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A simple and eco-friendly method has been used for the synthesis of novel compound 4-(3,5-di-tert-butyl-4-hydroxybenzylidene)-3-methylisoxazol-5(4H)-one. The synthesized compound was characterized by its physical andspectral data. This compound was screened for in-vitro antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH)and nitric oxide free radical scavenging assays at 100 µM concentration. The DPPH scavenging ability of evaluatedcompound was superior to the synthetic antioxidant butylated hydroxytoluene (BHT) and comparable to the standardascorbic acid. The nitric oxide scavenging ability of the compound was also found greater than the BHT. The insilico prediction of molecular properties and bioactivity scores of synthesized compound and BHT were carried outusing Molinspiration Cheminformatics online software. The study revealed that the predicted compounds obeyedLipinski’s rule of five and showed good intestinal absorption and membrane permeability indicating the drug-likenessproperties of predicted compounds. Finally, the in silico study identified the title compound as a nuclear receptorligand compared to BHT.
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Objective: The present work deals with the qualitative study of the phytoconstituents present in Aegialitis rotundifolia Roxb., ethanolic leaves extract and evaluate its antioxidant properties in vitro. Methods: The qualitative phytochemical analysis of the extract was performed first using preliminary phytochemical tests and then by liquid chromatography quadrupole-time-of-flight mass spectrometry (LC-Q-TOF-MS). The antioxidant properties were investigated comprehensively using seven in vitro models viz., 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, nitric oxide (NO) scavenging, hydrogen peroxide (H2O2) scavenging, superoxide (SOD) radical scavenging, lipid peroxidation (LPO) assay, reducing power (RP), and total antioxidant activity. Results: The preliminary phytochemical analysis revealed the presence of several important phytochemical groups whereas the LC-Q-TOF-MS analysis detected 25 phytoconstituents in the extract mostly belonging to flavonoids and alkaloids. The test extract showed strong dose-dependent antioxidant activity in all the seven in vitro models, however, the activity of the extracts was slightly lower compared to the reference standard ascorbic acid. Conclusion: The test extract showed strong antioxidant properties which could be possibly due to the phytoconstituents detected in the extract.
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The present study was undertaken to evaluate the in vitro and in vivo antioxidant effects of different extracts prepared from the leaves of Xanthium strumarium. Polyphenols and flavonoids contents in all extracts were determined by spectrophotometric assays, antioxidant and antiradical capacities of the extracts were assayed using 2, 2-diphenyl-1-picrylhydrazyl radical (DPPH) radical scavenging assay, reducing power, β-carotene and anti-hemolytic assay. In addition, the in vivo antioxidant activity of three concentrations of leaves crude extract was investigated. Antioxidant activity of the crude extract was examined using anti-hemolytic assay and the determination of Glutathione and malondialdehyde (MDA) contents and catalase activity. In vitro antioxidant assays showed that crude extract and its fractions have strong effects in scavenging DPPH and reducing power. These activities decreased in the following order: ethyl acetate extract (EAE) > aqueous extract (AqE) > crude extract (CrE) > chloroform extract (ChE). The β-carotene bleaching assay showed that the CrE had the highest antioxidant activity followed by the EAE, AqE and the ChE. However, the anti-hemolytic test demonstrated that the ChE was the most effective in protecting red blood cells, followed by the EAE, AqE and the CrE. Three concentrations of leaves crude extract were tested for the in vivo antioxidant assays, and anti-hemolytic Catalase activity and the content of both MDA and Glutathione (GSH) were estimated. Among these tests, X. strumarium crude extract exhibited a potent inhibition of lipid peroxidation. It was concluded that X. strumarium extracts contain high phenolic content and have powerful antioxidant capacity in vitro and in vivo. These extracts were found to be safe with no toxic effects. These findings support the traditional use of this plant as an anti-inflammatory remedy.
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Objective: To study physicochemical properties, antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids. Methods: The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization. Then the reaction of substituted coumarins (a-e) with potassium O-ethyl/methyl carbonodithioate (1) by using absolute ethanol as solvent,afforded coumarin-carbonodithioate (1a-1j) derivatives under microwave irradiation and the conventional method. The spectroscopic analysis was used for the characterization of coumarin derivatives. The title (1a-1j) compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard. Drug-likeness. In-silico toxicity was predicted with LD50 value and bioactivity score was also calculated for all the compounds. Results: All coumarin (1a-1j) compounds exhibited promising in-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs. All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule. It was observed that the synthesized compounds followed rule of five, indicating more 'drug-like' nature. Conclusions: All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities. From the physicochemical properties of coumarin derivatives, it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five. It is concluded that the coumarin-carbonodithioate hybrids act with more 'drug-like' nature.
