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Tài liệu Báo cáo khoa học: A novel type of highly negatively charged lipooligosaccharide from Pseudomonas stutzeri OX1 possessing two 4,6-O-(1-carboxy)-ethylidene residues in the outer core region ppt

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Tiêu đề A novel type of highly negatively charged lipooligosaccharide from Pseudomonas stutzeri OX1 possessing two 4,6-O-(1-carboxy)-ethylidene residues in the outer core region
Tác giả Serena Leone, Viviana Izzo, Alba Silipo, Luisa Sturiale, Domenico Garozzo, Rosa Lanzetta, Michelangelo Parrilli, Antonio Molinaro, Alberto Di Donato
Trường học Università degli Studi di Napoli Federico II
Thể loại báo cáo khoa học
Năm xuất bản 2004
Thành phố Napoli
Định dạng
Số trang 14
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All sugars were present as pyranose rings, as indicated by 1H- and 13C-NMR chemical shifts and by the HMBC spectrum that showed for all residues intraresidual scalar connectivity between

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A novel type of highly negatively charged lipooligosaccharide

Serena Leone1, Viviana Izzo2, Alba Silipo1, Luisa Sturiale3, Domenico Garozzo3, Rosa Lanzetta1,

Michelangelo Parrilli1, Antonio Molinaro1and Alberto Di Donato2

1

Dipartimento di Chimica Organica e Biochimica and2Dipartimento di Chimica Biologica, Universita` degli Studi di Napoli Federico II, Napoli, Italy;3Istituto per la Chimica e la Tecnologia dei Materiali Polimerici – ICTMP – CNR, Catania, Italy

Pseudomonas stutzeriOXI is a Gram-negative

microorgan-ism able to grow in media containing aromatic

hydrocar-bons A novel lipo-oligosaccharide from P stutzeri OX1

was isolated and characterized For the first time, the

pres-ence of two moieties of 4,6-O-(1-carboxy)-ethylidene

resi-dues (pyruvic acid) was identified in a core region; these two

residues were found to possess different absolute

configur-ation The structure of the oligosaccharide backbone was

determined using either alkaline or acid hydrolysis Alkaline

treatment, aimed at recovering the complete carbohydrate

backbone, was carried out by mild hydrazinolysis

(de-O-acylation) followed by de-N-acylation using hot KOH The

lipo-oligosaccharide was also analyzed after acid treatment,

attained by mild hydrolysis with acetic acid, to obtain

information on the nature of the phosphate and acyl groups

The two resulting oligosaccharides were isolated by gel permeation chromatography, and investigated by composi-tional and methylation analyses, by MALDI mass spectro-metry, and by1H-,31P- and13C-NMR spectroscopy These experiments led to the identification of the major oligosac-charide structure representative of core region-lipid A All sugars areD-pyranoses and a-linked, if not stated otherwise Based on the structure found, the hypothesis can be ad-vanced that pyruvate residues are used to block elongation

of the oligosaccharide chain This would lead to a less hydrophilic cellular surface, indicating an adaptive response

of P sutzeri OX1 to a hydrocarbon-containing environment Keywords: Pseudomonas stutzeri OXI; lipopolysaccharide; NMR spectroscopy; mass spectrometry; pyruvic acid

Environmental pollution is recognized worldwide as an

emergency for its negative effects on the biosphere and on

human health Bioremediation strategies have recently been

devised, based on microbial biotransformations, given the

metabolic potential of selected microorganisms, in

partic-ular by Gram-negative bacteria, and their adaptability to

many different pollutants [1]

Pseudomonas stutzeriOX1 is a Gram-negative bacterium

isolated from the activated sludge of a wastewater treatment

plant, and endowed with unusual metabolic capabilities for

the degradation of aromatic hydrocarbons [2] In fact, in

contrast with other Pseudomonas strains, this microrganism

is able to grow on a large spectrum of aromatic compounds

including phenol, cresol and dimethylphenol, and on

nonhydroxylated molecules such as toluene and o-xylene,

the most recalcitrant isomer of xylene Moreover, it is able to metabolize tetrachloroethylene (PCE), one of the ground-water pollutants commonly resistant to degradation [3] Degradation of aromatic hydrocarbons by aerobic bac-teria comprises an upper pathway, which produces dihy-droxylated aromatic intermediates by the action of monooxygenases, and a lower pathway, which processes these intermediates to molecules that enter the citric acid cycle [4] We have recently cloned, expressed and charac-terized three different enzymatic systems from P.stutzeri OX1: (a) toluene-o-xylene monooxygenase (ToMO) [5], endowed with a broad substrate specificity [6] and (b) phenol hydroxylase (PH) [7], both belonging to the upper pathway; and (c) catechol 2,3 dioxygenase (C2,3O) (A di Donato, unpublished observations), the gateway enzyme

to the lower pathway However, chemical toxicity of wastes can hamper the use of this and other microorganisms in bioremediation strategies, especially when organic solvents are present at high concentrations

