Synthetic chalcones with potent antioxidant ability on H2O2-induced apoptosis in PC12 cells.

Chalcone derivatives (E)-3-(4-hydroxy-3-methoxyphenyl)-1-(4-methoxyphenyl) prop-2-en-1-one and (E)-3-(4-hydroxyphenyl)-1-(4-methoxyphenyl) prop-2-en-1-one (Compounds 1 and 2) have been demonstrated to be potent anti-inflammatory agents in our previous study. In light of the relationship of intracellular mechanisms between anti-inflammatories and antioxidants, we further designed and synthesized a series of chalcone derivatives based on 1 and 2, to explore their antioxidant efficacy. The majority of the derivatives exhibited strong protective effects on PC12 (PC12 rat pheochromocytoma) cells exposed to H2O2, and all compounds were nontoxic. A preliminary structure-activity relationship was proposed. Compounds 1 and 1d ((E)-2-methoxy-4-(3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl) phenyl acrylate) exerted the action in a good dose-dependent manner. Quantitative RT-PCR (qRT-PCR) and western blot analysis showed that 1 and 1d significantly improve the expression of nuclear factor erythroid 2 p45-related factor 2 (Nrf2)-dependent antioxidant genes g-Glutamylcysteine Ligase Catalytic Subunit (GCLC) and heme oxygenase-1 (HO-1) and their corresponding proteins (γ-glutamyl cysteine synthase (γ-GCS) and HO-1) in PC12 cells. Inhibition of GCLC and HO-1 by specific inhibitors, L-buthionine-S-sulfoximine (BSO) and zinc protoporphyrin (ZnPP), respectively, partially reduce the protective effect of 1 and 1d. These data present a series of novel chalcone analogs, especially compounds 1 and 1d, as candidates for treating oxidative stress-related disease by activating the Nrf2-antioxidant responsive element (ARE) pathway.

[Effects of low intensity resistance training of blood flow restriction with different occlusion pressure on lower limb muscle and cardiopulmonary function of college students].

Objective: The study compared the effects of low intensity resistance training with blood flow restriction (BFR) with different occlusion pressure on lower limb muscle and cardiopulmonary function. Methods: Twenty-seven college students were randomly divided into three groups by different occlusion pressure: 0 mmHg (group C), 120 mmHg (group L) and 180 mmHg (group H). Before and after training (3 times a week for 12 weeks) with an inflatable cuff (20% 1RM, half squat), the muscle thickness(MTH)of rectus femoris and medius femoris, relative peak knee extensor moment(rM), peak power(P), relative maximal oxygen uptake(rVO2max), stroke volume(SV), cardiac output(CO), ejection fraction(EF) and other indicators were measured for all subjects. Results: When compared with pre-training, and rectus femoris, the MTH of medius femoris, rM, rVO2max, SV, CO and EF were significantly increased in group L and group H after 12 weeks training(P＜0.05, P＜0.01), as well as compared with group C after training(P＜0.05, P＜0.01). There was no significant difference between group L and group H after training. Conclusion: BFR training protocols under 120 mmHg or 180 mmHg pressure were effective in improving muscle and cardiopulmonary function.

Curcumin analogue A501 induces G2/M arrest and apoptosis in non-small cell lung cancer cells.

Curcumin and its analogues have been reported to exert anti-cancer activity against a variety of tumors. Here, we reported A501, a new curcumin analogue. The effect of A501 on cell viability was detected by MTT assay, the result showed that A501 had a better inhibiting effect on the four non-small cell lung cancer (NSCLC) cells than that of curcumin. Moreover, Colony forming experiment showed A501 significant restrained cell proliferation. Flow cytometry displayed A501 can cause G2/M arrest and induce apoptosis. Western blotting showed that A501 decreased the expression of cyclinB1, cdc-2, bcl-2, while increased the expression of p53, cleaved caspase-3 and bax. In conclusion, curcumin analogues A501 played antitumor activity by inhibiting cell proliferation and inducing apoptosis of NSCLC cells. And it was likely to be a promising starting point for the development of curcumin-based anticancer drugs.