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Issue 1, June 2001

Biological & Biomedical Sciences
A Review of the Progression of Transgenic Plants Used to Produce Plantibodies For Human Usage

Elisa Ferrante and David Simpson
University of Virginia
Advisor: Timothy C. Scott, Ph.D.
University of Virginia

Abstract

Antibody production in plants has acquired significance as an emerging system for the production of many recombinant proteins, particularly including those intended for therapeutic purposes. The use of transgenic plants would not have been possible without important advances in genetics and medical engineering fields. Such advances include the sequencing of DNA, the discovery of restriction enzymes and various evolving techniques of molecular biology. These developments, combined with the recognition that plants can be used as a human antibody production system, have stimulated much research and discoveries. This article presents a general review on the subject, discussing successful accomplishments in research during the past years, the several applications of plant-produced substances and the advantages and disadvantages of these methods of production. Comments on methods of suppression and past and current research are also included, with emphasis on the use of plantibodies in oral vaccines for medical purposes.

Introduction

There was a time not too long ago when most medicinal compounds came from plants: the potent heart stimulant digitalis from foxglove, for example, and opium from poppy plant. But beginning about 50 years ago, chemistry took over from botany, with most new drugs being artificially produced in pharmaceutical labs (Moffat, 1995). Nowadays, one of the most promising methods of producing proteins and other medicinal substances, such as antibodies and vaccines, is the use of transgenic plants.

A transgenic plant contains a gene or genes that has been artificially inserted. The inserted gene sequence, known as the transgene, may come from an unrelated plant, or from a completely different species. One of the purposes of inserting a combination of genes in a plant is to make it as useful and productive as possible. This process provides advantages such as higher yield, improved quality, pest or disease resistance, and tolerance to heat, cold and drought. However, transgenic plants can also be produced in such a way that they express foreign proteins with industrial or pharmaceutical value (see Tables 1 and 2). Transgenic plants represent an economical alternative to fermentation-based production systems. Plant-made vaccines or antibodies (plantibodies) are especially striking, as plants are free of human diseases, thus reducing screening costs for viruses and bacterial toxins (Herbers et al. 1999).

The first transgenic plants were reported in 1983. Since then, many recombinant proteins have been expressed in several important agronomic species of plants including tobacco, corn, tomato, potato, banana, alfalfa and canola (Hammond et al. 1999). The choice of plant system was initially driven by convenience and the need to evaluate genetic constructs quickly. For this reason, tobacco plants were generally used, however, potatoes and bananas were considered for the purpose of acquiring a delivery system of vaccines for humans.

Foreign gene expression in plants can be accomplished either by stable integration of foreign DNA, which results in transformation of the nuclear genome, or by transient expression using modified plant viruses (Figure 1). Stable genomic integration is accomplished by introducing foreign DNA in the plant either by Agro bacterium T-DNA vectors or by direct means. The integration method has the advantage of permitting large scale cloning, maintenance of selected high-expressing genes and the ability to sexually cross transgenes to obtain multiple proteins expressed in the same plant (Tacket et al. 1998). On the other hand, transient expression using viral vectors is harder to initiate, because the viral vector must be inoculated into individual host plants, but gives a greater yield of protein.

Advantages and Disadvantages

Recombinant protein production using transgenic plants as bioreactors is likely to be more economical than alternative systems, especially for large-scale needs. Factors in favor of plant systems as sources of animal derived proteins, compared with other conventional methods, include:

  • The potential for large-scale, low-cost biomass production using agriculture.
  • Low risk of product contamination by mammalian viruses, blood-borne pathogens, oncogenes and bacterial toxins.
  • The capacity of plant cells to correctly fold and assemble, not only antibody fragments and single chain peptides, but also full-length multimeric proteins.
  • Low downstream processing requirements for proteins administered orally.
  • Elimination of the purification requirement when the plant containing the recombinant proteins is edible, such as potatoes.
  • The ability to introduce new or multiple transgenes by sexual crossing of plants.
  • The avoidance of ethical problems associated with transgenic animals.
  • Formulated in seeds, plant-made enzymes have been found to be an extremely convenient method for reducing storage and shipping costs, for an indefinite amount of time, under ambient conditions.
  • Production size is flexible and easily adjustable to the needs of changing markets.
Plants are also capable of synthesizing and assembling virtually any kind of antibody molecule, ranging from the smallest antigen-binding domains and fragments, to full length, and even multimeric antibodies.

There are, however, potential issues of concern for plant protein production:
  • Allergic reactions to plant protein glycans and other plant antigens.
  • Plant and product contamination by mycotoxins, pesticides, herbicides and endogenous metabolites.
  • Regulatory uncertainty, particularly for proteins requiring approval for human drug use (Doran 1999).
 

