Kim Ka Hwi, Chae Jung-Il, Oh Hana, Cho Jin Hyoung, Lee Ra-Ham, Yoon Goo, Cho Seung-Sik, Cho Young-Sik, Lee Mee-Hyun, Liu Kangdong, Lee Hyun-Jeong, Shim Jung-Hyun
Department of Pharmacy, College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam 534-729, Republic of Korea.
Department of Dental Pharmacology, School of Dentistry and Institute of Oral Bioscience, BK21 Plus, Chonbuk National University, Jeonju 651-756, Republic of Korea.
Oncol Rep. 2016 Jul;36(1):117-24. doi: 10.3892/or.2016.4801. Epub 2016 May 10.
Manumycin A (Manu A) is a natural product isolated from Streptomyces parvulus and has been reported to have anti-carcinogenic and anti-biotic properties. However, neither its molecular mechanism nor its molecular targets are well understood. Thus, the aim of the present study was to explore the possibility that Manu A has cancer preventive and chemotherapeutic effects on malignant pleural mesothelioma (MPM) through regulation of Sp1 and induction of mitochondrial cell death pathway. Manu A inhibited the cell viability of MSTO-211H and H28 cells in a concentration‑dependent manner as determined by MTS assay. IC50 values were calculated as 8.3 and 4.3 µM in the MSTO-311H and H28 cells following 48 h incubation, respectively. Manu A induced a significant increase in apoptotic indices as shown by DAPI staining, Annexin V assay, multi-caspase activity and mitochondrial membrane potential assay. The downregulation of Sp1 mRNA and protein expression by Manu A led to apoptosis by suppressing Sp1-regulated proteins (cyclin D1, Mcl-1 and survivin). Manu A decreased the protein levels of BID, Bcl-xL and PARP while it increased Bax levels. Manu A caused depolarization of the mitochondrial membrane with induction of CHOP, DR4 and DR5. Our results demonstrated that Manu A exerted anticancer effects by inducing apoptosis via inhibition of the Sp1-related signaling pathway in human MPM.
马尼霉素A(Manu A)是从小球链霉菌中分离出的一种天然产物,据报道具有抗癌和抗菌特性。然而,其分子机制和分子靶点尚不清楚。因此,本研究的目的是探讨Manu A通过调节Sp1和诱导线粒体细胞死亡途径对恶性胸膜间皮瘤(MPM)具有癌症预防和化疗作用的可能性。通过MTS试验测定,Manu A以浓度依赖性方式抑制MSTO-211H和H28细胞的细胞活力。在孵育48小时后,MSTO-311H和H28细胞中的IC50值分别计算为8.3和4.3μM。如DAPI染色、膜联蛋白V测定、多胱天蛋白酶活性和线粒体膜电位测定所示,Manu A诱导凋亡指数显著增加。Manu A对Sp1 mRNA和蛋白表达的下调通过抑制Sp1调节的蛋白(细胞周期蛋白D1、Mcl-1和生存素)导致细胞凋亡。Manu A降低了BID、Bcl-xL和PARP的蛋白水平,同时增加了Bax水平。Manu A通过诱导CHOP、DR4和DR5导致线粒体膜去极化。我们的结果表明,Manu A通过抑制人MPM中Sp1相关信号通路诱导细胞凋亡发挥抗癌作用。