Phytochemistry Letters
·
2015
·
IF 1.45
Zhen-Jie Lia,Chun-Ping Wan,Le Cai,Shu-Quan Li,Xi Zheng,Yan Qi,Jian-Wei Dong,Tian-Peng Yin,Zhi-Xian Zhou,Ning-Hua Tan,Zhong-Tao Ding
Twenty terpenoids, including a new triterpenoid ( 1 ) and a new monoterpenoid ( 20 ), were isolated from the branches and leaves of Pyrus pashia . The structures of two new compounds were determined to be 2α, 3β, 27-trihydroxyolean-12-en-28-oic acid ( 1 ) and (4α)-3-(5,5-dimethyltetrahydrofuranyl)-1-buten-3-ol 3- O -β- d -glucopyranoside ( 20 ) on the basis of spectroscopic analysis (IR, HRESIMS, 1D and 2D NMR) and chemical method. Some of the isolated compounds were evaluated for their cytotoxic activity against a panel of human cancer cell lines by MTT assay, using cisplatin as a positive control. Compound 14 exhibited cytotoxic activities against A549 (IC 50 = 19.18 ± 4.26 μM), Hela (IC 50 = 12.56 ± 3.89 μM), SGC7901 (IC 50 = 10.48 ± 1.95 μM) and NHI-1975 (IC 50 = 7.38 ± 2.31 μM) cell lines as well as compound 12 displayed cytotoxic activities against A549 (IC 50 = 14.71 ± 1.47 μM) and Hela (IC 50 = 12.22 ± 1.88 μM) cell lines.
研究领域:
植物化学
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药理学
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肿瘤学
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产品关联
DOI
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2021
·Vol. 30
·期 10
·1856-1867
·
IF 1.965
Yin Yu-dong,Liu Jing-jing,Liao Wen-fei,Guo Xian-kun,Zhang Li-shan,Mo Wei-bin,Cheng Ke-guang
As 17 β -estradiol and its derivatives have good affinity with estrogen receptors and have unique antitumor properties, O 1 -propargyl- N 4 , N 4 -bis(2-chloroethyl)-4-aminophenol and N 4 , N 4 -dipropargyl- N 1 , N 1 -bis(2-chloroethyl)-1,4-phenylenediamine were respectively combined with 17 β -estradiol through linkers of different lengths. These targeted novel nitrogen mustard 17 β -estradiol derivatives were tested antiproliferative activity using the MTT assay. The results illustrated that these compounds were less toxicity to HL-7702 (human liver cells) and SKOV-3, though all their activity potency was moderate or weak aganist the MDA-MB-231, MCF-7 and BEL-7404 cell lines. The inhibitory activity of the O 1 -propargyl- N 4 , N 4 -bis (2-chloroethyl)-4-aminophenol derivatives (compounds III-1~6 and VII-1~4 ) were obviously better than the N 4 -dipropargyl- N 1 , N 1 -bis (2-chloroethyl) -1,4-phenylenediamine derivatives (compounds IV-1~6 and VIII-1~4 ) against tested tumor cell lines. And three hybrids (compounds III-2 , III-6 , and VII-3 ) exhibited good inhibitory activity against BEL-7404 cell line (IC 50 = 13.5, 15.3 and 13.9 μM, respectively). After that, we performed KEGG pathway analysis on compound III-6 , and the results showed that III-6 mainly induced breast cancer cell apoptosis by regulating the expression of the proteins in NF-κ B pathway.
