| As the main reason of destroying human's health and leading to death, tumor together with Viral disease and Senile disease are considered as three challenges of modern medicine. People in the whole world never stop seeking the effective methods to treat cancer, and just because of these unremitting efforts, it has already been possible to cure more than 30% of tumors. Pharmacotherapy is one of the three treatments for cancer, and after 40 years endeavor, people have found several dozens of medicines that function to counteract tumor, which contribute to great curative effects for a variety of tumors. The majority of familiar entity tumors such as lung cancer, hepatocarcinoma, carcinoma of colon, and pancreatic carcinoma, nevertheless, are still devoid of effective medicines. As a number of antineoplastics cause to tolerance in the process of clinical application, it is imperative to investigate new type of antineoplastics.Traditional Chinese Medicine has recorded and discussed a great deal about tumor, and has diffenrent opinions on the cause of tumor, most of which deem it pertinent to the stasis of cancer toxin. Cancer toxin struggle with zhengqi, and consequently come the various symptoms of cancer patients. Therefore, cancer toxin is one of the key parts of tumor pathology. Among a host of managements and medicines for tumor therapy, which come down from the medicine of past dynasties and folk medicine, is taking assaulting toxin as the main purpose that has played an important role. Arenobufagin is one of the familiar drugs. Modern clinical research has proved that there is satisfying curative effect when arenobufagin is used to treat many malignant tumors.Phrynin ligand compounds are the main chemical materials in arenobufagin, which include bufalin, resibufogenin, cinobufagin, and so on. Research studies have indicated that bufalin is one of the main components of arenobufagin that effectively counteract tumors, and has significant growth suppression actions to sorts of tumor cells in vitro, the mechanism of which is relevant to inducing tumor cells to their differentiation and apoptosis. Cinobufagin has some anticancer function in vitro, either. As to resibufogenin, prescribed in pharmacopeia as one of the two identification constituents of arenobufagin, in the field of anticancer, only Kamano etc. have discovered its obvious cytotoxic activity to hepatocarcinoma cell PLC/PRF/5. To attest the anticancer function of resibufogenin, our experiment observed its growth suppression action to human leukemia HL-60 and cervix cancer Hela cells in vitroand to nude mice transplant tumors that come from human cervix cancer Hela cells in vivo, and studied its mechanism of anticancer.The results of experiments in vitro shows that resibufogenin has remarkable inhibition action to the growth of human leukemia HL-60 and cervix cancer Hela cells. This action appears to have time-dependent relation and dosage-dependent relation, and IC50 lies in approximate 10-1.00(mol/L. Flow cytometry and results of agarose gel electrophoresis evidence that the mechanism of the cytotoxic action of resibufogenin to the two kinds of cancer cells mentioned above is close to apoptosis.The experiments in vivo demonstrate that high-dose resibufogenin (15mg/kg) has prominent suppression action to nude mice transplant tumor that come from human cervix cancer Hela cells, and there is no following suppression action after stopping using it; the intensity of inhibiting the growth of tumor cells of 15mg/kg resibufogenin corresponds to that of 5mg/kg Bleomycin A5; it has no patent influence on the weight of mice with Hela cells, while high-dose resibufogenin (15mg/kg) has somewhat strong acute neurotoxicity, but there has been no proof to show that it has immediate toxicity Combining both results of vitro and vivo, we believe that resibufogenin does have significant anticancer function, the mechanism of which may be relevant to accelerating the apoptosis of cancer cells, and that it is the main anticancer component of arenobufag... |
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