Abstract
Oleanolic (OA) and ursolic (UA) acids are recognized triterpenoids with anti-cancer properties, showing cell-specific activity that can be enhanced when loaded into polymeric nanoparticles. The cytotoxic activity of OA and UA was assessed by Alamar Blue assay in three different cell lines, i.e., HepG2 (Human hepatoma cell line), Caco-2 (Human epithelial colorectal adenocarcinoma cell line) and Y-79 (Human retinoblastoma cell line). The natural and synthetic mixtures of these compounds were tested as free and loaded in polymeric nanoparticles in a concentration range from 2 to 32 µmol/L. The highest tested concentrations of the free triterpene mixtures produced statistically significant cell viability reduction in HepG2 and Caco-2 cells, compared to the control (untreated cells). When loaded in the developed PLGA nanoparticles, no differences were recorded for the tested concentrations in the same cell lines. However, in the Y-79 cell line, a decrease on cell viability was observed when testing the lowest concentration of both free triterpene mixtures, and after their loading into PLGA nanoparticles.
Highlights
Pentacyclic triterpenes are known for their multiple pharmacological properties [1,2,3], which are attributed to their resemblance to biogenesis to steroids in the cyclization of squalene
Resomer® RG756 S [poly (d,l-lactide-co-glycolide) acid (PLGA)] of 98,000 Da of molecular weight (MW) and 75/25 molar ratio of lactide/glycolide was a kind gift from Boehringer (Ingelheim, Germany)
All other reagents were of analytical or high-performance liquid chromatography (HPLC) grade obtained from Fisher Scientific (Leicestershire, UK)
Summary
Pentacyclic triterpenes are known for their multiple pharmacological properties [1,2,3], which are attributed to their resemblance to biogenesis to steroids in the cyclization of squalene. In the present work, selected pentacyclic triterpenes have oleanane and ursane based structures, i.e., the oleanolic acid (OA) (of chemical name: 3β-3-hydroxyolean-12-en-28-oic acid) and its isomer, ursolic acid (UA) (of chemical name: 3β-3-hydroxyurs-12-en-28-oic acid). Due ttooththeeirirsismimilailrarchcehmemicaiclal strsutrcutcutruer,et,htehbeiboilolgoigciaclaalcatcivtiivtyityanadndthtehrearpaepuetuicticinitnetreersetsot foOf OAAanadndUUAAaraererartahtehresrimsimilailra, rw, whihchichisis hihgihglhylryerlaetleadtetdottohtehireidrodsoes-ed-edpeepnednednetnctyctyototxoicxiitcyitpyrporfiolefil[e6][.6]P.rPerveivoiuosusstustduidesiehsahvaevsehsohwown tnhtahtatthtehseese trittreitreprepneenseesxehxihbiibteitdedcyctyottootxoixcictyityininsesveevrearlatlytpyepseosfocfacnacnecrecrecllellinliense[s6–[68–].8]B. eBseidsiedsetsatragregteintigngtutmumoror cecllesllbs ybyinidnudcuticotinonofoafpaoppotpotsois,iso,loealenaonloicliacnadndurusrosloicliaccaidcisdaslsaolsommodoudluatlaetethtehteutmumoroernevnivroirnomnmenetnt exehxihbibtiintignganantitainanggioioggenenicicaannddaannttii--iinnflflaammmmaattoorryy activities, ttooggeetthheerrwwitihthanatniotixoixdiadnatnetffeeffcetsctasnadncdell cedllifdfeiffreenretinattiiaotnio(ne.(ge..,g[.3, ][)3.]A). sAthsetheeffeicffiaccyacoyf oefacehacshinsginleglceomcopmopuonudnmd imghigt hdtifdfeiffr ewr iwthitrhesrpesepctecttottohe thiediednetniftiiefidedbiboiaocatcivtivtiietsie, st,htehecocommbbininataitoinonoofftthheessee ssuubbssttaanncceess in aa ssiinngglleeddoossaaggeefoformrmmmigihgthht ahvaeve sysnyenregrigstiisctiecffeefcfetsctisnitnhtehteretaretmatemnet notf ocfancacnerce[r9][.9]
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