Synthesis, characterization, and pharmacological evaluation of thiourea derivatives

AbstractThioureas and their derivatives are organosulfur compounds having applications in numerous fields such as organic synthesis and pharmaceutical industries. Symmetric thiourea derivatives were synthesized by the reaction of various anilines with CS2. The synthesized compounds were characterized using the UV-visible and nuclear magnetic resonance (NMR) spectroscopic techniques. The compounds were screened for in vitro inhibition of α-amylase, α-glucosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE) enzymes and for their antibacterial and antioxidant potentials. These compounds were fed to Swiss male albino mice to evaluate their toxicological effects and potential to inhibit glucose-6-phosphatase (G6Pase) inhibition. The antibacterial studies revealed that compound 4 was more active against the selected bacterial strains. Compound 1 was more active against 2,2-diphenyl-1-picrylhydrazyl and 2,2’-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals, AChE, BuChE, and α-glucosidase. Compound 2 was more potent against α-amylase and G6Pase. Toxicity studies showed that compound 4 is safe as it exerted no toxic effect on any of the hematological and biochemical parameters or on liver histology of the experimental animals at any studied dose rate. The synthesized compounds showed promising antibacterial and antioxidant potential and were very active (both in vitro and in vivo) against G6Pase and moderately active against the other selected enzymes used in this study.

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In Vitro and In Vivo Anti-Inflammatory Effects of Sulfated Polysaccharides Isolated from the Edible Brown Seaweed, Sargassum fulvellum

Marine Drugs ◽

10.3390/md19050277 ◽

2021 ◽

Vol 19 (5) ◽

pp. 277

Author(s):

Lei Wang ◽

Hye-Won Yang ◽

Ginnae Ahn ◽

Xiaoting Fu ◽

Jiachao Xu ◽

...

Keyword(s):

Nitric Oxide ◽

Brown Seaweed ◽

Sulfated Polysaccharides ◽

Raw 264.7 ◽

Raw 264.7 Macrophages ◽

Sargassum Fulvellum ◽

Pharmaceutical Industries ◽

Anti Inflammatory

In the present study, the in vitro and in vivo anti-inflammatory effects of the sulfated polysaccharides isolated from Sargassum fulvellum (SFPS) were evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and zebrafish. The results indicated that SFPS improved the viability of LPS-stimulated RAW 264.7 macrophages from 80.02 to 86.80, 90.09, and 94.62% at the concentration of 25, 50, and 100 µg/mL, respectively. Also, SFPS remarkably and concentration-dependently decreased the production levels of inflammatory molecules including nitric oxide (NO), tumor necrosis factor-alpha, prostaglandin E2, interleukin-1 beta, and interleukin-6 in LPS-treated RAW 264.7 macrophages. In addition, SFPS significantly inhibited the expression levels of cyclooxygenase-2 and inducible nitric oxide synthase in LPS-treated RAW 264.7 macrophages. Furthermore, the in vivo test results indicated that SFPS improved the survival rate of LPS-treated zebrafish from 53.33 to 56.67, 60.00, and 70.00% at the concentration of 25, 50, and 100 µg/mL, respectively. In addition, SFPS effectively reduced cell death, reactive oxygen species, and NO levels in LPS-stimulated zebrafish. Taken together, these results suggested that SFPS possesses strong in vitro and in vivo anti-inflammatory activities, and could be used as an ingredient to develop anti-inflammatory agents in the functional food and pharmaceutical industries.

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Safety Evaluation of Multiple Strains ofLactobacillus plantarumandPediococcus pentosaceusin Wistar Rats Based on the Ames Test and a 28-Day Feeding Study

The Scientific World JOURNAL ◽

10.1155/2014/928652 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 4

Author(s):

Cheng-Chih Tsai ◽

Sew-Fen Leu ◽

Quan-Rong Huang ◽

Lan-Chun Chou ◽

Chun-Chih Huang

Keyword(s):

