| Resveratrol,proven to be beneficial to human health,has been reported to exhibit a wide range of biological and pharmacological activities,including anticancer,prevention human from cardiovascular disease,antimutation,antimicrobial,anti-inflarnmation,antioxidant, induction of apoptwis in cells and estrogen-modulation.As an important phytoalexin,Resveratrol can increase the resistance of plant to pathogens.So biological and medical researchers pay great attention to the study on Resveratrol.At present,Resveratrol is widely used for the treatment of hyperlipemia,but Resveratrol injection used clinically has some disadvantages including short half-life,low drug concentration in tissues.Polyonum cuspidatum Sieb.etZucc is an important wild plant resource and also a traditional Chinese medicinal material.It contained some medicinal worthily ingredients.The main compounds isolated from the dry roots involved Anthraquinone,stilbene,flavonoids,Phenols etc.The natural aquinones which were effecitive composition of Chinese traditional medicine exhibited anti-inflammatory,antiturrior and antimicrobial activities.Liposomes are well recognized as drug delivery vehicles that have target effents,delayed drug release and degraded drug toxicity.Thus, in this study we intend to prepare the Resveratrol liposome to improve its pharmacokinetics characters such as half-life and target effect and enhance therapeutic efficacy.The subject optimized the dissolvent,method and so on by cross experiment.Using the technique of macroporous resin and chromatography extracted Giant Knotweed Rhizome's effectivepart,Resveratrol.Then making sure what we hayed got is Resveratrol by light spectrum.Using modern liposome technique made liposome which has the efficacy of promoting blood flow,removing blood stasis,dredging the meridian passage and alleviating pain.Its main use is to cure heart and Cerebral vessels disease and supply special chinese new medicine.Methods and results:1 Using cellulase,a new technology of extracting resveratrol from Polygonum cusp/datum Sieb.et Zucc.was developed.The crude powder of P.cusp/datum was treated by means of cellulase before extraction by relfuxing with ethanol.The enzyme-based extraction technology was characterized by its high extraction yield and gentle extraction conditions,which were determined experimently as follows:enzymolysis temperature 50℃,pH value of extraction media 7.0,enzymolysis time 90 min and cellulose 30U mL-1.Compared with traditional extracting technoloyg by ethenol,yield of resveratrol was increased by 33.3%by using this enzyme-based extraction technoloyg;2 To study 5 different kinds of macroreticular resin's static adsorption action,the result shows that NKA-Ⅱresin is the best;3 We adopted NKA-Ⅱresin to purify Resveratrol,the result shows that when the concentration of sophora extract is 0.10g·mL-1,the flow rate is 0.50 mL·mi-1and the ethanol concentration is 60%.The static adsorbtion capacity and elutive ratio were good;4 Adopting the technique of silica gel column chromatography to purify Resveratrol and ethanol and acetylacetic ether are the condition of elution.Yhe structure was check by light.spectrum;5 The content of Resveratrol was determined by HPLC and study on the methodology.According to pharmacopoeia(2005),the methods of envelopment ratio was established;6 Studing the membrane material purchased in the market by oxidizing index method,the result shows that the soybean phosphatide fulfills the requirement.The liposomes were prepared by the following methods:TFV, REV(reverse-phase evaporation vesicle method),technique of ethanol infusion and aether infusion.The result indicats the encapsulation of liposomes prepared by TFV is the highest;7 Resveratrol lipsomes were prepared by thin layer ultrasonic technique. The formulation was optimized by orthogonal design test.Entrapment efficiency(EE)was determined by HPLC;8 The quality of Resveratrol lipsomes were evaluated.The lipsomes shape was spherical or ellipsoidal,and their size was 146-585nm by TEM. The surface charge of lipsomes was negative by electrophoresis and pH=6.87±0.13.The encapsulation ratio of Resveratrol in lipsomes was 73.68%. The lipsomes was stored in 3-5℃;9 To compare with water solution,biological half-life of liposomes, the concentrations of Resveratrol in liver,lung,spleen of mice were improved obviously.Conclusion1 We choosed four factors such as the temperatureof enzymolysis,enzyme concentration,pH value of extraction media and time of enzymolysis and three level to carry out the orthogonal design,and the reasonable technical method was set;2 NKA-Ⅱresin has a good effect on the adsorption and desorption of piceid from Resveratrol cuspidatum;3 The method of HPLC was sensitive,convenience and reliable;4 The result of tissues distribution showed that Resveratrol liposomes had better tissues targeting and slow-release effect than Resveratrol. |
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