scholarly journals ANTIOXIDANT PROPERTIES AND EFFECTS OF APORPHINE ALKALOIDS AND THEIR PHENANTHRENE SECO-ISOMERS ON ACETYLCHOLINESTERASE ACTIVITY

2021 ◽  
pp. 237-246
Author(s):  
Salima Salimovna Khizrieva ◽  
Sergey Nikolaevich Borisenko ◽  
Elena Vladimirovna Maksimenko ◽  
Elena Vladimirovna Vetrova ◽  
Nikolay Ivanovich Borisenko ◽  
...  

For the first time, model’s phenanthrene seco-alkaloids (seco-glaucine and seco-boldine) obtained in the medium of subcritical water SBW) from plant aporphine alkaloids were studied as antioxidants and inhibitors of acetylcholinesterase (AChE). Antioxidant activity (in vitro) of model’s aporphine and phenanthrene alkaloids: boldine, seco-boldine, glaucine and seco-glaucine, (BD, s-BD, GL and s-GL) was studied in the reaction with a stable free radical DPPH (1,1- diphenyl-2-picrylhydrazyl). In vivo, antioxidant activity was determined in a bioluminescent test system using genetically modified E. coli strains. In experiments in vitro (DPPH-test) and in vivo (biotest) phenanthrene alkaloids s-GL and s-BD demonstrate the higher antioxidant activity than their aporphine precursors GL and BD. For the study (in vitro) of the anticholinesterase activity of alkaloids and their phenanthrene seco-isomers used the “Ellman’s method” with minor modifications. The data on the inhibitory activity of the AChE enzyme with aporphine and phenanthrene alkaloids, expressed as IC50 values obtained from dose-response curves, demonstrate that the inhibitory activity for seco-boldine (IC50 = 0.21 mM) and seco-glaucine (IC50 = 0.04 mM ) is higher than for the initial aporphine alkaloids boldine (IC50 = 0.29 mM) and glaucine (IC50 = 0.44 mM), respectively. Thus, it has been shown that phenanthrene alkaloids obtained in SBW exhibit higher antioxidant activity and better inhibiting AChE-activity than their aporphine precursors.

Author(s):  
Sri Ningsih ◽  
Fahri Fahrudin

 Objective: Hyperuricemia (high uric acid levels) prevalence increased year by year. This study was aimed to elaborate the in vitro xanthine oxidase (XO) inhibitory activity and in vivo lowering hyperuricemic effect of Uncaria gambir (Hunter) Roxb) (gambir), Caesalpinia sappan L. (secang) and the combined extract of secang and gambir (formulae extract [FE]).Methods: Gambir and secang extracts were prepared by maceration with ethanol and FE was the proportioned combination of these two extracts. XO inhibitory activity was determined by measuring the formation of uric acid in the xanthine/XO system in vitro using allopurinol as a positive control at 100 ug/mL. Antioxidant activity was by 1,1-diphenyl-2-picrylhydrazyl radical reducing methods. The in vivo experiments were conducted in the oxonate-induced hyperuricemia rat model, in which FE was gavaged p.o. at the arrange dose of 75, 150, and 300 mg/kg bw for 2 weeks. Polyphenol content was measured using Folin–Ciocalteu reagent spectrophotometrically.Results: The XO inhibitory activity of FE was 80% of allopurinol, while secang and gambir were 98% and 50%, respectively. The strength was appropriate to the total polyphenol content, in which it decreased in the order of secang (99%) > FE (86%) > gambir (46%). Furthermore, FE at all tested doses was able to decrease uric acid levels. FE also demonstrated antioxidant activity with a value of 74% relative to Vitamin C at 4 ug/mL.Conclusion: These studies could be concluded that FE exhibited the ability to decrease uric acid level so that it was potential to be developed further as a uric acid-lowering agent.


