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Metformin inhibits human spermatozoa motility and signalling pathways mediated by protein kinase A and

The association and dissociation of a fluorescent ligand was visualised and

quantified at the single-cell level using a perfusion system as described by

LSM710 confocal microscope. A pressure pump was connected to a closed

perfusion system, which allowed the constant perfusion of fluid from six

reservoirs through an imaging chamber and into a runoff (Figure 2.4). Cells

were grown to near confluence on 32 mm glass coverslips placed into wells of

6-well plates (see Cell culture) one day prior to experimentation. Where

transient transfection of cells with BiFC DNA constructs was required, the cells

were plated out three days prior to experimentation and then prepared as

described above (see Confocal microscopy). On the day of the experiment, the

growth medium was removed from one 6-well plate and the wells were

washed once in pre-warmed (37 °C) imaging buffer (HBSS containing 4.5 mM

D-glucose) and subsequently kept in 2 mL imaging buffer at 37 °C until used

for experimentation (the cells were kept in these conditions for no longer

than 2 hours). To start experimentation, the coverslip was placed into a

specially designed imaging chamber, which was tightly closed and then placed

onto a heated (37 °C) microscope stage where it was connected to tubes on

either side that facilitated the flow of fluid through the imaging chamber.

Following this, the reservoir supplying the imaging buffer was switched on to

perfuse over the cells in a laminar flow imaging chamber that holds a total

L

L M et al., 2010a). Following this, an area of cells was selected using the eyepiece of the microscope and the required laser, emission filters

and time series mode were set up. BODIPY-TMR-CGP was excited using a 543

nm Helium-Neon laser on the Zeiss LSM510 microscope and a 561 nm Helium-

Figure 2.4 The set-up of the closed perfusion system in conjunction with the Zeiss LSM510 confocal microscope. The pump allows the flow of fluid at constant pressure from a reservoir through the imaging chamber (imaging cell) and into a runoff. The entire system is temperature-controlled and kept at 37 °C. Figure taken from May et

560 and 565 nm long-pass filter, respectively; BODIPY630/650-S-PEG8-

propranolol was excited using a 633 nm argon laser and a 650 nm long-pass

filter at both confocal microscopes. Where cells transiently transfected with

BiFC DNA constructs were used, YFP and BODIPY-TMR-CGP were excited using

a 488 nm argon laser and 561 nm Helium-Neon laser, respectively with

emission being captured through a 505-550 nm narrow band-pass and a 565

nm long band-pass filter, respectively (these experiments were carried out

using the Zeiss LSM710 confocal microscope).

Association and dissociation kinetic binding experiments

The association and dissociation kinetics of increasing concentrations (3-100

nM) of BODIPY-TMR-CGP and BODIPY630/650-S-PEG8-propranolol were

investigated. Both fluorescent ligands used in perfusion experiments were

diluted in ddH2O to working concentrations (100x desired final concentrations)

and subsequently kept on ice. When used, 400 µL of the ligand (at working

concentration) was added to 40 mL imaging buffer in a designated reservoir.

First, a 20-30 second baseline fluorescence read was taken in the presence of

only imaging buffer. To initiate association of the fluorescent ligand, the flow

of fluid from the reservoir containing imaging buffer (reservoir 1) was stopped

and the reservoir containing the fluorescent ligand (reservoir 2) was switched

on for a given length of time (e.g. 5 minutes). After that, flow of fluid from

reservoir 2 was stopped and reservoir 1 was again switched on to begin

dissociation of the fluorescent ligand (generally performed for the same

remove the labelled ligand, which is possible due a sharp change in

concentration caused by the selected pressure and flow rate for these

experiments (May et al., 2010a). Throughout the experiment (from baseline

to dissociation read) transmitted light and fluorescence images were captured

every 2-3 seconds (512x512 pixels, 2 averages per images). The first glass

coverslip (slide) was used to establish the optimal microscope settings (laser

power, gain and offset) as described above in Confocal microscopy. These

settings were then kept constant within each experiment and between

CHO 1-CS (used to

measure total binding) and CHO-CS cells (used to measure non-specific

binding levels) to allow for direct comparison of total and non-specific

fluorescent ligand binding levels at the different concentrations tested.

Dissociation kinetic binding experiments in the presence of

unlabelled ligands

All unlabelled ligands were diluted in ddH2O to working concentrations

(10,000x desired final concentration) and 4 µL of the ligand at working

concentration was added to 40 mL imaging buffer in designated reservoir

(reservoir 3). The association of the fluorescent ligand was achieved as

outlined above. Following association, the flow of fluid from reservoir 2

(imaging buffer containing the fluorescent ligand; as defined above) was

stopped and reservoir 3 was switched on, thus initiating the dissociation of

the fluorescent ligand in the presence of an unlabelled ligand (for a given

any unlabelled ligand were performed on each experimental day. Transmitted

light and fluorescence images were captured every 2-3 seconds and the

microscope settings were set using the first slide (as described above) and

then kept constant within each experiment, but adjusted, if necessary,

between experiments on different days. Dissociation kinetic data was

therefore expressed in % fluorescent intensity, allowing experimental data

from different days to be grouped.

Data collection

During each experiment, 8bit images recording the fluorescence intensity of

the fluorescent ligand binding to cells in the perfusion imaging chamber were

captured. To analyse and quantify the association and dissociation kinetics of

the fluorescent ligands, regions of interest (ROIs) were drawn around the

membranes of ten single cells of each imaged slide. Cells containing

oversaturated pixels were identified using the range palette and were

excluded from the analysis. For cells with low fluorescent intensity, the

transmitted light image was used to aid cell selection. The Zeiss software then

provided average pixel intensity values for each ROI (10 ROIs per slide), which

were plotted against time. The changes in fluorescent intensity over time

were then analysed to obtain association and dissociation rates (see Data

analysis) for either each single cell or per slide (i.e. grouped data from 10

single cells). For kinetic data shown in this thesis, an n number of 1 refers to

data obtained from one slide. Within each experiment, each condition (e.g.

Throughout this thesis, the number of different experimental days, in which

the n numbers were acquired, is also stated.