Several mechanisms have been described that contribute

to solvent resistance in Gram-negative bacteria, all based on structural changes in outer and inner membranes [8] Different short- and long-term responses have been observed including modifications of the fatty acid and phospholipid composition of the membrane, extrusion mechanisms using vesicles, and energy-dependent active efflux pumps that export toxic organic solvents outside the cytoplasm [9]

Correspondence to A Molinaro, Dipartimento di Chimica Organica e

Biochimica, Universita` di Napoli Federico II, Complesso

Universitario Monte S Angelo, via Cintia 4, 80126 Napoli, Italy.

Fax: + 39 081 674393, Tel.: + 39 081 674123,

E-mail: molinaro@unina.it

Abbreviations: DEPT, distorsionless enhancement by polarization

transfer; GlcN, 2-amino-2-deoxy-glucose; Hep, L -glycero- D

-manno-heptose; Kdo, 3-deoxy- D -manno-oct-2-ulosonic acid;

LOS, lipooligosaccharide; LPS, lipopolysaccharide.

(Received 1 March 2004, revised 23 April 2004,

accepted 30 April 2004)

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Even though lipopolysaccharides (LPSs) are major

components of the outer membrane of Gram-negative

bacteria, little is known about their role and their chemical

modifications under environmental stress [1,9] It is certain,

however, that LPSs are unique and vital components of

these microorganisms and that they play an important role

in their survival and their interaction with the environment

[10,11] Smooth-form lipopolysaccharides (S-LPSs) include

three regions, the O-specific polysaccharide (or O-antigen),

the oligosaccharide region (core region) and the lipid part

(lipid A) Conversely, rough (R) form LPSs do not possess

an O-specific polysaccharide and are frequently named

lipo-oligosaccharides (LOSs) LOSs have been found either in

wild-type strains and in mutant strains harboring mutations

in the genes encoding enzymes of the biosynthesis and/or

the transfer of the O-specific polysaccharide [12,13]

The core region from both smooth and rough forms of

enteric bacteria generally includes oligosaccharides built of

up to 11 units [12,13], and consists of two distinct domains:

an inner core, characterized by the presence of 3-deoxy-D

-manno-oct-2-ulosonic acid (Kdo) and L-glycero-D

-manno-heptose (Hep), and an outer core, which contains common

sugars It is worth noting that the core oligosaccharide of

LOSs has been reported to play a role in the interaction of

the microorganism with the environment [12,13]

In this paper, the structural characterization of the

carbohydrate backbone of the rough form LPS of P stutzeri

OX1 is reported, obtained by chemical analyses,

MALDI-TOFmass spectrometry and two-dimensional NMR

spectroscopy This novel oligosaccharide chain was found

to possess unusual structural features, which might be

biologically relevant Among these is a GalN residue

substituted by two gluco-configured residues, which are

blocked at position O-4 and O-6 by a pyruvate ketal linkage,

a structure peculiar and new to lipopolysaccharide core

regions

Based on this finding, the hypothesis can be advanced

that the insertion of pyruvate residues at the end of the

oligosaccharide chain blocks its elongation, thereby leading

to a shorter LOS and hence to a less hydrophilic cellular

surface Moreover, as it has already been proposed [1,9],

these residues may also contribute to the rigidity and

stability of the Gram-negative cell wall by binding cations

Experimental procedures

Bacterial growth and LPS extraction

Cells were routinely grown on M9-agar plates supplemented

with 10 mMmalic acid as the sole carbon source, at 27C

For growth in liquid medium, 1 mL was inoculated with a

single colony from a fresh plate, and grown for 18 h at 27C

with constant shaking This saturated culture was used to

inoculate 100 mL of the same medium and grown at 27C

until D600 1 Final growth was started by inoculating the

appropriate volume of the latter culture into 1 L of fresh

medium, to D600¼ 0.02 Cells were grown at 27 C, until

D600¼ 1 was reached and then recovered by centrifugation

at 3000 g for 15 min at 4C, washed with an isotonic buffer

and lyophilized Growth was carried out in M9 salt medium

supplemented with 4 mM phenol as the sole carbon and

energy source Dried cell yield was 0.13 gÆL)1

Dried cells were extracted three times with a mixture of aqueous 90% phenol/chloroform/petroleum ether (50 mL,

