Studies on Scutellariae Radix. VII. Anti-arthritic and anti-inflammatory actions of methanolic extract and flavonoid components from Scutellariae Radix.

Kubo, Michinori; Matsuda, Hideaki; Tanaka, Motoharu; Kimura, Yoshiyuki; Okuda, Hiromichi; Higashino, Masayuki; Tani, Tohru; Namba, Kei; Arichi, Shigeru

doi:10.1248/cpb.32.2724

Cited by 137 publications

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“…15 There is a correlation between the in vivo antiinflammatory activity and the in vitro antioxidative activities of baicalein. 11 In a previous study, baicalein was found to attenuate glutamate neurotoxicity through the 12/15-lipoxygenase pathway in the ischemic brain.…”

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confidence: 99%

Attenuation of neurological injury with early baicalein treatment following subarachnoid hemorrhage in rats

Kuo¹,

Chen³

et al. 2013

JNS

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ObjectBaicalein has been shown to offer neuroprotection in the ischemic brain, but its effect in subarachnoid hemorrhage (SAH) is unknown. The authors used a double-hemorrhage model to study the role of early baicalein treatment in SAH.MethodsSubarachnoid hemorrhage was induced in male Wistar rats through a repeat injection of autologous blood at a 48-hour interval. Rats subjected or not subjected to SAH received a 30-mg/kg baicalein injection 3 hours after SAH and daily for 6 consecutive days, and results were compared with those obtained in vehicle-treated control rats. Mortality of the rats was recorded. Neurological outcome was assessed daily. Cerebrospinal fluid dialysates were collected and examined for glutamate concentrations. Cerebral vasospasm (CVS), brain water content, neuron variability, expression of glutamate transporter–1 (GLT-1), immunoreactivity of astrocyte, and level of malondialdehyde, activities of superoxide dismutase (SOD), and catalase in brain tissues content were determined on post-SAH Day 7.ResultsMortality rate, neuronal degeneration, brain water content, and CVS were decreased and neurological function improved in the baicalein-treated rats. Baicalein increased astrocyte activity and preserved GLT-1, which attenuated the glutamate surge after SAH. Baicalein also provided antioxidative stress by preserving activities of SOD and catalase and decreased malondialdehydelevel after SAH. The glutamate, body weight, neurological scores, and glial fibrillary acidic protein activity were significantly correlated. The CVS was correlated with neuronal degeneration, and GLT-1 was correlated with oxidative stress.ConclusionsEarly baicalein treatment attenuated CVS and limited neurological injury following SAH. These data may indicate clinical utility for baicalein as an adjunct therapy to reduce brain injury and improve patient outcomes.

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confidence: 99%

Attenuation of neurological injury with early baicalein treatment following subarachnoid hemorrhage in rats

Kuo¹,

Chen³

et al. 2013

JNS

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“…In addition, HPLC/MS/MS analyses identified the unknown peak in the plasma extract with a retention time of 5.1 min as B6G by comparing its HPLC/MS (Fig. 2) 2 . Plasma B6G and BG after Oral Administration of BG or B After oral administration of BG to rats, it was detected in their plasma as described previously, 13) and B6G was also detected at higher concentrations than BG (Fig.…”

Section: Identification Of B6g As the Main Plasma Metabolitementioning

confidence: 99%

Baicalein 6-<i>O</i>-β-d-Glucopyranuronoside Is a Main Metabolite in the Plasma after Oral Administration of Baicalin, a Flavone Glucuronide of Scutellariae Radix, to Rats

