Lysophosphatidic Acid (LPA, CAS 18891-11-7)
Lysophosphatidic Acid (LPA, CAS 18891-11-7) is a simplest glycerophospholipid acting as a critical extracellular signaling molecule. Derived from phospholipase-mediated hydrolysis of phosphatidylcholine, LPA regulates cell proliferation, migration, and inflammation via G-protein-coupled receptors (LPARs). Clinically, it shows promise in wound healing, dermatology, and cardiovascular disease therapy.
溶血磷脂酸（LPA，CAS 18891-11-7）是结构最简单的甘油磷脂，作为关键细胞外信号分子，通过G蛋白偶联受体（LPARs）调控细胞增殖、迁移及炎症反应。临床研究显示其在创面修复、皮肤护理及心血管疾病治疗中潜力显著。
1. Basic Information
- Chemical Name: Lysophosphatidic Acid (LPA)
- CAS Number: 18891-11-7
- Molecular Formula: C₃H₇O₅P
- Molecular Weight: 154.06 g/mol
- Sources: Derived from phosphatidylcholine via phospholipase A1/A2 hydrolysis; also synthesized via autotaxin (ENPP2) enzymatic activity.
- 化学名称：溶血磷脂酸
- CAS号：18891-11-7
- 分子式：C₃H₇O₅P
- 分子量：154.06 g/mol
- 来源：磷脂酰胆碱经磷脂酶A1/A2水解生成；亦可由自分泌运动因子（ENPP2）催化合成。
2. Key Physicochemical Properties
| Parameter | Details |
|---|---|
| Solubility | Highly water-soluble; forms micelles in aqueous solutions. |
| Surface Activity | Amphiphilic structure enables emulsification and membrane interaction. |
| Stability | Stable under physiological pH (6–8); susceptible to oxidation. |
| 参数 | 详情 |
|---|---|
| 溶解性 | 高度水溶性，水溶液中可形成胶束。 |
| 表面活性 | 两亲性结构赋予其乳化及膜相互作用能力。 |
| 稳定性 | 生理pH（6–8）下稳定；易被氧化破坏。 |
3. Mechanisms of Action
- Receptor Activation: Binds LPAR1-6 (GPR87, P2Y10), activating pathways like Rho/ROCK, PI3K/Akt, and PLC.
- Cellular Effects:
- Proliferation: Enhances fibroblast and keratinocyte growth via MAPK signaling.
- Inflammation: Modulates cytokine release (e.g., TNF-α, IL-6) in macrophages.
- Angiogenesis: Promotes endothelial cell migration and tube formation.
- 受体激活：结合LPAR1-6（GPR87、P2Y10），激活Rho/ROCK、PI3K/Akt、PLC等通路。
- 细胞效应：
- 增殖：通过MAPK信号促进成纤维细胞和角质形成细胞增殖。
- 炎症：调控巨噬细胞细胞因子（如TNF-α、IL-6）释放。
- 血管生成：促进内皮细胞迁移及管状结构形成。
4. Applications
- Dermatology:
- Wound Healing: Accelerates re-epithelialization via keratinocyte migration (↑30% in murine models).
- Hair Growth: Stimulates follicular development by activating perifollicular fibroblasts.
- Cardiovascular:
- Atherosclerosis: Reduces plaque inflammation by modulating macrophage phenotype.
- Hypertension: Improves endothelial function via NO/cGMP pathway.
- Pharmaceuticals:
- Drug Delivery: Enhances skin permeation for topical formulations.
- 皮肤科：
- 创面修复：通过角质形成细胞迁移加速再上皮化（小鼠模型中↑30%）。
- 毛发生长：激活毛周纤维母细胞促进毛囊发育。
- 心血管：
- 动脉粥样硬化：调控巨噬细胞表型减轻斑块炎症。
- 高血压：通过NO/cGMP通路改善内皮功能。
- 药物制剂：
- 透皮递送：增强局部制剂皮肤渗透性。
5. Production & Engineering
- Natural Sources: Isolated from egg yolk phospholipids or soybean lecithin.
- Synthetic Methods:
- Chemical Synthesis: Phosphorylation of lysophosphatidylcholine using POCl₃.
- Biotechnological: Engineered E. coli strains overexpressing autotaxin for LPA production.
- 天然来源：从蛋黄磷脂或大豆卵磷脂中提取。
- 合成方法：
- 化学合成：POCl₃催化溶血磷脂酰胆碱磷酸化。
- 生物技术：改造大肠杆菌过表达自分泌运动因子（ENPP2）生产LPA。
6. Safety & Challenges
- Safety: Generally recognized as safe (GRAS) at ≤10 μM; high doses (>50 μM) induce hemolysis.
- Challenges:
- Rapid enzymatic degradation in vivo (half-life <2 h).
- Costly large-scale synthesis.
- 安全性：≤10 μM浓度下视为安全；高剂量（>50 μM）引发溶血。
- 挑战：
- 体内酶解迅速（半衰期<2小时）。
- 大规模合成成本高昂。
7. Research Frontiers
- LPAR6 Antagonists: Targeting hair loss (e.g., LPAR6 mutations cause hypotrichosis).
- LPA-Loaded Nanoparticles: Sustained release for dermal and ocular therapies.
- Cancer Therapy: LPA signaling in metastasis and angiogenesis modulation.
- LPAR6拮抗剂：针对脱发治疗（LPAR6突变导致先天性少毛症）。
- LPA纳米颗粒：缓释技术用于皮肤及眼部疾病。
- 肿瘤治疗：LPA信号在转移及血管生成中的作用。
8. Regulatory Status
- FDA: Generally Recognized as Safe (GRAS) for cosmetic and dietary applications.
- EU: Approved as a food additive (E470a) in limited concentrations.
Summary
LPA’s dual role as a signaling lipid and functional emulsifier positions it as a multifunctional biomolecule. While its therapeutic potential in dermatology and vascular health is well-documented, challenges in stability and cost require innovative solutions. Emerging LPAR-targeted therapies and nanotechnology applications may unlock new frontiers in precision medicine.
溶血磷脂酸（LPA）兼具信号脂质与功能乳化剂特性，是多效生物分子。尽管其在皮肤科及血管健康领域的疗效明确，稳定性与成本问题仍需突破。靶向LPAR的新型疗法及纳米技术应用或将为精准医疗开辟新方向。
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