Synthesis and Biological Evaluation of Scutellarein Alkyl Derivatives as Preventing Neurodegenerative Agents with Improved Lipid Soluble Properties

2019 ◽  
Vol 15 (7) ◽  
pp. 771-780
Author(s):  
He-Min Li ◽  
Ting Gu ◽  
Wen-Yu Wu ◽  
Shao-Peng Yu ◽  
Tian-Yuan Fan ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Neuronal Damage ◽  
Thiobarbituric Acid ◽  
Rat Hepatocytes ◽  
Biological Evaluation ◽  
Thiobarbituric Acid Reactive Substance ◽  
Alkyl Derivatives ◽  
Promising Therapeutic Approach ◽  
Microsomal Membranes

Background: Exogenous antioxidants are considered as a promising therapeutic approach to treat neurodegenerative diseases since they could prevent and/or minimize the neuronal damage by oxidation. Objective: Three series of lipophilic compounds structurally based on scutellarein (2), which is one metabolite of scutellarin (1) in vivo, have been designed and synthesized. Methods: Their antioxidant activity was evaluated by detecting the 2-thiobarbituric acid reactive substance (TBARS) produced in the ferrous salt/ascorbate-induced autoxidation of lipids, which were present in microsomal membranes of rat hepatocytes. The lipophilicity of these compounds indicated as partition coefficient between n-octanol and buffer was investigated by ultraviolet (UV) spectrophotometer. Results: This study indicated that compound 5e which had a benzyl group substituted at the C4'- OH position showed a potent antioxidant activity and good lipophilicity. Conclusion: 5e could be an effective candidate for preventing or reducing the oxidative status associated with the neurodegenerative processes.

scholarly journals Evaluation of theIn VitroandIn VivoAntioxidant Potentials ofSudarshanaPowder

2018 ◽  
Vol 2018 ◽  
pp. 1-5 ◽  
Author(s):  
Weerakoon Achchige Selvi Saroja Weerakoon ◽  
Pathirage Kamal Perera ◽  
Dulani Gunasekera ◽  
Thusharie Sugandhika Suresh
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Capacity ◽  
Thiobarbituric Acid ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Control Group ◽  
Thiobarbituric Acid Reactive Substance ◽  
Trolox Equivalent ◽  
Antioxidant Effects

Sudarshanapowder (SP) is one of the most effective Ayurveda powder preparations for paediatric febrile conditions. The objective of the present study was to evaluate thein vitroandin vivoantioxidant potentials of SP. Thein vitroantioxidant effects were evaluated using ABTS radical cation decolourization assay where the TROLOX equivalent antioxidant capacity (TEAC) was determined. Thein vivoantioxidant activity of SP was determined in Wistar rats using the Lipid Peroxidation (LPO) assay in serum. Thein vitroassay was referred to as the TROLOX equivalent antioxidant capacity (TEAC) assay. For thein vivoassay, animals were dosed for 21 consecutive days and blood was drawn to evaluate the MDA level. Thein vitroantioxidant activity of 0.5 μg of SP was equivalent to 14.45 μg of standard TROLOX. The percentage inhibition against the radical formation was50.93±0.53%. The SP showed a statistically significant (p<0.01) decrease in the serum level of thiobarbituric acid-reactive substance in the test rats when compared with the control group. These findings suggest that the SP possesses potent antioxidant activity which may be responsible for some of its reported bioactivities.

scholarly journals IN VIVO ANTIOXIDANT ACTIVITY OF LIMNOPHILA HETEROPHYLLA AND MICHELIA CHAMPACA

2017 ◽  
Vol 9 (12) ◽  
pp. 241 ◽  
Author(s):  
Raja S, ◽  
Ravindranadh K.
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Thiobarbituric Acid ◽  
Thiobarbituric Acid Reactive Substance ◽  
Reactive Substance ◽  
Reducing Ability ◽  
Liver And Kidney ◽  
Michelia Champaca ◽  
Different Doses

