Biological Properties of Baicalein in Cardiovascular System

Abstract

The dried roots of Scutellaria baicalensis (S. baicalensis) Georgi (common name: Huangqin in China) have been widely employed for many centuries in traditional Chinese herbal medicine as popular antibacterial and antiviral agents. They are effective against staphylococci, cholera, dysentery, pneumococci and influenza virus. Baicalein, one of the major flavonoids contained in the dried roots, possesses a multitude of pharmacological activities. The glycoside of baicalein, baicalin is a potent anti-inflammatory and anti-tumor agent. This review describes the biological properties of baicalein (Table 1), which are associated with the prevention and treatment of cardiovascular diseases. Baicalein is a potent free radical scavenger and xanthine oxidase inhibitor, thus improving endothelial function and conferring cardiovascular protective actions against oxidative stress-induced cell injury. Baicalein lowers blood pressure in renin-dependent hypertension and the in vivo hypotensive effect may be partly attributed to its inhibition of lipoxygenase, resulting in reduced biosynthesis and release of arachidonic acid-derived vasoconstrictor products. On the other hand, baicalein enhances vasoconstricting sensitivity to receptor-dependent agonists such as noradrenaline, phenylephrine, serotonin, U46619 and vasopressin in isolated rat arteries. The in vitro effect is likely caused by inhibition of an endothelial nitric oxide-dependent mechanism. The anti-thrombotic, anti-proliferative and anti-mitogenic effects of the roots of S. baicalensis and baicalein are also reported. Baicalein inhibits thrombin-induced production of plasminogen activator inhibitor-1, and interleukin-1beta- and tumor necrosis factor-alpha-induced adhesion molecule expression in cultured human umbilical vein endothelial cells. The pharmacological findings have highlighted the therapeutic potentials of using plant-derived baicalein and its analogs for the treatment of arteriosclerosis and hypertension.

Screening for novel quorum-sensing inhibitors to interfere with the formation of Pseudomonas aeruginosa biofilm

“…Anti-QS activity has also been noted in a number of traditional medicinal plants (Adonizio et al, 2006). Rhubarb (named Dahuang in Chinese), a medicinal plant, displays diverse pharmacological activities such as bacteriostatic, antiviral, antifungal and antitumour activities (Huang & Zhen, 2001;Kim et al, 2004;Basu et al, 2005;Huang et al, 2005). Emodin, one of the free anthraquinone compounds extracted from rhubarb, is the major active constituent (Ma et al, 2008) that inhibits the expression of the tumour necrosis factor alpha (TNF-a) gene and tumour metastasis in vitro and in vivo (Kwak et al, 2006).…”

Inhibitory activities of baicalin against renin and angiotensin-converting enzyme

“…However, in 2003, a nonpeptide small molecule compound, aliskiren (IC 50 = 0.6 nM), with highly inhibitory activity against renin, was discovered via molecular design and pioneered a new field for studying renin inhibitors Wood et al, 2003). Despite the great devotions to renin inhibitors, little attention has been paid to natural products, especially the compounds used in traditional Chinese medicine such as baicalin and baicalien (Huang et al, 2005) isolated from Scutellaria baicalensis Georgi, a traditional Chinese medicine (China Pharmacopoeia Committee, 2010). This work aims at the renin and ACE inhibitory activities of baicalin (7-glucuronic acid-5,6-dihydroxylflavone, C21H18O11, MW: 446.38), which is the quality control marker of this herb.…”

Wogonin ameliorates lipotoxicity-induced apoptosis of cultured vascular smooth muscle cells via interfering with DAG-PKC pathway

“…Therefore, antiapoptotic therapies for VSMCs may benefit the prevention and treatment of atherosclerosis [8,10] . Scutellaria baicalensis Georgi (S baicalensis) is a traditional Chinese herb (Baikal Skullcap) that is widely used for the treatment of inflammation, infection, cancer, hypertension, and cardiovascular disease [13,14] . Wogonin (5,7-dihydroxy-8-methoxyflavone) is a major bioactive component of the flavonoids from S baicalensis.…”