bubble column enables higher reaction rate for

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General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights. Users may download and print one copy of any publication from the public portal for the purpose of private study or research. You may not further distribute the material or use it for any profit-making activity or commercial gain You may freely distribute the URL identifying the publication in the public portal If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. Downloaded from orbit.dtu.dk on: Jan 07, 2022 Bubble Column Enables Higher Reaction Rate for Deracemization of (R,S)1 Phenylethanol with Coupled Alcohol Dehydrogenase/NADH Oxidase System Dias Gomes, Mafalda; Bommarius, Bettina; Anderson, Shelby; Feske, Brent D.; Woodley, John; Bommarius, Andreas Published in: Advanced Synthesis and Catalysis Link to article, DOI: 10.1002/adsc.201900213 Publication date: 2019 Document Version Peer reviewed version Link back to DTU Orbit Citation (APA): Dias Gomes, M., Bommarius, B., Anderson, S., Feske, B. D., Woodley, J., & Bommarius, A. (2019). Bubble Column Enables Higher Reaction Rate for Deracemization of (R,S)1Phenylethanol with Coupled Alcohol Dehydrogenase/NADH Oxidase System. Advanced Synthesis and Catalysis, 361(11), 2574-2581. https://doi.org/10.1002/adsc.201900213

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Page 1: Bubble Column Enables Higher Reaction Rate for

General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights.

Users may download and print one copy of any publication from the public portal for the purpose of private study or research.

You may not further distribute the material or use it for any profit-making activity or commercial gain

You may freely distribute the URL identifying the publication in the public portal If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim.

Downloaded from orbit.dtu.dk on: Jan 07, 2022

Bubble Column Enables Higher Reaction Rate for Deracemization of (R,S)1Phenylethanol with Coupled Alcohol Dehydrogenase/NADH Oxidase System

Dias Gomes, Mafalda; Bommarius, Bettina; Anderson, Shelby; Feske, Brent D.; Woodley, John;Bommarius, Andreas

Published in:Advanced Synthesis and Catalysis

Link to article, DOI:10.1002/adsc.201900213

Publication date:2019

Document VersionPeer reviewed version

Link back to DTU Orbit

Citation (APA):Dias Gomes, M., Bommarius, B., Anderson, S., Feske, B. D., Woodley, J., & Bommarius, A. (2019). BubbleColumn Enables Higher Reaction Rate for Deracemization of (R,S)1Phenylethanol with Coupled AlcoholDehydrogenase/NADH Oxidase System. Advanced Synthesis and Catalysis, 361(11), 2574-2581.https://doi.org/10.1002/adsc.201900213

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Title: Bubble Column Enables Higher Reaction Rate forDeracemization of (R,S)-1-Phenylethanol with Coupled AlcoholDehydrogenase/NADH Oxidase System

Authors: Mafalda Dias Gomes, Bettina Bommarius, Shelby Anderson,Brent D. Feske, John Woodley, and Andreas Bommarius

This manuscript has been accepted after peer review and appears as anAccepted Article online prior to editing, proofing, and formal publicationof the final Version of Record (VoR). This work is currently citable byusing the Digital Object Identifier (DOI) given below. The VoR will bepublished online in Early View as soon as possible and may be differentto this Accepted Article as a result of editing. Readers should obtainthe VoR from the journal website shown below when it is publishedto ensure accuracy of information. The authors are responsible for thecontent of this Accepted Article.

To be cited as: Adv. Synth. Catal. 10.1002/adsc.201900213

Link to VoR: http://dx.doi.org/10.1002/adsc.201900213

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VERY IMPORTANT PUBLICATION FULL PAPER

DOI: 10.1002/adsc.201((will be filled in by the editorial staff))

Bubble Column Enables Higher Reaction Rate for

Deracemization of (R,S)-1-Phenylethanol with Coupled Alcohol

Dehydrogenase/NADH Oxidase System

Mafalda Dias Gomes†,a, Bettina R. Bommarius†,b, Shelby R. Anderson b, Brent D.

Feskec John M. Woodley a* and Andreas S. Bommarius b*

a Department of Chemical and Biochemical Engineering, Technical University of Denmark, Building 229, Søltofts Plads,

DK-2800 Kgs. Lyngby, Denmark

+45 45 25 28 85

[email protected]

b School of Chemical and Biomolecular Engineering, Krone Engineered Biosystems Building, Georgia Institute of

Technology, 950 Atlantic Drive N.W., Atlanta, GA 30332, USA

+1 (404) 385-1334

[email protected]

c Department of Chemistry and Biochemistry, Georgia Southern University, Science Center Suite 1505, 11935 Abercorn

St., Savannah, GA 31419

+1 (912) 344-3210

[email protected]

†: contributed equally

Received: ((will be filled in by the editorial staff))

Supporting information for this article is available on the WWW under http://dx.doi.org/10.1002/adsc.201######.

