scholarly journals Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives

2020 ◽  
Vol 67 (4) ◽  
pp. 1139-1147
Author(s):  
Fatih Tok ◽  
Bedia Koçyiğit-Kaymakçıoğlu
Keyword(s):  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Spectroscopic Methods ◽  
Design Synthesis ◽  
Reference Drug ◽  
Ic50 Values ◽  
Adme Properties ◽  
Anti Inflammatory ◽  
In Vitro Antioxidant Activity

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the α-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 μM) and their IC50 values were in the range of 0.68 and 4.45 μM. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski’s and Veber’s rules.

scholarly journals Design, Synthesis, in Vitro Antioxidant, Anti-Inflammatory and Antidiabetic Evaluation of New N-Substitutedbenzylidene-5-(4-Formylphenyl)-(3-Hydroxyphenyl)-4,5-Dihydropyrazole-1-Carbothioamide Derivatives

2020 ◽  
Author(s):  
Sucheta Singh Singh ◽  
sumit Tehlan Tehlan ◽  
prabhakar kumar verma
Keyword(s):  
Antioxidant Activity ◽  
Heterocyclic Compounds ◽  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Clinical Potential

Abstract A series of N-substitutedbenzylidene-5-(4-formylphenyl)-(3-hydroxyphenyl)-4,5-dihydropyrazole-1-carbothioamide derivatives was designed, synthesized and examined for their therapeutical potential against prooxidant (oxidative stress), inflammation and diabetes. Biological results showed antioxidant activity with IC50 value 37.68 mol/L, anti-inflammatory activity with IC50 value 26.40 mol/L and antidiabetic activity with IC50 value 17.12 mol/L. The results of antioxidant activity showed that compounds Y9 and Y17 exhibited excellent antioxidant activity with IC50 values 17.43 mol/L and 18.98 mol/L, results of anti-inflammatory activity showed that compounds Y2, Y3 and Y7 exhibited excellent anti-inflammatory activity with IC50 values 23.23 mol/L, 22.09 mol/L and 19.05 mol/L respectively and results of antidiabetic activity showed that compounds Y1, Y5and Y6 exhibited excellent antidiabetic activity with IC50 values 17.08 mol/L, 8.36 mol/L and 13.50 mol/L. When compared with ascorbic acid, aspirin and acarbose as standard drug respectively. Heterocyclic compounds have diversity in their structure which makes them broad and economical therapeutic agents. Pyrazole is a five membered ring containing three carbon and two neighboring nitrogen atoms. Pyrazole and its derivatives have various biological as well as clinical potential thus considered for further research. Due to wide range of therapeutical activities pyrazole makes interest among researcher to explore it further for more activities. Pyrazole is present in various biological moieties eg. antimicrobial, antidiabetic, anti-inflammatory, antioxidant, antiviral, anticonvulsant, anticancer, anti-HIVand anti-tuberculosis agents.

scholarly journals Demonstration of Phytochemicals and In-vitro Antioxidant and Anti-inflammatory activity by methanolic extract of Elettaria cardamomum

2020 ◽  
Vol 3 (3) ◽  
pp. 01-04
Author(s):  
Md. Shahidul Islam
Keyword(s):  
Methanolic Extract ◽  
Research Work ◽  
Inflammatory Activity ◽  
Pharmacological Activities ◽  
Elettaria Cardamomum ◽  
Ic50 Values ◽  
Phytochemical Profile ◽  
Anti Inflammatory ◽  
Dpph Scavenging

