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Schweda1 1 Clinical Research Centre, Karolinska Institutet and University College of South Stockholm, Huddinge, Sweden; 2 Molecular Infectious Diseases Group and Department of Paediatric

Trang 1

Structural diversity in lipopolysaccharide expression in nontypeable

Haemophilus influenzae

Identification of L- glycero -D- manno -heptose in the outer-core region in three clinical isolates

Martin Ma˚nsson1, Derek W Hood2, E Richard Moxon2and Elke K H Schweda1

1

Clinical Research Centre, Karolinska Institutet and University College of South Stockholm, Huddinge, Sweden;

2

Molecular Infectious Diseases Group and Department of Paediatrics, Weatherall Institute of Molecular Medicine,

John Radcliffe Hospital, Oxford, UK

Structural elucidation of the lipopolysaccharide (LPS) from

three nontypeable Haemophilus influenzae clinical isolates,

1209, 1207 and 1233 was achieved using NMR

spectro-scopy and ESI-MS on O-deacylated LPS and core

permethylated dephosphorylated OS It was found that the

organisms expressed a tremendous heterogeneous

glyco-form mixture resulting from the variable length of the OS

chains attached to the common structural element of

H influenzae, L-a-D–Hepp-(1fi2)-[PEtnfi6]-L-a-D

–Hepp-(1fi3)-[b-D-Glcp-(1fi4)]-L-a-D

–Hepp-(1fi5)-[PPEtnfi4]-a-Kdop-(2fi6)-Lipid A Notably, the O-6 position of the

b-D-Glcp residue could either be occupied by PCho or

L-glycero-D-manno-heptose (L,D–Hep), which is a location

for L,D–Hep that has not been seen previously in

H influenzae LPS The outer-core L,D–Hep residue was

further chain elongated at the O-6 position by the

struc-tural element b-D-GalpNAc-(1fi3)-a-D-Galp-(1fi4)-b-D -Galp, or sequentially truncated versions thereof The distal heptose residue in the inner-core was found to be chain elongated at O-2 by the globotetraose unit, b-D -GalpNAc-(1fi3)-a-D-Galp-(1fi4)-b-D-Galp-(1fi4)-b-D-Glcp, or sequentially truncated versions thereof Investigation of LPS from an lpsA mutant of isolate 1233 and a lic1 mutant

of isolate 1209 was also performed, which aside from confirming the functions of the gene products, simplified elucidation of the OS extending from the proximal heptose (the lpsA mutant), and showed that the organism exclu-sively expresses LPS glycoforms comprising the outer-core

L,D–Hep residue when PCho is not expressed (the lic1 mutant)

Keywords: Haemophilus; lipopolysaccharide; L

-glycero-D-manno-heptose; phase variation; ESI-MSn

Haemophilus influenzae is an important cause of human

disease worldwide and is found in both encapsulated (types

a–f) and unencapsulated (nontypeable) forms Nontypeable

H influenzae (NTHi) strains routinely colonize the

naso-pharynx of healthy carriers and cause otitis media and

respiratory tract infections [1] The outer membrane

com-ponent lipopolysaccharide (LPS) can influence each stage of the pathogenesis of H influenzae infection H influenzae LPS is composed of a membrane-bound lipid A moiety connected to the core oligosaccharide (OS) via a single phosphorylated 3-deoxy-D-manno-oct-2-ulosonic acid (Kdo) residue The carbohydrate regions provide targets for recognition by host immune responses and expression of certain OS epitopes can alter the virulence of the pathogen [2] Some of these OS epitopes have been found to mimic human antigens, possibly allowing the bacteria to evade the host immune system [3,4] The OS portion of H influenzae LPS is subject to high-frequency phase variation (on/off switching of expression) of terminal epitopes, contributing

to the vast LPS heterogeneity usually found within a single strain [2] This heterogeneity may be an advantage to the bacteria, allowing them to better confront different host compartments and microenvironments and to survive the host immune response [5] The availability of the complete genome sequence of H influenzae strain Rd [6] has facili-tated a comprehensive study of LPS biosynthetic loci in the homologous strain RM118 [7] and in the type b strains Eagan (RM153) and RM7004 [8] Gene functions have been identified that are responsible for most of the steps in the biosynthesis of the OS portion of their LPS molecules

Correspondence to E Schweda, University College of

South Stockholm, Clinical Research Centre, NOVUM,

S-141 86 Huddinge, Sweden.

Fax: + 46 8585 838 20, Tel.: + 46 8585 838 23,

E-mail: elke.schweda@kfc.ki.se

Abbreviations: CE, capillary electrophoresis; Kdo, 3-deoxy- D

-manno-oct-2-ulosonic acid; AnKdo-ol, reduced anhydro Kdo; Hep,

heptose; D , D -Hep, D -glycero- D -manno-heptose; L , D -Hep,

L -glycero- D -manno-heptose; Hex, hexose; HexNAc,

N-acetylhexos-amine; HMBC, heteronuclear multiple-bond correlation; lipid A-OH,

O-deacylated lipid A; LPS, lipopolysaccharide; LPS-OH,

O-deacylated LPS; MSn, multiple step tandem mass spectrometry;

Neu5Ac, N-acetylneuraminic acid; NTHi, nontypeable Haemophilus

influenzae; OS, oligosaccharide; PCho, phosphocholine; PEtn,

phosphoethanolamine; PPEtn, pyrophosphoethanolamine.

