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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2022 · IF 4.831

A naphthol hydrazone Schiff base bearing benzothiadiazole unit for fluorescent detection of Fe3+ in PC3 cells

Brian Musikavanhu,Dongwei Zhu,Mengran Tang,Zhaoli Xue,Shengjun Wang,Long Zhao

Naphthol hydrazone derivatives are recognized as efficient chelating agents for both qualitative and quantitative detection of metal ions. Here we design a naphthol hydrazine-based chemosensor with covalently linking a strong electron-withdrawing benzothiadiazole group to modulate the molecular electronic structure, nominated as NtHzBtd . The fluorescent probe performs excellent selectivity and sensitivity towards Fe 3+ with 1:1 binding stoichiometry, while exhibiting a quick response at 55 s with a relatively low limit of detection of 0.036 µM. A series of spectroscopic measurements in tandem with theoretical calculations suggest that the probe undergoes both intramolecular charge transfer (ICT) and chelation enhanced quenching (CHEQ) processes. Successful color rendering of paper strips and bioimaging in PC3 cells demonstrate the promising applicability of NtHzBtd for portable Fe 3+ detection in real samples and biosystems.

研究领域: 分析化学 · 生物医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF LIPOSOME RESEARCH · 2019 · IF 2.507

Optimization on conditions of podophyllotoxin-loaded liposomes using response surface methodology and its activity on PC3 cells

Zeyu Wu,Tingting Wang,Yonghong Song,Yang Lu,Tianyun Chen,Pengpeng Chen,Ailing Hui,Yan Chen,Haixiang Wang,Wencheng Zhang

The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400 W). The experimental EE of PPT-Lips was 90.425%, which was consistent with the theoretically predicted value. The characterization studies showed that PPT-Lips were well-dispersible spherical particles with an average size of 106 nm and a zeta potential of –10.1 mV. A gradual and time-dependent pattern of PPT from liposomes was found in in vitro drug release with a cumulative release amount up to 70.3% in 24 h. Results of cell viability experiments on PC3 cells demonstrated that PPT-Lips exhibited more effective anticancer activity in comparison with free PPT. Therefore, PPT-Lips represent an efficient and promising drug delivery system for PPT.

研究领域: 药剂学 · 肿瘤学 · 药物递送
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ONCOLOGY REPORTS · 2018 ·Vol. 39 ·期 6 ·3055-3063 · IF 2.976

Huaier suppresses proliferative and metastatic potential of prostate cancer PC3 cells via downregulation of Lamin B1 and induction of autophagy

Ailin Yang,Yanan Zhao,Ying Wang,Xiaojun Zha,Yunfang Zhao,Pengfei Tu,Zhongdong Hu

Prostate cancer is one of the most common malignancies occurring in males. Although large advances have been made in the pathogenesis of prostate cancer, the development of drugs with high efficacy and low toxicity for the treatment of prostate cancer is urgently needed. Recently, more and more attention has been paid to the antitumor effect of Traditional Chinese Medicine (TCM) worldwide. Trametes robiniophila Murr. (Huaier) has been applied as a type of TCM drug for ~1,600 years. Huaier exhibits excellent clinical efficacy in the treatment of cancer, including prostate cancer. However, the mechanisms underlying the anti-prostate cancer effect of Huaier remain largely unclear. In the present study, we revealed that Huaier aqueous extract inhibited the proliferative and metastatic capabilities of human prostate cancer PC3 cells through CCK-8 assay, in vitro scratch assay and Transwell assay. Moreover, decreased Lamin B1 was implicated in Huaier-induced suppression of proliferative and metastatic potential of PC3 cells. Intriguingly, we demonstrated that Huaier treatment induced autophagic cell death in PC3 cells. This study sheds new light on the mechanisms underlying the activity of Huaier against prostate cancer and provides a new theoretical basis for the clinical application of Huaier in prostate cancer.

