Synthesis of Asymmetric 1-Thiocarbamoyl Pyrazoles as Potent Anti- Colon Cancer, Antioxidant and Anti-Inflammatory Agent

2019 ◽  
Vol 18 (15) ◽  
pp. 2117-2123 ◽  
Author(s):  
Dattatraya G. Raut ◽  
Sandeep B. Patil ◽  
Vikas D. Kadu ◽  
Mahesh G. Hublikar ◽  
Raghunath B. Bhosale
Keyword(s):  
Colon Cancer ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Assay Method ◽  
Anticancer Activities ◽  
Cancer Society ◽  
Standard Drug ◽  
Anti Inflammatory

Background: Cancer is one of the leading diseases responsible for deaths in the society. According to the American cancer society, there will be 95,270 new cases of colon cancer in the U.S. in 2016. When a normal cell turns cancerous they develop into tumours, which produce various pro-inflammatory and inflammatory cytokines and chemokines that attract leukocytes to the site of growth. The main aim of this paper is to introduce readers about the increased number of cancer patient, effects of cancer and need of research on same. Methods: The target molecules were prepared by reacting pyrazolealdehyde with appropriate aromatic ketone by using polyethylene glycol (PEG-300) as green solvent and catalyst to yield chalcone. Furthermore, the reaction of chalcones with thiosemicabazide yields asymmetric 1-thiocarbamoyl pyrazoles. All the newly synthesized compounds were in vitro screened for their anticancer activities against Colon SW-620 by employing the sulforhodamine B (SRB) assay method. Also all the synthesized compounds tested for in vitro antioxidant and anti-inflammatory activity by using known literature methods. Results: Preliminary in vitro evaluation indicated that most of the compounds 4c, 4d and 4e possess distinct cytotoxicity profile against Colon SW-620 cell line compared to standard drug adriamycin. All the tested compounds showed good to excellent antioxidant activity against one or more reactive (H2O2, DPPH, SOR and NO) radical scavenging species. Additionally, all the synthesized compounds were screened for their in vitro antiinflammatory activity. Compounds 4a, 4b and 4e shows potent anti-inflammatory activity as compared to diclofenac sodium as a standard reference. Conclusion: New anti- Colon SW-620 cancer agents are the need of time, we trust that 1-thiocarbamoyl pyrazole derivatives 4c, 4d and 4e constitute an interesting template for the evaluation of new anticancer agent also antioxidant and anti-inflammatory work may provide an interesting insight for further development.

scholarly journals In-vitro Antioxidant and Anti-inflammatory Activities of Quisqualis indica Linn. Leaves Extract

2019 ◽  
pp. 1-13
Author(s):  
Pallavi Pal ◽  
Ajeet Singh
Keyword(s):  
Protein Denaturation ◽  
Radical Scavenging Activity ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Total Phenolic ◽  
Scavenging Activity ◽  
Standard Drug ◽  
Anti Inflammatory

Aim: In this study antioxidant and anti-inflammatory effect of ethanolic extract of Quisqualis indica leaves was evaluated. Study Design: In-vitro analysis of Quisqualis indica leaf extract. Place and Duration of Study: Molecular Biology laboratory, Department of Biotechnology, G.B Pant Engineering College, Pauri, between July 2015 and July 2016. Methods: Non-enzymatic and enzymatic assays such as DPPH (1, 1diphenyl-2-picryl hydrazyl), FRAP assay, superoxide dismutase SOD (EC 1.15.1.1), catalase (EC 1.11.1.6), for radical scavenging activity of ethanolic extracts of Quisqualis indica Linn. plant leaves had done. For estimation of anti-inflammatory action, two methods were employed: protein denaturation method and membrane stabilization method. Results: Ethanolic extract of leaves on higher concentration had better antioxidant potential when compared with reference standard ascorbic acid. They exhibited strong antioxidant radical scavenging activity values for ethanolic extract of leaves. Results of anti-inflammatory method suggested better potential values for ethanolic extract and compared with standard drug diclofenac sodium respectively. A significant relationship between antioxidant, anti-inflammatory capacity and total phenolic content was examined, indicating that phenolic compounds are the major contributors for the antioxidant and anti-inflammatory properties of this plant. Conclusion: Ethanolic extract of Q. indica exhibited strong anti-inflammatory and antioxidant activity and this can be used for designing novel drug inhibitors with better efficacy.

