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"Zhao, Jin-Xin"
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Design, Synthesis, and Biological Evaluation of HDAC Inhibitors Containing Natural Product-Inspired N-Linked 2-Acetylpyrrole Cap
2024
Drawing inspiration from the structural resemblance between a natural product N-(3-carboxypropyl)-2-acetylpyrrole and phenylbutyric acid, a pioneer HDAC inhibitor evaluated in clinical trials, we embarked on the design and synthesis of a novel array of HDAC inhibitors containing an N-linked 2-acetylpyrrole cap by utilizing the pharmacophore fusion strategy. Among them, compound 20 exhibited potential inhibitory activity on HDAC1, and demonstrated notable potency against RPMI-8226 cells with an IC50 value of 2.89 ± 0.43 μM, which was better than chidamide (IC50 = 10.23 ± 1.02 μM). Western blot analysis and Annexin V-FTIC/propidium iodide (PI) staining showed that 20 could enhance the acetylation of histone H3, as well as remarkably induce apoptosis of RPMI-8226 cancer cells. The docking study highlighted the presence of a hydrogen bond between the carbonyl oxygen of the 2-acetylpyrrole cap group and Phe198 of the HDAC1 enzyme in 20, emphasizing the crucial role of introducing this natural product-inspired cap group. Molecular dynamics simulations showed that the docked complex had good conformational stability. The ADME parameters calculation showed that 20 possesses remarkable theoretical drug-likeness properties. Taken together, these results suggested that 20 is worthy of further exploration as a potential HDAC-targeted anticancer drug candidate.
Journal Article
Genomic Analysis and Characterization of Pseudotabrizicola formosa sp. nov., a Novel Aerobic Anoxygenic Phototrophic Bacterium, Isolated from Sayram Lake Water
by
Ye, Yu-Qi
,
Zhao, Jin-Xin
,
Han, Ji-Ru
in
aerobic anoxygenic phototrophic bacteria
,
anoxygenic photosystem II
,
Aquatic environment
2022
Aerobic anoxygenic photosynthetic bacteria (AAPB) are a kind of heterotrophic prokaryote that can use bacteriochlorophyll (BChl) for photosynthesis without oxygen production and they are widely distributed in aquatic environments, including oceans, lakes, and rivers. A novel aerobic anoxygenic photosynthetic bacterium strain XJSPT was isolated during a study of water microbial diversity in Sayram Lake, Xinjiang Province, China. Strain XJSPT was found to grow optimally at 33 °C, pH 7.5 with 1.0% (w/v) NaCl, and to produce bacteriochlorophyll a and carotenoids. Phylogenetic analysis based on 16S rRNA gene sequence and concatenated alignment sequences of 120 ubiquitous single-copy proteins both supported that strain XJSPT belonged to the genus Pseudotabrizicola. Both average nucleotide identity (ANI) and DNA–DNA hybridization (DDH) values were below the species delineation threshold. The primary polar lipids were phosphatidylcholine, phosphatidylglycerol, phosphatidylethanolamine, one unknown lipid, and one unidentified phospholipid. Based on the results of polyphasic analyses performed in this study, strain XJSPT represents a new member of the genus Pseudotabrizicola, for which the name Pseudotabrizicola formosa sp. nov. is proposed. The type strain is XJSPT (= KCTC 52636T = MCCC 1H00184T = SDUM 107003T). Comparative genomic analysis showed that four species of the genus Pseudotabrizicola shared 2570 core genes and possessed a complete anoxygenic photosystem II.
