema (31.84±6.76 vs 92.72±6.05%) (p<0.05, n=5). DN12 (10 mg/kg, per os) induced rat paw oedema prevention similar to that of acetylsalicylic acid (10 mg/kg, per os) administered in the same conditions (29.28±5.88 vs 30.96±7.25%; ns, n=5). The analgesic and anti-inflammatory activities of triterpenes isolated from C. glutinosum leaves are similar to those of non-steroidal anti-inflammatory drugs such acetylsalicylic acid, justifying the use of this plant in traditional medicine to manage pain and inflammation.


2020 ◽  
Vol 16 (8) ◽  
pp. 1099-1111
Author(s):  
Uzma Salar ◽  
Khalid M. Khan ◽  
Almas Jabeen ◽  
Aisha Faheem ◽  
Farwa Naqvi ◽  
...  

Background: A number of non-steroidal anti-inflammatory drugs (NSAIDs) including aspirin, indomethacin, ibuprofen, flufenamic acid, and phenylbutazone are being clinically used to treat inflammatory disorders. These NSAIDs are associated with serious side effects such as gastric ulceration, nephrotoxicity, and bleeding. Therefore, the identification of potent and safe therapy for inflammatory disorders is still of great interest to the medicinal chemist. Methods: A series of varyingly substituted benzoyl, acetyl, alkyl ester, and sulfonate ester substituted coumarins 1-64 were screened for the inhibition of ROS, generated from zymosan activated whole blood phagocytes, using luminol-enhanced chemiluminescence technique. Results: Among all tested compounds, 8 (IC50 = 65.0 ± 3.1 μM), 24 (IC50 = 41.8 ± 1.5 μM), 26 (IC50 = 10.6 ± 2.8 μM), 28 (IC50 = 20.9 ± 1.5 μM), and 41 (IC50 = 4.6 ± 0.3 μM) showed good anti- inflammatory potential as compared to standard antiinflammatory drug ibuprofen (IC50 = 54.3 ± 1.9 μM). Specifically, compounds 24, 26, 28, and 41 showed superior activity than standard antiinflammatory drug. Furthermore, compounds 12 (IC50 = 219.0 ± 1.4 μM), 14 (IC50 = 216.5 ± 6.2 μM), 16 (IC50 = 187.4 ± 2.2 μM), and 20 (IC50 = 196.2 ± 2.0 μM) showed moderate ROS inhibitory activity. Limited SAR study revealed that the hydroxy-substituted compound showed better ROS inhibition potential in case of 3-benzoyl and 3-ethylester coumarin derivatives. Whereas, chloro substitution was found to be important in case of 3-acetyl coumarin derivatives. Similarly, in case of sulfonate ester, chloro, and nitro groups especially at positions -4 and -3 of ring “R” played vital role in ROS inhibition. Furthermore, cytotoxicity of all active compounds was also checked on NIH-3T3 cell line. Compounds 12, 14, and 20 were found to be non-cytotoxic. Whereas, 8, 16, 24, 26, 28, and 41 were found to be very weak cytotoxic as compared to standard cycloheximide (IC50 = 0.13 ± 0.02 μM). Conclusion: Identified ROS inhibitors offer the possibility of additional modifications that could give rise to lead structures for further research in order to obtain more potent, and safer antiinflammatory agent.


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