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对从山矢车菊(Centaurea behen L.)和绵毛火绒草(Rhaponticum repens (L.) Hidalgo)中分离得到的不同倍半萜内酯诱导的几种生物活性进行筛选。

Screening of several biological activities induced by different sesquiterpene lactones isolated from Centaurea behen L. and Rhaponticum repens (L.) Hidalgo.

作者信息

Shakeri Abolfazl, Amini Elaheh, Asili Javad, Masullo Milena, Piacente Sonia, Iranshahi Mehrdad

机构信息

a Department of Pharmacognosy , School of Pharmacy, Mashhad University of Medical Sciences , Mashhad , Iran.

b Department of Animal Biology, Faculty of Biological Sciences , Kharazmi University , Tehran , Iran.

出版信息

Nat Prod Res. 2018 Jun;32(12):1436-1440. doi: 10.1080/14786419.2017.1344661. Epub 2017 Jun 23.

Abstract

This study aims to evaluate the in vitro cytotoxic, in vitro and in ovo anti-angiogenic effects and antimicrobial activity of sesquiterpene lactones (SLs) from two plants Centaurea behen and Rhaponticum repens (L.). Five SLs, including cynaropicrin (1), 4β,15-dehydro-3-dehydrosolstitialin A (2), aguerin B (3), janerin (4), cebellin E (5), and a flavone hispidulin (6) were isolated from C. behen (compounds 1-3) and R. repens (compounds 4-6). Cynaropicrin (1) and aguerin B (3) were characterised by strong cytotoxic activities against A2780 cells with IC values of 1.15 and 1.62 μg mL, respectively, comparable to that of doxorubicin (IC = 1.17 μg mL). The anti-angiogenic study showed the remarkable inhibitory effect of cynaropicrin (1) and aguerin B (3) on the proliferation and migration of HUVECs. In addition, cynaropycrin and aguerin B exhibited significant angio-inhibitory effects in CAM assay. These findings may be useful for the development of novel chemotherapeutic agents for the treatment of cancer.

摘要

本研究旨在评估来自两种植物——披针叶矢车菊(Centaurea behen)和新疆款冬(Rhaponticum repens (L.))的倍半萜内酯(SLs)的体外细胞毒性、体外和卵内抗血管生成作用以及抗菌活性。从披针叶矢车菊(化合物1 - 3)和新疆款冬(化合物4 - 6)中分离出了5种SLs,包括菜蓟苦素(1)、4β,15 - 脱氢 - 3 - 去氢异土木香内酯A(2)、阿尔泰款冬素B(3)、雅内里因(4)、策贝林E(5)以及一种黄酮类化合物滨蓟黄素(6)。菜蓟苦素(1)和阿尔泰款冬素B(3)对A2780细胞具有很强的细胞毒性活性,IC值分别为1.15和1.62 μg/mL,与阿霉素(IC = 1.17 μg/mL)相当。抗血管生成研究表明,菜蓟苦素(1)和阿尔泰款冬素B(3)对人脐静脉内皮细胞(HUVECs)的增殖和迁移具有显著的抑制作用。此外,菜蓟苦素和阿尔泰款冬素B在鸡胚绒毛尿囊膜(CAM)试验中表现出显著的血管抑制作用。这些发现可能有助于开发用于治疗癌症的新型化疗药物。

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