BIOLOGICAL & PHARMACEUTICAL BULLETIN
·
2020
·Vol. 43
·期 1
·102-109
·
IF 1.863
Qing-Xuan Zheng,Rui Wang,Yan Xu,Chang-Xin He,Cai-Yun Zhao,Zhi-Fang Wang,Rui Zhang,Wim Dehaen,Hui-Jing Li,Qi-Yong Huai
Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20 µM, respectively.
研究领域:
药理学
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肿瘤学
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药物化学
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DOI
PubMed
高影响因子
Chinese Herbal Medicines
·
2018
·
IF 0
Ding Liu,Yan-peng Li,Hong-xiu Shen,Yang Li,Jun He,Qi-zhi Zhang,Yun-mei Liu
Objective To design and synthesize a series of chrysin derivatives and evaluate the antitumor activities with MTT assay , so as to investigate molecular structure-activity relationship with molecular docking . Methods Target products were synthesized with high yield by substitution reaction, hydrolysis reaction, esterification reaction, and saponification reaction in sequence, and activities of all compounds were evaluated with human gastric carcinoma cell lines MGC-803 and human breast carcinoma cell lines MCF-7 through standard MTT assay. Molecular docking results were calculated with Surflex Geom X programme of Sybyl X-2.0 version workstation. Results 7- O -amino acids chrysin derivatives 6a – 6l were synthesized and their inhibitory effects were evaluated by comparing the material chrysin with positive control drug 5-fluorouracil (5-FU). Among these derivatives, compound 5b (IC 50 = 24.50 ± 2.26 µmol/L), 5k (IC 50 = 24.30 ± 2.19 µmol/L), and 6f (IC 50 = 24.61 ± 2.01 µmol/L) showed better inhibitory activities against MGC-803 cell lines, and compound 5g (IC 50 = 13.15 ± 1.73 µmol/L) and 5j (IC 50 = 12.34 ± 1.25 µmol/L) showed better inhibitory activities against MCF-7 cell lines than chrysin and 5-FU. Molecular docking scores showed a credible consistency compared with MTT results. Conclusion Compounds 5b, 5d, 5g, 5j, 5k , and 6f showed good antiproliferative effects on specific tumor cells, and compound 5g should be researched further when according to molecular docking.
研究领域:
药理学
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肿瘤学
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药物化学
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产品关联
DOI
CHEMISTRY & BIODIVERSITY
·
2024
·
IF 2.3
Jingmei Li,Yuhao Ji,Baitao Xian,Jianlai Liu,Deye Qu,Deming Han
In this experiment, Bi2Sn2O7/ZnO composite photocatalytic materials were synthesized by a hydrothermal method and characterized by XRD, SEM, and EDS, etc. The prepared Bi2Sn2O7/ZnO has a nanorod structure and high phase purity. The photocatalytic antimicrobial performance of Bi2Sn2O7/ZnO against bacteria and fungi under visible light was significantly better than that of single Bi2Sn2O7 and ZnO. In particular, 1000 mg/L 1:3 Bi2Sn2O7/ZnO showed an antimicrobial rate of more than 97% against Escherichia coli, Staphylococcus aureus, and Candida albicans, which are widely present in the nature. The free radical trapping experiments were selected and the antimicrobial mechanism was investigated, and the results showed that the antimicrobial process of the Bi2Sn2O7/ZnO system was regulated by the free radicals such as ·OH, h+, and e-, which were generated by its unique photocatalytic activity. Finally, MTT cytotoxicity experiments demonstrated that the Bi₂Sn₂O₇/ZnO composite was not toxic to cells. In addition, the antimicrobial performance of Bi2Sn2O7/ZnO on real livestock wastewater and the real-life application of the prepared Bi2Sn2O7/ZnO PCL composite antibiotic film for antimicrobial treatment of freshly cut fruits' surfaces under visible light were experimentally investigated. This study provides a new idea for Bi2Sn2O7/ZnO as a photocatalytic antimicrobial agent.
研究领域:
微生物学
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材料科学
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环境科学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2021
·Vol. 11
·期 43
·26594-26606
·
IF 3.361
Yang Yu,Shifei Wu,Jianqing Zhang,Jiayuan Li,Changliang Yao,Wenyong Wu,Yingying Wang,Hongjian Ji,Wenlong Wei,Min Gao,Yun Li,Shuai Yao,Yong Huang,Qirui Bi,Hua Qu,De-an Guo
Thirty-seven diterpenoid alkaloids (DAs) with diverse structures were isolated and identified from the lateral roots of Aconitum carmichaelii Debx., comprising eight C20-DAs and twenty-nine C19-DAs. Besides the 31 known DAs identified by comparing the 1H NMR and 13C NMR data with those reported in the literature, the structures of four new compounds (1, 14, 17, and 25), and two other compounds (26 and 37) which were reported to be synthesized previously, were also elucidated based on the comprehensive analysis of their HR-ESI-MS, 1D and 2D NMR spectra, including 1H–1H COSY, HSQC and HMBC and NOESY/ROESY. Among them, compound 1 represents the first example of a C20-DA glucoside. Besides, the anti-tumor activities of all the isolated compounds against human non-small-cell lung cancer A549 and H460 cells were systematically evaluated by MTT methods. The results revealed that all of the C19-DAs possessed moderate activities against both of the two cell lines with IC50 values ranging from 7.97 to 28.42 μM, and their structure–activity relationships indicated the active sites of C-8, C-10, and C-14 positions and the nitrogen atom in the C19-DA skeleton. In addition, all of the isolated DAs, with chemical structures confirmed, were further applied for network pharmacology analysis, in order to give an insight into the possible mechanisms of their anti-tumor activities. As a result, 173 potential targets and three most important pathways related to non-small-cell lung carcinoma were finally unearthed.
