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Light-activated ruthenium (II)-bicalutamide prodrugs for prostate cancer.

PMID: 31054419
Journal of Inorganic Biochemistry 196 (2019) 110684 ContentslistsavailableatScienceDirect Journal of Inorganic Biochemistry journal homepage: www.elsevier.com/locate/jinorgbio Light-activated ruthenium (II)-bicalutamide prodrugs for prostate cancer T Jian Zhaoa, Nannan Liua, Shuchen Suna, Shaohua Goua,⁎ , Xinyi Wanga, Zhimei Wanga, Xiaoyan Lib, Wenjing Zhangb,⁎ aResearchCenterandSchoolofChemistryandChemicalEngineering,andJiangsuProvinceHi-TechKeyLaboratoryforBiomedicalResearch,SoutheastUniversity, Nanjing211189,China bTheCollegeofChemistryandMolecularEngineering,ZhengzhouUniversity,Zhengzhou,HenanProvince450001,China ARTICLE INFO ABSTRACT Keywords: Targeteddeliveryofclinicallyapprovedanticancerdrugtotumorsitesisaneffectivewaytoachieveenhanced Ruthenium(II)complexes drugefficacyaswellasreducedsideeffectsandtoxicity.HerebicalutamideiscagedbytheRu(II)centerthrough Photoactivatedchemotherapy thenitrilegroup,andthreephotoactiveRu(II)complexesweredesignedandsynthesized.Dockingstudyshowed Bicalutamide that the ruthenium(II)fragmentscaneffectively blockthebinding of complexes1–3 with AR(androgenre- Anticancer ceptor)owingtothelargestericstructures,thusbicalutamideincomplexes1–3couldnotinteractwithAR-LBD (ligandbindingdomain).Onceirradiationwithbluelight(465nm),complexes1–3canreleasebicalutamideand anticancerRu(II)fragments,whichpossessesdual-actionofARbindingandDNAinteractionsimultaneously.In vitrocytotoxicitystudyonthesecomplexesfurtherconfirmedthatcomplexes1–3exhibitedconsiderablecy- totoxicityuponirradiationwithbluelight.Significantly,complex3couldbeactivatedat660nm,whichgreatly increasesthescopeofcomplex3totreatdeeperwithintissue.Theoreticalcalculationsshowedthatthelowest singletexcitationenergyofcomplex3islowerthanthoseofcomplexes1–2,whichexplainstheexperimental resultswell.Moreover,the3MC(metalcentered)statesofthesecomplexesaremorestablethantheir3MLCT (metaltoligandchargetransfer)states,indicatingthatthephotoactiveprocessesofthesecomplexesarelikelyto resultinliganddissociation. 1. Introduction which enables maximum tissue penetration with minimum damage [29,37–40]. Recently, ruthenium-based PACT agents with high se- Prostatecancerisoneoftheleadingcausesofcancerdeathformen lectivityandlowtoxicityhavebeenattractingmuchattention[41–44], worldwide [1]. The development and growth of prostate cancer is as they can be used to deliver a wide variety of bioactive molecules, found to be initially dependent on androgens, and androgen receptor including enzyme inhibitors, neurotransmitters and so on [45–53]. A (AR)islargelyinvolvedintheprogressionofthiscancer[2,3].There- majority of clinically approved anticancer drugs are small molecular fore,therapeuticstrategiesbyregulatingtheARactivitycaneffectively compounds. Their efficacy has been well studied and established. lead to a reduction of prostate cancer [4–9]. Because AR is widely However,thesecompoundstendtohavewidebiodistributionsamong distributed in the human tissues, including the prostate and seminal various tissues after intravenous administration, which may result in vesicles, skin, cardiac muscle, adrenal cortex, liver, and so on [10]. widespread systemic toxicity and suboptimal efficacy. Thus, targeted Thus,improvingtheselectivityandactivityoftheARantagonistarethe delivery of clinically approved anticancer drugs to tumor sites is an keypointsforthetreatmentofprostatecancer. effective way to achieve enhanced drug efficacy and to reduce side Photoactivated chemotherapy (PACT) is a promising strategy for effectsandtoxicity. tumortargeteddelivery[11–19],whichcanbetriggeredbyirradiation Inthisstudy,bicalutamide,themostwidelyusedARantagonistin toreleasetheactivespecieswithinthetumor[20–32].Generally,such clinic, is chosen to coordinate