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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-380714


Objective To detect the expression of TGF-β1 mRNA and ERβwt mRNA in peripheral blood monoanclear cells (PBMCs) in patients with chronic fatigue syndrome (CFS), and their relationship with pathogenesis of CFS. Methods Fluorescence quantitative RT-PCR (FQ-RT-PCR) was used to examine TGF-β1 mRNA and ERβwt mRNA expression of peripheral blood monocytes in 63 cases with CFS,50 cases with other diseases, and 50 healthy controls. The gene expression levels were calculated with the formula △Ct=Ct(target gene) - Ct(internal control). Results The mean TGF-β1 mRNA expression of CFS patients (△Ct = 3.27 ± 0. 58) was higher than that of disease controls (△Ct = 4. 54 ± 1.05, t = 8. 11, P <0.01) and that of healthy controls (△Ct = 4. 37 ± 1.00, t = 7. 02, P < 0. 01). The mean ERβwt mRNA expression of CFS patients (△Ct =9. 34 ±0. 92) was lower than that of disease controls(△Ct =7.12±0. 47, t = 15.44 ,P < 0. 01) and that of healthy controls(△Ct = 7. 10 ±0. 48, t = 15.47, P < 0. 01). Conclusions The TGF-β1 mRNA and ER βwt mRNA expression levels of PBMCs are siguificantly elevated in patients with CFS. It may be implicated in the pathogenesis of CSF.

Article in Chinese | WPRIM | ID: wpr-965102


@#Objective To analyze the instruments for post stroke fatigue, Fatigue Severity Scale (FSS),Checklist Individual Strength (CIS) and Fatigue Impact Scale (FIS). Methods The FSS,CIS and FIS were applied in 214 cases with cerebral infarction. They were combined together at the (sub)scale level, and evaluated with Mokken Scale Analysis for Polytomous Items, for validity and reliability. Results and Conclusion Three scales were and The combined scale proved to be acceptable (H>0.5). 3 components were extracted in factor analysis, and the their total cumulative contribution was 77.504%, with reliability (α) of 0.8097,0.7094 and 0.8019 respectively. FSS put emphasis on the fatigue experiences of stroke patients, CIS on the influence of fatigue on, and FIS on the social function.

Article in Chinese | WPRIM | ID: wpr-964918


@# Objective To introduce Checklist Individual Strength(CIS)into China,and evaluate its reliability and validity.Methods CIS was translated into Chinese language and the reverse translation was done by several experts.Validity and reliability were implemented in 214 cases with cerebral infarction.Results 4 components were extracted in factor analysis,and the total cumulative contribution was 78.984%.By correlation analysis,the twenty items were divided into 4 domains:subjective feeling of fatigue,concentration,motivation and physical activity,it was same as in the English version.Cronbach α of four domains were 0.9256,0.9072,0.7598,and 0.9157,respectively.Conclusion Psychometric properties(reliabilities and validities)of CIS Chinese version is met with satisfaction and seems to be adaptable to Chinese cerebral infarction patients.