RESUMO
Objective: To investigate the mechanism by which total alkaloids of Sophora alopecuroides (TASA) and matrine (MT) impair biofilm to increase the susceptibility of Staphylococcus epidermidis (S. epidermidis) to ciprofloxacin. Methods: The minimum biofilm inhibitory concentration (mBIC) was determined using a 2-fold dilution method. Structure of biofilm of S. epidermidis was examined by Confocal Laser Scanning Microscope (CLSM). The cellular reactive oxygen species (ROS) was determined using a DCFH-DA assay. The key factors related to the regulation of ROS were accessed using respective kits. Results: TASA and MT were more beneficial to impair biofilm of S. epidermidis than ciprofloxacin (CIP) (P < 0.05). TASA and MT were not easily developed resistance to biofilm-producing S. epidermidis. The mBIC of CIP decreased by 2–6-fold following the treatment of sub-biofilm inhibitory concentration (sub-BIC) TASA and MT, whereas the mBIC of CIP increased by 2-fold following a treatment of sub-BIC CIP from the first to sixth generations. TASA and MT can improve the production of ROS in biofilm-producing S. epidermidis. The ROS content was decreased 23%−33% following the treatment of sub-mBIC CIP, whereas ROS content increased 7%−24% following treatment with TASA + CIP and MT + CIP combination from the first to sixth generations. Nitric oxide (NO) as a ROS, which was consistent with the previously confirmed relationship between ROS and drug resistance. Related regulatory factors-superoxide dismutase (SOD) and glutathione peroxidase (GSH) could synergistically maintain the redox balance in vivo. Conclusion: TASA and MT enhanced reactive oxygen species to restore the susceptibility of S. epidermidis to ciprofloxacin.
RESUMO
Objective To evaluate the effect of total alkaloids of Sophora alopecuroides L on the nervous behavior and the expression of neurotransmitters in rats. Methods 48 male SD rats were randomly divided into 4 groups:blank group,total alkaloids of Sophora alopecuroides L treatment with 4 mg·kg-1 ·d-1 ( low dose group) ,8 mg·kg-1 ·d-1( medium dose group) and 16 mg·kg-1 ·d-1( high dose group) groups. After successive intragastric administration for 30 days,the locomotor activity was applied to test the nervous behavior and emotional state of rats in each group. After behavioral tests were finished,the contents of trypto-phan (Trp),5-hydroxytryptophan (5-HTP),5-serotonin (5-HT),5-hydroxyindoleacetic acid (5-HIAA), norepinephrine (NE),epinephrine (E) and dopamine (DA) were detected by ELISA in serum and brain. Results In the experiment of locomotor activity,compared with blank group ((95.33±12.75) times),the numbers of horizontal movement of Sophora alopecuroides L in medium and high dose group ( ( 61. 64 ± 5.91),(64.62±5.79)times both P0.05). Correlation analysis indicated that the degree of au-tonomic activity in rats with the content of 5-HT,5-HIAA and DA in serum was negatively correlated (P<0.05, P<0.01) ,the degree of emotional stress and the content of 5-HT,5-HIAA in brain was negatively cor-related (P<0.05, P<0.01) . Conclusion The total alkaloids of Sophora alopecuroides L can reduce the ac-tivity of rats and increase the degree of emotional stress. And the mechanism may be correlated with the in-creasing level of 5-HT and 5-HIAA in serum and brain.
RESUMO
Objective: To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides (TASA) was prepared. Methods: The pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. Results: The pellet core consisted of 40% TASA, 1:2 in ratio of Bletilla striata polysaccharide (BSP), an enzyme-degradable material, to microcrystalline cellulose (MCC), filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit S100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h. And the similarity factor f of sophoridine and matrine of release curve for investigated formulation was internal in (50-100) and > 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. Conclusion: The coated pellets achieve a certain colon-specific release and synchronous release.