• Natural Product Sciences
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• v.13 no.3
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• pp.190-194
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• 2007

Two new flavonoid compounds, 8,8'-bisbaicalein 1 and baicalein-7-O-caffeate 2 along with six known flavonoids, baicalein, chrysin, scutellarein, 6-hydroxyluteolin, 6-methoxyluteolin and baicalein-7-Oglucoside and ${\beta}-sitosterol$ have been isolated from the stem-bark of Oroxylum indicum (Bignoniaceae) and identified on the basis of spectroscopic and chemical studies. 6-Hydroxyluteolin and 6-methoxyluteolin are reported for the first time from this plant.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.6
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• pp.2729-2734
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• 2012

Despite clinical advances in anticancer therapy, there is still a need for novel anticancer metabolites, with higher efficacy and lesser side effects. Oroxylum indicum (L.) Vent. is a small tree of the Bignoniaceae family which is well known for its food and medicinal properties. In present study, the chemopreventive properties of O. indicum hot and cold non-polar extracts (petroleum ether and chloroform) were investigated with MDA-MB-231 (cancer cells) and WRL-68 (non-tumor cells) by XTT assay. All the extracts, and particularly the petroleum ether hot extract (PHO), exhibited significantly (P<0.05) higher cytotoxicity in MDA-MB-231 when compared to WRL-68 cells. PHO was then tested for apoptosis induction in estrogen receptor (ER)-negative (MDA-MB-231) and ER-positive (MCF-7) breast cancer cells by cellular DNA fragmentation ELISA, where it proved more efficient in the MDA-MB-231 cells. Further, when PHO was tested for anti-metastatic potential in a cell migration inhibition assay, it exhibited beneficial effects. Thus non-polar extracts of O. indicum (especially PHO) can effectively target ER-negative breast cancer cells to induce apoptosis, without harming normal cells by cancer-specific cytotoxicity. Hence, it could be considered as an extract with candidate precursors to possibly harness or alleviate ER-negative breast cancer progression even in advanced stages of malignancy.

• Biomolecules & Therapeutics
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• v.24 no.3
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• pp.283-290
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• 2016

Oroxylum indicum has long been used in Asian traditional medicine to prevent and treat respiratory diseases, diabetes, diarrhea and other conditions. Oroxylin A is a flavone that is present in Oroxylum indicum and in Scutellaria baicalensis. Because the root extracts of both plants have been shown to have anti-allergic effects, the authors investigated whether oroxylin A is likely to have beneficial effects on allergic asthma using female Balb/c mice and rat RBL-2H3 mast cells. Antigen-induced degranulation was measured in vitro by measuring b-hexosaminidase activity. A murine ovalbumin-induced allergic asthma model was used to test the in vivo efficacy of oroxylin A. Sensitization and challenge of ovalbumin induced allergic asthma responses, the accumulations of eosinophils and Th2 cytokine levels in bronchoalveolar lavage fluid and lung tissues. Oroxylin A administration decreased numbers of inflammatory cells, especially eosinophils, and reduced the expression and secretion of Th2 cytokines, including IL-4 and IL-13, in lung tissues and bronchoalveolar lavage fluid. Histologic studies showed oroxylin A reduced inflammatory signs and mucin production in lungs. These findings provide evidence that oroxylin A has potential use as an anti-allergic therapeutic.

• Natural Product Sciences
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• v.18 no.1
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• pp.47-51
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• 2012

Among 38 Vietnamese medicinal plant extracts investigated for their ${\alpha}$-glucosidase inhibitory activity, 35 extracts showed $IC_{50}$ values below $250{\mu}g/mL$. The MeOH extracts of the heartwood of Oroxylum indicum, the seeds of Caesalpinia sappan, and the fruits of Xanthium strumarium exhibited strong ${\alpha}$-glucosidase inhibitory activity with $IC_{50}$ values less than $50{\mu}g/mL$. Fractionation of the MeOH extract of the heartwood of O. indicum led to the isolation of oroxylin A (1), oroxyloside (2), hispidulin (3), apigenin (4), ficusal (5), balanophonin (6), 2- (1-hydroxymethylethyl)-4H,9H-naphtho[2,3-b]furan-4,9-dione (7), salicylic acid (8), p-hydroxybenzoic acid (9), protocatechuic acid (10), isovanillin (11), and ${\beta}$-hydroxypropiovanillon (12). Compounds 1 - 3, 5, 6, 8, 10, and 12 showed more potent activities, with $IC_{50}$ values ranging from 2.13 to $133.51{\mu}M$, than a positive control acabose ($IC_{50}$, $241.85{\mu}M$). The kinetic study indicated that oroxyloside (2) displayed mixed-type inhibition with inhibition constant (Ki) was $3.56{\mu}M$.