Wistar Rats ◽

Clinical Chemistry ◽

Toxicity Study ◽

Bacterial Strains ◽

Oral Toxicity ◽

Short Term ◽

Mutagenic Potential ◽

Multiple Strains

Three lactic acid bacterial strains,Lactobacillus plantarum, HK006, and HK109, andPediococcus pentosaceusPP31 exhibit probiotic potential as antiallergy agents, both in vitro and in vivo. However, the safety of these new strains requires evaluation when isolated from infant faeces or pickled cabbage. Multiple strains (HK006, HK109, and PP31) were subject to a bacterial reverse mutation assay and a short-term oral toxicity study. The powder product exhibited mutagenic potential inSalmonellaTyphimurium strains TA98 and TA1535 (with or without metabolic activation). In the short-term oral toxicity study, rats received a normal dosage of 390 mg/kg/d (approximately9×109 CFU/kg/d) or a high dosage of 1950 mg/kg/d (approximately4.5×1010 CFU/kg/d) for 28 d. No adverse effects were observed regarding the general condition, behaviour, growth, feed and water consumption, haematology, clinical chemistry indices, organ weights, or histopathologic analysis of the rats. These studies have demonstrated that the consumption of multiple bacterial strains is not associated with any signs of mutagenicity ofS.Typhimurium or toxicity in Wistar rats, even after consuming large quantities of bacteria.

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In vitro and in vivo screening of antagonistic bacterial strains from vineyards to controlBotrytis cinereain grapevine tissues

Acta Horticulturae ◽

10.17660/actahortic.2016.1144.12 ◽

2016 ◽

pp. 85-92 ◽

Cited By ~ 1

Author(s):

R. Haidar ◽

C. Calvo-Garrido ◽

J. Roudet ◽

T. Gautier ◽

A. Deschamps ◽

...

Keyword(s):

Bacterial Strains ◽

In Vivo Screening

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Solvolysis of the Tumor-Inhibiting Ru(III)-Complex trans-Tetrachlorobis(Indazole)Ruthenate(III)

Metal-Based Drugs ◽

10.1155/mbd.2000.225 ◽

2000 ◽

Vol 7 (4) ◽

pp. 225-232 ◽

Cited By ~ 19

Author(s):

Thomas Pieper ◽

Wolfgang Peti ◽

Bernhard K. Keppler

Keyword(s):

Sodium Salt ◽

Buffer System ◽

Spectroscopic Techniques ◽

Tumor Models ◽

Solubility In Water ◽

Aqueous Acetonitrile ◽

Hydrolysis Of

The ruthenium(III) complex Hlnd trans-[RuCl4,(ind)2], with two trans-standing indazole (ind) ligands bound to ruthenium via nitrogen, shows remarkable activity in different tumor models in vitro and in vivo. The solvolysis of the complex trans-[RuCl4,(ind)2]- has been investigated by means of spectroscopic techniques (UV/vis, NMR)in different solvents. We investigated the indazolium as well as the sodium salt, the latter showing improved solubility in water. In aqueous acetonitrile and ethanol the solvolysis results in one main solvento complex. The hydrolysis of the complex is more complicated and depends on the pH of the solution as well as on the buffer system.

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In vitro and in vivo antimicrobial activity of Ulva lactuca Linn. (Green algae) associated endophytic bacterial Strains

Journal of Applied Pharmaceutical Science ◽

10.7324/japs.2016.601019 ◽

2016 ◽

pp. 138-146 ◽

Cited By ~ 2

Author(s):

Prasanna Habbu ◽

Vijayanand Warad ◽

Rajesh Shastri ◽

Chetan Savant ◽

Smita Madagundi ◽

...

Keyword(s):

Antimicrobial Activity ◽

Green Algae ◽

Ulva Lactuca ◽

Bacterial Strains

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Solubility and ADMET profiles of short oligomers of lactic acid

ADMET & DMPK ◽

10.5599/admet.843 ◽

2020 ◽

Cited By ~ 1

Author(s):

Daniela Dascălu ◽

Diana Larisa Roman ◽

Madalina Filip ◽

Alecu Aurel Ciorsac ◽

Vasile Ostafe ◽

...