研究领域:
药理学
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化学
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肿瘤学
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植物科学
✓ 已验证
DOI
PubMed
高影响因子
NATURAL PRODUCT RESEARCH
·
2021
·
IF 2.862
Meitao Duan,Ahmed Mahal,Ban Mohammed,Yongyan Zhu,Huaming Tao,Shaoyu Mai,Maysoon Al-Haideri,Quanhong Zhu
Three new derivatives of tetrahydrocurcumin 6, 7 and 9 have been prepared as potent antitumor agents using copper(II)-catalyzed ‘click chemistry’. Their structures were identified using 1H-NMR, 13C-NMR and HRMS techniques. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay has been carried out to investigate the in vitro cytotoxicity against human cervical carcinoma (HeLa), human lung adenocarcinoma (A549), human hepatoma carcinoma (HepG2) and human colon carcinoma (HCT-116). Compound 6 has showed significant inhibitory activity against HCT-116 cell line with an IC50 value of 17.86 μM compared to tetrahydrocurcumin (50.96 μM) and positive control etoposide (19.48 μM) while showed no inhibitory activity against NCM460 cell line. Compounds 7 showed moderate inhibitory activity compared to tetrahydrocurcumin and etoposide while compound 9 showed no obvious inhibitory activity. The results suggested further structure modifications of tetrahydrocurcumin to improve its anticancer activity.
研究领域:
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
PubMed
高影响因子
TALANTA
·
2020
·
IF 5.339
Jianmei Chen,Yurui Xu,Ya Gao,Lei Sun,Xia Meng,Kai Gu,Yu Zhang,Xinghai Ning
Rapid detection of cell viability is of importance for various aspects of basic and applied research. However, the most commonly used MTT assay suffers from some disadvantages of time-consuming, poor solubility of formazan crystals, and interference of cell extracts, resulting in either delayed results or inconsistent cell viability. Accumulating evidences show that mitochondrial activity is closely associated with cell proliferation and apoptosis, making it valuable for real-time monitoring of cell fates. Herein, we present a novel type of cell-permeant mitochondrial dyes, composed of coumarin-quinoline conjugates (CQCs), for assessing cell viability through monitoring mitochondrial dynamic changes. CQCs exhibited superior preference for mitochondria, and could sensitively monitor their fissions under pathological conditions. Particularly, CQCs could accurately assess the cell viability within 10 min, allowing for rapidly evaluating therapeutic effects with high sensitivity and accuracy, in comparison of MTT assay. Therefore, CQCs provide a proof-of-concept assay that is appropriately practical either independently or in complementation with other assays for the analysis of cellular viability in broad range of biomedical applications.
研究领域:
细胞生物学
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药理学
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生物医学工程
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DOI
PubMed
高影响因子
EUROPEAN POLYMER JOURNAL
·
2024
·
IF 5.8
Chenyu Liu,Shuli Yue,Ruizhi Li,Lin Wang,Kun Zhang,Shiwei Wang,Simiao Yu,Farishta Shafiq,Yao Liu,Weihong Qiao
In response to the pain, swelling, and redness resulting from inadequate wound hemostasis and anti-inflammatory measures, there is a pressing need to develop wound repair materials capable of promptly stopping bleeding, facilitating painless dressing changes, and expediting wound closure to enhance skin wound recovery. However, comprehensive research is deficient concerning the conformational relationship of hyaluronic acid (HA) with various molecular weights concerning the structure of hydrogel materials. This study aims to address this need by utilizing aminated hyaluronic acid (AHA) and aldehyde-modified dextran (DA) to prepare dextran-based hyaluronic acid hydrogels (DA-AHA) via Schiff base reaction, imbuing them with acute inflammation repair and wound healing promotion properties. In vitro, coagulation experiments demonstrated that the DA-AHA hydrogel could rapidly coagulate blood within 60 s. Subsequent animal experiments corroborated these findings, revealing the hydrogel’s efficacy in significantly shortening wound healing time and accelerating wound closure efficiency. Moreover, MTT and live-death experiments affirmed the non-cytotoxic nature of the synthesized hydrogel. The study delved into the structural regularity and wound-healing efficacy of DA-AHA hydrogel materials featuring various molecular weights. Additionally, it compared the hemostatic and wound-healing properties of (high molecular weight dextran-aminated hyaluronic acid hydrogel) HDA-AHA, demonstrating its superiority in both aspects.
