Scutellaria Baicalensis Root Research Articles

Baicalein suppresses inflammation and attenuates acute lung injury by inhibiting glycolysis via HIF‑1α signaling.

Baicalein, a flavonoid monomer compound isolated from the dried root of the traditional Chinese herb Scutellaria baicalensis, has several pharmacological activities, such as anti‑inflammatory, anti‑angiogenic, antitumor, antimicrobial and antiviral properties. Acute lung injury (ALI) is characterized by injury of the alveolar epithelium and capillary endothelium, which results in decreased lung volume, decreased lung compliance, ventilation/perfusion mismatch, intrapulmonary edema, alveolar edema and even acute hypoxemic respiratory failure. The present study aimed to investigate the effects of baicalein on lung injury and inflammation. Bioinformatics analysis using network pharmacology predicted that the hypoxia inducible factor‑1α (HIF‑1α) and glycolysis signaling pathways were involved in the mechanism underlying the therapeutic effects of baicalein. Further in vitro and in vivo experiments, such as immunohistochemistry, immunofluorescence and PCR, verified that baicalein could inhibit HIF‑1α signaling, thus suppressing glycolysis, and improving inflammatory responses and ALI. Taken together, the results of the present study suggested that the anti‑inflammatory effects of baicalein on treating ALI were associated with its ability to suppress glycolysis via the HIF‑1α signaling pathway.

ANTI-OXIDANT, ANTI-BACTERIAL, AND ANTI-INFLAMMATORY ACTIVITY OF Scutellaria baicalensis ROOT SUPERCRITICAL FLUID EXTRACTS

Scutellaria baicalensis (S. baicalensis) root extract has been used for a long time in Oriental medicine and the cosmetics industry due to its natural anti-oxidant properties in disease treatment. However, comprehensive studies comparing the physiological activities of different S. baicalensis root extracts are lacking. Specifically, there is a need to compare S. baicalensis root hydrothermal extract (SBHE), S. baicalensis root 75% ethyl alcohol extract (SBAE), and S. baicalensis root supercritical fluid extracts (SBSEs) simultaneously. In this study, we extracted S. baicalensis roots using three different methods: hydrothermal, 75% ethyl alcohol, and supercritical fluid extraction. We then evaluated their radical scavenging activities, SOD-like activity, anti-bacterial activities, and the production of inflammatory factors. Among the extracts tested, the S. baicalensis root supercritical fluid 35°C extract (SBSE35) exhibited superior overall physiological activities. Notably, only the SBSEs demonstrated anti-bacterial activity against Staphylococcus aureus, whereas SBHE and SBAE did not. SBHE and SBAE increased interleukin (IL)-6 levels (p ≤ 0.05). Additionally, SBHE and SBAE showed a slight decrease in IL-8 at low concentrations, but an increase in IL-8 production in a concentration-dependent manner. In contrast, SBSE35 significantly reduced both IL-6 and IL-8 levels (p ≤ 0.05). These findings suggest that SBSE35 has greater potential for improving human health in the cosmetics and pharmaceutical fields. Keywords: Scutellaria baicalensis root; supercritical fluid extraction; anti-oxidant; anti-bacterial; anti-inflammation

The Effect of the Extraction Conditions on the Antioxidant Activity and Bioactive Compounds Content in Ethanolic Extracts of Scutellaria baicalensis Root.

Ethanolic extracts of Baikal skullcap (Scutellaria baicalensis) root were obtained using various techniques, such as maceration, maceration with shaking, ultrasound-assisted extraction, reflux extraction, and Soxhlet extraction. The influence of the type and time of isolation technique on the extraction process was studied, and the quality of the obtained extracts was determined by spectrophotometric and chromatographic methods to find the optimal extraction conditions. Radical scavenging activity of the extracts was analyzed using DPPH assay, while total phenolic content (TPC) was analyzed by the method with the Folin-Ciocalteu reagent. Application of gas chromatography with mass selective detector (GC-MS) enabled the identification of some bioactive substances and a comparison of the composition of the particular extracts. The Baikal skullcap root extracts characterized by both the highest antioxidant activity and content of phenolic compounds were obtained in 2 h of reflux and Soxhlet extraction. The main biologically active compounds identified in extracts by the GC-MS method were wogonin and oroxylin A, known for their broad spectrum of biological effects, including antioxidant, anti-inflammatory, antiviral, anticancer, and others.

