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▎What is Testagen?
At the molecular level, Testagen belongs to the class of short peptides, composed of four amino acids linked by peptide bonds. This specific amino acid sequence endows Testagen with unique biological characteristics and functions. In cellular environments, it exists as a short peptide capable of interacting with multiple intracellular components, thereby influencing cellular physiological activities.
▎Testagen Structure
Source: PepDraw | Molecular Formula: C22H30N6O6 Molecular Weight: 474.53g/mol |
▎Testagen Research
What is the research background of Testagen?
Against the backdrop of advancing modern biotechnology and biomedical research, the exploration of bioactive peptides has become a significant research direction in the field. As a synthetic peptide, Testagen holds notable research significance due to its potential value in cellular processes, tissue regeneration, metabolic pathways, and other physiological and biochemical systems. Belonging to the category of bioactive peptides, Testagen is composed
of amino acid sequences that may influence cell-molecule interactions. Its structure is designed to mimic or support endogenous biological processes, thus presenting potential as a research subject in molecular biology, biochemistry, and regenerative research.
Figure 1. Bioregulation system of a multicellular organism.
Source: MDPI[1]
What is the mechanism of action of Testagen?
Cell Penetration: Studies have shown that after incubating HeLa cells with fluorescein isothiocyanate-labeled Testagen, distinct fluorescence was observed in the cytoplasm, cell nucleus, and nucleolus, indicating that Testagen has the ability to penetrate animal cells and their nuclei. Its capacity to traverse cell membranes and nuclear membranes into the cell interior may be related to certain transport proteins on the cell membrane or membrane fluidity. The cell membrane is not a completely impermeable structure; it contains channels and transport mechanisms. Testagen may enter cells by interacting with these transport proteins or via endocytosis-like mechanisms utilizing membrane fluidity, laying the foundation for its subsequent effects[2].
Specific Interactions with Nucleic Acids: Different intact peptides of origin exhibit varying effects on the fluorescence of 5,6-carboxyfluorescein-labeled deoxyoligonucleotides and DNA-ethidium bromide complexes. By measuring Stern-Volmer constants, it was found that Testagen, compared to other short peptides, induces different degrees of fluorescence quenching in single-stranded and double-stranded fluorescently labeled deoxyoligonucleotides, depending on the peptide’s primary structure. This demonstrates specific interactions between Testagen and nucleic acid structures. When binding to nucleic acids, Testagen can distinguish between different nucleotide sequences and even recognize their cytosine methylation status. For example, Testagen appears to preferentially bind to deoxyoligonucleotides containing CAG sequences. Such specific binding may be achieved through non-covalent interactions such as hydrogen bonds and electrostatic interactions between amino acid residues on the Testagen molecule and the bases or phosphate backbones of nucleic acids. This specificity allows Testagen to precisely localize to specific nucleic acid regions, thereby influencing processes such as gene expression[2].
Epigenetic Regulation of Cellular Genetic Functions: Due to its ability to specifically bind to DNA, Testagen’s site-specific interactions with DNA can control cellular genetic functions at the epigenetic level. Epigenetic regulation does not alter the DNA base sequence but influences gene expression through DNA modifications (e.g., methylation) and histone modifications. Testagen may bind to specific DNA regions, affecting chromatin structure in those regions or recruiting epigenetic regulatory protein factors to modulate gene transcriptional activity. Such regulation of gene activity may have played a critical role in the early stages of life’s origin and biological evolution, helping organisms precisely regulate gene expression in different environments to adapt to changes and complete life processes[2].
Effects on Endocrine Function in Chronic Non-Bacterial Prostatitis Patients: In medical research, studies on patients with chronic non-bacterial prostatitis (IIIA) have found that after one month of conservative treatment with a regimen including Testagen (α1-adrenergic blockers + rectal suppositories containing non-steroidal anti-inflammatory drugs), urodynamic parameters significantly improved, prostatic inflammation levels decreased, and serum total testosterone levels increased. This suggests that Testagen may regulate endocrine balance through certain mechanisms. A plausible mechanism is that Testagen influences signaling pathways related to testosterone synthesis in Leydig cells. Testosterone synthesis is a complex process involving multiple enzymes and signaling molecules. Testagen may activate or inhibit related signaling pathways by binding to intracellular receptors, thereby promoting testosterone synthesis, improving the patient’s endocrine status, and alleviating symptoms of chronic non-bacterial prostatitis[3].
What are the applications of Testagen?
