Abstract
Stephania cepharantha Hayata is a traditional Chinese herbal medicine used to treat lung cancer, and its alkaloids, especially cepharanthine (CEP), were reported to be its effective ingredients. Therefore, the extraction of potential antitumor ingredients from the plant was of interest. We first explored the optimized solvent extraction of antitumor agents from S. cepharantha Hayata guided by an in vitro antitumor activity assay. The solvent for extraction and its concentration, the liquid to material ratio, extraction duration, particle size, macerating time, and the frequency of extraction were investigated using a single-factor experiment. An orthogonal design (L9, 34) was constructed to determine the suitable extraction conditions. The crude extract was then purified sequentially by macroporous adsorption resins (MR) for the enrichment of CEP. Under these optimal conditions, the yield of total alkaloids in the herbs was 3.4%, whereas the CEP content was 2.9%. Total alkaloids exhibited significant anti-proliferative activities in the A549 cell line. Our study provides means for the further development and use of the antitumor components from S. cepharantha, which has potential for application in the pharmaceutical industry.
Highlights
Lung cancer is the leading cause of cancer mortality in both men and women worldwide [1].The effectiveness of current treatment is severely limited, with an age-standardized mortality rate of 3 per 10,000 [2]
We studied the influence of selected operational variables on the extraction of total alkaloids with antitumor activity from S. cepharantha, using the orthogonal test and macroporous adsorption resins (MR)
We investigated the ability of three types of MR, D101, HPD-100, and AB-8, to obtain CEP and total alkaloid from crude extracts
Summary
Lung cancer is the leading cause of cancer mortality in both men and women worldwide [1]. The effectiveness of current treatment is severely limited, with an age-standardized mortality rate of 3 per 10,000 [2]. The application of cis-diamminedichloroplatinum (cisplatin, CDDP)-based chemotherapy and epithelial growth factor receptor tyrosine kinase inhibitor (EGFR-TKIs) is common, the five-year survival rate of stage III non-small cell lung cancer (NSCLC) patients is about 10%, and that of stage IV. The emergence of drug resistance has been a crucial factor in the failure of clinical treatment [3,4]. Natural phytochemicals obtained from medicinal plants have significantly contributed to the treatment of several human diseases including cancer [5]. Natural products derived from plants are receiving considerable attention because of their considerable antitumor activities [7].
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