• Natural Product Sciences
• /
• v.16 no.1
• /
• pp.1-5
• /
• 2010

$\beta$-Glucuronidases (E.C. 3.2.1.31) from Escherichia coli, Helix pomatia, and bovine liver activity have been investigated on 7-O-glucuronides (baicalin, wogonoside, and luteolin-7-O-glucuronide) and 3-O-glucuronides (quercetin-3-O-glucuronide and kaempferol-3-O-glucuronide). Bovine liver enzyme was not active on any of these substrates. E. coli and H. pomatia enzymes were active on 7-O-glucuronides, however, 3-O-glucuronides were resistant to $\beta$-glucuronidase hydrolysis. These results suggest that glucuronic acid at 7-position is more susceptible to E. coli and H. pomatia $\beta$-glucuronidases than that at 3-position. In addition, the subtle difference of aglycone structure on 7-O-glucuronides affected the preference of enzyme. E. coli enzyme was favorable for the hydrolysis of baicalin, however, H. pomatia enzyme was found to be efficient for the hydrolysis of wogonoside. Both enzymes showed the similar hydrolytic activity towards luteolin-7-O-glucuronide. When the Scutellaria baicalensis crude extract was subjected to enzymatic hydrolysis, baicalin and wogonoside were successfully converted to their aglycone counterparts with H. pomatia at 50 mM sodium bicarbonate buffer pH 4.0. Accordingly, the enzymatic transformation of glycosides may be quite useful in preparing aglycones under mild conditions.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.42 no.4
• /
• pp.512-519
• /
• 2013

The antioxidant activities of ethanolic extracts obtained from medicinal plants (Scutellaria baicalensis Georgi, Acanthopanax sessiliflorum Seeman, Pueraria lobata Ohwi, Portulaca oleracea Linne, Crataegus pinnatifida Bunge var. typica Schneider, Euonymus alatus Apterus, Hovenia dulcis Thunberg, Prunus yedoensis Matsumura, Albizzia julibrissin Durazz., Chrysanthemum indicum Linne) were evaluated for total phenolic content, total flavonoid content, DPPH radicals, nitrites, $Superoxide^-$ radicals, $ABTS^+$ radical scavenging activity, and reducing power. Antioxidant capacities were the highest in Prunus yedoensis Matsumura for DPPH radical scavenging activity ($IC_{50}$ $5.39{\mu}g/mL$), reducing power (2.72, $A_{700}$), and nitrite scavenging activity ($IC_{50}$ $167.94{\mu}g/mL$). Hovenia dulcis Thunberg and Acanthopanax sessiliflorum Seeman were effective for their nitrite scavenging activities (over 90% at 1 mg/mL). The $Superoxide^-$ radical scavenging activity of Prunus yedoensis Matsumura ($IC_{50}$ $43.39{\mu}g/mL$) was stronger than tannic acid ($IC_{50}$ $46.51{\mu}g/mL$). Five samples (Prunus yedoensis Matsumura, Acanthopanax sessiliflorum Seeman, Hovenia dulcis Thunberg, Crataegus pinnatifida Bunge var. typica Schneider, Scutellaria baicalensis Georgi) were effective for their $ABTS^+$ radical scavenging activity (more than 90% at 0.5 mg/mL). These results suggest that the ethanolic extracts of Prunus yedoensis Matsumura could be used as a functional ingredient in food products.

• Asian Pacific Journal of Cancer Prevention
• /
• v.14 no.12
• /
• pp.7179-7186
• /
• 2013

Background and Aims: Scutellaria is one of the most popular traditional Chinese herbal remedies against various human diseases, including cancer. In this study, we examined the active effects of Scutellaria extract and its main flavonoid constituents on the proportion of side population cells within human multiple myeloma cell line RPMI8226 in vitro and explored the potential molecular mechanisms involved. Materials and Methods: The contents of flavonoids in ethanolic extract of Scutellaria baicalensis Georgi were determined using high performance liquid chromatography. The antiproliferative effect of the ethanolic extract on RPMI-8226 was determined by CCK assay. Apoptosis was measured by annexin combining with propidium iodide in a flow cytometer. Cell cycle analysis was performed by propidium iodide staining in combination with flow cytometry analysis. Hoechst 33342 exclusion assay was used for the identification of side population within RPMI8226 cells. The expression of ABCG2 protein was assessed by Western blotting assay. Results: The content of major flavonoids constitutents of Scutellaria extract was baicalin (10.2%), wogonoside (2.50%), baicalein (2.29%), and wogonin (0.99%), respectively. The crude Scutellaria extract did not show significant anti-proliferative effect, apoptosis induction and cell cycle arrest in RPMI-8226 within the concentrations of $1-75{\mu}g/mL$. However, the ethanolic extract, baicalein, wogonin and baicalin reduced the side population cells in RPMI-8226, and data showed that baicalein and wogonin had stronger inhibitory effects. Correspondingly, they also exhibited significant effects on decreasing the expression level of ABCG2 protein in RPMI-8226 in vitro. Conclusions: Our results for the first time demonstrated a novel mechanism of action for Scutellaria extract and its main active flavonoids, namely targeting SP cells by modulating the expression of ABCG2 protein. This study provides an insight for new therapeutic strategies targeting cancer stem cells of multiple myeloma.

