Due to the limitations of current anti-HBV therapies, the HBV core (HBc or HBcAg) protein assembly modulators (CpAMs) are believed to be potential anti-HBV agents. Therefore, discovering safe and efficient CpAMs is of great value. In this study, we established a HiBiT-based high-throughput screening system targeting HBc and screened novel CpAMs from an in-house marine chemicals library. A novel lead compound 8a, a derivative of the marine natural product naamidine J, has been successfully screened for potential anti-HBV activity. Bioactivity-driven synthesis was then conducted, and the structure‒activity relationship was analyzed, resulting in the discovery of the most effective compound 11a (IC₅₀ = 0.24 μmol/L). Furthermore, 11a was found to significantly inhibit HBV replication in multiple cell models and exhibit a synergistic effect with tenofovir disoproxil fumarate (TDF) and IFNa2 in vitro for anti-HBV activity. Treatment with 11a in a hydrodynamic-injection mouse model demonstrated significant anti-HBV activity without apparent hepatotoxicity. These findings suggest that the naamidine J derivative 11a could be used as the HBV core protein assembly modulator to develop safe and effective anti-HBV therapies.

Objective:To evaluate the clinical efficacy of lumbar spine warming needle moxibustion of Jiaji and Traditional Chinese Medicine (TCM) fumigation combined with conventional western medicine therapy on patients with acute inflammatory period of lumbar disc herniation (LDH).Methods:Randomized controlled trial. A total of 140 patients with acute inflammation of LDH in our hospital from December 2019 to December 2021 were selected as observational objects, and the patients meeting the inclusion criteria were divided into 2 groups with 70 patients in each group by random number table method. The control group was treated with conventional western medicine therapy, and the observational group was treated with warming needle moxibustion of Jiaji combined with TCM fumigation on the basis of control group treatment. Both groups received continuous treatment for 1 month. TCM syndrome scores were performed before and after treatment, the degree of lumbar pain was assessed by VAS, the degree of lumbar dysfunction was assessed by Japanese Orthopaedic Association Evaluation Treatment (JOA score), and serum CRP, IL-6 and TNF-α levels were measured by ELISA.Results:The total effective rate was 95.71% (67/70) in the observation group and 82.86% (58/70) in the control group, and there was significant difference between the two groups ( χ2=6.05, P=0.014). After treatment, TCM syndrome score [(4.45±1.09) vs. (10.67±2.82), t=16.85], VAS score [(1.54±0.43) vs. (3.28±1.04), t=12.94] lower than those in the control group ( P<0.01), subjective feeling [(7.54±2.87) vs. (6.24±1.76), t=5.72], physical signs [(6.76±2.00) vs. (4.34±1.67), t=7.77], limited daily activities [(9.56±3.27) vs. (7.89±2.97), t=3.16], bladder function score [(2.88±0.84) vs. (2.63±0.64), t=2.89] and the total score [(25.04±7.44) vs. (20.35±6.87), t=4.63] were higher than those in the control group ( P<0.01). After treatment, serum IL-6 [(18.12±4.23) μg/L vs. (26.46±4.58) μg/L, t=11.19], CRP [(18.87±6.07) mg/L vs. (25.89±5.72) mg/L, t=7.04] and TNF-α levels [(24.42±5.37) ng/L vs. (29.45±5.44) ng/L, t=5.51] were lower than those in the control group ( P<0.01). Conclusion:The warming needle moxibustion of Jiaji and TCM fumigation combined with conventional western medicine therapy can improve the lumbar pain of LDH patients in acute inflammatory stage, reduce the level of inflammatory factors, improve clinical efficacy.

Objective To compare the clinical outcomes between open reduction and fixation with cannulated screws via the modified Burks-Schaffer approach versus arthroscopic EndoButton plating for avulsion fracture of the tibial attachment of the posterior cruciate ligament(PCL).Methods From February 2013 to August 2017,41 patients with acute displaced avulsion fracture of the tibial PCL attachment were treated operatively at Department of Trauma Surgery,The Affiliated Hospital to Qingdao University.They were 24 men and 17 women,aged from 18 to 65 years (average,39 years).The lefi knee was injured in 22cases and the right knee in 19.They were divided into 2 groups according to their different fixation methods.The open reduction and fixation group (23 cases) received open reduction and fixation with cannulated screws via the modified Burks-Schaffer approach while the arthroscopic group (18 cases) arthroscopic Endobutton plating.The 2 groups were compared in terms of operation time,bleeding,objective knee scores and knee range of motion (ROM) after operation.Results All the 41 patients were followed up from 23 to 40months (average,27.2 months).Their follow-up revealed no incision infection,malunion,nonunion or loosening of the implants.Their knee X-ray films at the final follow-ups showed bony union of all the avulsion fractures.There were significant differences between the open reduction and fixation group and the arthroscopic group in operation time (52.6±7.3 min versus 86.8±9.2 min) and bleeding (63.9±12.7 mL versus 19.7 ± 10.2 mL) (P ＜ 0.05).There was no significant difference in the objective knee scores or knee ROM between the 2 groups (P ＞ 0.05).Conclusions Both open reduction and cannulated screw fixation via the modified Burks-Schaffer approach and arthroscopic EndoButton plating can achieve satisfactory clinical outcomes in the treatment of avulsion fracture of the tibial PCL attachment.Although the 2 methods make no significant differences in stability of the knee joint or in clinical scores,the latter leads to less bleeding and the former shorter operation time.

OBJECTIVETo find an inhibitor to reduce the volatilization of formalin.

METHODThe saturated solution of sodium hydrosulphite (SHS) was sprayed on the surface of the anatomy specimens, then the concentration of formaldehyde in the air was tested.

RESULTSThe concentration of formaldehyde in the air of SHS sprayed group [(3.10 +/- 1.22) mg/m3] was significantly lower than that of the control group [(8.36 +/- 4.11) mg/m3, P < 0.01].

CONCLUSIONSHS may be a volatilization inhibitor for formalin, which could reduce the concentration of formaldehyde in the air.

Air Pollution, Indoor ; prevention & control ; Anatomy ; Formaldehyde ; analysis ; chemistry ; Sulfites ; chemistry ; Volatilization