scholarly journals In Vivo Enzymes Activities of Some Ru(II) Compounds with N-Alkylphenothiazines

2016 ◽  
Vol 66 (4) ◽  
pp. 497-508
Author(s):  
P. Milena Krstić ◽  
Z. Sunčica Borozan ◽  
P. Sofija Sovilj ◽  
R. Sanja Grgurić-Šipka ◽  
M. Jelena Oljarević

Abstract The purpose of the present study was to investigate and compare the effects of two ruthenium complexes with trifluoperazine on acethylcholinesterase enzyme activity and lactate dehydrogenase levels in vivo under physiological conditions in rats blood. Complexes 1 and 2 showed positive effects on acethylcholinesterase at all doses and did not disturb its normal activity. Total LDH activity was inhibited in the presence of both complexes, but Ru(II) complexes showed different effects on the activity of LDH isoenzymes. The activities of LDH1 and LDH2 isoenzymes were decreased in all applied doses of the complex 2, while the activity of LDH2 reduced using complex 1 in the same doses. Results of the present study suggest the neuro- and cardio protective potential of oral administration of complexes 1 and 2, as non-toxic compounds under physiological conditions. These protective effects are the result of their potent antioxidant activity.

2019 ◽  
Author(s):  
C. Tigrine ◽  
A. Kameli

In this study a polyphenolic extract from Cleome arabica leaves (CALE) was investigated for its antioxidant activity in vitro using DPPH•, metal chelating and reducing power methods and for its protective effects against AraC-induced hematological toxicity in vivo using Balb C mice. Results indicated that CALE exhibited a strong and dose-dependent scavenging activity against the DPPH• free radical (IC50 = 4.88 μg/ml) and a high reducing power activity (EC50 = 4.85 μg/ml). Furthermore, it showed a good chelating effects against ferrous ions (IC50 = 377.75 μg/ml). The analysis of blood showed that subcutaneous injection of AraC (50 mg/kg) to mice during three consecutive days caused a significant myelosupression (P < 0.05). The combination of CALE and AraC protected blood cells from a veritable toxicity. Where, the number of the red cells, the amount of hemoglobin and the percentage of the hematocrite were significantly high. On the other hand, AraC cause an elevation of body temperature (39 °C) in mice. However, the temperature of the group treated with CALE and AraC remained normal and did not exceed 37.5 °C. The observed biological effects of CALE, in vitro as well as in vivo, could be due to the high polyphenol and flavonoid contents. In addition, the antioxidant activity of CALE suggested to be responsible for its hematoprotective effect.


2018 ◽  
Vol 1 ◽  
Author(s):  
Kazuo Miyashita ◽  
Masashi Hosokawa

Marine organisms produce a variety of carotenoids with unique functional groups such as allene, acetylene, acetyl, and hydroxymethyl. Astaxanthin and fucoxanthin are representative marine carotenoids on which numerous studies have been performed. Due to the characteristic conjugated polyene chain and terminal ring structures, both carotenoids can act as strong antioxidants. Major nutritional effects of astaxanthin, such as cardio-, skin-, and ocular-protective effects, are based on its in vivo antioxidant activity. However, the antioxidant activity of fucoxanthin is not largely involved in its characteristic nutritional activity and anti-obesity and anti-diabetic effects. The major molecular mechanisms of both effects involve modulating the expression of related genes and proteins by fucoxanthin metabolites.


2019 ◽  
Vol 8 (10) ◽  
pp. 1699
Author(s):  
Xiaoyu Cai ◽  
Liang Gao ◽  
Magali Cucchiarini ◽  
Henning Madry

The deleterious effects of nicotine on various health conditions have been well documented. Although many orthopedic diseases are adversely affected by nicotine, little is known about its preclinical effects on chondrogenesis or osteogenesis, cartilage formation, osteoarthritis (OA), and osteochondral repair. A systematic review was conducted examining the current scientific evidence on the effects of nicotine on chondrogenesis or osteogenesis in vitro, possible consequences of prenatal nicotine exposure (PNE) on cartilage and OA susceptibility in the offspring, and whether nicotine affects OA development and osteochondral repair in vivo, always focusing on their underlying mechanisms. The data reveal dose-dependent effects on articular chondrocytes and on the chondrogenesis and osteogenesis of medicinal signaling cells in vitro, with lower doses often resulting in positive effects and higher doses causing negative effects. PNE negatively affects articular cartilage development and induces OA in the offspring without or with nicotine exposure. In contrast, protective effects on OA development were only reported in monosodium iodoacetate-induced small animal models. Finally, nicotine repressed MSC-based osteochondral repair in vivo. Future studies need to investigate dose-dependent clinical effects of smoking on cartilage quality in offspring, OA susceptibility and progression, and osteochondral repair more in detail, thus identifying possible thresholds for its pathological effects.


Cancers ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1372 ◽  
Author(s):  
Goran Hamid Mohammad ◽  
Vessela Vassileva ◽  
Pilar Acedo ◽  
Steven W. M. Olde Damink ◽  
Massimo Malago ◽  
...  

