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Tiêu đề Enzymatic and electron paramagnetic resonance studies of anabolic pyruvate synthesis by pyruvate: ferredoxin oxidoreductase from Hydrogenobacter thermophilus doc
Tác giả Takeshi Ikeda, Masahiro Yamamoto, Hiroyuki Arai, Daijiro Ohmori, Masaharu Ishii, Yasuo Igarashi
Trường học The University of Tokyo
Chuyên ngành Biotechnology
Thể loại Journal article
Năm xuất bản 2009
Thành phố Tokyo
Định dạng
Số trang 10
Dung lượng 809,39 KB

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of anabolic pyruvate synthesis by pyruvate: ferredoxinoxidoreductase from Hydrogenobacter thermophilus Takeshi Ikeda1,*, Masahiro Yamamoto1,, Hiroyuki Arai1, Daijiro Ohmori2, Masaharu Is

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of anabolic pyruvate synthesis by pyruvate: ferredoxin

oxidoreductase from Hydrogenobacter thermophilus

Takeshi Ikeda1,*, Masahiro Yamamoto1,, Hiroyuki Arai1, Daijiro Ohmori2, Masaharu Ishii1and Yasuo Igarashi1

1 Department of Biotechnology, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Japan

2 Department of Chemistry, School of Medicine, Juntendo University, Chiba, Japan

Introduction

Pyruvate: ferredoxin oxidoreductase (POR; pyruvate

synthase, EC 1.2.7.1) catalyzes the thiamine

pyrophos-phate (TPP)-dependent oxidative decarboxylation of

pyruvate to form acetyl-CoA and CO2 POR contains

one or multiple iron-sulfur clusters in addition to TPP

[1]; the two electrons that arise during oxidation of pyruvate at the TPP site are sequentially transferred via the iron-sulfur cluster(s) to external electron accep-tors The physiological electron acceptor is a small iron-sulfur protein ferredoxin or FMN-containing

Keywords

Hydrogenobacter thermophilus; iron-sulfur

cluster; pyruvate: ferredoxin oxidoreductase;

reductive tricarboxylic acid cycle; thiamine

pyrophosphate

Correspondence

M Ishii, Department of Biotechnology,

Graduate School of Agricultural and Life

Sciences, The University of Tokyo, 1-1-1

Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan

Fax: +81 3 5841 5272

Tel: +81 3 5841 5143

E-mail: amishii@mail.ecc.u-tokyo.ac.jp

Present address

*Research Institute for Nanodevice and Bio

Systems, Hiroshima University, Japan

Institute of Biogeoscience, Japan Agency

for Marine-Earth Science and Technology

(JAMSTEC), Kanagawa, Japan

(Received 11 September 2009, revised 17

November 2009, accepted 19 November

2009)

doi:10.1111/j.1742-4658.2009.07506.x

Pyruvate: ferredoxin oxidoreductase (POR; EC 1.2.7.1) catalyzes the thia-mine pyrophosphate-dependent oxidative decarboxylation of pyruvate to form acetyl-CoA and CO2 The thermophilic, obligate chemolithoauto-trophic hydrogen-oxidizing bacterium, Hydrogenobacter thermophilus TK-6, assimilates CO2 via the reductive tricarboxylic acid cycle In this cycle, POR acts as pyruvate synthase catalyzing the reverse reaction (i.e reduc-tive carboxylation of acetyl-CoA) to form pyruvate The pyruvate synthesis reaction catalyzed by POR is an energetically unfavorable reaction and requires a strong reductant Moreover, the reducing equivalents must be supplied via its physiological electron mediator, a small iron-sulfur protein ferredoxin Therefore, the reaction is difficult to demonstrate in vitro and the reaction mechanism has been poorly understood In the present study,

we coupled the decarboxylation of 2-oxoglutarate catalyzed by 2-oxogluta-rate: ferredoxin oxidoreductase (EC 1.2.7.3), which generates sufficiently low-potential electrons to reduce ferredoxin, to drive the energy-demanding pyruvate synthesis by POR We demonstrate that H thermophilus POR catalyzes pyruvate synthesis from acetyl-CoA and CO2, confirming the operation of the reductive tricarboxylic acid cycle in this bacterium We also measured the electron paramagnetic resonance spectra of the POR intermediates in both the forward and reverse reactions, and demonstrate the intermediacy of a 2-(1-hydroxyethyl)- or 2-(1-hydroxyethylidene)-thia-mine pyrophosphate radical in both reactions The reaction mechanism of the reductive carboxylation of acetyl-CoA is also discussed

