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Brassica napus soluble epoxide hydrolase BNSEH1Cloning and characterization of the recombinant enzyme expressed in Pichia pastoris Stefan Bellevik1, Jiaming Zhang2and Johan Meijer1 1 Dep

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Brassica napus soluble epoxide hydrolase (BNSEH1)

Cloning and characterization of the recombinant enzyme expressed in

Pichia pastoris

Stefan Bellevik1, Jiaming Zhang2and Johan Meijer1

1 Department of Plant Biology, Genetics Center, Swedish University of Agricultural Sciences, Uppsala, Sweden; 2 National

Biotechnology Laboratory of Tropical Crops, Chinese, Academy of Tropical Agricultural Sciences, Chengxi, Haikou, China

Epoxide hydrolase (EC 3.3.2.3) in plants is involved in the

metabolism of epoxy fatty acids and in mediating defence

responses We report the cloning of a full-length epoxide

hydrolase cDNA (BNSEH1) from oilseed rape (Brassica

napus) obtained by screening of a cDNA library prepared

from methyl jasmonate induced leaf tissue, and the 5¢-RACE

technique The cDNA encodes a soluble protein containing

318 amino acid residues The identity on the protein level is

85% to an Arabidopsis soluble epoxide hydrolase (sEH) and

50–60% to sEHs cloned from other plants A 5· His tag

was added to the N-terminus of the BNSEH1 and the

con-struct was over-expressed in the yeast Pichia pastoris The

recombinant protein was recovered at high levels after

Ni-agarose chromatography of lysed cell extracts, had a

molecular mass of 37 kDa on SDS/PAGE and cross-reacted

on Western blots with antibodies raised to a sEH from Arabidopsis thaliana BNSEH1 was shown to be a monomer

by gel filtration analysis The activity was low towards cis-stilbene oxide but much higher using trans-cis-stilbene oxide as substrate with Vmaxof 0.47 lmolÆminÆmg)1, Kmof 11 lM

and kcat of 0.3 s)1 The optimum temperature of the recombinant enzyme was 55C and the optimum pH 6–7 for trans-stilbene oxide hydrolysis The isolation of BNSEH1 will facilitate metabolic engineering of epoxy fatty acid metabolism for functional studies of resistance and seed oil modification in this important oilcrop

Keywords: epoxide hydrolase, oilseed rape, yeast, recom-binant enzyme, stilbene oxide

Epoxide hydrolases [1] are hydrolytic enzymes that have

been found in mammals, plants, yeast, fungi, insects and

bacteria In mammals several forms exist with a

heteroge-neous tissue distribution of which microsomal and soluble

(sEH) epoxide hydrolases have been most extensively

studied These enzymes differ from each other in several

aspects such as substrate preference, turnover rate,

sensitiv-ity to inhibitors, pH optimum, etc [2] Several geometrically

different but related epoxides such as cis-stilbene oxide

(CSO) and trans-stilbene oxide (TSO) have been found to be

useful substrates in order to distinguish soluble from

membrane bound epoxide hydrolases [3,4] These substrate

pairs can be applied to crude extracts to assess the relative

contribution of membrane bound and soluble forms to the

total epoxide hydrolase activity in many species

Based on sequence homology analysis epoxide hydrolase

was classified as a member of a super family of hydrolytic

enzymes including esterases and lipases, united by an a/b

hydrolase fold and a similar catalytic triad motif [5] The

three-dimensional structure of epoxide hydrolase has been resolved for mouse [6], fungal [7] and bacterial enzymes [8] These studies have confirmed the predicted a/b fold struc-ture, provided a detailed picture of the active site and proposed a mechanism of the catalytic reaction supported by site-directed mutagenesis Epoxide hydrolases act through a two-step mechanism in which an acidic nucleophile attacks the epoxide ring, forming a covalent intermediate, which is then hydrolysed by a polarized water molecule [9]