(Received 5 September 2002, revised 19 November 2002,

accepted 26 November 2002)

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Molecular structural studies of LPS from H influenzae

strains [9–19] have resulted in a structural model consisting

of a conserved phosphoethanolamine (PEtn)-substituted

triheptosyl inner-core moiety (labelled HepI–HepIII) in

which each of the heptose residues can provide a point for

attachment of OS chains or noncarbohydrate substituents

(Scheme 1) HepIII and the b-D-Glcp residue that is linked

to HepI (labelled GlcI) have an especially wide range of

alternatives in the substitution-pattern HepIII has been

found to be substituted by a b-D-Glcp residue either at O-2

[12] or O-3 [15] Alternatively, substitution can occur by a

b-D-Galp residue either at O-2 [10] or O-3 [18] Analysis of

LPS from lpsA mutants established in a number of strain

backgrounds supports a role for LpsA in each of the

alternative glycose substitutions of HepIII HepIII has also

been found to be substituted by the noncarbohydrate

substituents Ac (either at O-2 [15] or O-3 [14]), Gly [15,20],

P(at O-4 [11]) and PEtn [9] For GlcI, the O-4 position has

been found to be substituted by a b-D-Galp residue [9] or a

b-D-Glcp residue [10], while in other strains, O-6 was

substituted by phosphocholine (PCho) [12] orD

-glycero-D-manno-heptose (D,D–Hep) [13] In NTHi strains SB 33

and 176 [16,18], disubstitution by b-D-Glcp (at O-4) and

PCho (at O-6) occurs, while in strain RM118 [19],

disubstitution by b-D-Galp (at O-4) and PCho (at O-6)

was found In NTHi strain 1003 [17], disubstitution by Ac

(at O-4) and PCho (at O-6) was shown In each strain

analysed, PCho addition has been shown to be directed by

the products of the lic1 locus Our recent studies have

focussed on the structural diversity of LPS expression and

the genetic basis for that diversity in a representative set

consisting of 24 NTHi clinical isolates obtained from otitis

media patients In the present study we report on the

structural analysis of LPS from three of these isolates (1209,

1207 and 1233) which introduces a new glycosyl substituent

on GlcI

Experimental procedures

Bacterial strains used in this study

NTHi middle ear isolates 1209, 1207 and 1233 were obtained

from the Finnish Otitis Media Study Group [20a] Isolates

1209 and 1207 are from a single patient on the same day but

from different ears 1233 was isolated from a different patient

on a different date Molecular epidemiological data follow-ing DNA sequence analysis showed that 1233 is identical

to 1209 and 1207 except for one nucleotide change in one of the housekeeping genes investigated (unpublished results) Strains 1233lpsA and 1209lic1 were constructed

by transformation of the designated isolate with plasmid clones containing the relevant gene(s) interrupted by an antibiotic resistance cassette, as described previously [7,8] Bacterial cultivation and preparation of LPS

Bacteria were grown in brain-heart infusion broth supple-mented with haemin (10 lgÆmL)1) and NAD (2 lgÆmL)1) LPS was extracted from lyophilized bacteria by using phenol/chloroform/light petroleum, as described by Galanos

et al [21], but modified with a precipitation step of the LPS with diethyl ether/acetone (1 : 5, v/v; 6 vol.) LPS was purified by ultracentrifugation (82 000 g, 4C, 12 h) Chromatography

Gel filtration chromatography and GLC were carried out as described previously [15]

Preparation of OS material O-Deacylation of LPS O-Deacylation of LPS was achi-eved with anhydrous hydrazine as described previously [15,22]

Mild acid hydrolysis of LPS Reduced core OS material was obtained after mild acid hydrolysis (1% aqueous acetic acid, pH 3.1, 100C, 2 h) and simultaneous reduction (borane-N-methylmorpholine complex) of LPS from 1209 (120 mg), 1207, 1233, 1233lpsA (75 mg) and 1209lic1 The insoluble lipid A was separated by centrifugation and the water-soluble part was purified by gel filtration, giving one major OS-containing fraction from 1209 (OS-1, 22.5 mg),

1207, 1233, 1233lpsA (OS-2, 8.0 mg) and 1209lic1 An NH3 -treated part of OS-1 (OS-1¢) was repeatedly chromato-graphed, giving a major (OS-1¢-A, 4.4 mg) and a minor (OS-1¢-B, 1.0 mg) fraction OS-2 was rechromatographed, resulting in i.a OS-2-A (3.0 mg) and OS-2-B (1.8 mg)

material was performed with 48% aqueous HF as described previously [17]

Mass spectrometry GLC-MS was carried out with a Hewlett-Packard 5890 chromatograph equipped with a NERMAG R10–10H quadrupole mass spectrometer ESI-MS was performed as described previously [15] ESI-MSn on permethylated dephosphorylated OS was performed on a Finnigan-MAT LCQ ion trap mass spectrometer (Finnigan-MAT, San Jose, CA, USA) in the positive ion mode The samples were dissolved in methanol/water (7 : 3) containing 1 mM

NaOAc to a concentration of about 1 mgÆmL)1, and were injected into a running solvent of identical composition at

10 lLÆmin)1 Scheme 1 R 1 ¼ H, PCho or D , D –Hep, R 2 , R 4 , R 5 ¼ H, Glc, Gal or

Ac, R 3 ¼ H or Glc, Y ¼ Gly, P or PEtn.