Abbreviations

DTNB, 5,5¢-dithiobis-(2-nitrobenzoic acid); EPR, electron paramagnetic resonance; HE-TPP, 2-(1-hydroxyethyl)- or 2-(1-hydroxyethylidene)-thiamine pyrophosphate; LDH, lactate dehydrogenase; OGOR, 2-oxoglutarate: ferredoxin oxidoreductase; OR, 2-oxoacid oxidoreductase; POR, pyruvate: ferredoxin oxidoreductase; TCA, tricarboxylic acid; TPP, thiamine pyrophosphate.

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flavodoxin By contrast to pyruvate dehydrogenase

multienzyme complex, which irreversibly catalyzes the

same reaction utilizing NAD+as an electron acceptor

in mitochondria and respiratory bacteria, POR can

also catalyze the reverse reaction (i.e the reductive

car-boxylation of acetyl-CoA) provided that a sufficiently

low-potential electron donor is available The reverse

reaction (pyruvate synthesis) is a central step for some

autotrophic bacteria because it serves to assimilate

CO2into cell carbon [1]

Hydrogenobacter thermophilus TK-6 is a

faculta-tive aerobic, thermophilic, obligate

chemolithoauto-trophic hydrogen-oxidizing bacterium [2] The optimum

growth temperature range for H thermophilus TK-6 is

70–75C Phylogenetic analyses of 16S ribosomal

RNA sequences have shown that the genus

Hydroge-nobacteris a member of the deepest branching order in

the domain Bacteria [3] H thermophilus assimilates

CO2 via the reductive tricarboxylic acid (TCA) cycle

[4], which is one of the microbial CO2 fixation

path-ways [5] The reductive TCA cycle is a reversal of the

oxidative TCA cycle, and is an endergonic anabolic

pathway that requires reducing equivalents to complete

the cycle [6,7] POR is one of the key enzymes of the

reductive TCA cycle, and catalyzes the anabolic

reduc-tive carboxylation of acetyl-CoA Two [4Fe-4S]

ferre-doxins, Fd1 and Fd2, from this bacterium are

considered to serve as low-potential electron donors

for this key reaction [8]

POR is distributed among archaea, bacteria and

anaerobic protozoa, and is a member of the 2-oxoacid

oxidoreductase (OR) family, which catalyzes the

oxida-tive decarboxylation of 2-oxoacids to their acyl- or

aryl-CoA derivatives [9] OR enzymes can be

homodi-meric [10,11], heterodihomodi-meric [12,13] or heterotetrahomodi-meric

[14], depending on the organism These three types of

OR are phylogenetically related and the

heterotetra-meric enzyme has been proposed to be the common

ancestor that underwent gene rearrangement and

fusion to generate homo- and heterodimeric ORs

[9,13,15] We recently found novel heteropentameric

ORs [POR and 2-oxoglutarate: ferredoxin

oxidoreduc-tase (OGOR; 2-oxoglutarate synthase, EC 1.2.7.3)] in

H thermophilus and its close relatives [16,17]; in these

organisms, the heteropentameric POR and OGOR

function as the key components of the reductive TCA

cycle and catalyze the anabolic reductive carboxylation

of acetyl-CoA and succinyl-CoA, respectively [17,18]

Four of the five subunits correspond to those of the

heterotetrameric ORs, suggesting that the

heteropenta-meric ORs might have evolved from an ancestral

het-erotetrameric enzyme by the acquisition of a unique

fifth polypeptide of unknown function Sequence

align-ments suggest that H thermophilus POR contains one TPP and three [4Fe-4S]2+⁄ 1+clusters per catalytic unit [17]; the enzyme contains all of the motifs required for cofactor binding that were identified in the crystal structure of the homodimeric Desulfovibrio africanus POR [19]

