| Objectives:Previous studies showed fungus plant extract AMH (Antimutagen-He) had significant anticancer, cancer chemopreventive and antimutagenic effects. D6B2is one of the anticancer bioactive compounds separated from AMH. Present study was to separate D6B2from AMH, to study its anticancer activities both in vitro and in vivo, and to observe its toxic effects on animal’s body and organ. Present study can provide scientific data for the utilization of compound D6B2as an anticancer drug.Methods:D6B2was isolated and purified by organic solvent extraction and column chromatography, combined with anticancer activity tracing. The in vitro anticancer effects of D6B2on human nasopharyngeal carcinoma cell CNE, human hepatocellular carcinoma cell Hep G2, human cervical carcinoma cell HeLa, human cholangio carcinoma cell QBC939, human erythromyeloblastoid leukemia cell K562and its combinative anticancer effects with DDP were detected by cell counting or MTT assay. The in vivo anticancer effects on human lung cancer NCI-H460and its toxicity were investigated on BALB/c nude mice.Results:(1)15g D6B2(purity more than99.8%) was obtained from38kg fungus plant powder, and the yield was0.04%.(2) The inhibitory ratio of D6B2(25μM,50μM,100μM,150μM,200μM) on human nasopharyngeal carcinoma cell CNE were24.95%,42.11%,65.74%,70.22%,73.11%; on human hepatocellular carcinoma cell Hep G2were23.15%,54.56%,62.95%,70.14%,75.18%;on human cervical carcinoma cell HeLa were31.34%,60.76%,78.43%,85.78%,90.75%; on human cholangio carcinoma cell QBC939were5.97%,12.05%,28.44%,35.28%,51.31%; on human erythromyeloblastoid leukemia cell K562were18.20%,35.48%,46.76%,58.44%,57.32%. Evident dose-effects existed in the anticancer activity. The IC50for CNE, Hep G2, HeLa, QBC939and K562were66.9μM,60.98μM,40.7μM,197.07μM and120.06μM respectively. HeLa was the most sensitive one.(3) The inhibitory ratio of D6B2(25μM,50μM,100μM,150μM,200pM) on HeLa were7.96%,9.56%,10.98%,14%,17.33%at24h;0.62%,25.96%,47.63%,48.24%,49.03%at48h;18.08%,53.68%,85.55%,87.86%,82.07%at72h, the in vitro anticancer effects on Hela was time-dependent.(4) The q values of D6B2at25μM,50μM and100μM were1.02,1.01and0.99when used with DDP at10μM respectively.(5) The relative proliferation ratio of D6B2(30mg/kg)on NCI-H460were77.53%,64.9%,62.91%,60.53%and51.96%at day4,8,12,16and20respectively. The tumor weight inhibitory ratio was43.51%.(6) The body weight of Control were22.54g,22.88g,23.68g,24.38g and24.43g at day4,8,12,16and20respectively, meanwhile, the body weight of D6B2group were20.94g,19.78g,20.15g,20.64g and19.95g. The organ coefficiency of Control were6.69(liver),1.44(spleen),1.72(kidney),0.84(testis), and the organ coefficiency of D6B2group were6.02(liver),0.90(spleen),1.74(kidney),0.92(testis).Conclusions:(1)15g D6B2was obtained from38kg fungus plant powder, the purity was more than99.8%, and the yield was0.04%.(2) D6B2showed significant in vitro anticancer effects on all the tested cancer cell lines, Hela was the most sensitive one.(3) The in vitro anticancer effects of D6B2was time-dependent and dose-dependent.(4) D6B2and DDP had additive in vitro anticancer effects.(5) D6B2(30mg/kg) showed significant in vivo anticancer effects on NCI-H460transplanted tumor in BALB/c nude mice.(6) D6B2showed toxic effects on the growth of body, liver and spleen, but did not affected kidney and testis. |
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