Oleanane triterpenes as protein tyrosine phosphatase 1B (PTP1B) inhibitors from Camellia japonica

作者: Mohammad Nasir Uddin , Govinda Sharma , Jun-Li Yang , Hong Seok Choi , Seong-IL Lim

DOI: 10.1016/J.PHYTOCHEM.2014.04.002

关键词: Breast cancerTheaceaeMedicinal plantsBiochemistryCytotoxicityCytotoxic T cellTerpeneLineweaver–Burk plotBiologyCamellia japonica

摘要: Protein tyrosine phosphatase 1B (PTP1B) plays a key role in metabolic signaling, thereby making it an exciting drug target for type 2 diabetes and obesity. Besides, there is substantial evidence that shows its overexpression involved breast cancer, which suggests selective PTP1B inhibition might be effective cancer treatment. As part of our continuous research on inhibitors from medicinal plants, four oleanane-type triterpenes were isolated EtOAc-soluble extract fruit peels Camellia japonica (Theaceae), together with 6 previously known compounds this class. Their structures determined the basis spectroscopic data analysis (UV, IR, (1)H (13)CNMR, HMBC, HSQC, NOESY, MS). All isolates evaluated their inhibitory effects PTP1B, as well cytotoxic against human cell lines MCF7, MCF7/ADR, MDA-MB-231. Several OH-3 or/and COOH-28 functionalities showed strong activity (IC50 values ranging 3.77±0.11 to 6.40±0.81 μM) significant cytotoxicity 0.51±0.05 13.55±1.44 μM).

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