Hu C.-L.,Fudan University |
Xiong J.,Fudan University |
Li J.-Y.,Fudan University |
Gao L.-X.,CAS Shanghai Institute of Materia Medica |
And 5 more authors.
European Journal of Organic Chemistry | Year: 2016
Two rare rearranged cuparane-type sesquiterpenoid C-10 epimers [beshanzuenones A (1) and B (2)] and two bisabolane-type sesquiterpenoid spirolactones [beshanzuenones C (3) and D (4)] featuring an unusual [6/6/5]-fused tricyclic ring system were isolated from the shed trunk barks of Abies beshanzuensis, one of the critically endangered plant species in the world. The structures of these four new enone-containing sesquiterpenoids were determined by spectroscopic analyses and single-crystal X-ray diffraction or electronic circular dichroism (ECD) calculations. Compounds 1 and 2 showed considerable activity against the H3N2 virus, whereas 3 and 4 exhibited significant inhibition on PTP1B. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
PubMed | University of Science and Technology of China, Lishui Institute of Agricultural science Lishui and Zhejiang Chinese Medical University
Type: Journal Article | Journal: American journal of translational research | Year: 2016
Overexpression of ABCB1 in cancer cells is one of the main reasons of cancer multidrug resistance (MDR). Wallichinine is a compound isolated from piper wallichii and works as an antagonist of platelet activiating factor receptor to inhibit the gathering of blood platelet. In this study, we investigate the effect of wallichinine on cancer MDR mediated by ABCB1 transporter. Wallichinine significantly potentiates the effects of two ABCB1 substrates vincristine and doxorubicin on inhibition of growth, arrest of cell cycle and induction of apoptosis in ABCB1 overexpressing cancer cells. Furthermore, wallichinine do not alter the sensitivity of non-ABCB1 substrate cisplatin. Mechanistically, wallichinine blocks the drug-efflux activity of ABCB1 to increase the intracellular accumulation of rhodamine 123 and doxorubicin and stimulates the ATPase of ABCB1 without alteration of the expression of ABCB1. The predicted binding mode shows the hydrophobic interactions of wallichinine within the large drug binding cavity of ABCB1. At all, our study of the interaction of wallichinine with ABCB1 presented herein provides valuable clues for the development of novel MDR reversal reagents from natural products.