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
·
肿瘤学
·
药物化学
✓ 已验证
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
·
化学
·
肿瘤学
·
植物科学
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DOI
PubMed
高影响因子
PHARMACEUTICAL CHEMISTRY JOURNAL
·
2024
·Vol. 57
·期 8
·1174-1178
·
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
·
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
✓ 已验证
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
·
药理学
·
肿瘤学
·
化学生物学
·
结构生物学
✓ 已验证
DOI
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
·
遗传学
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肿瘤学
·
药理学
·
分析化学
✓ 已验证
DOI
高影响因子
Drug Design Development and Therapy
·
2017
·
IF 2.822
Jingrun Chen,Junjie Liu,Dongxiao Cui,Chaoqun Yan,Liqiang Meng,Liqian Sun,Shurong Ban,Rui Ge,Taigang Liang,Qingshan Li
This study deals with the design and synthesis of a series of novel 4-methoxy-substituted and 5-methyl-substituted (3′S,4′S)-(−)-cis-khellactones. The newly synthesized compounds were characterized by 1H nuclear magnetic resonance (NMR), 13C-NMR, mass spectrometry, and elemental analysis. All the derivatives were subjected to in vitro cytotoxicity screening against HEPG-2 (human liver carcinoma), SGC-7901 (human gastric carcinoma), and LS174T (human colon carcinoma), by using the MTT assay. The results revealed that several of the 4-methoxy-substituted compounds exhibited potent cytotoxicity. Among these, compound 12e showed the highest activity against cancer cells which 50% inhibitory concentration (IC50) values were in the range of 6.1–9.2 μM with low toxicity on normal human hepatocyte. Preliminary investigation of possible mechanisms of action of compound 12e against HEPG-2 cells indicated possible induction of apoptosis, as determined by morphological observations and Annexin V/propidium iodide (PI) double staining, in addition to apparent dissipation of mitochondrial membrane potential (MMP), as measured by 5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethyl-imidacarbocyanine iodide (JC-1) staining in combination with the activation of caspase-9 and caspase-3 by Western blot analysis. Overall, the data suggest that compound 12e may be a promising potential anti-cancer agent that could act primarily by inducing apoptosis through the mitochondria-mediated intrinsic pathway in human hepatoma cells.
研究领域:
药理学
·
肿瘤学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）