Comparative pharmacokinetics of baicalin after oral administration of pure baicalin, Radix scutellariae extract and Huang-Lian-Jie-Du-Tang to rats

Tong, L.; Song, Jue; Huang, Fang; Deng, Yejun; Xie, Lin; Wang, Guangji; Liu, Xiaodong

doi:10.1016/j.jep.2006.09.036

Cited by 158 publications

(129 citation statements)

References 26 publications

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“…Schisandra lignans are the major constituents of Schisandra chinensis and more than 40 of them have been isolated, in which the most abundant ingredients include schisandrin, lignans, deoxyschizandrin etc. Several papers focused on how the individual component in the compound prescription interact with other ingredients (Zuo et al, 2003;Bochu et al, 2005;Di et al, 2006;Lu et al, 2007). Schisandra lignans have been shown to have various biological activities, they are usually considered as the main pharmacological effective compounds (Hancke et al, 1999), such as hepatoprotective effect, potent antioxidative property, anticarcinogenic activity through the activation of key liver enzymes and strong inhibitory effect on human immunodeficiency virus reported recently.…”

Section: Introductionmentioning

confidence: 99%

Influence of Supercritical CO<sub>2</sub> Extraction of Schisandra Chinensis on Antioxidant Status, Carcass and Meat Quality of AA Broilers

et al. 2013

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The experiment was conducted to investigate the effect of dietary supplementation with different level of supercritical CO 2 extraction of Schisandra Chinensis (SCESC) (0.1%, 0.2%, and 0.4%) on antioxidant status and meat quality of broilers. The results showed that the total superoxide dismutase (T-SOD) activity in heart and liver was increased significantly by supplementing with SCESC in the diet of birds, the malonaldehyde (MDA) concentration in heart of birds was lower in the SCESC group than the control, and the glutathion reductase (GR) activity in liver and kidney of the birds was increased significantly. There was a significant reduction of the abdominal fat in the experimental group. The drip loss of breast meat was significantly decreased through supplementing with SCESC in the diet of birds. The pH was higher in the 0.1% SCESC group than the control. The shear force of breast meat from broilers was decreased by 0.2% SCESC supplementation. Compared to the control, the content of crude fat of breast meat from broilers was increased significantly. At the same time, diets supplemented with 0.2% SCESC increased the crude protein content of breast meats. Furthermore, diets supplemented with 0.4% SCESC had an increased Inosinic Acid (IMP) content significantly. On the basis of these observations, we concluded that diets supplemented with SCESC improved antioxidant enzyme activity of tissues and improved meat tenderness and nutritional value of breast and thigh meat.

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Section: Introductionmentioning

confidence: 99%

Influence of Supercritical CO<sub>2</sub> Extraction of Schisandra Chinensis on Antioxidant Status, Carcass and Meat Quality of AA Broilers

et al. 2013

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“…It is generally assumed that baicalin is poorly absorbed from the gastrointestinal tract in its native form and must be hydrolyzed by intestinal microflora in the intestine to their aglycones in human and rats [11,12] . The metabolite, baicalein, is subsequently conjugated to baicalin, baicalein 6-O-β-glucuronide-7-O-sulfate and baicalein 6,7-diglucuronide in the gut mucosae, liver, and blood [13][14][15][16][17] . Akao et al suggested that baicalin might be hydrolyzed to baicalein by intestinal bacteria, absorbed into the blood and conjugated with glucuronic acid and/or sulfuric acid [11] .…”

Section: Introductionmentioning

confidence: 99%

Anti-pruritic effect of baicalin and its metabolites, baicalein and oroxylin A, in mice