Baicalein alleviates cardiomyocyte death in EAM mice by inhibiting the JAK-STAT1/4 signalling pathway

BackgroundThe experimental autoimmune myocarditis (EAM) model is valuable for investigating myocarditis pathogenesis. M1-type macrophages and CD4+T cells exert key pathogenic effects on EAM initiation and progression. Baicalein (5,6,7-trihydroxyflavone, C15H10O5, BAI), which is derived from the Scutellaria baicalensis root, is a primary bioactive compound with potent anti-inflammatory and antioxidant properties. BAI exerts good therapeutic effects against various autoimmune diseases; however, its effect in EAM has not been thoroughly researched. PurposeThis study aimed to explore the possible inhibitory effect of BAI on M1 macrophage polarisation and CD4+T cell differentiation into Th1 cells via modulation of the JAK-STAT1/4 signalling pathway, which reduces the secretion of pro-inflammatory factors, namely, TNF-α and IFN-γ, and consequently inhibits TNF-α- and IFN-γ-triggered apoptosis in cardiomyocytes of the EAM model mice. Study design and methodsFlow cytometry, immunofluorescence, real-time quantitative polymerase chain reaction (q-PCR), and western blotting were performed to determine whether BAI alleviated M1/Th1-secreted TNF-α- and IFN-γ-induced myocyte death in the EAM model mice through the inhibition of the JAK-STAT1/4 signalling pathway. ResultsThese results indicate that BAI intervention in mice resulted in mild inflammatory infiltrates. BAI inhibited JAK-STAT1 signalling in macrophages both in vivo and in vitro, which attenuated macrophage polarisation to the M1 type and reduced TNF-α secretion. Additionally, BAI significantly inhibited the differentiation of CD4+T cells to Th1 cells and IFN-γ secretion both in vivo and in vitro by modulating the JAK-STAT1/4 signalling pathway. This ultimately led to decreased TNF-α and IFN-γ levels in cardiac tissues and reduced myocardial cell apoptosis. ConclusionThis study demonstrates that BAI alleviates M1/Th1-secreted TNF-α- and IFN-γ-induced cardiomyocyte death in EAM mice by inhibiting the JAK-STAT1/4 signalling pathway.

Promising Role of the Scutellaria baicalensis Root Hydroxyflavone–Baicalein in the Prevention and Treatment of Human Diseases

Plant roots, due to a high content of natural antioxidants for many years, have been used in herbal medicine. It has been documented that the extract of Baikal skullcap (Scutellaria baicalensis) has hepatoprotective, calming, antiallergic, and anti-inflammatory properties. Flavonoid compounds found in the extract, including baicalein, have strong antiradical activity, which improves overall health and increases feelings of well-being. Plant-derived bioactive compounds with antioxidant activity have for a long time been used as an alternative source of medicines to treat oxidative stress-related diseases. In this review, we summarized the latest reports on one of the most important aglycones with respect to the pharmacological activity and high content in Baikal skullcap, which is 5,6,7-trihydroxyflavone (baicalein).

New Insights into Baicalein's Effect on Chlorpyrifos-Induced Liver Injury in Carp: Involving Macrophage Polarization and Pyropto sis.

