scholarly journals Hepatoprotective influence of quercetin and ellagic acid on thioacetamide-induced hepatotoxicity in rats

2018 ◽  
Vol 96 (6) ◽  
pp. 624-629 ◽  
Author(s):  
Nehal A. Afifi ◽  
Marwa A. Ibrahim ◽  
Mona K. Galal

Despite all the studies performed to date, therapy choices for liver injuries are very few. Therefore, the search for a new treatment that could safely and effectively block or reverse liver injuries remains a challenge. Quercetin (QR) and ellagic acid (EA) had potent antioxidant and anti-inflammatory activities. The current study aimed at evaluating the potential hepatoprotective influence of QR and EA against thioacetamide (TAA)-induced liver toxicity in rats and the underlying mechanism using silymarin as a reference drug. Fifty mature male rats were orally treated daily with EA and QR in separate groups for 45 consecutive days, and then were injected with TAA twice with 24 h intervals in the last 2 days of the experiment. Administration of TAA resulted in marked elevation of liver indices, alteration in oxidative stress parameters, and significant elevation in expression level of fibrosis-related genes (MMP9 and MMP2). Administration of QR and EA significantly attenuated the hepatic toxicity through reduction of liver biomarkers, improving the redox status of the tissue, as well as hampering the expression level of fibrosis-related genes. In this study, QR and EA were proved to attenuate the hepatotoxicity through their antioxidant, metal-chelating capacity, and anti-inflammatory effects.

2019 ◽  
pp. 82-87
Author(s):  
B. V. Pristupa ◽  
I. O. Shyshkin ◽  
Ya. V. Rozhkovsky ◽  
V. O. Gelmboldt

In the last decade, high cariesprophylactic efficacy of ammonium hexafluorosilicates, including salts with substituted biologically active ammonium cations, has been demonstrated. Among the promising anti-caries agents are recently synthesized 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates, for whose cations anti-inflammatory activity is expected. The aim of the work is to assess the presence of anti-inflammatory activity in the series of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates in the experiment. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates (I–III, respectively) were synthesized according to the previously proposed technique, carrageenan is a commercial preparation, reference drug is a indomethacin. Experiments on the anti-inflammatory activity of hexafluorosilicates were performed on 77 white Wistar male rats weighing 174–190 g using the carrageenan model of inflammation. The inflammatory reaction was reproduced by subplantary administration of 0.1 ml of a 0.2% solution of carrageenan, the studied compounds were administered orally in doses 1/10, 1/20, 1/50 from LD50 for the compound III. It was established that after administration of carrageenan, animals of the control group showed marked paw edema, which gradually increased and was maximal after 24 hours of observation. According to the data obtained, the indices for compounds I-III practically do not differ from those of the control group. This indicates that, despite the results of the PASS forecast and the presence of acetic acid residue, an anti-inflammatory pharmacofor, in compounds I-III, the compounds under study do not have an anti-inflammatory effect in the carrageenan model. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates do not show the expected anti-inflammatory activity in the carrageenan model of inflammation.


2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Halyna M. Kuznietsova ◽  
Maryna S. Yena ◽  
Iryna P. Kotlyar ◽  
Olexandr V. Ogloblya ◽  
Volodymyr K. Rybalchenko

In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2,5-dione (MI-1) on rat colon cancer model. Therefore anti-inflammatory effect of MI-1 on rat acetic acid induced ulcerative colitis (UC) model was aimed to be discovered. The anti-inflammatory effects of MI-1 (2.7 mg/kg daily) compared to reference drug Prednisolone (0.7 mg/kg daily) after 14-day usage were evaluated on macro- and light microscopy levels and expressed in 21-grade scale. Redox status of bowel mucosa was also estimated. It was shown that in UC group the grade of total injury (GTI) was equal to 9.6 (GTIcontrol=0). Increase of malonic dialdehyde (MDA) by 89% and protein carbonyl groups (PCG) by 60% and decrease of superoxide dismutase (SOD) by 40% were also observed. Prednisolone decreased GTI to 3 and leveled SOD activity, but MDA and PCG remained higher than control ones by 52% and 42%, respectively. MI-1 restored colon mucosa integrity and decreased mucosa inflammation down to GTI = 0.5 and leveled PCG and SOD. Thus, MI-1 possessed anti-inflammatory properties, which were more expressed that Prednisolone ones, as well as normalized mucosa redox balance, and so has a prospect for correction of inflammatory processes.


