摘要
皮下注射紫草素(shikonin)10mg.kg-1对小鼠巴豆油耳炎症和大鼠酵母性足肿有明显抑制作用;在白细胞体外温孵系统中,紫草素在10-4~10-7mol·L-1浓度范围内可浓度依赖性地抑制LTB4和5-HETE生物合成,其50%抑制浓度(IC50)分别为6.2×10-7mol.L-1和2.6×1O-7mol·L-1。此外,还报道紫草素几个天然衍生物对LTB4生物合成的影响。
Shikonin is
one of the active components isolated from the dry root of
Arnebiaeuchrona(Royle) Johnst(AERJ).It has been shown to have anti
inflammatory activity on formalde-hyde induced paw swellil1g in rats.
Preparations of AERJ has been used clinically in curing phlebitisand
vascular purpura,In the present study ,sc administered shikonin was
shown to have significantinhibitory effects on ear edema induced by
croton oil in mice and paw swelling induced by yeast inrats.In order
to investigate the influence of shikonin on biosynthesis of LTB4 and
5-HETE, an in vitroleukocyte incubation svstem was adopted.The
results showed that shikonin has fairly strong inhibitoryeffects on
LTB4 and 5-HETE biosynthesis.Its effects and concentrations fit a
positive relationshipwithin the range of 10-7~10-4mol·L-1.The
equations of inhibition(Y)versus concentration(X,LogC)obtained by
linear regression were Y= 166+18. 7X(r=0. 9319) for LTB4 and Y=
173+18.7X(r=0.9856)for 5-HETE. The IC50 were 6.2× 10-7 and 2.6×
10-7mol·L-1,respec-tively.The results also indicate that natural
shikonin derivatives have similar inhibitory effects onLTB4
biosynthesis. These results suggest that inhibition of LTB4 and
5-HETE may play a major role inthe mechanism of anti inflammatorv
effects of shikonin。
出处
《药学学报》
CAS
CSCD
北大核心
1994年第3期161-165,共5页
Acta Pharmaceutica Sinica
关键词
紫草素
萘醌
白三烯B4
抗感染药
Shikonin
Naphthoquinone
Anti
inflammatory drug
Leukotriene B4