In most cases, the enzyme activity of POR is assayed

by monitoring the reduction of an artificial electron carrier, methyl viologen, during the oxidative decar-boxylation of pyruvate However, when the anabolic role of the novel heteropentameric POR in H thermo-philus is considered, the reverse reaction [i.e the reduc-tive carboxylation of acetyl-CoA (pyruvate synthesis)] needs to be assayed However, this reverse reaction has proven more difficult to study because a strong reduc-tant is required to drive the reaction Hence, the cata-lytic mechanism of the reductive carboxylation catalyzed by POR is poorly understood, whereas that

of the oxidative decarboxylation has been intensively investigated [20,21] In the present study, we developed

an assay system to demonstrate the reductive carboxyl-ation catalyzed by H thermophilus POR with reduced ferredoxin as an electron donor Specifically, we uti-lized another OR-family enzyme, OGOR from H ther-mophilus, to supply reduced ferredoxin for anabolic pyruvate synthesis mediated by POR OGOR also cat-alyzes the oxidative decarboxylation of 2-oxoglutarate using (oxidized) ferredoxin as an electron acceptor By coupling the OGOR decarboxylation, we demonstrate that H thermophilus POR catalyzes the anabolic reductive carboxylation of acetyl-CoA to form pyru-vate We also investigated the inter- and intramolecu-lar electron transfer during the reductive carboxylation

by electron paramagnetic resonance (EPR) spectros-copy to clarify its catalytic mechanism

Results

In vitro assay for pyruvate synthesis by POR: the coupled assay with OGOR and lactate

dehydrogenase (LDH; EC 1.1.1.27) Because the synthesis of pyruvate from acetyl-CoA and CO2 is an energetically unfavorable reaction with

a reduction potential of )540 mV [22], this reaction requires a strong reductant Pyruvate dehydrogenase multienzyme complex cannot catalyze the react-ion because the requisite electron donor, NADH (E0¢ =)320 mV), is much too weak an electron source to drive the transformation For the enzyme assay, the reducing power must be supplied in vitro by the physiological electron donor for POR, ferredoxin

A possible strategy is to couple the POR reaction to a

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ferredoxin-reducing enzyme For example, POR from

Moorella thermoacetica biosynthesizes pyruvate using

ferredoxin reduced by CO dehydrogenase [23];

Chloro-bium tepidum POR has been shown to catalyze

pyru-vate synthesis mediated by ferredoxin reduced by the

light-driven reactions of spinach chloroplasts or

Chloro-biumreaction centers [24,25] However, H thermophilus

does not possess these ferredoxin-reducing systems

In this bacterium, reducing equivalents are derived

from hydrogen oxidization catalyzed by multiple

hydrogenases [26], although the physiological electron

transfer pathway(s) from hydrogen to ferredoxin has

not yet been clarified Instead, we utilized OGOR from

this bacterium to reduce the low-potential ferredoxin

(Fig 1) The oxidative decarboxylation of

2-oxogluta-rate catalyzed by OGOR gene2-oxogluta-rates low-potential

electrons that reduce ferredoxins as follows:

2-oxoglut-arate + CoA fi succinyl-CoA + CO2+ H++ 2e),

E0¢ = )520 mV [27] The reactions catalyzed by POR

and OGOR were further coupled to the LDH reaction to

detect pyruvate formation spectrophotometrically

(Fig 1) Pyruvate generated by coupling the POR and

OGOR reactions was reductively converted to lactate

with NADH as an electron donor Thus, the rate of

pyru-vate formation was monitored as the decrease in A340as a

result of NADH oxidation The thermostable LDH from

a thermophilic bacterium Thermus caldophilus [28] was

used for the assay because the reaction was performed at

70C, which is the optimum temperature for H

thermo-philus Table 1 shows the overall reaction of this coupled

assay

Using the coupled assay with OGOR and LDH,

H thermophilusPOR was found to catalyze the

reduc-tive carboxylation of CoA Indeed,

acetyl-CoA-dependent NADH oxidation was observed with

either reduced Fd1 or Fd2 as an electron donor

(Fig 2) It was confirmed that pyruvate synthesis by

POR was rate-limiting in this coupled system A slight

decrease in A340 in the absence of acetyl-CoA was a

result of the spontaneous thermal degradation of

NADH [29] The reductive carboxylation depended on

the presence of POR, OGOR, LDH, ferredoxin,

2-oxo-glutarate and acetyl-CoA (data not shown), indicating that the coupled assay shown in Fig 1 proceeded as expected However, this reaction did not depend on the presence of NaHCO3 (CO2) and CoA (Fig 2B) Because CO2 was produced from 2-oxoglutarate by OGOR in this coupled assay, the addition of NaHCO3 was not necessarily required for the total reaction (Fig 1, dashed arrow) By contrast to CO2, CoA was

an essential substrate to initiate this coupled reaction; nevertheless, the reaction actually proceeded without the addition of CoA with a higher reaction rate than

Fig 1 Schematic representation of the coupled enzyme assay.

