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Scutellaria planipes, a species of Scutellaria, was explored by comparing to Scutellaria baicalensis, a pharmacopoeia species. Four principle flavonoids in both the plant roots were analyzed by using a reversed-phase chromatographic system with a chemically bonded ODS silica gel column and phosphate buffer:methanol (68:32 and 1:1) as mobile phase. Their contents were similar in both plant roots. Antiallergic and antibacterial activities in vitro and acute toxicity were compared. The results provided valuable data for S. planipes as a potential medicinal resource.
From the roots of Scutellaria amabilis HARA, eleven new flavonoids, 5,7,2'-trihydroxy-8-methoxyflavone 7-O-beta-D-glucopyranoside, 5,7,2'-trihydroxy-8-methoxyflavone 2'-O-beta-D-glucopyranoside, 5,7-dihydroxy-8,2'-dimethoxyflavone 7-O-beta-D-glucopyranoside, 5,7,2'-trihydroxyflavone 2'-O-beta-D-glucopyranoside, 5,7,2',5'-tetrahydroxyflavone 7-O-beta-D-glucuronopyranoside, (2S)-5,7,2',5'-tetrahydroxyflavanone, (2S)-5,7,2',5'-tetrahydroxyflavanone 7-O-beta-D-glucopyranoside, (2S)-5,7,2',5'-tetrahydroxyflavanone 7-O-beta-D-glucuronopyranoside, (2S)-7,2'-dihydroxy-5-methoxyflavanone 7-O-beta-D-glucuronopyranoside, (I-2S)-I-5,II-5,I-7,II-7,I-2',II-2',II-5'-heptahydroxy-[I-6,II-6']-flavanonylflavone and (I-2S)-I-5,II-5,I-7,II-7,I-2',II-2',I-5',II-5'-octahydroxy-[I-6,II-6']-flavanonylflavone, were isolated, together with ten known flavonoids, wogonin (5,7-dihydroxy-8-methoxyflavone), 5,7-dihydroxy-8,2'-dimethoxyflavone, (2S)-5,7,2'-trihydroxyflavanone, scutevulin (5,7,2'-trihydroxy-8-methoxyflavone), 5,7,4'-trihydroxy-8-methoxyflavone, alpinetin ((2S)-7-hydroxy-5-methoxyflavanone), 5,7,2'-trihydroxyflavone, 5,7,2',5'-tetrahydroxyflavone, (2S)-7,2'-dihydroxy-5-methoxyflavanone and 5,7-dihydroxy-8,2'-dimethoxyflavone 7-O-beta-D-glucuronopyranoside. The structures were determined on the basis of chemical and spectral data.
From the leaves of Scutellaria alpina L., four new neo-clerodane diterpenes (1-4) were isolated. The structures of 1-4 were shown to be (4S)-19-acetoxy-8 beta-hydroxy-6 alpha-benzoyloxy-4,18-epoxy-neo-cleroda-11,13- dien-15,16-olide, (4S)-19-acetoxy-8 beta-hydroxy-6 alpha-tigloyloxy-4,18-epoxy-neo-cleroda-11,13- dien-15,16-olide, (4S, 11S)-11-acetoxy-8 beta,19-dihydroxy-6 alpha-tigloyloxy-4,18-epoxy-neo- clerod-13-en-15,16-olide, and (4S)-19-acetoxy-8 beta-hydroxy-6 alpha, 7 beta-dibenzoyloxy-4,18-epoxy-neo- cleroda-11,13-dien-15,16-olide, respectively, by the chemical and spectral data.
Recently several procedures have been reported for the simultaneous separation of flavonoid glycosides by high performance liquid chromatography (HPLC), and reversed phase column is more suitable than normal phase column. Even so, the simultaneous separation of flavonoids with closely related structures is not easy. We investigated a successful procedure for the simultaneous separation of glucuronyl flavonoids with 5-hydroxyl group by using a reversed phase column combined with gradient elution in the constituent studies of Scutellaria ikonnikovii Juz.. We have also studied the relationship between the retention time and the position of hydroxyls and glucuronyls in the chemical structure.
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Dried aerial parts of Scutellaria galericulata L. (Labiatae; marsh skullcap) and Scutellaria lateriflora L. (Labiatae; mad dog skullcap) are mainly used as skullcap, a medicinal herb, in Europe and the United States. The respective dried aerial parts of the two species are difficult to distinguish morphologically from each other. We attempted to discriminate among six species (Scutellaria altissima L. (Labiatae), Scutellaria baicalensis Georgi (Labiatae), Scutellaria galericulata, Scutellaria incana Spreng. (Labiatae), Scutellaria indica L. (Labiatae) and Scutellaria lateriflora) of Scutellaria, which include three medicinal species (Scutellaria galericulata, Scutellaria lateriflora and Scutellaria baicalensis), by comparing the respective nucleotide sequences of the plastid rpl16 gene and the rpl16-rpl14 spacer region. Comparisons of these sequences allowed us to identify each of the six species unequivocally.
