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In Situ Investigation of Peptide–Lipid Interaction BetweenKhoi Tan Nguyen1,2 Received: 14 September 2015 / Accepted: 6 February 2016 Springer Science+Business Media New York 2016 Abstra

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In Situ Investigation of Peptide–Lipid Interaction Between

Khoi Tan Nguyen1,2

Received: 14 September 2015 / Accepted: 6 February 2016

 Springer Science+Business Media New York 2016

Abstract Sum frequency generation vibrational

spec-troscopy (SFG) was utilized to investigate the interaction

between PAP248–286and the two lipid bilayer systems The

present study also provides spectroscopic evidence to

confirm that, although PAP248–286 is unable to penetrate

into the hydrophobic core of the lipid bilayers, it is capable

of interacting more intimately with the fluid-phase POPG/

POPC than with the gel-phase DPPG/DPPC lipid bilayer

The helical structure content of lipid-bound PAP248–286

was also observed to be high, in contrast to the results

previously reported using nuclear magnetic resonance

(NMR) Collectively, our SFG data suggest that

lipid-bound PAP248–286actually resembles its structure in 50 %

2,2,2-trifluoroethanol better than the structure when the

peptide binds to SDS micelles This present study questions

the use of SDS micelles as the model membrane for NMR

studies of PAP248–286due to its protein denaturing activity

Keywords Gel-phase and fluid-phase model lipid

bilayers PAP248–286  Peptide conformation  SDS

micelles

Introduction The entry of the human immunodeficiency virus (HIV) into the host cell is believed to be increased 4–5 orders of magnitude by amyloid fibrils contained in semen, specifically, semen-derived enhancer of viral infection (SEVI) (Munch et al 2007; Rusert et al 2004) These amyloid fibrils allow HIV, which would normally be considered a weak pathogen, to easily enter the host cells and hence facilitate the AIDS pandemic that has killed 40 million people since it was first clinically observed in

1981 It has recently been found that SEVI fibrils form by self-assembly of the peptide PAP248–286, a proteolytic cleavage product of prostatic acid phosphate protein abundantly found in semen.(Arnold et al 2012; Munch

et al 2007; Roan et al 2011) To shed light on the mechanism of this viral entry enhancement of these amyloid fibrils, an extensive amount of research has been done using nuclear magnetic resonance, circular dichro-ism, differential scanning calorimetry and transmission electron microscopy (Brender et al 2009, Brender et al

2011; Easterhoff et al 2011; Nanga et al 2009; Olsen

et al 2012) However, the mechanism of the fibril for-mation remains poorly understood due to its inherited structural complexity as well as the hard to achieve physiological conditions of the phenomenon

In the current study, sum frequency generation vibra-tional spectroscopy (SFG) was used to investigate the interaction between PAP248–286and model cell membranes

at very low peptide concentrations within the range of 0.2–1.0 lM As an intrinsically surface sensitive technique with superior sensitivity, SFG has been utilized extensively

in studies of protein–lipid interactions in the last decade (Mauri et al.2014; Nguyen2015; Volkov and Bonn2013; Weidnerw and Castner 2013; Yan et al 2014; Ye et al

Electronic supplementary material The online version of this

article (doi: 10.1007/s00232-016-9878-1 ) contains supplementary

material, which is available to authorized users.

& Khoi Tan Nguyen

k.nguyen9@uq.edu.au

1 School of Chemical Engineering, The University of

Queensland, Brisbane, QLD 4072, Australia

2 School of Biotechnology, International University, Vietnam

National University, Ho Chi Minh City, Vietnam

DOI 10.1007/s00232-016-9878-1

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2014; Zhang et al 2014) It has been generally known

