BIOMEDICAL CHROMATOGRAPHY
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2017
·Vol. 32
·期 2
·e4094
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IF 1.613
Guogai Zhang,Lifang Zhao,Jiancheng Zhu,Yifan Feng,Xia Wu
Alpinia officinarum is used for its anti-inflammatory activity historically in China. Diarylheptanoids isolated from A. officinarum play important biological roles in the prevention and treatment of inflammatory disorders. Seven diarylheptanoids (1–7) were isolated from A. officinarum . The cell viabilities and anti-inflammatory activities of diarylheptanoids were evaluated by MTT assay and tumor necrosis factor- α production in Kdo2-lipid A-stimulated RAW 264.7 cells in vitro . The relationships between their anti-inflammatories and structure-activities are discussed. The results indicated that compounds 1 and 3–7 had significant anti-inflammatory activities. The relationships between inflammation and phospholipids metabolism were elucidated by multivariate data analysis. Twenty-two potential biomarkers were identified in inflammatory group vs. blank group, and 11 potential biomarkers were identified for inflammatory group vs. drug-treatment groups. Ten common phospholipids were characterized. On the basis of a previous study in our laboratory, we found that phosphatidylethanolamine (18:0/18:1) might be the important glycerophospholipid biomarker in inflammation. In this study, we firstly combined anti-inflammatory activities and glycerophospholipids changes of traditional Chinese medicine. This work suggests that the anti-inflammatory activities of diarylheptanoids might be significantly related to glycerophospholipids and could provide a useful database for investigating the anti-inflammatory effects of traditional Chinese medicine.
研究领域:
药理学
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生物化学
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中药学
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细胞生物学
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DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2023
·Vol. 24
·期 4
·1-18
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IF 3.3
Cao Xia,Liu Qi,Adu-Frimpong Michael,Shi Wenwan,liu Kai,Deng Tianwen,Yuan Hui,Weng Xuedi,Gao Yihong,Yu Qingtong,Deng Wenwen,Yu Jiangnan,Wang Qilong,Xiao Gao,Xu Ximing
Glioma, in which a malignant tumor cell occurs in neural mesenchymal cells, has a rapid progression and poor prognosis, which is still far from desirable in clinical treatments. We developed a lab-on-a-chip (LOC) device for the rapid and efficient preparation of vitexin/indocyanine green (ICG) liposomes. Vitexin could be released from liposome to kill cancer cell, which can potentially improve the glioma therapeutic effect and reduce the treatment time through synergistic photodynamic/photothermal therapies (PDT/PTT). The vitexin/ICG liposome was fabricated via LOC and its physicochemical property and release in vitro were evaluated. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and live/dead staining were used to examine the enhanced antitumor effect of vitexin/ICG liposome in cooperation with PDT/PTT, while the related mechanism was explored by flow cytometry and western blot. The results were as follows: (1) The prepared vitexin/ICG liposome was smaller in size, homogenous in particle size distribution with significant low polydispersity index (PDI), and enhanced cumulative release in vitro . (2) We found that the formulated liposome presented strong cancer cell inhibition and suppression of its migration in a dose-dependent manner. (3) Further mechanistic studies showed that liposome combined with near-infrared irradiation could significantly upregulate levels of B cell lymphoma 2-associated X (Bax) protein and decrease B cell lymphoma 2 (Bcl-2) at protein levels. The vitexin/ICG liposomes prepared based on a simple LOC platform can effectively enhance the solubility of insoluble drugs, and the combined effect of PTT/PDT can effectively increase their antitumor effect, which provides a simple and valid method for the clinical translation of liposomes. Graphical Abstract
研究领域:
肿瘤学
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药学
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生物医学工程
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纳米技术
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DOI
PubMed
高影响因子
SYNTHETIC COMMUNICATIONS
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2023
·
IF 2.1
Jun Yang,Guang-Ping Liang,Xiong-Li Liu
To investigate the effects and mechanisms of 4-(1H-indol-1-yl)-4-oxobutanoic acid spliced podophyllotoxin derivatives (3a–3l) on tumor cells. The MTT method was adopted to evaluate (3a–3l) antitumor activity in vitro against A549 cells, A549/DDP cells, MCF-7 cells. The results showed that compound 3l had the most prominent inhibitory effect and high selectivity with IC50 18.53 ± 1.51 µM against A549/DDP cells. Meanwhile, the effects of compound 3l on the nuclear state, cell cycle and apoptosis of A549/DDP cells showed that compound 3l induced apoptosis by delaying the G2/M phase of A549/DDP cell cycle. In addition, molecular docking of compound 3l also showed that it could form a good hydrogen bond with ARG-158 (d = 2.6, 2.7 Å) and HIS-406 (d = 2.5 Å) at the colchicine site of tubulin. Compound 3l could provide lead compound for the development of new multi-drug resistant anti-tumor drugs.