The reductive carboxylation catalyzed by POR was coupled with

the OGOR and LDH reactions Fdox, oxidized ferredoxin; Fdred,

reduced ferredoxin.

Table 1 Enzymatic reactions.

POR (reductive carboxylation)

Acetyl-CoA + CO2+ 2 · Fd red fi pyruvate + CoA + 2 · Fd ox

OGOR (oxidative decarboxylation)

2-Oxoglutarate + CoA + 2 · Fd ox

fi succinyl-CoA + CO 2 + 2 · Fd red

fi lactate + succinyl-CoA + NAD + a

Protons are omitted from the reactions for simplicity Fd ox , oxidized ferredoxin; Fdred, reduced ferredoxin.

A

B

Fig 2 Reductive carboxylation catalyzed by POR in the coupled enzyme assay The assay mixture contained 1 m M acetyl-CoA,

10 m M NaHCO3, 10 m M 2-oxoglutarate, 0.5 m M CoA, 0.2 m M NADH, 1 m M fructose 1,6-bisphosphate, 10 m M MgCl 2 , 1 m M di-thiothreitol, 0.5 m M TPP, 0.03 U of OGOR, 0.2 U of LDH and

10 l M Fd1 (A) or Fd2 (B) in 100 m M Hepes buffer (pH 8.0) Open circles, complete reaction; filled circles, acetyl-CoA omitted; open squares, NaHCO3omitted; filled squares, CoA omitted.

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that of the complete reaction (Fig 2B, filled square).

This was the result of a trace amount of CoA in the

assay mixture CoA quantification by the

5,5¢-dithiobis-(2-nitrobenzoic acid) (DTNB) assay showed

that 100 mm acetyl-CoA stock solution contained

2.4 mm CoA, corresponding to 24 lm CoA in the

stan-dard assay mixture (i.e without the addition of CoA

solution) The Km value for CoA of the OGOR

enzyme is reported to be 80 lm [30] Thus,

decarboxyl-ation of 2-oxoglutarate can proceed as a result of CoA

contamination of the acetyl-CoA solution When the

reaction commences, CoA is regenerated by the

reduc-tive carboxylation of acetyl-CoA (Fig 1, dashed

arrow) The reaction rate of this coupled assay was

significantly affected by the concentration of CoA

(Fig 2B) Although CoA was an essential substrate of

this assay, pyruvate synthesis by POR was inhibited in

the presence of excess CoA, which caused the reverse

reaction (oxidative decarboxylation of pyruvate) This

impasse prevented any further kinetic analysis of the

reaction

In this assay, the reductive carboxylation activity of

POR was determined to be 0.23 UÆmg)1 with 10 lm

Fd1, or 0.19 UÆmg)1 with 10 lm Fd2 These values

were comparable to those of the oxidative

decarboxyl-ation of pyruvate with Fd1 or Fd2 as an electron

acceptor (0.55 UÆmg)1 or 0.43 UÆmg)1, respectively;

data not shown), suggesting that H thermophilus POR

functions as an active pyruvate synthase

EPR measurements of POR during the oxidative

decarboxylation

The purified H thermophilus POR showed an EPR

sig-nal (g1,2,3= 1.973, 2.012 and 2.024) attributed to the

oxidized S = 1⁄ 2 [3Fe-4S]1+cluster [31] (Fig 3A) In

the dithionite-reduced state, the [3Fe-4S] signal

disap-peared and a new signal attributed to the reduced

S= 1⁄ 2 [4Fe-4S]1+ clusters was observed (Fig 3B)

This new signal is an overlap of a major signal with

g-values of 1.910, 1.922 and 2.040 and a minor signal

(approximately 4% of the major signal; determined by

spectral simulation) with g-values of 1.880, 2.003 and

2.020 (note that the minor feature around g = 2.00 in

Fig 3B was a result of this minor signal and not a

TPP radical intermediate described later) The relative

amount of the [3Fe-4S]1+ cluster in Fig 3A was

< 10% that of the [4Fe-4S]1+ clusters in Fig 3B

(determined by comparing the double integrals of the

EPR spectra), indicating that a substoichiometric

amount of the [3Fe-4S] cluster was derived from the

oxygen-sensitive [4Fe-4S] by partial oxidative damage,

as reported for other ORs [14,32–34] In the presence

of 20 mm pyruvate, POR showed a strong sharp signal centered at g = 2.0040 (Fig 3C), whereas 0.5 mm CoA did not affect the signal of POR (data not shown), indicating that the oxidative decarboxylation reaction begins with the binding of pyruvate, but not