Applications


The production of foreign proteins in plants has become an attractive alternative to conventional production systems for pharmaceutical polypeptides. Potential proteins produced by this method include cytokines, hormones, enzymes, epidermal growth factors, interferons, human protein C, and pharmaceutical foodstuff considered for oral immunization.

The capacity of plants to produce different classes of proteins with pharmaceutical value and the need for new technology for the production and delivery of inexpensive vaccines has led to the use of transgenic plants (see Table 1). In addition, large amounts of antibodies can be produced at relatively low cost, using agriculture instead of sophisticated and expensive cell culture-based expression systems. Oral vaccines, as opposed to parenteral vaccines, offer the hope of more convenient immunization strategies and more practical means for implementing universal vaccination programs throughout the world.

The pathogens responsible for the greatest burden of human disease make initial contact with the human host at mucosal sites in the respiratory tract, gastrointestinal tract or genital tract. Therefore, stimulation of immune responses of suitable strength and quality to protect against illness is particularly desirable at these sites (Tacket et al. 1999).

The best way of achieving mucosal immunization is to apply the vaccine directly to the mucosal surface, inducing systemic and cellular immune responses as well as local immune responses. Mucosal vaccines have been sought because of the potential for stronger immune responses directed at the initial site of interaction between the pathogen and host. Many infectious agents colonize or invade epithelial membranes. These include bacteria and viruses that are transmitted in contaminated food, water or by sexual contact. Transgenic plants that express antigens in their edible tissue might be used as an inexpensive oral-vaccine production and delivery system (Mason et al. 1995). Therefore, immunization might be possible through consumption of an "edible vaccine" to provide passive immunization. Also, it may be possible to use genetically engineered plants and plant viruses to produce vaccines against several human diseases from tooth decay to life-threatening infections such as diphtheria, cholera and AIDS (Moffat, 1995).

Several issues will still have to be resolved before this intriguing idea can become a reality. Some of the proteins used in experiments may be extraordinarily potent inducers of immune responses. On the other hand, other immunizing proteins may not work as well when taken orally. In fact, they can have the opposite effect, because many proteins in a diet induce tolerance, making the immune system less able to mount a response against them. In addition, some other compounds in plants may compromise the ability of the vaccine protein to induce immunity. The food containing it must be palatable and some foods need to be heated before ingested, which could possibly cause the vaccine protein to denature, reducing or eliminating its ability to elicit immunity.

Oral vaccines, whether living or nonliving, must be protected during passage through the hostile environment of the stomach and intestine to the sites where immune stimulation occurs (Tacket et al. 1999). In recent years, a variety of delivery systems have been developed for presenting nonliving antigens to mucosal surfaces, which will allow these antigens to persist and survive in the hostile gastric and enteric environments. These include polylactide/polyglycolide, microspheres, liposomes, proteosomes, cochleates, virus-like particles, and immune-stimulating complexes.

One of the most promising methods, however, is the production of antigens in the plants themselves, which assemble into ordered structures such as virus-like particles. This gives the hope that they will be more resistant to digestion and more likely to reach the gut-associated lymphoid tissue.


Methods of Production

Conventional Method

Pharmaceutical and therapeutic antibodies synthesized in plants can be produced in a variety of ways. Conventional methods use stable transformation and transient expression to introduce new genes into a host cell. Once DNA from the transformant host cell is isolated and purified, it can be injected into the embryo of a maturing plant. The plant can then propagate in an open field allowing for large-scale production of antibodies. As mentioned before, however, purification of these proteins is generally long and tedious. Upon isolation of the antibody, several proteins, organic molecules, glycan and herbicides must also be isolated, leading to a complex purification process (Kusnadi et al. 1997).


In Vitro Cell Tissue Cultures

Plant tissue cultures offer an economically favorable method for producing antibodies from plants. Using this approach, plant cells in differentiated or dedifferentiated states are grown in a nutrient medium in bioreactors under controlled conditions, with foreign proteins harvested from either the biomass or culture liquid or a combination of both (Doran 1999).

This method of production of human antibodies is not suitable for the production of edible vaccines (simply because the antibody is produced in a cell culture and not in a fruit or vegetable) but offers many advantages to the conventional methods of extracting and purifying a protein from a live plant. First, plant tissue cultures offer larger amounts of proteins in shorter amounts of time (Doran 1999). This is because the bioreactors provide a much more controlled and reproducible environment than an open field.

