Abstract
Betula platyphylla bark has been evaluated for the treatment of dermatitis, inflammatory conditions, and cancer. Diarylheptanoids are the major constituents of the B. platyphylla bark and possess various pharmacological effects. Our previous study confirmed the selective antiproliferative effect of platyphylloside (BPP) isolated from B. platyphylla on colon cancer and leukemic cells using 60 different cancer cell lines from thr National Cancer Institution (NCI). In line with previous reports, this study focuses on the apoptotic pathway of BPP, a phenolic glycoside composed of two aromatic rings joined by a seven-carbon chain. Cytotoxicity assays in solid tumor and blood cancer cell models demonstrated that BPP possesses potent antiproliferative activity. The level of apoptosis increased with BPP treatment, causing cell cycle arrest at the G1 phase along with the downregulation of IκBα phosphorylation and BCL-2, as well as upregulation of cleaved caspase 3 and BAX proteins. In addition, BPP displayed potent mitochondrial depolarization effects in Jurkat cells. The combined findings revealed that the cytotoxic effects of BPP were mediated by intracellular signaling, possibly through a mechanism involving the upregulation of mitochondrial reactive oxygen species (ROS). Thus, BPP could be a potential multitarget therapeutic agent in leukemia and colon cancer.
Highlights
Cancer is the second leading cause of death in the United States, and colorectal cancer (CRC) is one of the most common cancers in both men and women worldwide [1]
We employed solid tumor and blood cancer cell lines to evaluate the potential of BPP as a multitarget therapeutic agent, in both colon cancer and leukemia
We found that BPP downregulated the response to BPP (20 μM) treatment were analyzed using western blots (WB)
Summary
Cancer is the second leading cause of death in the United States, and colorectal cancer (CRC) is one of the most common cancers in both men and women worldwide [1]. In Korea, cancer headed the list of the top 10 leading causes of death, and colorectal cancer (CRC) is the third most common cancer in men and women, with more than one million cases diagnosed each year worldwide [2]. Chemotherapeutic regimens, including 5-fluorouracil (5-FU), oxaliplatin, and irinotecan, are reportedly efficacious in colon cancer [3]. Additional targeted agents, including anti-EGFR or anti-VEGF antibodies, are considered to be effective in metastatic CRC cases (mCRC) [3]. Leukemia is a type of blood cancer that usually begins in the bone marrow and results in high abnormal blood cell counts. The four main leukemia types include acute lymphocytic leukemia or acute lymphoblastic leukemia (ALL), chronic lymphocytic leukemia (CLL), acute myelocytic leukemia (AML), and chronic myelocytic leukemia or Molecules 2019, 24, 2960; doi:10.3390/molecules24162960 www.mdpi.com/journal/molecules
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