A

B

C

D

E

F

Fig 3 EPR spectra of H thermophilus POR The purified POR was incubated with the components: (A) no substrate (as purified); (B) dithionite, (C) pyruvate; (D) pyruvate and CoA; (E) Fd1, OGOR, 2-oxoglutarate and CoA; (F) acetyl-CoA, Fd1, OGOR, 2-oxoglutarate and CoA Instrument settings were: temperature, 10 K; microwave power, 100 lW for (A), 250 lW for (B, D–F) or 1 lW for (C); micro-wave frequency, 9.024 GHz; modulation frequency, 100 kHz; mod-ulation amplitude, 0.2 mT The arrow indicates the signal of the TPP radical intermediate generated during the reductive carboxyla-tion of acetyl-CoA.

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CoA These results are consistent with a ping-pong

cat-alytic mechanism with pyruvate as the primary

sub-strate [35] (Note that the microwave power for

Fig 3C was 1 lW, 250-fold lower than that for the

others; the intensity of EPR signals is proportional to

the square root of the microwave power under

nonsat-urating conditions.) Although the [3Fe-4S]1+ signal in

Fig 3A disappeared at temperatures exceeding 30K,

the g = 2.0040 signal remained even at 70K (data

not shown), indicating that this signal was the result of

a TPP-radical intermediate Indeed, this radical is

pro-posed to be the common intermediate in pyruvate

decarboxylation catalyzed by all PORs [36], which is

generated by the binding of pyruvate to TPP and the

resultant decarboxylation Although the chemical

structure of this intermediate is still controversial [37–

39], it is often referred to as a 2-(1-hydroxyethyl)- or

2-(1-hydroxyethylidene)-TPP (HE-TPP) radical The

hyperfine structure of the radical was determined in

detail at 70K, at which the EPR signals of iron-sulfur

clusters are not detectable (Fig 4A) The hyperfine

splitting pattern is essentially the same as reported in

other studies [11,36–38,40,41] The HE-TPP radical is

generated by one-electron transfer; one of the two

elec-trons that are generated during decarboxylation of

pyruvate remains on the TPP intermediate, and the

other electron moves to the intramolecular iron-sulfur

cluster [42] Consistent with this mechanism, the

oxi-dized [3Fe-4S]1+ signal in Fig 3A disappeared in Fig 3C, indicating that the cluster was reduced by this electron However, no reduced [4Fe-4S] signal was detectable in Fig 3C This is probably because a reduced [4Fe-4S] cluster(s) can be reoxidized by a trace amount of oxygen [42] Because the redox potential

of [3Fe-4S] clusters is generally much higher than that of [4Fe-4S] clusters ()150  )100 mV versus )650  )250 mV) [43], the [3Fe-4S] cluster in the enzyme was not reoxidized Upon further addition of CoA, the signal of the HE-TPP radical markedly decreased, accompanied by concomitant formation of

a reduced [4Fe-4S] signal, which was similar to that of the dithionite-reduced POR (Fig 3D), indicating the second electron transfer from the radical to the [4Fe-4S] cluster(s) The presence of both pyruvate and CoA allows catalysis to proceed until all the oxygen is con-sumed [40], preventing reoxidation of the reduced [4Fe-4S] cluster(s) Because iron-sulfur clusters can receive only one electron at a time, multiple clusters should be reduced in this state These electrons are then readily released to external electron mediators Indeed, in the presence of Fd1, the rhombic

S= 1⁄ 2 [4Fe-4S]1+ signal of the reduced Fd1 [8] was clearly observed (data not shown)

EPR measurements of POR during the reductive carboxylation

Addition of 1 mm acetyl-CoA did not affect the EPR signal of POR (data not shown), indicating that elec-tron transfer from external elecelec-tron donors is a key step to initiate the carboxylation reaction To supply reducing equivalents to POR via ferredoxin, we utilized OGOR as described above In the presence of 2-oxoglutarate, CoA, OGOR and Fd1, the reduced [4Fe-4S] signal of POR was observed, overlapping with the rhombic [4Fe-4S]1+ signal of Fd1 (gz,y,x= 2.08, 1.94 and 1.92) [8] (Fig 3E) Upon further addition of acetyl-CoA, a signal with g = 2.0040 was observed (Fig 3F, arrow) (It was confirmed that this signal was not a result of the OGOR intermediate.) The hyperfine structure of this signal shows essentially the same hyperfine splitting pattern as that of the HE-TPP radi-cal intermediate observed during the decarboxylation

of pyruvate (Fig 4), indicating that the HE-TPP radi-cal was a common intermediate in both the oxidative and reductive reactions The HE-TPP radical was formed only after the reduction of the iron-sulfur clus-ters of the enzyme, suggesting that the electrons sup-plied via external ferredoxin molecules played an important role in forming the radical intermediate from TPP with bound acetyl-CoA

