ABSTRACT
Objective: To observe the effects of Dangshen Yuanzhi Powder microemulsion on protein expression of AchE and ChAT, and the contents of Ach and AchE in brain tissue of Alzheimer’s disease model mice and analyze its mechanism based on cholinergic theory. Methods: Mice were divided into control group, model group, BME group, Piracetam group, water extractant group and microemulsion extractant group, with 15 mice in each group. Alzheimer’s disease mice model was established by intraperitoneal injection with D-gal and NaNO2. Meanwhile, each group was given by gavage for six weeks with distilled water, BME, Piracetam tablets, water extractant and microemulsion extractant. Water maze was used to conduct behavior study. Contents of Ach and AchE in brain tissue were also measured. HE staining was used to observe pathological changes and IHC staining was used to detect expression of AchE and ChAT in hippocampal CA1 region and cerebral cortex of mice. Results: Compared with the model group, learning and memory abilities of mice were significantly improved (P < 0.05), content of Ach was significantly improved (P < 0.01), content of AchE was significantly decreased (P < 0.01), pathological changes of hippocampal CA1 region and cerebral cortex were improved, AChE expression was significantly downregulated (P < 0.01), and ChAT expression was markedly upregulated (P < 0.01) in microemulsion extractant group. Conclusion: Dangshen Yuanzhi Powder microemulsion can control the progression of Alzheimer’s disease by upregulating ChAT expression and inhibiting AChE expression in hippocampal CA1 region and cerebral cortex of mice.
ABSTRACT
The purpose of this study was to design and prepare a biocompatible microemulsion of Andrographis paniculata (BMAP) containing both fat-soluble and water-soluble constituents. We determined the contents of active constituents of BMAP and evaluated its bioavailability. The biocompatible microemulsion (BM), containing lecithin and bile salts, was optimized in the present study, showing a good physical stability. The mean droplet size was 19.12 nm, and the average polydispersity index (PDI) was 0.153. The contents of andrographolide and dehydroandrographolide in BMAP, as determined by high performance liquid chromatography (HPLC), were higher than that in ethanol extraction. The pharmacokinetic results of BMAP showed that the AUC0-7 and AUC0→∞ values of BMAP were 2.267 and 27.156 μg·mL(-1)·h(-1), respectively, and were about 1.41-fold and 6.30-fold greater than that of ethanol extraction, respectively. These results demonstrated that the bioavailability of and rographolide extracted by BMAP was significantly higher than that extracted by ethanol. In conclusion, the BMAP preparation displayed ann improved dose form for future clinical applications.