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Background: N-acetyl cysteine, a mucolytic agent, demonstrates free radical scavenging and anti-inflammatory properties, and prevents endothelial dysfunction by inhibition of NF-KB and formation of no adducts. This has a potential role to tackle cytokine storms, endothelial dysfunction and prothrombotic state observed in COVID-19 manifestations like ARDS and Multi organ dysfunction.Methods: Institution based descriptive cross sectional study, 164 patients from laboratory confirmed RT PCR positive COVID-19 patients, in the study period from 27th May 2020 to 10th August 2020, were assessed, in medical college Kolkata, a dedicated COVID-19 care facility.Results: It was observed that moderate-severe patients who received N-acetyl cysteine along with standard therapy had average hospital stay duration of 12 days, higher rate of discharge, average duration of oxygen therapy of 8 days, less number of deaths and reduced transfer to critical care facilities.Conclusions: N-acetyl cysteine can be considered as an adjunctive therapy with standard protocol driven care, due to its beneficial anti-inflammatory and free radical scavenging properties.
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The present study aimed at the evaluation of chemical composition and bioactive potential of methanolic extract obtained from Lepista sordida in terms of antioxidative and antimicrobial efficacy. The macrofungus is recognized for its high nutritional value and medicinal properties. However, to the best of our knowledge bioactivity of its methanolic extract is yet to be explored. In this investigation, quantitative analysis of mycochemicals revealed the extract contained significant amount of phenolic compounds such as phenols and flavonoids. Ascorbic acid was found in higher amount than β carotene and lycopene which were present in vestigial amounts. A phenolic profile was also determined using high performance liquid chromatography that further confirmed the presence of 10 phenolic constituents in the extract. Furthermore, the extract was subjected for determining antioxidant potential in different in-vitro assays. The findings showed remarkable 2, 2-Diphenyl-1-picrylhydrazyl and ABTS radical scavenging ability which was evident by low EC50 values, 330 µg/mL and 30 µg/mL respectively. The extract also demonstrated good chelating and reducing ability, an important marker of antioxidant compounds. Antimicrobial screening displayed positive results against Staphylococcus aureus and Escherichia coli. Altogether, the observations recommend therapeutic application of this mycotaxon on a commercial basis.
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Objective:To evaluate the antioxidant and antidiabetic activities of Sutherlandia montana E.Phillips & R.A.Dyer leaf extracts using the in vitro model.Methods:The antioxidant activities of aqueous,decoction,ethanol and hydro-ethanol extracts of the plant were determined using seven different assays;the antidiabetic potential was evaluated through the inhibition of key carbohydrate hydrolysing enzymes (α-amylase and α-glucosidase),while the modes of the enzymes inhibition were assessed using enzyme kinetic analysis.Results:The ethanol extract exhibited the best scavenging activity (IC5o:0.47,0.36,0.20,0.29 and 0.01 mg/mL) against the tested radicals like 1,1-diphenyl-2-picrylhydrazyl,2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid),nitric oxide,hydroxyl and superoxide anion,respectively.It also showed the best reducing power efficiency when compared with the standard (silymarin),while the decoction extract displayed the strongest metal chelating potential (IC50:0.71 mg/mL).The ethanol (IC50:5.52 mg/mL)and decoction (IC50:0.05 mg/mL) extracts exhibited mild and strong inhibitory effects on the specific activities of α-amylase and α-glucosidase respectively,through an uncompetitive and non-competitive mode of action.Conclusions:The observed properties might be linked to the presence of active principles as shown by the results of the phytochemical analyses of the extracts.This research has validated the folkloric application of Sutherlandia montana as a potential antidiabetic agent,which is evident from the inhibition of specific activities of key enzymes involved in carbohydrate metabolism.