Journal Article
Digestive Tract Morphology and Gut Microbiota Jointly Determine an Efficient Digestive Strategy in Subterranean Rodents: Plateau Zokor
2022
Rodents’ lifestyles vary in different environments, and to adapt to various lifestyles specific digestion strategies have been developed. Among these strategies, the morphology of the digestive tracts and the gut microbiota are considered to play the most important roles in such adaptations. However, how subterranean rodents adapt to extreme environments through regulating gut microbial diversity and morphology of the digestive tract has yet to be fully studied. Here, we conducted the comparisons of the gastrointestinal morphology, food intake, food assimilation, food digestibility and gut microbiota of plateau zokor Eospalax baileyi in Qinghai-Tibet Plateau and laboratory rats Rattus norvegicus to further understand the survival strategy in a typical subterranean rodent species endemic to the Qinghai-Tibet Plateau. Our results revealed that plateau zokor evolved an efficient foraging strategy with low food intake, high food digestibility, and ultimately achieved a similar amount of food assimilation to laboratory rats. The length and weight of the digestive tract of the plateau zokor was significantly higher than the laboratory rat. Particularly, the weight and length of the large intestine and cecum in plateau zokor is three times greater than that of the laboratory rat. Microbiome analysis showed that genus (i.e., Prevotella, Oscillospira, CF231, Ruminococcus and Bacteroides), which are usually associated with cellulose degradation, were significantly enriched in laboratory rats, compared to plateau zokor. However, prediction of metagenomic function revealed that both plateau zokor and laboratory rats shared the same functions in carbohydrate metabolism and energy metabolism. The higher digestibility of crude fiber in plateau zokor was mainly driven by the sizes of cecum and cecum tract, as well as those gut microbiota which associated with cellulose degradation. Altogether, our results highlight that both gut microbiota and the morphology of the digestive tract are vital to the digestion in wild rodents.
Journal Article
1,2-Difunctionalized bicyclo1.1.1pentanes
by
Spangler, Jillian E.
,
Montgomery, T. Patrick
,
He, Chi
in
Aromatic compounds
,
Benzene
,
Biological Assay
2021
The development of a versatile platform for the synthesis of 1,2-difunctionalized bicyclo[1.1.1]pentanes to potentially mimic ortho/meta-substituted arenes is described. The syntheses of useful building blocks bearing alcohol, amine, and carboxylic acid functional handles have been achieved from a simple common intermediate. Several ortho- and meta-substituted benzene analogs, as well as simple molecular matched pairs, have also been prepared using this platform. The results of in-depth ADME (absorption, distribution, metabolism, and excretion) investigations of these systems are presented, as well as computational studies which validate the ortho- or meta-character of these bioisosteres.
Journal Article
Natural products inspired 3 + 2 cycloaddition enables efficient construction of hydroxylated tetrahydrofuran acetals and concise syntheses of lignans
2024
Mimicking biosynthetic pathways of hongkonoids led to the development of a new Cu(I)-catalyzed [3 + 2] cycloaddition of α-hydroxyketone and β-keto enol ethers, affording tetrahydrofuran acetals in a highly diastereoselective manner and 100% atom economy. Computational studies on the mechanism disclosed a concerted but asynchronous Michael addition/aldol reaction. Of the same importance, this methodology provides a practical biomimetic approach for one-step construction of the dibenzylbutyrolactol lignan backbone starting from two phenyl propane derivatives, opening up a powerful new approach for lignan synthesis, which is showcased by succinct total syntheses of two biologically important aryltetralin-type lignans, β-apopicropodophyllin and cycloolivil. Given the mild and operationally simple conditions, the developed chemistry might have a promising prospect in potential industrial applications.
Journal Article
Kordiimonas sediminis sp. nov., isolated from a sea cucumber culture pond
by
Zhang, Heng-Xi
,
Chen, Guan-Jun
,
Zhao, Jin-Xin
in
Alphaproteobacteria - classification
,
Alphaproteobacteria - genetics
,
Alphaproteobacteria - growth & development
2016
A marine bacterium, designated strain N39ᵀ, was isolated from a sediment sample collected at a sea cucumber culture pond in Weihai, China. Cells of strain N39ᵀ were observed to be Gram-stain negative, facultatively anaerobic, motile rods showing catalase and oxidase negative reactions. Strain N39ᵀ was found to grow optimally at pH 8.0–8.5, 35–37 °C and in the presence of approximately 3.0 % (w/v) NaCl. Phylogenetic analysis based on 16S rRNA gene sequences indicated that strain N39ᵀ belongs to the genus Kordiimonas in the family Kordiimonadaceae, appearing closely related to Kordiimonas lacus JCM 16261ᵀ (95.9 %), Kordiimonas aquimaris MEBiC06554ᵀ (95.1 %), Kordiimonas gwangyangensis JCM 12864ᵀ (94.2 %) and Kordiimonas aestuarii 101-1ᵀ (93.8 %). Ubiquinone 10 (Q-10) was found to be the major respiratory quinone. The dominant cellular fatty acids were identified as iso-C₁₇:₁ ω9c, iso-C₁₇:₀, iso-C₁₅:₀ and C₁₇:₁ ω6c. The predominant polar lipids were found to be phosphatidylglycerol, phosphatidylethanolamine and diphosphatidylglycerol. The DNA G + C content of strain N39ᵀ is 50.8 %. On the basis of genotypic, chemotaxonomic and phenotypic data, strain N39ᵀ is concluded to represent a novel species within the genus Kordiimonas, for which the name Kordiimonas sediminis sp. nov. is proposed. The type strain is N39ᵀ (=KCTC 42590ᵀ = MCCC 1H00112ᵀ).