Scientifica ◽  
2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Tekeshwar Kumar ◽  
Vishal Jain

The aim of this study was to determine the impending antioxidant properties of different extracts of crude methanolic extract (CME) of leaves ofLannea coromandelica(L. coromandelica) and its two ethyl acetate (EAF) and aqueous (AqF) subfractions by employing various establishedin vitrosystems and estimation of total phenolic and flavonoid content. The results showed that extract and fractions possessed strong antioxidant activityin vitroand among them, EAF had the strongest antioxidant activity. EAF was confirmed for its highest phenolic content, total flavonoid contents, and total antioxidant capacity. The EAF was found to show remarkable scavenging activity on 2,2-diphenylpicrylhydrazyl (DPPH) (EC5063.9 ± 0.64 µg/mL), superoxide radical (EC508.2 ± 0.12 mg/mL), and Fe2+chelating activity (EC506.2 ± 0.09 mg/mL). Based on ourin vitroresults, EAF was investigated forin vivoantioxidant assay. Intragastric administration of the EAF can significantly increase levels of superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), and glutathione peroxidase (GSH-Px) levels, and decrease malondialdehyde (MDA) content in the liver and kidney of CCl4-intoxicated rats. These new evidences show thatL. coromandelicabared antioxidant activity.


1988 ◽  
Vol 64 (5) ◽  
pp. 2092-2099 ◽  
Author(s):  
E. R. Pacht ◽  
W. B. Davis

Lung epithelial lining fluid (ELF) is a thin layer of plasma ultrafiltrate and locally secreted substances that may provide antioxidant protection and serve as a "front-line" defense for the lower respiratory tract epithelium. To characterize the antioxidant properties of ELF, young, healthy, nonsmoking volunteers underwent bronchoalveolar lavage with determination of ELF volumes and ELF proteins. ELF (greater than 0.4 ml) is a potent inhibitor of lipid peroxidation as measured by malondialdehyde (MDA) production in an in vitro iron-dependent assay system. Two serum proteins, transferrin and ceruloplasmin, were quantitated in ELF and found to be potent inhibitors of lipid peroxidation. Other ELF components, including vitamin E, vitamin C, and albumin, did not function as antioxidants in this system. Several experimental observations suggest that ELF transferrin was more important than ceruloplasmin in inhibiting lipid peroxidation: 1) ELF concentrations of transferrin were 20-fold higher than those for ceruloplasmin; 2) ELF antioxidant activity was abolished by preincubation with Fe3+; 3) ELF antioxidant activity was minimally affected by sodium azide, which is known to inhibit ceruloplasmin ferroxidase activity; and 4) ELF ceruloplasmin ferroxidase activity was virtually nondetectable. ELF possesses a significant antioxidant activity that may be important in vivo in protecting the lung from oxidant injury.


Author(s):  
Soumia Bouzidi ◽  
Benkiki Naima ◽  
Allaoua Zina

ABSTRACTObjective: The aim of this study is to evaluate the in vitro antioxidant activity of Paronychia capitata various extracts, acute toxicity, the in vivoantipyretic and anti-inflammatory activities of the n-butanol extract.Methods: The antioxidant properties were tested using 2,2-diphenyl 1-picrylhydrazyl radical scavenging and β-carotene linoleic acid system, thetotal phenolic and flavonoid contents were determined. Furthermore, anti-inflammatory activity and antipyretic activity of the n-butanol extractwere assessed on male Wistar rats at the dose levels 250, 500 mg/kg body weight, using the egg albumin-induced edema, and brewer’s yeast-inducedpyrexia method, respectively.Results: The n-butanol extract of P. capitata had considerably the highest antiradical activity with inhibitory concentration 50 value of 8.667 μg/ml.Conclusion: The experimental data demonstrated that n-butanol extract of P. capitata possess significantly remarkable anti-inflammatory andantipyretic activities compared to the standard drugs.Keywords: Caryophyllaceae, Flavonoid, Inflammation, Fever, Paronychia capitata.


