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A series of novel 1,3,4-oxadiazole-artemisinin hybrids have been designed and synthesized. An MTT assay revealed that most of tested hybrids showed more enhanced anti-proliferative activities than artemisinin, among which A8 had the superior potency with IC50 values ranging from 4.07 μM to 9.71 μM against five tested cancer cell lines. Cell colony formation assays showed that A8 could inhibit significantly more cell proliferation than artemisinin and 5-fluorouracil. Further mechanism studies reveal that A8 induces apoptosis and ferroptosis in MCF-7 cells in a dose-dependent manner, and CYPs inhibition assays reveal that A8 has a moderate inhibitory effect on CYP1A2 and CYP3A4 in the human body at 10 μM. The present work indicates that hybrid A8 may merit further investigation as a potential therapeutic agent. [ABSTRACT FROM AUTHOR]

Large scale batch scheduling problems with complex constraints are difficult and time-consuming to solve. Therefore, this paper addresses the green batch scheduling problem on non-identical parallel machines with time-of-use electricity prices. The objective of the problem is to minimise total electricity costs (TEC) in production. Two kinds of algorithms—single-population genetic algorithms (SPGA) and multi-population genetic algorithm (MPGA)—are proposed to solve the problem. In the algorithms, the products are allocated into batches and are then allocated to machines randomly. A greedy strategy is designed to arrange the production sequence and the starting time of the batches. Furthermore, a self-adaptive parameter adjustment strategy is proposed to enhance the adaptability of the algorithm. Computational experiments with CPLEX solver have been conducted to evaluate the performance of the algorithms. On small instances, both SPGA and MPGA can achieve approximate results compared with those obtained by CPLEX, and can also achieve smaller TEC on large instances with less computing time. In addition, the proposed MPGA implemented by parallel computing outperforms SPGA in getting better results with nearly the same computing time. [ABSTRACT FROM AUTHOR]

Time-of-Use (TOU) electricity pricing provides an opportunity for industrial users to cut electricity costs. Although many methods for Economic Load Dispatch (ELD) under TOU pricing in continuous industrial processing have been proposed, there are still difficulties in batch-type processing, since power load units are not directly adjustable and nonlinearly depend on production planning and scheduling. In this paper, for hot rolling, a typical batch-type and energy intensive process in steel industry, a production scheduling optimization model for ELD is proposed under TOU pricing, in which the objective is to minimize electricity costs while considering penalties caused by jumps between adjacent slabs. A NSGA-II based multiobjective production scheduling algorithm is developed to obtain Pareto optimal solutions, and then TOPSIS based multicriteria decision-making is performed to recommend an optimal solution to facilitate field operation. Experimental results and analyses show that the proposed method cuts electricity costs in production, especially in case of allowance for penalty score increase in a certain range. Further analyses show that the proposed method has effect on peak load regulation of power grid. [ABSTRACT FROM AUTHOR]

Chemotherapy is one of the major treatment methods for cancer. However, failure in chemotherapy is not uncommon, mainly due to dose-limiting toxicity associated with drug resistance. Management of drug resistance is important towards successful chemotherapy. There are many reports in the Chinese literature that natural products can overcome cancer cell drug resistance, which deserve sharing with scientific and industrial communities. We summarized the reports into four categories: (1) in vitro studies using cell line models; (2) serum pharmacology; (3) in vivo studies using animal models; and (4) clinical studies. Fourteen single compounds were reported to have antidrug resistance activity for the first time. In vitro, compounds were able to overcome drug resistance at nontoxic or subtoxic concentrations, in a dose-dependent manner, by inhibiting drug transporters, cell detoxification capacity, or cell apoptosis sensitivity. Studies in vivo showed that single compounds, herbal extract, and formulas had potent antidrug resistance activities. Importantly, many single compounds, herbal extracts, and formulas have been used clinically to treat various diseases including cancer. The review provides comprehensive data on use of natural compounds to overcome cancer cell drug resistance in China, which may facilitate the therapeutic development of natural products for clinical management of cancer drug resistance. [ABSTRACT FROM AUTHOR]

ABSTRACT Introduction Sepsis often causes diaphragm contractile dysfunction. Dihydropyridine receptors (DHPRα1s and DHPRα1c) and ryanodine receptors (RyR1, RyR2, and RyR3) are essential for excitation-contraction coupling in striated muscles. However, their expression in diaphragm during sepsis have not been explored. Methods: Eight rats received endotoxin, and 8 more rats received placebo. After 24 hours, 3) diaphragm isometric contractile force was measured. The mRNA and protein levels of DHPRs and RyRs in diaphragm muscles were determined. Results: Sepsis weakened diaphragm contractile function. The expression levels of DHPRα1s and RyR1 were significantly lower in septic rats than in control rats. The expression levels of DHPRα1c and RyR3 were unaffected by sepsis. RyR2 was undetectable at both mRNA and protein levels in the control and sepsis groups. Conclusions: Weakened diaphragm contraction in the septic rats was associated with reduced mRNA and protein expression of DHPRα1s and RyR1, the isoforms of skeletal muscles. Muscle Nerve 48:745-751, 2013 [ABSTRACT FROM AUTHOR]