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What are Peptides?

Peptides are compounds formed by connecting α-amino acids with peptide bonds (an amide bond). They are intermediate products of protein hydrolysis in organisms and are the direct executors of life activities. Active peptides have all or part of the functions and properties of proteins, and the most important thing is that they can be mass-produced through chemical synthesis. Since the production of peptides by solid-phase synthesis in the 1990s, the industrialization of peptides has progressed rapidly, and their applications in industries such as drugs, health products, and cosmetics have become increasingly widespread. With the development of personalized medical treatment, the peptide industry will usher in a new round of leap-forward development.

Peptide Structure

Peptides are connected to each other by removing a molecule of water from -NH of one amino acid molecule and -COOH of another amino acid molecule to form -CH-NH. Depending on the number of amino acids (usually 10 to 100), they are called dipeptides, tripeptides, tetrapeptides, pentapeptides, etc. Among them, peptides composed of three or more amino acid molecules are called polypeptides. In addition, with different types and quantities of amino acids, each peptide has a unique composition structure, which determines and produces different functions. Peptides are one of the most complex classes of compounds in terms of type and function. Compared to amino acids, peptides have faster absorption rates, low or no energy consumption, and unsaturation.

Peptide and peptide chain

Benefits of Peptides

Peptides naturally occur in the skin, and the human body can synthesize and degrade peptides according to physiological conditions. Natural peptides come from the enzymatic breakdown products of structural proteins in the epidermis and dermis. They can regulate hormone activity, enhance or inhibit immune responses, regulate cell life cycles, activate aging cells, and comprehensively regulate and promote various major systems of the human body. The effects of peptides on human cells include but are not limited to:

Improve immunity and enhance disease resistanceMultiple research results have proven that small molecule peptides have powerful killing effects on most bacteria, fungi, protozoa, viruses and cancer cells. In addition, clinical trials have shown that small molecule active peptides can increase the phagocytic activity of macrophages and promote the proliferation of lymphocytes, which can comprehensively and quickly improve human immunity and enhance anti-viral capabilities.
Activate cellsSmall molecule peptides can activate cell activity, clean up free radicals in the human body, prevent free radicals from damaging cells, so that human cells can function normally and be in a healthy state.
Repair cellsPeptides can also repair damaged and diseased cells in the human body and improve cell metabolism. Make cells healthier and more energetic.
Remove body toxinsPeptides can promote cell metabolism, provide nutrients and energy to cells, and can also promote the absorption of other nutrients. They can help the body quickly eliminate waste and toxins from the body and maintain normal cell metabolism.
Delay and reverse agingPeptides are considered in the field of cosmetics to inhibit free radical peroxidation. It can accelerate the repair of damaged cells, maintain body vitality, reduce pigmentation, whiten spots, activate cells, promote metabolism, delay cell aging, regulate human growth and development, delay and reverse aging, etc.

Peptide Synthesis

There are currently three main sources of active peptides: chemical synthesis, extraction from animals and plants, and genetic engineering. Among them, chemical synthesis is the mainstay, and solid-phase synthesis technology has greatly promoted the development of peptides. The content of peptides in animals and plants is low and their purity is not enough. Genetic engineering, also called DNA recombination, refers to the process of exchanging and recombining DNA fragments due to the breakage and connection of different DNA strands, thereby forming new DNA. This method is mainly used for the preparation of long peptides. However, the cost is high, the success rate is low, and the product cannot be extracted in large quantities, so it still needs to be improved.

Synthesis of peptide bond

Chemical synthesis of peptides has become a mainstream synthesis method of peptides, especially in the field of pharmaceuticals, which are basically chemically synthesized peptides. Compared with peptides from other sources, it was found that the production cost of chemically synthesized peptides is controllable and easy for industrial production. Moreover, the amino acid length can be 2-50, the impurity content is predictable, the quality standards are easy to establish, and non-naturally occurring peptide types can be produced. Fully chemical synthesis of peptides can be divided into liquid phase synthesis (LPPS) and solid phase synthesis (SPPS) depending on the synthesis environment.