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NMR spectroscopy

NMR spectra were obtained at 22C for OS and LPS-OH

samples either on a Varian UNITY 600 MHz spectrometer

as described previously [15,17] or on a JEOL JNM-ECP500

spectrometer using the previously described experiments

[15,17], except that a mixing time of 200 ms was used in all

NOESY experiments

Analytical methods

Sugars were identified as their alditol acetates as previously

described [23] Methylation analysis was performed as

described earlier [15] The relative proportions of the various

alditol acetates and partially methylated alditol acetates

obtained in sugar- and methylation analyses correspond to

the detector response of the GLC-MS Permethylation of

dephosphorylated OS was performed in the same way as in

the methylation analyses [15] but without the prior

acety-lation step The absolute configurations of the hexoses were

determined by the method devised by Gerwig et al [24] The

total content of fatty acids was analysed as described

previously [25]

Results

NTHi isolates 1209, 1207 and 1233 and selected mutant

strains were cultivated in liquid media and the LPS was

extracted using the phenol/chloroform/light petroleum

method

Characterization of LPS from NTHi isolate 1209

Compositional sugar analysis of the LPS sample indicated

D-glucose (Glc), D-galactose (Gal),

2-amino-2-deoxy-D-glucose (GlcN) and L-glycero-D-manno-heptose (L,D–

Hep) in the ratio 31 : 43 : 1 : 25, as identified by

GLC-MS of their corresponding alditol acetate and 2-butyl

glycoside derivatives [24] As described earlier, the LPS

contained ester-linked glycine [20] and a low level of

N-acetylneuraminic acid (Neu5Ac) [26] as shown by

high-performance anion-exchange chromatography, following

treatment of samples with 0.1MNaOH and neuraminidase, respectively

Treatment of the LPS with anhydrous hydrazine under mild conditions afforded water-soluble O-deacylated material (LPS-OH) ESI-MS data (Table 1) indicated a heterogeneous mixture of glycoforms consistent with each molecular species containing a conserved PEtn-substituted triheptosyl inner-core moiety attached via a phosphorylated Kdo linker to the putative O-deacylated lipid A (lipid A-OH) Quadruply charged ions were observed at m/z 650.1/680.8 (major) and at m/z 690.4/721.2 corresponding

to glycoforms with the respective compositions PCho• Hex3•Hep3•PEtn1)2•P1•Kdo•Lipid A-OH and PCho• Hex4•Hep3•PEtn1)2•P1•Kdo•Lipid A-OH (Fig 1) Quad-ruply charged ions were also observed at m/z 697.2/728.0 and at m/z 737.7/768.6 (minor) indicating the presence of glycoforms containing four heptose residues with the compositions Hex4•Hep4•PEtn1)2•P1•Kdo•Lipid A-OH and Hex5•Hep4•PEtn1)2•P1•Kdo•Lipid A-OH, respect-ively Quadruply charged ions of very low abundance could also be observed at m/z 609.4/640.4 and at m/z 741.2/772.1 consistent with the respective compositions PCho•Hex2• Hep3•PEtn1)2•P1•Kdo•Lipid A-OH and PCho•HexNAc1• Hex4•Hep3•PEtn1)2•P1•Kdo•Lipid A-OH Thus, ESI-MS data indicated the presence of two subpopulations of glycoforms; a major subpopulation in which the glycoform compositions comprised three heptoses and PCho (Hep3-glycoforms), and a minor subpopulation with compositions comprising four heptoses but lacking PCho (Hep4-glyco-forms) NTHi LPS glycoforms with four heptoses have previously been observed ([13], M Ma˚nsson, E R Moxon and E K H Schweda, unpublished results), and in those cases the fourth heptose has theD-glycero-D -manno-confi-guration and is situated in the outer-core region of the LPS

AsD,D–Hep was completely absent in the sugar analysis,

it was concluded that the fourth heptose here has the

L-glycero-D-manno-configuration

Characterization of OS from NTHi isolate 1209 Partial acid hydrolysis of LPS with dilute aqueous acetic acid afforded an insoluble lipid A and core OS material,

Table 1 Negative ion ESI-MS data and proposed compositions for LPS-OH of NTHi isolate 1209 Average mass units were used for calculation of molecular mass values based on proposed compositions as follows: Hex, 162.14; Hep, 192.17; Kdo, 220.18; P, 79.98; PEtn, 123.05; PCho, 165.13 and Lipid A-OH, 953.02 Relative abundance was estimated from the area of molecular ion peak relative to the total area (expressed as percentage) Peaks representing less than 5% of the base peak are not included in the table Very minor amounts of glycoforms with the compositions PCho•Hex 2 •Hep 3 •PEtn 1)2 •P 1 •Kdo•Lipid A-OH and PCho•HexNAc 1 •Hex 4 •Hep 3 •PEtn 1)2 •P 1 •Kdo•Lipid A-OH were also indicated by quadruply charged ions at m/z 609.4/640.4 and at m/z 741.2/772.1.

