{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,31]],"date-time":"2026-01-31T09:13:55Z","timestamp":1769850835603,"version":"3.49.0"},"reference-count":21,"publisher":"MDPI AG","issue":"13","license":[{"start":{"date-parts":[[2020,7,1]],"date-time":"2020-07-01T00:00:00Z","timestamp":1593561600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/100000060","name":"National Institute of Allergy and Infectious Diseases","doi-asserted-by":"publisher","award":["AI125657"],"award-info":[{"award-number":["AI125657"]}],"id":[{"id":"10.13039\/100000060","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000001","name":"National Science Foundation","doi-asserted-by":"publisher","award":["1453287"],"award-info":[{"award-number":["1453287"]}],"id":[{"id":"10.13039\/100000001","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Mosquito-transmitted Plasmodium parasites cause millions of people worldwide to suffer malaria every year. Drug-resistant Plasmodium parasites and insecticide-resistant mosquitoes make malaria hard to control. Thus, the next generation of antimalarial drugs that inhibit malaria infection and transmission are needed. We screened our Global Fungal Extract Library (GFEL) and obtained a candidate that completely inhibited Plasmodium falciparum transmission to Anopheles gambiae. The candidate fungal strain was determined as Aspergillus aculeatus. The bioactive compound was purified and identified as asperaculane B. The concentration of 50% inhibition on P. falciparum transmission (IC50) is 7.89 \u00b5M. Notably, asperaculane B also inhibited the development of asexual P. falciparum with IC50 of 3 \u00b5M, and it is nontoxic to human cells. Therefore, asperaculane B is a new dual-functional antimalarial lead that has the potential to treat malaria and block malaria transmission.<\/jats:p>","DOI":"10.3390\/molecules25133018","type":"journal-article","created":{"date-parts":[[2020,7,2]],"date-time":"2020-07-02T05:00:08Z","timestamp":1593666008000},"page":"3018","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":15,"title":["Fungal Metabolite Asperaculane B Inhibits Malaria Infection and Transmission"],"prefix":"10.3390","volume":"25","author":[{"given":"Guodong","family":"Niu","sequence":"first","affiliation":[{"name":"Department of Biological Sciences, Biomolecular Sciences Institute, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yue","family":"Hao","sequence":"additional","affiliation":[{"name":"College of Public Health, South China University, Hengyang, Hunan 421001, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiaohong","family":"Wang","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences, Biomolecular Sciences Institute, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jin-Ming","family":"Gao","sequence":"additional","affiliation":[{"name":"Shaanxi Key Laboratory of Natural Products Chemical Biology, College of Science, Northwest A&amp;F University, Yangling, Shaanxi 712100, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2121-3393","authenticated-orcid":false,"given":"Jun","family":"Li","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences, Biomolecular Sciences Institute, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2020,7,1]]},"reference":[{"key":"ref_1","unstructured":"WHO (2018). World Malaria Report 2017, World Health Organization: WHO. World Malaria Report."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"73","DOI":"10.1016\/j.pestbp.2018.08.007","article-title":"Resistance: A problem without an easy solution","volume":"151","author":"Hemingway","year":"2018","journal-title":"Pestic. Biochem. Physiol."},{"key":"ref_3","first-page":"2553","article-title":"Plasmodium falciparum: Multi-drug resistance","volume":"27","author":"Rout","year":"2019","journal-title":"Chem. Biol. Drug Des."},{"key":"ref_4","doi-asserted-by":"crossref","first-page":"385","DOI":"10.1007\/s00436-018-6175-1","article-title":"Current scenario and future strategies to fight artemisinin resistance","volume":"118","author":"Pasupureddy","year":"2019","journal-title":"Parasitol. Res."},{"key":"ref_5","doi-asserted-by":"crossref","unstructured":"Ouji, M., Augereau, J.M., Paloque, L., and Benoit-Vical, F. (2018). Plasmodium falciparum resistance to artemisinin-based combination therapies: A sword of Damocles in the path toward malaria elimination. Parasite, 25.","DOI":"10.1051\/parasite\/2018021"},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"3805","DOI":"10.1038\/s41467-018-05777-2","article-title":"A high throughput screen for next-generation leads targeting malaria parasite transmission","volume":"9","author":"Delves","year":"2018","journal-title":"Nat. Commun."