Antischistosomal Activity of S-2-[[2-(2-Thiazolylcarbamoyl) Ethyl] Amino] Ethyl Hydrogen Thiosulfate In vitro and In vivo

1977 ◽  
Vol 63 (6) ◽  
pp. 1053 ◽  
Author(s):  
Ronald E. Voigtman ◽  
Paul E. Thompson
Keyword(s):  
Antischistosomal Activity

scholarly journals Antischistosomal Activities of Mefloquine-Related Arylmethanols

2012 ◽  
Vol 56 (6) ◽  
pp. 3207-3215 ◽  
Author(s):  
Katrin Ingram ◽  
William Ellis ◽  
Jennifer Keiser
Keyword(s):  
Body Weight ◽  
Worm Burden ◽  
Structural Features ◽  
Content Type ◽  
Antischistosomal Activity ◽  
Oral Doses ◽  
Related Compounds ◽  
Insight Into

ABSTRACTInteresting antischistosomal properties have been documented for the antimalarial mefloquine, a 4-quinolinemethanol. We evaluated the antischistosomal activities of nine mefloquine-related compounds belonging to the 4-pyridinemethanols, 9-phenanthrenmethanols, and 4-quinolinemethanols. Eight compounds revealed high activities againstSchistosoma mansoni in vitro, with two drugs (the 4-quinolinemethanols WR7573 and WR7930) characterized by significantly lower half-maximal inhibitory concentrations (IC50s) (2.7 and 3.5 μM, respectively) compared to mefloquine (11.4 μM). Mefloquine and WR7930 showed significantly decreased IC50s when incubated in the presence of hemoglobin. High worm burden reductions (WBR) were obtained with enpiroline (WBR, 82.7%; dosage, 200 mg/kg of body weight) and itsthreoisomers (+)-threo(WBR, 100%) and (−)-threo(WBR, 89%) and with WR7930 (WBR, 87%; dosage, 100 mg/kg) against adultS. mansoniin mice. Furthermore, excellentin vitroandin vivoantischistosomal activity was observed for two WR7930-related structures (WR29252 and WR7524). In addition, mefloquine (WBR, 81%), enpiroline (WBR, 77%), and WR7930 (WBR, 100%) showed high activities againstS. haematobiumharbored in mice following single oral doses of 200 mg/kg. These results provide a deeper insight into the structural features of the arylmethanols that rule antischistosomal activity. Further studies should be launched with enpiroline and WR7930.

The phosphodiesterase-4 inhibitor roflumilast impacts Schistosoma mansoni ovipositing in vitro but displays only modest antischistosomal activity in vivo

2020 ◽  
Vol 208 ◽  
pp. 107793
Author(s):  
Sanaa S. Botros ◽  
Naglaa M. El-Lakkany ◽  
Sayed H. Seif el-Din ◽  
Samia William ◽  
Abdel-Nasser Sabra ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Phosphodiesterase 4 ◽  
Antischistosomal Activity ◽  
Phosphodiesterase 4 Inhibitor

scholarly journals In vitro and in vivo antischistosomal activity of ferroquine derivatives

2014 ◽  
Vol 7 (1) ◽  
pp. 424 ◽  
Author(s):  
Jennifer Keiser ◽  
Mireille Vargas ◽  
Riccardo Rubbiani ◽  
Gilles Gasser ◽  
Christophe Biot
Keyword(s):  
Antischistosomal Activity

Licochalcone A-loaded solid lipid nanoparticles improve antischistosomal activity in vitro and in vivo

Nanomedicine ◽  
2021 ◽  
Author(s):  
Lívia Mara Silva ◽  
Danielle Gomes Marconato ◽  
Marcos Paulo Nascimento da Silva ◽  
Nádia Rezende Barbosa Raposo ◽  
Gabriela de Faria Silva Facchini ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Licochalcone A ◽  
Solid Lipid ◽  
Transmission Electron ◽  
High Shear Homogenization ◽  
Antischistosomal Activity

Aim: To isolate licochalcone A (LicoA) from licorice, prepare LicoA-loaded solid lipid nanoparticles (L-SLNs) and evaluate the L-SLNs in vitro and in vivo against Schistosoma mansoni. Materials & methods: LicoA was obtained by chromatographic fractionation and encapsulated in SLNs by a modified high shear homogenization method. Results: L-SLNs showed high encapsulation efficiency, with satisfactory particle size, polydispersity index and Zeta potential. Transmission electron microscopy revealed that L-SLNs were rounded and homogenously distributed. Toxicity studies revealed that SLNs decreased the hemolytic and cytotoxic properties of LicoA. Treatment with L-SLNs showed in vivo efficacy against S. mansoni. Conclusion: L-SLNs are efficient in reducing worm burden and SLNs may be a promising delivery system for LicoA to treat S. mansoni infections.

