scholarly journals 1, 3-Thiazolidine-4-Ones: Copper Nickel Oxide Bimetallic Nanoparticle Catalyzed Synthesis, Anticancer Potential and Molecular Modeling Studies

2021 ◽  
Author(s):  
Ramesh L. Sawant ◽  
Manisha R. Sawant ◽  
Jyoti B. Wadekar ◽  
Rushikesh D. Ukirde ◽  
Ganesh D. Barkade ◽  
...  
Keyword(s):  
Nickel Oxide ◽  
Radical Scavenging ◽  
Test Drug ◽  
Nickel Oxide Nanoparticles ◽  
Copper Nickel ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Anti Inflammatory ◽  
Radical Scavenging Assay

Abstract Background: Cancer is a leading cause of death worldwide. Inhibiting mitosis is the most effective clinical technique for cancer treatment. The most critical field of medicinal chemistry and drug development research is the discovery of innovative anticancer drugs. Thiazolidine is a multifunctional nucleus with anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic, antihyperlipidemic, and antiarthritic properties. Methods: In this investigation, copper-nickel oxide nanoparticles synthesized by electrochemical synthesis yielded a significant yield. The capping was done with cetyltrimethyl ammonium bromide (CTAB), and the characterization was done with UV, FTIR, XRD, SEM-EDS, and TEM SAED. The biologically significant 2-(2-substituted-4-oxo-thiazolidine-3-yl)-1, 9-dihydro-purin-6-ones (GB-1 to GB-12) have been synthesized using copper-nickel oxide nanoparticles as a catalyst and by applying a microwave-assisted tool. It was characterized by melting point, IR, 1H NMR, 13C NMR and LC-HRMS/MS spectroscopy. Using Sulforhodamine B (SRB) test, all newly synthesized compounds were evaluated in vitro for anti-cancer, anti-inflammatory, antioxidant, and angiogenesis activities. Results: The compounds GB-6 (GI50: 30 μM), GB-8 (GI50: 10 μM) and GB-10 (GI50: 30 μM) exhibited significant cell growth inhibitory activity. The compounds GB-6, GB-8, GB-10 exhibited significant in vitro anti-inflammatory activity in the range of IC50:179.65-194.59 μg/ml as compared with aceclofenac (IC50:191.19μg/ml) and the antioxidant activity by DPPH radical scavenging assay the compounds GB-6 (IC50:11.96 µg/ml), GB-8 (IC50:10.67 µg/ml) and GB-10 (IC50: 9.08 µg/ml) exhibited excellent radical scavenging activities compared to ascorbic acid (IC50:13.04 µg/ml) and by the KMnO4 radical scavenging assay the compounds GB-2 (IC50:15.33 µg/ml), GB-4 (IC50:23.60 µg/ml), GB-8 (IC50:24.93 µg/ml), GB-10 (IC50:24.96 µg/ml) exhibited good radical scavenging activities compared to ascorbic acid (IC50: 26.55 µg/ml). The compounds GB-4, GB-8 and GB-10 at 10 nM test drug concentration and the GB-6 compounds at 100 nM test drug concentration show the maximum capillary growth inhibitory activity compared with thalidomide as a standard drug. Conclusion: Further development of anticancer drugs may be enabled by the discovery of related compounds to the anticancer agent, such as compound (GB-6), compound (GB-8), and compound (GB-10) as polo-like kinase 1 inhibitors.

scholarly journals Phytogenic Synthesis of Nickel Oxide Nanoparticles (NiO) Using Fresh Leaves Extract of Rhamnus triquetra (Wall.) and Investigation of Its Multiple In Vitro Biological Potentials

Biomedicines ◽  
2020 ◽  
Vol 8 (5) ◽  
pp. 117 ◽  
Author(s):  
Javed Iqbal ◽  
Banzeer Ahsan Abbasi ◽  
Riaz Ahmad ◽  
Mahboobeh Mahmoodi ◽  
Akhtar Munir ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Nickel Oxide ◽  
Biological Activities ◽  
Radical Scavenging ◽  
New Drugs ◽  
In Vivo Studies ◽  
Oxide Nanoparticles ◽  
Nickel Oxide Nanoparticles ◽  
X Ray

