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Abbreviations FDH, flavodehydrogenase domain of flavocytochrome b 2 ; FMN•, anionic FMN semiquinone; FMNH, fully reduced FMN anion; FMNH•, neutral FMN semiquinone; LCHAO, recombinant lon

Trang 1

L-a-hydroxyacid-oxidizing flavoenzymes – a study

using nanosecond laser flash photolysis

Lars Lindqvist1, Simona Apostol1,*, Chaibia El Hanine-Lmoumene1and Florence Lederer2

1 Laboratoire de Photophysique Mole´culaire du Centre National de la Recherche Scientifique, Universite´ Paris-Sud, 91405 Orsay, France

2 Laboratoire de Chimie Physique, Centre National de la Recherche Scientifique UMR 8000, Universite´ Paris-Sud, 91405 Orsay, France

Introduction

Proton transfer is involved in most if not all biological

processes, as well as in formation of the structures

of biological macromolecules In soluble enzymes,

acid–base catalysis is of fundamental importance In

biomembranes, electron and proton transfers are often

coupled Determining the kinetics of proton transfers

in an individual system is of prime importance in understanding the fine details of the processes involved

at the functional and structural levels However, the dynamics of proton movements are not always easy to analyze for biological phenomena, either because of the lack of a directly observable signal, or because

Keywords

flavin semiquinone; flavocytochrome b2;

long-chain hydroxy acid oxidase;

nanosecond laser photolysis; proton transfer

kinetics

Correspondence

L Lindqvist, Laboratoire de Photophysique

Mole´culaire du CNRS, Universite´ Paris-Sud,

91405 Orsay Cedex, France

Fax: +33 1 69156777

Tel: +33 1 69157909

E-mail: lwlindqvist@gmail.com

*Present address

Physics Department, Faculty of Sciences

and Arts, Targoviste, Romania

(Received 10 October 2009, revised 2

December 2009, accepted 7 December

2009)

doi:10.1111/j.1742-4658.2009.07539.x

The reactions of the flavin semiquinone generated by laser-induced stepwise two-photon excitation of reduced flavin have been studied previously (El Hanine-Lmoumene C & Lindqvist L (1997) Photochem Photobiol 66, 591–595) using time-resolved spectroscopy In the present work, we have used the same experimental procedure to study the flavin semiquinone in rat kidney long-chain hydroxy acid oxidase and in the flavodehydrogenase domain of flavocytochrome b2 FDH, two homologous flavoproteins belonging to the family of FMN-dependent L-2-hydroxy acid-oxidizing enzymes For both proteins, pulsed laser irradiation at 355 nm of the reduced enzyme generated initially the neutral semiquinone, which has rarely been observed previously for these enzymes, and hydrated electron The radical evolved with time to the anionic semiquinone that is known to

be stabilized by these enzymes at physiological pH The deprotonation kinetics were biphasic, with durations of 1–5 ls and tens of microseconds, respectively The fast phase rate increased with pH and Tris buffer concen-tration However, this increase was about 10-fold less pronounced than that reported for the neutral semiquinone free in aqueous solution pKa values close to that of the free flavin semiquinone were obtained from the transient protolytic equilibrium at the end of the fast phase The second slow deprotonation phase may reflect a conformational relaxation in the flavoprotein, from the fully reduced to the semiquinone state The anionic semiquinone is known to be an intermediate in the flavocytochrome b2 catalytic cycle In light of published kinetic studies, our results indicate that deprotonation of the flavin radical is not rate-limiting for the intramolecu-lar electron transfer processes in this protein

Abbreviations

FDH, flavodehydrogenase domain of flavocytochrome b 2 ; FMN•), anionic FMN semiquinone; FMNH), fully reduced FMN anion; FMNH•, neutral FMN semiquinone; LCHAO, recombinant long-chain hydroxy acid oxidase from rat.