The advantages of this method allow desired antibodies to be produced, purified, and transferred to the consumer in a minimal amount of time. Also, purification of the proteins becomes easier (Doran 1999). In vitro cell cultures contain fewer biological proteins or molecules (along with herbicides and pesticides) than open field plants or bacterial/yeast cell cultures, which may contaminate the product. Furthermore, plant cells and organs can propagate indefinitely in tissue cultures (Doran 1999). Therefore, sexual reproduction is not needed to ensure the lifespan of the species. Without sexual reproduction, transgene stability is increased because of the absence of crossing over, segregation and recombination involved in sexual reproduction.

Inducible promoters may offer a solution to the problems associated with open field production of plantibodies. They would allow for better efficiency in the production of plantibodies. They would also provide the plant with a more stable mode of translation, leading to transgene stability (Doran 1999).


Breeding and Sexual Crossing

In 1989, Hiatt was the first to use sexual crossing as a way to produce a functional protein in plants (Hiatt et al. 1989). In this experiment, transformation was used to introduce kappa-chains of either light or heavy regions into tobacco plants. The same was done with gamma-chains of either light or heavy regions (Whitelam et al. 1994). Upon crossing one plant with kappa-chains and another plant with gamma-chains, an antibody was produced that expressed both chains (Hiatt et al. 1989). This experiment provided an ingenious way to produce antibodies in plants without the need for a double transformation.


Transgenic seeds

As mentioned above, using green plant tissue as a bioreactor is a great method of producing antibodies. Also discussed are certain limitations to this process. Further restrictions are gathered when plants are used as a storage system. Plants cannot store antibodies for an extended period of time. This is because certain proteases degrade the protein piece by piece.

Ulrike Fieldler and Udo Conrad showed that seeds of transgenic tobacco could be used for high-level production and long-term storage of antibodies. In their experiments, functionally active single chain Fv (scFv) accumulated up to 0.67% of the total soluble seed protein. In addition, storage of ripe transgenic tobacco seeds for one year at room temperature showed no loss of scFv or its antigen-binding activity (Fieldler et al. 1995). Seeds contain a low level of proteases that allows proteins to be stored without degradation (Kusnadi et al. 1997). This experiment suggests that seeds can be used as bioreactors and as natural storage organs.


Targeting and Compartmentalizing

In some cases, antibodies can be tagged with a small peptide sequence. This peptide sequence allows plant cells to direct an antibody or protein to specific organelles and compartments after processing. Compartmentalizing to easily isolated organelles provides a less complicated purification procedure (Kusnadi et al. 1997). Targeting also allows antibodies to be protected from proteases that exist in the cytoplasm of cells. Targeting, however, has to be specifically controlled. This involves proper cleavage of the targeting sequence. If incomplete processing occurs, the quality and amount of protein is lowered (Kusnadi et al. 1997).


Methods of Suppression

Gene Silencing

Recent studies with transgenic production of antibodies have shown that the transgene involved can undergo inactivation; this process is termed gene silencing. Gene silencing has been observed to occur where there exist multiple copy integrations at one or more sites, different base-composition between rDNA and the integration site, detrimental effects of sequences adjacent to the rDNA integration site and over-expression effects (Kusnadi et al. 1997).

There are certain ways to prevent the occurrence of inactivation: Screening/selection for plants with single copy rDNA; developing methods for single-copy integration; avoiding repetitive homologous sequences; flanking rDNA with scaffold attachment regions; selection/screening for stable rDNA expression; and developing site-specific recombination systems (Kusnadi et al. 1997).


Oral Tolerance

When vaccines are taken orally, either with potato tubers or with bananas, the intestinal immune response to these food-antigens is called tolerance. Oral tolerance is an active immunologic response, which prevents the development of responses to the many antigens ingested by a host (Tacket et al. 1999). Upon intake, the oral antigens are taken up by M cells. These M cells present antigens to specific suppressor T cells, which secrete cytokines that allow for the propagation of specific antibodies. Tolerance is dose- schedule-, and antigen-specific (Tacket et al. 1999). Therefore, an antigen that is orally administered and is tolerant will show no response, because the expression of that antigen has been suppressed. When synthesizing a protein from a transgenic plant, oral tolerance must be taken into consideration.