Reprogrammed glucose metabolism is one of the hallmarks of cancer, and increased expression of key glycolytic enzymes, such as pyruvate kinase M2 (PKM2) and lactate dehydrogenase A (LDHA), has been associated with poor prognosis in various malignancies. Targeting these enzymes could attenuate aerobic glycolysis and inhibit tumor proliferation. We investigated whether the PKM2 activator, TEPP-46, and the LDHA inhibitor, FX-11, can be combined to inhibit in vitro and in vivo tumor growth in preclinical models of pancreatic cancer. We assessed PKM2 and LDHA expression, enzyme activity, and cell proliferation rate after treatment with TEPP-46, FX-11, or a combination of both. Efficacy was validated in vivo by evaluating tumor growth, PK and LDHA activity in plasma and tumors, and PKM2, LDHA, and Ki-67 expression in tumor tissues following treatment. Dual therapy synergistically inhibited pancreatic cancer cell proliferation and significantly delayed tumor growth in vivo without apparent toxicity. Treatment with TEPP-46 and FX-11 resulted in increased PK and reduced LDHA enzyme activity in plasma and tumor tissues and decreased PKM2 and LDHA expression in tumors, which was reflected by a decrease in tumor volume and proliferation. The targeting of glycolytic enzymes such as PKM2 and LDHA represents a promising therapeutic approach for the treatment of pancreatic cancer.


Author(s):  
A. R. Qureshi ◽  
J. H. Wilkinson

During incubation with rabbit blood in vitro rabbit-muscle lactate dehydrogenase-5 was inactivated at a rate similar to that observed in vivo. By contrast plasma and plasma containing erythrocytes had no effect on the enzyme activity, but plasma containing leucocytes inactivated the enzyme at the same rate as whole blood. The results obtained support the concept that intravascular inactivation accounts for the disappearance of enzymes from the circulation.


2012 ◽  
Vol 5 (1) ◽  
pp. 51-56 ◽  
Author(s):  
MC Jagadeesh ◽  
M Sreepriya ◽  
Geetha Bali ◽  
D Manjulakumari

The effects of administration of Curcumin and Embelin on the levels of certain trace elements and other elements of clinical significance, during experimental hepatocarcinogenesis induced by Diethylnitrosamine/ Phenobarbital (DENA/PB) was studied in Wistar strain male albino rats. The levels of calcium, potassium and sodium were determined in the serum of control and experimental groups of rats. Additionally, the levels of chromium, copper, magnesium, molybdenum and zinc were also determined in the serum, liver and kidney of these rats. Furthermore, lactate dehydrogenase (LDH) activity was also assayed in the serum of these rats. Results revealed both significant and non-significant alterations in the levels of few elements during DENA/PB-induced experimental hepatocarcinogenesis. A statistically significant increase in LDH activity was found in the serum during the cancerous condition. Pre- and co-treatment with Curcumin and Embelin was found to protect the liver against the carcinogenic effects of DENA/PB. This protection was i) due to their ability to prevent changes in the levels of elements studied and ii) by the statistically significant decrease in the activity of LDH  that increased in DENA/PB-treated rats and LDH activity in the rats given only Embelin and Curcumin indicating their non-toxic effect. Our present results demonstrate the ability of Embelin and Curcumin to protect against DENA/PB-induced hepatocarcinogenesis in rats.DOI: http://dx.doi.org/10.3126/ijls.v5i1.5576 International Journal of Life Sciences Vol.5(1) 2011 51-56


2019 ◽  
Vol 14 (12) ◽  
pp. 1934578X1989667
Author(s):  
Jing-Jing Li ◽  
Ling Mo ◽  
Jia-Le Song

This study was to investigate antioxidant activities of the ethanol extract from young edible leaves of Ficus vasculosa in vitro and in vivo . Ficus vasculosa ethanol extract (FVEE) showed significantly higher reducing power and α,α-diphenyl-β-picrylhydrazyl (DPPH) radical scavenge activity than vitamin C ( P < 0.05). FVEE also showed an activity to resist the D-galactose-induced aging in mice assessed by serum and tissue levels of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GSH-Px). Total serum and tissue oxidative status, total antioxidantresponse, glutathione (GSH) and malondialdehyde (MDA) levels have been also measured. Pretreatment with FVEE at 200 mg/kg·body weight significantly increased enzyme activity of SOD and CAT in serum and hepatic tissue ( P < 0.05), as well as significantly increased enzyme activity of SOD in kidney ( P < 0.05). Furthermore, high concentration of FVEE pretreatment significantly increased the level of GSH in serum, hepatic tissue and kidney ( P < 0.05), meanwhile significantly decreased MDA production in hepatic tissue and kidney ( P < 0.05). In addition, the phytochemical investigation discovered six previously described compounds from FVEE, naringenin (1), vanillic acid (2), 9, 16-dioxo-10, 12, 14-octadeca-trienoic acid (3), 2, 6-dimethoxy-1, 4-benzoquinone (4), apigenin (5) and norartocarpetin (6), and all compounds were isolated from this plant for the first time. Among the various compounds found, the rare highly unsaturated fatty acid 9, 16-dioxo-10, 12, 14-octadeca-trienoic acid (3) has been identified, which had been isolated only once before from F. vasculosa. Evaluation of the antioxidant activity of isolated compounds showed naringenin (1) to be the most active. According to our research, FVEE present very high antioxidant activity in vitro due to the presence of several compounds known for their antioxidant activity such as flavonoid and phenolic acid. In vivo, the ethanol extract had improvement effects against D-galactose-induced aging by reducing oxidative stress.


