Protective effects of Baicalin injection on severe acute pancreatitis through regulating follistatin-like-1 signaling pathway by down-regulating miR-429 expression in mice

Abstract In China, Scutellaria is used for treating inflammatory-related diseases. Baicalin is the main active component of Scutellaria and has protective effects on acute pancreatitis. However, the mechanism of Baicalin is still unclear. In this study, the protective effects of baicalin on acute pancreatitis induced by taurocholate and its mechanism are investigated. In this study, mice were randomly divided into three groups: sham operation, model, and treatment groups. Acute pancreatitis in mice was induced by intraperitoneal injection of taurocholate (35 mg/kg). The treatment group was given baicalin (100 mg/kg) 2 h before acute pancreatitis induction. The mRNA expression levels of miR-429, nuclear factor kappa B65(NF-kB65), toll-like receptor 4(TLR4), TNF receptor associated factor6 (TRAF6), NF-kappa-B inhibitor(IkB), Follistatin-like 1 (FSTL1), and interleukin-1 receptor-associated kinase (IRAK) in the liver tissues 24 h after intraperitoneal injection were detected by RT-PCR. Then, the expression levels of NF-kB65, p-NF-κB65, TLR4, TRAF6, IkB, FSTL1, IRAK, p- IRAK, and p- IkB-а proteins were detected by Western blot. IL-6, TNF-α and IL-1 ß in plasma were measured by ELISA, and histopathological changes in the pancreases of the mice were observed. The results showed that after baicalin treatment, miR-429 expression in the pancreatic tissues and the expression levels of NF-kB65, TLR4, TRAF6, p-IkB-а, FSTL1, and p-IRAK decreased. Similarly, pancreatic myeloperoxidase (MPO) activity and the plasma levels of IL-6, TNF-а, IL-12, IL-1ß1, endotoxin, serum amylase, and lipase were reduced. Thus, the pancreatic injury induced by taurocholate was alleviated. The present study indicates that pretreatment with Baicalin can alleviate acute pancreatic injury induced by taurocholate in mice. The mechanism may be associated with the decreased miR-429 expression, reduced FSTL1 signaling pathway activity, TLR4 and TLR4/MyD88 signaling pathway inhibition, and reduced pancreatic inflammation. FSTL1 is the regulatory target for miR-429

Multi-index components of Scutellariae Barbatae Herba according to UHPLC-QTRAP-MS coupled with chemometrics / 中国中药杂志

The present study developed an ultra-fast liquid chromatography coupled with triple quadrupole-linear ion trap composite mass spectrometry(UHPLC-QTRAP-MS) to simultaneously determine the content of potential active components in Scutellariae Barbatae Herba and also to provide a reference approach for screening out the differential quality control components among different batches of Scutellariae Barbatae Herba. Chromatographic separations were conducted on a Thermo Acclaim~(TM) RSLC 120 C_(18) column(3.0 mm×100 mm, 2.2 μm) in a gradient program. The mobile phase consisted of 0.1% aqueous formic acid and acetonitrile, and the column temperature was maintained at 40 ℃. The flow rate was 0.4 mL·min~(-1) and the injection volume was 2 μL. The targeted compounds were monitored in the multiple reaction monitoring(MRM) mode. The acquired data were processed by hierarchical cluster analysis(HCA) and partial least square discriminant analysis(PLS-DA). Sixteen compounds all showed good linear relationship within the corresponding linear ranges and the R~2 values were all higher than 0.993 2. The RSDs of precision, repeatability, and stability were less than or equal to 3.7%. Mean recovery rates were in the range of 95.67% and 104.8% with RSDs≤3.2%. According to HCA and PLS-DA, all samples were clustered into four categories. Scutellarin, acteoside, scutellarein, and scutebarbatine X(VIP>1) were considered as differential chemical markers in the four categories. In conclusion, the developed method can be used for the simulta-neous determination of the multiple components and quality control of Scutellariae Barbatae Herba.

