Ligustilide reduces phenylephrine induced-aortic tension in vitro but has no effect on systolic pressure in spontaneously hypertensive rats.
Radix Angelica sinensis, known as Danggui in Chinese, has been used to treat cardiovascular diseases in traditional Chinese medicine for a long time. Experimental evidence showed that the essential oil of Danggui could reduce blood pressure in rabbits, cats or hypertensive dogs when given intravenously. In this study, we investigated the effects of Z-ligustilide, the main lipophilic component of the essential oil of Danggui on aortic tension induced by phenylephrine, an alpha-adrenergic agonist, in vitro and the systolic blood pressure in SHR rats. We demonstrated for the first time that ligustilide can significantly reduce the phenylephrine-induced aortic tension in vitro with IC(50) about 64 mug/ml, but has no in vivo effect on systolic blood pressure in SHR rats when administrated orally. The data on transport of ligustilide across Caco-2 monolayer suggested an efficient intestinal absorption of ligustilide in vivo, implying that the non-effectiveness of ligustilide in vivo is not due to the poor absorption in the gastrointestinal tract. Further studies on whether ligustilide is one of the main anti-hypertensive components of the essential oil are needed.
Du
Jun-Rong
JR
Laboratory of Iron Metabolism, Department of Applied Biology and Chemical Technology and National Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Hong Kong Polytechnic University, Kowloon, Hong Kong.
Yu
Yan
Y
Yao
Yao
Y
Bai
Bo
B
Zong
Xu
X
Lei
Yang
Y
Wang
Cheng-Yuan
CY
Qian
Zhong-Ming
ZM
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000494:pharmacology; D000284:Administration, Oral; D000316:Adrenergic alpha-Agonists / Q000009:adverse effects; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects*; D001692:Biological Transport; D018938:Caco-2 Cells; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D006801:Humans; D006973:Hypertension / Q000503:physiopathology; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D010656:Phenylephrine / Q000009:adverse effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013599:Systole / Q000502:physiology
D000316:Adrenergic alpha-Agonists; D004365:Drugs, Chinese Herbal; D010656:Phenylephrine; C027820:ligustilide; D015107:4-Butyrolactone