Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin

Curcumin (CUR) has been used in the treatment of various diseases such as cough, fever, skin disease, and infection because of various biological benefits such as anti-inflammatory, antiviral, antibacterial, and antitumor activity. However, CUR is a BCS class 4 group and has a limitation of low bioavailability due to low solubility and permeability. Therefore, the purpose of this study is to prepare a nanosuspension (NSP) loaded with CUR (CUR-NSP) using a statistical design approach to improve the oral bioavailability of CUR, and then to develop CUR-NSP coated with tannic acid to increase the mucoadhesion in the GI tract. Firstly, the optimized CUR-NSP, composed of sodium dodecyl sulfate (SDS) and polyvinylpyrrolidone/vinyl acetate (PVP/VA), was modified with tannic acid (TA). The particle size and polydispersity index of the formulation measured by laser scattering analyzer were 127.7 ± 1.3 nm and 0.227 ± 0.010, respectively. In addition, the precipitation in distilled water (DW) was 1.52 ± 0.58%. Using a differential scanning calorimeter and X-ray diffraction analysis, the stable amorphous form of CUR was confirmed in the formulation, and it was confirmed that CUR-NSP formulation was coated with TA through a Fourier transform-infrared spectroscopy. In the mucoadhesion assay using the turbidity, it was confirmed that TA-CUR-NSP had higher affinity for mucus than CUR-NSP under all pH conditions. This means that the absorption of CUR can be improved by increasing the retention time in the GI tract of the formulation. In addition, the drug release profile showed more than 80% release, and in the cellular uptake study, the absorption of the formulation (TA-CUR-NSP) containing TA acting as an inhibitor of P-gp was increased by 1.6-fold. In the evaluation of antioxidant activity, the SOD activity of TA-CUR-NSP was remarkably high due to TA, which improves cellular uptake and has antioxidant activity. In the pharmacokinetic evaluation, the maximum drug plasma concentration of the TA-coated NSP formulation was 7.2-fold higher than that of the pure drug. In all experiments, it was confirmed that the TA-CUR-NSP is a promising approach to overcome the low oral bioavailability of CUR.

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Radix Pseudostellariae protein-curcumin nanocomplex: Improvement on the stability, cellular uptake and antioxidant activity of curcumin

Food and Chemical Toxicology ◽

10.1016/j.fct.2021.112110 ◽

2021 ◽

Vol 151 ◽

pp. 112110

Author(s):

Xixi Cai ◽

Qingxia Weng ◽

Jiaming Lin ◽

Guiqing Chen ◽

Shaoyun Wang

Keyword(s):

Antioxidant Activity ◽

Cellular Uptake ◽

The Stability

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Antioxidant activity of rice plants sprayed with herbicides

Pesquisa Agropecuária Tropical ◽

10.1590/1983-40632016v4638011 ◽

2016 ◽

Vol 46 (1) ◽

pp. 28-34 ◽

Cited By ~ 5

Author(s):

Marcos André Nohatto ◽

Dirceu Agostinetto ◽

Ana Claudia Langaro ◽

Claudia de Oliveira ◽

Queli Ruchel

Keyword(s):

Oxidative Stress ◽

Lipid Peroxidation ◽

Antioxidant Activity ◽

Acetolactate Synthase ◽

Defense Behavior ◽

Sod Activity ◽

Rice Plants ◽

Synthase Inhibitor ◽

Acetyl Coenzyme A Carboxylase ◽

Lower Capacity

ABSTRACT Understanding the physiological defense behavior of plants subjected to herbicide application may help to identify products with higher or lower capacity to cause oxidative stress in crops. This study aimed at evaluating the effect of herbicides in the antioxidant activity of rice plants. The experimental design was completely randomized, with six replications. Treatments consisted of the herbicides bentazon (photosystem II inhibitor; 960 g ha-1), penoxsulam (acetolactate synthase inhibitor; 60 g ha-1), cyhalofop-butyl (acetyl coenzyme-A carboxylase inhibitor; 315 g ha-1) and a control. After the herbicides application, samples of rice shoots were collected at 12, 24, 48 and 96 hours after application (HAA). The components evaluated were hydrogen peroxide (H2O2), lipid peroxidation and activity of the antioxidant enzymes superoxide dismutase (SOD) and catalase (CAT). Bentazon (up to 24 HAA) and penoxsulam (48 and 96 HAA) reduced the CAT activity. Moreover, these herbicides increased the levels of H2O2, lipid peroxidation and SOD activity, indicating a condition of oxidative stress in rice plants. The cyhalofop-butyl herbicide did not alter the antioxidant activity, showing that it causes less stress to the crop.

