scholarly journals Identification of Fromiamycalin and Halaminol A from Australian Marine Sponge Extracts with Anthelmintic Activity against Haemonchus contortus

Marine Drugs ◽  
2019 ◽  
Vol 17 (11) ◽  
pp. 598 ◽  
Author(s):  
H. Herath ◽  
Sarah Preston ◽  
Abdul Jabbar ◽  
Jose Garcia-Bustos ◽  
Aya Taki ◽  
...  
Keyword(s):  
Haemonchus Contortus ◽  
Marine Invertebrates ◽  
Anthelmintic Activity ◽  
Marine Sponges ◽  
Parasitic Nematodes ◽  
Natural Ecosystems ◽  
Bioassay Guided Fractionation ◽  
Guanidine Alkaloids ◽  
Nematocidal Activity

There is an urgent need to discover and develop new anthelmintics for the treatment of parasitic nematodes of veterinary importance to circumvent challenges linked to drug resistant parasites. Being one of the most diverse natural ecosystems, the marine environment represents a rich resource of novel chemical entities. This study investigated 2000 extracts from marine invertebrates, collected from Australian waters, for anthelmintic activity. Using a well-established in vitro bioassay, these extracts were screened for nematocidal activity against Haemonchus contortus — a socioeconomically important parasitic nematode of livestock animals. Extracts (designated Mu-1, Ha-1 and Ha-2) from two marine sponges (Monanchora unguiculata and Haliclona sp.) each significantly affected larvae of H. contortus. Individual extracts displayed a dose-dependent inhibition of both the motility of exsheathed third-stage larvae (xL3s) and the development of xL3s to fourth-stage larvae (L4s). Active fractions in each of the three extracts were identified using bioassay-guided fractionation. From the active fractions from Monanchora unguiculata, a known pentacyclic guanidine alkaloid, fromiamycalin (1), was purified. This alkaloid was shown to be a moderately potent inhibitor of L4 development (half-maximum inhibitory concentration (IC50) = 26.6 ± 0.74 µM) and L4 motility (IC50 = 39.4 ± 4.83 µM), although it had a relatively low potency at inhibiting of xL3 motility (IC50 ≥ 100 µM). Investigation of the active fractions from the two Haliclona collections led to identification of a mixture of amino alcohol lipids, and, subsequently, a known natural product halaminol A (5). Anthelmintic profiling showed that 5 had limited potency at inhibiting larval development and motility. These data indicate that fromiamycalin, other related pentacyclic guanidine alkaloids and/or halaminols could have potential as anthelmintics following future medicinal chemistry efforts.

scholarly journals Anthelmintic activity of Cymbopogon citratus against Haemonchus contortus

2015 ◽  
Vol 24 (3) ◽  
pp. 268-275 ◽  
Author(s):  
Iara Tersia Freitas Macedo ◽  
Lorena Mayana Beserra de Oliveira ◽  
Wesley Lyeverton Correia Ribeiro ◽  
Jessica Maria Leite dos Santos ◽  
Kaline das Chagas Silva ◽  
...  
Keyword(s):  
Essential Oil ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Meriones Unguiculatus ◽  
Parasitic Nematodes ◽  
Control Group ◽  
Cymbopogon Citratus ◽  
Egg Hatching

Parasitic nematodes are of major economic importance in livestock. An alternative for the control of parasites is phytotherapy. This study evaluated the efficacy of Cymbopogon citratus decoction (CcD), C. citratus essential oil (CcEo) and citral against Haemonchus contortus using in vitro egg hatch test (EHT) and larval development test (LDT) and an in vivo test using a Meriones unguiculatus (gerbil) model. The effect of 800 mg/kg CcEo was evaluated in gerbils that had been artificially infected with 5,000 third-stage H. contortus larvae. The effective concentrations required to inhibit 50% (EC50) of egg hatching were 0.46, 0.14 and 0.13 mg/mL for CcD, CcEo and citral, respectively. The EC50 values in the LDT were 5.04, 1.92 and 1.37 mg/mL for CcD, CcEo and citral, respectively. H. contortus population in the group treated with C. citratus essential oil was reduced by 38.5% (P< 0.05) in comparison to the control group. These results suggest that it may be possible to use C. citratusessential oil to control of H. contortus parasite of small ruminant.

scholarly journals Comparative anthelmintic efficacy of Arundo donax, Areca catechu, and Ferula assa-foetida against Haemonchus contortus

2021 ◽  
Vol 30 (2) ◽  
Author(s):  
Syed Nadeem Badar ◽  
Zafar Iqbal ◽  
Muhammad Sohail Sajid ◽  
Hafiz Muhammad Rizwan ◽  
Muhammad Shareef ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Parasitic Nematodes ◽  
Egg Hatch ◽  
Faecal Egg Count ◽  
Areca Catechu ◽  
Better Than

