Author: Zhu, Qihua ; Song, Zhe ; Xu, Yungen ; Zou, Yi ; Shi, Shi ; Shao, Jialu ; Wufoyrwoth, Shepherd ; Yang, Jieping ; Gu, Hongfeng ; Lai, Wenwen ; Huang, Lei

The first examples of ataxia telangiectasia and Rad3-related (ATR) PROTACs were designed and synthesized. Among them, the most potent degrader, ZS-7, demonstrated selective and effective ATR degradation in ATM-deficient LoVo cells, with a DC₅₀ value of 0.53 μM. Proteasome-mediated ATR degradation by ZS-7 lasted approximately 12 h after washout in the LoVo cell lines. Notably, ZS-7 demonstrated reasonable PK profiles and, as a single agent or in combination with cisplatin, showed improved antitumor activity and safety profiles compared with the parent inhibitor AZD6738 in a xenograft mouse model of LoVo human colorectal cancer cells upon intraperitoneal (i.p.) administration.

10 Sep 2014·Journal of Agricultural and Food ChemistryQ1 · AGRICULTURAL & FORESTRY SCIENCE

Phytotoxic and Antibacterial Metabolites from Fusarium proliferatum ZS07 Isolated from the Gut of Long-horned Grasshoppers

Q1 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: Kong, Li-Chun ; Zhang, Ying-Lao ; Li, Shuai ; Lu, Yi-Hui ; Shao, Ming-Wei ; Jiang, Dong-Hua

In the proceeding of screening new bioactive natural products, the ethyl acetate extract of the fermentation broth of Fusarium proliferatum ZS07, a fungus residing in the gut of long-horned grasshoppers (Tettigonia chinensis), was found possessing selective phytotoxic activity against the radicle growth of Amaranthus retroflexus L. Bioactivity-guided fractionation lead to the isolation of six fungal metabolites 1-6, including a new polyketide derivate O-methylated SMA93 (2) and five known compounds SMA93 (1), rhodolamprometrin (3), radicinin (4), dehydroallogibberic acid (5), and 3-methyl-6,8-dihydroxyisocoumarin (6). Their structures were identified on the basis of spectroscopic analysis and by comparison of the corresponding data to those reported in the literature previously. Phytotoxic effects of the four isolated compounds 1-4 on the radicle growth of A. retroflexus L. seeds were investigated under laboratory conditions, and compounds 2 and 4 showed good phytotoxic activity in the concentration of 100 μg/mL, with the inhibition rates of 83.0 and 65.2%, respectively. Furthermore, the antibacterial activity of compounds 1-5 were evaluated against selected bacteria. Compounds 1-3 were found to possess potent antibacterial activity against Bacillus subtilis (ATCC 6633), with the minimum inhibitory concentration (MIC) values of 3.13-12.50 μg/mL, while Escherichia coli (ATCC 8739) and Salmonella typhimurium [CMCC(B) 50115] were not susceptible. These results suggest that the new polyketide derivate 2 and known compounds 1, 3, and 4 have potential to be used as biocontrol agents in agriculture.

01 Jan 2013·BioMed Research InternationalQ3 · BIOLOGY

Probiotic Potential and Safety Properties ofLactobacillus plantarumfrom Slovak Bryndza Cheese

Q3 · BIOLOGY

ArticleOA

Author: Belicová, Anna ; Dušinský, Roman ; Mikulášová, Mária

One hundred and twenty-five acid-resistant presumptive lactobacilli were isolated from Slovak Bryndza cheese and screened for their antimicrobial activity against eight bacterial pathogens using spot agar assay. Out of twenty-sixLactobacillusstrains with strong inhibition activity, twenty were identified asLactobacillus plantarumand six asLactobacillus fermentum. The most active elevenL. plantarumisolates were further characterizedin vitrofor some probiotic and safety properties. Only three isolates K10, K21, and ZS07 showed the ability to grow over 50% in the presence of 0.3% bile. Strong deconjugation efficiency was determined for CK06 and K21. The highestβ-galactosidase activity was shown in isolates ZS11, B01, CK06, and ZS07. Only three of the strains had the ability to produce tyramine: CK06, LM1, and ZS11. Strains K09, K21, ZS11, and ZS15 were susceptible to all tested antibiotics. Analysis of the results confirmed theL. plantarumisolates ZS07 and K21 as the most suitable for probiotic use, due to their desirable probiotic and safety characteristics.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	IND Application	CN	Zensun (Shanghai) Sci & Tech Co., Ltd.	30 Jan 2022

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