Screening The Effective Constituent Of Perilla Nankinensis Prescription On Anti-mice Motion Sickness

Traditional Chinese medicine commonly use perilla nankinensis, Zingiber,pericarpium citri reticulatae and mint as the main ingredients of motion sickness pills. Inorder to develop an anti-motion sickness medicine with low side effects, we use thesefour medicine food homology to make perilla nankinensis prescription and studied theeffect on anti-motion sickness.First, we established mice motion sickness model, using pica as an evaluation indexof motion sickness to optimize the modeling parameters such as rotation time and rotationmode. We found rotating40min with cis-trans alternating and variable speed is the bestmodeling method under current experimental environment.Then we used steam distillation method to gain volatile oil of Perilla frutescensprescription. Divided the prescription into volatile oil, aqueous extract, n-butanol extractand alcohol extract. We found the best extraction conditions for volatile oil is: distillingfive hours, solid-liquid ratio is1:10, soaking2hours.Under this conditions, the volatileoil extraction rate can reach a maximum value of0.25%. By mice motion sickness model,we found the volatile oil and n-butanol extract can effectively improve the symptoms ofmotion sickness of mice. Then the chemical constituents of the volatile oil and n-butanolextract of were analyzed. By GC-MS we found the volatile oil mainly contain limonene,caryophyllene, eucalyptol, limonene, pinene and other substances. Through pressurecolumn chromatography, silica gel column chromatography and HPLC-MS methods, weisolated and identified three compounds of n-butanol extract, one of them isPachyaximine A.We conjectured that anti-motion sickness mechanism of n-butanolextract may have a certain relationship with cholinolytic function of Pachyaximine A.In order to conduct the pharmacodynamic validation of effective parts, we usedanimal experiments to study the relationship among the n-butanol extract and volatile oiland the indicator AVP hormones and hormone CORT of motion sickness. We found then-butanol extract and volatile oil can reduce AVP levels, improve CORT levels, thusalleviate the symptoms of motion sickness of mice and help to adapt motion sickness.Using macroporous resin,we divided the parts of n-butanol into water part,25%ethanolpart,65%ethanol part and95%ethanol part and evaluated the effects of four componentson anti-motion sickness.The results of animal tests suggests that the four parts do not havea significant anti-motion sickness activity, indicating that the anti-motion sicknessactivity of butanol is attributed to four multi-component substances. Through feed theMice n-butanol extract with long time to verify whether n-butanol extract have long-termefficacy. We found n-butanol extract can only play a short-term effect on motion sickness,not long-term effect. Finally, n-butanol extract was made to sustained-release membrane. Its transdermalabsorption effect in vitro was studied and its optimized matrix is sodium carboxymethylcellulose: sodium polyacrylate: polyvinyl alcohol: gelatin: glycerin: kaolin: water=0.5:1:3:2:18:4:50. Its percutaneous absorption in vitro was in accordance with Higuchiequation: Qn=94.46t1/2+170.42, indicating it has a good sustained-release effect.