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Fig. 2.1 Schematic illustration of multiphoton absorption ... 18 Fig. 2.2 Absorption coefficient spectrum of water, together with the wavelength positions of the most widely used lasers ... 18 Fig. 2.3 Gibbs free energy versus specific volume of a pure substance for several temperatures starting at the saturation temperature up to the spinodal temperature ... 19 Fig. 2.4 Variation of vapor bubble nucleation rate with superheat temperature ... 19 Fig. 2.5 Schematic illustration of laser tsunami in water ... 19 Fig. 2.6 Plasma, shock wave, and cavitation bubble produced by Nd:YAG laser pulses of different duration and energy ... 20

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Fig. 2.7 Experimentally determined shock wave pressure ... 20

Fig. 2.8 Hydrophone signals measured at a distance of 10 mm from the emission center of the shock waves ... 20

Fig. 2.9 The diameter of the cavitation bubble in water as a function of time ... 21

Fig. 2.10 Spatially limited transient pressure generated by femtosecond laser can induce molecular nucleation in supersaturated solution ... 21

Fig. 2.11 Microscopic images of generated anthracene crystals (a) and a growth process of a bending film-like crystal created at the surface of a large laser-induced bubble (b-d) ... 22

Chapter 3 Experiment Fig. 3.1 Picture of mode-locked Ti:sapphire laser, Tsunami ... 24

Fig. 3.2 Absorption and emission spectra of Ti:sapphire ... 25

Fig. 3.3 The mode-locking principle in Tsunami ... 25

Fig. 3.4 Picture of Ti:sapphire regenerative amplifier system, Spitfire Pro ... 25

Fig. 3.5 The schematic illustration of CPA principle ... 26

Fig. 3.6 Laser light source and microscopic system for crystallization ... 27

Fig. 3.7 Picture of inverted microscope and other attachments ... 27

Fig. 3.8 Reflectance spectrum of the dichroic mirror used in the inverted microscope ... 27

Fig. 3.9 Transmittance spectrum of the objective lens used in the inverted microscope ... 28

Fig. 3.10 Illustration of the du Noüy ring method ... 30

Fig. 3.11 Illustration of the capillary method ... 30

Fig. 3.12 Picture of 1.5 ml glass bottle with 0.5 ml glycine solution inside ... 32

Fig. 3.13 Picture of crystallization plate ... 34

Chapter 4 Glycine Crystallization Fig. 4.1 The chemical structure of glycine ... 35

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Fig. 4.2 The shapes of (a) -polymorph and (b) -polymorph glycine crystals ... 36 Fig. 4.3 Pulse energy (J/pulse) dependence on glycine crystallization probability (%). ... 38 Fig. 4.4 The CCD image of cavitation bubble generation ... 39 Fig. 4.5 (a) Crystallization probability (%) and crystal morphology dependence on repetition rate (Hz). (b) Images obtained from CCD camera. (c) Picture taken by general camera. ... 40 Fig. 4.6 The crystallization probability (%) depending on the repetition rate (Hz) at the air/solution interface or glass/solution interface. ... 42 Fig. 4.7 The crystallization probability (%) depending on the distance from the air/solution interface (mm). ... 42 Fig. 4.8 The crystallization probability (%) depending on the repetition rate (Hz) at 3.0 M, 3.5 M and 4.0M ... 43 Fig. 4.9 The crystals obtained with different exposure times... 45 Fig. 4.10 (a) Raman image of obtained multiple crystals (b) Raman spectrum of obtained glycine crystal ... 46 Fig. 4.11 Mass spectra of standard sample and laser-induced crystal ... 47 Fig. 4.12 Glycine molecules in one unit cell. (Single crystal case) ... 49 Fig. 4.13 Illustration to explain the morphology difference because of the different repetition rates ... 50

Chapter 5 Application to Protein

Fig. 5.1 Three-dimensional conformation of hen egg white lysozyme (HEWL) ... 55 Fig. 5.2 The lysozyme crystal shape ... 55 Fig. 5.3 Crystallization probabilities and crystal images of lysozyme under spontaneous crystallization, irradiation inside the solution and irradiation at the air/solution interface (NaCl conc.: 10 mg/ml) ... 57 Fig. 5.4 Crystallization probabilities of lysozyme under spontaneous crystallization,

