Objective To investigate the waking-up and liver-protective effects of Jianpi Xingjiu Formula in patients with mild to moderate acute alcohol intoxication and to preliminarily analyze its potential mechanisms.

Methods A total of 98 patients with mild to moderate alcohol intoxication were selected as the study subjects, and randomly divided into treatment group (oral administration of Jianpi Xingjiu Formula, n=49) and control group (intravenous injection of naloxone hydrochloride, n=49). The waking-up time, the time for complete disappearance of symptoms and traditional Chinese medicine symptom scores were compared between the two groups. The levels of liver function indicators alanine aminotransferase (ALT), aspartate aminotransferase (AST) and γ-glutamyl transpeptidase (GGT), blood ethanol concentration, superoxide dismutase (SOD), lipopolysaccharide (LPS) and inflammatory factors tumor necrosis factor-α(TNF-α) and interleukin-6 (IL-6) in the blood of the two groups were measured, and the overall clinical effective rate was evaluated. An in vitro liver injury model was established by inducing AML-12 cells with a combination of ethanol and LPS. Cell morphology, cell viability, the release of lactate dehydrogenase (LDH) and the protein expressions of the Toll-like receptor 4 (TLR4)/nuclear factor-κB (NF-κB) pathway were observed.

Results There was no statistically significant difference in the waking-up time between the two groups (P>0.05), but the time for complete disappearance of symptoms in the treatment group was significantly shorter than that in the control group (P < 0.05). After treatment, the scores of symptoms such as dizziness/headache, fatigue and dry/bitter mouth in the treatment group were significantly lower than those in the control group (P < 0.05). After treatment, the levels of ALT, AST and GGT in the treatment group were significantly lower than those in the control group (P < 0.01). After treatment, the blood alcohol concentration in the treatment group was significantly lower than that in the control group, while the SOD level was significantly higher (P < 0.05). After treatment, the levels of LPS, TNF-α and IL-6 in the blood of patients in both groups were significantly lower than those before treatment, and those in the treatment group were significantly lower than those in the control group (P < 0.05 or P < 0.01). The overall effective rate in the treatment group was 93.75%, which was significantly higher than the 65.96% in the control group (P < 0.05). There was no statistically significant difference in the incidence of adverse reactions between the two groups (P>0.05). In vitro experiments showed that Jianpi Xingjiu Formula could significantly improve hepatocyte morphology, enhance cell viability, reduce LDH release, and inhibit the overactivation of the TLR4/NF-κB signaling pathway.

Conclusion Jianpi Xingjiu Formula can effectively alleviate the clinical symptoms of mild to moderate alcohol intoxication, promote the disappearance of symptoms, and improve liver function and oxidative stress status. Its mechanism of action may be related to the inhibition of the TLR4/NF-κB inflammatory pathway.