scholarly journals A pre-clinical trial study on Afzelin: Anti-human lung cancer, anti-cholinesterase, and anti-glucosidase properties

Author(s):  
Ming Cao ◽  
Bo Fan ◽  
Tianchang Zhen ◽  
Junling Wang

IntroductionAfzelin is a glycosyloxyflavone that is kaempferol attached to an alpha-L-rhamnosyl residue at position 3 via a glycosidic linkage. It has a role as a plant metabolite, an antimicrobial (Antibacterial and antifungal) agent and an anti-inflammatory agent. It is a glycosyloxyflavone, a trihydroxyflavone and a monosaccharide derivative. In this work, we determined the anticholinergic, antiepileptic, antidiabetic, and anti-human lung cancer capacities of afzelin.Material and methodsIC50 values were calculated for both acetylcholinesterase, and α-glycosidase as key enzymes effects of afzelin. The cytotoxicity and anticancer potential of human lung over the Afzelin using the common cytotoxicity test i.e., 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay in vitro condition.ResultsIC50 values obtained 365.11 nM for acetyl cholinesterase and 0.94 nM for α-glycosidase were calculated in this study. Indeed, for these enzymes, Ki values were found as 300.65±56.01 nM for acetyl cholinesterase and 1.65±0.11 nM for α-glucosidase. Cell viability of Afzelin was very low against lung poorly differentiated adenocarcinoma (PC-14), lung moderately differentiated adenocarcinoma (LC-2/ad), and lung well-differentiated bronchogenic adenocarcinoma (HLC-1) cell lines without any cytotoxicity on the normal cell line.ConclusionsAs mentioned, the Afzelin had significant antioxidant and anti-human lung cancer properties. It appears that the anti-human lung carcinoma effect of Afzelin is due to their antioxidant effects.

Author(s):  
Yawei Dou ◽  
shanshan Lv ◽  
Attalla F. El-kott ◽  
Ayman E. El-kenawy

IntroductionRecently, scientists have tried to increase organic chemistry productions for the treatment of many cancers such as lung cancers. In this regard, antioxidant molecules have a special place in the treatment of several cancers. The molecular docking method was found to calculate the biological activity of the 2′-Hydroxy-5′-methyl-3′-nitroacetophenone (2′-H-5′-M-3′-N) molecule against the enzymes studied.Material and methodsIn these calculations, the enzymes used are gluthation reductase (GR) enzyme and Glutathione S-Transferase (GT) enzyme, respectively. After the modeling calculations were completed, the ADME/T parameters were examined to calculate the future drug use properties of the 2′-H-5′-M-3′-N molecule. To survey the antioxidant properties of 2′-H-5′-M-3′-N, the DPPH test was used. Several human lung adenocarcinoma cell lines i.e., lung moderately differentiated adenocarcinoma (LC-2/ad), lung poorly differentiated adenocarcinoma (PC-14), and lung well-differentiated bronchogenic adenocarcinoma (HLC-1) cell lines were used to determine the anticancer properties of the recent molecule.ResultsCell viability of 2′-H-5′-M-3′-N was very low against PC-14, LC-2/ad, and HLC-1 cell lines without any cytotoxicity on the normal cell line. The IC50 values of 2′-H-5′-M-3′-N against LC-2/ad, PC-14, and HLC-1 cell lines were found 475, 250, and 691 µg/mL, respectively. The best anti-human lung cancer properties of 2′-H-5′-M-3′-N against the above cell lines was in the case of PC-14 cell line.ConclusionsAs mentioned, the 2′-H-5′-M-3′-N had significant antioxidant and anti-human lung cancer properties. It appears that the anti-human lung carcinoma effect of 2′-H-5′-M-3′-N is due to their antioxidant effects.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Ronggang Luo ◽  
Yi Zhuo ◽  
Quan Du ◽  
Rendong Xiao

Abstract Background To detect and investigate the expression of POU domain class 2 transcription factor 2 (POU2F2) in human lung cancer tissues, its role in lung cancer progression, and the potential mechanisms. Methods Immunohistochemical (IHC) assays were conducted to assess the expression of POU2F2 in human lung cancer tissues. Immunoblot assays were performed to assess the expression levels of POU2F2 in human lung cancer tissues and cell lines. CCK-8, colony formation, and transwell-migration/invasion assays were conducted to detect the effects of POU2F2 and AGO1 on the proliferaion and motility of A549 and H1299 cells in vitro. CHIP and luciferase assays were performed for the mechanism study. A tumor xenotransplantation model was used to detect the effects of POU2F2 on tumor growth in vivo. Results We found POU2F2 was highly expressed in human lung cancer tissues and cell lines, and associated with the lung cancer patients’ prognosis and clinical features. POU2F2 promoted the proliferation, and motility of lung cancer cells via targeting AGO1 in vitro. Additionally, POU2F2 promoted tumor growth of lung cancer cells via AGO1 in vivo. Conclusion We found POU2F2 was highly expressed in lung cancer cells and confirmed the involvement of POU2F2 in lung cancer progression, and thought POU2F2 could act as a potential therapeutic target for lung cancer.


1996 ◽  
Vol 14 (4) ◽  
pp. 351-357 ◽  
Author(s):  
Xin-Hai Pei ◽  
Yoichi Nakanishi ◽  
Koichi Takayama ◽  
Jun Yatsunami ◽  
Feng Bai ◽  
...  

Lung Cancer ◽  
1990 ◽  
Vol 6 (1-2) ◽  
pp. 63
Author(s):  
W Matthews ◽  
J Cook ◽  
JB Mitchell ◽  
RR Perry ◽  
S Evans ◽  
...  

2016 ◽  
Vol 37 (7) ◽  
pp. 919-929 ◽  
Author(s):  
Guo-dong Yao ◽  
Jing Yang ◽  
Qiang Li ◽  
Ye Zhang ◽  
Min Qi ◽  
...  

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