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Objective To evaluate the antioxidant and antidiabetic activities of Sutherlandia montana E. Phillips & R.A. Dyer leaf extracts using the in vitro model. Methods The antioxidant activities of aqueous, decoction, ethanol and hydro-ethanol extracts of the plant were determined using seven different assays; the antidiabetic potential was evaluated through the inhibition of key carbohydrate hydrolysing enzymes (α-amylase and α-glucosidase), while the modes of the enzymes inhibition were assessed using enzyme kinetic analysis. Results The ethanol extract exhibited the best scavenging activity (IC
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@#Objective To compare the effects of non-steroidal anti-inflammatory drugs (NSAIDs) and free radical scavengers (FRS) on formation of traumatic heterotopic ossification (HO) in rabbits. Methods 48 New Zealand rabbits were randomly divided into control group (n=12), NSAIDs group (n=12), FRS group (n=12) and combination group (n=12). The model of traumatic HO was established, and the NSAIDs group, FRS group and combination group were administered indometacin intragastrically, edaravone intravenously and both, respectively, while the control group was administered normal saline for 4 weeks. The incidence and severity of HO were observed with X-ray 8 and 12 weeks after modeling. Results 8 and 12 weeks after operation, the incidence of HO was 33.3% and 41.7% in the NSAIDs group, 43.0% and 45.8% in the FRS group, 29.2% and 37.5% in the combination group, and 70.8% and 75.0% in the control group, respectively. The incidence and severity of HO in all the treatment groups were significantly less than those in the control group (P<0.05), and there was no significant difference among the treatment groups (P>0.05). Conclusion The systemic application of FRS may prevent the formation of HO effectively, similar with the NSAIDs. There is no synergistic effect between them.
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Objective To compare the effects of non-steroidal anti-inflammatory drugs (NSAIDs) and free radical scavengers (FRS) on formation of traumatic heterotopic ossification (HO) in rabbits. Methods 48 New Zealand rabbits were randomly divided into control group (n=12), NSAIDs group (n=12), FRS group (n=12) and combination group (n=12). The model of traumatic HO was established, and the NSAIDs group, FRS group and combination group were administered indometacin intragastrically, edaravone intravenously and both, re-spectively, while the control group was administered normal saline for 4 weeks. The incidence and severity of HO were observed with X-ray 8 and 12 weeks after modeling. Results 8 and 12 weeks after operation, the incidence of HO was 33.3%and 41.7%in the NSAIDs group, 43.0%and 45.8%in the FRS group, 29.2%and 37.5%in the combination group, and 70.8%and 75.0%in the control group, respectively. The incidence and severity of HO in all the treatment groups were significantly less than those in the control group (P0.05). Conclusion The systemic application of FRS may prevent the formation of HO effectively, similar with the NSAIDs. There is no synergistic effect between them.
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Gypsophila pilulifera, Boiss & Heldr, Caryophyllaceae, is a perennial medicinal herb that grows in the southwestern region of Turkey. Except for only one report on the isolation of cytotoxic saponins from the underground parts of G. pilulifera, there are no published thorough phytochemical or bioactivity studies on this species. In the present study, the free-radical scavenging activity of extracts and fractions of the stems of G. pilulifera was evaluated, using a slightly modified and more precise version of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, reported here for the first time. The DPPH assay-guided HPLC-PDA-purification of the active solid-phase extraction fraction (50% methanol in water) of the methanolic extract exhibited verbascoside as the main free-radical scavenger present in this species. The structure of this active compound was resolved by spectroscopy, and the free-radical scavenging potential of verbascoside was determined.