Chlorpyrifos (CPF) is widely used in agriculture, plants, and buildings to kill pests and worms. Excessive environmental residues of CPF will result in soil and ecological contamination and toxicity to animals and humans. Baicalein (Bai), derived from the root of natural Scutellaria baicalensis, is a potent anti-inflammatory, antioxidant, and antitumor agent. The objective of this paper is to investigate the molecular mechanism by which Bai prevents CPF-induced hepatotoxic injury. Carp were kept in water containing CPF (23.2 μg/L) and/or fed diets containing Bai (0.15 g/kg). We found that Bai attenuated liver tissue damage and vacuolization caused by CPF. We confirmed that CPF causes M1/M2 polarization imbalance in macrophages and hepatocyte pyroptosis, which ultimately leads to liver injury. Further exploration of the internal mechanism shows that CPF participates in liver toxicity damage by destroying the AMPK/SIRT1/pGC-1α pathway and causing mitochondrial biogenesis and mitochondrial dynamics imbalance. Notably, Bai significantly attenuated CPF-induced inhibition of the AMPK/SIRT1/pGC-1α pathway. In summary, our results suggest that Bai alleviates CPF exposure-induced inhibition of the AMPK/SIRT1/pGC-1α pathway, thereby attenuating macrophage M1 hyperpolarization and pyroptosis by inhibiting the NF-κB pathway. These results may provide new insights into the detoxification mechanism of Bai on the same type of organophosphorus pesticides.

Combined Effects of Methyldopa and Baicalein or Scutellaria baicalensis Roots Extract on Blood Pressure, Heart Rate, and Expression of Inflammatory and Vascular Disease-Related Factors in Spontaneously Hypertensive Pregnant Rats.

The aim of the study was to investigate the effect of baicalein or Scutellaria baicalensis root extract interaction with methyldopa in pregnant spontaneously hypertensive rats (SHR) at the pharmacodynamic, molecular, and biochemical levels. The rats, after confirming pregnancy, received baicalein (200 mg/kg/day, p.o.) and extract (1000 mg/kg/day, p.o.), in combination with methyldopa (400 mg/kg/day; p.o.), for 14 consecutive days, 1 h before blood pressure and heart rate measurements. In the heart and placenta from mothers after giving birth to their offspring, mRNA expression of factors related to inflammatory processes (TNF-α, Il-1β, IL-6) and vascular diseases (TGF-β, HIF-1α, VEGF, PlGF) was measured. Levels of markers of oxidative stress (superoxide dismutase and malondialdehyde) in the placenta and indicators of myocardial damage (troponin cTnC and cTnI, creatine kinase, myoglobin, and lactate dehydrogenase) in the heart were also assessed. Baicalein co-administered with methyldopa was associated with reduced blood pressure, especially during the first three days. The interactions were more pronounced for such factors as TGF-β, HIF-1α, VEGF, and PlGF than TNF-α, Il-1β, and IL-6. Combined application of baicalein and extract with methyldopa may be of value in the development of a new antihypertensive medication intended for patients suffering from preeclampsia or pregnancy-induced hypertension.

Postharvest UV-A radiation affects flavonoid content, composition, and bioactivity of Scutellaria baicalensis root

Ultraviolet A (UV-A) radiation is the main component of solar radiation and can elicit a wide range of biochemical responses in plants. In this study, the effects of UV-A radiation on the flavonoid content, composition, and bioactivity in postharvest Scutellaria baicalensis roots were investigated. The total flavonoid content in S. baicalensis roots under postharvest UV-A radiation increased in a time-dependent manner and reached its maximum value (183.64 g kg−1) on the fifth day. Compared with the control group, the contents of four main flavonoids—baicalin, baicalein, wogonoside, and wogonin increased by 1.68 times, 3.00 times, 2.07 times, and 1.57 times, respectively; and new chemicals including pectolinarigenin, puerarin, isokaempferide, and jaceosidin were detected after 5 d of UV-A radiation. In addition, extracts of S. baicalensis roots exposed to postharvest UV-A radiation showed stronger antioxidant and antibacterial activities than control root extracts. Further correlation analysis revealed that baicalin and baicalein contents in the roots of S. baicalensis after postharvest UV-A radiation were positively correlated with antioxidant activity, while the main flavonoids showed different correlations with various bacteria. These results suggest that the appropriate duration of postharvest UV-A radiation is an effective way to enhance bioactive compound contents and their bioactivities in S. baicalensis roots.