Epoxide hydrolases in mammals are essential in the detoxification of epoxides that are toxic due to the electrophilic and unstable nature of the epoxide ring [2] The relevance of this enzyme for detoxification in plants is uncertain, however Certain plants store epoxy fatty acids in seeds, e.g Euphorbia lagascae contains up to 60% epoxy fatty acids in the seed oil [10] Epoxide hydrolase is probably needed for complete b-oxidation of epoxy fatty acids, e.g during germination when seed stores are broken down prior

to photosynthetic growth However, epoxide hydrolases are also present in plants low in epoxy fatty acids and have been cloned from several species such as potato [11], soybean [12,13], Arabidopsis [14] and Euphorbia [15] No microsomal epoxide hydrolase has been cloned from plants as yet, which indicates that this form is not necessary or that sEH may have a broader role in general

Engineering of epoxide hydrolase in a crop such as oilseed rape allows for agricultural and industrial applications Polymers of epoxy and hydroxy fatty acids are important constituents of the cutin layer and serve as a protective barrier against stress [16] Certain epoxy and hydroxy fatty acids have fungicidal activity in rice [17] and mediate defence responses in infected potato tubers [18] Modulation of

Correspondence to S Bellevik, Department of Plant Biology,

Genetics Center, Box 7080, Swedish University of Agricultural

ScI`ences, SE-750 07 Uppsala, Sweden.

Fax: + 46 18 673279, Tel.: + 46 18 673320,

E-mail: Stefan.Bellevik@vbiol.slu.se

Abbreviations: BNSEH1, soluble epoxide hydrolase 1 from Brassica

napus; CSO, cis-stilbene oxide; MeJa, methyl jasmonate; sEH, soluble

epoxide hydrolase; TSO, trans-stilbene oxide.

Enzymes: epoxide hydrolase (EC 3.3.2.3).

(Received 26 June 2002, revised 27 August 2002,

accepted 10 September 2002)

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epoxide hydrolase expression may thus be used to improve

crop protection Another possibility is the use of B napus as

a host to generate high amounts of epoxy or hydroxy fatty

acids in the seed for production of technical oils or plastics

[19] Successful engineering has already altered seed fatty acid

composition to create high laurate [20] and up-regulated

palmitate, stearate and c-linolenate (x-6) B napus lines [21]

Several genes encoding sEH exist in potato, soybean and

Arabidopsis[11,13,22] and apparently also in oilseed rape

(S Bellevik, J Lin & J Meier) Enzymatic characterization

is necessary to better understand the functional roles of the

isoforms and in this study we have used the yeast P pastoris

as host for over-expression of the first sEH cloned from

B napus(BNSEH1) We here present data concerning the

physico-chemical and biochemical properties of the

recom-binant enzyme

E X P E R I M E N T A L P R O C E D U R E S

Materials

Oligonucleotides were purchased from TAGC

(Copenha-gen, Denmark) All enzymes were purchased from MBI

Fermentas (Vilnius, Lithuania) unless stated otherwise

CSO and TSO (Aldrich Chemical Co., Milwaukee, WI,

USA); b-naphtoflavone, sodium-parahydroxymercuri

benzoate, quercitin (3,3¢,4¢,5,7-pentahydroxyflanone) (Sigma

Chemical Co., St Louis, MO); chalcone oxide (Lancaster

Synthesis, Morecambe, UK);

x-bromo-4-nitroacetophe-none (Fluka AG; Buchs, Switzerland);

1-ethyl-3-(3-dimethyl-aminopropyl) carbodiimide (Bio-Rad Laboratories, Hemel

Hempstead, UK); N,N¢-dicyclohexylcarbodiimide (kind gift

of A˚ke Engstro¨m, Uppsala University); dimethylsulfoxide

(Merck AG, Darmstadt, Germany); tetrahydrofurane

(Riedel-de-Ha¨en, Seelze, Germany) were purchased from

the sources indicated N,N¢-dicyclohexylcarbodiimide was

hydrolysed at 37C for 16 h to form the corresponding

urea (N,N¢-dicyclohexylurea) derivative [23]

