ABSTRACT
Bavachinin is a dihydroflavone isolated from dried ripe fruits of Psoralea corylifolia L.，which has various pharmacological activities, such as anti-tumor, anti-virus, anti-diabetes, anti-inflammatory and neuroprotective, and good potential in clinical applications. With the increasing concern about the safety of P. corylifolia applications in clinical, the bavachinin has been found to be one of the main components causing liver injury. In this paper, the pharmacological activities and hepatotoxicity of bavachinin in the recent 20 years were reviewed, in order to provide reference for the further study and clinical application.
ABSTRACT
@#Polydopamine (PDA) nanoparticles were prepared as a carrier, and bavachinin (BVA) was efficiently loaded by physical adsorption.The erythrocyte membrane was further utilized to modify and construct the erythrocyte membrane biomimetic nanoparticles (RBC-BP), the residence time in the body was extended and the in vivo analytical method was established to investigate their pharmacokinetics in mice.Polydopamine nanoparticles loaded with BVA (BP) were prepared by solvent replacement method, and the influencing factors of PDA loaded with BVA were investigated with the adsorption rate as the evaluation index.The erythrocyte membrane was extracted and separated, and RBC-BP was prepared by incubation coextrusion method. The effects of pH value on membrane coating and the extrusion times on the particle size and uniformity of RBC-BP were investigated.The particle size, potential, morphology, and cumulative release rate of RBC-BP were systematically characterized, and their pharmacokinetics in mice were preliminarily explored.The results showed that the adsorption rate of BP was as high as (92.08 ± 0.17) % and the drug loading rate was (42.05 ± 2.95) % at the PDA to BVA ratio of 1∶0.5, the solution pH value of 7, the incubation time of 6 h, and the incubation temperature of 20 °C, and that the erythrocyte membrane could be successfully oriented and coated on the surface of BP by the action of electric charge at the pH value of 4. The in vitro studies showed that RBC-BP has the apparent core-shell structure with the particle size of (308.63 ± 6.56) nm and good stability, and in vivo pharmacokinetic studies showed that RBC-BP can significantly extend the circulation time of nanoparticles in vivo.
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Aim To probe into the bavachinin toxic mechanisms in HepaRG cells. Methods MTT assay was used to determine toxicity and dose. After treated with 6.25,12.5 and 25 μmol·L-1bavachinin for 24 h,the cell death was investigated by Hoechst 33342/PI,LDH,caspase-3 activity,and Bax,Bcl-2 expression levels. Mitochondrial damage was detected by mito-chondrial membrane potential,ATP content,openness of mitochondrial permeability transition pore and cyto-chrome C level. Results Bavachinin administration up-regulated Bax/Bcl-2 ratio and caspase-3 activity with increase of drug concentration after 24 h. Apop-totic rate increased in a dose-dependent manner be-tween 6.25 and 25 μmol·L-1,but when reached to 25 μmol·L-1,cells showed more necrosis. Mitochon-drial injury indicators significantly increased after 24h. Conclusion Bavachinin induces HepaRG cell apopto-sis and necrosis through mitochondria injury.
ABSTRACT
Objective: To establish UPLC method for the simultaneous determination of 10 components, such as psoralen, isopsoralen, psoralidin, bavachinin, isobavaenin, corylifolin, isobavachalcone, corylin, neobavaisoflavone, and bakuchiol in Psoralea Fructus, and to study the effect of processing time on 10 components in stir-frying Psoralea Fructus with salt solution. Methods: The chromatographic separation was achieved on a C18 column (50 mm×4.6 mm, 1.8 μm) with acetonitrile (A)-water (B) as mobile phase at the flow rate of 1.0 mL/min for gradient elution; The column temperature was 30℃. The determination wavelength was 250 nm. Results: The 10 components were well separated within 15 min. The RSD values of reproducibility were less than 3%. The stability was good in 24 h. The linear relationship between the concentration and peak areas of the 10 components was good (r≥0.9970). The average recoveries were 96%-105% and the RSD values were all less than 3%. Conclusion: The method is simple, reliable and accurate, could be used for the quality control of Psoralea Fructus. With processing time prolonged, the content of coumarins showed first decreased, then increased and last decreased. Flavonoids, bakuchiol and the total content of 10 components above were decreased.
ABSTRACT
A simple, sensitive and selective method of high-performance liquid chromatography (HPLC) has been successfully developed for separation of bavachinin enantiomers in Fructus Psoraleae and rat plasma. The separation and detection conditions of HPLC were optimized. Chiral bavachinin were separated with the mobile phase of methanol and water (70:30, v/v) at a flow rate of 1.0 mL/min. The linear ranges were in the range of 20-1000 mg/mL. The detection limits were tested as 4 ng/mL and 6 ng/mL for (t)-bavachinin and (à)-bavachinin, respectively. The method has been applied to analyze chiral bavachinin in rat plasma. HPLC-MS method was used to test the accuracy.