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OBJECTIVE@#To evaluate phytopharmacologically eugenol and two extract products of Ocimum gratissimum Linn. (O. gratissimum) (Labiaceae) on free radical scavenging and antioxidant activity.@*METHODS@#Aqueous and methanol extract of fresh aerial part of O. gratissimum were prepared and eugenol (1-allyl-4-hydroxy-3-methoxybenzene) was isolated from fresh leaves and characterized by high performance liquid chromatography, fourier transform infrared spectroscopy, 1 h nuclear magnetic resonance. To establish the antioxidant potentiality of aqueous extract, methanol extract and eugenol, 1, 1-diphenyl-2-picrylhydrazyl radical, hydroxyl radical, nitric oxide scavenging activity, antioxidant activity by ferric thiocyanate and reducing power were measured in chemical system in vitro.@*RESULTS@#Significant (P<0.05) concentration-dependent free radical scavenging activity, antioxidant activity, and reducing power was observed by O. gratissimum products. Moreover, eugenol is more potent than the two extract products of O. gratissimum, but lower than potent antioxidant ascorbic acid.@*CONCLUSIONS@#Hence, O. gratissimum presents a potentially valuable source of natural antioxidant and bioactive material.
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Objective: To evaluate phytopharmacologically eugenol and two extract products of Ocimum gratissimum Linn. (O. gratissimum) (Labiaceae) on free radical scavenging and antioxidant activity. Methods: Aqueous and methanol extract of fresh aerial part of O. gratissimum were prepared and eugenol (1-allyl-4-hydroxy-3-methoxybenzene) was isolated from fresh leaves and characterized by high performance liquid chromatography, fourier transform infrared spectroscopy, 1 h nuclear magnetic resonance. To establish the antioxidant potentiality of aqueous extract, methanol extract and eugenol, 1, 1-diphenyl-2-picrylhydrazyl radical, hydroxyl radical, nitric oxide scavenging activity, antioxidant activity by ferric thiocyanate and reducing power were measured in chemical system in vitro. Results: Significant (P<0.05) concentration-dependent free radical scavenging activity, antioxidant activity, and reducing power was observed by O. gratissimum products. Moreover, eugenol is more potent than the two extract products of O. gratissimum, but lower than potent antioxidant ascorbic acid. Conclusions: Hence, O. gratissimum presents a potentially valuable source of natural antioxidant and bioactive material.
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The methanol extract of the aerial parts of the medicinal plant Pedicularis sibthorpii Boiss., Scrophulariaceae, growing in the Azerbaijan province of Iran, was found to be active in the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and the antibacterial agar well diffusion assays, but no general toxicity was observed in the brine shrimp lethality assay. A combination of solid-phase extraction (SPE) and preparative reversed-phase high-performance liquid chromatography (prep-RP-HPLC) analyses of the methanolic extract afforded three phenylethanoids (verbascoside, martynoside and isomartynoside), an iridoid (aucubin), a flavonoid (luteolin 7-O-β-D-glucopyranoside) and mannitol, and the structures of these compounds were elucidated unambiguously by spectroscopic means. The distribution of the isolated compounds within the genus Pedicularis has also been discussed.
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From the methanolic extract of the aerial parts of Ajuga chamaepitys (L.) Schreb., Lamiaceae, one of the Iranian medicinal plants, the phenylethanoid glycoside, acteoside, and two flavone glycosides, chrysoeriol 7-O-glucopyranoside (3'-methoxy-luteolin 7-O-glucopyranoside) and apigenin 7-O-rhamnopyranoside, were isolated by a combination of solid-phase extraction (SPE) and preparative reversed-phase high-performance liquid chromatography (prep-RP-HPLC) methods. Structures of the isolated compounds were elucidated by spectroscopic means. The free-radical-scavenging properties of the extracts, fractions and isolated compounds were determined by the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay. While among the extracts, the MeOH extract showed the highest level of free-radical-scavenging activity (RC50 1.15 × 10-1 mg/mL), chrysoeriol 7-O-glucopyranoside was the most active (RC50 3.00 × 10-3 mg/mL) among the isolated compounds. The GC-MS and the GC-FID analyses revealed α-pinene (23.66%), β-pinene (9.33%), 1-octen-3-ol (9.72%), β-phellandrene (8.70%) and germacrene-D (7.92%) as the major components of the essential oils derived from the aerial parts of this plant. The presence of phenolic glycosides and the α- and β-pinene-rich essential oils in A. chamaepitys may provide some rationale for the traditional medicinal uses of this species in Iran.