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The effect of bee venom and hyperthermia on the lipoperoxidation and antioxidant activity of the blood of tumor-bearing animals

JOURNAL of SIBERIAN MEDICAL SCIENCES ◽

10.31549/2542-1174-2021-3-25-33 ◽

2021 ◽

pp. 25-33

Author(s):

M.A. Shabalin ◽

◽

A.V. Deryugina ◽

V.V. Nazarova ◽

E.A. Gracheva ◽

...

Keyword(s):

Lipid Peroxidation ◽

Antioxidant Activity ◽

Malignant Tumors ◽

Combined Treatment ◽

Bee Venom ◽

Control Group ◽

Sod Activity ◽

Tumor Bearing ◽

Prolonged Effect ◽

Control Tumor

Introduction. Nowadays, it has been shown that one of the possible ways to increase the effectiveness of the treatment of malignant tumors is the use of combined treatment methods. Aim. To study the intensity of lipid peroxidation (LPO) and the activity of superoxide dismutase (SOD) in hyperthermia against the background of bee venom in the blood of tumor-bearing rats. Materials and methods. The experimental animals were divided into 5 groups: 1st — intact; 2nd — control (tumor-bearing animals (PS-1 tumor strain) with intraperitoneal (IP) administration of saline solution); 3rd, 4th and 5th groups — tumor-bearing animals with IP administration of 0.5 ml of bee venom against the background of hyperthermia 42, 43 and 44°C respectively. The content of diene and triene conjugates, Schiff bases (SB) and SOD activity in the blood of animals was determined. Results. From the 1st day after the end of the experiment, a statistically significant decrease in triene conjugates was recorded in all experimental groups compared to the control group. SB decreased on the 1st–7th day after the end of the experiment with the action of hyperthermia 42°C and bee venom, on the 7th–28th day — with the action of hyperthermia 43°C and bee venom, and on the 28th day — with the action of bee venom and hyperthermia 44°C, which was accompanied by an increase in SOD activity from the 7th day in all experimental groups compared to the control group. Conclusion. Hyperthermia in combination with the action of bee venom causes a decrease in lipid peroxidation products and an increase in antioxidant activity in the blood of tumor-bearing rats. The most effective action, in our opinion, is the use of bee venom against the background of hyperthermia of 43°C, at which a prolonged effect is recorded both with respect to a decrease in the concentration of SB and an increase in the activity of SOD.

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Novel 1,2-thiazine-pyridine hybrid: Design, synthesis, antioxidant activity and molecular docking study

Letters in Drug Design & Discovery ◽

10.2174/1570180819666220106112650 ◽

2022 ◽

Vol 19 ◽

Author(s):

Rania B. Bakr ◽

Nadia A.A. Elkanzi

Keyword(s):

