ABSTRACT
In order to investigate the feasibility of in vitro screening the antitumor activity of natural compounds by trypsin, porcine trypsin was used to for screening test, which is marked by inhibition of enzyme activity. Four compounds, namely daidzin, genistin, matrine and oxymatrine, were selected as test subjects. The natural antitumor drug camptothecin was used as the control. The inhibitory effect was detected by two experimental methods: direct detection of trypsin activity inhibition and hydrolysis of bovine serum albumin by trypsin. The results showed the inhibitory effects of the four natural compounds on trypsin, and the inhibition rates of the four natural compounds were significantly different. The enzyme activity assay showed that the inhibitory effect of matrine was better than that of oxymatrine, indicating that trypsin had a good screening resolution. The inhibitory effect was significantly increased with the increased ratio of sample to trypsin, suggesting the structure-activity correlation and dose-effect correlation of the screening methods. Altogether, the experimental method of screening antitumor activity of natural compounds by trypsin has good application values. Since porcine trypsin is similar to human trypsin in terms of molecular structure and performance, it is more applicable for screening of antitumor efficacy of natural pharmacodynamic compounds.
Subject(s)
Humans , Trypsin/chemistry , Alkaloids/pharmacologyABSTRACT
In order to study the potential application value of lavender volatile oil (LVO), the chemical composition of the volatile oil of lavender was analyzed by GC-MS, and the mouse model of Alzheimer's disease (AD) was established. Additionally, the antioxidant enzymes activity of T-SOD, GSH-PX, CAT and MDA content were studied. Experimental results showed that 55 kinds of chemical constituents including terpene, terpene alcohol and ester compounds from LVO were identified, and the content of linalool and linalyl acetate was the highest, accounting for 49.71% of the total volatile oil. The ability of mouse platform memory was improved significantly. The levels of GSH-PX, CAT and T-SOD of mouse brain tissue in the treatment group were significantly higher than those in the model group (P<0.05). The level of MDA reached the maximum value in the model group, while there was no notable difference between the levels of MDA in the drug group and the normal group. The result indicated the significant oxidative activity of LVO, the possibility of induced oxidative stress reduction in neurons, and the reversal effect of memory acquired disorder.
ABSTRACT
<p><b>OBJECTIVE</b>To create Atractylode macrocephala inspissation decoction pieces. The effect of ultrasonic wave on extraction of the active components in A. macrocephala was studied in a water solution.</p><p><b>METHOD</b>The factors including the ratio of material to liquid, ultrasonic power, ultrasonic time, soaking time, particle size etc, were studied. The best extraction method was found through the response surface method.</p><p><b>RESULT</b>The best extraction method was found as follows: the granularity of material 0.1 mm, the repetition times of ultrasonic process 3 times, the soaking time before the ultrasonic process 30 min, the ratio of liquid to material 10:1, the soaking time after the ultrasonic process 2.6 h, the time of the ultrasonic wave 15.5 min, the power of the ultrasonic wave 531 W, the rate of reservation of active components 88.5%, the rate of inspissation 1.6.</p><p><b>CONCLUSION</b>The ultrasonic wave can used in the extraction of the active components in A. macrocephala and a model equation that can be used to predict the experiment was get through the response surface method.</p>