INHIBITORY EFFECT OF ARTOCARPUS LOWII KING COMPOUNDS ON COX-2 AND 15-LO ACTIVITIES

2015 ◽  
Vol 76 (1) ◽  
Author(s):  
Mohamad Norisham Mohamad Rosdi ◽  
Hasnah Mohd Sirat ◽  
Siti Awanis Abdullah ◽  
Shajarahtunnur Jamil ◽  
Ida Idayu Muhamad ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Arachidonic Acid Metabolism ◽  
Cyclooxygenase 2 ◽  
Inflammatory Activity ◽  
Dependent Manner ◽  
Direct Inhibition ◽  
Noticeable Effect ◽  
Ic50 Value ◽  
Anti Inflammatory ◽  
Dose Dependent

Artocarpus lowii King is a rare species of plant in Moraceae family. In this study, the anti-inflammatory activity of cycloheterophyllin, isobavachalcone, 4-hydroxylonchocarpin and 2’,4’-dihydroxy-4-methoxy-3’-prenyldihydroxychalcone isolated from A. lowii King were investigated on classical enzymes in arachidonic acid metabolism pathways; cyclooxygenase and lipoxygenase. Isobavachalcone directly inhibited cyclooxygenase-2 enzyme in dose dependent manner, with IC50 value of 0.95 μM. No noticeable effect has been observed with the other tested compounds. In addition, none of the tested compounds displays a direct inhibition on 15-lipoxygenase when compared to the resveratrol as control with the IC50 value of 1.5 μM. Isobavachalcone showed inhibitory effect on cyclooxygenase-2. This study suggests that A. lowii King contains potential anti-inflammatory activity.

Synthesis and Assessment of Novel Anti-chlamydial Benzylidene Acylhydrazides Derivatives

2018 ◽  
Vol 15 (1) ◽  
pp. 31-36 ◽  
Author(s):  
Xiaofeng Bao ◽  
Ying Xue ◽  
Chao Xia ◽  
Yin Lu ◽  
Ningjing Yang ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dependent Manner ◽  
Iron Starvation ◽  
Hydrochloride Salt ◽  
Obligate Intracellular ◽  
Biphasic Life Cycle ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Dose Dependent ◽  
Better Than

Background: Chlamydiae, characterized by a unique biphasic life cycle, are a group of Gram-negative obligate intracellular bacterial pathogens responsible for diseases in a range of hosts including humans. Benzylidene acylhydrazide CF0001 could inhibit chlamydiae independent of iron starvation and T3SS inhibition. This finding promoted us to design and synthesize more benzylidene acylhydrazides to find novel anti-chlamydial agents. Methods: The carboxylic acids 1a-1d were coupled with Boc-hydrazide inpresence of EDCI and DMAP to obtain the intermediate 2a-2d in 60-62% yields. N-Boc deprotections were performed to obtain hydrazide hydrochloride salt 3a-3d. Nextly, the hydrazides were subjected to condensation with aldehydes to obtain benzylidene acylhydrazides 4a-4g in 30-52% yields in two steps. Results: Compound 4d exhibited best inhibitory effect on the formation and growth of chlamydial inclusions. The IC50 value of compound 4d for infectious progenies was 3.55 µM, better than 7.30 µM of CF0001. Conclusion: To find novel anti-chlamydial agents, we have designed and synthesized benzylidene acylhydrazides 4a-4g. Compounds 4a, 4d, 4g showed inhibitory activity on C. muridarum with the IC50 values from 3.55-12 µM. The 3,5-dibromo-4-hydroxyl substitutes on ring B are critical to keep their anti-chlamydial activity. Compound 4d inhibited C. muridarum in a dose-dependent manner without apparent cytotoxicity.

scholarly journals TAMARIND EXTRACT INHIBITS CYTOCHROME P450 (CYP3A4 ISOZYME) - AN IN VITRO STUDY

2018 ◽  
Vol 11 (7) ◽  
pp. 333
Author(s):  
Jagadish Rajkumaar R ◽  
Anitha Roy ◽  
Lakshmi T
Keyword(s):  
Room Temperature ◽  
Potassium Phosphate ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Fruit Pulp ◽  
Ic50 Value ◽  
Dose Dependent ◽  
Cytochrome P 450