2021 ◽  
Author(s):  
Adrieli Sachett ◽  
Matheus Gallas-Lopes ◽  
Radharani Benvenutti ◽  
Matheus Marcon ◽  
Gean Pablo S. Aguiar ◽  
...  

Curcumin, a polyphenol extracted from the rhizome of Curcuma longa L. (Zingiberaceae), is shown to have antioxidant, anti-inflammatory, neuroprotective, anxiolytic, and antidepressant properties in both preclinical and clinical studies. However, its low bioavailability is a limitation for its potential adoption as a therapeutic agent. The process of micronization can overcome this barrier by reducing the particle size and increasing the dissolution rate, potentially improving the bioavailability of the compounds of interest. In this study, we compared the in vitro antioxidant effects of curcumin (CUR) and micronized curcumin (MC) and studied their effects on behavioral and neurochemical parameters in zebrafish submitted to unpredictable chronic stress (UCS). MC (1 g/L) presented higher antioxidant activity in vitro as compared to CUR, as measured by iron-reducing antioxidant power (FRAP), 1,1-diphenyl-2-2-picyryl-hydrazyl radical removal (DPPH), and deoxyribose tests. UCS increased total distance traveled in the social interaction test (SI), while decreased crossings, time, and entries to the top area in the novel tank test (NTT). No effects of UCS were observed in the open tank test (OTT). The behavioral effects induced by UCS were not blocked by any curcumin preparation. UCS also decreased non-protein thiols (NPSH) levels, while increased glutathione reductase (GR) activity and thiobarbituric acid reactive substances (TBARS) levels on zebrafish brain. MC presented superior antioxidant properties than CUR in vivo, blocking the stress-induced neurochemical effects. Although this study did not measure the concentration of curcumin on the zebrafish brain, our results suggest that micronization increases the bioavailability of curcumin, potentiating its antioxidant activity both in vitro and in vivo. Our study also demonstrates that counteracting the oxidative imbalance induced by UCS is not sufficient to block its behavioral effects.


2013 ◽  
Vol 2013 ◽  
pp. 1-15 ◽  
Author(s):  
Denise McCormack ◽  
David McFadden

Pterostilbene (trans-3,5-dimethoxy-4-hydroxystilbene) is a natural dietary compound and the primary antioxidant component of blueberries. It has increased bioavailability in comparison to other stilbene compounds, which may enhance its dietary benefit and possibly contribute to a valuable clinical effect. Multiple studies have demonstrated the antioxidant activity of pterostilbene in bothin vitroandin vivomodels illustrating both preventative and therapeutic benefits. The antioxidant activity of pterostilbene has been implicated in anticarcinogenesis, modulation of neurological disease, anti-inflammation, attenuation of vascular disease, and amelioration of diabetes. In this review, we explore the antioxidant properties of pterostilbene and its relationship to common disease pathways and give a summary of the clinical potential of pterostilbene in the prevention and treatment of various medical conditions.


Author(s):  
Monika Gaba ◽  
Sarbjot Singh ◽  
Chander Mohan ◽  
Richa Dhingra ◽  
Monika Chauhan ◽  
...  