Abstract: One of the major drawbacks for many biocatalysts is their poor stability under industrial process conditions. A particularly interesting example is the supply of oxygen to biooxidation reactions, catalyzed by oxidases, oxygenases or alcohol dehydrogenases coupled with NAD(P)H (reduced nicotinamide adenine dinucleotide phosphate) oxidases, which all require the continuous supply of molecular oxygen as an oxidant or electron acceptor. Commonly, oxygen is supplied to the bioreactor by air sparging. To ensure sufficient oxygen transfer from the gas to the liquid phase, stirring is essential to disperse the gas bubbles and create high gas-liquid interfacial area. Studies indicate that the presence of gas-liquid interface induces enzyme deactivation by protein unfolding which then readily aggregates and can subsequently precipitate. This contribution has examined the effects of stirring and the presence of gas-liquid interface on the kinetic stability of water-forming NAD(P)H oxidase (NOX) (EC1.6.3.2).

These effects were studied separately and a bubble column apparatus was successfully employed to investigate the influence of gas-liquid interfaces on enzyme stability. Results showed that NOX deactivation increases in proportion to the gas-liquid interfacial area. While air enhances the rate of stability loss compared to nitrogen, stirring causes faster loss of activity in comparison to a bubble column. Finally, deracemization of 1-phenylethanol, using a coupled alcohol dehydrogenase /NADH oxidase system (ADH/NOX), proceeded with a higher rate in the bubble column than in quiescent or in a stirred solution, although, inactivation was also accelerated in the bubble column over a quiescent solution.

Keywords: Bubble column; NADH oxidase; deracemization; gas-liquid interface; biocatalysis

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Introduction

The integration of biocatalysis into synthetic

production schemes for pharmaceuticals and fine

chemicals continues to make significant progress.

Whilst an enzyme’s ability to catalyze useful

reactions under mild conditions is of great importance,

it is their excellent selectivity that draws attention for

wider applications in chemical synthesis. [1] [1a].

Additionally, biocatalysis offers economic and

environmental advantages over chemical routes,

contributing to the development of more sustainable

industrial processes. [2] [3]. However, despite the many

benefits of using biocatalysts, their stability under

relevant process conditions is frequently cited as a

drawback to the wider usage of enzymatic catalysis [4].

The oxidoreductases are one class of enzymes that

has become increasingly relevant in recent years. [5] [6] These enzymes can catalyze oxidation reactions to

produce molecules of considerable commercial

interest, that are otherwise difficult to obtain in a

single step using non-enzymatic methods. [7] [8]. [9] In

particular, oxidation of alcohols to ketones or

aldehydes, essential to produce many building blocks

for valuable chemicals, can be catalyzed using either

alcohol oxidases (AOXs) or alcohol dehydrogenases

(ADHs). The latter are better known operating in the

reductive direction [10]. Nevertheless, in the oxidative

mode, the ADHs have been more commonly used

than AOXs, since there are more discovered enzymes

with activity and selectivity towards molecules of

interest.[11] [12] Nevertheless, in the oxidative direction,

ADHs require NAD(P)+ as an electron acceptor,

which is an expensive cofactor and therefore needs to

be regenerated to achieve an economically feasible

process. [13]. One of the most interesting solutions to

this problem is the use of water-forming NAD(P)H

oxidases, NOX2 (herein termed NOX). Such

enzymes oxidize NAD(P)H to NAD(P)+ while

concomitantly reducing molecular oxygen to water

(Scheme 1). NOX2 enzymes from Lactobacillus

sanfranciscensis, [14] [15] Lactococcus lactis [15],

Lactobacillus pentosus, [16] Streptococcus mutans [17]

and Lactobacillus plantarum [18] have been

characterized (for a review, see [13]). Ultimately,

therefore both types of oxidative system, AOX and

ADH/NOX, need molecular oxygen as an oxidant in

stoichiometric amounts (0.5 mol O2/ mol product).

This is highly attractive for industrial manufacturing

processes since it avoids the use of harmful metal

oxidants. However, it also comes with some

limitations, especially with respect to enzyme

stability under the target process conditions.

Scheme 1. Enzymatic oxidation of racemic 1-

phenylethanol using a coupled ADH/NOX system.