Chemically nickel oxide nanoparticles (NiONPs) involve the synthesis of toxic products, which restrict their biological applications. Hence, we developed a simple, eco-friendly, and cost-efficient green chemistry method for the fabrication of NiONPs using fresh leaf broth of Rhamnus triquetra (RT). The RT leaves broth was used as a strong reducing, capping, and stabilizing agent in the formation of RT-NiONPs. The color change in solution from brown to greenish black suggests the fabrication of RT-NiONPs which was further confirmed by absorption band at 333 nm. The synthesis and different physicochemical properties of RT-NiONPs were investigated using different analytical techniques such as UV-Vis (ultraviolet−visible spectroscopy), XRD (X-ray powder diffraction), FT-IR (Fourier-transform infrared spectroscopy), SEM (scanning electron microscopy), TEM (transmission electron microscopy), EDS (energy-dispersive X-ray spectroscopy), DLS (dynamic light scattering) and Raman. Further, RT-NiONPs were subjected to different in vitro biological activities and revealed distinctive biosafe and biocompatibility potentials using erythrocytes and macrophages. RT-NiONPs exhibited potential anticancer activity against liver cancer cell lines HUH7 (IC50: 11.3 µg/mL) and HepG2 (IC50: 20.73 µg/mL). Cytotoxicity potential was confirmed using Leishmanial parasites promastigotes (IC50: 27.32 µg/mL) and amastigotes (IC50: 37.4 µg/mL). RT-NiONPs are capable of rendering significant antimicrobial efficacy using various bacterial and fungal strains. NiONPs determined potent radical scavenging and moderate enzyme inhibition potencies. Overall, this study suggested that RT-NiONPs can be an attractive and eco-friendly candidate. In conclusion, current study showed potential in vitro biological activities and further necessitate different in vivo studies in various animal models to develop leads for new drugs to treat several chronic diseases.

scholarly journals PHARMACOLOGICAL STUDIES: ANTIBACTERIAL, ANTIOXIDANT, AND ANTI-INFLAMMATORY EFFICACY OF CASUARINA EQUISETIFOLIA ROOT EXTRACTS

2018 ◽  
Vol 11 (8) ◽  
pp. 270 ◽  
Author(s):  
Saranya Vtk ◽  
Uma Gowrie S
Keyword(s):  
Hydrogen Peroxide ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Root Extract ◽  
Casuarina Equisetifolia ◽  
Root Extracts ◽  
Anti Inflammatory ◽  
Reducing Power Assay ◽  
Radical Scavenging Assay

Objective: The current study was aimed to investigate the potential phytoconstituents from Casuarina equisetifolia root extract. Qualitative, quantitative and gas chromatography–mass spectrometry (GC-MS) analysis of C. equisetifolia using various solvents of root extract was also carried out to characterize the presence of various bioactive compounds in the root. The research work was also targeted to reveal the antibacterial, antioxidant, and anti-inflammatory potential of the root extract of C. equisetifolia.Methods: Root samples of C. equisetifolia were collected from Nimilenchery village, Pondicherry Union territory. The qualitative screening of the root extracts was carried out to check the presence of various phytoconstituents which was then followed by the quantitative analysis of phenols, flavonoids, and tannins. Further, the phytochemicals in the root extract were evaluated using GC-MS studies. In vitro antibacterial activity was performed by the agar well diffusion method using aqueous and organic solvent-based root extract against four different bacterial pathogens. In vitro antioxidant assay of different solvent extracts was elucidated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, hydrogen peroxide radical scavenging assay, and reducing power assay. Anti-inflammatory potential was also studied using protein denaturation of albumin.Results: The qualitative phytochemical screening revealed the presence of various phytoconstituents which is of greater biological importance. Gallic acid equivalent (GAE) phenolic compound content (68.64±0.25 mg GAE/g of extract), quercetin equivalent flavonoid content (29.09±0.14 mg of QUE/g of extract), tannic acid equivalent (TAE) tannin content (51±0.42 mg TAE/g of extract), and terpenoid content (5.2%) were found to be significant in the methanol root extract of C. equisetifolia when compared with other solvents. GC-MS analysis revealed different peaks indicating the presence of different secondary metabolites. Prominent antibacterial activity was observed in methanol extract of root, with maximum zone of inhibition exhibited against Proteus vulgaris (23.45±0.28 mm). The methanol root extract was most effective with half maximal inhibitory concentration (IC50) 52.74±0.65 μg/ml for DPPH and 64.94±0.24 μg/ml for hydrogen peroxide scavenging activity. Maximum absorbance was observed by 80 μg/ml (IC50 51.79±0.26 μg/ml) of methanol root extract with respect to reducing power assay. In vitro anti-inflammatory activity had maximum inhibition of 84.6±0.26 with IC50 value of 33.6±0.23 μg/ml at 80 μg/ml.Conclusion: From this study, it is revealed that the species of C. equisetifolia is a source of potential phytoconstituents exhibiting significantly various biological activities leading to the development of novel drug.