that PAP248–286is not toxic to the cell due to its inability

to penetrate into the hydrophobic core of the lipid The

molecular conformation of PAP248–286(in 50 % TFE as

well as the SDS micelle-bound form) has been solved by

solution state NMR (Brender et al 2011; Nanga et al

2009) The helical content of PAP248–286 in 50 % TFE

was observed to be 57 %, significantly higher than its

SDS-bound form (30 %) (Brender et al 2009) In both

environments, the helical content of PAP248–286is

divi-ded into two helical segments which are almost

perpen-dicular to each other in the case of 50 % TFE (Fig.1,

PDB 2L77) In addition, the 3-10 helical component

which was suggested to play a role in the fibril formation

of the peptide (Nanga et al.2009) does not seem to exist

in the NMR structure of the peptide We believe that the

discrepancies between the structural properties proposed

by these NMR measurements originate from the possible

protein denaturing activity of SDS (Seddon et al 2004;

Warschawski et al 2011), making this surfactant an

inappropriate model membrane system at least for studies

of interactions between cell membranes and PAP248–286

While SDS micelles have been reported to be an

excel-lent model membrane system for studies of robust

transmembrane peptides/proteins (Tulumello and Deber

2009), it has been reported to denature some membrane

proteins/peptides, especially when these structures do not

penetrate into the hydrophobic core of the micelles

(Seddon et al.2004; Warschawski et al 2011) Because

the amyloidogenic activity of peptides is directly dictated

by their interactions with the surrounding media, it is

important to choose a model membrane system for

studies of PAP248–286 that does not alter the structural

property of the peptide To overcome the possibility of

protein denaturation by SDS surfactant, phospholipid

mixtures were used to make lipid bilayers mimicking

model membranes in our study

Experimental Section Materials

The PAP248–286peptide ([95 % purity) was purchased from Biomatik (Toronto, ON) Phospholipids POPC (1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine), POPG (1-palmi-toyl-2-sn-glycero-3-phospho-(10-rac-glycerol)), hydro-genated and deuterated DPPG/DPPC (1,2-dipalmitoyl (D62)-sn-glycero-3-phospho-glycerol/choline) were pur-chased from Avanti Polar Lipids Inc (Alabaster, AL) Freshly purified water (Ultrapure Milli-Q unit from Mil-lipore, USA) with a resistivity of 18.2 MX cm was used to make all the solutions in the experiments These lipid species chosen in our study have been commonly used in studies of the interactions between the lipid and peptides/ proteins Deposition of the lipid bilayers on to CaF2prisms were prepared by sequentially depositing the distal and proximal layers using a 622 Nima LB trough (Chen et al

2007) In brief, the CaF2prism was immersed in the water trough; then a lipid monolayer at 34 mN/m surface pres-sure was spread on the water surface This surface prespres-sure was maintained, while the prism was being lifted out of the subphase at the rate of 1 mm/min The second lipid leaflet deposition was made by bringing the first deposited lipid layer into contact with a lipid monolayer at 34 mN/m surface pressure Once the lipid bilayer was formed, it was kept hydrated until the completion of the experiment The protein reservoir with a volume of 4 ml was placed below the lipid bilayer deposited CaF2prisms during the SFG measurement The peptide solution was stirred by a mag-netic micro-stirrer at a rate of 40 rpm during the peptide– lipid interaction The pH of the bulk was stabilized with

20 mM phosphate buffer saline (PBS) at 7.2 containing

20 mM NaCl All experiments were carried out at room temperature (*23C) The SFG spectra in the amide I frequency region were collected from the lipid-bound

Dynamic α/3-10helix

Fig 1 Two structures of

PAP248–286in SDS micelles

(PDB = 2L3H, right) and 50 %

TFE (PDB = 2L77, left)

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PAP248–286after the peptide solution had been in contact

with the lipid bilayers for at least 1 h (to equilibrate and

ensure that no further time-dependent changes occurred)

