scholarly journals Chemical Investigation of the Indonesian Tunicate Polycarpa aurata and Evaluation of the Effects Against Schistosoma mansoni of the Novel Alkaloids Polyaurines A and B

Marine Drugs ◽  
2019 ◽  
Vol 17 (5) ◽  
pp. 278 ◽  
Author(s):  
Marcello Casertano ◽  
Concetta Imperatore ◽  
Paolo Luciano ◽  
Anna Aiello ◽  
Masteria Yunovilsa Putra ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Schistosoma Mansoni ◽  
Mammalian Cells ◽  
Egg Production ◽  
2D Nmr ◽  
Chemical Investigation ◽  
Computational Studies ◽  
The Novel ◽  
Thiadiazole Ring

A deep study of the metabolic content of the tunicate Polycarpa aurata, collected from Indonesian coast, afforded the isolation of two novel alkaloids, polyaurines A (1) and B (2), along with two new p-substituted benzoyl derivatives (3 and 4) and four known compounds (5–8). The structural elucidation of the new secondary metabolites was assigned by 1D, 2D NMR, and HRESIMS techniques. Computational studies resulted a useful tool to unambiguously determine in polyaurine B the presence of rarely found 1,2,4-thiadiazole ring. The effects of polyaurines A and B on mammalian cells growth and on the viability of different blood-dwelling Schistosoma mansoni (phylum: Platyhelminthes) stages, as well as egg production, were evaluated. Both compounds resulted not cytotoxic; interestingly some of the eggs produced by polyaurine A-treated adult pairs in vitro are smaller, deformed, and/or fragmented; therefore, polyaurine A could represent an interesting bioactive natural molecule to be further investigated.

scholarly journals High-resolution AP-SMALDI MSI as a tool for drug imaging in Schistosoma mansoni

2021 ◽  
Author(s):  
Annika S. Mokosch ◽  
Stefanie Gerbig ◽  
Christoph G. Grevelding ◽  
Simone Haeberlein ◽  
Bernhard Spengler
Keyword(s):  
Schistosoma Mansoni ◽  
Egg Production ◽  
Drug Repurposing ◽  
Cancer Drug ◽  
Ionization Mass ◽  
Parasitic Flatworm ◽  
Paired Female ◽  
First Time ◽  
Organ Tropism

AbstractSchistosoma mansoni is a parasitic flatworm causing schistosomiasis, an infectious disease affecting several hundred million people worldwide. Schistosomes live dioeciously, and upon pairing with the male, the female starts massive egg production, which causes pathology. Praziquantel (PZQ) is the only drug used, but it has an inherent risk of resistance development. Therefore, alternatives are needed. In the context of drug repurposing, the cancer drug imatinib was tested, showing high efficacy against S. mansoni in vitro. Besides the gonads, imatinib mainly affected the integrity of the intestine in males and females. In this study, we investigated the potential uptake and distribution of imatinib in adult schistosomes including its distribution kinetics. To this end, we applied for the first time atmospheric-pressure scanning microprobe matrix-assisted laser desorption/ionization mass spectrometry imaging (AP-SMALDI MSI) for drug imaging in paired S. mansoni. Our results indicate that imatinib was present in the esophagus and intestine of the male as early as 20 min after in vitro exposure, suggesting an oral uptake route. After one hour, the drug was also found inside the paired female. The detection of the main metabolite, N-desmethyl imatinib, indicated metabolization of the drug. Additionally, a marker signal for the female ovary was successfully applied to facilitate further conclusions regarding organ tropism of imatinib. Our results demonstrate that AP-SMALDI MSI is a useful method to study the uptake, tissue distribution, and metabolization of imatinib in S. mansoni. The results suggest using AP-SMALDI MSI also for investigating other antiparasitic compounds and their metabolites in schistosomes and other parasites. Graphical abstract

scholarly journals In vitro effects of artesunate on the survival of worm pairs and egg production of Schistosoma mansoni

2009 ◽  
Vol 83 (1) ◽  
pp. 7-11 ◽  
Author(s):  
Y. Mitsui ◽  
M. Miura ◽  
Y. Aoki
Keyword(s):  
Schistosoma Mansoni ◽  
Adult Worm ◽  
Survival Time ◽  
Egg Production ◽  
Inhibitory Effect ◽  
Male And Female ◽  
Paired Male ◽  
In Vitro Effects ◽  
Paired Female

