Activity Of Baicalin Research Articles

Effect of Baicalin on Transcriptome Changes in Piglet Vascular Endothelial Cells Induced by a Combination of Glaesserella parasuis and Lipopolysaccharide.

Glaesserella parasuis causes porcine Glässer's disease and lipopolysaccharide (LPS) induces acute inflammation and pathological damage. Baicalin has antioxidant, antimicrobial, and anti-inflammatory functions. Long noncoding RNAs (lncRNAs) play key regulatory functions during bacterial infection. However, the role of lncRNAs in the vascular dysfunction induced by a combination of G. parasuis and LPS during systemic inflammation and the effect of baicalin on lncRNA expression induced in porcine aortic vascular endothelial cells (PAVECs) by a combination of G. parasuis and LPS have not been investigated. In this study, we investigated the changes in lncRNA and mRNA expression induced in PAVECs by G. parasuis, LPS, or a combination of G. parasuis and LPS, and the action of baicalin on lncRNA expression induced in PAVECs by the combination of G. parasuis and LPS. Our results showed 133 lncRNAs and 602 genes were differentially expressed when PAVECs were stimulated with the combination of G. parasuis and LPS, whereas 107 lncRNAs and 936 genes were differentially expressed when PAVECs were stimulated with the combination of G. parasuis and LPS after pretreatment with baicalin. The Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis showed the dominant signaling pathways triggered by the combination of G. parasuis and LPS were the tumor necrosis factor signaling pathway, phosphatidylinositol signaling system, and inositol phosphate metabolism. Protein-protein interaction network analysis showed the differentially expressed target genes of the differentially expressed lncRNAs (DELs) were related to each other. A coexpression analysis indicated the expression levels of the DELs were co-regulated with those of their differentially expressed target genes. This is the first study to systematically compare the changes in lncRNAs and mRNAs in PAVECs stimulated with a combination of G. parasuis and LPS. Our data clarified the mechanisms underlying the vascular inflammation and damage triggered by G. parasuis and LPS, and it may provide novel targets for the treatment of LPS-induced systemic inflammation.

Antiviral effect of baicalin on Marek\u2019s disease virus in CEF cells

BackgroundBaicalin, the main metabolic component of Scutellaria baicalensis Georgi, has various pharmacological properties including anti-inflammatory, anti-oxidant, anti-apoptotic, anti-bactericidal and anti-viral. The purpose of this study was to investigate the anti-Marek’s disease virus (MDV) activities of baicalin in CEF cells.ResultsHere, we showed that baicalin could inhibit viral mRNA, protein levels and overall plaque formation in a time-dependent manner. We also found that baicalin could consistently inhibit MDV replication and directly affect the virus infectivity. Moreover, baicalin treatment has no effect on expression level of antiviral cytokine and inflammatory cytokines in MDV infected CEFs.ConclusionsThese results demonstrate that baicalin could be a potential drug against MDV infection.

The Stimulatory Activities of Baicalein and Baicalin Compounds Derived from <i>Scutellaria baicalensis</i> on Insulin Secretion <i>In Vitro</i>

The medicinal plant Scutellaria baicalensis Georgi has been used widely in traditional Chinese medicine for anti-inflammation, anticancer, antiviral and antibacterial infections, reducing the total cholesterol level and decreasing blood pressures. Baicalein and baicalin are two major flavonoid of Scutellaria baicalensis Georgi, exhibit various bioactivities. In the present study, the stimulatory activity of baicalin and baicalein derived from Scutellaria baicalensis on insulin secretion in vitro was investigated using HIT-T15 cell, a Syrian hamster transformed β-cell line. The survival rate of cells treated with baicalin or baicalein (0.01-0.5 mg/ml) increased significantly (P < 0.05). In the presence of 5.6 mM glucose, baicalin or baicalein (0.01-0.5 mg/ml) increased glucose-stimulated insulin secretion and cellular ATP levels in HIT-T15 cells. Baicalin and baicalein exhibited significant stimulatory activity in a dose-dependent manner without apparent cytotoxicity at concentrations less than 0.1 mg/ml. The results obtained in this study suggest that baicalin or baicalein increases the insulin secretion of HIT-T15 cells by the enhancement of β-cells activity and cellular ATP levels. Baicalin or baicalein could be candidates for a new class of anti-diabetic drugs.

