Antioxidant and Anti-Inflammatory Activities of Hydroxybenzyl Alcohol Releasing Biodegradable Polyoxalate Nanoparticles
Antioxidant and Anti-Inflammatory Activities of Hydroxybenzyl Alcohol Releasing Biodegradable Polyoxalate Nanoparticles
复制标题
DOI：
10.1021/bm100474w
复制
发表时间：
2010-08-01
影响因子：
6.2
通讯作者：
Lee, Dongwon
中科院分区：
文献类型：
--
作者：
Park, Hyunjin;Kim, Soojin;Lee, Dongwon
对羟基苄基醇（HBA）是中草药类酚类化合物之一，具有抗炎作用，在抗氧化损伤相关疾病中起关键作用。我们开发了一种新的可生物降解和抗炎的过草酸酯共聚物，其中HBA被化学结合到其主链中。以草酰氯、1,4-环己糖乙醇和HBA为原料，通过缩合反应合成了含HBA的共草酸酯（HPOX），并在水解降解过程中释放出具有药用活性的HBA。HPOX可以分散成单个乳液，用于制备平均直径为500 nm的纳米颗粒。纳米颗粒释放的HBA能够通过抑制脂多糖（LPS）激活的RAW 264.7巨噬细胞中诱导型一氧化氮合酶（iNOS）的表达来抑制一氧化氮（NO）的产生。h痘纳米颗粒也减少了肿瘤坏死因子- α (tnf - α)的产生。HPOX的显著特点是聚合物完全降解成小分子，降解产物之一是具有药用活性的化合物。我们预计HPOX在治疗炎症性疾病方面具有很强的效力和通用性。
p-Hydroxybenzyl alcohol (HBA) is one of phenolic compounds in herbal agents and plays a pivotal role in protection against oxidative damage-related diseases due to anti-inflammatory effects. We have developed a new biodegradable and anti-inflammatory peroxalate copolymer in which HBA is chemically incorporated into its backbone. The HBA-incorporated copolyoxalate (HPOX) was synthesized from a condensation reaction of oxalyl chloride, 1,4-cyclohexamethanol and HBA and was capable of releasing pharmaceutically active HBA during hydrolytic degradation. HPOX could be dispersed into a single emulsion for the formulation of nanoparticles which had a mean size similar to 500 nm in diameter. The nanoparticles released HBA which was able to inhibit the production of nitric oxide (NO) by suppressing the expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage cells. HPOX nanoparticles also reduced the production of tumor necrosis factor-alpha (TNF-alpha). The remarkable features of HPOX are that the polymer degrades completely into small molecules and one of degradation products is a pharmaceutically active compound. We anticipate that HPOX is highly potent and versatile for the treatment of inflammatory diseases.