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Objective: To study physicochemical properties, antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids. Methods: The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization. Then the reaction of substituted coumarins (a-e) with potassium O-ethyl/methyl carbonodithioate (1) by using absolute ethanol as solvent, afforded coumarin-carbonodithioate (1a-1j) derivatives under microwave irradiation and the conventional method. The spectroscopic analysis was used for the characterization of coumarin derivatives. The title (1a-1j) compounds were confirmed by spectroscopic methods. Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard. Drug-likeness. In-silico toxicity was predicted with LD
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AIM To optimize the subcritical aqueous extraction for polysaccharides from the leaves of Punica granatum L.and to evaluate the in vitro antioxidant activity.METHODS With reaction pressure,solid-liquid ratio,extraction time and extraction temperature as influencing factors,yield of polysaccharides as an evalution index,the extraction was optimized by Box-Behnken method on the basis of single factor test.Then the scavenging effects of polysaccharides on hydroxyl free radical,superoxide anion and DPPH free radical were detected.RESULTS The optimal conditions were determined to be 5 MPa for reaction pressure,1 ∶ 27 for solid-liquid ratio,11 min for extraction time,and 155 ℃ for extraction temperature,the yield of polysaccharides was 1.809％.There was a dose-effect relationship between scavenging rate and polysaccharides' concentration.0.1 mg/mL Polysaccharides displayed the strongest scavenging effects on hydroxyl free radical,superoxide anion and DPPH free radical with the clearance rates of 57.36％,70.51％ and 58.02％,respectively.CONCLUSION This stable and reliable method can be used for the subcritical aqueous extraction for polysaccharides from P.granatum leaves with obvious in vitro antioxidant activity.
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AIM To optimize the subcritical aqueous extraction for polysaccharides from the leaves of Punica granatum L.and to evaluate the in vitro antioxidant activity.METHODS With reaction pressure,solid-liquid ratio,extraction time and extraction temperature as influencing factors,yield of polysaccharides as an evalution index,the extraction was optimized by Box-Behnken method on the basis of single factor test.Then the scavenging effects of polysaccharides on hydroxyl free radical,superoxide anion and DPPH free radical were detected.RESULTS The optimal conditions were determined to be 5 MPa for reaction pressure,1 ∶ 27 for solid-liquid ratio,11 min for extraction time,and 155 ℃ for extraction temperature,the yield of polysaccharides was 1.809％.There was a dose-effect relationship between scavenging rate and polysaccharides' concentration.0.1 mg/mL Polysaccharides displayed the strongest scavenging effects on hydroxyl free radical,superoxide anion and DPPH free radical with the clearance rates of 57.36％,70.51％ and 58.02％,respectively.CONCLUSION This stable and reliable method can be used for the subcritical aqueous extraction for polysaccharides from P.granatum leaves with obvious in vitro antioxidant activity.
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In present study, leaf extract of Hoya parasitica Wall. was evaluated for in vitro antioxidant and membrane stabilizing activity along with in vivo gastro intestinal motility and acute toxicity. Five different assays were performed to evaluate antioxidant activity. In DPPH free radical scavenging activity, methanol, ethanol and chloroform extract exhibited IC50 value similar to standard ascorbic acid. The presence of flavonoid and phenolic contents was also similar in all the plant extracts. However, chloroform extract showed remarkable reducing power capacity (69.10% at 200μg/mL). In case of membrane stabilization, the chloroform extract showed maximum inhibition (32.62 %) of haemolysis, whereas the ethanol extract showed a significant (p<0.001) human RBC membrane stabilizing effect. In vivo gastrointestinal motility test indicates significant (p<0.001) increase in gastrointestinal motility by Methanol extract (100 and 200 mg/kg b.w.) and ethanol extract (200 mg/kg b.w.) compared to standard. Highest dose introduced as 1000, 2000 and 3000 mg/kg body weight of each extracts in acute toxicity study and did not shown any sign of toxicity in Swiss albino mice. The result obtained from this study, can be considered as preliminary and further sophisticated investigation is needed to isolate new bioactive compounds that might act as led compounds in future.
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Objective To prepare quercetin ( QUE) loaded chitosan nanoparticles ( CS-NPs), evaluate its physicochemical properties and antioxidation activity in vitro.Methods Quercetin chitosan nanoparticles were prepared by ionic crosslinking method and self-assembly method.The preparation method was optimized using entrapment efficiency (EE), drug loading (DL) and size as indexes.The best formulation and preparation conditions were optimized by orthogonal test based on single-factor test, evaluation indicator as particle size and EE.The physicochemical properties of the obtained QUE-CS-NPs were characterized by the following methods: the transmission electron microscope (TEM), dynamic light scattering (DLS) analysis for morphology, size distribution and Zeta potential.In vitro release behavior in 0.5% SDS solution was evaluated by dialysis tube method.In vitro antioxidant activity assays were performed by evaluating the abilities of the microspheres for hydroxide radicals and superoxide anions .Results TEM results revealed QUE-CS-NPs with round and uniform.Particle-size analysis showed that the diameters and Zeta potential of the QUE-CS-NPs were (282.9 ±20) nm and (30.5 ±2) mV, with uniform distribution (polydispersity below 0.185).DL and EE of QUE-CS-NPs were (8.81 ±0.65) %and (80.02 ±1.04) %, respectively.QUE-CS-NPs showed extended administration times with 66.2% cumulative release within 72 h.QUE-CS-NPs showed pronounced antioxidant activity and a concentration dependent, even more substantial than that of pure QUE.Conclusion QUE-CS-NPs show a good size, sustain release effect and pronounce antioxidant activity.