Since oxygen has a particularly low solubility in

water (where the reaction occurs) it cannot be

dissolved in solution prior to the reaction as would be

the case with other reactants, but instead it is

necessary to continuously supply it to the reaction

medium. Usually, this is done by bubbling (sparging)

air into the liquid, in a well agitated reactor. Stirring

is essential to break the gas into small bubbles,

increasing their surface area and thereby their

residence time in the reactor in order to ensure

sufficient oxygen transfer from the gas to the liquid

phase, where reaction occurs. To achieve industrially

relevant productivities [2], [19] fast oxygen transfer

from the gas to the liquid phase is needed. Therefore,

to obtain a high mass transfer coefficient (kla) a large

gas-liquid interfacial area is needed. However, it has

been shown that the presence of gas-liquid interface

can deactivate some enzymes. For instance,

Donaldson et al. (1980) [20] observed that acid

phosphatase deactivates in the presence of air-liquid

interfaces and that the rate of deactivation is

dependent upon the air-liquid contact time in a

laminar flow reactor. Later, it was found that

lysozyme deactivates when in contact with air-liquid

interfaces and also in the presence of gaseous

nitrogen. [21]. Around the same time, Patil et al.

(2000) and Mohanty et al.(2001) [22] [23] have also

shown that lipases deactivate in the presence of

surface aeration. Likewise, Bommarius & Karau

(2005) [24] found that formate dehydrogenase

deactivates at the gas-liquid interface (using both air

and gaseous oxygen). More recently, Findrik et al.

(2014) [25] revealed that the increase of aeration in a

stirred tank reactor decreased the stability of D-amino

acid oxidases. Finally, recent work developed in

shake flasks demonstrates that cellulases also

deactivate at the air-liquid interface. [26]. Nevertheless,

not all enzymes appear to be affected by the interface.

For example, Toftgaard Pedersen et al. (2015) [27]

showed that galactose oxidase did not lose any

activity when exposed to an air-liquid interface in a

stirred tank reactor.

Since sparging air into a stirred tank reactor is still

the most efficient and economical way of supplying

oxygen to biooxidations, the presence of a gas-liquid

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interface is unavoidable. As mentioned previously,

the stability of the biocatalyst is crucial for successful

application of biocatalytic oxidations in industry.

Therefore, the reasons for protein inactivation in the

presence of such interfaces needs to be better

understood. This is especially important for oxidases,

since oxygen is also a co-substrate in the reaction.

Additionally, methods that allow the study of the

deactivation of these proteins in the presence of gas-

liquid interfaces also need to be developed.

In order to explore the effect of gas-liquid

interfacial area on the stability of oxygen-dependent

enzymes, a bubble column was built (Figure 1) based

on previously published work by Bommarius &

Karau (2005) [24] where, inter alia, the deactivation of

formate dehydrogenase (FDH) at gas-liquid interfaces

was studied. The bubble column design was

reproduced and used specifically for NOXs. Aside

from using such a device with a controlled interfacial

area for investigations of the effect of the gas-liquid

interface on enzymes, we also reasoned that the

gentler conditions (in the absence of stirring) might

allow enzymes which would otherwise be sensitive to

such interfaces to be used effectively. Such an

equipment therefore represents a compromise, where

bubbles are formed to allow sufficient mass transfer,

whilst still avoiding mixing and therefore an excess

of interface which might otherwise deactivate the

enzymes. To test this concept, in the current

contribution we have tested an ADH/NOX system in

a bubble column.

Figure 1. Diagram of the bubble column setup. Inset:

image of bubbles during representative experiments.

The present work investigates the influence of air-

liquid interface on the stability of water-forming

NOXs from Lactobacillus plantarum (NoxV), [18]

both for NOX alone as well as in the context of

deracemization of a racemic secondary alcohol

catalyzed by ADH/NOX. The ADHs chosen belong

to the SDR (Short-chain Dehydrogenases/Reductase)

superfamily [28] and catalyze the respective

enantiomers of the chosen substrate 1-phenylethanol,

(R)-ADH from Lactobacillus brevis and (S)-ADH

from Bacillus subtilis. The (R)-ADH has been

employed frequently for enantioselective alcohol

production [29] including by some of us for oxidative

deracemization. [14] Aqueous solutions of both

enzymes were sparged with air (21% oxygen)

through a bubble column. As the presence of oxygen

is known to over-oxidize some amino acid residues in

oxidases, [30] the stability of these enzymes was also

tested in the presence of nitrogen gas (i.e. in the

absence of oxygen). Control experiments in quiescent

and in stirred solutions were also carried out to

account for time-dependent protein deactivation.

