Dark red crystals
Salvia quinone/Phenanthro[1,2-b]furan-10,11-dione, 1,6-dimethyl-/Tanshinone/Tanshinon I/tanshinone-I/Tanshinone 1/1,6-Dimethylphenanthro[1,2-b]furan-10,11-dione/TANSHINONES IIA/Tanshinquinone I/Tanshine I
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provides coniferyl ferulate(CAS#:568-73-0) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Vascular smooth muscle cell (VSMC) proliferation plays a critical role in arterial remodeling during various vascular diseases including atherosclerosis and hypertension. Tanshinone I, a major component of Salvia miltiorrhiza, exerts protective effects against cardiovascular diseases. In this study, we investigated the effects of tanshinone I on VSMC proliferation, as well as the underlying mechanisms. We found that this compound inhibited the proliferation of VSMCs in a dose-dependent manner, based on 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) and 5-ethynyl-2′-deoxyuridine (EdU) assays. Western blotting demonstrated that tanshinone I inhibited the expression of proliferation-related proteins, including cyclin-dependent kinase 4 (CDK4), cyclin D3, and cyclin D1, in a dose-dependent manner. Molecular docking showed that this compound docked to the inhibitor-binding site of the insulin-like growth factor 1 (IGF-1) receptor (IGF-1R), and the binding energy between tanshinone I and IGF-1R was -9.021 kcal/mol. Molecular dynamic simulations showed that the IGF-1R-tanshinone I binding was stable. We also found that tanshinone I dose-dependently inhibited IGF-1R activation and its downstream molecules, insulin receptor substrate (IRS)-1, phosphatidylinositol-3-Kinase (PI3K), Akt, glycogen synthase kinase-3 beta (GSK3β), mammalian target of rapamycin (mTOR), 70S6K, and ribosomal protein S6 (RPS6). Notably, activation of IGF-1R by recombinant IGF-1 rescued the activity of IGF-1R and its downstream molecules, and the proliferation of tanshinone I-treated VSMC. In addition, blocking PI3K signaling with LY294002 showed the important role of this pathway in tanshinone I-mediated suppression of VSMC proliferation. Collectively, these data demonstrated that tanshinone I might inhibit VSMC proliferation by inhibiting IGF-1R/PI3K signaling.
Copyright © 2019. Published by Elsevier B.V.
Akt; GSK3β; IGF-1R; PI3K; Proliferation; Tanshinone I; Vascular smooth muscle cell; mTOR
Tanshinone I inhibits vascular smooth muscle cell proliferation by targeting insulin-like growth factor-1 receptor/phosphatidylinositol-3-kinase signaling pathway.
Wu YT1, Bi YM1, Tan ZB1, Xie LP1, Xu HL1, Fan HJ1, Chen HM1, Li J1, Liu B2, Zhou YC3.
2019 Jun 15
A novel total synthesis of tanshinone I (1) via the intermediate 3-hydroxy-8-methyl-1,4-phenanthrenedione (8) is described. The low overall yields and the use of expensive reagents in the synthesis process were minimized by the use of the Diels-Alder reaction to directly construct the 1,4-phenanthrenedione scaffold, providing tanshinone I (1) in only three steps.
Total Synthesis of Tanshinone I.
Wu N1, Ma WC1, Mao SJ1, Wu Y1, Jin H1.
2017 May 26
Tanshinone I (Tan I) is a widely used diterpene compound derived from the traditional Chinese herb Danshen. Increasing evidence suggests that it exhibits anti-cancer activity in various human cancers. However, the in vitro and in vivo effects of Tan I on osteosarcoma (OS) remain inadequately elucidated, especially those against tumour metastasis. Our results showed that Tan I significantly inhibited OS cancer cell proliferation, migration and invasion and induced cell apoptosis in vitro. Moreover, treatment with 10 and 20 mg/kg Tan I effectively suppressed tumour growth in subcutaneous xenografts and orthotopic xenograft mouse models. In addition, Tan I significantly inhibited tumour metastasis in intracardiac inoculation xenograft models. The results also showed that Tan I-induced increased expression of the proapoptotic gene Bax and decreased expression of the anti-apoptotic gene Bcl-2 is the possible mechanism of its anti-cancer effects. Tan I was also found to abolish the IL-6-mediated activation of the JAK/STAT3 signalling pathway. Conclusively, this study is the first to show that Tan I suppresses OS growth and metastasis in vitro and in vivo, suggesting it may be a potential novel and efficient drug candidate for the treatment of OS progression.
© 2019 The Authors. Journal of Cellular and Molecular Medicine published by John Wiley & Sons Ltd and Foundation for Cellular and Molecular Medicine.
JAK/STAT3 signalling pathway; osteosarcoma; tanshinone I; tumour growth and metastasis
Tanshinone I inhibits the growth and metastasis of osteosarcoma via suppressing JAK/STAT3 signalling pathway.
Wang W1, Li J1, Ding Z1, Li Y1, Wang J1, Chen S1, Miao J1.
Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).