Observed ions (m/z) Molecular mass (Da)

Relative abundance (%) Proposed composition (M-4H) 4– (M-3H) 3– Observed Calculated

650.1 866.9 2604.0 2604.3 20 PCho•Hex 3 •Hep 3 •PEtn 1 •P 1 •Kdo•Lipid A-OH 680.8 908.0 2727.1 2727.3 43 PCho•Hex 3 •Hep 3 •PEtn 2 •P 1 •Kdo•Lipid A-OH 690.4 920.7 2765.4 2766.4 8 PCho•Hex 4 •Hep 3 •PEtn 1 •P 1 •Kdo•Lipid A-OH 721.2 962.0 2888.9 2889.5 7 PCho•Hex 4 •Hep 3 •PEtn 2 •P 1 •Kdo•Lipid A-OH 697.2 930.0 2792.9 2793.5 6 Hex 4 •Hep 4 •PEtn 1 •P 1 •Kdo•Lipid A-OH 728.0 970.9 2915.8 2916.5 12 Hex 4 •Hep 4 •PEtn 2 •P 1 •Kdo•Lipid A-OH 737.7 983.7 2954.4 2955.6 2 Hex 5 •Hep 4 •PEtn 1 •P 1 •Kdo•Lipid A-OH 768.6 1025.0 3078.2 3078.7 2 Hex 5 •Hep 4 •PEtn 2 •P 1 •Kdo•Lipid A-OH

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which was purified by gel filtration chromatography, giving

OS-1 ESI-MS indicated OS-1 to contain O-acetylated (0–3

Ac) and/or O-glycylated glycoforms (0–2 Gly), where the

most abundant peaks within each subpopulation of

glyco-forms corresponded to compositions comprising two acetyl

groups but lacking glycine (data not shown) On treatment

of OS-1 with 1% aqueous NH3 (giving OS-1¢), ESI-MS

showed major doubly charged ions at m/z 785.3 and 879.9

corresponding to the respective compositions PCho•Hex3•

Hep3•PEtn1•AnKdo-ol and Hex4•Hep4•PEtn1•AnKdo-ol

(Table 2)

In order to obtain sequence and branching information,

OS-1 was dephosphorylated and permethylated and

sub-jected to ESI-MSn [27,28] Due to the increased MS

response obtained by permethylation in combination with

added sodium acetate [27], several glycoforms were

observed in the MS spectra (positive mode) that were not

detected in underivatized samples (Fig 2A) Sodiated adduct ions were identified corresponding to the composi-tions Hex1)6•Hep3•AnKdo-ol, HexNAc1•Hex4)5•Hep3•

Hex5)6•Hep4•AnKdo-ol (Tables 3 and 4) The monosac-charide sequence and branching for the different glycoforms were obtained following collision-induced dissociation (CID) of the glycosidic bonds [27,28] Through the ion mass distinction between reducing, nonreducing and inter-nal fragments resulting from the bond ruptures [27], the topology could be determined for all compositions found in the MS profiling spectrum (Tables 3 and 4) For most compositions, the presence of several (2–3) isomeric com-pounds were revealed by identifying product ions in the

MS2spectra resulting from glycosidic cleavage between the heptose residues MS3 experiments were employed when necessary to confirm the structures

Fig 1 Negative ion ESI-MS spectrum of O-deacylated LPS from NTHi isolate 1209 showing quadruply charged ions The peak at m/z 650.1 corresponds to a glycoform with the composition PCho•Hex 3 •Hep 3 •PEtn 1 •P 1 •Kdo•Lipid A-OH The peak at m/z 697.2 corresponds to a glycoform with the composition Hex 4 •Hep 4 •PEtn 1 •P 1 •Kdo•Lipid A-OH Sodiated adduct ions are indicated by asterisks (*).

Table 2 Negative ion ESI-MS data and proposed compositions for NH 3 -treated OS preparations OS-1¢, OS-1¢-A and OS-1¢-B derived from LPS of NTHi isolate 1209 Average mass units were used for calculation of molecular mass values based on proposed compositions as follows: Hex, 162.14; HexNAc, 203.19; Hep, 192.17; AnKdo-ol, 222.20; PEtn, 123.05 and PCho, 165.13 Relative abundance was estimated from the area of molecular ion peak relative to the total area (expressed as percentage) ND, not detected.

Observed ions (m/z)

(M-2H)2–

Molecular mass (Da) Relative abundance (%)

Proposed composition Observed Calculated OS-1¢ OS-1¢-A OS-1¢-B

623.4 1248.8 1249.0 Trace a ND 5 PCho•Hex 1 •Hep 3 •PEtn 1 •AnKdo-ol

785.3 1572.6 1573.3 70 80 30 PCho•Hex 3 •Hep 3 •PEtn 1 •AnKdo-ol

968.2 1938.4 1938.6 Trace 2 ND PCho•HexNAc 1 •Hex 4 •Hep 3 •PEtn 1 •AnKdo-ol

798.8 1599.6 1600.4 Trace ND 3 Hex 3 •Hep 4 •PEtn 1 •AnKdo-ol

a Trace amounts, defined as peaks representing less than 1% of the base peak.