Furthermore, the causes of enzyme deactivation in

the presence of a gas-liquid interface were addressed

and discussed.

Results and Discussion

Influence of reaction environment on the

stability of NOX and ADH

With the purpose of achieving enzymatic

deracemization of (R/S)-phenylethanol employing the

ADH/NOX system, and since the supply of molecular

oxygen is required for the reaction to occur, we tested

the influence of gas-liquid interface on the kinetic

stability of NOX. Several control experiments were

performed to compare three distinct reaction

environments: (1) quiescent liquid (2) agitated/stirred

liquid and (3) sparged liquid. As observed in Figure 2,

the NOX deactivation kinetics were close to first-

order. Accordingly, a deactivation rate constant (kd)

was calculated from the slope of the natural logarithm

of the residual activity over time. [31]. Deactivation

rate constants kd and enzyme half-lives t1/2 are

presented in Table 1.

Figure 2. Residual activity of NOX as a function of time.

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NOX was incubated in quiescent conditions in the

presence of low interfacial areas of pure nitrogen and

air (21 % O2; 79 % N2), by filling the headspace of

the vials independently with each of the two gases.

NOX was significantly more stable (i.e. longer half-

life) in the absence than in the presence of oxygen,

with half-lives of 53 and 21 h, respectively (Table 1

and Supporting Information, Table S1). Furthermore,

NOX kinetic stability was tested in stirred solution in

the presence of pure nitrogen and air. Under nitrogen,

the NOX half-life was found to be shorter compared

to quiescent conditions, 40 vs 53 h, indicating that

mixing increases NOX deactivation (Supporting

Information, Table S1). In aerated, stirred solution,

NOX deactivation was almost doubled compared to

quiescent solution (t1/2 of 12 vs 21 h, Table 1).

Table 1 Deactivation of NOX in the presence of air under

three reaction environments, with and without

(R,S)-1-phenylethanol (substrate) present.

Reaction a) kd b) (h-1) t 1/2 (h) c)

Quiescent 0.033 21

Stirred 0.06 12

Sparged

Quiescent, substrate

Stirred, substrate

Sparged, substrate

0.031

0.032

0.021

0.05

22

22

32

13 a) reaction conditions for NOX, pH 7, 25 oC. b) rate constant of

enzyme deactivation c) enzyme half-life (t1/2 = ln 2/kd).

Figure 3: A Deactivation of NOX in the presence of either (R) or (S)-ADH during conversion of 1-phenylethanol. B

Corresponding HPLC analysis of consumed (R,S)-1-phenylethanol. C Deactivation of NOX in the presence of both (R)

and (S)-ADH during conversion of 1-phenylethanol. D Corresponding HPLC analysis of consumed 1-phenylethanol. All

experiments were performed with sparged air. All measurements for the experiments were done in duplicates with a

standard deviation of 1.5 %. The experiment with both ADH in C,D was repeated twice with similar results within the time

frame of 6 hours.

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Therefore, to eliminate the effect of mixing and to

investigate the effect of the gas-liquid interface alone,

we incubated NOX in the bubble column sparged

with air or N2. The enzyme was exposed to larger

interfacial areas with increasing incubation times.

Sparging with air, we observed that NOX was

significantly more stable in the bubble column than in

stirred conditions, indeed, as stable as in quiescent

solution (Table 1). Sparging with nitrogen, we

observed a slightly reduced half-life compared to

quiescent solution but enhanced stability compared to

stirred solution (Supporting Information, Table S1).

During substrate deracemization in the bubble

column, the low solubility of the product

acetophenone resulted in its precipitation, which first

decreased bubble size and then clogged the needle,

both of which decreased NOX stability (last data

point in Table 1). In contrast, incubation of NOX

with the ADH substrate 1-phenylethanol under

quiescent conditions with air was found to have no

effect on the kinetic stability of the enzyme (Table 1).

NOX was found to be most stable in a quiescent

liquid followed by a sparged liquid and, finally, in an

agitated liquid. While not relevant for the ADH/NOX

system which requires the presence of oxygen to

function, NOX was more stable in the presence of

nitrogen than in air (Table 1 and Supporting

Information, Table S1). Importantly, these results

therefore support the idea of using a bubble column

for the ADH/NOX system, since it avoids severe

agitation.

In comparing NOX stability in the bubble column

with quiescent conditions over the same time scale,

we see that the deactivation of NOX in the bubble

column is dependent on the gas-liquid interfacial area

(Supporting information, Figure S2), and not on the

incubation time, in accordance with previous

observations with formate dehydrogenase (FDH). [24].

