欧前胡素性质、用途与生产工艺
欧前胡素(imperatorin)和异欧前胡素(iso-impemtorin)属于6.7-峡喃香豆素类，广泛分布于植物界，尤其伞形科常用中药如白芷、独活、前胡、羌活、北沙参等含且丰富，而且是其主要药理效应成分。
在自然界中的含有欧前胡素的植物主要有以下几种：
1.大风子科(Flacourtiaceae)
罗旦梅Flacourtia jangomas(Lour.) Raeusch茎，皮
2.芸香科(Rutaceae)
米申酒饼簕* Atalantia missionis Oliver 根，茎皮(收率：4.1%)
被小绒毛芸香* Eriostemon tomentellus 地上部分
三狭叶藤桔* Luvunga angustifolia茎(收率：0.0026%)
3.伞形科(Umbelliferae)
宽叶高伞* Agasyllis latifolia
密花岩风 Libanotis condensata (L.) Crantz
西吉藁本* Ligusticum seguieri Koch根
欧前胡 Peucedanum ostruthium L.根
克氏邪蒿* Seseli krylovii
短尖邪蒿 Seseli mucronatum根
抗疟作用:欧前胡素对恶性疟原虫的IC50为2.4μg/mL，IC90为9.3μg/mL。
抗菌作用:对革兰阳性菌有选择性活性。
Imperatorin 是一种有效的 NO synthesis 抑制剂，IC50 为 9.2 μmol，也是 BChE 抑制剂，IC50 为 31.4 μmol。Imperatorin 是 TRPV1 的微弱激动剂，EC50 为 12.6±3.2 μM。
IC50: 9.2 μmol (NO synthesis), 31.4 μmol (BChE)EC50: 12.6±3.2 μM (TRPV1)
Imperatorin is a plant secondary metabolite belonging to the coumarins-specifically the furanocoumarins. Imperatorin enhances the GABA-induced chloride ion current (I
GABA
) through the α
1
β
2
γ
2S
receptors. Imperatorin potentiates I
GABA
at 100 μmol by 50.5±16.3 % and at 300 μmol by 109.8±37.7 %, respectively. Imperatorin, together with Phellopterin, found in the roots of A. dahurica, inhibit [
3
H]diazepam binding to the benzodiazepine site of the rat brain GABA
A
receptor in vitro with an IC
50
of 12.3 μmol for Imperatorin and 400 nmol for Phellopterin. Imperatorin, in a concentration ranging from 3.5 to 14 mmol, significantly and irreversibly inhibits GABA-T in a time-dependent and concentration-dependent manner, by irreversibly binding with the active site of GABA-T.Imperatorin is a reversible acetylcholinesterase (AChE) inhibitor, and acts in dose-dependent manner. The AChE and BChE inhibitory activities of Imperatorin and a crude extract from the fruits of
Angelica archangelica
L. is tested by the spectrophotometric method at concentrations of 12.5, 25, 50, and 100 μg/mL. Imperatorin displays low inhibition towards AChE (13.75-46.11 %), whereas it has remarkable inhibitory effect against BChE (37.46-83.98 %). Imperatorin shows selectivity toward BChE rather than AChE, with an IC
50
for BChE of 31.4 μmol. Imperatorin, together with (+)-Byakangelicol, are found to be the most effective BACE-1 inhibitors, with IC
50
s of 91.8 and 104.9 μmol, respectively. Imperatorin (IC
50
=9.2 μmol) is also effective as an inhibitor of NO synthesis. Imperatorin is a weak agonist of TRPV1, a channel implicated in detecting several noxious stimuli, exhibiting EC
50
of 12.6±3.2 μM.
At doses of 10 and 20 mg/kg and 30 min after injection, Imperatorin shows an anxiolytic effect and improved different stages of memory and learning processes-both acquisition and consolidation. It is also shown that acute administration Imperatorin at doses of 10 and 20 mg/kg reduced the anxiogenic effect of nicotine (0.1 mg/kg, subcutaneous, s.c.). At 30 and 40 mg/kg, i.p. Imperatorin significantly potentiates the anticonvulsant activity of carbamazepine against maximal electroshock-induced seizures expressed by lowering the ED
50
from 10.8 to 6.8 mg/kg (by 34 %) and 6 mg/kg (by 42 %), respectively. Moreover, Imperatorin at 30 mg/kg and carbamazepine at 6.8 mg/kg shows increases the total brain concentration of carbamazepine from 1.260 to 2.328 μg/mL (by 85%), which may be caused by modifying the blood-barrier permeability or acting like an inhibitor of multi-drug resistance proteins. Imperatorin, a naturally occurring furanocoumarin, inactivates gamma-aminobutyric acid transaminase and inhibits acetylcholinesterase activity. Imperatorin administered acutely at the doses of 5 and 10 mg/kg prior to the injection of scopolamine (1 mg/kg) improves memory acquisition and consolidation impaired by scopolamine. Furthermore, repeatable (7 days, twice daily) administration of the highest dose of Imperatorin (10 mg/kg) significantly attenuates the effects of scopolamine on memory acquisition, whereas the doses of 5 and 10 mg/kg of this furanocoumarin are effective when memory consolidation is measured .
化学性质
来源于大风子科(Flacourtiaceae) 罗旦梅 Flacourtiajangomas(Lour.)Raeusch茎,
用途
用于含量测定/鉴定/药理实验等。
药理药效:欧前胡素具有抗菌、平喘及抗过敏等作用。
用途
一种存在于柑橘类水果中的糠香豆素,用于HIV-1研究。Imperatorin is a furocoumarin present in citrus fruits, which is used in HIV-1 research. Studies indicate that the transcription factor Sp1 is essential in the inhibitory functions of Imperatorin. In addition, Imperatorin inhibits cyclin D1 expression and stops the cell cycle at G1. These studies also suggest that Imperatorin suppresses HIV-1 replication in primary T lymphocytes and transformed cell lines. Furthermore, it has been suggested that the inhibitory effects of Imperatorin on HIV-1 at the transcriptional level can be monitored effectively in HeLa cells. Imperatorin can also cause apoptosis in human promyelocytic leukaemia, HL-60 via the cytochrome c/caspase-9 pathway.
欧前胡素
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