Bioactive Constituents And Quality Evaluation Of Physalis Alkekengi Var. Franchetii

Jindenglong,Calyx seu fructus physalis,a commonly used Chinese herb,is the dried calyxes of Physalis alkekengi L.var.franchetii(Mast.) Makino(Family Solanaceae).Its action is considered as clearing away heat and toxic material, relieving sore throat,dissipating phlegm,diureses and so on.It is distributed in most areas of China and is used widely as a treatment for different illnesses.Based on the review on the chemical constituents and pharmacological research of Physalis,the chemical constituents of Physalis alkekengi var.francheti and their antitumor activities were researched.On the basis of systematic research on its chemical constituents,the thesis focused on the quality-related topics of Jindenglong, such as(1)quantitative determination of 2 major physalins simultaneously in Jindenglong using HPLC method,(2) the stability study on physalin D.The results were summarized as below.1 Chemical Constituents of Physalis alkekengi var.franchetiBy means of many different chromatographic methods such as silica gel, sephadex LH-20 and ODS column chromatography,37 compounds have been separated from the calyxes of Physalis alkekengi var.francheti and 31 of them were identified by chemical and spectral methods,including 9 physalins,10 flavonoids,5 phenols,3 coumarins and 4 other miscellaneous compounds.Among them,there is one new compound identified as 5α-hydroxy-25,27-dihydro-4,7-didehydro-7-deoxyneophysalin A.11 compounds were isolated from the Physaliphorous for the first time,and 1 compound was found from this plant for the first time.The antitumor activities of the new neophysalin and eight known physalins isolated from the calyxes of Physalis alkekengi var.francheti were tested.It was found that all physalins inhibited cell growth against Bel 7402 cell,in which compound PA-9 was the most potent and PA-11 was the most inpotent.However, compound PA-9 can also inhibite the normal human liver cells LO-2 seriously.The cytotoxic activities of the new compound were evaluated according to MTT assay against the PC-3(human prostate cancer) and LNCaP(human prostate cancer) cell lines.The cytotoxicity data(IC₅₀ values) are 5.266 and 0.7285μg ml^-1, respectively.2 Quality assessments on Physalis alkekengi var.franchetiA novel method has been developed for quantitative determination of 2 major physalins simultaneously by HPLC method in 20 samples of P.alkekengi var. francheti as well as 4 samples of P.angulata,1 sample of P.minima,different parts of P.alkekengi var.francheti,P.angulata and P.minima.3 Stability and kinetics study of physalin DThe chemical dynamics of physalin D was investigated by using HPLC with DAD detection.The influence factors of pH value,temperature and light on the stability of physalin D in solution were carried out respectively.The results indicated that physalin D was degraded when pH value exceeded 10.The optimal stability condition was at normal temperature,pH＜10 and away from light.