Objective: The aim of the present study was to analyze the effect of the aqueous fruit pulp extract of Tamarindus indica L. (tamarind extract) on cytochrome P 450 isoform CYP3A4.Methods: Tamarind extract at different concentrations from 5 to 100 μg/ml was examined for its inhibitory property toward cytochrome P 450 isoform CYP3A4. The various concentrations of tamarind extract, potassium phosphate buffer, CYP450 reagent, and substrate 7-Benzyloxy-4- trifluoromethylcoumarin were added to a 96-well plate. The mixtures were preincubated for 20 min at room temperature. The reaction was started by a mixture of free constituted substrate and NADP+ and incubated at room temperature for 30–60 min. The reaction was stopped by Tris-HCl buffer, pH 10.5. The fluorescent intensities of the products were measured by PerkinElmer Enspire fluorescence reader using an excitation and emission wavelength of 405 nm and 460 nm, respectively. Inhibitory concentration (IC50) was calculated by plotting concentrations of tamarind extract against the corresponding percentage inhibition.Results: All the tested concentrations of extract except 5 μg/ml showed good inhibition against CYP3A4 in a dose-dependent manner. The IC50 value of tamarind for CYP3A4 inhibitory activity was found to be 27.89 μg/ml.Conclusion: T. indica aqueous fruit pulp extract exhibited an inhibitory effect on CYP34A, thereby indicating the possibilities of herb-drug interaction if these extracts are coadministered with the prescribed drugs that are metabolized by CYP3A4.

scholarly journals Topical Anti-Inflammatory Activity of Essential Oils of Alpinia calcarata Rosc., Its Main Constituents, and Possible Mechanism of Action

2020 ◽  
Vol 2020 ◽  
pp. 1-19
Author(s):  
Madhuvanthi Chandrakanthan ◽  
Shiroma M. Handunnetti ◽  
Galbada Sirimal Arachchige Premakumara ◽  
Selvaluxmy Kathirgamanathar
Keyword(s):  
Skin Inflammation ◽  
Inflammatory Activity ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Proinflammatory Mediators ◽  
Mouse Ear ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Topical Analgesic

This study aimed at investigating the anti-inflammatory potential of essential oil from rhizome and leaf of Alpinia calcarata Rosc. (ACEO) with the focus of its topical anti-inflammatory activity along with its dominant compounds 1,8-cineole and α-terpineol using mouse ear edema model. ACEOs were analyzed by GC-MS. The anti-inflammatory activity was determined by studying the inhibition of overproduction of proinflammatory mediators—nitric oxide, reactive oxygen species, prostaglandins, cyclooxygenases, and cytokines induced by lipopolysaccharides in murine macrophages. Topical anti-inflammatory and antinociceptive activity was studied by 12-O-tetradecanoylphorbol-13-acetate (TPA) induced skin inflammation and formalin-induced pain model in mice, respectively. Rhizome oil has 1,8-cineole (31.08%), α-terpineol (10.31%), and fenchyl acetate (10.73%) as major compounds whereas the ACEO from leaves has 1,8-cineole (38.45%), a-terpineol (11.62%), and camphor (10%). ACEOs reduced the production of inflammatory mediators in vitro in a concentration-dependent manner. Further, ACEO and its major compounds reduced ear thickness, weight, myeloperoxidase, and cytokines significantly (p<0.01) in mouse ear. Dose-dependent reduction in flinching and licking in both the phases of pain sensation concludes the topical analgesic effect. Our findings suggest the potency of topical use of ACEOs for inflammatory disease conditions.

scholarly journals Anti-inflammatory activity of Syzygium cumini leaf against experimentally induced acute and chronic inflammations in rodents

2011 ◽  
Vol 1 (1) ◽  
pp. 6 ◽  
Author(s):  
Anirban Roy ◽  
Sanjib Bhattacharya ◽  
Jitendra N. Pandey ◽  
Moulisha Biswas
Keyword(s):  
Inflammatory Activity ◽  
Dependent Manner ◽  
Syzygium Cumini ◽  
Large Size ◽  
Paw Oedema ◽  
Chronic Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Dose Dependent ◽  
Rat Paw Oedema