2 : 5 : 8 v/v/v) as described previously [14] After removal of the organic solvents under vacuum, the LOS fraction was precipitated from phenol with water, washed first with aqueous 80% (v/v) phenol, and then three times with cold acetone, each time centrifuged as above, and lyophilized (the yield was 90 mg of LOS, about 4.3% of the dry mass) Sodium dodecyl sulfate polyacrylamide gel electrophor-esis (SDS/PAGE) was performed as described previously [15] For detection of LPS and LOS, gels were stained with silver nitrate [15]

Isolation of oligosaccharides

An aliquot of LOS (40 mg) was dissolved in anhydrous hydrazine (2 mL), stirred at 37C for 90 min, cooled, poured into ice-cold acetone (20 mL), and allowed to precipitate The precipitate was then centrifuged (3000 g,

30 min, 4C), washed twice with ice-cold acetone, dried, dissolved in water and lyophilized (32 mg, 80% of the LOS) This material was de-N-acylated with 4MKOH as described [16] Salts were removed using a Sephadex G-10 (Pharmacia) column (50· 1.5 cm) The resulting oligosac-charide 1 constitutes the complete carbohydrate backbone

of the lipid A-core region (16 mg, 40% of the LOS) Another aliquot of LOS (40 mg) was hydrolyzed in 1% (v/v) acetic acid (100C, 2 h) and the precipitate (lipid A) was removed by centrifugation (8000 g, 30 min) The supernatant was separated by gel-permeation chromatog-raphy on a P-2 column (85· 1.5 cm) Two fractions were obtained, the first contained oligosaccharide 2 (28 mg, 70%

of the LOS), whereas the second fraction contained a mixture of reducing pyranose, furanose, anhydro and lactone forms of 3-deoxy-D-manno-oct-2-ulosonic acid (3 mg, 7.5% of the LPSs)

General and analytical methods Determination of Kdo, neutral sugars, carbamoyl analysis, including the determination of the absolute configuration of the heptose residues, organic bound phosphate, absolute configuration of the hexoses, fatty acids and their absolute configuration, GLC and GLC-MS were all carried out as described previously [17–21] For methylation analysis of Kdo region, LOS was carboxy-methylated with methanolic HCl (0.1M, 5 min) and then with diazomethane to improve its solubility in dimethyl sulfoxide Methylation was carried out as described [22,23] LOS was hydrolyzed with 2M

trifluoroacetic acid (100C, 1 h), carbonyl-reduced with NaBD4, carboxy-methylated as described above, carboxyl-reduced with NaBD4(4C, 18 h), acetylated and analyzed

by GLC-MS

Methylation of the complete core region was carried out

as described previously [22–24] The sample was hydrolyzed with 4Mtrifluoroacetic acid (100C, 4 h), carbonyl-reduced with NaBD4, acetylated and analyzed by GLC-MS NMR spectroscopy

For structural assignments of oligosaccharides 1 and 2, 1D and 2D1H-NMR spectra were recorded on a solution of

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5 mg in 0.6 mL of D2O, at 55C or at 30 C, at pD 14 and

7 (uncorrected values), respectively 1H- and 13C-NMR

experiments were carried out using a Varian Inova 500 or a

Varian Inova 600 instrument, whereas for31P-NMR spectra

a Bruker DRX-400 spectrometer was used Spectra were

calibrated with internal acetone [dH 2.225, dC 31.45]

Aqueous 85% phosphoric acid was used as external

reference (0.00 p.p.m.) for31P-NMR spectroscopy

Nuclear Overhauser enhancement spectroscopy

(NOESY) and rotating frame Overhauser enhancement

spectroscopy (ROESY) were measured using data sets

(t1· t2) of 4096· 1024 points, and 16 scans were acquired

A mixing time of 200 ms was used Double quantum-filtered

phase-sensitive COSY experiments were performed with

0.258 s acquisition time, using data sets of 4096· 1024

points, and 64 scans were acquired Total correlation

spectroscopy experiments (TOCSY) were performed with a

spinlock time of 80 ms, using data sets (t1· t2) of

4096· 1024 points, and 16 scans were acquired In all

homonuclear experiments the data matrix was zero-filled in

the F1 dimension to give a matrix of 4096· 2048 points and

was resolution enhanced in both dimensions by a shifted

sine-bell function before Fourier transformation Coupling

constants were determined on a first-order basis from 2D

phase sensitive double quantum filtered correlation

spectro-scopy (DQF-COSY) [25,26] Intensities of NOE signals were

classified as strong, medium and weak using cross-peaks

from intraring proton-proton contacts for calibration

Heteronuclear single quantum coherence (HSQC) and

heteronuclear multiple bond correlation (HMBC)