SFG Setup

In the SFG experiments, the visible and the tunable IR

beams were spatially and temporally overlapped on the

solution interface The visible beam was generated by

frequency-doubling the fundamental output pulses

(1064 nm, 10 Hz) of 36 ps pulse-width from an EKSPLA

solid state Nd:YAG laser (PL2241) The tunable IR beam

was generated by an EKSPLA optical parametric

genera-tion/amplification and difference frequency system based

on LBO and AgGaS2 crystals Fluctuations in the beam

energies were only 3 % standard deviation in the tunable

IR beam and 1.5 % in the visible beam In the current SFG

measurements, the incident angle for visible beam was

avis= 60 and for the IR beam it was aIR = 54 The

near-total-internal reflection experimental geometry was

adop-ted to collect the SFG signals from interfacial PAP248–286

using a right angle CaF2prism as the solid substrate In this

study, each presented data point was averaged over 100

acquisitions

The quantities vð2Þssp (s polarized SFG, s polarized visible

and p polarized infrared polarization combination) and vð2Þppp

(p polarized SFG, p polarized visible and p polarized

infrared polarization combination) reflect the observed

SFG intensities in the laboratory frame They are related to

vð2Þyyz and vð2Þzzz as follows:

vð2Þssp¼ LyyðxÞLyyðx1ÞLzzðx2Þ sin b2vð2Þyyz ð1Þ

vð2Þppp¼

LxxðxÞLxxðx1ÞLzzðx2Þ cos b cos b1sin b2vð2Þxxz

LxxðxÞLzzðx1ÞLxxðx2Þ cos b sin b1cos b2vð2Þxzx

þLzzðxÞLxxðx1ÞLxxðx2Þ sin b cos b1cos b2vð2Þzxx

þLzzðxÞLzzðx1ÞLzzðx2Þ sin b sin b1sin b2vð2Þzzz



















 ð2Þ where LiiðxÞ is a Fresnel coefficient corrected for local

fields; and b, b1and b2are the angles of the signal, visible

and IR beams with respect to the surface normal,

respec-tively For a C3v symmetry point group on an isotropic

surface, vð2Þxzx¼ vð2Þzxx The Fresnel coefficient LxxðxÞ can be

calculated as follows:

Lxx¼ 2n1cosðhtÞ

where aiand htare the incident and the transmitted angles

of the optical beam, respectively Because the

near-total-internal reflection geometry was used in this study, the

quantity LxxðxÞ in (3) will be close to zero since the angle

of the transmitted beam, ht; will approach 90 We thus have

vð2Þppp¼ LzzðxÞLzzðx1ÞLzzðx2Þ sin b sin b1sin b2vð2Þzzz ð4Þ The SFG signals are deconvoluted using the Lorentzian line shape function described as follows:

vð2Þeff ¼ vð2Þnr þX

q

Aq

xIR xqþ iCq

ð5Þ

where vð2Þnr is the nonresonating contribution; Aq is the amplitude of the vibrational mode q; xIR and xq are the input IR and the resonance IR of the vibrational q mode frequencies, respectively; and C denotes the damping coefficient of the SFG peak

Results and Discussions Interaction Between PAP248–286and 3:7 DPPG/ DPPC Lipid Bilayers

The interactions between PAP248–286 and DPPG:DPPC (3:7) lipid bilayers were studied at two peptide concen-trations of 200 nM and 1.0 lM This 3:7 lipid ratio is commonly used to simulate a mixed anionic/zwitterionic membrane system It is worth noting that both DPPC and DPPG are in the gel phase at 23C, which allows for the SFG spectral specificity of the distal and proximal leaflets using isotope labelling as previously demonstrated by Chen

et al (2007) In particular, deuterated 3:7 dDPPG/dDPPC was deposited on to the CaF2prism as the distal leaflet, and protonated 3:7 DPPG/DPPC was then deposited as the proximal leaflet.dDPPC and DPPC were used to reduce the density of negative charges in the lipid bilayer thus less-ening the electrostatic interaction between the model membrane and PAP248–286 Despite this lessening of elec-trostatic interaction, PAP248–286was bound strongly to the lipid bilayer, demonstrated by the strong SFG amide I band

at both peptide concentrations of 200 nM and 1.0 lM (Fig.2)

