Study On Synthesis And Activity Evaluation Of Albaspidin Andits Derivatives

Male fern rhizome are the dry root?stem and petiole residues of Cyrtomium rhizome,shows various bioactivity such asantidiabetes,antiviral,antioxidant,anti-inflammatory,antitumoret al.Although natural polyphenol compounds can be elicited from many soybean plants,they are typically obtained as a complex mixture and very small quantities which leads to its limiting of development.Albsapidins are the main active polyphenol ingredients.The situation has prompted explorations towards the production of albaspidins by artificial chemical synthesis.In this paper,it developed the simple and low-cost procedures to synthesize three series of albaspidins.The antitumor and antioxydantactivities of all synthesized products were also investigated.The research will be helpful to the further investigation of albaspidin-based drugs.The design and synthesis of albaspidins and their derivatives were started fromphloroglucinol.The synthesis process were optimized.The key steps of our scheme are regional selective Friedel-Craftcetoxylation,and Friedel-Craftalkylation,selective protection.Albaspidins and their derivatives were synthesized strating fromphloroglucinolby 7 steps in23%-44%overall yields.The structures of the key intermediates and target compounds were confirmed by 1D and 2D-NMRs and LC-MS.Finally,the antitumor activity evaluation of target compounds against hepatocytes cells(HepG2)leukemia cells(K562)and colon cells(HT-29)indicated that carbon chain in 2,6,6' has a positive correlation with its antitumor activities,as well as substituent in 11,also,the antioxident activity evaluation of target compounds demonstrate that carbon chain in 2,6,6' has a positive correlation with its antioxident activities,substituent in 11 has few influence.The studies on synthesis and activity of these series of natrual and artificial synthesd compounds have important significance for structure-activity relationship and new drug development of albaspidin.