Cloning ofB napus sEH

One partial B napus sEH cDNA clone (BNSEH1) was

isolated by hybridization screening of a reamplified

(oli-godT)-primed cDNA library prepared from rapeseed leaves

exposed to methyl jasmonate (MeJa) for 5 h (Clontech,

Palo Alto, CA, USA) using a heterologous EST clone

(#140O6t7, Arabidopsis Ohio Stock Center) as a probe This

EST corresponds to an earlier described Arabidopsis

epo-xide hydrolase cDNA (AtsEH1) [14] but also contains

intron sequences (S Bellevik & J Meier) BB4 was used as

bacterial host strain in the hybridization screening and

XL1-Blue for conversion to pXL1-Bluescript The probe was

random-primed using [32P]dCTP (Amersham International, Bucks,

England), purified by gel filtration and used at  106

c.p.m.ÆmL)1 Hybridization was performed at high

strin-gency conditions using Hybond N+nylon filters

(Amer-sham Biosciences, Uppsala, Sweden) according to the

manufacturer’s instructions Signals were detected after

36–56 h exposure on Biomax MS X-ray films (Amersham

Biosciences) One of the positive phage clones was excised

from Lambda Zap II using R408 helper phage coinfection

but was found to lack the initial bases of the 5¢-end

(including the initiating methionine codon)

5¢-Rapid amplification of cDNA ends (RACE)

A SMARTTMRACE cDNA Amplification kit (Clontech) was employed to amplify the missing 5¢-region of the cDNA Total RNA from young B napus cv Hanna seedlings were isolated after grinding in liquid nitrogen using phenol/chloroform extraction and precipitation with lithium chloride Several RACE PCR products correspond-ing to the cDNA clone were obtained uscorrespond-ing one nested primer pair after the first cDNA synthesis In the first strand synthesis Superscript IITMRnase H–Reverse Transcriptase (Life Technologies, Ta¨by, Sweden) was used with the RACE kit The first PCR was performed with the Advant-age 2 Polymerase Mix supplied using the Universal Primer Mix and a gene specific primer (5¢ AGG ACC GAA AGA GAA AGG AAC AGA 3¢) by cycling for 35 cycles at 94 C for 10 s, 65C for 20 s and 72 C for 1 min The first PCR reaction was diluted 50-fold and 5 lL used in the second PCR The primers used for the nested reaction used the nested universal primer and a second gene specific primer (5¢ TGC GAA AAG ACA AAG ATA CCA AGC G 3¢) with a thermo profile as in the first PCR but for 30 cycles

No product could be visualized in the first PCR but in the nested reaction a 400-bp band appeared on an ethidium bromide stained agarose gel The 5¢-RACE products were sequenced on an ABI PrismTM 377XL DNA sequencer based on a D YEnamicTMET kit (Amersham Biosciences) The cDNA sequence has been deposited in the EMBL database under the accession number AJ459780

Cloning of BNSEH1 into pPIC3.5K and expression

inP pastoris For over-expression we used the P pastoris expression system (Invitrogen, Groningen, the Netherlands) The complete BNSEH1 cDNA was generated with a forward primer (5¢ AGA ATG GGA TCC ACC ATG GAT CAC CAT CAC CAT CAC ATG GAG CAC CGA AAG TTA AGA GGT AAC GG 3¢) containing five His codons, a BamH1 site, a Kozak consensus sequence for a proper translation initiation in P pastoris and also the nine initial bases missing in the isolated cDNA clone The reverse primer (5¢ AAG GTA GGA ATT CCT AGA ATT TGG AGA TGA AGT C 3¢) contained an EcoR1 site after the stop codon The PCR product was amplified using Taq DNA polymerase (Stratagene, La Jolla, CA, USA) and blunt-end cloned into the pPCR-Script AMP SK(+) cloning vector After sequencing the chosen clone was digested with BamH1 and EcoR1, transformed into E coli

by electroporation and subcloned into the P pastoris expression vector pPIC3.5K (Invitrogen) JM106 electro-competent cells were transformed, the selected clone cultured and prepared by a Qiagen plasmid Midi kit, linearized with Stu1 and purified with a PCR purification kit (Qiagen, Hilden, Germany) Competent GS115 yeast cells were electroporated with 15 lg of linearized plasmid before plating onto selective media The resulting colonies were tested in liquid culture for epoxide hydrolase activity after