Comparative Genome Analysis of Scutellaria baicalensis and Scutellaria barbata Reveals the Evolution of Active Flavonoid Biosynthesis / 基因组蛋白质组与生物信息学报·英文版

Scutellaria baicalensis (S. baicalensis) and Scutellaria barbata (S. barbata) are common medicinal plants of the Lamiaceae family. Both produce specific flavonoid compounds, including baicalein, scutellarein, norwogonin, and wogonin, as well as their glycosides, which exhibit antioxidant and antitumor activities. Here, we report chromosome-level genome assemblies of S. baicalensis and S. barbata with quantitative chromosomal variation (2n = 18 and 2n = 26, respectively). The divergence of S. baicalensis and S. barbata occurred far earlier than previously reported, and a whole-genome duplication (WGD) event was identified. The insertion of long terminal repeat elements after speciation might be responsible for the observed chromosomal expansion and rearrangement. Comparative genome analysis of the congeneric species revealed the species-specific evolution of chrysin and apigenin biosynthetic genes, such as the S. baicalensis-specific tandem duplication of genes encoding phenylalanine ammonia lyase and chalcone synthase, and the S. barbata-specific duplication of genes encoding 4-CoA ligase. In addition, the paralogous duplication, colinearity, and expression diversity of CYP82D subfamily members revealed the functional divergence of genes encoding flavone hydroxylase between S. baicalensis and S. barbata. Analyzing these Scutellaria genomes reveals the common and species-specific evolution of flavone biosynthetic genes. Thus, these findings would facilitate the development of molecular breeding and studies of biosynthesis and regulation of bioactive compounds.

Induction of Apoptosis Scutellaria baicalensis Georgi Root Extract by Inactivation of the Phosphatidyl Inositol 3-kinase/Akt Signaling Pathway in Human Leukemia U937 Cells

BACKGROUND: The roots of Scutellaria baicalensis Georgi (Labiatae) have been widely used in traditional medicine for treatment of various diseases. In this study, we investigated the effects of ethanol extracts of S. baicalensis roots (EESB) on the growth ofn human leukemia U937 cells. METHODS: The effect of EESB on cell viability was measured by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay. Apoptosis was determined using 4,6-diamidino-2-phenyllindile staining and flow cytometry. The effects of EESB on the expression of regulatory proteins of apoptosis and phosphatidyl inositol 3-kinase (PI3K)/Akt signaling were determined by Western blotting. Caspase activity and mitochondrial membrane potential (MMP) were measured using flow cytometric analysis.

Comprehensive Evaluation of the Anti-Helicobacter pylori Activity of Scutellariae Radix

The aim of this study was to evaluate the anti-Helicobacter pylori activity of fractions and major aglycon compounds (baicalein, chrysin, oroxylin A, wogonin) of Scutellariae Radix. Minimum inhibitory concentration (MIC) measurement, DPPH radical-scavenging assay, DNA protection assay, and urease inhibition analysis were performed. The ethyl acetate (EtOAc) fraction showed the potent anti-Helicobacter activity, and therefore, compounds in the EtOAc fraction were subjected to further assay. The MICs of chrysin, oroxylin A, and wogonin against Helicobacter pylori 26695 were 6.25, 12.5 and 25 µg/mL, respectively. Baicalein exhibited the most effective DPPH radical-scavenging activity. DNA protection using Fenton reaction, chrysin, oroxylin A, and wogonin showed effective DNA protective effect. This result was also confirmed by quantitative real-time polymerase chain reaction (qRT-PCR). Regarding Jack bean urease (0.5 mg/mL, 50 unit/mg) inhibition, 20 mM ofbaicalein and chrysin inhibited urease activity by 88.2% and 72.5%, respectively.

