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Article

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

1
Department of Biosciences, Melbourne Veterinary School, Faculty of Veterinary and Agricultural Sciences, The University of Melbourne, Parkville, VIC 3010, Australia
2
School of Science (Applied Chemistry and Environmental Science), RMIT University, Melbourne, VIC 3001, Australia
3
Peter MacCallum Cancer Centre, Melbourne, VIC 3010, Australia
*
Authors to whom correspondence should be addressed.
Pathogens 2020, 9(7), 550; https://doi.org/10.3390/pathogens9070550
Received: 10 June 2020 / Revised: 26 June 2020 / Accepted: 1 July 2020 / Published: 9 July 2020
(This article belongs to the Special Issue Animal Parasitic Diseases)
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. View Full-Text
Keywords: algae; Caulocystis cephalornithos; natural compound; anthelmintic; in vitro-activity; Haemonchus contortus algae; Caulocystis cephalornithos; natural compound; anthelmintic; in vitro-activity; Haemonchus contortus
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MDPI and ACS Style

Taki, A.C.; Brkljača, R.; Wang, T.; Koehler, A.V.; Ma, G.; Danne, J.; Ellis, S.; Hofmann, A.; Chang, B.C.H.; Jabbar, A.; Urban, S.; Gasser, R.B. Natural Compounds from the Marine Brown Alga Caulocystis cephalornithos with Potent In Vitro-Activity against the Parasitic Nematode Haemonchus contortus. Pathogens 2020, 9, 550. https://doi.org/10.3390/pathogens9070550

AMA Style

Taki AC, Brkljača R, Wang T, Koehler AV, Ma G, Danne J, Ellis S, Hofmann A, Chang BCH, Jabbar A, Urban S, Gasser RB. Natural Compounds from the Marine Brown Alga Caulocystis cephalornithos with Potent In Vitro-Activity against the Parasitic Nematode Haemonchus contortus. Pathogens. 2020; 9(7):550. https://doi.org/10.3390/pathogens9070550

Chicago/Turabian Style

Taki, Aya C., Robert Brkljača, Tao Wang, Anson V. Koehler, Guangxu Ma, Jill Danne, Sarah Ellis, Andreas Hofmann, Bill C.H. Chang, Abdul Jabbar, Sylvia Urban, and Robin B. Gasser 2020. "Natural Compounds from the Marine Brown Alga Caulocystis cephalornithos with Potent In Vitro-Activity against the Parasitic Nematode Haemonchus contortus" Pathogens 9, no. 7: 550. https://doi.org/10.3390/pathogens9070550

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