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irradiation inside the solution and irradiation at the air/solution interface (NaCl conc.: 10, 20,

30 mg/ml) ... 58

Fig. 5.5 The reconstructed lysozyme molecular structures from the X-ray analysis data under different laser conditions (NaCl conc.: 10 mg/ml) ... 64

Fig. 5.6 Electron density distribution of one of -helices under different laser conditions (NaCl conc.: 10 mg/ml)... 64

Fig. 5.7 Electron density distribution of one of disulfide bonds under different laser conditions (NaCl conc.: 10 mg/ml)... 64

Fig. 5.8 Lysozyme concentration (mg/ml) dependence on surface tension ... 65

Fig. 5.9 NaCl concentration (mg/ml) dependence on surface tension ... 65

Fig. 5.10 Conformation changes of protein take place at interfaces... 66

Fig. 5.11 Salting out can keep lysozyme molecules refolding and can localize them even at the air/solution interface ... 67

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List of Tables

Chapter 4 Glycine Crystallization

Table 4.1 The lattice constants and R-factors of glycine crystals with different morphologies…...………...49

Chapter 5 Application to Protein

Table 5.1 The lattice constants of lysozyme crystals under various experimental conditions………..………63

1

Chapter 1 Introduction

Laser light is regarded as a monochromatic light source showing high energy density

with high degree of spatial and temporal coherence. Laser beam can be focused to a very tiny

spot, and can be delivered at a large distance with extremely low divergence [1]. Therefore,

laser exhibits high potential and has been applied widely in diverse fields inclusive of physics,

chemistry, material science and so on. Undoubtedly, laser also plays an essential role in

various contemporary and interdisciplinary studies.

As one of laser applications, photoetching, an essential technique for microfabrications,

was first demonstrated when a pulsed ultraviolet excimer laser light with high enough

intensity was irradiated at a surface of organic polymer film and some morphological changes

were induced [2, 3]. Laser ablation was given to describe this phenomenon induced by pulse

laser irradiation at a solid material with intensity higher than a threshold [4]. If laser ablation

takes place in liquid or gaseous phase, the phenomenon is usually described as optical

breakdown. In fact, optical breakdown can be generated in water when focused femtosecond

laser pulses with high intensity are irradiated inside water [5]. The accompanying phase

2

transition of water from liquid to gas gives transient mechanical stress. The optical breakdown

has been employed for biological applications such as cellular surgery [6, 7], and the

consequent mechanical stress is applied to cellular arrangement or micropatterning [8] and

nanoparticle injection to single cells [9]. Nowadays, the application of optical breakdown has

been expanding to the studies on crystallization and crystal growth and has received much

attention [10-13].

Crystal is a solid material composed of atoms, molecules or even macromolecules which

are three-dimensionally arranged in a long-range order, and crystallization is the process from

atoms or molecules to a crystal. Making crystal is not only an important technique for

purification and separation, but also an indispensable process in determining crystal structures

both of inorganic solid-state materials and biological molecular crystals at atomic resolution

with X-ray diffraction analysis [14].

Among the biological macromolecules inclusive of proteins, nucleic acids and

carbohydrates, proteins constitute the largest group. Enzymes are the most diverse class of

proteins because nearly every chemical reaction in a cell requires a specific enzyme. In order

to understand cellular processes or design new structure-based drugs or pharmacological

agents, knowledge of the three-dimensional structure, functions and properties of enzymes

3

and other macromolecules are undoubtedly vital [15, 16]. X-ray diffraction of crystals and

nuclear magnetic resonance (NMR) are two widely-used techniques for the structural

determination of macromolecules at atomic resolution. While NMR does not require protein

crystals and provides more detailed information on the dynamics of the molecule in question,

it can be used only for biopolymers with molecular weight of less than 30,000. X-ray

crystallography can be applied to compound with molecular weight up to at least 106. For

many proteins, the difference is decisive in favor of X-ray diffraction [15]. Accordingly, a

major challenge to the full exploitation of X-ray diffraction technique is that the protein must

first be crystallized [16].