to ruthenium(II) fragments through its agentsasprodrugsarekineticallyinertandnontoxicintheabsenceof nitrilegroupwhichwasreportedasanimportantbioactive“warheads” light, but rapidly give rise to toxic effects upon photoexcitation often engaging in key hydrogenbonding interaction with protein tar- [33–36].Anidealcandidateforaphotoactivatableagentshouldhave gets [54]. Although the nitrile groups are widely present in medical the ability to be activated in the “therapeutic window”, 600–850nm, agents,onlyafewstudiesregardingthecagingofthebioactivenitriles ⁎Correspondingauthors. E-mailaddresses:sgou@seu.edu.cn(S.Gou),zhangwj@zzu.edu.cn(W.Zhang). https://doi.org/10.1016/j.jinorgbio.2019.03.024 Received14January2019;Receivedinrevisedform25March2019;Accepted28March2019 Available online 30 March 2019 0162-0134/ © 2019 Elsevier Inc. All rights reserved. J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 Fig.1.Chemicalstructuresofcompoundsstudied. throughRu(II)coordinationhavebeenreported[55–59].Herein,three whereascomplex3presentedobviouschangesunderthesamecondi- light-activated ruthenium(II) complexes were designed, synthesized tion, confirming that complex 3 could be activated in the PDT (pho- and biologically evaluated as potential PACT agents (Fig. 1). Ex- todynamictherapy)therapeuticwindow(Fig.S11).Thequantumyields pectedly, the designed compounds can rapidly release bicalutamide ofthefirststepofcompounds1–3werefoundtobe0.021,0.022and upon irradiation at the tumor site and leave the diaquaruthenium(II) 0.019inthesametestcondition(465nm),respectively.Thephotolysis moiety to interact with DNA, exhibiting dual-actions against prostate of complexes 1 and 3 was further confirmed by 1H NMR as well. cancercells. Complex1wasstableunder660nmirradiation,however,itunderwent liganddissociationwithirradiationat465nm(Fig.S12).Unlikecom- 2. Resultsanddiscussion plex1, spectralchangeswere observedforcomplex3after15minof irradiationat660nm,whichisconsistentwiththeUV–Visresults(Fig. 2.1. Synthesisandcharacterization S13). Complexes1–3werepreparedbyrefluxingamixtureofcis-RuL2Cl2 2.3. Theoreticalcalculations (L=2,2′-bipyridine, 1,10-phenanthroline and 2,2′-biquinoline), bica- lutamide (4.0equiv) and silver(I) hexafluorophosphate (2.4equiv) in Theoretical calculations were performed to gain further under- ethanol.Thetargetcomplexeswerecharacterizedby1Hand13CNMR standing of the photolysis of complexes 1–3. TDDFT (time-dependent spectroscopy,electrosprayionizationmassspectrometry(ESI-MS)and density functionaltheory)calculationsshowedthat thelowest-energy elemental analysis (Figs. S1–9). The ESI-MS diagrams of compounds excitedsingletstatesofcomplexes1–3are1MLLCT(MLLCT=metal- 1–3 showed the highest isotope at 637.06, 661.06 and 737.14, re- ligand-to-ligandchargetransfer)transitionsduetothecontributionsof spectively, corresponding to the dication of [RuL2(bicalutamide)2]2+. bicalutamide(Fig.3)[62],andthecorrespondingexcitationenergiesof Moreover,1Hand13CNMRspectraaswellaselementalanalysiswere complexes 1–3 are 2.76eV (449nm), 2.91eV (427nm) and 2.25eV in good conformity with the proposed molecular structures of com- (551nm),respectively(TableS1),whichisinaccordwiththeexperi- plexes1–3.ThelogPOW(theoctanol-waterpartitioncoefficient)values mental results that the absorption tail of complex 3 terminates at re- of the ruthenium(II) complexes were measured using the shake-flask latively longer wavelength as compared with complexes 1–2. More method, which were −0.46, −0.28 and −0.19 for complexes 1–3, intense absorption bands indicating the MLLCT transitions are pre- respectively. The stabilityofcomplexes1–3wasevaluatedbyUV–vis dicted at 320nm (f=0.0476), 341nm (f=0.0420) and 478nm spectral analysis at different times (Fig. S10) [60,61]. No detectable (f=0.0517) for complexes 1–3, respectively,which also corresponds