Shakeri Abolfazl, Amini Elaheh, Asili Javad, Masullo Milena, Piacente Sonia, Iranshahi Mehrdad
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.
Nat Prod Res. 2018 Jun;32(12):1436-1440. doi: 10.1080/14786419.2017.1344661. Epub 2017 Jun 23.
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.
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。