experi-ments were measured in the1H-detected mode via single

quantum coherence with proton decoupling in the 13C

domain, using data sets of 2048· 512 points, and 64 scans

were acquired for each t1value Experiments were carried

out in the phase-sensitive mode according to the method of

States et al [27] A 60 ms delay was used for the evolution

of long-range connectivities in the HMBC experiment In all

heteronuclear experiments the data matrix was extended to

2048· 1024 points using forward linear prediction

extra-polation [28,29]

MALDI-TOF analysis

MALDI mass spectra were carried out in the negative

polarity in linear or in reflector mode on a Voyager STR

instrument (Applied Biosystems, Framingham, MA, USA)

equipped with a nitrogen laser (k¼ 337 nm) and provided

with delayed extraction technology Ions formed by the

pulsed laser beam were accelerated through 24 kV Each

spectrum is the result of approximately 200 laser shots A

saturated solution of 2,4,6-trihydroxyacetophenone was

used as the matrix

Results

Isolation and characterization of the LOS fraction

The LOS fraction was isolated from dried cells by extraction

with phenol/chloroform/petroleum ether, and further

puri-fied with gel permeation chromatography SDS/PAGE

showed, after silver nitrate gel staining, the presence of fast

migrating species in agreement with their oligosaccharide

nature Compositional monosaccharide analysis of the LOS fraction led to the identification of L,D-Hep, D-GalN,

D-GlcN, D-Glc, Kdo (2 : 1.0 : 3.2 : 1.1 : 1.8) and trace amounts ofL-Rha 7-O-Carbamoyl-L,D-Hep was present in

a stoichiometric ratio withL,D-Hep Methylation analysis showed the presence of terminal Kdo, 6-substituted-HexN, 3-substituted-Hep, 4,5-disubstituted-Kdo, 3,4-disubstituted-HexN, 4,6-disubstituted-Glc, 4,6-disubstituted-HexN and,

in small amounts, terminal-Rha and 6-substituted-Glc

In addition, the disaccharide 7-O-carbamoyl-Hep-(1fi3)-Hep was found

Fatty acid analysis revealed the presence of typical fatty acids of pseudomonads LPS [30], i.e (R)-3-hydroxydodec-anoic acid [C12:0 (3-OH)], present exclusively in amide linkage and (R)-3-hydroxydecanoic [C10:0 (3-OH)] (S)-2-hydroxydecanoic [C12:0 (2-OH)] and dodecanoic acid (C12:0), present in ester linkage Moreover, phosphate colorimetric assays gave positive results

The LOS fraction was then subjected to both alkaline and acid degradations and complete structural characterization

NMR spectroscopy and MALDI-TOF MS spectrometry

of oligosaccharide 1 Oligosaccharide 1 was isolated by gel permeation chroma-tography after complete deacylation of the LOS of

P stutzeriOX1 The complete structure of fully deacylated oligosaccharide 1 (Fig 1) was determined by1H-,31P- and

13C-NMR spectroscopy Chemical shifts were assigned using DQF-COSY, TOCSY, NOESY, ROESY, 1H,13 C-DEPT-HSQC,1H,31P-HSQC,1H,13C-HMBC and1H,13 C-HSQC-TOCSY experiments Anomeric configurations were assigned on the basis of 1H and13C chemical shifts,

of3JH1,H2values determined from the DQF-COSY experi-ment (Table 1), and of1JC1,H1values derived by 1H,13 C-HSQC spectrum recorded without decoupling during acquisition

All sugars were present as pyranose rings, as indicated by

1H- and 13C-NMR chemical shifts and by the HMBC spectrum that showed for all residues intraresidual scalar connectivity between H-1/C-1 and C-5/H-5 atoms (for Kdo units, between C-2 and H-6) The anomeric region of the

