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Aspergillus sp. was cultured on a solid medium to support large-scale production of secondary metabolites. Molecular network analysis of extracts and subfractions allowed annotation of 22 molecules to guide purification. The EtOAc extract showed antiproliferative activity (3.2 ± 0.4 µg/mL, 48 h) against HT-29 colorectal cancer cells and no toxicity (30 µg/mL) in TNBC (MDA-MB-231) and non-cancerous HEK293 cells. Among five prenylated compounds, echinulin derivatives 1 and 2 were most active with IC50 values of 1.73 µM and 8.8 µM against HT-29.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":40,"@type":76,"position":81},"https://docshare.wps.com/document/research-report/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/in-vitro-antiproliferative-activity-of-echinulin-derivatives-from-endolichenic-fungus-aspergillus-sp-against-colorectal-cancer/328908/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/in-vitro-antiproliferative-activity-of-echinulin-derivatives-from-endolichenic-fungus-aspergillus-sp-against-colorectal-cancer/328908.png","ImageObject",300,407,{"name":92,"@type":93},"Miles","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-10-30","2026-09-21",true,{"@type":102,"interactionType":103,"userInteractionCount":52},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"How were the endolichenic fungus Aspergillus sp. samples obtained and prepared for metabolite production?","Question",{"text":112,"@type":113},"Aspergillus sp. was isolated from the lichen Xanthoparmelia conspersa harvested in France. It was then grown on a solid culture medium to enable large-scale production of secondary metabolites.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"What antiproliferative effect did the EtOAc extract show against colorectal cancer cells?",{"text":117,"@type":113},"The EtOAc extract displayed antiproliferative activity of 3.2 ± 0.4 µg/mL after 48 h against human colorectal cancer cells (HT-29).",{"name":119,"@type":110,"acceptedAnswer":120},"Which isolated compounds were most active and what were their IC50 values?",{"text":121,"@type":113},"Among five prenylated compounds, four were echinulin derivatives. 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In Vitro Antiproliferative Activity of Echinulin Derivatives from Endolichenic Fungus Aspergillus sp. against Colorectal Cancer. Molecules 2024, 29, 4117. [https://doi.org/10.3390/](https://doi.org/10.3390/)[ ](https://doi.org/10.3390/)molecules29174117  \nAcademic Editors: Irwin Rose Alencar Menezes, Henrique Douglas Melo Coutinho, Almir  \nGonçalves Wanderley and Jaime Ribeiro-Filho  \nReceived: 23 July 2024  \nRevised: 20 August 2024  \nAccepted: 25 August 2024  \nPublished: 30 August 2024  \nCopyright: © 2024 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ([https://](https://)[ ](https://)[creativecommons.org/licenses/by/](creativecommons.org/licenses/by/)[ ](creativecommons.org/licenses/by/)[4.0/](4.0/)) .  \n1 LABCiS, UR 22722, Faculté de Pharmacie, Univ. Limoges, F-87000 Limoges, France;  \nhind.makhloufi@unilim.fr (H.M.); aline.pinon@unilim.fr (A.P.); marion.millot@unilim.fr (M.M.);  \n[bertrand.liagre@unilim.fr](bertrand.liagre@unilim.fr) (B.L.); [guillaume.chemin@unilim.fr](guillaume.chemin@unilim.fr) (G.C.)  \n2 Univ. Limoges, CNRS, Inserm, CHU Limoges, BISCEm, UAR 2015, US 42, F-87025 Limoges, France; [yves.champavier@unilim.fr](yves.champavier@unilim.fr)  \n3 Laboratoire LIENSs, Université de La Rochelle, UMR CNRS 7266, F-17000 La Rochelle, France; [jennifer.saliba@univ-lr.fr](jennifer.saliba@univ-lr.fr) (J.S.); ingrid.fruitier@univ-lr.fr (I.F.-A.)  \n* Correspondence: [lengo.mambu@unilim.fr](lengo.mambu@unilim.fr); Tel.: +33-5-55-43-58-34  \nAbstract: The endolichenic fungus Aspergillus sp. was isolated from the lichen Xanthoparmelia conspersa harvested in France. Aspergillus sp. was grown on a solid culture medium to ensure the large-scale production of the fungus with a sufficient mass of secondary metabolites. The molecular network analysis of extracts and subfractions enabled the annotation of 22 molecules, guiding the purification process. The EtOAc extract displayed an antiproliferative activity of 3.2 ± 0.4 µg/mL at 48 h against human colorectal cancer cells (HT-29) and no toxicity at 30 µg/mL against human triple-negative breast cancer (TNBC) cells (MDA-MB-231) and human embryonic kidney (HEK293) non-cancerous cells. Among the five prenylated compounds isolated, of which four are echinulin derivatives, compounds 1 and 2 showed the most important activity, with IC 50 values of 1.73 µM and 8.8 µM, respectively, against HT-29 cells.  \nKeywords: endolichenic fungi; Aspergillus sp.; human colorectal cancer; chemoresistant cancers  \n1. Introduction  \nAccording to World Health Organization (WHO) reports, cancer constitutes a major health problem [1] . In the human body, healthy cells adhere to a highly regulated pattern of proliferation. Cell division is subject to stringent regulation and continuous monitoring to prevent abnormal proliferation; this constant coordination is essential for the proper functioning of the body. However, cancer cells deviate from these regulations, bypassing the normal controls over cell proliferation due to the deregulation of their division programs. This unchecked proliferation is often associated with the ability of certain cancer cells to migrate from their site of origin, detach, and travel through the bloodstream and lymphatic system. This leads to the invasion of surrounding tissues or even distant parts of the body, forming secondary tumors, a process known as metastasis [2] . Tumors formed by these","cbCaisEWZM53rZxX","https://ap.wps.com/l/cbCaisEWZM53rZxX","pdf",2949147,17,"English","# Introduction\n## Colorectal cancer burden and biology\n## Triple-negative breast cancer and treatment limitations","[{\"question\":\"How were the endolichenic fungus Aspergillus sp. samples obtained and prepared for metabolite production?\",\"answer\":\"Aspergillus sp. was isolated from the lichen Xanthoparmelia conspersa harvested in France. It was then grown on a solid culture medium to enable large-scale production of secondary metabolites.\"},{\"question\":\"What antiproliferative effect did the EtOAc extract show against colorectal cancer cells?\",\"answer\":\"The EtOAc extract displayed antiproliferative activity of 3.2 ± 0.4 µg/mL after 48 h against human colorectal cancer cells (HT-29).\"},{\"question\":\"Which isolated compounds were most active and what were their IC50 values?\",\"answer\":\"Among five prenylated compounds, four were echinulin derivatives. Compounds 1 and 2 showed the strongest activity against HT-29 cells with IC50 values of 1.73 µM and 8.8 µM, respectively.\"}]","In Vitro Antiproliferative Activity of Echinulin Derivatives from Endolichenic Fungus Aspergillus sp. against Colorectal Cancer | PDF",1789981607,43]