Platelet anti-aggregation activities of compounds from Cinnamomum cassia.
Cinnamomum cassia is a well-known traditional medicine for improvement of blood circulation. An extract of this plant showed both platelet anti-aggregation and blood anti-coagulation effects in preliminary testing. Among the 13 compounds obtained from this plant, eugenol (2), amygdalactone (4), cinnamic alcohol (5), 2-hydroxycinnamaldehyde (7), 2-methoxycinnamaldehyde (8), and coniferaldehyde (9) showed 1.5-73-fold greater inhibitory effects than acetylsalicylic acid (ASA) on arachidonic acid (AA)-induced aggregation (50% inhibitory concentration [IC₅₀] = 3.8, 5.16, 31.2, 40.0, 16.9, and 0.82 μM, respectively, vs. 60.3 μM) and 6.3-730-fold stronger effect than ASA on U46619 (a thromboxane A₂ mimic)-induced aggregation (IC₅₀ = 3.51, 33.9, 31.0, 51.3, 14.6, and 0.44 μM, respectively, vs. 321 μM). The other compounds, coumarin (3), cinnamaldehyde (6), cinnamic acid (10), icariside DC (11), and dihydrocinnacasside (12), also inhibited (2.5 to four times greater than ASA) U46619-induced aggregation. In addition, compounds 2, 4, 5, 6, 7, 8, and 9 were 1.3-87 times more effective than ASA against epinephrine-induced aggregation (IC₅₀ = 1.86, 1.10, 37.7, 25.0, 16.8, 15.3, and 0.57 μM, respectively, vs. 50.0 μM). However, the 13 compounds were only very mildly effective against blood coagulation, if at all. In conclusion, compounds 2, 4, 8, and 9 showed stronger inhibitory potencies than others on AA-, U46619-, and epinephrine-induced platelet aggregation. Eugenol (2) and coniferaldehyde (9) were the two of the most active anti-platelet constituents of C. cassia.
Kim
Sun Young
SY
Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul, Republic of Korea.
Koo
Yean Kyoung
YK
Koo
Ja Yong
JY
Ngoc
Tran Minh
TM
Kang
Sam Sik
SS
Bae
KiHwan
K
Kim
Yeong Sik
YS
Yun-Choi
Hye Sook
HS
D000818:Animals; D000925:Anticoagulants / Q000302:isolation & purification / Q000494:pharmacology; D001792:Blood Platelets / Q000737:chemistry; D032904:Cinnamomum aromaticum / Q000737:chemistry*; D005343:Fibrinolytic Agents / Q000302:isolation & purification / Q000494:pharmacology; D010314:Partial Thromboplastin Time; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D011517:Prothrombin Time; D051381:Rats; D017207:Rats, Sprague-Dawley; D013918:Thrombin Time; D013928:Thromboxane A2 / Q000097:blood; D013929:Thromboxane B2 / Q000097:blood
D000925:Anticoagulants; D005343:Fibrinolytic Agents; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; D013929:Thromboxane B2; D013928:Thromboxane A2