changesoftheabsorptionbandsofcomplexes1and2havebeenob- wellwiththeexperimentalresults. served within 15h, while tiny changes were observed for complex 3, Itisgenerallyacceptedthatthecomplexesarefirstexcitedbythe demonstratingthatcomplexes1and2weremorestablethancomplex desiredwavelengthoflightandthenundergointersystemcrossinginto 3. However, the changes of the absorption bands of complex 3 were a 3MLCT state, followed by internal conversion to a dissociative 3MC verysmall,indicatingthatnegligiblehydrolysiswashappenedduring stateandreleaseofthebicalutamide.Thus,twolow-lyingtripletstates thetesttime. of complexes 1–3 were optimized, corresponding to the 3MLCT and 3MC states (spin density surfaces). The 3MC states of complexes 1–3 2.2. Photolysisstudy corresponds to five-coordinate structures with a bicalutamide dis- sociatedfromtheRucenter.Notably,therelativeenergiesof3MCstates The photolysis of complexes 1–3 in 98% H2O/2% MeOH was stu- ofcomplexes1–3are0.35eV,0.45eVand0.28eVbelowtheir3MLCT died under irradiation with blue light (465nm) by using UV–Vis stats, respectively, indicating that the photoactive process of these spectroscopy. UV–Vis spectral changes were obviously observed for complexesismorelikelytoresultinliganddissociation[63,64]. these complexes after irradiation (Fig. 2). The metal-to-ligand charge transfer (MLCT) bands at 336nm and 359nm for complexes 1 and 2 2.4. Dockingstudy were graduallyreplacedby newMLCTbands at490nmand 480nm, respectively.Forcomplexes1and2,noisosbesticpointwasobserved, Inordertoevaluatethelikelihoodofcomplexes1–3bindingtothe indicatingthatthedissociationreactionwasmorethanonestep.Asfor androgen receptor, a docking study with crystal structure of AR-LBD complex 3, the initial MLCT was observed at λmax=515nm, which (ligand binding domain) (PDB: 1z95) was performed [65]. Bicaluta- showed bathochromic shift compared to complexes1 and 2 [44], de- midewasfirstlydockedwiththeAR-LBD,whichwassituatedinsidethe monstrating that the application of biquinoline in complex 3 can de- bindingpocketofARandshowedgoodoverlapwiththeco-crystallized crease the energy gap between the d-orbital of Ru(II) and the lowest bicalutamideintheARcrystalstructure,provingthatthemethodused unoccupied molecular orbital (LUMO) levels of the ligand. Moreover, issuitablefordockingstudy(Figs.4a,S16a).However,complexes1–3 complexes 1–3 were studied with irradiation at longer wavelength. werefoundtobesituatedonthesurfaceoftheprotein(Figs.4b,S16b, Neither1nor2showedanybandchangesuponirradiationat660nm, c), which could not enter theligand binding pocket ofAR due tothe 2 1.0 0.5 ↑ 0.0 300 400 500 600 700 largestericstructuresofthecomplexes.Moreover,theinteractionen- bicalutamide as a positive control. According to the IC50 values ergies of these complexes with AR were also calculated. As shown in (Table 1), bicalutamide showed moderate cytotoxicity against LNCaP Table S2, the binding energy of the bicalutamide molecule was cells with an IC50 value of 45.0μM, which was not affected by irra- −9.61kcal/mol,whichwasmuchlowerthanthoseofcomplexes1–3, diation.Complexes1–3werefoundtobelesscytotoxicinthedarkthan indicating that the ruthenium(II) fragments decreased the binding af- bicalutamide against LNCaP cells. However, the antiproliferative ac- finityofbicalutamidewithAR.Takentogether,thisstudyindicatedthat tivities of complexes 1–3 were greatly improved upon irradiation at theruthenium(II)fragmentsofcomplexes1–3caneffectivelyblockthe 465nm with PI (phototoxicity index: the toxicity in the dark vs. the binding of bicalutamide with AR owing to their large sizes, implying light) values of 9.6, 5.3 and 7.7, respectively. The ability of these thatcomplexes1–3wouldbebiologicallyinactiveprecursors. complexes activated by red light (660nm) was much attractive, be- causelongerwavelengthsoflightcanpenetratedeeperintothetissue withlessnormal-tissuedamage.Thecytotoxicityofcomplexes1and2 