scholarly journals In Vitro Antischistosomal Activity and Cytotoxicity of 5-Methoxylated Flavones fom Vochysia divergens, a Flood-Adapted Species from Brazilian Pantanal

2015 ◽  
Vol 04 (03) ◽  
Author(s):  
Pimenta LP Kellner Filho
Keyword(s):  
Antischistosomal Activity ◽  
Vochysia Divergens ◽  
Methoxylated Flavones ◽  
Brazilian Pantanal

5-methoxylated flavones from Vochysia divergens a flood-adapted species from Brazilian Pantanal

Planta Medica ◽  
2014 ◽  
Vol 80 (16) ◽  
Author(s):  
LP Pimenta ◽  
LC Kellner Filho ◽  
RG Liotti ◽  
MA Soares ◽  
PF Oliveira ◽  
...  
Keyword(s):  
Vochysia Divergens ◽  
Methoxylated Flavones ◽  
Brazilian Pantanal

scholarly journals Genotoxic and Chemopreventive Effects of Vochysia divergens Leaves (Pantanal, Brazil)

2018 ◽  
Vol 2018 ◽  
pp. 1-7
Author(s):  
Pollyanna Francielli de Oliveira ◽  
Suzana Amorim Mendes ◽  
Nathália Oliveira Acésio ◽  
Luis Claudio Kellner Filho ◽  
Leticia Pereira Pimenta ◽  
...  
Keyword(s):  
Protective Effect ◽  
Skin Diseases ◽  
Chemical Constituents ◽  
Test System ◽  
Negative Control ◽  
Control Group ◽  
Xtt Assay ◽  
Vochysia Divergens

The medicinal plant Vochysia divergens is a colonizing tree species of the Pantanal, a unique and little explored wetland region in Brazil. This species is used in folk medicine as syrups and teas to treat respiratory infections, digestive disorders, asthma, scarring, and skin diseases. The objectives of this study were to evaluate the antioxidant, cytotoxic, and genotoxic potential of the ethanolic extract of Vochysia divergens leaves (VdE), as well as the influence of VdE and its major component (the flavone 3′,5-dimethoxy luteolin-7-O-β-glucopyranoside; 3′5 DL) on MMS-induced genotoxicity. The extract significantly reduced the viability of V79 cells in the colorimetric XTT assay at concentrations ≥ 39 μg/mL. A significant increase in micronucleus frequencies was observed in V79 cell cultures treated with VdE concentrations of 160 and 320 μg/mL. However, animals treated with the tested doses of VdE (500, 1000, and 2000 mg/kg b.w.) exhibited frequencies that did not differ significantly from those of the negative control group, indicating the absence of genotoxicity. The results also showed that VdE was effective in reducing MMS-induced genotoxicity at concentrations of 20, 40, and 80 μg/mL in the in vitro test system and at a dose of 15 mg/kg b.w. in the in vivo test system. Its major component 3′5 DL exerted no protective effect, suggesting that it is not responsible for the effect of the extract. The results of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay showed that VdE was able to scavenge 92.6% of free radicals. In conclusion, the results suggest that the protective effect of VdE may be related, at least in part, to the antioxidant activity of its chemical constituents.

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.

scholarly journals Activity of Combinations of Antioxidants and Anthelmintic Drugs against the Adult Stage of Schistosoma mansoni

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Maria João Gouveia ◽  
Paul J. Brindley ◽  
Fátima Gärtner ◽  
Nuno Vale
Keyword(s):  
Schistosoma Mansoni ◽  
Therapeutic Approach ◽  
Adult Stage ◽  
Morphological Alterations ◽  
Single Drug ◽  
Antischistosomal Activity ◽  
Per Se ◽  
And Control ◽  
Novel Therapeutic

Schistosomiasis remains a major neglected tropical disease. The treatment and control of schistosomiasis rely on a single drug, praziquantel (PZQ). Despite its efficacy, treatment with PZQ presents some major drawbacks including an inability of the chemotherapy to reverse disease-induced fibrosis and the prospect of the emergence of drug resistance. Here, we investigated a novel therapeutic approach with antioxidant biomolecules in combination with PZQ against the adult developmental stage of Schistosoma mansoni and oviposition in vitro, given that this therapeutic approach achieved synergistic/additive activity against larval schistosomes. The antioxidants curcumin and oxadiazole per se exhibited antischistosomal activity against adult worms leading to severe morphological alterations and death. Additionally, the antioxidant flavone combined with vandetanib or imatinib improved antischistosomal activity against adult forms. By contrast, however, these antioxidant-anthelmintic combinations were not as effective against adults in comparison to larval schistosomes. Nevertheless, the antioxidants alone or combined with drugs inhibited oviposition.

