PMID- 30681694
OWN - NLM
STAT- MEDLINE
DCOM- 20190701
LR  - 20190701
IS  - 2042-650X (Electronic)
IS  - 2042-6496 (Linking)
VI  - 10
IP  - 2
DP  - 2019 Feb 20
TI  - Antiplatelet aggregation and antithrombotic benefits of terpenes and flavones 
      from hawthorn leaf extract isolated using the activity-guided method.
PG  - 859-866
LID - 10.1039/c8fo01862f [doi]
AB  - Hawthorn is a well-known functional food; at present, increasing attention has 
      been given to hawthorn leaf due to its numerous functional and nutritional 
      properties. In this study, the antithrombotic properties of hawthorn leaves were 
      evaluated using the activity-guided isolation process and high-performance liquid 
      chromatography-quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS). A 
      crude extract prepared in 75% ethanol was fractionated using macroporous resin 
      D101 and polyamide chromatography to obtain three active fractions (Fr.C, Fr.C-1 
      and Fr.C-2). Thereafter, the inhibitory activities of these fractions were 
      examined by platelet aggregation and antithrombus assays using a zebrafish model. 
      Using the HPLC-QTOF-MS technique, we identified 25 compounds in the active 
      fraction (Fr.C). The structures of these compounds were identified by comparing 
      the retention time (tR) and mass spectral data from the previous reports and 19 
      reference compounds. Based on the analysis, 21 peaks were detected in the mass 
      spectrum of Fr.C-1 and 8 peaks were detected in Fr.C-2, we found that 11 
      compounds in Fr.C-1 exhibited potent inhibitory effects on platelet aggregation, 
      including nine monoterpenoids, one diterpenoid and one flavanone. Accordingly, 
      monoterpenoids are suggested as the main anti-platelet aggregation constituents 
      from hawthorn leaves. Particularly, compounds 10 and 24 inhibited ADP-induced 
      platelet aggregation and delayed FeCl3-induced thrombus in zebrafish. 
      Furthermore, interactions between compounds 10 and 24 with two ADP receptors P2Y1 
      and P2Y12, serving as the target for key regulators of antiplatelet aggregative 
      activity, were investigated via molecular modeling. In addition, five flavones 
      were obtained from the active fraction (Fr.C-2). These results indicated that 
      monoterpenoid glycosides and some flavones were responsible for the 
      antithrombotic activity of hawthorn leaves. Moreover, this study shows that the 
      activity-guided isolation is a fast, efficient and systematic separation method 
      for the identification of active compounds in natural products.
FAU - Gao, Pinyi
AU  - Gao P
AD  - School of Traditional Chinese Materia Medica, Key Laboratory of Computational 
      Chemistry-Based Natural Antitumor Drug Research & Development, Liaoning Province, 
      Shenyang Pharmaceutical University, Shenyang 110016, China. 
      lilingzhijessie@163.com.
FAU - Li, Shuangshuang
AU  - Li S
FAU - Liu, Kechun
AU  - Liu K
FAU - Sun, Chen
AU  - Sun C
FAU - Song, Shaojiang
AU  - Song S
FAU - Li, Lingzhi
AU  - Li L
LA  - eng
PT  - Journal Article
PL  - England
TA  - Food Funct
JT  - Food & function
JID - 101549033
RN  - 0 (Fibrinolytic Agents)
RN  - 0 (Flavones)
RN  - 0 (Plant Extracts)
RN  - 0 (Terpenes)
SB  - IM
MH  - Animals
MH  - Crataegus/*chemistry
MH  - Fibrinolytic Agents/*pharmacology
MH  - Flavones/chemistry/*pharmacology
MH  - Medicine, Chinese Traditional
MH  - Models, Molecular
MH  - Molecular Structure
MH  - Plant Extracts/chemistry/*pharmacology
MH  - Plant Leaves/*chemistry
MH  - Platelet Aggregation/*drug effects
MH  - Terpenes/chemistry/*pharmacology
MH  - Zebrafish
EDAT- 2019/01/27 06:00
MHDA- 2019/07/02 06:00
CRDT- 2019/01/26 06:00
PHST- 2019/01/27 06:00 [pubmed]
PHST- 2019/07/02 06:00 [medline]
PHST- 2019/01/26 06:00 [entrez]
AID - 10.1039/c8fo01862f [doi]
PST - ppublish
SO  - Food Funct. 2019 Feb 20;10(2):859-866. doi: 10.1039/c8fo01862f.