Antioxidant Activity ◽

Ascorbic Acid ◽

Biological Activities ◽

Radical Scavenging ◽

Reducing Power ◽

Docking Study ◽

Molecular Docking Study ◽

Sod Activity ◽

Design Synthesis ◽

In Silico Docking

Background & objectives: 1,2-thiazine and pyridine heterocycles drew much attention due to their biological activities including antioxidant activity. Based upon fragment based drug design, novel pyrido[1,2]thiazines 9a-c, thiazolidinopyrido[1,2]thiazines 10a-c and azetidinopyrido[1,2]thiazines 11a-c were designed and prepared. Methods: These novel derivatives 9a-c, 10a-c and 11a-c were subjected to screening for their antioxidant activity via various assays as DPPH radical scavenging potential, reducing power assay and metal chelating potential. Results: All the assayed derivatives exhibited excellent antioxidant potential and the tested compounds 9a, 9b, 10a, 10b, 11a and 11b exhibited higher DPPH scavenging potential (EC50 = 32.7, 53, 36.1, 60, 40.6 and 67 µM, respectively) than ascorbic acid (EC50 = 86.58 µM). While targets 9a, 10a and 11a (RP50 = 52.19, 59.16 and 52.25 µM, respectively) exhibited better reducing power than the ascorbic acid (RP50 = 84.66 µM). Computational analysis had been utilized to prophesy the bioactivity and molecular properties of the target compounds. Conclusion: To predict the binding manner of the novel derivatives as antioxidants, in-silico docking study had been performed to all the newly prepared compounds inside superoxide dismutase (SOD) and catalase (CAT) active site. The most active antioxidant candidate 9a (EC50 = 32.7 µM, RP50 = 52.19 µM) displayed excellent binding with Lys134 amino acid residing at Cu-Zn loop of SOD with binding energy score = -7.54 Kcal/mol thereby increase SOD activity and decrease reactive oxygen species.

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Improving Oral Bioavailability of Luteolin Nanocrystals by Surface Modification of Sodium Dodecyl Sulfate

AAPS PharmSciTech ◽

10.1208/s12249-021-02012-y ◽

2021 ◽

Vol 22 (3) ◽

Author(s):

Jiali Liu ◽

Yongbing Sun ◽

Meng Cheng ◽

Qiaoming Liu ◽

Wan Liu ◽

...

Keyword(s):

Surface Modification ◽

Sodium Dodecyl Sulfate ◽

Oral Bioavailability ◽

Sodium Dodecyl ◽

Dodecyl Sulfate

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Characterization of Sporidiobolus ruineniae A45.2 Cultivated in Tannin Substrate for Use as a Potential Multifunctional Probiotic Yeast in Aquaculture

Journal of Fungi ◽

10.3390/jof6040378 ◽

2020 ◽

Vol 6 (4) ◽

pp. 378

Author(s):

Apinun Kanpiengjai ◽

Chartchai Khanongnuch ◽

Saisamorn Lumyong ◽

Aksarakorn Kummasook ◽

Suwapat Kittibunchakul

Keyword(s):

Staphylococcus Aureus ◽

Antioxidant Activity ◽

Gallic Acid ◽

Tannic Acid ◽

Feed Additive ◽

Intact Cells ◽

Produce Cell ◽

Viable Cells ◽

Probiotic Yeast ◽

Acid Substrate

At present, few yeast species have been evaluated for their beneficial capabilities as probiotics. Sporidiobolus ruineniae A45.2, a carotenoid-producing yeast, was able to co-produce cell-associated tannase (CAT), gallic acid and viable cells with antioxidant activity when grown in a tannic acid substrate. The aim of this research study was to identify the potential uses of S. ruineniae A45.2 obtained from a co-production system as a potential feed additive for aquaculture. S. ruineniae A45.2 and its CAT displayed high tolerance in pH 2.0, pepsin, bile salts and pancreatin. Furthermore, its viable cells were characterized by moderate hydrophobicity, high auto-aggregation and moderate co-aggregation with Staphylococcus aureus, Salmonella ser. Thyphimurium and Streptococcus agalactiae. These attributes promoted S. ruineniae A45.2 as a multifunctional probiotic yeast. In addition, the intact cells possessed antioxidant activities in a 100–150 μg gallic acid equivalent (GAE)/mL culture. Remarkably, the fermentation broth demonstrated higher antioxidant activity of 9.2 ± 1.8, 9.0 ± 0.9, and 9.8 ± 0.7 mg GAE/mL culture after FRAP, DPPH and ABTS assays, respectively. Furthermore, higher antimicrobial activity was observed against Bacillus cereus, Staphylococcus aureus and Strep. agalactiae. Therefore, cultivation of S. ruineniae A45.2 with a tannic acid substrate displayed significant potential as an effective multifunctional feed additive.