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For the major Hep3-glycoform with the composition

Hex3•Hep3•AnKdo-ol ([M + Na]+1671.8 Da), ion

selec-tion and collisional activaselec-tion of the precursor ion at m/z

1671.8 provided the MS2 spectrum shown in Fig 3 The

ions at m/z 1453.6 and 1249.5 indicated losses of a single

nonreducing terminal-Hex (t-Hex) and the nonreducing

fragment t-Hex-Hex, respectively The fragment at m/z

1001.5 (loss of t-Hex-Hex–Hep) and its trisaccharide

counterpart at m/z 693.4 resulting from cleavage between

HepII and HepIII, indicated the dihexose moiety to be

attached to HepIII The ions at m/z 753.4

(t-Hex–Hep-AnKdo-ol) and 941.4 (the counterpart) resulting from

cleavage between HepI and HepII, finally, showed a

terminal Hex residue to be linked to HepI Loss of the

terminal AnKdo-ol residue was also observed (as in almost

every MS2spectrum) from the ion at m/z 1393.5

For the Hep3-glycoform with the composition Hex4•

Hep3•AnKdo-ol ([M + Na]+ 1875.9 Da), three isomers

were shown to be present [Table 3, o¼ 3, q ¼ 1 (I), o ¼ 2,

q¼ 2 (II), o ¼ 1, q ¼ 3 (III)] Ions in the MS2spectrum at

m/z 1657.7, 1453.6 and 1249.5 corresponded to losses of t-Hex (from I, II and III), t-Hex-Hex (I, II and III) and t-Hex-Hex-Hex (I and III), respectively Isomer III could be derived from the ion pairs at m/z 753.3/1145.3 (cleavage HepI–HepII) and 1001.5/897.5 (cleavage HepII–HepIII) Isomer II was derived from the fragment pairs at m/z 957.5/ 941.3 and 1205.5/693.3 and isomer I, finally, from the ion pair at m/z 1161.4/737.4 and from the ion at m/z 1409.9

MS3 experiments on selected product ions confirmed the assigned structures For the structures containing HexNAc residues, it was observed that cleavage of the glycosidic bonds were highly favoured on the reducing side of the HexNAc residues [27] To obtain unambiguous results, it was often necessary to perform MS3 experiments on the product ion after loss of t-HexNAc or t-Hex-HexNAc

Fig 2 ESI-MS spectra of permethylated dephosphorylated OS derived

from LPS of NTHi isolates 1209 (A) and 1233 (B) showing singly

charged ions, [M + Na] + (A) Ions corresponding to selected

Hep3-glycoforms are labelled (B) Ions corresponding to selected

Hep4-glycoforms are labelled.

Table 3 Structures of the Hep3-glycoforms of NTHi isolates 1209 and

1233 as indicated by ESI-MSnon permethylated dephosphorylated OS Subscripts denoted by the letters m, n, o, p and q indicate the number

of glycose residues in the following structure:

ND, not determined.

Relative abun-dance a (%) Structure

Relative abundance b

Glycoform 1209 1233 m n o p q 1209 1233

0 0 0 0 1 Trace Hex2 3.6 2.1 0 0 2 0 0 Low Medium

0 0 1 0 1 High Medium

0 0 0 0 2 Trace Trace

0 0 2 0 1 – Trace

0 0 1 0 2 High Medium

0 0 0 0 3 – Trace Hex4 10.4 30.1 0 0 3 0 1 Trace Trace

0 0 2 0 2 Medium Low

0 0 1 0 3 Medium High Hex5 1.9 3.2 0 0 3 0 2 High Medium

0 0 2 0 3 Trace Medium Hex6 0.7 3.2 0 0 3 0 3 High High

HexNAc1Hex4 1.9 1.5 0 0 1 1 3 High High HexNAc1Hex5 0.7 0.9 0 0 2 1 3 Medium Medium

1 1 2 0 2 Medium Medium HexNAc1Hex6 – 1.0 1 1 2 0 3 High

a Relative abundance for each glycoform Estimated from the area

of molecular ion peak relative to the total area in the MS spectrum (expressed as percentage).bRelative abundance for the isomers of each glycoform Estimated from the intensity of the fragments in

MS2 experiments and indicated as follows: high (over 80%), medium (30–80%), low (2–30%), trace (below 2%).

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Elucidation of the Hep4-glycoforms introduced an

addi-tional level of complexity, as ions resulting from cleavages of

outer-core glycosidic linkages in some cases could not be

mass differentiated from fragments resulting from HepII–

HepIII ruptures It was thus necessary to identify product

ions resulting from cleavages between HepI and HepII with

unique masses due to the AnKdo-ol moiety For the major

Hep4-glycoform with the composition Hex4•Hep4

•AnKdo-ol ([M + Na]+ 2124.0 Da), ions in the MS2 spectrum

(precursor ion [M + 2Na]2+1073.5 Da) (Fig 4A) at m/z

1905.9, 1701.7 (counterpart at m/z 445.3) and 1453.6

(counterpart at m/z 693.3) corresponded to losses of

t-Hex, t-Hex-Hex and t-Hex-Hex–Hep The fragments at

m/z 1205.6 (loss of t-Hex-Hex–Hep–Hep) and 941.5 (the

counterpart) indicated a dihexose moiety to be linked to

HepIII An MS3experiment on m/z 1205.6 (Fig 4B) resul-ted in fragments at m/z 987.5 (loss of t-Hex), 739.3 (loss of t-Hex–Hep) and 693.3 (corresponding to t-Hex–Hep-Hex), which showed the trisaccharide element Hex–Hep-Hex to

be attached to HepI The topology of the other glycoforms were determined in a similar manner (data not shown)

Table 4 Structures of the Hep4-glycoforms of NTHi isolates 1209 and

1233 as indicated by ESI-MSnon permethylated dephosphorylated OS.

