1. Description
Chemical characteristics: VIP belongs to endogenous polypeptide hormones, with an amino acid sequence of His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Leu-Asn-NH ₂, C-terminal amidation modification enhances structural stability. The core targets are VIP receptors (VPAC1, VPAC2) and PAC1 receptors, which exert physiological effects by activating the adenylate cyclase (AC)/cAMP signaling pathway. The chemical properties are relatively stable, and it is not easily hydrolyzed in neutral to weakly alkaline (pH 6.0-8.0) environments. Its ability to resist peptidase degradation is superior to short chain peptides, and it has good compatibility with bioactive molecules such as prostaglandins and growth factors.
Physical properties: VIP is a white to off white crystalline powder at room temperature, odorless and tasteless, with excellent water solubility (solubility ≥ 100 mg/mL). It can quickly dissolve in aqueous systems such as pure water, physiological saline, and phosphate buffered saline (PBS), and is slightly soluble in ethanol and propylene glycol, but insoluble in non-polar solvents such as ethylene ether and petroleum ether. The molecular weight is 3326.8 Da, and it needs to be stored under dry, sealed, and dark conditions at -20 ℃ to avoid repeated freezing and thawing; The purity of research grade/preclinical grade products is ≥ 98% (HPLC detection), with single impurities ≤ 1.0%, acetate content of 5.0% -12.0%, and no residual endotoxins.
Source and preparation: VIP naturally exists in tissues such as the gastrointestinal tract, nervous system, and immune system of the human body, and is an endogenous regulatory peptide. In industry, high-purity L-type amino acids are used as raw materials for precise preparation through solid-phase peptide synthesis. After condensation, deprotection, peptide chain assembly, and C-terminal amidation modification, high-purity products are finally purified by high-performance liquid chromatography (HPLC); The synthesis process strictly controls the reaction conditions to ensure the integrity of the peptide chain structure and receptor binding activity, and verifies the purity of the product through mass spectrometry (MS) and amino acid sequence analysis.
2. Application
In the field of pharmaceutical clinical and preclinical research and development, VIP is used as a potential therapeutic drug for multi indication studies. In clinical practice, it has been used as an adjuvant therapy for vascular spasm (such as cerebral vasospasm after subarachnoid hemorrhage) and inflammatory bowel disease (Crohn's disease, ulcerative colitis); Indications in the preclinical research and development stage include dry eye syndrome (by promoting tear secretion), chronic obstructive pulmonary disease (COPD), neurodegenerative diseases (such as Parkinson's disease), and autoimmune diseases (such as rheumatoid arthritis), currently mainly in the form of injections, nebulizers, and other formulations.
In the field of biomedical research, VIP serves as a core tool and reagent for signal pathway research, used to explore the mechanisms of vascular regulation, inflammatory immune regulation, and neuroendocrine immune network (NEI network). Through in vitro models of vascular endothelial cells, immune cells (macrophages, lymphocytes), neuronal cells, and animal disease models (such as inflammatory bowel disease mice and cerebral ischemia models), analyze their regulatory effects on the VPAC receptor pathway and inflammatory cytokine expression, providing experimental evidence for the development of related disease drugs.
Potential functional health and medical beauty fields: VIP is based on its anti-inflammatory, tissue repair, and vasodilation properties, and has the potential to be applied in high-end functional supplements and medical beauty repair products. In the field of healthcare, it can be used to improve microcirculation disorders (such as poor microcirculation in the lower limbs of middle-aged and elderly people); In the field of medical beauty, it can be added to medical art post repair products (such as laser, micro acupuncture post essence), which can accelerate the repair of skin barrier by expanding local blood vessels, reducing inflammatory reaction, while improving skin dullness (promoting blood circulation). At present, relevant applications are in the pre clinical verification stage.
3. Main Efficacy
Vascular regulation and microcirculation improvement efficacy: The core mechanism of VIP is to activate VPAC receptors on vascular smooth muscle cells, relax vascular smooth muscle, dilate systemic blood vessels (especially cerebral and gastrointestinal vessels), reduce vascular resistance, and improve local microcirculation perfusion. In the subarachnoid hemorrhage model, VIP can significantly alleviate cerebral vasospasm, increase cerebral blood flow, and reduce cerebral tissue ischemic injury; For people with microcirculation disorders, it can improve tissue oxygen supply and nutrient delivery, alleviate limb numbness, skin dullness and other problems.
Anti inflammatory and immune regulatory effects: VIP inhibits the release of pro-inflammatory factors (TNF - α, IL-1 β, IL-6), while promoting the expression of anti-inflammatory factors (IL-10, TGF - β), regulating macrophage polarization (from M1 to M2), and alleviating local and systemic inflammatory responses. In inflammatory bowel disease, it can repair the intestinal mucosal barrier, inhibit intestinal inflammatory infiltration, and alleviate symptoms of diarrhea and abdominal pain; For autoimmune diseases, it can balance the activity of immune cells and reduce the damage of abnormal immune responses to tissues.
Organizational protection and repair efficacy: VIP has targeted protective effects on tissues such as nerves, gastrointestinal tract, respiratory tract, etc. By activating VPAC receptors in nerve cells, promoting the expression of neurotrophic factors (BDNF, NGF), inhibiting neuronal apoptosis, and having a repairing effect on neural tissue in models such as cerebral ischemia and Parkinson's disease; In the field of gastrointestinal tract, it can promote the proliferation of intestinal epithelial cells and mucosal repair, enhance intestinal barrier function; In the respiratory tract, it can relax airway smooth muscle, promote mucus secretion clearance, and improve ventilation function in COPD patients.
Safety advantages: VIP, as an endogenous peptide, has extremely high biocompatibility, no cytotoxicity (MTT assay shows cell survival rate>98% at concentrations ≤ 1 mg/mL), no mutagenicity, and no reproductive toxicity; In clinical use, adverse reactions are mild (occasional brief flushing and gastrointestinal discomfort), with no addictive or withdrawal reactions. It is suitable for short-term treatment and long-term health maintenance scenarios, and has better tolerance than artificially synthesized small molecule drugs.
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