Baicalein, wogonin, and Scutellaria baicalensis ethanol extract alleviate ovalbumin-induced allergic airway inflammation and mast cell-mediated anaphylactic shock by regulation of Th1/Th2 imbalance and histamine release / 대한해부학회지

Asthma is characterized by chronic inflammation, goblet cell hyperplasia, the aberrant production of the Th2 cytokines, and eosinophil infiltration into the lungs. In this study, we examined the effects of baicalein, wogonin, and Scutellaria baicalensis ethanol extract on ovalbumin (OVA)-induced asthma by evaluating Th1/Th2 cytokine levels, histopathologic analysis, and compound 48/80-induced systemic anaphylaxis and mast cell activation, focusing on the histamine release from rat peritoneal mast cells. Baicalein, wogonin, and S. baicalensis ethanol extract also decreased the number of inflammatory cells especially eosinophils and downregulated peribronchial and perivascular inflammation in the lungs of mice challenged by OVA. Baicalein, wogonin, and S. baicalensis ethanol extract significantly reduced the levels of tumor necrosis factor α, interleukin (IL)-1β, IL-4, IL-5 and the production of OVA-specific IgE and IgG1, and upregulated the level of interferon-γ and OVA-specific IgG2a. In addition, oral administration of baicalein, wogonin, and S. baicalensis ethanol extract inhibited compound 48/80-induced systemic anaphylaxis and plasma histamine release in mice. Moreover, baicalein, wogonin, and S. baicalensis ethanol extract suppressed compound 48/80-induced mast cell degranulation and histamine release from rat peritoneal mast cells. Conclusively, baicalein and wogonin as major flavonoids of S. baicalensis may have therapeutic potential for allergic asthma through modulation of Th1/Th2 cytokine imbalance and histamine release from mast cells.

Diterpenoids from Scutellaria strigillosa / 中国中药杂志

By means of preparative HPTLC and column chromatography over silica gel and Sephadex LH-20, nine diterpenoids were isolated and purified from the whole plants of Scutellaria strigillosa. Based on the physico-chemical properties and spectral data, their structures were elucidated as: 6-O-acetyl-7-O-nicotinoylscutebarbatine G(1), 6-O-nicotinoyl-7-O-acetylscutebarbatine G(2), 6,7-di-O-nicotinoylscutebarbatine G(3), scutebarbatine K(4), scutebarbatine B(5), 6-O-acetylscutehenanine A(6), 6-O-nicotinoylbarba- tin A(7), 6,7-di-O-acetoxylbarbatin A(8), scutebarbatine F(9). Compound 1 is a new diterpenoid, and compounds 2-9 were isolated from Scutellaria strigillosa for the first time.

Efeito analgésico e anti-inflamatório do extrato aquoso das folhas de trevo-roxo (Scutellaria agrestis A. St. -Hil. ex Benth. - Lamiaceae) em roedores / Analgesic and anti-inflammatory effect of the aqueous extract of "trevo-roxo" (Scutellaria agrestis A. St. -Hil. ex Benth. - Lamiaceae) leaves in rodents

Scutellaria agrestis é utilizada por comunidades ribeirinhas do Amazonas principalmente para o tratamento de otites por via tópica utilizando-se o extrato bruto obtido por maceração. O presente trabalho visou investigar preliminarmente o perfil fitoquímico, a segurança toxicológica e as ações analgésica, anti-inflamatória e antiedematogência do extrato aquoso das folhas de S. agrestis. Foram coletados 80 indivíduos da espécie no horto medicinal da Universidade Nilton Lins, Manaus, Brasil. O perfil fitoquímico foi obtido por meio de prospecção da droga vegetal para heterosídeos cianogênicos, terpenos, compostos fenólicos e alcaloides. A toxicologia foi avaliada pelo teste de toxicidade aguda. As atividades analgésicas/ anti-inflamatórias foram analisadas por meio dos testes de formalina em camundongos e a atividade antiedematogência, pelo teste de edema de pata em ratos. Os metabólitos detectados foram fenóis (taninos hidrolisáveis, cumarinas e várias classes de flavonoides) e terpenos (esteroides livres, saponinas). Não foi possível estabelecer DL50, haja visto que o extrato não provocou a morte de nenhum animal durante o teste de toxicidade aguda, provavelmente devido à ausência de heterosídeos cianogênicos na sua composição. Apesar de não provocar morte, considerou-se que o extrato apresenta uma discreta toxicidade, uma vez que foi observada a ocorrência de espasmos na primeira hora de observação dos animais. O extrato apresentou ainda efeito analgésico e anti-inflamatório significativo nas doses de 30, 100 e 300 mg/kg pelo teste da formalina, sendo o resultado na maior dose equivalente ao obtido com a droga padrão (fentanil). No entanto, não observamos efeito antiedematogênico nas doses testadas durante as 5 horas de registro do edema de pata. Os resultados obtidos nesta pesquisa conferem base científica preliminar quanto à segurança e ao efeito analgésico e antiinflamatório da droga vegetal, o que indica que tal espécie é promissora e expressamente recomendada para maiores estudos farmacológicos in vitro e in vivo.