Trang 2

another process is rate-limiting The most successful

method for studies in biological systems has been

laser-induced pH jump [1], where a transient pH

change is obtained by proton ejection from a

photodis-sociable dye Time-resolved studies of proton transfer

for a number of proteins using this method have been

reviewed by Gutman and Nachliel [2] and A¨delroth

and Brzezinski [3] However, the method is limited to

a narrow time window because of rapid pH relaxation

to the initial state after the pH jump

We have instead made use of the transformation of

a photoreactive species into a stable product – in this

case the FMN semiquinone, obtained from the fully

reduced FMN anion (FMNH)) – thus allowing a

time-resolved study of protolytic reactions involving

the flavin radical without limitation of the observation

time The photochemical reaction was achieved by

two-photon excitation of the reduced flavin Indeed,

our previous studies [4,5] of FMNH)in aqueous

solu-tion showed that pulsed laser excitasolu-tion of the reduced

flavin at 355 nm gives rise to one-electron ionization at

high laser intensities by stepwise two-photon

absorp-tion, with formation of the hydrated electron (eaq))

and the neutral FMN semiquinone (FMNH•):

FMNHþ 2hv ! FMNHþ eaq ð1Þ

In those experiments, the flavin radical appeared

initially as the neutral (blue) species (FMNH•) at pH

7-10; however, acid–base equilibrium of the radical was

attained within a few microseconds by deprotonation

of a proportion of the neutral radical to the anionic

(red) form (FMN•)) This laser-induced reaction

pro-vides an exclusive means of studying protolysis

dynam-ics in flavoenzymes In this paper, we report results

obtained for two members of a flavoenzyme family that

oxidizes l-2-hydroxy acids: rat long-chain hydroxy acid

oxidase (LCHAO, EC 1.1.3.15, isozyme B) and the

flavodehydrogenase domain (FDH) of flavocytochrome

b2, a lactate dehydrogenase from yeast (EC 1.1.2.3)

These proteins have been well characterized at the

func-tional and structural level [6,7] Their crystal structures

show a high degree of similarity, both in the b8a8 fold

and around the flavin [8–10] Family members stabilize

the anionic semiquinone at physiological pH [11–15]

This has been demonstrated to be the case for

flavo-cytochrome b2and its FDH domain [11,12] and should

be the case for LCHAO, which is an isozyme of

spin-ach glycolate oxidase [6,16] The semiquinone pKa has

been determined only for lactate oxidase from

Aerococcus viridans, and was found to be 6.0 [14] Part

of the present results have been presented previously in

preliminary form [17]

Results Photoionization reaction The flavoprotein solutions in the relevant buffer (see Fig 1 for details) flushed with argon were exposed to laser pulses of varying fluence The appearance of eaq ) was measured at the 715 nm absorption peak of this species [18] at the end of the laser pulse, and the eaq ) concentration was calculated using the extinction coef-ficient 1.85· 104m)1Æcm)1 [18] The results (Fig 1) revealed that eaq)is formed for both proteins, confirm-ing the occurrence of photoionization (Eqn 1) The

eaq) then disappeared within about one microsecond

A previous study of the FDH domain by transient absorption spectroscopy at sub-picosecond time resolu-tion [19] showed that the excited singlet state of the fully reduced flavin has a lifetime long enough in this protein (approximately 1.5 ns) to be populated to a large extent by the laser pulse and to absorb a second photon at the fluence rates used here

As photoionization is a two-photon process, one would expect the eaq ) yield to increase quadratically with the laser fluence However, a previous study of free FMNH) in aqueous solution [5] showed that the formation of eaq) was proportional to the square of the laser fluence only at the lowest fluences, and then increased quasi-linearly with the fluence The deviation from a quadratic response was ascribed to depletion of ground-state flavin during the laser pulse, concurrent with screening effects caused by absorption of the laser light by transient species The present results show the same behaviour: formation of eaq)was noticeable only above a certain fluence threshold and then increased almost linearly with the fluence

5 10

15

LCHAO

0 0.02 0.04 0.06 0

0 0.02 0.04 0

2 4 6

FDH

FMNH·

Fig 1 Yields of eaq)and FMNH • obtained upon laser excitation at the end of the laser pulse for the FDH domain (70 l M in 25 m M

Tris ⁄ H 2 SO4, pH 7.8) and LCHAO (150 l M in 10 m M Tris ⁄ HCl,

pH 7.5).

