Team:Shanghai city/Implementation

Implementation

New Choices of Antidepressant

As a neurotransmitter, insufficient 5-HT is found to be connected with anxiety and depression. Thereafter, reuptake inhibitors of 5-HT has been widely used in antidepressant drugs to enhance the concentration of 5-HT, and then alleviate depression. Since the late 1980s, the U.S. and the world have been benefited by the selective serotonin reuptake inhibitors (SSRIs). These antidepressants — fluoxetine (Prozac), sertraline (Zoloft), paroxetine (Paxil), fluvoxamine (Luvox), citalopram (Celexa), and escitalopram (Lexapro) — are the medications that are most widely prescribed among the world. However, theses antidepressants, for instance SSRIs, has strong side effects such as insomnia, skin rashes, headaches, joint and muscle pain, stomach upset, nausea, and diarrhea.

To address the problems faced by current antidepressant, we wanted to develop an antidepressant equipped with fast efficacy and limited side effects.

Instead of following the logic of 5-HT reuptake inhibitor, we tried to increase the concentration of this neurotransmitter by enhancing the production of 5-HT in vivo, so as to achieve an antidepressant effect. Therefore, we considered how to solve this problem from two research levels.

Rin 14b cell screening platform and drug development

Product Concept

As reported, 95% of serotonin of the human body was released into the gut by intestinal enterochromaffin cells so that we used the Rin 14b cell to simulate the EC cell for building a screening platform. With this screening model, we could explore those compounds with great potential to further develop drugs for curing depression by stimulating EC cells to release 5-HT inside the human body. It is planned to use patch-clamp technology to establish a Rin14B cell drug screening platform and screen out candidate antidepressant compounds.

We have already obtained positive lead compounds, which may be functional in adjusting the 5-HT concentration level in vivo. (Please refer to our experiment results page) Our next plan may be set to find pharmaceutical companies (Such as Zhejiang Huahai Pharmaceutical Co.,Ltd we visited before) to develop cooperation on our compounds. We believe that pharmaceutical companies will be experienced in conducting further research and development work on our compounds. Hopefully these compounds may be further developed into antidepressant drugs, and come to the market in the future.

Safety Concerns and Challenges to Promote our Compounds

  • Side effects of our compounds

    We will make further experiments to clarify the possible side effects of our compounds and make essential cautions when promoting them.

  • Consumer safety of our compounds in further experiments

    We will try to investigate the safety environment of pharmaceutical companies that we want to cooperate with, ensuring that our compounds to be safely used.

  • Pharmaceutical companies' willingness to cooperate with us

    We will make specific promotion plans, winning academic and business support from distinguished institutions, such as CAS, Fudan University, Shanghai Jiao Tong University, Fosun Pharmaceutical and etc.,

  • Long-term plan


It usually takes decades and billions of dollars from the research and development of a new drug to the market. The cost of developing each new drug is enormous.

  1. Discovery and Development 2-3 years (Time is for reference only)

    The lab will start by studying disease and then looking for compounds that have the potential to treat that this disease.

    1. Drug target discovery and identification

    2. Screening and synthesis of compounds

    3. Validation and optimization of active compounds

  2. Preclinical Research 2-4 years

    The purpose of this stage is to evaluate the pharmacology, toxicological effects and optimal dosage, absorption, distribution, metabolism, and excretion of the drug.

  3. Clinical Research 3-7 years

    IND (Investigational New Drug) materials need to be submitted to the local Food and Drug Administration for approval of clinical trials.

    1. Phase I clinical 20-100 normal subjects for safety and dose purposes.

    2. Phase ii trials of 100-300 patients, aimed at efficacy and side effects.

    3. Phase iii 300-3000 patients, expanded sample size, the purpose is to observe adverse reactions.

  4. Drug Review

    NDA (New Drug Application) application materials. “All information about a drug is included in the NDA -- from preclinical data to phase 3 trial data. The developer must include reports of all studies, data, and analyses.”

    After Food and Drug Administration approve NDA. The new drug is officially on the market.

  5. Post-market study

    Phase IV trials may be required in some countries. More than 2000 subjects were required, and a social study was conducted.

P.S: Each country's policies are different, but very similar. But the policy is very strict.

Probiotics beverage

Product Concept

We constructed a biosynthetic pathway for exogenous synthesis of serotonin in Escherichia coli and using L-tryptophan as substrate, L-tryptophan can be converted into 5-hydroxytryptophan through whole cell catalysis, therefore being able to realize the use of gene recombinant Escherichia coli to produce serotonin in vivo.

In part, a recombinant Escherichia coli system is used to increase the level of serotonin in vivo. The recombinant Escherichia coli contains tryptophan hydroxylase TPH gene and tryptophan decarboxylase TDC gene, and the said tryptophan hydroxylase TPH gene and tryptophan decarboxylase TDC gene can be expressed in the Escherichia coli cells, forming active tryptophan hydroxylase TPH and tryptophan decarboxylase TDC gene. We also obtained quite encouraging results in this part. (Specific results details may be found on our experiment results page) Relying on our experiment results, we set our future goals to design oral beverages or health supplements to increase the level of serotonin in the human body, thereby improving dysthymia and alleviating depression. Our major clients are the people at high incidence age of depression. (Adolescents, and people faced with moderate to high work or living pressures).

Safety Concerns and Challenges about our Implementation Plan of Probiotics

  • Safety issues of Escherichia coli in producing probiotics

    Escherichia coli is not an ideal vector to produce probiotics, thus it is essential for us to make further experiments using other chassis, such as Bacillus subtilis or Lactobacillaceae, to further verify our experiment results and consolidate our probiotic plan;

  • Government Regulation about GMO Products

    Government imposes strict regulations on GMO products, thereafter, we must adhere to the relevant rules and regulations in our future plan;

  • Market Response to GMO Products

    Our potential clients may not be able to purchase our GMO products, thus a systematic production line and promotion plans should be specified.

Reference

  1. GBD 2017 Disease and Injury Incidence and Prevalence Collaborators. (2018). Global, regional, and national incidence, prevalence, and years lived with disability for 354 diseases and injuries for 195 countries and territories, 1990–2017: a systematic analysis for the Global Burden of Disease Study 2017. The Lancet. DOI.

  2. Nozawa K, Kawabata-Shoda E, Doihara H, et al. TRPA1 regulates gastrointestinal motility through serotonin release from enterochromaffin cells[J]. Proc Natl Acad Sci U S A, 2009, 106(9): 3408-13.

  3. Pompili Maurizio,Lionetto Luana,Curto Martina,Forte Alberto,Erbuto Denise,Montebovi Franco,Seretti Maria Elena,Berardelli Isabella,Serafini Gianluca,Innamorati Marco,Amore Mario,Baldessarini Ross J,Girardi Paolo,Simmaco Maurizio. Tryptophan and Kynurenine Metabolites: Are They Related to Depression?[J]. Neuropsychobiology,2018.