CAS / MDL: 88899-55-2
研究领域: 肿瘤学 · 中药学 · 细胞生物学 · 药理学
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APPLIED MICROBIOLOGY AND BIOTECHNOLOGY · 2019 ·Vol. 103 ·期 13 ·5367-5377 · IF 3.67

Exogenous addition of alkanoic acids enhanced production of antifungal lipopeptides in Bacillus amyloliquefaciens Pc3

Ding Lianshuai,Guo Wenbin,Chen Xinhua

The bacterium, Bacillus amyloliquefaciens Pc3, was previously isolated from Antarctic seawater and has been found to show antagonistic activity against the fungus, Rhizoctonia solani ACCC 36316, which causes a severe disease known as Sclerotinia sclerotiorum in rapeseed plants. Bacillus lipopeptides had been widely used as biocontrol agents for plant diseases. In this study, we isolated 11 lipopeptide compounds from B. amyloliquefaciens Pc3 culture broth via reversed-phase high-performance liquid chromatography (RP-HPLC) and used matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF-MS) to identify these as iturin A (C 14 , C 15 , C 16 , C 17 ), fengycin B (C 14 , C 15 , C 16 , C 17 ), and surfactin (C 14 , C 15 , C 16 ). We further found that the addition of exogenous alkanoic acids, including myristic acid, pentadecanoic acid, palmitic acid, heptadecanoic acid, octadecanoic acid, and nonadecanoic acid, to the bacterial growth media could promote lipopeptide production and enhance the antifungal activities of crude lipopeptide extracts from B. amyloliquefaciens Pc3. In addition, the transcriptional levels of three lipopeptide synthesis genes, ituD , fenA , and srfA-A , and two fatty acid metabolism–related genes, FabI , which encodes enoyl-ACP reductase, and FadB , which encodes enoyl-CoA hydratase, were found to be upregulated in cells grown with exogenous alkanoic acids. Among the six alkanoic acids tested, those with odd carbon chain lengths had a greater effect on lipopeptide production, antifungal activity, and target gene upregulation than those with even carbon chain lengths. These results provide a practical approach for the efficient production of lipopeptides in Bacillus amyloliquefaciens Pc3.

研究领域: 微生物学 · 植物病理学 · 生物技术
✓ 已验证 DOI 高影响因子
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BIOORGANIC CHEMISTRY · 2023 · IF 5.1

Discovery of dolutegravir-1,2,3-triazole derivatives against prostate cancer via inducing DNA damage

Shuyi Zhou,Xixi Hou,Ling Li,LiHao Guo,Huili Wang,Longfei Mao,Leilei Shi,Miaomiao Yuan

Prostate cancer (PCa) is the second most frequently diagnosed cancer among men, causing a huge number of deaths each year. Traditional chemotherapy for PCa mostly focused on targeting androgen receptors. However, some of the patients would develop resistance to hormonal therapy. In these cases, it is suggested for these patients to administer treatments in combination with other chemotherapeutics. Current chemotherapeutics for metastatic castration-resistant PCa could hardly reach satisfying effects, therefore it is crucial to explore novel agents with low cytotoxicity. Herein, a common drug against the human immunodeficiency virus (HIV), the dolutegravir (DTG) was modified to become a series of dolutegravir-1,2,3-triazole derivatives. Among these compounds, the 4d and 4q derivatives were verified with high anti-tumor efficiency, suppressing the proliferation of the prostate cancer cells PC3 and DU145. These compounds function by binding to the poly (adenosine diphosphate-ribose) polymerase (PARP), inactivating the PARP and inducing DNA damage in cancer cells. It is noteworthy that the 4d and 4q derivatives showed almost no impact on normal cells and mice. Thereby, the results reveal that these dolutegravir-1,2,3-triazole compounds are potential chemotherapeutics for PCa treatment.

