PROCESS BIOCHEMISTRY
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2021
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IF 3.757
Lining Zheng,Cheng Zhang,Xian Wu,Ling Liu,Hao Zhang
Tomato gray mold, caused by Botrytis cinerea , is one of the most devastating diseases affecting tomato plants. In this study, Pantoea jilinensis D25 fermentation broth (PJFB) was used to inhibit B. cinerea growth. The optimum fermentation time was 7 days. PJFB antifungal activity decreased when PJFB was heated to ≥60°C, whereas it was the strongest at pH 8. Moreover, ultraviolet treatment for a long time reduced its antifungal effect. PJFB, applied at 10 % (v/v), could inhibit B. cinerea growth by inhibiting its mycelial diameter, conidial production, and mycelial dry weight with the inhibition rates of 57.3 %, 51.2 %, and 78.6 %, respectively. PJFB could also increase conductivity and malondialdehyde (MDA) content in B. cinerea . Furthermore, PJFB inhibited B. cinerea on not only the leaf tissues but also the seedlings of tomato. The secondary metabolites in PJFB were determined through gas chromatography–mass spectrometry. Through laboratory toxicity analysis, we found that the major compounds in PJFB were 1,2-benzenedicarboxylic acid bis(2-methylpropyl) ester (14.3098 %), 2,4-di- tert -butylphenol (3.8036 %), 2,6,10,14-tetramethyl pentadecane (2.9947 %), and 1,3-dimethyl naphthalene (1.8586 %).
研究领域:
植物病理学
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微生物学
✓ 已验证
DOI
高影响因子
JOURNAL OF MEDICINAL CHEMISTRY
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2024
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IF 6.8
Qiang Li,Linmao Ke,Dandan Yu,Han Xu,Zixuan Zhang,Rilei Yu,Tao Jiang,Yue-Wei Guo,Mingzhi Su,Xin Jin
Mitogen-activated protein kinase-interacting protein kinases (MNKs) and phosphorylate eukaryotic initiation factor 4E (p-eIF4E) play a critical role in regulating mRNA translation and protein synthesis associated with the development of cancer, metabolism, and inflammation. This study undertakes the modification of a 4-(3-(piperidin-4-yl)-1H-pyrazol-5-yl)pyridine structure, leading to the discovery of 4-(3-(piperidin-4-yl)-1H-pyrazol-5-yl)-1H-pyrrolo[2,3-b]pyridine (D25) as a potent and selective MNK inhibitor. D25 demonstrated inhibitory activity, with IC50 values of 120.6 nM for MNK1 and 134.7 nM for MNK2, showing exceptional selectivity. D25 inhibited the expression of pro-inflammation cytokines in RAW264.7 cells, such as inducible NO synthase, cyclooxygenase-2, and interleukin-6 (IL-6). In the lipopolysaccharide-induced sepsis mouse model, D25 significantly reduced p-eIF4E in spleen tissue and decreased the expression of tumor necrosis factor α, interleukin-1β, and IL-6, and it also reduced the production of reactive oxygen species, resulting in improved organ injury caused by inflammation. This suggests that D25 may provide a potential treatment for sepsis and sepsis-associated acute spleen injury.
研究领域:
药理学
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免疫学
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传染病
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF MEDICINAL CHEMISTRY
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2025
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IF 6.8
Qiang Li,Cunrui Li,Yuanmin Chang,Mingzhi Su,Rilei Yu,Zhangjian Huang,Yue-Wei Guo,Xin Jin
The inhibition of Rho-associated coiled-coil kinase (ROCK) has emerged as a promising strategy for reducing intraocular pressure (IOP) and treating glaucoma. Here, we report the synthesis and evaluation of novel ROCK inhibitors, D25 and R3, which were designed to optimize selectivity, efficacy, and ocular bioavailability. D25 potently inhibited ROCK1/2 with IC50 values of 47.2 nM and 33.8 nM, respectively, surpassing Netarsudil. Compound R3 had weaker ROCK inhibition but demonstrated favorable lipophilicity (logP) and good selectivity to ROCKs, which enhances its potential and safety for ocular delivery. In human trabecular meshwork (HTM) cells, R3 showed lower cytotoxicity than Netarsudil and effectively mitigated oxidative damage, enhanced cellular integrity, and reduced inflammatory cytokine secretion. In rabbit models, D25 significantly lowered IOP, outperforming (S)-Netarsudil. R3 exhibited weaker IOP-lowering efficacy but better selectivity. D25 is a promising glaucoma treatment candidate, with R3 as a safer alternative for further optimization.
研究领域:
药理学
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眼科
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）