scholarly journals Natural Compounds from the Marine Brown Alga Caulocystis cephalornithos with Potent In Vitro-Activity against the Parasitic Nematode Haemonchus contortus

Pathogens ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 550
Author(s):  
Aya C. Taki ◽  
Robert Brkljača ◽  
Tao Wang ◽  
Anson V. Koehler ◽  
Guangxu Ma ◽  
...  

Eight secondary metabolites (1 to 8) were isolated from a marine sponge, a marine alga and three terrestrial plants collected in Australia and subsequently chemically characterised. Here, these natural product-derived compounds were screened for in vitro-anthelmintic activity against the larvae and adult stages of Haemonchus contortus (barber’s pole worm)—a highly pathogenic parasitic nematode of ruminants. Using an optimised, whole-organism screening system, compounds were tested on exsheathed third-stage larvae (xL3s) and fourth-stage larvae (L4s). Anthelmintic activity was initially evaluated on these stages based on the inhibition of motility, development and/or changes in morphology (phenotype). We identified two compounds, 6-undecylsalicylic acid (3) and 6-tridecylsalicylic acid (4) isolated from the marine brown alga, Caulocystis cephalornithos, with inhibitory effects on xL3 and L4 motility and larval development, and the induction of a “skinny-straight” phenotype. Subsequent testing showed that these two compounds had an acute nematocidal effect (within 1–12 h) on adult males and females of H. contortus. Ultrastructural analysis of adult worms treated with compound 4 revealed significant damage to subcuticular musculature and associated tissues and cellular organelles including mitochondria. In conclusion, the present study has discovered two algal compounds possessing acute anthelmintic effects and with potential for hit-to-lead progression. Future work should focus on undertaking a structure-activity relationship study and on elucidating the mode(s) of action of optimised compounds.

Marine Drugs ◽  
2021 ◽  
Vol 19 (12) ◽  
pp. 698
Author(s):  
Kelsey S. Ramage ◽  
Aya C. Taki ◽  
Kah Yean Lum ◽  
Sasha Hayes ◽  
Joseph J. Byrne ◽  
...  

High-throughput screening of the NatureBank marine extract library (n = 7616) using a phenotypic assay for the parasitic nematode Haemonchus contortus identified an active extract derived from the Australian marine sponge Citronia sp. Bioassay-guided fractionation of the CH2Cl2/MeOH extract from Citronia sp. resulted in the purification of two known hexachlorinated peptides, dysidenin (1) and dysideathiazole (2). Compound 1 inhibited the growth/development of H. contortus larvae and induced multiple phenotypic changes, including a lethal evisceration (Evi) phenotype and/or somatic cell and tissue destruction. This is the first report of anthelmintic activity for these rare and unique polychlorinated peptides.


2008 ◽  
Vol 82 (1) ◽  
pp. 25-31 ◽  
Author(s):  
U. López-Aroche ◽  
D.O. Salinas-Sánchez ◽  
P. Mendoza de Gives ◽  
M.E. López-Arellano ◽  
E. Liébano-Hernández ◽  
...  

AbstractTwenty extracts from plants from Sierra de Huautla Biosphere Reserve, Morelos, Mexico were evaluated against Haemonchus contortus infective larvae in an in vitro assay. The plant species evaluated were Bursera copallifera, B. grandifolia, Lippia graveolens, Passiflora mexicana, Prosopis laevigata, Randia echinocarpa and Urtica dioica. The plants were separated into their parts and macerated with different solvents (n-hexane, acetone, ethanol and methanol). An in vitro assay was used to evaluate the anthelmintic activity against unsheathed third stage H. contortus infective larvae. The experiment was carried out in 24-well cell culture plates at room temperature with three replicates per treatment and using a concentration of 20 mg ml− 1. Ten 5 μl aliquots were taken from the corresponding wells and deposited on a slide for microscopical observation at 24, 48, 72 and 96 h post-exposure. The evaluation criteria were based on the average numbers of live and/or dead larvae in the different treatments. Alive and dead larval numbers were statistically analysed through the ANOVA test (P>0.01). The Tukey test was used as a complementary tool to determine which treatment was different from the other treatments (P>0.05). The highest mortality was observed with P. laevigata hexanic extract from stem and leaves combined, which produced 51%, 81% and 86% larval mortality at 24, 48 and 72 h post-exposure, respectively. On the other hand, B. copallifera stem acetonic extract exhibited 18%, 59% and 66% nematicidal activity after 24, 48 and 72 h of exposure, respectively.


Acta Tropica ◽  
2021 ◽  
Vol 217 ◽  
pp. 105869
Author(s):  
Vivien Patricia Garbin ◽  
Beatriz Munguía ◽  
Jenny Carolina Saldaña ◽  
Cícero Deschamps ◽  
Roger Raupp Cipriano ◽  
...  

Author(s):  
Rachel A. Nwosu ◽  
Mohammed M. Suleiman ◽  
Hussaina J. Makun ◽  
Matthew P. Ameh ◽  
Manji A. Shetshak ◽  
...  

1992 ◽  
Vol 66 (4) ◽  
pp. 273-278 ◽  
Author(s):  
E. V. Warbrick ◽  
S. A. Ward

ABSTRACTVarious catecholamines and catecholamine antagonists have been examined for their effects on the third larval moult of the parasitic nematode, Dirofilaria immitis, cultured in vitro. The non-selective α and β agonist, noradrenaline, and the β agonist, isoprenaline, had no effect on the timing of the third stage moult when used at a concentration of 10−5M. The α-adrenergic antagonist. phentolamine, resulted in worm mortality at 10−5M. At 10−7M, both phentolamine and the β-antagonist, propranolol caused a significant reduction in the numbers of larvae capable of completing the third stage moult. Idazoxan, an a2-antagonist, at 10−5M did not affect worm mortality but did completely prevent ecdysis. The potential of these compounds as possible filaricides is discussed.