Treatment of Chronic Non-Bacterial Prostatitis: Chronic non-bacterial prostatitis (IIIA), often accompanied by lower urinary tract symptoms, negatively impacts patients’ quality of life. Testagen plays a significant role in treating such conditions[4] (Niu D, 2023). Studies using a conservative treatment regimen combining α1-adrenergic blockers, rectal suppositories with non-steroidal anti-inflammatory drugs, and Testagen achieved remarkable results after one month. Urodynamic parameters improved significantly, indicating enhanced micturition function and relief of lower urinary tract obstruction symptoms. Meanwhile, intraprostatic inflammation levels decreased, reducing tissue damage. More importantly, serum total testosterone levels increased. Testosterone is crucial for maintaining normal functions of the male reproductive system, sexual function, and overall metabolism, and its elevation helps improve endocrine disorders caused by the disease [3].
Cell Penetration and Nucleic Acid Interactions: As a short bioactive peptide, Testagen exhibits unique cellular properties that form the basis for its medical applications[2] (Fedoreyeva L I, 2011). In HeLa cell experiments, significant fluorescence was observed in the cytoplasm, nucleus, and nucleolus after incubation with fluorescein isothiocyanate-labeled Testagen, demonstrating its ability to penetrate animal cells and nuclei. This allows Testagen to enter cells and interact with intracellular components, enabling regulatory functions within cells.
Studies have found that different short bioactive peptides exert varying effects on the fluorescence of 5,6-carboxyfluorescein-labeled deoxyribooligonucleotides and DNA-ethidium bromide complexes. Fluorescence quenching levels, characterized by Stern-Volmer constants, vary among short peptides like Testagen depending on their primary structure when interacting with single-stranded and double-stranded fluorescently labeled deoxyribooligonucleotides, indicating specific interactions with nucleic acid structures. Further research shows that Testagen preferentially binds to deoxyribooligonucleotides containing CAG sequences. This ability to bind specific nucleic acid sequences suggests that Testagen may regulate cellular genetic functions at the epigenetic level through site-specific DNA interactions, playing a key role in gene activity regulation. This holds potential for developing gene regulation-based therapies—for example, in diseases associated with abnormal gene expression. Although direct clinical applications have not yet been reported, mechanistic studies at the cellular and molecular levels point to future medical applications.
Conclusion
In summary, Testagen has demonstrated therapeutic efficacy in treating chronic non-bacterial prostatitis, while its properties of cell penetration and nucleic acid interaction offer potential for broader medical applications. With further research, it is expected to play an important role in treating more diseases and medical interventions.
About The Author
The above-mentioned materials are all researched, edited and compiled by Cocer Peptides.
Scientific Journal Author
Niu, Dun is a prominent scholar in the fields of medicine and life sciences. Affiliated with prestigious institutions such as Army Medical University and University of South China, he focuses his research on Pharmacology & Pharmacy, Cell Biology, Immunology, and Biochemistry & Molecular Biology. These disciplines are crucial for uncovering disease mechanisms, advancing new drug development, and enhancing human health. Additionally, Niu, Dun conducts research in the Cardiovascular System & Cardiology, exploring the pathogenesis and treatment of cardiac diseases. His work provides significant theoretical foundations and practical guidance for the clinical diagnosis and treatment of cardiovascular diseases, reflecting his profound expertise and broad influence in medical research.. Niu, Dun is listed in the reference of citation [4].
▎Relevant Citations
[1] Khavinson V K, Popovich I G E, Linkova N S, et al. Peptide Regulation of Gene Expression: A Systematic Review[J]. Molecules, 2021,26(22},https://www.mdpi.com/1420-3049/26/22/7053
ARTICLE-NUMBER = {7053).DOI:10.3390/molecules26227053.
[2] Fedoreyeva L I, Kireev I I, Khavinson V, et al. Penetration of short fluorescence-labeled peptides into the nucleus in HeLa cells and in vitro specific interaction of the peptides with deoxy ribooligonucleotides and DNA[J]. Biochemistry-Moscow, 2011,76(11):1210-1219.DOI:10.1134/S0006297911110022.
[3] Rossikhin V, Hoshchenko Y, Osipov P. Efficacy of testosterone synthesis inductor application "testagen" in androgenic deficiency in patients with chronic abacterial prostatitis[J]. Problems of Endocrine Pathology, 2011,36:17-22.DOI:10.21856/j-PEP.2011.2.03.
[4] Niu D, Wu Y, Lian J. Circular RNA vaccine in disease prevention and treatment[J]. Signal Transduction and Targeted Therapy, 2023,8. https://api.semanticscholar.org/CorpusID:261662530.
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