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The formation of FMNH• at the end of the laser

pulse was measured at 570 nm in N2O-saturated

solutions to scavenge eaq) FMNH• concentrations

were obtained using the extinction coefficient

5· 103 m)1Æcm)1 reported for FMNH• obtained from

free flavin and several flavoproteins at the absorption

maximum in the visible spectrum [20,21] Figure 1

shows that the formation of FMNH•, as found for

eaq), increases almost linearly with the laser fluence;

however, the FMNH•concentration is higher than that

of eaq), in contrast to the stoichiometric formation

expected from Eqn (1) The reasons for this

discrep-ancy were investigated by comparing these results with

those obtained in parallel with free FMNH)under the

same conditions These experiments showed that

FMNH• is formed in equal amounts (within ±10%)

in both cases, assuming that the extinction coefficients

of the flavin radical have the same values in free and

protein-bound conditions This finding strongly

sug-gests that the photoionization efficiency is the same for

the FDH domain and for free FMNH) However,

comparison of the eaq) yields gave a considerably

lower value, approximately 60%, for the protein

com-pared to that for free FMNH) The deficit in eaq)yield

for the two proteins may be explained by assuming

that part of the eaq) just released by laser excitation

reacts in sub-nanosecond time with amino acid

resi-dues in the protein during its diffusion from the flavin

towards the surrounding aqueous solution, and thus

escapes observation It is interesting to note that a

pre-vious study of Desulfovibrio vulgaris flavodoxin [22]

showed that eaq) and the flavin radical are formed in

stoichiometric ratio, as expected from Eqn (1) The

fla-vin environment in flavodoxin is very different from

that of the two l-2-hydroxy acid dehydrogenases In

flavodoxin, a tyrosine residue protects part of the

fla-vin si face from the solvent, but the benzenoid ring

methyl groups are exposed [23] In the two

homolo-gous enzymes studied here, N5 is practically the only

FMN atom accessible to the solvent, in a shallow

active site, which may be occluded some of the time by

a mobile loop that is partly invisible in the crystal

structures of the two enzymes [8–10] How these

struc-tural differences compared with flavodoxin affect the

fate of eaq)is unclear

Flavin semiquinone spectra

The absorption spectra of the half-reduced flavin

formed upon laser excitation of the FDH domain and

of LCHAO, in 50 mm Tris buffer, pH 7.5-7.8, were

determined by measuring the transient absorbance

changes between 320 and 670 nm at the end of the

laser pulse in N2O-saturated solutions The difference spectra thus obtained were extrapolated to 100% con-version of the flavin to FMNH• (the laser pulse achieved up to 10% conversion) using the extinction coefficient 5· 103m)1Æcm)1 at 570 nm Addition of these difference spectra to the absorption spectra of the reduced flavoproteins gave the spectra shown in Fig 2, which are characteristic of neutral flavin radi-cals and compare well with spectra reported by others [20,21,24]

The ‘end-of-pulse’ spectra evolved within about 0.1 ms into spectra characteristic of the flavin anion radical as shown in Fig 2 It is known that the semi-quinone is anionic in the neutral pH range in the pres-ent flavoproteins [11,12,15]; therefore, the initially generated neutral radicals are expected to undergo deprotonation to yield the anionic radical in the pH range studied (7.5–9.7)

FMNH•deprotonation kinetics The deprotonation of FMNH•after the end of the laser pulse was studied in the wavelength range 360-600 nm

at various pH values Figure 3 shows individual curves illustrating the kinetics at 570 nm, where FMNH•is the only species absorbing significantly It can be seen that

LCHAO

300 400 500 600 700

300 400 500 600 0

4000 8000 12000 16000

Wavelength (nm)

FDH

Fig 2 Absorption spectra of the species formed upon laser excita-tion of the FDH domain and of LCHAO at pH 7.5–7.8 (50 m M Tris buffer) in N2O-saturated solutions The transient absorbance changes obtained on laser excitation were extrapolated to 100% conversion of the flavin to FMNH • (the laser pulse achieved up to 10% conversion) and added to the absorption spectra of the respective reduced flavoproteins Open triangles, FMNH•obtained

at the end of the laser pulse; closed circles, FMN•)obtained at the end of the ‘slow’ phase; full line, absorption spectra of the fully reduced proteins.