Combined Phyllostachys pubescens and Scutellaria baicalensis Prevent High-Fat Diet-Induced Obesity via Upregulating Thermogenesis and Energy Expenditure by UCP1 in Male C57BL/6J Mice

This study examined the anti-obesity effects of a Phyllostachys pubescens (leaf) and Scutellaria baicalensis root mixture (BS21), and its underlying mechanisms of action, in high-fat diet (HFD)-induced obese mice. Mice were fed a HFD with BS21 (100, 200, or 400 mg/kg) for 9 weeks. BS21 reduced body weight, white adipose tissue (WAT) and liver weights, liver lipid accumulation, and adipocyte size. Additionally, BS21 reduced serum concentrations of non-esterified fatty acid, triglyceride, glucose, lactate dehydrogenase, low-density lipoprotein cholesterol, total cholesterol, leptin, and insulin growth factor 1, but elevated the adiponectin concentrations. Furthermore, BS21 suppressed the mRNA levels of lipogenesis-related proteins, such as peroxisome proliferator–activated receptor (PPAR) γ, SREBP-1c, C/EBP-α, fatty acid synthase, and leptin, but increased the mRNA gene expression of lipolysis-related proteins, such as PPAR-α, uncoupling protein (UCP) 2, adiponectin, and CPT1b, in WAT. In addition, BS21 increased the cold-stimulated adaptive thermogenesis and UCP1 protein expression with AMPK activation in adipose tissue. Furthermore, BS21 increased the WAT and mRNA expression of energy metabolism-related proteins SIRT1, PGC-1α, and FNDC5/irisin in the quadriceps femoris muscle. These results suggest that BS21 exerts anti-obesity and antihyperlipidemic activities in HFD-induced obese mice by increasing the thermogenesis and energy expenditure, and regulating lipid metabolism. Therefore, BS21 could be useful for preventing and treating obesity and its related metabolic diseases.

Development and Evaluation of Thermosensitive Hydrogels with Binary Mixture of Scutellariae baicalensis radix Extract and Chitosan for Periodontal Diseases Treatment.

Scutellaria baicalensis root displays anti-inflammatory and antibacterial properties due to the presence of flavonoids, particularly baicalin, baicalein, and wogonin. Our work aimed at developing thermosensitive hydrogels containing a binary mixture of S. baicalensis radix lyophilized extract and chitosan as a novel approach for periodontal diseases treatment. Two types of chitosan were employed in preliminary studies on binary mixtures with S. baicalensis radix lyophilized extract standardized for baicalin, baicalein, and wogonin. Thermosensitive hydrogels were prepared of poloxamer 407, alginate sodium, and cellulose derivatives and evaluated in terms of rheological and mucoadhesive behavior. The presence of chitosan altered the release profile of active compounds but did not affect their in vitro permeation behavior in PAMPA assay. The synergistic effects of S. baicalensis radix lyophilized extract and chitosan toward ferrous ion-chelating activity, inhibition of hyaluronidase, and pathogen growth were observed. The thermosensitive gelling system showed shear-thinning properties, gelation temperature between 25 and 27 °C, and favorable mucoadhesiveness in contact with porcine buccal mucosa, which was enhanced in the presence of binary mixture of S. baicalensis radix extract and chitosan. The release tests showed that baicalin and baicalein were liberated in a prolonged manner with a fast onset from hydrogel formulations.

Propylene Glycol Improves Stability of the Anti-Inflammatory Compounds in Scutellaria baicalensis Extract

Scutellaria baicalensis root extracts have been useful for external skin care and have been commercialized for years. Here, a comprehensive study was conducted to investigate the difference between 20% propylene glycol (PG) and water used as the storage solvent for a time course analysis of their remaining biological activities and ingredient compositions versus their freshly prepared conditions. Of the four major components in the 20% PG solvent, more than 80% of the components were retained after storage for two months, but in water only baicalin and wogonin were retained. The relative antibacterial activities, antioxidant properties and anti-inflammatory activities of the 20% PG solvent group were better than those of the water solvent group. Taken together, we demonstrated that these activities improved when PG, a common solvent used in many product formulas, was used as the storage solvent for the S. baicalensis extract.

Anti-inflammatory activity of Scutellaria Baicalensis root extract in lipopolysaccharide-induced RAW 264.7 cells

Anti-inflammatory activity of Scutellaria Baicalensis root extract in lipopolysaccharide-induced RAW 264.7 cells

Pharmaceutical Advantages of GenoTX-407, A Combination of Extracts from Scutellaria baicalensis Root and Magnolia officinalis Bark.