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Catabolism of streptokinase and polyethylene glycol-streptokinase: evidence for transport of intact forms through the biliary system in the mouse

Blood ◽

10.1182/blood.v76.1.73.73 ◽

1990 ◽

Vol 76 (1) ◽

pp. 73-79 ◽

Cited By ~ 15

Author(s):

FH Brucato ◽

SV Pizzo

Keyword(s):

Molecular Weight ◽

Polyethylene Glycol ◽

Gel Electrophoresis ◽

Proteinase Inhibitors ◽

Polyacrylamide Gel Electrophoresis ◽

Sodium Dodecyl ◽

Gi Tract ◽

Substantial Fraction ◽

Sds Page ◽

Derivatives Of

Abstract The catabolism of streptokinase (SK) and polyethylene glycol derivatives of SK (PEG-SK) were studied in mice. The clearance and catabolism of SK:plasmin (SK:Pm) and PEG-SK:Pm activator complexes were also investigated. Native 125I-SK cleared rapidly (t1/2 = 15 minutes) from the circulation, with the majority of the ligand accumulating in the liver and gastrointestinal (GI) tract and a substantial fraction also localizing in the kidneys. SK, which was removed from the plasma by the liver, was secreted into bile and then the GI tract. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) demonstrated that 125I-SK recovered from liver and bile was homogeneous and of the same molecular weight (mol wt approximately 50,200) as native SK. PEG-125I-SK cleared slowly (t1/2 greater than 200 minutes), with more than 80% of the preparation localizing in liver and GI tract. The PEG-125I-SK secreted into the bile was also intact. The bile containing 125I-SK was incubated with stoichiometric amounts of plasminogen and electrophoresed under nondenaturing conditions. This study demonstrated that the secreted SK was able to form SK:Pg complexes. SDS-PAGE also showed activation of 125I-Pg that was incubated with recovered bile containing the SK. 125I-SK:Pm catabolism was also studied. In these experiments, the mol wt approximately 42,000 fragment obtained when SK is cleaved by plasmin was found in the bile. This fragment of 125I-SK was not recovered as part of a complex with plasmin, consistent with our previous observations that catabolism of SK:Pm involves transfer of the plasmin to plasma proteinase inhibitors while SK is catabolized independently. By contrast, when PEG-125I-SK:Pm was injected into mice, only intact PEG-125I-SK was found in the bile, consistent with our previous observations that the PEG derivatization blocks its degradation by plasmin.

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Red Grape Pomace Rich in Polyphenols Diet Increases the Antioxidant Status in Key Organs—Kidneys, Liver, and Spleen of Piglets

Animals ◽

10.3390/ani9040149 ◽

2019 ◽

Vol 9 (4) ◽

pp. 149 ◽

Cited By ~ 5

Author(s):

Veronica Sanda Chedea ◽

Laurentiu Mihai Palade ◽

Rodica Stefania Pelmus ◽

Catalin Dragomir ◽

Ionelia Taranu

Keyword(s):

Lipid Peroxidation ◽

Antioxidant Activity ◽

Antioxidant Status ◽

Total Antioxidant Status ◽

Good Health ◽

Grape Pomace ◽

Mesenteric Lymph Nodes ◽

Polyphenol Content ◽

Sod Activity ◽

Blood Biochemical

The aim of this work was to evaluate the influence of a diet containing 5% dried GP on the antioxidant status (total antioxidant status (TAS), antioxidant enzyme activity (catalase-CAT, superoxide dismutase-SOD, and gluthatione peroxidase-GPx), and lipid peroxidation) on the key organs of the liver, kidneys, and spleen in relation to health status as indicated by blood biochemical parameters and total polyphenol content in the blood, organs (liver, spleen, kidney, mesenteric lymph nodes, heart, and brain) and Longissimus dorsi muscle in piglets. The GP diet results in a significant increase of TAS in the liver, spleen, and kidneys, with increased CAT activity in the spleen and kidneys, increased SOD activity in the liver, kidneys, and spleen, and increased GPx activity in the kidneys, as well as a decrease in lipid peroxidation in the liver and kidneys. The GP included in the piglets’ feed contained polyphenols that showed antioxidant activity and were absorbed in the plasma, contributing to maintaining the good health of the animals. The inclusion of 5% GP inclusion in the diets of piglets is beneficial for overall normal blood constituent metabolism and helps to maintain piglet health by increasing the polyphenol content in blood plasma and antioxidant activity in the liver, spleen, and kidneys.

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