Scutellaria baicalensis is a widely used Chinese herbal medicine that has been used historically in anti-inflammatory and anticancer therapy. The purpose of this study is to verify its anticancer activity on head and neck squamous cell carcinoma (HNSCC) in vitro and in vivo and to investigate its effect on cyclooxygenase-2 (COX-2), which converts arachidonic acid to prostaglandin E(2) (PGE(2)) and is highly expressed in HNSCC. Two human HNSCC cell lines (SCC-25 and KB) and a nontumorigenic cell line (HaCaT) were tested in vitro for growth inhibition, proliferation cell nuclear antigen expression, and COX-2 activity and expression after treatment with Scutellaria baicalensis extract. Its effects were compared with those of baicalein (a flavonoid isolated from Scutellaria baicalensis), indomethacin (a nonselective COX inhibitor), and celecoxib (a selective COX-2 inhibitor). Four nude mice with s.c. inoculation of KB cells were tested for its anticancer activity in vivo by oral administration of Scutellaria baicalensis at a dose of 1.5 mg/mouse (75 mg/kg), five times/week for 7 weeks. Scutellaria baicalensis and other agents demonstrated a strong growth inhibition in both tested human HNSCC cell lines. No growth inhibition of HaCaT cells was observed with Scutellaria baicalensis. The IC(50)s were 150 micro g/ml for Scutellaria baicalensis, 25 micro M for celecoxib, and 75 micro M for baicalein and indomethacin. Scutellaria baicalensis, as well as celecoxib and indomethacin, but not baicalein, suppressed proliferation cell nuclear antigen expression and PGE(2) synthesis in both cell types. Scutellaria baicalensis inhibited COX-2 expression, whereas celecoxib inhibited COX-2 activity directly. A 66% reduction in tumor mass was observed in the nude mice. Scutellaria baicalensis selectively and effectively inhibits cancer cell growth in vitro and in vivo and can be an effective chemotherapeutic agent for HNSCC. Inhibition of PGE(2) synthesis via suppression of COX-2 expression may be responsible for its anticancer activity. Differences in biological effects of Scutellaria baicalensis compared with baicalein suggest the synergistic effects among components in Scutellaria baicalensis.
Scutellaria baicalensis Georgi (Labiatae) has been used in the treatment of inflammatory diseases. Drug processing (Poje) is the process of treating crude drugs by several methods before use. The aim of this study was to determine the effect of processed Scutellaria baicalensis on experimental ulcerative colitis induced by dextran sulfate sodium (DSS). The types of processed Scutellaria baicalensis used in this study were parched Scutellaria baicalensis (PS) and rice wine-baked Scutellaria baicalensis (RWBS). Experimental colitis was induced in mice using a daily treatment of 5% DSS in the drinking water for 7 days. The water extracts of processed Scutellaria baicalensis (1 g/kg) were administered orally once a day for 7 days. The mice were divided in four groups: i) water plus DSS group, ii) crude Scutellaria baicalensis (CS) plus DSS group, iii) PS plus DSS group, and iv) RWBS plus DSS group. RWBS ameliorated all of the inflammatory symptoms, such as body weight loss, rectal bleeding and histological damage, compared to CS. Furthermore, RWBS significantly reduced the mucosal myeloperoxidase activity, and TNF-alpha (tumor necrosis factor-alpha), COX-2 (cyclooxygenase-2), NF-kappaB (nuclear factor-kappa B) and chymase expression more than CS. But these effects were not shown in the PS plus DSS group. Efficacy of Scutellaria baicalensis was increased after rice wine baking, but not after parching. The findings in this study suggest that RWBS may be a useful therapeutic agent for ulcerative colitis.
