Analysis Of Phenolic Compounds In Hawthorn (Crataegus Spp.) Fruit And Their Bioactivity Evaluation

Phenolic profile and their bioactivities (antioxidant, anti-cancer, HUVEC protection and anti-diabetic activity) were investigated in 24 varieties of different parts of C. pinnatifida Bge, C. pinnatifida Bge. var. major N. E. Br. and C. hupehensis Sarg. fruit. The main results are as follows:1. Twenty-four phenolic compounds, including procyanidins, phenolic acids, flavonols, and anthocyanin were tentatively identified from hawthorn peel while 17 phenolic compounds from pulp. In addition, Idaein, flavonols (hyperoside, isoquercitrin, rutin and two unknowns) and p-coumaric acid derivative dominated in peel, whereas neochlorogenic acid were primarily found in pulp of some varieties like ’Yiduxiaohuang’. Above all, neochlorogenic acid and p-coumaric acid derivative were first reported in C. pinnatifida Bge. var. major N. E. Br. and C. hupehensis Sarg. Eleven phenolic compounds, such as Idaein, chlorogenic acid, neochlorogenic acid, epicatechin, PAB2, hyperoside, isoquercitrin, PAtrimer I, PA trimerⅡ, PA tetrame I, PA tetramer II profile varied among species. It indicated that C. pinnatifida Bge. has highest content of flavonols and C. hupehensis Sarg. was abundant in phenolic acids. Furthermore, C. pinnatifida Bge. var. major N. E. Br. has an advantage on procyanidins content over other two. Hierarchical cluster analysis showed that phenolic compounds in peel may be an important chemotaxonomic marker for differentiating species of hawthorn.2. As two antioxidant evaluation methods, DPPH and FRAP were used to divided 24 varieties hawthorn fruit in high antioxidant group and low antioxidant group, which demonstrated that there is a significant positive correlation between antioxidant activity and polyphenols. Thus seven varieties (’Fushunshanzha’,’Pingyitianhongzi’, ’Shanlihong’,’Xifenghong’,’Xiaohuangmianzha’,’Xinglongzirou’,’Yiduxiaohuang’) were selected for pharmacological activities. Results showed that’Xifenghong’, ’Xiaohuangmianzha’,’Yiduxiaohuang’ peel showed Protective effect on HUVEC under H2O2-induced stress, may related with hyperoside, chlorogenic acid and neochlorogenic acid.Partial hawthorn peel and pulp extract exhibited significant inhibitory effect on the growth of HepG2 liver, HL-60 leukemia, and MDA-MB-231 breast cancer cell lines. Results of antiproliferative activity of individual phenolic compounds indicated that chlorogenic acid exhibited significant inhibition effects on the proliferation of HepG2 and HL-60 activity, while epicatechin and neochlorogenic acid exhibited inhibition effects on HepG2, indicating that the antiproliferative activity exerted may partly attribute to phenolic compounds.Besides,’Shanlihong’,’Xinglongzirou’ and ’Yiduxiaohuang’ pulp showed increased effects on glucose consumption in HepG2 cells and a-glucosidase inhibitory activities while other varieties showed low activity. Results of individual phenolic compounds demonstrated that cells treated with epicatechin, chlorogenic acid and neochlorogenic acid showed increased consumption of glucose, which was similar to metformin. Therefore, the primary metabolites of hawthorn fruit may have hypoglycemic effect in vivo.In all, Hawthorn (Crataegus spp.), a medicinal and edible fruit, is rich in phenolic compounds with good health function and development potential. The research lad the foundation for furture study and provided a new basis for utilization and evaluation of hawthorn resources.