Protein crystallization is mainly a trial-and-error procedure in which protein is slowly

precipitated from its solution, so obtaining suitable single crystals is the least understood step

in the X-ray structural analysis of a protein [15]. As a matter of fact, there are still some

additional requirements for the crystallinity and size of the crystals if precise analysis results

are more likely to be obtained [17]. Moreover, since crystallization is a rate-limiting step from

single molecules to a crystal for some proteins such as membrane proteins which can be

attributed to inherent protein flexibility and to conformational inhomogeneity, it is also

necessary to shorten the crystallization time and elevate the crystallization possibility

simultaneously [18]. Therefore, laser-induced crystallization methods as novel crystallization

4

techniques have received much attention and have been proposed continually to try to satisfy

the present situation.

1.1 Introduction to conventional crystallization methods

Because amino acids are polar molecules, most of them can be dissolved well in water

rather than organic solvent. Accordingly, water is often used as solvent in crystallization. In an

aqueous solution at pH near isoelectric point, amino acids are in zwitterionic form, and their

zwitterionic property is still kept in crystal. For crystallization, general methods such as

cooling down saturated solution slowly, evaporating saturated solution slowly with adding

polar solvent such as alcohol, adding poor solvent into saturated solution, and adjusting pH to

lower the solubility of the solution are often used. If crystals with high quality are more likely

to be obtained, slow crystal growth at low supersaturated degree is preferred [14].

The history of protein crystal growth can be traced back about more than 150 years ago.

The first observed protein crystallization was published by Hünefeld in 1840, and the protein

was hemoglobin from earthworm. The crystals were obtained when the blood of an

earthworm was pressed between two slides of glass and allowed to dry very slowly. The

above description revealed that protein crystals can be obtained by controlling evaporation of

a concentrated protein solution. In other words, protein crystals can be produced by slow

5

dehydration which is one of the most acceptable concepts until now. Other conventional

methods such as temperature variation under otherwise constant conditions, the use of salt or

organic solvents as precipitating or crystallizating agents, and the use of metal ions were also

developed in the following decades [19].

The oldest crystallization technique is batch method which has been used for proteins

and nucleic acids crystallization for over 150 years and is regarded as one of the most reliable

crystallization methods. Batch method is attractive and convenient because of its inherent

simplicity and reproducibility. It requires nothing more than direct mixing of an unsaturated

protein solution with a precipitant solution and waiting for a period of time until spontaneous

nucleation commences. For instance, lysozyme, the most widely studied protein for protein

crystallization, is easily crystallized by batch method [19].

The most commonly used technique for protein crystallization is vapor diffusion

inclusive of hanging drop and sitting drop methods. Both of these two methods contain

sample solution and reservoir solution, and require a closed environment. At the early stage,

the sample solution has insufficient precipitate concentration for crystallization. After vapor

diffusion of solvent from sample solution to reservoir solution takes place and vice versa, the

precipitate concentration is slowly adjusted to an optimal degree for crystallization since the

6

Fig. 1.2 Schematic illustration of crystal formation from a disordered medium to a highly ordered phase [20].

amounts of solution are quite different between these two [14].

1.2 Introduction to crystallization process

Fig. 1.2 shows a schematic illustration of crystal formation from a disordered medium.

Compared with the final crystal phase, the initial disordered phase has higher free energy.

Crystallization starts from nucleation, in which a tiny embryo of a highly ordered phase with

lower free energy is formed. Nucleation seldom takes place spontaneously at unsaturated

concentration since it is relatively difficult for molecules to overcome some energy barriers

between these two phases. However, at high enough supersaturation, the energy barriers

decrease and the initial state becomes unstable, so that a tiny fluctuation can lead to the Fig. 1.1 Vapor diffusion for protein crystallization. (a) hanging drop

method (b) sitting drop method

(a) (b)

7

appearance of the new phase [20].

An illustration of phase separation during nucleation in detail is shown in Fig. 1.3. There

are two possible pathways from individual molecules to nucleation. When the size of

molecule accumulation increases to a critical size, the ordered nucleus forms and starts to

form crystal. On the other hand, dense liquid droplet or liquid-liquid phase separation

formation can be observed if the size of molecule accumulation continuously increases [20].