scholarly journals Garcinia Mangostana Leaf Extracts from Ivory Coast Possess Remarkable Antioxidant, Anti-Inflammatory, and Cytotoxicological Properties

2019 ◽  
Vol 12 (2) ◽  
pp. 571-578
Author(s):  
Inès Christelle Chadon Alphonsine Assemian ◽  
Abdelhakim Bouyahya ◽  
Nadia Dakka ◽  
Youssef Bakri
Keyword(s):  
Ivory Coast ◽  
Leaf Extract ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Total Phenolic ◽  
Garcinia Mangostana ◽  
Leaf Extracts ◽  
Standard Drug ◽  
Anti Inflammatory

Garcinia mangostana L. is medicinal plant. Its fruit, the mangosteen contains many bioactive xanthones. This study investigates the potential of organic leaf extracts of G. mangostana grown in Ivory Coast. We tested two organic leaf extracts: G. mangostana aqueous ethanolic leaf extract (ethanol: water, 80:20 v/v) (GMLE) and dichloromethane leaf extract (GMLD). We measured total phenolic and total Flavonoids. We analysed the in vitro anti-inflammatory, anti-radical and anti-proliferative activities of leaf extracts. Ethanol leaf extract showed a considerable amount of phenolic content (328.78±34.32 mg GAE/g) and moderate flavonoids content (43.60±1.48 mg QE/g), Dichloromethane extract had low values of phenolic (70.31±4.55 mg GAE/g) and flavonoids (8.49±0.69 mg QE/g). However, GMLD extract gave a significant anti-inflammatory activity (IC50=152.79±3.34 µg/mL), comparable to the standard drug diclofenac sodium (IC50=142.30±1.22 µg/mL), contrary to GMLE extract (IC50=652.33±12.23 µg/mL). The radical scavenging assay showed a very significant ability of ethanol leaf extract to reduce the DPPH radical (IC50=33.40±0.67 µg/mL) compared to references molecules such as Trolox (IC50=43.72±0.31 µg/mL) and acid ascorbic (IC50=27.20±0.17 µg/mL), dichloromethane extract results showed lowest activity (IC50 = 580.00±23.03 µg/mL). All the organic leaf extracts of G. mangostana had moderate anti-proliferative activity on L20B, RD and VS cell lines studied with IC50 values ranging from 110.89 ±4.82 µg/mL to 860.60±25.78 µg/mL). Our results prove the high potential of the G. mangostana leave extracts as anti-inflammatory and anti-oxidative stress drugs. However, further studies are to determine and validate all the medicinal properties of G. mangostana leaves extracts.

IN VITRO ANTI-INFLAMMATORY ACTIVITY OF METHANOLIC EXTRACT AND DIFFERENT FRACTIONS OF CENTELLA ASIATICA LEAVES BY PROTEIN DENATURATION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (06) ◽  
pp. 86-89
Author(s):  
S Sharma ◽  
◽  
R. Trivedi ◽  
N. K. Choudhary
Keyword(s):  
Petroleum Ether ◽  
Skin Diseases ◽  
Methanolic Extract ◽  
Protein Denaturation ◽  
Diclofenac Sodium ◽  
Centella Asiatica ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Anti Inflammatory