研究领域:
药理学
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肿瘤学
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分子生物学
✓ 已验证
DOI
高影响因子
CHEMISTRY & BIODIVERSITY
·
2018
·Vol. 15
·期 3
·e1700513
·
IF 1.617
Xiaoping Zhan,Yun Xu,Qi Qi,Yaolin Wang,Huiying Shi,Zhenmin Mao
A series of novel quinazolinone derivatives containing a substituted amino moiety were synthesized, evaluated for their cytotoxic and antibacterial activities. The results of MTT assay showed that all synthesized target compounds 5A – 5O showed potent cytotoxicity against SGC-7901 ( IC 50 , 0.72 – 1.41 μ m ). Moreover, the compounds 5D , 5I , and 5K showed better selectivity as compared with positive controls pemetrexed and MTX due to weak cytotoxicity against normal tissue cell line HUVSMC. Among synthesized compounds, the compounds 5E , 5J , 5L , and 5N showed broad-spectrum cytotoxic activities against at least four cancer cell lines at a micromolar level. The results of antibacteria evaluation revealed that all synthesized compounds showed good to moderate antibacterial activities against Gram -negative bacteria Escherichia coli . Among them, the MIC values of the compounds 5C , 5F , and 5M were 0.31 μg/mL. Graphical
研究领域:
药物化学
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肿瘤学
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微生物学
✓ 已验证
DOI
高影响因子
MOLECULES
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2013
·Vol. 18
·期 9
·11496-11511
·
IF 2.428
Rui Liu,Hongchi Zhang,Maosen Yuan,Jiao Zhou,Qin Tu,Jian-Jun Liu,Jinyi Wang
Two series of apigenin [5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one] derivatives,3a–3jand4a–4j, were synthesized. The apigenin and alkyl amines moieties of these compounds were separated by C2or C3spacers, respectively. The chemical structures of the apigenin derivatives were confirmed using1H-NMR,13C-NMR, and electrospray ionization mass spectroscopy. Thein vitroantibacterial and antiproliferative activities of all synthesized compounds were determined. Among the tested compounds,4a–4jdisplayed significant antibacterial activity against the tested strains (Staphylococcus aureus,Bacillus subtilis,Escherichia coli, andPseudomonas aeruginosa). Additionally,4ishowed the best inhibitory activity with minimum inhibitory concentrations of 1.95, 3.91, 3.91, and 3.91 μg/mL againstS. aureus,B. subtilis,E. coli, andP. aeruginosa, respectively. The antiproliferative activity of the apigenin derivatives was evaluated by an MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] assay. We determined that4a–4jdisplayed better growth inhibition activity against four human cancer cell lines, namely, human lung (A549), human cervical (HeLa), human hepatocellular liver (HepG2), and human breast (MCF-7) cancer cells, than the parent apigenin. Compound4jwas found to be the most active antiproliferative compound against the selected cancer cells. Structure-activity relationships were also discussed based on the obtained experimental data.Keywords:synthesis;biological evaluation;apigenin derivatives;antibacterial activity;antiproliferative activity;MTT assay
研究领域:
药理学
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化学
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微生物学
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肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
RUSSIAN JOURNAL OF COORDINATION CHEMISTRY
·
2014
·Vol. 40
·期 10
·764-767
·
IF 0.629
Li G. B.,Wang S. X.,Su W. Y.,Pan R. K.,Liu K. D.,Liu S. G.
A new cationic complex, [Co(Bpbp) 2 ](ClO 4 ) 2 · DMF · H 2 O, was synthesized by treatment Co(ClO 4 ) 2 · 6H 2 O with 2,6- bis (1-phenylbenzimidazol-2-yl)pyridine (Bpbp) in DMF solvent at room temperature. Its structure was characterized by element analysis, IR, and X-ray single crystal structure analyses (CIF file CCDC no. 970498). For complex, crystal system, triclinic, space group, \(P\bar \imath\) , a = 11.585(13), b = 13.939(16), c = 19.236(2) \(\mathop {\AA}\limits^\prime\) , α = 97.938(2)°, β = 102.814(2)°, γ = 90.556(2)°, V = 2861.1(6) Ǻ 3 , Z = 2. The Co 2+ ion octahedral geometry is coordinated by six nitrogen atoms from two ligand (Bpbp). The antiproliferative activities of the complex were screened by MTT assay against HepG2, Huh7, Eca109 and Eca9706 cancer cell. The complex exhibits inhibition on Eca9706 and Eca109 cancer cell but no HepG2 and Huh7 cancer cell.