• BMB Reports
• /
• v.47 no.6
• /
• pp.336-341
• /
• 2014

Endothelial cell protein C receptor (EPCR) plays important roles in blood coagulation and inflammation. EPCR activity is markedly changed by ectodomain cleavage and release as the soluble EPCR. EPCR can be shed from the cell surface, which is mediated by tumor necrosis factor-${\alpha}$ converting enzyme (TACE). Oroxylin A (OroA), a major component of Scutellaria baicalensis Georgi, is known to exhibit anti-angiogenic, antiinflammation, and anti-invasive activities. However, little is known about the effects of OroA on EPCR shedding. Data showed that OroA induced potent inhibition of phorbol-12-myristate 13-acetate (PMA), tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-$1{\beta}$ and on cecal ligation and puncture (CLP)-induced EPCR shedding through suppression of TACE expression and activity. In addition, treatment with OroA resulted in reduced PMA-stimulated phosphorylation of p38, extracellular regulated kinases (ERK) 1/2, and c-Jun N-terminal kinase (JNK). These results demonstrate the potential of OroA as an anti-sEPCR shedding reagent against PMA and CLP-mediated EPCR shedding.

• THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
• /
• v.5 no.1
• /
• pp.103-118
• /
• 1999

The activity of N-acetylglucosamitnyltransferase(GnT) III and V on a Melanoma B-16 was examined after incubation with interleukin 1 (IL-1). While augumenting cell proliferation, IL-1 resulted in a decrease of GnT-III activity and an increase of GnT-V activities. Consistant with this, Melanoma B-16 cultured with IL-1 showed increased affinlity to Daturam stramonium lectin, which recognizes asialo-tri- and asialeo-tetra-antenery N-linked oligosaccharides. These results indicate that IL-1 modulate glycosyltransferase activity and the oligosaccharide structure of target cells. On the other hand, to investigate whether or not TKM-SG affect GnT-V gene expression in lung metastatic carcinoma, we used RT-PCR methods. TKM-SG treated cell lines showed low levels of secretion of GnT-V mRNA transcription as elucidated by RT-PCR. Thus, with together lower GnT-V activity levels in the medium, TKM-SG was highly effective for lung cancer metastasis treatment and it was concluded that the medicine can be used as a potent anti-lung cancer metastasis medicine.

• Archives of Pharmacal Research
• /
• v.27 no.9
• /
• pp.930-936
• /
• 2004

Wogonin (5,7-dihydroxy-8-methoxyflavone), an active component originated from the root of Scutellaria baicalensis Georgi, has been reported to possess antioxidant and anti-inflamma-tory properties. In this study, we investigated the neuroprotective effect of wogonin in a focal cerebral ischemia rat model. Wogonin markedly reduced the infarct volume after 2 h middle cerebral artery occlusion followed by 22 h reperfusion. Wogonin decreased the production of nitric oxide and inflammatory cytokines such as TNF-$\alpha$ and IL-6 in lipopolisaccharide-stimu-lated microglial cells. While wogonin reduced the activity of NF-$textsc{k}$B, it did not change the activ-ity of mitogen-activated protein kinases family members, p38, ERK and JNK. The lipopolisaccharide-stimulated production of NO and cytokines was significantly blocked by vari-ous kinds of NF-$textsc{k}$B inhibitors such as N-acetyl cysteine, pyrrolidinedithiocarbamate and MG-132. The data may indicate that wogonin has neuroprotective effect by preventing the over-activation of microglial cells, possibly by inactivating NF-$textsc{k}$B signaling pathway