Abstract In the present study, anthelmintic activities of Arundo (A.) donax L., Areca (Ar.) catechu L., and Ferula (F.) assa-foetida L. were determined. Leaves of A. donax L., latex of F. assa-foetida L. and seeds of Ar. catechu L. in different solvent fractions were subjected to in vitro (egg hatch assay; EHA, and adult motility assay; AMA) and in vivo (faecal egg count reduction test; FECRT) tests of anthelmintic activity using Haemonchus contortus model. In the AMA, crude aqueous methanol extracts (CAME) and ethyl acetate fractions of F. assa-foetida at 10 hr post-treatment showed maximum mortality of H. contortus at 12.5-50 mg mL-1. In the EHA, CAME of F. assa-foetida was identified as a potent ovicide based on its low LC50 (16.9 µg mL-1), followed in order by Ar. catechu and A. donax. Results from the FECRT also showed the extract of F. assa-foetida L. to be more effective than those of Ar. catechu L. and A. donax L., against the gastrointestinal parasitic nematodes. Chloroform and ethyl acetate fractions showed better anthelmintic activities against the adult worms in vitro, while CAME of these plants were better than their crude powders in vivo. It is recommended to document and investigate indigenous knowledge of possible medicinal plants to plan scientific trials that may justify their endorsement.

scholarly journals High Throughput Screening of the NatureBank ‘Marine Collection’ in a Haemonchus Bioassay Identifies Anthelmintic Activity in Extracts from a Range of Sponges from Australian Waters

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5846
Author(s):  
Aya C. Taki ◽  
Joseph J. Byrne ◽  
Abdul Jabbar ◽  
Kah Yean Lum ◽  
Sasha Hayes ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Marine Invertebrates ◽  
Chemical Space ◽  
Anthelmintic Activity ◽  
Distinct Species ◽  
Parasitic Nematodes ◽  
Wild Type ◽  
Control Programs

Widespread resistance in parasitic nematodes to most classes of anthelmintic drugs demands the discovery and development of novel compounds with distinct mechanisms of action to complement strategic or integrated parasite control programs. Products from nature—which assume a diverse ‘chemical space’—have significant potential as a source of anthelmintic compounds. In the present study, we screened a collection of extracts (n = 7616) derived from marine invertebrates sampled from Australian waters in a high throughput bioassay for in vitro anti-parasitic activity against the barber’s pole worm (Haemonchus contortus)—an economically important parasitic nematode of livestock animals. In this high throughput screen (HTS), we identified 58 active extracts that reduced larval motility by ≥70% (at 90 h), equating to an overall ‘hit rate’ of ~0.8%. Of these 58 extracts, 16 also inhibited larval development by ≥80% (at 168 h) and/or induced ‘non-wild-type’ (abnormal) larval phenotypes with reference to ‘wild-type’ (normal) larvae not exposed to extract (negative controls). Most active extracts (54 of 58) originated from sponges, three from chordates (tunicates) and one from a coral; these extracts represented 37 distinct species/taxa of 23 families. An analysis of samples by 1H NMR fingerprinting was utilised to dereplicate hits and to prioritise a set of 29 sponge samples for future chemical investigation. Overall, these results indicate that a range of sponge species from Australian waters represents a rich source of natural compounds with nematocidal or nematostatic properties. Our plan now is to focus on in-depth chemical investigations of the sample set prioritised herein.

scholarly journals Anthelmintic Activity of Hymenodictyon pachyanta Stem Bark Extracts against Haemonchus Contortus

2019 ◽  
Vol 63 (2) ◽  
pp. 30-36
Author(s):  
D. O. Olayemi ◽  
M. M. Onakpa ◽  
O. C. Jegede
Keyword(s):  
Larval Development ◽  
Crude Extract ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Stem Bark ◽  
Parasitic Nematodes ◽  
Egg Hatching ◽  
Crude Extracts ◽  
Significant Difference