Inflammation might be a complex organic reaction to a hazardous stimulant such as pathogens, or injured tissues and mainly causes itching, swelling, skin redness, warm and slight pain. Herbal drugs are widespread in India for their effectiveness, easy availability at low cost and provide low toxicity as compared to modern drugs. Centella asiatica is one of the oldest Ayurvedic medicinal plants, used in treatment of various skin diseases. The aim of our present research was to evaluate the in vitro anti-inflammatory activity of methanolic extract and different fractions of C. asiatica leaves. In protein denaturation method, the percentage inhibition for methanolic extract was observed to be 40.22%. The petroleum ether and n-butanol fraction of methanolic extract of C. asiatica were observed to exhibits 54.12 and 44.42% inhibition, respectively. Diclofenac sodium was used as a standard drug. In comparison with other fractions petroleum ether and n-butanol fractions showed best activity. The preliminary phytochemical studies of n-butanol fractions and n-butanol fractions showed the presence of terpenoids, flavonoids etc., which are used in the treatment of inflammation. Thus, we can call the latter as intense anti-inflammatory agent.

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.

scholarly journals Assessment of in vitro Antioxidative and Anti-Inflammatory Effect of Caesalpinia Bonducella Seed Stabilized Silver Nanoparticles

2020 ◽  
Vol 11 (1) ◽  
pp. 693-701
Author(s):  
Gloria Jemmi Christobel R ◽  
Kasi Selvi N ◽  
Shyam Sundar J. ◽  
Abirami M.P. ◽  
Nebita Maria Jarrett ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Radical Scavenger ◽  
Frap Assay ◽  
Standard Drug ◽  
Wide Range ◽  
Caesalpinia Bonducella ◽  
Anti Inflammatory

Membrane lipid peroxidation and DNA, protein damage is mediated by free radicals, which form the basis of chronic pathological complications.AgNPs are an important class of nanomaterials for a wide range of biomedical applications. The present study endeavors in vitro antioxidant and anti-inflammatory activity of green synthesized silver nanoparticles (AgNPs) using medicinal plant extract from Caesalpinia bonducella seeds. Total flavonoid and phenolic contents were determined. The antioxidant potential of capped AgNPs was assessed using DPPH assay, Phosphomolybdenum assay, FRAP assay, metal chelating, hydrogen peroxide, and hydroxyl radical scavenging methods. In vitro anti-inflammatory assay of CB seed, AgNPs were performed against the standard drug. CB seed AgNPs possessed high flavonoid and phenol compared to aqueous CB seed extract. The antioxidant methods confirmed that the silver nanoparticles have more antioxidant activity as compared to vitamin C. The synthesized silver nanoparticles exhibited potential anti-inflammatory activity with the IC50 71.3µg/ml. Hence, this work clearly demonstrated that the coated AgNPs with CB seeds act as a potent free radical scavenger and could be considered as a potential source for anti-inflammatory drugs.

scholarly journals EVALUATION OF IN VITRO ANTIDIABETIC AND ANTI-INFLAMMATORY ACTIVITIES OF LEAVES EXTRACT OF BOEHMERIA RUGULOSA

2018 ◽  
Vol 11 (9) ◽  
pp. 200
Author(s):  
Abha Shukla ◽  
Anchal Choudhary
Keyword(s):  
Protein Denaturation ◽  
Diclofenac Sodium ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Standard Drug ◽  
Successive Extraction ◽  
Ic50 Value ◽  
Anti Inflammatory

Objective: The objective of the study is to evaluate in vitro antidiabetic and anti-inflammatory activity of different extracts of leaves of Boehmeria rugulosa by different methods.Methods: In vitro α-glucose and α-amylase were used for antidiabetic activity and lipoxygenase, and protein denaturation method of inhibition assays was used to measure anti-inflammatory activity. Successive extraction of leaves petroleum ether (PE), chloroform (CH), ethyl acetate (EA), acetone (AC), and ethanol (ETH) was performed, and extracts obtained from the extraction were applicable to these activities.Results: The AC extract of leaves shows significantly in vitro antidiabetic activity, and AC has offered significant result 470.07±0.65 μg/mL in the inhibition of α-glucosidase and also for α-amylase assay 698.15±1.71 μg/mL. Acarbose was used as standard. In lipoxidase method, AC had shown better results and in protein denaturation method EA shown the higher inhibition (78.06±0.5 μg/ml) than the other extracts. The standard drug diclofenac sodium also offered significant inhibition against lipoxidase enzyme method with IC50 value 21.76±1.29 μg/mL.Conclusion: These findings suggest that the AC and EA possess potent antidiabetic and anti-inflammatory activities in vitro conditions.