Background: Non-steroidal anti-inflammatory drugs (NSAIDs) derived local generation of reactive oxygen species (ROS) plays a crucial role in the formation of gastric ulceration. Objective: Therefore, anti-inflammatory analgesics with potent antioxidant activity could be a potential therapeutic strategy for the treatment of pain and inflammatory disorders without gastrointestinal (GI) side effects. Methods: In an effort to develop gastroprotective analgesic and anti-inflammatory agents, a series of 2-methylamino-substituted-1H-benzo[d] imidazol-1-yl) (phenyl) methanone derivatives were synthesized and evaluated in vitro for cyclooxygenase (COX) inhibition as well as anti-oxidant potential by the FRAP assay. The compounds with significant in vitro COX-1/COX-2 inhibitory activity and antioxidant activity were further screened in vivo for their anti-inflammatory and analgesic activities. Moreover, the ulcerogenic potential of test compounds was also studied. To gain insight into the plausible mode of interaction of compounds within the active sites of COX-1 and COX-2, molecular docking simulations were performed. Results: Among the various synthesized molecules, most of the compounds showed good cyclooxygenase inhibitory activity and efficient antioxidant activity in FRAP assay. After preliminary and indicative in vitro assays, three compounds exhibited most significant antiinflammatory and analgesic activity with better gastric tolerability during their in vivo evaluation. Ligand interaction studies indicated highest dock score -43.05 of 1,2- disubstituted benzimidazole derivatives in comparison to the reference ligand -30.70. Overall studies provided us (2-((4-methoxyphenylamino) methyl) -1h-benzo [d] imidazol- 1-yl) (phenyl) methanone as a lead with potent gastro-protective anti-inflammatory and analgesic activities that can be used for future research. Conclusion: From the above results, it can be concluded that designing of multifunctional molecules with COX-1/COX-2 inhibitory and anti-oxidant activities could hold a great promise for further development of GI-safer NSAIDs.


2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
L. C. Cruz ◽  
J. E. S. Batista ◽  
A. P. P. Zemolin ◽  
M. E. M. Nunes ◽  
D. B. Lippert ◽  
...  

We characterized, for the first time, the quality and identity of Brazilian Pampa biome honey and its antioxidant propertiesin vitro(FRAP, DDPH and ABTS). The potential protective effect of honey against oxidative stress induced by iron (Fe) and paraquat, (PQ) in aDrosophila melanogastermodel (in vivo) was also tested. The results indicated that all honey samples tested showed antioxidant activityin vitro. Flies treated with honey showed increased lifespan and were protected against oxidative stress induced by Fe and PQ. Despite the high concentration of sugars in honey (approximately 70–80%), our results demonstrate a hypoglycemic-like effect of honey inDrosophila. Thus, this study demonstrates the high quality of Brazilian Pampa biome honey as well as its significant antioxidant activityin vitroandin vivo, pointing to the potential use of this natural product as an alternative in the therapy of oxidative stress-associated diseases.


2018 ◽  
Vol 2018 ◽  
pp. 1-14 ◽  
Author(s):  
Ameur Ben Younes ◽  
Maryem Ben Salem ◽  
Hanen El Abed ◽  
Raoudha Jarraya

Background. This study investigates the biological activities ofAnthyllis henonianaflowers extracts.Materials and Methods. Antioxidant activity and thein vitroinhibitory effect of key digesting enzymes related to postprandial hyperglycemia were determined. Diabetic rats were orally and daily given the best extract from flowers ofAnthyllis henonianaat a dose of acarbose for one month.Results. Among the extracts, the ethyl acetate one displayed remarkable antioxidant activity including DPPH (IC50= 2.34 mg/mL) and was more effective in inhibitingα-glucosidase (IC50= 17μg/mL) thanα-amylase (IC50= 920μg /mL) activities.In vivo, the results proved that ethyl acetate extract at doses of 400 mg/kg bw decreased significantly the blood glucose level and lipid profile levels and increased the activities of antioxidant enzymes. These protective impacts ofAnthyllis henonianaethyl acetate flowers extract were confirmed by histological results.Conclusion. This study demonstrates, for the first time, thatAnthyllis henonianaflowers ethyl acetate extract is effective in inhibiting hyperglycemia and oxidative stress caused by diabetes.


1972 ◽  
Vol 28 (03) ◽  
pp. 351-358
Author(s):  
A.J Baillie ◽  
A. K Sim

SummaryThe activity of several synthetic compounds, rated from good to poor (or inactive) fibrinolytic activators, has been assessed by two different commonly-used in vitro methods. Compounds shown to be active over a narrow concentration range in the hanging clot test were shown to be inhibitors of plasmin and trypsin in the casein-olytic test. The inhibitory activity of these compounds was shown to increase with increasing substrate concentration and apparent activity in the hanging clot test. Possible explanations and relevance of these observations are discussed.


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