Delving into the Latest Updates on 福建省微生物研究所 with Synapse

概览

疾病领域	数量

肿瘤	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

CDC37 x HSP90	1

关联

2

项与福建省微生物研究所相关的药物

FW-04-806

靶点

CDC37 x HSP90

作用机制

CDC37拮抗剂 [+1]

在研机构

福建医科大学附属协和医院 [+1]

原研机构

福建医科大学附属协和医院 [+1]

在研适应症

乳腺癌

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

FIM-X13

靶点

mTOR

作用机制

mTOR抑制剂

在研机构-

原研机构

福建省微生物研究所

在研适应症-

非在研适应症

胃癌

最高研发阶段无进展

首次获批国家/地区-

首次获批日期-

100 项与福建省微生物研究所相关的临床结果

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0 项与福建省微生物研究所相关的专利（医药）

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183

项与福建省微生物研究所相关的文献（医药）

2024-06-01·Fitoterapia

Antimicrobial spiroketal macrolides and dichloro-diketopiperazine from Micromonospora sp. FIMYZ51

Article

作者: Jiang, Hong ; Wang, Yinuo ; Zhou, Chengzeng ; Wu, Bin ; Ge, Yichao ; Zhou, Jian ; Xie, Yang ; Zhao, Wei ; Ma, Yihan

Four compounds (1-4) featuring with an _L-rhodinose and spiroketal, possess uncommon continuous hydroxy groups in the macrolide skeleton, and a dichloro-diketopiperazine (5) were isolated from a marine derived Micromonospora sp. FIMYZ51. The determination of the relative and absolute configurations of all isolates was achieved by extensive spectroscopic analyses, single-crystal X-ray diffraction analysis, and ECD calculations. According to structural characteristic and genomic sequences, a plausible biosynthetic pathway for compound 1-4 was proposed and a spirocyclase was inferred to be responsible for the formation of the rare spirocyclic moiety. Compounds 1-4 exhibited potent antifungal activities which is equal to itraconazole against Aspergillus niger. Compounds 1-5 exhibited different degree of inhibitory activities against opportunistic pathogenic bacteria of endocarditis (Micrococcus luteus) with MIC values ranging from 0.0625 μg/mL to 32 μg/mL. Compounds 2 and 3 showed moderate cytotoxicity against drug-resistant tumor cell lines (Namalwa and U266). The result not only provides active lead-compounds, but also reveal the potential of the spirocyclase gene resources from Micromonospora sp., which highlights the promising potential of the strain for biomedical applications.

2024-04-17·Natural Product Research

Two new rakicidin derivatives from marine Micromonospora chalcea FIM-R160609

Article

作者: Liu, Wei ; Chen, Li ; Jiang, Honglei ; Zhou, Jian ; Xie, Lijun ; Lin, Feng ; Zhao, Wei ; Jiang, Hong

The establishment of structure activity relationship (SAR) for rakicidin derivatives is pretty vital to develop rakicidins as a new type of anti-cancer agents. Herein, two novel rakicidin derivatives, compounds B1-1 (1) and B1-2 (2), a cyclic depsipeptide and a chain lipopeptide, respectively, were isolated from culture broth of Micromonospora chalcea FIM-R160609, and their structures were elucidated clearly by extensive NMR and HR-ESI-MS analyses. Following, their cytotoxic activities were evaluated against HCT-8 and PANC-1 human cancer cell lines under hypoxic and normoxic conditions. Their activities were significantly decreased when compared with that of rakicidin B1. These results demonstrated that the double bond located on the position 9 and 10 of conjugated diene unit and cycle-type structure plays an important role in keeping the biological activity of rakicidins. Furthermore, the positive effect of double bond and cycle form on the anti-bacterial activities were also confirmed by testing their inhibitory activities against gram positive bacteria. This work will definitely diversify the SAR of rakicidins and provide the guidance for the design of new potent rakicidin analogues.

2024-04-01·Behavioural Brain Research

Mitophagy activation by rapamycin enhances mitochondrial function and cognition in 5×FAD mice

Article

作者: Chen, Zhou ; Li, Kualiang ; Wu, Kejun ; Zhou, Lele ; Zhong, Meihua ; Huang, Jie ; Liu, Libin ; Zheng, Wenrong

Alzheimer's disease (AD) is the most prevalent form of dementia, characterized by severe mitochondrial dysfunction, which is an intracellular process that is significantly compromised in the early stages of AD. Mitophagy, the selective removal of damaged mitochondria, is a potential therapeutic strategy for AD. Rapamycin, a mammalian target of rapamycin (mTOR) inhibitor, augmented autophagy and mitigated cognitive impairment. Our study revealed that rapamycin enhances cognitive function by activating mitophagy, alleviating neuronal loss, and improving mitochondrial dysfunction in 5 ×FAD mice. Interestingly, the neuroprotective effect of rapamycin in AD were negated by treatment with 3-MA, a mitophagy inhibitor. Overall, our findings suggest that rapamycin ameliorates cognitive impairment in 5 ×FAD mice via mitophagy activation and its downstream PINK1-Parkin pathway, which aids in the clearance of amyloid-β (Aβ) and damaged mitochondria. This study reveals a novel mechanism involving mitophagy regulation underlying the therapeutic effect of rapamycin in AD. This study provides new insights and therapeutic targets for rapamycin in the treatment of AD. However, there are still some shortcomings in this topic; if we can further knock out the PINK1/Parkin gene in animals or use siRNA technology, we can further confirm the experimental results.

100 项与福建省微生物研究所相关的药物交易

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100 项与福建省微生物研究所相关的转化医学

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