scholarly journals SYNTHESIS OF 1-BENZOYL-3-PHENYL-1H-PYRAZOLE-4-CARBALDEHYDE AND EVALUATION OF THEIR ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY

2021 ◽  
pp. 48-52
Author(s):  
BONO NAGA SUDHA ◽  
N YELLA SUBBAIAH ◽  
MANCHALA MAHALAKSHMI
Keyword(s):  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Proton Nuclear Magnetic Resonance ◽  
Significant Activity ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
Antioxidant Potency ◽  
Anti Inflammatory

Objective: The main objective of this study is to synthesize a series of 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives and evaluation of the synthesized compounds for their antioxidant and anti-inflammatory activity. Methods: A series of substituted acetophenones are condensed with hydrazides to the corresponding hydrazones which are subsequently cyclized by using vilsmier-Haack reaction to give final series of 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives respectively. All newly synthesized compounds were characterized on the basis of infrared, proton nuclear magnetic resonance and mass spectral data and screened for their antioxidant and anti-inflammatory activities. Results: In view of the significant biological activity profile of Pyrazole, the synthesized compounds (4a-e) were evaluated for their antioxidant potency by DPPH, Nitric oxide, Hydroxyl radical scavenging, and Hydrogen Peroxide method. Compounds 4c and 4e showed potent antioxidant activity then standard. Synthesized compounds were also screened for anti-inflammatory activity. Among all the molecules 4c, 4e, and 4d showed significant activity as compared to standard drug diclofenac sodium. Conclusion: in this study, we synthesized 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives. Further, these derivatives showed significant antioxidant and anti-inflammatory activity. Among them, two molecules 4c and 4e have shown near action to the standard.

Anti-Inflammatory Activity of Human Lens Crystallin Derived Peptide

2021 ◽  
Vol 18 ◽  
Author(s):  
Anuraag Muralidharan ◽  
Tenzin Tender ◽  
Pallavi K Shetty ◽  
Srinivas Mutalik ◽  
Krishna Sharma K ◽  
...  
Keyword(s):  
Free Radical ◽  
Skin Permeation ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Inflammatory Activity ◽  
Human Lens ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Inflammation has become the culmination point for several chronic diseases like skin diseases, asthma, neurological disorders, cancer and cardiovascular disorders. Mini αA-crystallin peptide, identified from a highly conserved region of human lens protein αA-crystallin, is known to have a chaperone-like function, hence has generated interest in exploring the anti-inflammatory potential of the peptide. Objective: The objective of the study was to evaluate anti-inflammatory potential of mini αA chaperone using in vitro, ex-vivo and in vivo models. Methods: The peptide was tested for its phosphodiestarase4 B inhibition, anti-inflammatory and free radical scavenging abilities in HaCat cells. Carbopol gel formulations with varying concentrations of mini αA-crystallin peptide and diclofenac sodium were prepared and optimized. Skin permeation studies of prepared formulations were carried out on excised abdominal skin of Wistar rat using a vertical type diffusion cell. Carrageenan induced rat paw oedema model was used for determining the anti-inflammatory potential of the peptide in prepared gel formulation with or without diclofenac sodium. Results: The peptide exhibited appreciable free radical scavenging and weak PDE4B inhibition. Gel formulation with 1% Tween-80, 1% carbopol and 10% ethanol showed better permeation compared to other formulations. The in vitro skin permeation studies revealed good improvement in permeation characteristics of diclofenac and peptide from the gels. The peptide was retained within the skin tissue, which is an ideal requirement for the delivery of anti-inflammatory topical formulation. In preclinical anti-inflammatory studies, gel formulation containing mini αA-peptide and diclofenac sodium showed a significant decrease in paw volume compared to other combinations tested. Conclusion: The study revealed the additive effect in anti-inflammatory activity by combining mini-αA peptide and diclofenac sodium which effectively reduced the inflammation.