To verify that the interaction between PAP248–286 and DPPG/DPPC lipid bilayer was electrostatically driven, a pure DPPC lipid bilayer was used in place of the 3:7 DPPG/DPPC mixture Results showed that no discernible SFG amide I band was observed (Fig S1, ESI) in the absence of the electrostatic lipid–peptide attraction Despite its strong binding to the membrane, PAP248–286 did not exhibit any ability to penetrate the 3:7 DPPG/DPPC bilayer as demonstrated in Fig.3 Upon time-dependent translocation calibration, the SFG signals of the terminal methyl C–H and C–D stretches suggest that the 3:7 DPPG/

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DPPC remained almost unchanged upon the binding of

PAP248–286 (Fig.3) The minor spectral differences

observed in Fig.3were most likely due to the minor stress

caused by PAP248–286 when it was bound to the lipid bilayer Given the fact that PAP248–286is nondisruptive to the 3:7 DPPG/DPPC bilayer, the main helical segment (G261–I277) should adopt a more or less horizontal ori-entation at the lipid surface and the observed SFG amide I band should be contributed by the more vertically oriented helical segment K251–G260 This vertically oriented helical segment may play an important role in promoting the bridging interactions between membranes due to its positive charges Since horizontally oriented helical seg-ments were calculated to produce weaker SFG amide I band in both ppp and ssp polarization combinations (Nguyen et al 2009; Wang et al 2008), the strong SFG amide I signals (as compared to that of transmembrane peptide magainin II in POPG/POPC lipid bilayer, Fig S2, ESI) suggest a high helical content of lipid-bound PAP248–286, which is contradictory to the previously reported low value of 30 % suggested by Brender et al using circular dichroism However, the authors concluded that this low value of 30 % was probably an underestimate caused by the visible aggregation of the lipid vesicles (Brender et al 2009) We thus believe that SDS-bound PAP248–286was denatured by the anionic surfactant SDS as commonly reported in the community (Seddon et al.2004; Warschawski et al.2011) It is worth noting that SDS is a charged soluble detergent which interacts with both the polar and nonpolar regimes of the peptides/proteins Beyond its critical micellar concentration of around 7–8 mM, there coexist both SDS micelles and molecular SDS molecules in the bulk medium, which will at some degree affect the folding of the proteins/peptides in the solution

Interaction Between PAP248–286and 3:7 POPG/ POPC Lipid Bilayers

Since both DPPC and DPPG are in gel phase under the current experimental conditions (at room temperature), another set of experiments in which PAP248–286 interacts with lipid bilayers in fluid phase is desirable The 3:7 POPG/POPC bilayer system was chosen for the current study because its electrostatic attraction to PAP248–286 should be similar to that of 3:7 DPPG/DPPC presented in the previous section (Haro et al.2003) With this system, it

is impossible to spectrally distinguish the distal and prox-imal leaflets by the method of isotope labelling of the fluid-phase lipid bilayers The flip-flopping rate of fluid-fluid-phase lipid bilayers is so rapid [t1/2 can be as low as 1.3 min at room temperature (Liu and Conboy 2005)], which almost instantly causes the lipid bilayer to become entirely sym-metric, leading to no spectral features being observable by SFG However, being a symmetry-sensitive technique, SFG can probe the symmetry deviation of interfaces SFG

0.00

0.10

0.20

0.30

wavenumber (cm -1 )

200 nM ssp

200 nM ppp

0.00

0.10

0.20

0.30

wavenumber (cm -1 )

1 μM ssp

1 μM ppp

Fig 2 SFG amide I band of 3:7 DPPG/DPPC lipid-bound PAP248–286

at peptide concentration of 200 nM (top) and 1 lM (bottom) in ssp

and ppp polarization combinations

0.00

0.02

0.04

0.06

0.08

0.10

2800 2850 2900 2950 3000

wavenumber (cm -1 )

before PAP248-286 aer 1 μM PAP248-286

CH 3 sym

CH 3 FR

CH 3 asym

0.00

0.01

0.02

0.03

0.04

0.05

wavenumber (cm -1 )

before PAP248-286 aer 1 μM PAP248-286

CD 3 sym

CD 3 asym

CD 2 asym CD 3 FR

(a)