BACKGROUND & OBJECTIVE: Various chemically synthetic anti-angiogenesis agents have serious side effects. The traditional Chinese medicine has attracted considerable attention because of its low toxicity. This study was to explore the inhibitory effects of Scutellaria barbatae D. Don, a kind of traditional Chinese medicinal anti-cancer herb, on tumor angiogenesis, and investigate its mechanism. METHODS: Matrigel plug and human umbilical vascular endothelial cells (HUVECs) were used to construct in vivo and in vitro models of angiogenesis to assess the effect of Scutellaria barbatae D. Don on angiogenesis. After cultured with Scutellaria barbatae D. Don, the migration of endothelial cells was examined by Transwell chamber; the expression of vascular endothelial growth factor (VEGF) in HeLa cells was detected by enzyme-linked immunosorbent assay (ELISA). RESULTS: Scutellaria barbatae D. Don significantly inhibited angiogenesis in Matrigel; the tube formation number was significantly lower in 20% and 40% medicated serum groups containing Scutellaria barbatae D. Don than in 20% and 40% drug-free serum groups (5.6+/-1.1 vs. 9.8+/-1.3, P=0.001; 1.0+/-0.7 vs. 13.4+/-1.1, P<0.001). Migrated endothelial cells was significantly fewer in 20% and 40% medicated serum groups containing Scutellaria barbatae D. Don than in 20% and 40% drug-free serum groups (19.75+/-2.63 vs. 24.25+/-2.06, P=0.038; 14.00+/-2.58 vs. 26.5+/-4.65, P=0.006). When treated for 24 h and 48 h, the expression of VEGF in HeLa cells was significantly lower in 40% medicated serum group containing Scutellaria barbatae D. Don than in 40% drug-free serum group (138.67+/-9.50 vs. 195.82+/-2.43, P=0.006; 93.84+/-41.11 vs. 193.68+/-18.37, P=0.036). CONCLUSION: Scutellaria barbatae D. Don could efficiently inhibit angiogenesis in tumor tissue which might relate with inhibition of endothelial cell migration and down-regulation of VEGF in tumor cells.
Scutellariae Radix, the dried root of Scutellaria baicalensis Georgi (Labiatae), was a commonly used traditional Chinese medicine in clinical practice. Baicalin was one of the effective ingredients enriched in Scutellariae Radix. Recent studies revealed baicalin or Scutellariae Radix extract exhibited various pharmacological activities on cerebral functions. In the present study the pharmacokinetic process of baicalin in normal rat blood and cerebral nuclei (cortex, hippocampus, striatum, thalamus and brain stem) was investigated with a newly established reverse-phase HPLC method after intravenous administration of baicalin-enriched Scutellariae Radix extract prepared according to the special protocol. The pharmacokinetic parameters were calculated by the pharmacokinetic program 3P97 and the regulations of baicalin in blood and cerebral nuclei were comparatively analyzed. The results indicated that the distribution of baicalin into brain was a subsequent process and baicalin tends to accumulate in the striatum, thalamus and hippocampus with the exhibition of large area under the concentration-time curve and mean residence time values (p < 0.05). All these pharmacokinetic data of baicalin in blood and cerebral nuclei would be useful to the dosage regime design when baicalin, Scutellariae Radix extract or the prescriptions containing Scutellariae Radix as the main ingredient are prescribed.
OBJECTIVE: To study the effect of Radix Scutellariae on the growth, metabolism of Porphyromonas endodontalis (P.e), as a preparation for studying the mechanism of Radix Scutellariae in treating pulp and periapical diseases. METHODS: P.e was chosen as the experimental bacteria. Radix Scutellariae was extracted by means of reflux with 80% ethanol. The value of MIC of Radix Scutellariae was measured by minute amount serial dilusion test, and the production of butyrate was measured by high liquid chromatograph(HPLC). RESULTS: Radix Scutellariae could inhibit the growth of P.e, of which the MIC was 100 mg/L. Following the increase in concentration of Radix Scutellariae, the amount of butyrate decreased to (3.527 +/- 0.009) mg/L, (3.048 +/- 0.005) mg/L, (2.490 +/- 0.011) mg/L, (2.209 +/- 0.016) mg/L, respectively (P < 0.05). CONCLUSION: Radix Scutellariae could inhibit the growth and metabolism of P.e and might be an effective agent in treating pulp and periapical diseases.
The effects of 17 flavonoids, isolated from two flavonoid-rich Scutellaria species (Scutellaria baicalensis Georgi and Scutellaria rivularis Wall) used in traditional Chinese medicine, on HL-60 cells were assessed by WST-8. Ten of the flavonoids inhibited the proliferation of HL-60, as shown by IC50 values used as indexes of the inhibition. 2',3',5,7-tetrahydroxy flavone (IC50=9.5 microM), apigenin (15.0 microM), viscidulin III (17.4 microM), wogonin (17.4 microM) and luteolin (18.4 microM) were more effective than baicalein (23.0 microM) which reportedly inhibits the proliferation of some cancer cell lines. Others were less effective, and oroxylin A stimulated the proliferation. Scutellaria rivularis, used for the treatment of tumors in the clinic, contained flavonoids that were more inhibitive than those in Scutellaria baicalensis. These results are demonstrative of some reasons for the use of Scutellaria rivularis as a crude antitumor drug.