Evaluation of antioxidant activity and toxicity of sulfur- or selenium-containing 4-(arylchalcogenyl)-1H-pyrazoles

Pyrazoles represent a significant class of heterocyclic compounds that exhibit pharmacological properties. The present study aimed to investigate the antioxidant potential of pyrazol derivative compounds in brain of mice in vitro and the effect of pyrazol derivative compounds in the oxidative damage and toxicity parameters in mouse brain and plasma of mice. The compounds tested were 3,5-dimethyl-1-phenyl-4-(phenylselanyl)-1H-pyrazol (1a), 3,5-dimethyl-4-(phenylselanyl)-1H-pyrazole (2a), 4-((4-methoxyphenyl)selanyl)-3,5-dimethyl-1-phenyl-1H-pyrazole (3a), 4-((4-chlorophenyl)selanyl)-3,5-dimethyl-1-phenyl-1H-pyrazole (4a), 3,5-dimethyl-1-phenyl-4-(phenylthio)-1H-pyrazole (1b), 3,5-dimethyl-4-(phenylthio)-1H-pyrazole (2b), 4-((4-methoxyphenyl)thio)-3,5-dimethyl-1-phenyl-1H-pyrazole (3b), 4-((4-chlorophenyl)thio)-3,5-dimethyl-1-phenyl-1H-pyrazole (4b), and 3,5-dimethyl-1-phenyl-1H-pyrazole (1c). In vitro, 4-(arylcalcogenyl)-1H-pyrazoles, at low molecular range, reduced lipid peroxidation and reactive species in mouse brain homogenates. The compounds also presented ferric-reducing ability as well nitric oxide-scavenging activity. Especially compounds 1a, 1b, and 1c presented efficiency to 1,1-diphenyl-2-picryl-hydrazyl-scavenging activity. Compounds 1b and 1c presented 2,20 -azino-bis(3-ethylbenzthiazoline-6-sulfonic acid)-scavenging activity. In vivo assays demonstrated that compounds 1a, 1b, and 1c (300 mg/kg, intragastric, a single administration) did not cause alteration in the of δ-aminolevulinic acid dehydratase activity, an enzyme that exhibits high sensibility to prooxidants situations, in the brain, liver, and kidney of mice. Compound 1c reduced per se the lipid peroxidation in liver and brain of mice. Toxicological assays demonstrate that compounds 1a, 1b, and 1c did not present toxicity in the aspartate aminotransferase, alanine aminotransferase, urea, and creatinine levels in the plasma. In conclusion, the results demonstrated the antioxidant action of pyrazol derivative compounds in in vitro assays. Furthermore, the results showed low toxicity of compounds in in vivo assays.

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Preliminary Study and Improve the Production of Metabolites with Antifungal Activity by a Bacillus Sp Strain IBA 33

Microbiology Insights ◽

10.4137/mbi.s995 ◽

2009 ◽

Vol 2 ◽

pp. MBI.S995 ◽

Cited By ~ 5

Author(s):

María Antonieta Gordillo ◽

Antonio Roberto Navarro ◽

Lidia María Benitez ◽

Marta Inés Torres De Plaza ◽

Maria Cristina Maldonado

Keyword(s):

Pathogenic Fungi ◽

Geotrichum Candidum ◽

Culture Conditions ◽

Penicillium Expansum ◽

In Vitro Assays ◽

Bacillus Sp ◽

In Vivo Assays ◽

Metabolites Production

Bacillus sp strain IBA 33 metabolites, isolated from decaying lemon fruits, were evaluated for the control of pathogenic and non-pathogenic fungi ( Penicillium digitatum, Geotrichum candidum, Penicillium expansum, Aspergillus clavatus, Aspergillus flavus, Aspergillus niger, and Fusarium moniliforme). These metabolites were recovered from Landy medium (LM) without aminoacids. In order to optimize metabolites production the LM was modified by adding different concentrations and sources of amino acids and carbohydrates at different culture conditions. Bacillus sp strain IBA 33 metabolites efficacy to control fungi were evaluated with in vitro and in vivo assays. A. flavus growth inhibition was 52% with the metabolites of Bacillus sp strain IBA 33 recovered from LM (MBLM) in vitro assays. MBLM supplemented with 0.5% glutamic acid, inhibited the growth of P. digitatum, G. candidum, A. clavatus, A. niger and F. moniliforme by 65%, 88.44%, 84%, 34% and 92% respectively. The highest inhibition of P. expansum was 45% with MBLM supplemented with 0.5% aspartic acid. Similar results were obtained in vivo assays. These results showed that Bacillus sp strain IBA 33 metabolites specificity against fungi depended on the composition of the LM.

