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Acta Pharmaceutica Sinica B ; (6): 629-638, 2018.
Article in English | WPRIM | ID: wpr-690877


Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus (EBOV) activities. Structure-activity relationship analysis indicated: (i) 12-dichlorobenzyl motif was beneficial for the activity; (ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound exhibited the most potent potency against EBOV with an IC value of 5.29 μmol/L and an SI value of over 37.8. Further anti-EBOV assay of identified its high effectiveness, and anti-MARV assay of suggested its inspiring broad-spectrum anti-filovirus activity. The results provided powerful information on further strategic optimization and development of this kind of compounds against filoviruses.

Article in Chinese | WPRIM | ID: wpr-357859


Heart rate variability (HRV) is the difference between the successive changes in the heartbeat cycle, and it is produced in the autonomic nervous system modulation of the sinus node of the heart. The HRV is a valuable indicator in predicting the sudden cardiac death and arrhythmic events. Traditional analysis of HRV is based on a multielectrocardiogram (ECG), but the ECG signal acquisition is complex, so we have designed an HRV analysis system based on photoplethysmography (PPG). PPG signal is collected by a microcontroller from human's finger, and it is sent to the terminal via USB-Serial module. The terminal software not only collects the data and plot waveforms, but also stores the data for future HRV analysis. The system is small in size, low in power consumption, and easy for operation. It is suitable for daily care no matter whether it is used at home or in a hospital.

Autonomic Nervous System , Cardiovascular Diseases , Diagnosis , Death, Sudden, Cardiac , Electrocardiography , Heart Rate , Humans , Monitoring, Ambulatory , Photoplethysmography , Sinoatrial Node , Software
Acta Pharmaceutica Sinica ; (12): 200-5, 2012.
Article in Chinese | WPRIM | ID: wpr-414955


A series of novel N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities. Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC50 values of 2.52 and 1.99 microg x mL(-1), respectively. Cell cycle was blocked at S phase of HepG2 cells treated with 9a by flow cytometry detection. Our results provided a basis for the development of a new series of anti-cancer candidates.