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evolution of the transient absorbance is complex,

comprising a ‘fast’ phase lasting 1–5 ls and a ‘slow’

phase lasting up to tens of microseconds The kinetics

could be expressed satisfactorily by bi-exponentials with

rate parameters independent of wavelength At the

end of the ‘slow’ phase, the absorbance was found to

correspond mainly to that of FMN•)(Fig 2) in the pH

range studied The amplitude of the ‘fast’ phase,

deter-mined by the disappearance of FMNH•, was found to

increase with pH at the expense of that of the ‘slow’

phase, as seen in Fig 3

The findings are illustrated in Fig 4, in which the

absorbance remaining at 570 nm at the end of the

‘fast’ phase (DAend, after 1–5 ls), normalized with

respect to the absorbance variation at the end of the

laser pulse (DA0), is plotted against pH If one assumes

that the ‘fast’ phase leads to a ‘temporary’ protolytic

equilibrium of the newly generated neutral radical with

the external solution, one can derive the pKa of the

radical at this stage The smooth curves in the figure

represent the calculated fractional absorbance of the

neutral flavin radical, fitted to the experimental values

by setting pKa= 8.1 for the FDH domain and 8.7 for

LCHAO It is striking that these values are close to

those (8.3–8.7) determined by diverse methods for the

neutral flavin radical free in aqueous solution [4,20,25–

28] Indeed, one would instead expect a semiquinone

pKa value below 7 for these proteins, as mentioned

above [12,14,16], and therefore complete

deprotona-tion However, the neutral radical still present at the

‘temporary’ equilibrium undergoes close to complete

deprotonation at the rate of the ‘slow’ phase, in

agree-ment with the result expected from the literature

The rate constants of the ‘fast’ and ‘slow’ phases (k1

and k2, respectively) reveal trends in the pH

depen-dence of the deprotonation rates (Table 1) For the FDH domain, k1 increases from pH 7.7 to 8.5 For LCHAO, the ‘fast’ phase is absent at pH 7.5, reflecting the higher pKa value of the flavin radical in this pro-tein at its ‘temporary’ protolytic equilibrium compared

to that in the FDH domain (Fig 4) However, the

‘fast’ phase appears at higher pH and its rate increases with pH, as for the FDH domain

0.0 0.2 0.4 0.6 0.8

1.0

LCHAO

pKa = 8.7

FDH

pKa = 8.1

Aend

A0

pH

Fig 4 Titration curves for the equilibrium FMNH • ⁄ FMN•) in the FDH domain (+) and for LCHAO (open circles) in 50 m M Tris buffer, obtained at the end of the ‘fast’ deprotonation phase of FMNH• The ratio of the absorbance variation at 570 nm at the end of this phase (DAend) to that at the moment of the laser pulse (DA0) is plotted against pH The smooth curves were obtained from the expression for DA end ⁄ DA 0 expected at protolytic equilibrium:

DAend⁄ DA 0 = 1 ) (1 ) r) ⁄ (10 (pK ) pH)+ 1), where r is the residual

absorbance due to the ‘slow’ phase The calculated curves were fitted to the experimental values by setting pK a to 8.1 (r = 0.03) for the FDH domain and to 8.7 (r = 0.2) for LCHAO.

0.00 0.02 0.04

pH 9.6

pH 8.45

LCHAO

pH 7.5

Time (µs)

0.00

0.01

0.02

0.03

FDH

pH 8.3

pH 7.7

Time (µs)

Fig 3 Time evolution of the flavin radical in the FDH domain and

in LCHAO, measured after the end of the laser pulse at various pH

values, in 50 m M Tris buffer, measured at 570 nm The smooth

lines are bi-exponential fits to the curves, using a computer

pro-gram based on the Levenberg–Marquardt non-linear least-squares

fit algorithm The curves show individual measurements but are

representative of a number of experiments.

Table 1 Rate parameters of FMNH•deprotonation Rate constants

of FMNH • deprotonation in the FDH domain and in LCHAO in

50 m M Tris buffer at various pH values, obtained from measure-ments of transient absorption decays at 570 nm The smooth lines are bi-exponential fits to the curves (see Fig 3) The parameters are mean values obtained from several independent experiments.