1H-NMR spectrum (Fig 2) showed seven major signals in the region between 5.46 and 4.47 p.p.m relative to seven different spin systems (A–G, in order of decreasing chemical shift), and in addition two AB methylene resonances at high fields, typical of Kdo residues (I–L) Each spin system was completely assigned by COSY and TOCSY starting from anomeric resonances For Kdo residues I and L the starting point was the H-3 diastereotopic methylene resonance Both spin systems A and D (5.46 and 5.27 p.p.m.) were characterized by low3JH1, H2and3JH2, H3values, indicative

of two a-manno-configured residues Moreover, all other cross peaks within each spin system were assigned in the TOCSY spectrum from H-2 proton signals, leading to their identification as two heptoses Residue B was identified as a-gluco-configured hexosamine on the basis of chemical shifts and 3JH,Hvalues Moreover, based on its anomeric signal at 5.42 p.p.m present as a double doublet (3JH1,H2¼ 2.9 Hz and3JH1,P¼ 8.3 Hz), with one of the couplings due

to a phosphate signal as shown below, it was identified as GlcN I of the lipid A skeleton The spin system at

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Table 1 1 H, 13 C and 31 P NMR chemical shifts (p.p.m) of deacylated core-lipid A backbone (oligosaccharide 1) of LOS from P stutzeri OX1 Chemical shifts are relative to acetone and external aq 85% (v/v) phosphoric acid (1H, 2.225 p.p.m.;13C, 31.45 p.p.m.;31P, 0.00 p.p.m at 55 C).

31

31

13

Fig 1 The structure of oligosaccharide 1 obtained by alkaline hydrolysis of the core region of the LPS of P stutzeri OX1.

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5.32 p.p.m (C;3JH1, H2¼ 3.6 Hz) was identified as a-GalN

by its JH,Hvalues for H-3/H-4 and H-4/H-5, diagnostic of a

galactoconfiguration (3.4 Hz and less than 1 Hz,

respect-ively) Three spin systems E, F and G (doublets;3JH1, H2¼

8.6, 7.8 and 7.7 Hz, respectively) were identified as

b-gluco-configured monosaccharides given their large3JH,H-values

A further indication of their b configuration was the

observation of NOE contacts in the ROESY spectrum

among H-1, H-3 and H-5, for all E, F, G residues

The H-3 methylene signals of two a-Kdo residues were

present at 1.82 p.p.m (H-3ax) and 2.07 p.p.m (H-3eq)

(residue I), and 2.00 p.p.m (H-3ax) and 2.34 p.p.m

(H-3eq) (residue L), respectively Their a configuration

was established on the basis of the chemical shift of their

H-3eq protons and by measurement of the 3JH7,H8aand

3JH7,H8b coupling constants [31,32] Two methyl singlet

signals were present at higher fields, at 1.48 and 1.62 p.p.m.,

respectively Each methyl signal was in a 3 : 1 ratio with the

anomeric signals, i.e in a stoichiometric ratio

The13C-NMR chemical shifts could be assigned by a

DEPT-HSQC experiment, using the assigned 1H-NMR

spectrum Seven anomeric carbon resonances were

identi-fied (Table 1), numerous carbon ring signals and four

nitrogen-bearing carbon signals assigned to C-2 of B, C, F

and G spin systems Considering the13C chemical shifts of

nonsubstituted residues [33], several low-field shifted signals

indicated substitutions at O-3 of residue A, O-6 of residue B,

O-3 and O-4 of residue C, O-3 of residue D, O-4 and O-6 of

residues E and F, O-6 of residue G, O-5 and O-4 of residue

L, whereas I was a terminal residue In the high field region

of the spectrum two cross peaks at 1.48/25.2 and 1.62/ 17.2 p.p.m were present

Phosphate substitution was established on the basis of

31P-NMR spectroscopy The31P-NMR spectrum showed the presence of five monophosphate monoester signals (Table 1) The site of substitution was inferred by a

1H,31P-HSQC spectrum that showed correlations of 31P signals with H-1 B (GlcN), H-4 A and H-2 A (Hep I), H-4 G (GlcN) and H-6 D (Hep II)

The sequence of the monosaccharide residues was determined using NOE effects of the ROESY (Fig 3) and NOESY spectra, and by1H,13C-HMBC correlations The typical lipid A carbohydrate backbone was eventually assigned on the basis of the NOE signal between H-1 G and H-6a,b B In the case of Kdo units, which lack the anomeric proton, the sequence was inferred by NOE contacts between the methylene-proton H-3eq of Kdo L and H-6 of Kdo I, whereas Kdo L was substituted by heptose A as indicated by the NOE effect found between H-1 A and H-5 L, and, in addition, between H-5 A and H-3axL All of these NOE contacts were characteristic of the sequence a-L-glycero-D -manno-heptose-(1fi5)-[a-D-Kdo-(2fi4)]-a-D-Kdo [34,35]