24 h of methanol induction (calculated as percentage substrate turnover/ODcell suspension) using the [3H]TSO assay [3] Selected clones were grown in 2-L Fernbach flasks under vigorous agitation to improve aeration and cells were harvested after 4 days of methanol induction, centrifuged at

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3000 g for 5 min and stored at)80 C if not processed at

once

Purification of recombinant BNSEH1

The frozen cell pellet was thawed and dissolved in start

buffer (20 mMTris/HCl, 40 mMimidazole, 500 mMNaCl,

1 mMbenzamidine, 1 mMphenylmethanesulfonyl fluoride,

20 mM2-mercaptoethanol, pH 7) and cells ruptured by at

least three passages through a 40K French pressure cell

press (SLM Aminco, Urbana, IL) prior to centrifugation

at 12 000 g for 10 min at 4C The supernatant was

sterile filtrated using 1.2 lm and 0.45 lm filters

HiTrapTM Chelating columns (Amersham Biosciences)

were loaded with 0.1M NiCl prior to addition of sample

The column was washed with start buffer and the enzyme

eluted with 150 mM imidazole The optimal imidazole

concentrations needed to remove contaminating proteins

in the washing step and to elute the recombinant enzyme

in the elution step were determined in preliminary

experiments Fractions were analysed for epoxide

hydro-lase activity and protein content based on the Peterson

procedure [24] using BSA as a standard, and also by SDS/

PAGE [25]

Western Blot analysis

Proteins were separated by SDS/PAGE, using 12.5%

polyacrylamide gels (Invitrogen) After completion of the

gel electrophoresis, separated proteins were detected by

Coomassie Brilliant Blue or by immunoblotting after wet

transfer to poly(vinylidene difluoride) filters (Schleicher &

Schull, Dassel, Germany) After blocking in milk/BSA,

filters were incubated with affinity purified rabbit polyclonal

anti-sEH Ig followed by HRP-conjugated swine anti-rabbit

Ig (Dako A/S, Glostrup, Denmark) and bands detected by

diaminobenzidine staining or ECL (Pierce, Rockford, IL,

USA) Antibodies were raised by immunization of rabbits

with recombinant sEH from A thaliana (AtsEH1) The

AtsEH1 corresponds to the EST clone used as probe for the

library screening (see above) Preimmune serum served as

the negative control The regional ethical committee

approved the animal experiments

Oligomerization analysis of BNSEH1 by gel filtration

A HiPrep 26/60 Sephacryl S-100 High Resolution column

(Amersham Biosciences) was chosen for native gel filtration

analysis of BNSEH1 dissolved in 0.1M potassium

phos-phate pH 7.2, 1 mM dithiothreitol The standard proteins

chymotrypsin A (horse heart, 1.8 mg), Cytochrome c

(1.8 mg), BSA (3.6 mg) and catalase (2.8 mg) (all from

Amersham Biosciences) were applied at a flow rate of

0.8 mLÆmin)1 The BNSEH1 (60 lg) was loaded at a total

volume of 500 lL, fractions collected and assayed for

enzyme activity and absorbance at 280 nm

Catalytic characterization of recombinant BNSEH1

Epoxide hydrolase activity was assayed based on conversion

of [3H]TSO or [3H]CSO synthesized as described [3] The

routine assays contained 100 lMfinal substrate

concentra-tion in 0.1 potassium phosphate, pH 7.0 and were run at

30C during a time period that assured significant activity within the linear range All measurements were performed

