According to the influence of the normal contact damping of joint surfaces on the dynamic characteristics of high-precision machinery (machine tool, robot, etc.), in this article, a three-dimensional fractal model of normal contact damping of dry-friction rough joint surfaces based on Hertz theory and fractal theory is established. The three-dimensional surface topography is constructed, according to the modified double variable Weierstrass–Mandelbrot function. The fractal model of strain energy , dissipated energy , damping loss factor , and normal contact damping are deduced in detail, and the influence of fractal parameters and dynamic friction coefficient on them are simulated. The simulation curves show that strain energy , dissipated energy , damping loss factor , and normal damping increase with the increase in the fractal roughness G; the influence of fractal dimension D on is more changeable, first decreases with the increase in D and then increases. , , and increase with the increase in D and , respectively; the effect of on is not obvious, so simple change in has no significant change in ; a comparative analysis of the theoretical calculation of normal damping and experimental results show that their general trend is consistent, and they increase with the increase in total normal contact load P, the relative error is 5%–25%. The theoretical model can provide reference for the design of normal contact damping of the joint surfaces.
1 December 2020 in European Journal of Medicinal Chemistry
In order to enhance the targeting efficiency and reduce the side effects and drug resistance, crizotinib (Cri) and F7 were co-loaded in a thermosensitive liposome (TSL) (F7-Cri-TSL), which showed enhanced permeability and retention in breast cancer model, as well as local controlled release by external hyperthermia. Cri is an inhibitor for cell proliferation and a promoter of apoptosis, by inhibiting the phosphorylation of intracellular ALK and c-Met, but its drug resistance limits its application. F7 is a novel drug candidate with significant resistance to cyclin-dependent kinase, but its use was restricted by its high toxicity. The F7-Cri-TSL was found with excellent particle size (about 108 nm), high entrapment efficiency (>95%), significant thermosensitive property, and good stability. Furthermore, F7-Cri-TSL/H had strongest cell lethality compared with other formulations. On the MCF-7 xenograft mice model, the F7-Cri-TSL also exhibited therapeutic synergism of Cri, F7 and hyperthermia. Meanwhile, it was shown that the TSL reduced the systemic toxicity of the chemotherapy drug. Therefore, the F7-Cri-TSL may serve as a promising system for temperature triggered breast cancer treatment.
28 January 2015 in Journal of Asian Natural Products Research
A natural xanthone, 1,3,6-trihydroxy-5-methoxyxanthone, was totally synthesized for the first time by six steps in 31% overall yield. The xanthone skeleton was formed by a one-step synthesis in 80% yield, and five of its novel derivatives were also obtained by this approach. This synthetic strategy and all the derivatives could be further used for the preparation of other natural xanthones. All the xanthones were characterized by NMR and ESI-MS, and the cytotoxicity of these xanthones was evaluated against HepG2 and HT-29 cells, and the preliminary structure-activity relationship was evaluated from the results. It was proved that the presence of 3-OH group in the molecule is crucial for its biological activity, while the presence of substituents at C-5 and C-6 may also be beneficial.