Heptose A was, in turn, substituted at the O-3 position

by heptose D, as demonstrated by the NOE cross peak between H-1 D and H-3 A A disaccharide

7-O-carbamoyl-Fig 2.1H-NMR spectrum of oligosaccharide 1 The spectrum was recorded under the following conditions: 5 mg of oligosaccharide 1 in 0.6 mL

D 2 O, pD 14 at 30 C.

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Hep-(1fi3)-Hep was also identified by methylation analysis

of the intact LOS, thus, the carbamoyl group should be

attached to O-7 of the heptose moiety D The GalN C was

attached to the O-3 position of this last heptose as shown by

the NOE effect between the anomeric proton of GalN and

H-3 of D

GalN is the branching point of the chain and,

conse-quently, it should carry two sugar residues at O-3 and O-4

Indeed, the anomeric proton of b-glucose E gave a NOE

effect with H-3 of GalN, whereas the anomeric proton of

b-glucosamine F gave a NOE effect with H-4 of GalN

In determining the L Kdo location, its linkage to unit G

was deduced by exclusion In particular, the linkage to O-6

of G was inferred by taking into account the downfield shift

of the carbon signal C-6 (63.7 p.p.m., Table 1) indicating its

involvement in a glycosydic linkage

The HMBC spectrum confirmed the sequence proposed

for oligosaccharide 1, as it contained the significant

long-range correlations required for the determination of the

sequence and of the attachment points In fact, together

with intraresidual long-range cross-peaks, interresidual

long-range connectivity was found between H-5/C-5 L

and C-1/H-1 A, H-3/C-3 A and C-1/H-1 D, H3/C-3 D and

C-1/H-1 C, H-1/C-1 E and C-3/H-3 C, H-1/C-1 F and C-4/

H-4 C, H-1/C-1 G and C-6/H-6 B

The HMBC experiment was also crucial for the

identification and localization of the two methyl

groups belonging to noncarbohydrate constituents Plain

long-range correlations (Fig 4A) were found in the spectrum for each methyl signal The signal at 1.48 p.p.m correlated to two different carbon signals at 101.9 and 175.5 p.p.m., whereas the signal at 1.62 p.p.m correlated to two other signals at 99.5 and 175.8 p.p.m None of these four carbon signals was present in the HSQC spectrum These data pointed to two cyclic ketals

of pyruvic acid present on two distinct residues, namely E and F, whose C-4 and C-6 signals experienced a downfield displacement This was confirmed by the HMBC spec-trum where each ketal carbon signal of pyruvate residues correlated to H-4 and H-6 of E and F residues (b-D-Glc and b-D-GlcN, respectively) It should be noted that the signal discrepancy in the1H and13C chemical shifts of the two pyruvate moieties is due to the different absolute configuration at C-2 In fact, the methyl signal occurring

at 1.48 and 25.2 p.p.m is assigned to the S-pyruvate group, whereas the one occurring at 1.62 and 17.2 p.p.m

is assigned to an R-pyruvate group, as already described [36] Moreover, the ROESY spectrum (Fig 4B) was in complete agreement with the assignment above In fact, the methyl signal of the R-pyruvate residue at 1.62 p.p.m gave a strong NOE effect with H-4 and H-6aof residue F This is in agreement with an axial orientation of the methyl group on a 1,3-dioxane ring in a chair-like conformation in which H-4 and H-6aare sin diaxial with respect to it The methyl signal of S-pyruvate, being in equatorial orientation, only gave NOE effect with the

Fig 3 Section of the ROESY spectrum of oligosaccharide 1 Monosaccharide labels are as indicated in Fig 1 NOE cross-peaks are in black, in antiphase with diagonal (grey lines) Spectrum was recorded at pD 14, 55 C.