in at least duplicates and repeated twice or more The pH dependence of the enzyme for TSO hydrolysis was tested in potassium phosphate buffers (pH 4.5–7), Tris/HCl buffers (pH 7–9) and glycine/NaOH buffers (pH 9–11) pKavalues were obtained from intersections of asymptotes to the curve plot of log(kcat) vs pH Activation enthalpy was calculated from Arrhenius plots of ln(kcat) vs 1/T based on values up

to the denaturation point (55C) For the kinetic param-eters a range of approximately 10-fold higher and lower substrate concentrations of the predicted Kmwas tested and substrate conversions were kept below 5% to obtain accurate estimates of initial velocities The data were used

to draw a Lineweaver-Burk plot and the line equation was used to calculate Kmand Vmaxvalues When inhibitors were tested the inhibitor was preincubated with enzyme for 5 min

at 30C before the substrate was added The control reactions received solvent alone No effect of the solvents on epoxide or diol partitioning between the organic and aqueous phases was found

R E S U L T S

Cloning of BNSEH1

An epoxide hydrolase clone was isolated from a cDNA library constructed from B napus leaves treated for 5 h with MeJa The library average insert size was 1.3 kb and the isolated BNSEH1 clone contained 1273 base pairs The cDNA was sequenced in both directions and contained 230 base pairs of untranslated 3¢-sequence but was observed to lack the 5¢-end of the coding sequence A 5¢-RACE PCR on total RNA uncovered the initiator methionine codon and the few downstream residues missing, as well as 100 base pairs of the 5¢-upstream region including the transcription start site The products from the 5¢-RACE contained two ambiguities Five of the 18 clones sequenced differed from the cDNA by having a T instead of C at positions 145 and

249, respectively Neither of the two variants resulted in amino acid substitutions, however The predicted translated product of the cDNA contained 318 amino acids with the C-terminal tripeptide SKF, and lacked long hydrophobic regions (Fig 1)

Expression in yeast and purification of recombinant BNSEH1

The BNSEH1 was expressed intracellularly in yeast cells at high levels (£ 10% of the total protein and routinely

> 5 mgÆL)1) upon induction with methanol Several trans-formants were assayed in order to find highly expressed clones since multiple copies can be inserted in this system One highly expressed clone was found and used for all subsequent analysis The sEH activity in the cells increased rapidly after addition of methanol and cells were usually harvested after four days of culture After several passages

of the yeast cells through a French press the lysis efficiency reached 90–95% as determined by phase-contrast micro-scopy The crude extract was filtered, centrifuged and passed through a nickel resin with affinity for the histidine tag Fractions with more than 80% purity of BNSEH1 were used for the biochemical analysis

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Physico-chemical properties of recombinant BNSEH1

The mass of BNSEH1 was estimated as 37 kDa based on

SDS/PAGE with Coomassie staining (Fig 2A) The

theor-etical mass of BNSEH1 calculated from the predicted

amino acid sequence of the cDNA corresponds to

36 164 Da (37 096 Da with his-tag) assuming no

post-translational modifications The BNSEH1 over-expressed

enzyme cross-reacted with antibodies raised against AtsEH1

and the sizes of the sEHs were indistinguishable upon

Western blot analysis (Fig 2B) Twice the amount of

BNSEH1 protein relative to AtsEH1 was needed to reach

an equal signal intensity No reaction was observed when

samples were incubated with preimmune serum or when a

P pastorisextract without BNSEH1 was probed with the

specific antibodies

Gel filtration analysis of recombinant BNSEH1

The BNSEH1 was subjected to size exclusion

chromato-graphy to determine its oligomeric state BNSEH1 eluted as

a distinct single peak based on absorbance at 280 nm and

TSO activity (results not shown) The size of the native

BNSEH1 corresponded to 45 kDa

Biochemical characterization of recombinant BNSEH1 The recombinant enzyme had low activity towards CSO with values of 15 and 18 nmolÆmin)1Æmg protein)1for the two preparations tested TSO on the other hand served as a better substrate with at least twofold higher turnover Kinetic parameters were determined for the recombinant enzyme towards TSO at 30C Based on the Lineweaver-Burk rate equation, Vmax was determined to 0.46 and 0.48 lmolÆmin)1Æmg)1 in two experiments while the Km value was 11 lM in both cases (Fig 3) The kcat was calculated to 0.3 s)1 for TSO Substrate saturation was observed above 50 lMTSO The temperature optimum for the enzyme using TSO as substrate was found to be around

