Identifying Anti-NSCLC Bioactive Compounds in Scutellaria via 2D NMR-Based Metabolomic Analysis of Pharmacologically Classified Crude Extracts.

We presented a strategy utilizing 2D NMR-based metabolomic analysis of crude extracts, categorized by different pharmacological activities, to rapidly identify the primary bioactive components of TCM. It was applied to identify the potential bioactive components from Scutellaria crude extracts that exhibit anti-non-small cell lung cancer (anti-NSCLC) activity. Four Scutellaria species were chosen as the study subjects because of their close phylogenetic relationship, but their crude extracts exhibit significantly different anti-NSCLC activity. Cell proliferation assay was used to assess the anti-NSCLC activity of four species of Scutellaria. 1H-13C HSQC spectra were acquired for the chemical profiling of these crude extracts. Based on the pharmacological classification (PCA, OPLS-DA and univariate hypothesis test) were performed to identify the bioactive constituents in Scutellaria associated with the anti-NSCLC activity. As a result, three compounds, baicalein, wogonin and scutellarin were identified as bioactive compounds. The anti-NSCLC activity of the three potential active compounds were further confirmed via cell proliferation assay. The mechanism of the anti-NSCLC activity by these active constituents was further explored via flow cytometry and western blot analyses. This study demonstrated 2D NMR-based metabolomic analysis of pharmacologically classified crude extracts to be an efficient approach to the identification of active components of herbal medicine.

Scutellarin, a flavonoid compound from Scutellaria barbata, suppresses growth of breast cancer stem cells in vitro and in tumor-bearing mice.

BACKGROUND: Scutellaria barbata D. Don (SB), commonly known as Ban Zhi Lian and firstly documented by Shigong Chen, is a dried whole plant that has been studied for its therapeutic effects on breast cancer, colon cancer, and prostate cancer. Among its various compounds, scutellarin (SCU) has been demonstrated with anti-tumor effects. PURPOSE: This study aimed to evaluate the effects of SB water extract (SBW) and scutellarin on breast cancer stem cells (BCSCs), and to investigate their potential therapeutic effects on breast tumors in mice. METHODS: BCSCs were enriched from human breast cancer cells (MDA-MB-231 and MDA-MB-361) and their characteristics were analyzed. The effects of varying concentrations of SBW and scutellarin on cell viability, proliferation, self-renewal, and migration abilities were studied, along with the underlying mechanisms. The in vivo anti-tumor effects of scutellarin were further evaluated in SCID/NOD mice. Firstly, mice were inoculated with naïve BCSCs and subjected to treatment with scutellarin or vehicle. Secondly, BCSCs were pre-treated with scutellarin or vehicle prior to inoculation into mice. RESULTS: The derived BCSCs expressed CD44, CD133 and ALDH1, but not CD24, indicating that BCSCs have been successfully induced from both MDA-MB-231 and MDA-MB-361 cells. Both SBW and scutellarin reduced the viability, proliferation, sphere and colony formation, and migration of BCSCs. In mice with tumors derived from naïve BCSCs, scutellarin significantly reduced tumor growth, expression of proliferative (Ki67) and stem cell markers (CD44), and lung metastasis. In addition, pre-treatment with scutellarin also slowed tumor growth. Western blot results suggested the involvement of Wnt/ß-catenin, NF-κB, and PTEN/Akt/mTOR signaling pathways underlying the inhibitory effects of scutellarin. CONCLUSION: Our study demonstrated for the first time that both SB water extract and scutellarin could reduce the proliferation and migration of BCSCs in vitro. Scutellarin was shown to possess novel inhibitory activities in BCSCs progression. These findings suggest that Scutellaria barbata water extract, in particular, scutellarin, may have potential to be further developed as an adjuvant therapy for reducing breast cancer recurrence.

In Vitro Assessment of Cortisol Release Inhibition, Bioaccessibility and Bioavailability of a Chemically Characterized Scutellaria lateriflora L. Hydroethanolic Extract.