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Objective: To evaluate the total phenolic, flavonoid contents and in vitro antioxidant activity of methanol extract of Dioscorea esculenta (Lour). Burkill. Methods: Total phenolic content was estimated using the Folin Ciocalteu method. The flavonoid content was determined using aluminium chloride. In vitro antioxidant activities and reducing power capacity were determined using standard methods. Results: Total phenolic content in methanol extract of Dioscorea esculenta was found to be 0.79g/100g and flavonoids content was found to be 0.26 g/100g. The extract was screened for its potential antioxidant activities using tests such as DPPH radical scavenging activity, hydroxyl radical scavenging activity, superoxide radical scavenging activity, ABTS radical cation scavenging activity and reducing power activity. Conclusions: The present studies confirm the methanol extracts have potential in vitro antioxidant activity. The phytochemical phenols and flavonoids could be the reason for its antioxidant activity.
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Objective: To evaluate the total phenolic, flavonoid contents and in vitro antioxidant activity of methanol extract of Xanthosoma sagittifolium corm. Methods: Total phenolic content was estimated using the Folin Ciocalteu method. The flavonoid content was determined using aluminium chloride. In vitro antioxidant activities were evaluated by studying DPPH radical scavenging activity, hydroxyl radical scavenging activity, superoxide radical scavenging activity, ABTS radical cation scavenging activity and reducing power capacity were determined using standard procedure. Results:Xanthosoma sagittifolium corm exhibited 0.32g100g-1 total phenolic; 0.26g100g-1 flavonoid and better scavenging activity of DPPH (78.22±0.56%), hydroxyl radical (69.11±0.21%), superoxide radical (83.27±0.08%) and ABTS radical cations(76.11±0.07%).Conclusions: The present studies confirm the methanol extracts have potential in vitro antioxidant activity.
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A new class of α–aminophosphoantes 4a-j have been synthesized by condensation of imines 3a-j with dialkyl phosphite under catalyst free conditions in dry toluene at reflux conditions via pudovik reaction in high yields. All the title compounds were confirmed by physico-spectral analysis. All the title compounds were screened for antioxidant properties by radical scavenging methods such as 1,1-diphenyl-2-picryl hydrazyl (DPPH), hydroxyl radical scavenging method and lipid peroxidation. They exhibited potent in vitro antioxidant activity dose dependently. Their bioassay showed them to possess significant antibacterial activity.
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Objective To investigate the scavenging abilities of ginkgo albumin to reactive oxygen in vitro, as well as the protection and mechanism of ginkgo albumin on damaged DNA. Methods Lotus Seedpod Procyanidin (LSPC) and bovine serum albumin (BSA) were used as control sample, the effect of ginkgo albumin on removal of superoxide anion was determined by Pyrogallol-Luminol system. Scavenging ability of ginkgo albumin on hydroxide free radical was determined by CuSO4-Phen-Vc-H2O2, FeSO4-Luminol-H2O2, and FeSO4-Luminol systems. Luminol-H2O2 system was used to measure the scavenging effect on hydrogen peroxide. Preventive effect of ginkgo albumin on in vitro damaged DNA was determined by CuSO4-Phen-Vc-H2O2-DNA system. Results Ginkgo albumin possessed a good scavenging potency on reactive oxygen and protection on damaged DNA, but promoted oxidation in the FeSO4-Luminol-H2O2 and Luminol-H2O2 chemiluminescence systems. Conclusion Not every chemiluminescences system is suitable for investigating the antioxidant activity of ginkgo albumin.
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AIM: To evaluate the antioxidant properties in vitro of Longxuejie Capsule (Sanguis draconis) (LC). METHODS: The antioxidant activities of Longxuejie Capsules were investigated by employing several external assay systems, including 1,1-diphenyl-2-picrylhydrazyl (DPPH?)/peroxide anion/hydroxyl radical-scavenging, reducing power assay system, peroxidation of polyunsaturated fatty acid from yolk lipoprotein induced by Fe~ 2+ method, and ?-carotene/linoleic acid assay system. RESULTS: The LC showed scavenging activity against free radicals, such as DPPH?, peroxide anion and hydroxyl radicals. LC also exhibited effective reducing power and powerful inhibitory effects on peroxidation of polyunsaturated fatty acid from yolk lipoprotein induced by Fe~ 2+ . Furthermore, LC showed markedly inhibitory effect on ?-carotene/linoleic acid assay system. CONCLUSION: Longxuejie Capsule has obvious antioxidant activities in vitro