2017 ◽  
Vol 95 (4) ◽  
pp. 396-403 ◽  
Author(s):  
Nema Ali Soliman ◽  
Doaa Hussein Zineldeen ◽  
Mohamed Alaa Katary ◽  
Darin Abd Ali

This study investigated the gastroprotective effects of N-acetylcysteine (NAC) against indomethacin-induced gastric ulcer in rats. Ulceration was induced by a single oral administration of indomethacin (30 mg/kg). 50 male albino rats were allocated into 5 equal groups: control group received normal saline orally, indomethacin group rats received normal saline orally for 5 days and indomethacin (50 mg/kg) on the last day, ranitidine group received ranitidine (reference drug) orally for 5 days (50 mg/kg) before receiving indomethacin (50 mg/kg) on the last day, and NAC groups received NAC orally at 300 and 500 mg/kg, respectively, for 5 days before receiving indomethacin (50 mg/kg) on the last day. Gastric tissue interleukin-1β (IL-1β), interferon-γ (IFN-γ), and caspase-3 levels were immunoassayed. Total thiol (T-SH), myeloperoxidase (MPO), and glucose-6-phosphate dehydrogenase (G6PD) were determined by spectrophotometry. Cytokine-induced neutrophil chemoattractant 2α (CINC-2α) gene expression was evaluated in addition to Bcl-2 immunohistochemistry. Pretreatment with NAC improved the inflammatory, apoptotic, and redox status in a dose-dependent manner particularly in NAC 500 mg/kg pretreated group. These results show a role for NAC in improving indomethacin-induced gastric ulceration via antioxidative, antiapoptotic, and anti-inflammatory interactive mechanisms.


2021 ◽  
pp. 103-110
Author(s):  
Л. М. Малоштан ◽  
К. О. Артемова ◽  
О. М. Шаталова

One of the important treatment landscape widely used for the various disease’s management is phytotherapy, or treatment with herbal medicines. Phytotherapy is used as an independent type of treatment in most cases, and in combination with other drugs as additional treatment. The pain and inflammation control continue as long as there is humanity itself. With old experience of traditional medicine know that Salicaceae have a pronounced anti-inflammatory and analgesic effects. The pharmacological study of the dry extract from Sakhalin willow shoots – the study of analgesic and anti-inflammatory activities in different pharmacological models – was the aim of this work. The analgesic and anti-inflammatory activity of the standardized dry extract from Sakhalin willow shoots (DESWS) was experimentally researched. The study of pharmacological activities of DESWS was carried out at the Educational and Scientific Institute of Applied Pharmacy of the National University of Pharmacy (Kharkov). The effect of DESWS on the course of the inflammatory process was studied in a model of carrageenan edema. Analgesic activity was studied in a model of thermal irritation in white male rats. The study of anti-inflammatory activity in rats on a model of carrageenan edema showed that an effective dose of the studied extract was 30 mg/kg. The greatest reduction in paw edema in rats on the model of carrageenan edema in the first hour of the experiment was observed in the group of animals treated with DESWS at a dose of 30 mg/kg. The anti-inflammatory activity of DESWS was 53.74%, but it was slightly inferior than in the reference drug Diclofenac. It was found that DESWS also shows pronounced analgesic properties at a dose of 30 mg/kg during the first and second hours of the experiment in the model of the limb’s thermal irritation «Hot Plate» in rats. After 120 minutes of experiment the studied activity didn’t change significantly and remained at the level 62.6%. The analgesic effect of DESWS was inferior to antinociceptive activity of the reference drug Metamizole sodium and superior to the studied activity of the reference drug Aspirin. Thus, the dry extract from the Sakhalin willow shoots can affect both pain and inflammation, and it is a potential remedy for further pharmacological research.


