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含1,2,3-三唑部分的新型7-氧代脱氢枞酸杂化物的合成与抗炎评价

Synthesis and Anti-Inflammatory Evaluation of Novel Hybrids of 7-Oxodehydroabietic Acid Bearing a 1,2,3-Triazole Moiety.

作者信息

Fang Wen-Tao, Lv Yong-Feng, Ren Fu-Cai, Zhang Hong, Xie Dong-Mei, Zhang Xiao-Bo, Fang Cheng-Wu, Liu Shou-Jin, Luo Han

机构信息

College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230011, China.

College of Science, Westlake University, Hangzhou 310024, China.

出版信息

Molecules. 2025 Feb 6;30(3):750. doi: 10.3390/molecules30030750.

DOI:10.3390/molecules30030750
PMID:39942853
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11820262/
Abstract

To discover novel, potent anti-inflammatory diterpenoids, a series of hybrids of 7-oxodehydroabietic acid bearing a 1,2,3-triazole moiety was designed and synthesized. The target compounds were characterized by means of H NMR, C NMR, and ESI-HRMS. All the compounds were evaluated for their anti-inflammatory activity towards BV2 cell lines using L-NMMA (IC = 42.36 ± 2.47 µM) as a positive control. Most showed good anti-inflammatory activities, especially compounds (IC = 8.40 ± 0.98 µM), (IC = 10.74 ± 2.67 µM), (IC = 10.96 ± 1.85 µM), and (IC = 9.76 ± 1.27 µM), which exhibited potent anti-inflammatory effects on BV2 cell lines.

摘要

为发现新型、高效的抗炎二萜类化合物,设计并合成了一系列带有1,2,3-三唑部分的7-氧代脱氢枞酸杂化物。通过1H NMR、13C NMR和ESI-HRMS对目标化合物进行了表征。以L-NMMA(IC = 42.36 ± 2.47 µM)作为阳性对照,评估了所有化合物对BV2细胞系的抗炎活性。大多数化合物表现出良好的抗炎活性,尤其是化合物(IC = 8.40 ± 0.98 µM)、(IC = 10.74 ± 2.67 µM)、(IC = 10.96 ± 1.85 µM)和(IC = 9.76 ± 1.27 µM),它们对BV2细胞系表现出强效抗炎作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/c75544b6001f/molecules-30-00750-sch003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/54626f684bfe/molecules-30-00750-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/9d9572c0e674/molecules-30-00750-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/c14259d2b0b3/molecules-30-00750-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/c75544b6001f/molecules-30-00750-sch003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/54626f684bfe/molecules-30-00750-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/9d9572c0e674/molecules-30-00750-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/c14259d2b0b3/molecules-30-00750-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b3c/11820262/c75544b6001f/molecules-30-00750-sch003.jpg

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