研究领域:
材料科学
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生物材料
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伤口愈合
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生物医学工程
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产品关联
DOI
高影响因子
RUSSIAN JOURNAL OF COORDINATION CHEMISTRY
·
2014
·Vol. 40
·期 10
·764-767
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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
Food Science & Nutrition
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2024
·
IF 3.5
Peiyu Xue,Hongmei Zhao,Xinyong You,Weiming Yue
Lactoferrin and polyphenols are common natural functional compounds. Their interactions and the consequential alterations in functional activity have received widespread attention. The work aimed to investigate the interaction between lactoferrin and kaempferol, as well as evaluate the in vitro anticancer properties of the lactoferrin–kaempferol complex. The results of the spectra experiments revealed that lactoferrin and kaempferol are capable of forming complexes to quench the endogenous fluorescence of lactoferrin. Further insight into the binding mechanism was gained through molecular docking and molecular dynamics simulations. These analyses suggest that both hydrophobic interactions and hydrogen bonding are essential factors in the interaction between lactoferrin and kaempferol. Furthermore, the MTT assay and apoptosis by flow cytometry were conducted, revealing a synergistic effect of kaempferol and lactoferrin on the inhibition of HeLa cell proliferation. The findings from this investigation could improve our understanding of lactoferrin's interaction with polyphenols and the role of the lactoferrin–kaempferol complex in inhibiting cancer cell proliferation.
研究领域:
药理学
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癌症研究
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分子生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
Oncology Letters
·
2018
·Vol. 15
·期 4
·5739-5743
·
IF 1.664
Hua Zhang,Yumei Cao,Yuru Chen,Guangxi Li,Hanshu Yu
The present study investigated the inhibitory effects of apatinib on the proliferation of the SMMC-7721 hepatocellular carcinoma cell line to explore the possible mechanism. The MTT assay was used to detect the inhibitory effects of the different concentrations of apatinib on the proliferation of SMMC-7721 cells. Annexin V/PI double staining was performed to investigate the effects of apatinib on the apoptosis of SMMC‑7721 cells. Expression of the apoptosis-related genes Bcl-2, Bax and caspase-9 after apatinib treatment was detected by reverse transcription‑quantitative PCR (RT-qPCR) and western blot analysis. Expression of the PI3K, p-PI3K, Akt and p-Akt proteins after apatinib treatment was detected using western blot analysis. The MTT results showed that apatinib inhibited the in vitro proliferation of SMMC-7721 cells. Annexin V/PI double staining showed that apatinib induced the apoptosis of SMMC‑7721 cells in a concentration-dependent manner. Results of RT-qPCR and western blot analysis showed that apatinib was able to induce the expression of pro-apoptotic genes Bax and caspase-9 and inhibited the expression of anti-apoptotic gene Bcl-2. In addition, the western blot analysis revealed that p-PI3K and p-Akt was significantly decreased following apatinib treatment, while no significant differences were found in the total protein levels of PI3K and Akt. The results of the present show that apatinib is capable of promoting the apoptosis of SMMC-7721 cells by inhibiting the PI3K/Akt signal transduction pathway, upregulating the expression of pro-apoptotic genes Bax and caspase-9, and downregulating the expression level of the anti-apoptotic gene Bcl-2.
研究领域:
肿瘤学
·
分子生物学
·
细胞生物学
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产品关联
DOI
PubMed
高影响因子
Materials Today Communications
·
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
·
高分子化学
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药学
·
生物医学工程
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2016
·
IF 3.138
Ke Ming,Yun Chen,Fangke Yao,Jintong Shi,Jingjing Yang,Hongxu Du,Xunyi Wang,Yixuan Wang,Jiaguo Liu
To screen effective anti-duck hepatitis A virus (DHAV) drugs, we applied STMP-STPP method to prepare phosphorylated Codonopsis pilosula polysaccharide (pCPPS), the phosphorylation-modified product of Codonopsis pilosula polysaccharide (CPPS). The IR spectrum and field emission scanning electron microscope (FE-SEM) were subsequently used to analyze the structure of pCPPS. Several tests were conducted to compare the anti-DHAV activities of CPPS and pCPPS. The MTT method was used to compare the effect of the drugs on DHAV-infected duck embryonic hepatocytes (DEHs), and the Reed-Muench assay was employed to observe changes in the virulence of DHAV. We also applied real-time PCR to examine the relationship between virus replication and the expression of IFN-β. The results indicated that CPPS could not inhibit the replication of DHAV. In contrast, pCPPS increased the virus TCID 50 , inhibited viral replication and, accordingly, increased the survival rate of DEHs infected with DHAV. Because DHAV induced the expression of IFN-β, and the IFN-β expression level was positively associated with the number of DHAV, the reduction of IFN-β expression levels after pCPPS treatment demonstrated a decrease in the number of virus particles. These results indicated that pCPPS, which reduces the number of DHAV, was more effective than CPPS in anti-DHAV activity.
研究领域:
病毒学
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药理学
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分子生物学
✓ 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）