Teratogenic Effects of Topiramate in a Zebra fish Model

 

Abstract

Topiramate is commonly used for treating epilepsy in both children and adults. Recent clinical data suggests that administration of topiramate to women during pregnancy increases the risk of oral clefts in their offspring. To better understand the effects of topiramate, an adult female zebrafish was dosed with topiramate, and the altered morphologies were investigated in the adult females and their off springs. It showed that topiramate-treated female fish had reduced oocyte maturation, and the survival rates of their offspring were seriously decreased during embryogenesis, in addition to cartilage malformation in some offsprings. Therefore, topiramate causes both impairment of mother oogenesis, and bone dysplasia.

Introduction

Topiramate is used for treatment of migraine prophylaxis and Lennox-Gustuat syndrome. Topiramate is derived from naturally occurring D-fructose, and have great effect in blocking the spread of seizures. It is classified as Pregnancy Category D according to the FDA drug grading that indicates positive evidence of human fetal risk. According to some studies, the exposure of topiramate during the first trimester of pregnancy, leads to an increase in the oral cleft rate in infants. However, variation in the given doses, changes the result in both the mother and the offsprings. Moreover, zebrafish was used as an animal model, since that it embryos are easily collected, they have rapid development, and they have genetic similarity to humans. In this study, it is noticed that after treatment with topiramate, the reproductive ability of the mother was decreased, and there is a connection between the maternal passages of the topiramate effect in offspring.

Materials and Methods

1- Zebrafish maintenance:

 first, maintain AB zebrafish stain under 14 h on/10 h off light cycle. Then collect embryos and culture them in petri dishes containing E3 water (5.0mM NaCl,0.17mM KCl,0.33mM CaCl2 and 0.33mM MgSO4) at 28 C, finally, add 1-phenyl 2 –thiourea during embryogenesis to inhibit pigment formation.

2- Topiramate treatment

Choose adult female fish (4 months old) that had reached sexual maturity to undergo the topiramate containing diet.Mate the females with males to completely ovulate eggs from their ovaries to begin new cycle of oogenesis. Now start the dosage process by feeding fish 0.5 mg/g/day of topiramate- blended dry food once per day for 7 days. At the end of the final day, breeding environment is set up, then collect embryos in the following day morning.

 


Figure 1. Experimental design scheme of topiramate treatment in Zebrafish

 

3- Preparation and Staining of Paraffin Section

Fix the whole ovarian tissues in 4% Paraformaldehyde. Then, rinse them in running water. On a microtome section the paraffin embedded blocks at a thickness of 5 µm. Deparaffinize the slides in 55 C water bath for 10 minutes. After that immerse them in xylene two times for 10 minutes and in ethanol in different concentrations for 5 minutes to rehydrate the tissues, finally, rinse them in distilled water before staining.

4- Hematoxylin and Eosin Staining

Stain the previous slides in hematoxylin for 3-5 minutes, and wash them in running water until sections turn blue. Stain them in 1% eosin Y for 10 minutes, then dehydrate the slides in 80%, 90%, 100% ethanol for 20 seconds each, then observe them under the microscope.

5- Tissue staining

Rinse the Paraformaldehyde-fixed embryos with 70% ethanol. Stain them with alcian blue solution, then rehydrate them with ethanol/H2O series (80%, 50%, 20%, and 0% ethanol). After that, rinse them with phosphate-buffered saline (PBS) for 15 min. Then, rinse them with trypsin. Remove excessive dye with 1% KOH/3% H2O2 (v/v) until conformation of cartilage was fully observed.

Note: For vertebrate skeletal observation, alizarin red staining was performed. Using the same fixation procedure as described above, specimens were stained with 0.1 mg/mL alizarin red in 0.5% (w/w) KOH at room temperature and distained with methanol.

