Amount Of Baicalin Research Articles

An analysis of the ingredients in decoctions and extracts of Kampo medicines: Amounts of baicalin and baicalein in Kampo medicines containing Scutellariae Radix

Kampo medicines containing Scutellariae Radix (the root of Scutellaria baicalensis Georgi; SR) sometimes cause serious adverse effects, including interstitial pneumonia and liver dysfunction. Baicalin (BL) is the major active component of SR and is presumed to be responsible for the adverse effects. We analyzed the amounts of BL in Kampo medicines to better understand how they can be used safely. We determined the amounts of BL in 28 Kampo decoctions containing SR (recommended daily dose: 1.5-4 g/day) and corresponding Kampo extract products by high-performance liquid chromatography. The amounts of BL in the Kampo decoctions were 1.7-4.0-fold higher than those of the corresponding Kampo extract products. Inter-product variations in the amounts of BL in Shosaikoto, Otsujito, Daisaikoto, Saibokuto, Orengedokuto, and Saireito Kampo extracts from various companies were also examined. Significant differences in the amounts of BL were observed for Shosaikoto, Otsujito, Daisaikoto, and Saibokuto extract products (up to 2.6, 1.6, 1.5, and 1.3-fold differences, respectively), whereas no significant differences were observed for Orengedokuto and Saireito extract products. Because the Kampo decoctions containing SR that we examined contained 1.7-4.0 times as much BL as the corresponding Kampo extract products, medical doctors and pharmacists should be aware that Kampo decoctions containing SR might cause more severe side effects than corresponding Kampo extract products. Furthermore, we recommend that the amounts of BL and its aglycone, baicalein (BA), in Kampo extract products be made known to practitioners and patients.

Flavonoids are identified from the extract of Scutellariae Radix to suppress inflammatory-induced angiogenic responses in cultured RAW 264.7 macrophages

Scutellariae Radix (SR), also named Huangqin in China, is the dried root of Scutellaria baicalensis Georgi. Historically, the usage of SR was targeted to against inflammation. In fact, chronic inflammation has a close relationship with hypoxia and abnormal angiogenesis in tumor cells. Hence, we would like to probe the water extract of SR in suppressing the inflammation-induced angiogenesis. Prior to determine the pharmaceutical values of SR, the first step is to analysis the chemical compositions of SR according to China Pharmacopeia (2015). From the results, the amount of baicalin was 12.6% by weight. Furthermore, the anti-angiogenic properties of SR water extract were evaluated in lipopolysaccharide (LPS) pre-treated cultured macrophage RAW 264.7 cells by detecting the inflammatory markers, i.e. Cox-2, cytokine and iNOS, as well as the translocation activity of NFκB and angiogenic biomarker, i.e. VEGF. This herbal extract was capable of declining both inflammatory and angiogenic hallmarks in a concentration-dependent manner. Moreover, the SR-derived flavonoids, i.e. baicalin, baicalein, wogonin and wogonoside, were shown to be active chemicals in the anti-inflammatory-induced angiogenesis. Therefore, the inflammation-induced angiogenesis is believed to be suppressed by SR water extract, or its major ingredients. These results shed light in the benefiting role of SR in the inflammation-induced angiogenesis in vitro.

Influence of Coptis Chinensis on pharmacokinetics of flavonoids after oral administration of Radix Scutellariae in rats

Radix Scutellariae (RS) and Coptis Chinensis (CC) are the most popular components in traditional Chinese medicine prescriptions. Flavonoids are the main effective ingredients in RS and berberine is the main effective ingredient in CC. The aim of this study was to determine the influence of CC on the pharmacokinetics of flavonoids following the administration of RS in rats and to investigate the effects of CC on the pharmacokinetic mechanism. Rats were administered RS or RS+CC by intragastric gavage (i.g.). Plasma concentrations of baicalin (baicalein 7-glucuronide) and wogonoside (wogonin 7-glucuronide) were measured by HPLC. Pharmacokinetic parameters were calculated from the plasma concentration time curve. The effect of CC on the metabolism of flavonoids in RS by rat intestinal flora was studied using rat fecal suspensions after ig administration of CC. The effect of berberine on the bi-directional transport of baicalein and baicalin was studied in Caco-2 monolayer models. The effect of CC on the metabolism of baicalein and baicalin by the liver was studied using rat liver microsomes after i.g. administration of CC. Compared to RS alone, RS+CC decreased AUC and C(max) of baicalin and wogonoside. CC decreased the hydrolyzation of baicalin and wogonoside by intestinal flora. Berberine decreased the amount of baicalein transported to the basolateral side and the amount of baicalin which appeared at the basolateral side. The results showed that CC may decrease the bioavailability of baicalin and wogonoside in RS and the mechanism was related to CC decreasing the transport of flavonoid aglycones from the mucosa side to the serosal side and the hydrolyzation of flavonoids by inhibiting intestinal flora.

Supercritical fluid extraction of flavonoids from Scutellariae Radix

An optimal condition of supercritical fluid extraction (SFE) for flavonoids of Scutellaria baicalensis was developed. In this study, various temperatures, pressures and modifiers were studied. The conventional extraction methods were conducted in parallel for comparison. The crude extracts were qualitatively compared by TLC and GC–MS, and the contents of flavonoids were determined by HPLC. The amounts of baicalin, baicalein and wogonin in the Scutellariae Radix obtained by supercritical fluid extraction and a conventional sonic shaking method were 137.6 mg/g, 8.6 mg/g and 2.2 mg/g, 113.5 mg/g, 5.7 mg/g and 2.3 mg/g, respectively. Application of SFE for extraction of the flavonoids from Scutellariae Radix was preferable. The optimal conditions of SFE was as follows: supercritical carbon dioxide–MeOH–water (20:2.1:0.9), 50°C and 200 bar.