Mechanism study of orientin protecting rat heart from myocardial ischemia/reperfusion injury based on mitochondrial quality control / 中草药

Objective To investigate the regulation effects of orientin on mitochondrial quality control in cardiomyocytes of rats with myocardial ischemia/reperfusion injury (MIRI). Methods A total of 75 Sprague-Dawley male rats were randomly divided into five groups: sham group, model group, and orientin preconditioning groups (1.0, 2.0, and 4.0 mg/kg). Except for sham group, all rats were exposed to modeling of MIRI with ligation of left anterior descending coronary artery (LADCA) for 30 min, and then releasing for 120 min. Mitochondrial membrane potential (MMP) and opening of mitochondrial permeability transition pore (mPTP) were detected by Microplate Reader; Activity of mitochondrial respiratory chain complexes I-IV was detected by Spectrophotometer; Cardiomyocyte apoptosis was detected by TUNEL method; Apoptosis and mitophagy related proteins were detected by Western Blot and the interaction between Parkin and p62 on mitochondria were detected by Co-IP. Results Orientin significantly restored MMP, mPTP opening threshold and activity of mitochondrial respiratory chain complexes I-IV, and reduced cardiomyocyte apoptosis. Additionally, orientin can dramatically inhibit the protein expression level apoptosis and mitophagy related proteins and weaken the interaction between Parkin and p62. Conclusion Orientin has a significant protective effect on cardiomyocyte mitochondria in MIRI rats. Its underlying mechanism is related to inhibition of hyperactivity of mitophagy in cardiomyocytes via Parkin-dependent and Parkin-independent signaling pathways.

Preparation of Kushen-Dilong nanoemulsion gel and transdermal characterization in vitro / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare Kushen-Dilong nanoemulsion and nanoemuls-ion gel, and investigate its content, physical and chemical properties. Their transdermal properties in vitro were studied as well.</p><p><b>METHOD</b>IPM acted as oil phase, EL35 as surfactant, EtOH as cosurfactant, Pheretima aqueous solution was added dropwise to the oil phase to prepare Kushen-Dilong nanoemulsion at room temperature using magnetic stirring. HPLC was used to determine the content of matrine and oxymatrine in the nanoemulsion. Transmission electron microscopy and laser particle size analyzer was used to determine the shape and size of the nanoemulsion. NP700 was used as substrate to prepare Kushen-Dilong nanoemulsion gel. Franz diffusion cell was used for the nanoemulsion and gel transdermal characteristics in vitro.</p><p><b>RESULT</b>The Kushen-Dilong nanoemulsion was O/W nanoemulsion, its uniform particle size was 20.6 nm with roundness appearance and stable content. The steady-state permeation rate of Kushen-Dilong nanoemulsion, nanoemulsion gel, saturated aqueous solution, hydro gel were 0.1484, 0.1183, 0.0306, 0.0321 mg x cm(-2) x h(-1), respectively.</p><p><b>CONCLUSION</b>The 24 h cumulative infiltration and infiltration rate of Kushen-Dilong nanoemulsion and nanoemulsion gel were better than the saturated aqueous solution and hydro gel, which could provide a new dosage form for Kushen-Dilong transdermal drug delivery.</p>

Physicochemical properties and skin penetration in vitro of total alkaloids of Sophora flavescens nanoemulsion / 中国中药杂志

The research aimed at investigating the physicochemical properties, stability and skin penetration in vitro of total alkaloids of Sophora flavescens nanoemulsion. Prepare total alkaloids of S. flavescens nanoemulsion and detect the determination of matrine and oxymatrine in the nanoemulsion using HPLC method. Transmission electron microscopy and laser particle size analyzer were utilized to detect the shape and size of the nanoemulsion respectively. And also the stability of nanoemulsion was studied under the conditions of low temperature (4 degrees C), normal temperature (25 degrees C) and high temperature (60 degrees C). Franz diffusion cell was used to research the transdermal absorption of nanoemulsion in vitro. The results found that the nanoemulsion we prepared presented appearance of rounded, uniform; its average diameter was (15.55 +/- 2.24) nm, and particle size distribution value was 0. 161; the appearance, diameter and percentage determination of total alkaloids of S. flavescens had no variations after 15 d under 4, 25, 60 degrees C respectively. The steady-state permeation rate was 4.564 1 microg x cm(-2) x h(-1), 24 h cumulative amount of penetration was 110.7 microg x cm(-2), which was 1.86 fold of 24 h cumulative amount of aqueous solution (59.41 microg x cm(-2)). All the results demonstrated total alkaloids of S. flavescens nanoemulsion had good permeability, and could provide a new preparation for its clinical application.