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A variety of 1,2-dihydropyrimido-[1,2-a]-benzimidazole-3-carbonitrile derivatives were synthesized under microwave irradiation using water and acetonitril as solvent system. All the compounds were tested in vitro for α-glucosidase inhibitory and DPPH free radical scavenging activity. 4-Amino-2-(4-flourophenyl)-1,2-dihydropyrimido [1,2-a]-benzimidazole-3-carbonitrile (4c) was found to be a potent intestinal α- glucosidase inhibi tory activity (IC50; 91μM) along with moderate DPPH scavenging property. This compound was further evaluated for cytotoxicity activity against HT-29 colon cancer cell line. The IC50 value for its cytotoxicity activity was found to be 662 μM.
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Herbal plants with antioxidant activities are widely used in Ayurvedic medicine for cardiac and other problems. Arjunolic acid is one such novel phytomedicine with multifunctional therapeutic applications. It is a triterpenoid saponin, isolated earlier from Terminalia arjuna and later from Combretum nelsonii, Leandra chaeton etc. Arjunolic acid is a potent antioxidant and free radical scavenger. The scientific basis for the use of arjunolic acid as cardiotonic in Ayurvedic medicine is proven by its vibrant functions such as prevention of myocardial necrosis, platelet aggregation and coagulation and lowering of blood pressure, heart rate and cholesterol levels. Its antioxidant property combined with metal chelating property protects organs from metal and drug induced toxicity. It also plays an effective role in exerting protection against both type I and type II diabetes and also ameliorates diabetic renal dysfunctions. Its therapeutic multifunctionality is shown by its wound healing, antimutagenic and antimicrobial activity. The mechanism of cytoprotection conferred by arjunolic acid can be explained by its property to reduce the oxidative stress by enhancing the antioxidant levels. Apart from its pathophysiological functions, it possesses dynamic insecticidal property and it is used as a structural molecular framework in supramolecular chemistry and nanoscience. Esters of arjunolic acid function as gelators of a wide variety of organic liquids. Experimental studies demonstrate the versatile effects of arjunolic acid, but still, further investigations are necessary to identify the functional groups responsible for its multivarious effects and to study the molecular mechanisms as well as the probable side effects/toxicity owing to its long-term use. Though the beneficial role of this triterpenoid has been assessed from various angles, a comprehensive review of its effects on biochemistry and organ pathophysiology is lacking and this forms the rationale of this review.
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Objective: To investigate the effect of edaravone on the pain sensitivity in rats with spinal nerve ligated and to probe into the related mechanism. Methods: Male adult SD rats were randomly divided into 3 groups: a sham (Sham) group, a spinal nerve ligation (SNL) group and edaravone(Eda) group. The paw withdrawal mechanical threshold(PWMT) was measured before and after ligation (once daily for 7 days). Rats were sacrificed at specified time points and the left(operation side) L4 and L5 dorsal root ganglia(DRG) and the right (control side) L5 DRG were obtained and immunostained to observe the changes of pJNK in DRG neurons and spinal cords, so as to observe the effect of edaravone on pJNK. Results: Edaravone can reduce the mechanical hyperalgesia induced by spinal nerve ligation. Immunostaining showed that the SNL group had an increased pJNK in the ipsilateral DRG neurons (L5) 24 hours after ligation; double immunofluorescence indicated that the expression of pJNK in the ipsilateral spinal astrocytes was increased 3 days after ligation. Edaravone can reduce pJNK expression in DRG neurons and spinal cords at corresponding time points. Conclusion: Edaravone can relieve the neuropathic pain induced by spinal nerve ligation, and the mechanism might be related to the inhibition of pJNK expression in DRG neurons and spinal cords.