Background: Extracts of Scutellaria baicalensis root (SBR) and Magnolia officinalis barks (MOB) possess significant antioxidant, anti-inflammatory, and antimicrobial properties; however, these also exert adverse effects such as cytotoxicity. To overcome the adverse effects, we formulated a combination of the extracts, named GenoTX-407, with SBR and MOB extracts mixed in 5:1 ratio. The antioxidant, antimicrobial, and anti-inflammatory activities of SBR and MOB extracts and GenoTX-407 were evaluated. Methods: To optimize the extraction conditions of SBR and MOB, different ethanol concentrations and extraction times and treatments of the extracts with different solvents for varying time periods were tested. Anti-inflammatory activity was assessed via NO scavenging assay and analysis of anti-inflammatory activity-related gene expression in RAW 264.7 cells. Agar disk diffusion and microdilution assays were used to determine the antimicrobial activity. Antioxidant activity was evaluated through DPPH assay and analyses of peroxidation and antioxidant-related protein expression in HeLa cells. Results: Extraction with 0% ethanol for 2 h and 1.5% phosphoric acid for 0.5 h yielded maximum SBR extracts. For MOB, 50% ethanol extraction for 2 h followed by further extraction in hexane for 0.5 h yielded the highest extracts. SBR (46.1 ± 0.9 %) and MOB (48.9 ± 1.0 %) extracts effectively inhibited NO production, and dose-dependently reduced the expression of TNF-α, iNOS, NF-κB, COX2, and IL-6. MOB and GenoTX-407 inhibited the growth of Escherichia coli, Staphylococcus aureus, Candida albicans, and Propionibacterium acnes, as evidenced in disk diffusion and microdilution assays. SBR (EC50, 107.7 µg/mL and 38.3 µg/mL), MOB (62.41 µg/mL and 72.45 µg/mL), and GenoTX-407 (7.7 µg/mL and 26.4 µg/mL) exhibited excellent antioxidant potency and could scavenge free radicals of DPPH and lipid peroxidation; additionally, SOD, CAT, HO-1, and Nrf2 expression was increased in HeLa cells. SBR showed more potent antioxidant activity than MOB. Contrastingly, MOB exhibited more potent anti-inflammatory and antimicrobial activities than SBR. Interestingly, GenoTX-407 was the most efficient in all the assays, compared with SBR and MOB. Conclusion: This study demonstrated that GenoTX-407, the combination of SBR and MOB, is a potential drug candidate exerting antioxidant and anti-inflammatory effects via the Nrf2/HO-1 and NF-κB signaling pathways.

An SERS analytical protocol for characterizing native Japanese plant extracts

AbstractThe identification of natural dyes in ancient textiles is a longstanding challenge for scientists; yet, the effort honours the skill and knowledge of master dyers by retracing traditional dyeing methods and assisting in conserving historical treasures for future generations. Here, the main constituents of selected native Japanese extracts from the roots of Lithospermum erythrorhizon and Scutellaria baicalensis, the barks of Phellodendron amurense and Morella rubra, the dried flower bud of Syzygium aromataticum, and the fruit of Terminalia chebula are determined by surface‐enhanced Raman spectroscopy following traditional Japanese extraction methods. The analytical amalgamation of data from SERS examinations on crude extracts and on subsequently refiltered and diluted extracts provides further effective and sensitive results for the combined identification of napthoquinones (shikonin and alkanin), alkaloid (berberine), polyhydroxyflavonoids (baicalin/baicalein, myricetin/myricitrin), diarylheptanoids, allylbenzene (eugenol), and tannins (gallic/ellagic acid). The comparison of results from this analytical protocol with those achieved by the more traditional chromatographic and mass spectrometric method provides and questions data regarding generally accepted marker components and enantioselective discriminations that serve to enrich the database of biological sources of colouring materials to be used in determining historically important Japanese colorants and dyestuffs.

