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Abstract: Free and Easy Wanderer Plus (FEWP) is a polyherbal preparation which therapeutic benefits have been extensively evaluated in patients with various depressive disorders. The purpose of this meta-analysis was to assess the overall effectiveness and safety of FEWP. Following systematic review, a total of 14 high-quality randomized controlled trials (RCTs) were identified and included in the meta-analysis. Statistically greater treatment effects were found in FEWP monotherapy compared to placebo and in FEWP combined with conventional anti-depressants (CADs) compared to CADs alone. Patients taking FEWP alone and combined with CADs experienced fewer adverse events of dizziness, headache, dry mouth, nausea, and constipation compared to CADs alone. These data suggest that FEWP may be an effective herbal agent in treating depressive symptoms. The addition of FEWP also enhances antidepressant effects of CADs. FEWP may have a higher safety profile compared to CADs. [Copyright &y& Elsevier]

A rapid and mild method for the selective hydrolysis of methyl ester in lithium chloride-N,N-dimethylformamide (LiCl-DMF) system under microwave irradiation has been developed. The effects of substituent, metal salt, and solvent on the reactivity and selectivity of the hydrolysis reaction have been investigated. Microwave irradiation significantly improves the reaction yield within a short time in an LiCl-DMF system. Moreover, the chiral α-carbon of methyl esters retained its configuration during the reaction. Finally, the catalytic mechanism of hydrolysis by LiCl salt has also been proposed. [ABSTRACT FROM AUTHOR]

Abstract: Pogonatherum paniceum (Lam.) Hack. is a rock plant with good potential for vegetative recovery on naked lands. A high frequency in vitro regeneration system was developed for P. paniceum. Calli were induced from explants of mature seeds, seedlings, young leaves, and stem segments on Murashige and Skoog (MS) medium supplemented with 1.0mgL−1 2,4-dichlorophenoxyacetic acid (2,4-D), 2.0mgL−1 α-naphthalene acetic acid (NAA) and 0.2mgL−1 6-benzylaminopurine (BAP). High induction rates (59.57%) and regeneration rates (100%) were obtained from mature seed explants; calli were sub-cultured for over 2 years and still retained a high regenerative capacity. One seed explant resulted in 69,997 plants in 1 year. Shoot buds derived from calli were used for encapsulation in liquid MS medium containing 3% sucrose and two different alginate matrices (3% sodium alginate (w/v)+MS medium containing 3% sucrose and 3% sodium alginate+1% activated carbon (w/v)+MS medium containing 3% sucrose) with a 20-min exposure to 2% CaCl2 and 0.3% bavistin (w/v). The capsule with 3.0% sodium alginate (w/v) and 1% activated carbon (w/v) showed a higher conversion rate (61.58%) and stronger plantlets under non-aseptic conditions. These systems are useful for the rapid clonal propagation and dissemination of artificial seed material of P. paniceum for eco-recovery. [Copyright &y& Elsevier]

Herein we report the discovery of a series of new small molecule inhibitors of histone lysine demethylase 4D (KDM4D). Molecular docking was first performed to screen for new KDM4D inhibitors from various chemical databases. Two hit compounds were retrieved. Further structural optimization and structure-activity relationship (SAR) analysis were carried out to the more selective one, compound 2 , which led to the discovery of several new KDM4D inhibitors. Among them, compound 10r is the most potent one with an IC 50 value of 0.41 ± 0.03 μM against KDM4D. Overall, compound 10r could be taken as a good lead compound for further studies. [ABSTRACT FROM AUTHOR]

Receptor interacting protein 1 ( RIP1) kinase plays an important role in necroptosis, and inhibitors of the RIP1 kinase are thought to have a potential therapeutic value in the treatment of diseases related to necrosis. Herein, we report the structural optimization of a RIP1 kinase inhibitor, 1-(2,4-dichlorobenzyl)-3-nitro-1 H-pyrazole ( 1a). A number of 1-benzyl-1 H-pyrazole derivatives were synthesized and structure-activity relationship ( SAR) analysis led to the discovery of a potent compound, 4b, which showed a Kd value of 0.078 μ m against the RIP1 kinase and an EC50 value of 0.160 μ m in a cell necroptosis inhibitory assay. Compound 4b also displayed considerable ability to protect the pancreas in an l-arginine-induced pancreatitis mouse model. [ABSTRACT FROM AUTHOR]

Despite a potential application of PRMT1 inhibitors in cancer treatment, very few of PRMT1 inhibitors have been reported. To obtain novel potent PRMT1 inhibitors, structure optimizations towards a hit compound, 4-((6-chloro-5-nitropyrimidin-4-yl)amino)benzimidamide, were carried out. A series of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives were synthesized. Structure–activity relationship analysis led to the discovery of a number of PRMT1 inhibitors. The most potent compound corresponds to compound 6d , which showed an IC 50 value of 2.0 μM against PRMT1. This compound also displayed a considerable anti-proliferative activity against three tumor cell lines, DLD-1, T24 and SH-SY-5Y, with IC 50 values of 4.4 μM, 13.1 μM and 11.4 μM, respectively. [ABSTRACT FROM AUTHOR]