INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yunwen Zhu,Yaping Li,Xue Li,Tongfei Chen,Hepeng Zhao,Hongli Zhou
Corn silk is the stigma and style of corn and is rich in polysaccharides. Despite the extensive research on its polysaccharides, the hemostatic characteristics of effective parts and the related activities remain insufficiently explored. Corn silk polysaccharide (CSP) was extracted with hot water and purified using a diethylaminoethyl cellulose membrane. Then, it was separated with sephadex G-150 to obtain five fractions. These fractions were investigated for their potential in hemostasis, antioxidant, immune response, and anti-lung cancer activities. CSP-2, CSP-3, and CSP-4 significantly affected the coagulation indicators activated partial thromboplastin time (APTT) and thrombin time (TT) at 125–500 μg/mL. Corn silk flavonoids and saponins at 32.25 μg/mL significantly prolonged APTT, TT, and prothrombin time (PT). CSP-2, with potent antioxidant ability, approaches Vitamin C. At 25 μg/mL, CSPs nearly reached the phagocytosis of neutral red of lipopolysaccharides. The five fractions promoted the proliferation of RAW264.7 cells at 25–800 μg/mL and stimulated NO secretion at 25–100 μg/mL. CSP-2 also showed an 86 % inhibition rate effect on A549 at 200 μg/mL. These results indicate that CSP not only has hemostatic effects but also has immune and anti-lung cancer activities. Thus, it is a potential candidate compound with immune activity for managing bleeding in cancer.
研究领域:
药理学
·
生物化学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ARCHIV DER PHARMAZIE
·
2022
·Vol. 355
·期 7
·2100465
·
IF 4.613
Yating Guo,Xiaoding Jiang,Qi Chang,Zhihong Xiao,Zhuo Chen,Dejian Jiang,Gaoyun Hu,Qianbin Li
A series of novel pyrazolo[3,4- b ]pyridine derivatives were designed, synthesized, and biologically evaluated for anti-lung cancer activity. Structure–activity relationship and AutoGPA models were constructed based on the in vitro antiproliferative potency of the compounds against a human lung adenocarcinoma cell line (A549). Compound 9d exhibits improved potency for A549 cell growth inhibition (3.06 ± 0.05 μM) compared with A-769662 (45.29 ± 2.14 μM). Compound 9d can elevate the phosphorylation levels of adenosine monophosphate-activated protein kinase (AMPK) and its substrate acetyl-CoA carboxylase and reduce the level of phosphorylated ribosomal S6 kinase (p-70S6K) at 1 μM, which is comparable to the activity of A-769662 at 20 μM. 9d induced G2/M cell cycle arrest, which was rescued when co-incubated with “Compound C,” a potent AMPK inhibitor. Taken together, compound 9d showed potential anti-lung cancer activity via inducing cell cycle arrest by regulation of the AMPK/70S6K pathway in A549 cells, which could provide a new lead for the discovery of anti-lung cancer agents.
研究领域:
药物化学
·
癌症研究
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
Drug Delivery and Translational Research
·
2019
·Vol. 9
·期 3
·667-678
·
IF 3.111
Zhang Qian,Tian Xin,Cao Xiufeng
In this study, we developed an intravenously injectable, transferrin-functionalised microemulsion that simultaneously carries β-elemene and celastrol (called Tf-EC-MEs) for enhanced anti-lung cancer treatment and reduced systemic toxicity. These dual-drug-loaded Tf-EC-MEs not only displayed synergistic antiproliferative effects on cultured cells in vitro, but also showed enhanced efficacy in vivo via active tumour targeting. In preparatory experiments, we found that β-elemene was capable of being used as oil phase, which enhanced drug-loading efficiency and allowed the mass ratio of β-elemene and celastrol to be optimised. In cellular studies, Tf-EC-MEs exhibited significantly improved A549 cellular uptake compared with β-elemene+celastrol (conventional combination treatment) and EC-MEs (non-active targeted treatment), demonstrating remarkable synergistic antiproliferative effects and higher rates of cell apoptosis. In A549-bearing xenograft mouse tumour models, Tf-EC-MEs exhibited enhanced antitumour activity compared to all other treatments. More importantly, Tf-EC-MEs did not cause the obvious systemic toxicity commonly found with mono-celastrol treatment. Collectively, these findings suggest that Tf-EC-MEs are a promising strategy for the combination drug treatment of lung cancer.
研究领域:
药学
·
肿瘤学
·
药物递送系统
·
癌症治疗
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
·
2013
·
IF 3.848
Lin-Hui Zhang,Yong-Liang Jia,Xi-Xi Lin,Hong-Quan Zhang,Xin-Wei Dong,Jun-Ming Zhao,Jian Shen,Hui-Juan Shen,Fen-fen Li,Xiao-Feng Yan,Wei Li,Yu-Qing Zhao,Qiang-Min Xie
Background Ginseng is a traditional Chinese herb that has been used for thousands of years. In the present study, effects and mechanisms of AD-1 were evaluated for its development as a novel anti-lung cancer drug. Methods The cytotoxic activity was evaluated by MTT assay. Flow cytometry was employed to detect cell cycle, apoptosis and ROS. Western blot and immunohistochemistry were used to analyze signaling pathways. Lung cancer xenograft models were established by subcutaneous implantation of A549 or H292 cells into nude mice. Results AD-1 concentration-dependently reduces lung cancer cell viability without affecting normal human lung epithelial cell viability. In A549 and H292 lung cancer cells, AD-1 induces G 0 /G 1 cell cycle arrest, apoptosis and ROS production. The apoptosis can be attenuated by a ROS scavenger — N-acetylcysteine (NAC). In addition, AD-1 up-regulates the expression of p38 and ERK phosphorylation. Addition of a p38 inhibitor SB203580, suppresses the AD-1-induced decrease in cell viability. Furthermore, genetic silencing of p38 attenuates the expression of p38 and decreases the AD-1-induced apoptosis. Treatment with NAC reduces AD-1-induced p38 phosphorylation, which indicates that ROS generation is involved in the AD-1-induced p38 activation. In mice, oral administration of AD-1 (10–40 mg/kg) dose-dependently inhibited the growth of xenograft tumors without affecting body weight and decreases the expression of VEGF, MMP-9 and CD34 in tumor tissue. TUNEL staining confirms that the tumors from AD-1 treated mice exhibit a markedly higher apoptotic index. Conclusions and general significance These data support development of AD-1 as a potential agent for lung cancer therapy.
研究领域:
肿瘤学
·
药理学
·
细胞生物学
·
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）