An Anti-radical, Cytoprotective, Anti-proliferative, Anti-inflammatory and Toxicological Assessment of Metallo-porphyrins Isolated from Fresh Leaves of Spinacia oleracea L.

Aim: Synthetic lead molecules are associated with host of adverse effects while medicinal molecules isolated from natural sources are blessed with both safety as well as efficacy. The ancient doctrine of Ayurveda ardently advocates the therapeutic virtues contained in green leaves of Spinacia oleracea L. The principal constituent of the leaves is the class of metalloporphyrin chlorophyll, which is also the floral counterpart of faunal heme. Chlorophyll-a (Chl-a) and chlorophyll-b (Chl-b) are the cardinal members of the chlorophyll family. Study design: Herein, we have explored the anti-radical, cytoprotective, anti-inflammatory and anti-proliferative efficacy of Chl-a and Chl-b in reference to standard drug and crude extract of Spinacia leaves. The current study is aimed to establish, naturally mined metaloporphyrins as safe and efficacious replacement of synthetic leads that are associated with a wide range of toxicological issues. Methodology: Using a combination of Silica Gel-G column chromatography and preparative thin layer chromatography, the two principal green metallo-porphyrins (Chl-a and Chl-b) were sequentially extracted and isolated from crude extract of Spinacia oleracea L leaves. Antiradical efficacy, of the isolated green porphyrins was quantified by DPPH and Hydrogen peroxide radical scavenging assay. Cytoprotective efficacy was evaluated using ex-vivo hemolysis assay and anti-inflammatory potency was attested employing carrageenan induced paw edema bioassay. To enumerate on the anti-proliferative potency, MTT assay was employed, while toxicology of the isolates was evaluated employing OECD 420 acute toxicity guidelines. Findings: The study confirmed that isolated green porphyrins Chl-a and Chl-b as well as crude extract all exerts significant anti-radical, cytoprotective, anti-inflammatory and anti-proliferative efficacy however while potency of Chl-a was at par with that of reference standard and superior to the crude extract, Chl-b clocked in a value inferior to both. Furthermore, acute toxicity study indicated that even at p.o. dose of 2000mg/Kg b.w, no toxicity was manifested in either of the metalloporpyrin treated groups thus ascertaining the safe nature of the naturally mined metalloporphyrin entities. Also naturally mined Chl-a is not only a safer alternative to synthetic medicine but it is more potent and safe than its parent extract popularly used in herbal medicine. Conclusion: The results of the study indicates that Chl-a having a more profound structural resemblance to heme than Chl-b can be further modulated as a cost-effective and safe anti-radical alternative to synthetic leads in inhibiting inflammation and untoward cell proliferative while extending cyto-protection from pathological ROS generated in diseased states.

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

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i1.1879 ◽

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.

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Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity

Medicinal Chemistry ◽

10.2174/1573406416666200930114340 ◽

2020 ◽

Vol 16 ◽

Author(s):

Bhim Bahadur Chaudhari ◽

Alka Bali ◽

Ajitesh Balaini

Keyword(s):

Antioxidant Activity ◽

Oral Absorption ◽

Radical Scavenging ◽

Reducing Power ◽

Antioxidant Potential ◽

Inflammatory Activity ◽

In Vivo Models ◽

Standard Drug ◽

Hybrid Molecules ◽

Anti Inflammatory

Background: NSAIDs are the most widely prescribed medications worldwide for their anti-inflammatory, antipyretic, and analgesic effects However, their chronic use can lead to several adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastro-sparing NSAIDs also suffer from serious adverse effects which limit their efficacy. Objective: Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine, etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant) potential. Method: The designing process utilized three dimensional similarity studies and utilized an isoxazole core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity. The compounds were assayed for their antiinflammatory activity in established in vivo models. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. Results: Compounds (5, 6, 9 and 10) showed anti-inflammatory activity comparable to the standard drugs and were also found to be non-ulcerogenic at the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0-50.0 µmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good oral absorption. Conclusion: A new series of isoxazole based compounds is being reported with good anti-inflammatory activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.