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adjacent H-6 of residue E Thus, all main spin systems

were assigned in the NMR spectra, and all chemical data

found a rational explanation

The presence of a minor spin system (10%) belonging to

rhamnose (anomeric signal at 4.89 p.p.m) and 6-substituted

glucose (overlapped with terminal glucose) might be

explained by the presence of a second outer core glycoform

in which rhamnose is attached at O-6 of the glucose residue,

which obviously lacks the pyruvate group

The MALDI mass spectrum confirmed the proposed

structure In fact, an ion peak at m/z 2188.4 (Fig 5A) was

present, corresponding to the complete carbohydrate

back-bone bearing five phosphate goups and two pyruvic acid

acetal residues Moreover, at higher laser intensity (Fig 5B)

various ion peaks related to fragments were found, all fitting

with the structure shown in Fig 1

In conclusion, the data above allowed the identification

of the carbohydrate backbone from alkaline degradation of

the rough form LPS from P stutzeri OX1

Isolation, NMR and MS analyses of oligosaccharide 2

from acetic acid hydrolysis

Further information on alkaline labile groups that could

be present in the core region (i.e acyl groups) was obtained

by treating the LOS with acetic acid to split the Kdo

linkage An oligosaccharide mixture was isolated after gel

permeation chromatography, which was purified further and the resulting oligosaccharide 2 (Fig 6) analyzed by compositional/methylation analyses, 2D NMR and mass spectrometry

Compositional and methylation analyses led to the identification of 3-substituted-L,D-Hep, 7-O-carbamoyl-3-substituted-L,D-Hep 3,4-disubstituted-D-GalN, terminal

D-glucose and terminal D-GlcN Traces of 5-substituted Kdo, 6-substituted-D-Glc and terminal L-rhamnose were also found

The1H-NMR spectrum revealed the absence of anomeric signals from GlcN I and GlcN II of Lipid A, the lack of pyruvate methyl groups, as a consequence of the cleavage of the ketal group under acid treatment, and the presence

of singlet signals at 2.00 p.p.m Methylene signals of Kdo were spread because of its presence as reducing end unit, i.e pyranose, furanose, anhydro and lactone forms present at same time The anomeric region of the spectrum consisted

of six main signals (Fig 6), five of which belonging to the main oligosaccharide backbone, named U–Z All

resonanc-es of the monosaccharidresonanc-es (Table 2) were obtained from 2D NMR spectroscopy (DQF-COSY, TOCSY, NOESY, ROESY, 1H,13C-DEPT-HSQC 1H,31P-HSQC, 1H,13 C-HMBC and 1H,13C-HSQC-TOCSY) Evaluation of chemical shifts and of 3JH,H coupling constants led to identification of residues Hep (U), 7-O-carbamoyl-Hep (V), GalN (X), GlcN (W), Glc (Z)

Fig 4 Sections of the high field region of the (A) ROESY and (B) HMBC spectra Correlations of pyruvate methyl groups are shown (A) The 4,6 Pyr-GlcN residue is drawn in the middle of the figure with arrows indicating the relevant NOE contacts between methyl protons of the R-pyruvate group and H-4 and H-6 of GlcN residue Spectra were recorded at pD 14, 55 C.

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Low-field shifted signals were present in the HSQC

spectrum indicating substitutions at O-3 (U, V and X) and

O-4 (X), whereas residues W and Z were not substituted

Cross-peaks were also detected only for two nitrogen atoms

bearing carbon signals, at 4.26/49.8 p.p.m (H-2/C-2 X) and

3.67/56.1 p.p.m (H-2/C-2 W), in agreement with the

absence of Lipid A disaccharide and with the presence of

a a-galacto and a b-gluco configured 2-amino-2-deoxy

hexoses Moreover, given the downfield H-2 chemical shifts

of the X and W residues, the amino groups should have

been present as acylamido

The high field proton region of the HMBC gave clues for

the identification of the nature of acyl groups Three

different singlet signals were present in this region (Fig 6),

two with a smaller area that probably account for the same

methyl group that experienced oligosaccharide

heterogen-eity All signals in the region of 2.0 p.p.m showed

long-range correlations with a carbonyl signal at 174.6 p.p.m

which in turn correlated to protons at 3.67 p.p.m (H-2 W)

and 4.26 p.p.m (H-2 X) These correlations indicated the

presence of two acetamido groups at the C-2 of GlcN W and GalN X Thus, the two smaller methyl signals are both due to GalN X and are consequences of oligosaccharide heterogeneity, possibly due either to the adjacent heptose V bearing heterogeneous phosphate substitution (see below)

or to a reducing Kdo residue

In addition, all diagnostic interresidue NOE effects were found in the ROESY spectrum This confirmed the oligosaccharide sequence as determined in the previous paragraph

Other information on noncarbohydrate substituents (phosphate and carbamoyl groups) was gained by the observation of the downfield displaced heptose signals, namely H-2/C-2 and H-4/C-4 of heptose U and H-6/C-6 and H-7a,bof heptose V

The H-7a,bdownfield shift was clearly due to the presence

of a carbamoyl group that did not undergo hydrolysis in mild acid conditions, and that has already been located at position O-7 of the second heptose residue on the basis of methylation analysis In agreement with this assignment, a

Fig 5 Negative ion MALDI-TOF mass spectra of oligosaccharide 1 obtained in linear mode at normal (A) and higher laser intensity (B) Assignments

of main ion peaks are shown P, phosphate; Pyr, pyruvic acid.