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Polystachyasaponin with Adjuvant Activity from Entada polystachya

Zeitschrift für Naturforschung B ◽

10.1515/znb-2010-0514 ◽

2010 ◽

Vol 65 (5) ◽

pp. 628-634 ◽

Cited By ~ 3

Author(s):

Bernadete P. da Silva ◽

José P. Parente

Keyword(s):

2D Nmr ◽

In Vitro Assays ◽

Triterpenoid Saponin ◽

Spectroscopic Techniques ◽

Adjuvant Activity ◽

In Vivo Assays ◽

Cellular Immune ◽

C Nmr

A new complex triterpenoid saponin, polystachyasaponin, was isolated from leaves of Entada polystachya (L.) DC. (Leguminosae) by using chromatographic methods. Its structure was established as 15,16-dihydroxy-3-[[O-β -D-xylopyranosyl-(1→2)-O-α-L-arabinopyranosyl-(1→6)-2- (acetylamino)-2-deoxy-β -D-glucopyranosyl]oxy]-(3β ,15α,16α)-olean-12-en-28-oic acid O-D-apio- β -D-furanosyl-(1→3)-O-β -D-xylopyranosyl-(1→2)-O-[β -D-glucopyranosyl-(1→4)]-6-O-[(2E,6R)- 6-hydroxy-2,6-dimethyl-1-oxo-2,7-octadienyl]-β -D-glucopyranosyl ester. Structural elucidation was performed using detailed analyses of 1H and 13C NMR spectra including 2D NMR spectroscopic techniques and chemical conversions. The hemolytic activity of the saponin was evaluated using in vitro assays, and its adjuvant potential on the cellular immune response against ovalbumin antigen was investigated using in vivo assays.

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Renewing potency assays: Moving forward from traditional methods

Biomedical Science and Engineering ◽

10.4081/bse.2019.97 ◽

2020 ◽

Author(s):

Francesco Nevelli

Keyword(s):

Growth Hormone ◽

Physiological Mechanism ◽

Global Market ◽

Hormone Deficiency ◽

In Vitro Assays ◽

In Vitro Methods ◽

In Vivo Assays ◽

Market Leader

Merck is global market leader in the fertility and growth hormone deficiency treatment. The quality control analytical panels for each new produced batch envisage the potency quantification that is estimated using a dedicated in vivo assay. Indeed, no in vitro methods for gonadotropin potency quantification are available in any pharmacopoeia. Merck Ivrea started a project to replace the in vivo assays with in vitro assays able to mimic the physiological mechanism of action of each gonadotropin and growth hormone.

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In vitro assays used in the evaluation of the quality of stored platelets: Correlation with in vivo assays

Transfusion and Apheresis Science ◽

10.1016/j.transci.2008.06.007 ◽

2008 ◽

Vol 39 (2) ◽

pp. 161-165 ◽

Cited By ~ 11

Author(s):

Stein Holme

Keyword(s):

In Vitro Assays ◽

In Vivo Assays

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Recent Reduction in Thrombogenic Enzyme Content of Prothrombin Complex Concentrates

10.1055/s-0039-1682482 ◽

1977 ◽

Author(s):

H.S. Kingdon

Keyword(s):