Excess cortisol release is associated with numerous health concerns, including psychiatric issues (i.e., anxiety, insomnia, and depression) and nonpsychiatric issues (i.e., osteoporosis). The aim of this study was to assess the in vitro inhibition of cortisol release, bioaccessibility, and bioavailability exerted by a chemically characterized Scutellaria lateriflora L. extract (SLE). The treatment of H295R cells with SLE at increasing, noncytotoxic, concentrations (5-30 ng/mL) showed significant inhibition of cortisol release ranging from 58 to 91%. The in vitro simulated gastric, duodenal, and gastroduodenal digestions, induced statistically significant reductions (p < 0.0001) in the bioactive polyphenolic compounds that most represented SLE. Bioavailability studies on duodenal digested SLE, using Caco-2 cells grown on transwell inserts and a parallel artificial membrane permeability assay, indicated oroxylin A glucuronide and oroxylin A were the only bioactive compounds able to cross the Caco-2 cell membrane and the artificial lipid membrane, respectively. The results suggest possible applications of SLE as a food supplement ingredient against cortisol-mediated stress response and the use of gastroresistant oral dosage forms to partially prevent the degradation of SLE bioactive compounds. In vivo studies and clinical trials remain necessary to draw a conclusion on the efficacy and tolerability of this plant extract.

Primary study on the effects and mechanisms of separate and combined decoctions of Scutellaria baicalensis Georgi - Coptis chinensis Franch extracts in relieving acute alcoholic liver injury in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Scutellaria baicalensis Georgi (SBG) and Coptis chinensis Franch (CCF) are traditional herbal medicine pairs used for clearing heat and eliminating dampness, stopping diarrhea, and detoxification. Traditionally, these two herbs are combined and decocted together, but the modern preparation procedures separate them to avoid the large amount of precipitation generated from co-decoction. Thus, a conflict lies between the traditional and modern extraction processes of Scutellaria baicalensis Georgi - Coptis chinensis Franch (SBG-CCF). AIM OF STUDY: There is a conflict between traditional medical practices of SBG-CCF and the modern formulation industry. In this study, we investigated the differences in the effects and mechanisms of SBG-CCF extracted by decocting separately and combining decoctions, as well as the scientific effectiveness of traditional and modern treatment methods on both. Acute alcoholic liver injury (ALI) rats were used as the pathological model. MATERIALS AND METHODS: SD rats were divided into 8 groups, including blank group, model group, low, medium, and high dose groups of SBG-CCF separated decoction, low, medium, and high dose groups of SBG-CCF combined decoction. Acute alcoholic liver injury model was induced in rats by gradually increasing the dose of alcohol through gavage everyday using white wine with an alcohol content 52%. Aspartate aminotransferase (AST), alanine aminotransferase (ALT), total cholesterol (TC), triglyceride (TG), lactate dehydrogenase (LDH), malondialdehyde (MDA), superoxide dismutase (SOD), and reduced glutathione (GSH) were used as indicators to assess the intervention effect of SBG-CCF. And the potential active ingredients of SBG-CCF and the targets related to ALI were screened using network pharmacology, and the prediction results of network pharmacology were verified by quantitative real-time fluorescence PCR (qRT-PCR). RESULTS: SBG-CCF decoction alone and six combinations of decoctions have different degrees of improvement on alcoholic liver injury, with significant efficacy in the middle-dose group, and the combined decoction was superior to the individual decoction. SBG-CCF gavage can reduce the activity of AST, ALT, TC, TG, LDH, and MDA in the serum and liver of ALI rats, while increasing the levels of SOD and GSH. Network pharmacological analysis identified 39 active components, mainly flavonoids and alkaloids. Enrichment analysis suggested that SBG-CCF may treat ALI through the regulation of tumor necrosis factor (TNF), mitogen-activated protein kinase (MAPK), interleukin-17 (IL-17), apoptosis, and the Toll-like receptor signaling pathways. The key targets in the Disease-Signaling Pathway-Target Network were MAPK8, IKBKB, MAPK10, MAPK3, MAPK1, and AKT1. qRT-PCR results indicated that targets regulating inflammation and lipid metabolism are MAPK8, MAPK10, MAPK3, and AKT1. CONCLUSION: SBG-CCF separately extracts and combines decoction can alleviate acute alcoholic liver injury, and the effect of combined decoction is more significant than separate decoction, implying that the precipitate produced by the combination of the two is also an active substance. The resistance mechanism of SBG-CCF ALI may be related to the modulation of lipid metabolism, inhibition of lipid peroxidation, and oxidative stress. SBG-CCF has the characteristics of multi-component, multi-pathway, and multi-target resistance to ALI.

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.

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.

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.

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.

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.

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

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(AU)

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(AU)

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.

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).

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.