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signal at 160.0 p.p.m in the HMBC spectrum correlated

with both protons H-7 of V

The degree of phosphorylation and localization of

phosphate substituents was established by 1D and 2D

31P-NMR spectroscopy (Fig 7, Table 2) Several signals

were found in the 31P-NMR spectrum, whose chemical

shift clearly indicated that they derived from phosphate

groups present in different magnetic/chemical

environ-ments In fact, in addition to a number of phosphate

monoester signals in the region of 1.4–3.2 p.p.m., two

peaks of lower intensity were present at )5.5 and

)9.7 p.p.m These last two signals derived from a

diphosphate monoester bond, i.e a pyrophosphate group

In particular, the signal at)5.5 p.p.m could be identified

as the distal phosphate group, while the phosphate at

)9.7 p.p.m was identified as the proximal phosphate

group The 1H,31P-HSQC spectrum showed correlation

between H-2 and H-4 of heptose U, with typical signals of

a phosphate monoester group The H-6 V resonance,

present as two different signals, showed two different

cross-peaks, one with a phosphate monoester group at

4.46/3.2 p.p.m and the other at 4.63/)9.7 p.p.m., with the

proximal phosphate of a diphosphate monoester residue

Thus, heptose U is substituted at O-2 and O-4 by a

phosphate group, whereas heptose V carries at O-6 a phosphate group or alternatively, a pyrophosphate group The MALDI-TOFmass spectrum (Fig 8) of oligosac-charide 2 confirmed all the assignments, as all ion peaks corresponding to the structures above were present In fact, ion peaks characteristic of an oligosaccharide were found, composed of two HexNAc, one Hex, two Hep, one Kdo, one carbamoyl group and two, three, four and five phosphate groups Moreover, additional peaks at Dm/z

146 accounted for the presence of a second core glycoform, which differs from the most abundant one by an additional rhamnose residue that must be linked at O-6 of glucose Ion peaks derived from the loss of water from molecular ions, probably Kdo lactone or anhydro-Kdo forms, were also present Furthermore, the MALDI-TOF mass spectrum also accounted for the presence of a very small amount of pentaphosphorylated species, which was not detected by NMR Because no different phosphate substitution was visible in 1D and 2D31P-NMR, we propose that the fifth phosphate group is present as pyrophosphate on heptose U

In conclusion, information derived from both acid and alkaline hydrolysis leads to the proposal of the following structure of the major oligosaccharide from the LOS of

P stutzeriOX1

Fig 6.1H-NMR spectrum of oligosaccharide 2 obtained by acetic acid hydrolysis The spectrum was recorded under the following conditions: 5 mg

of oligosaccharide 2 in 0.6 mL D 2 O, pD 7 Monosaccharides are as shown; rhamnose residue anomeric signal is not labeled as it belongs to the minor oligosaccharide Dotted bonds indicate a nonstoichiometric linkage Chemical shifts are shown in Table 2.

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Table 2. 1H,13C and31P NMR chemical shifts (p.p.m.) of the oligosaccharide product deriving from acetic acid treatment of the LOS from P stutzeri OX1 O-6 V resonances are given in parentheses when this position is monophosphorylated P/P refers to both resonances of pyrophosphate Because Kdo signals are spread due to its multiple forms, resonances are not given Resonances of the minor fragment Rha-C1fi6)-Glc are also shown at the bottom Chemical shifts are relative to acetone and external aq 85% (v/v) phosphoric acid (1H, 2.225 p.p.m.;13C, 31.45 p.p.m.;

31 P, 0.00 p.p.m at 30 C).

1

H/13C/31P

)9.7/)5.5 (3.2)

62.4

Fig 7 Section of the 1 H, 31 P-HSQC spectrum of oligosaccharide 2 The spectrum shows cross peaks relevant for the localization of the phosphate groups.

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