In vitro and In silico Evaluation of Piperine Compound as a Potential Anticancer Agent in Inhibiting Growth of Nasopharyngeal Carcinoma Cells

Adrianne Dien Yu, Vong (2024) In vitro and In silico Evaluation of Piperine Compound as a Potential Anticancer Agent in Inhibiting Growth of Nasopharyngeal Carcinoma Cells. Masters thesis, UNIMAS.

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Abstract

Piperine is a popular secondary metabolite derived from the fruits of black pepper plant. Prior researches have shown that piperine exhibited anticancer effects against numerous carcinoma cell lines. To date, there have not been any studies conducted to evaluate the anticancer effect of piperine against nasopharyngeal carcinoma (NPC) cell lines. Hence, this study aimed to investigate the cytotoxicity and selectivity potential of piperine on NPC cells and to study the molecular interaction of piperine and a panel of proteins via molecular docking technique. A total of five cell lines (NP69, TW01, HK1, TW04 and C666-1) were used in this study. The cytotoxicity assay revealed that piperine inhibited the proliferation of normal nasopharyngeal epithelial (NPE) and NPC cells. With reference to the reported IC50 value, SI value for all four NPC cell lines was recorded to be less than 1. This demonstrated that piperine treatment did not show selective toxicity for NPC cells. In addition, the in vitro results suggested that the caspase-3 activity of the NPE and NPC cell lines were effectively increased upon piperine treatment at 20 μg/mL and 40 μg/mL. Conversely, in the 60 μg/mL treatment group, the lowest caspase-3 activity was reported for all cell lines. This suggested a possibility for piperine to act through a different signalling pathway or cell death mechanisms in order to suppress cell proliferation. The AutoDock Vina software was used for the molecular docking simulation Generally, a negative binding value was recorded for all the protein-ligand complexes. This indicated a spontaneous binding between piperine and the relevant proteins. Additionally, a lower binding affinity was reported in several Toll like receptor (TLR) proteins which were TLR2, TLR6 and TLR8. This showed a higher potency for piperine to regulate cellular responses via the TLRs signalling pathway. In summary, the in vitro results showed that piperine suppressed the growth of NPC cells by the activation of apoptosis whereas the in silico data provided an additional information on the molecular interaction between piperine and the corresponding proteins.

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