2.5. ARbindingaffinity greatly decreased upon irradiation at 660nm compared with irradia- tionat465nm,whilethatofcomplex3wasslightlydecreasedwithaPI TheARbindingaffinityofcomplexes1–3weredeterminedbythe valueof5.8.AsforPC-3cells(AR-),bicalutamideshowednoapparent fluorescence polarization based binding assay. According to the IC50 activity, exhibiting that the cytotoxicity of bicalutamide is dependent values(Fig.4c,TableS3),complexes1–3showednegligibleARbinding on the expression of AR. In addition, complexes 1–3 had negligible affinity in the dark. In contrast, significant AR binding affinity was cytotoxicity with or without irradiation (Table S4). Taken together, observed forcomplexes1–3uponirradiationat465nm.Notably,the complexes1–3asconfirmedcouldbeactivatedbylight,whichshowed IC50valueofcomplex2waslowerthanthatofbicalutamide,demon- considerable cytotoxicity against AR+ LNCaP cells. Especially, com- strating that more than one equiv of bicalutamide was released from plex3couldbeactivatedbyredlightthatisknowntopenetratetissue complex 2. With irradiation at 660nm, the binding affinity of com- deeper. plexes1and2wasgreatlyweakened,whilecomplex3maintainedthe AR binding affinity with an IC50 value of 9.2μM. The result further indicated that complexes 1–3 are biologically inactive precursors, 2.7. DNAinteraction whichcouldbeactivateduponirradiationwithlight. The interaction of DNA with complex 3 was monitored by tapping 2.6. Invitrocytotoxicity modeatomicforcemicroscopy(AFM)[67].TheimageofpBR322DNA withoutrutheniumcomplexesisshowninFig.5a.Theaverageheightof The cytotoxicity and photocytotoxicity of complexes 1–3 were theDNAwas1.0nm(n=15).Whencomplex3wasaddedtothesolution evaluatedagainstAR-negativePC-3andAR-positiveLNCaPcellswith of DNA, no obvious morphological changes were observed. Once sbA (a) (b)1.5 ↓ 1.0 ↓ 0.5 ↑ 0.0 300 400 500 600 700 Wavelength (nm) sbA 0.4 0.3 0.2 ↑ ↓ ↓ 0.1 0.0 400 500 600 700 800 Wavelength (nm) sbA J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 (c) Wavelength (nm) Fig. 2.Electronic absorptions of a) complex 1, b) complex 2, c) complex 3 (25μM, 98% H2O/2% MeOH) upon irradiation with blue light (λirr=465nm, tirr=40min,10mWcm−2)every2min. Fig. 3.Relative energies of the 1MLLCT, 3MLCT and 3MC states for complexes 1–3, electron density difference maps (EDDMs) of the lowest-lying singlet transitions (yellow in- dicatesadecreaseinchargedensity,whileorangeindicatesan increase)andspindensityofT1and3MCstatesforthecom- plex 3. Both EDDMs and spin density were plotted by the GaussView (version 5.0) program, and those for complexes 1–2weregiveninFigs.S14–S15. 3 J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 Fig.4.Dockingstudiesofbicalutamideandcomplex 3 with AR-LBD (PDB: 1z95) using Autodock 4.2 [66].(a)Thedockingmodelofbicalutamideand(b) complex3withAR,yellowdashlinesrepresentthe H-bondinteractionbetweenbicalutamideandcom- plex3withAR;(c)ARbindingaffinityofcomplexes 1–3andbicalutamidewithorwithoutlightirradia- tion. Table1 staining and flow cytometry assay. As shown in Fig. 7, when LNCaP IC50values(μM)andphotoselectivityindexes(PI)ofcomplexes1–3inLNCaP cells were treated with Ru(II) complexes upon irradiation at 465nm, cells. the typical morphological changes of cell apoptosis such as cell Compound IC50(μM) PIa IC50(μM) PIa shrinkageandchromatincondensationwereobserved,whilenucleiof thecellsretainedtheregularroundcontoursinthedark,indicatingthat Dark 465nm 660m Ru(II) complexescausedlittlecell apoptosiswithout lightirradiation. Theresultswerefurtherexaminedbyflowcytometryassay.Underdark 1 85.7±4.8 8.9±0.6 9.6 75.3±3.8 1.1 conditions, the apoptoticrates ofLNCaP cells treated withcomplexes 2 71.4±2.5 13.6±1.9 5.3 68.5±4.5 1.0 3 91.9±5.7 11.9±1.2 7.7 15.8±1.7 5.8 1–3 were 16.51%, 15.9%, and 14.42%, respectively, which were Bicalutamide 45.0±4.9 42.3±3.4 1.0 47.4±2.1 1.0 