Abstract The development of host resistance to anthelmintics and the increasing cost of commercial anthelmintics have encouraged the need for the in vitro anthelmintic evaluation of crude extract and fractions of Hymenodictyon pachyanta plant as alternative drugs against Haemonchus contortus. H. contortus is one of the most prevalent and highly pathogenic parasitic nematodes in small ruminant farming globally. H. pachyanta stem bark is a prospective plant used by the local and indigenous farmers of Nsukka, Enugu state, Nigeria. The stem bark of H. pachyanta were collected, dried, pulverized and extracted with 80 % methanol. The purpose of this study was to investigate the in vitro anthelmintic effects of these crude extract and fractions against H. contortus in sheep and goats. The two extracts (crude and fractions) of H. pachyanta were tested by the egg hatch assay (EHA) and the larval development inhibition assays (LDIA) and to compared the results with albendazole (as the positive control). The concentrations for the crude extract and albendazole used for this study were 0.78, 1.56, 3.125, 6.25 and 12.5 mg.ml−1. The results demonstrated that the crude extracts, fractions and albendazole all at the concentration doses of 12.5 mg.ml−1 produced 100 % inhibition of egg hatching and larval development. Statistically, there was no significant difference (P > 0.05) in the mean percentage inhibition of egg hatching and larval development inhibition of the crude extracts and fractions when compared with albendazole. However, a significant difference (P < 0.05) was observed with n-butanol fraction which inhibited 96.17 % of egg hatchability. All of the extracts and albendazole showed ovicidal and larvicidal effects and were able to induce over 50 % of the egg hatching and mortality of larvae at the concentration ranges of 0.78—12.5 mg.ml−1. The results obtained from our study suggest that H. pachyanta had ovicidal and larvicidal activity against H. contortus and that the bioactive plants compounds responsible for this effect could be attributed to the presence of tannins, alkaloids and the saponins contained in the crude extracts.

scholarly journals Dysidenin from the Marine Sponge Citronia sp. Affects the Motility and Morphology of Haemonchus contortus Larvae In Vitro

Marine Drugs ◽  
2021 ◽  
Vol 19 (12) ◽  
pp. 698
Author(s):  
Kelsey S. Ramage ◽  
Aya C. Taki ◽  
Kah Yean Lum ◽  
Sasha Hayes ◽  
Joseph J. Byrne ◽  
...  
Keyword(s):  
Marine Sponge ◽  
Haemonchus Contortus ◽  
High Throughput Screening ◽  
Parasitic Nematode ◽  
Anthelmintic Activity ◽  
Tissue Destruction ◽  
Meoh Extract ◽  
Bioassay Guided Fractionation ◽  
Growth Development

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.

Chemical characterization and in vitro anthelmintic activity of Citrus bergamia Risso and Citrus X paradisii Macfad essential oil against Haemonchus contortus Kirby isolate

Acta Tropica ◽  
2021 ◽  
Vol 217 ◽  
pp. 105869
Author(s):  
Vivien Patricia Garbin ◽  
Beatriz Munguía ◽  
Jenny Carolina Saldaña ◽  
Cícero Deschamps ◽  
Roger Raupp Cipriano ◽  
...  
Keyword(s):  
Essential Oil ◽  
Haemonchus Contortus ◽  
Chemical Characterization ◽  
Anthelmintic Activity ◽  
Citrus Bergamia

In vitro anthelmintic activity of Dennettia tripetala G. Baker (Annonaceae) Fruits against Haemonchus contortus

2021 ◽  
Author(s):  
Rachel A. Nwosu ◽  
Mohammed M. Suleiman ◽  
Hussaina J. Makun ◽  
Matthew P. Ameh ◽  
Manji A. Shetshak ◽  
...  
Keyword(s):  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Dennettia Tripetala

In Vitro Nematocidal Effect and Anthelmintic Activity of Artemisia cina Against Haemonchus contortus in Gerbils and Relative Expression of Hc29 Gene in Transitional Larvae (L3–L4)

2021 ◽  
Author(s):  
Rosa Isabel Higuera-Piedrahita ◽  
Mariana Dolores-Hernández ◽  
Luis Gerardo Jiménez-Pérez ◽  
Brígida C. Camacho-Enríquez ◽  
Alejandro Zamilpa ◽  
...  
Keyword(s):  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Relative Expression

Anthelmintic activity in vitro of Citrus sinensis and Melaleuca quinquenervia essential oil from Cuba on Haemonchus contortus

2015 ◽  
Vol 76 ◽  
pp. 647-652 ◽  
Author(s):  
Yousmel Aleman Gaínza ◽  
Luciana Ferreira Domingues ◽  
Oriela Pino Perez ◽  
Márcio Dias Rabelo ◽  
Eugenio Roque López ◽  
...  
Keyword(s):  
Essential Oil ◽  
Haemonchus Contortus ◽  
Citrus Sinensis ◽  
Anthelmintic Activity ◽  
Melaleuca Quinquenervia

scholarly journals The effects of flubendazole and its metabolites on the larval development of Haemonchus contortus (Nematoda: Trichostrongylidae): an in vitro study

2010 ◽  
Vol 47 (4) ◽  
pp. 269-272 ◽  
Author(s):  
H. Bártíková ◽  
L. Skálová ◽  
J. Lamka ◽  
B. Szotáková ◽  
M. Várady
Keyword(s):  
Larval Development ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
In Vitro Study ◽  
Lethal Concentration ◽  
Resistant Isolate ◽  
Susceptible Isolate ◽  
Marked Resistance ◽  
Larval Development Test

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.

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