A

B

Fig 4 Hyperfine structures of the EPR signal of the TPP radical

intermediates (A) incubated with pyruvate and CoA (three scans);

(B) incubated with acetyl-CoA, Fd1, OGOR, 2-oxoglutarate and CoA

(five scans) Instrument settings were: temperature, 70 K;

micro-wave power, 1 lW for (A) or 100 lW for (B); modulation amplitude,

0.02 mT for (A) or 0.2 mT for (B); other settings were as described

in Fig 3 The higher power and wider modulation were used for (B)

to increase sensitivity because the amount of the radical

intermedi-ate was much less than for (A).

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In the present study, we demonstrate that H

thermo-philus POR catalyzes pyruvate synthesis from

acetyl-CoA and CO2, by the coupled assay with OGOR and

LDH (Fig 1) Although carboxylation activity is

gen-erally determined by monitoring the incorporation of

14CO2 to form [14C] pyruvate, OGOR catalyzes the

exchange reaction between CO2 and the carboxyl

group of 2-oxoglutarate [44], and therefore interferes

with the detection of [14C] pyruvate Instead, the rate

of pyruvate formation was determined by monitoring

the LDH-coupled oxidation of NADH to NAD+ The

coupled assay also demonstrated that Fd1 and Fd2

function as electron mediators for POR (and also for

OGOR) [45] in both the oxidative and reductive

reac-tions These results corroborate the operation of the

reductive TCA cycle in H thermophilus Specifically,

two irreversible reactions in the oxidative TCA cycle,

oxidative decarboxylation of pyruvate and

2-oxogluta-rate, are anabolically reversed by POR and OGOR,

respectively, as suggested by our early work [4], with

Fd1 and Fd2 acting as physiological electron donors

However, because this assay is a complex system

involving four proteins, kinetic analysis was not

possi-ble The substrates, CoA and CO2, were involved in

the two reactions catalyzed by POR and OGOR

(Fig 1, dashed arrows) In particular, CoA was a

sub-strate of OGOR as well as a product of POR, and

sig-nificantly affected the reaction rate of pyruvate

synthesis These problems were derived from the fact

that POR and OGOR are similar OR-family enzymes,

both reversibly catalyzing the CoA-dependent

oxidative decarboxylation of 2-oxoacids For further

analysis, an alternative enzyme that can generate

low-potential electrons to reduce ferredoxin is required

Thus far, two other enzymes that utilize ferredoxin as

an electron mediator have been purified from H

ther-mophilus: ferredoxin-NADP+ reductase (EC 1.18.1.2)

[46] and ferredoxin-dependent glutamate synthase

(EC 1.4.7.1) [47] However, the midpoint potentials of

the half reactions catalyzed by these enzymes are

higher than that mediated by OGOR, and are

there-fore unsuitable for the reduction of ferredoxin Thus,

the identification and characterization of enzymes that

transfer electrons to ferredoxins in vivo is of particular

importance for the improvement of this coupled assay

and also with respect to obtaining a deeper

under-standing of the metabolism of H thermophilus Indeed,

this would enable the kinetic analysis of the POR

reac-tions in both direcreac-tions In particular, the reaction rate

under physiological intracellular concentrations of

sub-strates needs to be determined to demonstrate that

H thermophilus POR functions toward pyruvate syn-thesis in vivo

To investigate the reaction mechanism of H thermo-philus POR, we measured the EPR spectra of the enzyme in the presence of various combinations of sub-strates Intra- and intermolecular electron transfer dur-ing the oxidative decarboxylation was essentially consistent with the catalytic cycle proposed by Menon and Ragsdale [36] We further measured the EPR spec-tra during the reductive carboxylation of acetyl-CoA, using OGOR to reduce ferredoxin as in the coupled assay In the presence of the reduced Fd1 and acetyl-CoA, the HE-TPP radical intermediate was formed (Figs 3F and 4B), indicating the intermediacy of the HE-TPP radical in both the oxidative and reductive reactions The results obtained also indicate that elec-tron transfer from external ferredoxin to the enzyme is