The existing research study attempts to untie novel avenues for development of the medicinal exercises of Elettaria cardamomum, fashionable known as the “Queen of Spices” and locally recognized as “elaichi”. Its seeds are utilized as abortifacient, acrid, alexiteric, aromatic, sweet, cardiac tonic, cooling, carminative, digestive, diuretic, expectorant, stimulant and also tonic beneficial in the asthma, haemorrhoids, bronchitis, strangury, renal in addition to vesical calculi, anorexia, halitosis, gastropathy dyspepsia as well as burning sensation. The prime goal of this research work is to evaluate antioxidant as well as anti-inflammatory properties of the traditional Bangladeshi medicinal extracts in addition to examine these activities. The aim in present work was to screen the phytochemical profile as well as pharmacological activities of the methanolic extract of this plant’s leaves. To explore pharmacological actions DPPH scavenging test and the HRBC membrane stabilization techniques were done for the antioxidant and also anti-inflammatory test respectively. The pharmacological works revealed that plant extracts might have noteworthy antioxidant effect which is possibly mediated by the inhibition of DPPH free radical which is accountable for oxidation. The IC50 values by the DPPH scavenging test observed for the standard and the leaves were 106.38µg/ml & 594.47µg/ml respectively. There is also moderate anti-inflammatory activity. The IC50 values for anti-inflammatory activity by standard & leaves were 35.04µg/ml and 944.0 µg/ml respectively.

scholarly journals Phenanthrenes in Chinese Yam Peel Exhibit Anti-inflammatory Activity, as Shown by Strong in Vitro Cyclooxygenase Enzyme Inhibition

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Qian Li ◽  
Chuan-Rui Zhang ◽  
Amila A. Dissanayake ◽  
Qun-yu Gao ◽  
Muraleedharan G. Nair
Keyword(s):  
Food Item ◽  
Inflammatory Activity ◽  
Spectroscopic Methods ◽  
Over The Counter ◽  
Chinese Yam ◽  
Inflammatory Drugs ◽  
In Vitro Bioassays ◽  
Anti Inflammatory ◽  
Cox 1

Chinese yam ( Dioscorea opposita), peeled or whole, is a popular food item that is considered to be healthy. Often, the yam is peeled before cooking. However, it is also consumed with peel. Therefore, in this study, the peel of this yam was extracted sequentially with n-hexane, ethyl acetate and methanol, and studied for its health-benefits, using in vitro bioassays. Bioactivity-guided purifications of extracts of the peel afforded phenanthrenes (1-4), as characterized by spectroscopic methods. Phenanthrene 1 is a novel analogue. The extracts and isolates were tested for anti-inflammatory activity using cyclooxygenase enzyme (COX-1 and -2) inhibitory assays. All phenanthrenes isolated from the yam peel showed higher inhibition of COX enzymes than the over-the-counter nonsteroidal anti-inflammatory drugs (NSAIDs) aspirin, ibuprofen and naproxen.

scholarly journals In-vitro Anti-diabetic and Antioxidant Efficacy of Methanolic Extract of Canthium coromandelicum Leaves

2020 ◽  
pp. 12-18
Author(s):  
S. Thiripura Salini ◽  
S. Shankar
Keyword(s):  
Diabetic Complications ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Antidiabetic Activity ◽  
Dpph Radical ◽  
Dpph Assay ◽  
Ic50 Value ◽  
Ic50 Values ◽  
In Vitro Antioxidant Activity

Oxidative stress plays a major role in diabetic complications. The study aim was to investigate the in-vitro antidiabetic and antioxidant activities of methanolic extract of Canthium coromandelicum leaves. The plant material was extracted with methanol and the methanolic extract was screened for in-vitro antioxidant activity using 1, 1-diphenyl-2-picryl hydrazyl (DPPH) assay. The efficiency of the antidiabetic activity of the plant extract was evaluated against α-amylase and α-glucosidase digestive enzymes. The study revealed that the C. coromandelicum extract exhibited significant α-amylase and α-glucosidase inhibitory activities with an IC50 value of 31.52 ± 0.42 and 41.49 ± 0.28 µg/mL respectively and compared with standard acarbose drug. The extract efficiently scavenging DPPH radical with IC50 values of 65.46 ± 0.50 µg/ml. Therefore, the extract could be a promising therapeutic in management of diabetic complications.

