具有抗纤维化活性的结构多样化的类化合物来自百足动物Scolopendra subspinipes mutilans
Bin-Yuan Hu1,2, Wu-Mei Sun1, Cheng-Tian Tao1
1Guangdong Key Laboratory of Chinese Medicine Ingredients and Gut Microbiomics, Institute for Inheritance-Based Innovation of Chinese Medicine, Marshall Laboratory of Biomedical Engineering, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen 518055, China.
这项研究从Scolopendra subspinipes mutilans中分离出了12种新的化物,其中一些显示出抗炎和抗纤维化活性. Lamp2被确定为抗纤维化作用的潜在目标.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 百脚Scolopendra subspinipes mutilans是一种生物活性天然产品的来源.
- 类化合物是一种具有显著药理潜力的多样性化合物.
研究的目的:
- 从Scolopendra subspinipes mutilans中分离和描述新的类化合物.
- 评估孤立类化合物的抗炎和抗纤维化活性.
- 为了确定观察到的生物活性的潜在分子标.
主要方法:
- 使用色谱技术分离和净化类化合物.
- 通过光谱数据分析 (NMR,MS) 阐明结构.
- 计算方法包括量子化学计算.
- 在体外测定抗炎和抗纤维化活性.
- 药物亲和度响应目标稳定性 (DARTS) 和RNA干扰 (RNAi) 测试.
主要成果:
- 确定了12种新的类化合物 (scolopenolines A-L) 和6种已知的类似物.
- 斯科洛佩诺林A具有独特的含瓜尼迪尔的C14类类化合物,具有6/6/5环脊柱.
- 斯科洛佩诺林B是一种含有硫的新型异构聚合物.
- 斯科洛佩诺林G具有一种罕见的C12类骨架.
- 1,8,10和15-18类化物表现出抗炎活性.
- 类10和16-18显示出抗纤维化活性.
- Lamp2被确定为类16抗纤维化作用的潜在标蛋白.
结论:
- 对Scolopendra subspinipes mutilans的化学研究产生了具有有前途的生物活性的新素类化合物.
- 已识别的化物,特别是10和16-18化物,显示出治疗炎症和纤维化的潜力.
- 兰普2成为开发新型抗纤维化疗法的重要分子标.
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