研究领域: 肿瘤学 · 药理学 · 化学生物学
✓ 已验证 DOI PubMed 高影响因子
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Frontiers in Pharmacology · 2020 · IF 4.225

Moringa oleifera Alkaloids Inhibited PC3 Cells Growth and Migration Through the COX-2 Mediated Wnt/β-Catenin Signaling Pathway

Xie Jing,Luo Feng-xian,Shi Chong-ying,Jiang Wei-wei,Qian Ying-yan,Yang Ming-rong,Song Shuang,Dai Tian-yi,Peng Lei,Gao Xiao-yu,Tao Liang,Tian Yang,Sheng Jun

Moringa oleifera Lam. (M. oleifera) is valuable plant distributed in many tropical and subtropical countries. It has a number of medicinal uses and is highly nutritious. M. oleifera has been shown to inhibit tumor cell growth, but this effect has not been demonstrated on prostate cancer cells. In this study, we evaluated the inhibitory effect of M. oleifera alkaloids (MOA) on proliferation and migration of PC3 human prostate cancer cells in vitro and in vivo. Furthermore, we elucidated the mechanism of these effects. The results showed that MOA inhibited proliferation of PC3 cells and induced apoptosis and cell cycle arrest. Furthermore, MOA suppressed PC3 cell migration and inhibited the expression of matrix metalloproteinases (MMP)-9. In addition, MOA significantly downregulated the expression of cyclooxygenase 2 (COX-2), β-catenin, phosphorylated glycogen synthase 3β, and vascular endothelial growth factor, and suppressed production of prostaglandin E2 (PGE2). Furthermore, FH535 (β-catenin inhibitor) and MOA reversed PGE2-induced PC3 cell proliferation and migration, and the effects of MOA and FH535 were not additive. In vivo experiments showed that MOA (150 mg/kg) significantly inhibited growth of xenograft tumors in mice, and significantly reduced the protein expression levels of COX-2 and β-catenin in tumor tissues. These results indicate that MOA inhibits the proliferation and migration, and induces apoptosis and cell cycle arrest of PC3 cells. Additionally, MOA inhibits the proliferation and migration of PC3 cells through suppression of the COX-2 mediated Wnt/β-catenin signaling pathway.

研究领域: 肿瘤学 · 药理学 · 细胞生物学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Nanomedicine · 2016 · IF 4.889

Preclinical evaluation of gold-DTDTPA nanoparticles as theranostic agents in prostate cancer radiotherapy

Karl T Butterworth,James R Nicol,Mihaela Ghita,Soraia Rosa,Pankaj Chaudhary,Conor K McGarry,Helen O McCarthy,Gloria Jimenez-Sanchez,Rana Bazzi,Stéphane Roux,Olivier Tillement,Jonathan A Coulter,Kevin M Prise

Aim: Gold nanoparticles have attracted significant interest in cancer diagnosis and treatment. Herein, we evaluated the theranostic potential of dithiolated diethylenetriamine pentaacetic acid (DTDTPA) conjugated AuNPs (Au@DTDTPA) for CT-contrast enhancement and radiosensitization in prostate cancer. Materials & methods:In vitro assays determined Au@DTDTPA uptake, cytotoxicity, radiosensitizing potential and DNA damage profiles. Human PC3 xenograft tumor models were used to determine CT enhancement and radiation modulating effects in vivo. Results: Cells exposed to nanoparticles and radiation observed significant additional reduction in survival compared with radiation only. Au@DTDTPA produced a CT enhancement of 10% and a significant extension in tumor growth delay from 16.9 days to 38.3 compared with radiation only. Conclusion: This study demonstrates the potential of Au@DTDTPA to enhance CT-image contrast and simultaneously increases the radiosensitivity of prostate tumors.

研究领域: 癌症研究 · 纳米技术 · 医学成像 · 放射肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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Oncology Letters · 2020 ·Vol. 20 ·期 4 ·1-1 · IF 2.311

Long non‑coding RNA CCAT2 promotes prostate cancer cell proliferation and invasion by regulating the Wnt/β‑catenin signaling pathway

