Ayaz, FatmaKüçükboyacı, NurgünGören, Nezhun AtesÇalış, İhsanUlukaya, EnginDuman, Hayri̇ D.Choudhary, Mohammed Iqbal2024-01-092024-01-092018-12-21Aydınlık, Ş. vd. (2018). "Bioassay-guided isolation of cytotoxic compounds from Chrysophthalmum montanum (DC.) Boiss". Journal of the Nepal Medical Association, 125, 10-20.0278-69151873-6351https://doi.org/10.1016/j.fct.2018.12.029https://www.sciencedirect.com/science/article/pii/S0278691518309025?via%3Dihubhttps://hdl.handle.net/11452/38871Bioassay-guided isolation of the 80% methanol extract of the aerial parts of Chrysophthalmum montanum (DC.) Boiss. (Asteraceae) led to the isolation of four known guaianolide-type sesquiterpene lactones, 6 alpha-acetoxy-4 alpha-hydroxy-113H-guaia-9.11(13)-dien-12.8a-olide (1), 6 alpha-acetoxy-4 alpha-hydroxy-9 beta.10 beta-epoxy-1 beta H-guaia-11(13)-en12.8 alpha-olide (2), 4 alpha,6 alpha-dihydroxy-1 beta H,5 alpha,7 alpha H-guaia-9(10),11(13)-dien-12,8 alpha-olide (3), and (4 alpha,5 alpha,8 beta,10 beta)-4,10-dihydroxy-1,11(13)-guaidien-12,8-olide (4), along a steroidal glycoside mixture (5a and 5b). The structures of the compounds were identified on the basis of spectroscopic data. Among them, 2, 4 and a steroidal glycoside mixture were obtained from C. montanum for the first time. All isolates were also first time assayed for in vitro cytotoxicities against four human cancer cell lines, i.e. breast (MCF-7, MDA-MB 231), colon (FIT-29), and lung (PC3). Among the isolates, 1-3 showed significant inhibitory effect on the proliferation of cancer cells with viability ranging from 6.86 to 26.51%, while steroidal glycoside mixture showed no cytotoxicity, except against HT-29 (viability 61.99%). Compound 4 exhibited strong and selective cell growth inhibition against HT-29 with viability 20.99% and was identified as a promising compound with high selectivity between cancer cells and normal human lung cells (SEAS-2B), especially against HT-29 (IC50 = 12.2 pg/mL) compared to that of cisplatin. These results suggested that 4 is worthy of further study to determine its cytotoxicity mechanisms.eninfo:eu-repo/semantics/closedAccessAsteraceaeSteroidal glycosidesChrysophthalmum montanumSesquiterpene lactonesCytotoxicityHT-29 colon cancer cell lineSesquiterpene lactonesPlantsConstituentsInuleaeAsteraceaeExtractsGuaianolidesFood science & technologyToxicologyAntineoplastic agents, phytogenicAsteraceaeBiological assayCell line, tumorDrug screening assays, antitumorHumansPlant components, aerialSpectrum analysisArticle0004633050000022-s2.0-85059058009102012530580030Food science & technologyToxicologyInula; Asteraceae; Dittrichia ViscosaAntineoplastic activityArticleAsteraceaeBeas-2b cell lineBioassayCancer inhibitionCell proliferationCell viabilityChrysophthalmum montanumControlled studyDrug cytotoxicityDrug mechanismDrug structureHt-29 cell lineIc50In vitro studyLung alveolus cellMcf-7 cell lineMda-mb-231 cell lineNonhumanSpectroscopyStructure analysisAerial plant partChemistryDrug screeningHumanIsolation and purificationProceduresTumor cell line(4 alpha 5 alpha 8 beta 10 beta) 4,10 dihydroxy 1,11(13) guaidien 12,8 olide(4 alpha 5 alpha 8 beta) 4,10 dihydroxy 1,11(13) guaidien 12,8 olide4 alpha, 6 alpha dihydroxy 1 beta, 5 alpha, 7 alpha h guaia 9(10),11(13) dien 12,8 alpha olide6 alpha acetoxy 4 alpha hydroxy 1 beta h guaia 9,11(13) dien 12,8 alpha olide6 alpha acetoxy 4 alpha hydroxy 9 beta, 10 beta h guaia 9,11(13) dien 12,8 alpha olideAntineoplastic agentCisplatinCytotoxic agentSitoglusideSitosterol 3 o beta glucopyranosideUnclassified drugAntineoplastic agent