JOURNAL OF COORDINATION CHEMISTRY
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2025
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IF 2.1
Hou Cong Li,Ming Zhu Wang,Ye Fan Zheng,Ning An,Min Hou,Jing Hu,Wen Ge Li
Three chlorinated metal complexes [Ni2(HL)2(C2H5OH)2Cl2]·2C2H5OH (complex 1), [Co(HL)(L)] (complex 2), and [Zn2(HL)2(CH3COO)2] (complex 3) derived from 5-chlorosalicylaldehyde and 2-(2-aminophenyl)-1H-benzimidazole Schiff base ligand (H2L). The crystal structures of the three complexes were characterized by elemental analysis, infrared spectroscopy, thermogravimetric analysis, X-ray single-crystal diffraction, and UV-visible absorption spectrum. The in vitro cytotoxicity of chlorinated ligand and its metal complexes were evaluated on four different tumor cell lines (A-549 lung cancer, SMMC-7721 liver cancer, MDA-MB-231 breast cancer, and CNE-2Z nasopharyngeal carcinoma), and normal ovarian epithelial cell (IOSE 80) was determined by MTT assay. The results indicated that chloro-benzimidazole Schiff base Co (III) complex (complex 2) displayed higher cytotoxicity against MDA-MB-231 cell line than cisplatin, while the cytotoxicity on IOSE 80 was lower than that of cisplatin. The results of further study of MDA-MB-231 cells by complex 2 showed that complex 2 could inhibit MDA-MB-231 cells in the G0/G1 phase, inhibit cell proliferation and migration, promote cell apoptosis, and increase intracellular ROS level. The Western blot analysis demonstrated that complex 2 could increase Bax protein expression and decrease Bcl-2 protein expression in MDA-MB-231 cells.
研究领域:
无机化学
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药理学
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肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2024
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IF 5.7
Ruo-Fei Bai,Yi-Wei Wang,Shan-Shan Yang,Yu-Hao Zhang,Bo-Hang Zhou,Cong-Wei Zhou,Le Zhou
As part of our continuing research on propiolic acid derivatives, a series of benzyl propiolate derivatives and analogues were designed, synthesized, and investigated for inhibition activity in vitro and in vivo on phytopathogenic fungi, structure–activity relationship (SAR) and action mechanism. The results showed that most of the compounds had potent and broad-spectrum antifungal activity in vitro at 50 μg/mL. Among the compounds, 2-bromobenzyl propiolate (3h) displayed the highest comprehensive activity with total activity index (TAI) of 4.57 against all the eight test fungi followed by 3-fluorobenzyl propiolate (3c) (TAI = 4.53), superior to positive fungicides thiabendazole (TAI < 4.12) and/or azoxystrobin (TAI < 2.90). Relative to the other fungi, Fusarium solani and Fusarium graminearum revealed higher total susceptibility indexes (TSI) of 11.1 and 8.98, respectively, for all compounds. 3h and 3g (4-chlorobenzyl propiolate) gave the smallest EC50 values of 0.86 and 0.67 μg/mL against F. solani and F. graminearum, respectively, superior or comparable with thiabendazole and azoxystrobin. As a representative, 3h at 200 μg/mL displayed 100% protection on F. solani infections on potatoes over 7 days and high safety for plant growth. In antifungal mechanism, 3h was able to change mycelial morphology, destroy the structures of both hypha and cell membrane, increase the intracellular ROS level, decrease the intracellular mitochondrial membrane potential level, and change the permeability of the cell membrane. The SAR showed that ethynyl is a key group for the activity, and the presence of halogen atoms at the 2-site of the benzene ring can significantly improve the activity in most cases. Thus, benzyl propiolate can be considered a novel antifungal lead compound, while 3h can be considered a promising fungicide candidate to develop new agricultural fungicides.
