Dipartimento di Farmacia, Università di Genova , Viale Cembrano 4, 16148 Genova, Italy.
Department of Pharmaceutical Sciences, University of Basel , Klingelbergstrasse 50, 4056 Basel, Switzerland.
J Nat Prod. 2017 Feb 24;80(2):503-514. doi: 10.1021/acs.jnatprod.6b01053. Epub 2017 Feb 10.
A surface extract of the aerial parts of Salvia chamaedryoides afforded 13 diterpenes (1-13), with seven compounds (1, 3, 4, 7-9, 12) described for the first time. The structures of the new compounds were established using 1D and 2D NMR spectroscopic methods, HRESIMS, and ECD data. The potential hypoglycemic effects of the crude extract, fractions, and pure compounds from S. chamaedryoides were investigated by inhibition of α-glucosidase and α-amylase enzymes. The extract and its fractions showed a moderate dose-dependent inhibition; the pure compounds exhibited differential inhibitory activity against these two enzymes. Molecular modeling studies were also performed to suggest the interaction mode of compound 3 in the α-glucosidase enzyme active site. The antimicrobial activity of the purified compounds was investigated against 26 clinical pathogens. No activity was detected for the Gram-negative species tested nor on Candida albicans and C. glabrata, while variable susceptibilities were observed using Gram-positive staphylococcal and enterococcal species.
从迷迭香地上部分的表面提取物中获得了 13 种二萜类化合物(1-13),其中 7 种化合物(1、3、4、7-9、12)为首次描述。新化合物的结构通过 1D 和 2D NMR 光谱方法、HRESIMS 和 ECD 数据确定。通过抑制α-葡萄糖苷酶和α-淀粉酶酶,研究了迷迭香地上部分的粗提取物、馏分和纯化合物的潜在降血糖作用。提取物及其馏分显示出适度的剂量依赖性抑制;纯化合物对这两种酶表现出不同的抑制活性。还进行了分子建模研究,以提出化合物 3 在α-葡萄糖苷酶酶活性部位的相互作用模式。对纯化化合物的抗菌活性进行了研究,以评估其对 26 种临床病原体的作用。测试的革兰氏阴性物种以及白色念珠菌和光滑念珠菌均未显示出活性,而对革兰氏阳性葡萄球菌和肠球菌物种则观察到不同的敏感性。