Author(s):  
Marwa Abdeltawab Mohammed ◽  
Doaa Mostafa Gharib ◽  
Hoda Ramadan Reyad ◽  
Alaa Aboud Mohamed ◽  
Fadwa A Elroby ◽  
...  

Valproic acid (VPA) is one of the most used anti-epileptic drugs inspite of its many adverse effects as anemia, leucopenia, thrombocytopenia, and liver toxicity. The hepatoprotective effect of alpha-lipoic acid (ALA) was confirmed. Aim of the study: The aim of this study was to detect the protective effect of ALA against the adverse effects of VPA. Materials& Methods: Thirty white albino Wistar male rats were divided into 4 groups. Group (1) was the control group; Group (2) included rats that received ALA (100mg/kg/day) orally for 14 days; Group (3) and Group (4) included rats that received VPA (500 mg/kg/day) for 15 days intraperitoneal, but group 4 rats received ALA (100mg/kg/day) orally for 14 days prior to VPA. Blood samples were collected and livers were excised from rats for colorimetric analysis and rt-PCR. Results: Rats that received VPA showed leucopenia, thrombocytopenia, a significant decrease of SOD, glutathione, Nrf2, and Sirt1, besides a significant increase of MDA and TNF alpha. Prior treatment with ALA prevented all these results. Conclusion: ALA protected against VPA-induced liver damage and hematological disturbance via anti-oxidant and anti-inflammatory properties.


2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Anh Thu Nguyen ◽  
Ki-young Kim

Acne is an inflammatory skin disorder; although some anti-inflammatory medicines for treating acne are available in a market, they have considerable side effects; therefore, new treatment options are needed. In the present study, among the 16 aqueous extracts of plants collected from Jeju Island in Korea which are used to test anti-inflammatory activity, B. davidii showed the strong decline of the proinflammatory cytokine expression against the inflammatory process caused by C. acnes in Human HaCaT keratinocyte cells. B. davidii downregulated the expression of 57% of COX-2, 41% of iNOS, and proinflammatory cytokines 29% of TNF-α, 32% of IL-1β, 21% of IL-6, and 35% of IL-8. Furthermore, B. davidii inhibited NF-κB and MAPK signaling cascades in keratinocytes that activated by toll-like receptor 2 (TLR-2) in response to C. acnes. Given those results, B. davidii is a potential agent to reduce the proinflammatory cytokine expression against C. acnes-induced inflammation and might provide an alternative to the current medications.


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3701
Author(s):  
Salah E. M. Eltom ◽  
Ahmed A. H. Abdellatif ◽  
Hamzah Maswadeh ◽  
Mohsen S. Al-Omar ◽  
Atef A. Abdel-Hafez ◽  
...  

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory in eczema and contact dermatitis. The anti-inflammatory effect of a γ-lactone (5-hexyl-3H-furan-2-one) isolated from ostrich oil and its formulated nano-emulsion in formalin-induced paw edema was investigated in this study. Ostrich oil was saponified using a standard procedure; the aqueous residue was fractionated, purified, and characterized as γ-lactone (5-hexyl-3H-furan-2-one) through the interpretation of IR, NMR, and MS analyses. The γ-lactone was formulated as nano-emulsion using methylcellulose (MC) for oral solubilized form. The γ-lactone methylcellulose nanoparticles (γ-lactone-MC-NPs) were characterized for their size, shape, and encapsulation efficiency with a uniform size of 300 nm and 59.9% drug content. The γ-lactone was applied topically, while the formulated nanoparticles (NPs) were administered orally to rats. A non-steroidal anti-inflammatory drug (diclofenac gel) was used as a reference drug for topical use and ibuprofen suspension for oral administration. Edema was measured using the plethysmograph method. Both γ-lactone and γ-lactone-MC-NPs showed reduction of formalin-induced paw edema in rats and proved to be better than the reference drugs; diclofenac gel and ibuprofen emulsion. Histological examination of the skin tissue revealed increased skin thickness with subepidermal edema and mixed inflammatory cellular infiltration, which were significantly reduced by the γ-lactone compared to the positive control (p-value = 0.00013). Diuretic and toxicity studies of oral γ-lactone-MC-NPs were performed. No diuretic activity was observed. However, lethargy, drowsiness, and refusal to feeding observed may limit its oral administration.


