As one portion of the National Natural Science Foundation of China(No.81873096),the study involves four chapters,literature review,investigation of chemical constituents in Gardenia jasminoides Ellis,the structural analysis of gardenia blue pigment and evaluation of its biological activities in vitro,and hepatoxicity assessment of gardenia blue pigment.Gardenia blue pigment is a pigment product,which was included in the list of Food Additives in China in 1990.Iridoids from the fruit of Gardenia jasminoides Ellis are essential for preparation of gardenia blue pigment.Gardenia blue pigment is obtained from the reaction of its hydrolytic aglycones with amino acids.Recently,studies have shown that gardenia blue pigment displays potent anti-depressive effect better than that of fluoxetine,a clinical anti-depressive drug.However,the chemical structure of gardenia blue pigment is still not clearly understood.In the present study,we isolated several iridoids from Gardenia jasminoides Ellis and identifiedthe structure of gardenia blue pigment.We evaluated the neuroprotective activity of gardenia blue pigment in vitro and hepatoxicity assessment in vivo as well.We identify eighteen chemical constituents,including jasminoside W(1)and six iridoids(2~7)using combination of 1D and 2D NMR,MS,and CD.Moreover,eight gardenia blue pigments A~H(19~26)are synthesized fromgeniposide(2),6α-hydroxygeniposide(4),and 6βhydroxygeniposide(5),and identified unambiguously.Based on the monoamine oxidase B suppression assay and the neuroprotective evaluation,we observed five gardenia blue pigments(B,D,E,G,H)were with potent neuroprotective activities.Hepatic toxicity test revealed that no significant change in liver functions(ALT,AST,TC,TG)of gardenia blue pigment treatment group,as compared to control group.This is consistent with the observation on liver pathology slides,suggesting gardenia blue pigment has no significant hepatoxicity and possesses a favourable safety profile.Furthermore,the application history of Gardenia jasminoides Ellis,advances in its chemical constituents and biotoxicity,the utilization profile of its resources,and the recent advances of gardenia blue pigment were summarized.Our study provides scientific basis for expanding the application of iridoids in Gardenia jasminoides Ellis,enhancing the utilization value of gardenia blue pigment,and improving the utilization efficiency of Gardenia jasminoides resources. |