| IntroductionColorectal cancer is one of the most common malignant gastro -intestinal cancers in both China and western world. According to the worldwide epidemiological survey, it has been the most common alimentary malignant cancer in North America, west Europe and Australia. In China, it is the forth most common cancer following gastric cancer, lung cancer and liver cancer. But with the improvement of human life in China, the incidence of colorectal cancer has been increasing year after year. The etiological factors of colorectal cancer have not been elucidated yet; we only know that it is related to genetic factors, diet factors, canceration of colon polyps and chronic coloni-tis. Early detection, early diagnosis and early surgical sectio^i still remain the only effective measures for early colorectal cancer patients. But in advanced patients with metastasis the prognosis is not satisfying after surgical section associated with chemotherapy and radical therapy. So one of the major tasks in molecular colorectal cancer field still remains to find new effective agents in therapy.The retinoids, including vitamin A and its metabolites, and thousands of synthetic derivatives structurally or functionally similar to vitamin A, are very strong potent drugs affecting cellular proliferation, inducing cell differetiation or apoptosis both in vitro and in vivo. Polarend group, annular end group and poly - aethylenum side chain compose the chemical structure of retinoids molecule. According to the different derivative molecular group of the drugs, thousands of current retinoids can be grouped into three generations; the first generation is the changes on the polar end group such as 9 - cis retinoic acid; the second generation is the changes on the annular end group such as all- trans retinoic acid ( ATRA) whereas the third generation is the changes on the poly - aethylenum side chain such as mofarotene Ro 40-8757. Preclincial and clinical studies have led to the development of first - and second - generation retinoids, used alone or in combination with cytotoxic drugs, in the treatment of acute promyelocytic leukemia ( APL) in both China and other countries. In an attempt to find new retinoids devoid of the side effects associated hypervitaminosis A syndrome in cancer therapy, the third - generation retinoids have caught more and more researchers eyes. They were also shown to be a potent compound with positive anti - proliferate activity against a variety of human cancer cell lines derived from breast, lung, uterus, pancreas and many other cancers. On some cancer cell lines derives from gastro - intestinal and pancreatic tissues, mofarotene has shown 70 times more potent effects compared to ATRA when evaluated by half -maximal inhibition of cell proliferation. Among the third generation retinoids, Ro 40 -8757 mofarotene (4 - [2 - [p - [ (E) 2(5,6,7, 8-Tetramethyl-2-naphthyl) propenyl] phenoxy] ethyl] - norpho-line) , a novel arotinoid with a morpholine structure on the poly -aethylenum side chain, is of particular interests. It inhibits the growth of various human cancer both in vitro and in vivo, and, moreover, protects the bone marrow from the toxic effects of cytophosphamide and 5 - fluorouracil (5 - FU) in vivo.In view of the high incidence of human colorectal carcinoma in China and in most western countries, we examined in this study the anti - proliferate effects of Ro 40 - 8757 on human colorectal carcinoma cell line CCL - 187 and attempt to clarify the mechanisms of these anti - proliferation effects.MaterialsHuman colorectal cancer cell line CCL - 187 is kindly presented by Dana - Farber Cancer Research Institute ( Harvard Medical School, USA) ; and Ro 40 - 8757 is a generous gift from Dr. Michael Glaus (F. Hoffmann-La Roche Ltd, Basle, Switzerland).MethodsIn this study, MTT method was used to demonstrate the anti -proliferation effects of Ro 40 - 8757 on human colorectal cancer cell line CCL - 187. Half - maximal inhibition of cell proliferation by the agent was obser...
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