A series of novel pyrazole-4-carboxamides bearing an ether group were designed and synthesized on the basis of the structure of commercial succinate dehydrogenase inhibitor (SDHI) fungicide flubeneteram via scaffold hopping and evaluated for their antifungal activities against five fungi. The bioassay results showed that most of the target compounds exhibited excellent in vitro antifungal activity against Rhizoctonia solani and some compounds exerted remarkable antifungal activities against Sclerotinia sclerotiorum, Botrytis cinerea, Fusarium graminearum, and Alternaria alternate. Particularly, compounds 7d and 12b displayed outstanding antifungal activity against R. solani, with an EC 50 value of 0.046 μg/mL, far superior to that of boscalid (EC 50 = 0.741 μg/mL) and fluxapyroxad (EC 50 = 0.103 μg/mL). Meanwhile, compound 12b also presented a broader fungicidal spectrum than other compounds. Moreover, in vivo anti-R. solani results showed that compounds 7d and 12b could significantly inhibit the growth of R. solani in rice leaves with excellent protective and curative efficacies. In addition, the results of the succinate dehydrogenase (SDH) enzymatic inhibition assay showed that compound 7d generated significant SDH inhibition, with an IC 50 value of 3.293 μM, which was about 2 times better than that of boscalid (IC 50 = 7.507 μM) and fluxapyroxad (IC 50 = 5.991 μM). Furthermore, scanning electron microscopy (SEM) analysis indicated that compounds 7d and 12b significantly destroyed the typical structure and morphology of R. solani hyphae. The molecular docking study revealed that compounds 7d and 12b could embed into the binding pocket of SDH and form hydrogen bond interactions with TRP173 and TRY58 at the activity site of SDH, which was in line with fluxapyroxad, indicating that they had a similar mechanism of action. These results demonstrated that compounds 7d and 12b could be promising candidates of SDHI fungicides, which deserved further investigation.
Stachyose (STA) is extracted from sugar beet and is used as a functional food. In this study, the effects of STA on immunosuppressed mice with intestinal mucosal damage induced by cyclophosphamide (CTX) are investigated. STA treatment can improve the amount of the leukocyte in the blood, the bone marrow cell density, and natural killer (NK) cell activity in the immunosuppressed mice. Furthermore, in immunosuppressed mice, the balance of intestinal bacteria is broken and intestinal mucosal integrity is disrupted. After treatment with STA, the amount of Enterococcus (6.504 ± 0.70) decreases and Bifidobacterium (7.207 ± 0.14) in cecum increases significantly (p < 0.05). Compared with CTX group, the ratio of villous height and crypt depth (V/C) in ileum increases from 2.525 ± 0.10 to 4.891 ± 0.16 (p < 0.001), and in jejunum increases from 2.719 ± 0.03 to 5.827 ± 0.19 (p < 0.001). The expression level of IL-2 and IL-1 gene in the spleen, and IL-1 and tumor necrosis factor alpha gene in the ileum in STA group significantly increases (p < 0.001) compared with the CTX group. In conclusion, STA is a potential prebiotic which exerts indirect and direct effects on the immune system and can counteract the side effects of CTX in the immunosuppressed mice.
In COREX operation, the Si and S contents in hot metal are relatively high and easy-fluctuating, which is one of the problems affecting the practical operation. Accurate predictions of Si and S contents can provide theoretical references for stabilizing the fluctuations and decreasing the contents of Si and S in hot metal. Therefore, the present work established the prediction model of Si and S contents in hot metal in COREX based on BP neural network. The results show that the root-mean-square errors between the predicted value and actual value for Si and S are 0.098 and 0.0037, respectively. They are 0.070 and 0.0040 when the time-sequence lapse method is adopted, which turns out to be better. Therefore, the model is accurate and reliable to predict the Si and S contents in hot metal in COREX.
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