1.Design, synthesis and antitumor activity of valproic acid salicylanilide esters.
Ming YUAN ; Jiaming LI ; Guangwei HE ; Guochen ZHONG ; Yanchun ZHANG
Acta Pharmaceutica Sinica 2013;48(6):874-80
A series of valproic acid salicylanilide esters were designed and synthesized based on the principle of prodrug. The structures of the target compounds were confirmed by MS, 1H NMR and 13C NMR. Anti-tumor activities of these compounds against K562, A549, A431 cells in vitro were investigated by MTT assay and SRB assay. The results indicated that the compounds 6h-6j were found to have stronger cell growth inhibitory action than gefitinib, and comparable to niclosamide, which are worth to be intensively studied further.
2.Synthesis of ferulic acid derivatives and their inhibitory effect on platelet aggregation.
Jiaming LI ; Yonghai ZHAO ; Guochen ZHONG ; Zijiang LONG ; Peng ZHOU ; Ming YUAN
Acta Pharmaceutica Sinica 2011;46(3):305-10
Ferulic acid, an useful compound of Chinese traditional medicine, was used as leading compound. Six ferulic acid derivatives were designed and synthesized based on bioisosterism. Their structures were characterized by IR, 1H NMR, 13C NMR and mass spectra. In vivo experiment showed that ferulic acid derivatives had good inhibitory effects on adenosine diphosphate (ADP) induced platelet aggregation, which were significantly higher than that of Ozagrel.
3.Clinical study on Guizhi Mahuang Geban Decoction combined with conventional western medicine in the treatment of post infections cough
Guochen WANG ; Yuehua LIN ; Dong XIE ; Changbao ZHONG
International Journal of Traditional Chinese Medicine 2022;44(8):874-877
Objective:To evaluate the clinical efficacy of Guizhi Mahuang Geban Decoction combined with conventional western medicine in the treatment of post infections cough (PIC), and to explore the mechanism.Methods:A total of 100 PIC patients in our hospital from January 2020 to July 2021 who met the inclusion criteria were divided into 2 groups according to the random number table method, with 50 in each group. The control group was treated with conventional western medicine, and the study group was treated with Guizhi Mahuang Geban Decoction and the treatment of the control group. Both groups were treated for 10 days. TCM symptom scores were performed before and after treatment. The levels of neurokinin A (NKA), substance P (SP), neurokinin B (NKB) and calcitonin gene related peptide (CGRP) were detected by ELISA. Adverse events were recorded and clinical effects were evaluated.Results:The total clinical effective rate was 90.0% (45/50) in the study group and 68.0% (34/50) in the control group, and there was significant difference between the two groups ( χ2=7.29, P=0.007). The scores of cough, expectoration, pharyngeal itch and total score in the study group were significantly lower than those in the control group ( t values were 8.04, 6.30, 9.03, 9.71, all Ps<0.01). After treatment, NKA [(86.08±18.21) ng/L vs. (137.68±28.29) ng/L, t=10.85], SP [(54.23±11.28) ng/L vs. (71.75±15.34) ng/L, t=6.51], NKB [(96.15±20.19) ng/L vs. (149.84±30.22) ng/L, t=10.45], CGRP [(62.93±18.35) ng/L vs. (89.59±23.25) ng/L, t=6.37] levels in the study group were significantly lower than those in the control group ( P<0.01). The incidence of adverse events was 8.0% (4/50) in the control group and 10.0% (5/50) in the study group, and there was no significant difference between the two groups ( χ2=0.13, P=0.727). Conclusions:Compared with western medicine alone, Guizhi Mahuang Geban Decoction combined with western medicine can rapidly improve patients' symptoms, improve curative effect and have better safety for PIC. Its mechanism may be related to the regulation of NKA, SP, NKB and CGRP levels.
4.Efficacy of microsurgical treatment in 58 patients with primary jugular foramen schwannomas
Guochen YANG ; Xixi LI ; Weijie SU ; Honglin WU ; Hongxing TANG ; Zhong DENG ; Yibin YANG ; Lixuan YANG
Chinese Journal of Neuromedicine 2022;21(11):1138-1142
Objective:To investigate the clinical efficacy of microsurgical resection in primary jugular foramen schwannomas (JFSs).Methods:A retrospective analysis was performed; the clinical data of 58 patients with JFSs treated by microsurgery in Department of Neurosurgery, First Affiliated Hospital of Sun Yat-sen University from May 2012 to June 2021 were collected. Seven patients accepted microsurgery via suboccipital retrosigmoid approach, and 51 patients accepted microsurgery via jugular foramen approach. Fifty-three patients were followed up for 4.5 years (ranged from 0.5-8.5 years); follow-ups included Karnofsky performance status (KPS) scores, postoperative complications, and imaging reexaminations. Results:Fifty patients (86.2%) achieved total tumor resection and 8 (13.8%) subtotal resection. The KPS scores at discharge were 68.6±14.9, which were significantly lower than the preoperative KPS scores (77.6±13.5, t=2.452, P=0.017). During the follow-up, 5 patients(9.4%) had tumor recurrence, and 39 patients (73.6%) had improved symptoms after surgery. One patient (1.9%, modified Samii D type) died of cerebellar hemorrhage and swelling after surgery. The main complications included new/aggravated hoarseness (11/53), cerebrospinal fluid leakage (7/53), new/aggravated dysphagia (5/53), and new facial paralysis (4/53). Conclusion:In microsurgical resection of JFSs, short-term symptoms of the lower cranial nerves may be exacerbated, but long-term results are good.