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By modifiating substituent of A cycle or D cycle in lignan of Cleistanthin A through chemical synthesis, various structure of aromatic aldehydes were used as basic materials to synthesis lignan analogues through a five-step reaction including Adol and Diels-Alder reaction, and its overall yield were 38.5-43.5%. Then, eight diphyllin glycosides analogues were synthesized from lignan analogues and 2-O-acetyl-3,4-di-O-methyl-α-xylopyranosyl bromide through the phase transfer catalysis (PTC). Lastly, using natural diphyllin glycosides Cleistanthin A as raw material, and then various chain aliphatic hydrocarbon were utilized to connect to the C-2” hydroxyl of glycosyl, and then connect different heterocyclic base, and a total of fourteen diphyllin glycoside heterocyclic analogues were synthesized. A549, HCT-116, HepG2 and Hela cell were exposed to 22 Cleistanthin A analogues. IC50 values were calculated to determine the anti-proliferative activities of these compounds by MTT assay. Ultraviolet–visible spectroscopy(UV-Vis) was used to measure the largest absorbing wavelength of 22 Cleistanthin A analogues in water-saturated solution and n-octyl alcohol solution, showing the absorption value in aqueous phase and oil phase. Then, calculating the octanol-water partition coefficient logP through the formula logP=log(Co/Cw). The IC50 values of 22 Cleistanthin A analogues were obtained by MTT assay. Results of structure-activity relationship showed that the anti-proliferative activities of compound through modifiating substituent of A cycle or D cycle in lignan were decreased compared to Cleistanthin A, while adding 3-hydroxy to D cycle increased its activities. The compound through adding various chain of heterocyclic base to hydroxyl of C-2” in the part of glycosyl-Cleistanthin A showed strong inhibitory activites, and its activity was gradually deceased along with the increased length of C-chain of glycosyl. While terminal base was morpholine or methyl piperazine, its activities were better than other base. Results also showed that the inhibitory activities of these 22 compounds against HCT-116 were stronger then other three cancer cell lines, and this indicated the selectivity to cancer cells. Higher logP value showed better fat-solublity, and inversely, the water solubity. The logP value less than 5 showed the better oral bioavailability, providing important evidence for pharmacodynamics. All the logP values of these 22 Cleistanthin A analogues were distributed between 2 and 6, suggesting the better oral bioavailability. |
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