scholarly journals Ethosomes and Transethosomes for Mangiferin Transdermal Delivery

Antioxidants ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 768
Author(s):  
Maddalena Sguizzato ◽  
Francesca Ferrara ◽  
Supandeep Singh Hallan ◽  
Anna Baldisserotto ◽  
Markus Drechsler ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Radical Scavenging ◽  
Human Keratinocytes ◽  
Antioxidant Response ◽  
Correlation Spectroscopy ◽  
Inflammatory Status ◽  
Transmission Electron ◽  
Anti Inflammatory

Mangiferin is a natural glucosyl xanthone with antioxidant and anti-inflammatory activity, making it suitable for protection against cutaneous diseases. In this study ethosomes and transethosomes were designed as topical delivery systems for mangiferin. A preformulation study was conducted using different surfactants in association with phosphatidylcholine. Vesicle dimensional distribution was monitored by photon correlation spectroscopy, while antioxidant capacity and cytotoxicity were respectively assessed by free radical scavenging analysis and MTT on HaCaT keratinocytes. Selected nanosystems were further investigated by cryogenic transmission electron microscopy, while mangiferin entrapment capacity was evaluated by ultracentrifugation and HPLC. The diffusion kinetics of mangiferin from ethosomes and transethosomes evaluated by Franz cell was faster in the case of transethosomes. The suitability of mangiferin-containing nanovesicles in the treatment of skin disorders related to pollutants was investigated, evaluating, in vitro, the antioxidant and anti-inflammatory effect of ethosomes and transethosomes on human keratinocytes exposed to cigarette smoke as an oxidative and inflammatory challenger. The ability to induce an antioxidant response (HO-1) and anti-inflammatory status (IL-6 and NF-kB) was determined by RT-PCR and immunofluorescence. The data demonstrated the effectiveness of mangiferin loaded in nanosystems to protect cells from damage. Finally, to gain insight into the keratinocytes’ uptake of ethosome and transethosome, transmission electron microscopy analyses were conducted, showing that both nanosystems were able to pass intact within the cells.

scholarly journals Semi-Synthesis of Harringtonolide Derivatives and Their Antiproliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1380
Author(s):  
Xiutao Wu ◽  
Lijie Gong ◽  
Chen Chen ◽  
Ye Tao ◽  
Wuxi Zhou ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Normal Cell ◽  
Selectivity Index ◽  
Cytotoxic Activities ◽  
Structure Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Hct 116 ◽  
Systematic Structure