slightlyincreasedascomparedwiththatoftheuntreatedcells(6.01%). Onceirradiationwasconducted(465nm),theapoptoticratesinduced a PI=darkIC50value/lightIC50value. bycomplexes1–3weresignificantlyincreasedincontrasttothedark group, which ranged from 70.29% to 72.56%. Particularly, when irradiationwasconducted(465nmor660nm),theformationofreticular complex 3 was irradiated with 660nm, the apoptotic rate reached structures was observed. This suggested that complex 3 with light irra- 67.84%whichwasmuchhigherthanthecontrol(9.01%)(Fig.S17). diationinducedcrosslinkingbetweenDNAmoleculesbyabridgingeffect, whicharepresumablyattributedtoDNAcovalentbindingeffect. 3. Conclusions 2.8. Gelelectrophoresisstudy Ruthenium(II) polypyridyl complexes are a kind of promising photo-triggereddrugdeliverysystem,whichofferspatialandtemporal The ability of complex 3 to bind DNA upon light activation was controloverthereleaseofthebioactivedrugs.Herein, furtherdeterminedbygelelectrophoresiswithpBR322plasmidDNA. three light-activated Ru(II)-bicalutamide prodrugs were designed AsshowninFig.6,adecreaseintherateofmigrationforclosedcircular andsynthesized,whichpossessbothARbindingandDNAinteraction DNA (form I) wasobserved upon 465nmand 660nmirradiation,in- actions.Dockingstudiesshowedthatthesecomplexescouldnotenter dicating the covalent binding of complex 3 with pBR322 DNA. How- theligandbindingpocketofARduetothelargestericstructuresofthe ever,nomigrationwasobservedforcomplex3inthedark.Moreover, Ru(II) fragments, implying that they would be biologically inactive theplasmidDNAgraduallydisappearedwithincreasingconcentrations precursors.However,whenirradiatedwithbluelight(465nm),these ofcomplex3,indicatingthatcomplex3inhibitedtheintercalationof complexescouldreleasebothbicalutamideandanticancerRu(II)frag- EtBrinplasmidDNAathighconcentrations.Thisstudyindicatesthat mentstoinhibitthegrowthofcancercellsviadifferentmodesofaction. complex3cancovalentlybindtoDNAuponirradiation. Invitrocytotoxicitystudyconfirmedthatcomplexes1–3couldbeac- tivated upon photoexcitation with blue light, exhibiting considerable 2.9. Apoptosisstudy cytotoxicity against the LNCaP (AR+) cells. Significantly, the antic- ancer activity of complex 3 was also retained when irradiated by red ThepotentialofthesecomplexestoinduceapoptosisinLNCaPcells light (660nm), hintingthat complex 3could be activatedin thePDT wasperformedunderlightanddarkconditionsbyHoechst33342DNA therapeutic window. Theoretical calculations showed that the singlet 4 J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 Fig.5.AFMimagesofpBR322plasmidDNAinHEPES(N-2- hydroxyethylpiperazine-N′-2-ethanesulfonic acid) buffer ad- sorbedonpeeledmica:(a)imagesofpBR322plasmidalone; (b) incubated with complex 3 in dark; (c) incubated with complex3uponirradiationat465nm;and(d)incubatedwith complex3uponirradiationat660nm. 4. Materialsandmethods 4.1. Materialsandinstrument All chemicals and solvents were of analytical reagent grade and used without further purification. Bicalutamide was obtained from AladdinasaracemicmixtureoftheRandSenantiomersandusedas received. Cis-RuL2Cl2 (L=2,2′-bipyridine, 1,10-phenanthroline and 2,2′-biquinoline)werepreparedaccordingtopreviousreports[37,68]. 1H and 13C NMR spectra were measured on Bruker Avance III-HD 600MHz spectrometer. UV–Vis spectra and kinetic traces were re- corded on a Shimadzu UV2600 instrument. Mass spectra were mea- suredbyanAgilent6224ESI/TOFMS(electrospray-ionizationtime-of- flightmassspectrometry)instrument.ElementalanalysisofC,H,andN used a Vario MICRO CHNOS elemental analyzer (Elementar). Cancer cells were obtained from Jiangsu KeyGEN BioTECH company(China). Cell apoptosis experiments were measured by flow cytometry (FAC Scan,BectonDickenson)andanalyzedbyCellQuestsoftware. 