Study on Anti-Human Herpes Virus 6 Effects of Baicalin

Human Herpes Virus 6 (HHV-6), which is different with Human Immunoddficiency Virus (HIV) was first isolated from peripheral blood mononuclearcells of six patients with AIDS and lymphoproliferative disorders in 1986. It is one of the most common viral infection in AIDS patients. The pathological changes caused by HHV-6 are usually serious and easy to recur. The infection affect prognosis of AIDS apparently. HHV-6 infection is related to various diseases, such as chronic fatigue syndrome, necrotizing lymphadenitis, mononucleosis-like syndromes, AIDS, recipients of organ transplantation and hepatitis. HHV-6 can be found even in healthy bodies. At present, little is known about the mechanism of latency and reactivation of HHV-6 so there is no effective specificity drug on HHV-6 infection. Therefore, it is very important to find safety and effective anti-HHV6 drugs. To study the anti-HHV-6 action of Baicalin, the human T-cell strain was used to do the anti-HHV-6 effect in vitro. The result shows that Baicalin has evident effect on cytopathic effect (CPE) caused by HHV-6 GS. This result prompts that Baicalin has therapeutical effect on infection caused by HHV-6t.

The Signal Pathways of Immune Inflammation Mediated by the Tlr3/Nf-Kappab and Activator Protein-1 in Cells Infected with Influenza A Virus Antagonized by Baicalin

Baicalin has better anti-inflammatory function, antioxidant function and antiviral activity, but the mechanism of the antiinfluenza viral activity of baicalin has not been revealed.Toll-like Receptor 3 and the signal pathways mediated by TLR3 were affected and controlled by the infections with influenza A virus. We report here the significant activity and part mechanism of baicalin against H3N2 influenza A viruses. Baicalin could well protect the damages of cells caused by influenza A virus, it also could effectively inhibit the production of CPE in cells caused by influenza A virus and the inhibition of cells growth. The mechanism of antiinfluenza virus infection of baicalin may be related with the following aspects: to decrease the transcriptional activity of the oxidative stress sensitive transcription factor NF-kappaB and AP-1 by moderately decrease the higher expression level of TLR3 mRNA and the higher expression level of protein; and to further inhibit the mRNA expression of the downstream target genes IL-1β, IL-8, RANTES and IFN-β thereby alleviate the inflammatory injuries and restore the stability and balance of immune function in vivro.

The Inhibitory Effect of Baicalin on the Short-Term Food Intake in C57BL/6J Mice

Abstract － Appetite is inhibited by the anorexigenic neuropeptides POMC (proopiomelanocortin) and CART (cocaine-amphetamine-regulated transcript) in the hypothalamus. The present study was performed to examine the inhibitory effects of baicalin against food intake and the upregulation of POMC/CART. Short-term food intake (48 h) was significantly inhibited by treatment with baicalin (10 mg/kg, p ＜0.05) in C57BL/6 mice. Immunohistochemical analysis showed that baicalin upregulated POMC and CART levels in the arcuate nucleus of the hypothalamus. These effects were also examined using an in vitro system. pPOMC-Luc or pCART-Luc plasmids were transformed into mouse N29-2 neuronal and human SH-SY5Y cells, and the activities of baicalin were examined in these cells. Baicalin increased POMC and CART promoter-driven luciferase activity in a dose-dependent manner without cytotoxic effects. These results suggest that baicalin downregulates short-term food intake while upregulating POMC and CART expression.Keywords: Baicalin,

Baicalin synergy with beta-lactam antibiotics against methicillin-resistant Staphylococcus aureus and other beta-lactam-resistant strains of S. aureus.

Bacterial resistance to antibiotics is a serious global problem and includes strains of beta-lactam-resistant Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Novel antimicrobials and/or new approaches to combat the problem are urgently needed. The Chinese herb Xi-nan Huangqin (Scutellaria amoena C.H. Wright) has been used in traditional Chinese medicine to treat a wide range of infectious diseases. In this study we have examined the antibacterial action of baicalin, a flavone isolated from the herb. When combined with 16 microg mL(-1) baicalin, minimum inhibitory concentrations (MICs) of benzylpenicillin against MRSA and penicillin-resistant S. aureus were reduced from 125 and 250 microg mL(-1) to 4 and 16 microg mL(-1), respectively. This activity of baicalin was dose-dependent. Viable counts showed that the killing of MRSA and beta-lactam-resistant S. aureus cells by 10 to 50 microg mL(-1) ampicillin, amoxycillin, benzylpenicillin, methicillin and cefotaxime was potentiated by 25 microg mL(-1) baicalin. From the study it was concluded that baicalin has the potential to restore the effectiveness of beta-lactam antibiotics against MRSA and other strains of beta-lactam-resistant S. aureus. In view of its limited toxicity baicalin offers potential for the development of a valuable adjunct to beta-lactam treatments against otherwise resistant strains of microorganisms.