AbstractThe effect of artesunate (ART) on the survival time of adult worm pairs of Schistosoma mansoni and on their egg output during in vitro culture was assessed. ART significantly decreased the survival time of both paired male and female worms at concentrations of 5, 10, 20 and 40 mg l− 1 during in vitro cultivation. An inhibitory effect of ART on the daily egg output of paired female worms during in vitro cultivation was also observed.

scholarly journals Oviposition by Schistosoma mansoni during in vitro cultivation

1996 ◽  
Vol 38 (6) ◽  
pp. 423-426 ◽  
Author(s):  
Leo Roberto Barth ◽  
Ana Paula Morais Fernandes ◽  
Vanderlei Rodrigues
Keyword(s):  
Schistosoma Mansoni ◽  
Egg Production ◽  
Culture Medium ◽  
Parasite Development ◽  
In Vitro Cultivation ◽  
Progressive Reduction ◽  
Maximum Period ◽  
Medium Time ◽  
Kinetics Of

Observation of Schistosoma mansoni oviposition during in vitro culture of adult worms for a maximum period of 10 days showed three well distinct phases in the kinetics of oviposition: an initial phase with low egg production, a period of maximum oviposition and finally a progressive reduction in the number of eggs during the late phases of culture. The kinetics of oviposition and the number of eggs laid by the parasites are influenced by the number of worm pairs per amount of RPMI 1640 medium, time of parasite development in the vertebrate host and type of serum utilized in the culture medium.

scholarly journals Therapeutic Effect of Diminazene Aceturate on Parasitic Blood Fluke Schistosoma mansoni Infection

2020 ◽  
Vol 64 (11) ◽  
Author(s):  
Mariana G. de Brito ◽  
Ana C. Mengarda ◽  
George L. Oliveira ◽  
Maria E. Cirino ◽  
Tais C. Silva ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Chronic Infection ◽  
Worm Burden ◽  
Egg Production ◽  
Laser Scanning Microscopy ◽  
Early Infection ◽  
Blood Fluke ◽  
Serum Aminotransferase ◽  
Content Type

ABSTRACT Praziquantel is currently the only drug available to treat schistosomiasis, a disease of enormous public health significance caused by a blood fluke of the genus Schistosoma. Diminazene, a drug approved by the FDA, has been successfully used to treat diseases caused by blood protozoan parasites. In this study, we evaluated the antiparasitic properties of diminazene against Schistosoma mansoni ex vivo and in mice harboring either chronic or early S. mansoni infections. In vitro, we monitored phenotypic and tegumental changes as well as the effects of the drug on pairing and egg production. In mice infected with either adult (chronic infection) or immature (early infection) worms, diminazene was administered intraperitoneally (10 to 100 mg/kg of body weight) or by oral gavage (100 to 400 mg/kg), and we studied the influence of the drug on worm burden and egg production. Liver and spleen pathologies and serum aminotransferase levels were also analyzed. In vitro, 50% effective concentrations (EC50) and EC90 revealed that diminazene is able to kill both immature and adult parasites, and its effect was time and concentration dependent. In addition, confocal laser scanning microscopy showed morphological alterations in the teguments of schistosomes. In an animal model, the influence of the drug on worm burden, egg production, hepatomegaly, and splenomegaly depended on the dosing regimen applied and the route of administration. Diminazene also caused a significant reduction in aminotransferase levels. Comparatively, diminazene treatment was more effective in chronic infection than in early infection. In tandem, our study revealed that diminazene possesses anthelmintic properties and inhibits liver injury caused by Schistosoma eggs.

scholarly journals Characterization of the cGMP-dependent protein kinase SmcGK1 of Schistosoma mansoni

2011 ◽  
Vol 83 (2) ◽  
pp. 637-648 ◽  
Author(s):  
Silke Leutner ◽  
Svenja Beckmann ◽  
Christoph G Grevelding
Keyword(s):  
Schistosoma Mansoni ◽  
Egg Production ◽  
Specific Inhibitor ◽  
Slow Motion ◽  
Molecular Evidence ◽  
Transcriptional Level ◽  
Data Set ◽  
Preferential Expression ◽  
Dependent Protein