pH k1(· 10 6 s)1) k2(· 10 4 s)1) FDH 7.7 0.23 ± 0.05 3 ± 1

8.0 0.43 ± 0.06 3 ± 1 8.3 0.53 ± 0.06 3 ± 1 8.5 0.60 ± 0.06 3 ± 1 LCHAO 7.5 0 2 ± 1

8.25 0.15 ± 0.05 2 ± 1 8.7 0.4 ± 0.1 7 ± 2 9.6 1.2 ± 0.3 16 ± 4

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As mentioned above, the neutral radical still present

at the end of the ‘fast’ phase undergoes deprotonation

at a slower rate to yield the protolytically stable

radi-cal in these proteins It can be seen from Table 1 that

the rate constant (k2) of the ‘slow’ phase is

approxi-mately the same for the two proteins (2–3· 104s)1) at

the lowest pH (pH 7.5-7.7), even when the ‘fast’ phase

is absent At higher pH, the k2 value appears to

increase with pH for LCHAO

The deprotonation may occur by transfer from the

radical to the various proton acceptors present in the

solutions (Tris, EDTA, H2O and OH)) and⁄ or to

pro-tein side chains Control runs at 2 and 5 mm EDTA

gave the same deprotonation rates Thus, a reaction

with EDTA can be neglected, and so can a reaction

with OH) at the pH values used here This leaves Tris

and H2O as possible proton acceptors:

FMNHþ Tris ! FMNþ TrisHþ ð2Þ

FMNHþ H2O! FMNþ H3Oþ ð3Þ

The contribution of Tris buffer to the deprotonation

was determined by studying the effect of its

concentra-tion on the ‘fast’ deprotonaconcentra-tion rates for the FDH

domain Figure 5A shows examples of transient

absor-bance curves obtained at 570 nm in 10 and 100 mm

Tris buffer (pH 7.7) It can be seen that the

deprotona-tion rate increases with increase in buffer

concentra-tion The rate constant of the ‘fast’ deprotonation

process, obtained from the transient absorbance at

570 nm, is shown in Fig 5B as a function of the Tris

concentration The rate constant increases linearly with

the buffer concentration, and can be expressed as k1=

k0+ kTris· [Tris], where kTris is approximately 1.4· 106m)1Æs)1 This value may be confronted with results obtained previously for free FMNH• in aque-ous solution [22] The deprotonation rate constant of the neutral flavin radical by Tris at pH 8.7 was deter-mined to be 2.2· 107m)1Æs)1, i.e one order of magni-tude faster in aqueous solution than in the protein environment This finding is in line with the idea that when partially embedded in the protein, the flavin is less accessible to the buffer than when it is fully exposed to the aqueous solution Figure 5B shows that the deprotonation is fast even in the absence of buffer, with a rate constant k0of 1.4· 105s)1

Discussion The two homologous enzymes analyzed in this study exhibit essentially the same behavior on exposure to laser flash excitation at 355 nm: at the end of the laser pulse, one electron has been ejected from the flavin, which is then in the neutral semiquinone state The

pKa of this species was found to be close to that of free flavin (Fig 4) This neutral radical then undergoes deprotonation to yield the stable anionic semiquinone, previously characterized by spectrophotometry [12] and EPR [11] Hazzard et al [29] proposed that a neu-tral semiquinone is formed in flavocytochrome b2 by electron transfer from FMNH) to heme b2 upon back reduction of the heme after partial enzyme oxidation

by the laser-generated triplet state of 5-deazariboflavin However, these authors did not study the fate over time of this neutral semiquinone

In the present study, the FMNH• deprotonation appears to be biphasic for both proteins In a first rapid phase, the radical protonation state adjusts to the buffer pH as if the semiquinone were free in solu-tion For the fast deprotonation phase of the FDH domain at pH 7.7, the Tris-dependent and Tris-inde-pendent rate constants were approximately 1.4· 106

m)1Æs)1and 1.4· 105s)1, respectively (Fig 5)

The conclusion must then be that it is water itself that is responsible for the Tris-independent deprotona-tion of the neutral semiquinone, according to Eqn (3) However, this idea raises a problem With H2O as the proton acceptor and a pKaof)1.74 for the hydronium ion, one would expect the Tris-independent rate to be

at least two orders of magnitude lower Furthermore, the value of the Tris-dependent rate constant is insuffi-cient to explain the variation of the fast phase rate with pH if the Tris-independent rate is constant, as expected for an exchange with water in the explored

pH range A tentative answer to the problem may be

0

0.01

0.02

0.03

0.04

0.05

10 m M Tris

100 m M Tris

Time (µs)

0.1 0.2 0.3

k1

[Tris] ( M )

Fig 5 Influence of buffer concentration on the kinetics of the

fla-vin radical evolution (A) Absorbance variation at 570 nm obtained

upon laser excitation of 70 l M FDH domain solutions (saturated

with N2O) buffered at pH 7.7 with 10 or 100 m M Tris Smooth

curves are bi-exponential fits to the experimental curves (B) Rate

constant (k 1 ) of the ‘fast’ phase describing deprotonation of the

neutral flavin radical measured at 570 nm, plotted against Tris

con-centration The linear fit gives k1= (1.4 · 10 5 + 1.4 · 10 6 · [Tris])

s)1.