To account for ADH stability, both enzymes were

incubated in sparged, stirred, and quiescent

conditions; similar deactivation behavior was

observed (Supporting Information, Table S1). All

experiments were performed at pH 7 since the

coupled reaction with ADH/NOX for deracemization

of 1-phenylethanol is most favorable at neutral pH 7. [14] [18]

ADH/NOX reactions in the bubble column

To demonstrate suitability of NOX for

deracemization reactions we chose to compare

phenylethanol oxidation catalyzed by ADH/NOX in a

bubble column, quiescent solution, and in an agitated/

stirred solution. ADH was chosen as the model

enzyme since both (R)-ADH and (S)-ADH were

readily available. The first two deracemization

experiments were performed using each ADH in

combination with NOX to achieve 50 % conversion

of the racemic substrate, 1-phenylethanol, at 50 mM

racemate.

Results depicted in Figure 3 reveal that use of the

bubble column enabled a reaction rate of 0.12

mM/min for (R)-ADH (Panel 3B), almost 10-fold the

rate in quiescent solution for the first 3 hours. It is

important to note that whereas the (R)-ADH is

enantioselective and the conversion stopped at 50 %

when using this ADH alone, the not fully

characterized (S)-ADH seems to be less selective, as

the conversion continued to about 40 % for the

sparged reaction and 22 % for quiescent conditions

(Panel 3B). Enantiomeric excess will be evaluated in

the future. When both (R)-ADH and (S)-ADH were

combined with NOX in the bubble column (Panel

3D), the reaction in the bubble column was almost

complete after 6 hours with a reaction rate of 0.19

mM/min for the first 2 hours, 6-fold higher than the

quiescent and twice as high as the stirred controls

(0.03 and 0.1 mM/min, respectively).

ADH/NOX-catalyzed deracemization of (R/S)-

phenylethanol proceeded 6-10 times faster in a

bubble column sparged with air than in air-saturated

quiescent solution; in a gently stirred solution

(Reynolds number Re 33; Re = Nd2/, with

density = 1015 kg/m3, rotational velocity of the

stirrer N = 2 s-1, stirrer diameter d of 5 mm, and

viscosity = 1.0510-3 kg/(ms)), the reaction

proceeded about twice as fast as in quiescent solution.

These advantages of sparged and stirred systems have

to be weighed against enhanced enzyme deactivation.

Incubation experiments of NOX, carried out in three

different reaction environments, showed that NOX is

indeed sensitive towards gas-liquid interfaces (Panels

3A and 3C). Results also reveal that the presence of

oxygen in the gas phase enhances the deactivation

rate of the enzyme (compared to solely nitrogen).

Furthermore, it was observed that NOX is more

stable in quiescent solution than in a sparged liquid,

which in turn was found to have a longer half-life

than NOX in stirred solution. Thus mixing results in a

higher deactivation rate constant than the presence of

gas-liquid interfaces. The ADH kinetic stability was

also tested and was found to follow the same trend as

NOX.

While both NOX and ADHs are most stable in

quiescent solution, the air-liquid interfacial area is

smaller in such a system than in sparged solution in

the bubble column. However, the smaller interfacial

area results in a lower oxygen transfer rate (OTR)

from the gas to the liquid phase. Then, under

quiescent conditions, oxygen transfer can limit the

reaction rate and thus volumetric productivity (space-

time yield). Although the enzyme stability may be

compromised in the bubble column, this set-up

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facilitates oxygen transfer, resulting in higher

reaction rates for oxygen-dependent reactions.

To demonstrate the positive effect of continuously

supplied air-liquid interface on the reaction rate of

ADH/NOX catalyzed deracemization of 1-

phenylethanol this reaction was performed in the

bubble column and in a quiescent solution.

Conclusion

For ADH/NOX-catalyzed deracemization of alcohols,

a bubble column with sparged air yields a higher

reaction rate than a quiescent solution but also

encounters a higher rate of enzyme deactivation.

Nevertheless, the half-life of NOX in the bubble

column was sufficient to achieve complete

conversion of 50 mM phenylethanol for the coupled

reaction with ADH. Therefore, the bubble column is

an attractive apparatus to run enzymatic oxidation

reactions using coupled ADH/NOX systems.

As had been observed for formate

dehydrogenase (FDH), deactivation of NOX in a

bubble column depends on interfacial area, not on

time. Sparging results in slower deactivation than in

stirred solution. Sparging or stirring in presence of

air rather than nitrogen enhances deactivation. These

trends were also followed by the alcohol

dehydrogenases employed in this study (details in the

supporting information).

