1.Inhibitory activities of 3-O-β-chacotriosyl pentacyclic triterpenoids against the entry of H5 N1 influenza viruses in vitro
Gaopeng SONG ; Xintian SHEN ; Sumei LI ; Yibin LI ; Jihong FAN ; Qianqian LIANG ; Shuwen LIU
Chinese Pharmacological Bulletin 2015;(5):647-654
Aim To study the inhibitory activities of potential new anti-influenza virus agents,3-O-β-chaco-triosyl pentacyclic triterpenoids against the entry of H5N1influenza viruses.Methods Three target com-pounds were designed and synthesized structurally re-lated to the lead compound 3-O-β-chacotriosyl dioscin derivative (1 )with inhibitory activities against H5N1 influenza viruses.The inhibitory activities of these tar-get compounds were tested at a cellular level pseudo vi-rus system targeting H5N1 influenza viruse entry.Re-sults All the compounds 1 a,1 b and 1 c showed po-tent inhibitory activities against the entry of A/Thai-land/Kan353/2004 pseudo virus into the target cells, of which compound 1 b showed the best inhibitory activ-ity with an IC50 value of (1.25 ±0.22)μmol·L-1. Conclusion The SARs analysis of these compounds indicated that replacement of the aglycone moiety of compound 1 with pentacyclic triterpenoids could in-crease antiviral activity.Different types of pentacyclic triterpen as aglycone residue had the significant influ-ence on the inhibitory activity (1 b >1 c >1 a),sug-gesting ursane type of triterpenes was superior to the two other kinds of triterpenes as aglycone residue.
2.3-O-β-chacotriosyl benzyl ursolate inhibits entry of H5N1 influenza virus into target cells.
Gaopeng SONG ; Xintian SHEN ; Yibin LI ; Yushan ZHENG ; Ping XIONG ; Shuwen LIU
Journal of Southern Medical University 2015;35(6):789-794
OBJECTIVETo study the inhibitory activities of 3-O-β-chacotriosyl benzyl ursolate and its derivatives as potential new anti-influenza virus agents against the entry of H5N1 influenza viruses into the target cells.
METHODSFour target compounds were designed and synthesized, which were structurally related to the lead compound 3-O-β-chacotriosyl methyl ursolate (1). The inhibitory activities of these compounds were tested at a cellular level psuedovirus system targeting H5N1 influenza viruse entry.
RESULTS AND CONCLUSIONThe compounds 1b, 1c and 1d showed potent inhibitory activities against the entry of A/Thailand/Kan353/2004 pseudovirus into the target cells, and among them compound 1d showed the strongest inhibitory activity with an IC50 value of 0.96 ± 0.10 µmol/L. The structure-activity relationship analysis of these compounds indicated that when 17-COOH of ursolic acid was esterified, introduction of Me groups rather than aryl groups more strongly enhanced the inhibitory activity. Changing 17-COOH of ursolic acid into amide could increase the antiviral activity and decrease the cytotoxicity of the compounds in MDCK cells.
Animals ; Antiviral Agents ; chemistry ; Dogs ; Influenza A Virus, H5N1 Subtype ; drug effects ; physiology ; Madin Darby Canine Kidney Cells ; Structure-Activity Relationship ; Triterpenes ; chemistry ; Virus Internalization ; drug effects
3.Atrial fibrillation detection using millimeter-wave radar
Hengji ZHOU ; Yihan YANG ; Yuanhui HU ; Yuguang CHU ; Xintian SHOU ; Yaping YOU ; Wenjing XUE ; Shaowei FAN ; Yong WANG ; Huiliang SHEN
Chinese Journal of Medical Physics 2024;41(1):81-87
A novel technology is proposed for non-contact and real-time detection of atrial fibrillation using millimeter-wave radar.A 60 GHz PCR millimeter wave radar is used to continuously detect the chest echo signal of the subject.After signal acquisition,I-Q signal is generated through I-Q demodulation,and the signal phase information is extracted using effective points phase trend evaluation for obtaining the signals from oscillations in the chest wall,from which the respiratory signals and cardiac signals are extracted through digital filtering for the analysis of cardiac movement.Whether the atrial fibrillation occurs or not is determined by the characteristics of atrial fibrillation wave in the time domain.The effective points phase trend evaluation for extracting more accurate signal phase information and the time-domain method for real-time atrial fibrillation detection are the innovations of the study.The experimental results show that the proposed method achieves a detection accuracy of 99.2%in clinic.
4.Postoperative hemorrhage after laparoscopic pancreaticoduodenectomy
Guoguang LI ; Wei CHENG ; Meifu CHEN ; Xinmin YIN ; Xianbo SHEN ; Xianhai MAO ; Jun WANG ; Xintian WANG ; Chuang PENG ; Bo JIANG ; Botao CHEN
Chinese Journal of Hepatobiliary Surgery 2021;27(6):425-428
Objective:To study and analyse the results of postoperative hemorrhage after laparoscopic pancreaticoduodenectomy (LPD).Methods:The clinical data of patients who underwent LPD from May 2011 to December 2019 at Hunan Provincial People's Hospital were retrospectively analyzed. The clinical characteristics of patients, onset time of postoperative hemorrhage, location of postoperative hemorrhage, postoperative biliary fistula, pancreatic fistula, infection and other short-term complications, reoperation and mortality rates were analyzed.Results:Of 356 patients who underwent LPD in this study, there were 200 males and 156 females, aged (58.0±10.5) years. The postoperative complication rate was 33.1% (118/356), the reoperation rate was 6.5% (23/356), and the mortality rate was 2.5% (9/356). The most common complications were postoperative hemorrhage [15.2% (54/356)], pancreatic fistula [14.6%(52/356)] and abdominal infection [13.8%(49/356)]. The onset time of postoperative hemorrhage was usually in the 1st - 14th day, and the highest rate of postoperative hemorrhage was 3.9% (14/356) on the first day after surgery. The postoperative hemorrhage rate then showed a downward trend, but increased again on the 7th day. The extraluminal hemorrhage locations were relatively widely distributed, and the incidence of gastrointestinal anastomotic hemorrhage in patients with intraluminal hemorrhage was the highest [67.9%(19/28)]. Of the 9 patients who died, 7 were related to postoperative bleeding.Conclusions:LPD resulted in a high incidence of complications. Postoperative hemorrhage was a complication that had the greatest impact on short-term recovery of patients. It was also an important cause of reoperation and death. In addition to postoperative bleeding caused by pancreatic fistula, gastrointestinal anastomotic bleeding was also clinically important.
5.New guaiane-type sesquiterpenoid dimers from
Lihua SU ; Xintian ZHANG ; Yunbao MA ; Changan GENG ; Xiaoyan HUANG ; Jing HU ; Tianze LI ; Shuang TANG ; Cheng SHEN ; Zhen GAO ; Xuemei ZHANG ; Ji-Jun CHEN
Acta Pharmaceutica Sinica B 2021;11(6):1648-1666
Leading by cytotoxicity against HepG2 cells, bioactivity-guided fractionation of the EtOAc fraction from