Objective: The present study was aimed at investigating the in-vivo antioxidant activity of the methanol extracts of Limnophila heterophylla and Michelia champaca leaves.Methods: Methanol extract of both plants were administered to rats separately at three different doses of 125, 250 and 500 mg/kg for 21 d to evaluate oxidative stress parameters such as ferric reducing ability of plasma (FRAP), thiobarbituric acid reactive substance (TBARS) and reduced glutathione (GSH) and to evaluate antioxidant enzyme levels of catalase (CAT) and superoxide dismutase (SOD).Results: The methanol extracts of both the plants significantly (p<0.05) elevated the ferric reducing ability of plasma (FRAP) on days 7, 14 and 21 of treatment. Significant (p<0.05) decrease of thiobarbituric acid reactive substance (TBARS) levels along with an increase in the superoxide dismutase (SOD) enzyme level in the liver and kidney at three different doses both the plants was observed. Treatment at a dose of 500 mg/kg b. w of both plants caused a significant increase only in the level of CAT in the liver and kidney. However, there was no significant effect of a thiobarbituric acid reactive substance (TBARS), superoxide dismutase (SOD) and catalase (CAT) in the heart and reduced glutathione (GSH) level in liver, heart and kidney at three different doses both the plants.Conclusion: These outcomes recommend that the leaves of Limnophila heterophylla and Michelia champaca have a potent antioxidant activity which may be responsible for some of its reported pharmacological actions. 

Antioxidant Properties of Deer Blood Hydrolysate and the Possible Mode of Action

2013 ◽  
Vol 634-638 ◽  
pp. 1435-1440 ◽  
Author(s):  
Shuai Wang ◽  
Li Cheng Zhong ◽  
Xue Chao Zhai ◽  
Dong Dong Yin ◽  
Xin Yu Wu
Keyword(s):  
Antioxidant Activity ◽  
Mode Of Action ◽  
Antioxidant Properties ◽  
Reducing Power ◽  
Thiobarbituric Acid ◽  
Degree Of Hydrolysis ◽  
Thiobarbituric Acid Reactive Substance ◽  
Hydrolysis Time ◽  
Reactive Substance ◽  
Tbars Values

Deer blood was hydrolyzed using Alcalase with hydrolysis time ranged form 0 to 6 h, and the degree of hydrolysis (DH) of protein hydrolysates increased with increasing hydrolysis time (P < 0.05). The reducing power, radicals scavenging activities and Cu2+-chelation ability of deer blood hydrolysate (DBH) significantly enhanced with increasing hydrolysis time (P < 0.05). The antioxidant activity of DBH, indicated by thiobarbituric acid-reactive substance (TBARS) values in a liposome-oxidizing system, increased with increasing DH (P < 0.05). The results indicated that antioxidant activity of DBH depended on hydrolysis time, and the hydrolyzed deer blood could be a potent food antioxidant.

scholarly journals BIOGENESIS OF ENDOPLASMIC RETICULUM MEMBRANES

1966 ◽  
Vol 30 (1) ◽  
pp. 73-96 ◽  
Author(s):  
Gustav Dallner ◽  
Philip Siekevitz ◽  
George E. Palade
Keyword(s):  
Endoplasmic Reticulum ◽  
Fatty Acid Composition ◽  
Fatty Acid ◽  
Rat Hepatocytes ◽  
Liver Fatty Acid ◽  
Adult Liver ◽  
Protein Ratio ◽  
Microsomal Membranes ◽  
Rough Er

The development of the endoplasmic reticulum of rat hepatocytes was studied during a period of rapid cell differentiation, i.e., from 3 days before to 8 days after birth. Before birth, the ER increases in volume, remaining predominantly rough surfaced; after birth, the increase continues but affects mainly the smooth-surfaced part of the system. These changes are reflected in variations of the RNA/protein and PLP/protein ratios of microsomal fractions: the first decreases, while the second increases, with age. The analysis of microsomal membranes and of microsomal lipids indicates that the PLP/protein ratio, the distribution of phospholipids, and the rate of P32 incorporation into these phospholipids show little variation over the period examined and are comparable to values found in adult liver. Fatty acid composition of total phosphatides undergoes, however, drastic changes after birth. During the period of rapid ER development in vivo incorporation of leucine-C14 and glycerol-C14 into the proteins and lipids of microsomal membranes is higher in the rough-than in the smooth-surfaced microsomes, for the first hours after the injection of the label; later on (∼10 hr) the situation is reversed. These results strongly suggest that new membrane is synthesized in the rough ER and subsequently transferred to the smooth ER.