Experimental Section

Materials

Potassium phosphate buffer was used for all pH 7

solutions. All chemicals used for protein purification

were of ACS chemical grade. DTT (Goldbio, St.

Louis, MO) was used for NOX purification. Lysates

and pure NOX from L. plantarum (NoxV) were

prepared and modified according to Park et al. (2011). [18] NADH was purchased from VWR (Radnor, PA,

USA).

Enzyme purification

NoxV in pET28a was expressed using BL21 plys

cells and overnight express media (VWR, Radnor,

PA, USA). Cells were harvested at 4000 g (Beckman,

Brea, CA) for 20 min and then lysed in 50 mM

sodium acetate pH 5.0 + 5 mM DTT. This resulted in

much improved lysate which then was further

purified to 90 % homogeneity using a

Phenylsepharose FF on an AKTA system and a linear

gradient from 2 M to 0 M ammonium sulfate, 50 mM

Tris pH 7.5 and 5 mM DTT.

(R)-ADH (Lactobacillus brevis) [29a] and (S)-ADH

(Bacillus subtilis) were purified using IMAC-Ni-

NTA technology, for the (R)-ADH 5 mM MgCl2 was

added to all solutions including reactions.

Control Experiments

Control experiments were performed in glass vials

(4 and 25 mL). A magnetic stirrer and a stirring plate

were used when agitation was desired. Pure NOX and

ADH were incubated for 72 hours, at room

temperature and pH 7. All experiments were carried

out with a pure enzyme solution of 10 % (v/v) in

phosphate buffer in a total volume of 4 mL. For each

experiment, two different control conditions were

tested: (1) incubation under a quiescent solution in 4

mL closed vials (2) incubation in the presence of

gentle agitation/stirring in a closed container (4 mL

vials). Samples were taken over time, stored on ice to

stop further the enzyme deactivation and the residual

activity was measured following the NOX/ADH

activity assay procedure described below. Control

experiments for the biocatalytic conversion were set

up accordingly and the corresponding substrate was

added in the concentration described in the results

section.

NOX activity assay

Initial activity of NOX was determined by

following absorption changes of NADH consumption

in a spectrophotometer at 340 nm (ɛ = 6.22 mM-1 cm-

1), at 25 °C with a light path of 1 cm. Absorbance was

measured for 2 minutes using 0.2 mM of NADH, 1 %

(v/v) of clarified lysate and phosphate buffer at pH 7

(concentrations in the cuvette). The cuvettes were

well mixed to ensure saturation of oxygen in the

solution with air at atmospheric pressure. One unit

(U) corresponds to 1 µmol of NAD+ produced per

minute at 25°C, pH 7 using phosphate buffer. NoxV

from L. plantarum had an average activity of 50

U/mL lysate and between 60-80 U/ml for the pure

NOX.

ADH activity assay

ADH activity after purification was assessed using

absorption changes of NADH consumption with 20

mM acetophenone as a substrate. Same NADH

conditions as above were applied. For monitoring

enzyme deactivation during the biocatalytic

conversions 50 mM phenylethanol and 0.4 mM

NAD+ were used to ensure separation from NOX

activity in the same experiment.

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Bubble column experiments

To investigate the deactivation of enzymes in the

presence of a gas-liquid interface, a bench scale

bubble column was used. In this defined and

controlled environment, gas bubbles rise in a stagnant

liquid solution under the influence of gravitational

force. The gas flow rate was defined so the bubbles

did not collide with each other and remained

spherical throughout the experiments. The bubbles

rose in a zig-zag and spiral pattern, hitting the column

wall in the same places. Even so, from the recorded

videos, the bubbles appear to remain nearly spherical

for the whole course of the experiment. The diameter

of the bubbles was observed to be 3 mm.

Bubble column setup

The bubble column was a glass tube with a length

of 48 cm and an inner diameter of 6.2 mm

(Supporting Information, Figure S1). A needle with

an inner diameter of approximately 0.6 mm was

attached to the bottom of the column and operated as

a nozzle (Supporting Information, Figure S1). Air and

nitrogen (99.9 % pure) were sparged through the

nozzle at a given flow rate (Q) of 14 mL min-1 (2.3

x10-7 m3 s-1). The gas bottles were connected to a

mass flow controller to measure the flow rate and

assure a constant value. The column had a liquid

height (L) of 25 cm and the residence time of a

bubble (θ) was approximately 1.7 seconds. A GoPro

Hero 6 camera (frame rate of 240 fps, San Mateo, CA,

USA) photographed and filmed the set-up to verify

the rising bubbles regime and that the bubbles did not

touch each other (for video URL, see Supplemental

Information). The bubble diameter (db) was

established by a photograph of the column that

contained a graduated scale. A tube connected to a

syringe was installed at the top of the column to fill in

the column with the enzyme solution and to collect

samples (sample port).