Antidepressant Effect of Baicalin Extracted from the Root of Scutellaria baicalensis. in Mice and Rats

The flavonoid baicalin, isolated from the dried root of Scutellaria baicalensis. G. (Labiatae), is widely used in traditional Chinese herbal medicine. In the present study, baicalin, at doses of 20, 40, and 80 mg/kg (p.o.), reduced immobility time in tail suspension test (TST) and the forced swimming test (FST) in mice. Baicalin also decreased immobility time at 12.5, 25, and 50 mg/kg (p.o.) in FST in rats. Furthermore, baicalin (25 mg/kg), as well as fluoxetine (FLU; 20 mg/kg), showed a significant recovery in sucrose intake compared with the vehicle-treated stressed animals for 5 weeks treatment in a chronic mild stress (CMS) model in rats. The effect of baicalin at the dose of 25 mg was as potent as that of reference antidepressant FLU (20 mg/kg) in the CMS model. With the monoamine oxidase (MAO A and B) assay, oral administration of baicalin at the doses of 12.5, 25, and 50 mg/kg significantly inhibited MAO A activity in a dose-dependent manner in rats. However, only baicalin at the doses of 25 and 50 mg/kg markedly inhibited MAO B activity. Neither baicalin nor FLU, at the doses tested, produced a significant effect on locomotor activity in mice. These results suggest that baicalin had a specific antidepressant-like effect in vivo.. The antidepressant activity of baicalin may be mediated in part through MAO A and B inhibition in rat brain.

In vitro studies of baicalin alone or in combination with Salvia miltiorrhiza extract as a potential anti-cancer agent

Traditional Chinese herbal medicines (TCM) that for centuries have been used in disease prevention and treatment are finding use as alternatives to Western cancer therapies. From a panel of TCM, we chose four compounds representing two functional classes of botanicals, the purified plant flavins scutellarin (a circulatory stimulant) and baicalin (antipyretic), and two extracts purified from Salvia miltiorrhiza (SM-470, circulatory stimulant) and Camellia sinensis (Cam-300, antipyretic), and examined their anti-proliferation effects on the human breast cancer cell lines MCF-7 and T-47D. All four compounds inhibited MCF-7 and T-47D cell proliferation, baicalin being the most potent inhibitor. Moreover, the combination of compounds from different classes offers enhanced potential therapeutic benefits; the combination of SM-470 with scutellarin, Cam-300 or baicalin, augmented the inhibition of cell proliferation. A synergistic inhibitory effect on MCF-7 cell proliferation was also observed when SM-470 and baicalin were applied together. In contrast, inhibition of T-47D cell proliferation using the same combination was dependent on baicalin only. The anti-proliferative effects of these compounds can be extended to other cancer types; the human head and neck cancer epithelial cell lines CAL-27 and FaDu were also sensitive to the four drugs. Overall, SM-470, Cam-300, scutellarin and baicalin inhibited the proliferation of human breast cancer cells and CAL-27 and FaDu cells with different potency. Baicalin and SM-470 in combination produced additive effects, suggesting these compounds may function by different mechanisms. T-47D, MCF-7, and FaDu cells may be useful in exploring the cellular and molecular mechanisms of action of baicalin and SM-470.

Zinc coupling potentiates anti-HIV-1 activity of baicalin

Baicalin (BA) has been shown with anti-HIV-1 activity. Zinc is a nutrient element. The anti-HIV-1 activity of zinc complex of baicalin (BA–Zn) in vitro was studied and compared with the anti-HIV-1 activities between BA and BA–Zn in the present study. Our results suggested that BA–Zn has lower cytotoxicity and higher anti-HIV-1 activity compared with those of BA in vitro. The CC50s of BA–Zn and BA were 221.52 and 101.73μM, respectively. The cytotoxicity of BA–Zn was about 1.2-fold lower than that of BA. The BA and BA–Zn inhibited HIV-1 induced syncytium formation, HIV-1 p24 antigen and HIV-1 RT production. The EC50s of BA–Zn on inhibiting HIV-1 induced syncytium formation (29.08μM) and RT production (31.17μM) were lower than those of BA (43.27 and 47.34μM, respectively). BA–Zn was more effective than BA in inhibiting the activities of recombinant RT and HIV-1 entry into host cells. Zinc coupling enhanced the anti-HIV-1 activity of baicalin.