Center of Excellence in Cannabis Research, Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok 65000, Thailand.
Université de Franche-Comté, PEPITE, 25000 Besançon, France.
Molecules. 2023 Aug 2;28(15):5821. doi: 10.3390/molecules28155821.
The objectives of this study were (1) to investigate the effect of extracts from some plants in the families Nelumbonaceae and Nymphaeaceae on phosphodiesterase 5 (PDE5) and arginase, which have been used in erectile dysfunction treatment, and (2) to isolate and identify the compounds responsible for such activities. The characterization and quantitative analysis of flavonoid constituents in the active extracts were performed by HPLC. Thirty-seven ethanolic extracts from different parts of plants in the genus and of Nymphaeaceae and genus of Nelumbonaceae were screened for PDE5 and arginase inhibitory activities. The ethanolic extracts of the receptacles and pollens of Gaertn., petals of Roxb. ex G.Don, Willd., and (Poepp.) Sowerby and the petals and receptacles of Willd. showed IC values on PDE5 of less than 25 μg/mL while none of the extracts showed effects on arginase. The most active extract, petal extract, was fractionated to isolate and identify the PDE5 inhibitors. The results showed that six flavonoid constituents including quercetin 3'-O--xylopyranoside (), quercetin 3-methyl ether 3'-O--xylopyranoside (), quercetin (), 3--methylquercetin (), kaempferol () and 3--methylkaempferol () inhibited PDE5 with IC values at the micromolar level.
(1) 研究来自莲科和睡莲科一些植物的提取物对已用于治疗勃起功能障碍的磷酸二酯酶 5（PDE5）和精氨酸酶的影响；(2) 分离并鉴定产生这种活性的化合物。通过 HPLC 对活性提取物中的类黄酮成分进行了表征和定量分析。对来自莲科属和睡莲科属不同部位的 37 种植物的乙醇提取物进行了 PDE5 和精氨酸酶抑制活性筛选。莲科属植物的花托和花粉、睡莲科属植物的花瓣、 和 的乙醇提取物对 PDE5 的 IC 值均小于 25μg/mL，而没有一种提取物对精氨酸酶有影响。活性最强的提取物为花瓣提取物，将其进行分离以鉴定 PDE5 抑制剂。结果表明，六种黄酮类成分，包括槲皮素 3'-O--吡喃木糖苷（）、槲皮素 3-甲基醚 3'-O--吡喃木糖苷（）、槲皮素（）、3--甲基槲皮素（）、山柰酚（）和 3--甲基山柰酚（），以微摩尔级别的 IC 值抑制了 PDE5。
