East China Woody Fragrance and Flavor Engineering Research Center of National Forestry and Grassland Administration, Camphor Engineering Research Center of National Forestry and Grassland Administration, College of Forestry, Jiangxi Agricultural University, Nanchang 330045, China.
National Engineering Laboratory for Biomass Chemical Utilization, Institute of Chemical Industry of Forest Products, Chinese Academy of Forestry, Nanjing 210042, China.
Int J Mol Sci. 2021 Oct 19;22(20):11299. doi: 10.3390/ijms222011299.
-pinene is a monoterpene isolated from turpentine oil and numerous other plants' essential oils, which has a broad spectrum of biological activities. In the current work, six novel -pinene quaternary ammonium (-PQA) salts were synthesized and evaluated in vitro for their antifungal, antibacterial and anticancer activities. The in vitro assay results revealed that compounds and presented remarkable antimicrobial activity against the tested fungi and bacteria. In particular, compound showed excellent activities against , , , and with EC values of 4.50, 10.92, 9.45, 10.82 and 6.34 μg/mL, respectively. Moreover, compound showed the best antibacterial action against , , and , with MIC at 2.5, 0.625, 1.25 and 1.25 μg/mL, respectively. The anticancer activity results demonstrated that compounds , , and exhibited remarkable activity against HCT-116 and MCF-7 cell lines, with IC values ranged from 1.10 to 25.54 μM. Notably, the compound displayed the strongest cytotoxicity against HCT-116 and MCF-7 cell lines, with the IC values of 1.10 and 2.46 μM, respectively. Furthermore, preliminary antimicrobial mechanistic studies revealed that compound might cause mycelium abnormalities of microbial, cell membrane permeability changes and inhibition of the activity of ATP. Altogether, these findings open interesting perspectives to the application of -PQA salts as a novel leading structure for the development of effective antimicrobial and anticancer agents.
-蒎烯是从松节油和许多其他植物精油中分离得到的单萜，具有广泛的生物活性。在目前的工作中，合成了六种新型 -蒎烯季铵盐（-PQA）并对其进行了体外抗真菌、抗菌和抗癌活性评价。体外实验结果表明，化合物 和 对测试的真菌和细菌具有显著的抗菌活性。特别是化合物 对 、 、 、 和 具有优异的活性，EC 值分别为 4.50、10.92、9.45、10.82 和 6.34 μg/mL。此外，化合物 对 、 、 和 表现出最佳的抗菌作用，MIC 值分别为 2.5、0.625、1.25 和 1.25 μg/mL。抗癌活性结果表明，化合物 、 、 和 对 HCT-116 和 MCF-7 细胞系表现出显著的活性，IC 值范围为 1.10 至 25.54 μM。值得注意的是，化合物 对 HCT-116 和 MCF-7 细胞系表现出最强的细胞毒性，IC 值分别为 1.10 和 2.46 μM。此外，初步的抗菌机制研究表明，化合物 可能导致微生物菌丝体异常、细胞膜通透性改变和抑制 ATP 活性。总之，这些发现为 -PQA 盐作为开发有效抗菌和抗癌药物的新型先导结构的应用提供了有趣的前景。
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