ARCHIVES OF PHARMACAL RESEARCH
·
2016
·Vol. 39
·期 7
·871-877
·
IF 2.49
Li Da-hong,Guo Jia,Bin Wen,Zhao Nan,Wang Kai-bo,Li Jian-yong,Li Zhan-lin,Hua Hui-ming
Two novel rare chloro-containing benzylisoquinoline alkaloids, thalfoliolosumines A ( 1 ) and B ( 2 ), along with eight known isoquinoline alkaloids ( 3 – 10 ) were isolated from the whole plant of Thalictrum foliolosum . The structures of these compounds were elucidated by spectral analyses, including 1D and 2D NMR (COSY, HSQC, HMBC and NOESY) experiments. The antiproliferative effects of all the isolated compounds were evaluated by MTT method against MCF-7, PC-3, and U937 cells, and trypan blue method against HL-60 cells. New compounds 1 and 2 exhibited moderate in vitro antiproliferative activity against MCF-7, PC-3, and HL-60 cells, and good inhibitory effects against U937 cells with IC 50 values of 7.50 and 6.97 μM, respectively. Compounds 7 and 10 showed the strongest in vitro antiproliferative with IC 50 values of 0.93 and 1.69 μM against HL-60 cell line. The antioxidant properties were also measured, bisbenzyltetrahydroisoquinoline alkaloids 3 – 6 showed the strongest antioxidant activities in ABTS assay.
研究领域:
药理学
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植物化学
·
肿瘤学
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产品关联
DOI
PubMed
高影响因子
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
·
药物化学
✓ 已验证
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
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
·
肿瘤学
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植物科学
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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
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
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产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL CHEMISTRY JOURNAL
·
2024
·Vol. 57
·期 8
·1174-1178
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IF 0.8
Zheng Qing-Xuan,Wang Rui,Li Hui-Jing,Dehaen Wim,Huai Qi-Yong
Oleanolic acid (OA) is a natural product with certain antitumor activity. In order to enhance its cytotoxicity, a total of five derivatives of OA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells), A549 cells (human nonsmall cell lung cancer cells) and BEAS-2B cells (human cervical cancer cells) were evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The results indicated that these target compounds have a wide molar activity range and some of them showed better activity than the commercial drug, doxorubicin. Compound 2a induces apoptosis of 14, 27, and 56% of MDA-MB-231 cells at 2, 4, and 8 mM respectively, and shows a linear correlation of concentration.
研究领域:
肿瘤学
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药物化学
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分子药理学
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天然产物化学
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转化医学
✓ 已验证
DOI
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2025
·
IF 2.5
Yun Liu,Xuefang Shang,Ashraf H. Abadi,Mingpan Cheng
To address the challenge of antibiotic resistance and enhance the functionality of pharmaceutical materials, aldehyde chitosan-based dynamic polymers (ACs) incorporating amikacin and cefotaxime, denoted as ACs-amikacin and ACs-cefotaxime, respectively, were synthesized. These polymer's chemical structure was characterized using 1H-NMR and FT-IR analysis. Subsequently, methylthiazolyldiphenyl-tetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays were employed to evaluate their safety. Furthermore, it was demonstrated that these polymers retained the antibacterial activity of the antibiotics. This study introduces a novel strategy for dynamic natural materials capable of exerting a synergistic effect in pharmaceutical applications through the conjugation of natural materials with active pharmaceutical agents.
研究领域:
药用材料
·
高分子化学
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抗菌研究
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药物递送系统
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产品关联
DOI
高影响因子
MOLECULAR DIVERSITY
·
2024
·Vol. 28
·期 6
·3713-3737
·
IF 3.9
Zhang Minjie,Chen Guifen,Chen Yafang,Sui Yi,Zhang Yan,Yang Wude,Yu Xiang
In order to develop new natural product-based anticancer agents, a series of 1,3,4-oxadiazole analogues based on petiolide A were prepared and evaluated for their anticancer activities by MTT method. The structures of all analogues were characterized by various spectral analyses, and B9 was further confirmed by X-ray crystallography. Among all the synthesized compounds, B1 displayed the most promising growth inhibitory effect on colon cancer cells (HCT116) with the IC 50 value of 8.53 μM. Flow cytometric analysis exhibited that B1 arrested the cell cycle at G2 phase and induced apoptosis. Additionally, network pharmacology analysis calculated that B1 might target several key proteins, including AKT serine/threonine kinase 1 (AKT1), SRC proto-oncogene, non-receptor tyrosine kinase (SRC) and epidermal growth factor receptor (EGFR). Furthermore, molecular docking study indicated that B1 had potentially high binding affinity to these three target proteins. Given these results, analogue B1 could be deeply developed as potential anticancer agents.