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Free radical plays a key role in the process of cerebral ischemic injury. It aggravates cell membrane damage through the peroxidation of unsaturated fatty acids, and then results in neuronal death and brain edema. Edaravone, a novel potent free radical scavenger, exerts its neuroprotective effect by inhibiting endothelial injury in cerebral ischemic areas and relieving neuronal damage. It also reduces thrombolytic therapy-induced brain edema and bleeding events after reperfusion. Clinical experiences suggest that the therapeutic time window of edaravone is very wide, and when it combines with thrombolytic therapy, it may reduce stroke mortality and promote the recovery of neurological deficit. This article reviews the course of development of edaravone from laboratory to clinical stage.
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<p><b>OBJECTIVE</b>Human diploid cells are more susceptible to oxidative stress at late passage than at early passage, presumably because of the decrease in cellular-reduced glutathione (GSH) concentration. Water-soluble protein (WSP) from broad beans scavenges free radicals. The effects of WSP on the glutathione system were examined in PDL 20 (early passage) and PDL 50 (late passage) human lung fibroblasts (TIG-1).</p><p><b>METHODS</b>To determine cytosolic glutathione peroxidase (GSH-Px) activities, glutathione reductase (GR) activities, oxidized glutathione (GSSG) concentrations, and GSSG/reduced glutathione (GSH) ratios, WSP and hydrocortisone (HC) treatments of TIG-1 cells (PDL 20→50 and PDL 50→75) were performed for 40 days. We also investigated the GSSG concentrations and GR activities in PDL 20 cells that were continuously treated with WSP until PDL 39 and 55.</p><p><b>RESULTS</b>GSSG concentrations decreased in WSP- and HC-treated PDL 50→75 cells. The GSSG/GSH ratios in PDL 50→75 cells became low after the treatments. Increases in GR activities were observed in treated PDL 50→75 cells. The decline in the GSSG concentration of PDL 50→75 cells correlated with the increase in GR activity. The GSSG levels in control cells were higher following cellular age, whereas the levels in treated cells were lower than those in the control. The studies on cellular age-related changes indicated that greater increases in GR activity were found in treated cells than in the control.</p><p><b>CONCLUSION</b>These results indicated that WSP influences the GSSG concentration that is associated with cellular aging, but the mechanism of GSSG reduction by WSP remains unknown. The enhancement of glutathione status following WSP treatment may be related to the delay in the cellular aging.</p>
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Objective: Human diploid cells are more susceptible to oxidative stress at late passage than at early passage, presumably because of the decrease in cellular-reduced glutathione (GSH) concentration. Water-soluble protein (WSP) from broad beans scavenges free radicals. The effects of WSP on the glutathione system were examined in PDL 20 (early passage) and PDL 50 (late passage) human lung fibroblasts (TIG-1). Methods: To determine cytosolic glutathione peroxidase (GSH-Px) activities, glutathione reductase (GR) activities, oxidized glutathione (GSSG) concentrations, and GSSG/reduced glutathione (GSH) ratios, WSP and hydrocortisone (HC) treatments of TIG-1 cells (PDL 20→50 and PDL 50→75) were performed for 40 days. We also investigated the GSSG concentrations and GR activities in PDL 20 cells that were continuously treated with WSP until PDL 39 and 55. Results: GSSG concentrations decreased in WSP- and HC-treated PDL 50→75 cells. The GSSG/GSH ratios in PDL 50→75 cells became low after the treatments. Increases in GR activities were observed in treated PDL 50→75 cells. The decline in the GSSG concentration of PDL 50→75 cells correlated with the increase in GR activity. The GSSG levels in control cells were higher following cellular age, whereas the levels in treated cells were lower than those in the control. The studies on cellular age-related changes indicated that greater increases in GR activity were found in treated cells than in the control. Conclusion: These results indicated that WSP influences the GSSG concentration that is associated with cellular aging, but the mechanism of GSSG reduction by WSP remains unknown. The enhancement of glutathione status following WSP treatment may be related to the delay in the cellular aging.