The Scutellaria agrestis is used by Amazonas riverine communities, especially for otitis externa topical treatment, by using the crude extract obtained by maceration. This study aimed to investigate the preliminary phytochemical profile, the safety/toxicity and the analgesic, anti-inflammatory and antiedematogenic activities of the aqueous extract of the S. agrestis leaves. Eighty individuals were collected at the Nilton Lins University medicinal garden, Manaus, Brazil. The phytochemical profile was obtained through a plant drug survey for cyanogenic heterosides, terpenes, alkaloids and phenolic compounds. The extract safety was evaluated by acute toxicity test. Analgesic and anti-inflammatory activities were accessed using formalin test in mice and the antiedematogenic activity, using paw edema test in mice. We detected phenolic (hydrolysable tannins, coumarins and several classes of flavonoids) and terpenoid (free steroids, saponins) metabolites. We could not establish LD50 because no animals died during the acute toxicity test, probably because of the absence of cyanogenic glycosides on the composition of the extract. However, we found that the extract is slightly toxic as animal spasms were observed in the first hour of the test. The extract showed significant analgesic and anti-inflammatory activity on the formalin test (30, 100 and 300 mg/kg p.o.), and the highest dose result was equivalent to the standard drug (Fentanyl). However, no significant antiedematogenic effect was observed during the paw edema test. The results obtained in this study provide preliminary scientific basis about the safety and analgesic/anti-inflammatory actions of the aqueous extract of S. agrestis, which indicates that this species is a promising option for further in vitro and in vivo pharmacological studies.

New advance in studies on antimicrobal activity of Scutellaria baicalensis and its effective ingredients / 中国中药杂志

In recent years, with the constant increase in the population with hypoimmunity, bacterial and fungal infections have been increasing. Due to the drug resistance, clinically optional anti-bacterial and antifungal medicines become increasingly limited. Scutellaria baicalensis, a species of perennial herbaceous plant of scutellaria genus of lamiaceae family, and its effective components have multiple pharmacological effects such as anti-inflammation, anti-oxidation, anti-tumor, anti-microbial. Especially, its remarkable antibacterial and antifungal activities are of great significance to treat the increasing number of cases with drug-fast bacterial and antifungal infections. In this paper, the authors summarized the advance in studies on antibacterial and antifungal effects and mechanisms in recent years on the basis of the domestic and foreign studies on S. baicalensis and its effective ingredients.

Scutellaria baicalensis in stroke management: nature's blessing in traditional Eastern medicine / 中国结合医学杂志

Scutellaria baicalensis Georgi is the most widely used medicinal plant in traditional Eastern medicine, especially in Chinese medicine. The major phytochemicals isolated from S. baicalensis are flavonoids, glycosides and their glucoronides such as baicalin, baicalein, wogonin etc. More than 30 different kinds of flavonoids are isolated from this plant. S. baicalensis and its flavonoids are reported to have several pharmacological activities, which includes anti-allergic, antioxidant, anti apoptic, anti-inflammatory effects and many more. Recently, S. baicalensis and its isolated flavonoids have been studied for their neuroprotective effects, through a variety of in vitro and in vivo models of neurodegenerative diseases, plausibly suggesting that S. baicalensis has salutary effect as a nature's blessing for neuroprotection. In this review, we are focousing on the neuroprotective effects of S. baicalensis and its flavonoids in ischemia or stroke-induced neuronal cell death. We aimed at compiling all the information regarding the neuroprotective effect of S. baicalensis in various experimental models of cerebral ischemia or stroke.