Journal Article
Mesonia sediminis sp. nov., isolated from a sea cucumber culture pond
2015
A yellow-pigmented, Gram-stain negative and facultatively anaerobic bacterium, designated MF326
T
, was isolated from a sample of sediment collected from a sea cucumber culture pond in Rongcheng, China (122°14′34″E 36°54′36″N). Cells of strain MF326
T
were found to be catalase negative and oxidase positive. Optimal growth was found to occur at 30 °C and pH 7.0–7.5 in the presence of 2.0–3.0 % (w/v) NaCl. Phylogenetic analysis based on 16S rRNA gene sequences revealed that strain MF326
T
is a member of the genus
Mesonia
and exhibits the high sequence similarity (94.3 %) with the type strain of
Mesonia ostreae
, followed by
Mesonia algae
(93.9 %). The dominant fatty acids of strain MF326
T
were identified as iso-C
15:0
, an unidentified fatty acid with an equivalent chain-length of 13.565 and anteiso-C
15:0
. The major polar lipids were found to be two unidentified lipids and phosphatidylethanolamine. The major respiratory quinone was found to be MK-6 and the genomic DNA G+C content was determined to be 40.7 mol%. On the basis of the phylogenetic analysis and differential phenotypic characteristics, it is concluded that strain MF326
T
(=KCTC 42255
T
=MCCC 1H00125
T
) should be assigned to the genus
Mesonia
as the type strain of a novel species, for which the name
Mesonia sediminis
sp. nov. is proposed.
Journal Article
Pontibacter locisalis Sy30T sp. nov. isolated from soil collected from an abandoned saltern
by
Xie, Zhi-Hong
,
Zhou, Yan-Xia
,
Chen, Guan-Jun
in
Bacterial Typing Techniques
,
Base Composition
,
Biomedical and Life Sciences
2016
A novel Gram-stain negative, red, rod-shaped, non-motile and aerobic bacterial strain, designated Sy30ᵀ, was isolated from dry soils of an abandoned marine saltern at Weihai, China. 16S rRNA sequence analysis indicated that strain Sy30ᵀ belongs to the genus Pontibacter in the family Cytophagaceae, with sequence similarities ranging from 93.3 to 96.4 % with other type species of the genus Pontibacter. The predominant cellular fatty acids were iso-C₁₅:₀ and summed feature 4 (iso-C₁₇:₁ I and/or anteiso-C₁₇:₁ B). The major menaquinone was MK-7. The major polyamine was sym-homospermidine. The DNA G+C content was 47.7 mol%. The major polar lipids consisted of phosphatidylethanolamine, phosphoaminolipid and two unidentified polar lipid. Based on phenotypic, chemotaxonomic and phylogenetic analysis, strain Sy30ᵀ represents a novel species of the genus Pontibacter in the family Cytophagaceae, phylum Bacteroidetes, for which the name Pontibacter locisalis sp. nov. is proposed. The type strain is Sy30ᵀ (=KCTC 42498ᵀ = CICC AB 2015060ᵀ).
Journal Article
The Basic Control System of an Ocean Exploration AUV
2013
Autonomous Underwater Vehicle (AUV) which could finish autonomous mission process is paid more and more attention. As an artificial intelligence system, AUV has high independence, reliability and adaptability to ocean environment. An efficient architecture of AUV plays an important roll in achieving those properties. A newly developed AUV, ZT-AUV, which is used for ocean exploring, is introduced. And its basic control system architecture is depicted. Both the hardware and software in the control system are described. Finally, the experiments in tank and those at sea are conducted to test the architecture and the methods of the control system, and the results prove that the control system of the AUV is reliable, flexible and extensible.
Journal Article