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Abstract
In the course of our continuing research in development and evaluation of novel skin cancer chemopreventive agents from marine sources, five semi-synthetic cembranoids derived from the marine natural product sarcophine, isolated from the soft coral Sarcophyton glaucum, were synthesized and shown to exhibit a remarkable chemopreventive activity in the in-vitro Epstein Barr Virus Early Antigen (EBV-EA) activation assay. These compounds were assayed in vivo using the two-stage carcinogenesis test of mouse skin tumors induced by 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator, and 12-O-tetradecanoylphorbol-13-acetate (TPA) as a promoter by topical administration. They showed potent inhibition of both percentage incidence of skin tumor as well asthe multiplicity of skin tumors per mouse compared to untreated controls.Semi-synthetic Cembranoids from Marine Sources
Highlights
It is well-documented that marine natural products have great potential applications in the treatment of human diseases [1]
In our previous work [15,16,17,18], we have reported a new class of compounds obtained by chemical modification of a marine natural product, sarcophine that is the main secondary metabolite of the soft coral Sarcophyton glaucum, and is much more abundant than sarcophytol A
All the five newly prepared semi-synthetic sarcophine derivatives exhibited significant inhibitory effects on the tumor promotion induced by DMBA and TPA
Summary
It is well-documented that marine natural products have great potential applications in the treatment of human diseases [1]. Sarcophytol A is a cembranoid isolated from the soft coral Sarcophyton glaucum, and was shown to inhibit the development of several tumors in experimental animals [2,3], skin cancer [2]. Chemoprevention of skin cancer involves the administration of chemical agents to prevent the initiation, and/or promotion, and/or progression events that occur during the multistage process of neoplastic development [10,11].
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