Xu Ya-Ming, Wijeratne E M Kithsiri, Calderon-Rivera Aida, Loya-López Santiago, Perez-Miller Samantha, Khanna Rajesh, Gunatilaka A A Leslie
Southwest Center for Natural Products Research, School of Natural Resources and the Environment, College of Agriculture and Life Sciences, University of Arizona, 1064 E. Lowell St., Tucson, Arizona 85719, United States.
NYU Pain Research Center and Department of Molecular Pathobiology, College of Dentistry, New York University, 433 First Avenue, New York, New York 10010, United States.
ACS Omega. 2023 May 25;8(22):20085-20095. doi: 10.1021/acsomega.3c02302. eCollection 2023 Jun 6.
Four new triterpenes, 25-dehydroxy-25-methoxyargentatin C (), 20-hydroxyargentatin C (), 20-hydroxyisoargentatin C (), and 24--argentatin C (), together with 10 known triterpenes (-) were isolated from the aerial parts of . The structures of - were elucidated by detailed analysis of their spectroscopic data, and the known compounds - were identified by comparison of their spectroscopic data with those reported. Since argentatin C () was found to exhibit antinociceptive activity by decreasing the excitability of rat and macaque dorsal root ganglia (DRG) neurons, and its new analogues - were evaluated for their ability to decrease the excitability of rat DRG neurons. Of the argentatin C analogues tested, 25-dehydroxy-25-methoxyargentatin C () and 24--argentatin C () decreased neuronal excitability in a manner comparable to . Preliminary structure-activity relationships for the action potential-reducing effects of argentatin C () and its analogues -, and their predicted binding sites in pain-relevant voltage-gated sodium and calcium channels (VGSCs and VGCCs) in DRG neurons are presented.
从[植物名称]的地上部分分离出了四种新的三萜类化合物,即25-脱氢-25-甲氧基银叶素C()、20-羟基银叶素C()、20-羟基异银叶素C()和24--银叶素C(),以及10种已知的三萜类化合物(-)。通过对其光谱数据的详细分析阐明了-的结构,并通过将其光谱数据与已报道的数据进行比较鉴定了已知化合物-。由于发现银叶素C()通过降低大鼠和猕猴背根神经节(DRG)神经元的兴奋性而表现出抗伤害感受活性,因此对其新类似物-降低大鼠DRG神经元兴奋性的能力进行了评估。在所测试的银叶素C类似物中,25-脱氢-25-甲氧基银叶素C()和24--银叶素C()降低神经元兴奋性的方式与[银叶素C]相当。本文介绍了银叶素C()及其类似物-降低动作电位的初步构效关系,以及它们在DRG神经元中与疼痛相关的电压门控钠通道和钙通道(VGSCs和VGCCs)中的预测结合位点。