Author(s):  
Rosa Isabel Higuera-Piedrahita ◽  
Mariana Dolores-Hernández ◽  
Luis Gerardo Jiménez-Pérez ◽  
Brígida C. Camacho-Enríquez ◽  
Alejandro Zamilpa ◽  
...  

2015 ◽  
Vol 76 ◽  
pp. 647-652 ◽  
Author(s):  
Yousmel Aleman Gaínza ◽  
Luciana Ferreira Domingues ◽  
Oriela Pino Perez ◽  
Márcio Dias Rabelo ◽  
Eugenio Roque López ◽  
...  

2010 ◽  
Vol 47 (4) ◽  
pp. 269-272 ◽  
Author(s):  
H. Bártíková ◽  
L. Skálová ◽  
J. Lamka ◽  
B. Szotáková ◽  
M. Várady

AbstractThe anthelmintic effects of flubendazole (FLU), its two main metabolites reduced flubendazole (FLU-R) and hydrolyzed flubendazole (FLU-H), and thiabendazole (TBZ) were compared using an in vitro larval development test in two isolates of Haemonchus contortus, a fully susceptible isolate (HCS) and a multi-resistant isolate (HCR). Results were quantified as 50 % lethal concentration (LC50), 99 % lethal concentration (LC99), efficacy factor (EF), and resistance factor (RF). For HCS, both LC50 and LC99 of FLU were lower than those of the reference TBZ. The anthelmintic activity of FLU-R in HCS and HCR was 13 and 6 times lower than the activity of FLU, respectively. The anthelmintic activity of FLU-H was negligible (approximately 363–853 times lower) compared to that of FLU. Although a marked resistance of the HCR isolate to TBZ was confirmed, only a low tolerance to FLU-R and slightly higher tolerance to FLU were found.


Author(s):  
A. Aïssa ◽  
F. Manolaraki ◽  
H. Ben Salem ◽  
H. Hoste ◽  
K. Kraiem

Background: Mediterranean shrub species cover more than 70% of the total area in Tunisia and in summer when the herbaceous species have wilted, they constitute feeding resource for livestock. The use of tanniniferous shrubs seems to be a good alternative to control gastrointestinal nematodes infections in small ruminants. This study evaluated the in vitro anthelmintic (AH) effect of Ceratonia siliqua (C. siliqua), Periploca angustifolia Labill. (P. angustifolia) and Medicago arborea (M. arborea) against Haemonchus contortus third stage larvae (L3). Methods: The larval exsheathment assay (LEA) was used to determine the proportions (%) of exsheathment of five acetonic extracts at different concentrations (1200, 600, 300, 150 μg/ml). To confirm the role of tannins in the AH effects of extracts, polyvinyl polypyrolidone (PVPP) was used as deactivating chemical tannins. Result: The highest % L3 exsheathed was recorded for M. arborea (55.01%) and the lowest value was founded for C. siliqua and P. angustifolia leaves (16.26%). Our results were concentration-dependent (P less than 0.001). The % of exsheathment increased as the time of incubation increased (P less than 0.001). P. angustifolia pods recorded the lowest EC50 value (P less than 0.05). After PVPP addition, all the acetonic extracts showed a restoration of L3 exsheathment values similar to control values (P less than 0.001).


2020 ◽  
Vol 2020 ◽  
pp. 1-7 ◽  
Author(s):  
Aliyi Hassen Ahmed ◽  
Mebrat Ejo ◽  
Teka Feyera ◽  
Dereje Regassa ◽  
Bahar Mummed ◽  
...  

Gastrointestinal nematodes (GINs) are the major limiting factor for the successfulness of livestock production throughout the world. Emergence of resistance strains as well as scarcity and high cost of the currently available drugs has led to the evaluation of other alternative helminth control options, mainly from plants. The current study is aimed at investigating the in vitro anthelmintic efficacy of crude methanolic extracts of two traditionally important medicinal plants, Artemisia herba-alba and Punica granatum, against Haemonchus contortus using adult motility assay (AMA) and egg hatch inhibition assay (EHIA). Four graded concentrations of the extracts were tested for both the AMA (10, 5, 2.5, and 1.25 mg/mg) and EHIA (0.1, 0.25, 0.5, and 1 mg/mL) in replicates. Albendazole and phosphate-buffered saline (AMA) or distilled water (EHIA) were used as the positive and negative controls, respectively. The crude extracts of A. herba-alba and P. granatum exhibited a potential anthelmintic activity at all dose levels in a concentration- and time-dependent fashion. The highest concentration (10 mg/mL) of all the extracts caused a significantly (p<0.05) superior nematocidal activity compared to the negative control. Moreover, significant and concentration-dependent egg hatching inhibition effect was observed from both plant extracts. Maximal (98.67%) egg hatching inhibition effect was exhibited by the flower extract of A. herba-alba at 1 mg/mL concentration. The relative egg hatch inhibition efficacy indicated that both plants caused a significantly (p<0.05) greater egg hatch inhibition within 48 hr of exposure. The current study validated the traditional use of both plants as a natural anthelmintic against H. contortus justifying a need to undertake detail pharmacological and toxicological investigation on both plants.


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