Oxidation of olive oil fortified with quercetin, caffeic acid, tyrosol and hydroxytyrosol

2015 ◽  
Vol 45 (3) ◽  
pp. 493-508 ◽  
Author(s):  
Anne Kristine Etherton ◽  
Stanley T. Omaye
Keyword(s):  
Olive Oil ◽  
Caffeic Acid ◽  
Thiobarbituric Acid ◽  
Monounsaturated Fatty Acids ◽  
Polyphenolic Compounds ◽  
Thiobarbituric Acid Reactive Substance ◽  
Content Type ◽  
Health Promoting

Purpose – This paper aims to evaluate effects of the fortification of polyphenolic compound mixtures of quercetin, caffeic acid, tryrosol and hydroxytyrosol in olive oil oxidation. Design/methodology/approach – The authors measured olive oxidation initiated by copper using thiobarbituric acid reactive substance, as an indicator of lipid peroxidation. Findings – Overall, most mixture combinations exhibited oxidation similar to olive oil alone. Some mixture combinations of polyphenolic compounds acted as antioxidants; however, as the concentrations were changed, they became prooxidant in nature. Research limitations/implications – In vitro studies have limitations for extrapolation to in vivo and clinical studies. Practical implications – Such information will be useful in determining optimal concentrations and combinations of antioxidants for reducing rancidity and perhaps as models that could be used to modulate various chronic diseases that are associated with oxidative stress. Originality/value – Olive oil, along with fruits, vegetables and fish, are important constituents of health promoting diets, such as the Mediterranean diet. Active ingredients include monounsaturated fatty acids, oleic acid and a variety of antioxidants including various polyphenolic compounds.

SYNTHESIS, BIOLOGICAL EVALUATION AND DOCKING STUDIES OF NON HEPATOTOXIC 5-SUBSTITUTED THIAZOLIDINE-2, 4-DIONES AS ANTIDIABETIC, ANTI-HYPERLIPIDEMIC, ANTI-OXIDANT AND CYTOTOXIC AGENTS

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (09) ◽  
pp. 19-37
Author(s):  
Karuna S. Shukla ◽  
Shailendra Pandey ◽  
A Pooja Chawla
Keyword(s):  
Antioxidant Activity ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Assay Method ◽  
Diabetic Rat ◽  
Standard Drug ◽  
Docking Score ◽  
Starting Point ◽  
Dpph Method

A series of eleven thiazolidine-2, 4-dione (TZD) derivatives, were synthesized and characterized by FT-IR, 1 H NMR and mass spectral analysis. All the synthesized TZD derivatives were screened for their in vitro and in vivo anti-diabetic and antioxidant, activities and cytotoxicity. In vivo antihyperglycemic effect was assessed by measuring plasma glucose (PG) levels in alloxan-induced type II diabetic rat models. The compound 4h exhibited better blood glucose lowering activity than the standard drug rosiglitazone. The synthesized TZD derivatives were evaluated for hepatotoxicity and pancreatic tissue studies. Antioxidant activity was evaluated by DPPH method and H2 O2 method. Compounds 4a and 4b exhibited potent antioxidant activity. Among the tested compounds for cytotoxicity using MTT assay method, compound 4i exhibited better viability and cytotoxicity activity. Thiazolidinedione derivatives were evaluated for their affinity towards target PPARg, using rosiglitazone as the reference compound molecular docking visualization through FlexX docking program. From selected anti-diabetic targets, the proposed derivatives exhibited better interaction with PPARγ receptor, where rosiglitazone showed docking score of -19.891 kJ/ mol, compound 4h exhibited highest docking score of -31.6068 kJ/mol. The study showed that all the studied compounds were showing higher docking score when compared to control drug rosiglitazone and it could be a remarkable starting point to evaluate structure activity relationships to develop new lead molecules with potential anti-diabetic activities.

scholarly journals In vivo antioxidant potential of Teucrium polium, as compared to α-tocopherol