Harringtonolide (HO), a natural product isolated from Cephalotaxus harringtonia, exhibits potent antiproliferative activity. However, little information has been reported on the systematic structure−activity relationship (SAR) of HO derivatives. Modifications on tropone, lactone, and allyl positions of HO (1) were carried out to provide 17 derivatives (2–13, 11a–11f). The in vitro antiproliferative activity against four cancer cell lines (HCT-116, A375, A549, and Huh-7) and one normal cell line (L-02) was tested. Amongst these novel derivatives, compound 6 exhibited comparable cell growth inhibitory activity to HO and displayed better selectivity index (SI = 56.5) between Huh-7 and L-02 cells. The SAR results revealed that the tropone and lactone moieties are essential for the cytotoxic activities, which provided useful suggestions for further structural optimization of HO.

scholarly journals IN VITRO ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITIES OF HINGULESWARA RASABASED HERBOMINERAL FORMULATIONS

2018 ◽  
Vol 11 (14) ◽  
pp. 24
Author(s):  
Abhishek Chatterjee ◽  
Dileep Singh Baghel ◽  
Bimlesh Kumar ◽  
Saurabh Singh ◽  
Narendra Kumar Pandey ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Standard Drug ◽  
Three Samples ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Antioxidant Effects ◽  
Made In ◽  
In Vitro Antioxidant Activity

Objective: The aims of the present investigation were to develop the herbal and/or herbomineral formulations of Hinguleswara rasa and to compare their anti-inflammatory and antioxidant activities, in vitro, with that of standard drug samples.Methods: This study was an interventional investigation in three samples: In the first sample, Hinguleswara rasa (HR1) was prepared as per methodology described in Rasatarangini using Shuddha Hingula (10 g), Shuddha Vatsanabha (10 g), and Pippali (10 g). In the second and third sample, respectively, Hinguleswara rasa was prepared by replacing Shuddha Hingula with Kajjali where Kajjali made from Hingulotha parada and Sodhita parada constitutes two varieties of Hinguleswara rasa, i.e. HR2 and HR3. In vitro antioxidant activity was studied using 2,2-diphenyl-1-picrylhydrazyl, and the absorbance was recorded at 517 nm. For evaluating the in vitro anti-inflammatory studies, the inhibition of albumin denaturation technique was performed.Results: The results showed that the formulation of Hinguleswara rasa has shown dose-dependent activity which was observed in 100 μg concentration. HR1, HR2, and HR3 showed 36.11, 17.22, and 16.11% radical scavenging activity.Conclusion: It could be concluded that the changes made in the formulations did not affect the in vitro anti-inflammatory and antioxidant effects of the herbomineral formulations.

scholarly journals Plasmodium falciparum Line-Dependent Association ofIn VitroGrowth-Inhibitory Activity and Risk of Malaria

2012 ◽  
Vol 80 (5) ◽  
pp. 1900-1908 ◽  
Author(s):  
Josea Rono ◽  
Anna Färnert ◽  
Daniel Olsson ◽  
Faith Osier ◽  
Ingegerd Rooth ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Inhibitory Activity ◽  
Content Type ◽  
Phenotypic Differences ◽  
Erythrocyte Invasion ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Control Study

ABSTRACTPlasmodium falciparum's ability to invade erythrocytes is essential for its survival within the human host. Immune mechanisms that impair this ability are therefore expected to contribute to immunity against the parasite. Plasma of humans who are naturally exposed to malaria has been shown to have growth-inhibitory activity (GIA)in vitro. However, the importance of GIA in relation to protection from malaria has been unclear. In a case-control study nested within a longitudinally followed population in Tanzania, plasma samples collected at baseline from 171 individuals (55 cases and 116 age-matched controls) were assayed for GIA using threeP. falciparumlines (3D7, K1, and W2mef) chosen based on their erythrocyte invasion phenotypes. Distribution of GIA differed between the lines, with most samples inhibiting the growth of 3D7 and K1 and enhancing the growth of W2mef. GIA to 3D7 was associated with a reduced risk of malaria within 40 weeks of follow-up (odds ratio, 0.45; 95% confidence interval [CI], 0.21 to 0.96;P= 0.04), whereas GIA to K1 and W2mef was not. These results show that GIA, as well as its association with protection from malaria, is dependent on theP. falciparumline and can be explained by differences in erythrocyte invasion phenotypes between parasite lines. Our study contributes knowledge on the biological importance of growth inhibition and the potential influence ofP. falciparumerythrocyte invasion phenotypic differences on its relationship to protective immunity against malaria.

