1.Study on Quality Standard for Shengxinfa Capsule
Weifeng FAN ; Shiyong WANG ; Danxuan HE ; Zhiwen YE ; Qin LI
Chinese Journal of Information on Traditional Chinese Medicine 2013;(7):59-60,61
Objective To establish the quality standard for Shengxinfa Capsule. Methods TLC was used to identify Praeparata, Psoraleae Fructus and Gastrodiae Rhizoma in Shengxinfa Capsule, and 2,3,5,4’-the four-stilbene-2-O-β-D-glucoside was identified by HPLC. The column of Agilent TC-C18 (4.6 mm×250 mm, 5 μm) was used. The mobile phase was acetonitrile-water (15∶85). The flow was 1.0 mL/min and column temperature was 30 ℃. UV detecting wavelength was 320 nm. Results Praeparata, Psoraleae Fructus and Gastrodiae Rhizoma could be identified by TLC. The linear range of 2,3,5,4’-the four-stilbene-2-O-β-D-glucoside was in the range of 0.05-0.50 μg. The average recovery was 97.8% (RSD=0.39%). Conclusion The method is feasible and accurate. The quality of Shengxinfa Capsule can be controlled effectively with the established quality standard.
2.Synthesis of novel acacetin derivatives and evaluation of their activities
Yanjie LI ; Jing LI ; Shiyong FAN ; Menghua LI ; Yuanyuan ZHOU ; Bohua ZHONG ; Weiguo SHI
Journal of International Pharmaceutical Research 2017;44(6):580-584
Objective To improve the in vivo analgesic activity of acacetin and find leads for the development of new drugs, novel acacetin derivatives containing alkyl amide groups with different length of carbon chain were designed and synthesized according to the molecular structure of the active hit compound found in our previous work. Methods Using apigenin as the initial chemical ma-terial,the acacetin was synthesized through 3 steps,then the target compounds were prepared by conjugating hydroxy group of acace-tin at position 7 with bromoalkyl amides. The analgesic activity of the target compounds was evaluated by acetic acid writhing model of mice. Results and Conclusion Novel acacetin alkyl amide derivatives showed more potent analgesic activities than that of clinical medicine diclofenac,which could be used as leads for further development of new drugs.
3.Emergency disposal experience and enlightenment of chemical defense in″Tianjin Port 8·12 Explosion Accident″
Zhiyong NIE ; Rigao DING ; Hanbin WANG ; Zheng YONG ; Shiyong FAN ; Zhikui YANG ; Yongan WANG
Chinese Journal of Pharmacology and Toxicology 2015;(5):842-846
″Tianjin Port 8 · 12 Catastrophic Explosion Accident″ affected the national people′s heart. After the disaster,the chemical defense,medical,explosion and so on various relevant profes?sional experts and rescue teams responded to the national call. Taking the bull by the horns,pooling the wisdom and efforts,the experts and rescue teams carried out and implemented the decision spirit of ″it should not hurt one man,and should not appear serious secondary disasters in the late treat?ment″which put forward by the Party Central Committee and State Council. In order to better learn and sum up experience,the cause of the disaster,the disaster rescue and disposal process,the enlighten?ment brought by the disaster and the recommendations deal with unexpected chemical incidents in the future was discussed in this paper.
4.Effect of Danhuansan on high glucose-induced vascular endothelial cells injury by activating PINK 1/Parkin signaling pathway
Yi FAN ; Chunling ZHANG ; Wei ZHAO ; Lu CHEN ; Tietao DI ; Shiyong ZHOU ; Lianggang WEI ; Yan ZHANG ; Yuanyuan DONG
Acta Universitatis Medicinalis Anhui 2023;58(12):2101-2106
Objective To investigate the effect of Danhuangsan on high glucose-induced vascular endothelial cell injury based on PINK 1/Parkin signaling pathway,and to explore its specific mechanism.Methods Human um-bilical vein endothelial cells were cultured in vitro and randomly divided into control group,growth factor group,Danhuangsan group,high glucose group,high glucose+growth factor group,high glucose+Danhuangsan group,with 3 cases in each group,treated for 48 hours.Cell scratch test was used to detect cell migration rate,and Transwell test was used to detect cell invasion rate.Immunofluorescence was used to detect the expression of anti-apoptotic protein Bcl-2,Beclin-1 and pro-apoptotic protein Bax.Western blot was used to detect the protein expression levels of PINK 1,Parkin and LC 3-Ⅱ.Results Cell scratch test and Transwell test showed that under normal environment and high glucose treatment,Danhuangsan could reduce the cell migration and invasion rate(P<0.05).Immunofluorescence assay showed that under normal environment and high glucose treatment,Danhuang-san up-regulated the expression levels of Bcl-2 and Beclin-1 protein in cells(P<0.05).Western blot results showed that under normal environment and high glucose treatment,Danhuangsan increased the protein expression levels of PINK 1,Parkin and LC 3-Ⅱ in cells and down-regulated the expression levels of Bax protein(P<0.05),and the effects of Danhuang powder were significantly better than those of blank serum and growth factor(P<0.05).Conclusion Danhuangsan can alleviate high glucose-induced endothelial cell injury by activating PINK 1/Parkin pathway,and the mechanism may be related to promoting mitophagy and enhancing the repair of damage.
5.Antibody-drug conjugates: Recent advances in linker chemistry.
Zheng SU ; Dian XIAO ; Fei XIE ; Lianqi LIU ; Yanming WANG ; Shiyong FAN ; Xinbo ZHOU ; Song LI
Acta Pharmaceutica Sinica B 2021;11(12):3889-3907
Antibody-drug conjugates (ADCs) are gradually revolutionizing clinical cancer therapy. The antibody-drug conjugate linker molecule determines both the efficacy and the adverse effects, and so has a major influence on the fate of ADCs. An ideal linker should be stable in the circulatory system and release the cytotoxic payload specifically in the tumor. However, existing linkers often release payloads nonspecifically and inevitably lead to off-target toxicity. This defect is becoming an increasingly important factor that restricts the development of ADCs. The pursuit of ADCs with optimal therapeutic windows has resulted in remarkable progress in the discovery and development of novel linkers. The present review summarizes the advance of the chemical trigger, linker‒antibody attachment and linker‒payload attachment over the last 5 years, and describes the ADMET properties of ADCs. This work also helps clarify future developmental directions for the linkers.