Comparative pharmacokinetics of baicalin, wogonoside, baicalein and wogonin in plasma after oral administration of pure baicalin, Radix scutellariae and Scutellariae-paeoniae couple extracts in normal and ulcerative colitis rats

The aim of this study was to investigate the pharmacokinetic profiles of baicalin, wogonoside, baicalein and wogonin after oral administration of pure baicalin, Radix scutellariae and Scutellariae-Paeoniae couple extracts were administered and the pharmacokinetics profiles were compared between normal and ulcerative colitis rats. The plasma concentrations of the four flavonoids were determined by using a simple and rapid high-performance liquid chromatography method. All the rats were divided randomly into two groups [ulcerative colitis and normal groups]. Each group contained three subgroups: pure baicalin, Radix scutellariae and Scutellariae-paeoniae couple extracts subgroup. Each group received oral administration of pure baicalin, Radix scutellariae and Scutellariae-paeoniae couple extracts at the same dose of 200 mg/kg baicalin. The results showed that wogonoside, possibily as a methylated product of baicalin, was found in plasma after oral administration of pure baicalin or formulas to rats. Baicalin and wogonoside demonstrated bimodal phenomenon. Baicalin and wogonoside in Scutellariae-Paeoniae couple extract had shown better absorption than which inpure baicalin and Radix scutellariae extract. Whether oral administration of pure baicalin, Radix Scutellariae or Scutellariae-paeoniae couple extracts, ulcerative colitis rats showed better absorption than normal rats. For example AUC[0-t] of baicalin were: [41.46 +/- 0.62], [59.12 +/- 6.42] and [104.87 +/- 0.86] [micro g/mL] h in UC groups vs [17.77 +/- 0.66], [28.04 +/- 4.06] and [49.01 +/- 4.61] [micro g/mL] h in normal groups, respectively. The pharmacokinetics properties of the four flavonoids differed between ulcerative colitis and normal rats, including AUC[0-t] and C[max] [p < 0.05]

Tamizaje fitoquímico de Scutellaria havanensis Jacq / Phytochemical screening of Scutellaria havanensis JacQ

Introducción: la especie Scutellaria havanensis Jacq., conocida como escudo de La Habana, es una planta endémica de Cuba, empleada para el tratamiento de la escabiosis, como diaforético y febrífugo. Sin embargo, no se han realizado estudios fitoquímicos de esta planta. Objetivo: realizar un tamizaje fitoquímico de los extractos etéreo, metanólico y acuoso de las partes aéreas (hojas y tallos) de la especie Scutellaria havanensis Jacq. Métodos: se recolectaron las partes aéreas frescas y se extrajeron con éter dietílico, metanol y agua. Los extractos se filtraron y se les realizaron las pruebas fitoquímicas de identificación. Resultados: en el extracto etéreo se identificaron alcaloides, coumarinas, triterpenos y esteroides; en los extractos acuoso y metanólico se encontraron alcaloides, grupos aminos, azúcares, flavonoides, quinonas y resinas; mientras que en el extracto acuoso se detectaron saponinas y principios amargos. Conclusiones: Scutellaria havanensis, planta endémica cubana, contiene varios grupos de compuestos como flavonoides, alcaloides, entre otros, que pudieran tener interés farmacológico potencial. Estos resultados constituyen un apoyo para continuar los estudios fítoquímicos y farmacológicos de los diversos extractos

Introduction: Scutellaria havanensis Jacq. species, known as Escudo de La Habana (Havana skullcap), is an endemic Cuban plant, etnomedically used for the treatment of scabies and as a diaphoretic and a febrifuge. However, no phytochemical study of this plant has been made so far. Objective: to conduct a phytochemical study of the ethereal, methanol and aqueous extracts from aerial parts (leaves and stems) of Scutellaria havanensis Jacq. species. Methods: fresh aerial parts were harvested and extracts were obtained with diethyl ether, methanol and water. The extracts were filtered and subjected to the phytochemical identification tests. Results: alkaloids, coumarins, triterpenes and steroids were identified in the ethereal extracts, whereas alkaloids, amino groups, sugars, flavonoids, quinones and resins were found in the methanol and aqueous extracts, and saponins and bitter principles in the aqueous extract. Conclusions: Scutellaria havanensis, an endemic Cuban plant, contains several groups of compounds of potential pharmacological interest like flavonoids and alkaloids, among others. These results encourage continuing the phytochemical and pharmacological studies of several extracts