Evaluation of the genotoxic properties of nickel oxide nanoparticles in vitro and in vivo

2018 ◽  
Vol 836 ◽  
pp. 47-53 ◽  
Author(s):  
Raíne F. De Carli ◽  
Débora dos S. Chaves ◽  
Tatiane R. Cardozo ◽  
Ana Paula de Souza ◽  
Allan Seeber ◽  
...  
Keyword(s):  
Nickel Oxide ◽  
Oxide Nanoparticles ◽  
Nickel Oxide Nanoparticles

2,5-disubstituted-4-thiazolidinones: Synthesis, anti-inflammatory, free radical scavenging potentials and structural insights through molecular docking

2021 ◽  
Vol 18 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A Chawla ◽  
Rohit Bhatia ◽  
Shamsher Singh
Keyword(s):  
Free Radicals ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Assay Method ◽  
Acidic Group ◽  
Active Compounds ◽  
Cox 2 ◽  
Anti Inflammatory

: The present work reports synthesis and screening of fifteen 2,5-disubstituted-4-thiazolidinones with different substitutions of varied arylidene groups at imino. The structures of the compounds were confirmed by spectral characterization. The compounds were subjected to in vivo anti-inflammatory and in vitro antioxidant activities. The derivatives possessed remarkable activities quite close to standard drugs used. Unlike conventional non-selective NSAIDs, the synthesized compounds did not contain any acidic group, thereby ensuring a complete cure from ulcers. To further substantiate the claim for safer derivatives, the active compounds were docked against the cyclooxygenase (COX)-2 enzyme. It was found that 4-fluorophenylimino substituent at 2- position and 3-nitro moiety on a 5-benzylidene nucleus of the 4-thiazolidinone derivative fitted in the COX-2 binding pocket. The compounds exhibited remarkable activity in scavenging free radicals, as depicted by the DPPH assay method. The structure-activity relationship was also established in the present work with respect to the nature and position of the substituents. The active compounds were evaluated for drug-like nature under Lipinski’s rule of five, and the toxicity behaviour of active compounds was predicted using ADMETlab software. The compounds have the potential to target degenerative disorders associated with inflammation and the generation of free radicals.

Evaluation of Anti-oxidant and Anti-pyretic activity of fruits of Garcinia pedunculata

2021 ◽  
pp. 2635-2638
Author(s):  
Mrinmoy Basak ◽  
Moksood Ahmed Laskar ◽  
Priyanka Goswami
Keyword(s):  
Methanol Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Traditional Use ◽  
Synthetic Drugs ◽  
Long Time ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Dpph Radical Scavenging

Most of the synthetic drugs used at present as analgesic and anti-inflammatory agents cause many side effects and toxic effects. Many medicines of plant origin with analgesic and anti-inflammatory activity have been used since long time without adverse effects. The purpose of the study was to explore the anti-pyretic and anti-oxidant activity of fruits of Garcinia pedunculata. The fruit of G. pedunculata was collected from Shillong, Meghalaya and extraction is done by using methanol as a solvent. The methanol extract shows the presence of carbohydrate, glycoside, alkaloids, phenol and flavonoids. Acute anti-pyretic activity for the extract was investigated in pyrexia rat. Temperature level was determined after 1hours, 4 hours, 8 hours and 12 hours after giving the extract dose of 100mg/kg and 200mg/kg body weight, and it was found to produce a significant reduce in fever. DPPH radical scavenging activity (In-vitro anti-oxidant activity of G. pedunculata) of methanolic extract shows 38.31 as IC50 (µg/ml) whereas Ascorbic acid as standard in the same concentration shows 34.81 IC50 (µg/ml). The obtained result justified the traditional use of G. pedunculata as anti-pyretic and antioxidant purpose.

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