研究领域:
无机化学
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药物化学
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肿瘤学
✓ 已验证
DOI
高影响因子
Materials Today Communications
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2021
·
IF 3.383
Zhaosheng Hou,Jinwei Teng,Jinjian Wei,Tiantian Hao,Zhengqi Liu
The objective of this study is to offer a highly pH-sensitive biodegradable polyurethane for application as an intelligent drug delivery carrier. A new pyridinyl diol ((3-((2-(pyridin-4-yl)ethyl)thio) propane-1,2-diol, PyDH) was first synthesized via thiol-ene “click” reaction. Then, PyDH-based poly(ether-ester-urethane) (PEEU-Py) was designed and prepared through the condensation polymerization of PyDH diol, poly(ether-ester) diol and diisocyanate. The pendent pyridine groups and the polyester segments could endow the polymers with pH sensitivity and degradability, respectively. The bulk structures and physicochemical properties of PEEU-Py were characterized via 1 H NMR, FT-IR, GPC, thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and tensile testing. The cast membranes exhibited a sharp transition of the equilibrium swelling ratio (ESR) at pH 8.5∼9.0, and ESR increases of more than twofold and eightfold at pH 1.5 relative to pH 7.4 and pH 12.0, respectively. In vitro drug release studies showed that the release efficiency from the membranes was increased with decreasing pH value. The pH-sensitive release behaviors were related mainly to the swelling ability, and the slow hydrolytic degradation rate of PEEU-Py membranes had minimal influence on it. In addition, the in vitro cytotoxicity was evaluated by an MTT assay with L929 fibroblasts, and a cell viability of more than 75 % indicated satisfactory cytocompatibility. All the results demonstrate the potential application of PEEU-Py as a biological on–off switch for drug carriers that is triggered by an external pH change.
研究领域:
材料科学
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高分子化学
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药学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
Results in Chemistry
·
2023
·
IF 2.3
Jianhua Deng,Daosheng Li,Rui Chen,Xiangsheng Zeng,Yu Liu
The possibility of fabricating metal nanoparticles using plant extracts has already been explored in phytomedicines. Nanobiotechnology has a wide range of potential applications, including the cosmetics industry, packaging, coatings, biomedicine, and the enhancement of biological activity. Nickel oxide (NiO) was fabricated in a waste-free, low-cost method and then used to adorn Marsdenia tenacissima extract (MTE), a crucial plant leaf. After forming the nanoparticles, MTE@NiO-NPs were also tested for their optical and biological qualities. The morphological characteristics of NiO-NPs are rhombohedra and slightly agglomerated, and the particle size of the biosynthesized NiO-NPs is observed in the range of ∼ 15 nm. The in vitro cytotoxicity of Marsdenia tenacissima extract (MTE) and nanoparticles on lung cancer cells (A549 and H1299) by MTT assay. The in vitro cytotoxicity assay results revealed that the newly fabricated nanoparticles effectively kill cancer cells with low minimal inhibitory concentration. The various biochemical staining assays assessed the cell death and morphological investigation. Furthermore, the mode of cell death was evaluated by mitochondrial membrane potential (Δψm) and reactive oxygen species (ROS). Therefore, the study concludes that the plant leaves extract of Marsdenia tenacissima is a powerful reducing/capping agent in fabricating MTE@NiO-NPs, demonstrating useful biological features.