an indispensable step to form the radical in the reductive reaction From the data obtained in the present study, along with evidence available from the literature, we are able to propose the catalytic mechanism of the reductive carboxylation of acetyl-CoA (Fig 5) (1) The TPP carb-anion is generated by proton extraction from C2 carbon atom of the thiazolium ring by the tautomeric 4¢ imino group of the 4¢-aminopyrimidine ring [48], as is the case for all TPP-dependent enzymes; this process is also com-mon to the oxidative decarboxylation catalyzed by this enzyme (2) The nucleophilic TPP C2-carbanion attacks the carbonyl carbon of acetyl-CoA (as it attacks the car-bonyl carbon of pyruvate in the oxidative decarboxyl-ation) to form a transient tetrahedral intermediate (3) The tetrahedral intermediate undergoes CoA release and one-electron transfer to the adduct of TPP to form the HE-TPP radical intermediate It is not known whether CoA release and one-electron reduction occur

in a stepwise manner [possibly forming the acetyl-TPP

as an intermediate (3¢-a)] or simultaneously However,

we believe the latter process is more likely because dur-ing the oxidative decarboxylation the binddur-ing of CoA appears to be tightly coupled to electron transfer from the HE-TPP radical [49] (4) The generated HE-TPP radical is reduced to the HE-TPP C2a carbanion by a second electron transfer and then (5 and 6) the resultant carbanion attacks CO2, which might be tightly bound to the active site of the enzyme [37], to form pyruvate These latter steps (4, 5 and 6) correspond to the exchange reaction between CO2and the carboxyl group

of pyruvate catalyzed by this enzyme [50]

Further studies are being planed to confirm the above catalytic mechanism Moreover, the investigation

of the reductive reaction using the coupled system developed in this study is not only highly important itself, but also would provide further insights into the

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reverse, oxidative reaction and vice versa Thus, further

studies on the POR reactions in both directions would

lead to a deeper understanding of the overall reaction

mechanism of this enzyme

Materials and methods

Bacterial strains and growth conditions

Escherichia coli JM109 and BL21(DE3) were used as hosts

for derivatives of pUC19 and pET21c, respectively E coli

MV1184 was used as a host for the expression of T

caldo-philusLDH E coli strains were grown in tryptic soy broth

or LB medium at 37C When necessary, ampicillin

(100 lgÆmL)1) was added to the medium for plasmid

selection

Heterologous expression and purification of POR,

OGOR and ferredoxins

Because H thermophilus POR (UniProt accession numbers

Q9LBF7–Q9LBG1) is oxygen-sensitive, as is the case for

other ORs [51], the recombinant POR was expressed under

microaerobic conditions and purified under anaerobic

con-ditions as described previously [17] In preparation for EPR

spectroscopy, dithionite was removed from the purification buffers H thermophilus has two isozymes of OGOR, het-erodimeric Kor (UniProt accession numbers Q9AJL9 and Q9AJM0) and heteropentameric For (UniProt accession numbers Q93RA0–Q93RA4) [16,30] Because the former is much more active than the latter, we utilized the recombi-nant Kor in the present study Kor, Fd1 (UniProt accession number Q75VV9) and Fd2 (UniProt accession number Q4R2T6) were heterologously expressed and purified as described previously [8,52]

Heterologous expression and purification of LDH The plasmid, p8T4, carrying the gene encoding T caldophi-lus LDH (UniProt accession number P06150) [53] was a kind gift from Professor Hayao Taguchi (Tokyo University

of Science) LDH was heterologously expressed and purified

to apparent homogeneity (M Aoshima, A Nishiyama and

Y Igarashi, unpublished results) The enzyme activity of the recombinant LDH was assayed at 70C by monitoring the lactate-dependent NADH oxidation as the decrease in

A340 The standard assay mixture contained 1 mm lactate, 0.2 mm NADH and 1 mm fructose 1,6-bisphosphate (an allosteric effector of T caldophilus LDH) [28] in 100 mm Hepes buffer (pH 8.0 at 20C) The oxidation of NADH

N S H

H

N

H 3 C N

N

N S

H 3 C

O SCoA

TPP C2-carbanion

N S

OH

H3C

H3C

N S

HO SCoA

HE-TPP radical

e– CoASH

OH

H 3 C

N S

CO2

H 3 C

N S

HO COO–

H3C

O COO–

e–

HE-TPP C2 α-carbanion

4

5 6

1

N S

O

H 3 C

CoASH

3 ′-a 3 ′-b

e–

Fig 5 Proposed catalytic mechanism for the reductive carboxylation of acetyl-CoA catalyzed by POR The HE-TPP radical is illustrated on the basis of the model proposed by Barletta et al [57] with the unpaired electron on the C2a carbon, although its chemical structure is still controversial [37–39].

