| Objective: To extract and purify fresh Gekko.swinhonis.Gunther anticancer active component. To manufacture fresh Gekko.swinhonis.Gunther antineoplasmic activity component extractive liposome and study antitumor pharmacodynamics for Gekko.swinhonis.Gunther anticancer active component, investigate its antitumor mechanism in vivo and vitro.METHODS:To capture fresh Gekko.swinhonis.Gunther and distinguished with lizard,to sieve out the best extrat schema by MTT,to hypersound extrat fresh Gekko.swinhonis.Gunther anticancer active component with 85% alcohol. To perpare antineoplasmic active component liposome with antiphase evaporation method,film dispersion method,spin film–hypersound method.Using particle diameter, particle size distribution, envelopment efficency, drug loading as target,the single factor was investigated,such as lipoid materials usage amount,drug usage, hypersound intensity,hypersound time and aqueous bath temperature. Anticancer active component liposome was prepared with turning membrane- hypersoun. MTT and was used to detect CT-26 and Heper-G2 growth activity according to different drug concentration in vitro.The experimental animal mould was BALB/C mouse which age was 4～6 weeks and weight was 22±2g ,♀.Athymic mouse was hypodermic inoculated CT-26 cell suspension in its left hind limb dorsi,it was routine rear of constant temperature(25℃) and constant humidity(45%).CT-26 and Heper-G2 tumor cells treated for 24-144h by various concentrations suspension of fresh Gekko.swinhonis.Gunther antineoplasmic activity component extraction (FGE) were assessed in vitro. Antiproliferation was obtained by MTT. The transplant tumor model of CT-26 in BALB/C mice was established. CT-26 tumor model mice were divided randomly into five groups ,the Cytoxan positive group,the FGE group and the negative control group,they were treated respectively with intraperitoneal injection of Cytoxan 100 mg·kg-1, FGE 10mg·kg-1,5mg·kg-1and 1mg·kg-1 respectively,and equal volume of saline, intragastric administration of Gekko pulvis 100 mg·kg-1. The medication was given for 12 times totally, and mice were to take in food and water freely , after putting to death by dislocation to measure mice body weight, to dissect subcutaneouly tumor.The anti-tumor activity was evaluated by tumor tissue weighing. Antiproliferation rate of tumor cell was detected in vivo and in vitro. The light microscop results manifested that typical apoptosis cell morphology change in administer experiment group ,cell membrane integrated, cell volume became smaller,synapse became shorter,cell shrinked to round, cell outline became clear. RESULTS: The pharmaco-essay manifested that Antiproliferation rate of extractive with 85% alcohol hypersound method was 46.95 % . The liposome of fresh Gekko.Swinhonis.Gunther antineoplasmic activity component was prepared by turnning film - hypersound.The similar round was seen with transmission electron microscope, which mean diameter was 355.6±51.2nm,EE was 52.50%,DL was 4.16%, pH 5.85,the liposome diameter consisitent with target desire. The pharmacodynamics experiment in vitro manifested that fresh Gekko.Swinhonis.Gunther antineoplasmic activity component suspension could obviously inhibit cell proliferate in a time-and dose-dependet manner in vitro and vivo,the ratio of inhibiting was 9.52%～62.30%,Heper-G2 cell was expose to FGE of 1 mg/ml,10.0mg/ml for 48h,Apoptosis ratio was enhanced gradually according to increasing FGE concentration .Higher dosage groups (apoptosis ratio: 33.2%) hadn't significant difference compared with positive control group, apoptosis ratio of lower dosage groups hadn't significant difference compared with control group(P>0.05) .The animal experimental results manifested that FGE could inhibit mouse cancer growth with some dosage-efficency relationship. The content of TNF-αin eyeball blood and NO secreted by mouse macrophage had significant difference compared with control group(P<0.05). The mean inhibiting ratio of high dosage group of FGE liposome was 52.17%,which had significant difference compared with'Tianlongsan'group(P<0.01), Antiproliferation rate of liposome had significant enhance compared with FGE in same concentration. CONCLUSION: Our test results showed that fresh Gekko.swinhonis.Gunther antineoplasmic activity component suspension could effectively decrease CT-26, Heper-G2 cell proliferation both in vitro and vivo,suggesting that antineoplasmic activity component extraction of fresh Gekko.Swinhonis.Gunther might be a potential anticancer drugs. The extract antineoplasmic activity component effective was best with 85% alcohol-hypersound,EE was higher with turning membrane-hypersound to prepare liposome. The extraction can inhibit several varieties of tumor cell. In the limited scope of drug concentration, the ratio of anti-cancer rises with the drug concentration rising.This study first confirmed that fresh Gekko.swinhonis.Gunther antineoplasmic activity component suspension induced BALB/C model mouse tumour cell apoptosis might be by enhancing TNF-αlevel to bring into full playing antitumouse effect,it provided experimental evidence for fresh Gekko.swinhonis.Gunther antineoplasmic activity component suspension anticancer mechanism .
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