Author(s):  
Eunyoung Park ◽  
Johnathan G. Lyon ◽  
Melissa Alvarado‐Velez ◽  
Martha I. Betancur ◽  
Nassir Mokarram ◽  
...  

Author(s):  
Yong Fu ◽  
Gailing Ma ◽  
Yuqian Zhang ◽  
Wenli Wang ◽  
Tongguo Shi ◽  
...  

Abstract Background Interleukin-10 (IL-10) is a potent immunoregulatory cytokine that plays a pivotal role in maintaining mucosal immune homeostasis. As a novel synthetic inhibitor of salt-inducible kinases (SIKs), HG-9-91-01 can effectively enhance IL-10 secretion at the cellular level, but its in vivo immunoregulatory effects remain unclear. In this study, we investigated the effects and underlying mechanism of HG-9-91-01 in murine colitis models. Methods The anti-inflammatory effects of HG-9-91-01 were evaluated on 2, 4, 6-trinitrobenzene sulfonic acid (TNBS)-, dextran sulfate sodium–induced colitis mice, and IL-10 knockout chronic colitis mice. The in vivo effector cell of HG-9-91-01 was identified by fluorescence-activated cell sorting and quantitative real-time polymerase chain reaction. The underlying mechanism of HG-9-91-01 was investigated via overexpressing SIKs in ANA-1 macrophages and TNBS colitis mice. Results Treatment with HG-9-91-01 showed favorable anticolitis effects in both TNBS- and DSS-treated mice through significantly promoting IL-10 expression in colonic macrophages but failed to protect against IL-10 KO murine colitis. Further study indicated that HG-9-91-01 markedly enhanced the nuclear level of cAMP response element-binding protein (CREB)-regulated transcription coactivator 3 (CRTC3), whereas treatment with lentiviruses encoding SIK protein markedly decreased the nuclear CRTC3 level in HG-9-91-01–treated ANA-1 macrophages. In addition, intracolonic administration with lentiviruses encoding SIK protein significantly decreased the nuclear CRTC3 level in the lamina propria mononuclear cells and ended the anti-inflammatory activities of HG-9-91-01. Conclusions We found that HG-9-91-01 promoted the IL-10 expression of colonic macrophages and exhibited its anticolitis activity through the SIK/CRTC3 axis, and thus it may represent a promising strategy for inflammatory bowel disease therapy.


2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Qiangqiang Zhao ◽  
Duanfeng Jiang ◽  
Xiaoying Sun ◽  
Qiuyu Mo ◽  
Shaobin Chen ◽  
...  

Abstract Background Non-Hodgkin’s lymphoma (NHL) is a malignant disease of lymphoid tissue. At present, chemotherapy is still the main method for the treatment of NHL. R-CHOP can significantly improve the survival rate of patients. Unfortunately, DOX is the main cytotoxic drug in R-CHOP and it can lead to adverse reactions. Therefore, it is particularly important to uncover new treatment options for NHL. Results In this study, a novel anti-tumor nanoparticle complex Nm@MSNs-DOX/SM was designed and constructed in this study. Mesoporous silica nanoparticles (MSNs) loaded with Doxorubicin (DOX) and anti-inflammatory drugs Shanzhiside methylester (SM) were used as the core of nanoparticles. Neutrophil membrane (Nm) can be coated with multiple nanonuclei as a shell. DOX combined with SM can enhance the anti-tumor effect, and induce apoptosis of lymphoma cells and inhibit the expression of inflammatory factors related to tumorigenesis depending on the regulation of Bcl-2 family-mediated mitochondrial pathways, such as TNF-α and IL-1β. Consequently, the tumor microenvironment (TME) was reshaped, and the anti-tumor effect of DOX was amplified. Besides, Nm has good biocompatibility and can enhance the EPR effect of Nm@MSNs-DOX/SM and increase the effect of active targeting tumors. Conclusions This suggests that the Nm-modified drug delivery system Nm@MSNs-DOX/SM is a promising targeted chemotherapy and anti-inflammatory therapy nanocomplex, and may be employed as a specific and efficient anti-Lymphoma therapy.


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