研究领域:
农业化学
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植物病理学
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药物化学
✓ 已验证
DOI
PubMed
高影响因子
Arabian Journal of Chemistry
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2022
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IF 6.212
Chengyang Ni,YaJu Wu,Mei Ran,Jingyan Li,Hong Li,Cai Lan,Jian Liu,Ping Dai,Jianming Wu,Fangyao Li
In the present study, novel representatives of the important group of biologically-active, dehydroabietic acid-bearing dithiocarbamate moiety, were synthesized and characterized by 1 H NMR, 13 C NMR, HR-MS. The in vitro antiproliferative activity evaluation (MTT) indicated that these compounds exhibited potent inhibitory activities in various cancer cell lines (HepG-2, MCF-7, HeLa, T-24, MGC-803). Particularly, compound III -b possessed extraordinary cytotoxicity with low micromolar IC 50 values ranging from 4.07 to 38.84 µM against tested cancer cell lines, while displayed weak cytotoxicity on two normal cell lines (LO-2 and HEK 293 T). Subsequently, the potential mechanisms of representative compound III -b were elementarily investigated by Transwell experiment, which showed III -b can inhibit cancer cells migration. Annexin-V/PI dual staining showed that the compound can induce HepG-2 cells apoptosis in a dose-dependent manner. Meanwhile this apoptosis may be related to the upregulated protein expression of cleaved-caspase 3, cleaved-caspase 9, Bax and downregulated of Bcl-2 indicated by Western Blot. Later study further confirmed that ROS levels in HepG-2 cells increased significantly with the rise of concentrations. In addition, through the network pharmacology data analyzing, the core targets and signaling pathways of compound III -b for treatment of liver neoplasms were forecasted. Molecular docking model showed that compound III -b had high affinity with hub targets (CASP3, EGFR, HSP90AA1, MAPK1, ERBB2, MDM2), suggesting that compound III -b might target the hub protein to modulate signaling activity. Taken together, these data indicated that dehydroabietic acid structural modification following the “Molecular hybridization” principle is a feasible way to discover the potential multi-targeted antitumor compounds.
研究领域:
肿瘤学
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药理学
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药物化学
✓ 已验证
DOI
高影响因子
JOURNAL OF ALLOYS AND COMPOUNDS
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2022
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IF 6.371
Hang Jia,Zewei Wang,Rui Cai,Zhouli Wang,Yahong Yuan,Tianli Yue
Bacterial drug resistance caused by the abuse of antibiotics poses a serious threat to human health. Thus, the development of alternative strategies for the replacing of antibiotics is necessary. Herein, a hierarchical three-dimensional Bi 2 S 3 (BS) nanoflowers were facile fabricated and employed as supporter for the growth of silver nanoparticles (Ag NPs). Combining the excellent antimicrobial activity of Ag NPs, the as-resulted Ag/BS exhibited broad-spectrum antibacterial activity against pathogenic bacteria. Investigation on antibacterial mechanism revealed the treatment of Ag/BS damages the bacterial cell membrane , leading to the loss of intracellular substances. The compromised membrane caused the reduction of membrane bound enzymes activity , resulting in the arrest of metabolic activity. Simultaneously, Ag/BS broke the bacterial antioxidant defense system by raising the intracellular ROS levels, caused the oxidative damage , resulting in the loss of bacterial viability. Moreover, the satisfactory biocompatibility and effective antibacterial performance of Ag/BS were confirmed by performing in vitro cytotoxicity and in vivo antibacterial assay. Accordingly, this work opens up possibility for the construction of Bi 2 S 3 based multifunctional nanomaterials and its application for pathogenic bacteria control.
研究领域:
纳米技术
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材料科学
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生物医学工程
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微生物学
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药学
✓ 已验证
产品关联
DOI
高影响因子
Small
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2025
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IF 12.1
Qiao Chen,Xu Yang,Yao Yu,Xinmei Duan,Rongrong Ni,Guojing Song,Li Zhu,Yuan Zhong,Kai Qu,Xian Qin,Kun Zhang,Yang Luo,Wei Wu
Theranostic applications in atherosclerosis plaque microenvironment-triggered nanoplatforms are significantly compromised by the complex synthesis procedure, non-specific distribution, and limited therapeutic function. Therefore, development of a facile and feasible method to construct a pathology-based stimuli-responsive nanoplatform with satisfactory theranostic performance remains a demanding and highly anticipated goal. Herein, a novel class of multifunctional supra-carbon dots (CDs), denoted as MM@Ce-CDs NPs, by a simple nanoassembly and a subsequent coating with macrophage membrane (MM), is developed for the targeted reactive oxygen species-trigged theranostic and positive regulation of the pathological plaque microenvironment in AS. The harvested MM@Ce-CDs NPs exhibit activatable fluorescence properties, photoacoustic characteristics, and cascade enzyme performances, which can be effectively activated under ROS stimulation in the plaque pathological microenvironment, enabling precise control over theranostic functions, while markedly enhancing diagnostic accuracy and therapeutic efficacy for AS management. Besides, MM@Ce-CDs NPs can effectively manipulate the plaque microenvironment by reducing ROS levels and inflammation, alleviating M1 macrophage infiltration, and inhibiting foam cell formation, all together suppressing the pathological plaque development through the synergistic mechanisms. In addition, MM@Ce-CDs NPs inherit the biomimetic biological functions from MM, facilitating a highly specific target delivery to AS.