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Humans , Glutathione Disulfide , Cell Biology , GlutathioneABSTRACT
PURPOSE: The green tea polyphenol (GTPP) has been known to exert antioxidant activity as a radical scavenger as well as cancer preventive and cancer growth inhibition effect. The aim of this study was to identify whether GTPP not only potentiate the growth inhibition effect in gamma-irradiated human cancer cell but also exert protection action for irradiated human normal cell. MATERIALS AND METHODS: GTPP (80% catechin including > 45% EGCG) added in the HL60, human leukemia, and NC37, human lymphoblast, before irradiation. After establishing the amount of GTPP and the dose of radiation, the cells were treated with the GTPP for 6 hours and irradiated with the determined doses. RESULTS: Viability when 10 mug/ml GTPP added before gamma-irradiation with 1 Gy to NC37 cells was not different in comparison with control but it when was irradiated with 3 Gy significantly different (1 Gy; P=0.126, 3 Gy; P=0.010). 20 mug/ml GTPP did not show significant difference in both NC37 cells irradiated with 1 Gy and 3 Gy (1 Gy; P=0.946, 3 Gy; P=0.096). Viabilities were significantly decreased with concentration of additional GTPP in HL60 with 1 or 3 Gy (1 Gy; 69.0+/-1.7% vs 42.4+/-1.3%, 3 Gy; 66.9+/-3.9% vs 44.2+/-1.6 %). CONCLUSION: In vitro study, we certified that when the cells were irradiated with dose below 3 Gy, GTPP provide not only anticancerous effect against cancer cells but also radioprotective effect in normal cells simultaneously. Theses results suggest the possibility that consumption of green tea could give the radioprotective effect and maximize the effect on internal radiation such as radioiodine therapy concomitantly.
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Humans , Catechin , Leukemia , TeaABSTRACT
PURPOSE: To investigate the effect of intravitreal melatonin on retina in rabbit. METHODS: In four pigmented rabbit, melatonin was intravitreally injected 100 mu g/0.1 ml, 300 mu g/0.1 ml concentration in left eye, DMSO was injected in right eye as control. we examined gross fundus finding and electroretinogram and then light and electronic microscopic findings at 24 hours and 1 week with both eye. RESULTS: intravitreally melatonin injected eye at 100 mu g/0.1 ml, 300 mu g/0.1 ml concentration and control eye at 1 day and 1 week, significant difference was not shown in gross fundus finding, electroretinogram, light and electronic microscopic finding. Additionally edema, toxic effect change was not found in retina. CONCLUSIONS: Intravitreally injected melatonin has not influenced on retina grossly, histologically, physiologically at 100 mu g/0.1 ml and 300 mu g/0.1 ml concentration. Further study is required about toxic effect of melatonin over 300 mu g/0.1 ml concentration and clinical usefulness of melatonin in retina.
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Dimethyl Sulfoxide , Edema , Intravitreal Injections , Melatonin , RetinaABSTRACT
Objective To observe the curative effects of treatment with Edaravone for acute massive cerebral infarction.Methods 48 patients with acute massive cerebral infarction were randomized into the treatment with Edaravone group(Edaravone group,24 patients) and the conventional treatment control group(control group,24 patients).Two groups patients were admitted conventional treatment for cerebral infarction.Edaravone group patients were admitted with Edaravone 30 mg into 100 ml saline infusion introvenously,twice a day,linked 20 ～ 25 d.Respectively before and after the treatment,neurologic function dificit score(NDS),plasma fibrinogen(Fib) content,coagulation blood function,activity of superoxide dismutase(SOD) were examined.The clinical efficacy was compared between the two groups.Results NDS of tow groups after treatment were significantly lower than those of before treatment,activity of SOD were significantly increased than those before treatment(all P0.05).Significant efficiency ratio of the Edaravone group(87.5%) was significantly higher than that of the control group(45.8%)(P