ONCOLOGY / CLINICAL RESEARCH
A pre-clinical trial study on afzelin: anti-human lung cancer, anti-cholinesterase, and anti-glucosidase properties
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1
Department of Cerebral Surgery, The First Hospital Affiliated with Shandong First Medical University, Jinan, Shandong Province, China
2
Department of Respiratory and Critical Care, The First Hospital Affiliated with Shandong First Medical University, Lixia District, Jinan, Shandong Province, China
Submission date: 2021-04-16
Final revision date: 2021-04-27
Acceptance date: 2021-04-29
Online publication date: 2021-05-14
Corresponding author
Junling Wang
Department of Respiratory and Critical Care, The First Hospital Affiliated with Shandong First Medical University, No.16766, Lixia District,Jingshi Road,Jinan,Shandong Province,250014,China., China
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ABSTRACT
Introduction:
Afzelin is a glycosyloxyflavone that consists of kaempferol attached to an α-L-rhamnosyl residue at position 3 via a glycosidic linkage. It has a role as a plant metabolite, an antibacterial agent and an anti-inflammatory agent. It is a glycosyloxyflavone, a trihydroxyflavone and a monosaccharide derivative. In this study, we determined the anticholinergic, antiepileptic, antidiabetic, and anti-human lung cancer capacities of afzelin.
Material and methods:
IC50 values were calculated for both acetylcholinesterase and α-glycosidase as key enzymes affected by afzelin. The cytotoxicity and anticancer potential of afzelin in human lung was evaluated using the common cytotoxicity test, i.e. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay in in vitro conditions.
Results:
IC50 values of 365.11 nM for acetyl cholinesterase and 0.94 nM for α-glycosidase were calculated in this study. For these enzymes, Ki values were found to be 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 towards the normal cell line.
Conclusions:
Afzelin shows significant antioxidant and anti-human lung cancer properties. It appears that the anti-human lung carcinoma effect of afzelin is due to its antioxidant effects.