Wogonin inhibits IGF-1-stimulated cell growth and estrogen receptor α expression in breast adenocarcinoma cell and angiogenesis of chick chorioallantoic membrane / 生理学报

The aim of the present study was to investigate the involvements of insulin-like growth factor-1 (IGF-1) and estrogen receptor α (ERα) in the inhibitory effect of wogonin on the breast adenocarcinoma growth. Moreover, the effect of wogonin on the angiogenesis of chick chorioallantoic membrane (CAM) was also investigated. MCF-7 cells (human breast adenocarcinoma cell line) were subjected to several drugs, including IGF-1, wogonin and ER inhibitor ICI182780, alone or in combination. MTT assay was used to detect breast cancer proliferation. Western blot was used to analyze ERα and p-Akt expression levels. CAM models prepared from 6-day chicken eggs were employed to evaluate angiogenesis inhibition. The results showed wogonin and ICI182780 both exhibited a potent ability to blunt IGF-1-stimulated MCF-7 cell growth. Either of wogonin and ICI182780 significantly inhibited ERα and p-Akt expressions in IGF-1-treated cells. The inhibitory effect of wogonin showed no difference from that of ICI182780 on IGF-1-stimulated expressions of ERα and p-Akt. Meanwhile, wogonin at different concentrations showed significant inhibitory effect on CAM angiogenesis. These results suggest the inhibitory effect of wogonin on breast adenocarcinoma growth via inhibiting IGF-1-mediated PI3K-Akt pathway and regulating ERα expression. Furthermore, wogonin has a strong anti-angiogenic effect on CAM model.

Estimating medicinal yield of Seutellaria baicalensis in Beijing-Tianjin-Hebei region based on 3S technology / 中国中药杂志

Resources survey of traditional Chinese medicine and reserves estimation are found to be the most important issues for the protection and utilization of traditional Chinese medicine resources, this paper used multi-spatial resolution remote sensing images (RS) , geographic information systems (GIS) and global positioning system (GPS) , to establish Scutellaria resources survey of 3S data platform. Combined with the traditional field survey methods, small-scale habitat types were established based on different skullcap reserve estimation model, which can estimate reserves of the wild Scutellaria in Beijing-Tianjin-Hebei region and improve the estimation accuracy. It can provide an important parameter for the fourth national survey of traditional Chinese medicine resources and traditional Chinese medicine reserves estimates based on 3S technology by multiple spatial scales model.

Anti-leukemic effect of scutellaria extract SBX and its mechanisms / 中国实验血液学杂志

This study was aimed to explore the anti-leukemic effect of scutellaria extract SBX in human leukemia cell lines and its mechanism. The leukemia cell lines, including HL-60, NB4, U937, K562 and Jurkat, were cultured in vitro and proliferative inhibition of these cell lines was detected by CellTiter-Glo Luminescent Cell Viability Assay in order to screen the most sensitive cell line. The effect of SBX on cell cycle was analyzed by flow cytometry and the protein expressions determined by Protein Pathway Array respectively. The results indicated that SBX (10 - 200 µmol/L, for 72 h) significantly inhibited the proliferation of different leukemia cell lines in a dose-dependent manner (r value was 0.86, 0.88, 0.95, 0.94, 0.96, respectively), the HL-60 was the most sensitive cell line. Flow cytometric analysis showed that SBX (50, 10 µmol/L, for 48 h) arrested HL-60 cells in the G(0)/G(1) phase. In addition, protein expression of p-PKC α/βII, p-p38, Cdc25B, XIAP of HL-60 cells increased, and p-AKT, p-SAPK/JNK, Notch4, Cdk4, Cdc2, cyclin E, Akt, Bcl-2, Bax, cdc42, TNF-α, p27, CaMKKa decreased after exposure to SBX (50 µmol/L, for 48 h). It is concluded that SBX can inhibit the proliferation of different leukemia cell lines, and HL-60 is a sensitive cell line. SBX significantly influences EGFR, Ras/Raf/MAPK and Notch signaling pathway, through which effects the expression of cell cycle-related proteins resulting in arrest of HL-60 cells in G(0)/G(1).