Keyword(s):

Molecular Weight ◽

Glucocorticoid Receptors ◽

Degradation Products ◽

Organic Anion ◽

Toxicity Tests ◽

Medical Applications ◽

Eye Injuries ◽

Toxicological Effects

Polylactic acid (PLA) is a polymer with an increased potential to be used in different medical applications, including tissue engineering and drug-carries. The use of PLA in medical applications implies the evaluation of the human organism's response to the polymer inserting and to its degradation products. Consequently, within this study, we have investigated the solubility and ADMET profiles of the short oligomers (having the molecular weight lower than 3000 Da) resulting in degradation products of PLA. There is a linear decrease of the molar solubility of investigated oligomers with molecular weight. The results that are obtained also reveal that short oligomers of PLA have promising pharmacological profiles and limited toxicological effects on humans. These oligomers are predicted as potential inhibitors of the organic anion transporting peptides OATP1B1 and OATP1B3, they present minor probability to affect the androgen and glucocorticoid receptors, have a weak potential of hepatotoxicity, and may produce eye injuries. These outcomes may be used to guide or to supplement in vitro and/or in vivo toxicity tests such as to enhance the biodegradation properties of the biopolymer.

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An In-Silico Study on Selected Organosulfur Compounds as Potential Drugs for SARS-CoV-2 Infection via Binding Multiple Drug Targets

10.26434/chemrxiv.12505343 ◽

2020 ◽

Author(s):

Liya Thurakkal ◽

Satyam Singh ◽

Sushabhan Sadhukhan ◽

Mintu Porel

Keyword(s):

Drug Targets ◽

Target Prediction ◽

Multiple Drug ◽

Organosulfur Compounds ◽

Potential Candidate ◽

Health Crisis ◽

Drug Molecules ◽

Main Protease

The emerging paradigm shift from ‘one molecule, one target, for one disease’ towards ‘multi-targeted small molecules’ has paved an ingenious pathway in drug discovery in recent years. This idea has been extracted for the investigation of competent drug molecules for the unprecedented COVID-19 pandemic which became the greatest global health crisis now. Perceiving the importance of organosulfur compounds against SARS-CoV-2 from the drugs under clinical trials, a class of organosulfur compounds effective against SARS-CoV were selected and studied the interaction with multiple proteins of the SARS-CoV-2. One compound displayed inhibition against five proteins (both structural and non-structural) of the virus namely, main protease, papain-like protease, spike protein, helicase and RNA dependent RNA polymerase. Consequently, this compound emanates as a potential candidate for treating the virulent disease. The pharmacokinetics, ADMET properties and target prediction studies carried out in this work further inflamed the versatility of the compound and urge to execute in-vitro and in-vivo analysis on SARS-CoV-2 in the future.

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IN VITRO ANTIOXIDANT AND IN VIVO ANTIDIABETIC ACTIVITY OF TWO POTENTIAL PROBIOTIC ENTEROCOCCUS SPP. ON ALLOXAN-INDUCED DIABETIC RATS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2021.v14i3.40321 ◽

2021 ◽

pp. 94-98

Author(s):

KAMNI RAJPUT ◽

RAMESH CHANDRA DUBEY

Keyword(s):

Diabetic Rats ◽

Antidiabetic Activity ◽

Control Group ◽

Albino Rats ◽

Bacterial Cells ◽

Bacterial Strains ◽

Animal Group ◽

Enterococcus Spp

Objective: In vitro antioxidant activity, in vivo antidiabetic property and intestinal attachment by two potential probiotic bacterial strains, namely, Enterococcus faecium and Enterococcus hirae were studied using albino rats. Methods: Antioxidant the activity was assessed using 2,2-Diphenyl-1-picrylhydrazyl radicals scavenging assay. Alloxan was administered intraperitoneally to induce diabetic conditions in experimental rats. Animals were treated with oral administration of Enterococcus spp., such as E. faecium, and E. hirae isolated from goat and sheep milk. The control animal group received normal saline for the same days. Glibenclamide drug was used as a positive control against probiotic bacterial cells. Results: However, administration of probiotic bacterial strains E. faecium and E. hirae, in albino rats significantly (p<0.05) at varying doses lowered blood glucose levels in diabetic rats as compared to the diabetic control group. Both the species of Enterococcus increased the bodyweight of experimental rats. However, E. faecium was the best antidiabetic strain having the antioxidant activities also in comparison to E. hirae. The attachment of probiotic bacterial cells E. faecium on the rat’s intestine wall against pathogens was examined. Furthermore, E. faecium showed its aggregation with pathogens by attachment of the intestines of albino rats. This showed that both the bacterial strains exhibited in vivo antidiabetic effect. Conclusion: The results of this study showed that probiotic bacteria possess antioxidant, antidiabetic activities, and attachment of intestine.

