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1.
Acta Pharmaceutica Sinica B ; (6): 2138-2151, 2023.
Article in English | WPRIM | ID: wpr-982831

ABSTRACT

Using chemoproteomic techniques, we first identified EIF2AK2, eEF1A1, PRDX3 and VPS4B as direct targets of berberine (BBR) for its synergistically anti-inflammatory effects. Of them, BBR has the strongest affinity with EIF2AK2 via two ionic bonds, and regulates several key inflammatory pathways through EIF2AK2, indicating the dominant role of EIF2AK2. Also, BBR could subtly inhibit the dimerization of EIF2AK2, rather than its enzyme activity, to selectively modulate its downstream pathways including JNK, NF-κB, AKT and NLRP3, with an advantage of good safety profile. In EIF2AK2 gene knockdown mice, the inhibitory IL-1β, IL-6, IL-18 and TNF-α secretion of BBR was obviously attenuated, confirming an EIF2AK2-dependent anti-inflammatory efficacy. The results highlight the BBR's network mechanism on anti-inflammatory effects in which EIF2AK2 is a key target, and inhibition of EIF2AK2 dimerization has a potential to be a therapeutic strategy against inflammation-related disorders.

2.
Chinese Journal of Digestive Endoscopy ; (12): 917-922, 2019.
Article in Chinese | WPRIM | ID: wpr-800295

ABSTRACT

Objective@#To evaluate the safety and efficacy of foam sclerotherapy for bleeding internal hemorrhoids.@*Methods@#Consecutive adult patients (aged 18-60 years) with bleeding hemorrhoids were prospectively enrolled between March 2017 and March 2018. All patients were randomly assigned to the foam sclerotherapy (FS) group and the liquid sclerotherapy (LS) group. The foam and liquid sclerotherapy of hemorrhoids nucleus was performed by cap-assisted colonic endoscopy.@*Results@#A total of 108 patients were enrolled, including 62 males (57.4%) with mean age of 44.0±7.6 years. There was no significant difference in gender, age, or body mass index between the FS (n = 55) group and the LS (n =53) group. The total amount of lauromacrogol injection in the FS group was 3.7±0.9 mL, which was significantly lower than that in the LS group (8.0±2.2 mL, P<0.001). In the LS group, 8 patients (15.1%) developed bleeding after needle removal, which was significantly higher than that in the FS group [5.5%(3/53), P=0.022]. Significant pain was found in 2 patients (3.8%) in the LS group and 0 in the FS group (P= 0.025). The short-term cure rate and effective rate of the FS group were 87.3% (48/55) and 9.1% (5/55), while those were 69.8% (37/53) and 22.6% (12/53) in the LS group, respectively (P=0.046).@*Conclusion@#Foam sclerotherapy is safe and effective in the treatment of bleeding internal hemorrhoids.

3.
Chinese Journal of Digestive Endoscopy ; (12): 917-922, 2019.
Article in Chinese | WPRIM | ID: wpr-824835

ABSTRACT

Objective To evaluate the safety and efficacy of foam sclerotherapy for bleeding internal hemorrhoids. Methods Consecutive adult patients (aged 18-60 years) with bleeding hemorrhoids were prospectively enrolled between March 2017 and March 2018. All patients were randomly assigned to the foam sclerotherapy (FS) group and the liquid sclerotherapy (LS) group. The foam and liquid sclerotherapy of hemorrhoids nucleus was performed by cap-assisted colonic endoscopy. Results A total of 108 patients were enrolled, including 62 males ( 57. 4%) with mean age of 44. 0 ± 7. 6 years. There was no significant difference in gender, age, or body mass index between the FS ( n = 55) group and the LS ( n =53) group. The total amount of lauromacrogol injection in the FS group was 3. 7±0. 9 mL, which was significantly lower than that in the LS group (8. 0±2. 2 mL, P<0. 001). In the LS group, 8 patients (15. 1%) developed bleeding after needle removal, which was significantly higher than that in the FS group [5. 5%(3/53), P=0. 022]. Significant pain was found in 2 patients (3. 8%) in the LS group and 0 in the FS group (P= 0. 025). The short-term cure rate and effective rate of the FS group were 87. 3%( 48/55) and 9. 1%( 5/55) , while those were 69.8% (37/53) and 22.6% (12/53) in the LS group, respectively (P=0.046). Conclusion Foam sclerotherapy is safe and effective in the treatment of bleeding internal hemorrhoids.

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