4.2. Preparationofcompounds Fig.6.GelelectrophoreticmobilitypatternofpBR322plasmidDNAincubated withvariousconcentrationsofcomplex3.Lane1–8(0,10,20,40,80,160,320, Generalprocedureforsynthesisofcomplexes1–3.Amethanolso- 640μM)+DNA.a)dark;b)irradiationat465nmfor;c)irradiationat660nm. lution (50mL) of RuL2Cl2 (0.20mM), AgPF6 (0.12g, 0.48mM) and bicalutamide (0.34g, 0.8mM) was heated at reflux for 12h in the excited energy of complex 3 is lower than those of complexes 1–2, absenceoflight.ThenthesolutionwasfilteredtoremoveAgClandthe which can explain the experimental results well. Moreover, the 3MC reaction mixture was concentrated to 5mL. The crude product was states of these complexes are more stable than their 3MLCT state, in- collected and recrystallized from methanol. Complexes 1–3 were iso- dicating that the photoactive processes of these complexes are more latedasracemicmixtures(seesupportingFig.S18). likelytocauseligand dissociation.Inall,ourstudyindicatedthatca- Complex1.Yield:0.16g(50.6%).Dark-redpowder.Anal.Calcd(%) ging of bicalutamide through its nitrile group is an efficient way to forC56H44F20N8O8P2RuS2:C43.00,H2.84,N7.16.Found:C43.09,H increasingitsselectivity.Therefore,photocagingofclinicallyapproved 2.88,N7.08;ESI-MS:m/z[M/2–PF6]+=637.06;1HNMR(600MHz, anticancer drugs using ruthenium(II) polypyridyl complexes is an ef- DMSO‑d6)δ1.38(s,6H),3.72(s,1H),3.74(s,1H),3.90(s,1H),3.93(s, fectivewaytodiscovernewclinicalagents. 1H), 6.46 (m, 2H), 7.36–7.39 (t, 4H, J=8.8Hz), 7.48–7.51 (t, 2H, 5 Control Complex 1 Complex 2 Complex 3 Bicalutamide Control Complex 1 Complex 2 Complex 3 Bicalutamide (b) Control Complex 1 Complex 2 Complex 3 Bicalutamide AnnexinV-FITC Control Complex 1 Complex 2 Complex 3 Bicalutamide J=6.7Hz), 7.78–7.79 (d, 2H, J=5.4Hz), 7.90–7.92 (m, 4H), 2.96,N6.37;ESI-MS:m/z[M/2–PF6]+=737.14;1HNMR(600MHz, 8.00–8.02(t,2H,J=6.5Hz),8.16–8.19(t,2H,J=7.9Hz),8.26(m, CD3OD)δ1.30(s,6H),3.45(s,1H),3.47(s,1H),3.85(s,1H),3.89(s, 4H),8.36(m,2H),8.45–8.48(m,2H),8.80–8.82(d,2H,J=8.2Hz), 1H), 6.77–6.84 (m, 4H), 7.04–7.08 (m, 4H), 7.44–7.46 (t, 2H, 8.93–8.94 (d, 2H, J=8.3Hz), 9.48–9.49 (d, 2H, J=5.4Hz), 10.44 J=7.4Hz), 7.77–7.80 (m, 4H), 7.86–7.87 (d, 2H, J=7.9Hz), (m, 2H) ppm; 13C NMR (150MHz, DMSO‑d6) δ 16.97, 26.47, 56.94, 7.91–8.00(m,10H),8.09–8.10(m,2H),8.28–8.30(d,2H,J=8.0Hz), 63.60,73.22,100.81,115.66,115.81,117.46,121.29,122.41,122.48, 8.34–8.36(m,4H),8.69–8.70(d,2H,J=8.6Hz),9.62(m,2H)ppm; 123.10, 123.74, 124.09, 127.10, 128.05, 131.36, 131.43, 133.52, 13C NMR (150MHz, CD3OD) δ 26.43, 53.41, 63.51, 73.14, 100.64, 133.73, 136.87, 136.89, 137.12, 138.64, 138.97, 143.69, 151.71, 115.61, 115.76, 117.37, 118.84, 120.05, 121.00, 122.45, 122.81, 153.43,157.00,157.73,164.90,166.58,173.98ppm. 123.42, 127.51, 128.87, 129.09, 129.70, 130.00, 131.33, 131.40, Complex2.Yield:0.17g(52.3%).Dark-redpowder.Anal.Calcd(%) 133.05, 133.27, 133.83, 136.74, 137.06, 140.05, 140.71, 143.88, forC60H44F20N8O8P2RuS2:C44.70,H2.75,N6.95.Found:C44.79,H 149.17,150.43,160.36,160.59,164.85,166.53,173.86ppm. 2.74,N6.86;ESI-MS:m/z[M/2–PF6]+=661.06;1HNMR(600MHz, CD3OD)δ1.32(s,6H),3.46(s,1H),3.49(s,1H),3.86(s,1H),3.89(s, 1H), 5.38 (m, 1H), 7.07–7.10 (m, 4H), 7.49–7.52 (d-d, 2H, J=5.3, 4.3. LogPOWdetermination 2.8Hz), 7.79–7.81 (m, 4H), 7.89–7.94 (m, 4H), 7.98–7.99 (d, 2H, J=8.7Hz), 8.03–8.04 (m, 2H), 8.15–8.16 (d, 2H, J=8.9Hz), ThelogPOWdeterminationofcomplexes1–3wasperformedusing 8.23–8.26 (m, 2H), 8.28–8.29 (d, 2H, J=8.9Hz), 8.50–8.52 (d, 2H, the shake-flaskmethod. An excess ofcomplexes1–3 wasdissolved in J=8.2Hz), 8.88–8.89 (m, 2H), 9.83–9.84 (d, 2H, J=5.1Hz) ppm; double-distilled water presaturated with n-octanol for 24h at 37°C. 13C NMR (150MHz, CD3OD) δ 26.45, 63.57, 73.19, 100.81, 115.63, Thesolutionwasfilteredtoremoveundissolvedrutheniumcomplexes. 