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Bacterial endosymbiont inhabiting Leucaena leucocephala leaves and their antioxidant and antidiabetic potential

Journal of Complementary and Integrative Medicine ◽

10.1515/jcim-2020-0203 ◽

2020 ◽

Vol 0 (0) ◽

Author(s):

Sridevi Chigurupati ◽

Shantini Vijayabalan ◽

Kesavanarayanan Krishnan Selvarajan ◽

Ahmad Alhowail ◽

Fatema Kauser

Keyword(s):

Free Radical ◽

Crude Extract ◽

Leucaena Leucocephala ◽

Endophytic Bacteria ◽

Radical Scavenging ◽

16S Rrna Gene Sequencing ◽

Free Radical Scavenging ◽

Rrna Gene ◽

Standard Drug

AbstractObjectivesResearch on endosymbionts is emerging globally and is considered as a potential source of bioactive phytochemicals. The present study examines the antioxidant and antidiabetic of the endophytic crude extract isolated from Leucaena leucocephala leaves.MethodsEndophytic bacteria were isolated from the leaves of L. leucocephala and 16S rRNA gene sequencing was used to establish their identity. The in vitro antioxidant effect of endophytic crude extract (LL) was evaluated using 2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) free radical scavenging methods. The in vitro antidiabetic properties of LL were evaluated using α-amylase and α-glucosidase enzyme inhibition assay.ResultsThe isolated endophytic bacteria were identified as Cronobacter sakazakii. LL displayed potent free radical scavenging effect against ABTS and DPPH radicals with an inhibitory concentration 50% (IC50) value of 17.49 ± 0.06 and 11.3 ± 0.1 μg/mL respectively. LL exhibited α-amylase and α-glucosidase inhibition with an IC50 value of 23.3 ± 0.08 and 23.4 ± 0.1 μg/mL respectively compared to the standard drug (acarbose). Both glucose loaded normoglycemic rats and STZ induced diabetic rats treated with LL (200 mg/kg) exhibited a considerable reduction in blood glucose levels p<0.01 after 8 h of treatment when compared to normal and diabetic control rats respectively.ConclusionsThus, the study shows that LL has a wellspring of natural source of antioxidants, and antidiabetic agents and phytoconstituents present in endophytes could be the rich source for bioactive compounds.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11s2.28535 ◽

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.

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Phytochemical screening and HPLC- UV method quantiϐication of Flavonoids in Coffee Arabica green seeds

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11ispl4.4395 ◽

2020 ◽

Vol 11 (SPL4) ◽

pp. 1895-1904

Author(s):

Bothiraj K V ◽

Kalaivani P ◽

Murugan K ◽

Vanitha V

Keyword(s):

Radical Scavenging Activity ◽

Radical Scavenging ◽

Biologically Active ◽

Coffee Bean ◽

Green Coffee ◽

High Concentration ◽

Antimitotic Activity ◽

Wide Range ◽

Anti Inflammatory ◽

Green Coffee Bean

The green coffee bean is the most commonly used beverages in India and it is one of the most commercialised food products. They have a rich source of biologically active compounds that are important for human health. The coffee tree or a shrub belongs to the family Rubiaceae. Commercially available, two species of green coffee bean are Coffea Arabica and Coffea canephora. Cancer is the most important cause of death. Apart from cancer, quercetin can also prevent Osteoporosis. The phytochemicals present in the green coffee bean can be used as an alternate therapy for cancer due to its antimitotic activity and free radical scavenging activity. Total antioxidant shows IC50 value 45.81. Kaempferol is a potent antioxidant that can defence against free radicals and cure chronic diseases. Flavonoids are phenolic substances that act as an antioxidant, anti-inflammatory, anti-allergenic, antiviral and also have vasodilating actions. Green coffee bean shows a high concentration of Flavonoids in hydroethanolic extraction. The aim of this study is used to analyse the presence of Flavonoids in green coffee bean by using High-performance Liquid Chromatography (HPLC). Flavonoids are potent antioxidant that can bind to a protein. Flavonoids show a wide range of biological and pharmacological activities like anti-allergic, anti-inflammatory, anti-cancer and anti-microbial activity.

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Nauclea latifolia Sm. Leaf Extracts Extenuates Free Radicals, Inflammation, and Diabetes-Linked Enzymes

Oxidative Medicine and Cellular Longevity ◽

10.1155/2020/5612486 ◽

2020 ◽

Vol 2020 ◽

pp. 1-13 ◽

Cited By ~ 1

Author(s):

Franklyn Nonso Iheagwam ◽

Emmanuel Nsedu Israel ◽

Kazeem Oyindamola Kayode ◽

Opeyemi Christianah DeCampos ◽

Olubanke Olujoke Ogunlana ◽

...