Subscripts denoted by the letters m, n, o and p indicate the number of

glycose residues in the following structure:

ND, not determined.

Glycoform

Relative

abundance a

(%) Structure

Relative abundanceb

1209 1233 m n o p 1209 1233

0 0 0 1 Low Medium

0 1 0 1 Medium Medium

0 0 0 2 Medium Medium

0 1 0 2 High Medium

Hex5 2.7 12.6 0 2 0 2 Medium Medium

0 1 0 3 Medium Medium

HexNAc1Hex5 0.4 0.7 1 2 0 2 Medium Medium

0 1 1 3 Medium Medium HexNAc1Hex6 0.3 1.2 1 2 0 3 Medium Medium

0 2 1 3 Medium Medium

a Relative abundance for each glycoform Estimated from the area

of molecular ion peak relative to the total area in the MS spectrum

(expressed as percentage) b Relative abundance for the isomers of

each glycoform Estimated from the intensity of the fragments in

MS2 experiments and indicated as follows: high (over 80%),

medium (30–80%), low (2–30%), trace (below 2%).

Fig 3 ESI-MS2 analysis of permethylated dephosphorylated OS derived from LPS of NTHi isolate 1209 Product ion spectrum of [M + Na]+m/z 1671.8 corresponding to a glycoform with the com-position Hex 3 •Hep 3 •AnKdo-ol The proposed structure is shown in the inset.

Fig 4 ESI-MSn analysis of permethylated dephosphorylated OS derived from LPS of NTHi isolate 1209 (A) MS2 spectrum of [M + 2Na]2+ m/z 1073.5 corresponding to a glycoform with the composition Hex 4 •Hep 4 •AnKdo-ol The proposed structure is shown

in the inset (B) MS3spectrum of the fragment ion at m/z 1205.6.

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A large number of structural types were observed for the

Hep3-glycoforms (15 found) and Hep4-glycoforms (13

found), all of which can be represented by structures I and

II (Hep3-glycoforms) and structure III (Hep4-glycoforms)

in Scheme 2

Structural characterization of the major glycoforms was

achieved by NMR spectroscopy (see below) In order to

decrease the OS heterogeneity and thereby simplify the

elucidation by NMR, OS-1¢ was repeatedly

chromato-graphed on a P-4 column with intermediate selection for the

Hep3- and Hep4-glycoforms (by ESI-MS) The final result

was a major fraction (OS-1¢-A, 4.4 mg) in which the

Hep3-glycoforms accounted for about 95%, and a minor fraction

(OS-1¢-B, 1.0 mg) in which the Hep4-glycoforms accounted

for about 60% (Table 2) Sugar analysis of OS-1¢-A and

OS-1¢-B indicated Glc, Gal and L,D–Hep in ratios of

26 : 48 : 26 and 29 : 37 : 34, respectively Methylation

analysis of OS-1¢-A (Table 5) indicated terminal-Gal

(t-Gal), 4-substituted-Gal (4-Gal), 4-Glc, 3-Gal, 6-Glc,

4,6-disubstituted-Glc (4,6-Glc), 2–Hep, 3,4–Hep and 2,6–Hep in

the relative proportions 27 : 7 : 37 : 2 : 2 : 2 : 17 : 4 : 2

The methylation analysis of OS-1¢-B showed significantly

higher levels of 6-Glc and 6–Hep, of which the latter sugar

derivative indicated the substitution-pattern for the fourth

heptose residue (shown below)

Characterization of OS fractions and LPS-OH

from NTHi isolate 1209 by NMR

The1H NMR resonances of OS material and LPS-OH were

assigned by 1H-1H chemical shift correlation experiments

(DQF-COSY and TOCSY) Subspectra corresponding to

the individual glycosyl residues were identified on the basis

of spin-connectivity pathways delineated in the1H chemical

shift correlation maps, the chemical shift values, and the

vicinal coupling constants From the glycoform

composi-tions of the different oligosaccharide fraccomposi-tions determined

by ESI-MS (Table 2), the spin-systems could more easily be

identified as originating from either the Hep3- or the

Hep4-glycoform population The 13C NMR resonances of OS

fractions and LPS-OH were assigned by heteronuclear

1H-13C chemical shift correlation in the1H detected mode (HSQC) The chemical shift data obtained for the Hep4-glycoforms are summarized in Table 6 and are consistent

Scheme 2 Structures representing the various Hep3- and Hep4-glycoforms in isolates 1209 and 1233 Truncated structures are indicated by ÆÆÆÆ.