Trang 8

was calculated using an extinction coefficient of

6200 m)1Æcm)1 One unit of enzyme activity was defined as

the oxidation of 1 lmolÆmin)1of NADH

POR enzyme assays

The oxidative decarboxylation activity of POR was assayed

at 70C by monitoring the ferredoxin-mediated reduction

of metronidazole [54] The standard assay mixture

con-tained 20 mm pyruvate, 0.5 mm CoA, 10 lm ferredoxin,

0.1 mm metronidazole, 10 mm MgCl2, 1 mm dithiothreitol

and 0.5 mm TPP in 100 mm Hepes buffer (pH 8.0 at

20C) The decrease in A320was measured under an argon

atmosphere The reduction of metronidazole was calculated

using an extinction coefficient of 9300 m)1Æcm)1 One unit

of enzyme activity was defined as the reduction of 2

lmolÆ-min)1 of metronidazole (corresponding to the

decarboxyl-ation of 1 lmolÆmin)1 of pyruvate on the assumption that

the bleaching of the chromophore is a one-electron process)

[55] The reductive carboxylation activity of POR was

determined at 70C by the coupled assay with OGOR and

LDH (see Results) The standard assay mixture contained

1 mm acetyl-CoA, 10 mm NaHCO3, 10 mm 2-oxoglutarate,

0.5 mm CoA, 0.2 mm NADH, 1 mm fructose

1,6-bisphos-phate, 10 mm MgCl2, 1 mm dithiothreitol, 0.5 mm TPP,

0.03 U of OGOR, 0.2 U of LDH and 10 lm ferredoxin

(Fd1 or Fd2) in 100 mm Hepes buffer (pH 8.0) The assay

mixture without NADH and acetyl-CoA was incubated at

70C under an argon atmosphere The reaction was started

by adding the NADH, acetyl-CoA and enzyme solutions to

the mixture, and the decrease in A340as a result of NADH

oxidation was measured One unit of enzyme activity was

defined as the reduction of 1 lmolÆmin)1 of NADH

(corresponding to the carboxylation of 1 lmolÆmin)1 of

acetyl-CoA)

Quantification of CoA

The concentration of CoA was quantified using DTNB,

which reacts with free thiol groups (e.g CoA-SH) to

pro-duce 2-nitro-5-thiobenzoate with an extinction coefficient of

13 600 m)1Æcm)1 at 412 nm [56] The assay mixture

contained 0.1 mm DTNB in 100 mm Tris–HCl buffer (pH

8.0) Measurement of A412was performed after the addition

of the sample solution

EPR measurements

The enzyme solution was incubated with a substrate(s) in

an EPR sample tube at 70C for 5–10 min under a gentle

argon flow that had passed through a deoxidizing column

(Gasclean GC-RP; Nikka Seiko, Tokyo, Japan) The

reac-tion was stopped by immersion of the tube in liquid

nitro-gen EPR spectra were measured on a JES-FA300

spectrometer (JEOL, Tokyo, Japan) using a cylindrical

cavity (TE101 mode) The measurement temperature was controlled with a JEOL ES-CT470 cryostat system and

a digital temperature indicator⁄ controller model 9650 (Scientific Instruments, West Palm Beach, FL, USA) The magnetic field was calibrated with a JEOL NMR field meter ES-FC5 The g-values were determined by spectral simulation using JEOL anisimu⁄ fa software, version 2.0.0

Acknowledgements

The authors thank Professor Hayao Taguchi (Tokyo University of Science) for the gift of the plasmid carry-ing the LDH gene from T caldophilus; Dr Miho Aoshima and Ms Ayako Nishiyama for the preparation

of the recombinant LDH; and Dr Ki-Seok Yoon (Iba-raki University) for helpful discussions This research was supported in part by Grants-in-Aid for Scientific Research from the Japan Society for the Promotion of Science

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