et al. 2010

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Aim: To explore whether intestinal microflora plays a role in anti-pruritic activity of baicalin, a main constituent of the rhizome of Scutellaria baicalensis (SB). Methods: Baicalin was anaerobically incubated with human fecal microflora, and its metabolites, baicalein and oroxylin A, were isolated. The inhibitory effect of baicalin and its metabolites was accessed in histamine-or compound 48/80-induced scratching behavior in mice. Results: Baicalin was metabolized to baicalein and oroxylin A, with metabolic activities of 40.2±26.2 and 1.2±1.1 nmol·h -1 ·mg -1 wet weight of human fecal microflora, respectively. Baicalin (20, 50 mg/kg) showed more potent inhibitory effect on histamine-induced scratching behavior when orally administered than intraperitoneally. In contrast, baicalein and oroxylin A had more potent inhibitory effect when the intraperitoneally administered. The anti-scratching behavior activity of oral baicalin and its metabolites was in proportion to their inhibition on histamine-induced increase of vascular permeability with oroxylin A more potent than baicalein and baicalin. In Magnus test using guinea pig ileum, oroxylin A is more potent than baicalein and baicalin in inhibition of histamine-induced contraction. The anti-scratching behavioral effect of oral baicalin was significantly reduced when oral antibiotics were simultaneously administered, whereas the effect of baicalein and oroxylin A were not affected. Conclusion: Oral baicalin may be metabolized by intestinal microflora into baicalein and oroxylin A, which ameliorate pruritic reactions through anti-histamine action.

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“…Recent studies have shown that pharmacological activities may differ between the isolated components and the total extracts [2,3] , indicating that the interactions among these known and unknown components may play an essential role in the activity of the prescription as a whole. These differences in biological activities are also generally reflected in the pharmacokinetic behaviors of these ingredients [4][5][6][7] . For example, baicalin in Huang-Lian-Jie-Du-Tang influenced the pharmacokinetic behavior of wogonoside [5] .…”

Section: Introductionmentioning

confidence: 99%

“…These differences in biological activities are also generally reflected in the pharmacokinetic behaviors of these ingredients [4][5][6][7] . For example, baicalin in Huang-Lian-Jie-Du-Tang influenced the pharmacokinetic behavior of wogonoside [5] .…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic interactions induced by content variation of major water-soluble components of Danshen preparation in rats

et al. 2010

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Aim: To investigate the pharmacokinetic interactions induced by content variation of the main water-soluble components of Danshen injection in rats. Methods: Intravenous Danshen injection (control) or Danshen injection with danshensu (DSS), protocatechuic aldehyde (PAL), salvianolic acid A (Sal A) or salvianolic acid B (Sal B) were administered to female Sprague Dawley rats . Plasma concentrations of DSS, Sal A, PAL and its oxidative metabolite protocatechuic acid (PA) were analyzed simultaneously with LC-MS/MS; concentrations of Sal B were determined by the LC-MS method. Non-compartmental pharmacokinetic parameters were calculated and compared for identifying the pharmacokinetic interactions among these components. Results: Compared with the control group, the DSS, Sal A, and Sal B groups had significant increases in AUC 0-∞ in response to elevated concentrations of PAL ( by 78.1%, 51.0%, and 82.9%, respectively), while the clearances (CL) were markedly reduced (by 42.5%, 32.9%, and 46.8%, respectively). Similarly, Sal A increased the AUC 0-∞ of DSS and Sal B (26.7% and 82.4%, respectively) and substantially decreased their clearances (21.4% and 45.6%, respectively). In addition, the pharmacokinetics of DSS and Sal B were significantly affected by the content variation of the other major components; the AUC 0-∞ increased by 45.1% and 52.1%, respectively, the CL dropped by 29.6% and 27.1%, respectively, and the T 1/2 was decreased by 22.0% and 19.6%, respectively. Conclusion: Complex, extensive pharmacokinetic interactions were observed among the major water-soluble constituents in the Danshen injection. The content variation of PAL had the most significant effect on the pharmacokinetic behaviors of other major constituents. Furthermore, the pharmacokinetics of DSS and Sal B were the most susceptible to the content change of other components.

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Comparative pharmacokinetics of baicalin after oral administration of pure baicalin, Radix scutellariae extract and Huang-Lian-Jie-Du-Tang to rats

Cited by 158 publications

References 26 publications

Influence of Supercritical CO<sub>2</sub> Extraction of Schisandra Chinensis on Antioxidant Status, Carcass and Meat Quality of AA Broilers

Influence of Supercritical CO<sub>2</sub> Extraction of Schisandra Chinensis on Antioxidant Status, Carcass and Meat Quality of AA Broilers

Anti-pruritic effect of baicalin and its metabolites, baicalein and oroxylin A, in mice

Pharmacokinetic interactions induced by content variation of major water-soluble components of Danshen preparation in rats

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