Calcium Ions ◽

Calcium Ion ◽

Deae Cellulose ◽

In Vitro Assays ◽

Prothrombin Complex Concentrates ◽

In Vivo Assays ◽

Prolonged Contact ◽

Plasma Fractions

In previous studies of prothrombin complex concentrates, it was demonstrated that there was a high content of potentially thrombogenic enzymes in the products from certain manufacturers, and that the enzyme conteat correlated closely with in vivo assays for thrombogenicity and with the observed incidence of thrombotic episodes following infusion (Thromb. Diath. Haemorrh. 33, 617, 1 975\Subsequently, it was shown that the thrombogenic enzymes could be generated by prolonged contact with DEAE-cellulose or calcium ions during preparation or later handling (Blood, 49, 159, 1977). In view of. these observations, efforts have been made to reduce the contact time of plasma fractions with either DEAE-cellulose or calcium ion during purification of these fractions for therapeutic use. In vitro assays for thrombogenic enzymes using the nonactivated partial thromboplastin time (NAPTT) were recently repeated on some of the currently available therapeutic materials. Assays were standardized and compared with previous results by using a provisional standard provided by Dr. David Aronson, Bureau of Biologies, USFDA. In the 1975 study, one manufacturer was identified as making a concentrate virtually free of thrombogenic enzyme. The concentrate currently being made by this manufacturer still does not significantly shorten the NAPTT. In the 1975 study, 2 manufacturers were shown to be making concentrates with high titers of thrombogenic enzyme. The current products of these two manufacturers contain detectable but significantly lower levels of thrombogenic enzymes. Thus it appears that for these two manufacturers, minor changes in production procedures have led to a product containing less potentially thrombogenic material.

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In vitro assays misrepresent in vivo lineage potentials of murine lymphoid progenitors

Blood ◽

10.1182/blood-2010-05-287102 ◽

2011 ◽

Vol 117 (9) ◽

pp. 2618-2624 ◽

Cited By ~ 44

Author(s):

Lauren I. Richie Ehrlich ◽

Thomas Serwold ◽

Irving L. Weissman

Keyword(s):

T Cell ◽

The Other ◽

In Vitro Assays ◽

In Vivo Assays ◽

Other Hand ◽

Multipotent Progenitors ◽

Lymphoid Progenitors

Abstract The identity of T-cell progenitors that seed the thymus has remained controversial, largely because many studies differ over whether these progenitors retain myeloid potential. Contradictory reports diverge in their use of various in vitro and in vivo assays. To consolidate these discordant findings, we compared the myeloid potential of 2 putative thymus seeding populations, common lymphoid progenitors (CLPs) and multipotent progenitors (MPPs), and the earliest intrathymic progenitor (DN1), using 2 in vitro assays and in vivo readouts. These assays gave contradictory results: CLP and DN1 displayed surprisingly robust myeloid potential on OP9-DL1 in vitro stromal cocultures but displayed little myeloid potential in vivo, as well as in methylcellulose cultures. MPP, on the other hand, displayed robust myeloid potential in all settings. We conclude that stromal cocultures reveal cryptic, but nonphysiologic, myeloid potentials of lymphoid progenitors, providing an explanation for contradictory findings in the field and underscoring the importance of using in vivo assays for the determination of physiologic lineage potentials.

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In vitro and in vivo Antioxidant Properties of Extracts from the Root of Curcuma longa Linn

European Journal of Medicinal Plants ◽

10.9734/ejmp/2020/v31i630241 ◽

2020 ◽

pp. 6-12

Author(s):

Abdulrashid Mohammed ◽

Muhammad Ibrahim Usman ◽

Alhassan Muhammad Wudil ◽

Adamu Jibrin Alhassan ◽

Salisu Maiwada Abubakar ◽

...

Keyword(s):

Antioxidant Activity ◽

Methanol Extract ◽

Radical Scavenging Activity ◽

Curcuma Longa ◽

Radical Scavenging ◽

Diabetic Rats ◽

Scavenging Activity ◽

Liver And Kidney

Many plants possess antioxidants that exhibit additive or synergistic activities. The antioxidant activities of the root of Curcuma longa Linn extracts extracted different solvents were investigated by using several established in vitro systems: α,α-diphenyl-β-picrylhydrazyl (DPPH) radical scavenging activity, hydrogen Peroxide scavenging activity (HPSA), nitric oxide radical scavenging activity (NOSA) and ferric reducing antioxidant power (FRAP). The result showed that methanol extract exhibited greater antioxidant activity in vitro which was statistically significant compared to the other extracts. Based on the in vitro results, the methanol extract was subjected to column chromatography. Six pooled fractions (FI-FVI) were evaluated for in vivo antioxidant activity in liver and kidney of alloxan-induced diabetic rats using a total of forty-five (45) rats which were grouped into nine (9) groups of five (5) rats. The in vivo antioxidants showed a significant decrease in superoxide dismutase (SOD), catalase (CAT) and gluthatione peroxidase (GPx) levels in both liver and kidney of Alloxan-induced diabetic rats. These changes were significantly reversed after treatment with methanol fraction II and the standard drug. Thus, Curcuma longa Linn may be useful in the management of diabetes and oxidative stress.

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