Fig. 1.3 Schematic illustration of the formation of ordered crystalline nuclei as a result of the superposition of a density and a structure fluctuations [20].

8

1.3 Light-induced crystallization

Light-induced crystallization can be realized with various light sources through different

mechanisms such as photochemical and nonphotochemical (or photophysical) processes. The

used light source can be Xe lamp, continuous wave laser or pulse laser at different

wavelengths ranged from UV region to NIR region.

1.3.1 Photochemical reaction-induced nucleation

Okutsu et al. have reported photochemical reaction-induced nucleation of anthracene

[21], hen egg-white lysozyme (HEWL) [22], thaumatin [23], and ribonuclease A (RNaseA)

[24]. In the lysozyme crystallization experiment, they exposed UV light (wavelength; 280,

300 and 400 nm) from Xe short arc lamp (wavelength; 200-800 nm, USHIO UXL-300D) to

Fig. 1.4 (a) Mechanism of the photochemically induced nucleation of lysozyme (b) enhancement of protein crystallization by a photochemical reaction [22].

9

supersaturated but metastable lysozyme solution and produced photochemical intermediate

(Fig. 1.4). Since the photoproduct has lower solubility in mother solution, it works as a

nucleus and triggers crystallization eventually [22]. Okutsu et al. gave a representative

demonstration of photochemical reaction-induced nucleation. However, it is not known for

sure how radical formation affects the purity of the obtained protein crystal.

1.3.2 Kerr effect-induced nucleation

Garetz et al. discovered that intense nanosecond NIR laser pulses (pulse duration; 20 ns,

repetition rate; 10 Hz, wavelength; 1.06 m) can induce nucleation of urea solution in 1996.

This phenomenon was named as nonphotochemical laser-induced nucleation (NPLIN).

Because it was observed that the initially forming needle-shaped crystals tend to be aligned

parallel to the electric field vector of the light, they proposed that the electric field-induced

realignment of urea molecules results in cluster formation and this mechanism is known as the

optical Kerr effect [25]. Nucleation of glycine [26] was also demonstrated, and the polymorph

of glycine was controlled by changing polarization of laser beam [27] or by additionally

applying strong DC electric field to enhance the optical Kerr effect [28].

10

1.3.3 Laser trapping crystallization

Continuous wave (CW) laser-induced crystallization has been developed very fast

recently. Fig. 1.5 shows the principle of laser trapping. When a highly focused laser beam

passes through sphere-like medium with a greater refractive index from surrounding, the

sphere-like medium acts like a weak positive lens and it will be moved toward the focal point

by a substantial net backward trapping force [29]. In laser trapping crystallization, tightly

focused CW NIR laser beam is employed to gather molecules or clusters, forming a high

concentration area at the focal spot, where the nucleation is eventually achieved. Since laser

trapping is actually a dynamic process against diffusion of trapped molecules or clusters from

the focal spot, in order to reach stable laser trapping condition, laser irradiation at a certain

point for a period of time is necessary. Therefore, selecting laser wavelength at which both of

solvent and solute have merely no absorption is quite important. Photons at NIR wavelength

Fig. 1.5 Diagram showing the ray optics of a spherical Mie particle trapped in water by the highly convergent light of a single-beam gradient force trap [29].

11

have lower energy and can be less absorbed by biological molecules or systems. However,

water as a common solvent is not applicable since it has vibrational absorption over 1000 nm

[30]. The absorption of water generates a serious problem in temperature elevation which

increases the solubility of solution, and crystallization becomes more difficult. In order to

solve this problem, it is necessary to replace water with deuterated water (heavy water) as

solvent in this crystallization method.

