[Impact of land use pattern on water quality under different riparian buffer zone scales in Gaya River Basin, Northeast China]. / 不同河岸缓冲区尺度下土地利用方式对嘎呀河流域水质的影响.

River water quality is influenced by land use and landscape distribution patterns. Quantifying the relationship between land use, landscape pattern and water quality factor at different riparian buffer zone scales is of great significance for rational land use planning and water quality improvement. Based on water quality data from 91 sites in May 2021 in the Gaya River Basin, we analyzed the spatial characteristics of land use types and landscape patterns at the riparian buffer zone scales. With redundancy analysis (RDA) and generalized additive models (GAM), we examined the effects of land use and landscape patterns on river water quality. The results showed that water quality was primarily impacted by total nitrogen (TN). Farmland was the dominant land use type at riparian buffer zone of 50, 100 and 500 m. The sampling sites were classified into farmland dominant group and farmland other group. Forest was dominant at riparian buffer zone of 1000, 1500, 2000 m, and the sampling sites were classified into forest dominant group and forest other group. 100 m riparian buffer zone was the strongest scale in the Gaya River, and 1000 m was the second. Land use types in the forest dominant group were closely related with electrical conductivity, dissolved oxygen, phosphate, permanganate index and ammonium (NH4+-N) of water. NH4+-N was positively correlated with proportion of forest and farmland area. Phosphate was significantly affected by Shannon diversity index (SHDI). SHDI and largest patch index (LPI) was the key landscape indices affecting permanganate index. TN was significantly impacted by area proportion of forest, grassland and LPI in farmland dominant group, showing decreasing trend with the area proportion of forest increasing from 8% to 40%. Total suspended solids in farmland other group were significantly correlated with proportion of farmland area, while negatively correlated with proportion of forest area. Water quality in the Gaya River was mainly affected by proportion of forest area, followed by proportion of farmland area. The combined effects of LPI, SHDI and other land use types played an important role in affecting water quality.

Syntheses, biological activities and SAR studies of novel carboxamide compounds containing piperazine and arylsulfonyl moieties.

A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthesized. The bioassay results showed that some compounds exhibited favorable herbicidal activities against dicotyledonous plants and many of them possessed excellent antifungal activities. Among 24 novel compounds, some showed superiority over the commercial fungicides Chlorothalonil, Dimethomorph, Thiophanate-methyl, Iprodione, and Zhongshengmycin at 500 mg/L concentration. Some compounds also exhibited high KARI inhibitory activity at 100 µg/mL concentration and could be used as new KARI lead inhibitors for further studies. Moreover, SAR of these new compounds were comprehensively investigated using different computational methods in which 3D-QSAR model obtained provided useful information for further structural optimization for the discovery of new fungicides. The results of this research will contribute to explore comprehensive biological activities of piperazine-containing compounds in different areas of chemistry.

Inhibition of autophagy enhances the radiosensitivity of nasopharyngeal carcinoma by reducing Rad51 expression.

Radiotherapy has long been considered as the mainstay of treatment for nasopharyngeal carcinoma (NPC). However, locoregional recurrence or distant metastasis may occur in some patients due to the radiation resistance of cancer cells. Autophagy plays a vital role in protecting cells against radiation. However, the mechanism of autophagy in radiation therapy remains obscure. In the present study, we demonstrated that suppression of autophagy related 5 (Atg5) aggravated ionizing radiation (IR)-induced DNA damage and apoptosis in human NPC cells without accelerating the cell cycle, whereas regulation of the cell cycle has been widely regarded as the most important determinant of IR sensitivity. Further study showed that inhibition of autophagy suppressed the mRNA expression of Rad51, a key protein of homologous recombination that has been demonstrated to play a critical role in the repair of DNA double-strand breaks induced by radiation. Moreover, suppression of Atg5 had no impact on the radiosensitivity when cells were pre-treated by the Rad51 inhibitor, and the enhanced radiosensitivity by Atg5 suppression was reversed by overexpression of Rad51 in human NPC cells. Our results suggest that inhibition of autophagy enhances the susceptibility of NPC cells to radiation by reducing Rad51 expression. Therefore, Rad51 targeted therapy may be investigated as a potential novel agent for the adjuvant treatment of traditional radiation of NPC.

Design, synthesis, and fungicidal activity of novel carboxylic acid amides represented by N-benzhydryl valinamode carbamates.

Carboxylic acid amide (CAA) fungicides are an important class of agricultural fungicide with oomycete activity and low toxicity toward mammalian cells. To find CAA analogues with high activity against resistant pathogens, a series of substituted N-benzhydryl valinamide carbamate derivatives were designed and synthesized by introducing substituted aromatic rings into valinamide carbamate leads. Bioassays showed that some title compounds exhibited very good in vitro fungicidal activity against Phytophthora capsici and in vivo fungicidal activities against Pseudoperonospora cubensis. Topomer CoMFA was performed to explore the structure-activity relationship on the basis of the in vitro data. The dimethoxy substituted aromatic analogue 9e was found to display higher in vitro fungicidal activity against Phytophthora capsici than iprovalicarb but lower activity than mandipropamid, and higher in vivo fungicidal activity against Pseudoperonospora cubensis than dimethomorph at a dosage of 6.25 µg mL(-1).

Synthesis and biological evaluation of isosteric analogs of mandipropamid for the control of oomycete pathogens.

A series of isosteric analogs of mandipropamid were designed and synthesized via 'click chemistry'. The amide bond of mandipropamid was substituted by a 1,2,3-triazole functional group. The bioassay results have indicated that some of the title compounds exhibited moderate fungicidal activity against Pseudoperonospora cubensis, and the activity has been systematically studied as a function of molecular structure. The low activity of the mandipropamid analog that contains a lipid chain is likely due to the presence of a weak hydrogen bond donor in the 1,2,3-triazole. Furthermore, we have performed the molecular modeling and found that N-methylamide could be more effective than amide as the surrogates to 1,2,3-triazole, which ultimately leads to a longer distance (1.1 Å longer) between the two substitutes in the 1,4-disubstituted 1,2,3-triazole compound.