scholarly journals IN VITRO ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY OF THE FLOWER EXTRACTS OF OPUNTIA STRICTA

2019 ◽  
pp. 208-212
Author(s):  
PRABHAKARAN D ◽  
RAJESHKANNA A ◽  
SENTHAMILSELVI MM
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Radical Scavenging ◽  
Ethyl Acetate Fraction ◽  
Inflammatory Activity ◽  
Assay Method ◽  
No Production ◽  
Dpph Radical ◽  
Anti Inflammatory

Objective: The objective of this study was to evaluate the antioxidant and anti-inflammatory activities of the solid powder obtained from the ethyl acetate fraction from the flower Opuntia stricta. Methods: The flower extract was evaluated for antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay and reducing power assay was carried out by ferric-reducing capacity (FRC) assay method. The in vitro anti-inflammatory activity was evaluated using human peripheral blood mononuclear cells (PBMCs) stimulated by lipopolysaccharide (LPS) to evaluate nitric oxide (NO) production method. Results: The solid powder obtained from the ethyl acetate fraction from the flower O. stricta showed a good antioxidant activity in scavenging DPPH radical and FRC assay with compared standard sample. This solid powder also showed good anti-inflammatory activity in cell viability (LPS-induced PBMCs) assay and NO assay. Conclusion: These results suggest that the solid powder obtained from the ethyl acetate fraction from the flower O. stricta has significant antioxidant and anti-inflammatory activities.

scholarly journals EVALUATION OF THE ANTI-INFLAMMATORY ACTIVITY OF COMBINATION OF ETHANOL EXTRACTS OF AZADIRACHTA INDICA (NEEM) AND LAWSONIA INERMIS (HENNA)

2016 ◽  
Vol 9 (5) ◽  
pp. 256
Author(s):  
Tirupathi Rao ◽  
Renuka P ◽  
Akhil P ◽  
Divya P ◽  
Devi Priyanka P
Keyword(s):  
Azadirachta Indica ◽  
Protein Denaturation ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Cell Protein ◽  
Inhibition Activity ◽  
Lawsonia Inermis ◽  
Standard Drug ◽  
Anti Inflammatory

ABSTRACTObjective: The aim of the present study was to investigate the in vitro anti-inflammatory activity of Azadirachta indica (neem) and Lawsonia inermis(henna) individual extract and in combination using the same solvent.Methods: The leaf material of A. indica and L. inermis was collected from surroundings of Aditya College of Pharmacy, Kakinada, East Godavari.Powdered material was subjected to successive solvent extraction process. The yield was collected and prepared different concentrations (50, 100,and 200 µg/ml) of plant extracts. Diclofenac sodium was used as standard drug. The anti-inflammatory activity was performed by in vitro methodssuch as albumin denaturation method and human red blood cells membrane lysis method.Results: Denaturation of proteins is a well-documented cause of inflammation. Neem showed a significant membrane stabilizing activity of 46.62%and protein denaturation inhibition activity of 57.32% at concentration of 200 µg/ml. Henna showed a significant membrane stabilizing activityof 39.89% and protein denaturation inhibition activity of 53.75% at 200 µg/ml. In combination, both the extracts showed a significant membranestabilizing activity of 56.63% and protein denaturation inhibition activity of 67.69% at concentration of 200 µg/ml.Conclusion: The present study concluded that combination of A. indica and L. inermis possesses significant anti-inflammatory activity when comparedwith individual extract.Keywords: Anti-inflammatory, Human red blood cell, Protein denaturation, Lawsonia inermis, Azadiracta indica.

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