Evaluation of the antioxidant and cytotoxic activities of zinc oxide nanoparticles synthesized using scutellaria baicalensis root

The authors describe a simple green method for the preparation of zinc oxide nanoparticles (ZnONPs) using the aqueous root extract of Scutellaria baicalensis. The synthesized ZnONPs were characterized by UV–Vis spectroscopy, FTIR, TEM, SEM and EDX. They were spherical in shape and with sizes ranging from 33.14–99.03 nm. The ZnONPs produced exhibited significant free radical scavenging effects. An in-vitro study showed a dose-dependent cytotoxic effect on HeLa cells.

Triggering of Autophagy by Baicalein in Response to Apoptosis after Spinal Cord Injury: Possible Involvement of the PI3K Activation.

High level apoptosis induced by spinal cord injury (SCI) evokes serious damage because of the loss and dysfunction of motor neurons. Our previous studies showed that inhibition of autophagy evokes the activation of apoptosis. Interestingly, Baicalein, a medicine with anti-apoptosis activity that is derived from the roots of herb Scutellaria baicalensis, largely induces autophagy by activating phosphatidylinositol 3-kinase (PI3K). In this study, we investigated the effects of intraperitoneal injection of Baicalein on autophagy and apoptosis in SCI mice and evaluated the relationship between autophagy and apoptosis. We demonstrated that Baicalein promoted the functional recovery of motor neurons at 7 d after SCI. In addition, Baicalein enhanced neuronal autophagy and the autophagy-related factor PI3K, while inhibiting the p62 protein. Baicalein treatment decreased neuronal apoptosis at 7 d after SCI. Moreover, when inhibiting autophagy, apoptosis was upgraded by Baicalein treatment after injury. Thus, Baicalein attenuated SCI by inducing autophagy to reduce apoptosis in neurons potentially via activating PI3K.

Synergistic Antitumor Effect of Genitinib (Iressa®) with Flavonoids from the Scutellaria baicalensis Root on the Non-Small Cell Lung Cells

Background: As was reported, gefitinib (Iressa®) showed a strong growth inhibitory effect on non-small-cell lung cancer PC-9 cells with mutant EGFR, but did not so much on A549 cells with wild-type EGFR. Observation: We here demonstrated by isobolograms and combination index analyses that the paired combinations of gefitinib with flavonoids from Wogon (Scutellaria baicalensis root): wogonin, oroxylin A and chrysin exerted synergistic anti-tumor effects against A549 cells. Result: The cell cycle analyses revealed that the combination of gefitinib and oroxylin A in A549 cells induced more apoptotic cells than other paired combinations as well as gefitinib alone. Thus, it is anticipated that oroxylin A could help to enhance the remission rate in the gefitinib therapy for the patients with non-small cell cancer cells with wild-type EGFR which provide a poor prognosis. Conclusion: Since the Wogon flavonoids, wogonin, oroxylin A and chrysin, accelerated the acetylation of Lysine residues of histone proteins, it is suggested that they put forth anti-tumor activities through inhibition of histone deacetylases which mediated the post-translational modification of histones.

Baicalein protects rat insulinoma INS-1 cells from palmitate-induced lipotoxicity by inducing HO-1.

Objectiveβ-Cell dysfunction plays a central role in the pathogenesis of type 2 diabetes (T2D), and the identification of novel approaches to improve β-cell function is essential to treat this disease. Baicalein, a flavonoid originally isolated from the root of Scutellaria Baicalensis, has been shown to have beneficial effects on β-cell function. Here, the authors investigated the molecular mechanism responsible for the protective effects of baicalein against palmitate (PA)-induced impaired β-cell function, and placed focus on the role of heme oxygenase (HO)-1.MethodsRat pancreatic β-cell line INS-1 cells or mouse pancreatic islets were cultured with PA (500 μM) to induce lipotoxicity in the presence or absence of baicalein (50 μM), and the expressions of the ER stress markers, ATF-3, CHOP and GRP78 were detected by Western blotting and/or qPCR. The involvement of HO-1 was evaluated by HO-1 siRNA transfection and using the HO-1 inhibitor ZnPP.ResultsBaicalein reduced PA-induced ER stress and inflammation and enhanced insulin secretion, and these effects were associated with the induction of HO-1. Furthermore, these protective effects were attenuated by ZnPP and by HO-1 siRNA. Pretreatment of PD98059 (an ERK inhibitor) significantly inhibited the protective effects of baicalein and blocked HO-1 induction. On the other hand, CO production by RuCO (a CO donor) ameliorated PA-induced ER stress, suggesting that CO production followed by HO-1 induction may contribute to the protective effects of baicalein against PA-induced β-cell dysfunction.ConclusionBaicalein protects pancreatic β-cells from PA-induced ER stress and inflammation via an ERK-HO-1 dependent pathway. The authors suggest HO-1 induction in pancreatic β-cells appears to be a promising therapeutic strategy for T2D.