<p><em>Syzygium cumini<strong> </strong></em>(L.) Skeels (Myrtaceae), commonly known as <em>Jam </em>in Bengali, <em>Jamun</em> in Hindi and <em>Black Plum</em> or <em>Black Berry</em> in English, is a large size evergreen tree indigenous to India and is cultivated for its fruits. In the present study, the methanol extract of leaves from <em>S. cumini </em>(MESC) was evaluated for anti-inflammatory activity in experimental acute (carrageenan, histamine and serotonin induced rat paw oedema) and chronic models (cotton pellet induced rat granuloma). In all models, the MESC (100 and 200 mg/kg body wt. p.o.) exhibited significant anti-inflammatory activity (<em>p &lt; 0.001</em>) in a dose dependent manner. These findings revealed that the <em>S. cumini </em>leaf had remarkable acute and chronic anti-inflammatory actions in the tested rodent models.</p>

scholarly journals Anti-inflammatory activity of soluble chito-oligosaccharides (CHOS) on VitD3-induced human THP-1 monocytes

PLoS ONE ◽  
2021 ◽  
Vol 16 (2) ◽  
pp. e0246381
Author(s):  
Paiboon Jitprasertwong ◽  
Munthipha Khamphio ◽  
Phornsiri Petsrichuang ◽  
Vincent G. H. Eijsink ◽  
Wanangkan Poolsri ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Vitamin D3 ◽  
Biological Effects ◽  
Water Soluble ◽  
Inflammatory Activity ◽  
Low Molecular Weight ◽  
Dependent Manner ◽  
Human Immune ◽  
Anti Inflammatory ◽  
Dose Dependent

Chito-oligosaccharides (CHOS) are oligomers of D-glucosamine and N-acetyl-glucosamine. Anti-inflammatory activities of a wide variety of CHOS mixtures have previously been reported, mainly based on studies with mouse models and murine macrophages. Since the mouse and human immune systems are quite different, gaining insight into the activity of CHOS on human cell lines, using well-characterized CHOS mixtures, is of considerable interest. Bacillus subtilis chitosanase (BsCsn46A) can efficiently convert chitosan to mixtures of water soluble low molecular weight CHOS. Here, the anti-inflammatory activity of a properly characterized CHOS mixture was studied, using human THP-1 cells that were differentiated to mature monocytes using vitamin D3. Addition of CHOS reduced the production of multiple pro-inflammatory cytokines associated with bacterial lipopolyssacharide (LPS)-stimulated inflammation, in a dose-dependent manner and without affecting cell viability. Interestingly, only minimal effects of CHOS were observed in similar experiments with phorbol 12-myristate 13-acetate- (PMA-) differentiated, macrophage-like, THP-1 cells. Altogether, in addition to showing promising biological effects of well-characterized low molecular weight soluble CHOS in a human system, the present study also points at Vitamin D3-stimulated THP-1 cells as a favorable system for assessing the anti-inflammatory activity of bioactive compounds.

scholarly journals Anti-Inflammatory Activity of Four Triterpenoids Isolated from Poriae Cutis

Foods ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 3155
Author(s):  
Lijia Zhang ◽  
Mengzhou Yin ◽  
Xi Feng ◽  
Salam A. Ibrahim ◽  
Ying Liu ◽  
...  
Keyword(s):  
High Speed ◽  
High Performance ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Dose Dependent

In this study, triterpenoid compounds from Poriae Cutis were separated by high-speed countercurrent chromatography (HSCCC) and identified using ultra-high performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry (UHPLC-QTOF-MS/MS) and nuclear magnetic resonance (NMR). The in vitro anti-inflammatory activities of the purified triterpenoids on RAW 264.7 cells were also investigated. Triterpenoids, poricoic acid B, poricoic acid A, dehydrotrametenolic acid, and dehydroeburicoic acid were obtained; their levels of purity were 90%, 92%, 93%, and 96%, respectively. The results indicated that poricoic acid B had higher anti-inflammatory activity than those of poricoic acid A by inhibiting the generation of NO in lipopolysaccharide (LPS)-induced RAW 264.7 cells. However, dehydrotrametenolic acid and dehydroeburicoic acid had no anti-inflammatory activity. In addition, the production of cytokines (TNF-α, IL-1β, and IL-6) in cells treated with poricoic acid B decreased in a dose-dependent manner in the concentration range from 10 to 40 μg/mL. The results provide evidence for the use of Poriae Cutis as a natural anti-inflammatory agent in medicines and functional foods.