Schistosomes are trematode parasites and of worldwide medical importance for humans and animals. Growth and development of these parasites require a specific host environment, but also permanent communication processes between the two genders. Accumulating molecular evidence indicates that the responsible interactions are mediated by signal transduction processes. Conserved signaling molecules were identified, and first approaches made for their characterization. However, no representative of the conserved family of cGMP-dependent protein kinases (cGKs) has been described in this parasite yet. Within the Schistosoma mansoni genome data-set we identified cGK homologs, of which one was investigated in more detail in this study. We present the cloning of SmcGK1, whose sequence shows homology to cGKs of higher eukaryotes. SmcGK1 was found to be gender-independently transcribed in adult schistosomes. The occurrence of SmcGK1 sense and antisense transcripts suggests that the expression of this gene is controlled at the post-transcriptional level. In situ hybridization experiments demonstrated a gonad-preferential expression profile in both genders indicating a role of SmcGK1, at least during sexual development of schistosomes. Using a cGK-specific inhibitor to treat adult schistosomes in vitro finally resulted in a multifaceted phenotype including slow motion, oocyte congestion, and reduced egg production.

Aerobic and Anaerobic Carbohydrate Metabolism and Egg Production of Schistosoma mansoni In vitro

1975 ◽  
Vol 61 (3) ◽  
pp. 385 ◽  
Author(s):  
Everett L. Schiller ◽  
Ernest Bueding ◽  
Virginia M. Turner ◽  
Jean Fisher
Keyword(s):  
Schistosoma Mansoni ◽  
Carbohydrate Metabolism ◽  
Egg Production ◽  
Aerobic And Anaerobic

scholarly journals Isolation, Characterization and Antiproliferative Activity of Secondary Metabolites from Tanacetum alyssifolium (Bornm.) Grierson

2020 ◽  
Vol 15 (2) ◽  
pp. 122-129
Author(s):  
Ekrem Köksal ◽  
Yakup Ulutaş ◽  
Samed Şimşek ◽  
aha Bayraktar ◽  
Ahmet Altay ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Cell Line ◽  
Sesquiterpene Lactones ◽  
2D Nmr ◽  
Xtt Assay ◽  
Acetophenone Derivatives ◽  
Nmr Techniques ◽  
Cytotoxic Molecules ◽  
Mcf 7

Secondary metabolites of Tanacetum alyssifolium (Bornm.) Grierson (Asteraceae) were investigated for the first time. Thirteen compounds including axillarin (1), Luteolin-7-O-β-glucoside (8) and rutin (13) as flavonoids, fraxetin (7), isofraxidin (9), isofraxidin-7-O-glucoside (11) and fraxidin (12) as coumarins, tatridin A (2), altissin (3), tamirin (4) and tanachin (5) as sesquiterpene lactones and 2,4-dihydroxy-6-methoxy acetophenone (6) and picein (10) as acetophenone derivatives were isolated from the methanol extract of the species. The structures of all isolated compounds were elucidated by 1D and 2D-NMR techniques and by comparing with the literature data. In addition, in vitro cytotoxic activity of all isolated compounds was evaluated against breast cancer MCF-7 cell line by XTT assay. Sesquiterpene lactones; tatridin A (2), tamirin (4) and tanachin (5) were found to be the most cytotoxic molecules against MCF-7 cell line.

Secondary Metabolites from the Barks of Eucommia ulmoides and Their Bioactivities

2019 ◽  
Vol 41 (1) ◽  
pp. 169-169
Author(s):  
Wen Yan Liu Wen Yan Liu ◽  
Zi Ling Zi Ling ◽  
Dong Dong ◽  
Ke Huan Li Ke Huan Li ◽  
Jian Hua Shao Jian Hua Shao ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Antioxidant Activities ◽  
Ethanol Extract ◽  
2D Nmr ◽  
Eucommia Ulmoides ◽  
Antioxidant Power ◽  
Ic50 Values ◽  
Ferric Reducing Antioxidant Power ◽  
Intense Activity

Eucommia ulmoides Oliv., exhibiting diverse bioactivities including antimicrobial, antioxidant, neuroprotective, anti-tumor and anti-inflammatory properties, has long been known as an active ingredient commonly used in antihypertensive herbal prescriptions in China. The 95% ethanol extract of the barks of E. ulmoides showed antimicrobial and antioxidant activities and then was isolated by bioactivity-guided fractionation to obtain a new cinnamyl glucoside, 1-O-trans-cinnamoyl-β-D-apiofuranosyl-(1→6)-β-D-glucopyranose (1), together with twenty known secondary metabolites (2–21). And their structures were identified by extensive spectroscopic analyses, including 1D and 2D NMR, UV, IR and HRESIMS, and chemical methods. All secondary metabolites were evaluated for their antimicrobial and antioxidant activities in vitro. Compounds 7, 8, 11, and 21 exhibited moderately antimicrobial activity. In the antioxidant activity assay, compounds 3, 7, 11, and 14 showed intense activity in ferric reducing antioxidant power (FRAP) with the values of 9.82 mmol/g, 19.25 mmol/g, 14.52 mmol/g, and 12.58 mmol/g in comparison to Trolox (9.02 mmol/g). And compounds 2, 11, and 14–16 showed more potent activity with IC50 values ranging from 18.34 to 24.36 M than Trolox (26.35 M) in ABTS+• scavenging assay.