HVC1 ameliorates hyperlipidemia and inflammation in LDLR\u2212/\u2212 mice

BackgroundHVC1 consists of Coptidis Rhizoma (dried rhizome of Coptischinensis), Scutellariae Radix (root of Scutellariabaicalensis), Rhei Rhizoma (rhizome of Rheum officinale), and Pruni Cortex (cortex of Prunusyedoensis Matsum). Although the components are known to be effective in various conditions such as inflammation, hypertension, and hypercholesterolemia, there are no reports of the molecular mechanism of its hypolipidemic effects.MethodsWe investigated the hypolipidemic effect of HVC1 in low-density lipoprotein receptor-deficient (LDLR−/−) mice fed a high-cholesterol diet for 13 weeks. Mice were randomized in to 6 groups: ND (normal diet) group, HCD (high-cholesterol diet) group, and treatment groups fed HCD and treated with simvastatin (10 mg/kg, p.o.) or HVC1 (10, 50, or 250 mg/kg, p.o.).ResultsHVC1 regulated the levels of total cholesterol, triglyceride (TG), low-density lipoprotein (LDL) cholesterol, and high-density lipoprotein (HDL) cholesterol in mouse serum. In addition, it regulated the transcription level of the peroxisome proliferator-activated receptors (PPARs), sterol regulatory element-binding proteins (SREBP)-2, 3-hydroxy-3-methylglutaryl (HMG)-CoA reductase, lipoprotein lipase (LPL), apolipoprotein B (apo B), liver X receptor (LXR), and inflammatory cytokines (IL-1β, IL-6, and TNF-α). Furthermore, HVC1 activated 5′ adenosine monophosphate-activated protein kinase (AMPK).ConclusionOur results suggest that HVC1 might be effective in preventing high-cholesterol diet-induced hyperlipidemia by regulating the genes involved in cholesterol and lipid metabolism, and inflammatory responses.

A Wogonin-rich Fraction of scutellaria baicalensis Root Extract Exerts Chondroprotective Effects by Suppressing il-1β-induced Activation of AP-1 in Human OA Chondrocytes

Osteoarthritis (OA) is a common joint disorder with varying degrees of inflammation and sustained oxidative stress. The root extract of Scutellaria baicalensis (SBE) has been used for the treatment of inflammatory and other diseases. Here, we performed activity-guided HPLC-fractionation of SBE, identified the active ingredient(s) and investigated its chondroprotective potential. We found that the Wogonin containing fraction-4 (F4) was the most potent fraction based on its ability to inhibit ROS production and the suppression of catabolic markers including IL-6, COX-2, iNOS, MMP-3, MMP-9, MMP-13 and ADAMTS-4 in IL-1β-treated OA chondrocytes. OA chondrocytes treated with F4 in the presence of IL-1β showed significantly enhanced expression of anabolic genes ACAN and COL2A1. In an in vitro model of cartilage degradation treatment with F4 inhibited s-GAG release from IL-1β-treated human cartilage explants. The inhibitory effect of F4 was not mediated through the inhibition of MAPKs and NF-κB activation but was mediated through the suppression of c-Fos/AP-1 activity at transcriptional and post transcriptional levels in OA chondrocytes. Purified Wogonin mimicked the effects of F4 in IL-1β-stimulated OA chondrocytes. Our data demonstrates that a Wogonin-rich fraction of SBE exert chondroprotective effects through the suppression of c-Fos/AP-1 expression and activity in OA chondrocytes under pathological conditions.