  • Liquid Phase Peptide Synthesis

Liquid-phase peptide synthesis is still widely used. It has the significant advantages of large scale and low synthesis cost in the synthesis of short peptides and peptide fragments. And because the reaction is carried out in the liquid phase, the reaction conditions that can be selected are more abundant, such as some catalytic hydrogenation, alkaline hydrolysis and other conditions, which can be used. This method cannot be used in solid-phase peptide synthesis due to low reaction efficiency and side reactions. Two reaction strategies, BOC and Z, are mainly used in liquid phase peptide synthesis.

  • Solid Phase Peptide Synthesis

Solid-phase synthesis has many advantages such as a wide selection of protective groups, low cost, and easy scale-up of synthesis. Compared with solid-phase synthesis, the main disadvantage of liquid-phase synthesis is that the synthesis range is small, and it generally focuses on the synthesis of peptides within 10 amino acids. In addition, intermediates need to be purified during synthesis, which takes a long time and requires a lot of work. There are currently two main strategies used in solid-phase peptide synthesis: BOC and FMOC. In the BOC method, TFA needs to be used repeatedly to remove BOC during the peptide synthesis process, and HF needs to be used to cleave the peptide from the resin at the end. Since HF must be operated using specialized instruments, and side reactions are easy to occur during peptide cleavage, its use is now restricted by experimental conditions and its use is gradually decreasing. The reaction conditions of the FMOC method are mild and peptide synthesis can be carried out under general experimental conditions. Therefore, it has also been widely used.

What are Peptides Used For?

  • Peptides for Pharmaceuticals

Marketed peptide drugs have been quite widely implemented in treating diseases, including diabetes, cancer, osteoporosis, multiple sclerosis, HIV infection. This field has emerged many blockbuster drugs. These include the GLP-1 receptor agonists Exenatide and Liraglutide for the treatment of diabetes, and the gonadotropin-releasing hormone analogs (GnRHa) Leuprolide and Goserelin for the treatment of cancer. Long-acting, non-injectable formulation will be the focus of research and development in the future.

  • Peptides for Foods

Peptides showing remarkable characteristics of processing stability, moisturizing property, low viscosity and foaming property endow their extensively applications in food industry. Moreover, they have the advantages of abundant sources, functional diversity and high bioavailability making their applications in functional foods and dietary supplements. Pea peptides are with more nutrients containing 8 essential amino acids required by human body, high water retention, gel formation and good emulsion stability, thus are used as an excellent additive in meat products processing. Due to its foaming properties and other properties, it can be added to pastry products instead of eggs and to noodle products to improve the nutritional value, strength and tenderness of noodles, and the appearance and taste of food.

  • Peptides for Agriculture

As plant protectants, peptides can activate plant growth potential, regulate plant metabolism, enhance plant water and fertilizer absorption, promote plant flower bud differentiation, improve crop fruit quality and induce plant resistance to fungal diseases, bacterial diseases, viral diseases and other diseases after being applied on the plant surface. Besides, peptides can be developed into plant immune inducers, fungicides, insecticides and chelated micronutrients, etc.

  • Peptides for Cosmetics

Peptides are showing huge potential in cosmetic industry, exerting multiple functions as skin tightening, rapid wrinkle repair, muscle relaxation and skin comfort, etc. Argireline, also known as acetyl hexapeptide-3 has the main effect of reducing the wrinkles caused by the contraction of facial expression muscles and wrinkles around the forehead or eyes. Besides, it can promote collagen production, which helps to rebuild skin tissue. Palmitoyl tripeptide-5 is a nutritional anti-wrinkle ingredient used by many famous international cosmetic brands. It helps to improve facial elasticity, reduce facial wrinkles, improve skin water content, and enhance skin radiance, etc.

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