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.

Study on chemical constituents of Scutelliaria regeliana / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents in ethyl acetate fraction from the root of Scutelliaria regeliana.</p><p><b>METHOD</b>The compounds were isolated by silica gel column chromatography and HPLC, and their structures were elucidated by means of spectral analyses.</p><p><b>RESULT</b>23 compounds were isolated and identified.</p><p><b>CONCLUSION</b>Compound 1 is new, named as scutellariae flavonol, and the others were isolated from S. regeliana for the first time.</p>

Effects of baicalin against oxidative stress injury of SH-SY5Y cells by up-regulating SIRT1 / 药学学报

This study is to investigate the effect of baicalin (BL) against oxidative injury stress of SH-SY5Y cells induced by H2O2 and the possible mechanism. SH-SY5Y cells were pre-incubated with baicalin (25, 50, and 100 micromol x L(-1)) for 12 h prior to exposure to H2O2 (150 micromol x L(-1)) for 24 h. The viability of SH-SY5Y cells was measured by MTT assay. The contents of LDH and NO were determined. The percentage of apoptotic cells was assessed by flow cytometry (FCM). The content of Caspase-3 was tested by immunofluorescence histochemical method. BL at 50 and 100 micromol x L(-1) separately increased the cell viability and up-regulated SIRT1, reduced the contents of LDH, NO, Caspase-3 and the apoptotic percentage of SH-SY5Y cells. This study results suggest that baicalin could inhibit the H2O2-induced neuronal apoptosis. The further mechanism studies show that baicalin inhibit apoptosis via reducing Caspase-3 expression and up-regulating SIRT1.

Scutellaria baicalensis Inhibits Mast Cell-Mediated Anaphylactic Reactions / 체질인류학회지

Mast cells play a critical role in the effector phase of immediate hypersensitivity and allergic diseases. Scutellaria baicalensis is a widely used herb in traditional oriental medicine with anticancer, antiviral, antibacterial and anti-inflammatory properties. However, the roles of Scutellaria baicalensis in mast cell-mediated anaphylactic reactions have not fully been investigated. In this study, we examined the influences of the methanol extract of Scutellaria baicalensis (MESB) on compound 48/80- or anti-dinitrophenyl (DNP) IgE-induced anaphylaxis-like response in vivo. To further prove these in vivo results, the inhibitory effect of MESB on mast cell activation was evaluated, focusing on the histamine release from rat peritoneal mast cells (RPMC). MESB inhibited compound 48/80-induced systemic anaphylaxis-like reaction, plasma histamine release and ear swelling response in mice. MESB also attenuated passive systemic and cutaneous anaphylaxis evoked by anti-DNP IgE. In in vitro experiments, MESB dose-dependently reduced histamine release from RPMC activated by compound 48/80 or anti-DNP IgE. Moreover, compound 48/80-elicited calcium uptake was suppressed in a concentration-dependent manner of MESB. Furthermore, MESB transiently increased the level of intracellular cAMP. From these results, it is suggested that MESB possesses effective anti-anaphylactic activity.

Determination of baicalin in Shuanghuanglian oral liquid on composite mercury film electrode based on chemical modified / 中国中药杂志

<p><b>OBJECTIVE</b>A novel Eu-PB composite mercury film electrode (GC/Eu-PB/MFE) based on chemical modified was developed for the determination of baicalin and the investigation of its the electrochemical behavior.</p><p><b>METHOD</b>Cyclic voltammetry and differential pulse voltammetry were used.</p><p><b>RESULT</b>The adsorption characteristic of baicalin was observed in Britton-Robinson buffer solution (pH 6.0) at GC/Eu-PB/MFE. The reduction peak of baicalin was observed at -1.22 V (vs SCE) and peak current was linear to the baicalin from 8.0 x 10(-9) to 1.0 x 10(-6) mol x L(-1) (r = 0.9992, n=8). The limit of detection was 1.2 x 10(-9) mol x L(-1) (S/N = 3). The average recovery was 99.83%, with RSD of 2.3% (n=8). The baicalin in Shuanghuanglian oral can be directly determined without pretreatment.</p><p><b>CONCLUSION</b>The GC/Eu-PB/MFE was used to determine baicalin in Shuanghuanglian oral with good repeatability and high sensitivity. The method can be used for the quality control of Chinese traditional medicines containing Scutellaria baicalensis.</p>