| Rhubarb is the dry root of Rheum Palmatum L., also named Radix et Rhizoma Rhei Palmati, having a bitter and cold nature. Studies on rhubarb have gained great achievements since 1980s. It was proved that rhubarb can be effectively used in such areas as antitumor, diarrhea treatment, antibacterial, and adjusting functions of kidneys. In recent years, the antitumor effect of active anthraquinone components in rhubarb attracted great attentions worldwide. The main anthraquinone components include rhein, emodin, chrysophanol, and aloe-emodin. It was shown that emodin can inhibit the growth of tumor strain such as Hela and K562. The aloe-emodin is a new selective antitumor compound, which shows inhibition against neuroectoderm tumor of immune deficient mouse without affecting to the animals or the growth of the normal fibroblast cell. The other anthraquinone components in rhubarb also have good antitumor effect. In our previous work, these anthraquinone components have been found to possessing bone affinity property by hydroxyapative (HA) affinity experiment in vitro, which is similar to the tetracycline. The anthraquinone components in rhubarb are ideal and novel bone affinity compounds. This paper focus on the antitumor effect and bone affinity of anthraquinone components in rhubarb, link them to the known antitumor drugs for searching a new series of bone affinity antitumor compounds with higher effect and lower toxic. Starting materials emodin and chrysophanol were linked to 5-fiuorouracil or its derivatives after structure modification to prepare a series derivatives of anthraquinone components.In this paper, 28 target compounds are synthesized. All compounds are new and identified by ~1H-NMR and MS. All target compounds were carried out the antitumor activity screening and bone affinity assay in vitro. The result shows that the bone affinity of most synthetic compounds was better than tetracycline, but the antitumor activity were not significant in vitro. |
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