In vitro anticancer activity of Betulinic acid and derivatives thereof on equine melanoma cell lines from grey horses and invivo safety assessment of the compound NVX-207 in two horses

Chemico-biological Interactions
G LiebscherReinhard Paschke

Abstract

Betulinic acid, a pentacyclic triterpene, and its derivatives are promising compounds for cancer treatment in humans. Melanoma is not only a problem for humans but also for grey horses as they have a high potential of developing melanoma lesions coupled to the mutation causing their phenotype. Current chemotherapeutic treatment carries the risk of adverse health effects for the horse owner or the treating veterinarian by exposure to antineoplastic compounds. Most treatments have low prospects for systemic tumor regression. Thus, a new therapy is needed. In this in vitro study, Betulinic acid and its two derivatives B10 and NVX-207, both with an improved water solubility compared to Betulinic acid, were tested on two equine melanoma cell lines (MelDuWi and MellJess/HoMelZh) and human melanoma (A375) cell line. We could demonstrate that all three compounds especially NVX-207 show high cytotoxicity on both equine melanoma cell lines. The treatment with these compounds lead to externalization of phosphatidylserines on the cell membrane (AnnexinV-staining), DNA-fragmentation (cell cycle analysis) and activation of initiator and effector caspases (Caspase assays). Our results indicate that the apoptosis is induced in the equine melan...Continue Reading

References

Apr 24, 2001·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·N M EnweremP A Akah
Dec 6, 2001·Cancer Letters·Valentina ZucoFranca Formelli
Jul 27, 2002·Journal of Veterinary Internal Medicine·Katherine Cole MacGillivrayFabio Del Piero
Feb 16, 2005·Apoptosis : an International Journal on Programmed Cell Death·M MourdjevaS Kyurkchiev
Nov 17, 2006·Journal of the American Veterinary Medical Association·Christina A Hewes, Kenneth E Sullins
May 17, 2007·Journal of the American Veterinary Medical Association·Alain P ThéonLarry D Galuppo
Dec 31, 2008·Apoptosis : an International Journal on Programmed Cell Death·Franziska B MullauerJan Paul Medema
Mar 25, 2009·European Journal of Clinical Investigation·M WillmannE Selzer
Aug 21, 2009·Journal of Natural Products·Fatma M Abdel BarKhalid A El Sayed
Aug 29, 2013·In Vitro Cellular & Developmental Biology. Animal·Monika H SeltenhammerAnna Golovko
Jun 8, 2014·Biochimica Et Biophysica Acta·Marcin BroniatowskiPaweł Miśkowiec
Jun 10, 2014·Expert Opinion on Therapeutic Patents·René Csuk

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Citations

Mar 21, 2016·Journal of Pharmaceutical Sciences·Huixin QiHongjian Zhang
Apr 29, 2019·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Janaina FernandesMorgana T L Castelo-Branco
Nov 21, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Anna SpivakUsein Dzhemilev
Jun 3, 2021·International Journal of Molecular Sciences·Dorina CoricovacMirela Danina Muntean

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