研究领域:
药物化学
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药理学
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肿瘤学
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化学生物学
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结构生物学
✓ 已验证
DOI
高影响因子
ENVIRONMENTAL POLLUTION
·
2019
·
IF 5.714
Da Lv,Yi Gu,Ming Guo,Ping Hou,Yan Li,Ronghui Wu
To better understand the toxicological activities of perfluorooctanoic acid (PFOA), we examined the effects of PFOA on apoptosis and its molecular mechanism in SMMC-7721 hepatoma cells. Cell viability was evaluated by MTT assay and apoptosis was determined by flow cytometry. Western blot and quantitative real-time PCR were used to examine the protein and gene expressions of Bax and Bcl-2. Our results showed that PFOA inhibited SMMC-7721 cell growth and induced apoptosis. PFOA treatment increased Bax expression and increased Bcl-2 expression at both gene and protein levels. Our study demonstrated that PFOA had toxic effects on SMMC-7721 cells, such as inhibiting cell proliferation and inducing apoptosis. Furthermore, we showed that PFOA-mediated induction of apoptosis involved inducing Bax and decreasing Bcl-2 expression as a molecular mechanism of its toxicological effects.
研究领域:
毒理学
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细胞生物学
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癌症研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Biobased Materials and Bioenergy
·
2022
·Vol. 16
·期 1
·117-126
·
IF 0.687
Feng Nianjie,She Shaowen,Hu Chuanqin,Wu Qian
To find new plant-derived antitumor drugs, hydrolysate and fractions of poplar were analyzed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for their inhibitory effect against liver cancer HepG-2 cells. Strong cytotoxicity of hydrolysate was revealed at
processing temperature of 180 °C or above. The hydrolysate formed at 180 °C was sequentially extracted using organic solvent to obtain five fractions, and only the diethyl ether-soluble fraction (F
De) showed specific cytotoxicity. The eluted fraction of acetone/n-hexane
(F
1) was further isolated by column chromatography separation from the F
De fraction at a yield of 70%, and could severely decrease cell viability. LC-MS chromatography indicated that 5-hydroxymethyl furfural, ρ-hydroxybenzoic acid and syringaldehyde
were the main compounds in the F
1 fraction. Furthermore, the results of flow cytometry, Western blotting, and polymerase chain reaction indicated that syringaldehyde could tightly control the growth and metabolism of HepG-2 cells. The findings could move forward the value-added
applications of lignocellulosic hydrolysate on traditional medicines.
研究领域:
植物学
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遗传学
·
肿瘤学
·
药理学
·
分析化学
✓ 已验证
DOI
高影响因子
ACS Omega
·
2023
·
IF 4.1
Yimei Tang,Kuan Yang,Siyu Zhao,Qingqing Chen,Lan Qin,Bei Qin
To solve the problems associated with poorly water-soluble nonsteroidal anti-inflammatory drugs (NSAIDs), naproxen-based ionic liquids (ILs) containing naproxen as an active pharmaceutical ingredient (API) anion were prepared with benzalkonium (tetradecyldimethylbenzyl ammonium), choline, and 1-octyl-3-methylimidazole as the cation. The structures and thermal properties were analyzed. Through the conductivity method, the solubility at 25 and 37 °C and the critical micelle concentration (CMC) at 25 °C were determined in water and ethanol. The octanol–water partition coefficients (Kow) at 25 °C were measured with the shake-flask method. The cytotoxicity was evaluated with the MTT method. The results showed that the conversion of naproxen into the API-ILs increased the API’s solubility in water by more than 850 times compared with the original API, and the thermostability was satisfactory with a lower glass transition temperature (tg). Moreover, the variation trends of solubility, hydrophilicity, and Kow were consistent with the different structures of naproxen-based ILs, except for benzalkonium naproxen. The CMC (10–5–10–6 M) in water and ethanol demonstrated that the naproxen-based ILs were surface activite ILs. The IC50 values exhibited the low cytotoxicity of the naproxen-based ILs, which was better than 100 μM. The results provide essential information and a research basis for future topical and transdermal administration and oral administration of naproxen-based ILs.
研究领域:
药学
·
化学
·
药理学
✓ 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）