Procedure

First, the gas flow rate was set to 14 mL min-1.

When it was constant, 10 mL NOX solution of 10 %

(v/v) in buffer was slowly injected from the sample

port. Samples were collected at regular time intervals,

stored on ice to stop further enzyme deactivation and

tested for residual activity following the NOX

activity assay described above. Before starting an

experiment, the column was cleaned with acetone so

the path of the bubbles was not interrupted. The

concentration of enzyme solution was kept the same

to ensure constant surface tension. For conversion

experiments, 50 mM racemic 1-phenylethanol was

employed as the substrate in the ADH/NOX

experiments.

HPLC analysis

50 µl samples were taken of each tested conditions

((1) quiescent liquid (2) agitated/stirred liquid and (3)

sparged liquid.) that underwent biocatalytic

conversion of 50 mM 1-phenylethanol at several time

points. These samples were diluted 1:5 in acetonitrile

and filtered to remove protein matter. 5 µl of these

samples were separated on a C18 YMC ODS-AQ

column (5.5 µm, 3x100 mm, YMC, America) using a

Shimadzu ULPC 20A system with a water-

acetonitrile mobile phase. A step gradient from 5% to

15% in 2 min and then up to 40 % acetonitrile in 20

min was used to separate alcohol from ketone. The

alcohol eluted at 10.5 min and the ketone at 14 min

(Figure S3).

Product characterization

For Mass spectrometry analysis, the product peak

observed in HPLC was fractionated (see Figure S3),

fractions collected, extracted with 100 % chloroform,

dried and analyzed via Mass Spec. High

resolution mass spectra (HRMS) were obtained on a

Thermo Scientific Q Exactive Plus Orbitrap Mass

Spectrometer. The sample was dissolved in 50 %

acetonitrile/ 50 % formic acid (0.1%) for analysis in

positive ion mode (Figure S4, panel A).

For NMR analysis, after 6h conversion with

ADH/NOX the reactor volume was collected,

extracted with chloroform and evaporated affording a

colorless crude oil.

The resulting crude oil was then purified by flash

chromatography (solvent 8 Hex:1 EtOAc) to afford 9

mg of acetophenone in a 15 % yield as a colorless oil. 1H NMR (300 MHz CDCl3) δ: 7.2-7.7 (m, 5H), 2.36

(s, 3H); 13C NMR (300 MHz CDCl3) δ: 198, 136.9,

132.9, 128.4, 128.1, 26.5; mass (EI) 51, 77, 105, 120.

Acknowledgements

MDG acknowledges financial support from the Technical University of Denmark (DTU). BB and ASB gratefully acknowledge financial support from National Science Foundation of the United States (NSF) grant IIP-1540017, BDF and ASB gratefully acknowledge financial support from NSF grant CBET-1512848. We wish to acknowledge the Systems Mass Spectrometry Core Facility at the Parker H. Petit Institute for Bioengineering and Bioscience at the Georgia Institute of Technology for the use of their shared equipment, services and expertise.

References

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Page 10: Bubble Column Enables Higher Reaction Rate for

8

[1] a) D. J. Pollard, J. M. Woodley, Trends

Biotechnol. 2007, 25, 66-73; b) J. M.

Woodley, M. Breuer, D. Mink, Chem. Eng.

Res. Des. 2013, 91, 2029-2036.

[2] J. M. Woodley, Comput. Chem. Eng. 2017,

105, 297-307.

[3] R. A. Sheldon, J. M. Woodley, Chem. Rev.

2018, 118, 801-838.

[4] A. S. Bommarius, Annu. Rev. Chem. Biomol.

Eng. 2015, 6, 319-345.

[5] J. Dong, E. Fernandez-Fueyo, F. Hollmann,

C. E. Paul, M. Pesic, S. Schmidt, Y. Wang, S.

Younes, W. Zhang, Angew. Chem. Int. Ed.

Engl. 2018, 57, 9238-9261.

[6] N. J. Turner, Chem. Rev. 2011, 111, 4073-

4087.

[7] N. Turner, in Enzyme Catalysis and Organic

Synthesis 2012.

[8] G. Grogan, Curr. Opin. Chem. Biol. 2018, 43,

15-22.