(b)

Fig 3 ssp SFG signals of the proximal (a) and distal (b) lipid leaflets

before and after peptide interaction

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data reveal that the fluid-phase 3:7 POPG/POPC lipid

bilayer exhibits a noticeable decrease in the degree of

symmetry upon interacting with PAP248–286, demonstrated

by the vibrational modes of the terminal methyl groups

starting to appear with the presence of the peptide (Fig.4)

This observation can be simply explained by the stresses

stemming from the lipid headgroup–PAP248–286binding

It is noted in Fig.4that the baseline of the SFG signal in

the 2800–3000 cm-1range of the 3:7 POPG/POPC bilayer

became weaker after the peptide interaction, which is due

in part to the peptide binding that reduces the number of

interfacial water molecules On the other hand, it is also

possible that the charge neutralization by the peptide

binding dictates the interfacial water orientation and leads

to the reduction in the SFG signal baseline (Fig S3, ESI) (Ding et al 2013) Further information about the binding behaviour of PAP248–286to POPG/POPC can be derived by analysing the SFG amide I band of the interfacial peptide molecules Interestingly, both the ssp and ppp SFG amide I signal intensities obtained were similar as occurred when 3:7 DPPG/DPPC was used at peptide concentrations of

200 nM and 1.0 lM PAP248–286 (Fig.5), indicative of a similar nondisruptive binding mode of PAP248–286 stem-ming from its low hydrophobicity and high positive net charge (?10)

Despite the above similarity in the PAP248–286 SFG amide I signal intensities, there were some minor spectral shifts observed that indicate secondary structure content shifts of PAP248–286upon interacting with the lipids High-resolution technique NMR suggested that PAP248–286 consists of mainly helical (a- or 310-) and random coil structures (PDB codes 2L77 and 2L3H, respectively Fig-ure1) (Nanga et al.2009) The structure of PAP248–286 in TFE suggested by Ayyalusamy et al (PDB code 2L77) contains significantly more helical content than when the peptide binds to SDS micelles (2L3H) In the current SFG measurements, since SFG is insensitive to unordered structures, random coil components would not make a substantial contribution to the strong amide I band shown

0.00

0.10

0.20

0.30

0.40

2800 2850 2900 2950 3000

wavenumber (cm -1 )

before PAP248-286 aer 1 μM PAP248-286

Fig 4 3:7 POPG/POPC lipid bilayer before and after interacting with

PAP248–286

0.00

0.10

0.20

0.30

wavenumber (cm -1 )

200 nM ppp

200 nM ssp

0.00

0.10

0.20

0.30

wavenumber (cm -1 )

1 μM ssp

1 μM ppp

Fig 5 SFG amide I band of 3:7 DPPG/DPPC lipid-bound PAP248–286

at peptide concentration of 200 nM (top) and 1 lM (bottom) in ssp

and ppp polarization combinations

0.00 0.10 0.20 0.30

wavenumber (cm -1 )

data fit

1605 cm-1

1630 cm-1

1650 cm-1

1685 cm-1

0.00 0.10 0.20 0.30

wavenumber (cm -1 )

data fit

1605 cm-1

1630 cm-1

1650 cm-1

1685 cm-1

(a)

(b)

Fig 6 ppp SFG amide I band fitting of lipid-bound PAP248–286 at peptide concentration of 1 lM: a with 3:7 DPPG/DPPC and b with 3:7 POPG/POPC The insets are the zoom-ins to show the smaller contribution peaks

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in Figs.2 and 5, as has previously been computationally