55C (Fig 4A) At this temperature a threefold higher activity was reached compared to standard conditions chosen at 30C The enzyme was almost completely inactivated at 64C and at higher temperatures The enthalpy of activation of the reaction was estimated from Arrhenius plots to  47 kJÆmol)1 The pH optimum for enzymatic TSO hydrolysis was found to be broad and around pH 6–7 (Fig 4B) At pH 4.5 almost 50% of maximum activity was obtained while activity dropped rapidly at higher alkaline pH The activity in potassium

Fig 1 Protein sequence alignment ( CLUSTALW 1.8) ofcloned plant epoxide hydrolases The terminal asterisks illustrate the suggested peroxisomal targeting signal The following sequences were retrieved for analysis from the GenBank database; B_napus (AJ459780), A_thaliana (D16628), G_max (CAA55294), S_tuberosum (U02497), E_lagascae 1 (AF482450), N_tabacum (AAB02006) The predicted catalytic residues are bolded and indicated

by * in the alignment Identical and similar residues are shown with black and grey backgrounds, respectively.

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phosphate buffer at pH 6–6.5 was similar to Tris/HCl

buffer at pH 7 It was noted also for the Arabidopsis

recombinant sEH that enzyme activity was higher in Tris

buffer compared to potassium phosphate at the same pH

[26] Apparent pKavalues for the active site were calculated

to 6.1 and 7.4, probably corresponding to the histidine and

tyrosine residues, respectively [6–8]

Effects of inhibitors on recombinant BNSEH1 enzyme activity

Several compounds were tested for potential inhibitory effects on the hydrolysis of TSO by the recombinant enzyme (Fig 5) N,N¢-dicyclohexylcarbodiimide was found to be a potent inhibitor and 10 lM of this compound abolished enzyme activity The corresponding N,N¢-dicyclohexylurea caused 30% inhibition at 10 lM and almost abolished activity at 1 mM The sulfhydryl reagent parahydroxy-mercuribenzoate and the histidine-reactive x-bromo-4-nitro-acetophenone gave intermediate inhibition (Fig 5A) The solvent tetrahydrofuran was found to cause a linear decrease in activity at increasing concentrations of the solvent (Fig 5B) Quercitin and chalcone oxide had weaker effects but caused 75% and 98% inhibition at 1 mM

concentration, respectively b-Naphtoflavone had no effect

up to 100 lMbut caused 50% inhibition at 1 mM 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide had no effect on the enzyme activity up to 1 mM b-naphtoflavone, quercitin and N,N¢-dicyclohexylcarbodiimide did not dissolve completely

at 1 mM final concentration so the free concentration is actually lower Addition of ethanol alone had only a minor effect on the enzyme activity while addition of dimethyl-sulfoxide caused almost 20% reduction in activity and the solvent control was set to 100%

Fig 3 Kinetic analysis ofrecombinant BNSEH1 Enzyme activity was

determined using TSO at different concentrations from 0.98 to

187.5 l M in 0.1 M potassium phosphate, pH 7, using 0.1 lg of

BNSEH1 enzyme A Lineweaver-Burk plot used to calculate the

kin-etic parameters is shown based on data from one out of two

repre-sentative experiments.

Fig 4 Effects oftemperature and pH on recombinant BNSEH1 enzyme activity (A) Enzyme activity was measured using 100 l M TSO in 0.1 M

potassium phosphate buffer (pH 7) at different temperatures during

11 min using 0.1 lg of BNSEH1 enzyme Results from two experi-ments (j and d symbols, respectively) are shown (B) Enzyme activity was measured using 100 l M TSO in 0.1 M potassium phosphate buffers (pH 4.5–7) (d,s), 0.1 M Tris/HCl buffers (pH 7–9) (j,h) or 0.1 M glycine buffers (pH 9–11) (m,n) using 0.1 lg of BNSEH1 enzyme Results from two experiments are shown.