Single-Dose Oral Toxicity of Fermented Scutellariae Radix Extract in Rats and Dogs

The aim of this study was to investigate the acute oral toxicity of fermented Scutellariae Radix (JKTMHGu-100) in rats and dogs. JKTM-HGu-100 was orally administered at a dose of 2,000 mg/kg in Sprague-Dawley rats. An escalating single-dose oral toxicity test in beagle dogs was performed at doses of 500, 1000, and 2000 mg/kg with 4-day intervals. Clinical signs, changes in body weight, mortality, and necropsy findings were examined for 2 weeks following oral administration. No toxicological changes related to the test substance nor mortality was observed after administration of a single oral dose of JKTM-HGu-100 in rats or dogs. Therefore, the approximate lethal dose (LD) for oral administration of JKTMHGu-100 in rats was considered to be over 2,000 mg/kg, and the maximum tolerance doses (MTDs) in rats and dogs were also estimated to be over 2,000 mg/kg. These results indicate that JKTM-HGu-100 shows no toxicity in rodents or non-rodents at doses of 2,000 mg/kg or less.

The Evaluation of Skin Safety and Skin Cell Toxicity for Scutellaria baicalensis Georgi Extract according to Extraction Conditions / 대한피부과학회지

BACKGROUND: Scutellaria baicalensis Georgi extract is used as a traditional herbal medicine. The efficacy of Scutellaria baicalensis Georgi extract is known for antioxidative activity, antiinflammation effect, antibacterial effect, inhibitory effect of melanin synthesis, sun protection effect, antiallergy effect, and etc. OBJECTIVE: We confirmed the cell viability or inhibitory effect of melanin synthesis in HaCaT (human keratinocyte cell line) and B16F10 (murine melanoma cell line) cells and the skin safety test through a clinical test (dermal irritation study) for Scutellaria baicalensis Georgi extract, according to the extraction methods. METHODS: We checked the cell viability, using MTT assay and inhibitory effect of melanin synthesis in B16F10 cells or HaCaT cells for thirty one Scutellaria baicalensis Georgi extract, according to the extraction methods. Then, we evaluated the skin safety for selected eight Scutellaria baicalensis Georgi extract through a primary dermal irritation test. RESULTS: Among the thirty one Scutellaria baicalensis Georgi extracts, according to the extraction methods, we selected eight Scutellaria baicalensis Georgi extracts that were not detected with cell toxicity in HaCaT cells and B16F10 cells, and could have inhibited the melanin synthesis in B16F10 cells. The selected eight Scutellaria baicalensis Georgi extracts identified the skin safety through a primary dermal irritation test. CONCLUSION: We expect clinical trials for whitening efficacy based on inhibitory effect of melanin synthesis and human skin safety for Scutellaria baicalensis Georgi extracts.

Determination of four effective components from total flavonoids of Scutellaria barbata by high performance liquid chromatography / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To establish a HPLC method for simultaneous determination of 4 effective components from total flavonoids of Scutellaria barbata (FSB).</p><p><b>METHODS</b>The HPLC method was developed on an Agilent Zorbax C₁₈ column (4.6 mm × 250 mm, 5 μm). The mobile phase was composed of 1% HAc and CH₃OH:CH₃CN (80:20) with a linear gradient elution. The flow rate was 1.0 ml/min, and UV detection wave length was set at 280 nm. The column temperature was maintained at 30°C.</p><p><b>RESULT</b>The linear range of 4 effective components (scutellarin, isoscutellarein-8-O-glucuronide, isoscutellarein and luteolin) was 0.14-11.20 μg, 0.03-2.40 μg, 0.007-0.560 μg and 0.027-2.160 μg, respectively. The average recovery for 4 effective components was (101.9 ± 1.4)%, (103.5 ± 0.6)%, (98.1 ± 2.9)% and (100.5 ± 2.3)%, respectively. The contents of 4 flavonoids were determined, with scutellarin 7.3%-14.3%, isoscutellarein-8-O-glucuronide 2.4%-9.3%, isoscutellarein 0.3%-0.5%, and luteolin 0.2%-0.6%, respectively.</p><p><b>CONCLUSION</b>The method can be used effectively to evaluate the quality of FSB.</p>