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obtained by considering that the reaction between

FMNH• and water does not take place in bulk water

but at the surface of the protein Inspection of the

FDH domain crystal structure [9,10] appears to rule

out the possibility that amino acid side chains in the

vicinity of the flavin could take part directly in the

deprotonation, as these chains (two tyrosines and a

histidine) are too distant and⁄ or in a wrong

orienta-tion for direct hydrogen bonding to the N5 hydrogen

of FMNH•as required for proton abstraction

Never-theless, the active site of these enzymes on the flavin si

side is highly polar, with two arginines and ionizable

side chains such as a histidine and two tyrosines in the

FDH domain, with one of the latter being replaced in

LCHAO by a phenylalanine The pKa of the tyrosines

is not known, but it has been determined for

flavocyto-chrome b2 that the active site histidine (H373) has an

abnormal pKa of 9.1 in the reduced enzyme [30] The

crystal structure suggests that the pKaof this residue is

still elevated when the flavin is in the semiquinone

state [10] It is thus not impossible that electrostatic

factors, together with interaction of the active-site

resi-dues with specific water molecules via hydrogen

bond-ing, may accelerate the Tris-independent deprotonation

compared to what is expected in bulk water The

variation of the electrostatic environment with pH may

then contribute to the variation of the fast phase rate

with pH In addition, a role may also be played by

residues in mobile loop 4 of the b barrel, which are

partly invisible in the crystal structures of both

proteins [8–10] The boundaries of the invisible region

lie 15–20 A˚ away from the flavin, but there is

experi-mental evidence that modifications in this loop have

an impact on the flavin environment [6,31]

In the second ‘slow’ phase, the pKa of the radical

shifts to a value below 7 as expected from the

litera-ture The origin of the slow phase is intriguing We

propose that evolution of the flavin radical pKa in

these enzymes is due to protein conformational

changes upon passing from the fully reduced state to

the half-reduced state At the time of laser-induced

generation of the flavin radical, the protein is present

in its conformation in the fully reduced state, but then

undergoes relaxation to the conformation in the

half-reduced state The high pKa values associated with the

fast deprotonation phase would then correspond to the

pKa of the half-reduced flavin before conformational

relaxation A lower pKa prevails in the

conformation-ally relaxed protein, thus explaining the transition to

the anionic semiquinone On the basis of this

hypothe-sis, the deprotonation rate of the slow phase would be

the rate of the conformational change(s) Yet, at

pres-ent, there is no experimental evidence in support of

this hypothesis The crystal structure of the FDH domain in holo-flavocytochrome b2 is known at 2.3 A˚ resolution [9,10] At that resolution, the structure shows no significant difference between the fully reduced subunit and the subunit with flavin in the semiquinone state complexed with the product pyru-vate In both subunits, the flavin ring is slightly bent, and the rmsd for atomic positions of the FMN groups

is 0.17 A˚, with most of the deviations being localized

in the phosphate regions [9] Structures at atomic resolution are required in order to see whether the structural adjustment between the two redox states is due to a difference in the flavin planarity For LCHAO, only the structure of the oxidized enzyme is known [8]

LCHAO is an oxidase; the fully reduced flavin is re-oxidized at the expense of oxygen, with formation of hydrogen peroxide Although this enzyme stabilizes the anionic semiquinone, the latter has never been observed

as an intermediate in the catalytic cycle, no more than in most other flavo-oxidases [32,33] In contrast, in the flavocytochrome b2 catalytic cycle, the semiquinone is

an EPR-detectable intermediate [11] After being reduced by the substrate in a two-electron reaction, the flavin yields electrons one at a time to the heme in the same subunit [7] NMR studies at neutral pH demon-strated that, in the reduced enzyme, the flavin is proton-ated at N5 [34]; therefore it must lose the proton in order to form the anionic semiquinone after the first electron is transferred to the heme Values for the rate of FMN•) formation from FMNH)(equal to the rate of heme reduction by FMNH)) have been calculated from stopped-flow experiments under various experimental conditions [11,35–37] In 10 mm Tris⁄ HCl, with I = 0.1 (25C), conditions close to those used here, the heme reduction rate was estimated to be of the order of 1.5· 103s)1 [35,38] Thus, the rate determined in this work for the slow event leading to deprotonation of the neutral radical is about 10-fold faster than the electron transfer rate estimated in independent kinetic studies The loss of the N5 proton initially present in FMNH)is therefore not rate-limiting for heme reduction