Fig 2 Electrophoretic analysis ofrecombinant BNSEH1 (A) SDS/

PAGE was performed using 12.5% acrylamide gels The samples

analysed were molecular mass standard (lane 1), Pichia extract (lane 2)

and recombinant BNSEH1 enzyme purified on nickel-agarose resin

(1.5 lg protein) with sizes as indicated in kDa to the left (B) Western

blot analysis using antibodies raised to recombinant sEH1 from

A thaliana (AtsEH1) The samples analysed were purified

recombin-ant AtsEH1 enzyme (lane 1), purified recombinrecombin-ant BNSEH1 enzyme

(lane 2) and Pichia extract (lane 3) The molecular mass standard with

sizes indicated in kDa is to the left.

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D I S C U S S I O N

The BNSEH1 was cloned and found to encode a protein of

318 amino acid residues The recombinant enzyme was

functional and readily detected by assay of TSO hydrolysis

in yeast extracts upon over-expression in P pastoris using a

methanol inducible promoter [27] The his-tagged BNSEH1

was obtained at > 80% purity after one-step purification

on Ni-agarose and the subunit mass could be determined to

37 kDa No misfolding seemed to occur since all protein

fractions recovered from the affinity chromatography

displayed activity and a symmetrical active peak was

obtained upon gel filtration analysis of the native enzyme

Of the plant sEH sequences available in the database,

BNSEH1 is most closely related to the Arabidopsis AtsEH1

with 85% identity in the predicted amino acid sequence

Identity to the other plant sEHs was in the range 50 to 60%

with a higher similarity to soybean (Glycine max) and

potato than to tobacco and E lagascae sEH (Fig 1) The

five catalytic residues of sEH in plants and mammals [9] are

conserved also in BNSEH1 suggesting that the properties

are similar to the potato and Arabidopsis enzymes [4]

Gel filtration analysis showed that the recombinant

BNSEH1 is a monomer The apparent native mass of

45 kDa is slightly higher than expected for a monomeric

BNSEH1 but can be due to an altered diffusion in the gel matrix because of the histidine tag Potato and Arabidopsis AtsEH1 were also shown to be monomers [4] while a soybean sEH was reported to be a dimer [12] An obvious difference between the soybean and the other plant sEH is

an N-terminal extension of 25 amino acids (Fig 1) The function of these residues is not clear but it is tempting to assign to it a role for dimerization The mammalian sEHs have a N-terminal extension of 250 amino acids, which the plant enzymes lack It has been proposed that this extension, containing a proline-rich sequence of 30 amino acids, is capable of dimerization transition [6] These prolines are not present in the soybean N-terminal (Fig 1) In mammals, a conserved signal sequence of three amino acids in the C-terminus (PTS1) is necessary and sufficient to direct proteins to peroxisomes [28] Further work is necessary to determine if the C-terminus, SKF, as found in BNSEH1 and AtsEH1, is a true peroxisomal targeting signal (PTS1)

in these plants

The BNSEH1 is active towards TSO but much less active towards the CSO isomer This substrate pair thus seems to give similar results on oilseed rape sEH as earlier shown also for the Arabidopsis and potato enzymes [4] The efficiency is lower for the oilseed rape enzyme compared to the Arabi-dopsisenzyme, AtsEH1, expressed in P pastoris [26] The Arabidopsisenzyme had a Vmaxof 2 lmolÆminÆmg)1and Km

