SONAS, EA921, Universtiy of Angers, SFR QUASAV, Faculty of Health Sciences, Department of Pharmacy, 16 Bd Daviers, 49045, Angers, France.
Université Rennes, CNRS, ISCR - UMR 6226, F-35000 Rennes, France; BioCIS, Université Paris-Sud, CNRS, Université Paris-Saclay, 5 Rue J.-B. Clément, 92290 Châtenay-Malabry, France.
Fitoterapia. 2018 Nov;131:182-188. doi: 10.1016/j.fitote.2018.10.015. Epub 2018 Oct 16.
Secondary metabolites from lichens are known for exhibiting various biological effects such as anti-inflammatory, antioxidant and antibacterial activities. Despite this wide range of reported biological effects, their impact on the formation of advanced glycation end products (AGEs) remains vastly unexplored. The latter are known contributors to lifestyle and age-related diseases such as Alzheimer and Parkinson. Moreover, the development of atherosclerosis and arterial stiffness is causally linked to the formation of AGEs. With this in mind, the present work evaluated the inhibitory effects of secondary lichen metabolites on the formation of pentosidine-like AGEs' by using an in vitro, Maillard reaction based, fluorescence assay. Overall, thirty-seven natural and five synthetically modified compounds were tested, eighteen of which exhibiting IC values in the range of 0.05 to 0.70 mM. This corresponds to 2 to 32 fold of the inhibitory activity of aminoguanidine. Targeting one major inhibiting mechanism of AGEs formation, all compounds were additionally evaluated on their radical scavenging capacities in an DPPH assay. Furthermore, as both AGEs' formation and hypertension are major risk factors for atherosclerosis, compounds that were available in sufficient amounts were also tested for their vasodilative effects. Overall, and though some of the active compounds were previously reported cytotoxic, present results highlight the interesting potential of secondary lichen metabolites as anti-AGEs and vasodilative agents.
从地衣中提取的次生代谢产物以具有各种生物活性而闻名，如抗炎、抗氧化和抗菌活性。尽管有报道称这些次生代谢产物具有广泛的生物活性，但它们对晚期糖基化终产物（AGEs）形成的影响仍未得到充分研究。AGEs 是导致阿尔茨海默病和帕金森病等生活方式和年龄相关疾病的主要因素之一。此外，动脉粥样硬化和动脉僵硬的发展与 AGEs 的形成有因果关系。有鉴于此，本研究采用体外 Maillard 反应荧光测定法，评估了次生地衣代谢物对戊糖素样 AGEs 形成的抑制作用。总的来说，测试了 37 种天然化合物和 5 种合成修饰化合物，其中 18 种化合物的 IC 值在 0.05 至 0.70mM 范围内。这相当于氨基胍抑制活性的 2 到 32 倍。针对 AGEs 形成的主要抑制机制之一，所有化合物还在 DPPH 测定中评估了它们的自由基清除能力。此外，由于 AGEs 的形成和高血压都是动脉粥样硬化的主要危险因素，因此还测试了具有足够量的化合物的血管扩张作用。总的来说，尽管一些活性化合物以前被报道具有细胞毒性，但目前的结果突出了次生地衣代谢物作为抗 AGEs 和血管扩张剂的有趣潜力。