Keyword(s):

Competitive Inhibition ◽

Radical Scavenging ◽

Reducing Power ◽

Peroxide Radical ◽

Hypotonic Solution ◽

Leaf Extracts ◽

Inhibitory Activities ◽

Anti Inflammatory ◽

Nauclea Latifolia

This study was carried out to assess the in vitro antioxidant, anti-inflammatory and antidiabetic effects of Nauclea latifolia (Sm.) leaf extracts. Ethanolic (NLE) and aqueous (NLA) extract of N. latifolia leaves were prepared and assessed for their anti-inflammatory activity, antioxidant potential, α-amylase and α-glucosidase inhibitory activities, and the mechanism of enzyme inhibition in vitro using standard established methods. From the results, phytochemicals such as flavonoids, phenolics, glycosides, and tannins were detected in both extracts of N. latifolia with NLE having a significantly (p<0.05) higher phytochemical content. NLE displayed significantly (p<0.05) better total antioxidant capacity, reducing power, 2,2-diphenyl-2-picrylhydrazyl, and hydrogen peroxide radical scavenging activities. For anti-inflammatory activities, 70.54±2.45% albumin denaturation inhibition was observed for NLE while 68.05±1.03% was recorded for NLA. Likewise, 16.07±1.60 and 14.08±1.76% were obtained against hypotonic solution and heat-induced erythrocyte haemolysis, respectively, for NLE while 20.59±4.60 and 24.07±1.60% were respective NLA values. NLE (IC50: 4.20±0.18 and 1.19±0.11 mg/mL) and NLA (IC50: 11.21±0.35 and 2.64±0.48 mg/mL) α-glucosidase and α-amylase inhibitory activities were dose-dependent with uncompetitive and competitive inhibition elicited, respectively, by the extracts. A significant positive association (p<0.01 and 0.05) was identified between antioxidant activity and carbohydrate-metabolising enzyme inhibitory activity. The obtained result suggests N. latifolia leaf could serve as an alternative candidate for managing diabetes mellitus due to its antioxidant and anti-inflammatory association with diabetes-linked enzymes.

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Comparative Anti-Inflammatory and Analgesic Activities of Qurs-Saffron and Quknar Polyherbal Tablets in Mouse Model

RADS Journal of Pharmacy and Pharmaceutical Sciences ◽

10.37962/jpps.v7i4.342 ◽

2020 ◽

Vol 7 (4) ◽

pp. 199-205

Author(s):

Muhammad Shoaib Akhtar ◽

Abdul Malik ◽

Haroon Arshad ◽

Nabiha Pervez ◽

Nadeem Irshad

Keyword(s):

Radical Scavenging ◽

Toxicity Testing ◽

Paw Edema ◽

Standard Drug ◽

Analgesic Effects ◽

Parametric Data ◽

Anti Inflammatory ◽

Analgesic Activities ◽

Radical Scavenging Properties ◽

One Way Anova

Objective: We aimed to study the anti-inflammatory and analgesic effects for two polyherbal tablets in animal model. Methods: Suspensions of Qurs-Saffron and Quknar polyherbal formulations (p.o.) were evaluated for their anti-inflammatory (in carrageenan-induced paw edema) and analgesic activities (in formalin-induced paw licking test) in albino mice using Ibuprofen (50 mg/kg, orally) as standard drug. Acute toxicity testing of suspensions from Qurs-Saffron and Quknar tablets was also performed at doses 1, 2 and 3 gm/kg, orally. Parametric data were evaluated by one way ANOVA followed by Tukey’s test while graphics were made using GraphPad Prism. Results: Administration of Qurs-Saffron (1000, 1500, 2000 mg/kg) and Quknar (500, 750, 1000 mg/kg) suspensions showed significant (P < 0.05) inhibition of paw edema and at later time point (after 3 hours), both suspensions showed highly significant (P < 0.001) inhibition of paw edema. In another experiment (formalin-induced paw licking test), Qurs-Saffron (2000 mg/kg) and Quknar (1000 mg/kg) showed the highly significant (P < 0.001) analgesic activity. Conclusion: Qurs-Saffron and Quknar tablets possessed anti-inflammatory and analgesic effects that were most likely due to flavonoids and phenolic compounds with free radical scavenging properties which significantly reduced inflammation and pain in treated mice and were also found safe in toxicity testing.

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Preparation and Photosynthesis-Inhibiting Activity of Novel Dihalogenated 3-Hydroxynaphthalene-2-carboxanilides

Proceedings ◽

10.3390/ecsoc-23-06596 ◽

2019 ◽

Vol 41 (1) ◽

pp. 30

Author(s):

Jiri Kos ◽

Tomas Gonec ◽

Tomas Strharsky ◽

Michal Oravec ◽

Josef Jampilek

Keyword(s):

Electron Transport ◽

Photosystem Ii ◽

Spinacia Oleracea ◽

Photosynthetic Electron Transport ◽

Microwave Assisted Synthesis ◽

Inhibiting Activity ◽

Microwave Assisted ◽

Spinacia Oleracea L ◽

Wide Range

In this study, a series of nine 3-hydroxynaphthalene-2-carboxanilides, disubstituted on the anilide ring by fluorine, chlorine and bromine in various positions, was prepared by microwave-assisted synthesis and characterized. The compounds were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The PET-inhibiting activity of the compounds was within a wide range, but rather moderate; the highest activity within the series of the compounds was observed for N-(3,5-difluorophenyl)-3-hydroxynaphthalene-2-carboxamide (IC50 = 9.8 µM). The compounds were found to inhibit PET in photosystem II.