6- Microinjection

First, inject topiramate into the embryo during 1-to 4 cell stage. Second, Inject 0.5, 1. 2 ng of topiramate between the boarder of the cell and the yolk of the embryo. Third, raise the injected embryos and analyze them.

Results

1- Topiramate Showed No Effect on Weight of Experimental Female Fish.

For the experimental group:

Its average weight was 0.88g (range0.7–1.1g) at the beginning of the experiment which increased to 0.96g (range 0.9–1.1 g) after treatment.

For the control group:

Its average weight was also 0.88(range 0.7-1.1g) at the beginning of the experiment which increased to 1.05 (range 1.0–1.1 g).

The experimental group weight increased 0.08g, while the control group weight increased 0.2 g.

Therefore, there is no significant statistical difference when comparing the weight of the two groups.

2- Topiramate Impairs the Maturation of Oogenesis

For the control group:

A large portion of ovarian tissue was filled with mature oocytes.

For the experimental group:

There is a significant decrease in the % of mature oocytes at both stages primary growth (I) and cortical alveolus (II), only 40 % of the female fish were able to lay eggs.

This means that the uptake of topiramate in female fish affects oogenesis and suggested that it may lead to abnormal embryogenesis in offspring.

 








3-Effect of Topiramate on Cartilage Development in Offspring

Compared to the control group, the experimental group showed a lack or shortage of cranial and pharyngeal development.In the experimental group, the ventral view showed a transformation in Meckel`s cartilage, ceratohyal, and ethmoid plate.The lateral view showed that the ceratobranchial was severely underdeveloped.Even that different individuals causes divergent degrees of drug response, it is observed a similar under-developed status in the craniofacial cartilage region in diverse topiramte- treated offspring, and some of them have complete cartilage development.Along the offspring's, only 23% showed cartilage abnormality.

Thus, it is suggested that topiramate had a serious impact on cartilage development; teratogenic factors were indeed passed from mother to offspring.



4- Craniofacial Malformations on Topiramate-Treated Offspring

Topiramate-treated mother fish showed the following, significantly decreased L/W within the craniofacial region. Ossification reduction in the post-cranial axial skeleton. Impaired ossification in the regions of ceratohyal and Meckel’s cartilage.Decreased number of spinal columns from 13.2 to 6.2 was shown in the treated offspring.

So, not only cartilage development, but also bone formation was impaired by topiramate treatment.

5- Topiramate Affects Epiboly Progression of Offspring Fish

Embryos from topiramate- treated fish showed a lower survival rate than usual.An average of 16.3 ± 15.6% of early developmental malfunction, including aberrant epiboly migration at the 5.3 hpf stage, and failure to differentiate was detected at 8 hpf embryos. The embryo was able to initiate epiboly progress with blastoderm formed, but the enveloping layer of cells failed to migrate to the vegetal pole and accumulated at the animal pole, forming a bubble like shape. The blastoderm was unable to cover the yolk cell and halted before 50% coverage.As we increase topiramate dosage, we observe that the survival rate decreases.

Therefore, topiramate is transmittal, it causes epiboly deficiency.



 
















Discussion

The reduction of weight and skeletal development were observed side effects of topiramate with maternal toxicity. To know the topiramate effect direct injection into embryos was done, the dosages was calculated based on the assumption of absorption per clutch of eggs from topiramate-treated mother fish. Precise calculation was ensured so as not to overdose the fish and cause artificial toxicity and lead to experimental bias. Therefore, based on this assumption, the teratogenic effects are due to topiramate treatment.It is possible that infertility occurs in women who have epilepsy and this may be due to the side effects of antiepileptic medication.The fertility rate in women with epilepsy has been reported to be lower compared with their nonepileptic female siblings. In fact, only 40% of maternal fish were fertile in our study.Craniofacial abnormality is one of the most common congenital birth defects, which affects the development of the head, face, and neck. Thus In this study,the ratio of zebrafish with cartilage malformation was about 23%, which is much higher than shown in a clinical study on humans.

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