Past and Current Research

Creating SIgA

Secretory immunoglobulin A (SIgA) is the most abundant form of immunoglobulin in mucosal secretions (Julian et al. 1994). It is composed of two monomeric IgA antibody units, a small J-chain and a secretory component (Figure 2). In an experiment, which four plants expressing each of the polypeptides were sexually crossed, it was found that a functional SIgA antibody could be produced (Julian et al. 1994). In this experiment, the functionality of the protein was studied by enzyme linked immunosorbent assay (ELISA). SA I/II was used as the antigen to be recognized on the transgenically produced SIgA antibodies (Julian et al. 1995). SA I/II is a cell surface protein of Streptococcus mutans (Julian et al. 1995), which can cause dental caries in humans. This experiment provided insight that allowed researchers to conclude that the nature of association in plants is similar to that in mammals and therefore antibodies produced in plants could be used in mammals. CaroRxTM: An anti- S. mutans SigA CaroRxTM is a clinically advanced SIgA plantibody that protects humans from dental caries (Larrick et al. 1998). In a preliminary study of CaroRxTM, anti-S. mutans antibodies were orally administered to 84 human subjects. Upon the application of SA I/II, monoclonal antibodies prevented the colonization of artificially and naturally implanted S. mutans (Larrick et al. 1998). In addition, protection from recolonization (with just 3 weeks of application) lasted for two years.


Production of an Oral Cholera vaccine

From 1995 to 1998, extensive research was conducted in the usage of potatoes as an antigen delivery system to initiate an immune response (Arakawa et al. 1998, Haq et al. 1995). Of particular interest was the CT or cholera toxin antigen. CT is composed of an A subunit and B pentamer subunit. CTA is an enzymatically active protein, which enters epithelial cells of the gut and causes water loss from these cells. CTB is enzymatically inactive and binds to Gm-gangliosides of epithelial cells, which allows for the intake of CTA (Tacket et al. 1998).

In one experiment, Arakawa, Chong and Langridge used mice to study the effects of a CT oral vaccine. The mice were fed transgenic potato tissue containing thirty micrograms or CTB/gram (Arakawa et al. 1998). They were fed four times, on days zero, six, seventeen, and twenty-four, and received a booster feeding on day sixty-five. Ten mice were fed one gram of transgenic potato expressing CTB while eight mice were fed three grams of transgenic potato expressing CTB. In addition, five mice acted as a negative control and were fed one gram of untransformed potato while eight mice were used as a positive control and fed thirty micrograms of bacterial CTB in sodium bicarbonate buffer (Arakawa et al. 1998). It was observed that during the 70-day experiment, mice immunized with thirty micrograms of bacterial CTB showed 55% protection (here protection is defined as the percent of reduction in intestinal fluid accumulation). In addition, there was 42% protection for mice immunized with one gram of transgenic potato, and 62% protection for mice immunized with three grams of transgenic potato (Arakawa et al. 1998). From these experiments, it could be concluded that oral delivery of antibodies was an effective way to treat certain diseases, at least in animals. Similar experiments were done with LT-B or heat labile enterotoxin (Aratzen, 1998), which showed similar results (Haq et al. 1995).


Human studies with transgenic potato

The successful outcomes with the studies involving CTB and LT-B in mice finally led to experimentation with human subjects. It was hypothesized that a mucosal immune response would occur upon ingestion of raw potato tubers expressing CTB or LT-B (Tacket et al. 1999). Fourteen human subjects were fed one hundred grams or transgenic potato, fifty grams of transgenic potato, or fifty grams of wild type potato. Each transgenic potato contained a variable amount of LT-B that ranged from 3.7 to 15.7 micrograms per gram (Tacket et al. 1999). This variability is a result of the different promoters used in the experiment. During the experiment, 91% of subjects who ingested transgenic potatoes developed IgG and anti-LT antibodies. In addition, 55% of the subjects who ingested transgenic potatoes developed a four-fold rise in IgA and anti-LT(Tacket et al. 1999). The results of this experiment suggest that vaccines from plants can be taken orally through some food substances. The only problem is that humans normally do not eat raw potatoes. It was shown however, that transgenic potatoes could be boiled for 3 minutes with only a 50% loss of LT-B (Tacket et al. 1999). In addition, new studies are being carried out using fruits, such as bananas, to deliver antibodies produced in plants.

Conclusion

The advancements made with transgenic plants have and will continue to have a great impact on the lives of many. Transgenic plants offer a new approach to producing and administering human antibodies. The recent research with transgenic plants has played a captivating role in providing edible vaccines, which are cheap and easy to administer. The progression of transgenic plant technology now has allowed for the progression of human life and other medicinal advancements. Hiatt was the first to demonstrate that plants could produce human antibodies and since that time, researchers have continued to build upon his findings. Since 1983, progress in the field of antibody production in plants has drastically increased, and it is projected that in the near future, many of the necessary human antibodies will have an origin as a plantibody.


References

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Journal of Young Investigators. 2001. Volume Four.
Copyright © 2001 by Elisa Ferrante, David Simpson and JYI. All rights reserved.
 
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