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来自变种的萜类化合物及其生物活性。

Terpenoids from var. and their biological activities.

作者信息

Kim Dong Hyun, Ham Song Lim, Khan Zahra, Kim Sun Yeou, Choi Sang Un, Kim Chung Sub, Lee Kang Ro

机构信息

School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.

Department of Biopharmaceutical Convergence, Sungkyunkwan University, Suwon 16419, Republic of Korea.

出版信息

Beilstein J Org Chem. 2022 May 17;18:555-566. doi: 10.3762/bjoc.18.58. eCollection 2022.

Abstract

var. (common name: ground ivy) has been used for the treatment of asthma, bronchitis, cholelithiasis, colds, and inflammation. In the present study, three new sesquiterpene glycosides (-), two new diterpene glycosides ( and ), and four known compounds (-) were isolated from its MeOH extract. A structure elucidation was performed for the five new compounds (-) using 1D and 2D NMR, HRESIMS, DP4+ and ECD calculations, and chemical methods. All the isolates (-) were assessed for their antineuroinflammatory activities on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 cells, nerve growth factor (NGF) secretion stimulation activities in C6 glioma cells, and cytotoxic activities against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15). Compounds and - exhibited inhibitory effects on the NO production with IC values of 52.21, 47.90, 61.61, and 25.35 μM, respectively. Compound also exhibited a significant stimulating effect on NGF secretion (122.77 ± 8.10%). Compound showed potent cytotoxic activity against SK-OV-3 (IC = 3.76 μM) and SK-MEL-2 (IC = 1.48 μM) cell lines, while displayed a strong cytotoxic activity against the SK-MEL-2 (IC = 9.81 μM) cell line.

摘要

变种(俗名:欧亚活血丹)已被用于治疗哮喘、支气管炎、胆石症、感冒和炎症。在本研究中,从其甲醇提取物中分离出三种新的倍半萜糖苷(-)、两种新的二萜糖苷( 和 )以及四种已知化合物(-)。使用一维和二维核磁共振、高分辨电喷雾电离质谱、DP4 + 和电子圆二色光谱计算以及化学方法对五种新化合物(-)进行了结构解析。评估了所有分离物(-)对脂多糖(LPS)激活的BV - 2细胞中一氧化氮(NO)产生的抗神经炎症活性、对C6胶质瘤细胞中神经生长因子(NGF)分泌的刺激活性以及对四种人类癌细胞系(A549、SK - OV - 3、SK - MEL - 2和HCT15)的细胞毒性活性。化合物 和 - 对NO产生具有抑制作用,IC值分别为52.21、47.90、61.61和25.35 μM。化合物 对NGF分泌也表现出显著的刺激作用(122.77 ± 8.10%)。化合物 对SK - OV - 3(IC = 3.76 μM)和SK - MEL - 2(IC = 1.48 μM)细胞系显示出较强的细胞毒性活性,而 对SK - MEL - 2(IC = 9.81 μM)细胞系表现出较强的细胞毒性活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49f8/9127242/b9b4bfeac076/Beilstein_J_Org_Chem-18-555-g002.jpg

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