(by NLOPredict) and experimentally (by SFG)

demon-strated (Ding et al.2013; Nguyen et al.2010b; Wang et al

2008) Besides, random coil structure should give rise to

rather broad amide I bands (if observable) due to

unpre-dicted coupling among the backbone C=O units (Fu et al

2011) In this study, the strong SFG amide I bands of

PAP248–286possess well-defined spectral shape that can be

fit nicely using three or four component peaks as shown in

Fig.6and Table1 For these two main reasons, it is safe to

assume that the SFG amide I contribution of the random

structures of PAP248–286 was negligible in the illustrated

spectra

Although the amide I band of 3:7 POPG/POPC-bound

PAP248–286was well fit using three peaks featuring the

a-helical and b-sheet structures, we could not detect the

chiral SFG signal in either psp or spp polarization

combi-nation (Fig S1, ESI) Furthermore, our attempt to use the

interference method (Belkin et al 2000; Nguyen et al

their interference with the achiral components failed to

detect any chiral signal from the lipid-bound PAP248–286

Our inability to probe any chiral signal can be explained

either by the non-existence of the b-sheet structure or by

the b-sheet content being insufficient to produce any

detectable SFG chiral signal We believe the latter

expla-nation is more sensible because a small b-sheet

confor-mation does exist in the structure of PAP248–286 (residues

L283–Y286) and the two minor peaks used to fit the achiral

spectrum (Fig.6b; Table1) closely match the assignments

of the B2 and B1 vibrational modes previously reported

(Baio et al.2013; Nguyen et al.2010a)

Whilst the existence of a small and transient/dynamic

310-helical segment at the C terminus has been proposed in

an NMR study on SDS-bound PAP248–286 (Brender et al

2009), there was no 310-helical SFG signal detected in our

study The small peak at 1630 cm-1 could not have been

contributed by the 310-helical structure because this

struc-ture would also give rise to a peak at 1670 cm-1 when

coupled with the a-helical structures (Ye et al.2012,2010)

It is noted that the 310-helix was not observed in the

structure of PAP248–286, either (PDB code 2L77)

Since PAP248–286 does not penetrate into the hydrophobic core of lipid bilayers, its molecular orientation

at the lipid interface can be reasonably assumed to be independent of the phase of the lipid bilayers The higher SFG signal amplitudes of the 1630 and 1685 cm-1 peaks observed when PAP248–286 binds to fluid-phase lipids can

be attributed to the slight peptide conformational/orienta-tional alteration induced by the more intimate binding PAP248–286 causes to the lipid This peptide conforma-tional/orientational alteration demonstrates that the con-formational preferences of the monomeric PAP248–286 are rather sensitive to the peptide/lipid interaction, which may provide important insights into the aggregation pathways and the formation of the eventual amyloid fibre

Conclusion This study used sum frequency generation vibrational spectroscopy (SFG) to show that the molecular structure of the lipid-bound PAP248–286 may vary with the phase of lipid bilayer system Furthermore, PAP248–286 was observed to interact more intimately with the 3:7 POPG/ POPC lipid bilayer than with its gel-phase counterpart, causing the lipid bilayer to become asymmetric The dis-crepancies between our results and NMR measurements on SDS-bound PAP248–286might be due to the choice of 3:7 POPG/POPC lipid bilayer versus SDS micelles used to mimic the cell membranes, which brings into question whether SDS micelles are a good system for such studies The current study also suggests a potentially higher helical content of lipid-bound PAP248–286than the 30 % calculated using circular dichroism In addition, this study demon-strates the importance of the choice of lipid–bilayer system when conducting studies on the aggregation pathways and amyloid fibre formation of the SEVI precursor peptide PAP248–286

Acknowledgments This research is funded by the Vietnam National Foundation for Science and Technology Development (NAFOSTED) under Grant Number 106.16-2012.67 The author sincerely thanks Dr Gay Marsden for her generous assistance in the manuscript preparation.

Table 1 ppp SFG amide I band fitted amplitude/damping coefficient ratio (A/C) of PAP248–286peptide interacting with 3:7 DPPG/DPPC and 3:7 POPG/POPC

Secondary structure Peak centre (cm-1) 3:7 DPPG/DPPC A/C 3:7 POPG/POPC A/C

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Compliance with Ethical Standards

Conflict of interest The authors declare no competing financial

interests.

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