1.Ozone injection combined with radiofrequency ablation for the treatment of far lateral lumbar disc herniation:observation of the curative effect
Yuan WANG ; Shiwu YIN ; Tingmiao XIANG ; Zonggen GAO ; Shengquan PAN ; Huilin ZHANG ; Haideng LONG ; Ju WANG
Journal of Interventional Radiology 2015;(9):789-791
Objective To investigate the clinical efficacy of ozone injection combined with radiofrequency ablation (RFA) for the treatment of far lateral lumbar disc herniation (FLLDH). Methods A total of 60 patients with FLLDH, who were admitted to authors’ hospital during the period from March 2013 to March 2014, were randomly and equally divided into the study group (n=30) and the control group (n=30). Simple ozone injection treatment was employed for the patients of the control group, while ozone injection combined with radiofrequency ablation was adopted for the patients of the study group. The same other adjunctive medication was used in both groups. All the patients were followed up at one week as well as at one, 3 and 6 months after the treatment. The clinical effect and the complications of both g roups were recorded. Results Successful operation was obtained in all 60 patients, no perioperative complications occurred, and the technical success rate was 100%. The excellent clinical results evaluated at one week, and one, 3 and 6 months after the treatment in the control group and in the study group were 73.3%, 76.7%, 70%, 60% and 70%, 76.7%, 83.3%, 90% respectively. The 3-month and 6-month clinical results of the study group were significantly better than those of the control group. Conclusion For the treatment of FLLDH, ozone injection combined with radiofrequency ablation is safe and effective. This technique should be recommended in clinical practice.
2.Improved synthesis and pharmacological evaluation of racemic 11-demethylcalanolide A
Lin WANG ; Xingquan ZHANG ; Hongshan CHEN ; Peizhen TAO ; Yan LI ; Yu BAI ; Jinping HU ; Tao MA ; Zhentang XING ; Zonggen PENG ; Chunmei ZHOU ; Qi GAO ; Gang LIU
Acta Pharmaceutica Sinica 2008;43(7):707-718
An improved and practical synthesis of racemic 11-demethylcalanolide A [(±)-1] was developed. This improved process involved Pechmann reaction on phloroglucinol with ethyl butyrylacetate to give 5, 7,-dihydroxy-4-n-propylcoumarin(3). Poly phosphoric acid (PPA) catalyzed acylation of compound(3) with crotonic acid, then intramolecular cyclization was achieved simultaneously in one step to afford the key intermediate chromanone(4). A microwave assisted synthetic method preparing chromene(6) using chromenynation of chromanone(4) with 1, 1-diethoxy-methyl-2-butene was conducted. Luche reduction of chromene(6) using NaBH<,4> with CeCl3·7H2O preferably gave (±)-1. The overall yield of this four step synthesis of (±)-1 was around 32% increasing one fold more than that of the previous method. An in vitro investigation showed that (±)-1 exhibited inhibitory activities against both wild-type and drug-resistant HIV-1 in HIV-1 RT and cell culture assay, and significant synergistic effects in combination with AZT, T-20, and indinavir. Its LD50 of acute toxicity in mice by intragastric administration and by intraperitoneal injection were 735.65mg·kg-1 and 525.10mg·kg-1, respectively. The C<,max> and AUC<,0-∞> were 0.54μg·mL-1 and 1.08(μg·mL-1)·h, respectively. The dynamics study of the inhibition of mice sera on HIV-1 RT showed that mice treated with 100mg·kg-1 (±)-1 once intraperitoneally were similar to that of 5mg·kg-1 of known clinical effective anti-HIV-1 drug neverapine. The results suggested that further investigation of the anti-HIV candidate (±)-1 was warranted.
3.Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents.
Yinghong LI ; Zonggen PENG ; Limei GAO ; Danqing SONG
Acta Pharmaceutica Sinica B 2014;4(4):307-312
Chronic hepatitis C virus (HCV) infection has become a major public health burden worldwide. Twenty-two sophocarpinic acid or matrine derivatives were synthesized and their anti-HCV activities were evaluated in vitro. The structure-activity analysis revealed that (i) sophocarpinic acids with a D-seco 3-ring structure scaffold were more favorable than matrines with a 4-ring scaffold; (ii) the introduction of an electron-withdrawing group on the phenyl ring in 12-N-benzenesulfonyl Δ (βγ) sophocarpinic acids was beneficial for the antiviral activity against HCV. Among them, compounds 9h and 9j exhibited the most potent inhibitory activities on HCV replication with selectivity indies of 70.3 and 30.9, respectively. Therefore, both were selected as antiviral candidates for further investigation.
4.Replication priority of hepatitis C virus genotype 2a in a Chinese cohort.
Zhen YANG ; Yongxin YU ; Hongzhong ZHANG ; Guifang SHANG ; Jialiang GAO ; Jian-Dong JIANG ; Zonggen PENG
Acta Pharmaceutica Sinica B 2014;4(4):266-269
HCV genotypes have been documented in clinical practice. The aim of this study was to determine the replication priority of different HCV genotypes in a Chinese HCV positive cohort. Serum samples from 491 apparently healthy Chinese blood donors testing positive for HCV antibodies and naive to antiviral drug therapy were tested. Genotyping analysis showed that genotypes 1b and 2a were predominant and accounted for 77.6% of the HCV infections. Among the genotype groups, individuals infected with genotype 2a had an HCV RNA viral load (10(8) copies/mL) about 200-fold (lg, 2.3) greater than those infected with other genotypes (10(4)-10(5) copies/mL) indicating a replication priority of genotype 2a. However, there was no correlation between HCV genotype and antibody response suggesting that the amplification advantage of genotype 2a results from a favorable interaction with the host cellular environment. In conclusion, HCV genotypes 1b and 2a are the predominant genotypes in China and genotype 2a possesses a significant replication priority compared with the other genotypes. This suggests the existence of host cellular factors that may act as drug-targets for entirely clearing HCV infection in the future.