2007 ◽  
Vol 57 (1) ◽  
pp. 123-129 ◽  
Author(s):  
Parisa Hasani ◽  
Nargues Yasa ◽  
Sanaz Vosough-Ghanbari ◽  
Azadeh Mohammadirad ◽  
Gholamreza Dehghan ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Thiobarbituric Acid ◽  
Antioxidant Potential ◽  
Thiobarbituric Acid Reactive Substances ◽  
Antioxidant Power ◽  
Dry Extract ◽  
Total Antioxidant ◽  
Teucrium Polium

In vivo antioxidant potential of Teucrium polium, as compared to α-tocopherol The present study was undertaken to explore antioxidant potential of Teucrium polium (Lamiaceae) in vivo. Antioxidant activity was measured by three tests including inhibition of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, total antioxidant power (TAP), and thiobarbituric acid reactive substances (TBARS) in serum. Rats received dry extract of T. polium in 80% ethanol by intragastric intubation at doses of 50, 100 and 200 mg kg-1 daily for 14 days. Treatment of rats with T. polium extract showed significant antioxidant activity in the DPPH test as compared to the control. T. polium extract at doses of 50 and 100 mg kg-1 significantly increased rats TAP and decreased TBARS compared to the control. Administration of T. polium at a dose of 200 mg kg-1 per day did not significantly alter serum TAP and TBARS. Antioxidant activities of T. polium at a doses of 50 and 100 mg kg-1 were in all experiments comparable to that of α-tocopherol (10 mg kg-1).

Review on Methods Used to Determine Antioxidant Activity of Origanum majorana

2021 ◽  
Vol 17 ◽  
Author(s):  
Gyanendra Narayan Mohapatra ◽  
Bimala Tripathy ◽  
B.V.V. Ravi Kumar ◽  
Bimalendu Chowdhury ◽  
Rajaram Das
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Activity ◽  
Free Radicals ◽  
Radical Scavenging ◽  
Thiobarbituric Acid ◽  
Antioxidants Activity ◽  
Origanum Majorana ◽  
Online Library

Background: Presence of free radicals in human body are harmful and cell systems are induce many diseases like cardiovascular, diabetes, cancer, inflammation, neuro-degenerative disorder, atherosclerosis, cataract, etc. Antioxidants can balance the effect of free radicals. Antioxidant-rich herbs are identified for preparation of drugs that can be administered to neutralize the free radicals. In the present context the selected medicinal plant is “Origanum majorana” (Family- Lamiaceae) widely known as Marwa in India sub-continent. As the medical professionals show their desires towards composite or lateral treatment, application of drugs with herbal origin gained its importance. Objective: This review presented various in vitro and in vivo methods used in the antioxidant activity study of O.majorana and observed its efficacy to reduce oxidative stress. Methods: Referred many reliable sources like Research gate, PubMed, Science Direct, Google scholar, Wiley online library, books to collect all information about the antioxidant activity of the selected plant. Results: Used several methods to determine the antioxidants activity of O.majorana, such as superoxide radical scavenging, ferric ion reducing antioxidant potency, thiobarbituric acid reactive substances, hydrogen peroxide scavenging, hydroxyl radical scavenging, lipid peroxidation inhibition, etc. The selected plant contains many phytoconstituents such as gallic acid, ferulic acid, apigenin, catechin, rutin, quercetin, luteolin, linolenic acid, β-sitosterol, and essential oils, which may be responsible for antioxidant activity. Conclusions : The review article provides information for investigating and developing new antioxidant methods and major phytoconstituents from O.majorana for better therapy of oxidative stress-mediated complications.