scholarly journals Discovery of a Novel Diterpene in Brown Propolis from the State of Parana, Brazil

2016 ◽  
Vol 11 (2) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Shigemi Tazawa ◽  
Yasuko Arai ◽  
Sho Hotta ◽  
Taichi Mitsui ◽  
Hiroshi Nozaki ◽  
...  
Keyword(s):  
Human Cancer ◽  
2D Nmr ◽  
The State ◽  
The Novel ◽  
Human Cancer Cell Lines ◽  
Spectroscopic Analyses ◽  
Potent Inhibition ◽  
Plant Sources ◽  
Mcf 7

Propolis is a resinous substance collected by honeybees from certain plant sources. The components of propolis depend on the vegetation of the area in which apiculture is practiced. In Brazil, there are several types of propolis including ‘green,’ ‘red’ and ‘brown'. Brazilian brown propolis from the state of Parana characteristically includes diterpenes, and we discovered a novel clerodane diterpene, rel-(5 S,6 S,8 R,9 R,10 S,18 R,19 S)-18,19-epoxy-2-oxocleroda-3,12( E),14-triene-6,18,19-triol 18,19-diacetate 6-benzoate (3) and five known diterpenes (1, 2, 4, 5 and 6). The chemical structure of the novel diterpene 3 was determined using 1D- and 2D-NMR spectroscopic analyses. Furthermore, the activities of the isolated diterpenes on growth inhibition of several human cancer cell lines (LNCaP, MCF-7, DLD-1 and A549) were evaluated in vitro; diterpene 3 exhibited a potent inhibition of cell growth, and its activity was approximately 15 times higher than that of the other diterpenes.

scholarly journals Tyrosine Phosphorylation Modulates Peroxiredoxin-2 Activity in Normal and Diseased Red Cells

Antioxidants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 206
Author(s):  
Alessandro Mattè ◽  
Enrica Federti ◽  
Elena Tibaldi ◽  
Maria Luisa Di Paolo ◽  
Giovanni Bisello ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Functional Characterization ◽  
Bioinformatic Analysis ◽  
Red Cells ◽  
Red Cell ◽  
The Novel ◽  
Peroxiredoxin 2 ◽  
Globally Distributed

Peroxiredoxin-2 (Prx2) is the third most abundant cytoplasmic protein in red blood cells. Prx2 belongs to a well-known family of antioxidants, the peroxiredoxins (Prxs), that are widely expressed in mammalian cells. Prx2 is a typical, homodimeric, 2-Cys Prx that uses two cysteine residues to accomplish the task of detoxifying a vast range of organic peroxides, H2O2, and peroxynitrite. Although progress has been made on functional characterization of Prx2, much still remains to be investigated on Prx2 post-translational changes. Here, we first show that Prx2 is Tyrosine (Tyr) phosphorylated by Syk in red cells exposed to oxidation induced by diamide. We identified Tyr-193 in both recombinant Prx2 and native Prx2 from red cells as a specific target of Syk. Bioinformatic analysis suggests that phosphorylation of Tyr-193 allows Prx2 conformational change that is more favorable for its peroxidase activity. Indeed, Syk-induced Tyr phosphorylation of Prx2 enhances in vitro Prx2 activity, but also contributes to Prx2 translocation to the membrane of red cells exposed to diamide. The biologic importance of Tyr-193 phospho-Prx2 is further supported by data on red cells from a mouse model of humanized sickle cell disease (SCD). SCD is globally distributed, hereditary red cell disorder, characterized by severe red cell oxidation due to the pathologic sickle hemoglobin. SCD red cells show Tyr-phosphorylated Prx2 bound to the membrane and increased Prx2 activity when compared to healthy erythrocytes. Collectively, our data highlight the novel link between redox related signaling and Prx2 function in normal and diseased red cells.

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