The diterpenoid 7-keto-sempervirol, derived from Lycium chinense, displays anthelmintic activity against both Schistosoma mansoni and Fasciola hepatica

PLoS Neglected Tropical Diseases
Jennifer EdwardsKarl F Hoffmann

Abstract

Two platyhelminths of biomedical and commercial significance are Schistosoma mansoni (blood fluke) and Fasciola hepatica (liver fluke). These related trematodes are responsible for the chronic neglected tropical diseases schistosomiasis and fascioliasis, respectively. As no vaccine is currently available for anti-flukicidal immunoprophylaxis, current treatment is mediated by mono-chemical chemotherapy in the form of mass drug administration (MDA) (praziquantel for schistosomiasis) or drenching (triclabendazole for fascioliasis) programmes. This overreliance on single chemotherapeutic classes has dramatically limited the number of novel chemical entities entering anthelmintic drug discovery pipelines, raising significant concerns for the future of sustainable blood and liver fluke control. Here we demonstrate that 7-keto-sempervirol, a diterpenoid isolated from Lycium chinense, has dual anthelmintic activity against related S. mansoni and F. hepatica trematodes. Using a microtiter plate-based helminth fluorescent bioassay (HFB), this activity is specific (Therapeutic index = 4.2, when compared to HepG2 cell lines) and moderately potent (LD50 = 19.1 μM) against S. mansoni schistosomula cultured in vitro. This anti-schistosomula e...Continue Reading

References

May 1, 1985·Stain Technology·A L Franklin, W G Filion
Nov 1, 1972·The Journal of Pharmacy and Pharmacology·P M BakerW Vichnewski
Feb 1, 1974·Experimental Parasitology·D G Colley, S K Wikel
Jan 28, 1999·Memórias do Instituto Oswaldo Cruz·J R Machado-SilvaD C Gomes
Nov 17, 2001·Current Opinion in Pharmacology·A B da RochaG Schwartsmann
Aug 26, 2003·Parasitology Research·O KayserS L Croft
Jul 21, 2004·Journal of Ethnopharmacology·M F GuerreroL San Román
Sep 13, 2005·Journal of Helminthology·I Fairweather
Dec 1, 2006·Advances in Parasitology·Patrick J Skelly, R Alan Wilson
Dec 15, 2006·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Jennifer M FitzpatrickKarl F Hoffmann
Feb 20, 2007·Memórias do Instituto Oswaldo Cruz·R Alan Wilson, Patricia S Coulson
Nov 3, 2007·Current Opinion in Infectious Diseases·Jennifer Keiser, Jürg Utzinger
Mar 18, 2008·Nature Medicine·Ahmed A SayedDavid L Williams
May 9, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Alejandro UrzúaLoretta Vásquez
Jul 11, 2009·Science·Jesse W-H Li, John C Vederas
Nov 4, 2009·PLoS Neglected Tropical Diseases·Jennifer M FitzpatrickKarl F Hoffmann
Aug 25, 2010·Antimicrobial Agents and Chemotherapy·Urs DuthalerJennifer Keiser
Feb 15, 2011·Acta Tropica·Carla KirchhoferJennifer Keiser
Aug 11, 2011·Nature Communications·Kathrin K GeyerKarl F Hoffmann
May 1, 2012·PLoS Neglected Tropical Diseases·Sara LustigmanMaría-Gloria Basáñez
May 23, 2012·Current Pharmaceutical Design·Raymond J PierceGuilherme Oliveira
May 23, 2012·Current Pharmaceutical Design·Hsin-Hung HuangDavid L Williams
Jun 30, 2012·Current Opinion in Infectious Diseases·Miguel M Cabada, A Clinton White
Oct 9, 2012·Current Opinion in Infectious Diseases·Timothy G Geary
Oct 23, 2012·Experimental Parasitology·Natcha LorsuwannaratPrasert Sobhon
Nov 8, 2012·PLoS Pathogens·Stanley Ching-Cheng HuangEdward J Pearce
Dec 6, 2012·Current Medicinal Chemistry·N S RadulovićN M Stojanović
Oct 1, 2007·Expert Opinion on Drug Discovery·Bernadette RamirezSolomon Nwaka

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Citations

Nov 30, 2016·Phytotherapy Research : PTR·Marcus Vinícius Oliveira Barros de AlencarMd Torequl Islam
Jan 29, 2019·PLoS Neglected Tropical Diseases·Sören FrahmClarissa Prazeres da Costa
Feb 19, 2020·Phytotherapy Research : PTR·Muhammad Torequl IslamJavad Sharifi-Rad
Jul 28, 2016·Chemistry & Biodiversity·Carly H G BorgesSérgio R Ambrósio
Oct 20, 2020·PLoS Neglected Tropical Diseases·Helen WhitelandKarl F Hoffmann
Jan 23, 2021·RSC Medicinal Chemistry·Godwin Akpeko DziwornuKelly Chibale

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Methods Mentioned

BETA
scanning electron microscopy
confocal microscopy

Software Mentioned

MetaXpress
ImageXpress micro XL
Excel
ImageXpress

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