scholarly journals In vitro antioxidant activity of crude extracts of Harpagophytum zeyheri and their anti-inflammatory and cytotoxicity activity compared with diclofenac

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Sibonokuhle F. Ncube ◽  
Lyndy J. McGaw ◽  
Emmanuel Mfotie Njoya ◽  
Hilton G. T. Ndagurwa ◽  
Peter J. Mundy ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Inflammatory Activity ◽  
In Vitro Assays ◽  
Tnf Α ◽  
Low Toxicity ◽  
Anti Inflammatory ◽  
Ethyl Acetate Extracts ◽  
In Vitro Antioxidant Activity

Abstract Background This study evaluated the in vitro antioxidant activity and comparison of anti-inflammatory and cytotoxic activity of Harpagopytum zeyheri with diclofenac. Methods In vitro assays were conducted using water, ethanol, and ethyl acetate extracts of H.zeyheri. The antioxidant activity was evaluated using the 2,2′-diphenyl-1-picrylhydrazy (DPPH) and 2,2′- azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. The anti-inflammatory activity was determined by measuring the inhibition of nitric oxide (NO) on lipopolysaccharide (LPS)-induced RAW 264.7 mouse macrophages as well as cytokine (TNF-α and IL-10) expression on LPS-induced U937 human macrophages. For cytotoxicity, cell viability was determined using the 3-(4, 5-dimethylthiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results The ethyl acetate extract had the lowest IC50 values in the DPPH (5.91 μg/ml) and ABTS (20.5 μg/ml) assay compared to other extracts. Furthermore, the ethyl acetate extracts effectively inhibited NO and TNF-α and proved to be comparable to diclofenac at some concentrations. All extracts of H. zeyheri displayed dose-dependent activity and were associated with low levels of human-IL-10 expression compared to quercetin. Furthermore, all extracts displayed low toxicity relative to diclofenac. Conclusions These findings show that H. zeyheri has significant antioxidant activity. Additionally, similarities exist in the inflammatory activity of H. zeyheri to diclofenac at some concentrations as well as low toxicity in comparison to diclofenac.

scholarly journals EVALUATION OF ANTI-INFLAMMATORY AND ANTIDIABETIC ACTIVITY OF SIMAROUBA GLAUCA BARK EXTRACT: AN IN VITRO STUDY

2020 ◽  
pp. 74-78
Author(s):  
ALEESHA R ◽  
BHARAT MISHRA
Keyword(s):  
In Vitro Study ◽  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Bark Extract ◽  
Potential Candidate ◽  
Bioactive Constituents ◽  
Ic50 Value ◽  
Anti Inflammatory ◽  
Simarouba Glauca

Objectives: The present study was envisaged to identify the effect of anti-inflammatory and antidiabetic activity for methanolic bark extracts of Simarouba glauca. Methods: The present study design was to evaluate the in vitro anti-inflammatory and in vitro antidiabetic activity of S. glauca methanolic bark extract. To examine the antidiabetic activity, the samples were studied for their effect on inhibition of alpha-amylase and glucose transport across the dialysis membrane. In vitro anti-inflammatory activity was evaluated using albumin denaturation assay and membrane stabilization method. Results: Our current results indicate that the various bioactive constituents detected in S. glauca may be responsible for its in vitro antidiabetic and anti-inflammatory effects. The ability of plant extract on anti-inflammatory activity showed that it was effective in inhibiting heat-induced albumin denaturation with an IC50 value of test and standard was found to be 46.42 μg/ml and 24.09 μg/ml. In addition to this, heat-induced hemolysis was also performed. The IC50 values of the test and standard were found to be 43.51 μg/ml and 21.41 μg/ml, respectively. The percentage inhibition of the test sample varied from the concentration range of 75 to 100 μg/ml. The IC50 value of the test and standard was found to be 19.08 μg/ml and 9.08 μg/ml, respectively. Conclusion: The findings of the present study concluded that S. glauca bark has the potential to treat diabetes and a novel natural anti-inflammatory agent as a good source. Thus, S. glauca may be a potential candidate for the development of future antidiabetic and anti-inflammatory compounds. However, still further studies and standardization of the plant research may be required to develop them as medicine.