Thiazolidine-2, 4-Diones as Non-Hepatotoxic Tri-action Drug Candidates: Design, Synthesis, Characterization, Biological Evaluation and Docking Studies

2020 ◽  
Vol 17 (9) ◽  
pp. 659-679
Author(s):  
Karuna S. Shukla ◽  
Shailendra Pandey ◽  
Pooja A. Chawla
Keyword(s):  
Antioxidant Activity ◽  
Molecular Docking ◽  
Benzoic Acid ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Standard Drug ◽  
Peripheral Tissues ◽  
Docking Score ◽  
Dpph Method

Thiazolidine-2, 4-diones and their derivatives are a well-established chemical class of compounds that express their pharmacological actions through insulin sensitization and enhanced glucose utilization in peripheral tissues. In the current research different approaches have been employed to synthesize thiazolidine-2, 4-dione derivatives and these synthesized compounds were chemically characterized for the establishment of their chemical structures. A series of thiazolidine-2, 4-dione (TZD) derivatives, Scheme 1 (3A-3V) 22 compounds, were synthesized and characterized by FT-IR, 1H NMR and mass spectral analysis. The title compounds were screened for their in vitro and in vivo antidiabetic, antioxidant, and cytotoxicity studies. In vivo antihyperglycemic effect was assessed by measuring plasma glucose (PG) levels in alloxan-induced type II diabetic rat models. The synthesized TZD derivatives were evaluated for hepatotoxicity and pancreatic tissue integrity. Antioxidant activity was evaluated by the DPPH method and H2O2 method. Thiazolidinedione derivatives were subjected to predict free energy of binding towards target PPAR&#947;, using rosiglitazone as the reference compound for molecular docking visualization through the FlexX docking program. Molecular docking studies are also performed for understanding the binding of a ligand to a receptor. The compound 3V 4-(5- (naphthalen-1-ylmethylene)-2, 4-dioxothiazolidin-3-yl) benzoic acid exhibited better blood glucoselowering activity than that of the standard drug rosiglitazone. Compound 3T and 3U exhibited potent antioxidant activity. Among the tested compounds for cytotoxicity using an MTT assay, compound 3H 5-(4-chlorobenzylidene)-2, 4-dioxothiazolidin-3-yl) benzoic acid exhibited better viability and cytotoxicity activity. From selected anti-diabetic targets, the proposed derivatives exhibited better interaction with PPAR&#947; receptor, for example, while rosiglitazone showed a docking score of -19.891 kJ/mol, compound 3V exhibited highest docking score of -31.6617 kJ/mol. Computational molecular docking study demonstrated the selectivity and provided a binding model for the further refinement of this chemotype. Therefore, this series of thiazolidine-2, 4-diones derivatives (3A-3V) have considerable importance for development as a potential antihyperglycemic and hypolipidemic agents.

scholarly journals In vivo and in vitro antioxidant effects of three Veronica species

2012 ◽  
Vol 7 (3) ◽  
pp. 559-568 ◽  
Author(s):  
Jelena Živković ◽  
Tatjana Ćebović ◽  
Zoran Maksimović
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Thiobarbituric Acid ◽  
Butylated Hydroxytoluene ◽  
Antioxidant Systems ◽  
Antioxidant Power ◽  
Antioxidant Effects

AbstractThe aim of the present study was to examine the antioxidant activity of three Veronica species (Plantaginaceae). The antioxidant potential of various extracts obtained from aerial flowering parts was evaluated by DPPH-free (1,1-diphenyl-2-picrylhydrazyl-free) radical scavenging activity and ferric-reducing antioxidant power assays. Considerable antioxidant activity was observed in the plant samples (FRAP values ranged from 0.97 to 4.85 mmol Fe2+/g, and DPPH IC50 values from 12.58 to 66.34 µg/ml); however, these levels were lower than the activity of the control compound butylated hydroxytoluene (BHT) (FRAP: 10.58 mmol Fe2+/g; DPPH IC50: 9.57 µg/ml). Also, the in vivo antioxidant effects were evaluated in several hepatic antioxidant systems in rats (activities of glutathione peroxidase, glutathione reductase, peroxidase, catalase, xanthine oxidase, glutathione content and level of thiobarbituric acid reactive substances) after treatment with different Veronica extracts, or in combination with carbon tetrachloride (CCl4). Pretreatment with 100 mg/kg b.w. of Veronica extracts inhibited CCl4-induced liver injury by decreasing TBA-RS level, increasing GSH content, and bringing the activities of CAT and Px to control levels. The present study suggests that the extracts analyzed could protect the liver cells from CCl4-induced liver damage by their antioxidative effect on hepatocytes.

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