Phytochemical, Quantitative Proximate and In vitro Anti-inflammatory Study of the Crude Methanol Extract of Stachytarpheta indica Leaves (Verbenaceae)

2019 ◽  
pp. 153-162
Author(s):  
Cyril Ogbiko ◽  
Dickson Achimugu Musa ◽  
Musa Usman Dabai ◽  
Ibeabuchi Jude Ali ◽  
Abubakar Sani Yelwa ◽  
...  
Keyword(s):  
Cardiac Glycosides ◽  
Methanol Extract ◽  
Proximate Analysis ◽  
Water Soluble ◽  
Inflammatory Activity ◽  
Dependent Manner ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Crude Methanol Extract

Herbal medicine despite its increase usage globally is being plagued by inadequate research on their effectiveness. Stachytarpheta indica commonly known as snakeweed is used locally in the management of asthma, headache, alopecia, bronchitis, bruise, chest cold, constipation, itch, diarrhea, skin sore, vermifuge, dysentery, dysmenorrhea among others. This study investigated the phytochemical composition, quantitative proximate parameters and in vitro anti-inflammatory activity of the leaves of S. indica using established methods. Results confirmed the presence of alkaloids, saponins, carbohydrate, cardiac glycosides, terpenoid, tannin, anthraquinones, phenolics and flavonoid. Moisture content (9.16 ± 0.04%), total ash (19.42 ± 0.15%), water insoluble ash (7.17 ± 0.22%), acid insoluble ash (3.63 ± 0.26%), alcohol soluble extractive (0.99 ± 0.06%) and water-soluble extractive (0.36 ± 0.02%) values were obtained from the quantitative proximate analysis. An infusion of the methanol leaf extract of Stachytarpheta indica demonstrated significant anti-inflammatory activity in a dose dependent manner comparable to that of indomethacin standard.

scholarly journals Neutral Lipids, Glycolipids, and Phospholipids, Isolated from Sandfish (Arctoscopus japonicus) Eggs, Exhibit Anti-Inflammatory Activity in LPS-Stimulated RAW264.7 Cells through NF-κB and MAPKs Pathways

Marine Drugs ◽  
2020 ◽  
Vol 18 (9) ◽  
pp. 480
Author(s):  
Weerawan Rod-in ◽  
Chaiwat Monmai ◽  
Il-sik Shin ◽  
SangGuan You ◽  
Woo Jung Park
Keyword(s):  
Nuclear Translocation ◽  
Neutral Lipids ◽  
Inflammatory Activity ◽  
Raw264.7 Cells ◽  
Dependent Manner ◽  
Tnf Α ◽  
Lipid Fractions ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Raw264.7 Macrophage

Total lipids were extracted from sandfish (Arctoscopus japonicus), and then they were separated into the following three lipid fractions: neutral lipids, glycolipids, and phospholipids. In this study, we analyzed the lipid fractions of A. japonicus eggs and we determined their anti-inflammatory activity in RAW264.7 macrophage cells. In these three lipid-fractions, the main fatty acids were as follows: palmitic acid (16:0), oleic acid (18:1n-9), docosahexaenoic acid (DHA, 22:6n-3), and eicosapentaenoic acid (EPA, 20:5n-3). Among the lipid fractions, phospholipids showed the highest concentration of DHA and EPA (21.70 ± 1.92 and 18.96 ± 1.27, respectively). The three lipid fractions of A. japonicus significantly suppressed the production of NO in macrophages. Moreover, they also significantly inhibited the expression of iNOS, COX-2, IL-6, IL-1β, and TNF-α, in a dose-dependent manner. Furthermore, the lipid fractions of A. japonicus suppressed the nuclear translocation of NF-κB p65 subunits in a dose-dependent manner. In addition, they attenuated the activation of MAPKs (p38, ERK1/2, and JNK) phosphorylation in LPS-stimulated RAW264.7 cells. These results indicate that all the lipid fractions of A. japonicus exert anti-inflammatory activity by suppressing the activation of NF-κB and MAPK pathways. Therefore, the lipid fractions of A. japonicus might be potentially used as anti-inflammatory agents.