Peng He,Guoguang Xiong,Wei Guo,Guanjun Jiang,Yun Li,Hao Li

Long non‑coding RNA colon cancer associated transcript 2 (CCAT2) is dysregulated in a number of different types of human cancer, and affects cancer progression via the Wnt/β‑catenin signaling pathway. However, the roles of CCAT2 and the Wnt/β‑catenin signaling pathway in prostate cancer (PCa) are not completely understood. The present study aimed to investigate the potential mechanism of CCAT2 in PCa. In the present study, the reverse transcription‑quantitative PCR (RT‑qPCR) results indicated that CCAT2 expression was significantly upregulated in PCa tissues, and DU145 and PC3 cell lines compared with normal prostate tissues and the epithelial RWPE‑1 cell line, respectively. Functional assays indicated that CCAT2 downregulation inhibited DU145 and PC3 cell proliferation, cell cycle, migration and invasion. In addition, the luciferase reporter assay, RT‑qPCR and western blotting results indicated that CCAT2 regulated transcription factor 7 like 2 (TCF7L2) expression by binding to microRNA‑217. Further western blotting and TOPFlash assays indicated that CCAT2‑knockdown inhibited the Wnt/β‑catenin signaling pathway in DU145 and PC3 cell lines by inhibiting the expression of TCF7L2. However, CCAT2‑knockdown‑mediated effects were reversed by the Wnt/β‑catenin signaling pathway activator lithium chloride (LiCl). Further cell experiments suggested that LiCl treatment reversed CCAT2‑knockdown‑mediated inhibition of PCa cell proliferation, cell cycle, epithelial‑mesenchymal transition, migration and invasion. Overall, the results indicated that CCAT2 regulated PCa via the Wnt/β‑catenin signaling pathway; therefore, CCAT2 may exhibit key role during the progression of PCa and may serve as a therapeutic target for the disease.

研究领域: 肿瘤学 · 分子生物学 · 细胞生物学 · 癌症遗传学
✓ 已验证 DOI PubMed 高影响因子
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FOLIA BIOLOGICA · 2022 ·Vol. 68 ·期 2 ·59-71 · IF 1.167

Docosahexaenoic Acid Reverses Epithelial-Mesenchymal Transition and Drug Resistance by Impairing the PI3K/AKT/ Nrf2/GPX4 Signalling Pathway in Docetaxel-Resistant PC3 Prostate Cancer Cells.

Shao ZC,Zhu BH,Huang AF,Su MQ,An LJ,Wu ZP,Jiang YJ,Guo H,Han XQ,Liu CM

Drug resistance is a serious problem in cancer therapy. Growing evidence has shown that docosahexaenoic acid has anti-inflammatory and chemopreventive abilities. Studies have shown that autophagy inhibition and ferroptosis are promising therapeutic strategies for overcoming multidrug resistance. This study was aimed to examine whether docosahexaenoic acid (DHA) could reverse docetaxel resistance in prostate cancer cells. Cell survival was examined by MTT and colony formation. Protein expression was determined by Western blot. Reactive oxygen species (ROS) production was measured by flow cytometry. DHA displayed anti-cancer effects on proliferation, colony formation, migration, apoptosis, autophagy and epithelial mesenchymal transition. Glutathione-S-transferase π is an enzyme that plays an important role in drug resistance. DHA inhibited GSTπ protein expression and induced cytoprotective autophagy by regulating the PI3K/AKT signalling pathway in PC3R cells. DHA combined with PI3K inhibitor (LY294002) enhanced apoptosis by alleviating the expression of LC3B, (pro-) caspase- 3 and (uncleaved) PARP. DHA induced ferroptosis by attenuating the expression of glutathione peroxidase 4 (GPX4) and nuclear erythroid 2-related factor 2 (Nrf2). DHA-treated PC3R cells produced ROS. The ROS and cytotoxicity were reversed by treatment with ferrostatin-1. DHA combined with docetaxel inhibited EMT by regulating the expression of E-cadhein and N-cadherin. In summary, DHA reversed drug resistance and induced cytoprotective autophagy and ferroptosis by regulating the PI3K/AKT/Nrf2/GPX4 signalling pathway in PC3R cells. We propose that DHA could be developed as a chemosensitizer and that the PI3K/AKT /Nrf2/GPX4 signalling pathway might be a promising therapeutic target for overcoming cancer drug resistance.