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Supplementation of Superfine Powder Prepared fromChaenomeles speciosaFruit Increases Endurance Capacity in Rats via Antioxidant and Nrf2/ARE Signaling Pathway

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2014/976438 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 6

Author(s):

Ka Chen ◽

Jia You ◽

Yong Tang ◽

Yong Zhou ◽

Peng Liu ◽

...

Keyword(s):

Antioxidant Activity ◽

Ascorbic Acid ◽

Antioxidant Enzymes ◽

Raw Material ◽

Endurance Capacity ◽

Swimming Time ◽

Pharmaceutical Industries ◽

Herb Medicine

Chaenomeles speciosafruit is a traditional herb medicine widely used in China. In this study, superfine powder ofC. speciosafruit (SCE), ground by supersonic nitrogen airflow at −140°C, was investigated to assess itsin vitroantioxidant activity andin vivoantiphysical fatigue activity. SCE was homogenous(d<10 μm)and rich in antioxidants like polyphenols, saponins, oleanolic acid, ursolic acid, ascorbic acid, and SOD. According to thein vitroexperiments, SCE displayed promising antioxidant activity with powerful FARP, SC-DPPH, and SC-SAR activities. According to thein vivoexperiments, rats supplemented with SCE had prolonged exhaustive swimming time (57%) compared to the nonsupplemented rats. Meanwhile, compared to the nonsupplemented rats, the SCE-supplemented rats had higher levels of blood glucose and liver and muscular glycogen and lower levels of LA and BUN. Lower MDA, higher antioxidant enzymes (SOD, CAT, and GSH-Px) activities, and upregulated Nrf2/ARE mediated antioxidant enzymes (HO-1, Trx, GCLM, and GCLC) expression were also detected in the supplemented group. This study indicates that SCE is a potent antioxidant and antifatigue agent, and SCE could be a promising raw material for the food and pharmaceutical industries.

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Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

Journal of Nanomaterials ◽

10.1155/2017/4362046 ◽

2017 ◽

Vol 2017 ◽

pp. 1-11 ◽

Cited By ~ 7

Author(s):

Susana Suely Rodrigues Milhomem-Paixão ◽

Maria Luiza Fascineli ◽

Luis Alexandre Muehlmann ◽

Karina Motta Melo ◽

Hugo Leonardo Crisóstomo Salgado ◽

...

Keyword(s):

Room Temperature ◽

Future Application ◽

Hydrodynamic Diameter ◽

Therapeutic Application ◽

Mtt Test ◽

Carapa Guianensis ◽

Toxicological Effects ◽

Nih 3T3

Andiroba oil (AO) is obtained from an Amazonian plant and is used in traditional medicine. We carried out a comparative study to test the cytotoxicity, genotoxicity, and hematotoxicity of the oil and its nanoemulsion (AN) in vitro (fibroblasts, lineage NIH/3T3) and in vivo (Swiss mice). The AN was characterized by DLS/Zeta, and its stability was investigated for 120 days. The biological activity of AN was assessed in vitro by MTT test and cell morphology analyses and in vivo by micronucleus, comet, and hematotoxicity tests. The AN presented a hydrodynamic diameter (Hd) of 142.5±3.0 and PDI of 0.272±0.007 and good stability at room temperature. The MTT test evidenced the cytotoxicity of AO and of AN only at their highest concentrations, but AN showed lower cytotoxicity than AO. A lower cytotoxicity of AN, when compared to AO, is in fact an interesting data suggesting that during therapeutic application there will be a lower impact in the cell viability of healthy cells. Cytotoxicity, genotoxicity, and hematotoxicity were not observed in vivo. These tests on the biological and toxicological effects of andiroba oil and nanostructured oil are still initial ones but will give a direction to future application in cosmetics and/or the development of new phytotherapics.

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