研究领域:
纳米技术
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生物医学工程
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心血管疾病
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材料科学
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诊疗一体化
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Gut Microbes
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2024
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IF 12.2
Fangfang Chen,Songhe Guo,Yiqiu Li,Yongfan Lu,Le Liu,Shengxin Chen,Jun An,Ge Zhang
The intracellular bacterium Fusobacterium nucleatum (Fn) mediates tumorigenesis and progression in colorectal cancer (CRC). However, the origin of intratumoral Fn and the role of Fn-infected immunocytes in the tumor microenvironment remain unclear. Here, we observed that Fn-infected neutrophils/macrophages (PMNs/MΦs), especially PMNs, accumulate in tumor tissues and fecal Fn abundance correlates positively with an abundance of blood PD-L1+ PMNs in CRC patients. Moreover, Fn accumulates in tumor tissues of tumor-bearing mice via intragingival infection and intravenous injection. Mechanistically, Fn can survive inside PMNs by reducing intracellular ROS levels and producing H2S. Specifically, the lysozyme inhibitor Fn1792 as a novel virulence factor of Fn suppressed apoptosis of phagocytes by inducing CX3CR1 expression. Furthermore, Fn-driven CX3CR1+PD-L1+ phagocytes transfer intracellular Fn to tumor cells, which recruit PMNs/MΦs through the CXCL2/8-CXCR2 and CCL5/CCR5 axes. Consequently, CX3CR1+PD-L1+ PMNs infiltration promotes CRC metastasis and weakens the efficacy of immunotherapy. Treatment with the doxycycline eradicated intracellular Fn, thereby reducing the CX3CR1+PD-L1+ PMNs populations and slowing Fn-promoted tumor growth and metastasis in mice. These results suggest phagocytes as Fn-presenting cells use mutualistic strategies to home to tumor tissues and induce immunosuppression, and treatment with ROS-enhanced antibiotics can inhibit Fn-positive tumor progression.
研究领域:
肿瘤学
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免疫学
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微生物学
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药理学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2023
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IF 3.8
Yong-Po Zhang,Qing He,Xin-Hui Zhou,Guang-Huan Liu,Ai-Qin Yue,Chun-Yan Gao,Jin-Zhong Zhao,Wei-Jun Du,Shi-Ping Yan
Two new Cu(І) complexes, [Cu 2 (L 1 ) 2 (μ-Br) 2 ] (1) and [Cu 2 (L 1 ) 2 (μ-Cl) 2 ] (2) were synthesized from Cu(II) halogen salts and the reduced Schiff base ligand. Stable Cu(І) complexes were obtained via in situ reduction of Cu(II) to Cu(I) and the C N was oxidize to C = N in the ligand. The structures of two complexes were characterized by X-ray single crystal diffraction analysis as well as IR and UV–Vis spectra. The two complexes have potential antioxidant capacity and exhibit efficiently self-activated DNA cleavage activity and hydroxyl radical ROS cleavage mechanism. MTT was used to assay cytotoxicity of the complexes toward a series of tumor cell and HUVEC cell lines. Both complexes exhibited higher selective cytotoxicity against tumor cells than normal cells, which is significantly superior to the positive control. The complexes could induce cell apoptosis via mitochondrial pathway by increase of ROS levels and decrease of mitochondrial membrane potential (Δψ m ). Furthermore, the complexes can obviously inhibit the migration and invasion of the quiz tumor cells, as well as inhibit the angiogenesis of HUVEC cells.
研究领域:
化学
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生物化学
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分子生物学
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癌症研究
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药学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）