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Grain of high yield and quality is needed worldwide due to the needs of a rapidly increasing human population. However, diseases caused by some stubborn types of phytopathogenic bacteria can limit the health and yields of crops. Even worse, conventional commercial bactericides have limited efficacy against such diseases. Therefore, exploring some efficacious bactericidal alternatives is urgently needed. In this work, a new type of 3-(piperazin-1-yl)propan-2-ol modified carbazole derivatives was synthesized and assessed for their bactericidal activity. Among them, compound B16 was the optimal active molecule, giving the EC50 values of 3.11 (Xanthomonas oryzae pv. oryzae), 3.20 (Xanthomonas axonopodis pv. citri) and 3.54 μg/mL (Pseudomonas syringae pv. actinidiae). Pot experiments revealed compound B16 to be able to control rice bacterial leaf blight. Some biochemical assays illustrated that our designed compounds could destroy the integrality of bacterial cell membranes and thereby leading to leaking the intracellular protein. These findings may be regard as a reference for the design of novel membrane-targeting antimicrobial agents for managing stubborn plant bacterial diseases.

The increasing resistance problems of pathogens have drastically reduced the efficiency of existing drugs and agricultural chemicals, increasing the difficulty of preventing and controlling bacterial diseases. To create effective bactericide alternatives, a series of novel 3-(piperazin-1-yl)propan-2-ol decorated carbazole derivatives was fabricated, and their bioactivities and drug-likeness properties were evaluated. The in vitro bioassays showed that target molecules had outstanding antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas axonopodis pv. citri (Xac), and Pseudomonas syringae pv. actinidiae (Psa), with optimal EC50 values of 6.80 μg/mL (A9), 6.37 μg/mL (A9), and 10.75 μg/mL (A10), respectively. Furthermore, a series of biochemical assays indicated that title molecules could negatively impact the function of bacteria by irreversibly damaging their cell membranes, resulting in cytoplasmic components leakage (nucleic acids and proteins). In addition, phytotoxicity test and in silico toxicity predictions suggested that compound A9 had low phytotoxicity, and possessed acceptable drug-like properties. Our results showed that carbazole derivatives containing an 3-(piperazin-1-yl)propan-2-ol moiety were promising skeletons to develop novel bactericides with low toxicity for controlling refractory microbial diseases by targeting cell membranes.

Background Matrine is a traditional Chinese medicine with significant inhibitory activity against malignant tumors. Its effects on the invasiveness and metastasis of malignant tumors have rarely been reported. Aim To investigate whether matrine can inhibit the metastasis-related activities of the human malignant melanoma cell line A375 in vitro. Methods 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay and Annexin-V–fluorescein isothiocyanate/propidium iodide (Annexin-V-FITC/PI) affinity assay were used to examine the effects of matrine on the proliferation and apoptosis induction of A375 cells. The morphologic changes of A375 cells were observed by light and electron microscopy. Semiquantitative reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting were performed to evaluate the expression of heparanase mRNA and protein. The effect of matrine on the adhesion ability and invasiveness of treated A375 cells was tested by cell–Matrigel adhesion assay and Matrigel invasion assay, respectively. Results Matrine showed significant inhibition of the proliferation of A375 cells in a dose- and time-dependent manner. It also induced apoptosis in a dose-dependent manner. Compared with the control group, the levels of heparanase mRNA and protein expression of A375 cells treated with different concentrations of matrine were decreased significantly, as were their adhesion ability and invasiveness. Conclusions These findings indicate that matrine inhibits the invasiveness and metastasis of A375 cells in vitro. The mechanisms may be linked to the inhibition of cellular proliferation, induction of apoptosis, and downregulation of heparanase mRNA and protein expression. [ABSTRACT FROM AUTHOR]

Dyskeratosis congenita (DKC) is a rare and fatal congenital syndrome characterized by the triad of reticular skin pigmentation, nail dystrophy and mucosal leukoplakia, and the predisposition to bone marrow failure and malignancies. Mutations in DKC1 gene encoding dyskerin are responsible for the X-linked dyskeratosis congenita. Here we report mutation analysis of two Chinese pedigrees with dyskeratosis congenita. The 15 coding exons of DKC1 and their flanking regions were amplified from genomic DNA by PCR. DNA sequencing and restriction endonuclease digestion were used for mutation detection. Transition mutation of 1226C→T (P409L) found in the first pedigree is a novel mutation. In the second pedigree, the proband's mother phenotypically normal carried a de novo transition mutation of 1058C→T (A353 V) in one allele, and transmitted the mutant allele to her two sons who had typical manifestations of dyskeratosis congenita. [ABSTRACT FROM AUTHOR]

The article describes the identification of a new mutation of the TGM1 gene in a Chinese patient with the phenotype of severe lamellar ichthyosis. The 42 year old Chinese man was presented with generalized, large, gray-brown, plate-like scales covering the whole body surface including the face and flexures. He was treated with urea cream, salicylic acid cream and adapalene gel and his clinical features improved with regular follow ups.

A letter to the editor is presented in response to the article "Edematous erythema, subcutaneous plaques, and severe pain in the lower extremities in an immunocompromised patient," by YG Ding and H. Fang in issue number 2013;309(15).