• Biomolecules & Therapeutics
• /
• v.24 no.5
• /
• pp.552-558
• /
• 2016

Severe complications associated with EV71 infections are a common cause of neonatal death. Lack of effective therapeutic agents for these infections underlines the importance of research for the development of new antiviral compounds. In the present study, the anti-EV71 activity of norwogonin, oroxylin A, and mosloflavone from Scutellaria baicalensis Georgi was evaluated using a cytopathic effect (CPE) reduction method, which demonstrated that all three compounds possessed strong anti-EV71 activity and decreased the formation of visible CPEs. Norwogonin, oroxylin A, and mosloflavone also inhibited virus replication during the initial stage of virus infection, and they inhibited viral VP2 protein expression, thereby inhibiting viral capsid protein synthesis. However, ribavirin has a relatively weaker efficacy compared to the other drugs. Therefore, these findings provide important information that will aid in the utilization of norwogonin, oroxylin A, and mosloflavone for EV71 treatment.

• Korean Journal of Plant Resources
• /
• v.22 no.6
• /
• pp.489-497
• /
• 2009

In this study, we evaluated and compared the protective effects of two major constituents, baicalein and baicalin, against oxidative DNA and cell damages caused by hydroxyl radical. Antioxidant properties were evaluated using DPPH and hydroxyl radicals scavenging assays and $Fe^{2+}$ chelating assay. ${\varphi}X$ 174 RFI plasmid DNA and intracellular DNA migration assay were used to evaluate the protective effect against oxidative DNA damage. Also, MTT and lipid peroxidation assays were used to evaluate their protective effects against oxidative cell damage. Both baicalein and baicalin prevented intracellular DNA and cells from oxidative damage caused by hydroxyl radical via antioxidant activities. Baicalein demonstrated a stronger antioxidant activity in scavenging DPPH radicals and chelating $Fe^{2+}$ while baicalin scavenged hydroxyl radicals more efficiently. The differences in the level of baicalein and baicalin pose a different pathological pathway for each. The antioxidant activity of baicalin was due to its ability to scavenge hydroxyl radical whilst baicalein was a stronger $Fe^{2+}$ chelator. Further investigation to compare the molecular mechanisms of antitumor activities of baicalein and baicalin is vital to anticancer research.

• Archives of Pharmacal Research
• /
• v.29 no.6
• /
• pp.503-507
• /
• 2006

Flavonoids are known as natural anti-inflammatory agents. In this investigation, an anti-inflammatory potential of new topical preparation (SK Ato $Formula^{\circledR}$) containing flavonoid mixtures from Scutellaria baicalensis Georgi roots and Ginkgo biloba L. leaves with an extract of Gentiana scabra Bunge roots was evaluated in an animal model of chronic skin inflammation. Multiple 12-O-tetradecanoylphorbol-13-acetate treatments for 7 consecutive days on ICR mouse ear provoked a chronic type of skin inflammation: dermal edema, epidermal hyperplasia and infiltration of inflammatory cells. When topically applied in this model, this row formulation $(5-20\;{\mu}L/ear/treatment)$ reduced these responses. Furthermore, it inhibited prostaglandin $E_2$ generation (17.1-33.3%) and suppressed the expression of proinflammatory genes, cyclooxygenase-2 and $interleulin-1{\beta}$ in the skin lesion. Although the potency of inhibition was lower than that of prednisolone, all these results suggest that Ato $Formula^{\circledR}$ may be beneficial for treating chronic skin inflammatory disorders such as atopic dermatitis.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.29 no.1
• /
• pp.101-113
• /
• 2015

Application of herbal medicines as natural preservatives has been increased because of its low toxicity or side effect, compared to artificial preservatives. In this study, papers and patents researching anti-microbial activity of herbal medicine were collected and analyzed by the year of publishment, species of bacteria, fungi, or yeasts, and herbal medicines used. After early 2000's, the number of paper publishment has been decreased, while that of patent registration has been increased up to early 2010's. Most studied species were Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa, as gram-positive or gram-negative bacteria, and Candida albicans and Aspergillus niger as fungi. The bark of Cinnamomum cassia (L.) J. Presl was most frequently studies herbal medicine, followed by the roots of Scutellaria baicalensis Georgi and Sophora flavescens Ait. This study demonstrates that herbal medicines can be used as natural preservatives against diverse species of bacteria, fungi, or yeasts with their wide-ranged anti-microbial activities.