Table 5 Linkage analysis data for OS preparations derived from LPS of NTHi isolates 1209 and 1233 Trace amounts (defined as peaks representing less than 3% of the base peak) of 2,3,4,6-Me 4 -Glc [assigned as D -Glcp-(1fi], 2,3,4,6,7-Me 5 –Hep [ L , D –Hepp-(1fi], 2,3,4,6-Me 4 -GalN [ D -GalpNAc-(1fi] and 2,3,6-Me 3 -GlcN [fi4)- D -GlcpNAc-(1fi] were also indicated.

Methylated sugara T gm

b

Relative detector response (%)

Linkage assignment

a 2,3,4,6-Me 4 -Glc represents 1,5-di-O-acetyl-2,3,4,6-tetra-O-methyl- D -glucitol-1-d 1 , etc b Retention times (T gm ) are reported relative to 2,3,4,6-Me -Glc (T 1.00).

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with each D-sugar residue being present in the pyranosyl

ring form Further evidence for this conclusion was

obtained from NOE data which also served to confirm

the anomeric configurations of the linkages and, together

with an HMBC experiment on OS-1¢, determined the

monosaccharide sequence

Characterization of the Kdo-lipidA-OH element ESI-MS

data (Table 1), fatty acid compositional analysis (yielding

3-hydroxytetradecanoic acid) and NMR experiments on

LPS-OH (data not shown, giving similar results as for

NTHi strains 486 [15] and 1003 [17]) indicated the presence

of the usual Kdo-lipid A-OH element in isolate 1209 As

observed earlier [15,17], two spin-systems could be traced

for the single a-linked Kdo residue, probably due to the

partial occurrence of PEtn attached to the phosphate group

at O-4 of Kdo [11,12,15]

Structure of the core region of the Hep3-glycoforms In

the 1H NMR spectra of OS-1¢-A (Fig 5A) and OS-1¢

(Fig 5B), anomeric resonances corresponding to the

inner-core region and GlcI could be observed at d 5.70–5.63

(HepII), 5.15–5.04 (HepI), 5.12 (HepIII) and 4.51 (GlcI),

respectively In addition, anomeric signals corresponding to

a globotetraose unit and sequentially truncated versions

thereof linked to HepIII, were identified at d 4.96 (t-a-D

-Galp), 4.93 (weak, 3-a-D-Galp), 4.70 (4-b-D-Glcp), 4.64

(weak, t-b-D-GalpNAc), 4.52 (4-b-D-Galp) and 4.46 (t-b-D

-Galp) as previously described for strain RM118 [12]

Spin-systems for the additional glycose residues shown by MSn

(see Scheme 2) could not be rationalized due to weak and

overlapping signals Signals for methyl protons of PCho were observed at d 3.25 and spin-systems for ethylene protons from this residue and from PEtn were similar to those observed earlier [15,17] 1H-31P NMR correlation studies (data not shown) demonstrated PCho to be located

at O-6 of GlcI and PEtn to substitute HepII at O-6, as previously observed in strain RM118 [12] and NTHi strain

1003 [17] The positions of the O-acetyl groups were determined from NMR experiments on OS-1 Intense signals from methyl protons of the O-acetyl groups were observed at d 2.20/2.18, which correlated to13C signals at d 21.1 in the HSQC spectrum For GlcI, a spin-system was found where characteristic downfield shifts were obtained for the signals from H-4 and C-4, consistent with acetylation

at O-4 as previously described for NTHi strain 1003 [17] HepIII was indicated to be acetylated at O-3 as character-istic downfield shifts were obtained for the signals from H-3 and C-3, as previously described for strain 1003 [17] A crosspeak from the ester-linked glycine substituent was also observed at d 3.99/40.7 (in the HSQC spectrum) due to correlation between the methylene proton and its carbon From the combined data, the structure in Scheme 3 is proposed for the globotetraose-containing Hep3-glycoform (HexNAc1Hex4) of NTHi isolate 1209

Structure of the core region of the Hep4-glycoforms In the 1H NMR spectrum of OS-1¢-B (Fig 5C), anomeric resonances of the three heptose residues (HepI–HepIII) in the inner-core region were observed at d 5.73–5.62 (1H, not resolved), 5.18–5.05 (1H, not resolved) and 4.99 (1H, not resolved) The Hep ring systems were identified on the basis

Table 6.1H and13C NMR chemical shifts for Hep4-glycoforms of OS-1¢-B derived from LPS of NTHi isolate 1209 Data was recorded in D 2 O at

22 C Pairs of deoxyprotons of reduced AnKdo were identified in the DQF-COSY spectrum at 2.19–1.55 p.p.m.

Residue Glycose unit H-1/C-1 H-2/C-2 H-3/C-3 H-4/C-4 H-5/C-5 H-6 A /C-6 H-6 B H-7 A /C-7 H-7 B

HepI fi3,4)- L -a- D –Hepp-(1fi 5.05–5.18a 4.00–4.06a 4.01–4.04a 4.25b –c 4.13b – –

97.4–98.8 a 71.1–71.2 a 73.8 74.3 – 68.5 – HepII fi2)- L -a- D –Hepp-(1fi 5.62–5.73a 4.18 3.94 3.96 3.77 4.57 3.71 3.89

6›

GlcI fi6)-b- D -Glcp-(1fi 4.51 3.40 3.44 3.52 3.59 3.87 3.96

GlcII fi4)-b- D -Glcp-(1fi 4.54 3.41 3.72 3.71 3.71 3.84 4.00

GalII* fi4)-b- D -Galp-(1fi 4.52 3.59 3.75 4.05 3.79 d – –

62.7 40.8

a Several signals were observed for HepI and HepII due to heterogeneity in the AnKdo moiety b H-4/H-6 of HepI were identified at d 4.25/ 4.13 by NOE from GlcI c –, not obtained owing to the complexity of the spectrum d Tentative assignment from NOE data.