The enhancing effect of Angelica dahurica extracts on absorption of baicalin--the active composition of Scutellaria / 药学学报

To explore the mechanism of the absorption enhancement of Angelica dahurica extract (Ade), the absorption mechanism of baicalin in the Scutcllaria water extraction as well as the effect of Angelica dahurica extract on absorption of baicalin were investigated. In order to determine the main absorption site, everted intestinal sac model was used to study the effect of Angelica dahurica extract on the absorption of baicalin at duodenum, jejunum, ileum and colon. In situ single pass intestinal perfusion model was performed to study the absorption of various concentrations of baicalin and the effect of Angelica dahurica extract on the absorption of baicalin at the main absorption site. To authenticate the consequence of perfusion by getting the blood from the hepatic portal vein and determine the concentration of the baicalin in the blood. The result showed that baicalin could be absorbed at all of the four intestinal segments with increasing absorption amount per unit as follows: ileum > colon > jejunum > duodenum. The absorption ofbaicalin in the duodenum significantly increased with Angelica dahurica extract, thus, duodenum was chosen to be the studying site. Apparent permeability values (Papp) and absorption rate constant (Ka) of baicalin in the duodenum increased gradually with higher concentrations. When the concentration of baicalin rises to a certain degree, the absorption increase had a saturable process, the absorption of baicalin may be an active transportation. Baicalin may be not a substrate of P-gp as verapamil which had not significantly affected the Papp and Ka of baicalin. The absorption of baicalin in the duodenum significantly increased (P < 0.01) in the two models with Angelica dahurica extract and the concentration of baicalin in the blood from the hepatic portal vein showed that the Angelica dahurica extract can increase the absorption of baicalin.

Effects of scutellaria stem-leaf total flavonoids on cardiocyte apoptosis induced by hypoxia/reoxygenation / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To study the effect of Scutellaria baicalensis stem-leaf total flavonoids (SSTF) on cardiocyte apoptosis of neonatal rats induced by hypoxia/reoxygenation and its action of mechanism. METHODS Sixty one to two days old rats, male or female, were selected. Hypoxia/reoxygenation injured model was established in cultured cardiocytes of neonate rats. The cultured neonatal rat cardiocytes were divided into 5 groups, i.e., the normal control group, the hypoxia/reoxygenation injury group (as the model group, cultured cardiocytes were exposed to hypoxia 2 h and subsequently reoxygenated for 4 h), the hypoxia/reoxygenation injury plus 50 mg/L SSTF group (as the low dose SSTF group), the hypoxia/reoxygenation plus 100 mg/L SSTF group (as the middle dose SSTF group), and the hypoxia/reoxygenation plus 200 mg/L SSTF group (as the high dose SSTF group). The cell viability was detected by methyl thiazolyl tetrazolium (MTT) colorimetry. The apoptosis of cardiocytes was determined by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) and the apoptosis rate calculated. The Bcl-2 and Bax protein expressions were determined by immunohistochemistry.</p><p><b>RESULTS</b>Compared with the normal control group, the cell viability, Bcl-2 protein contents and Bcl-2/Bax decreased, the apoptosis rate and Bax protein contents increased in the model group (all P<0.01). Compared with the model group, the cell viability, Bcl-2 protein contents and Bcl-2/Bax increased, while the apoptosis rate and Bax protein contents decreased in each SSTF treated group (P<0.05, P<0.01). Compared with the low dose SSTF group, significant difference existed in each index of the high dose SSTF group (all P<0.05).</p><p><b>CONCLUSIONS</b>SSTF had protection on hypoxia/reoxygenation induced cardiocyte apoptosis. Its protective mechanism might be correlated with its up-regulation of the expression of Bcl-2 protein ahd down-regulation of the expression of Bax protein.</p>