[9] W. R. Birmingham, N. J. Turner, ACS Catal.

2018, 8, 4025-4032.

[10] S. M. A. De Wildeman, T. Sonke, H. E.

Schoemaker, O. May, Accounts Chem. Res.

2007, 40, 1260-1266.

[11] J. Brummund, T. Sonke, M. Müller, Org.

Process Res. Dev. 2015, 19, 1590-1595.

[12] J. Liu, S. Wu, Z. Li, Curr. Opin. Chem. Biol.

2018, 43, 77-86.

[13] G. Rehn, A. T. Pedersen, J. M. Woodley, J.

Mol. Catal. B: Enzymatic 2016, 134, 331-339.

[14] B. R. Riebel, P. R. Gibbs, W. B. Wellborn, A.

S. Bommarius, Adv. Syn. Catal. 2003, 345,

707-712.

[15] G. T. Lountos, R. Jiang, W. B. Wellborn, T.

L. Thaler, A. S. Bommarius, A. M. Orville,

Biochemistry 2006, 45, 9648-9659.

[16] C. Nowak, B. Beer, A. Pick, T. Roth, P.

Lommes, V. Sieber, Front. Microbiol. 2015,

6, 957.

[17] B. Petschacher, N. Staunig, M. Muller, M.

Schurmann, D. Mink, S. De Wildeman, K.

Gruber, A. Glieder, Comput. Struct.

Biotechnol. J. 2014, 9, e201402005.

[18] J. T. Park, J.-I. Hirano, V. Thangavel, B. R.

Riebel, A. S. Bommarius, J. Mol. Catal. B:

Enzymatic 2011, 71, 159-165.

[19] P. Tufvesson, J. Lima-Ramos, J. S. Jensen, N.

Al-Haque, W. Neto, J. M. Woodley,

Biotechnol. Bioeng. 2011, 108, 1479-1493.

[20] T. L. Donaldson, E. F. Boonstra, J. M.

Hammond, J. Colloid Interface Sci. 1980, 74,

441-450.

[21] a) M. Caussette, A. Gaunand, H. Planche, S.

Colombié, P. Monsan, B. Lindet, Enzyme

Microb. Technol. 1999, 24, 412-418; b) S.

Colombié, A. Gaunand, B. Lindet, Enzyme

Microb. Technol. 2001, 28, 820-826.

[22] N. S. Patil, R. S. Ghadge, S. B. Sawant, J. B.

Joshi, AIChE J. 2000, 46, 1280-1283.

[23] M. Mohanty, R. S. Ghadge, N. S. Patil, S. B.

Sawant, J. B. Joshi, A. V. Deshpande, Chem.

Eng. Sci. 2001, 56, 3401-3408.

[24] A. S. Bommarius, A. Karau, Biotechnol.

Prog. 2005, 21, 1663-1672.

[25] Z. Findrik, I. Valentović, Đ. Vasić-Rački,

Appl. Biochem. Biotechnol. 2014, 172, 3092-

3105.

[26] S. Bhagia, R. Dhir, R. Kumar, C. E. Wyman,

Sci. Rep. 2018, 8, 1350.

[27] A. Toftgaard Pedersen, W. R. Birmingham,

G. Rehn, S. J. Charnock, N. J. Turner, J. M.

Woodley, Org. Proc. Res. Dev. 2015, 19,

1580-1589.

[28] M. Gräff, P. C. F. Buchholz, P. Stockinger,

B. Bommarius, A. S. Bommarius, J. Pleiss,

Proteins 2019, 1-9; 10.1002/prot.25666. [29] a) N. H. Schlieben, K. Niefind, J. Muller, B.

Riebel, W. Hummel, D. Schomburg, J. Mol.

Biol. 2005, 349, 801-813; b) J. Schumacher,

M. Eckstein, U. Kragl, Biotechnol. J. 2006, 1,

574-581.

[30] A. Slavica, I. Dib, B. Nidetzky, Appl.

Environ. Microbiol. 2005, 71, 8061.

[31] A. Sadana, Biocatalysis 1989, 2, 175-216. ä

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epte

d M

anus

crip

t

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FULL PAPER

Bubble Column Enables Higher Reaction Rate for Deracemization of 1-Phenylethanol with Coupled Alcohol Dehydrogenase/NADH Oxidase System

Adv. Synth. Catal. Year, Volume, Page – Page

Mafalda Dias Gomes†, Bettina R. Bommarius†, Shelby R. Anderson, Brent D. Feske, John M. Woodley* and Andreas S. Bommarius*

10.1002/adsc.201900213

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