scholarly journals Heterocornols from the Sponge-Derived Fungus Pestalotiopsis heterocornis with Anti-Inflammatory Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 585
Author(s):  
Hui Lei ◽  
Xiaoxu Bi ◽  
Xiuping Lin ◽  
Jianglian She ◽  
Xiaowei Luo ◽  
...  
Keyword(s):  
Chemical Study ◽  
Antimicrobial Activities ◽  
Sea Salt ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Inos Protein Expression ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Dose Dependent

One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus Pestalotiopsis heterocornis XWS03F09 resulted in the production of new secondary metabolites. The chemical study of the fermentation, cultivated on 3% artificial sea salt in the rice media, led to the isolation of twelve compounds, including eight new polyketide derivatives, heterocornols Q–X (1–8), one new ceramide (9), and three known analogues (10–12). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data and calculated ECD analysis. Heterocornols Q (1) and R (2) are novel 6/5/7/5 tetracyclic polyketide derivatives featuring dihydroisobenzofuran and benzo-fused dioxabicyclo [4.2.1] nonane system, which might be derived from the acetyl-CoA by epoxidation, polyene cyclization, and rearrangement to form the core skeleton. Compound 12 showed moderate or weak antimicrobial activities against with MIC values ranging from 25 to 100 μg/mL. Heterocornols T and X (7 and 8) could inhibit the production of LPS-induced NO significantly, comparable to dexamethasone. Further Western blotting analysis showed 7 and 8 markedly suppressed the iNOS protein expression in LPS-induced RAW 264.7 cells in a dose-dependent manner. The result showed that 7 and 8 might serve as potential leads for development of anti-inflammatory activity.

scholarly journals EVALUATION OF THE CYTOCHROME P450 INHIBITORY EFFECT OF THYME OLEORESIN FROM THYMUS VULGARIS L. - AN IN VITRO STUDY

2018 ◽  
Vol 11 (9) ◽  
pp. 149
Author(s):  
Adeline Persia R ◽  
Anitha Roy ◽  
Lakshmi T
Keyword(s):  
Cytochrome P450 ◽  
Potassium Phosphate ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Thymus Vulgaris ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Ic50 Value ◽  
Dose Dependent

Objective: The objective of this study was to evaluate the effect of thyme oleoresin on cytochrome P450 (CYP3A4) enzyme.Materials and Methods: The different concentrations of thyme (5–100 μg/ml) were examined for its inhibitory property toward cytochrome P450 isoform (CYP3A4). Thyme, potassium phosphate buffer, CYP450 reagent, and substrate 7-Benzyloxy-4-trifluoromethylcoumarin were added to a 96-well plate. The mixtures were preincubated for 20 min at room temperature. The fluorescent intensities of the products were measured by PerkinElmer Enspire fluorescence reader using an excitation and emission wavelength of 405 nm and 460 nm, respectively. Values are expressed as mean ± standard error mean (n=3). IC50 was calculated by plotting concentrations of thyme against the corresponding percent inhibition.Results: All the tested concentrations of thyme showed inhibitory effect against CYP3A4 in a dose-dependent manner. At 5 μg/ml, it showed a percentage inhibition of 1.82±0.61, whereas 100 μg/ml showed 66.05±0.16. The IC50 value of thyme for CYP3A4 inhibitory activity was found to be 39.14 μg/ml.Conclusion: This study proves that the inhibitory effect of thyme oleoresin on cytochrome P450. The inhibitory effects of thyme indicate the possibilities of herb-drug interaction if this extract is coadministered with prescribed drugs that are metabolized by CYP3A4.

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