Akao¹,

Sato²,

He³

et al. 2013

Biological & Pharmaceutical Bulletin

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Baicalin (BG) and its aglycone, baicalein (B) are strong antioxidants that exert various pharmacological actions and show unique metabolic fates in the rat. The aim of the present study was to identify major metabolite(s) besides BG in rat plasma after oral administration of BG or B. The main metabolite was detected by HPLC equipped with an electrochemical detector at a potential of +500 mV and identified as baicalein 6-O-β-d-glucopyranuronoside (B6G) by HPLC/MS/MS. When BG at a dose of 20 mg/kg was administered orally to Wistar rats, the level of B6G in plasma was higher than that of BG. C max and the area under the concentration-curve from 0 to 24 h (AUC 0-24 h ) values of the plasma B6G were 1.66±0.34 µm and 19.8±3.9 µm·h, respectively, whereas those of BG were 0.853±0.065 µm and 10.0±3.1 µm·h, respectively. When B was administered, similar results were also obtained. B6G-producing activities from B were found in microsomes of both rat jejunum and liver, in spite of the low activity. Rat everted jejunal sacs formed B6G after application of B, but only in a small amount that was excreted into the mucosal side, and not the serosal side, indicating little contribution to the appearance of B6G in plasma. On the other hand, when B was injected into the rat portal vein, B6G was detected at a higher level than BG in the systemic circulation, demonstrating the hepatic contribution to the appearance of plasma B6G.Key words baicalin; baicalein 6-O-β-d-glucopyranuronoside; metabolite; rat Scutellariae Radix, the root of Scutellaria baicalensis GeorGi (Labiatae), is used in combination with other herbs in Chinese traditional (Kampo, in Japanese) medicines, and contains baicalin (BG, 5,6,7-trihydroxyflavone-7-β-d-glucuronide; Fig. 1) as its main active constituent. BG and its aglycone, baicalein (B), have wide-ranging pharmacological effects, such as antiallergic, 1) anti-inflammatory, 2) antiviral, 3,4) antiproliferative, 5) and antitumor 6) effects, and also show strong antioxidant activity. 7,8) In addition, they inhibit prostaglandin E2 production, and prevent the gene expression of inducible nitric oxide synthase and cyclooxygenase-2. 9) B also has an anxiolytic-like effect 10) and a protective effect against amnesia. 11)BG has been detected in rat plasma after its oral administration, 12) suggesting that it is absorbed directly from the gastrointestinal tract. However, in our previous study when BG was given to germ-free rats, only a small amount of BG was detected in their plasma. In addition, BG, and not B, has been detected even after oral administration of B to rats. 13) On the other hand, many kinds of metabolites such as B-glucuronides and B-sulfates besides BG have been found in bile after oral administration of either BG or B to rats.14) Many kinds of B-metabolites have also been detected in bile and urine after oral administration of Scutellariae Radix extract or Chinese traditional medicines that include Scutellariae Radix. 15) In addition, unidentified metabolites besides BG in rat plasma have been found ...

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“…Scutellaria baicalensis, known as Chinese skullcap and Huang Qin, contains several flavonoids and is a widely used herb in traditional Chinese medicine with antitumor, antiviral, antibacterial and anti-inflammatory properties (7)(8)(9)(10)(11). Baicalein and wogonin are flavonoid-like chemical compounds which are found in Scutellaria baicalensis and have been reported to inhibit cell growth and induce apoptosis in various tumors (12,13).…”

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confidence: 99%

Antitumor actions of baicalein and wogonin in HT-29 human colorectal cancer cells

Kim

et al. 2012

Molecular Medicine Reports

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Abstract. The purpose of this study was to determine the effects of baicalein and wogonin, which are compounds derived from the Chinese herb Scutellaria baicalensis, in suppressing the viability of HT-29 human colon cancer cells. Following treatment with baicalein or wogonin, several apoptotic events were observed, including DNA fragmentation, chromatin condensation and increased cell cycle arrest in the G1 phase. Baicalein and wogonin decreased Bcl-2 expression, whereas the expression of Bax was increased in a dose-dependent manner compared with the control. Furthermore, the induction of apoptosis was accompanied by an inactivation of phosphatidylinositol 3-kinase (PI3K)/Akt in a dose-dependent manner. The administration of baicalein to mice resulted in the inhibition of the growth of HT-29 xenografts without any toxicity following 5 weeks of treatment. The results indicated that baicalein induced apoptosis via Akt activation in a p53-dependent manner in the HT-29 colon cancer cells and that it may serve as a chemopreventive or therapeutic agent for HT-29 colon cancer.

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Studies on Scutellariae Radix. VII. Anti-arthritic and anti-inflammatory actions of methanolic extract and flavonoid components from Scutellariae Radix.

Cited by 137 publications

References 0 publications

Attenuation of neurological injury with early baicalein treatment following subarachnoid hemorrhage in rats

Attenuation of neurological injury with early baicalein treatment following subarachnoid hemorrhage in rats

Baicalein 6-<i>O</i>-β-d-Glucopyranuronoside Is a Main Metabolite in the Plasma after Oral Administration of Baicalin, a Flavone Glucuronide of Scutellariae Radix, to Rats

Antitumor actions of baicalein and wogonin in HT-29 human colorectal cancer cells

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