In conclusion, the study shows that the experimental method proposed here makes possible the investigation

of protolytic reactions in flavoproteins at high tempo-ral resolution The results reveal an unexpected complexity in the kinetics of these reactions for the two enzymes studied, attributed hypothetically to a conformational relaxation induced by the change in the flavin redox state However, extension of the study

to other flavoenzyme classes and other buffers as well

as additional structural information are required to substantiate this hypothesis

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Experimental procedures

Laser flash photolysis

The laser flash photolysis set-up has been described

previ-ously [5,39] The third harmonic (k = 355 nm) obtained

from a pulsed (approximately 2 ns full width at half

pulsed Xe UV lamp was used as the probing light source,

in crossed-beam configuration Samples under study were

and equipped with glass tubing for degassing The laser

beam was shaped to 1 cm width and 0.3 cm height at the

laser entrance window A ground silica plate in front of the

window ensured homogeneous irradiation A diaphragm at

path adjacent to the laser entrance window The intensity

of the transmitted probe light was measured at selected

wavelengths as a function of time using a

The fluence of the laser pulses at the entrance window of

the sample cuvette was determined by ‘anthracene triplet

actinometry’ [40] In this case, the laser intensity was

atten-uated using calibrated neutral filters to avoid saturation

effects

The reduced flavoproteins are weakly fluorescent The

fluorescence emitted during the laser pulse interfered with

the measurement using the Xe lamp, and the measurements

during and immediately after the laser pulse (up to 5 ls)

were therefore performed using this lamp at a light intensity

that was high enough to make the perturbation by the

fluo-rescence pulse acceptable The intensity of the probe light

remained constant within 1% over 5 ls under this regime

For measurements at longer times, the Xe lamp was used

at a lower intensity Under this regime, the probe light

remained constant to within 0.5% over 5 ls after laser

exci-tation (absorbance error ±0.001) and within 2% over

100 ls (absorbance error ±0.004)

Protein preparations

Recombinant LCHAO was prepared as described previously

[6], except that DEAE Sepharose Fast Flow (Pharmacia,

Orsay, France) was used instead of DEAE cellulose for the

second chromatographic step Samples (0.1–0.3 mm) were

The recombinant FDH domain was prepared as described

previously [12] For the laser flash experiments, 0.06-0.12 mm

chloride ion has been reported to inhibit the enzyme by

binding to the active site [12]

The flavoprotein solutions (3 mL) were de-aerated in the

the solution surface over 1 h on ice with gentle rocking The cuvettes were then closed by means of a septum, and

a DC Xe lamp, ensuring photoreduction of the flavin by the EDTA present in the solutions In the case of the FDH domain, it was necessary to reduce the major part of the flavin by adding 200 lL of 30 mm lithium l-lactate before photoreduction The final l-lactate concentration (1.9 mm) was far below the concentration that inhibits the enzyme by binding to the reduced form (several hundred millimolar [41]) Similarly, the amount of pyruvate formed (in princi-ple no more than the enzyme concentration) should have been low compared to that required for binding to the reduced or semiquinone forms [12,42] Therefore, this pro-cedure did not introduce a bias in the comparison with LCHAO

Exposure to the UV laser pulses resulted in oxidation of the reduced flavoproteins to a slight extent The solutions were therefore regularly exposed to visible light to re-reduce oxidized flavin However, the polypeptide chains were also gradually destroyed as shown by activity tests, and the solutions were discarded after a few tens of laser shots (5–10% activity loss) The results were not affected by degradation within this limit

At the enzyme concentrations used in this work, sponta-neous flavin dissociation could not have taken place

on the observation conditions [7] No values have been determined for the recombinant FDH domain or LCHAO, but these proteins appeared as stable in this respect during

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