| Fomitopsis officinalis is one kind of perennial large medicinal fungi which has lots of compounds, and most of them are triterpene compounds and fatty acids. This fungi has many pharmacological activities, such as anti-tumor, and asthma.This paper studied on the compounds and pharmacological activities of the fruiting body of Fomitopsis officinalis. And make a pharmacokinetic study of 3-keto-dehydrosulfurenic acid which is one of Fomitopsis officinalis’ effective components.This paper’s first part used gradient extraction by petroleum ether, ethyl acetate, acetone, methanol to get different extracts of the fruiting body of Fomitopsis officinalis. And make a determination of terpene and sterol content in these extracts by spectrophotometric method. At the same time, nine compounds was separated from Et OAc fraction of Fomitopsis officinalis in this paper, and five of them were identified by NMR as 3-keto-dehydrosulfurenic acid, dehydroeburiconic acid, and fomefficinic acids A, B,C.At the secend part, a test was made to evaluate the effects of 3-keto-dehydrosulfurenic acid and dehydroeburiconic acid by viz. inhibition rates of tumor. The detection index were inhibitory rate, thymus index, spleen index, and made the paraffin section of tumor which removed from these tumor-burdened mice for HE staining and S-P immunohistochemical method(streptomycin avidin peroxidase) to made a detection of RUNX3 antibody. The results showed that both of them had a good effect, and the 3-keto-dehydrosulfurenic acid was better than the dehydroeburiconic acid, its inhibitory rate can reach 70.08% at the dose of 9 mg/ml, close to the positive control group(76.42%). Each group of the thymus index and spleen index were extremely significant difference with the negative group, shows that they can improve the immunity of animals. The results of the HE staining and S-P immunohistochemical showed that they were useful, the tumor cells were deformation or fracture in paraffin section of HE staining. every groups could 3-keto-dehydrosulfurenic acid’s high dose group(9mg/m L), dehydroeburiconic acid’s high dose(9mg/m L) and middle dose group(6mg/m L) could reduce the Bcl-2 expression of cells, and could made the cells had a higher expression of Bax.The pharmacokinetic study was made by 3-keto-dehydrosulfurenic acid at third part. After oral administration or intravenous administration of 3-keto-dehydrosulfurenic acid to rats, take their blood and guts in different times, and detection by high performance liquid(HPLC). Drawn the results into a drug concentration- time curves and a histogram. Agilent Eclipse XDB-C18 column(250mm×4.6mm,0.5μm)was used in this paper. The detection wave length was 242 nm and the column temperature was 25 ℃, 58% acetonitrile-42% water was used as the mobile phase was at the flow rate of 0.8 m L/min. The recording time is 40 min, and the peak time of sample was about 25 min.Stability experiments in vivo and in vitro showed the 3-keto-dehydrosulfurenic acid’s stability is good. The detection of oral administration after 1 h had a better result, so did the samples which placed in vitro 0-6 h, but the urine and feces samples which collected in 0-6 h did not detect obvious samples. Following oral administration, the average Tmax was 35 min, the V/F and CL/F showed that 3-keto-dehydrosulfurenic acid can rapid distribution in the whole body, and can be rapidly metabolized. Meanwhile, after intravenous administration, the average t1/2 were 40 min. The distribution results of 3-keto-dehydrosulfurenic acid in visceral organs showed that the liver had highest content of drugs after oral administration, while the heart had highest content of drugs at the earilst after intravenous administration.Nine compounds were get form the Fomitopsis officinalis, and five of them were identified by NMR. Pharmacological activities of 3-keto-dehydrosulfurenic acid and dehydroeburiconic acid were confirmed by experiments.3-keto-dehydrosulfurenic was the better one. Some conclusions were get in the pharmacokinetic study. Distribution and elimination of this compound were fast in the rats’ body, at the same time it was a stable compounds. And it reached the peak in the liquid phase detection soon. All the studies in this paper was laid a solid foundation for the research of the Fomitopsis officinalis and the 3-keto-dehydrosulfurenic acid. |
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