Author(s):  
Azita Faraki ◽  
Fatemeh Rahmani

Probiotics and Lactic Acid Bacteria play important roles such as the production of antimicrobial compounds and other metabolites. So they have positive effects on human health. When reactive oxygen species generated in excess or cellular defenses are deficient, biomolecules can be damaged by the oxidative stress process. Various studies have shown that the best way to protect the human body from the effects of oxidation reactions is to avoid them, which can be accomplished by using antioxidants. Due to the damages of synthetic antioxidants, their usage has been discussed. Nowadays natural antioxidants derived from bio-resources have recently gained a lot of attention as a potential replacement for synthetic antioxidants. Probiotic bacteria are thought to defend against oxidative stress by restoring the gut microbiota, according to hypothesis of some scientists. This type of microorganisms indicated their antioxidant activity by producing and increasing antioxidant enzymes, production of secondary metabolites, small hydrolyzed peptides in food, resistance to the presence of hydrogen peroxide, and production of intracellular and extracellular compounds such as Exopolysaccharides. Also, they have shown their positive effect on in vivo models. In conclusion, according to the results of studies, lactic acid bacteria and probiotics are significant sources of natural antioxidants. Therefore, they have important research value and market development potential. Also, it should be noted that the mechanism of antioxidant activity of this group of microorganisms has not been fully investigated, this requires further research.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Armin Mooranian ◽  
Susbin Raj Wagle ◽  
Bozica Kovacevic ◽  
Ryu Takechi ◽  
John Mamo ◽  
...  

AbstractThe antilipidemic drug, probucol (PB), has demonstrated potential applications in Type 2 diabetes (T2D) through its protective effects on pancreatic β-cells. PB has poor solubility and bioavailability, and despite attempts to improve its oral delivery, none has shown dramatic improvements in absorption or antidiabetic effects. Preliminary data has shown potential benefits from bile acid co-encapsulation with PB. One bile acid has shown best potential improvement of PB oral delivery (ursodeoxycholic acid, UDCA). This study aimed to examine PB and UDCA microcapsules (with UDCA microcapsules serving as control) in terms of the microcapsules’ morphology, biological effects ex vivo, and their hypoglycemic and antilipidemic and anti-inflammatory effects in vivo. PBUDCA and UDCA microcapsules were examined in vitro (formulation studies), ex vivo and in vivo. PBUDCA microcapsules exerted positive effects on β-cells viability at hyperglycemic state, and brought about hypoglycemic and anti-inflammatory effects on the prediabetic mice. In conclusion, PBUDCA co-encapsulation have showed beneficial therapeutic impact of dual antioxidant-bile acid effects in diabetes treatment.


Genetics ◽  
1992 ◽  
Vol 131 (2) ◽  
pp. 413-421 ◽  
Author(s):  
S Merkle ◽  
J Favor ◽  
J Graw ◽  
S Hornhardt ◽  
W Pretsch

Abstract Two ethylnitrosourea-induced heterozygous mouse mutants with approximately 58 and 50% of wild-type lactate dehydrogenase (LDH) activity and a gamma-ray-induced heterozygous mutant with 50% of wild-type LDH activity in blood, liver and spleen (expressing predominantly the Ldh-1 gene) were recovered in mutagenicity experiments following spermatogonial treatment. Physiological and genetic studies revealed no indications for differences in fertility as well as hematological or other physiological traits between heterozygotes of each mutant line and wild types. This suggests that neither the mutations in the heterozygous state per se nor the resulting approximate 42 to 50% LDH deficiency affect metabolism and fitness. Physicochemical and immunological studies clearly demonstrated that the two mutations with 50% deficiency in heterozygotes result from null alleles of the Ldh-1 structural locus, generating neither enzyme activity nor immunological cross-reacting material. In contrast, the heterozygous mutant with approximately 58% of normal blood LDH activity was shown to be due to a Ldh-1 allele creating protein subunits, which in random assortment with wild-type subunits in vivo exhibit a reduced specific activity and further alterations of kinetic and physicochemical characteristics. All the mutations in the homozygous state were found to be lethal at an early postimplantation stage of embryonic development, probably due to a block of glycolysis with the corresponding loss of the main source of metabolic energy during this ontogenetic stage. The distinct physiological consequences of the total absence of a functioning LDH-A subunit in mice and humans are discussed.(ABSTRACT TRUNCATED AT 250 WORDS)


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