Spatial Variations in Soil Chemistry and Organic Matter Content across a Vochysia divergens Invasion Front in the Brazilian Pantanal

2011 ◽  
Vol 75 (4) ◽  
pp. 1554-1561 ◽  
Author(s):  
George L. Vourlitis ◽  
Francisco de Almeida Lobo ◽  
Marcelo Sacardi Biudes ◽  
Carmen Eugenia Rodríguez Ortíz ◽  
Jose de Souza Nogueira
Keyword(s):  
Organic Matter ◽  
Soil Chemistry ◽  
Organic Matter Content ◽  
Matter Content ◽  
Spatial Variations ◽  
Invasion Front ◽  
Vochysia Divergens ◽  
Brazilian Pantanal

scholarly journals In vitro Antischistosomal Activity of Clerodendrum umbellatum Poir (Labiateae) Leaves Aqueous Extract and Derived Fractions against Schistosoma mansoni Adult Worms

2020 ◽  
pp. 40-49
Author(s):  
Mérimé Christian Kenfack ◽  
Hermine Boukeng Jatsa ◽  
Nestor Gipwe Feussom ◽  
Emilienne Tienga Nkondo ◽  
Ulrich Membe Femoe ◽  
...  
Keyword(s):  
Motor Activity ◽  
Schistosoma Mansoni ◽  
Aqueous Extract ◽  
Culture Medium ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Phytochemical Screening ◽  
Methanol Fraction ◽  
Antischistosomal Activity

Aims: Treatment against schistosomiasis relies on praziquantel. Its treatment failure and the possible development of resistant schistosomes strains have been reported in the literature. Clerodendrum umbellatum leaves are used in Africa for the treatment of intestinal helminthiasis. The aim of this study was to evaluate the in vitro activity of C. umbellatum leaves aqueous extract and derived fractions on Schistosoma mansoni adult worms. Methodology: Five male and five female Schistosoma mansoni adult worms were incubated in each well for 48 h in a GMEM culture medium with C. umbellatum aqueous extract (125 to 4000 µg/mL) or its n-hexane, ethyl acetate and methanol fractions or the aqueous residue (62.5 to 2000 µg/mL). The main parameters assessed were the worm’s mortality and the reduction of motor activity. Phytochemical screening of all our tested substances was also performed. The cytotoxicity assay using mouse melanoma liver cells line was performed on the aqueous extract and on the most active fraction. Results: Our study shown that C. umbellatum leaves aqueous extract and its derived fractions promoted worm mortality. The aqueous extract disclosed a LC50 of 805.21 µg/mL while the LC50 of the methanol fraction was 343.10 µg/mL. With this lowest LC50, the methanol fraction from C. umbellatum aqueous extract was therefore the most active. Moreover, it showed low level of toxicity on hepatocytes. Incubation of worms with C. umbellatum aqueous extract and fractions also resulted in a significant reduction of the motor activity of survival worms with a 39.54 to 100% reduction after 48h. The phytochemical screening of C. umbellatum aqueous extract and fractions revealed the presence of alkaloids, phenols, flavonoids, tannins, saponins and terpenoids. Conclusion: The present study demonstrated the in vitro activity of C. umbellatum aqueous extract and derived fractions on S. mansoni adult worms and could then justify its empirical use to combat schistosomiasis.

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 Assessment of the In Vitro Antischistosomal Activities of the Extracts and Compounds from Solidago Microglossa DC (Asteraceae) and Aristolochia Cymbifera Mart. & Zucc. (Aristolochiaceae)

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Poliana da Silva Costa ◽  
Ohana Oliveira Zuza da Silva ◽  
Danilo de Souza Costa ◽  
Lara Aparecida de Oliveira Silva ◽  
Priscila de Faria Pinto ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Motor Activity ◽  
Laser Scanning ◽  
Acid Methyl Ester ◽  
Vero Cells ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Acid Methyl ◽  
Antischistosomal Activity

Schistosomiasis, caused by helminth flatworms of the genus Schistosoma, is a neglected tropical disease that afflicts over 230 million people worldwide. Currently, treatment is achieved with only one drug, praziquantel (PZQ). In this regard, the roots of Solidago microglossa (Asteraceae) and Aristolochia cymbifera (Aristolochiaceae) are popularly used as anthelmintic. Despite their medicinal use against helminthiasis, such as schistosomiasis, A. cymbifera, and S. microglossa have not been evaluated against S. mansoni. Then, in this work, the in vitro antischistosomal activity of the crude extracts of A. cymbifera (Ac) and S. microglossa (Sm) and their isolated compounds were investigated against S. mansoni adult worms. Sm (200 μg/mL) and Ac (100–200 μg/mL) were lethal to all male and female worms at the 24 h incubation. In addition, Sm (10–50 μg/mL) and Ac (10 μg/mL) caused significant reduction in the parasite’s movements, showing no significant cytotoxicity to Vero cells at the same range of schistosomicidal concentrations. Confocal laser scanning microscopy revealed that Sm and Ac caused tegumental damages and reduced the numbers of tubercles of male schistosomes. Chromatographic fractionation of Sm leads to isolation of bauerenol, α-amirin, and spinasterol, while populifolic acid, cubebin, 2-oxopopulifolic acid methyl ester, and 2-oxopopulifolic acid were isolated from Ac. At concentrations of 25–100 μM, bauerenol, α-amirin, spinasterol, populifolic acid, and cubebin showed significant impact on motor activity of S. mansoni. 2-oxopopulifolic acid methyl ester and 2-oxopopulifolic acid caused 100% mortality and decreased the motor activity of adult schistosomes at 100 μM. This study has reported, for the first time, the in vitro antischistosomal effects of S. microglossa and A. cymbifera extracts, also showing promising compounds against adult schistosomes.

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