KPV

KPV is a tripeptide (Lys-Pro-Val) derived from the C-terminal sequence of α-melanocyte-stimulating hormone (α-MSH). Unlike the parent hormone, KPV retains strong anti-inflammatory and tissue-repair properties without inducing pigmentation.

Structure

Tripeptide sequence: Lys–Pro–Val
Molecular weight: ~341 Da
C-terminal fragment of α-MSH

Mechanism of Action

• NF-κB Inhibition: Suppresses transcription of pro-inflammatory cytokines (e.g., TNF-α, IL-1β, IL-6).
• TLR4/ROS Modulation: Reduces toll-like receptor signaling and oxidative stress.
• Barrier Protection: Enhances epithelial integrity in gut mucosa and skin.
• Immune Regulation: Inhibits neutrophil migration and shifts macrophages toward an anti-inflammatory M2 phenotype.

Indications
(Preclinical and early-stage studies) :

Inflammatory Bowel Disease (IBD): Crohn’s disease, ulcerative colitis.

Dermatology: Psoriasis, acne, wound healing.

Mucosal & Epithelial Repair: Gut barrier protection, accelerated tissue healing.

LL-37

LL-37 is the only human cathelicidin-derived antimicrobial peptide (AMP). It is produced by proteolytic cleavage of the precursor protein hCAP18 at its C-terminal end. LL-37 is an essential component of the innate immune system, providing broad-spectrum antimicrobial activity while also regulating immune responses, tissue repair, and angiogenesis.

Structure

37–amino acid peptide
Derived from the C-terminal region of hCAP18 (human cationic antimicrobial protein)
Amphipathic, α-helical conformation that facilitates interaction with microbial membranes

Mechanism of Action

• Direct Antimicrobial Activity: Disrupts bacterial, viral, and fungal membranes through pore formation and lysis.
• Immunomodulation: Functions as a chemoattractant for neutrophils, monocytes, and T cells; modulates cytokine release via pathways such as NF-κB and MAPK, leading to context-dependent pro- or anti-inflammatory effects.
• Wound Healing & Angiogenesis: Enhances migration and proliferation of keratinocytes and endothelial cells, promotes extracellular matrix remodeling, and stimulates angiogenesis during tissue repair.

Indications
(Preclinical and early-stage studies):

Infectious Diseases: Potential as a novel antimicrobial agent against resistant bacteria, viruses, and fungi.
Chronic Non-Healing Wounds: Acceleration of healing in diabetic foot ulcers and pressure ulcers.
Inflammatory Skin Disorders: Modulation of psoriasis, atopic dermatitis, and rosacea.
Autoimmune/Auto-inflammatory Conditions: Regulation of immune activation in systemic and localized inflammation.

 

Thymosin Alpha-1

Thymosin Alpha-1 (Tα1) is a naturally occurring 28–amino acid peptide originally isolated from the thymus gland. It is a potent immunomodulator that enhances adaptive immunity, particularly by promoting T-cell maturation, differentiation, and activity. Tα1 also contributes to restoring immune homeostasis in states of chronic infection, immune suppression, and cancer.

Structure

28–amino acid peptide
Sequence: Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn
N-terminally acetylated peptide

Mechanism of Action

• T-cell Maturation: Stimulates differentiation and maturation of CD4+ and CD8+ T cells in the thymus.
• Immune Enhancement: Increases cytokine production (e.g., IFN-γ, IL-2) and enhances dendritic cell antigen presentation, strengthening adaptive immune responses.
• Immune Tolerance & Anti-inflammation: Helps rebalance immune activity, reducing chronic inflammation and preventing excessive immune activation in autoimmune or persistent infection settings.

Indications
(Preclinical, clinical, and approved uses depending on country):

Vaccine Adjuvant: Enhances immunogenicity of vaccines by strengthening T-cell and antibody responses.
Chronic Viral Infections: Used in hepatitis B and C for immune modulation and viral load reduction.
Immunodeficiency Disorders: Supportive therapy for secondary immunodeficiency (e.g., chemotherapy-induced).
Oncology (Adjunct): Applied in certain cancers (e.g., hepatocellular carcinoma, non-small cell lung cancer, melanoma) to improve immune surveillance and treatment response.

 

Thymulin

Thymulin is a nonapeptide (9–amino acid) hormone secreted by thymic epithelial cells. Its biological activity requires the presence of zinc (Zn²⁺), which is essential for its structural stability and receptor binding. Thymulin plays a pivotal role in T-cell differentiation, immune regulation, and neuro–immune interactions.

Structure

9–amino acid peptide: Glu–Ala–Lys–Ser–Gln–Gly–Gly–Ser–Asn
Requires zinc ion (Zn²⁺) binding for biological activity
Classified as a thymic peptide hormone

Mechanism of Action

• T-cell Differentiation: Promotes maturation of thymocyte precursors into functional CD4+ and CD8+ T lymphocytes.
• Immunomodulation: Regulates the activity of mature T-cells, enhancing helper T-cell function and modulating cytokine secretion.
• Neuro–Immune Interaction: Acts within the neuroendocrine–immune axis, influencing hormone release (e.g., ACTH, prolactin) that in turn shapes immune activity.

Indications
(Preclinical and investigational uses):

Age-related Thymic Involution / Immunosenescence: Counteracting thymic atrophy and restoring immune competence in aging.
Primary & Secondary Immunodeficiencies: Support of immune restoration in congenital or acquired immunodeficiency states.
Autoimmune Diseases: Potential to rebalance immune responses and reduce pathogenic autoimmunity.
 

 

Thymalin

Thymalin is a complex, natural polypeptide extract obtained from the thymus glands of calves. It is a biological response modifier containing multiple thymic peptides, including thymulin and Thymosin Alpha-1 (Tα1), which act synergistically to regulate and restore immune function.

Structure

Complex, standardized mixture of multiple polypeptides isolated from animal thymus tissue
Includes short thymic peptides such as Thymulin and Thymosin Alpha-1 (Tα1)
Although there is no single defined peptide sequence; composition includes other immunoregulatory peptides contributing to its polyvalent activity

Mechanism of Action

• Immune System Restoration: Normalizes T-cell and B-cell function, enhancing immune responses in immunodeficiency and modulating overactive immune responses in autoimmune conditions.
• Hematopoiesis Stimulation: Promotes bone marrow stem cell proliferation, supporting regeneration of multiple blood cell lineages.
• Tissue Repair: Facilitates repair and regeneration in various tissues, aiding recovery after surgery, trauma, or chronic damage.

Indications
(Preclinical, clinical, and approved uses depending on region):

Immune Deficiency Correction: Supportive therapy after chemotherapy, chronic infections, or other states of suppressed immunity.
Recovery & Wound Healing: Accelerates post-surgical or post-injury tissue repair.
Suppressed Immune Function: Used in conditions associated with immune insufficiency.
Anti-Aging / Immunosenescence: Potential application to counteract age-related decline in immune function.