• Korean Journal of Pharmacognosy
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• v.41 no.4
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• pp.289-296
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• 2010

Aldose reductase (AR), the principal enzyme of the polyol pathway, has been shown to play an important role in the development of the diabetic complications. Evaluating natural sources for ARI potential may lead to the development of safer and more effective agents against diabetic complications. Sixty four Chinese herbal medicines have been investigated for inhibitory activities on AR. Among them, thirteen herbal medicines, Inula helianthus-aquatilis C. Y. Wu ex Ling. (whole plant), Erigeron breviscapus (Vant.) Hand. Mazz. (whole plant), Lonicera hypoglauca Miq. (leaf, stem), Scutellaria orthocalyx Hang. Mazz. (whole plant), Berchemia floribunda Brongn. (leaf, stem), Michelia alba DC. (flower), Oroxylum indicum (seed), Punica granatum L. (peel), Elsholtzia capituligera (whole plant), Trachelospermum jasminoides (Lindl.) Lem. (whole plant), Elsholtzia strobilifera Benth. (whole plant), Agrimonia pilosa var. nepalensis (D. Don) Nakai (whole plant) and Aster poliothamnus Diels (whole plant) exhibited a significant inhibitory activity against AR. Particularly, Inula helianthus-aquatilis C. Y. Wu ex Ling. showed seven times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

• Molecular & Cellular Toxicology
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• v.4 no.4
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• pp.331-337
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• 2008

This study was conducted to quantitatively evaluate the recovery effects of herbal medicines on acetaminophen-induced hepatotoxicity. In the present study, the recovery effects of 251 herbal medicines on THLE-2 cells that had been damaged by acetaminophen were evaluated using an MTS assay. THLE-2 cells were cultured in 96-well plates and then pretreated with or without 60 ${\mu}M$ acetaminophen (${IC}_{50}$ value: 35.84) for 1 hr. Next, different herbal medicines were added to the wells, after which the cells were reincubated at $37^{\circ}C$ for 24 hr. After first round of screening, the candidate herbal medicines were selected based on a recovery rate of greater than 40% and their efficacy were then determined by dose response kinetic analysis. Among these extracts, 8 herbal medicines (Terminalia chebula, Pueraria lobata, Acronychia laurifolia, Lopatherum gracile, Oroxylum indicum, Cynanchum atratum, Senecio scandens, and Sophora flavescens) had a strong recovery effect on acetaminophen-induced damage in THLE-2 cells. Dose response non-linear regression analysis demonstrated that Senecio scandens showed the best recovery rate (98%), and that its ${EC}_{50}$ was 19.54 ng/mL. Additional studies of these herbal medicines should be conducted to determine if they possess novel therapeutic agents for the prevention or treatment of liver disorders.

• The Korean Journal of Physiology and Pharmacology
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• v.19 no.5
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• pp.441-449
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• 2015

Flavonoids are plant pigments that have been demonstrated to exert various pharmacological effects including anti-cancer, anti-diabetic, anti-atherosclerotic, anti-bacterial, and anti-inflammatory activities. However, the molecular mechanisms in terms of exact target proteins of flavonoids are not fully elucidated yet. In this study, we aimed to evaluate the anti-inflammatory mechanism of scutellarein (SCT), a flavonoid isolated from Erigeron breviscapus, Clerodendrum phlomidis and Oroxylum indicum Vent that have been traditionally used to treat various inflammatory diseases in China and Brazil. For this purpose, a nitric oxide (NO) assay, polymerase chain reaction (PCR), nuclear fractionation, immunoblot analysis, a kinase assay, and an overexpression strategy were employed. Scutellarein significantly inhibited NO production in a dose-dependent manner and reduced the mRNA expression levels of inducible NO synthase (iNOS) and tumor necrosis factor (TNF)-${\alpha}$ in lipopolysaccharide (LPS)-activated RAW264.7 cells. In addition, SCT also dampened nuclear factor (NF)-${\kappa}B$-driven expression of a luciferase reporter gene upon transfection of a TIR-domain-containing adapter-inducing interferon-${\beta}$ (TRIF) construct into Human embryonic kidney 293 (HEK 293) cells; similarly, NF-${\kappa}B$ nuclear translocation was inhibited by SCT. Moreover, the phosphorylation levels of various upstream signaling enzymes involved in NF-${\kappa}B$ activation were decreased by SCT treatment in LPS-treated RAW264.7 cells. Finally, SCT strongly inhibited Src kinase activity and also inhibited the autophosphorylation of overexpressed Src. Therefore, our data suggest that SCT can block the inflammatory response by directly inhibiting Src kinase activity linked to NF-${\kappa}B$ activation.