The health benefits of
Osthole
Feb 2009
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Osthole is an active constituent isolated from the fruit of Cnidium monnieri (L.) Cusson, a
Chinese herbal medicine, which has been used to treat anti-inflammation, anti-osteoporosis
and anti-tumor for many years. Recently, researchers from Medical School of Soochow
University, China, found that 4-week-supplementation of osthole could inhibit alcohol or high
fat-induced fatty liver in mice, probably associated with its anti-oxidation and suppression of
TNF-alpha production. [1-4]

Anti-inflammatory Action

Researchers from Gannan Medical College, China, found that osthole suppressed
inflammatory responses on nitric oxide levels in a dose-dependent manner in a study of rats.
The mechanism is related to inhibition of calcium entry and elevating cGMP levels way. [5]

Osthole may benefit people suffered from some chronic conditions.

Osthole exhibited a significant induction of differentiation in two human osteoblast-like cell
lines-MG-63 and hFOB. Researchers from Chia-Nan University of Pharmacy and Science,
Taiwan, claimed that osthole may benefit people suffered from osteoporosis. [6] In a study of
ovariectomized rats, osthole was as effective as 17beta-estradiol to suppress bone loss
due to ovariectomy but the researchers were not sure how osthole suppress bone loss. [8]

Because of its unique structure, the location of a butenyl group at position-8, researchers
from Nippon Chemiphar Co., Ltd, believe s osthole is a good candidate l for liver cancer
(hepatocellular carcinomas) [7]

Osthole may benefit people at risk of hypertension.

Osthole causes hypotension in vivo or lowers the blood pressure of animals, and inhibits
platelet aggregation and smooth muscle contraction in vitro. Researchers noted that the
mechanism might work via interfering the calcium influx and cyclic nucleotide
phosphodiesterases. [9]

In 1991, osthole was already known as antiplatelet agent. Thirty min after
intraperitoneal (i.p.) administration of osthole, tail bleeding time of mice was prolonged
markedly in a dose-dependent manner. [13]

Researchers from National Taiwan University noticed osthole inhibited norepinephrine
-induced phasic and tonic contractions in rat thoracic aorta in a concentration-dependent
manner. They further found that osthole relaxed rat thoracic aorta by virtue of its
Ca(2+)-channel blocking properties and by elevating cGMP levels in vascular smooth
muscle. [10]

This research group also found that osthole suppressed the contraction response curves of
tracheal smooth muscle of guinea-pig caused by carbachol, calcium chloride or other
agents in a concentration-dependent manner. Again, osthole inhibited the activity of cAMP
and cGMP phosphodiesterases in a concentration-dependent manner. They concluded that
osthole exerts a non-specific relaxant effect on the trachealis by inhibiting the cAMP and
cGMP phosphodiesterases. [11]

Researchers from Xian Medical University confirmed their findings by comparing the effects
of osthole and verapamil on the isolated guinea-pig ileum and taeniae coli. Both inhibited
the contractions induced by acetylcholine (ACh), histamine (His) and KCl in a
dose-dependent manner. [12]

Reference:

[1] Sun F, Xie ML, Zhu LJ, Xue J, Gu ZL. Inhibitory effect of osthole on alcohol-induced fatty liver in mice. Dig Liver Dis. 2009
Feb;41(2):127-33. Epub 2008 Mar 12. [2] Zhang Y, Xie ML, Xue J, Gu ZL. Osthole regulates enzyme protein expression of CYP7A1
and DGAT2 via activation of PPARalpha/gamma in fat milk-induced fatty liver rats. J Asian Nat Prod Res. 2008
Jul-Aug;10(7-8):807-12. [3] Zhang Y, Xie ML, Zhu LJ, Gu ZL. Therapeutic effect of osthole on hyperlipidemic fatty liver in rats. Acta
Pharmacol Sin. 2007 Mar;28(3):398-403. [4] Song F, Xie ML, Zhu LJ, Zhang KP, Xue J, Gu ZL. Experimental study of osthole on
treatment of hyperlipidemic and alcoholic fatty liver in animals. World J Gastroenterol. 2006 Jul 21;12(27):4359-63. [5] Liu J, Zhang
W, Zhou L, Wang X, Lian Q. Anti-inflammatory effect and mechanism of osthole in rats. Zhong Yao Cai. 2005 Nov;28(11):1002-6. [6]
Kuo PL, Hsu YL, Chang CH, Chang JK. Osthole-mediated cell differentiation through bone morphogenetic protein-2/p38 and
extracellular signal-regulated kinase 1/2 pathway in human osteoblast cells. J Pharmacol Exp Ther. 2005 Sep;314(3):1290-9. Epub
2005 Jun 13. [7] Okamoto T, Kobayashi T, Yoshida S. Chemical aspects of coumarin compounds for the prevention of hepatocellular
carcinomas. Curr Med Chem Anticancer Agents. 2005 Jan;5(1):47-51. [8] Li XX, Hara I, Matsumiya T. Effects of osthole on
postmenopausal osteoporosis using ovariectomized rats; comparison to the effects of estradiol. Biol Pharm Bull. 2002
Jun;25(6):738-42. [9] Hoult JR, Payá M. Pharmacological and biochemical actions of simple coumarins: natural products with
therapeutic potential. Gen Pharmacol. 1996 Jun;27(4):713-22. [10] Ko FN, Wu TS, Liou MJ, Huang TF, Teng CM. Vasorelaxation of
rat thoracic aorta caused by osthole isolated from Angelica pubescens. Eur J Pharmacol. 1992 Aug 14;219(1):29-34. [11] Teng CM,
Lin CH, Ko FN, Wu TS, Huang TF. The relaxant action of osthole isolated from Angelica pubescens in guinea-pig trachea. Naunyn
Schmiedebergs Arch Pharmacol. 1994 Feb;349(2):202-8. [12] Institute of Clinical Pharmacology, Xian Medical University. Effects of
osthole on the isolated guinea-pig ileum and taeniae coli Yao Xue Xue Bao. 1993;28(12):899-904. [13] Teng CM, Ko FN, Wang JP,
Lin CN, Wu TS, Chen CC, Huang TF. Antihaemostatic and antithrombotic effect of some antiplatelet agents isolated from Chinese
herbs. J Pharm Pharmacol. 1991 Sep;43(9):667-9.