研究领域:
纳米技术
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药理学
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癌症研究
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生物技术
✓ 已验证
产品关联
DOI
高影响因子
INORGANIC CHEMISTRY
·
2022
·
IF 5.436
Yuhao Wu,Yirong Wang,Yun Sun,Zhen Li,Xianghong Li,Zhiguo Zhou,Dingguo Tang
A novel family of ruthenium nitrosyl complexes [Ru(bpy)(C∧N)(MeCN)NO](PF6)2 (2a–2e, bpy = 2,2′-bipyridine, HC∧N = 2-phenylpyridine and its derivatives) has been prepared by reacting cyclometalated ruthenium complexes [Ru(bpy)2(C∧N)][PF6] (1a–1e) with NO+, which were comprehensively characterized by mass, IR, NMR, and UV–vis spectra as well as the single-crystal X-ray structure determinations. Herein, the coordination geometry of Ru atoms in 2a–2e is a distorted octahedron and {RuII–NO+}6 is present in these complexes. Theoretical calculations suggest that the reactions involving dissociation of one bipyridine and coordination with NO+ proceed spontaneously (ΔG < 0) and the transformation from 1a–1e to the intermediates is dominated by substituents (ΔGRI varies from −1.19 to −1.53 eV), which influence the binding energy between Ru(II) and NO+ in complexes 2a–2e (−89.42 to −101.17 kcal/mol) and thus control the photorelease of NO on a certain scale. The weak absorption bands in the visible region could be attributed to the contribution of dπ(RuII) → π*(NO+), which were enhanced greatly under light, indicating the possible release of NO. The photoinduced NO, as well as singlet oxygen (1O2), was then confirmed by EPR spectra, and the amount of NO released from 2a–2e was estimated via Griess reagent assay. The cytotoxicity of these complexes with or without visible light irradiation was also investigated using an MTT assay.
研究领域:
无机化学
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配位化学
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光化学
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生物化学
✓ 已验证
DOI
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2021
·Vol. 31
·期 1
·165-176
·
IF 1.965
Zhang Fuli,Lai Qingfu,Lai Weihong,Li Ming,Jin Xiaobao,Ye Lianbao
Phloroglucinol compounds isolated from Dryopteris fragrans (L.) Schott showed a variety of biological activities, such as anticancer and anti-inflammatory. In this study, we have made a number of modifications around the scaffold of phloroglucinol and synthesized phloroglucinol derivatives A1–A9, B1–B9 , and C1–C3 . We synthesized these compounds and investigated their effect on four human cancer cell lines (A-549, MCF-7, Hela, HepG2 cell lines) via MTT assay in vitro. The results revealed that all compounds exhibited certain antiproliferative activities on cancer cell lines and excellent inhibitory effects on MCF-7, in which compound C2 was the best with the IC 50 value of 18.49 μM, exceeding that of 5-fluorouracil. Moreover, the cell apoptosis test showed that compound C2 induced apoptosis in a concentration-dependent manner. Furthermore, the results of molecular docking analysis explained the probable interaction between the active compounds and active sites of target protein 4I22 and 1OG5.
研究领域:
药理学
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化学
·
肿瘤学
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分子生物学
✓ 已验证
DOI
高影响因子
BIOMATERIALS
·
2013
·
IF 7.604
Feifei Yang,Wei Huang,Yunfei Li,Shan Liu,Mingji Jin,Yuli Wang,Lihua Jia,Zhonggao Gao
Recently, survivin has been attracting great attention because it plays an important role in inhibiting the apoptosis process of tumor cells. Down-regulating the expression of survivin gene by small interfering RNA (siRNA) offers a promising method for anti-tumor therapy. However, lack of appropriate siRNA delivery vector has significantly hindered the successful application of survivin-targeted siRNA in anti-tumor therapy. The purpose of this study was to use polysaccharide vector TAT-g-CS we synthesized to deliver functional siRNA and evaluate its in vivo anti-tumor activity. TAT-g-CS vector was firstly synthesized and well structurally characterized. MTT assay showed that TAT-g-CS vector exhibited good biocompatibility . TAT-g-CS complexed with siRNA offering nanoparticles with an average particle size of 212.2 nm and a polydispersity index of 0.121, and the zeta potential of the nanoparticles was +18.58 mV. Results from reporter gene assay suggested that luciferase-targeted siRNA when delivered by TAT-g-CS could down-regulate the expression of luciferase gene with 75.3% reduction. Most importantly, we use siRNA Sur targeting survivin gene to assess the in vitro and in vivo delivery capacity of TAT-g-CS and its anti-tumor effects. Our results demonstrated that TAT-g-CS/siRNA Sur nanoparticles not only strongly inhibited the in vitro proliferation of 4T1-Luc tumor cells via inducing cell apoptosis, but also effectively inhibited the in vivo growth and metastasis of malignant breast tumor, which suggested that TAT-g-CS/siRNA nanoparticle was a highly efficient non-viral system for siRNA delivery, especially for anti-tumor therapy based on siRNA therapeutics.
