Preliminary Study On The Synthesis Of Amino Acid Derivatives Of Corosolic Acid And Its Hypoglycemic Effect

Diabetes is one of the most important human health problems in recent years,so the research and development of drugs for the treatment of diabetes is also one of the hot spot on pharmacy in the past two decades.Corosolic acid from natural sources has action on anti-cancer,lowering blood sugar,anti-inflammatory,anti-viral and anti-cardiovascular disease.Especially it can play a physiological role similar to insulin,so he is also known as "plant insulin".With good anti-diabetics activity,it has been developed into a variety of domestic and foreign health care products and got a widespread concern currently.However,because of the poor water-solubility,Corosolic acid leads to low bioavailability.There is an urgent need for derivatization by modifying its structure to increase its hydrophilicity,thereby improving its bioavailability and pharmacological activity.In this paper,we introduced glycine（Gly）,alanine（Ala）,serine（Ser）,leucine（Leu）,phenylalanine（Phe）and proline（Pro）,kinds of natural a-amino acids,in the 28 carboxy of Crosolic acid.A new synthesis of six kinds of Corosolic acid derivatives was completed.Structural characterizations of these compounds were carried out with ¹HNMR,¹³CNMR and ESI-MS.In preliminary pharmacological studies,we determined using gop-pod to measure the glucose content in culture medium of each group,with average value of each blank well as the control group.Using the changes in the value of the group to calculate the glucose content（GC）in the culture medium each well.Meanwhile,the OD value was measured by MTT assay culture medium in each group on a microplate reader,the final GC/MTT represents the sugar consumption of cell in each unit.