OBJECTIVE: To explore the inhibition of artesunate on growth of transplanted human gastric cancer through Toll-like receptor（TLR） 4/nuclear factor κB（NF-κB） signaling pathway and its effects on expression of proliferating cell nuclear antigen（PNCA） and ZNF139. METHODS: Forty BALB/c nude mice were inoculated with human gastric cancer cell line SGC7901 for modeling and randomly divided into the model group（0.9% sodium chloride solution）

cisplatin group（cisplatin 4 mg/kg）

artesunate group（artesunate for injection 100 mg/kg） and combination group（cisplatin 4 mg/kg + artesunate for injection 100 mg/kg）. Intratumoral injection was performed twice a week for 4 weeks. The appetite

activity

mental state and tumor growth of nude mice were recorded. Hematoxylin and Eosin staining were used for pathological detection

MTT assay was used to detect the growth of primary cells

reverse transcriptase polymerase chain reaction was used to detect the mRNA expression of PCNA

ZNF139

TLR4

MyD88 and NF-κB

and Western blotting was used to detect the relative protein expression. RESULTS: Compared with the model group

the average tumor weight of cisplatin group

artesunate group and combined group decreased significantly; compared with the cisplatin group

the average tumor weight increased and the tumor inhibition rate decreased in the artesunate group; the average tumor weight of the combination group was lower than that of the cisplatin group and artesunate group

and the tumor inhibition rate was higher than that of the cisplatin group and artesunate group

with statistically significant differences（P<0.05）. After 48 h of culture

the OD values of cisplatin group

artesunate group and combination group were lower than those of model group; the OD value of the combination group was lower than that of the cisplatin group and artesunate group

and the inhibition rate was higher than that of the cisplatin group and artesunate group

with statistically significant differences（P<0.05）. Compared with the model group

the mRNA expression of PCNA

ZNF139

TLR4

MyD88 and NF-κB in the cisplatin group

artesunate group and combination group significantly decreased; the mRNA expression of PCNA

ZNF139

TLR4

MyD88 and NF-κB of the cisplatin group were significantly lower than those of the artesunate group; the mRNA expression of PCNA

ZNF139

TLR4

MyD88 and NF-κB of the combination group were significantly lower than those of the cisplatin group and artesunate group

with statistically significant differences（P<0.05）. CONCLUSIONS: Artesunate may inhibit the growth of human gastric cancer through inhibiting the TLR4/NF-κB signaling pathway

which can down-regulate the expression of PCNA and ZNF139 and affect the proliferation

invasion and metastasis of tumor.