},{"key":"ref_7","doi-asserted-by":"crossref","first-page":"716","DOI":"10.1128\/AAC.01144-06","article-title":"High-throughput Plasmodium falciparum growth assay for malaria drug discovery","volume":"51","author":"Baniecki","year":"2007","journal-title":"Antimicrob. Agents Chemother."},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"14694","DOI":"10.1038\/srep14694","article-title":"Targeting mosquito FREP1 with a fungal metabolite blocks malaria transmission","volume":"5","author":"Niu","year":"2015","journal-title":"Sci. Rep."},{"key":"ref_9","doi-asserted-by":"crossref","first-page":"20675","DOI":"10.1073\/pnas.1321024110","article-title":"Genome-block expression-assisted association studies discover malaria resistance genes in Anopheles gambiae","volume":"110","author":"Li","year":"2013","journal-title":"Proc. Natl. Acad. Sci. USA"},{"key":"ref_10","doi-asserted-by":"crossref","first-page":"16490","DOI":"10.1074\/jbc.M114.623165","article-title":"Anopheles Midgut FREP1 Mediates Plasmodium Invasion","volume":"290","author":"Zhang","year":"2015","journal-title":"J. Biol. Chem."},{"key":"ref_11","doi-asserted-by":"crossref","first-page":"11960","DOI":"10.1074\/jbc.M116.773564","article-title":"The fibrinogen-like domain of FREP1 protein is a broad-spectrum malaria transmission-blocking vaccine antigen","volume":"292","author":"Niu","year":"2017","journal-title":"J. Biol. Chem."},{"key":"ref_12","doi-asserted-by":"crossref","first-page":"325","DOI":"10.3390\/molecules20010325","article-title":"Asperaculanes A and B, two sesquiterpenoids from the fungus Aspergillus aculeatus","volume":"20","author":"Gao","year":"2014","journal-title":"Molecules"},{"key":"ref_13","doi-asserted-by":"crossref","first-page":"10898","DOI":"10.3390\/molecules190810898","article-title":"Dereplication guided discovery of secondary metabolites of mixed biosynthetic origin from Aspergillus aculeatus","volume":"19","author":"Petersen","year":"2014","journal-title":"Molecules"},{"key":"ref_14","doi-asserted-by":"crossref","first-page":"18414","DOI":"10.1002\/anie.201910200","article-title":"The Biosynthesis of Norsesquiterpene Aculenes Requires Three Cytochrome P450 Enzymes to Catalyze a Stepwise Demethylation Process","volume":"58","author":"Lee","year":"2019","journal-title":"Angew Chem. Int. Ed. Engl."},{"key":"ref_15","doi-asserted-by":"crossref","first-page":"315","DOI":"10.1021\/np9802623","article-title":"Okaramines H and I, new okaramine congeners, from aspergillus aculeatus","volume":"62","author":"Hayashi","year":"1999","journal-title":"J. Nat. Prod."},{"key":"ref_16","doi-asserted-by":"crossref","first-page":"129","DOI":"10.3114\/sim.2007.59.13","article-title":"Diagnostic tools to identify black aspergilli","volume":"59","author":"Samson","year":"2007","journal-title":"Stud. Mycol."},{"key":"ref_17","doi-asserted-by":"crossref","first-page":"161","DOI":"10.1016\/bs.aambs.2017.03.001","article-title":"Diversity, Application, and Synthetic Biology of Industrially Important Aspergillus Fungi","volume":"100","author":"Park","year":"2017","journal-title":"Adv. Appl. Microbiol."},{"key":"ref_18","doi-asserted-by":"crossref","first-page":"1225","DOI":"10.1007\/s00216-009-3081-5","article-title":"Review of secondary metabolites and mycotoxins from the Aspergillus niger group","volume":"395","author":"Nielsen","year":"2009","journal-title":"Anal. Bioanal. Chem."},{"key":"ref_19","doi-asserted-by":"crossref","first-page":"2049","DOI":"10.1021\/np9003883","article-title":"Aspergillusol A, an alpha-glucosidase inhibitor from the marine-derived fungus Aspergillus aculeatus","volume":"72","author":"Ingavat","year":"2009","journal-title":"J. Nat. Prod."},{"key":"ref_20","doi-asserted-by":"crossref","first-page":"303","DOI":"10.7164\/antibiotics.30.303","article-title":"Studies on aculeacin. II. Isolation and characterization of aculeacins B, C, D, E, F and G","volume":"30","author":"Satoi","year":"1977","journal-title":"J. Antibiot."},{"key":"ref_21","doi-asserted-by":"crossref","first-page":"16096","DOI":"10.1021\/jacs.7b10053","article-title":"Total Synthesis of the Sesquiterpenoid Periconianone A Based on a Postulated Biogenesis","volume":"139","author":"Liffert","year":"2017","journal-title":"J. Am. Chem. Soc."}],"container-title":["Molecules"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1420-3049\/25\/13\/3018\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T09:46:07Z","timestamp":1760175967000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1420-3049\/25\/13\/3018"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2020,7,1]]},"references-count":21,"journal-issue":{"issue":"13","published-online":{"date-parts":[[2020,7]]}},"alternative-id":["molecules25133018"],"URL":"https:\/\/doi.org\/10.3390\/molecules25133018","relation":{},"ISSN":["1420-3049"],"issn-type":[{"value":"1420-3049","type":"electronic"}],"subject":[],"published":{"date-parts":[[2020,7,1]]}}}