研究领域:
药理学
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肿瘤学
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化学
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分子生物学
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DOI
高影响因子
Drug Design Development and Therapy
·
2017
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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
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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
SEPARATION AND PURIFICATION TECHNOLOGY
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2024
·
IF 8.1
Xin Liang,Sheng Wang,Jing Zhou,Tengfei Lu,Kaiyu Ruan,Yuqian Xia,Tong Wang
Despite the considerable attention received by switchable solvents in natural product extraction and biorefinery. To tackle this issue, the present study has the following innovative endeavors: (1) Developing an innovative high-speed homogenization assisted extraction method using the DES/SHS/H 2 O system and applying it to the integrated extraction of phenolics, flavonoids, and essential oil from Flos Chrysanthemi Indici . The switching process was characterized using 1 H NMR, the extraction process was optimized employing response surface methodology, the components of extracted essential oils were analyzed by GC–MS, and the cytotoxicity and anti-inflammatory activity of essential oils were determined through MTT and ELISA. Our findings demonstrate that the incorporation of DES can significantly augment the CO 2 switching kinetics of SHS, resulting in a 32.7 % reduction in switching time and a remarkable decrease of 73.7 % residual content within the aqueous phase. The innovative DES/SHS/H 2 O based extraction method exhibited substantial enhancements in phenolics, flavonoids, and essential oil extraction efficiency compared to conventional approaches, yielding extracts with superior chemical profiles and enhanced anti-inflammatory activity. Therefore, the proposed strategy of enhancing the CO 2 switching kinetic properties and extraction ability of SHS by incorporating DES is feasible, providing valuable guidance for the rational design of innovative smart solvent systems. The developed DES/SHS/H 2 O system, exhibiting improved performance, holds significant application and research prospects.
研究领域:
化学工程
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药学
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分析化学
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生物技术
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天然产物研究
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DOI
高影响因子
Arabian Journal of Chemistry
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2023
·
IF 6
Tianming Zhao,Guang Fan,You Tai,Xinhe Shu,Fu Tian,Shuliang Zou,Qin Wu
Illicium lanceolatum is a medicinal and aromatic plant widely distributed in the south of China. The reports on chemical composition and biological activities of its essential oils (EOs) were very limited. In this study, Illicium lanceolatum EOs were extracted by hydro distillation, and analyzed by GC–MS and GC-FID. DPPH radical scavenging assay, ABTS cation radical scavenging assay and ferric reducing/antioxidant power (FRAP) assay were used for antioxidant activity evaluation. Minimum inhibitory concentrations (MICs) and minimum microbiocidal concentrations (MMCs) against 9 microorganisms were determined. The inhibitory effects on tyrosinase, α -glucosidase and cholinesterases were evaluated and cytotoxic activities were evaluated using MTT assay. The results revealed 110 identified compounds, with asaricin, eucalyptol, linalool and caryophyllene oxide as major compounds. Eucalyptol was the most abundant compound in the stem, leaf and fruit EOs while asaricin accounted for 50.52 ± 0.33 % in the root EO. Very weak radical scavenging capacities were noticed for all EOs, but the root EO showed moderate antioxidant activity (176.33 ± 4.52 mg TE/g of EO) in the FRAP assay, which could be attributed to asaricin. The root EO displayed better antimicrobial activities than other three EOs, with MIC values as 3.13 mg/mL against three bacteria including Staphylococcus aureus BNCC 186335, Bacillus cereus BNCC 103930 and Listeria monocytogenes BNCC 336877. Camphor and borneol were found to be important antimicrobial compounds. No inhibitory effect on α -glucosidase was found. The leaf EO displayed better acetylcholinesterase inhibitory activity (17.79 ± 0.32 mg GE/g of EO) while the root EO showed better tyrosinase (30.34 ± 0.40 mg KAE/g of EO) and butyrylcholinesterase (43.25 ± 1.50 mg GE/g of EO) inhibitory activities. Molecular docking between active compounds and enzymes revealed the main interactions as hydrophobic interaction, hydrogen bond and π -stacking. All EOs displayed weak cytotoxicity to HK-2 cells of normal kidney at six tested concentrations. The leaf EO showed strong anticancer activities to HepG2 cells at the concentration of 500 μg/mL. I. lanceolatum EOs showed promising prospects with possible applications in pharmaceutical and cosmetic industries.
研究领域:
药理学
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生物化学
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微生物学
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植物科学
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药物化学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）