Comparative pharmacokinetics of a marker compound, baicalin in KOB extract after oral administration to normal and allergic-induced rats

Baek, Jong-Suep; Hwang, Chan-Ju; Jung, Hyo-Won; Park, Yong‐Ki; Kim, Young Ho; Kang, Jong Seong; Cho, Cheong-Weon

doi:10.3109/10717544.2013.876561

Cited by 12 publications

(5 citation statements)

References 21 publications

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“…In contrast, no pharmacokinetic changes of baicalin were observed in allergy-induced rats [28]. After an oral administration with 1667 mg/kg KOB extract which is a polyherbal medicine for the treatment of hyperhidrosis, containing 100 mg/kg baicalin, to normal and allergy-induced rats, the obtained pharmacokinetic parameters, such as C max and AUC of baicalin, in allergy-induced rats were similar with those in normal rats [28].…”

Section: Role Of Intestinal Microbiota In Pharmacokinetics Of Baicmentioning

confidence: 99%

Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics

et al. 2016

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Since many glycoside compounds in natural products are hydrolyzed by intestinal microbiota when administered orally, it is of interest to know whether their pharmacological effects are derived from the glycoside itself or from the aglycone form in vivo. An interesting example is baicalin versus baicalein, the aglycone of baicalin, which is contained in some herbs from Labiatae including Scutellaria baicalensis Georgi and Scutellaria lateriflora Linne. The herbs have been extensively used for treatment of inflammatory diseases in Asia. Although there have been numerous reports regarding the pharmacological effects of baicalin and baicalein in vivo and in vitro, some reports indicated that the glycoside form would hardly be absorbed in the intestine and that it should be hydrolyzed to baicalein in advance for absorption. Therefore, the role of metabolism by intestinal microbiota should also be considered in the metabolism of baicalin. In addition, baicalin contains a glucuronide moiety in its structure, by which baicalin and baicalein show complex pharmacokinetic behaviors, due to the interconversion between them by phase II enzymes in the body. Recently, concerns about drug interaction with baicalin and/or baicalein have been raised, because of the co-administration of Scutellaria species with certain drugs. Herein, we reviewed the role of intestinal microbiota in pharmacokinetic characteristics of baicalin and baicalein, with regards to their pharmacological and toxicological effects.

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Section: Role Of Intestinal Microbiota In Pharmacokinetics Of Baicmentioning

confidence: 99%

Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics

et al. 2016

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“…Baicalin is principally used in Asian countries as a herbal supplement because of its wide variety of health benefits, including anti-neuroinflammatory 3 , anti-cancer 4 and anti-anxiety effects 5 . It can also improve lung function 6 and fertility 7 .The most common mechanism of Baicalin being against pathogenesis is its protective effect by reducing the production of oxidative stress 8 . Interestingly, Qi et al 9 reported that Baicalin could enhance the developmental competence of mouse embryos through suppressing cellular apoptosis and HSP70 expression, and activating DNA methylation.…”

Section: Introductionmentioning

confidence: 99%

Baicalin administration attenuates hyperglycemia-induced malformation of cardiovascular system

et al. 2018

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In this study, the effects of Baicalin on the hyperglycemia-induced cardiovascular malformation during embryo development were investigated. Using early chick embryos, an optimal concentration of Baicalin (6 μM) was identified which could prevent hyperglycemia-induced cardiovascular malformation of embryos. Hyperglycemia-enhanced cell apoptosis was reduced in embryos and HUVECs in the presence of Baicalin. Hyperglycemia-induced excessive ROS production was inhibited when Baicalin was administered. Analyses of SOD, GSH-Px, MQAE and GABAA suggested Baicalin plays an antioxidant role in chick embryos possibly through suppression of outwardly rectifying Cl(−) in the high-glucose microenvironment. In addition, hyperglycemia-enhanced autophagy fell in the presence of Baicalin, through affecting the ubiquitin of p62 and accelerating autophagy flux. Both Baicalin and Vitamin C could decrease apoptosis, but CQ did not, suggesting autophagy to be a protective function on the cell survival. In mice, Baicalin reduced the elevated blood glucose level caused by streptozotocin (STZ). Taken together, these data suggest that hyperglycemia-induced embryonic cardiovascular malformation can be attenuated by Baicalin administration through suppressing the excessive production of ROS and autophagy. Baicalin could be a potential candidate drug for women suffering from gestational diabetes mellitus.

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“…The absorption and bioavailability of baicalin from herbal extracts was shown to be higher in rats with ulcerative colitis than in otherwise healthy rats [167,190]. In experimentally allergic rats, though, no differences were seen in the pharmacokinetics of baicalin when compared with normal controls [279].…”

Section: Intra-species Differences (Pk Variability)mentioning

confidence: 99%

Pharmacokinetics of B-Ring Unsubstituted Flavones

et al. 2019

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B-ring unsubstituted flavones (of which the most widely known are chrysin, baicalein, wogonin, and oroxylin A) are 2-phenylchromen-4-one molecules of which the B-ring is devoid of any hydroxy, methoxy, or other substituent. They may be found naturally in a number of herbal products used for therapeutic purposes, and several have been designed by researchers and obtained in the laboratory. They have generated interest in the scientific community for their potential use in a variety of pathologies, and understanding their pharmacokinetics is important for a grasp of their optimal use. Based on a comprehensive survey of the relevant literature, this paper examines their absorption (with deglycosylation as a preliminary step) and their fate in the body, from metabolism to excretion. Differences among species (inter-individual) and within the same species (intra-individual) variability have been examined based on the available data, and finally, knowledge gaps and directions of future research are discussed.

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Comparative pharmacokinetics of a marker compound, baicalin in KOB extract after oral administration to normal and allergic-induced rats

Cited by 12 publications

References 21 publications

Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics

Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics

Baicalin administration attenuates hyperglycemia-induced malformation of cardiovascular system

Pharmacokinetics of B-Ring Unsubstituted Flavones

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