来自Ganoderma theaecolum果实体中的神经保护和抗糖尿病兰诺斯坦类型的三烯酸
Jiaocen Guo1, Li Yang2, Luting Dai2
1School of Breeding and Multiplication (Sanya Institute of Breeding and Multiplication), Hainan University, Sanya 572025, China; Key Laboratory of Research and Development of Natural Product from Li Folk Medicine of Hainan Province & National Key Laboratory for Tropical Crop Breeding, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China.
来自Ganoderma theaecolum的新型兰诺斯坦三类药物显示出强大的神经保护作用. 化合物4保护氧化应激,而化合物12,26和28抑制了与糖尿病和神经退行性疾病有关的关键酶.
科学领域:
- 自然产品 化学 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:
- 甘菌种类是生物活性化合物的丰富来源.
- 拉诺斯坦三类化合物具有多种不同的药理活性.
- 氧化应激和酶失调与神经退行性疾病和糖尿病有关.
研究的目的:
- 从Ganoderma theaecolum中分离和描述新型的兰诺斯坦三烯酸.
- 评估隔离化合物的神经保护作用,以防止过氧化引起的损伤.
- 评估化合物对蛋白氨酸酸酶1B (PTP1B) 和α-葡萄糖酶的抑制活性.
主要方法:
- 化合物的隔离和结构阐明使用综合光谱方法,包括ECD和NMR计算.
- 在体外测试评估神经保护作用在人类神经母细胞瘤SH-SY5Y细胞.
- 对PTP1B和α-葡萄糖酶的酶抑制试验,包括酶动力学和分子对接.
主要成果:
- 确定了8种新的lanostane三类化合物 (ganothenoids A-H),以及24种已知的化合物.
- 化合物4通过防止细胞循环停止,减少活性氧物种 (ROS) 和抑制亡,表现出显著的神经保护作用.
- 化合物26,12和28显示PTP1B抑制活性,而化合物12显示α-葡萄糖酶抑制.
结论:
- 草 (Ganoderma theaecolum) 是结构多样化的兰三类植物的宝贵来源.
- 化合物4显示为抗氧化应激的神经保护剂的承诺.
- 化合物12,26,28具有对PTP1B和α-葡萄糖酶的抑制潜力,这表明对代谢和神经退行性疾病的治疗应用.
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