scholarly journals In Vitro Anti-Inflammatory Activity in Arthritic Synoviocytes of A. brachypoda Root Extracts and Its Unusual Dimeric Flavonoids

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5219
Author(s):  
Carlota Salgado ◽  
Hugo Morin ◽  
Nayara Coriolano de Aquino ◽  
Laurence Neff ◽  
Cláudia Quintino da Rocha ◽  
...  
Keyword(s):  
High Speed ◽  
Inflammatory Activity ◽  
Enzyme Linked Immunosorbent Assay ◽  
Root Extract ◽  
Traditional Use ◽  
Ic50 Values ◽  
Anti Inflammatory ◽  
Counter Current

Arrabidaea brachypoda is a plant commonly used for the treatment of kidney stones, arthritis and pain in traditional Brazilian medicine. Different in vitro and in vivo activities, ranging from antinociceptive to anti-Trypanosoma cruzi, have been reported for the dichloromethane root extract of Arrabidaea brachypoda (DCMAB) and isolated compounds. This work aimed to assess the in vitro anti-inflammatory activity in arthritic synoviocytes of the DCMAB, the hydroethanolic extract (HEAB) and three dimeric flavonoids isolated from the DCMAB. These compounds, brachydin A (1), B (2) and C (3), were isolated both by medium pressure liquid and high-speed counter current chromatography. Their quantification was performed by mass spectrometry on both DCMAB and HEAB. IL-1β activated human fibroblast-like synoviocytes were incubated with both extracts and isolated compounds to determine the levels of pro-inflammatory cytokine IL-6 by enzyme-linked immunosorbent assay (ELISA). DCMAB inhibited 30% of IL-6 release at 25 µg/mL, when compared with controls while HEAB was inactive. IC50 values determined for 2 and 3 were 3-fold higher than 1. The DCMAB activity seems to be linked to higher proportions of compounds 2 and 3 in this extract. These observations could thus explain the traditional use of A. brachypoda roots in the treatment of osteoarthritis.

scholarly journals EVALUATION OF IN VITRO ANTI-INFLAMMATORY ACTIVITY OF CITRUS MACROPTERA MONTR

2020 ◽  
pp. 101-103
Author(s):  
SONAM BHUTIA
Keyword(s):  
In Vitro Model ◽  
Diclofenac Sodium ◽  
Test Sample ◽  
Scientific Data ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Vitro Model

Objective: The use of naturally occurring medicines dependent on essential oils (EOs) is nowadays of great interest. In addition, within the human body, EO shows high efficacy as antioxidants and anti-inflammatory drugs. The present experiment was conducted to access the anti-inflammatory activity of EO obtained from the fruit peels of Citrus macroptera Montr. (Rutaceae) against the denaturation of protein in vitro model. Methods: The test sample (EO) was incubated under controlled laboratory conditions at varying concentrations with egg albumin and was subjected to absorbance determination for the anti-inflammatory property analysis. Diclofenac sodium was used as the standard reference drug for the experiment. Results: The results show a concentration-dependent inhibition of protein (albumin) denaturation by the test oil. This was concluded by comparing their IC50 average values. Citrus macroptera Montr. EO possessed IC50 average value 54.6+0.07 μg/mL, whereas that of diclofenac sodium was found to be 52.89+0.06 μg/ml. The result shows that the test oil is more effective than the standard drug. Conclusion: From the above experimental finding, it can be concluded that Citrus macroptera Montr. EO has significance anti-inflammatory effect against the denaturation of the protein in vitro model. The activity may be due to the presence of terpene polyphenolic component or some other active compound present in the oil. The provided information was first of its kind of knowledge to keep the scientific data for future reference.

Sign in / Sign up

Export Citation Format

Share Document