115.79, 117.32, 121.04, 122.40, 122.62, 125.46, 126.59, 127.67, Subsequently,thesolutionwasaddedtoanequalvolumeofn-octanol 127.89, 130.77, 131.11, 131.34, 131.40, 133.41, 133.62, 136.87, (presaturatedwithwater).Theheterogeneousmixturewasshakenfor 137.04, 137.51, 137.95, 143.59, 147.71, 148.18, 152.77, 154.52, 2h before centrifuging for 15min to achieve phase separation. The 164.87,166.56,173.93ppm. initialandfinalconcentrationsofcompoundsinanaqueousphasewere Complex3.Yield:0.22g(61.3%).Dark-redpowder.Anal.Calcd(%) determined by the UV–vis spectrum method, and the water-octanol forC72H52F20N8O8P2RuS2:C49.01,H2.97,N6.35.Found:C49.12,H partitioncoefficients(logPOW)werecalculated. IP AnnexinV-FITC IP J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 (a) 20 μm 20 μm 20 μm 20 μm 20 μm 20 μm 20 μm 20 μm 20 μm 20 μm (c) (d) Fig.7.CellapoptosisinductiononLNCaPcellsaftertreatmentwithcomplexes1–3andcisplatinat30μM:morphologicalchangeswithHoechst33342stainingin theabsence(a)andpresencebluelight(b);FlowcytometryanalysisforapoptosisofLNCaPcellsintheabsence(c)andpresencebluelight(d). 6 J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 4.4. Photolysisstudy first and then diluted to 0.5mM with hepes buffer (the final con- centration of DMF was less than 0.4%). The solutions of complex 3 Photolysisofcomplexes1–3wasrecordedonaShimadzuUV2600 (20μL)andpBR322(20μL)weremixturetogether,andirradiatedwith instrument equipped with a thermostatically controlled cell holder. blue light (465nm, 30min) or red light (660nm, 1h). After 24h in- Stock solutions of 1–3 were prepared in methanol and diluted with cubation,themixturewasdroppedontofreshlycleavedmica.Thenthe watertogiveafinalwater/methanolcompositionof98:2.Thecuvette sampleswere rinsed for10s withdeionized waterand dried withni- was irradiated with a directional LED light at 465 ± 10nm trogen gas. The images were obtained in air at room temperature on (10mWcm−2)or660 ± 10nm(50mWcm−2),andtheoutputpower areasof5×5μm2. density of the LED was controlled by an LED controller. UV–Vis ab- sorbancespectrawererecordedatregularintervals(2minfor465nm 4.9. Gelelectrophoresisstudy irradiation,5minfor660nm).Ferrioxalateactinometrywasusedasa reference to determine the photon flux of our LED light source. The DNA binding properties of complex 3 was also investigated by quantumyieldsofthefirststepofcomplexes1–3werecalculatedac- agarose gel electrophoresis. Desired concentrations of the complex 3 cordingtothemethoddescribedbefore[57] werepreparedbydilutionofthecompoundwithTris-H3PO4(100mm) buffer. pBR322 DNA (5μL) was added to each tube. The mixtures of 4.5. DFTcalculation complex3andpBR322plasmidDNAweremixturetogether,andirra- diatedwithbluelight(465nm,30min)orredlight(660nm,1h).After AllcalculationswereperformedusingtheGaussian09suitofpro- 24h incubation, the agarose gel (made up to 1% w/v) was prepared gram[69].Thegroundstate(S0),thelowest-lyingtripletstate(T1),and withTAbuffer(50mmTris-acetate,pH7.4).Themixtureswithloading the dissociated structures of complexes 1–3 were optimized by using buffer (1mL) were submitted to electrophoresis in agarose gel in TA theB3LYPdensityfunctional[70]withtheLanL2DZbasissetandef- bufferat100Vfor90min.Agarosegelswerethendyedwithethidium fective core functional [71]used for the Ruatom while the 6-31G(d) bromide (0.5mg/L) for 20min. Bands were imaged by using a basisset[72,73]fortheotheratoms.Allstructureswereconfirmedto MolecularImager(Bio-Rad,USA)underUVlight. be minima by harmonic vibrational frequency calculations. The time- dependent density functional theory (TD-DFT) [74–76] calculations 4.10. MTTassay were performed at the same level to predict the singlet electronic transitionsandtheUV–visiblespectra.The3MLCT,and3MCelectronic Cytotoxicityofcomplexes1–3andbicalutamideagainstLNCaPand configurationswerecharacterizedbyexaminingthespindensities,and PC-3 cells was determined by means of the MTT (3-(4,5-di- the 1MLLCT state were identified by analyzing the molecular orbital methylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay. Cells populations. The electron density