研究领域: 肿瘤学 · 药理学 · 细胞生物学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2024 · IF 3.1

Metabolic characteristics of prostate cancer cells with high metastatic potential revealed by (S)-ethyl 1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylate inhibition

Baoyan Ding,Wei Meng,Xiaoling Zang,Zhihua Lv

A small molecule, (S)-ethyl 1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylate (SEC), has been reported to be capable of suppressing metastasis of prostate cancer (PCa) cells. In this study, SEC was used to study the metabolic responses of PCa cell lines (LNCaP, PC3, and DU145) with different metastatic potential and the alterations of mTOR, p-mTOR, AMPK, and p-AMPK levels, when the PCa cells were inhibited. The ultra-high performance liquid chromatography-high resolution mass spectrometry (UHPLC-HRMS)-based analysis showed that SEC induced the decreases of intracellular metabolites including glutamic acid, glutamine, and histidine (LNCaP); creatinine, citric acid/isocitric acid, and aspartic acid (PC3); and spermidine, S-hydroxymethylglutathione, LPE (20:3), and palmitic amide (DU145), and the increases of intracellular LPC (18:0) (LNCaP); tyrosine, pyroglutamic acid/pyrroline hydroxycarboxylic acid (PC3); and tyrosine, phenylalanine, phenylacetylglycine, spermine, histidine, and choline (DU145). SEC also caused the decrease of extracellular N1-acetylspermidine (LNCaP), erythronic acid/threonic acid (PC3 and DU145), and nicotinic acid/picolinic acid (DU145), and the increase of extracellular 5’-methylthioadenosine (DU145). High metastatic PC3 and DU145 cells exhibited changes in aromatic amino acid metabolism including tyrosine metabolism, phenylalanine, tyrosine, and tryptophan metabolism, and phenylalanine metabolism (PC3 and DU145), TCA cycle (PC3), arginine and proline metabolism, and glycerophospholipid metabolism (DU145), different from the low metastatic LNCaP cells, which had changes in alanine, aspartate, and glutamate metabolism, and arginine biosynthesis. In addition, the levels of p-mTOR and p-AMPK were shown to be obviously downregulated and upregulated, respectively, in high metastatic PC3 and DU145 cells upon SEC inhibition, while this behavior was not detected in LNCaP cells.

研究领域: 肿瘤学 · 代谢组学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SENSORS AND ACTUATORS B-CHEMICAL · 2021 · IF 7.46

Dual detection of mercury (II) and lead (II) ions using a facile coumarin-based fluorescent probe via excited state intramolecular proton transfer and photo-induced electron transfer processes

Selvaraj Muthusamy,Kanagaraj Rajalakshmi,Dongwei Zhu,Weihua Zhu,Shengjun Wang,Kang-Bong Lee,Haijun Xu,Long Zhao

A Schiff base fluorophore coumarin incorporated 4-(diethylamino)salicylaldehyde ( Cou-S ) is designed and synthesized to allow an excited state intramolecular proton transfer and photo-induced electron transfer processes for detecting toxic heavy metal ions of Hg 2+ and Pb 2+ in aqueous samples. The solid blue emission of Cou-S was gradually quenched to weak cyan in Hg 2+ detection and to green channels in the presence of Pb 2+ . The coordination behaviours of the probe with Hg 2+ /Pb 2+ are studied using a series of spectroscopic measurements and density functional theory (DFT) calculations. The probe exhibited good water solubility, great selectivity and excellent sensitivity with the LOD values of 8.3 and 10.5 nM for Hg 2+ and Pb 2+ in aqueous medium, respectively. The utility of Cou-S towards dual ions detection was explored in various sources of water samples, Whatmann paper strips, Boolean logic NOR gate operations and PC3 live cells, demonstrating the promising on-site visualization of the probe in controlling the toxicity levels in waste water sources and biosystems.

研究领域: 分析化学 · 环境科学 · 材料科学 · 生物化学
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