around 5 lMfor TSO Also the CSO rate was higher for the Arabidopsisenzyme Unfortunately kinetic analyses of these enzymes towards CSO are hampered of the low solubility of the substrate at higher concentrations Morisseau et al [23] reported that carboxylate modifying agents such as N,N¢-dicyclohexylcarbodiimide and its hydrolysis product, N,N¢-dicyclohexylurea, showed strong inhibition of mam-malian sEH using 4-nitrophenyl-trans-2,3-epoxy-3-phenyl-propyl carbonate or 1,3-diphenyl-trans-propene oxide as substrates Also the B napus sEH, using TSO as substrate, was inhibited by these carboxylate modifying compounds (Fig 5), most probably through interference with the activating tyrosine residues [29] Chalcone oxides that originally were reported as potent inhibitors for mammalian sEH [30] does not seem to be very efficient on plant sEHs including AtsEH1 [4] and BNSEH1 Recent experiments with the soybean sEH, using the substrate 9,10-epoxystearic acid, suggested that also the enantioselectivity differs between plant and mammalian sEHs [31]

The BNSEH1 clone was isolated from a cDNA library prepared from MeJa-treated leaves sEH has been described

to be up-regulated at the transcript level by MeJa in potato [11] but in Vicia sativa seedlings sEH activity remained unaffected by MeJa treatment [32] No MeJa induction of sEH transcripts was observed in B napus seedlings kept in hydroponic cultures (S Bellevik, F Sitbon & J Meier) suggesting that BNSEH1 probably has a constitutive expression The only plant hormone besides MeJa reported

to induce sEH is auxin, which increased transcript levels of a sEH in Arabidopsis within 1 h of treatment [14] Analysis of such experiments must keep in mind that sEHs recently have been identified in multiple copies in several plants Preliminary Southern blot data suggest that at least four epoxide hydrolase genes are present in B napus (S Bellevik,

J Lin & J Meier) In Arabidopsis, the known and putative epoxide hydrolase genes inferred by data mining of the genome sequence [22] are intrinsically divergent

Fig 5 Effects ofinhibitors on recombinant BNSEH1 enzyme activity.

Enzyme activity was determined using 100 l M TSO in the presence of

various inhibitors in 0.1 M potassium phosphate, pH 7, using 0.1 lg

BNSEH1 enzyme The inhibitors tested were (A)

sodium-parahyd-roxymercuribenzoate (s), x-bromo-4-nitroacetophenone (m),

N,N¢-dicyclohexylcarbodiimide (j), and N,N¢-dicyclohexylurea (d)

(B) tetrahydrofuran The solvent control was set to 100% activity.

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(S Summerer & J Meier) We have over-expressed cDNAs

and measured activity on three of the Arabidopsis genes so

far, proving that several predicted isoforms are functional

(S Summerer & J Meier) The BNSEH1 sequence is highly

similar to AtsEH1 with an even distribution of mismatches

throughout the alignment (Fig 1) The homology is also

reflected in the cross-reaction of BNSEH1 with antibodies

specific to the AtsEH1 (Fig 2) Arabidopsis and oilseed rape

belong to the same family, Brassicaceae, and extensive

synteny and multiplicated genome segments seem to be

common [33] B napus is amphidiploid and the number of

sEH genes can be expected to be higher than for

Arabid-opsis When the B napus and Arabidopsis sEH gene families

are further characterized it will become possible to

deter-mine a more specific gene relationship between these species

Oilseed rape is the third largest oil crop in the world and

there are potential industrial applications for transgenic

plants modified for enzymes such as epoxide hydrolases

For example, overproducing oxylipins in the vegetative

tissues resulting in a better endogenous biotic stress

protection would be useful for the agriculture and

environ-ment in terms of reduced pesticide spraying and increased

crop yields A modified lipid composition in the seeds of

B napus is also interesting as a renewable source for

technical oils [19] Knowledge of the function and regulation

of epoxide hydrolase isoforms in plants open up possibilities

for future engineering to redirect fatty acid metabolism into

the desired products

A C K N O W L E D G E M E N T S

This work was supported by grants from the Foundation for Strategic

Research We are grateful to Mikael Widersten, Uppsala University,

for discussions on enzyme kinetics.

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