研究领域:
癌症生物学
·
药学
·
纳米技术
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Medicinal Chemistry
·
2024
·
IF 4.1
Qi Wang,Si-Min Liang,Zhi-Chen Mao,Xian-Li Ma,Jian-Hua Wei,Ri-Zhen Huang,Ye Zhang
A set of biotin-polyethylene glycol (PEG)-naphthalimide derivatives 4a–4h with dual targeting of ferroptosis and DNA were designed and optimized using docking simulation as antitumor agents. Docking simulation optimization results indicated that biotin-PEG4-piperazine-1,8-naphthalimide 4d should be the best candidate among these designed compounds 4a–4h, and therefore, we synthesized and evaluated it as a novel antitumor agent. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay and MGC-803 and U251 xenograft models identified 4d as a good candidate antitumor agent with potent efficacy and safety profiles, compared with amonafide and temozolomide. The findings of the docking simulations, fluorescence intercalator displacement (FID), western blot, comet, 5-ethynyl-2′-deoxyuridine (EdU), flow cytometry, transmission electron microscopy, and BODIPY-581/591-C11, FerroOrange, and dihydroethidium (DHE) fluorescent probe assays revealed that 4d could induce DNA damage, affect DNA synthesis, and cause cell cycle arrest in the S phase in MGC-803 cells. Also, it could induce lipid peroxidation and thus lead to ferroptosis in MGC-803 cells, indicating that it mainly exerted antitumor effects through dual targeting of ferroptosis and DNA. These results suggested that it was feasible to design, optimize using docking simulation, and evaluate the potency and safety of biotin-PEG-1,8-naphthalimide as a antitumor agent with dual targeting of ferroptosis and DNA, based on a multi-target drug strategy.
研究领域:
肿瘤学
·
药理学
·
分子生物学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
Molecular Medicine Reports
·
2019
·Vol. 20
·期 6
·5084-5090
·
IF 1.851
Jinsan Yang,Cao Ma,Maoshu Zhang
Diabetes mellitus adversely affects human bones and increases the risk of developing osteoporosis. In the present study, treatment with 30 mmol/l glucose was used to establish a high glucose (HG) cell model in vitro. Plasmids were used to overexpress the P2X purinoceptor 7 (P2X7) gene. Brilliant blue G and (4‑benzoyl‑benzoyl)‑ATP were used as a P2X7 antagonist and agonist, respectively. Proliferation of osteogenic MC3T3‑E1 cells and alkaline phosphatase (ALP) activity were determined using MTT and colorimetric assays, respectively. Alizarin Red S was used to assess calcification of MC3T3‑E1 cells. Western blotting and reverse transcription‑quantitative PCR were performed to determine protein and mRNA expression levels. The results demonstrated that HG inhibited MC3T3‑E1 cell proliferation and P2X7 expression, reduced calcification, and downregulated the expression levels of ALP and osteocalcin (Ocn) in MC3T3‑E1 cells. Overexpression of P2X7 in HG conditions increased calcification and proliferation, and upregulated the levels of ALP and Ocn in MC3T3‑E1 cells. Inhibition of P2X7 downregulated the expressions of ALP and Ocn in MC3T3‑E1 cells under HG conditions. Therefore, the present results indicated that HG caused damage to osteogenic MC3T3‑E1 cells. Thus, P2X7 may be a regulatory factor that may be used to counteract the effects of HG on osteogenesis.
研究领域:
内分泌学
·
细胞生物学
·
分子生物学
·
糖尿病研究
·
骨骼生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）