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of the observed small J1,2-values and their a-configurations

were confirmed by the occurrence of single intraresidue

NOE between the respective H-1 and H-2 resonances as

observed earlier [15,17] Several signals for methylene

protons of AnKdo-ol were observed in the DQF-COSY

and TOCSY spectra of OS-1¢-B in the region d 2.19–1.55

As previously observed [10,15,17], several anhydro-forms of

Kdo are formed during the hydrolysis by elimination of

phosphate or pyrophosphoethanolamine from the C-4

position, which causes both the signal splitting of the

methylene protons and the appearance of several anomeric

signals for HepI and HepII (Table 6) The occurrence of intense transglycosidic NOE connectivities between the proton pairs HepIII H-1/HepII H-2, HepII H-1/HepI H-3 (LPS-OH and OS-1¢-B) and HepI H-1/Kdo H-5 and H-7 (LPS-OH) confirmed the sequence of the heptose-contain-ing trisaccharide unit and the point of attachment to Kdo as

L-a-D–Hepp-(1fi2)-L-a-D–Hepp-(1fi3)-L-a-D –Hepp-(1fi5)-a-Kdop 1H-31P NMR correlation studies demonstrated PEtn to be linked to O-6 of HepII as a31P resonance at d 0.03 correlated to the signals from H-6 of HepII (d 4.57) and the methylene proton pair of PEtn (d 4.13)

Fig 5 600 MHz 1 H NMR spectra of OS-1¢-A (A), OS-1¢ (B) and OS-1¢-B (C) derived from LPS of NTHi isolate 1209 showing the anomeric regions (A) Anomeric resonances that are characteristic for the Hep3-glycoforms are labelled Also indicated is an ethylene proton signal from PCho at d 4.38 (C) Anomeric resonances that are characteristic for the Hep4-glycoforms are labelled.

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In OS-1¢-B, relatively large J1,2-values (about 7.7 Hz) of

the anomeric resonances observed at d 4.54, 4.52 (weak),

4.51, 4.51 and 4.46 indicated each of the corresponding

residues to have the b-anomeric configuration The residues

with anomeric signals at d 4.96 (not resolved) and 4.96

(weak, J 4.0 Hz) were identified as having the a-anomeric

configuration Further evidence for the anomeric

configu-rations was obtained from the occurrence of intraresidue

NOE between the respective H-1, H-3 and H-5 resonances

(b-configuration) or between H-1 and H-2

(a-configur-ation) On the basis of the chemical shift data and the large

J2,3, J3,4and J4,5-values (9 Hz), the residues with anomeric

shifts of d 4.51 and 4.54 could be attributed to the 6-Glc

(GlcI) and 4-Glc (GlcII) identified by methylation analysis

(Table 5) On the basis of low J3,4and J4,5-values (< 4 Hz)

and chemical shift data, the residues with anomeric

resonances at d 4.51, 4.46, 4.96 (weak, J 4.0 Hz) and

4.52 were attributed to the t-Gal (GalI, GalII and GalIII)

and 4-Gal (GalII*) identified by linkage analysis The

residue with anomeric signal at d 4.96 (not resolved) was

attributed to the 6–Hep (HepIV) identified in the methyla-tion analysis, on the basis of the small J1,2-value and chemical shift data

Interresidue NOE were observed between the proton pairs GalI H-1/HepIV H-6, HepIV H-1/GlcI H-6A, H-6B and GlcI H-1/HepI H-4 and H-6 (Fig 6) which established the presence of the tetrasaccharide unit b-D-Galp-(1fi6)-L -a-D–Hepp-(1fi6)-b-D-Glcp-(1fi4)-L-a-D–Hepp-(1fi This monosaccharide sequence was also confirmed by transgly-cosidic correlations in an HMBC experiment, where corre-lations were seen between GalI C-1/HepIV H-6, GalI H-1/ HepIV C-6 and HepIV H-1/GlcI C-6 The occurrence of interresidue NOE connectivities between the proton pairs GalII H-1/GlcII H-4 and GlcII H-1/HepIII H-1 and H-2 (Fig 6) established the sequence of a disaccharide unit and its attachment point to HepIII as b-D-Galp-(1fi4)-b-D -Glcp-(1fi2)-L-a-D–Hepp-(1fi The lactose element was shown to be further chain extended by an a-D-Galp residue

as transglycosidic NOE between GalIII H-1/GalII* H-4 and GalII* H-1/GlcII H-4 were observed Spin-systems for Scheme 3 Structure proposed for a Hep3-glycoform (HexNAc1Hex4) of NTHi isolate 1209.

Fig 6 Selected regions from the 600 MHz 2D NOESY spectrum (mixing time 200 ms) of OS-1¢-B derived from LPS of NTHi isolate 1209 Both regions were plotted at the same contour levels Cross-peaks that are characteristic for the Hep4-glycoforms are labelled.

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