scholarly journals Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity

2019 ◽  
Vol 9 ◽  
pp. 35-43 ◽  
Author(s):  
Sanaa S. Botros ◽  
Samia William ◽  
Abdel-Nasser A. Sabra ◽  
Naglaa M. El-Lakkany ◽  
Sayed H. Seif el-Din ◽  
...  
Keyword(s):  
Antischistosomal Activity

scholarly journals Antischistosomal Activity of Zingiber officinale, Piper nigrum, and Coriandrum sativum Aqueous Plant Extracts on Hamster Infected with Schistosoma mansoni

2021 ◽  
Vol 2021 ◽  
pp. 1-21
Author(s):  
Mohamed F. Abou El-Nour ◽  
Yousef Fadladdin
Keyword(s):  
Schistosoma Mansoni ◽  
Zingiber Officinale ◽  
Coriandrum Sativum ◽  
World Health ◽  
Piper Nigrum ◽  
The World ◽  
Antischistosomal Activity ◽  
Health Organization

Schistosomiasis continues to affect the health and quality of life of millions of people around the world. Schistosomiasis has been ranked the second disease after malaria in terms of importance as a targeted tropical disease. Praziquantel (PZQ) is the only drug approved by the World Health Organization (WHO) for the treatment of schistosomiasis. Being the only drug, parasite resistance to this drug has developed. Therefore, the search for new alternatives has been the goal of many researchers. In this study, the effects of aqueous extracts of Zingiber officinale, Piper nigrum, and Coriandrum sativum on Schistosoma mansoni infected golden hamsters (Egyptian strain) were evaluated in vitro and in vivo at different doses of 500, 250, 125, 62.5, and 31.25 μg/ml. In vitro, adult worms of S. mansoni were tested in RPMI-1640 medium for 48 hrs. The results showed that the concentrations 500, 250, and 125 μg/ml of Zingiber officinale and Piper nigrum caused dead of 100% of adult worms within 6 and 12 hrs of incubation, respectively. Although, aqueous extract of Coriandrum sativum at concentrations 500, 250, and 125 μg/ml resulted dead of 100% parasites after 12 to 24 hrs of incubation. In conclusion, Zingiber officinale and Piper nigrum showed efficacy against schistosomiasis in both in vitro and biological experiments of Egyptian schistosome strain, while Coriandrum sativum gave less effective results than the previous ones. Therefore, Zingiber officinale and Piper nigrum may become an innovative treatment for schistosomiasis.

scholarly journals In Vitro Metabolic Profile and in Vivo Antischistosomal Activity Studies of (η6-Praziquantel)Cr(CO)3 Derivatives

2013 ◽  
Vol 56 (22) ◽  
pp. 9192-9198 ◽  
Author(s):  
Malay Patra ◽  
Katrin Ingram ◽  
Anna Leonidova ◽  
Vanessa Pierroz ◽  
Stefano Ferrari ◽  
...  
Keyword(s):  
Metabolic Profile ◽  
Antischistosomal Activity

Induction and Differentiation of Dental Epithelium in Vivo and in Vitro

1982 ◽  
Vol 40 ◽  
pp. 142-145
Author(s):  
E. J. Kollar
Keyword(s):  
Connective Tissue ◽  
Oral Mucosa ◽  
Basal Lamina ◽  
Functional Derivatives ◽  
Specific Source ◽  
Dental Epithelium ◽  
Connective Tissue Stroma

The differentiation and maintenance of many specialized epithelial structures are dependent on the underlying connective tissue stroma and on an intact basal lamina. These requirements are especially stringent in the development and maintenance of the skin and oral mucosa. The keratinization patterns of thin or thick cornified layers as well as the appearance of specialized functional derivatives such as hair and teeth can be correlated with the specific source of stroma which supports these differentiated expressions.

Ultrastructural Correlations between Clonal Human Tumor Colonies and in Vivo Neoplasms

1982 ◽  
Vol 40 ◽  
pp. 210-211
Author(s):  
M.J. Murphy ◽  
R.R. Price ◽  
J.C. Sloman
Keyword(s):  
Cultured Cells ◽  
Human Tumor ◽  
Cell Type ◽  
Tumor Mass ◽  
Initial Cell ◽  
Cloning Assay ◽  
Human Tumor Cloning ◽  
The Relationship

The in vitro human tumor cloning assay originally described by Salmon and Hamburger has been applied recently to the investigation of differential anti-tumor drug sensitivities over a broad range of human neoplasms. A major problem in the acceptance of this technique has been the question of the relationship between the cultured cells and the original patient tumor, i.e., whether the colonies that develop derive from the neoplasm or from some other cell type within the initial cell population. A study of the ultrastructural morphology of the cultured cells vs. patient tumor has therefore been undertaken to resolve this question. Direct correlation was assured by division of a common tumor mass at surgical resection, one biopsy being fixed for TEM studies, the second being rapidly transported to the laboratory for culture.

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