difference maps (EDDMs) of the were cultured in RPMI-1640 medium with 10% fetal bovine serum lowest-lyingsinglettransitionsofthethreecomplexeswereplottedby (FBS).Allmediawerealsosupplementedwith100mg/mLofpenicillin theGaussView(version5.0). and 100mg/mL of streptomycin. Cells (105 per well) with better vi- talitywereseededin96-wellplates.Thecompoundsweredissolvedby 4.6. Dockingstudy DMF and diluted with medium to various concentrations (the final concentrationofDMFwaslessthan0.4%).Afterbeingincubatedinthe Docking studies were carried out using Autodock Dock 4.2. The darkfor4h,cellswereirradiatedwithbluelight(465nm)for30min crystalstructureofAR-LBD(ligandbindingdomain)wasobtainedfrom orredlight(660nm)for1h,andthenthecellswereincubatedinthe theProteinDataBank(PDBID:1z95).Bicalutamidein1z95werere- dark for a further 48h. After that, cells were stained with 3-(4,5-di- movedprior tothedockingby softwarePyMOL.Thedockingsimula- methyl-2-thiazolyl)-2,5-diphenyl-2Htetrazoliumbromide(MTT)(5mg/ tionwasperformedwiththeLamarckiangeneticalgorithmforasmuch mL) for another 5h, and then the medium was thrown away and re- as150dockingruns.Eachrunofthedockingoperationwasterminated placedby150mLDMSO.Theinhibitionofcellgrowthinducedbythe after a maximum of 2,500,000 energy evaluations. During docking tested complexes was detected by measuring the absorbance of each studies,theproteinstructurewaskeptrigid.Rotationinthecomplexes wellat570/630nmusingenzymelabelinginstrument.TheIC50values 1–3waspermittedaboutallsinglebonds. werecalculatedbySPSSsoftwareafterthreeparallelexperiments. 4.7. ARligandbindingaffinity 4.11. ApoptosisassessmentbyHoechst33342staining The fluorescence polarization technique was applied to study the LNCaPcellswereseededin24-wellplatesat1×105cells/welland binding of complexes 1–3 and bicalutamide to the androgen receptor incubated overnight. Cells were incubated with 30μM of the tested usingthePolarScreen™ARCompetitorAssay,Green(lifetechnologies, compounds,andthenirradiatedwithbluelight(465nm,30min)orred A15880)accordingtothemanufacturer'sinstructions.Complexes1–3 light(660nm,1h).Thecellswereincubatedinthedarkforafurther withdesiredconcentrationswereirradiatedwithadirectionalLEDlight 24h.Afterthat,thecellswererinsedtwiceinPBS(phosphate-buffered at465nm(30min)or660nm(1h),andthenweretitratedagainsta saline)andstainedwithHoechst33342fluorescentdyefor10minin preformed complex of Fluormone™ AL Green and the AR-LBD (GST). thedarkat37°C.Cellapoptosiswasexaminedunderthefluorescence The assay mixture was incubated at room temperature for 4h, after microscopewithexcitationwavelengthof330–380nm. which the fluorescence polarization values were measured in a SpectraMax® Paradigm® Multi-Mode Detection Platform using an ex- 4.12. Apoptosisanalysisbyflowcytometry citationwavelengthof485nmandanemissionwavelengthof535nm. Data analysis for the ligand binding assays was performed using LNCaP cells were grown in a 6-well plate and cultured overnight. GraphPadPrismsoftware. The tested complexes were added with the final concentration of 30μM.Afterincubationfor24h,cellswereirradiatedwithbluelight 4.8. Atomicforcemicroscopy(AFM) (465nm,30min)orredlight(660nm,1h).Afterthat,thecellswere incubatedinthedarkforafurther24h,andcollectedbycentrifugation ThepBR322plasmidDNA(200ng/μL)wasdilutedto5ng/μLwith (5min,25°C,2000rpm).Then,thecellswerewashedtwicewithcold hepes (N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid) buffer water, resuspended in binding buffer (10mM hepes, 140mM NaCl, (40mMhepes,5mMMgCl2,pH7.4).Complex3wasdissolvedinDMF 2.5mMCaCl2,pH7.4).Thecellswerestainedwith5μLofAnnexinV- 7 J.Zhao,etal. Journal of Inorganic Biochemistry 196 (2019) 110684 FITC(fluoresceinisothiocyanate)andthenwith5μLofpropidiumio- 6(2015)2342–2346. dide (20μg/mL) for 15min in the dark at room temperature. 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