Sugiyama et al. has firstly demonstrated crystallization of glycine by an intense focused

CW-YVO4 laser beam (wavelength; 1064 nm) at the air/solution interface. It was observable

by a CCD camera that the glycine crystal grew from focus to a certain size within a few

seconds [31]. Furthermore, Rungsimanon et al. have investigated the method to control

glycine phase by tuning laser power. It was found that the competing result between photon

pressure and temperature elevation at a certain high laser power led to the probability increase

to find -polymorph glycine crystal, which is not available under ambient conditions [32]. On

the other hand, Yuyama et al. have demonstrated the preparation of a millimeter-scale dense

liquid droplet of glycine induced by laser trapping effect. After focusing a CW NIR laser

beam at the glass/solution interface of a thin film of its supersaturated heavy water solution

and forming the droplet, they found that crystallization starts immediately just after the focal

position is shifted to the air/solution interface. It is considered that the droplet formation is

12

possibly the early stage of the multistep crystallization process and plays an important role in

photon pressure-induced crystallization of glycine [33].

1.3.4 Molecular assembling induced by optical trapping

Tsuboi et al. reported that the aggregation of lysozyme as nucleus induced by optical

trapping in solution can trigger nucleation [34]. They also observed the assembling of amino

acids (glycine, proline, serine and alanine) induced by laser trapping in solution, and

considered that the observed glycine assembling may be experimentally verified as a

precursor for the crystal nucleus by Sugiyama et al. [35]. The differences between inducing

molecular aggregation as nucleus and forming a local high concentration area by trapping

laser are the focal position and the necessary time for observation. Molecular assembling is

induced in solution and takes several hours for observation, whereas laser trapping

crystallization can only be achieved at the air/solution interface and the crystal grows within

several seconds.

1.3.5 Femtosecond laser-induced crystallization

Femtosecond laser-induced crystallization of HEWL was firstly demonstrated in 2003 by

Hosokawa et al. [10]. Besides, urea [12], DAST (4-(dimethylamino)-N-methyl-4-stilbazolium

13

tosylate) [11], anthracene [13] and glucose isomerase (GI) [36] crystallizations were also

reported in following years. The mechanism will be introduced in detail in Chapter 2.

1.4 Motivation

In this work, we have focused on femtosecond laser-induced crystallization and tried to

clarify how laser parameters inclusive of pulse energy, repetition rate, focal position and

exposure time affect the crystallization probability, crystal morphology and crystalline phase.

Firstly, we demonstrated glycine crystallization since glycine crystal shows several

polymorphs and is well-studied in the field of crystal chemistry [14]. Then we applied our

obtained results to lysozyme crystallization since lysozyme is also a representative protein in

protein crystallography [19]. It is expected to sharpen present crystallization techniques with

optimizing laser parameters and simultaneously establish a remarkable milestone to study

molecular dynamics of femtosecond laser-induced crystallization under appropriate

conditions.

14

Chapter 2 Principle

The mechanism of femtosecond laser-induced crystallization is completely different

from other methods because only this technique triggers nucleation by multiphoton absorption

of solvent leading to optical breakdown and is less related with solute. Firstly, principle of

multiphoton absorption is explained with its schematic illustration in Fig. 2.1. Since the

energy of a single photon is not enough to excite a molecule from the ground state to a higher

electronic state, the molecule can be excited only by absorbing more than one photons

simultaneously and the energy difference between the two states is equal to the sum of the

energy of the photons. Figure 2.2 reveals that water has much higher absorption in UV region

due to electronic transition than in visible and NIR region due to vibrational overtone

absorption [37], so it supports that water molecule are excited by photons at 800 nm through

multiphoton absorption.

By focusing intense laser into water, multiphoton absorption of water occurs, and leads

to optical breakdown of water giving vigorous evaporation if the superheated condition is

satisfied. When the rate of volumetric energy deposition provided by laser irradiation is more

15

rapid than the rate of energy consumed by vaporization and normal boiling, the liquid water is

driven to a metastable superheated state. The liquid can remain metastable until the spinodal

temperature is reached. By viewing a plot of the Gibbs free energy versus specific volume at

ambient pressure as shown in Fig. 2.3, unique features of the spinodal temperature can be

appreciated. At the spinodal temperature, the equilibrium between saturated liquid state and

saturated vapor state becomes extremely unstable, so the liquid undergoes spinodal

decomposition, a spontaneous process by which a thermodynamically unstable liquid relaxes

decomposition, a spontaneous process by which a thermodynamically unstable liquid relaxes

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