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Radical scavenging potency of 2-(benzofuran-2-yl)-2-oxoethyl 3-(methyl/amino)benzoate: synthesis, crystal structure and Hirshfeld surface analysis

Zeitschrift für Kristallographie - Crystalline Materials ◽

10.1515/zkri-2017-2083 ◽

2018 ◽

Vol 233 (2) ◽

pp. 125-134

Author(s):

Li Yee Then ◽

C.S. Chidan Kumar ◽

Huey Chong Kwong ◽

Siau Hui Mah ◽

Wan-Sin Loh ◽

...

Keyword(s):

Crystal Structures ◽

Molecular Conformation ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Three Dimensional ◽

Computational Method ◽

Peroxide Radical ◽

Standard Drug ◽

Scavenging Effect ◽

Phenyl Rings

AbstractTwo novel 2-(benzofuran-2-yl)-2-oxoethyl 3-(methyl/amino)benzoates2(a–b), were synthesized under mild conditions and characterized by spectroscopic analysis. The three-dimensional (3D) crystal structures of these compounds were further determined using single crystal X-ray diffraction technique and revealed that both compounds tend to twist away with respect to their attached carbonyl groups at the C(=O)–C–O–C(=O) connecting bridge, exhibiting a nearly perpendicular conformation with torsion angle in a range of 75–94°. In both compounds, each of the benzofuran and substituted phenyl rings are individually planar while almost perpendicular to each other. Their molecular conformation are comparable with related structures from the Cambridge Structural Database (CSD). Furthermore, the intermolecular interactions in these crystal structures were quantified and analyzed using Hirshfeld surfaces computational method. The quantitative data on the percentage contributions of overall interactions on the molecules 2a and 2b (A&B) is calculated by the 2-D fingerprint plots from the HS analysis. These structures were evaluated for their antioxidant properties by diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ferrous ion chelating (FIC) and hydrogen peroxide radical scavenging assays (H2O2). Noteworthy, compound2bwith an amino substituent attached to the phenyl ring exhibited an IC50value of 45.37 μg/mL in H2O2scavenging assay, which showed better scavenging effect than the standard drug, ascorbic acid (IC50=81.02 μg/mL).

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STEROLS BIOACTIVITY OF RUTA GRAVEOLENS L. AND MURRAYA PANICULATA L.

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.15790 ◽

2017 ◽

Vol 9 (2) ◽

pp. 103

Author(s):

Doha H. Abou Baker ◽

Eman A. Ibrahim ◽

Ahmed Kandeil ◽

Farouk K. El Baz

Keyword(s):

Anticancer Activity ◽

Antioxidant Activities ◽

Diclofenac Sodium ◽

Radical Scavenging ◽

A549 Cells ◽

Ruta Graveolens ◽

Plant Leaves ◽

Standard Drug ◽

Murraya Paniculata ◽

Anti Inflammatory

Objective: Ruta graveolens L. (R. graveolens) and Murraya paniculata L. (M. paniculata) are medicinal plants belonging to Rutaceae family have many uses in traditional medicine. The aim of the present study was to investigate sterols bioactivity of the two Rutaceae plant leaves.Methods: Sterols of the two Rutaceae plant leaves were identified using GC/MS. The antioxidant activities of the sterols of these herbs were evaluated by three different methods; free radical scavenging using 2,2′-Azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), 1,1-Diphenyl-2-picryl-hydrazyl (DPPH) and total antioxidant activity. The anticancer activity of the sterols was determined by MTT assay against colorectal cancer HCT116, breast cancer MCF7, liver cancer HepG2 and lung cancer A549 cell lines. Anti-inflammatory activity was evaluated using albumin denaturation assay and antiviral activities against H5N1 virus were carried out using plaque reduction assay.Results: GC/MS assay showed β-Sitosterol (36%) as the most abundant sterols of R. graveolens followed by stigmasterol (18%), while stigmasterol (25.2%) was the most abundant one of M. paniculata steroids. The anti-inflammatory potential of R. graveolens steroids was significantly higher than that of diclofenac sodium (standard drug). M. paniculata sterols have higher antiviral activity (IC50= 0.15 of µg/ml) than R. graveolens sterols (IC50= 7.8 of µg/ml). The sterols of R. graveolens showed anticancer activity against MCF7 and A549 cells with inhibition 84.3 and 81%, at 100 µg/ml respectively. While M. paniculata sterols showed 77.3% inhibition against A549 cells.Conclusion: The current study suggests that the sterols of M. paniculata have more anti-viral activity than R. graveolens sterols which showed more anticancer and anti-inflammatory activities.

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